Author:
soren101
ID:
149734
Filename:
MS2_PHARM_GEN_FINAL.txt
Updated:
2012-04-24 00:27:22
Tags:
NPLWEKNFV
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Description:
PHARMACOLOGY MS2 FINAL
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  1. PHOSPHODIESTERASE INHIBITORS
    THREE SILLY PAPA CALFS

    • THREOPHYLLINE
    • SILDENAFIL
    • PAPAVERINE
    • CAFFEINE

    MOA -- TPC Prevents phosphodiesterase from changing cAMP back à 5´-AMP.

    SIL -- Prevents phosphodiesterase from changing cGMP back → 5´-GMP

    • THEO --bronchodilator (Not used as much anymore). Relieves airflow obstruction
    • of chronic asthma. *Seizures *Poss fatal arrhythmias
  2. THEOPHYLLINE
    PDE INH

    MOA -- PREVENTS PDE FROM CHANGING cAMP BACK TO 5'-AMP

    PHARM -- BRONCH-DILATOR

    THERA -- INFREQ USED; RELIEVES AIRFLOW OBST OF CHRONIC ASTHMA

    ADVERSE -- SEIZURES, POSS FATAL ARRHYTHMIAS
  3. CAFFEINE
    PDE INH

    MOA -- PREVENTS PDE FROM CHANGING cAMP TO 5'-AMP (SIMILAR TO THREO

    THERA -- RELAX SMOOTH MUSC OF BRONCHs IN ASTHMA Pt
  4. PAPAVERINE
    PDE INH

    MOA --PREVENTS PDE FROM CHANGING cAMP BACK TO 5'-AMP
  5. SILDENAFIL
    PDE INH

    MOA --PREVENTS PDE FROM CHANGING cGMP BACK TO 5'GMP

    • PHARM -- cGMP produces smooth muscle
    • relaxation → inc blood flow into corpus cavernosa

    THERA -- IMPOTENCE
  6. INC/DEC URINARY pH
    • ACETAZOLAMIDE (MORE BASIC / ALKALINE)
    • -GLAUCOMA (CARBONIC ANHYD INH)

    AMMONIUM CHLORIDE (MORE ACIDIC)
  7. ACh SYNTH / RELEASE
    BOTULINUM TOXIN (-)

    *HEMICHOLINIUM: prevents ACh synthesis by blocking choline uptake in parasympathetic fiber.

    *TETANUS TOXIN: prevents inhibitory NT --> increase ACh --> spastic paralysis

    *Black widow spider toxin (α-latrotoxin): binds to neurexins --> excessive ACh release

    --Drugs affecting degradation of ACh

    • •Slowly reversible carbamate inhibitors (neostigmine)
    • •Irreversible organophosphate inhibitors (malathion)

    BOTOX

    Transported into cholinergic receptor via receptor mediated endocytosis (Local i.m. injection)

    Light chain of botox (protease) → hydrolyzes proteins involved in the synaptic storage & exocytotic release of ACh

    → No more cholinergic transmission at NMJ

    → muscle paralysis (FLOPPY BABY)

    • THERAPEUTIC -->
    • *blepharospasm
    • *strabismus
    • *cervical dystonia
    • *spasmodic torticollis
    • *laryngeal dystonia
    • *hemifacial spasm
    • *myofacial pain syndrome

    • **all require multiple treatments b/c hydrolyzed
    • enzymes are replaced -->regain function
  8. ACh
    CHOLINERGIC AGONIST

    • MOA -- GIVEN IV
    • 1o M EFFECTS (N EFFECTS ONLY AFTER M RECEPTORS BLOCKED BY ATROPINE)

    PHARM -- AFTER IV INJ: RAPID & TRANSIENT DEC IN BP VIA NO FROM ENDO CELLS --> BAROREFLEX TACHYCARDIA. NO DIRECT CARDIAC SUPPRESSION

    AFTER RX WITH ATROPINE, MUCH LARGER DOSE AF ACh --> INC BP & HR BY SYMP GANG

    THERA -- NOT USED SYSTEMICALLY BC EFFECTS MULTI ORGANS.

    RAPIDLY DEGRADED BY HYDROLYSIS (PLASMA PSEUDO-CHOLINESTERASE)

    USED TO PROD RAPID & COMPLETE MIOSIS (20-60 min) BEFORE OR AFTER SURGERY INVing ANT EYE
  9. BETHANECHOL
    CHOLINERGIC AGONIST

    MOA -- GIVEN P.O. BUT F IS LOW

    M RECEPTOR AGONIST W/ SELECTIVE GI & GU EFFECTS

    • PHARM --
    • INC ACID SECRETION
    • INC MOTILITY & TONE
    • RELAX SPHINC
    • STIM SECRETION IN GI
    • CONTRACT DETRUSOR MUSC
    • RELAX EXTERNAL SPHINC

    • THERA --
    • BOWEL STASIS
    • POST-OP PARALYTIC ILEUS
    • URINARY RETENTION (POST-OP OR NEURO)
    • *TREATS PROBS W/ BOWEL/BLADDER

    • CONTRA --
    • ASTHMA
    • COPD
    • PEPTIC ULCER
    • CHF
    • HYPERTHYROIDISM
  10. SUCCINYLCHOLINE
    CHOLINERGIC AGONIST

    MOA -- SINGLE IV INJ

    INITIAL SINGLE CONTRACTION OF SKEL MUSC --> 3-5 MINS FLACCID PARALYSIS

    N2 CHOL RECEPTORS AT NMJ OF SKEL MUSC

    PHARM -- FLACCID PARALYSIS: CONSTANT DEPOL OF MEP = DEPOL BLOCKADE = NON-COMP BLOCKADE

    MOST OF IV DOSE DEGRADED BY PLASMA CHOLase BEFORE REACHING NMJ. NOT DEGRADED BY TISSUE ACE

    PARTIAL REPOL POSS WHILE SUCC STILL PRESENT BUT NMJ BLOCKADE PERSISTS

    PEEPS WITH GENETIC VARIANT OF PLASMA ACE SEE EFFECTS LASTING 1-3hr LONGER

    THERA -- MUSC RELAXATION & SHORT TERM PARALYSIS
  11. PILOCARPINE
    CHOL AGONIST

    MOA -- 3* AMINE

    SELECTIVE M AGONIST OF BOTANICAL ORIGIN

    DEGRADED BY HEP ENZs (NOT BY ACE OR pseudo-ACE)

    PHARM -- CONTRACTION OF MERIDIONAL FIBERS OF CILIARY MUSC

    • --> INC IRIDIOCORNEAL ANGLE AND/OR TONE AND ALIGN OF TRABECULAE
    • --> AQ FLOW BETTER INTO CANAL OF SCHLEMM

    • THERA -- GLAUCOMA: LOWER IOP BY 20%
    • DRY MOUTH ASSIC W/ SJORGREN'S SYND

    ADVERSE -- GLAUCOMA --> LENS FIXATION IMPAIRS FAR VISION. PERSISTANT MIOSIS CAUSES POOR NIGHT VISION

    • CONTRAINDICATION --
    • ASTHMA & COPD (BRONCH-CONSTRICT)

    PEPTIC ULCER (INC GASTRIC ACID)

    HYPERTHYROIDISM (ATRIAL FLUTTER OR FIB)

    DIALATED HEART (ATRIAL FLUTTER OR FIB)
  12. CEVIMELINE
    CHOL AGONIST

    MOA -- SYNTHETIC M AGONIST

    PHARM -- INC SALIVATION

    THERA -- DRY MOUTH & EYES ASSOC W. SJOGREN'S SYND

    • ADVERSE --
    • GI CRAMPING
    • SWEATING
    • UTI
    • RHINITIS
  13. METHACHOLINE
    CHOLINERGIC AGONIST

    MOA -- M RECEPTOR AGONIST

    PHARM -- CONTRICTION OF BRONCH MUSC

    THERA -- PROVOCATIVE AGENT IN Dx OF BRONCH ASTHMA (meTHAcholine IS FOR asTHMA)
  14. CARBACHOL / CARBAMYLCHOLINE
    CHOLINERGIC AGONIST

    MOA -- N & M RECEPTOR AGONIST

    PHARM -- SLOW ONSET MIOSIS (4-8 hr)

    THERA -- MIOSIS AFTER SURGERY ON THE ANT CHAMBER OF EYE. EYE DROPS
  15. CHOLINERGIC AGONISTS
    "AMC BETHANNE SUCCS PILO"

    • ACh
    • METHACHOLINE
    • CARBACHOL (CARBAMYCHOLINE)
    • BETHANECHOL
    • SUCCINYLCHOLINE (nicotinic also)
    • PILOCARPINE

    • ACh -- Given i.v.
    • Exerts 1o Muscr effects
    • (Nicotinic effects seen only after Muscr receptors are blocked by atropine)

    • After i.v. injection:
    • Rapid & transient decr in BP (via NO from endothelial cells) → baroreflex tachycardia
    • (No direct cardiac suppression)

    • After Rx w/ atropine, a much larger dose of ACh →
    • incr BP & HR by stim N1-chol receptors at sympathetic ganglia

    • THERA --> Not used systemically b/c:
    • *Affects multiple organs
    • *Rapidly degraded by hydrolysis (plasma
    • pseudo-cholinesterase)

    Used to produce rapid & complete miosis (20-60 min) before or after surgery involving ant. part of eye

    • CARBACHOL
    • MOA -- N&M RECEPTOR AGONIST
    • PHARM -- SLOW ONSET MIOSIS (4-8hr)
    • THER -- CAUSED MIOSIS AFTER SURGERY ON THE ANT CHAMBER OF THE EYE -- EYE DROPS

    • METHACHOLINE
    • MOA -- M RECEPTOR AGONIST
    • PHARM -- CONTRACTION OF BRONCH MUSC
    • THER -- PROVOCATIVE AGENT IN Dx OF BRONCH ASTHMA (meTHAchol IS FOR asTHMa

    • BETHANECHOL
    • MOA -- GIVEN p.o. BUT F IS LOW. M RECEPTOR AG W/ SELECTIVE GI & GU EFFECTS
    • PHARM -- INC ACID SECRETION, INC MOTILITY & TONE, RELAX SPHINCs, STIM SEC IN GI, CONTRACT DETRUSOR MUSC, RELAX EXT SPHINC
    • THER -- BOWEL STASIS, POST-OP PARALYTIC ILEUS, URINARY RETENTION (POST-OP OR NEURO)
    • CONTRAIND -- ASTHMA, COPD, PEPTIC ULCER, CHF, HYPERTHYROIDISM

    • SUCC
    • MOA -- IV SINGLE INJ. INITIAL SINGLE CONTRAC OF SKEL MUSC --> 3-5 MIN FLACID PARALYSIS. N2 CHOL RECEPTORS AT NMJ
    • PHARM -- FLACCID PARAL: CONSTANT DEPOL OF MEP = DEPOL BLOCKADE = NONCOMP BLOCKADE.

    MOST IV DOSE DEGRADED BY PLASMA CHOLase BEFORE REACHING NMJ.

    PARTIAL REPOL POSS WHILE SUCC STILL PRESENT BUT NMJ BLOCKADE PERSISTS.

    NMJ BLOCKADE TERMINATED BY DRUG DIFFUSING AWAY FROM NMJ

    THER -- MUSC RELAXATION & SHORT TERM PARALYSIS

    • PILO
    • MOA -- 3o AMINE. SELECTIVE M AGONIST OF BOTANICAL ORIGIN

    DEGRADED BY HEP ENZs

    NOT METABed BY AChase OR PSEUDO-AChase

    PHARM -- CONTRACTION OF MERIDONAL FIBERS OF CILIARY MUSC --> INC IRIDIOCORNEAL ANGLE AND/OR TONE AND ALIGNMENT OF TRABECULAE --> AQUEOUS HUM FLOW MORE EASILY INTO CANAL OF SCHLEMM

    THER -- GLAUCOMA, LOWER IOP BY 20%

    DRY MOUTH ASSOC W/ SJOGREN'S SYND

    FOR GLAUCOMA CAN CAUSE LENS FIXATION IMPAIRING FAR VISION AND PERSIST MIOSIS CAUSING POOR NIGHT VISION

    • CONTRAIND -- ASTHMA & COPD (BRONCHOCONSTRIC)
    • PEPTIC ULCER (INC GASTRIC ACID)
    • HYPERTHYROIDISM (ATRIAL FLUTTER OR FIB)
    • DILATED HEART (ATRIAL FLUTTER OR FIB)
  16. EPINEPHRINE
    GLAUCOMA

    • EPI
    • MOA -- a1 AGONIST

    PHARM -- a1 RECEPTOR STIM --> INC OUTFLOW OF AQ HUM VIA PRESS DEP NORMAL PATHWAY. MYDRIASIS VIA RADIAL MUSC DIPIVEFRIN TOO (HYDROed TO EPIN

    THER -- GLAUCOMA

    ADVERSE -- MYDRIASIS VIA a1 STIM OF RADIAL MUSC OR IRIS

    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"

    • EPINEPHRINE
    • BI-MATO-PROST
    • MANNITOL
    • BETAX-OLOL
    • PILOCARPINE
    • APRA-CLONI-DINE
    • LAN-TANO-PROST
    • TIM-OLOL (b-adren antagonist)
    • ACETA-ZOLA-MIDE
    • ECHO-THIO-PHATE (op AChase inh also)
    • ISO-FLUO-PHATE (DFP)
    • DOR-ZOLA-MIDE
  17. DRUGS THAT INC OUTFLOW OF AQ HUM THROUGH THE UVEOSCLERAL PATHWAY
    Tx OPEN-ANGLE GLAUCOMA

    • LATANOPROST (PGF2a ANALOG)
    • BIMATOPROST - EYELASHES
  18. DRUGS THAT INC AQ HUM OUTFLOW THROUGH THE NORMAL PRESSURE-DEPENDENT PATHWAY
    Tx FOR OPEN-ANGLE GLAUCOMA

    PILOCARPINE (m AGONIST)

    EPINEPHRINE (a1-BLOCKER)

    • ISOFLUROPHATE (OP ACE INH)
    • ECHOTHIOPHATE ''
  19. DRUGS THAT DECREASE RATE OF AQ HUM PRODUCTION
    Tx FOR OPEN-ANGLE GLAUCOMA

    • BETAXOLOL (b-BLOCKER)
    • TIMOLOL ''
    • --NOT PROPRANOLOL BC ANESTHETIC EFFECT

    APRACLONIDINE (a2-BLOCKER)

    • ACETAZOLAMIDE (CARB ANH INH, MANY Sx)
    • DORZOLAMIDE '' -- USE
  20. BIMATOPROST & LATANOPROST
    GLAUCOMA

    MOA -- STABLE ANALOG OF PGF-2a

    PHARM -- INC UVEOSCLERAL OUTFLOW

    THER -- LATANO LOWERS IOP BY 20-25%. BIMATO INC LENGTH/THICKNESS OF EYELASHES

    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"

    • EPINEPHRINE
    • BI-MATO-PROST
    • MANNITOL
    • BETAX-OLOL
    • PILOCARPINE
    • APRA-CLONI-DINE
    • LAN-TANO-PROST
    • TIM-OLOL (b-adren antagonist)
    • ACETA-ZOLA-MIDE
    • ECHO-THIO-PHATE (op AChase inh also)
    • ISO-FLUO-PHATE (DFP)
    • DOR-ZOLA-MIDE
  21. MANNITOL
    GLAUCOMA -- ACUTE ATTACK OF ANGLE CLOSURE

    MOA -- OSMOTIC DIURETIC AGENTS

    PHARM -- HYPEROSMOLAR ECF CAUSES CELLULAR DEHYDRATION --> FALL IN IOP

    THERA -- ACUTE ATTACKS OF ANGLE-CLOSURE GLAUCOMA

    COMBINE GLAUCOMA DRUGS WITH DIFF MOA FOR COMBO EFFECT:

    MANN, ACETA, PILO

    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"
  22. BETAXOLOL & TIMOLOL
    GLAUCOMA & b-BLOCKER

    • BETAX MOA
    • --SELECTIVE b1-ANTAGONIST (CARDIO SELECTIVE AT LOW DOSE).

    --b-BLOCKERS HAVE NO EFFECT ON PUPIL SIZE OR VISUAL ACCOMODATION

    PHARM -- DEC PROD OF AQ HUM BY UNKNOWN MECH (20-30%)

    THERA -- SYSTEMIC ABS --> TIMOLOL BRONCH-CONSTRICT b2 & BRADYCARDIA

    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"
  23. APRACLONIDINE
    GLAUCOMA

    MOA -- SELECTIVE a2 AGONIST

    PHARM -- SELECTIVE a2 STIM --> DEC PROD OF AQ HUM

    THERA -- PREVENTS POST-SURGICAL OCULAR HYPERTENSION AFTER LASER TRABECULOPLASTY

    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"
  24. ACETAZOLAMIDE
    GLAUCOMA

    MOA -- GIVEN P.O. & TOPICAL.

    CARBONIC ANHYDRASE INH (DORZOLAMIDE TOO)

    *ALSO INC URINE pH!

    • PHARM -- DEC PROD OF AQ HUM.
    • CARBONIC ANHYD IN CILIARY BODIES PROD AQ HUM --> INH CARB ANHYD STOPS AQ HUM PROD

    THERA -- GLAUCOMA

    • ADVERSE ACETA -- DON'T GIVE P.O. IF:
    • HEADACHE
    • DEC LIBIDO
    • METALLIC TASTE
    • KIDNEY STONES
    • URINARY FREQ

    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"
  25. ECHOTHIOPHATE
    GLAUCOMA

    MOA -- TOPICAL OP AChase INH

    PHARM -- LOWER IOP BY INC AMT OF ACh AVAILABLE TO CONTRACT CILIARY MUSC

    THERA -- GLAUCOMA (TOPICAL Rx)

    AVERSIVE -- LAST RESORT DRUG IN Pt WHEN OTHER Rx FAIL --> CONTRACTS & GENERAL TOXICITY

    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"
  26. ISOFLUOPHATE (DFP)
    GLAUCOMA (SAME AS ECHOTHIOPHATE)

    MOA -- TOPICAL OP CHOLase INH

    PHARM -- LOWER IOP BY INC AMT OF ACh AVAILABLE TO CONTRACT CILIARY MUSC

    THERA -- GLAUCOMA (TOPICAL Rx)

    AVERSIVE -- LAST RESORT DRUG IN Pt WHEN OTHER Rx FAIL --> CONTRACTS & GENERAL TOXICITY

    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"
  27. DORZOLAMIDE
    GLAUCOMA

    • MOA -- TOPICAL. CARBONIC ANHYD INH
    • (ACETAZOLAMIDE TOO)

    PHARM -- TOPICAL DEC PROD OF AQ HUM

    THERA -- GLAUCOMA. LOWER IOP BY 10-20%

    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"
  28. TREATMENT OF GLAUCOMA
    "EPIN BUYs, MAN BETA PILO APRON LANTERNS that TIM ACE's ECHO ISO DORABLE!"

    • EPINEPHRINE
    • BI-MATO-PROST
    • MANNITOL
    • BETAX-OLOL
    • PILOCARPINE
    • APRA-CLONI-DINE
    • LAN-TANO-PROST
    • TIM-OLOL (b-adren antagonist)
    • ACETA-ZOLA-MIDE
    • ECHO-THIO-PHATE (op AChase inh also)
    • ISO-FLUO-PHATE (DFP)
    • DOR-ZOLA-MIDE
    • ----------------
  29. GLAUCOMA: CLASSES OF DRUGS TO TREAT FORMATION OF AQ HUM & OUTFLOW
    • FORMATION:
    • b-ADREN ANTAGONISTS
    • CARB ANHYD
    • a2-ADREN AGONISTS

    • OUTFLOW:
    • PGF-2a
    • a1-ADREN AGONIST
    • PILO, ISO
  30. NMDA RECEPTOR AGONIST
    MEMANTINE

    ALZ Tx

    GLUTAMATE NMDA ANTAGONIST -- EXCESS NMDA STIM --> Na + Ca ENTRY --> EXCITOTOXICITY AND NEURONAL CELL DEATH
  31. PHYSOSTIGMINE
    CARBAMATE AChase INH (REVERSIBLE)

    MOA -- 3*AMINE; FREELY ENTERS CNS

    NON-COMP SLOWLY REVERSIBLE INH OF AChase

    --CARBAMOYLATION RATHER THAN NL ACETYLATION OF ACTIVE SITE OF AChase

    HYDROL OF CARBAMOYL ENZ OCCURS SPONT W/ t1/2 OF 15-30 min

    NO DIRECT EFFECT AT ACh RECEPTORS

    PHARM -- INH ACTION OF AChase --> ACh WILL STAY LONGER

    THERA -- NOT USED BC SIDE EFFECTS. ALZ BUT NEWER DRUGS USED (DONEPEZIL = ARICEPT)

    OVERDOSE & POISONING W/ ANTI-CHOL AGENTS

    ADVERSE -- NUMEROUS CNS EFFECTS
  32. DONEPEZIL
    CARBAMATE AChase INH (REVERSIBLE)

    MOA -- CARBAMATE COMPOUND

    PHARM -- INH ACTION OF AChase

    THERA -- DOC FOR ALZ BC MORE SELECTIVE OF CNS

    • DECREASES:
    • APATHY
    • ANX
    • HALLUCINATIONS
    • BEH PROBS

    • ADVERSE -- PNS STIM:
    • DIARRHEA
    • MUSC CRAMPS
    • FATIGUE / BRADYCARDIA
    • INSOMNIA
    • ANOREXIA
    • N/V
  33. NEOSTIGMINE
    CARBAMATE AChase INH (REVERSIBLE)

    • MOA -- 4*AMINE
    • DIRECT AGONIST AT N2 RECEPTOR

    INH AChase BY CARBAMOYLATION AT ALL PERIPH SITES

    • PHARM -- INH OF AChase
    • INC THE CONC OF ACh AT N2 OF NMJ

    INC CONC OF ACh AT M SITES (ex HEART, SALIVARY GLAND, etc)

    • THERA -- POST-OP PATALYTIC ILEUS
    • ATONIA OF GI & GU

    MYASTHENIA GRAVIS

    REVERSAL OF MUSC PARALYSIS CAUSED BY COMP NEUROMUSC BLOCKING AGENTS (d-TUBOCURARE)

    ADVERSE -- NO CNS EFFECTS. INC CONC OF ACh AT M SITES (HEART, SAL, etc)

    ATROPINE GIVEN TO PREVENT THESE UNWANTED EFFECTS
  34. PYRIDOSTIGMINE (given p.o.)
    CARBAMATE AChase INH (REVERSIBLE)

    MOA -- LIKE NEOSTIG. 4*AMINE

    DIRECT AGONIST AT N2 RECEPTOR

    INH AChase BY CARBAMOYLATION AT ALL PERIPH SITES

    PHARM -- INH ACTION OF AChase

    • THERA --
    • LONG TERM p.o. DOSING Rx MYASTHENIA GRAVIS

    MILD OCULAR Sx (+ CORTICOSTEROIDS)

    MILD/MOD GENERAL Sx (+ THYMECTOMY)

    MOD/SEVERE GENERAL Sx (+ AZATHIOPRINE IMMUNOSUPPRESSANT)
  35. EDROPHONIUM
    CARBAMATE AChase INH (REVERSIBLE)

    USED TO Dx MYASTHENIA GRAVIS

    GIVEN IM OR IV BC VERY SHORT t1/2

    • MOA -- 4*AMINE
    • INH AChase AT ALL PERIPH CHOL NERVE JUNCTION BUT MOST ACTION AT NMJ FROM DIRECT STIM OF CHOL N2 RECEPTORS

    PHARM -- ?

    THERA --MYASTHENIA GRAVIS

    • UNDER Rx --> MYASTHENIC CRISIS
    • OVER Rx --> CHOLINERGIC CRISIS

    • BETTER W/ EDRO --> MYASTHENIC
    • WORSE W/ EDRO --> CHOLINERGIC

    COMBO IV ATROPINE --> REVERSE COMP NEUROMUSC BLOCKADE BY DRUGS (ex d-TUBOCURARINE)

    ADVERSE -- NO CNS EFFECTS
  36. Sx OF INH OF AChase AT MUSCARINIC SITES
    EXCESSIVE SALIVATION

    RHINITIS

    BRADYCARDIA

    BRONCHOSPASM

    BOWEL CRAMPING

    DIARRHEA / VOM

    URINARY INCONTINENCE
  37. CARBARYL
    CARBAMATE INSECTICIDE (REVERSIBLE)

    AChase INH

    MOA -- CARBAMATE INSECTICIDE USED AROUND HOUSE (LIPID SOLUBLE)

    PHARM -- GROUPED W/ OP AChase INH BC POISINING W/ CARBARYL --> SIMILAR EFFECTS OF OP

    THERA -- CARBARYL POISONING ONLY W/ ATROPINE (3*M ANTAGONIST)

    ADVERSIVE -- CNS EFFECTS!!!
  38. RIVASTIGMINE
    INDIRECT REVERSIBLE INH OF AChase (CARBAMATE)

    EXELON -- PATCH
  39. GALANTAMINE
    INDIRECT REVERSIBLE INH OF AChase (CARBAMATE)
  40. Dx FOR COGNITIVE LOSS
    MEMANTINE (NMDA)

    PHYSOSTIGMINE (CARB)

    TACRINE (CARB)

    DONEPEZIL (DOC -- CARB)

    GALANTAMINE (CARB)

    RIVASTIGMINE (CARB -- EXELON PATCH)
  41. CARBAMATE REVERSIBLE AChase INHIBITORS
    DON RIVA'S GAL PHYS ED a NEW CAR-BAR-ATOR PIE

    **NEGATED BY DRUGS THAT BLOCK CENTRAL M RECEPTORS:

    ANTI-CHOL INCLUDING OLDER HISTAMINES DIPHENHYDRAMINE,

    URGE INCONT TOLTERODINE

    TRICYC ANTI-DEP IMIPRAMINE

    ----------------------------------------------

    • DONEPEZIL
    • RIVASTIGMINE
    • GALANTAMINE
    • PHYSOSTIGMINE
    • EDROPHONIUM
    • a
    • NEOSTIGMINE
    • CARBARYL
    • PYRIDOSTIGMINE
  42. DIMPYLATE
    OP AChase INH (DIP ME)

    MOA -- INSEC LAWN & GARDEN

    PHOS AChase ACTIVE SITE

    SPONT RATE OF HYDROL OF PHOS ENZ IS SUPER LOW
  43. ISOFLUOPHATE (DFP)
    OP AChase INH (IRREVERS) (DIP ME)

    MOA -- GIVEN LOCALLY, TOPICAL

    PHARM -- LOWER IOP BY INC AMT OF ACh AVAILABLE TO CONTACT CILIARY MUSC

    THERA -- GLAUCOMA

    ADVERSE -- LAST RESORT Rx --> CATARACTS & GENERAL TOXICITY

    SAME AS ECHOTHIOPHATE
  44. ECHOTHIOPHATE
    OP AChase INH (IRREVERS) "DIP ME"

    MOA -- GIVEN LOCALLY, TOPICAL

    PHARM -- LOWER IOP BY INC AMT OF ACh AVAILABLE TO CONTACT CILIARY MUSC

    THERA -- GLAUCOMA

    ADVERSE -- LAST RESORT Rx --> CATARACTS & GENERAL TOXICITY

    SAME AS ISOFLUOPHATE (DFP)
  45. PARATHION
    OP AChase INH (IRREVERS) "DIP ME"

    MOA -- INSECTICIDE CONVERTED TO ACTIVE METABOLITE PARAOXON BY CYP450

    ADVERSE -- ACCIDENTAL POISONING / DEATH
  46. MALATHION
    OP AChase INH (IRREVERS) (DIP ME)

    MOA -- INSECTICIDE, MAMMALS & BIRDS HAVE PLASMA CARBOXYESTERASES WHICH DESTROY MALATHION

    THERA -- SPRAY FOR MOSQ. DERM PREP TO KILL HEAD LICE

    ADVERSE -- MUCH SAFER THAN PARATHION
  47. ORGANOPHOSPHATE AChase INHIBITORS
    • DIM-PYL-ATE
    • ISO-FLUO-PHATE
    • PARATHION
    • MALATHION
    • ECHO-THIO-PHATE (glaucoma also)
  48. PRALIDOXIME
    Tx OF OP POISONING

    PRALI-DOX-IME (2-PAM)

    MOA -- 4*PRALI DOCKS THE ORGANOPHOS TO TAKE IT AWAY FROM AChase TO ALLOW NORMAL FUNCTION

    GREATLY INC RATE OF HYDROLYSIS OF PHOSED ENZ, ESP AT NMJ

    LESS EFFECTIVE IF "AGING" OF PHOSED AChase HAS OCCURED (NEED Rx IMMEDIATELY)

    NOT USED FOR CARBAMATE POISONING BC WILL NOT INC RATE OF HYDROL OF CARBAMOYLATED AChase

    ADVERSE -- DOSN'T ENTER CNS. PROB IF SEVERE CNS EFFECTS
  49. ATROPINE
    3* M ANTAGONIST

    PHARM -- VARIOUS SENSITIVITIES PER ORGAN

    • SMALL DOSE --> --> --> LARGE DOSE
    • GLANDS -> HRT -> BWL, BLADR -> EYE

    AT THERA DOSE --> NO CNS EFFECTS (UNLIKE SCOPOLAMINE)

    THERA -- PERIOPERATIVE USE (ALSO GLYCOPYRROLATE)

    DEC PROD OF SALIV/PULM SECRETIONS

    • COUNTERACT BRADYCARDIA FROM:
    • OCULAR PRESSURE
    • VISCERAL TRACTION
    • CAROTID SINUS STIM
    • INJ OF MULTI DOSES OF SUCC

    OP POISONING (REV CNS/PNS TOX)

    IV ATROPINE + EDRO --> REV COMPETITIVE NEUROMUSC BLOCKADE

    CONJUNCTIVAL "SAC" SCOPE, CYCLOPENT, & ATROPINE --> MYDRIASIS & CYCLOPLEGIA TO DET REFRACTIVE ERROR OF LENS & CATARACT SRGY

    • ADVERSE -- TOXICITY
    • RED AS A BEET
    • MAD AS A HATTER
    • DRY AS A BONE
    • HOT AS A PISTOL

    • Tx FOR OVERDOSE:
    • GASTRIC LAVAGE
    • RESP & CIRC SUPPORT
    • SPONGE BATH
    • FOLEY CATH
    • DARK ROOM
    • BENZO FOR SEDATION

    • CNS Sx:
    • NERVOUSNESS
    • EXCITIATION
    • CONF
    • HALL
    • WEAKNESS
    • GIDDINESS
    • MUSC
    • INCOORD
    • HYPERTENSE
    • MANIA

    • PNS:
    • DRY MOUTH / THIRST
    • HOT, DRY, FLUSHED SKIN
    • MYDRIASIS / BLURRED VISION
    • TACHYCARDIA
  50. SCOPOLAMINE
    3* M ANTAGONIST

    BELLADONNA ALKALOIDS

    MIX ATRO + EDRO OR GLYCOPYR + NEOSTIG GIVEN IV

    ATRO + GLYCOPYR PREVENT UNWANTED M STIM RESULTING FROM AChase INH AT PARASYMP SITES

    MOA -- LITTLE EFFECT ON HR

    REVERSE EFFECTS FROM d-TUBOCURARE

    • PHARM --
    • IRIS - RELAX SPHINC MUSC

    CILIARY MUSC - RELAX FOR FAR VISION

    ATRIA & VENT - INC dp/dt

    SA NODE - INC HR

    ATRIA - INC CONDUCTION VELOCITY

    AV NODE - INC CONDUCTION VELOCITY & AUTOMATICITY. DEC APD & ERP

    GI - DEC MOT & TONE

    GU, DETRUSOR, BRONCH - RELAX

    SALIVERY, LACRIMAL, SWEAT, BRONCH, GASTRIC GLANDS --> DEC SECRETION

    THERA -- INDUCE MYDRIASIS & CYCLOLEGIA BY "SAC": SCOPE, ATRO, CYCLOPENT

    DOC (ALSO ATROPINE) --> RELAX SPHINC & CIL MUSC --> DEC PAIN

    MOTION SICKNESS (VESTIB NUC & RETIC FORMATION) -- TRANSDERMAL PATCH

    AMNESIA esp DURING PARTUITION

    ADVERSE -- CNS EFFECTS AT THERA DOSES (UNLIKE ATROPINE)

    • SOMNOLENCE
    • AMNESIA
    • REDUCED REM SLEEP
    • ANT-GRADE AMNESIA (WORSE W/ ETOH)
  51. CYCLOPENTOLATE
    3* M ANTAGONIST

    • PHARM --
    • IRIS - RELAX SPHINC MUSC

    DOC FOR REFRACTIVE ERROR -- SHORT DURATION

    CILIARY MUSC - RELAX FOR FAR VISION. CAUSES "PUPLILARY BLOCK"

    ATRIA & VENT - INC dp/dt

    SA NODE - INC HR

    ATRIA - INC CONDUCTION VELOCITY

    AV NODE - INC CONDUCTION VELOCITY & AUTOMATICITY. DEC APD & ERP

    GI - DEC MOT & TONE

    GU, DETRUSOR, BRONCH - RELAX

    SALIVERY, LACRIMAL, SWEAT, BRONCH, GASTRIC GLANDS --> DEC SECRETION

    THERA -- DOC "SAC" MYDRIASIS & CYCLOPLEGIA
  52. TROPICAMIDE
    3*M ANTAGONIST

    MOA -- AT EYE. "SUNGLASSES IN TROPICS"

    PHARM -- SAME AS ATROPINE / SCOPE

    THERA -- DOC FOR MYDRIASIS FOR FUNDOSCOPIC EXAM OF RETINA & OPTIC DISK (SHORT t1/2)
  53. BENZOTROPINE
    3*M ANTAGONIST

    MOA -- AT CENTRAL M RECEPTOR

    PHARM -- SAME AS ATROPINE & SCOPE

    THERA -- PARKINSON'S
  54. TRIHEXYPHENIDYL
    3*M ANTAGONIST

    MOA -- AT CENTRAL M RECEPTOR

    PHARM -- SAME AT ATROPINE & SCOPE

    THERA -- PARKINSON'S
  55. DICYCLOMINE
    3*M ANTAGONIST

    MOA -- AT GI TRACT

    PHARM -- SAME AS ATROPINE & SCOPE

    THERA -- PREVENT BOWEL SPASM & DEC PAIN W/ IBS
  56. HYOSCYAMINE
    3*M ANTAGONIST

    MOA -- AT GI TRACT

    PHARM -- SAME AS ATROPINE & SCOPE

    THERA -- PREVENT BOWEL SPASM & DEC PAIN W/ IBS
  57. OXYBUTYNIN
    3*M3 ANTAGONIST

    URGE INCONTINENCE

    "DOTTS"

    MOA -- DIRECT ANTISPASMODIC EFFECT AT DETRUSOR MUSCLE

    PHARM -- SAME AS ATROPINE & SCOPE

    THERA -- URGE INCONTINENCE (OAB)

    ADVERSE -- DROWSINESS, SOMNOLENCE, DIZZINESS
  58. TOLTERODINE
    3*M3 ANTAGONIST

    "DOTTS"

    MOA -- ?

    PHARM -- SAME AS ATROPINE & SCOPE

    THERA -- URGE INCONTINENCE (OAB)

    ADVERSE -- DRY MOUTH, BLURRED VISION, CONSTIP & SOMNOLENCE
  59. SOLIFENACIN
    3*M3 ANTAGONIST

    "DOTTS"

    MOA -- SELECTIVE M3 ANTAGONIST (DETRUSOR)

    PHARM -- SAME AS ATROPINE & SCOPE

    THERA -- URGE INCONTINENCE (OAB)

    ADVERSE -- FEWER CNS EFFECTS.

    LESS DRY MOUTH THAN OXYBUTIN, TOLTERIDINE TROSPIUM?
  60. DARIFENACIN
    3*M3 ANTAGONIST

    "DOTTS"

    MOA -- SELECTIVE M3 ANTAGONIST

    PHARM -- SAME AS ATROPINE & SCOPE

    THERA -- URGE INCONTINENCE (OAB)

    ADVERSE -- NO CNS OR CV EFFECTS!

    LESS DRY MOUTH THAN OXYBUTIN, TOLTERIDINE, TROSPIUM
  61. MYASTHEMIA GRAVIS
    GIVE N2 AGONIST NEOSTIGMINE AND PYRIDOSTIGMINE WHICH ALSO BLOCK AChase.

    EFFECT NMJ AND PERIPH SITES --> SAL, RHINITIS, BRADYCARDIA, BRONCHSPASM, BOWEL CRAMP, DIARRHEA, AND URINARY INCONT

    GIVE M ANTAGONIST ATROPINE TO PREVENT S/E
  62. PARKINSONS
    LACK OF DA STIM AND RESULTANT INC M STIM IN NIGROSTRIATAL TRACK OF BRAIN

    INH OF AChase WHICH ENTER CNS LIKE PHYSOSTIGMINE WORSEN Sx

    • "BBAT!" -- BLOCK CENTRAL M RECEPTORS
    • 1) BENZTROPINE (COGENTIN)
    • 2) BIPERIDEN (AKINETON)
    • 3) ATROPINE
    • 4) TRIHEXYPHENIDYL (ARTANE)
    • 5) DIPHENHYDRAMINE (ANTI-HIST BENADRYL)

    MOST EFFECTIVE AGAINST TREMOR, SOME AGAINTS RIGIDITY, AND LITTLE AGAINST AKINESIA/DYSKINESIA

    S/E -- CYCLOPLEGIA, CONSTIP, URINARY RET, DRY MOUTH
  63. S/E OF ATROPINE-LIKE DRUGS
    M ANTAGONISTS

    • RED AS A BEET
    • MAD AS A HATTER
    • DRY AS A BONE
    • HOT AS A PISTOL

    • Tx FOR OVERDOSE:
    • GASTRIC LAVAGE
    • RESP & CIRC SUPPORT
    • SPONGE BATH
    • FOLEY CATH
    • DARK ROOM
    • BENZO FOR SEDATION

    • CNS Sx:
    • NERVOUSNESS
    • EXCITIATION
    • CONF
    • HALL
    • WEAKNESS
    • GIDDINESS
    • MUSC INCOORD
    • HYPERTENSE
    • MANIA

    • PNS:
    • DRY MOUTH / THIRST
    • HOT, DRY, FLUSHED SKIN
    • MYDRIASIS / BLURRED VISION
    • TACHYCARDIA
    • URINE RET
    • ABSENT BOWEL SOUNDS
  64. MOTION SICKNESS
    CAUSED BY EXCESSIVE M RECEPTORS IN VEST NUC AND RET FORMATION

    SCOPOLAMINE (PATCH) -- CAUSES ANTEROGRADE AMNESIA! ACCENTUATED BY ETHANOL

    DIPHENHYDRAMINE (DRAMAMINE)
  65. DIPHENHYDRAMINE
    BENADRYL

    3*M ANTAGONIST

    MOA -- AT CENTRAL M RECEPTORS & ANTIHIST

    PHARM -- SAME AS ATROPINE & SCOPE

    THERA -- CAN BE USED FOR PARKINSON'S
  66. OVERACTIVE BLADDER DRUGS
    "DOTTS"

    3*M ANTAGONISTS

    • DARIFENACIN
    • OXYBUTYNIN
    • TOLTERODINE
    • TROSPIUM (4*M)
    • SOLIFENACIN
  67. TERTIARY MUSCARINIC RECEPTOR ANTAGONISTS
    "ABC 3D TRIPLE-T HOSS"

    • ATROPINE
    • BENZTROPINE
    • CYCLO-PENTO-LATE

    • DI-CYCLOMINE
    • DI-PHEN-HYDRA-MINE
    • DAR-IDEN-ACIN

    • TRI-HEXY-PHEN-IDYL
    • TOL-TERO-DINE
    • TROPIC-AMIDE

    • HY-OSCY-AMINE
    • OXY-BUTY-NIN
    • SCOPOLAMINE
    • SOLI-FEN-ACIN
  68. N-METHYLATROPINE
    4*M ANTAGONIST

    PHARM -- SAME AS 3*M. DOES NOT ENTER CNS!
  69. METHSCOPOLAMINE
    4*M ANTAGONIST

    PHARM -- SAME AS 3*M. DOES NOT ENTER CNS
  70. N-METHYLHOMATROPINE
    4*M ANTAGONIST

    PHARM -- SAME AS 3*M ANT. DOES NOT ENTER CNS
  71. TROSPIUM
    4*M ANTAGONIST

    "DOTTS" OVER-ACTIVE BLADDER DRUG

    MOA -- NON-SELECTIVE MUSC ANTAGONIST

    THERA -- URGE INCONTINENCE (OAB)

    ADVERSE -- PERIPH ANTI-M Sx
  72. IPRATROPIUM
    4*M ANTAGONIST
  73. GLYCOPYRROLATE
    4*M ANTAGONIST

    MOA -- ALSO PREVENTS UNWANTED M STIM RESULTING FROM AChase INH AT SITES INNERVATED BY PNS. LIKE ATROPINE

    PHARM -- SAME AS 3*M ANT. DOES NOT ENTER CNS

    THERA -- PERI-OP USE

    DEC PROD OF SALIV / PULM SECRETIONS

    • COUNTER BRADYCARDIA CAUSED BY:
    • OCULAR PRESSURE
    • VISCERAL TRACTION
    • CAROTID SINUS STIM
    • INJ OF MULTI DOSES OF SUCC

    COMBO IV GLYCOPYRROLATE + NEOSTIG: REVERSE COMPETITIVE NEUROMUSC BLOCKADE CAUSED BY DRUGS (ex d-TUBOCURARINE)
  74. TIOTROPIUM
    4*M ANTAGONIST
  75. QUATERNARY MUSCARINIC RECEPTOR ANTAGONIST
    • N-METHYL-ATROPINE
    • METH-SCOPOLAMINE
    • TIO-TROP-IUM
    • IPRA-TROP-IUM
    • GLYCO-PYROL-ATE
  76. NICOTINE
    N RECEPTOR AGONIST

    MOA -- DIRECT STIM OF PERIPH N1 & N2 CHOL RECEPTORS

    BENZOPYRENE IN CIG SMOKE INDUCES HEP CYP450

    CNS: DIRECT STIM N1 --> RELEASES NA & DA. MAY INC/DEC RELEASE OF ACh

    *ADDICTION -- DA RELEASE FROM NUC ACCUMB

    • PHARM -- SMOKING:
    • ACUTE CNS EFFECTS:
    • INC ALERTING PATTERN ON EEG,

    FAC OF ATTENTION & MEM,

    DEC AGGRESSION,

    DEC APPETITE,

    DEC SKEL MUSC TONE & DTR VIA STIM OF RENSHAW INTERNEURONS,

    INC PHYSIO TREMOR

    • ACUTE CARDIO EFFECTS:
    • INC SBP, DBP, PP, HR VIA STIM OF SYMP GANG & AORTIC CHEMORECEPTORS

    TOLERANCE DEVS RAPIDLY --> LONG-TERM EFFECTS ON BP & HR ARE SLIGHT

    DEC SKIN TEMP & DIGITAL BLOOD FLOW

    • SNUFF:
    • CARDIO -- INC CV DISEASE esp HYPERTNSN, INC PLASMA INSULIN & FIBRINOGEN. SNUFF FEWER CNS EFFECTS THAN SMOKING

    • ORAL CANCER
    • -ORAL LEUKOPLAKIA
    • -LOCAL PERIODONTAL DISEASE (GUMS)
    • -SMOKELESS TOB DOES NOT INC RISK OF ORAL/DIGEST CANCER, BUT CIGS & ALC --> HI RISK; PROPORTIONAL TO USE
    • ADVERSE -- VERY H20 SOLUBLE --> PASSES QUICK FROM BLOOD TO BRAIN. RAPIDLY ABS FROM BUCCAL, RESP, & SKIN

    • **ACUTE TOX:
    • ORAL INGESTION --> VOMITING INDUCED BY CNS EFFECTS OF NICOTINE --> ELIMS MOST OF TOBACCO & LIMITS TOX

    INSECTICIDES, N/V ABDOM CRAMPING & DIARRHEA, SAL & SWEAT, HEADACH, DIZZY, DISORIENTATION, MUSC WEAK, BP FALLS, HR IRREG, SHALLOW BREATHING, CARDIO COLLAPSE & CONVULSIONS OFTEN PRECEDE DEATH FROM RESP FAILURE

    • **CHRONIC TOX:
    • INC LDL AND TG, LOWER HDL

    DEC PGI2 AND NO --> CONSTRIC ARTERIOLS & PLATELET AGGREGATION

    NEUTROPHIL ACTIVATION AND AGG --> INFLAM DAMAGE

    CARDIAC DYSRHYTHMIA VIA CO

    CANCER --> BENZOPRENES DAMAGE p53 TUMORE SUPPRESSOR

    COPD & ASTHMA (REDUCE CILIARY ACTIVITY)

    SMOKER'S FACE: WRINKLING

    TREATMENT -- GASTRIC LAVAGE OR DRUG-INDUCED EMESIS, INTUBATION & ARTIFICIAL RESP, DRUG THERA FOR SHOCK & CONVULSIONS
  77. SUCCINYLCHOLINE
    N AGONIST

    • MOA --
    • GIVEN IV

    INITIAL SINGLE CONTRACTION OF SKEL MUSC FOLLOWED BY 3-5 MINS OF FLACCID PARALYSIS

    PHARM -- FLACCID PARALYSIS

    MOST OF IV DOSE DEGRADED BY PLASMA CHOLase BEFORE REACHING NMJ

    NOT METABOLIZED BY TISSUE AChase

    PARTIAL REPOL POSS WHILE SUCC STILL PRESENT BUT NMJ BLOCKADE PERSISTS

    NMJ BLOCKADE IS TERMINATED BY DRUG DIFFUSING AWAY
  78. NICOTINIC RECEPTOR AGONIST
    NICOTINE SUCCS!

    • NICOTINE
    • SUCCINYL-CHOLINE (cholinergic also)
  79. GANGLIONIC BLOCKING DRUGS
    N1-RECEPTOR ANTAGONISTS

    TRIMETHAPHAN -- CONTROLLED HYPER TENSION DURING HEAD & NECK SURGERY. CAN ALSO CAUSE HIST RELEASE --> FURTHER VASODILATION

    MECAMYLAMINE -- FOR AUTONOMIC HYPER-REFLEXIA -- CONTROLS BY PREVENTING PAROXYSMAL INC IN SYMP ACTIVITY
  80. MECAMYLAMINE
    N1 ANTAGONIST

    GANGLIONIC BLOCKING DRUG

    MOA -- GIVEN P.O.

    COMP BLOCKADE N1-CHOLINERGIC RECEPTORS IN AUTONOMIC GANGLIA

    -->PREVENTS ALL SYMP & PARASYMP NERVE ACTIVITY FROM REACHING THE EFFECTOR ORGAN

    PHARM -- KNOW IF SYMP OR PARASYMP IS DOMINANT IN EACH ORGAN

    BLOCKADE OF SYMP:

    ARTERIODILATION --> DEC TPRVENODILATION --> DEC PRELOAD

    DEC CARDIAC dp/dt

    DEC CO --> HYPOTENSION (DEC TPR ALSO)

    DEC SWEATING

    IMPOTENCE

    • BLOCKADE OF PARA GANGLIA:
    • TACHYCARDIA

    MYDRIASIS & CYCLOPLEGIA

    DEC SAL & LACRIM

    DEC GI SEC, MOT, TONE

    DEC GASTRIC ACID SEC

    DEC RELEASE OF PANC ENZ & BILE

    CONSTIP & URINARY RETENSION

    IMPOTENCE

    THERA -- PROD CONTROLLED HYPOTENSION DURING HEAD & NECK SURGERY

    CAUSE HIST RELEASE --> FURTHER VASODILATION

    AUTONOMIC HYPERREFLEXIA IN pt W/ HI LEVEL SPINAL INJURIES (T5 & ABOVE)

    • Sx:
    • HYPERTENSION --> POSS MI, HEMORR STROKE & RENAL HEMORR

    BRADYCARDIA (2* TO HYPERTN)

    SWEATING

    PILOERECTION

    *CONTROLS Sx BY PREVENTING PAROXYSMAL INC IN SYMP (MECAMYLAMINE)
  81. TRIMETHAPHAN
    N1 ANTAGONIST

    GANGLIONIC BLOCKING DRUG

    MOA -- GIVEN IV

    COMP BLOCKADE N1-CHOLINERGIC RECEPTORS IN AUTONOMIC GANGLIA -->

    PREVENTS ALL SYMP & PARASYMP NERVE ACTIVITY FROM REACHING THE EFFECTOR ORGAN

    PHARM -- KNOW IF SYMP OR PARASYMP IS DOMINANT IN EACH ORGAN

    • BLOCKADE OF SYMP:
    • ARTERIODILATION --> DEC TPR

    VENODILATION --> DEC PRELOAD

    DEC CARDIAC dp/dt

    DEC CO --> HYPOTENSION (DEC TPR ALSO)

    DEC SWEATING

    IMPOTENCE

    • BLOCKADE OF PARA GANGLIA:
    • TACHYCARDIA

    MYDRIASIS & CYCLOPLEGIA

    DEC SAL & LACRIM

    DEC GI SEC, MOT, TONE

    DEC GASTRIC ACID SEC

    DEC RELEASE OF PANC ENZ & BILE

    CONSTIP & URINARY RETENSION

    IMPOTENCE

    THERA -- PROD CONTROLLED HYPOTENSION DURING HEAD & NECK SURGERY

    CAUSE HIST RELEASE --> FURTHER VASODILATION

    AUTONOMIC HYPERREFLEXIA IN pt W/ HI LEVEL SPINAL INJURIES (T5 & ABOVE)

    • Sx:
    • HYPERTENSION --> POSS MI, HEMMORRHAGIC STROKE & RENAL HEMORR

    BRADYCARDIA (2* TO HYPERTN)

    SWEATING

    PILOERECTION

    *CONTROLS Sx BY PREVENTING PAROXYSMAL INC IN SYMP (MECAMYLAMINE)
  82. NE
    DIRECT ADRENERGIC AGONIST

    LOCAL (NOT A CIRC HORMONE)

    IN PLASMA, CLEARED BY LIVER (PHASE I - COMT, MAO & PHASE II (CONJ) & LUNGS

    MOA -- a & b AGONIST

    a > b1 > B2

    VASOCONSTRICT --> ARTERIOLES IN SKIN, KID, & GI TRACT CONTAIN PRIMARILY a RECEPTORS

    VASODILATE --> ARTERIOLES IN LIVER & SKEL MUSC CONTAIN PRIMARILY b2 RECEPTORS

    PHARM -- ONLY b EFFECTS ARE INC CARDIAC dp/dt, INC VENOUS RETURN VIA DEC HEP VENOUS RESISTANCE

    ENDOG NE RELEASE --> DIRECT b1 STIM --> INC HR

    vs.

    NE GIVEN IV --> INC BP --> BAROREFLEX MEDIATED DEC HR

    MOSTLY a EFFECTS:

    DIRECT

    ARTERIOLAR VASOCONSTRICTION (a1) --> INC TPR --> INC DBP

    DEC BLOOD FLOW TO CUTANEOUS, KID, GI, & SKEL MUSC

    INDIRECT

    INC DBP --> BAROREFLEX MEDIATED BRADYCARDIA VIA INC VAGAL TONE

    SV UNCHANGED (STARLING) EVEN THOUGH INC AFTERLOAD

    DEC HR --> INC SV DESPITE NO CHANGE OR SLIGHT DEC IN CO

    INC DBP PREVENTS INC SV & CO WHICH OCCURS WHEN dp/dp & VENOUS RETURN INC

    THERA -- DIRECT AGONIST: VASOPRESSOR AGENT WHEN CO & TISSUE PERFUSION ARE RELATIVELY NORMAL (ex SPINAL SHOCK)

    VASOCONSTRICTOR AGENT W/ LOCAL ANESTHETIC DRUGS

    ADVERSE -- CARDIAC ARRHYTHMIAS (b)

    ANGINA IN pt W/ CAD (b)

    CEREBROVASC HEMORR (INC BP)

    PULM EDEMA (INC TPR)

    TREMOR (b2)
  83. EPI
    DIRECT ADRENERGIC AGONIST

    CIRCULATING HORMONE

    MET BY PHASE I - COMT, MAO & PHASE II IN LIVER

    NOT CLEARED BY LUNGS

    SEC IN VENA CAVA --> BYPASS LIVER IN ROUTE TO HRT

    FIGHT OR FLIGHT

    MOA -- a & b AGONIST

    b2 > b1 > a

    VASOCONSTRICT --> ARTERIOLES IN SKIN, KID & GI CONTAIN PRIMARILY a RECEPTORS

    VASODILATE --> ARTERIOLES IN LIVER & SKEL MUSC CONTAIN PRIMARILY b2

    PHARM --

    SMALL IV DOSE: PHYSIO PLASMA LEVELS

    DEC TPR --> SLIGHT DEC DBP

    NET VASODIL VIA b2 STIM (LIVER, SKEL MUSC > a --> KID, GI

    LARGE IV DOSE:

    INC TPR --> INC DBP

    NET VASOCONST VIA a STIM

    • b1 STIM --> INC dp/dt --> INC PP
    • ------------------

    BOTH SMALL & LARGE IV DOSES:

    • INC CARDIAC dp/dt
    • INC HR
    • INC SV --> INC PP & SBP
    • DEC BLOOD FLOW TO KID, GI, SKIN

    • INC HRT WORK (O2 DEMAND) --> INC COR BLOOD FLOW
    • ------------------------

    GIVEN S.C. TO Rx ANAPHYLACTIC rxn:

    • INC PP
    • INC SBP
    • INC DBP

    Dec DBP to produce max incr in SV/CO for incr tissue perfusion w/o incr BP (DBP falls)

    Incr blood flow to lungs, liver & brain

    THERA -- DOC FOR ANAPHYL rxn: REVERSE BRONCH-CONST & LARYNG EDEMA

    DOC PRIAPISM INJECTION OF DILUTE SOLUTION INTO CORPORA CAVERNOSA --> a STIM --> CONTRACTS SMOOTH MUSC

    BRONCH-DIL IN pt W. ASTHMA & COPD

    TOPICAL: LOWERS IOP BY INC OUTFLOW OF AQ HUM (a1)

    VASOCONST AGENT W/ LOCAL ANESTHETIC DRUGS. PREVENTS ANESTH FROM FLOWING AWAY. PREVENTS BLEEDING

    USED AS + INOTROPIC & CHRONOTROPIC AGENT IN CARDIAC ARREST pts (1/3 SAVED W/ EPI; 2/3 W/ DC COUNTERSHOCK

    ADVERSE -- CARDIAC ARRHYTHMIAS (b)

    ANGINA IN pts W/ CAD (b)

    CEREBROVASC HEMORR (INC BP)

    PULM EDEMA (INC TPR)

    TREMOR (b2)

    ANX
  84. DOPAMINE
    ADRENERGIC AGONIST

    STIM IS DOSE DEPENDENT (D1 > b1 > a1)

    • MOA --
    • SMALL DOSE (0.5 - 2)
    • D1 -- DILATE RENAL AFFERENT ARTERIOLS --> INC RBF

    --> INC GFR & Na SEC VIA DEC IN FILT FRAC (HEMODYNAMIC DIURESIS)

    SMALL DEC OR NO CHANGE IN DBP FROM DEC RENAL VASC RESISTANCE

    • MEDIUM DOSE:
    • D1 (RENAL) & b1 (HRT) STIM --> INC dp/dt w/ LITTLE EFFECT ON HR

    INC dp/dt --> INC SV/CO --> FURTHER INC RBF & GFR --> FURTHER INC Na/H2O EXCRETION

    • LARGE DOSE:
    • BEGINS TO STIM a RECs IN RESISTANCE ARTERIOLES & VENULES

    INC TPR --> INC AFTERLEAD (DBP) --> DEC SV/CO B/C HRT DAMAGED BY MI (STARLING MECH) DESPITE DA STIM STILL INCREASING dp/dt

    VENOCONST --> INC VENO RETURN & CARD FILLING PRESSURE:

    INC AFTERLOAD --> (-) EFFECT ON SV SO LV WALL TENSION INC DURING DIASTOLE

    --> INC O2 DEMAND --> FURTHER ISCHEMIA TO ALREADY DAMAGED MYOCARDIUM

    PREVENT/REVERSE VIA IV OF DOBUTAMINE OR SODIAM NITROPRUSSIDE (VIA RELEASE NO TO DIL ART & VEN (BALANCED VASODILATION))

    • PHARM --
    • INC CO POST MI

    INC BP IN SEPTIC & HEMORRHAGIC SHOCK

    INC CO IN CHF WHICH IS REFRACTORY TO DIGOXIN PLUS DIURETICS

    INC URINE FLOW IN Rx OF BARBITURATE & SALICYCLATE POISONING

    SMALL DOSE USED TO MAINTAIN URINE FLOW IN ICU

    • ADVERSE --
    • SMALL & MEDIUM: LITTLE EFFECT ON HR

    LARGE: TACHYCARDIA --> WORSEN ISCH & POSS PRECIPITATE DYSRHYTHMIAS

    ALSO INC TPR

    PULMONARY EDEMA (INC TPR)

    CARDIAC ARRHYTHMIAS (b)

    ANGINA IN PTs W/ CAD (b)

    PT POSS DEV TOLERENCE TO (+) INOTROPIC EFFECTS OF DA & DOBUTAMINE (DOWN REG RECs)
  85. TERBUTALINE
    ADREN AGONIST

    MOA -- SELECTIVE b2

    b2 >> b1

    PHARM -- RELAX BRONC MUSC

    THERA -- ASTHMA COPD, BRONCHITIS

    • ADVERSE --
    • *Cardiac arrhythmias (β)

    *Angina in pts w/ CAD (β)

    *Tremor (β2)
  86. ALBUTEROL
    ADREN AGONIST

    MOA -- SELECTIVE b2

    b2 >> b1

    PHARM -- RELAX BRONC MUSC

    THERA -- ASTHMA COPD, BRONCHITIS

    EVENTUALLY DESENSITIZE (RECEPTOR DOWN REG). USE CORTICOSTEROIDS FOR CHRONIC TREATMENT AND ALB FOR ACUTE.

    • ADVERSE --
    • *Cardiac arrhythmias (β)

    *Angina in pts w/ CAD (β)

    *Tremor (β2)
  87. OXYMETAZOLINE
    ADREN AGONIST

    MOA -- a ONLY

    THERA -- NASAL DECONG

    OXYMETAZOLINE LONGER DURATION OF ACTION > PHENYLEPHRINE

    • ADVERSE --
    • RENAL & MESENTERIC ISCH (a)

    REBOUND NASAL CONG (NASAL VC)
  88. TYRAMINE
    INDIRECT ADREN AGONIST

    MOA -- RELEASE OF STORED ENDOGENOUS NE FROM NORADREN FIBERS

    • PHARM --
    • INC BP TO SOME EXTENT BC RELEASE NE FROM SYMP NERVES WHICH INNERVATE BLD VESS
    • --NATURAL CONSTITUENT OF MANY FOODS, esp FERMENTED LIKE CHEESE WINE BEER PICLED HERRING

    --EFFECTS ARE CONFINED TO PERIPH BC QUARTERNARY

    THERA -- NOT USED AS A THERA AGENT

    ADVERSE -- CEREBROVASC HEMORR (INC BP)
  89. PSEUDOEPHEDRINE
    MIXED ADREN AGONISTS

    STERIOISOMERS OF EPHEDRINE

    MOA -- DIRECT AGONIST AT ADRENO

    CAUSE RELEASE OF ENDO NE

    PHARM -- LIPID SOL AGENT ENTERS CNS

    CAUSES LESS CNS EXCITIATION & LESS INC IN HR & BP THAN EPHEDRINE

    THERA -- NASAL & SINUS DECONG

    DEC NASAL BLD VESS SWELLING & DEC FEELING OF PRESSURE

    • ADVERSE --
    • --INSOMNIA
    • --*cardiac arrhythmias (β)
    • --*Angina in pts w/ CAD (β)
    • --*Cerebrovasc hemorrhage (incr BP)
    • --*Tremor (β2)
    • --*Rebound nasal congestion (nasal VC
  90. EPHEDRINE
    MIXED ADREN AGONIST

    MOA -- DIRECT AGONIST AT b1 & b2

    RELEASE OF ENDOG NE --> STIM a&b ADREN RECs

    PHARM -- LIPID SOL AGENT --> ENTERS CNS

    • DIRECT b STIM:
    • --BRONCHDIL IN ASTHMA
    • --INC AV COND IN AV BLOCK

    • INDIRECT a ACTION:
    • --MYDRIASIS
    • --INC BP
    • --NASAL DECONG

    • USED AS PRESSOR AGENT TO REVERSE HYPOTENSE DURING ANESTHESIA
    • --BOLUS GIVEN IV INC BP BY 10-20 MMHg IN 60sec
    • --INC BP PERSISTES FOR 60 mins

    • NE IN BRAIN:
    • --CENTRAL EXCITATION, MILDER < AMPHETAMINE

    • NET EFFECT:
    • --INC BP, HR, CO, AV COND
    • --BRONCH-DIL w/ INC FEV1
    • --MYDRIASIS
    • --INSOMNIA

    THERA --

    • DIRECT b
    • --ASTHMA
    • --INC AV COND IN AV BLOCK

    • INDIRECT a
    • --MYDRIASIS
    • --INC BP
    • --NASAL DECONG
    • --HYPERTENSE DURING ANESTHESIA

    --ON PROSCRIBED LIST FOR ATHLETES

    ADVERSE --

    • DIET DRUG
    • --ACUTE PSYCHOTIC REACTION
    • --INC HTN
    • --INSOMNIA
    • --CARDIAC ARRYTHMIA (b)
    • --ANGINA IN pt w/ CAD (b)
    • --CEREBROVASC HEMORR (INC BP)
    • --TREMOR (b2)
    • --REBOUND NASAL CONG (NASAL VC)
  91. AMPHETAMINE
    INDIRECT ADREN AGONIST ("TAP")

    MOA -- RELEASE OF STORED NE FROM NORADREN FIBERS

    ALSO BLOCKS UPTAKE

    PHARM -- INC BP TO SOME EXT BC RELEASE NE FROM SYMP NERVES WHICH INNERVATE BLD VESS

    • LIPID SOL AGENT:
    • ENTERS CNS --> CENTRAL & PERIPH RELEASE OF NE

    THERA -- ADHD & ADD

    • ADVERSE -- ENTERS CNS
    • --INSOMNIA

    --CEREBRAVASC HEMORR (INC BP)

    --PSYCH DISTURBANCES AFTER PROLONGED USE!!!
  92. PHENYLEPHRINE
    ADREN AGONIST

    MOA -- a1 SELECTIVE

    GIVEN IV

    PHARM -- "PURE a"

    • GIVEN IV --> NE EFFECTS:
    • --INC DBP & INC SBP
    • --SV UNCHANGED
    • --DEC HR VIA BAROREFLEX

    • CV EFFECTS ARE SAME AS NE:
    • --ART VASOCONST --> INC TPR --> INC DBP
    • --BAROREFLEX-MEDIATED BRADYCARDIA
    • --DEC BLD FLOW TO ALL ORGANS

    • THERA --
    • --SYSTEMIC VASOCONST AGENT

    --LOCAL APP RELIEVES NASAL CONG BY CONST BLD VESS IN MUCOSA

    --OXYMETAZOLINE LONGER DURATION OF ACTION > PHENYLEPHRINE

    --LOCAL APP PRODs MYDRIASIS BY CONTRACTION OF RADIAL MUSC OF IRIS. USED FOR FUNDO EXAMS & OCULAR APPEARANCE

    • ADVERSE --
    • --RENAL & MESENTERIC ISCH (a)

    --CEREBROVASC HEMORR (INC BP)

    --REBOUND NASAL CONG (NASAL VC)

    --??PULMONARY EDEMA (INC TPR)
  93. RITODRINE
    ADREN AGONIST

    MOA -- SELECTIVE b2

    b2 >> b1

    PHARM -- RELAX UTERINE SMOOTH MUSC

    THERA -- DELAY PARTURITION (NOT USED MUCH ANYMORE)

    MOVE FETUS OUT OF BREECH POS (EXT VERSION OF FETUS TO A VERTEX POSITION PRIOR TO BIRTH

    • ADVERSE --
    • *Cardiac arrhythmias (β)

    *Angina in pts w/CAD (β)

    *Tremor (β2)
  94. PIRBUTEROL
    ADREN AGONIST

    MOA -- SELECTIVE b2

    b2 >> b1

    • ADVERSE --
    • *Cardiac arrhythmias (β)

    *Angina in pts w/ CAD (β)

    *Tremor (β2)
  95. SALMETEROL
    ADREN AGONIST

    MOA -- SELECTIVE b2

    b2 >> b1

    PHARM -- RELAX BRONC MUSC

    THERA -- ASTHMA COPD, BRONCHITIS

    • ADVERSE --
    • *Cardiac arrhythmias (β)

    *Angina in pts w/ CAD (β)

    *Tremor (β2)
  96. ISOPROTERENOL
    ADREN AGONIST

    MOA -- GIVEN IV

    PURE b STIM (b1 = b2)

    • PHARM --
    • LIKE EPI EXCEPT NO a STIM

    b1 STIM --> INC dp/dt, HR, SV --> INC PP

    INC PP FROM DEC DBP. SBP UNCHANGED / DEC DESPITE INC SV

    b2 STIM --> VASODIL @ ALL VASC --> DEC TPR & DEC DBP

    ?? INC FALL IN TPR & DBP & INC IN BLD FLOW THRU KIDNEY, GI, SKEL MUSC, LIVER

    • THERA --
    • INC AV CONDUCTION IN AV BLOCK

    USED AS (+) INOTROPIC (INFLUENCE dp/dt) & CHRONOTROPIC (AFFECT HB) AGENT IN CARDIAC ARREST

    • ADVERSE --
    • CARDIA ARRHYTHMIAS (b)

    ANGINA IN pts w/ CAD (b)

    TREMOR (b2)

    TACHYCARDIA (ISOPROTERENOL > ALBUTEROL)
  97. DOBUTAMINE
    ADREN AGONIST

    MOA -- RACEMIC MIX OF (+) (-) ENANTIOMERS --> BOTH STIM b1 & b2

    • (-) = a1 AGONIST
    • (+) = a2 ANTAGONIST
    • (+/-) CANCEL OUT

    b1 >= b2

    • PHARM --
    • (+) ENANT BLOCK VASOCONST CAUSED BY (-)

    b1 STIM --> INC SV

    • b2 STIM:
    • --ARTERIODILATION --> DEC TPR --> POSS DEC DBP

    --VENODIL --> DEC VENOUS RETURN & DEC CARDIAC FILLING PRESSURE IN pt w/ MI

    INC GFR SOLELY FROM INC CO.

    NO EFFECT @ RENAL D1 RECs

    • THERA --
    • ***DOBUTAMINE >> DOPA***
    • DISTINCT ADVANTAGES IN Rx MI

    • 1) DOBUT DOSNT INC DBP
    • 2) DOBUT IS LESS LIKELY TO CAUSE TACHYCARDIA
    • 3) DOBUT CAUSES VENODIL --> DEC VEN RET, SO CARDIAC FILLING PRESSURE IS DEC

    INC CO AFTER MI

    INC CO IN SEPTIC & CARDIOGENIC SHOCK

    a-BLOCK & b2 STIM --> PREVENTS/REVERSES INC TPR CAUSED BY INC DOSE DA

    • ADVERSE --
    • EXCESSIVE DOSE:

    TACHYCARDIA

    CARDIA DYSRYTHMIAS

    CARDIAC ARRHYTHMIAS (b)

    ANGINA IN pts w/ CAD (b)

    TREMOR (b2)

    pt POSS DEV TOLERANCE TO (+) INOTROPIC EFFECTS OF DA & DOBUTAMINE (DOWN REG RECs)
  98. ADRENERGIC AGONISTS
    NED PEA DUMB-BUTT ISO TERRIBLE, RIGHT? PHEN EFFRINE ALL-BUTT TRIED OXY-SALMON

    • NOREPINEPHRINE
    • EPINEPHRINE
    • DOPAMINE
    • PSEUDO-EPHEDRINE
    • EPHEDRINE
    • AMPHETAMINE
    • DOBUTAMINE
    • ISO-PROTER-ENOL
    • TERBUTALINE
    • RITODRINE
    • PHENYL-EPHRINE
    • ALBUTEROL
    • TYRAMINE
    • OXY-META-ZOLINE
    • SALMETEROL
  99. PHENOXYBENZAMINE
    a BLOCKER

    MOA -- NONCOMP REC BLOCKADE DUE TO COVALENT BINDING (ALKYLATION) OF RECs

    a1 >> a2

    • PHARM --
    • --DEC TPR & BP
    • --INC VENOUS CAPACITANCE
    • --INC HR
    • --INC dp/dt

    NET EFFECT -- NO CHANGE IN CO

    THERA -- CONTROL BP IN pts w/ MAL TUMORS

    • ADVERSE --
    • --*angina → produce baroreflex incr in HR, dp/dt & O2 demand
    • --*tachycardia
    • --* Miosis (α1)
    • --*Inhb of ejaculation (α1)
    • --*Incr insulin release (α2)
  100. PHENTOLAMINE
    a BLOCKER

    a1 = a2

    • PHARM
    • --DEC TPR & BP
    • --INC VENOUS CAPACITANCE
    • --INC HR
    • --INC dp/dt

    • THERA
    • --PERI-OP w/ NONSELECTIVE b-BLOCKER TO CTR BP DURING MANIP OF PHEOCHROMOCYTOMA TUMOR

    --LOCAL USE TO REVERSE ISCH & TISS NEC CAUSED BY EXTRAVASATION OF DA FROM VEINS DURING IV (DA CAUSES MAJOR VC AT INC DOSE)

    --IMPOTENSE (INJ INTO CORP CAV)

    • ADVERSE
    • --*angina → produce baroreflex incr in HR, dp/dt & O2 demand
    • --*tachycardia
    • --* Miosis (α1)
    • --*Inhb of ejaculation (α1)
    • --*Incr insulin release (α2)
  101. PRAZOSIN (terazosin, doxazosin)
    a BLOCKER

    MOA -- ONLY a1 BLOCK

    • PHARM
    • --DEC TPR & BP
    • --INC VENOUS CAPACITANCE

    • NET EFFECT
    • --NO CHANGE HR, dp/dt & CO!!!

    • THERA
    • --1st LINE IN MILD TO MOD HTN

    --PERI-OP w/ NONSELECT b-BLOCKER FOR BP DURING MANIP OF PHEOCHROMOCYTOMA

    --MOST USEFUL IN Rx OF CONDITIONS ASSOC W/ MARKED VASOCONST (RAYNAUD'S SYND, FROSTBITE & CHRON VASOSPASM)

    --SMALL DOSE CAN RELIEVE URINARY OBST TO INC URINE FLOW RATE IN pt W/ PROSTATIC HYPERTROPHY

    • ADVERSE
    • --MIOSIS (a1)
    • --INH OF EJEC (a1)
  102. TAMSULOSIN
    a BLOCKER

    MOA -- ONLY a1A BLOCK

    THERA -- DOC FOR BPH

    SMALL DOSE CAN RELIEVE URINARY OBST TO INC URINE FLOW RATE (FLOMAX) IN pt w PROSTATIC HYPERTROPHY
  103. Tx OF ESSENTIAL TREMOR
    NON-SELECTIVE b-BLOCKER:

    PROPRANOLOL OR TIMOLOL

    ENHANCED BY EXCESSIVE INTAKE OF CAFFEINE, LACK OF SLEEP, ALC, HANGOVER AND STREN EXCERSISE.
  104. DRUGS FOR PHEOCHROMOCYTOMA TO CONTROL BP DURING SURGERY
    • PRAZOSIN (a1)
    • OR
    • PHENTOLAMINE (a1 = a2)

    +

    NON-SELECTIVE b ANATAGONIST (PROPRANOLOL)
  105. LABETALOL
    a BLOCKER

    MOA -- BLOCKS a1, b1 & PARTIAL AGONIST FOR b2 (intrinsic sympathomimetic activity)

    • PHARM
    • --DEC TPR, BP, dp/dt
    • --DEC NO CHANGE HR
    • --NO CHANGE CO

    • THERA
    • -1st LINE IN MILD TO NED HTN
    • --LOWER BP SLOWLY IN pt w HTN EMERGENCY
    • --NOT EFFECTIVE IN CTR BP IN pt w PHEOCHROMOCYTOMA

    • ADVERSE
    • --MIOSIS (a1)
    • --INH OF EJAC (a1)
  106. PAPAVERINE
    Tx OF IMPOTENCE

    MOA -- PDE INH

    (SILDENAFIL ALSO)
  107. ALPROSTADIL
    Tx OF IMPOTENCE

    MOA -- TOPICAL OR INJ INTO CORPUS CAVERNOSA

    PGE-1 ANALOG
  108. PHENTOLAMINE
    IMPOTENCE Tx

    MOA -- INJ INTO CORPUS CAVERNOSA

    COMPET BLOCK OF a1 & a2 REC (a1 = a2)

    • PHARM
    • --DEC TPR & BP
    • --INC VENOUS CAPACITANCE
    • --INC HR & dp/dt

    NET EFFECT -- NO CHANGE IN CO

    • THERA
    • --USED PERI-OP w NON-SPECIFIC b-BLOCKER TO ctr BP DURING MANIP OF PHEOCHROMOCYTOMA TUMOR

    --LOCAL USE TO REVERSE ISCH & TISS NEC CAUSED BY EXTRAVASATION OF DA FROM VEINS DURING IV
  109. POSSIBLE S/E OF ALL a-BLOCKERS
    • --ORTHOSTATIC HYPOTENSION
    • --FAILURE TO EJAC / RETRO-EJAC
    • --MIOSIS (UNOPPOSED PARASYMP)
    • --NASAL CONG (UNOPPOSED PARASYMP)
    • --ABDOM CRAMPING (UNOPPOSED PARASYMP)

    --SOME pt SLOWLY RETAIN Na/H2O TO INC ECF VOLUME
  110. ERGOTAMINE
    a BLOCKER (really partial a agonist)

    ALSO DIHYDROERGOTAMINE

    MOA -- PARTIAL a AGONIST

    PHARM -- SLIGHTLY CONSTIC CEREBRAL BLD VESS --> DEC MIGRAINE PAIN

    THERA -- MIGRAINE

    • ADVERSE
    • --SPONT ABORT
    • --MUSC PAIN
    • --PARESTHESIAS
    • --DIGITAL VASOSPASM
    • --GANGRENE

    • --MIOSIS (a1)
    • INH OF EJAC (a1)
    • INH INSULIN (a2)
  111. YOHIMBINE
    a BLOCKER

    MOA -- a2 >> a1

    PHARM -- VERY LIPID SOL

    • CENTRAL a2 BLOCKADE IN THE BAROREFLEX ARC --> INC PREGANG SYMP ACTIVITY
    • --TACHYCARDIA
    • --TREMOR
    • --SLIGHT INC IN BP

    THERA -- NOT EFFECTIVE FOR ERECTILE DYSF

    • ADVERSE
    • --TACHYCARDIA
    • --TREMOR
    • --SLIGHT INC IN BP
    • --RESTLESSNESS
    • --IRRITABILITY
    • --ANX
    • --INC INSULIN RELEASE (a2)
  112. a-ADRENOCEPTOR ANTAGONISTS
    • PHEN-OXY-BENZ-AMINE
    • PHEN-TOL-AMINE
    • PRAZOSIN
    • TERAZOSIN
    • DOXAZOSIN
    • TAMSULOSIN
    • LABETALOL
    • YOHIMBINE
    • ERGOTAMINE
    • DIHYDRO-ERGOTAMINE
  113. Tx OF IMPOTENCE
    "FUN PAPA SOLD ALL"

    • PHENTOLAMINE
    • PAPAVERINE
    • SILDENAFIL
    • ALPROSTADIL
  114. ATENOLOL
    b-BLOCKER

    MOA -- CARDIO SELECTIVE (b1)

    --BAM! BETAX, ATEN, METOPRO

    • ------------------------------------------------
    • REST SAME FOR ALL b-BLOCKERS

    • PHARM
    • --DEC BASAL HR, CO, dp/dt
    • --MYOCARDIAL O2 DEMAND & CORONARY BLD FLOW

    --PREVENT TACHYCARDIA CAUSED BY EXCERCISE, STRESS, ANTI-HTN & ANTI ANGINAL VD DRUGS, & VALSALVA

    --DEC CONDUC VELICITY IN AV NODE, ATRIA & VENTs

    • NOT EFFECT
    • --SLOWLY DEV DEC BP EVEN IN NORMOTENSIVE pts

    --BASAL RENIN RELEASE DEC BY 30-50% --> PRA & PLASMA AngII CONC DEC

    --IN HTN, pts DEC IN BP MAY INC Na/H2O RET & INC ECF

    --DEC IOP BY DEC PROD OF AQ HUM BY UNKNOWN MECH (not propanolol bc of anesth of eye)

    --BLOCK LIPOLYSIS (b1 ADIPOCYTES)

    --BLOCK GLYCOGENOLYSIS (b2 LIVER & SKEL MUSC) --> ATTENUATED INC IN PLASMA GLUC & LAC CONC BY EPI

    • WITH NON-SELECTIVE ANTAGONIST:
    • --DEC FEV-1
    • --RED DIGITAL BLD FLOW

    • THERA:
    • --*cardiac dysrhythmias, esp supraventricular arrhythmias assot’d w/ anxiety, stress,hyperthyroidism (Grave’s disease)

    --*may prevent stress-induced PVC

    --*post-MI (w/ aspirin) to prevent sudden death fr catcholamine-induced ventr dysrhythmia

    --*angina pectoris: decr O2 demand

    --*HTN: decr BP w/o ortho. hypo.

    --*heart failure: incr CO (i.e. metoprolol)

    --*hyperthyroidism (Grave’s): Blocks tremor, tachy & atrial fib

    --*pheochromocytoma: non-selectv before & during surgery in combo w/ α blocker.

    --*essential tremor: non-selectv (β2)

    --*portal hypertension: decr CO (i.e., propanolol)

    --*Migraine headache (prophylactic)

    • Glaucoma:
    • --Local use to lower IOP by decr aqueous humor
    • production.
    • --W/o miosis or cyclopledia.
    • (i.e., Betaxolol, Timolol)
    • (except Propanolol→ anesth.of eye)

    • ADVERSE
    • *decr dp/dt ((-) inotropic) --> heart failure & global edema

    *bradycardia → contraindicated in AV block by digoxin.

    • * Up-regulation of β recptrs
    • --sudden withdrawal of Rx (propanol w/d syndrome) → cardiac palpitations & tremor --> angina or MI

    *Contraindicated in pts w/ DM type 2

    *Impotence (No erection)

    ---- Non-selective agents ----

    Contraindicated: Raynaud’s & Bueger’s

    Contraindicated in asthma, COPD & chronic bronchitis (b/c incr airway resistance → decr FEV1)

    *Exercise intolerance in non-anginal pts

    • *Decr digital blood flow (β2)
    • (smoking worsens)

    • *DM type 1 pts: mask signs of hypoglycemia &
    • HTN in presence of hi plasma EPI
  115. DIGOXIN
    LIKE 3* CHOL AGONIST

    ACTS IN CNS TO INC VAGAL TONE --> AV BLOCK

    COUNTER WITH ATROPINE
  116. METOPROLOL
    b-BLOCKER "BAM!"

    MOA -- CARDIOSELECTIVE (b1) REC

    • ---------------------------------------------------
    • REST SAME FOR ALL b-BLOCKERS

    • PHARM
    • --DEC BASAL HR, CO, dp/dt
    • --MYOCARDIAL O2 DEMAND & CORONARY BLD FLOW

    --PREVENT TACHYCARDIA CAUSED BY EXCERCISE, STRESS, ANTI-HTN & ANTI ANGINAL VD DRUGS, & VALSALVA

    --DEC CONDUC VELICITY IN AV NODE, ATRIA & VENTs

    • NOT EFFECT
    • --SLOWLY DEV DEC BP EVEN IN NORMOTENSIVE pts

    --BASAL RENIN RELEASE DEC BY 30-50% --> PRA & PLASMA AngII CONC DEC

    --IN HTN, pts DEC IN BP MAY INC Na/H2O RET & INC ECF

    --DEC IOP BY DEC PROD OF AQ HUM BY UNKNOWN MECH (not propanolol bc of anesth of eye)

    --BLOCK LIPOLYSIS (b1 ADIPOCYTES)

    --BLOCK GLYCOGENOLYSIS (b2 LIVER & SKEL MUSC) --> ATTENUATED INC IN PLASMA GLUC & LAC CONC BY EPI

    • WITH NON-SELECTIVE ANTAGONIST:
    • --DEC FEV-1
    • --RED DIGITAL BLD FLOW

    • THERA:
    • --*cardiac dysrhythmias, esp supraventricular arrhythmias assot’d w/ anxiety, stress,hyperthyroidism (Grave’s disease)

    --*may prevent stress-induced PVC

    --*post-MI (w/ aspirin) to prevent sudden death fr catcholamine-induced ventr dysrhythmia

    --*angina pectoris: decr O2 demand

    --*HTN: decr BP w/o ortho. hypo.

    --*heart failure: incr CO (i.e. metoprolol)

    --*hyperthyroidism (Grave’s): Blocks tremor, tachy & atrial fib

    --*pheochromocytoma: non-selectv before & during surgery in combo w/ α blocker.

    --*essential tremor: non-selectv (β2)

    --*portal hypertension: decr CO (i.e., propanolol)

    --*Migraine headache (prophylactic)

    • Glaucoma:
    • --Local use to lower IOP by decr aqueous humor
    • production.
    • --W/o miosis or cyclopledia.
    • (i.e., Betaxolol, Timolol)
    • (except Propanolol→ anesth.of eye)

    • ADVERSE
    • *decr dp/dt ((-) inotropic) --> heart failure & global edema

    *bradycardia → contraindicated in AV block by digoxin.

    • * Up-regulation of β recptrs
    • --sudden withdrawal of Rx (propanol w/d syndrome) → cardiac palpitations & tremor --> angina or MI

    *Contraindicated in pts w/ DM type 2

    *Impotence (No erection)

    ---- Non-selective agents ----

    Contraindicated: Raynaud’s & Bueger’s

    Contraindicated in asthma, COPD & chronic bronchitis (b/c incr airway resistance → decr FEV1)

    *Exercise intolerance in non-anginal pts

    • *Decr digital blood flow (β2)
    • (smoking worsens)

    • *DM type 1 pts: mask signs of hypoglycemia &
    • HTN in presence of hi plasma EPI
  117. ESMOLOL
    b-BLOCKER

    MOA -- CARDIOSELECTIVE (b1)

    USED VIA IV IN ER OF SHORT TERM BLOCKADE (t1/2 9 mins)

    • ----------------------------------------------
    • REST SAME FOR ALL b-BLOCKERS

    • PHARM
    • --DEC BASAL HR, CO, dp/dt
    • --MYOCARDIAL O2 DEMAND & CORONARY BLD FLOW

    --PREVENT TACHYCARDIA CAUSED BY EXCERCISE, STRESS, ANTI-HTN & ANTI ANGINAL VD DRUGS, & VALSALVA

    --DEC CONDUC VELICITY IN AV NODE, ATRIA & VENTs

    • NOT EFFECT
    • --SLOWLY DEV DEC BP EVEN IN NORMOTENSIVE pts

    --BASAL RENIN RELEASE DEC BY 30-50% --> PRA & PLASMA AngII CONC DEC

    --IN HTN, pts DEC IN BP MAY INC Na/H2O RET & INC ECF

    --DEC IOP BY DEC PROD OF AQ HUM BY UNKNOWN MECH (not propanolol bc of anesth of eye)

    --BLOCK LIPOLYSIS (b1 ADIPOCYTES)

    --BLOCK GLYCOGENOLYSIS (b2 LIVER & SKEL MUSC) --> ATTENUATED INC IN PLASMA GLUC & LAC CONC BY EPI

    • WITH NON-SELECTIVE ANTAGONIST:
    • --DEC FEV-1
    • --RED DIGITAL BLD FLOW

    • THERA:
    • --*cardiac dysrhythmias, esp supraventricular arrhythmias assot’d w/ anxiety, stress,hyperthyroidism (Grave’s disease)

    --*may prevent stress-induced PVC

    --*post-MI (w/ aspirin) to prevent sudden death fr catcholamine-induced ventr dysrhythmia

    --*angina pectoris: decr O2 demand

    --*HTN: decr BP w/o ortho. hypo.

    --*heart failure: incr CO (i.e. metoprolol)

    --*hyperthyroidism (Grave’s): Blocks tremor, tachy & atrial fib

    --*pheochromocytoma: non-selectv before & during surgery in combo w/ α blocker.

    --*essential tremor: non-selectv (β2)

    --*portal hypertension: decr CO (i.e., propanolol)

    --*Migraine headache (prophylactic)

    • Glaucoma:
    • --Local use to lower IOP by decr aqueous humor
    • production.
    • --W/o miosis or cyclopledia.
    • (i.e., Betaxolol, Timolol)
    • (except Propanolol→ anesth.of eye)

    • ADVERSE
    • *decr dp/dt ((-) inotropic) --> heart failure & global edema

    *bradycardia → contraindicated in AV block by digoxin.

    • * Up-regulation of β recptrs
    • --sudden withdrawal of Rx (propanol w/d syndrome) → cardiac palpitations & tremor --> angina or MI

    *Contraindicated in pts w/ DM type 2

    *Impotence (No erection)

    ---- Non-selective agents ----

    Contraindicated: Raynaud’s & Bueger’s

    Contraindicated in asthma, COPD & chronic bronchitis (b/c incr airway resistance → decr FEV1)

    *Exercise intolerance in non-anginal pts

    • *Decr digital blood flow (β2)
    • (smoking worsens)

    • *DM type 1 pts: mask signs of hypoglycemia &
    • HTN in presence of hi plasma EPI
  118. PROPANOLOL
    b-BLOCKER

    MOA -- NONSELECTIVE (b1 & b2)

    LIKE TIMOLOL

    • ------------------------------------------
    • REST SAME FOR ALL b-BLOCKERS

    • PHARM
    • --DEC BASAL HR, CO, dp/dt
    • --MYOCARDIAL O2 DEMAND & CORONARY BLD FLOW

    --PREVENT TACHYCARDIA CAUSED BY EXCERCISE, STRESS, ANTI-HTN & ANTI ANGINAL VD DRUGS, & VALSALVA

    --DEC CONDUC VELICITY IN AV NODE, ATRIA & VENTs

    • NOT EFFECT
    • --SLOWLY DEV DEC BP EVEN IN NORMOTENSIVE pts

    --BASAL RENIN RELEASE DEC BY 30-50% --> PRA & PLASMA AngII CONC DEC

    --IN HTN, pts DEC IN BP MAY INC Na/H2O RET & INC ECF

    --DEC IOP BY DEC PROD OF AQ HUM BY UNKNOWN MECH (not propanolol bc of anesth of eye)

    --BLOCK LIPOLYSIS (b1 ADIPOCYTES)

    --BLOCK GLYCOGENOLYSIS (b2 LIVER & SKEL MUSC) --> ATTENUATED INC IN PLASMA GLUC & LAC CONC BY EPI

    • WITH NON-SELECTIVE ANTAGONIST:
    • --DEC FEV-1
    • --RED DIGITAL BLD FLOW

    • THERA:
    • --*cardiac dysrhythmias, esp supraventricular arrhythmias assot’d w/ anxiety, stress,hyperthyroidism (Grave’s disease)

    --*may prevent stress-induced PVC

    --*post-MI (w/ aspirin) to prevent sudden death fr catcholamine-induced ventr dysrhythmia

    --*angina pectoris: decr O2 demand

    --*HTN: decr BP w/o ortho. hypo.

    --*heart failure: incr CO (i.e. metoprolol)

    --*hyperthyroidism (Grave’s): Blocks tremor, tachy & atrial fib

    --*pheochromocytoma: non-selectv before & during surgery in combo w/ α blocker.

    --*essential tremor: non-selectv (β2)

    --*portal hypertension: decr CO (i.e., propanolol)

    --*Migraine headache (prophylactic)

    • Glaucoma:
    • --Local use to lower IOP by decr aqueous humor
    • production.
    • --W/o miosis or cyclopledia.
    • (i.e., Betaxolol, Timolol)
    • (except Propanolol→ anesth.of eye)

    • ADVERSE
    • *decr dp/dt ((-) inotropic) --> heart failure & global edema

    *bradycardia → contraindicated in AV block by digoxin.

    • * Up-regulation of β recptrs
    • --sudden withdrawal of Rx (propanol w/d syndrome) → cardiac palpitations & tremor --> angina or MI

    *Contraindicated in pts w/ DM type 2

    *Impotence (No erection)

    ---- Non-selective agents ----

    Contraindicated: Raynaud’s & Bueger’s

    Contraindicated in asthma, COPD & chronic bronchitis (b/c incr airway resistance → decr FEV1)

    *Exercise intolerance in non-anginal pts

    • *Decr digital blood flow (β2)
    • (smoking worsens)

    • *DM type 1 pts: mask signs of hypoglycemia &
    • HTN in presence of hi plasma EPI
  119. TIMOLOL
    b-BLOCKER

    MOA -- NONSELECTIVE (b1 & b2)

    LIKE PROPANOLOL

    • -----------------------------------------
    • REST SAME FOR ALL b-BLOCKERS

    • PHARM
    • --DEC BASAL HR, CO, dp/dt
    • --MYOCARDIAL O2 DEMAND & CORONARY BLD FLOW

    --PREVENT TACHYCARDIA CAUSED BY EXCERCISE, STRESS, ANTI-HTN & ANTI ANGINAL VD DRUGS, & VALSALVA

    --DEC CONDUC VELICITY IN AV NODE, ATRIA & VENTs

    • NOT EFFECT
    • --SLOWLY DEV DEC BP EVEN IN NORMOTENSIVE pts

    --BASAL RENIN RELEASE DEC BY 30-50% --> PRA & PLASMA AngII CONC DEC

    --IN HTN, pts DEC IN BP MAY INC Na/H2O RET & INC ECF

    --DEC IOP BY DEC PROD OF AQ HUM BY UNKNOWN MECH (not propanolol bc of anesth of eye)

    --BLOCK LIPOLYSIS (b1 ADIPOCYTES)

    --BLOCK GLYCOGENOLYSIS (b2 LIVER & SKEL MUSC) --> ATTENUATED INC IN PLASMA GLUC & LAC CONC BY EPI

    • WITH NON-SELECTIVE ANTAGONIST:
    • --DEC FEV-1
    • --RED DIGITAL BLD FLOW

    • THERA:
    • --*cardiac dysrhythmias, esp supraventricular arrhythmias assot’d w/ anxiety, stress,hyperthyroidism (Grave’s disease)

    --*may prevent stress-induced PVC

    --*post-MI (w/ aspirin) to prevent sudden death fr catcholamine-induced ventr dysrhythmia

    --*angina pectoris: decr O2 demand

    --*HTN: decr BP w/o ortho. hypo.

    --*heart failure: incr CO (i.e. metoprolol)

    --*hyperthyroidism (Grave’s): Blocks tremor, tachy & atrial fib

    --*pheochromocytoma: non-selectv before & during surgery in combo w/ α blocker.

    --*essential tremor: non-selectv (β2)

    --*portal hypertension: decr CO (i.e., propanolol)

    --*Migraine headache (prophylactic)

    • Glaucoma:
    • --Local use to lower IOP by decr aqueous humor
    • production.
    • --W/o miosis or cyclopledia.
    • (i.e., Betaxolol, Timolol)
    • (except Propanolol→ anesth.of eye)

    • ADVERSE
    • *decr dp/dt ((-) inotropic) --> heart failure & global edema

    *bradycardia → contraindicated in AV block by digoxin.

    • * Up-regulation of β recptrs
    • --sudden withdrawal of Rx (propanol w/d syndrome) → cardiac palpitations & tremor --> angina or MI

    *Contraindicated in pts w/ DM type 2

    *Impotence (No erection)

    ---- Non-selective agents ----

    Contraindicated: Raynaud’s & Bueger’s

    Contraindicated in asthma, COPD & chronic bronchitis (b/c incr airway resistance → decr FEV1)

    *Exercise intolerance in non-anginal pts

    • *Decr digital blood flow (β2)
    • (smoking worsens)

    • *DM type 1 pts: mask signs of hypoglycemia &
    • HTN in presence of hi plasma EPI
  120. LABETOLOL
    b-BLOCKER

    MOA -- NONSELECTIVE (b1, b2, & a)

    SEE ALSO a-BLOCKER

    • ----------------------------------------------
    • REST SAME FOR ALL b-BLOCKERS

    • PHARM
    • --DEC BASAL HR, CO, dp/dt
    • --MYOCARDIAL O2 DEMAND & CORONARY BLD FLOW

    --PREVENT TACHYCARDIA CAUSED BY EXCERCISE, STRESS, ANTI-HTN & ANTI ANGINAL VD DRUGS, & VALSALVA

    --DEC CONDUC VELICITY IN AV NODE, ATRIA & VENTs

    • NOT EFFECT
    • --SLOWLY DEV DEC BP EVEN IN NORMOTENSIVE pts

    --BASAL RENIN RELEASE DEC BY 30-50% --> PRA & PLASMA AngII CONC DEC

    --IN HTN, pts DEC IN BP MAY INC Na/H2O RET & INC ECF

    --DEC IOP BY DEC PROD OF AQ HUM BY UNKNOWN MECH (not propanolol bc of anesth of eye)

    --BLOCK LIPOLYSIS (b1 ADIPOCYTES)

    --BLOCK GLYCOGENOLYSIS (b2 LIVER & SKEL MUSC) --> ATTENUATED INC IN PLASMA GLUC & LAC CONC BY EPI

    • WITH NON-SELECTIVE ANTAGONIST:
    • --DEC FEV-1
    • --RED DIGITAL BLD FLOW

    • THERA:
    • --*cardiac dysrhythmias, esp supraventricular arrhythmias assot’d w/ anxiety, stress,hyperthyroidism (Grave’s disease)

    --*may prevent stress-induced PVC

    --*post-MI (w/ aspirin) to prevent sudden death fr catcholamine-induced ventr dysrhythmia

    --*angina pectoris: decr O2 demand

    --*HTN: decr BP w/o ortho. hypo.

    --*heart failure: incr CO (i.e. metoprolol)

    --*hyperthyroidism (Grave’s): Blocks tremor, tachy & atrial fib

    --*pheochromocytoma: non-selectv before & during surgery in combo w/ α blocker.

    --*essential tremor: non-selectv (β2)

    --*portal hypertension: decr CO (i.e., propanolol)

    --*Migraine headache (prophylactic)

    • Glaucoma:
    • --Local use to lower IOP by decr aqueous humor
    • production.
    • --W/o miosis or cyclopledia.
    • (i.e., Betaxolol, Timolol)
    • (except Propanolol→ anesth.of eye)

    • ADVERSE
    • *decr dp/dt ((-) inotropic) --> heart failure & global edema

    *bradycardia → contraindicated in AV block by digoxin.

    • * Up-regulation of β recptrs
    • --sudden withdrawal of Rx (propanol w/d syndrome) → cardiac palpitations & tremor --> angina or MI

    *Contraindicated in pts w/ DM type 2

    *Impotence (No erection)

    ---- Non-selective agents ----

    Contraindicated: Raynaud’s & Bueger’s

    Contraindicated in asthma, COPD & chronic bronchitis (b/c incr airway resistance → decr FEV1)

    *Exercise intolerance in non-anginal pts

    • *Decr digital blood flow (β2)
    • (smoking worsens)

    • *DM type 1 pts: mask signs of hypoglycemia &
    • HTN in presence of hi plasma EPI
  121. NAME THE b-ADRENOCEPTOR ANTAGONISTS (b-BLOCKERS)
    "ATENsion, BET TIM's LAB MET ES a PRO!"

    • BETAXOLOL
    • ATENOLOL
    • METOPROLOL
    • ESMOLOL
    • PROPANOLOL
    • TIMOLOL (glaucoma)
    • LABETALOL
  122. COCAIN
    ALTER NE METABOLISM

    • COCAIN HCl
    • --SNORTED
    • --INJ
    • --P.O.
    • --LOCAL APP TO SUBLING, VAG, URETH, RECT MUCOSA

    • MOA
    • --LOCAL ANESTH --> BLOCKS Na CHN IN NEURONAL MEM OF SENSORY PAIN FIBERS

    --NON-COMP BLOCKADE OF MAO UPTAKE-1 TRANPORTER IN CENT/PERIPH NEURONS

    -->AMPs POSTJUNC EFFECTS OF NE, DA, EPI, & 5-HT

    --ACTS CENTRALLY TO INC PERIPH SYMP OUTFLOW

    • CNS
    • --EUPHORIA & ADDICTIVE PROP RESULT FROM INC DA RELEASE IN NUC ACCUMB

    (ACTUALLY: PREVENT DA REUPTAKE --> BUILD UP IN NERVE JUNC

    • PHARM
    • --LOCAL ANASTHET & INTENSE VC

    --LOCAL HEMOSTASIS WHEN USED AS A TOPICAL ANESTH

    --CNS: EUPH & VERY ADDICTIVE

    • --DOSE RELATED
    • ----INC BP & HR

    • --INDIR VC ACT
    • ----NON-COMP BLOCK OF UPTAKE-1 --> INC NE CONC IN NERVE JUNC --> NE STIM a1 @ ADVENTITIAL SURFACE OF VSM

    • THERA
    • --LOCAL ANESTH IN OCULAR & NASAL SURGERY

    ADVERSE

    *cardiac dysrhythmias:

    • 1. Blockade of cardia Na channels → impairs
    • ventr impulse conduction

    2. Incr NE release (central effect)

    3. potentiates cardiac actions of NE (block uptake-1)

    *MI: poss w/ pt w/ normal coronary arteries

    *chest pain (sim to MI)

    *pulmonary edema: From direct decr dp/dt & incr afterload

    *CVA: subarachnoid hemorrhage or ischemic stroke

    *respiratory disease: barotrauma, pulmonary hemorrhage & hypersenstv pneumonia

    *seizures

    *sudden death

    * “crack” burns of larynx

    *necrosis of nasal septum
  123. GUANETHIDINE
    SYMPATHOLYTIC

    MOA -- ADREN NEURONAL BLACKING DRUG

    DIRECTLY INH NERVE-STIMULATED NE RELEASE

    ***MAIN ACTION IS INH OF NERVE-STIM RELEASE FROM PERIPH SYMP NEURONS

    INH VESICULAR STORAGE OF NE

    INH EXOCYTOTIC RELEASE OF NE BY ACTION POTENTIAL

    • PHARM
    • --POORLY LIPID SOL --> NO CNS

    • NET EFFECT
    • --BALANCED VD --> PASSIVE VD
    • ----@ ARTERIOLES; DEC TPR --> DEC DBP
    • ----@ VENULES; INC VEN CAP --> DEC VEN RETURN

    --UNCHANGED / SLIGHT DEC IN HR

    --UNCHANGED / SLIGHT DEC IN CO

    --DEC RENAL PERF --> INC FILT FRAC --> Na/H2O RET

    • THERA
    • --NOT USED TO Rx HTN ANYMORE

    ADVERSE

    *orthostatic hypotension

    *edema

    *No/retrograde ejaculation

    • *SUPERSENSITIVITY to directly-acting sympathomimetic amines due to
    • UPREGULATION of adrenoceptors

    • *Unopposed parasymp activity can cause:
    • --Bradycardia
    • --Diarrhea
    • --incr secretion of gastric acid
    • --nasal congestion
  124. RESERPINE
    SYMPATHOLYTIC "aRG!"

    MOA -- ALKALOID OF BOTANICAL ORIGIN

    **DESTROYS INTRACELL STORAGE VESICLES FOR NT IN CENTRAL & PERIPH MONOAMINERGIC NEURONS

    SMALL DOSES AFFECT ONLY PERIPH SYMP NEURONS

    INH VESICULAR STORAGE OF NE

    • PHARM
    • --SLOWED DEPLETION OF NE --> DEC NE RELEASE BY NERVE IMPULSES @ BLD VESS

    --DOES NOT SUPPRESS TONIC SYMP ACT TO BLD VESS (LIKE a-MD) BUT LESS NE RELEASED --> SAME END RESULT

    • --*BALANCED VASODIL --> PASSIVE VD
    • ----AT ARTERIOLES, DEC TPR --> DEC DBP
    • ----AT VENULES, INC VENOUS CAP --> DEC VENOUS RET

    --DEC HR

    --UNCHANGED / SLIGHTLY DEC CO

    --DEC RENAL PERF --> INC FILT FRAC --> Na/H2O RET

    --INC MOTILITY & TONE IN GI FROM UNOPPOSED PARASYM NERVE ACT

    --INC PROLACTIN SEC FROM PIT VIA DEC RELEASE OF DA (DA --> TONIC PRL INH)

    • THERA
    • --NOT USED TO Rx HTN ANYMORE

    ADVERSE

    • Contraindicated:
    • 1. Pregnant ♀
    • 2. Hx of depression

    *TERATOGENIC

    *sedation

    *depression w/ suicidal tendencies

    *Parkinsonian-like movements!!!

    *orthostatic hypotension!

    *No/retrograde ejaculation

    *hyperprolactinemia (DA)!!

    • *SUPERSENSITIVITY to direct-acting sympathomimetic amines! (Up-regulation
    • of periph α & β)

    • *Unopposed parasymp activity can cause:
    • --Bradycardia
    • --Diarrhea
    • --incr secretion of gastric acid
    • --nasal congestion
  125. a-METHYLDOPA
    • SYMPATHOLYTIC
    • --DIR OR IND DEC RELEASE OF NE FROM PERIPH SYMP NEURONS --> DEC BP 1* BY DEC TPR

    VIA NE & DOPA SYNTH enz --> a-METHYL-NE

    --Stored as a ntr in vseicles of central & peripheral noradrenergic neurons → released by action potential.

    --NOT degraded by MAO → stored in cytoplasm & NE vesicles

    MOA -- INDIR BLOCKS RELEASE OF NE FROM SYMP NEURONS

    **STIMS a2 @ ROSTRAL VL MEDULLA --> DEC PREGANG SYMP ACTIVITY (ACTS CENTRALLY TO MIMIC INC BARORECEPTOR INPUT FROM CAROTID SINUS

    **DEC SYMP ACTIVITY --> DEC AMOUNT OF NE @ a-METHYL-NE RELEASED FROM PERIPH SYMP FIBERS WHICH INNERV HRT & BLD VESSs

    • PHARM
    • --VASOCONST IN BLD VESS (as effecacious as NE)

    --NET BALANCED VASO-DIL. DEC TONIC SYMP VC --> PASSIVE VD. ARTERIOLES DEC DBP

    --SLIGHT DEC HR

    --ATTENUATED INC IN HR THAT OCC WHEN MOVING FROM A SUPINE TO STANDING POS

    --UNCHANGED/SLIGHT DEC CO

    --DEC BYOCARDIAL O2 DEMAND

    --DEC IN RENAL PERF --> POSS INC FILT FRAC --> SLOWLY CAUSE Na/H2O RET

    -DEC PLASMA RENIN ACT

    --DEC PLASMA AngII CONC

    --INC PROLACTIN SEC FROM PIT VIA DEC RELEASE OF DA (DA --> TONIC PRL INH)

    • THERA
    • --DOC FOR HTN IN CHILDREN & PREG bc NOT TERATOGINIC

    • ADVERSE
    • --SEDATION & SOMN
    • --DRY MOUTH & NASAL CONG
    • --EDEMA
    • --SOME ORTHOSTATIC INTOLERANCE
    • --FLU-LIKE SYND
    • --(+) COOMB'S TEST
    • --HEP (HYPERSENSITIVITY rxn)

    • --HYPERPROLACTINEMIA
    • ----MALES: GYNECOMASTIA, OLIGOSPERMIA & IMP / DEC LIBIDO

    ----FEMALES: AMENORRHEA & GALACTORRHEA
  126. SYMPATHOLYTIC DRUGS
    ARG!

    • a-METHYLDOPA
    • RESERPINE
    • GUAN-ETH-IDINE
  127. NEURONAL NE UPTAKE 1
    COCAINE
  128. PHARMACODYNAMICS & KINETICS
    DYNAMICS - WHAT A DRUG DOES TO THE BODY

    KINETICS - WHAT THE BODY DOES TO A DRUG. THE STUDY STUDY OF THE TIME COURSE OF THE ABSORPTION, DISTRIBUTION, METABOLISM, AND ELIMINATION OF DRUGS
  129. ENTERAL ROUTES
    BUCCAL

    PER OS (p.o) -- SLOW ABS & SUBJECT TO HIGH FIRST PASS FILTERING

    RECTAL - DELAYED FIRST PASS. USED WHEN pt IS NAUSEATED
  130. PARENTERAL ROUTES
    • INJECTION:
    • IV -- RAPID ACTION (4 SEC). DRUGS WITH SHORT HALF LIFE --> PEPTIDES AND INSOLUBLE DRUGS

    IM -- FAIRLY RAPID ABS. DEPOT FORMS (PEN)

    SUBCUTANEOUS -- RAPID ABS WITH AQUEOUS PREPS. FAIRLY RAPID VASOACTIVE DRUGS WHICH ARE DANGEROUS TO GIVE IV (EP FOR ANAPHYLACTIC REACTION)
  131. ROUTES OTHER THAN ENTERAL/PARENTERAL
    PULMONARY -- LARGE SURFACE AREA AND HIGH BLOOD FLOW ALLOW RAPID ABS OF GASSES (ANESTHETIC ENFLURANE)

    TOPICAL -- LOCAL EFFECT (EYE, SKIN, NOSE, THROAT, VAG, RECTUM, LUNG)

    TRANSDERMAL (PATCH) -- SLOW ABS LEADS TO CONSTANT AMT OF DRUG IN BLOOD FOR PERIODS AS LONG AS ONE WEEK (NITROGLYCERINE, SCOPOLAMINE, CLONIDINE, ESTROGEN)
  132. CHEMICAL NATURE OF DRUGS
    ALMOST ALL ARE LOW MOL WEIGHT AND EITHER ACIDIC OR BASIC

    ACIDIC -- ANION FORMING (CONTAIN CARBOXYL GRP -COOH). USUALLY HAVE pKa > 7 BUT EXCEPTIONS (PHENYTOIN, HYDROCLOROTHIOZIDE, PENTAZOCINE)

    BASIC -- CATION FORMING (CONTAIN AMINE GRP -NH2). USUALLY HAVE pKa < 7 BUT EXCEPTIONS (VINCRISTINE, DIAZEPAM, METFORMIN)
  133. DRUG ABS IN GI
    MOST ABS BY PASSIVE DIFFUSION DRIVEN BY CONC GRADIENT

    PASSIVE DIFF OCCURS THROUGH AQ COMPARTMENTS AND LIPID MEMS

    LIPID SOLUBILITY MAJOR CHAR OF PASSIVE DIFF --> ELECTRICAL CHARGE OR NOT

    UNCHARGED FORM IS BEST ABS -- ELEC CHARGE DETERMINED BY pKa AND pH

    • HH USED TO CALC FRACTION OF NONIONIZED DRUG IF THE pKa AND pH ARE KNOWN: LOG (PROT/UNPROT) = pKa - pH
    • WHEN pKa = pH, CONC HALF IONIZED

    • LOW pH --> HIGH ABS OF ACIDIC DRUGS (STOM)
    • HIGH pH --> HIGH ABS OF BASIC DRUGS (SMALL BOWEL)

    OIL/WATER PARTITION COEF: 10 IF VERY LIPID SOL (WILL PASS THROUGH LIPID MEM) AND 0.1 IF POORLY LIPID SOL

    *REAL WORLD -- REGARLESS OF pKa, MAJORITY OF ANY DRUG WILL ABS IN SMALL INT BC OF LARGE SURFACE AREA
  134. BIOEQUIVALENCE OF GENERIC DRUGS
    MUST PRODUCE PLASMA CONC VS. TIME CURVE AFTER p.o. DOSING COMPARABLE TO PROPRIETARY.

    BIOEQ IS PRIMARILY A FUNC OF BIOAVAILABILITY
  135. DRUG BIOTRANSFORMATION
    BT = METABOLISM

    HEPATIC BT MAKES DRUGS MORE WATER SOL SO EXCRETED BY KIDNEYS

    MAINLY BY LIVER: DETERMINED BY CONC, HEP EXTRACTION RATION (FRAC OF DRUG REMOVED FROM BLOOD), HEP BLOOD FLOW

    • 2 ENZ REACTIONS:
    • PHASE I -- CHANGE CHM STRUCT BY OX, HYDROX, DEAM, AND DEALK

    PHASE II -- CONJUGACTION OR COUPLING TO ENDOGENOUS COMPOUNDS (GLUCURONIDATION, ACETYLATION, SULFATION)

    • MAY ACTIVATE PRODRUGS
    • ENALAPRIL --> ENALAPRILAT
    • MINOXIDIL --> MINOXIDIL SULFATE
    • LORATADINE (CLARATIN) --> DESCARB OETHOXYLORATADINE (DESLORATADINE OR CLARINEX)
  136. INDUCERS OF HEPATIC CYP450 AND CLINICAL SIG
    • PHENOBARBITOL & OTHER BARBS
    • RIFAMPIN
    • PHENYTOIN
    • CARBAMAZEPINE
    • ETHANOL (CHRONIC ONLY)
    • BENZOPRENE (CIG SMOKE)

    • QUEEN
    • *BARB
    • STEALS
    • *PHEN-PHEN
    • *REFUSES
    • GREASY
    • *CARBS
    • *ETHANOL (chronic)
    • *MARCEDES-BENZ-OPREIN

    • dioxin (tccd) present in agent orange
    • ddt (insecticide)
    • polychorinated biphenyls (pcb)

    EFFECTS OF OTHER DRUGS DIMINISHED

    MAJOR CAUSE OF PHARMACOKINETIC TOLERANCE
  137. INHIBITORS OF CYP450 AND CLINICAL SIG
    • KETOCONAZOLE
    • ISONIAZID (TB)
    • CIMETIDINE
    • ERYTHROMYCIN
    • ETHANOL (acute only)
    • FURANOCOUMARIN (GF JUICE)

    • KEETON
    • IS
    • CIMPLE
    • he
    • EATS
    • ETHANOL (ACUTE)
    • GRAPEFRUIT JUICE (FURANOCOUMARIN)

    EFFECTS OF OTHER DRUGS ENHANCED

    MAJOR CAUSE OF DRUG TOXICITY
  138. ENTEROHEPATIC SECRETION
    COMPOUND SECRETED INTO BILE AND ENTERS GI

    RE-ABS FROM GI --> LIVER --> BACK TO BILE

    DRUG CONJUGATES HYDROLYZED BY BAC ENZ IN LARGE INT TO RELEASE PARENT DRUG WHICH IS THEN RE-ABS (ex ESTROGENIC COMPONENTS IN ORAL CONTRACEPTIVES)
  139. RENAL EXCRETION
    GLOMERULAR FILTRATION = PASSIVE

    SECRETION = ACTIVE TRANSPORT INTO PROX TUBULE

    ONLY FREE DRUGS NOT BOUND BY PLASMA PROTS FILTERED/SECRETED. DRUG CAN THEN BE RE-ABS FROM TUBULAR URINE IF NOT IONIZED BY pH

    RATE OF ACIDIC AND BASIC DRUG EXCRETION CAN BE TWEEKED BY MANIPULATING URINE pH --> "ION TRAPPING"

    INCREASE EXCRETION OF BASIC AMPHETAMINE BY LOWERING URINE pH WITH AMMONIOM CHOLIDE

    ACIDIC SALICYCLIC ACID EXCRETION BY MAKING URINE MORE ALKALINE (BASIC, INC pH) BY GIVING CARBONIC ANHYDRASE INH ACETAZOLAMIDE OR SODIUM BICARB
  140. GENERAL PHARMICOKINETIC MODEL
    REVOLVES DAROUND FREE DRUG (NOT BOUND TO PLASMA OR TISSUE PROTS)

    ALL CALCULATIONS BASED ON THE PLASMA CONC

    PLASMA CONC REPORTED BY LAB IS THE TOTAL CONC AND DOES NOT REVEAL HOW MUCH OF TOTAL CONC IS FREE/BOUND

    SOME PORTION OF ALL DRUGS ARE BOUND TO PLASMA PROTS. ACIDIC DRUGS BIND MOSTLY TO ALBUMIN AND OTHERS LIKE a-1 ACID GLYCOPROT. MANY DRUG-DRUG INTERACTIONS INVOLVE DISPLACEMENT OF FIRST DRUG FROM PLASMA PROTS BY A 2ND

    ONLY FREE DRUGS PASS THROUGH BIO-MEMS. BUT, CELL MEMs IMPERMIABLE TO LOTS EXCEPT WATER SO MUST BE ACTIVELY TRANSed OR VERY LIPID SOL TO PASS

    LIVE PRIMARY SITE OF BIO-TRANSFORMATION. ONLY FREE DRUG IS MET BY LIVER DURING FIRST PASS AND RECIRCULATION

    ONLY FREE DRUG IS FILTERED BY GLOM OR SECRETED BY KIDNEYS

    ONLY FREE DRUG PASSES INTO TISSUE FOR STORAGE (MAINLY MUSCLE AND ADIPOSE)

    ONLY FREE DRUGS ACTIVATE RECEPTORS
  141. ONE-COMPARTMENT OPEN MODEL
    BODY DEPICTED AS SINGLE HOMOGENOUS COMPARTMENT

    ABS AND DISTRIBUTION IS INSTANTANEOUS

    ELIMINATION OF ALMOST ALL DRUGS OCCURS AS A FIRST-ORDER RATE CONSTANT (ex TOTAL DRUG IN BODY x k(1/h) = mg/h k(1/h)=elim frac
  142. BIOAVAILABILITY (F)
    • BIOAVAILABILITY (F) IS FRAC OF DRUG DOSE THAT REACHES SYSTEMIC
    • CIRCULATION UNCHANGED FOLLOWING EXTRAVASCULAR DOSING. DOES NOT APPLY TO IV INJECTIONS.

    • (F) GIVEN BY P.O. DETERMINED BY:
    • 1. % ABS FROM GI
    • 2. % MET BY BUT WALL ENZs
    • 3. % REMOVED BY FIRST PASS

    F= (P.O. AUC) / (IV AUC). AUC DETERMINED BY (Cp X TIME) GRAPH
  143. APPARENT VOLUME OF DISTRIBUTION (Vd)
    HYPOTHETICAL VOL

    DOES NOT REFER TO REAL VOL BUT MAY CORRESPOND TO VOL OF ONE OF THE FLUID COMPARTMENTS OF THE BODY

    EXPRESSED IN L, L/Kg, OR L/m^2.

    Vd = (Xo x F) / (Cp at time zero). Xo is dose administered in mg.

    USED TO CALC LOADING DOSE

    ONE OF 2 MAJOR DETERMINANTS OF HALF LIFE

    ESTIMATE Cp AT TIME ZERO

    • USED TO CALC CLEARANCE
    • HIGH Vd MEANS MUCH OF THE DRUG IS ABS INTO THE TISSUES

    PROBLEMS GIVEN WITH Vd AS L/Kg. WEIGHT OF Pt CAN BE DETERMINED BY (Vd = L/Kg X Kg = L)
  144. ELIMINATION RATE CONSTANT
    • K = (0.7) / (t1/2)
    • INC K, DEC t1/2

    t1/2 = 0.7 (Vd/Cl)

    (K)tot = Krenal + Knon-renal

    FIRST-ORDER RATE PROCESS BY WHICH A CONSTANT FRACTION OR % OF DRUG IS REMOVED FROM THE BODY PER UNIT TIME

    BODY ABLE TO REMOVE A CONSTANT FRAC PER UNIT TIME bc ENZ SYSTEMS RARELY SATURATE

    ACTUAL AMOUNT OF DRUG REMOVED PER UNIT TIME (RATEout = RATE OF ELIMINATION) IS DEPENDENT ON TOTAL AMOUNT OF DRUG IN BODY

    K AND RATE OF ELIM ARE RELATED BUT NOT THE SAME THING
  145. Cpss
    PLASMA CONC OF DRUG AT STEADY STATE

    REMAINS CONSTANT bc RATE IN (DOSING RATE) = RATEout (RATE OF ELIMINATION)

    Cpss IS ALWAYS GREATER THAN Cp PRODUCED BY SINGLE p.o. DOSE

    TIME NEEDED TO ATTAIN Cpss IS INDEPENDENT OF DOSAGE

    Cpss IS PROPORTIONAL TO THE DOSING RATE -- GIVING A DRUG DOSE MORE FQly WILL RESULT IN A HIGHER Cpss
  146. RULE OF 4s
    RELATIONSHIP BETWEEN t1/2 AND CONSTANT DOSING RATE

    93% Cpss OCCURS AFTER 4 T1/2

    FIXED DOSE x 4(t1/2) = 93% Cpss
  147. CLEARANCE (Cl)
    AMOUNT OF BLOOD OR PLASMA CLEARED OF PARENT DRUG PER UNIT TIME

    Cl = RATEout / Cp = L/h

    Cp ~ TOTAL DRUG IN BODY

    Cl = K x Vd

    Cl = X / (Cp x DOSE INT)

    • Cl -- THINK FLOW
    • RATEout -- THINK ACTUAL AMOUNT AT THAT TIME

    IF Cp IS DOUBLED, Cl REMAINS THE SAME BECAUSE RATEout ALSO DOUBLES
  148. RENAL CLEARANCE VALUES: FILTERED vs. SECRETED AND RE-ABS vs. NOT
    0-120 FILTERED AND PARTIALLY RE-ABS

    120 FILTERED AND NOT RE-ABS (CREATININE & INULIN)

    120-600 SECRETED AND PARTIALLY RE-ABS

    600 SECRETED AND NOT RE-ABS (PAH)
  149. LOADING DOSE
    GET Cp WITHING THERAPEUTIC WINDOW AS FAST AS POSSIBLE

    USUALLY 2-2.5 LARGER THAN MAINENANCE DOSE

    XL = (Cp x Vd) / F

    AFTER LOADING DOSE IS GIVEN TO REACH THERAPEUTIC WINDOW, A PERIOD OF 4 t1/2 IS STILL REQUIRED TO REACH Cpss
  150. CALCULATE Cpo
    Cpo = (Xo x F) / Vd

    USE TO CALC Vd AND Xo ALSO

    Vd MUST BE IN L, SO IF GIVEN IN L/Kg -- MUST MULTIPLY BY Pt WEIGHT IN Kg
  151. SLOW ACETYLATORS
    "SHIP"

    LIKELY TO DEV TOXICITY

    • Sulfapyridine
    • - hepatic damage & blood dyscrasias

    • Hydralazine
    • - lupus-like syndrome

    • Isoniazid
    • - peripheral neuropathy

    Procainamide - lupus-like syndrome
  152. ACETAZOLAMIDE
    MAKES URINE MORE BASIC (ALKALINE)

    THERA -- Rx OVERDOSE: INC EXCRETION OF WEAK ACIDS (ex ASPRIN)
  153. AMMONIUM CHLORIDE
    MAKES URINE MORE ACIDIC

    THERA -- Rx OVERDOSE --> INC EXCRETION OF WEAK BASES (ex amphetamine)
  154. DRUGS USED TO AFFECT URINARY pH
    Ammonium chloride -- Makes urine more acidic. THERAPEUTIC --> Rx overdose: Incr excretion of weak BASES (e.g. amphetamine)
  155. Acetazolamide -- Makes urine more alkaline. THERAPEUTIC --> Rx overdose: Incr excretion of weak ACIDS (e.g. aspirin)
  156. a1-ADRENORECEPTORS FOUND IN:
    • POSTJUNCTIONAL SITES:
    • EFFECTOR ORGANS, TISSUES AND GLANDS INNERVATED BY SYMP NERVES

    INC INTRACELLULAR INH OF ADEN CYCL --> DEC cAMP

    SIGNAL BY IP3 & DAG
  157. a2 - ADRENORECEPTORS FOUND AT
    • 1. POSTJUNCTIONAL SITES:
    • EFFECTOR ORGANS, TISSUES AND GLANDS INNERVATED BY SYMP NERVES

    INC INTRACELLULAR INH OF ADEN CYCL --> DEC cAMPIP3 & DAG

    • 2. PREJUCTIONAL SITES:
    • SYMP NEURONS (AUTO --> Gi INC K)

    PARASYMP NEURONS OF SA, SPHINC OF IRIS, GI, (HETERO --> Gi INC K)
  158. b1-ADRENORECEPTORS FOUND AT
    • POSTJUNCIONAL SITES:
    • CARDIAC MUSCLES

    CARDIAC CONDUCTION TISSUE

    ADIPOCYTES

    JG CELLS OF RENAL AFFERENT ARTERIOL
  159. b2-ADRENORECEPTORS FOUND AT
    • POSTJUNTIONAL SITES:
    • ARTERIOLS AND VENULES

    BRONCHIOLS

    UTERUS

    GI

    LIVER

    • PREJUNCTIONAL SITES:
    • SYMP NEURONS (HETERO)
  160. SYMP MUSCLES OF EYE
    RADIAL, IRIS -- a1

    SMOOTH MUSC OF EYELID --a?

    CANAL OF SCHLEMM -- NOT INERVATED BUT:

    • a1 -- ENHANCED OUTFLOW
    • a2 -- DEC PROD
  161. DISTRIBUTION OF a AND b2 IN ARTERIOL BEDS
    b2 PREDOMINATE IN SKEL MUSC

    a PREDOMINATE IN GI AND KIDNEY
  162. HYPERTHYROIDISM
    GRAVE'S DISEASE

    EXCESSIVE THYROXINE INC THE SYNTH OF b-RECEPTORS

    USE b-BLOCKERS TO DEC THE SYMP-MEDIATED MANIFESTATIONS SUCH AS TREMOR, TACHYCARDIA, AND A-FIB
  163. EPI, NE, AND PE SELECTIVITY
    • EPI -- b2 > b1 > a
    • NE -- a > b1 > b2
    • PE -- a1 ONLY

    PE = PHENYLEPHRINE
  164. a1 RECEPTOR: LOCATIONS AND ACTION
    • Arterioles
    • constriction

    • Eye
    • enhanced normal
    • outflow of canal of schlemm


    • Eye
    • radial muscle
    • contraction of iris (dilation, mydriasis)


    • Kidney
    • proximal tubule
    • increased sodium/water reabsorption


    • Lung
    • bronchial gland
    • secretion decrease


    • Salivary Glands
    • water and K+ secretion (viscous and sticky)


    • Skin
    • pilomotor muscle
    • contraction


    • Urethra
    • contraction


    • Venules
    • constriction

    • --a1a--
    • Male Sex Organs
    • vas deferens, ampulla, prostate gland and seminal vesicles emission and ejaculation


    • Urinary Tract
    • trigone and ext. sphincter
    • contraction
  165. a2 RECEPTOR: LOCATIONS AND ACTION
    • Arterioles
    • constriction
  166. Eye
    decreased production of aq fluid in eye
  167. Pancreas
    • islet (B) cells
    • (insulin) decreased secretion
  168. Platelets
    aggregation
  169. Stomach and Intestines
    motility and tone decreased
  170. Stomach and Intestines
    secretion is inhibited
  171. Venules
    constriction
  172. b2 RECEPTOR: LOCATIONS AND ACTION
    • Arterioles
    • dilation (via circulating Epi)
  173. Gallbladder and ducts
    relaxation
  174. Liver
    glycogenolysis and gluconeogenesis increase
  175. Lung
    • bronchial muscle
    • relaxation
  176. Skeletal Muscle
    glycogenolysis, K+ uptake, tremor, and increased contractility
  177. Uterus
    relaxation for pregnant and nonpregnant women
  178. Venules
    dilation (via circulating Epi)