341 Final.txt

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341 Final.txt
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341 pharmacology December exam
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  1. cyclosporin A
    • calcineurin inhibitor, immunosuppressant
    • -binds to cyclophilins, mediators of protein folding-> bind calcineurin, block phosphatase activity on NFAT.
    • -psoriasis
    • -----------
    • - IBD, effective but frequent relapses, so short term only
    • - SE: nephrotoxicity, hairy lip (hirsuitism), neurotoxicity, hypertension, gingival hyperplasia
  2. sirolimus
    • rapamycin inhibitor
    • - binds to tac bp (fkbp) too, blocks 2nd messenger cascade induced by IL, so blocks prolif.
    • - no nephrotox, but dec. wbc, dec. platelets, hyperlipidemia
  3. lidocaine
    • local anesthetic, amide
    • - all routes of admin
    • - mod. lipid solub
    • - mod. toxicity ( esp if absorbed systemically)
  4. mycophenolate mofetil
    • purine biosynth inhib. (antiprolif)
    • - reversible, non-comp. inhib. of IMP dehydrogenase
    • - build up of IMP, dec. prolif
    • - blocks prolif of T cells & suppresses Ab formation by B cells
  5. procaine
    • local anesthetic, ester
    • - by infiltration ( dental)
    • - low lipid solub, low tox
  6. dobutamine
    • B1-selective agonist, also A1 (vascular beds -> VC)
    • - inc. peripheral R, inc. cardiac output
    • - for hypotensive emergency
  7. phenylephrine
    • selective A agonist (A1 & 2)
    • - decongestant ( constrict b.v. in mucous membranes)
    • - mydriasis
    • - inc. bp in emergency
  8. clonidine
    • A2-selective agonist
    • - dec. bp at CNS to dec. SNS output
    • - affect B1 (dec. Chrono / ino), A1 (dec. vasc tone)
    • - no effect on baroreceptors
    • - but if inject directly into bv, VC.
    • - antihypertensive, analgesia
    • - SE dry mouth, constip.
  9. solifenacin
    • M3-selectiveish, antimuscarinic
    • - esp. in smooth muscle (
    • bladder), not salivary.
    • - SE less common dry mouth.
  10. phentolamine
    • non-selective A-agonist (competitive)
    • - also inhibs responses of serotonin
    • - agonist at musc + h1 h2 receptors
    • - SE reflex tachy and antag of presyn a2 receptors
    • - use in reverse local VC,pheochromocytoma, male erectile dysfxn
  11. tetrodotoxin
    • natural toxin, Na channel blocker
    • - low lethal dose, due to paralysis of diaphragm and dec. bp
    • - pain and cardiac fibres very resistant.
  12. thromboxane
    • txa2
    • - platelet aggreg, VC
    • - txa2 receptor antag/ synth inhibitors
    • - developed for cvs indication, but not used yet
  13. saxitoxin
    • natural toxin, Na channel blocker
    • - from shellfish @red tide
    • - lethal @ low doses
    • - pain and cardiac fibre resistant
  14. basiliximab
    • IL-2 receptor antag
    • - inhibit association of IL2 beta +gamma subunits
    • - blocks IL-2 signal path
    • - competitive antag of IL-2 induced T cell prolif
    • - SE hypersensitivity
  15. mecamylamine
    • non-comp ganglion blocker
    • - open channel block of nicotinic receptor ( inc. Ach cannot overcome)
    • - not quaternary NH4+ cpd, can cross BBB
    • - 1st orally effective antihypertensive
    • (used for essential hypertens, but bad SE
  16. cevimeline
    • M1, M3 selective musc agonist
    • (low aff for M2 cardiac)
    • - Sjogren's syndrome; autoimmune: Abs against mucous membrane --> dry mouth
    • - used to inc. salivation, but inc. nausea and less bradycardia
  17. prostacyclin (eprostenol)
    • PGI2, agonist for IP
    • - vasodilator
    • - inhib platelet aggreg.
    • - vasc homeostasis
    • - used for pulm. hypertension
  18. coal tar
    • antipruritic (phenolic) + antiinflamm
    • - SE irritant folliculitis, phototoxicity, allergic contact dermatitis
    • - for psoriasis
  19. cyanopindolol
    • B3-selective agonist
    • - but not really selective
    • - B3: inc. lipolysis, but also tachy and tremor from other B receptors being stimd
    • - may work to relax overreactive detrusor muscle of bladder
  20. sulprostone
    • selective EP3 R agonist (some EP1)
    • - not on market
    • - but may be useful for GI effects
  21. alitretinoin
    • non-selective retinoid R agonist
    • - isomer of retinoic acid
  22. alprostadil
    • prostaglandin EP R agonist
    • - PGE1 = PGE2 analogue
    • - used for VD, maintain ductus arteriosus, treat erectile dysfxn (intracavernous or urethral supp)
    • - SE penile pain, PGE effects
  23. atropine
    • musc. receptor antag: antimusc
    • - competitive antag @ all MRs
    • - effects: opposite to PSNS
    • - used for Acute MI (keep heart faster), preop antinauseant (anesth induced), pesticide overdose (counters inc. Ach effect)
    • - ***increases distension pain thresholds in esophagus, b/c inhibit chol. mediated esophageal contraction and gastric acid secretion.
  24. trimethaphan
    • comp. gang blocker
    • - antag of NN receptor subtype
    • - prevent depol of ANS effector
    • - direct peripheral VD from A-adrenergic block
    • - polar: cannot cross CNS
    • - used to treat hypertens emerg
  25. prazosin
    • A1 selective antag
    • - relaxes arterial + venous smooth muscle
    • - used to treat hypertension, mild benign prostatic hyperplasia
  26. pralidoxime
    • cholinesterase reactivator
    • - reverses toxic effects of Ach-esterase inhibs tog. w/ atropine
    • - cleaves dialkylphosphate group from active site. only works acutely.
  27. latanoprost
    • PGF2 analogue, agonist for FP
    • - lowers IOP (treat glaucoma)
    • - increase matrix metalloproteinase levels to remodel extracellular matrix between ciliary muscle cells (open holes between muscle bundles)
    • - inc. uveoscleral outflow by 60-100%- SE: conjunctival hyperemia,
    • iris darkening (stimulation of melanogenesis in iridial melanocytes),
    • increased browth and darkness of eyelashes.
  28. tyramine
    • indirect sympathomimetic
    • - releases stored catecholamines
    • - metabolized by MAO
    • - high 1st pass metab @liver
  29. zileuton
    • leukotriene inhibitor
    • - treat asthma, 2o choice in mild-mod persistent
    • - direct inhibition of enzyme 5-lipoxygenase
    • - SE (broad b/c blocks all LTs), GI, headache, nausea
    • - metabd by cyt p450 (warf, theophyll, prop)
    • -**LTD4 is 100x more pitent than histamine at causing bronchoconstriction
  30. benztropine
    • antimuscarinic (non-selective)
    • - CNS > periphery
    • - treat tremor in pts w/ Parkinsons
    • - less drooling too
  31. ipratropium
    • antimuscarinic
    • - inhaled: low systemic SE (anticholinergic)
    • - topical bronchoD and decrease mucus secretion (b/c block M3 for bronchoD, and prevent vagal stimulation)
    • - SE: causes dry mouth
    • - not rescue
    • - useful if lots of vagally mediated bronchoC, mucous plugs
  32. calcipotriene
    • synth vit d3 deriv
    • - for psoriasis treatment
    • - inc. differentiation and dec. prolif of keratinocytes
    • - VDR and RXR: DNA target gene
    • - SE burning, itching, dryness, erythema, hypercalcemia
  33. nicotine
    • nicotinic receptor agonist
    • - nonselective neuronal and skeletal m
    • - activates PSNS and SNS
    • - CNS effects bc cross BBB - tremors, nausea (chemoreceptors)
    • - SNS heart (hypertens, tachy)
    • - PSNS bronchoC, inc. resp sec, GI (N/V), inc.VP
  34. acebutolol
    • B1 selective antag, partial agonist
    • - for hypertens, angina
    • - SE fatigue, dizziness, (less brady, affect lipid)
  35. carbachol
    • nonselective musc & nic agonist
    • - resistant to cholinesterases
    • - for open angle glaucoma ( inc. trabecular outflow by tugging on trabecular meshwork)
    • - SE: blurred vision(cycloplegia), dimmed vision, bad night vision, ciliary muscle spasm, cataracts.
  36. pilocarpine
    • musc. selective agonist
    • - treat open-angle glaucoma (dec. IOP by inc. trabecular outflow, pull on trab. meshwork)
    • - treat xerostomia (dry mouth) from cancer chemo or Sjogren's syndrome
    • - increases salivation and sweat
    • - SE: blurred vision (cycloplegia), dimmed vision, bad night vision, ciliary muscle spasm (headache), cataracts
  37. scopolamine
    • anti-muscarinic
    • - competitive antag @ all MRs
    • - crosses BBB better than atropine, so causes drowsiness/fatigue
    • - SE mydriasis, cycloplegia, less effect on HR
    • - treat motion sickness (but dec. saliva, acts on CNS to dec. nausea)
  38. azathioprine
    • purine biosynthesis inhib (antiprolif), immunosuppressant
    • - pro-drug -> converted to 6-mercaptopurine -> 6-mp ribonucleotide
    • - looks like IMP, competes
    • - inc. [IMP] = -ve feedback, dec. prolif
    • - acts early during prolif cycle of T and B cells
    • ------------
    • - induce and maintain remission in UC and CD
    • - 3-6 mo of treatment, 50-60% pts get remiss.
    • - can allow steroid reduction/elimination
    • - SE: increased risk of infection, N/V, leukopenia, hepatotoxicity, pancreatitis, alopecia
  39. butaprost
    • selective EP2 agonist
    • - cause joint inflamm
    • - not on market
  40. tolterodine
    • anti-musc
    • - may be selective for bladder > salivary
    • - vs. Oxybut: less dry mouth, but less effective
    • - may selectively antag M2?
    • - blocks PSNS inhib. of SNS med'd relax
    • - also causes tachycardia
  41. acetylcholine
    • non-selective cholinergic
    • - but most effects from muscarinic
    • - PSNS effects plus:
    • - sweating (musc, even though SNS)
    • - VD (MR on vascular epi) -> hypotension -> baroreceptors -> reflex tachy
    • - dec. inotropy (ventricular force)
    • -------------------------
    • - IPAN release ACh, induce vagal excitation
    • - ENS excitatory neurotransmission -> interneurons -> enteric motor neurons on smooth muscle (M3)
  42. epinephrine
    • direct-acting sympathomimetic
    • non-selective adrenergic agonist
    • - made in adrenal glands
    • - not cross BBB, but indirect CNS effects: fear, tremor...
    • - mydriasis, VC (skin), VD (skeletal muscle)
    • - inc. HR (inc. SBP), VD skm (dec. DBP), bronchoD, dec. GI motility, dec. VP, sweating, palor
  43. norepinephrine
    • non-selective adrenergic agonist
    • - + inotrope (force), + chronotrope (HR)
    • - VC - more potent than epinephrine
    • - less VD of skeletal muscle and bronchoD
    • - decrease both DBP & SBP
  44. tubocurarine
    • non-selective ganglion blocker (comp)
    • non-depol NM receptor blocker - postsynaptic (muscle relax)
    • - can be diag. agent for MG
    • - SE histamine release, increased saliva
  45. black widow spider toxin
    • presyn mech @ NMJ
    • - cause massive release of ACh
    • - empties vesicles, prevents refill -> paralysis of muscles -> death
  46. hemicholinium
    • non-comp ganglion blocker
    • - open channel block of NR
    • - depletes choline @ presyn. bouton, blocks reuptake
    • - dec. efficacy of synaptic transmission
  47. selegiline
    • MAO inhibitor
    • - blocks breakdown of NE + other catecholamines
    • - 2 types of MAO:
    • - A -> liver
    • - B -> more CNS, so if inhibit B, can still allow A to fxn in liver and breakdown stuff
  48. metoprolol
    • B1 selective antag, not partial agonist
    • - use in hypertension, angina, post MI, pref. for diabetes
    • - B2 not blocked, so no bronchoC
    • - SE fatigue, dizzy, bradycardia
  49. phenoxybenzamine
    • A1 selective antag (irreversible)
    • - inhib. reuptake of NE, blocks histamine, Ach, serotonin
    • - SE postural hypotension + tachy
  50. NSAID
    • COX inhibitor
    • - analgesia - blocks formation of all PGs (PGE2)
    • - dysmenorrhea (from inc. PGE2 and PGF2)
    • - treat patent ductus arteriosus (PGE2 keeps it open after birth)
  51. ephedrine
    • direct mixed agonist (A and B)
    • - enhances NE release
    • - mild stimulant
  52. pancuronium
    • non-depol. NMJ blocker
    • - SE no histmaine release/ganglion blockade
    • - only affects NMJ - selective
  53. benzocaine
    • local anesthetic - ester
    • - topical (skin, mucous memb)
    • - moderate lipid solub
    • - toxicity = methemiglobinemia
  54. daclizumab
    • IL-2 receptor antag (human/rodent combo Ab)
    • - inhibits association of IL2 beta and gamma subunits, so blocks IL2 signalling path
    • - and competitive antag of IL2 induced T cell prolif
    • - SE rare hypersensitivity
  55. isoproterenol
    • B-selective agonist (B1 and B2)
    • - B1 effects (+ chrono/ino)
    • - B2 effects (vasodilator)
    • - inc. cardiac output (w/ little change bp)
    • - decrease DBP, increase SBP
  56. mifepristone
    • glucocorticoid R antagonist
    • - act by preventing dissociation of glucocorticoid receptor from heat shock protein
    • - also strong antiprogestin -> abortion
  57. reserpine
    • blocks NE uptake + storage
    • - leads to catecholamine depletion
    • - antihypertensive and serious depression
    • - must be used with diuretic b/c alone causes sodium retention
  58. pimecrolimus
    • calcineurin inhibitor (immunosuppressant)
    • - bind tacrolimus binding protein (fkbp)
    • - bind calcineurin-->inhibit T cell prolif
  59. labetalol
    • mixed= A1-selective blocker, non-selective B-blocker, B2 agonist activity
    • - causes hypotension w/ less tachy than A-blockers b/c B blockade prevents reflex tachy via baroreceptor reflex.
  60. Parathion, Diazinon, Malathion (organophosphorus insecticides)
    • acetylcholinesterase inhibitor
    • - cause ACh toxicity: DUMMBELSSS
  61. 4-aminopyridine
    • presynaptic NMJ mech
    • K+ channel blocker
    • - prevents repolarization, prolonged action potentional allows conduction thru damaged nerves
    • - used for MS, MG, spinal cord injury
  62. dantrolene
    • @ muscle cells, decrease release of Ca2+ from sarcoplasmic reticulum
    • - muscle relax b/c of dec. Ca2+
    • - crosses BBB -> drowsy
    • - treat malignant hyperthermia, spasticity
  63. succinylcholine
    • depolarizing NMJ blocker (non-comp)
    • - maintain depol --> desensitize NR
    • - broken down by pseudocholinesterases in blood
    • - non-selective
    • - SE arrhythmias, vomit, musclar pain, inc. IOP
  64. alpha-bungarotoxin
    • non-depolarizing NMJ blocker
    • - from snake (cobra) bite
    • - rapid paralysis of skeletal muscles and diaphragm
    • - death from resp. failure
  65. adapalene
    • selective agonist for RAR-gamma
    • - derivative of naphthoic acid
    • - SE burning, stinging, peeling, erythema, inc. photosensitivity
  66. tazarotene
    • selective RAR-beta/gamma agonist
    • - prodrug --> tazarotenic acid
    • - anti-inflamm, antiprolif
    • - absorbed percutaneously --> teratogen
    • - therefore, female must be on contraception
  67. isotretinoin
    • non-selective agonist of retinoid receptors
    • oral retinoid, synthetic Vit. A derivative
    • - not made or converted in body
    • - toxicity: like Vit A induced
    • - inc. cholesterol + TG
    • - headache, corneal opacities, inc. IOP, teratogenicity
  68. benzoyl peroxide
    • antibiotic for acne
    • - penetrates stratum corneum, metabolized to benzoic acid @ epidermis/dermis
    • - antimicrobial, peeling, comedolytic
    • - irritation concentration dependent, contact sensitizer
    • - oxidant --> bleaching
  69. bexarotene
    • selective RXR agonist
    • - useful for cancers, i.e. cutaneous T-Cell lymphoma
    • - SE inc. TG, inc. cholsterol, hypothyroidism, leukopenia
  70. corticosteroids & NSAIDs
    • prostaglandin synthesis inhibitors
    • - corts: block all PG + LT
    • - NSAID: block COX, promote LT synth (because inc. arachadonic acid)
  71. prostaglandins
    • products of cyclooxygenase pathway
    • - COX1 -> housekeeping
    • - COX2 -> expression depends on stimuli
  72. isoprostanes
    • prostaglandin isomers
    • - COX not needed to make isoprostanes
    • - potent VC, may dec. inflamm?
  73. dinoprostone
    • PGE1 = PGE2 analogue
    • - promotes uterine contractions (induce birth)
    • - @ end of term-> delivery, otherwise abortion
    • - SE abdominal discomfort, diarrhea
  74. oxybutnin
    • selective anti-muscarinic
    • (M1 + M3 >>> M2) = less CVS SE
    • - dec. frequency of detrusor muscle contraction
    • - delay desire to void
    • - treat urinary incontinence
    • - SE dry mouth, drowsiness, constipation, blurred vision
  75. acitretin
    • synthetic non-sel. Vit A derivative
    • - oral, for pustular forms of psoriasis
    • - avoid ethanol, promotes drug
    • - retinoic acid + tazarotene for less severe psoriasis
  76. amphetamine, methamphetamine
    • indirect sympathomimetic
    • - reuptake inhibitors
    • - inc. activity of CNS
  77. misoprostol
    • PGE1 = PGE2 analogue, acts at EP1 and EP3
    • - cytoprotective @ low dose
    • - inhibit gastric acid secretion @ high dose
    • - prevent NSAID ulcers, abortion
    • - SE abdominal discomfort, diarrhea
  78. propranolol
    • non-selective B-blocker
    • - treats hypertens, angina, migraine, tremor, dec. sudden death post MI, hyperthyroidism
    • - SE get into CNS (fatigue, dizzy), brady, inc. TG levels significantly
  79. xylometazoline/oxymetazoline
    • selective A-agonist
    • - topical decongestant
    • - oxy may cause hypotens b/c sig. affinity for A2 receptors, and therefore inc. nasal congestion b/c better perfusion in nasal mucous membrane
  80. azelaic acid
    • topical antibiotic
    • - straight chain sat'd dicarboxylic acid
    • - antimicrobial, testosterone -/-> dihydrotestosterone
    • - decreases inflammation + erythema
    • - treats acne vulgaris, rosacea
    • - SE redness, dryness
  81. salbutamol
    • B2 selective agonist (short-acting)
    • - for asthma
    • - bronchodilation effect lasts 3-6 hours
    • - for intermittent asthma, or rescue medication for acute asthma attacks in persistent asthma
    • - not for frequent use, this indicates worsening control
  82. montelukast
    • leukotriene receptor antagonist
    • competitive antag @ CystLT1 (end target of C4 D4 E4)
    • - treat asthma, allergic rhinitis
    • - more selective, so less SE than Zileuton
    • - very expensive
  83. tacrolimus
    • calcineurin inhibitor (immunosuppressant)
    • - binds tacrolimus binding protein (fkbp)
    • - binds calcineurin and inhibits T cell prolif
    • - less hypercholesteremia
  84. pyridostigmine
    • cholinesterase inhibitor
    • - drug of choice for MG
  85. neostigmine
    • cholinesterase inhibitor (indirect)
    • - treat post-op ileus (bowels stop)
    • - treat post-op urinary retention
    • - can be used for MG
  86. guanethidine + bretylium
    • indirect sympathomimetic
    • - prevent release of NE, used as antihypertensive
    • (bretylium = antiarrythmic)
  87. dopamine
    • 1. selective adrenergic agonist
    • - D1: vascular sm relax
    • - D2: suppress NE release, inc. VD renal bf
    • - B1: heart
    • --@ low doses: dec. peripheral R
    • --@ high doses: mimic epinephrine? inc. work of heart, better perfusion
    • --------------------
    • 2. inhibitory neurotransmitter of ENS
    • - inhibit GI motility via presynaptic D2 receptors
    • - dec. ACh release by myenteric neurons
  88. lubiprostone
    • prostaglandin E analogue
    • but not act on EP receptors when orally
    • - GI: activate voltage dep. Cl- channels
    • --inc. Cl- in intestinal tract, inc. fluid secretion, inc. GI transit
    • - used for constipation
    • - SE N/V, cramps
  89. atacurium
    • non-depolarizing NMJ blocker
    • - slight histamine release
    • - short acting
    • - can be given to kidney/liver dysfxn pts
  90. botulinum toxin
    A (botox)
    B (myobloc)
    • blocks vesicle release (ACh) @ NMJ by cleaving docking proteins
    • - A - cleave SNAP 25 (longer lasting)
    • - B - cleave VAMP/synaptobrevin --> flaccid paralysis of skeletal muscle
  91. betamethasone/dexamethasone
    • potent anti-inflamm
    • - no mineral cort. action b/c selective for GC receptor
  92. prednisone
    • corticosteroid
    • - used to treat Myasthenia Gravis
    • - weak anti-inflamm, but 5x more potent than HC
  93. edrophonium
    • acetylchilnesterase inhibitor
    • - reverses paralysis from non-depol. NM blockers
    • - MG diagnostic agent (will cause inc. muscle strength if MG)
    • - no CNS effects
    • - *** increases pain sensitivity for GERD b/c in inc. cholinergic mediated esophageal/GI smooth muscle contractions and increases gastric acid secretion.
  94. muromonab-CD3 (anti-CD3 ab)
    • lymphocyte-depleting agent
    • - binds CD3 on T cell surface, prevents Ag binding to recognize complex, so cell-mediated cytotoxicity blocked
    • - may cause cytokine release syndrome, human Ab against mouse to decrease efficacy
  95. bethanechol
    • musc-selective agonist
    • - mostly act on GI & urinary tract
    • - treat urinary retention and GERD in kids
  96. pirenzapine
    • M1-selective antagonist
    • - lower incidence of dry mouth
    • - decreases GI acid secretion, so once used to treat PUD
  97. antithymocyte globulin
    • lymphocyte-depleting agent (immunosuppressant)
    • - rapid dec. in T and B lymphoid cells
    • - knock out cell-mediated immunity, therefore inc. risk of malignancy + opportunistic infection
    • - cort + calcineurin inhib. sparing
  98. epibatidine
    • - high affinity for neuronal + muscle (more potent than nicotine)
    • - muscarinic antagonist too
    • - potent analgesic (200x > morphine)
    • - too toxic b/c activates all NRs
    • - from poison dart frog
  99. tamsulosin
    • selective antag for alpha1A + D
    • - greater effect on prostate sm than vascular sm
    • - treat mild benign prostatic hyperplasia
    • - but cause lots of dizziness
  100. alefacept
    • anti-CD2 Ab
    • - blocks CD4 T Cell activation
    • - slows down cell-mediated immunity
    • - dec. T cell count, inc. risk of cancer
    • - treat mod/severe plaque psoriasis
  101. vesamicol
    • non-selective, presynaptic cholinergic mech
    • - blocks ACh uptake into vesicles
    • - @ all cholinergic terminals (including NMJ)
  102. retinoic acid (tretinoin)
    • non-selective agonist of retinoid R
    • - acid form of Vit A
    • - stabilize lysosomes, inc. RNA pol activity
    • - dec. cohesion btwn epidermal cells
    • - inc. expulsion of comedones, white --> black
  103. leflunomide
    • purine biosynth inhib (antiprolif)
    • - inhib. dihydroorotate dehydrogenase
    • - depletes UMP, so dec. prolif b/c block de novo DNA synth
    • - treat rheumatoid arthritis
    • - SE no leukopenia or thrombocytopenia
  104. bupivacaine
    • local anesthetic, amide
    • - all routes of admin
    • - high lipid solub
    • - high toxicity (cardiotoxic)
  105. timolol
    • non-selective B-blockers
    • - dec. aq humor production & inc. trabecular outflow by B2 mechanism
    • - SE: well tolerated, major problem: dry eyes, systemic effects (bronchoconstriction...)
  106. levobunolol
    • non-selective B-blockers
    • - dec. aq humor production & inc. trabecular outflow by B2 mechanism
    • - SE: well tolerated, major problem: dry eyes, systemic effects (bronchoconstriction...)
  107. betaxolol
    • B1-selective-blocker
    • - dec. aq humor production & inc. trabecular outflow by B2 mechanism
    • - SE: well tolerated, major problem: dry eyes, systemic effects
    • - B1 selectiveness not relevant as eye drop: [drug] inc. lots, so it can block B2 too.
    • - advantage: if systemic absorption, will not affect lungs b/c not B2 blocker, so less SE.
  108. apraclonidine
    • A2-agonist
    • - dec. aqueous humor production
    • - inc. uveoscleral outflow
    • - SE: less effective than B-blocker, allergic conjunctivitis
    • - if get into CNS: sedation & hypotension (act like clonidine and decrease SNS output.)
  109. brimonidine
    • A2-agonist
    • - dec. aqueous humor production
    • - inc. uveoscleral outflow
    • - SE: less effective than B-blocker, allergic conjunctivitis
    • - if get into CNS: sedation & hypotension (act like clonidine and decrease SNS output.)
  110. physostigmine
    • cholinesterase inhibitor
    • - for open angle glaucoma ( inc. trabecular outflow by tugging on trabecular meshwork)
    • - SE: blurred vision(cycloplegia), dimmed vision, bad night vision, ciliary muscle spasm, cataracts.
  111. travoprost
    • PGF2 analogue, agonist for FP- lowers IOP (treat glaucoma)
    • - increase matrix metalloproteinase levels to remodel extracellular
    • matrix between ciliary muscle cells (open holes between muscle bundles)
    • - inc. uveoscleral outflow by 60-100%
    • - SE: conjunctival hyperemia, iris darkening (stimulation of melanogenesis in iridial melanocytes), increased browth and darkness of eyelashes.
  112. bimatoprost
    • PGF2 analogue, agonist for FP- lowers IOP (treat glaucoma)
    • - increase matrix metalloproteinase levels to remodel extracellular
    • matrix between ciliary muscle cells (open holes between muscle bundles)
    • - inc. uveoscleral outflow by 60-100%- SE: conjunctival hyperemia,
    • iris darkening (stimulation of melanogenesis in iridial melanocytes),
    • increased browth and darkness of eyelashes.
  113. dorzolamide
    • topical carbonic anhydrase inhibitor
    • - decreases rate of aqueous humor formation by blocking bicarbonate formation (bicarb is produced by ciliary muscle carbonic anhydrase)
    • - topical less effective than oral
    • - CI: avoid if sulfa allergy
    • - SE: fatigue, depression, paresthesias (burning/prickling sensations)
  114. brizolamide
    • topical carbonic anhydrase inhibitor
    • - decreases rate of aqueous humor formation by blocking bicarbonate
    • formation (bicarb is produced by ciliary muscle carbonic anhydrase)
    • - topical less effective than oral
    • - CI: avoid if sulfa allergy
    • - SE: fatigue, depression, paresthesias (burning/prickling sensations)
  115. acetazolamide
    • oral carbonic anhydrase inhibitor
    • - decreases rate of aqueous humor formation by blocking bicarbonate
    • formation (bicarb is produced by ciliary muscle carbonic anhydrase)
    • - topical less effective than oral
    • - CI: avoid if sulfa allergy
    • - SE: fatigue, depression, paresthesias (burning/prickling sensations)
  116. budesonide
    • inhaled corticosteroid
    • - for maintenance/prophylaxis of asthma, most effective controller
    • - reduce symptoms, inc. QOL and lung function, dec. airway hyperresponsiveness and bronchoC
    • - reduce freq and severity of asthma exacerbations and decrease asthma morbidity and mortality
    • - rare to have HPA-axis suppression at low dose
    • - rinse mouth after: risk oral candidiasis
    • - SE: cough and oral thrush
    • - SE of systemic: weight gain, osteoporosis, thin skin, PUD, decreased muscle mass...
  117. beclomethasone
    • inhaled corticosteroid
    • - for maintenance/prophylaxis of asthma, most effective controller
    • - reduce symptoms, inc. QOL and lung function, dec. airway hyperresponsiveness and bronchoC
    • - reduce freq and severity of asthma exacerbations and decrease asthma morbidity and mortality
    • - rare to have HPA-axis suppression at low dose
    • - rinse mouth after: risk oral candidiasis
    • - SE: cough and oral thrush
    • - SE of systemic: weight gain, osteoporosis, thin skin, PUD, decreased muscle mass...
  118. fluticasone
    • inhaled corticosteroid
    • - for maintenance/prophylaxis of asthma, most effective controller
    • - reduce symptoms, inc. QOL and lung function, dec. airway hyperresponsiveness and bronchoC
    • - reduce freq and severity of asthma exacerbations and decrease asthma morbidity and mortality
    • - rare to have HPA-axis suppression at low dose
    • - rinse mouth after: risk oral candidiasis
    • - SE: cough and oral thrush
    • - SE of systemic: weight gain, osteoporosis, thin skin, PUD, decreased muscle mass...
    • - fluticasone (newer) have less systemic activity than older compounds (triamcinolone)
  119. albuterol
    • B2 selective agonist (short-acting)- for asthma- bronchodilation effect lasts 3-6 hours
    • - for intermittent asthma, or rescue medication for acute asthma attacks in persistent asthma
    • - not for frequent use, this indicates worsening control
  120. salmeterol
    • B2 agonist (long-acting)
    • - for asthma
    • - BD effect lasts 12 hours
    • - 3rd line, add only after used ICS and SABA and still inadequate effect.
    • - should never be used for asthma without antiinflammatory medication (i.e. cort)
    • - SE: skeletal muscle tremor, tachy, tolerance
    • - overuse - decreased B receptor responsiveness, increased cardiovascular events (death in black males)
  121. formoterol
    • B2 agonist (long-acting)
    • - for asthma
    • - BD effect lasts 12 hours
    • - 3rd line, add only after used ICS and SABA and still inadequate effect.
    • - should never be used for asthma without antiinflammatory medication (i.e. cort)
    • - SE: skeletal muscle tremor, tachy, tolerance
    • - overuse - decreased B receptor responsiveness, increased cardiovascular events (death in black males)
  122. theophylline (aminophylline)
    • methylxanthine, adenosine receptor antagonist
    • - bronchodilation, inc. mucociliary clearance, affects eosinophils/t-cells
    • - inhibit cyclic nucleotide phosphodiesterase to inhibit degrad. of cAMP & cGMP
    • - at high doses, stimulant -> inhibit sleep.
    • - used orally for severe asthma.
    • - SE: tachy, increased cardiac output, potential to induce tachyarrthymias (sudden death), gastric upset, weak diuresis
    • - caffein: moderate bronchoD, mimics effect of theophylline
  123. cromolyn sodium, nedocromil
    • mast cell stabilizer
    • - blocks bronchoconstriction for exercise-induced/allergic asthma, mild persistent
    • - inhibit release of inflammatory mediators (histamine from mast cells)
    • - altered PSNS response, leukocyte fxn
    • - SE: cough, dryness, unpleasant taste. rare dermatitis/myositis
    • - nedocromil more effective than cromolyn, may reduce ICS usage.
  124. montelukast
    • leukotriene inhibitor
    • - recomb. monoclonal antibody against IgE
    • - competitive antag @ CystLT1 receptor, so it affects smooth muscle constriction, immune cell infiltration, and vascular changes (edema)
    • - sig. less effective (and $$$$) than ICS
    • - add-on therapy, preventative, less SE than oral corts
    • - SE: minor GI, headache, nausea
    • - **LTD4 is 100x more potent than histamine at causing bronchoC
  125. omalizumab
    • leukotriene inhibitor
    • - bind FC receptor on IgE, so prevents IgE from binding to mast cells --> prevent mast cell degranulation.
    • - affects new IgE only, not those already bound; but blocks degranulation even if IgE already present on mast cell.
    • - target strong allergic associated asthma
    • - iv, can cause anaphylaxis (because mouse Ab)
    • - for pts not optimally controlled on standard therapies or have sig. SE from ICS
    • - **LTD4 is 100x more potent than histamine at causing bronchoC
  126. adenosine triphosphate ATP
    • non-cholinergic excitatory neurotransmitter for ENS, between myenteric interneurons and from interneurons-> inhibitory motor neurons.
    • - acts on P2X and P2Y receptors
    • - P2X: ligand-gated cation channels (like nicotinic), fast excitatory responses
    • - P2Y: G-protein coupled receptor, slow excitatory effects
    • - regulated release of ATP can activate sensory nerve terminals to transduce distension. Overdistension also triggers pain.
    • - injury inc. ATP, so more peristaltic activity (cramping in gut injury)
  127. serotonin (aka 5-hydroxy-tryptamine)
    • non-chol. excitatory neurotransmitter for ENS
    • - activates on 5-HT3 and 5-HT4 receptors
    • - 5-HT3(cation), 5-HT4(G-protein)
    • - 60-90% of total 5-HT is in enterochromaffin cells of GI mucosa
    • - released by: ingestion of food, dec. pH, presence of a.a. or f.a., mucosal distortion, obstruction of gut motility.
    • - modulates smooth muscle fxn (contract/relax), intestinal secretion, responses to visceral pain
    • - eliminated by MAO
    • ----------------
    • peripheral serotonin modulates:
    • - CVD fxns: platelet aggregation, smooth muscle contraction
    • - GI tract motility (found in enterochromaffin cells and neurons of ENS)
    • - musculoskeletal pain (receptors on nerve fibres that convey noxious input to brain)
    • central roles:
    • - serotonergic neurons found in raphe nuclei (brain stem, involved in mood, sleep, vomiting, pain...)
    • -----------------
    • Serotonin actions upon injection:
    • 1) immediate chemoreceptor reflex: dec. HR/CO/BP
    • 2) reciprocal inc. BP b/c of vasoconstriction (in all b.v. except skeletal muscles)
    • 3) slow onset dec. in BP b/c of vasodilation in skeletal muscle b.v.
  128. substance P
    • non-chol. excitatory neurotransmitter for ENS
    • - activates tachykinin NK-1 receptor (also by neurokinin A & B) in GI and CNS (central emetic pathways)
    • - NK-1 is G-protein, so slow.
    • - increased motility, perceived as discomfort (pain too, but not in humans)
    • - in chemically-induced nausea/emesis, maybe IBD
    • - * chemo-induced nausea: acute from 5-HT, delayed from substance P?
  129. aprepitant
    • NK-1 antagonist for chemo-induced emesis (esp cisplatin)
    • - was initially made as analgesic, but didnt work on humans
    • - poor solubility so cannot give IV/SC, must be PO. But when pt. nauseated, don't want PO...so not used often.
    • - interacts with cyt P 450 --> DIs
    • - very $$$$$$$$$$$
  130. adenosine
    • - inhibitory neurotrans of ENS
    • - acts on A1, A2a, A2b, A3 receptors
    • - modulates peristaltic activity and mucosal secretions
    • - relaxation of intestines (slow down peristalsis) by A1 and A2b
    • - antagonists at A1 receptors can enhance release of ACh or tachykinins from myenteric ganglia to speed up peristalsis (e.g. caffeine)
  131. metoclopramide
    • non-selective dopamine receptor antagonist
    • - prokinetic drug
    • - non-selective, but acts especially on D2 in gut
    • - by enhancing ACh release, increase GI motility, esophageal peristaltic amplitude and sphincter pressure, gastrick emptying
    • - no effect on small intestion or colonic motility
    • - crosses BBB to CNS, so brain effects too: may block D2 receptors in chemoreceptor trigger zone (antinausea and antiemetic).
    • - SE: CNS restlesness, drowsiness, agitation...
  132. domperidone
    • non-selective dopamine receptor antagonist
    • - prokinetic drug
    • - non-selective, but acts especially on D2 in gut
    • - increases GI motility by enhancing ACh release
    • - domperidone does NOT cross BBB.
    • - SE: well tolerated, but elevate prolactin levels (breast enlargement, tenderness...)
  133. B-endorphin, methionine-enkephalin
    • endogenous pain suppressors, mu, delta, kappa receptor agonists; opioid peptide
    • - primarily mu receptor agonist
    • - decrease release of ACh to delay GI transit --> constipation
    • - inhibit intestinal ion and fluid secretion, increase intestinal fluid, may block propulsive motility by evoking tonic spasms.
  134. loperamide
    • peripheral mu-opioid receptor agonist
    • - does not penetrate CNS, so no effects on cognition or arousal
    • - slows GI transit, inc. intestinal water absorption, increase resting sphincter tone...never lose effect.
    • - used to treat diarrhea, IBS, pain(?...may have analgesic effects if work peripherally on mu-receptors in sensory fibres)
    • - SE: constipation, cramping, dry mouth, nausea
  135. entero-endocrine cells and hormones
    • released when sense luminal contents, activate afferent nerve endings.
    • D-cells: release somatostatin to inhibit afferent fibres
    • Enterochromaffin cells: release serotonin to activate secretory, peristaltic, sensory reflexes
    • G-cells: gastrin to increase acid
    • Response to food -> G-cells in antrum release gastrin into blood -> gastrin activates CCK2 receptors on ECL-cells -> ECL release histamine -> histamine act on parietal cells to pump acid out at H+/K+ ATPase -> acid release suppresses gastrin release.
  136. sumatriptan
    • 5-HT1B/D agonist
    • - causes vasoconstriction of cerebral arteries to terminate migraine
    • - but not very selecive for cerebral arteries, so can cause coronary vasospasm --> worse for elderly males
    • - used to treat acute migraine headache
    • - SE: chest discomfort from coronary vasospasm
  137. ketanserin
    • 5-HT2 receptor antagonist
    • - blocks vascular A1 adrenoreceptors, and has hypotensive action b/c of A1 blockade.
    • - blocks 5-HT2A effects (platelet aggreg, vascular smooth muscle contraction), 5-HT2B effects (skeletal muscle/heart vasodilation)
    • - originally marketed for antihypertensive, but withdrawn b/c of arrhythmic effects
    • - SE: proarrhythmic
  138. ondansetron
    • prototypical 5-HT3 antagonist, non-competitive channel blocker (get stuck in channel)
    • - can block nauseating effect of serotonin
    • - used in prevention of N/V associated with surgery or chemo (when enterochromaffin cells damaged)
    • - SE: constipation, diarrhea, headache
  139. cisapride
    • 5-HT4 agonist
    • - was used to treat GERD/motility disorders b/c speed clearance of food from stomach to intestines.
    • - but proarrhythmic (blocks K channels) so removed
    • (small bowel: mediate relaxation of smooth muscle cells)
  140. tegaserod
    • 5-HT4 partial agonist
    • - activate, but not as strong as serotonin; may also be a serotonin reuptake inhibitor? but not supported.
    • - stimulates peristaltic reflex (release CGRP to stim. contraction of intestine)
    • - claimed to dec. visceral afferent signaling (GI pain)
    • - SE: diarrhea, heart attack, stroke, worsening heart pain
    • - used to treat IBS w/ constipation, but withdrawn from market because of SE.
  141. alosetron
    • 5-HT3 receptor antagonist
    • - reduce visceral sensitivity and colonic transit, ab pain, diarrhea
    • - SE: severe constipation/ischemic colitis
    • - used to treat IBS with diarrhea (but can make u become constipated!)
  142. histamine
    • injection (don't do it!)
    • 1) dec. SBP and DBP b/c of direct vasodilation
    • 2) tachy (histamine stim. heart and reflex tachy)
    • 3) flushing, warmth, headache
    • 4) edema (protein extravasation)
    • 5) mild wheezing--> bronchoC
    • ---------
    • peripheral actions:
    • - gastric acid release (found in ECL cells)
    • - inflammation (injury-related release to cause VD, leakage of inflammatory mediators complement, CRP, antibody invasion)...
    • - pain: stimulate sensory nerve endings mediating pain and itching
    • -------------
    • central roles of histamine:
    • - histaminergic neurons in tuberomamillary body (hypothalamus) --> neuroendocrine control, CVD reg, thermal/body weight reg, arousal.
  143. diphenhydramine, chlorpheniramine, dimenhydrinate
    • H1 receptor antagonist (neg. effect on H2 and H3)
    • - "first generation"
    • - penetrate CNS, strong sedative effects, anticholinergic, alpha-adrenergic antagonist.
    • - uses:
    • - allergic rxns (prevent/treat symptoms, acute urticaria)
    • - antinausea/antiemetic actions: prevent motion sickness, treat N/V, suppress effects on extrapyramidal symptoms associated with antipsychs
    • (e.g. Diclectin: doxylamine + dimenhydrinate for pregs)
    • - sedation: antimusc, effective for mild insomnia, temorary relief, cause daytime drowsiness, tolerance. (but kids may get excitation instead of sedation)
    • - local anesthesia (topically): diphenhydramine blocks sodium channels like lidocaine, more potent than procaine. used when patient is allergic to conventional l.a. drugs
    • - SE: unwanted sedation (50%), dry mouth, urinary retention, blurred vision (anticholinergic), orthostatic hypotension (alpha-adrenergic receptor antagonist effect)
  144. loratadine, cetirizine
    • second-generation H1 receptor antagonist
    • - poor CNS pen, so little/no sedation
    • - used in allergic conditions (hay fever, rhinitis, chronic urticaria)
    • - SE: unwanted sedation (7%), tolerance.
  145. ranitidine
    • H2 Receptor Antagonist (highly selective)
    • - competitive inhibition at parietal cell H2 receptors, so reduces histamine release from ECL cells and blocks direct stimulation of parietal cell by histamine.
    • - suppresses basal and meal-stim'd acid secretion, each dose 50% reduction for 10 hours
    • - 2nd line for ulcers
    • - GERD, dyspepsia, stress-related ulcers (dec. incidence of bleeding)
    • - SE: diarrhea, headache, fatigue, myalgias, constip...confusion, hallucinations, agitation in ICU/elderly.
    • - may cause brady b/c of blocking H2, but rare.
    • - crosses placenta, breast-milk.
  146. famotidine
    • H2 Receptor Antagonist (highly selective)
    • - competitive inhibition at parietal cell H2 receptors, so reduces
    • histamine release from ECL cells and blocks direct stimulation of
    • parietal cell by histamine.
    • - suppresses basal and meal-stim'd acid secretion, each dose 50% reduction for 10 hours
    • - 2nd line for ulcers
    • - GERD, dyspepsia, stress-related ulcers (dec. incidence of bleeding)
    • - SE: diarrhea, headache, fatigue, myalgias, constip...confusion, hallucinations, agitation in ICU/elderly.
    • - may cause brady b/c of blocking H2, but rare.
    • - crosses placenta, breast-milk.
  147. omeprazole
    • proton pump inhibitor
    • - inactive, acid-labile pro-drug, lipophilic weak base, enteric coated for delayed release in duodenum
    • - upon absorption, diffuses accross lipid membranes into acidified compartments
    • - become protonated, concentrated, converted to reactive thiophilic sulfonamide cation --> non-competitive, suicide inhibitor
    • - sulfonamide forms covalent disulfide linkage with H+/K+ ATP-ase, only on active PPs.
    • - max activity of PP during meals, so give 1 hour before a meal.
    • - SE: diarrhea, headache, abdominal pain...increase risk of infection?
  148. soraprazan, revaprazan
    • potassium-competitive acid blockers (P-CABs)
    • - compete with K+ for binding site on proton pump (prevent acid from getting pumped out)
    • - fast onset, full effect with 1st dose, greater acid suppression than PPI, but still in development.
    • - for PUD
  149. sucralfate
    • mucosal protective agent
    • - sucrose X sulfated aluminum hydroxide
    • - breaks down into sucrose sulfate (-), binds to (+) proteins in base of ulcers to form physical barrier
    • - admin as slurry thru nasogastric tube to reduce stress ulcers in pts at risk from infection (spare antacids, H2As, PPIs)
    • - no systemic absorption. rare constipation
  150. erythromycin
    • macrolide antibiotic, prokinetic
    • - directly stimulates motilin receptors on GI smooth muscle, accelerates gastric emptying
    • - used for gastroparesis (slowed stomach emptying), but tolerance develops rapidly.
  151. sulfasalazine
    • azo compound, progenitor compound, for IBD
    • - 5-ASA bound to sulfapyridine, not absorbed in stomach or intestines
    • - azoreductase (bacterial enzyme) in colon converts to 5-ASA and sulfapyridine
    • - SE (caused by sulfapyridine): nausea, GI upset, headache, arthralgias, myalgias, bone marrow suppression, malaise, oligospermia
    • - slow acetylators of sulfapyridine at greater risks of ADR
    • - allergic reaction to sulfa.
  152. 5-aminosalicylic acid (5-ASA)
    • aka mesalamine, azo compound, for IBD
    • - absorbed from small intestine, but low absorption from colon.
    • - topical antiinflam. MOA not identified, but NOT blockade of COX (NSAIDs may exacerbate.)
    • - use: 1st line to treat mild-mod UC, 1st line to treat mild-mod CD in higher doses but less effective.
    • - SE: well tolerated, less side effects than sulfasalazine; high serum 5-ASA --> interstitial nephritis
    • - different formulations cause different release:
    • --mesalamine DR: release sooner, all GI tract
    • --mesalamine pH sensitive: ileum and colon
    • --Olsalazine (two 5-ASA linked by azo bond, converted into single molecules by azoreductase): colon
    • --sulfasalazine: colon
  153. glucocorticoids (prednisone, prednisoline, hydrocortisone, budesonide)
    • - used to treat IBD
    • - MOA: activate GC receptors to act on promoters of target genes and regulate their transcription
    • - antiinflammatory and immunosuppressive
    • - used for attacks of mod-severe IBD or non-responders to 5-ASA.
    • - rectal administration is prefered if disease in rectum/colon b/c of lower systemic absorption
    • - not useful to maintain remission, most patients lose response over time.
  154. infliximab
    • biological response modifier, anti-TNF-alpha therapy
    • - chimeric mouse-human monoclonal Ab to TNFa (increased levels of TNFa are associated with CD)
    • - bind to TNFa to make it impossible for binding to receptor
    • - IV infusion stays in plasma 8-12 weeks
    • -***etanercept is not effective in CD, but ok in rheumatoid arthritis
    • - used in mod-sev CD and UC, 2/3 respond, 1/3 remiss. response takes 2 weeks. 1/3 of responders lose response (ab to infliximab?) responders can be treated with repeat IV infusions q8weeks
    • - SE: infection (TB b/c supressed TH1 inflammatory response), ab against mouse portion, fever, headache, dizziness, urticaria, cardiopulmonary (chest pain, dyspnea), hypotension, SOB, muscle spasms, chest discomfort, serum sickness-like infusion rxn, mylagia, arthralgia, jaw tightness, rash, edema...

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