PHARM_MSII_RESP_DRUGS

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soren101
ID:
97156
Filename:
PHARM_MSII_RESP_DRUGS
Updated:
2011-08-30 12:11:48
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PHARMACOLOGY RESPIRATORY DRUGS
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Description:
PHARMACOLOGY RESPIRATORY DRUGS
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  1. EPINEPHRINE
    SYPATHOMIMETIC

    MOA -- Β2 > Β1 > Α

    • GIVEN S.C.
    • → RAPID ONSET OF ACTION (30 SEC)
    • ----------------------------
    • PHARM
    • § BRONCHODILATION VIA DIRECT Β2 STIM

    § VASOCONSTRICTION OF SMALL BLOOD VESSELS VIA Α STIM → DECR LOCAL CONGESTION & EDEMA

    • § CNS: INCR RR & TV → DECR CO2 IN ALVEOLI
    • ------------------------------

    THERA -- ASTHMA

    • ---------------------------------
    • ADVERSE

    S/E OF Β-AGONISTS:

    --FEWER S/E WHEN GIVEN BY INHALATION

    --MAY CAUSE PARADOXICAL BRONCHOSPASM AFTER EXCESSIVE INHALATION

    • GIVEN P.O.:
    • --CARDIAC ARRHYTHMIAS (SINUS TACHYCARDIA & PALPITATIONS)
    • --HYPERGLYCEMIA
    • --HYPOKALEMIA
    • --DIZZINESS
    • --HEADACHE
    • --NERVOUSNESS
    • --TREMOR

    **USE THESE DRUGS W/ CARE IN PTS W/ PRE-EXISTING TACHYCARDIA, HYPERTENSION, CAD, DM OR HYPERTHYROIDISM
  2. SALMETEROL
    SYPATHOMIMETIC

    • MOA -- SELECTIVE b2 > b1 AGONIST
    • -------------------------------------
    • PHARM
    • --BRONCHODILATION VIA DIRECT Β2 STIM

    --PREFERENTIALLY DILATE SMALLER & MORE PERIPHERAL AIRWAYS

    --INHB RELEASE OF INFLAMM CMPDS FR MAST CELLS

    § INHB ACCUM OF EOSINOPHILS

    § IMPROVE MUCOCILIARY TRANSPORT IN PROXIMAL & DISTAL AIRWAYS

    • § DOWN-REG OF Β2 → TOLERANCE (BUT INHALED STEROIDS REVERSE DOWN-REG)
    • -------------------------------------------

    • THERA
    • --ASTHMA

    --NEVER USE ALONE!

    --VERY SLOW ONSET OF ACTION

    --VERY LONG ACTING; BRONCHODILATION ~ 24 HR

    --STILL NEED RX W/ SHORT-ACTING Β2-AGONIST

    --DO NOT USE IN PTS W/ DETERIORATING ASTHMA

    • --NOT A SUBSTITUTE FOR CORTICOSTEROIDS
    • -------------------------------------
    • ADVERSE

    • S/E OF Β-AGONISTS:
    • --FEWER S/E WHEN GIVEN BY INHALATION

    --MAY CAUSE PARADOXICAL BRONCHOSPASM AFTER EXCESSIVE INHALATION

    • GIVEN P.O.:
    • --CARDIAC ARRHYTHMIAS (SINUS TACHYCARDIA & PALPITATIONS)
    • --HYPERGLYCEMIA
    • --HYPOKALEMIA
    • --DIZZINESS
    • --HEADACHE
    • --NERVOUSNESS
    • --TREMOR

    **USE THESE DRUGS W/ CARE IN PTS W/ PRE-EXISTING TACHYCARDIA, HYPERTENSION, CAD, DM OR HYPERTHYROIDISM
  3. TERBUTALINE
    SYPATHOMIMETIC

    • MOA -- SELECTIVE b2 > b1 AGONIST
    • -----------------------------------
    • PHARM

    § BRONCHODILATION VIA DIRECT Β2 STIM

    • § PREFERENTIALLY DILATE
    • SMALLER & MORE PERIPHERAL AIRWAYS

    § INHB RELEASE OF INFLAMM CMPDS FR MAST CELLS

    § INHB ACCUM OF EOSINOPHILS

    § IMPROVE MUCOCILIARY TRANSPORT IN PROXIMAL & DISTAL AIRWAYS

    § DOWN-REG OF Β2 → TOLERANCE

    • (BUT INHALED STEROIDS REVERSE DOWN-REG)
    • -----------------------------------
    • THERA -- ASTHMA
    • ----------------------------------

    • ADVERSE
    • S/E OF Β-AGONISTS:
    • §
    • FEWER S/E WHEN GIVEN BY INHALATION

    • §
    • MAY CAUSE PARADOXICAL
    • BRONCHOSPASM AFTER EXCESSIVE INHALATION

    • § GIVEN P.O.:
    • - CARDIAC ARRHYTHMIAS (SINUS TACHYCARDIA & PALPITATIONS)
    • -
    • HYPERGLYCEMIA
    • -
    • HYPOKALEMIA
    • -
    • DIZZINESS
    • -
    • HEADACHE
    • -
    • NERVOUSNESS
    • -
    • TREMOR

    *USE THESE DRUGS W/ CARE IN PTS W/ PRE-EXISTING TACHYCARDIA, HYPERTENSION, CAD, DM OR HYPERTHYROIDISM
  4. ALBUTEROL
    SYMPATHOMIMETIC

    • MOA -- SELECTIVE b2 > b1 AGONIST
    • -------------------------------

    • PHARM
    • § BRONCHODILATION
    • VIA DIRECT Β2 STIM

    • § PREFERENTIALLY DILATE
    • SMALLER & MORE PERIPHERAL AIRWAYS

    § INHB RELEASE OF INFLAMM CMPDS FR MAST CELLS

    § INHB ACCUM OF EOSINOPHILS

    § IMPROVE MUCOCILIARY TRANSPORT IN PROXIMAL & DISTAL AIRWAYS

    • § DOWN-REG OF Β2 → TOLERANCE
    • (BUT INHALED STEROIDS REVERSE DOWN-REG)
    • ------------------------------

    THERA

    • ASTHMA
    • R(-) ISOMER → BRONCHODILATION

    S(+) ISOMER → INACTIVE OR POSS INCR AIRWAY HYPERREACTIVITY & INFLAM RESPONSE TO ALLERGENS

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

    ADVERSE

    • S/E OF Β-AGONISTS:
    • §
    • FEWER S/E WHEN GIVEN BY INHALATION

    • §
    • MAY CAUSE PARADOXICAL
    • BRONCHOSPASM AFTER EXCESSIVE INHALATION

    • § GIVEN P.O.:
    • --CARDIAC ARRHYTHMIAS (SINUS TACHYCARDIA & PALPITATIONS)

    • --HYPERGLYCEMIA
    • -
    • HYPOKALEMIA
    • -
    • DIZZINESS
    • -
    • HEADACHE
    • -
    • NERVOUSNESS
    • -
    • TREMOR

    **USE THESE DRUGS W/ CARE IN PTS W/ PRE-EXISTING TACHYCARDIA, HYPERTENSION, CAD, DM OR HYPERTHYROIDISM
  5. BECLOMETHASONE
    CORTICOSTEROIDS (ICS = INHALED CS) -SONE -LONE -LIDE -NIDE

    MOA: PLA2 INHIBITION →

    PREVENT THE RELEASE OF ARACHIDONIC ACID

    • → INHB BOTH LT & COX PATHWAYS
    • (*SEE PHARM EFFECTS →)

    BUDESONIDE & FLUTICASONE:

    HIGH 1ST PASS METABOLISM ☺

    • DO NOT WANT SYSTEMIC STEROIDS (ESP CHILDREN) B/C S/E → DEGRADE SWALLOWED ICS SOONER THE BETTER
    • --------------------------------------

    • PHARM
    • INHB RECRUITMENT OF LEUKOCYTES & MONOCYTES/MACROPHAGES INTO AFFECT AREAS

    → ALSO PREVENT RELEASE OF AUTOCOIDS FROM THESE CELLS

    • PREVENT & REVERSE EARLY PHASE OF INFLAMM PROCESS:
    • --EDEMA
    • --FIBRIN DEPOSITION
    • --CAPILLARY DILATION
    • --MIGRATION OF LEUKOCYTES INTO INFLAMED AREA & PHAG ACTVY

    • PREVENT & REVERSE LATE PHASE OF INFLAMM PROCESS:
    • --PROLIF OF CAPILLARIES & FIBROBLASTS
    • --DEPOSITION OF COLLAGEN
    • --CICATRIZATION

    • INHB SYNTHESIS AND/OR RELEASE OF:
    • --PGS & LTS (VIA LIPOCORTIN PRODN)
    • --PAF
    • --TNF
    • --IL-1
    • --PLASMINOGEN ACTIVATOR
    • ----------------------------------------

    • THERA
    • ASTHMA: INHALATION OF STEROIDS → LESS S/E THAN SYSTEMIC ADMIN

    • IF ICS INADEQUATE, INCR DOSE ≤ 4X
    • BEFORE RESORTING TO P.O. STEROID RX

    • SYSTEMIC ADMIN = P.O. = DESCENDING
    • DOSE PACK
    • --RX ACUTE EXACERBATIONS 5-10 DAYS
    • (LITTLE TOXICITY)
    • --ADRENAL SUPPRESSION DISSIPATES W/IN 1-2 WKS
    • ----------------------------------------

    ADVERSE

    • GIVEN BY INHALATION:
    • MINOR
    • --BONE REABSORPTION
    • POSS (DOSE-DEPENDENT)

    --ADRENAL SUPPRESSION (HIGHER DOSES)

    • --PURPURA POSS (DOSE-RELATED)
    • [FOCAL HEMORRHAGE IN SKIN]

    NO → GROWTH RETARDATION, CATARACTS, OR CHO/LIPID METAB

    • MAJOR
    • --DYSPHONIA
    • --OROPHARYNGEAL CANDIDIASIS

    ~PREVENTION/LESSEN:

    • RINSE MOUTH/THROAT AFTER USE
    • & USE SPACER OR RESERVOIR DEVICE

    • GIVEN P.O.
    • --LONG TERM RX REQUIRES ALTERNATE
    • DAY THERAPY & USUAL PRECAUTIONS UPON CESSATION OF THERAPY
  6. BUDESONIDE
    CORTICOSTEROIDS (ICS = INHALED CS) -SONE -LONE -LIDE -NIDE

    MOA: PLA2 INHIBITION →

    PREVENT THE RELEASE OF ARACHIDONIC ACID

    • → INHB BOTH LT & COX PATHWAYS
    • (*SEE PHARM EFFECTS →)

    BUDESONIDE & FLUTICASONE:

    HIGH 1ST PASS METABOLISM ☺

    • DO NOT WANT SYSTEMIC STEROIDS (ESP CHILDREN) B/C S/E → DEGRADE SWALLOWED ICS SOONER THE BETTER
    • --------------------------------------

    • PHARM
    • INHB RECRUITMENT OF LEUKOCYTES & MONOCYTES/MACROPHAGES INTO AFFECT AREAS

    → ALSO PREVENT RELEASE OF AUTOCOIDS FROM THESE CELLS

    • PREVENT & REVERSE EARLY PHASE OF INFLAMM PROCESS:
    • --EDEMA
    • --FIBRIN DEPOSITION
    • --CAPILLARY DILATION
    • --MIGRATION OF LEUKOCYTES INTO INFLAMED AREA & PHAG ACTVY

    • PREVENT & REVERSE LATE PHASE OF INFLAMM PROCESS:
    • --PROLIF OF CAPILLARIES & FIBROBLASTS
    • --DEPOSITION OF COLLAGEN
    • --CICATRIZATION

    • INHB SYNTHESIS AND/OR RELEASE OF:
    • --PGS & LTS (VIA LIPOCORTIN PRODN)
    • --PAF
    • --TNF
    • --IL-1
    • --PLASMINOGEN ACTIVATOR
    • ----------------------------------------

    • THERA
    • ASTHMA: INHALATION OF STEROIDS → LESS S/E THAN SYSTEMIC ADMIN

    • IF ICS INADEQUATE, INCR DOSE ≤ 4X
    • BEFORE RESORTING TO P.O. STEROID RX

    • SYSTEMIC ADMIN = P.O. = DESCENDING
    • DOSE PACK
    • --RX ACUTE EXACERBATIONS 5-10 DAYS
    • (LITTLE TOXICITY)
    • --ADRENAL SUPPRESSION DISSIPATES W/IN 1-2 WKS
    • ----------------------------------------

    ADVERSE

    • GIVEN BY INHALATION:
    • MINOR
    • --BONE REABSORPTION
    • POSS (DOSE-DEPENDENT)

    --ADRENAL SUPPRESSION (HIGHER DOSES)

    • --PURPURA POSS (DOSE-RELATED)
    • [FOCAL HEMORRHAGE IN SKIN]

    NO → GROWTH RETARDATION, CATARACTS, OR CHO/LIPID METAB

    • MAJOR
    • --DYSPHONIA
    • --OROPHARYNGEAL CANDIDIASIS

    ~PREVENTION/LESSEN:

    • RINSE MOUTH/THROAT AFTER USE
    • & USE SPACER OR RESERVOIR DEVICE

    • GIVEN P.O.
    • --LONG TERM RX REQUIRES ALTERNATE
    • DAY THERAPY & USUAL PRECAUTIONS UPON CESSATION OF THERAPY
  7. FLUNISOLIDE
    CORTICOSTEROIDS (ICS = INHALED CS) -SONE -LONE -LIDE -NIDE

    MOA: PLA2 INHIBITION →

    PREVENT THE RELEASE OF ARACHIDONIC ACID

    • → INHB BOTH LT & COX PATHWAYS
    • (*SEE PHARM EFFECTS →)

    BUDESONIDE & FLUTICASONE:

    HIGH 1ST PASS METABOLISM ☺

    • DO NOT WANT SYSTEMIC STEROIDS (ESP CHILDREN) B/C S/E → DEGRADE SWALLOWED ICS SOONER THE BETTER
    • --------------------------------------

    • PHARM
    • INHB RECRUITMENT OF LEUKOCYTES & MONOCYTES/MACROPHAGES INTO AFFECT AREAS

    → ALSO PREVENT RELEASE OF AUTOCOIDS FROM THESE CELLS

    • PREVENT & REVERSE EARLY PHASE OF INFLAMM PROCESS:
    • --EDEMA
    • --FIBRIN DEPOSITION
    • --CAPILLARY DILATION
    • --MIGRATION OF LEUKOCYTES INTO INFLAMED AREA & PHAG ACTVY

    • PREVENT & REVERSE LATE PHASE OF INFLAMM PROCESS:
    • --PROLIF OF CAPILLARIES & FIBROBLASTS
    • --DEPOSITION OF COLLAGEN
    • --CICATRIZATION

    • INHB SYNTHESIS AND/OR RELEASE OF:
    • --PGS & LTS (VIA LIPOCORTIN PRODN)
    • --PAF
    • --TNF
    • --IL-1
    • --PLASMINOGEN ACTIVATOR
    • ----------------------------------------

    • THERA
    • ASTHMA: INHALATION OF STEROIDS → LESS S/E THAN SYSTEMIC ADMIN

    • IF ICS INADEQUATE, INCR DOSE ≤ 4X
    • BEFORE RESORTING TO P.O. STEROID RX

    • SYSTEMIC ADMIN = P.O. = DESCENDING
    • DOSE PACK
    • --RX ACUTE EXACERBATIONS 5-10 DAYS
    • (LITTLE TOXICITY)
    • --ADRENAL SUPPRESSION DISSIPATES W/IN 1-2 WKS
    • ----------------------------------------

    ADVERSE

    • GIVEN BY INHALATION:
    • MINOR
    • --BONE REABSORPTION
    • POSS (DOSE-DEPENDENT)

    --ADRENAL SUPPRESSION (HIGHER DOSES)

    • --PURPURA POSS (DOSE-RELATED)
    • [FOCAL HEMORRHAGE IN SKIN]

    NO → GROWTH RETARDATION, CATARACTS, OR CHO/LIPID METAB

    • MAJOR
    • --DYSPHONIA
    • --OROPHARYNGEAL CANDIDIASIS

    ~PREVENTION/LESSEN:

    • RINSE MOUTH/THROAT AFTER USE
    • & USE SPACER OR RESERVOIR DEVICE

    • GIVEN P.O.
    • --LONG TERM RX REQUIRES ALTERNATE
    • DAY THERAPY & USUAL PRECAUTIONS UPON CESSATION OF THERAPY
  8. FLUTICASONE
    CORTICOSTEROIDS (ICS = INHALED CS) -SONE -LONE -LIDE -NIDE

    MOA: PLA2 INHIBITION →

    PREVENT THE RELEASE OF ARACHIDONIC ACID

    • → INHB BOTH LT & COX PATHWAYS
    • (*SEE PHARM EFFECTS →)

    BUDESONIDE & FLUTICASONE:

    HIGH 1ST PASS METABOLISM ☺

    • DO NOT WANT SYSTEMIC STEROIDS (ESP CHILDREN) B/C S/E → DEGRADE SWALLOWED ICS SOONER THE BETTER
    • --------------------------------------

    • PHARM
    • INHB RECRUITMENT OF LEUKOCYTES & MONOCYTES/MACROPHAGES INTO AFFECT AREAS

    → ALSO PREVENT RELEASE OF AUTOCOIDS FROM THESE CELLS

    • PREVENT & REVERSE EARLY PHASE OF INFLAMM PROCESS:
    • --EDEMA
    • --FIBRIN DEPOSITION
    • --CAPILLARY DILATION
    • --MIGRATION OF LEUKOCYTES INTO INFLAMED AREA & PHAG ACTVY

    • PREVENT & REVERSE LATE PHASE OF INFLAMM PROCESS:
    • --PROLIF OF CAPILLARIES & FIBROBLASTS
    • --DEPOSITION OF COLLAGEN
    • --CICATRIZATION

    • INHB SYNTHESIS AND/OR RELEASE OF:
    • --PGS & LTS (VIA LIPOCORTIN PRODN)
    • --PAF
    • --TNF
    • --IL-1
    • --PLASMINOGEN ACTIVATOR
    • ----------------------------------------

    • THERA
    • ASTHMA: INHALATION OF STEROIDS → LESS S/E THAN SYSTEMIC ADMIN

    • IF ICS INADEQUATE, INCR DOSE ≤ 4X
    • BEFORE RESORTING TO P.O. STEROID RX

    • SYSTEMIC ADMIN = P.O. = DESCENDING
    • DOSE PACK
    • --RX ACUTE EXACERBATIONS 5-10 DAYS
    • (LITTLE TOXICITY)
    • --ADRENAL SUPPRESSION DISSIPATES W/IN 1-2 WKS
    • ----------------------------------------

    ADVERSE

    • GIVEN BY INHALATION:
    • MINOR
    • --BONE REABSORPTION
    • POSS (DOSE-DEPENDENT)

    --ADRENAL SUPPRESSION (HIGHER DOSES)

    • --PURPURA POSS (DOSE-RELATED)
    • [FOCAL HEMORRHAGE IN SKIN]

    NO → GROWTH RETARDATION, CATARACTS, OR CHO/LIPID METAB

    • MAJOR
    • --DYSPHONIA
    • --OROPHARYNGEAL CANDIDIASIS

    ~PREVENTION/LESSEN:

    • RINSE MOUTH/THROAT AFTER USE
    • & USE SPACER OR RESERVOIR DEVICE

    • GIVEN P.O.
    • --LONG TERM RX REQUIRES ALTERNATE
    • DAY THERAPY & USUAL PRECAUTIONS UPON CESSATION OF THERAPY
  9. IPRATROPIUM
    MUSCARAINIC ANTAGONIST (4O)

    MOA -- MUSCARINIC BLOCKADE IN SMOOTH MUSCLE OF LARGE & SMALL AIRWAYS →

    --PREVENTS (CN X) VAGAL-MEDIATED BRONCHOCONSTRICTION & BRONCHIAL SECRETIONS

    • --------------------------------------------
    • PHARM

    4* → POORLY LIPID-SOLB.

    • DOES NOT ENTER CNS OR CROSS
    • PLACENTA.

    IPRA: BRONCHODILATION W/IN 10 MIN OF INHALATION, PEAKS 1-2 HRS & PERSISTS 4-8 HRS

    • TIO:
    • --BRONCHODILATION W/IN 30 MIN OF INHALATION, PEAKS 1.5-3 HRS & PERSISTS ~24 HRS

    --DILATES LARGE & SMALL AIRWAYS

    --NO EFFECT ON PULMONARY GAS EXCHANGE OR ARTERIAL PO2

    • **NO: ANTIHISTAMINE,
    • ANTI-INFLAMM OR MAST CELL DEGRANULATION INHIBITION
    • --------------------------------

    THERA

    **DOC: COPD

    --PROPHYLAXIS: PREVENT ATTACKS IN PTS W/ EITHER A POOR RESPONSE TO/INTOLERANCE OF Β2-AGONISTS

    --Pt RESPONSE IS HIGHLY VARIABLE BUT DRUG TOLERANCE DOES NOT DEVELOP

    • --AFTER IPRA INCR FEV1 → Β2-AGONIST
    • FURTHER INCR FEV1

    • --3RD LINE IN ASTHMA
    • 1ST: ICS/ABLUTEROL
    • 2ND: ICS/ALBUTEROL + SALMETEROL
    • -------------------------------------

    • ADVERSE
    • --DRY MOUTH
    • --BITTER TASTE

    • USE W/ CAUTION FOR PT W/:
    • --ANGLE-CLOSURE GLAUCOMA
    • --GI OR GU OBSTRUCTION
    • --PROSTATIC HYPERTROPHY
  10. TIOTROPIUM
    MUSCARAINIC ANTAGONIST (4O)

    MOA -- MUSCARINIC BLOCKADE IN SMOOTH MUSCLE OF LARGE & SMALL AIRWAYS →

    --PREVENTS (CN X) VAGAL-MEDIATED BRONCHOCONSTRICTION & BRONCHIAL SECRETIONS

    • --------------------------------------------
    • PHARM

    4* → POORLY LIPID-SOLB.

    • DOES NOT ENTER CNS OR CROSS
    • PLACENTA.

    IPRA: BRONCHODILATION W/IN 10 MIN OF INHALATION, PEAKS 1-2 HRS & PERSISTS 4-8 HRS

    • TIO:
    • --BRONCHODILATION W/IN 30 MIN OF INHALATION, PEAKS 1.5-3 HRS & PERSISTS ~24 HRS

    --DILATES LARGE & SMALL AIRWAYS

    --NO EFFECT ON PULMONARY GAS EXCHANGE OR ARTERIAL PO2

    • **NO: ANTIHISTAMINE,
    • ANTI-INFLAMM OR MAST CELL DEGRANULATION INHIBITION
    • --------------------------------

    THERA

    **DOC: COPD

    --PROPHYLAXIS: PREVENT ATTACKS IN PTS W/ EITHER A POOR RESPONSE TO/INTOLERANCE OF Β2-AGONISTS

    --Pt RESPONSE IS HIGHLY VARIABLE BUT DRUG TOLERANCE DOES NOT DEVELOP

    • --AFTER IPRA INCR FEV1 → Β2-AGONIST
    • FURTHER INCR FEV1

    • --3RD LINE IN ASTHMA
    • 1ST: ICS/ABLUTEROL
    • 2ND: ICS/ALBUTEROL + SALMETEROL
    • -------------------------------------

    • ADVERSE
    • --DRY MOUTH
    • --BITTER TASTE

    • USE W/ CAUTION FOR PT W/:
    • --ANGLE-CLOSURE GLAUCOMA
    • --GI OR GU OBSTRUCTION
    • --PROSTATIC HYPERTROPHY
  11. ZAFIRLUKAST
    LEUKOTRIENE (LT) ANTAGONISTS

    • MOA
    • COMPETITIVE ANTAGONISTS OF LTC4 & LTD4 RECEPTORS

    (LTC4 & LTD4 = ACTIVE CMPDS IN SRS-A, ANAPHYLAXIS)

    • PULMONARY TOXICITY OF LT:
    • 1. BRONCHOCONSTRICTION
    • 2. INC MUCUS PRODUCTION
    • 3. INC VASCULAR PERMIABILITY
    • 4. EOS/NEUTRO CHEMOTAXIS
    • 5. INCR LEUKOCYTE ADHESION
    • ------------------------------------

    PHARM

    --DECR LATE BRONCHOCONSTRICTION CAUSED BY CHALLENGES W/ ALLERGENS

    --MAX EFFECT ~1 WK AFTER

    THERAPY → DEC NEED FOR RESCUE W/ Β2-AGONIST (ALBUTEROL)

    • USED AS ALTERNATIVE TO LOW-DOSE CORTICOSTEROIDS OR CROMOLYN
    • SODIUM
    • -------------------------------------------

    THERA

    ASTHMA

    ** INC FEV1, DEC SYMP OF ASTHMA & USE OF BETA2 AGONISTS & CORTICOSTERs

    USED IN TREATMENT OF MILD/MOD ASTHMA

    • PREVENTS ASPIRIN INDUCED ASTHMA
    • ------------------------------------

    ADVERSE

    HEADACHE

    • * INHIBITING CYP450 → CAN INCR
    • PLASMA CONC OF OTHER DRUGS

    HEADACHES
  12. CROMOLYN SODIUM
    (NASALCROM)
    INHIBITORS OF MAST CELL DEGRANULATION

    MOA

    • AVAILABLE AS:
    • --POWDER IN CAPSULES FOR INHALATION
    • --POWDER IN AEROSOL, NASAL SPRAY, OPHTHALMIC DRUGS

    MUST BE USE PROPHYLACTICALLY! (10-15 MIN BEFORE ALLERGEN EXPOSURE)

    • PROPHYLAXIS: PREVENTS IMMED & DELAYED AG-INDUCED DEGRANULATION OF MAST CELLS
    • ------------

    • PREVENTS THE INCR IN INTRACELLULAR
    • CA2+ CONC (INDUCED BY THE FORMATION OF IGE-AG BRIDGES ON THE CELL SURFACE)

    → PREVENTS RELEASE OF CHEMICAL MEDIATORS FROM MAST CELLS

    • DOES NOT AFFECT:
    • --BINDING OF IGE TO MAST CELLS
    • --BINDING OF AG TO IGE ON SURFACE OF MAST CELL
    • --BASAL TONE OF BRONCHIAL SM MUSC
    • --BRONCHOCONSTRICTION CAUSE BY ACH, LTS, & HISTAMINE

    • NO DIRECT ANTI-HISTAMINE OR ANTI-INFLAMM EFFECTS
    • -------------------------------------------

    PHARM

    • LIPID-SOLB BUT →
    • ONLY 10% ABSORBED FROM LUNGS & GI TRACT!

    • --REDUCES FREQ & SEVERITY OF BRONCHOSPASM
    • --BENEFITS MAY TAKE 3-4 WKS TO DEVELOP

    • --PREVENT BRONCHIAL DAMAGE CAUSED BY THE MAST CELL PRODUCTS → LONG-TERM RX CAN REDUCE OVERALL BRONCHIAL REACTIVITY TO HISTAMINE & LTS
    • ------------------------------------------

    THERA

    ASTHMA

    REDUCE FREQ & SEVERITY OF BRONCHOSPASM

    • PREVENT BRONCHIAL DAMAGE BY MAST CELL PRODUCTS (HISTAMINE & LTS)
    • ----------------------------------------

    ADVERSE

    NO CONTRAINDICATIONS

    USE AEROSOL W/ CARE IN PTS W/ CARDIAC ARRHYTHMIAS OR CAD:

    • HYDROCARBON PROPELLANTS CAN
    • ELICIT ADVERSE CARDIAC EFFECTS

    • LONG-TERM RX:
    • --FEW ADVERSE EFFECTS

    • MAY CAUSE:
    • --THROAT IRRITATION
    • --COUGH
    • --DRY MOUTH
    • --WHEEZING
  13. THEOPHYLLINE
    P.O.
    PHOSPHODIESTERASE (PDEASE) INHIBITORS

    • MOA
    • --INHB PDEASE WHICH DEGRADES CAMP

    --A SPECIFIC ADENOSINE RECEPTOR ANTAGONIST

    ELIMINATED BY HEPATIC METAB.

    T1/2 DEC IN CIGARETTE SMOKERS.

    CROSSES PLACENTA.

    SECRETED IN MILK: USUALLY NO EFFECT ON NURSING CHILDREN, BUT POSS IRRITABILITY/EXCITATION.

    IN OTC ASTHMA REMEDIES

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

    PHARM

    • LUNGS:
    • --RELAX SM MUSC →DILATES LG & PERIPH AIRWAYS

    --INCR CONTRACTION OF DIAPHRAGM & ACCESS RESPIRATORY MUSC → IMPROVES VENTILATION

    --DOSE-RELATED INCR IN FEV1 & FVC

    --TOLERANCE DOES NOT DEVELOP

    • MAST CELL:
    • --INHB DEGRANULATION IN RESPIRATORY TRACT → PREVENTS HISTAMINE RELEASE & LT SYNTH

    • CNS:
    • --INCR CO2 SENSITIVITY @ MEDULLARY RESPIRATORY CENTERS → INCR VENTILATION

    --CAUSES CENTRAL STIMULATION

    • HEART & BLOOD VESSELS:
    • --SLIGHT DECR TPR W/ INCR HR & INCR DP/DT → TRANSIENT RISE IN CO & ORGAN PERFUSION

    --DECR CVP & PRELOAD

    --DIRECT EFFECT ADRENAL GLAND → INCR PLASMA EPI (POSS REASON FOR INCR HR & INCR DP/DT)

    --CEREBRAL VASOCONSTRICTION (POSS VIA NE RELEASE)

    • KIDNEY:
    • --DECR FILTRATION FRACTION → TRANSIENT DIURESIS W/ A WEAK NATRIURESIS

    • GI TRACT:
    • --INCR GASTRIC ACID SECRETION

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

    THERA -- ASTHMA

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

    ADVERSE

    --NO WARNING: SERIOUS TOXICITY NOT ALWAYS PRECEDED BY LESS SEVERE S/E

    --CAREFUL DOSE TITRATION OF THEO NECESS TO MAXIMIZE BENEFITS & MINIMIZE S/E

    • --CONTRAINDICATED IN PTS W/ ACTIVE
    • ULCER DISEASE

    • USE W/ CARE IN PRESENCE OF:
    • --CAD OR RECENT MI (TACHYCARDIA & INCR DP/DT)
    • --CHF
    • --HEPATIC DISEASE (DECR METAB)

    • CNS EFFECTS:
    • --RESTLESSNESS
    • --NERVOUSNESS
    • --EXCITATION
    • --HEADACHE
    • --INSOMNIA
    • --TREMOR
    • --SEIZURES (40+ MG/L; CTRL W/ DIAZEPAM)

    • CARDIOVASCULAR:
    • --RAPID I.V. INJECTION → HT & CARDIAC ARRHYTHMIAS

    • GI TRACT:
    • --GI DISCOMFORT (COMMON)
    • --NAUSEA (COMMON)
    • --HIGHLY ALKALINE → DIRECT GASTRIC IRRITATION
    • --ACTION IN CHEMORECEPTOR TRIGGER ZONE → EMESIS WHEN PLASMA CONC = 15+ MG/L

    • *DRUG INTERACTIONS:
    • --CIMETIDINE, DILTIAZEM, ERYTHROMYCIN, VERAPAMIL & OCPS BLOCK HEPATIC METAB → INC PLASMA THEO
  14. AMINOPHYLLINE
    I.V.
    (86% THEOPHYLLINE)
    MORE WATER SOLB
    PHOSPHODIESTERASE (PDEASE) INHIBITORS

    • MOA
    • --INHB PDEASE WHICH DEGRADES CAMP

    --A SPECIFIC ADENOSINE RECEPTOR ANTAGONIST

    ELIMINATED BY HEPATIC METAB.

    T1/2 DEC IN CIGARETTE SMOKERS.

    CROSSES PLACENTA.

    SECRETED IN MILK: USUALLY NO EFFECT ON NURSING CHILDREN, BUT POSS IRRITABILITY/EXCITATION.

    IN OTC ASTHMA REMEDIES

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

    PHARM

    • LUNGS:
    • --RELAX SM MUSC →DILATES LG & PERIPH AIRWAYS

    --INCR CONTRACTION OF DIAPHRAGM & ACCESS RESPIRATORY MUSC → IMPROVES VENTILATION

    --DOSE-RELATED INCR IN FEV1 & FVC

    --TOLERANCE DOES NOT DEVELOP

    • MAST CELL:
    • --INHB DEGRANULATION IN RESPIRATORY TRACT → PREVENTS HISTAMINE RELEASE & LT SYNTH

    • CNS:
    • --INCR CO2 SENSITIVITY @ MEDULLARY RESPIRATORY CENTERS → INCR VENTILATION

    --CAUSES CENTRAL STIMULATION

    • HEART & BLOOD VESSELS:
    • --SLIGHT DECR TPR W/ INCR HR & INCR DP/DT → TRANSIENT RISE IN CO & ORGAN PERFUSION

    --DECR CVP & PRELOAD

    --DIRECT EFFECT ADRENAL GLAND → INCR PLASMA EPI (POSS REASON FOR INCR HR & INCR DP/DT)

    --CEREBRAL VASOCONSTRICTION (POSS VIA NE RELEASE)

    • KIDNEY:
    • --DECR FILTRATION FRACTION → TRANSIENT DIURESIS W/ A WEAK NATRIURESIS

    • GI TRACT:
    • --INCR GASTRIC ACID SECRETION

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

    THERA -- ASTHMA

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

    ADVERSE

    --NO WARNING: SERIOUS TOXICITY NOT ALWAYS PRECEDED BY LESS SEVERE S/E

    --CAREFUL DOSE TITRATION OF THEO NECESS TO MAXIMIZE BENEFITS & MINIMIZE S/E

    • --CONTRAINDICATED IN PTS W/ ACTIVE
    • ULCER DISEASE

    • USE W/ CARE IN PRESENCE OF:
    • --CAD OR RECENT MI (TACHYCARDIA & INCR DP/DT)
    • --CHF
    • --HEPATIC DISEASE (DECR METAB)

    • CNS EFFECTS:
    • --RESTLESSNESS
    • --NERVOUSNESS
    • --EXCITATION
    • --HEADACHE
    • --INSOMNIA
    • --TREMOR
    • --SEIZURES (40+ MG/L; CTRL W/ DIAZEPAM)

    • CARDIOVASCULAR:
    • --RAPID I.V. INJECTION → HT & CARDIAC ARRHYTHMIAS

    • GI TRACT:
    • --GI DISCOMFORT (COMMON)
    • --NAUSEA (COMMON)
    • --HIGHLY ALKALINE → DIRECT GASTRIC IRRITATION
    • --ACTION IN CHEMORECEPTOR TRIGGER ZONE → EMESIS WHEN PLASMA CONC = 15+ MG/L

    • *DRUG INTERACTIONS:
    • --CIMETIDINE, DILTIAZEM, ERYTHROMYCIN, VERAPAMIL & OCPS BLOCK HEPATIC METAB → INC PLASMA THEO
  15. AMINOPHYLLINE
    TREATMENT OF CHEYNE-STOKES BREATHING & NEONATAL APNEA

    MOA

    --INHB PDEASE WHICH DEGRADES CAMP

    --A SPECIFIC ADENOSINE RECEPTOR ANTAGONIST

    ELIMINATED BY HEPATIC METAB.

    T1/2 DECR IN CIGARETTE SMOKERS.

    CROSSES PLACENTA.

    SECRETED IN MILK:

    • USUALLY NO EFFECT ON NURSING
    • CHILDREN, BUT POSS IRRITABILITY/EXCITATION.

    • IN OTC ASTHMA REMEDIES
    • ---------------------------------------

    THERA

    • GIVEN I.V.:
    • --NORMALIZES RESPIRATION IN PTS W/ CHEYNE-STOKES.

    --INC RR & IMPROVES BLOOD GASES IN PRE-TERM INFANTS W/ INTERMITTENT APNEA.
  16. CAFFEINE
    TREATMENT OF CHEYNE-STOKES BREATHING & NEONATAL APNEA

    FOR CHEYNE-STOKES -- USE AMINOPHYLLINE


    MOA

    --INHB PDEASE WHICH DEGRADES CAMP

    --A SPECIFIC ADENOSINE RECEPTOR ANTAGONIST

    ELIMINATED BY HEPATIC METAB.

    T1/2 DECR IN CIGARETTE SMOKERS.

    CROSSES PLACENTA.

    SECRETED IN MILK:

    • USUALLY NO EFFECT ON NURSING
    • CHILDREN, BUT POSS IRRITABILITY/EXCITATION.

    • IN OTC ASTHMA REMEDIES
    • ---------------------------------------

    THERA

    • GIVEN I.V.:
    • --INCR RR & IMPROVES BLOOD GASES IN PRE-TERM INFANTS W/ INTERMITTENT APNEA.
  17. NITRIC OXIDE (NO)
    (INOMAX)
    TREATMENT OF HYPOXIC RESPIRATORY FAILURE

    ASSOCIATED W/ SIGNS & SYMPTOMS OF PULMONARY HTN DUE TO INCR PULMONARY VASCULAR RESISTANCE.

    MOA

    • NO RELAXES SMOOTH MUSCLE
    • ----------------------------------------

    PHARM

    • GIVEN INHILATION
    • --DEC PULM VASC RESISTANCE --> IMPROVES PULM PERF
    • ----------------------------------------

    THERA

    NEONATAL HYPOXIC RESPIRATORY FAILURE
  18. CORTISONE
    P.O. & PARENTERAL
    ANTI-INFLAMMATORY DRUGS: CORTICOSTEROIDS

    MOA

    • --ACTIVATE GENE EXPRESSION FOR A PROTEIN (LIPOCORTIN)
    • → INHB PHOSPHOLIPASE A2
    • → BLOCK RELEASE OF ARACHIDONIC ACID

    BLOCK SYNTH OF ALL EICOSANOIDS (PGS & LTS)

    • BLOCK EXPRESSION OF GENES WHICH CODE FOR MANY INFLAM CMPNDS
    • --COX-2
    • --PLA2
    • --CYTOKINES
    • --ADHESION MOLECULES
    • --INDUCIBLE NITRIC OXIDE SYNTHASE (INOS)
    • -------------------------------------------

    THERA

    • *ALLERGIC RXNS
    • *ARTHRITIS
    • *ASTHMA
    • *NEPHRITIC SYNDROME

    (SEE INHALED CORTICOSTEROIDS)

    ASTHMA: INHALATION OF STEROIDS → LESS S/E THAN SYSTEMIC ADMIN

    • IF ICS INADEQUATE, INCR DOSE ≤ 4X
    • BEFORE RESORTING TO P.O. STEROID RX

    • SYSTEMIC ADMIN = P.O. = DESCENDING
    • DOSE PACK:
    • --RX ACUTE EXACERBATIONS 5-10 DAYS
    • (LITTLE TOXICITY)

    • ADRENAL SUPPRESSION DISSIPATES W/IN 1-2 WKS
    • --------------------------------------------------

    ADVERSE

    1. DIABETES & CHANGES IN CHO METABOLISM

    2. INFECTION PRONE & POOR WOUND HEALING

    3. OSTEOPOROSIS

    (SEE INHALED CORTICOSTEROIDS)

    • GIVEN BY INHALATION:
    • MINOR
    • --BONE REABSORPTION POSS (DOSE-DEPENDENT)
    • --ADRENAL SUPPRESSION (HIGHER DOSES)
    • --PURPURA POSS (DOSE-RELATED)
    • [FOCAL HEMORRHAGE IN SKIN]

    • NO → GROWTH RETARDATION,
    • CATARACTS, OR CHO/LIPID METAB

    • MAJOR
    • --DYSPHONIA
    • --OROPHARYNGEAL CANDIDIASIS

    • PREVENTION/LESSEN:
    • --RINSE MOUTH/THROAT AFTER USE
    • & USE SPACER OR RESERVOIR DEVICE

    • GIVEN P.O.
    • --LONG TERM RX REQUIRES ALTERNATE DAY THERAPY & USUAL PRECAUTIONS UPON CESSATION OF THERAPY
  19. HYDROCORTISONE
    P.O. & PARENTERAL
    ANTI-INFLAMMATORY DRUGS: CORTICOSTEROIDS

    MOA

    • --ACTIVATE GENE EXPRESSION FOR A PROTEIN (LIPOCORTIN)
    • → INHB PHOSPHOLIPASE A2
    • → BLOCK RELEASE OF ARACHIDONIC ACID

    BLOCK SYNTH OF ALL EICOSANOIDS (PGS & LTS)

    • BLOCK EXPRESSION OF GENES WHICH CODE FOR MANY INFLAM CMPNDS
    • --COX-2
    • --PLA2
    • --CYTOKINES
    • --ADHESION MOLECULES
    • --INDUCIBLE NITRIC OXIDE SYNTHASE (INOS)
    • -------------------------------------------

    THERA

    • *ALLERGIC RXNS
    • *ARTHRITIS
    • *ASTHMA
    • *NEPHRITIC SYNDROME

    (SEE INHALED CORTICOSTEROIDS)

    ASTHMA: INHALATION OF STEROIDS → LESS S/E THAN SYSTEMIC ADMIN

    • IF ICS INADEQUATE, INCR DOSE ≤ 4X
    • BEFORE RESORTING TO P.O. STEROID RX

    • SYSTEMIC ADMIN = P.O. = DESCENDING
    • DOSE PACK:
    • --RX ACUTE EXACERBATIONS 5-10 DAYS
    • (LITTLE TOXICITY)

    • ADRENAL SUPPRESSION DISSIPATES W/IN 1-2 WKS
    • --------------------------------------------------

    ADVERSE

    1. DIABETES & CHANGES IN CHO METABOLISM

    2. INFECTION PRONE & POOR WOUND HEALING

    3. OSTEOPOROSIS

    (SEE INHALED CORTICOSTEROIDS)

    • GIVEN BY INHALATION:
    • MINOR
    • --BONE REABSORPTION POSS (DOSE-DEPENDENT)
    • --ADRENAL SUPPRESSION (HIGHER DOSES)
    • --PURPURA POSS (DOSE-RELATED)
    • [FOCAL HEMORRHAGE IN SKIN]

    • NO → GROWTH RETARDATION,
    • CATARACTS, OR CHO/LIPID METAB

    • MAJOR
    • --DYSPHONIA
    • --OROPHARYNGEAL CANDIDIASIS

    • PREVENTION/LESSEN:
    • --RINSE MOUTH/THROAT AFTER USE
    • & USE SPACER OR RESERVOIR DEVICE

    • GIVEN P.O.
    • --LONG TERM RX REQUIRES ALTERNATE DAY THERAPY & USUAL PRECAUTIONS UPON CESSATION OF THERAPY
  20. PREDNISONE
    P.O. & PERENTERAL
    ANTI-INFLAMMATORY DRUGS: CORTICOSTEROIDS

    MOA

    • --ACTIVATE GENE EXPRESSION FOR A PROTEIN (LIPOCORTIN)
    • → INHB PHOSPHOLIPASE A2
    • → BLOCK RELEASE OF ARACHIDONIC ACID

    BLOCK SYNTH OF ALL EICOSANOIDS (PGS & LTS)

    • BLOCK EXPRESSION OF GENES WHICH CODE FOR MANY INFLAM CMPNDS
    • --COX-2
    • --PLA2
    • --CYTOKINES
    • --ADHESION MOLECULES
    • --INDUCIBLE NITRIC OXIDE SYNTHASE (INOS)
    • -------------------------------------------

    THERA

    • *ALLERGIC RXNS
    • *ARTHRITIS
    • *ASTHMA
    • *NEPHRITIC SYNDROME

    (SEE INHALED CORTICOSTEROIDS)

    ASTHMA: INHALATION OF STEROIDS → LESS S/E THAN SYSTEMIC ADMIN

    IF ICS INADEQUATE, INCR DOSE ≤ 4XBEFORE RESORTING TO P.O. STEROID RX

    • SYSTEMIC ADMIN = P.O. = DESCENDINGDOSE PACK:
    • --RX ACUTE EXACERBATIONS 5-10 DAYS (LITTLE TOXICITY)

    ADRENAL SUPPRESSION DISSIPATES W/IN 1-2 WKS

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

    • ADVERSE
    • 1. DIABETES & CHANGES IN CHO METABOLISM

    2. INFECTION PRONE & POOR WOUND HEALING

    3. OSTEOPOROSIS

    (SEE INHALED CORTICOSTEROIDS)

    • GIVEN BY INHALATION:
    • MINOR
    • --BONE REABSORPTION POSS (DOSE-DEPENDENT)
    • --ADRENAL SUPPRESSION (HIGHER DOSES)
    • --PURPURA POSS (DOSE-RELATED)
    • [FOCAL HEMORRHAGE IN SKIN]

    NO → GROWTH RETARDATION,CATARACTS, OR CHO/LIPID METAB

    • MAJOR
    • --DYSPHONIA
    • --OROPHARYNGEAL CANDIDIASIS

    • PREVENTION/LESSEN:
    • --RINSE MOUTH/THROAT AFTER USE& USE SPACER OR RESERVOIR DEVICE

    • GIVEN P.O.
    • --LONG TERM RX REQUIRES ALTERNATE DAY THERAPY & USUAL PRECAUTIONS UPON CESSATION OF THERAPY
  21. FLUNISOLIDE
    AEROSOL
    ANTI-INFLAMMATORY DRUGS: CORTICOSTEROIDS

    SAME AS CORTISONE
  22. COX-1
    PGH SYNTHETASE I

    • CONSTITUTIVE “HOUSE-KEEPING” ENZYME,
    • ESP STOMACH & KIDNEY

    ACTIVITY CAN BE INDUCED 2-4X

    · VASCULAR ENDOTHELIUM/SMOOTH MUSCLE

    · STOMACH

    · KIDNEY

    · PLATELETS -- TXA2

    • INHIBITED BY:
    • --ASPIRIN (1&2 irrev)
    • --SALICYLATE (1&2 rev
    • --IBUPROFEN (1&2 rev

    • --INDOMETHACIN (1 rev)
    • --SULINDAC (1 rev)
  23. COX 2
    PGH SYNTHETASE II

    AN EARLY INDUCIBLE ENZYME IN THE INFLAMMATORY RESPONSE

    (CONSTITUTIVE: LUNGS & KIDNEY)

    ACTIVITY CAN BE INDUCED 10-20X

    • ·
    • INFLAMMATORY CELLS (I.E., MACROPHAGES)

    “2 HOT TO HANDLE”

    • INHIBITED BY NONSELECTIVE:
    • --ASPIRIN (irrev)
    • --SALICYLATE (rev)
    • --IBUPROFEN (rev)
    • --GLUCOCORTs

    • SELECTIVE 2 INH:
    • --CELEXCOXIB
  24. ASPRIN SENSITIVITY
    NOT TRUE ANAPHYLACTIC RXN B/C NO MAST CELL DEGRANULATION

    W/IN ~ 3 HR OF I.V. INJECTION

    NSAIDS INHB PG SYNTHETASE → SHUNT: INCR LT SYNTH → SYMPTOMS

    LT INHIBITORS (ZAFIR & MONTE) PREVENT SHUNTING

    • SYMPTOMS:
    • --RHINOCONJUNCTIVITIS
    • --ANGIOEDEMA
    • --URTICARIA

    NASAL POLYPS (→ INCR LT PROD) & ADULT ONSET ASTHMA

    SENSTV TO ONE → SENSTV TO ALL NSAIDS!

    RX W/ ACETAMINOPHEN INSTEAD (ANTI-PYRETIC & ANALGESIC; NOT ANTI-INFLAM)
  25. PGs IN PREGNANCY
    INCR PGS IN AMNIOTIC FLUID AT TERM

    → INCR NORMAL RHYTHMIC CONTRACTION THAT CAUSE CHILD BIRTH
  26. STOMACH PGs
    STOMACH PROD PGE’S

    • MAINTAIN INTEGRITY OF THE MUCOSA BY:
    • --INHB SECRETION OF HCL

    --STIM SECRETION OF BICARB

    --STIM SECRETION OF MUCUS

    --INCR MUCOSAL BLOOD FLOW

    --STIM CELL GROWTH & REPAIR
  27. ASPRIN
    ACETYLSALICYCLIC ACID

    NSAID

    MOA

    *IRREV INHB COX-1 & COX-2 BY ACETYLATION OF THE ACTIVE SITE

    • ACETYLATION OCCURS IN PORTAL CIRC B/C ASPIRIN CONVERTED TO SALICYLATE BY 1ST PASS METAB
    • ---------------------------------

    PHARM

    • PLATELETS CANNOT SYNTH NEW PROT → INHB COX-1 FOR LIFE OF PLATELET (9-14
    • DAYS)

    PREVENTS IL-1 FROM STIM PGE2 SYNTH --> PGE2 INCR THE THERMOREGULATORY SET-POINT --> FEVER

    --PREVENTS PG’S FROM SENSITIZING SENSORY PAIN FIBERS

    PREVENTS PROD OF TXA2 WHICH IS PROD BY PLATELETS & MONOCYTES & STRONGLY ENHANCES PLATELET AGGREGATION

    • IRREV INH OF COX-1 VIA ACETYLATION OCCURS IN THE PORTAL CIRC
    • --------------------------------------

    THERA

    “BABY ASPIRIN” (80-325 MG/DAY) PREVENTS CYCLICAL ISCHEMIA BY PLATELET CLOTS (UNSTABLE ANGINA)

    DECR MI & 2O MI

    DECR STROKE/DEATH IN ♂ W/ TIAS OR CHRONIC ATRIAL FIB

    • DECR FREQ OF TIA
    • --------------------------------------

    ADVERSE

    ASPIRIN-SENSITIVITY

    DECR RENAL FUNCTION

    NA/H2O RETENTION

    HYPERKALEMIA

    INTERSTITIAL NEPHRITIS

    REV. ACUTE RENAL FAILURE (ARF)

    GI ULCERATION & BLEEDING

    • PT AT GREATEST RISK:
    • -- >60 Y.O.
    • --TAKING CORTICOSTEROIDS
    • --PRIOR HX OF GI ULCERATION

    MISOPROSTOL (PGE1 STABLE ANALOG) RX GASTRIC EROSION & ULCERATION CAUSED BY NSAIDS & CORTICOSTEROIDS.

    DEC RATE OF HEALING FRACTURED BONES

    • *INDOMETHACIN (PRE-TERM INFANTS)
    • RENAL DYSFUNC & BLEEDING
  28. SALICYLATE
    NSAID

    MOA

    • *REV INHB COX-1 & COX-2
    • ---------------------------------

    PHARM

    • PLATELETS CANNOT SYNTH NEW PROT → INHB COX-1 FOR LIFE OF PLATELET (9-14
    • DAYS)

    PREVENTS IL-1 FROM STIM PGE2 SYNTH --> PGE2 INCR THE THERMOREGULATORY SET-POINT --> FEVER

    --PREVENTS PG’S FROM SENSITIZING SENSORY PAIN FIBERS

    PREVENTS PROD OF TXA2 WHICH IS PROD BY PLATELETS & MONOCYTES & STRONGLY ENHANCES PLATELET AGGREGATION

    • IRREV INH OF COX-1 VIA ACETYLATION OCCURS IN THE PORTAL CIRC
    • --------------------------------------

    ADVERSE

    ASPIRIN-SENSITIVITY

    DECR RENAL FUNCTION

    NA/H2O RETENTION

    HYPERKALEMIA

    INTERSTITIAL NEPHRITIS

    REV. ACUTE RENAL FAILURE (ARF)

    GI ULCERATION & BLEEDING

    • PT AT GREATEST RISK:
    • -- >60 Y.O.
    • --TAKING CORTICOSTEROIDS
    • --PRIOR HX OF GI ULCERATION

    MISOPROSTOL (PGE1 STABLE ANALOG) RX GASTRIC EROSION & ULCERATION CAUSED BY NSAIDS & CORTICOSTEROIDS.

    DEC RATE OF HEALING FRACTURED BONES

    • *INDOMETHACIN (PRE-TERM INFANTS)
    • RENAL DYSFUNC & BLEEDING
  29. IBUPROPHEN
    NSAID

    MOA

    • *EQUAL REV INHB COX-1 & COX-2
    • --------------------------------

    PHARM

    • PLATELETS CANNOT SYNTH NEW PROT → INHB COX-1 FOR LIFE OF PLATELET (9-14
    • DAYS)

    PREVENTS IL-1 FROM STIM PGE2 SYNTH --> PGE2 INCR THE THERMOREGULATORY SET-POINT --> FEVER

    --PREVENTS PG’S FROM SENSITIZING SENSORY PAIN FIBERS

    PREVENTS PROD OF TXA2 WHICH IS PROD BY PLATELETS & MONOCYTES & STRONGLY ENHANCES PLATELET AGGREGATION

    • IRREV INH OF COX-1 VIA ACETYLATION OCCURS IN THE PORTAL CIRC
    • --------------------------------------

    THERA

    • PREVENT REV Sx OF 1* DYSMENORRHEA
    • --------------------------------------

    ADVERSE

    ASPIRIN-SENSITIVITY

    DECR RENAL FUNCTION

    NA/H2O RETENTION

    HYPERKALEMIA

    INTERSTITIAL NEPHRITIS

    REV. ACUTE RENAL FAILURE (ARF)

    GI ULCERATION & BLEEDING

    • PT AT GREATEST RISK:
    • -- >60 Y.O.
    • --TAKING CORTICOSTEROIDS
    • --PRIOR HX OF GI ULCERATION

    MISOPROSTOL (PGE1 STABLE ANALOG) RX GASTRIC EROSION & ULCERATION CAUSED BY NSAIDS & CORTICOSTEROIDS.

    DEC RATE OF HEALING FRACTURED BONES

    • *INDOMETHACIN (PRE-TERM INFANTS)
    • RENAL DYSFUNC & BLEEDING
  30. INDOMETHACIN
    NSAID

    MOA

    • *RELATIVELY SELECTIVE COX-1 INH
    • ---------------------------------

    PHARM

    • PLATELETS CANNOT SYNTH NEW PROT → INHB COX-1 FOR LIFE OF PLATELET (9-14
    • DAYS)

    PREVENTS IL-1 FROM STIM PGE2 SYNTH --> PGE2 INCR THE THERMOREGULATORY SET-POINT --> FEVER

    --PREVENTS PG’S FROM SENSITIZING SENSORY PAIN FIBERS

    PREVENTS PROD OF TXA2 WHICH IS PROD BY PLATELETS & MONOCYTES & STRONGLY ENHANCES PLATELET AGGREGATION

    • IRREV INH OF COX-1 VIA ACETYLATION OCCURS IN THE PORTAL CIRC
    • --------------------------------------

    THERA

    • GIVEN IV
    • --INH PREMATURE LABOR
    • --CLOSE Pt DUCTUS ART IN PRE-TERM INFANT (WHEN DIURETICS, DIFITALIS & RESP SUPPORT DONT WORK

    • S/E
    • --RENAL DYSFUNC
    • --BLEEDING
    • --------------------------------------

    ADVERSE

    ASPIRIN-SENSITIVITY

    DECR RENAL FUNCTION

    NA/H2O RETENTION

    HYPERKALEMIA

    INTERSTITIAL NEPHRITIS

    REV. ACUTE RENAL FAILURE (ARF)

    GI ULCERATION & BLEEDING

    • PT AT GREATEST RISK:
    • -- >60 Y.O.
    • --TAKING CORTICOSTEROIDS
    • --PRIOR HX OF GI ULCERATION

    MISOPROSTOL (PGE1 STABLE ANALOG) RX GASTRIC EROSION & ULCERATION CAUSED BY NSAIDS & CORTICOSTEROIDS.

    DEC RATE OF HEALING FRACTURED BONES

    • *INDOMETHACIN (PRE-TERM INFANTS)
    • RENAL DYSFUNC & BLEEDING
  31. CELECOXIB
    NSAID

    MOA

    • *SELECTIVE REV COX-2 INH
    • ---------------------------------

    PHARM

    • PLATELETS CANNOT SYNTH NEW PROT → INHB COX-1 FOR LIFE OF PLATELET (9-14
    • DAYS)

    PREVENTS IL-1 FROM STIM PGE2 SYNTH --> PGE2 INCR THE THERMOREGULATORY SET-POINT --> FEVER

    --PREVENTS PG’S FROM SENSITIZING SENSORY PAIN FIBERS

    PREVENTS PROD OF TXA2 WHICH IS PROD BY PLATELETS & MONOCYTES & STRONGLY ENHANCES PLATELET AGGREGATION

    • IRREV INH OF COX-1 VIA ACETYLATION OCCURS IN THE PORTAL CIRC
    • --------------------------------------

    ADVERSE

    ASPIRIN-SENSITIVITY

    DECR RENAL FUNCTION

    NA/H2O RETENTION

    HYPERKALEMIA

    INTERSTITIAL NEPHRITIS

    REV. ACUTE RENAL FAILURE (ARF)

    GI ULCERATION & BLEEDING

    • PT AT GREATEST RISK:
    • -- >60 Y.O.
    • --TAKING CORTICOSTEROIDS
    • --PRIOR HX OF GI ULCERATION

    MISOPROSTOL (PGE1 STABLE ANALOG) RX GASTRIC EROSION & ULCERATION CAUSED BY NSAIDS & CORTICOSTEROIDS.

    DEC RATE OF HEALING FRACTURED BONES

    • *INDOMETHACIN (PRE-TERM INFANTS)
    • RENAL DYSFUNC & BLEEDING
  32. RELEASE OF EICOSANOIDS
    EICOSANOIDS = PROSTAGLANDINS AND LEUKOTRIENES

    DIETARY LINOLEIC ACID CONVERTED TO ARACHI ACID --> STORED IN CELL MEMs AS TGs, CHOLS, AND PHOSPHOLIPID ESTERS

    PHOSPHOLIPASE A2 (PLA2) CLEAVES ARACHI ACID FROM ESTERS, AND PLA2 IS ACT BY VASOCONST AGENTS (bradykinin, thrombin, tissue inj inc menses, and ischemia inc mi)

    • FREE ARACHI ACID
    • --REINCORPORATED INTO CELL MEMs

    --SUBSTRATE FOR COX, PGH SYNTHASE, PG SYNTHASE WHICH MAKES PGG2 AND PGH2 --> PRECURSORS OF ALL PGs

    --SUBSTRATE FOR ENZ 5-LIPOOXYGENASE --> HPETE --> LEUKOTRIENS
  33. EFFECTS OF CORTICOSTEROIDS
    ACTIVATE EXPRESSION OF LIPOCORTIN WHICH INH PLA2 --> NO RELEASE OF ARACHI ACID

    BLOCKS SYNTH OF ALL EICOSAMOIDS (ie PGs AND LTs)

    • GIVEN po EXERT (-)FEEDBACK ON HYPOTHAL:
    • --INH OF CRH RELEASE --> NO ACTH RELEASE --> DEC IN PLASMA CORTISOL AND ATROPHY OF ADRENAL CORT

    --INH OF TRH RELEASE --> DEC THYROXINE AND POSS OF HYPOTHYROIDISM

    --INH OF GnRH RELEASE --> DEC FSH --> AMENORRHEA IN FEMALES AND AZOOSPERMIA IN MALES
  34. MNEMONIC FOR ADVERSE EFFECTS OF po CORTICOSTEROIDS
    PREDNISONE

    PEPTIC ULCERS

    RETENSION OF Na/H2O --> HT, HYPO-K/Cl, MET ____ALKALOSIS

    EXTRA FAT IN TRUNK AND FACE (moon face)

    DIABETES AND CHANGES IN CHO MET

    NEUROSIS AND PSYCHOSIS

    INF PRONE, POOR WOUND HEALING

    SUPPRESSION OF PIT-ADREN AXIS

    OSTEOPOROSIS

    NEG NITROGEN BALANCE WITH MUSC WASTING AND STRIAE

    EYE - POSTERIOR SUBCAPSULAR CATARACTS AND GLAUCOMA

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