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42 Cards in this Set
- Front
- Back
What are the endogenous catecholamines?
Which receptors do they act on? Effects? General therapeutic uses? |
-Norepinephrine (NE) = noradrenalin
-Epinephrine (EPI) = adrenalin -Dopamine (DA) = dopamine -They are mixed alpha & beta adrenergic receptor agonists -Dopamine activates D receptors -Effects of activation of sympathetic NS -Autonomic NS effects |
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EPINEPHRINE
Receptors? General physilogical Effects? |
-beta 1 & 2, alpha 1 & 2
-Depends on dosage -low dose: beta effects predominate -high dose: alpha effects |
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EPINEPHRINE
Effects on the heart? Effects on the vasculature? Effects on Respration? Effects on Genitourinary? Effects on the eye? |
-Increase HR & strength of ventricular contraction
-Low doses: decreased TPR & diastolic pressure, High dose: increased TPR & BP -Relaxes SM of airways: bronchodialation, inhibits inflammatory mediator release from mast cells, decreases vascular permeability in lung, decrease plasma protein extravasation, Increases cilia beat freq (beta receptors) -Relaxes detrussor muscle in bladder & relaxes uterus -Dilates pupil by relaxing ciliary muscle, increases aqueous humor outflow & decreases production |
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EPINEPHRINE
Therapeutic uses? |
-Bronchospasm: Activates beta 2 to relax SM
-Anaphylaxis: Epi pen's for shock, beta 2 bronchodialation, alpha 1 vasoconstriction, beta 1 increase cardiac output -Local hemostasis: prolong actions of local anesthetics by decreasing blood flow to area (alpha 1) |
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EPINEPHRINE
Adverse effects on: Heart? Vasculature? Respiratory? |
Too much leads to:
-Cardiac: Palpitations, arrhythmias, angina (beta 1) -Vascular: Pallor, stroke (alpha 1) -Respiratory: distress/pulmonary edema (alpha 1 causes resistance) |
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EPINEPHRINE
Contraindications/Precautions |
-Patients on beta receptor antagonists (beta blockers)=>Leads to massive a-1 response
-cardiovascular disease (increased cardiac workload w/ EPI) -diabetes(beta 2 & increase in gluconeogenesis) -hyperthyroidism (elevated heart rate) -taking MAOI's or tricyclics(block NE transporters so don't clear it) -pregnant (alpha 1 loss of blood to fetus) |
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NOREPINEPHRINE
Receptors? Physilogical effects? |
-Both alpha & beta w/ greater beta 1
-Vasculature: increased vasoconstriction => Increased TPR -Cardiac: depends on patient status |
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NOREPINEPHRINE
Therapeutic uses? |
-Blood pressure control in acute hypotensive states: alpha 1
-Cardiac arrest & profound hypotension: beta 1 -beta 1 in heart & alpha 1 in vasculature |
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NOREPINEPHRINE
Adverse effects? Contraindications? |
-Cardiac: Bradycardia, arrhythmias
-Vascular: decreased blood flow to vital organs, extravasation necrosis @ IV site -Respiratory: distress, edema -Mesenteric or peripheral vascular thrombosis -Precaution: extravasation @ IV site -MAOI's or tricyclics |
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NOREPINEPHRINE
Contraindications? |
-Pheochromocytomas: tumors producing NE & EPI
-Uncorrected tachyarrhythmias or ventricular fibrillation -Occlusive vascular disease -MAOI's |
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DOPAMINE
Receptors? Physiological Effects? Heart? Vasculature? Kidney? |
-Depends on dose: D>beta>alpha
-D1 >> D2 -Cardiac: increased HR & output (B-1) -Vascular: High dose = increased BP (a-1) -Renal: Increased glomerular filtration, blood flow, natriuresis/diuresis(treat hypertension) -D1 = Na+ & H2O out |
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DOPAMINE
Therapeutic uses? Adverse effects? |
-Shock/hemodynamic imbalance
-Heart failure -Cardiac: tachycardia -Vascular: hypertension, local ischemic necrosis |
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ALPHA 1 AGONISTS
List the drugs |
PHENYLEPHRINE
MIDODRINE OXYMETAZOLINE |
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ALPHA 1 AGONISTS
Physiological effects? |
Vascular: increased MAP
Cardiac: decreased HR Ocular: mydriasis (pupil dilation) Genitourinary: urinary retention |
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ALPHA 1 AGONISTS
Therapeutic uses? |
-Treat hypotension/shock
-Nasal decongestion (alpha 1 to mucosa vasculature) -Mydriasis (pupil dilation) |
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ALPHA 1 AGONISTS
Adverse effects? Contraindications? |
-Cardiovascular: Hypertension/stroke/MI;bradycardia
-Urinary retention -Severe hypertension or ventricular tachycardia -MAOI's or tricyclics |
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ALPHA 2 AGONISTS
List the drugs Treats what main disease? |
BRIMONIDINE
apraclonidine THINK GLAUCOMA |
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ALPHA 2 AGONISTS
Physiological effect? Therapeutic Uses? |
-Decreases production of aqueous humor & increases uveoscleral outflow
-Treats open-angle glaucoma |
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ALPHA 2 AGONISTS
Adverse effects? Contraindications/Precaution? |
-Eye redness or stinging
-Allergic reactions -bradycardia -MAOI's(contraindication) & tricyclics(precaution) |
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Beta Agonists
Non-Selective drugs? Beta-2 selective drugs? |
-ISOPROTERENOL
-ALBUTEROL -LEVALBUTEROL -TERBUTALINE -FORMOTEROL |
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ISOPROTERENOL
|
Non-selective beta agonist
Limited in use |
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ALBUTEROL
Mode of administration? Therapeutic use? |
Beta-2 selective
Oral or inhalation Given in ER nebulized for acute exacerbations of asthma |
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LEVALBUTEROL
-Mode of administration? -Therapeutic use? |
-R-isomer of albuterol
-Inhalation -Used in relief & prevention of bronchospasm |
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TERBUTALINE
-Mode of administration? -Therapeutic use? |
-Oral, injection
-ONLY beta-2 bronchodilator, used as IV admin in ER treatment of status asthmaticus |
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FORMOTEROL
Unique characteristic? Contraindications? |
-2X the potency, more lipophilic = Longer duration
-BLACK BOX WARNING: may increase risk of ashtma-related death |
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BETA AGONISTS
Physiological effects? |
-Bronchodilation
-Enhanced mucociliary clearance -Inhibits mast cell release of inflammatory mediators -Decreased TPR -Increased cardiac output |
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BETA AGONISTS
Therapeutic uses? |
-Bronchospasm: beta-2 agonists are the DRUGS OF CHOICE for sympathomimetic in treating ASTHMA
-Cardiovascular (Isoproterenol only) -Heart block -Cardiac arrest -Hypovolemic states/shock |
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BETA AGONISTS
Adverse effects? How do you limit these effects? |
**All side effets are less likely w/ administration by inhalation**
-Cardiac: palpitations, tachycardia -Skeletal muscle tremor: develop tolerance |
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BETA AGONISTS
Contraindications/Precautions? |
-tachyarrhythmias, vetricular arrhythmias, angina, heart block caused by digitalis(isoproterenol)
-cardiovascular disorders(precaution for B-2's) -Diabetes(precaution) |
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MIXED AGONISTS
List drugs |
DOBUTAMINE
EPHEDRINE PSEUDOEPHEDRINE |
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DOBUTAMINE
Physiological effect? Therapeutic uses? |
-Binds BOTH alpha & beta with predominant B-1 effects on heart
-More potent inotropic effects -Peripheral resistance unchanged -Cardiac decompensation due to organic heart disease or cardiac surgery |
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DOBUTAMINE
Adverse effects? Contraindications/Precautions? |
-Cardiac: Increase HR
-Vascular: Increase BP -Tachyphylaxis(avoid w/continuous low dose infusion) -Idiopathic hypertrophic subaortic stenosis(obstruction to cardiac flow) |
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EPHEDRINE & PSEUDOEPHEDRINE
-Receptors? Physiological effets? |
**Pseudoephedrine is less potent**
-Act on both alpha & beta receptors indirectly by releasing NE -Cardiac: Increased HR & contractility -Vascular: variable change in TPR -Respiratory: Bronchodilation -CNS: Penetrates BBB, CNS stimulation |
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EPHEDRINE & PSEUDOEPHEDRINE
Therapeutic uses? |
Hypotension: a1
Nasal decongetion: a1 OTC asthma: b-2 bronchodilation |
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EPHEDRINE & PSEUDOEPHEDRINE
Adverse effects? Contraindications/Precautions? |
-Cardiac: palpitaiton, arrhythmias, tachycardia or bradycardia
-Vascular: hypertension -Genitourinary: urinary obstruction w/ benign prostatic hypertrophy -CNS: nervousness, restlessness, psychological disturbances -MAOI's -Cardovascular disease, hyperthyroidism, diabetes, prostatic hypertrophy |
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DOPAMINE RECEPTOR AGONISTS
List the drugs |
FENOLDOPAM
|
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FENOLDOPAM
Receptors? Physiological effects? |
D1 receptor activation
-Vascular: hypotension & renal vasodilation -Renal: Natriuresis & diuresis |
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FENOLDOPAM
Therapeutic use? Adverse effects? Contraindications/Precautions? |
-Hypertension: given IV
-Headach most common, hypotension, tachycardia -Glaucoma |
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INDIRECT AGONISTS/SYMPATHOMIMETICS
List drugs |
COCAINE
METHYLPHENIDATE TYRAMINE dextroamphetamine/amphetamine |
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COCAINE
Pharmacology? Therapeutic uses? |
-Blocks re-uptake of catecholamines =>Increases dopamine & NE
-Hemostasis: Used in ENT surgery -Local anesthesia |
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METHYLPHENIDATE
Pharmacology? |
-Blocks reuptake of catecholamines
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TYRAMINE
Pharmacology? Clearance by which enzyme? Contraindications? Adverse effects? |
-by-product of tyrosine metabolism
-metabolized by MAO (MAOI's contraindicated) -Can produce hypertensive crisis due to excessive NE release |