Mkgrady8 Neuro 3 Adrenergic Antagonists And Sympatholytic Agents

Front 1

adrenergic receptor antagonists: alpha receptor antagonists: non selective and alpha1 selective

Back 1

non selective= phenoxybenzamine; alpha1 selective= prazosin, tamsulosin;

Front 2

adrenergic receptor antagonists: beta receptor antagonists: non selective and beta1 selective

Back 2

non selective= propranolol and timolol; beta1 selective= atenolol and metoprolol

Front 3

what is a pheochromocytoma

Back 3

a neuroendocrine tumor of the medulla of the adrenal glands; secretes large amounts of catecholamines epi and norepi; treated with prazocin; 25% genetic contribution

Front 4

what is benign prostatic hyperplasia

Back 4

nonmalignant enlargement of the prostate due to growth of either epithelia/glandular (mechanical obstruction) or smooth muscle (dynamic obstruction urethra); symptoms= hesitancy, urgency, increased frequency, dysuria, nocturia, straining, dribbling, etc; incidence= 50% of age>60, 90% of age>85; if they have symptoms then treat with alpha1 adrenergic antagonists (prazocin and tamsulosin) because it decreases the dynamic obstruction of the urethra (relaxes the smooth muscle of the capsule, urethra, and bladder neck)

Front 5

nonselective alpha antagonists: clinical uses, adverse effects

Back 5

clinical uses are limited= phenoxybenzamine for pheochromocytoma and benign prostatic obstruction and use ergot alkaloids for migraine headache; adverse effects= cardiovascular (tachycardia (reflex), orthostatic hypotension, nasal congestion), non cardiovascular (GI (phentolamine), impotence (phenoxybenzamine), potential mutagen (phenoxybenzamine)

Front 6

non selective alpha blockers effect on prejunctional alpha2 receptor

Back 6

alpha2 component= prejunctional blockade --> reflex tachycardia; influence in treatment of hypertension non selective give tachycardia

Front 7

selective alpha1 antagonists: advantage over non selective agents, uses

Back 7

prazosin; advantage over non selective agents= lack of alpha2 component (less prejunctional blockage --> less reflex tachycardia); uses= benign prostatic hyperplasia, hypertension, congestive heart failure, pheochromocytoma

Front 8

selective alpha1 antagonists: adverse effects

Back 8

orthostatic hypotension= usually becomes tolerated, give first dose at night; nasal congestion

Front 9

phenoxybenzamine: receptor, clinical uses, MOA, adverse effects, contraindications

Back 9

alpha antagonist; clinical uses= symptomatic management of pheochromacytoma, treatment of hypertensive crisis caused by sympathomimetic amines, micturition problems; MOA= irreversible alpha antagonist, decreased vasoconstriction by epi and NE; adverse effects= decrease blood pressure, GI, postural hypotension, reflex CV stimulation, pupil constriction, partial agon/antag at 5HT2A; contraindications= drug sensitivity

Front 10

prazocin: receptor, clinical uses, MOA, adverse effects, contraindications

Back 10

alpha1 antagonist; clinical uses= hypertension, PTSD, benign prostatic hyperplasia, scorpion stings; MOA= alpha1 antagonist, relaxes smooth muscle, lowers blood pressure, PDE inhibition; adverse effects= postural hypotension, SYNCOPE; contraindications= drug sensitivity

Front 11

uroselective alpha1A antagonist: name, clinical use, adverse effects

Back 11

tamsulosin; clinical use= benign prostatic hyperplasia (BPH); adverse effects= retrograde ejaculation (secondary to relaxation of bladder beck (sphincter) smooth muscle), avoids orthostatic hypotension in most

Front 12

uses of beta antagonists: cardiovascular and non cardiovascular

Back 12

cardiovascular= hypertension, angina, arrhythmias, myocardial infarction, heart failure, CV symptoms of hyperthyroidism, pheochromocytoma, and aortic aneurysm, migraine headache; non cardiovascular= glaucoma, somatic symptoms of anxiety (e.g. stage fright), fine muscle tremors

Front 13

beta antagonists: prototype name, what does it do, metabolism

Back 13

propranolol is prototype; pure antagonist, no intrinsic sympathomimetic activity (i.e. not a partial agonist); nonselective to beta subtypes; high lipid solubility (enters gut and CNS); high first pass metabolism causing low bioavailability; has membrane stabilizing activity= quinidine like effects, NA+ channel blockade (local anesthetic), avoid for topical administration to eye (glaucoma Tx)

Front 14

beta antagonists: adverse effects

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cardiovascular= induce CHF or bradycardial arrhythmia, sudden withdrawal in anginal pts may cause sudden death (probably due to receptor super sensitivity) (SO WEAN THEM OFF); cholesterol levels; BRONCHIOSPASM; CNS sleep disturbance, depression; mask symptoms and recognition of hypoglycemia

Front 15

beta antagonists uses and contraindicaations

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use in hypertension (1st choice if stable angina present), decrease BP and protects heart, in older pts with isolated systolic HT often used with diuretics as DOC; use in angina; use in heart failure both acute (MI) and chronic (decrease heart work and protect against arrhythmias); don't use if asthma or other bronchospasm (cause bronchoconstriction); don't use in diabetes or hypoglycemia (mask symp of insulin induced hypoglycemia and glycogenolysis is inhibited, augment insulin induced hypoglycemia); it raises VLDL and lowers HDL cholesterol levels; less effective than other anti HT in blacks

Front 16

beta antagonists: the non selective and selective beta1s (names)

Back 16

nonselective= propranolol and timolol; beta1 selective= atenolol, metoprolol

Front 17

propranolol: receptor, clinical uses, MOA, adverse effects, contraindications

Back 17

beta antagonist; clinical uses= hypertension, angina, arrhythmias/tachycardia, pheochromocytoma, prophylaxis of migraine, tremor, parkinson, alcohol withdrawal; MOA= beta non selective antagonist, constricts bronchial smooth muscle; adverse effects= CV angina, CNS, GI disturbance, others (extensive); contraindications= drug sensitivity, congestive heart failure, COPD

Front 18

timolol: receptor, clinical uses, MOA, adverse effects, contraindications

Back 18

beta antagonist; clinical uses= open angle glaucoma (low anesthetic properties, better tolerated than pilocarpine), ischemic heart disease; MOA= beta antagonist; adverse effects= cardiac arrhythmias, bradycardia, blurred vision, GI disturbance, bronchospasms; contraindications= bronchial asthma, COPD, heart failure

Front 19

atenolol: receptor, clinical uses, MOA, adverse effects, contraindications

Back 19

clinical uses= hypertension, elderly pts with isolated systolic HT (effective when given in combo with diuretic), angina, post MI treatment; MOA= beta1 antagonist; adverse effects= bradycardia, CNS, GI disturbance, impotence; contraindications= drug sensitivity, bradycardia, pregnancy

Front 20

metoprolol: receptor, clinical uses, MOA, adverse effects, contraindications

Back 20

beta1 antagonist; clinical uses= hypertension (more effective when combo with diuretic), angina, heart failure; MOA= beta1 antagonist; adverse effects= slow heart rate and symptoms of heart failure, CNS dizziness, drowsiness, tiredness, shortness of breath, mood swings, depression; contraindications= severe bradycardia, cardiogenic shock, drug sensitivity

Front 21

indirect acting drug list and MOAs

Back 21

block transport at nerve terminal= cocaine; promotion of exocytosis and displacement of transmitter= amphetamine; inhibition to transmitter degradation= depression tranylcypromine