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Pharm Test 1 CPR

QuestionAnswer
Neurotransmitter of the adrenal medulla and sweat glands ACh (sympathetic nervous system NT exceptions)
receptors that mediate sympathetic nervous system alpha and beta receptors
NT at renal vascular smooth muscle Dopamine
1) Choline acetyltransferase 2) Acetylcholinesterase 1) enzyme synthesizes Acetylcholine 2) enzyme breaks down Acetylcholine
Muscarinic Receptors: M1, M2, M3, M4, M5 1 = nerve 2/3 = heart & smooth muscle 4 = sm muscle and glands mostly parasympathetic; G-protein coupled receptors.
What does Trimethaphan block? Nn (NeuroNicotinic) R's in autonomic ganglia, adrenal medulla and CNS are blocked by this
odd-numbered subtypes of mAChR's are what type? what do they produce? coupled to phospholipase C signaling cascade via the Gq protein -> produces inositol-1,4,5-triphosphate (IP3 induces Ca release) and diacylglycerol (DAG activates protein kinase C)
even-numbered subtypes of mAChR's do what and produce what? coupled to adenylyl cyclase via the Gi or Go protein -> alpha subunit inhibits adenylyl cyclase activity, decreasing the production of cyclic AMP (thus reducing chrono-& inotropic events in heart) & betagamma subunit opens K channels
Name the 5 compounds in the biosynthesis of catecholamines Tyrosine - DOPA - Dopamine - Norepinephrine - Epinephrine
NE release is increased by what? Blocked by what? increased by amphetamine & ephedrine Blocked by Guanethidine & reserpine
What blocks neuronal reuptake (Uptake 1) of catecholamines? cocaine & imipramine
What affect does Isoproterenol have on heart rate, and why? large increase in HR b/c it will stimulate beta1 receptors which increases tachycardia and it will stimulate beta2 which causes vasodilation which decreases BP which will increase HR
what does Idoproterenol stimulate? almost pure beta adrenergic agonist
what receptors does NorEpi stimulate? powerful alpha adrenergic agonist & also Beta1
which receptors does Epinephrine stimulate? stimulates all adrenoreceptors
Phenylephrine Alpha1 agonist, weak beta; vasoconstrictor treats hypotension. Decongestant, mydriasis.
Methoxamine alpha1 agonist; vasoconstrictor treats hypotension; longer acting (not metabolized by COMT or MAO). No effect on BetaR
Clonidine alpha2 agonist; direct vasoconstrictor is antihypertensive b/c it decreases NE release (central suppression); rebound HT.
Dobutamine Beta1 agonist also stimulates beta2 and alpha; inotropic; vasodilation for heart failure, preserves renal & GI blood flow
Terbutaline & Albuterol Beta2 agonist: bronchodilator (inhalation), inhibits premature labor; reduced cardiac risk; long duration action (not metabolized COMT/MAO; 4-8 hrs)
(Dextro-/Meth-)Amphetamine induces NE release - alpha and beta indirect agonist. CNS stimulant increases alertness, physical performance, concentration. Decreases appetite/fatigue. Dextro-/Meth- more CNS, less peripheral effects.
Ephedrine Mixed: Indirect = +NE release; Direct = alpha (pressor, decongestant) & beta (bronchodilator) agonist. stress incontinence, CNS stimulant, appetite suppressant
Pseudoephedrine mixed agonist, decongestant, meth ingredient
Metaraminol mixed agonist treats hypotension. Direct: alpha1 agonist, weak beta effects (like phenylephrine) Indirect: false NT (replaces NE in storage granules, dec NE)
Phenoxybenzamine alpha antagonist, irreversible block (likes alpha1 slightly more). Treats pheochromocytoma, urinary obstruction in BPH, autonomic hyperreflexia. SE: hypotension, congestion, ejaculatory dysfxn
Phentolamine alpha antagonist, reversible. Treats pheochromocytoma, inject for Erection. SE: hypotension, reflex tachycardia, congestion
~Prazosin ~Terazosin ~Tamsulosin alpha1 antagonist; antihypertensive, limited reflex tachycardia, dilates vasc beds (dec venous return), +urinary flow in BPH, "1st dose phenomenon" ~ drug lasts much longer ~ hypotension less common, more specific for prostatic sm m.
Propranolol Beta antagonist (1&2) - treats hypertension, ischemic HD (little effect on heart at rest), hyperthyroidism, glaucoma. Causes bronchochonstriction (no asthma, COPD!), hypoglycemia, membrane stabilization (like anesthetic)
Timolol like propranolol, but no anesthetic & is also topical ocular hypotensive
Metoproplol, Atenolol Beta1 antagonist - antihypertensive, ischemic HD (no effect on resting heart); less chance of bronchoconstriction
Labetalol alpha & beta antagonist - hypotensive w/ less tachycardia than alpha-block only
Guanethidine replaces NE in vesicles, interferes w/ NE release = sympatholytic. powerful antihypertensive (oral, 5day halflife, dilates vasc beds); orthostatic hypotension, diarrhea, ejaculatory distrubances. No MAOIs
Reserpine inhibits amine uptake into vesicles; irreversible (long actions!); inhibits DO uptake, blocks NE storage and synthesis. treats mild-mod HTN. CNS effects = depression, suicide, sedation
Methyl Tyrosine inhibits tyrosine hydroxylase (rate limiting step)(decreases catecholamines) Treats pheochromocytoma. Causes sympathetic depression, sedation, anxiety.
alpha-Methyldopa NE depleted, replaced in granules w/ this a-methyl-NE. Antihypertensive allows renal blood flow. Decreased sympathetic activity; sedation. USED FOR HT IN PREGNANCY
Cocaine, imipramine inhibitor of uptake 1 - accumulation of NE - overstimulation
Bethanechol direct cholinergic agonist selective for GI/urinary tract; postop/neurogenic urinary retention, reflux esophagitis, postop abdominal distention
Carbachol direct cholinergic agonist, muscarinic and nicotinic. glaucoma, cataract surgery: reduce intraocular P & produce miosis
Pilocarpine direct cholinergic agonist, muscarinic specific (minimal nicotinic). Reverses effects of mydriatic & cyclopegic agents. Most common cholinergic agonist for GLAUCOMA; promotes salivation.
Side effects of direct cholinergic agonists sweating, salivating, bronchoconstriction, miosis, vasodilation, N/V/Diarrhea, changes in HR, hypotension
Created by: meganca
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