robbypowell's version from 2016-10-10 22:30

Adrenergic drugs

Question Answer
______ _______ releases adrenaline/epinephrine; _______ ______ release noradrenaline/norepinephrineAdrenal Medulla; Nerve Terminals
_______ drugs mimic SYMPATHETIC stimulation and the effects of epinephrine... and their effects are much greater than normal sympathetic stimulationAdrenergic
_______ autonomic nervous system has LONG preganglionic fiber and SHORT postganglionic fiberParasympathetic
_______ autonomic nervous system has SHORT preganglionic fiber and LONG postganglionic fiberSympathetic
In the sympathetic nervous system Acetylcholine released preganglionically and then the neurotransmitter, _______, is released postganglionically to affect heart, smooth muscles, glands (not sweat)Norepinephrine
In the sympathetic nervous system Acetylcholine released preganglionically and then the neurotransmitter, _______, is released postganglionically to affect sweat glands and blood vessels (not heart)Acetylcholine
T/F: Somatic nervous system has no ganglionTrue
5-10% of NT released by sympathetic nerves is _____; the majority is _____Norepinephrine; Epinephrine (majority)
Synthesis of Norepinephrine begins with uptake of _____ and/or ______Tyrosine; Phenylalanine
Norepi is broken down by _____ & _____MAO (Monoamine Oxidase) & COMT (Catechol-O-methyltransferase)
The major way to control Norepinephrine is to use (uptake 1/uptake 2)... cocaine inhibits thisUptake 1
this enzyme is only found in the adrenal medulla and is used to convert Norepinephrine to Epinephrinephenylethanolamine N-methyltransferase
phenylethanolamine N-methyltransferase is only found where... and does what?Adrenal Medulla; converts Norepi to Epi
All adrenergic receptors are what mechanistic type of receptors?G-protein coupled receptors
Main adrenergic receptor in the airway... its agonism causes bronchodilationB2 receptor
Main adrenergic receptor in the heart ... its antagonism blocks arrhythmia or heart failureB1 receptor
What is the secondary messenger of Adrenergic receptors?cAMP
_____ (neurotransmitter) has no substitutions on NH2 so it is more selective on alpha receptorsNorepinephrine
_____ (neurotransmitter) has 1 substitution and so effects both alpha and beta adrenergic receptorsEpinephrine
_____ (neurotransmitter) has 2 substitution (bulky) --> little binding to alpha, more binding to beta adrenergic receptorsIsoproterenol (synthetic)
The more substitutions on NH2 (of catecholamines) the higher the affinity for _____ receptorsB2
A1 selective drugPhenylephrine (little CNS effect, potent direct vasoconstriction)
A2 selective drugclonidine (direct effect on CNS receptors)
Non-selective Beta adrenergic receptor agonistIsoproterenol
list 4 Selective B2 adrenergic receptor agonistsAlbuterol, Metaproterenol, Tabutaline, Bitoltrenol
Hepatitis may be caused by what Adrenergic agonist drug?Methyldopa
class of competitive nonselective alpha receptor antagonistImidazolines (e.g. Phentolamine)
Acute HTN that can't be treated with normal HTN drugs would be treated with what drug?Phentolamine (competitive nonselective alpha receptor antagonist; Imidazoline drug family)
class of non-competitive nonselective alpha receptor antagonistB-halo-alkenes (e.g. Phenoxybenzamine/PBZ)
What drug forms irreversible/covalent binding with alpha receptor and permanently deactivates itPhenoxybenzamine (PBZ)
This drug is ONLY used for pheochromocytoma bc it non selectively binds to and permanently deactivates alpha receptorsPhenoxybenzamine (PBZ)
Main A1 selective receptor anatagonistPrazosin (HTN treated by affective BV's)
T/F: A2 selective receptor antagonists are not used clinically because they cause hypertension... but are used as aphrodisiacsTrue
E.G. of Nonselective Beta blockers (also has some LA activity at high doses)Propranolol
e.g. B1 selective blockerAtenolol (cardioselective, with minimum airway effects)
B2 blockade can decrease glycogenolysis causing _______Hypoglycemia
Abrupt withdrawal of _____ causes heart problems due to B receptor super sensitivitypropranolol
2 examples of Nonselective adrenergic blockers (alpha and beta receptors)Labetalol & Carvedlilol
this drug causes depletion of catecholamines, • Reserpine: acts at intracellular vesicles and inhibits vesicular uptake and storage of NTs (both centrally and peripherally) → due to irreversible binding in vesicular membraneReserpine
T/F: Reserpine causes xerostomiaTrue
this class of drugs lowers blood pressure by unknown mechanismMAO inhibitors
2 drugs used to reduce CNS sympathetic outflowClonidine (most frequent) and Methyldopa (pro-drug)
Ergot Alkaloid drug that stimulates central DA receptors to suppress excessive prolactine secretion (seen in tumor of anterior pituitary gland) and for treating parkinsonsBromocriptine (Ergot Alkaloid)
T/F: Meperidine is contraindicated with MAOITrue
T/f: Clonidine and other A2 agonists cause xerostomiaTrue

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