Pharm 4- abebe

olola's version from 2016-10-11 00:53


Question Answer
ACh is hydrolyzed by _______BOTH acetylcholinesterase + pseudo-/plasma-/butyrylcholinesterase
MCh is hydrolyzed by _______acetylcholinesterase
vasodilation of blood vessels of peripheral muscarinic action is due toendothelial release of nitric oxide
reversible inhibitor of Acetylcholinesterase that acts by covalent binding, which is readily hydrolyzableNeostigmine
organophosphates are _________irreversible acetylcholinesterase (inactivates the enzyme by forming irreversible covalent binding), used as insectisides and lethal nerve gases
therapeutic uses of anticholinesterasesglaucoma, MS, Alzheimers, reversal of nondepolarizing muscle relaxants
Ach interacts with AchE at which 2 sitescholine binding, esteratic sites (Ach is split at esteratic site by enzyme)
_______ do not cross the BBBNeostgmine + Erophonium b/c they have quaternary NH4 structure (note that these are also direct acting drugs)
Treatment of acute toxicity with organophosphatesRemove victim from source; give atropine (however, does not act at NMJ); maintain airways; give BDZ if atropine fail to relieve convulsion (CNS-mediated effect), and administer pralidoxime
Antidote for atropine (anticholinergic drug) poisoningPhysiostigmine (Neostigmine and quaternary NH4 salts do not enter CNS and are not used)
Treatment of Paralytic ileus and bladder atony (that usually occur after surgery)Neostigmine
commonly used in dentistry to treat xerostomiaPilocarpine
used to treat duodenal ulcersPropantheline (quaternary NH4 compound, have greater selectivity for GIT)
used to treat heavy metal poisoning, and Parkinsonsatropine
cholinesterase reactivatorPralidoxime (helps remove the inhibitor drug from the enzyme)
thoracolumbarsympathetic nervous system, adrenergic
craniosacralparasympathetic nervous system, cholinergic
long presynaptic, short postganglionic nervesparasympathetic / craniosacral
example of optical isomerismD-Amphetamine has increased CNS stimulation
clonidine binds selectively to ________ receptorsalpha-2, produce direct effect on CNS receptors
phenylephrine binds selectively to ______ receptorsalpha-1, little CNS effect but causes potent direct vasoconstriction
Hepatitis is an adverse effect associated with _____Methyldopa, an adrenergic agonist
treats pheochromocytomaPhentolamine, an Imidazoline
Dobutamine binds selectively to _______Beta-1 receptors
______ binds selectively to B-2 receptorsalbuterol, terbutaline, bitolterol, salmeterol, ritodrine -used to treat asthma
Radial muscle of iris ("_____") contracts due to __________ mydriasis, alpha-1 receptor stimulation
Ritrodrine usesfor short term uterine relaxation in pre-term labor via B2 stimulation
Timololnonselective B blocker used to treat glaucoma, heart attacks, hypertension, migraines
treatment of malignant hyperthermiaDantrolene
used for endotracheal intubations and mandibular fracturessuccinylcholine
herbs that cause xerostomiaSt. Johns wort, Gingko biloba
2nd messenger used in parasympatheticcGMP
2nd messenger used in sympatheticcAMP

Adrenergic drugs

Tritillium inhibits release of ___ → different mechanism : Norepinephrine
Question Answer
________ (drug class) have lots of side effects and CNS effects → reserved mainly for atypical depressionMAO Inhibitors
T/F: A2 receptors are PREsynaptic, but rest of alpha receptors are POSTsynapticTrue
What type adrenergic receptor associated with most blood vesselsA1
What type adrenergic receptor associated with CNS and Presynaptic actionA2
What type adrenergic receptor associated with HeartB1
What type adrenergic receptor associated with Lung/airway SM, some blood vesselsB2
What are 2 other stimulants (natural) for A1 receptors (in addition to Norepi)Epinephrine & Phenylephrine
What is another stimulant for A2 receptors (in addition to Norepi)Clonidine
What are 2 other stimulants for B1 receptors (in addition to Norepi)Isoproterenol & Dobutamine
What are 4 other stimulants for B2 receptors (in addition to Norepi)Albuterol, Terbutaline, Metaproterenol, & Bitolterol
T/F: Amphetamines are Indirect-acting SympathomimeticsTrue
T/F: Amphetamines are NE reuptake blockersFalse (indirect Sympathomimetic)
T/F: A2 receptors are PREsynaptic, but rest of alpha receptors are POSTsynapticTrue
T/F: A1 receptors are PREsynaptic, but rest of alpha receptors are POSTsynapticFalse (A2)
_____ (alpha/beta) receptors respond better to NE, then epi, and last isoproterenol; opposite effect in _____ receptors (iso > epi > NE)Alpha; Beta
you Can use ________ for asthma because it more selectively binds to B2 receptors = bronchodilation (more potent effect than epi bc of higher binding affinity)Isopr
______ blocks a1 receptors (anti-HTN)Prazosin
_______ is effective a2 agonist = used for Anti-HTNClonidine
Terbutaline, Albuterol, metaproterenol, and bitolterol are effective selective ___ agonist = asthma medB2
______ _______ 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