Kaplan Pharm Flashcards
choline uptake is inhibited by (hemicholinium/botulinum toxin)
hemicholinium
(hemicholinium/botulinum toxin) interacts with synaptobrevin to prevent ACh release
botulinum toxin
(hemicholinium/botulinum toxin) is used in blepharospasm, strabismus/hyperhydrosis, dystonia
botulinum toxin
M receptor activation (increases/decreases) CV function
decreases
M receptor activation (increases/decreases) secretions and (increases/decreases) smooth muscle contractions
increases both
all M receptor activators and blockers are (specific/nonspecific)
nonspecific
blood vessels are solely innervated by (symp/parasymp), so stimulation of autonomic ganglia results in vasoconstriction
sympathetic nervous system
the GI tract is dominated by (symp/parasymp) so ganglionic stimulation causes increased GI motility and secretions
parasymp
(ACh/bethanechol/methacholine/pilocarpine): treats glaucoma and xerostomia
pilocarpine
(ACh/bethanechol/methacholine/pilocarpine): treats bronchial hyperreactivity
methacholine
(ACh/bethanechol/methacholine/pilocarpine): treats ileus (postop/neurogenic), urinary retention
bethanechol
(ACh/bethanechol/methacholine/pilocarpine): short half life, no clinical use
ACh
ACh, bethanechol, methacholine, pilocarpine are muscarinic (agonists/antagonists)
agonists
(edrophonium/physostigmine/neostigmine and pryidostigmine/donepezil/organophosphates): treats glaucoma, lipid soluble, irreversible inhibitor
organophosphates
(edrophonium/physostigmine/neostigmine and pryidostigmine/donepezil/organophosphates): treats glaucoma, antidote in atropine overdose, enters CNS
physostigmine
(edrophonium/physostigmine/neostigmine and pryidostigmine/donepezil/organophosphates): treats ileus, urinary retention, myasthenia, reversal of nondepolarizing NM blockers
neostigmine and pyridostigmine
(edrophonium/physostigmine/neostigmine and pryidostigmine/donepezil/organophosphates): treats myasthenia; used to differentiate myasthenia from cholinergic crisis
edrophonium
(edrophonium/physostigmine/neostigmine and pryidostigmine/donepezil/organophosphates): treats Alzheimer disease
donepezil
ACh inhibitor poisoning mnemonic
Dumbbeelss
Dumbbeelss (ACh inhibitor mnemonic) stands for:
diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis, excitation (CNS/muscle), lacrimation, salivation, sweating
edrophonium, physostigmine, neostigmine, pyridostigmine, donepezil, organophosphates are: _____ (drug class)
AChE inhibitors (indirect acting cholinomimetics)
atropine, tropicamide, ipratropium, tiotropium, scopolamine, benztropine, trihexyphenidyl are: Muscarinic receptor (agonists/antagonists)
antagonists
(atropine/tropicamide/ipratropium and tiotropium/scopolamine/benztropine and trihexyphenidyl): lipid soluble (CNS entry), Parkinsons, acute extrapyramidal symptoms induced by antipsychotics
benztropine, trihexyphenidyl
(atropine/tropicamide/ipratropium and tiotropium/scopolamine/benztropine and trihexyphenidyl): used in motion sickness, causes sedation and short-term memory block
scopolamine
(atropine/tropicamide/ipratropium and tiotropium/scopolamine/benztropine and trihexyphenidyl):asthma and COPD, no CNS entry, no change in mucus viscosity
ipratropium, tiotropium
(atropine/tropicamide/ipratropium and tiotropium/scopolamine/benztropine and trihexyphenidyl): opathalmology
tropicamide
(atropine/tropicamide/ipratropium and tiotropium/scopolamine/benztropine and trihexyphenidyl): antispasmodic, antisecretory, management of AChE inhibitor overdose, antidiarrheal, opthalmology
atropine
Fenoldopam is a D1 (agonist/antagonist) used for severe HTN
agonist
(beta/alpha) receptors are usually more sensitive to activators than (alpha/beta) receptors
beta more sensitive than alpha
phenylephrine for nasal congestion and opthalmologic use: an alpha1 (agonist/antagonist)
agonist
clonidine and methyldopa for HTN: alpha (1/2) (agonist/antagonist)
alpha2 agonist
isoproterenol is a beta (agonist/antagonist)
agonist. effect on B1=B2
dobutamine is a beta (agonist/antagonist)
agonist. effect on B1 > effect on B2
isoproterenol is a beta agonist used for treatment of: (three conditions)
bronchospasm, heart block, bradyarrhthmias
dobutamine is a beta agonist used for treatment of: (one condition)
CHF
selective beta (1/2) agonists: salmeterol, albuterol, terbutaline (for asthma)
beta 2 agonists
(salmeterol/albuterol/terbutaline): beta 2 agonist used in premature labor
terbutaline
tyramine, amphetamines, ephedrine, cocaine, and tricyclic antidepressants are (direct/indirect) acting adrenergic receptor agonists
indirect
(releasers/reuptake inhibitors): tyramine, amphetamines, ephedrine
releasers
(releasers/reuptake inhibitors): cocaine, tricyclic antidepressants
reuptake inhibitors
nonselective alpha (agonist/blocker): phentolamine, phenoxybenzamine
blocker
(phentolamine/phenoxybenzamine): competitive inhibitor of alpha receptors
phentolamine
(phentolamine/phenoxybenzamine): noncompetitive inhibitor of alpha receptors
phenoxybenzamine
alpha receptor (agonists/blockers): used for HTN, pheochromocytoma, benign prostatic hyperplasia
blockers
prazosin, doxazosin, terazosin, tamsulosin: alpha (1/2) (agonist/blocker)
alpha 1 blocker
mirtazapine (antidepressant): alpha (1/2) (agonist/blocker)
alpha 2 blocker
(alpha/beta) (1/2) blockade: ↓HR, ↓SV, ↓CO, ↓renin release
beta 1 blockade
(alpha/beta) (1/2) blockade: bronchospasm, ↓aqueous humor production, blocks glycogenolysis, blocks gluconeogenesis
beta 2 blockade
three beta 1 selective blockers: (acebutolol/timolol/atenolol/pindolol/propranolol/metoprolol)
acebutolol, atenolol, metoprolol
three beta non selective blockers: (acebutolol/timolol/atenolol/pindolol/propranolol/metoprolol)
pindolol, propranolol, timolol
atenolol, beta blocker, (can/cannot) enter the CNS
cannot
propranolol, acebutolol, esmolol are beta blockers used for:
arrhythmias
(timolol/atenolol/propranolol) is a beta blocker used for glaucoma
timolol
(timolol/atenolol/propranolol) is a beta blocker used for migraine, thyrotoxicosis, performance anxiety, essential tremor
propranolol
labetalol and carvedilol have beta blocking and (alpha 1 blocking/K channel blocking) activity
alpha 1 blocking
(labetalol/carvedilol): used in CHF
carvedilol
(labetalol/carvedilol): used in hypertensive emergencies
labetalol
sotalol is a beta blocker with (alpha 1 blocking/K channel blocking) activity
K channel blocking
mixed agonist (epi/norepi): alpha 1, alpha 2, beta 1
norepi
mixed agonist (epi/norepi): alpha 1, alpha 2, beta 1, beta 2
epi
(M1/M2/M3) activation: miosis (sphincter contraction), ciliary muscle contraction for near vision accommodation
M3
(M1/M2/M3) activation: decrease in HR (SA node) and conduction velocity (AV node)
M2
(M1/M2/M3) activation: bronchospasm (bronchiole contraction), lung gland secretion
M3
(M1/M2/M3) activation: increase stomach motility (cramps), intestine contraction (diarrhea, involuntary, defecation)
M3
(M1/M2/M3) activation: increase GI gland secretion
M1
(M1/M2/M3) activation: bladder contraction (detrusor), relaxation (trigone/sphincter), voiding, urinary incontinence
M3
(M1/M2/M3) activation: sphincter relaxation except lower esophageal, which contracts
M3
(M1/M2/M3) activation: gland secretion (sweat, salivation, lacrimation)
M3
(M1/M2/M3) activation: dilation of blood vessels via NO/endothelium-derived relaxing factor
M3
(pilocarpine and echothiophate/timolol): activation of M receptors causes contraction of ciliary muscle, which increases flow through the canal of Schlemm
pilocarpine and echothiophate
(pilocarpine/echothiophate): AChE inhibitor to increase outflow in treatment of glaucoma
echothiophate (organophosphate)
(pilocarpine and echothiophate/timolol): blocks action of NE at ciliary epithelium, decreases aqueous humor formation
timolol
methyl p-tyrosine blocks which enzyme in the catecholamine synthesis pathway
tyrosine hydroxylase (tyrosine to dopa)
alpha 2 Gi coupled receptor (increases/decreases) cAMP
decreases
beta 1, beta 2, D1 Gs coupled receptor (increases/decreases) cAMP
increases
____: autacoid released from mast cells and basophils by type I HSR, drugs, venoms, and trauma
histamine
H1 activation: (increases/decreases) capillary dilation
increases, via NO
H1 activation: (increases/decreases) blood pressure
decreases, via capillary dilation
H1 activation: (increases/decreases) capillary permeability
increases
H1 activation: (increases/decreases) edema
increases, via increased capillary permeability
H1 activation: (increases/decreases) bronchiolar smooth muscle contraction
increases
H1 activation: (increases/decreases) activation of peripheral nociceptive receptors
increases (increases pain and pruritus)
H1 activation: (increases/decreases) AV nodal conduction
decreases
(H1/H2) activation: increases gastric acid secretion, increasing GI ulcers
H2
(H1/H2) activation: increased SA nodal rate, positive inotropism
H2
H1 antagonists act as (competitive/noncompetitive) antagonists of histamine
competitive
since H1 antagonists act competitively, they are (equally effective/ineffective) at high levels of histamine
ineffective
H1 antagonist adverse effect: (N/M) block and sedation
M block
H1 antagonists require metabolism in the _____ and (do/do not) cross the placental barrier
liver, do cross the placental barrier
most widely used H1 antagonist: (meclizine/chlorpheniramine/promethazine/cetirizine/loratadine/diphenhydramine/fexofenadine)
diphenhydramine
H1 antagonist with strong M blocking, sedation, antimotion, and some alpha block, local anesthetic action: (meclizine/chlorpheniramine/promethazine/cetirizine/loratadine/diphenhydramine/fexofenadine)
promethazine
(meclizine/chlorpheniramine/promethazine/cetirizine/loratadine/diphenhydramine/fexofenadine): H1 antagonist with possible CNS stimulation
chlorpheniramine
(meclizine/chlorpheniramine/promethazine/cetirizine/loratadine/diphenhydramine/fexofenadine): strongest antimotion properties
meclizine
(meclizine/chlorpheniramine/promethazine/cetirizine/loratadine/diphenhydramine/fexofenadine): three H1 antagonists that don’t cross the BBB, only used for allergic rxns
cetirizine (zyrtec), loratadine, fexofenadine
_____: autacoid synthesized and stored in GI cells, neurons, and platelets. MAO type A degrades it
serotonin 5HT
5HT3 receptor is a (GPCR/ion channel)
ion channel
six out of the seven 5HT receptor types are (GPCRs/ion channels)
GPCRs
5HT (1/2/3): found in CNS (usually inhibitory), smooth muscle (excitatory or inhibitory)
1
5HT (1/2/3): found in CNS (excitatory)
2
5HT (1/2/3): found in area postrema, peripheral sensory and enteric nerves
3
5HT (1/2/3): drugs are buspirone and sumatripan and other -tripans
1
5HT (1/2/3): drugs are olanzapine and cyproheptadine
2
5HT (1/2/3): drugs are ondansetron and -setrons
3
(buspirone/sumatripan): anxiolytic for generalized anxiety disorder
buspirone
(buspirone/sumatripan): decrease migraine pain
sumatripan
(buspirone/sumatripan): side effects could include asthenia, chest or throat pressure or pain
sumatripan
(olanzapine/cyproheptadine): atypical antipsychotic
olanzapine
(olanzapine/cyproheptadine): used in carcinoid, GI tumors, postgastrectomy, anorexia nervosa
cyproheptadine
ondansteron decreases emesis via which receptor
5HT3
ergotamine acts as partial agonists at both (alpha/beta) and (H1/5HT1/5HT2) receptors in the vasculature and possibly CNS
alpha and 5HT2
ergotamine: vaso (constriction/dilation) to cerebral vessels
vaso constriction: decrease pulsation
use ergotamine for (chronic/acute) migraines
acute attack
ergotamine is contraindicated in pregnancy because…
highly vasoconstrictive, will cause abortion near term