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76 Cards in this Set
- Front
- Back
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effects of Epi on BP, HR, PVR
low dose vs. high dose |
low dose: ↑pulse pressure, little to no ∆ in BP, ↑HR, ↓PVR
β effects dominant high dose: α dominates, so ↑BP, ↑PVR also see ↑blood glucose & renin |
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effects of NE on BP, HR, PVR
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↑BP
↓HR ↑PVR |
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effects of isoproterenol on BP, HR, PVR
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↓BP
↑HR ↓TPR |
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what drug is used for dry mouth, with few side effects?
what class & receptor? what drug is a worse choice (due to side effects) for dry mouth? |
cevimeline (evoxac)
direct acting cholinergic agonist M3 receptors worse choice: pilocarpine ⇒ profuse sweating |
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what choline ester, quaternary amine is used for GI? what are the indications?
what class & receptor? |
bethanechol - stimulate peristalsis (decr bowel act w/o obstruction, post-op ileus, congenital megacolon)
also facilitates urine voiding direct acting cholinergic agonist M receptors |
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what are the contraindications for direct acting cholinergic agonists?
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peptic ulcers, coronary insufficiency, asthma, hyperthyroid
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what are the uses of pilocarpine?
what are the side effects? |
used for:
open angle glaucoma narrow angle if used w/ AChE inhibitor dry mouth side effects: blurred vision SWEATING |
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what is use for carbachol?
what class & receptor? |
use in eye ⇒ decreased pressure & miosis
direct acting cholinergic agonist M & N receptors |
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what happens w/ nicotine stimulation?
what happens w/ nicotine OD? |
initial stim of skeletal mm.
not broken down quickly, so ⇒ desensitization of NMJ ⇒ flaccid paralysis OD: vomiting, convulsions followed by coma & respiratory arrest, paralysis, HTN, cardiac arrhythmia |
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what drug is used for smoking cessation?
how does it work? what subtype of receptor is it acting on? what are the side effects? |
varenicline (chantix)
partial agonist of N receptor in the brain - α4β2 subtype it substitues for nicotine to relieve craving & blocks action of nicotine if they do smoke (b/c partial agonist) SE: N/V, CNS sx - sleep disturbances, nightmares, psychosis, mania, anxiety, suicide ideation |
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what drug can be used to dx MG or determine if med dosing is correct?
what is another use of this drug? what class? |
edrophonium - short duration of action
can also reverse NMJ blockade after surgery AChE inhibitor |
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what drug is given PO for MG?
what class? |
neostigmine
given PO even though it is a quaternary amine (poor absorption) AChE inhibitor it also has some direct stimulatory effect on NMJ, making it a good choice for MG |
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what is the use for physostigmine?
why isn't it used very often? what class? |
can be used for narrow angle glaucoma
rarely used b/c of side effects - it's a tertiary amine, so it gets into the CNS AChE inhibitor |
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what drug is good for long-term control in glaucoma emergencies? why?
what class? |
echothiophate
it is an organophosphate w/ a long duration of action - irreversible biding AChE inhibitor |
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why do you have to give 2-PAM quickly w/ organophosphates? how does 2-PAM work?
what other drug do you apply w/ 2-PAM? what do you look for? |
organophosphates phosphorylate AChE
in the early stages, it is reversible, but the bond undergoes "aging" and becomes irreversible 2-PAM is a strong nucleophile that can be added before the aging process to remove the organophsophate, preventing aging also give atropine and watch for pupils to dilate |
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what is the use of donepizil?
what class? |
used for alzheimer's
AChE inhibitor |
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what is the little saying to remember the effects of atropine?
what class is atropine? |
dry as a bone
blind as a bat mad as a hatter red as a beet cholinergic (muscarinic) antagonist |
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what are the indications for atropine?
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reverse bradycardia due to excessive vagal tone
reverse AV block treatment of cholinergic poisoning treatment of muscarine poisoning |
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what are the effects of increasing dose of atropine? (i.e. what order are the tissues affected - the stair step diagram)
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1 - dry mouth & decreased sweating
2 - increased HR, very dry mouth, thirst 3 - blurred vision, tachycardia, palpitations 4 - GI effects, urinary retention, hot & dry skin, restlessness, fatigue 5 - rapid & weak pulse, ataxia, hallucinations, delirium, coma |
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what drug is used for motion sickness?
how is it applied? what are side effects of this drug? what class? |
scopolamine
patch excitement, euphoria, hallucinations, coma w/ high dose (it enters the CNS ⇒ sedation & amnesia) cholinergic (muscarinic) antagonist |
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what is the preferred drug for overactive bladder in the elderly? why?
what class & receptor? |
tolderodine (detrol)
it is not lipid soluble & has few CNS effects, so good for elderly cholinergic (muscarinic) antagonist M3 receptor selective |
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what is oxybutynin (ditropan) used for?
what class? |
prevent bladder spasm after prostate surgery
cholinergic (muscarinic) antagonist |
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what is the use for glycopyrrolate (robinul)?
what class? |
used in surgery to prevent vagal response when viscera is handled
decrease M side effects when using neostigmine for MG cholinergic (muscarinic) antagonist |
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what is dicyclomine (bentyl) used for?
what class? |
inhibits motility & secretions of GI tract
used as GI antispasmodic cholinergic (muscarinic) antagonist |
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what is solifenacin (vesicare) used for?
what makes it a good choice? what class? |
used for overactive bladder & urinary frequency
it's good b/c it has little effect on salivation cholinergic (muscarinic) antagonist M3 selective |
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what is ipratropium (atrovent) used for? what about its structure makes it a good choice? what are the side effects?
what class? |
used to treat asthma & COPD
it works well b/c it is a quaternary amine and is not absorbed well. when inhaled, it stays in the lungs SE: dry mouth cholinergic (muscarinic) antagonist |
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what is tropicamide (mydriacil) used for? what is the contraindication?
what class? |
mydriasis & cycloplegia
used for eye exam don't use w/ narrow angle glaucoma cholinergic (muscarinic) antagonist |
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what is the opioid that is combined with atropine? what is it used for?
what class? |
diphenoxylate-atropine (lomotil) is used to treat diarrhea
cholinergic (muscarinic) antagonist |
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what is seen in the "train of four" for non-depolarizing NMJ blockers?
what about depolarizing? |
non-depol: see fade represented by reduced twitch height; undergo post-tetanic potentiation
depol: size of each twitch is reduced, but no fade; NO post-tetanic potentiation |
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which non-depol NMJ blocker has a rapid onset & intermediate duration of action?
what is its use? |
rocuronium (zemuron)
use for intubation |
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which non-depol NMJ blocker is most commonly used? why is a good choice?
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cisatracurium (nimbex)
it is spontaneously hydrolyzed and had low toxicity also, it does not cause histamine release (unlike d-tubocurarine) |
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what is the onset/duration of action of pancuronium (pavulon)?
how about vecuronium (norcuron)? |
these are both non-depolarizing NMJ blockers
pan - slow onset & long duration vec - slow onset & intermediate duration |
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what is the order of muscles affected by non-depol NMJ blockade?
what is the order of recovery? what is the prototype of this class? |
1st - small muscles (eye, jaw, larynx)
2nd - larger muscles last - diaphragm & intercostals recover in the opposite order d-tubocurarine is prototype |
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what class is succinylcholine?
describe phase I & phase II blockades. |
depolarizing NMJ blocker
phase I - prolonged depol; fasciculations followed by flaccid paralysis; effects are NOT reversed w/ AChE inhibitors; proper clinical use produces phase I blockade phase II - occurs w/ prolonged exposure (should not occur clinically); membrane is repolarized and desensitized - looks like block seen w/ non-depol (i.e. PTP, AChE inhib may reverse) |
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what things increase the effects of succinylcholine?
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aminoglycoside antibiotics (enhance due to Ca channel blockage)
tetracyclines (enhance due to Ca chelation) Ca channel blockers also enhance |
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what are the contraindications for succinylcholine?
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burns
severe trauma rhabdomyolysis spinal cord injury muscular dystrophy kids <8yo unless emergency causes release of K+ into blood - cardiac arrest |
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what are the ganglion blockers?
what receptor is in the ganglia? what are the effects in the eye, BVs, heart, GU, skin, and reflexes? what do these things have to do with tone? |
mecamylamine (inversine)
hexamethonium Nn receptor eye: cycloplegia, mydriasis (blocked PNS tone, so see SNS effect) BVs: vasodilation, orthostatic hypotension (blocking SNS tone) heart: decr contractility, tachycardia (blocking vagal tone) GU: urinary retention, can't get erection or ejaculation skin: no sweating, have to control temp by vasodilation (red face) decreased autonomic reflexes |
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what are the indications for use of Epi?
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anaphylactic shock
cardiac arrest & complete heart block vasoconstriction to decrease diffusion of local anesthetic glaucoma asthma emergency (rare) |
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which receptors does epi act on?
NE? isoproterenol? |
E: α, β1, β2
NE: α, β1 [no lung effects] I: β1, β2 [no α, so no BV effects] |
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what are the effects of low dose dopamine?
high dose? |
low: activate D1 receptor in renal vascular beds ⇒ vasodilation, ↑renal blood flow (↑GFR & Na excretion)
also dilates coronary & mesenteric aa higher: stimulate β1 in the heart ⇒ +inotropic & chronotropic effect may release NE to stimulate α1 (⇒ vasoconstriction & ↑BP like high Epi dose) |
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what is the indication for dopamine?
how is it applied? side effects? |
IV treatment for cardiac shock
SE: N/V, tachycardia, angina, arrhythmias, HA, peripheral vasoconstriction |
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what is the class & receptor for phenylephrine (neo-synephrine)?
what are its uses? |
α1 agonist
causes vasoconstriction -use as nasal decongestant (can get rebound effect) -use in hypotensive emergency to ↑BP -mydriasis w/o affecting accomodation - eye exam |
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what is the class & receptor of pseudoephedrine?
what is the use? who needs to be careful w/ its use? |
α agonist
OTC decongestant use caution w/ HTN |
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what drug can be applied orally or w/ a patch for HTN?
what class & receptor? how does it work? other uses? |
clonidine
α2 agonist decrease NE release by acting on PREsynaptic terminals in CNS ⇒ ↓BP & HR also used for addiction/alcoholism, menopause (↓hot flashes), pre-anesthetic (sedates) |
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what is the use for apraclonidine?
what class & receptor? |
used in eye to ↓pressure by reducing formation of aqueous humor (via vasoconstriction)
α2 agonist |
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what is the class & receptor for ritrodine (yutopar)?
what is it used for? |
β2 agonist
relax uterus and suppress pre-term labor |
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what 2 β2 agonists are used for asthma?
side effects? |
albuterol
terbutaline (brethine) SE: HA, tremors, tacycardia (b/c they can have small effect on β1, too) |
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what class & receptor for dobutamine (dobutrex)?
what does it do? when is it used? |
β1 agonist
↑renin release +inotrope, chrontrope ↑CO w/ little effect on PVR 1/2 life is 2 min, so can be used for cardiac stress test if pt can't exercise incr CO for cardiogenic shock & CHF |
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what is ephedrine?
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a MIXED acting adrenergic stimulant - denervation will ↓ its effect
acts on α & β receptors it is similar to epi but is less pronounced and has longer duration it is a CNS stimulant |
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how does amphetamine act?
what can it be used to treat? what are the side effects? |
indirect acting - displaces NE & DA from vesicles, ↑ their release from neurons; CNS stimulant
tx enuresis - strong contraction of urinary bladder sphincter SE - tremor, tachycardia, HTN, psychosis, dizziness, restlessness, irritability, fever, aggression, HA, cerebral hemorrhage, convulsions, coma |
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why does methylphenidate (ritalin) work for ADHD?
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it has a paradoxical effect in someone w/ ADHD ⇒ decrease in activity
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how does cocaine act?
what can it be used for? what are the side effects? |
indirect acting
inhibits reuptake of NE & DA into nerve terminal has amphetamine-like effect that is shorter acting & more intense used in nasopharyngeal surgery to ↓blood flow & local anesthesia SE: addiction; severe HTN, stroke, tachycardia, arrhythmia, MI, psychosis |
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how does tyramine act?
what can happen w/ a large dose? what are the contraindications? |
indirect acting - increases release of catecholamines from nerve
gets taken up into vesicles & displaces NE w/ false NT (octopamine) w/ large dose get massive release ⇒ tachyphylaxis CI - MAOIs ⇒ severe HTN crisis |
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what is fendolopam (corlopam)?
what are its uses? |
DA agonist - D1 receptor
causes dilation of vascular beds & ↓BP used short-term to ↓BP in severe HTN |
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what class is phentolamine?
uses? side effects? contraindications? |
α blocker (1 & 2)
↓BP & PVR - used for short-term tx of HTN crisis in pheochromocytoma or HTN crisis due to tyramine or abrupt clonidine withdrawal SE: tachycardia, myocard ischemia, abd pain, arrhythima, low BP CI: peptic ulcer, CAD (caution); viagra-absolute |
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what class is phenoxybenzamine?
uses? side effects? CI? |
α blocker (1 & 2)
IRREVERSIBLE - good for use in pheochromocytoma b/c their high secretion of catecholamines can overcome reversible blockade postural hypotension, tachycardia, nasal stuffiness, inhibition of ejaculation CI - viagra absolute |
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what class is prazosin (minipress)?
uses? how often do you give it? what about giving it to someone w/ CHF? SE? CI? |
α1 blocker
used for HTN - BID also BPH CHF - half life is 2x SE: first dose phenomenon; inhibit ejaculation; dizziness; nasal stuffiness CI: viagra absolute |
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what are terazosin & doxazosin used for? why are they good?
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sim to prazosin - α1 blockers
used for BPH good b/c long 1/2 life (qd) & ↓prostate size by causing apoptosis |
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what is tamsulosin (flomax)?
what is its use? why is it more selective? |
α1 blocker
used for BPH, works rapidly more selective for α1A (prostate) than α1B (BVs), so little BP effect |
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what the class of yohimbine?
what was it marketed as? what drug does it interact with? |
α2 blocker
claimed to be natural alternative to viagra antagonizes clonidine |
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why do you have to use caution when giving a β1-blocker to COPD or asthma pts?
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selectivity is not absolute - high dose can block β2 as well
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what is the class of propanolol?
what are its effects? |
β-blocker (1&2)
• – chronotrope, dromotrope, inotrope • ↓renin release • ↓aqueous humor production • ↓glycogenolysis & mask sx of hypoglycemia (caution in DM type I) • chronic use ⇒ ↑VLDL & ↓HDL • interfere w/ K+ buffering by catecholamines - ↑plasma [K] • local anesthetic |
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what things affect the effectiveness of propanolol?
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metabolized by liver - varies in each pt
metabolism reduced by: cimetidine (causes increase in the antihypertensive effect) metab increased by: barbiturates, phenytoin, rifampin, smoking Ca channel blockers have additive effect |
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what is timolol (timoptic) used for?
what are the contraindications? |
β-blocker (1&2)
used for open angle glaucoma CI - pheochromocytoma (must give α-blocker to prevent vasoconstriction); asthma; type I DM (caution); Ca channel blockers |
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what is metoprolol (lopressor) used for?
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β1-blocker
used for HTN, ↑life expectancy w/ MI, migraine prophylaxis have better exercise tolerance b/c don't block β2 also ↓risk of causing hypoglycemia |
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what is atenolol (tenormin)?
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β1-blocker
sim to metoprolol, but w/o anesthetic effect ↑risk for developing type II DM |
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what is esmolol (brevibloc)?
use? |
β1-blocker
use via IV when you want a short β blockade (duration ~8min) |
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what is betaxolol (betoptic)?
use? |
β1-blocker
open angle glaucoma w/ fewer side effects than timolol |
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what is nebivolol (bystolic)?
what makes it a good drug? |
β1-blocker
most selective β1 antagonist on the market causes vasodilation due to ↑NO release significantly ↓C, TAGs, glucose |
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what are the 2 β-blockers w/ intrinsic sympathetic activity?
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pindolol (visken)
acebutolol (sectral) used for HTN, angina ↓risk of bradycardia b/c don't ↓HR much acebutolol is local anesthetic, don't use for gualcoma |
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what are the 2 combined bockers?
what do they do? which is used w/ CHF & why? |
lebetalol (normodyne)
carvedilol (coreg) both ↓BP w/o ↑HR (compensatory increase is blocked) use carvedilol w/ CHF b/c it inhibits vascular sm mm mitogenesis |
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what is guanethidine (ismelin)?
how does it act? side effects? |
NT release blocker
transported into terminal & replaces NE to gradually deplete NE stores SE: complete loss of SNS ⇒ postural hypotension, ↓blood to brain & heart |
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what is reserpine?
how does it act? SE? |
NT release blocker
interferes w/ uptake & storage of biogenic amines in nerve terminal - depletes NE, DA, 5-HT in brain low doses ↓BP (not used clinically) SE: severe diarrhea, depression, sedation, parkinson-like |
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what is metyrosine (desmer)?
how does it act? use? |
synthesis inhibitor - tyrosine analogue
blocks tyrosine hydroxylase (rate limiting) ⇒ ↓DA, NE, E synthesis pre-surgical tx in pheochromocytoma (combined w/ phenoxybenzamine) |
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what are the 4 β-blockers w/ local anesthetic effects?
what is the contraindication for these? |
lebetalol
acebutolol propanolol metoprolol don't use w/ glaucoma - don't want to anesthetize the cornea (the other β-bockers [esp. timolol & betaxolol] are used for glaucoma b/c they ↓humor production) |
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match the receptors to their second messenger system
Gs Gi Gq sodium channel M1, M2, M3 Nn, Nm β1, β2, β3 α1, α2 D1, D2, D3, D4, D5 |
Gs (stimulate AC ⇒ ↑cAMP)
β1, β2, β3, D1, D5 Gi (inhibit AC ⇒ ↓cAMP) M2, α2, D2, D3, D4 Gq (PLC, IP3, DAG, ↑Ca2+) M1, M3, α1 sodium channels Nn, Nm |
