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140 Cards in this Set
- Front
- Back
mechanism and effect of guanethidine
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inhibits NE vesicle fusion/release (net decrease in NE)
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name modulating receptors on noadrenergic terminal
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alpha 2, angiotensin II, and M1 (Ach)
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bethanechol
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cholinomimetric direct agonist on bowel and bladder s.m., used for post-op and neurogenic ileus and urinary retention
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carbachol
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direct cholinomimetic agonist, activates ciliary muscle of eye (open angle glaucoma) and pupillary sphincter (narrow angle glaucoma)
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pilocarpine
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direct cholinomimetic agonist, activates ciliary muscle of eye (open angle glaucoma) and pupillary sphincter (narrow angle glaucoma)
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neostigmine (3)
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anti CE, used for post-op ileus and urinary retention, MG, reversal NMJ block
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pyridostigmine
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anti CE used for MG
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edrophonium
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dx of MG (anti CE short t1/2)
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physiostigmine
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anti CE, used for glaucoma (crosses BBB) and atropine OD
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echothiophate
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glaucoma, anti CE
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parathion
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an organoP (poison CE), causing DUMBBLESS (diarrhea, urination, miosis, bronchospasm, bradycardia, excitation mscl and CNS, lacrimation, sweating, salivation, abd cramp)
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antidote to organoP
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atropine (muscarinic antag) and pralidoxime (regenerates CE)
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effects of atropine, used to tx
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dilate eye, decr GI acid, motility, decr respir sxns, treat organoP
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what use for atropine OD
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physistigmine (anti CE)
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tx MG
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dx with edrophonium, tx with neostigmine, pyridostigmine
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muscarinic cholinoR blockers include
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atropine, beztropine (PD), scopolamine (motion sickness), ipratropium (asthma, COPD)
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SE of atropine
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hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter (
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cause pupil to dilate (2meds and their R)
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alpha 1 phenylphrine, and antiAch stropine
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ephedrine
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indirect general symp agonist used for nasal decongestion, urinary incontinence, and hypotension
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phenylphrine
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alpha 1>alpha2 sympath, dilates pupil, vasoconstrict, nasal decongestion
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clonidine
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central acting alpha agonist decr adrenergic outflow, used for HTN, esp in renal disease (maintains renal BF) and in preg
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alpha-methyldopa
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central acting alpha agonist decr adrenergic outflow, used for HTN, esp in renal disease (maintains renal BF) and in preg
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cocaine
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general sympathomimetic, inhibits uptake , causing vasoconstriction and local anesthesia
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amphetamine
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indirect general sympathomimetric used for narcolepsy, obesity, ADD
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epinephrine acts on which R
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all (alpha1,2, and beta1,2)
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effect BP epinephrine
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incr SBP, decr DBP, MAP maintained
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use of epinephrine
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anaphylaxis, glaucoma open angle, asthma, hypotension (maintain RBF)
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NE acts on which R
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alpha 1,2 and beta1
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effect BP NE
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all increase, with reflex bradycardia
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hexamethonium
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nicotinic Ach R blocker, used to prevent reflex bradycardia from NE
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dopamine acts on which R
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D1=D2>beta>alpha
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effect alpha 1 R
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-vasoconstriction GI
-mydriasis -GI sphincter contraction -ejac |
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effect alpha 2 R (3)
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-presynapt - NE release and para Ach
-insulin -decr aq humor of eye |
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effect beta 1 (4)
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-heart incr rate and contractility
-renin -aq humor -incr lipolysis |
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effect beta 2
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-vasodilation skel muscle
-allow BF organs -relax bronchi and GI -uterus -glucagon -epi on beta 2 + NE release |
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effect beta 3
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adipose
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receptor control of aq humor, alpha and beta effect
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alpha controls outflow and syn
beta controls sxn Ach controls cxn and outflow PG controls outflow alpha 2 decr, beta 1 increase, Ach R on drainage |
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control of insulin/glucagon by adrenergic receptors
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alpha 2 controls insulin, beta 2 controls glucagon
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name neuro path for symp
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symp pregang rel Ach binds nicotinic R which rel NE on adrenergic R
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name path for parasymp
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para pregang release Ach on nicotinic R which releases Ach on muscarinic R
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name path for somatic
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(no ganglia) Ach released on nictonic R on striated muscle
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receptors dobutamine act on, use
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beta1>beta2, used in CHF and shock
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phenoxybenzamine
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irrev alpha blocker, used for pheo
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SE phenoxybenzamine
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(irrev alpha blocker, used for pheo) orthostatic HTN, reflex tachycardia
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phentolamine
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reversible alpha blocker (like irrev phenoxybenzamine) used for pheo
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prazosin
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alpha 1 blocker, used for HTN, urinary retention in BPH
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SE prazosin
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(alpha 1 blocker, used for HTN, urinary retention in BPH) 1st dose orthostatic, dizziness, HA
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mirtazapine
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alpha 2 blocker used for depression
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SE mirtazapine
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(alpha 2 blocker used for depression) sedation, incr chol, incr appetite
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if phentolamine given, then epi what happens to BP
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net decrease (the alpha effect is blocked, so net beta 2 response)
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if phentolamine given, then phenylphrine
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nothing (alpha effect blocked)
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SE beta blockers
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impotence, asthma, bradycardia, AV block, CHF, sedation, sleep, careful in DM
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name nonselective beta blockers
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propanolol, timolol, pindolol
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labetalol
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blocks b1, b2, and alpha 1 (preventing reflex tachycardia)
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name beta 1 selective blockers
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A BEAM=Acebutolol, betaxolol, esmolol (short t1/2), atenolol, metoprolol
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alpha agonists used in glaucoma
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epinephrine and brimonidine
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SE epinephrine in tx glaucoma
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mydriasis, stinging DO NOT USE in closed-angle glaucoma
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tx options for glaucoma (classes of drugs)
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alpha agonist, beta blocker, acetazolamide, cholinomimetics, prostaglandin
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cholinomimetics used tx glaucoma: names (4), mech, SE
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pilocarpine, carbachol, physiostigmine, echothiophate
mech: incr outflow, contract ciliary mscl and open trabecular meshwork SE: miosis, cyclospasm pilocarpine and carbachol direct agonist, others - ACE |
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name prostaglandin used tx glaucoma, mech, SE
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latanoprost, incr outflow, SE: darkens color of iris
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brimonidine
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alpha agonist used in glaucoma to decr aq humor syn (no SE)
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use of acetazolamide beside diuretic
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glaucoma, decr aq humor by decr HCO3 by - carbonic anhydrase
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classes of agents used in PD
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-DA agonist
-MAO inhibitor -anti muscarinic -COMT inhibitor |
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5 ex DA agents used in PD
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Ldopa/carbidopa, bromocriptine, pramipexole, ropinirole, amantadine
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ex MAOI used in PD,
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selegiline, selective MAO B inhibitor
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use benztropine in PD (class, mech, effect)
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antimuscarinic that improves tremor and rigidity, but not bradykinesia
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name COMT inhib used in PD
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entacapone, tolcapone (adjunct to levodopa)
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SE levodopa/carbidopa
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arrhythmia from peripheral conversion to DA, diskinesia (carbidopa inhibits decarboxylase)
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selegiline, mech, use, SE
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used in PD as adjunct to Ldopa, inhibits MAO-B increasing availability of DA,
SE: may enhance adverse effects of L-dopa |
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sumatriptan, use, mech, SE
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5HT1D agonist used in acute migraine or cluster HA
SE: chest discomfort, mild tingling CI: CAD, prinzmetal angina |
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phenytoin MOA
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increases Na channel inactivation--use dependent Na channels
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SE phenytoin
-most mundane -most unique -most dangerous -most annoying -Cb/CNS |
nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, anemias, teratogen, peripheral neuro, rare malignant hyperthermia
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carbamzepine MOA, neuro use
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increase Na channel inactiv for partial sz and tonic clonic generalized
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SE carbamazepine
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1) diplopia, ataxia,
2) agranulocyt, aplastic anemia 3) induce P450, liver toxicity (check LFTs) |
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lamotrigine
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used in partial sz and generalized tonic clonic,
mech: blocks voltage gated Na |
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SE lamotrigine
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(sz med) life threatening rash, Stephen-Johnson
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ethosuximide
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anti-epileptic but only for absence general sz, works by blocking thalamic T type Ca channels
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phenobarbital
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anti-epileptic for partial and general t/c, works by incr GABAa action
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topiramate
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for partial sz only,
mech: block Na channels, increase GABA action |
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gabapentin
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used for partial and general t/c sz
mech: incr GABA release |
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how benzos work in sz? and which sz can they be used for
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mech: increase GABAa action by increasing frequency Cl opening,
use: status epilepsy ONLY |
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SE ethosuximide
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anti-epileptic but only for general sz, works by blocking thalamic T type Ca channels
GI distress, lethargy, HA, urticaria, Stevens-Johnson |
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SE phenobarbital
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anti-epileptic for partial and general t/c, works by incr GABAa action
sedation, induce P450, tolerance, dependence |
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valproic acid
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used in t/c sz and absence sz,
mech increase Na channel inactiv, incr GABA concentration |
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SE valproic acid (3)
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measure LFT, rare but fatal hepatotoxicity
NT defects (spina bifida), GI |
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SE gabapentin
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sedation, mvmt
used for partial and general t/c sz mech: incr GABA release |
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SE topiramate
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sedation, mental dulling, kidney stones, weight loss
for partial sz only, mech: block Na channels, increase GABA action |
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2 uses of phenytoin, mech
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1) sz all partial, t/c general, and status epilepitus
2) IB antiarrhythmic use-dependent blockade of Na channels |
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barbituates, mech and use (3)
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mech: increase duration Cl open, facilitating GABAa action
use: sedative for sz, insomnia, induction anesth (thiopental) |
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thiopental
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barbituate used in induction anesth (IV)
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secobarbital
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barbituate (anything -barbital)
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when are barbituates contraindicated
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prophyrias
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toxicity of barbituates
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dependence, additive depression of CNS w EtOH + respir and cardio depression, induction P450 drug-drug interactions
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benzodiazepines: use, mech
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use: anxity, spasticity, status epilepticus (diazepam), detox (EtOH wdrawal DT)
mech: incr freq of Cl channel for GABAa note: most have long t1/2 and active metabolites |
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toxicity of benzodiazepine
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dependence, additive CNS depression w EtOH, less respir depression and risk of coma than barbituates
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tx OD benzos
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flumazenil (competit antag at GABA R)
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chlordiazepoxide
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a benzo
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antipsychotics name 4
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thioridazine, haloperidol, fluphenazine, chlorpromazine
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use and mech antipsych
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block D2 R
use: schizo, psychosis |
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short acting benzos
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triazolam, oxazepam, midazolam
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evolution EPS SE
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4h acute dystonia
4d akinesia 4wk akathisia 4mo tradive dyskinesia (irrev) |
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general toxicity of antipsych
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EPS, sedation, endo, SE from blocking muscarinic, alpha and His R
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toxicity (syndrome) of antipsych
and tx? |
1) Neuroeleptic malignant syndrome-rigidity, auto instability, hyperpyrexia
tx: dantrolene and D agonist |
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mech tardive dyskinesia
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oral facial mvmt due to D R sensitization long term anti-psych use
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name atypical antipsych
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clozapine, olanzapine, risperidone
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fluphenazine
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an anti-psych
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thioridazine
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anti psych
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chlorpromazine
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anti psych
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olanzapine
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atypical anti psych used for schizo, as well as OCD, anxiety, depression,
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mech atypical anti psych
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block 5HT2 and D R
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advantages of atypical anti psych
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useful for + and - sx
fewer EPS, antichol |
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SE atypical anti-psych
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fewer EPS and antichol, clozapine requires wkly WBC bc agranulocytosis
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Lithium, mech and use
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mech: ? inhibits phosphoinositol cascade
use: bipolar, acute/relapse mania |
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SE Lithium (4)
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tremor, hypothyroid, polyuria (nephrogenic DI), teratogen.
narrow therapeutic range requires close monitor serum levels |
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Citalopram
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SSRI
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Sertraline
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SSRI
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toxicity of SSRI
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CNS stim, anxiety, insomnia, tremor, anorexia, N/V
-Serotonin syndrome w MAOI (hyperthermia, mscl rigidity, CVS collapse) |
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serotonin syndrome
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SSRI + MAOI (hyperthermia, mscl rigidity, CVS collapse)
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name 4 SSRIs
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fluoxetine, sertraline, paroxetine, citalopram
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takes how long for SSRI to work?
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2-3 wks
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mech and use TCA
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mech: block reuptake NE, serotonin
use: depression, bedwet (imipramine), OCD (clomipramine) |
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doxepin
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TCA
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clomipramine
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TCA also for OCD
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desipramine
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TCA, least sedating
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nortriptyline
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2 TCA (less anti-chol than 3TCA)
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amitriptyline
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3 TCA, with more anti chol than 2 TCA
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toxicity of TCAs
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convulsions, coma, cardiotoxicity (arrhythmias), respir depression, hyperpyrexia.
elderly: confusion, hallucinations (2/2 anti chol) |
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trazodone
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heterocyclic used in depression, inhibits serotonin
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SE trazodone
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sedation, nausea, priapism, hypotension
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buproprion
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heterocyclic, mech unknown, used for depression and smoking cessation
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SE buproprion
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stimulant (tachycardia, agitation), dry mouth, aggravation of psychosis
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venlafaxine
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heterocyclic, inhibit serotonin, NE, and D reuptake, use depression and general anxiety disorder
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SE venlafaxine
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stimulant (anxiety, agitation, HA, insomnia)
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mirtazapine, mech
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alpha 2 agonist (incr NE, serotonin, potent 5HT2 antagonist)
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SE mirtazapine
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sedation, incr cholesterol and appetite
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maprotiline
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heterocyclic blocks NE uptake use in depression
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tranylcypromine
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MAOI for atypical depression (w pyschotic, phobias) anxiety, hypochondriasis
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phenelzine
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MAOI for atypical depression (w pyschotic, phobias) anxiety, hypochondriasis
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name 2 MAOI, use
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tranylcypromine, phenelzine
MAOI for atypical depression (w pyschotic, phobias) anxiety, hypochondriasis |
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SE MAOI
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HTN crisis w tyramine and meperidine, CNS stim
contraindicated w SSRI, b agonist!!! |