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140 Cards in this Set

  • Front
  • Back
mechanism and effect of guanethidine
inhibits NE vesicle fusion/release (net decrease in NE)
name modulating receptors on noadrenergic terminal
alpha 2, angiotensin II, and M1 (Ach)
bethanechol
cholinomimetric direct agonist on bowel and bladder s.m., used for post-op and neurogenic ileus and urinary retention
carbachol
direct cholinomimetic agonist, activates ciliary muscle of eye (open angle glaucoma) and pupillary sphincter (narrow angle glaucoma)
pilocarpine
direct cholinomimetic agonist, activates ciliary muscle of eye (open angle glaucoma) and pupillary sphincter (narrow angle glaucoma)
neostigmine (3)
anti CE, used for post-op ileus and urinary retention, MG, reversal NMJ block
pyridostigmine
anti CE used for MG
edrophonium
dx of MG (anti CE short t1/2)
physiostigmine
anti CE, used for glaucoma (crosses BBB) and atropine OD
echothiophate
glaucoma, anti CE
parathion
an organoP (poison CE), causing DUMBBLESS (diarrhea, urination, miosis, bronchospasm, bradycardia, excitation mscl and CNS, lacrimation, sweating, salivation, abd cramp)
antidote to organoP
atropine (muscarinic antag) and pralidoxime (regenerates CE)
effects of atropine, used to tx
dilate eye, decr GI acid, motility, decr respir sxns, treat organoP
what use for atropine OD
physistigmine (anti CE)
tx MG
dx with edrophonium, tx with neostigmine, pyridostigmine
muscarinic cholinoR blockers include
atropine, beztropine (PD), scopolamine (motion sickness), ipratropium (asthma, COPD)
SE of atropine
hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter (
cause pupil to dilate (2meds and their R)
alpha 1 phenylphrine, and antiAch stropine
ephedrine
indirect general symp agonist used for nasal decongestion, urinary incontinence, and hypotension
phenylphrine
alpha 1>alpha2 sympath, dilates pupil, vasoconstrict, nasal decongestion
clonidine
central acting alpha agonist decr adrenergic outflow, used for HTN, esp in renal disease (maintains renal BF) and in preg
alpha-methyldopa
central acting alpha agonist decr adrenergic outflow, used for HTN, esp in renal disease (maintains renal BF) and in preg
cocaine
general sympathomimetic, inhibits uptake , causing vasoconstriction and local anesthesia
amphetamine
indirect general sympathomimetric used for narcolepsy, obesity, ADD
epinephrine acts on which R
all (alpha1,2, and beta1,2)
effect BP epinephrine
incr SBP, decr DBP, MAP maintained
use of epinephrine
anaphylaxis, glaucoma open angle, asthma, hypotension (maintain RBF)
NE acts on which R
alpha 1,2 and beta1
effect BP NE
all increase, with reflex bradycardia
hexamethonium
nicotinic Ach R blocker, used to prevent reflex bradycardia from NE
dopamine acts on which R
D1=D2>beta>alpha
effect alpha 1 R
-vasoconstriction GI
-mydriasis
-GI sphincter contraction
-ejac
effect alpha 2 R (3)
-presynapt - NE release and para Ach
-insulin
-decr aq humor of eye
effect beta 1 (4)
-heart incr rate and contractility
-renin
-aq humor
-incr lipolysis
effect beta 2
-vasodilation skel muscle
-allow BF organs
-relax bronchi and GI
-uterus
-glucagon
-epi on beta 2 + NE release
effect beta 3
adipose
receptor control of aq humor, alpha and beta effect
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
control of insulin/glucagon by adrenergic receptors
alpha 2 controls insulin, beta 2 controls glucagon
name neuro path for symp
symp pregang rel Ach binds nicotinic R which rel NE on adrenergic R
name path for parasymp
para pregang release Ach on nicotinic R which releases Ach on muscarinic R
name path for somatic
(no ganglia) Ach released on nictonic R on striated muscle
receptors dobutamine act on, use
beta1>beta2, used in CHF and shock
phenoxybenzamine
irrev alpha blocker, used for pheo
SE phenoxybenzamine
(irrev alpha blocker, used for pheo) orthostatic HTN, reflex tachycardia
phentolamine
reversible alpha blocker (like irrev phenoxybenzamine) used for pheo
prazosin
alpha 1 blocker, used for HTN, urinary retention in BPH
SE prazosin
(alpha 1 blocker, used for HTN, urinary retention in BPH) 1st dose orthostatic, dizziness, HA
mirtazapine
alpha 2 blocker used for depression
SE mirtazapine
(alpha 2 blocker used for depression) sedation, incr chol, incr appetite
if phentolamine given, then epi what happens to BP
net decrease (the alpha effect is blocked, so net beta 2 response)
if phentolamine given, then phenylphrine
nothing (alpha effect blocked)
SE beta blockers
impotence, asthma, bradycardia, AV block, CHF, sedation, sleep, careful in DM
name nonselective beta blockers
propanolol, timolol, pindolol
labetalol
blocks b1, b2, and alpha 1 (preventing reflex tachycardia)
name beta 1 selective blockers
A BEAM=Acebutolol, betaxolol, esmolol (short t1/2), atenolol, metoprolol
alpha agonists used in glaucoma
epinephrine and brimonidine
SE epinephrine in tx glaucoma
mydriasis, stinging DO NOT USE in closed-angle glaucoma
tx options for glaucoma (classes of drugs)
alpha agonist, beta blocker, acetazolamide, cholinomimetics, prostaglandin
cholinomimetics used tx glaucoma: names (4), mech, SE
pilocarpine, carbachol, physiostigmine, echothiophate
mech: incr outflow, contract ciliary mscl and open trabecular meshwork
SE: miosis, cyclospasm

pilocarpine and carbachol direct agonist, others - ACE
name prostaglandin used tx glaucoma, mech, SE
latanoprost, incr outflow, SE: darkens color of iris
brimonidine
alpha agonist used in glaucoma to decr aq humor syn (no SE)
use of acetazolamide beside diuretic
glaucoma, decr aq humor by decr HCO3 by - carbonic anhydrase
classes of agents used in PD
-DA agonist
-MAO inhibitor
-anti muscarinic
-COMT inhibitor
5 ex DA agents used in PD
Ldopa/carbidopa, bromocriptine, pramipexole, ropinirole, amantadine
ex MAOI used in PD,
selegiline, selective MAO B inhibitor
use benztropine in PD (class, mech, effect)
antimuscarinic that improves tremor and rigidity, but not bradykinesia
name COMT inhib used in PD
entacapone, tolcapone (adjunct to levodopa)
SE levodopa/carbidopa
arrhythmia from peripheral conversion to DA, diskinesia (carbidopa inhibits decarboxylase)
selegiline, mech, use, SE
used in PD as adjunct to Ldopa, inhibits MAO-B increasing availability of DA,
SE: may enhance adverse effects of L-dopa
sumatriptan, use, mech, SE
5HT1D agonist used in acute migraine or cluster HA
SE: chest discomfort, mild tingling
CI: CAD, prinzmetal angina
phenytoin MOA
increases Na channel inactivation--use dependent Na channels
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
carbamzepine MOA, neuro use
increase Na channel inactiv for partial sz and tonic clonic generalized
SE carbamazepine
1) diplopia, ataxia,
2) agranulocyt, aplastic anemia
3) induce P450, liver toxicity
(check LFTs)
lamotrigine
used in partial sz and generalized tonic clonic,
mech: blocks voltage gated Na
SE lamotrigine
(sz med) life threatening rash, Stephen-Johnson
ethosuximide
anti-epileptic but only for absence general sz, works by blocking thalamic T type Ca channels
phenobarbital
anti-epileptic for partial and general t/c, works by incr GABAa action
topiramate
for partial sz only,
mech: block Na channels, increase GABA action
gabapentin
used for partial and general t/c sz
mech: incr GABA release
how benzos work in sz? and which sz can they be used for
mech: increase GABAa action by increasing frequency Cl opening,
use: status epilepsy ONLY
SE ethosuximide
anti-epileptic but only for general sz, works by blocking thalamic T type Ca channels
GI distress, lethargy, HA, urticaria, Stevens-Johnson
SE phenobarbital
anti-epileptic for partial and general t/c, works by incr GABAa action
sedation, induce P450, tolerance, dependence
valproic acid
used in t/c sz and absence sz,
mech increase Na channel inactiv, incr GABA concentration
SE valproic acid (3)
measure LFT, rare but fatal hepatotoxicity
NT defects (spina bifida), GI
SE gabapentin
sedation, mvmt
used for partial and general t/c sz
mech: incr GABA release
SE topiramate
sedation, mental dulling, kidney stones, weight loss
for partial sz only,
mech: block Na channels, increase GABA action
2 uses of phenytoin, mech
1) sz all partial, t/c general, and status epilepitus
2) IB antiarrhythmic
use-dependent blockade of Na channels
barbituates, mech and use (3)
mech: increase duration Cl open, facilitating GABAa action
use: sedative for sz, insomnia, induction anesth (thiopental)
thiopental
barbituate used in induction anesth (IV)
secobarbital
barbituate (anything -barbital)
when are barbituates contraindicated
prophyrias
toxicity of barbituates
dependence, additive depression of CNS w EtOH + respir and cardio depression, induction P450 drug-drug interactions
benzodiazepines: use, mech
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
toxicity of benzodiazepine
dependence, additive CNS depression w EtOH, less respir depression and risk of coma than barbituates
tx OD benzos
flumazenil (competit antag at GABA R)
chlordiazepoxide
a benzo
antipsychotics name 4
thioridazine, haloperidol, fluphenazine, chlorpromazine
use and mech antipsych
block D2 R
use: schizo, psychosis
short acting benzos
triazolam, oxazepam, midazolam
evolution EPS SE
4h acute dystonia
4d akinesia
4wk akathisia
4mo tradive dyskinesia (irrev)
general toxicity of antipsych
EPS, sedation, endo, SE from blocking muscarinic, alpha and His R
toxicity (syndrome) of antipsych
and tx?
1) Neuroeleptic malignant syndrome-rigidity, auto instability, hyperpyrexia
tx: dantrolene and D agonist
mech tardive dyskinesia
oral facial mvmt due to D R sensitization long term anti-psych use
name atypical antipsych
clozapine, olanzapine, risperidone
fluphenazine
an anti-psych
thioridazine
anti psych
chlorpromazine
anti psych
olanzapine
atypical anti psych used for schizo, as well as OCD, anxiety, depression,
mech atypical anti psych
block 5HT2 and D R
advantages of atypical anti psych
useful for + and - sx
fewer EPS, antichol
SE atypical anti-psych
fewer EPS and antichol, clozapine requires wkly WBC bc agranulocytosis
Lithium, mech and use
mech: ? inhibits phosphoinositol cascade
use: bipolar, acute/relapse mania
SE Lithium (4)
tremor, hypothyroid, polyuria (nephrogenic DI), teratogen.
narrow therapeutic range requires close monitor serum levels
Citalopram
SSRI
Sertraline
SSRI
toxicity of SSRI
CNS stim, anxiety, insomnia, tremor, anorexia, N/V
-Serotonin syndrome w MAOI (hyperthermia, mscl rigidity, CVS collapse)
serotonin syndrome
SSRI + MAOI (hyperthermia, mscl rigidity, CVS collapse)
name 4 SSRIs
fluoxetine, sertraline, paroxetine, citalopram
takes how long for SSRI to work?
2-3 wks
mech and use TCA
mech: block reuptake NE, serotonin
use: depression, bedwet (imipramine), OCD (clomipramine)
doxepin
TCA
clomipramine
TCA also for OCD
desipramine
TCA, least sedating
nortriptyline
2 TCA (less anti-chol than 3TCA)
amitriptyline
3 TCA, with more anti chol than 2 TCA
toxicity of TCAs
convulsions, coma, cardiotoxicity (arrhythmias), respir depression, hyperpyrexia.
elderly: confusion, hallucinations (2/2 anti chol)
trazodone
heterocyclic used in depression, inhibits serotonin
SE trazodone
sedation, nausea, priapism, hypotension
buproprion
heterocyclic, mech unknown, used for depression and smoking cessation
SE buproprion
stimulant (tachycardia, agitation), dry mouth, aggravation of psychosis
venlafaxine
heterocyclic, inhibit serotonin, NE, and D reuptake, use depression and general anxiety disorder
SE venlafaxine
stimulant (anxiety, agitation, HA, insomnia)
mirtazapine, mech
alpha 2 agonist (incr NE, serotonin, potent 5HT2 antagonist)
SE mirtazapine
sedation, incr cholesterol and appetite
maprotiline
heterocyclic blocks NE uptake use in depression
tranylcypromine
MAOI for atypical depression (w pyschotic, phobias) anxiety, hypochondriasis
phenelzine
MAOI for atypical depression (w pyschotic, phobias) anxiety, hypochondriasis
name 2 MAOI, use
tranylcypromine, phenelzine
MAOI for atypical depression (w pyschotic, phobias) anxiety, hypochondriasis
SE MAOI
HTN crisis w tyramine and meperidine, CNS stim
contraindicated w SSRI, b agonist!!!