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117 Cards in this Set
- Front
- Back
- 3rd side (hint)
vmax is directly proportional to
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enzyme conc
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as you decr Km, you _____ affinity
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incr
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as you incr y-intercept, you _____ vmax
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decr
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the further to the right the x intercept is, the _______ Km
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greater
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effect of inhibitors on vmax
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comp inhib: unchanged
noncomp: decr |
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effect of inhibitors on Km
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comp inhib: incr
noncomp: unchanged |
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clearance
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rate of elimination of drug divided by plasma drug conc
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half-life
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0.7 x Vd divided by CL
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in renal/liver dz, maintenance dose is ______ and loading dose is ________
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decr, unchanged
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freq of dosing is affected by
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half life
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zero-order
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Cp decrease linearly with time. phenytoin, ethanol, aspirin
PEA |
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first order
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constant fraction of drug
Cp decr exponentially with time |
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ionization and drug excretion
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ionized species are trapped in urine and cleared quickly
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trapped in basic environments
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phenobarbital, mtx, asa (acids)
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trapped in acid
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amphetamines (base). treat OD with ammonium chloride
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p450
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makes things slightly polar, often still active
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phase II conjugation
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makes things very polar, inactive metabolites
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flumazenil is what kind of inhibitor at GABA
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competitive
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phenoxybenzamine and NE are what kind of inhibitors at alpha receptors
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noncomp
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morphine and buprenorphine are what kind of inhibitors at opioid receptors
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partial agonists
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safer drugs have ______TI values
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higher
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sympathetic sweat gland innervation
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M ACh
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D1 receptors
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sympathetic. renal vascular smooth muscle
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skeletal muscle innervation
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N ACh
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adrenal medulla innervation
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Ach (but sympathetic)
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nicotinic Ach receptors
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ligand-gated Na/K channels
Nn in autonomic ganglia Nm in NMJ |
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alpha 1 receptors
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incr vasc SM contract,incr pupillary dilator muscle contract (mydriasis), incr intestinal and bladder sphincter muscle contract
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alpha 2 receptors
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decr symp outflow, decr insulin release
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beta 1
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incr renin, incr lipolysis
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beta 2
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vasodil, bronchodil, incr HR, incr contract, incr lipolysis, incr insulin release, decr uterine tone
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M1
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CNS, enteric nervous system
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M2
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decr HR and contract of atria
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M3
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incr exocrine, incr peristalsis, incr bladder contract, bronchoconstric, incr pupillary sphincter muscle contract (miosis), cililary muscle contract (accommodation)
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MAD 2s
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Gi
M2, alpha 2, D2 |
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hemicholinium
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inhibits choline uptake
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vesamicol
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inhibits acetyl CoA + choline
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release of NE from symp nerve modulated by
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NE acting on alpha 2
ACh ATII |
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Carbachol
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glaucoma, pupillary contraction, relief of IOP
cholinomimetic |
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cholinomimetics
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-Chol
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pilocarpine
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cholinomimetic
potent stimulator of sweat, tears, saliva contracts ciliary muscle of eye (open angle) and pupillary sphincter (narrow angle) |
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methacholine
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cholinomimetic
challenge test to dx asthma |
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anticholinesterases
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-stigmine
watch for exacerbation of COPD, asthma, PUD |
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neostigmine
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postop/neurogenic ileus and urinary retention, myasthenia gravis, reversal of postop NMJ block
anticholinesterases |
NEO CNS + NO CNS
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pyRIDostigmine
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long acting, myasthenia gravis
anticholinesterases |
get RID of myasthenia gravis
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edrophonium
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dx myasthenia gravis (short)
anticholinesterases |
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PHYsostigmine
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glaucoma and atropine OD
anticholinesterases |
crosses BBB. PHYxes atropine OD. PHEYES.
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echothiophate
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glaucoma
anticholinesterases |
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donepezil
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AD
anticholinesterases |
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anticholinesterase poisoning
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organophosphates (irreversible)
excitation of skeletal muscle and CNS, and parasym sx |
antidote is atropine and pralidoxime
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atropine
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mydriasis, cycloplegia
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antimuscarinic
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antimuscarinics
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-trop
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oxybutynin, glcopyrrolate
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antimuscarinic
reduce bladder spasms |
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methscopolamine, pirenzepine, propantheline
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antimuscarinic
peptic ulcers |
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atropine tox
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acute angle closure glaucoma
hot as a hare dry as a bone red as a beet blind as a bat mad as a hatter |
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norepinephrine prefers
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alpha receptors
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isoproterenol prefers
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beta receptors
rare AV block sympathomimetic |
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dopamine prefers
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D1>beta>alpha
ionotropic, chronotropic sympathomimetic |
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dubutamine prefers
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beta 1
heart failure, cardiac stress testing, ionotropic but not chronotropic sympathomimetic |
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phenylephrine prefers
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alpha 1
pupillary dilation, vasoconstrict, nasal decongest sympathomimetic |
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metaproterenol, albuterol, salmeterol
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sympathomimetic
prefers beta 2 M/A acute asthma |
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terbutaline, ritodrine
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prefer beta 2.
sympathomimetic reduce premature uterine contractions |
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amphetamine
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releases stored catecholamines
use: narcolepsy, obesity, ADD |
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ephedrine
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releases stored catecholamines
use: hypotension, urinary incontinence |
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cocaine
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indirect general agonist, uptake inhibitor
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clonidine, alpha methyldopa
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alpha 2 agonists
use: htn, esp with renal dz |
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phenoxybenzamine
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irreversible nonselective alpha blocker.
for pheo tox: ortho hypo, reflex tachy |
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phentolamine
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reversible nonselective alpha blocker
use: MAOi pts who eat tyramine |
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prazosin, terazosin, doxazosin
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alpha 1 blockers
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mirtazapine
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alpha 2 blocker.
use: depression tox: sedation, incr chol, incr appetite |
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autonomic drugs for SVTs
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propranolol, esmolol
decr AV conduction velocity |
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beta blocker for glaucoma
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timolol
decr secretion of aqueous humor |
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beta blocker toxicity
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impotence, asthma exacerbation, AV block, CHF, sedation, caution in diabetics
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A BEAM of beta blockers
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beta 1 selectives
acebutolol (partial agonist) betaxolol esmolol (short) atenolol metoprolol |
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Please Try Not Being Picky
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nonselective antagonists
Propranolol Timolol Ndolol Pindolol |
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nonselective alpha and beta antags (vasodil)
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carvedilol
labetalol |
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partial beta agonists
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pindolol
acebutolol PAPA |
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tylenol antidote
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N-acetylcysteine (replenishes glutathione)
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salicylate antidote
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NaHCO3 (alkalinize urine)
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beta blocker antidote
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glucagon
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digitalis antidote
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normalize K, lidocaine, Mg, anti dig Fab
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lead, Hg, arsenic, gold, copper antidote
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CaEDTA (lead only), dimercaprol (not Cu), succimer (not Cu), penicillamine (not mercury)
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cyanide antidote
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nitrite, hydroxycobalamin, thiosulfate
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TCA antidote
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NaHCO3 (plama alkalinization)
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tPA, streptokinase antidote
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aminocaproic acid
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theophylline antidote
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beta blocker
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can cause torsades de pointes
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class III (sotalol)
class IA (quinidine) |
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Agranulocytosis Could Certainly Cause Pretty Major Damage
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Agranulocytosis
Clozapine Carbamazepine Colchicine PTU Methimazole Dapsone |
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Aplastic anemia
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Chloramphenicol
benzene NSAID PTU methimazole |
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coombs pos hemolytic anemia
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methyldopa
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hemolysis in G6PD
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aspirin, ibuprofen, nitrofurantoin, INH
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megaloblastic anemia
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phenytoin, mtx, sulfa
have a blast with PMS |
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focal to massive hepatic necrosis
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halothane, acetaminophen, valproic acid, amanita phalloides
liver HAVAc |
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hepatitis
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INH
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hypothyroidism
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lithium, amiodarone, sulfas
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hyperglycemia
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niacin, tacrolimus, protease inhibitors
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fat redistribution
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protease inhibitors
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ginigival hyperplasia
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phenytoin, verapamil
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gout
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lasix, hctz, niacin, cyclosporin, pyrazinamide
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myopathy
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Fish N CHIPS Give you myopathies
Fibrates, Niacin, Colchicine, Hydroxycholoroquine, Interferona, Penicillinamine, Statins, Glucocorticoids |
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osteoporosis
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heparin
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photosen
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SAT for photo
sulfa, amiodarone, tetra |
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Stevens Johnson
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anti-convulsives
sulfa allopurinol PCN |
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DI
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lithium, demeclocycline
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fanconi
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expired tetra
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interstitial nephritis
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methicillin, NSAID, furosemide
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hemorrhagic cystitis
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cyclophosphamide, ifosfamide (give mesna to prevent)
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SIADH
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carbamazepine
cyclophosphamide |
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cinchonism
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quinidine
quinine |
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parkinsons
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reserpine
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seizures
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imipenem/cilastatin
INH |
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antimuscarinic
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TCA, H1blockers, neuroleptics, dig
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disulfiram
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cephalos, procarbazine, 1st gen sulfonylureas
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nephro/oto
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vanco, loops, cisplatin
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p450 inducers
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quinidine
barbituates st johns wort phenytoin refampin griseofulvin carbamazepine chronic alcohol |
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p450 inhibitors
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MAGIC RACK
macrolides, amiodarone, grapefruit, INH, cimitidine, ritonavir, acute alcohol, cipro, ketoconazole, sulfas |
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sulfas
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probenecid, acetazolamide, celecoxib
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-azines
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phenothiazines. neuroleptics, antiemetics
ie. chlorpromazine |
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