laracrystalo's version from 2015-06-09 21:42


Question Answer
Vmax is related toIncrease Vmax --> increased EFFICACY
Km is related toAffinity and Potency. Increase Km --> decreased POTENCY (and decreased affinity)
relationship between Potency, EC50 and MAC?Increase potency --> decreased EC50 and decreased MAC
competitive inhibitors affectPOTENCY. Competitive inhibitors increase the Km and decrease the potency (shift R on curve)
noncompetitive inhibitors affectEFFICACY. Noncompetitive inhibitors decrease Vmax and decrease Efficacy (shift down on graph)
competitive inhibitors have no effect onVmax and efficacy
noncompetitive inhibitors have no effect onKm and potency
partial agonists affectdecrease the EFFICACY (decrease Vmax)
what kinds of factors affect Vd?obese people, pregnant people, and people with hypoalbuminemia have higher Vds!
if protein binding is decreased, then Vd is?increased
Low Vd drugs go where?Blood
Mid Vd drugs go where?ECF
High Vd drugs go where?all tissues
zero orderconstant AMOUNT is eliminated, the line goes down to 0 (phenytoin, ethanol, aspirin, heparin). CAPACITY LIMITED
first ordermost drugs. constant FRACTION is eliminated, the line never gets to zero. FLOW DEPENDENT
loading doseCp x Vd / (F) --> this is affected by changing in protein binding. Stays the same in most cases.
maintenance doseCp x CL x time / (F) --> this is affected by changes in metabolism, so fast acetylators need higher maintenance doses and renal or hepatic disease needs lower maintenance doses
who needs higher maintenance doses?fast acetylators
who needs lower maintenance doses?slow acetylators, people with renal or hepatic disease
who needs a lower loading dose?people with hypoalbuminemia
what phase are toxins often turned into carcinogens?phase I
where does phase I happen?SER of hepatocytes
where does phase II happen?cytoplasm of hepatocytes
therapeutic index?toxic dose / effective dose --> higher TI is safer
drugs with low TI?lithium, digoxin, theophylline, warfarin
phase I yields what kinds of metabolites?partially active and slightly polar
phase II yields what kinds of metabolites?very polar and inactive
what phase decreases in the elderly?phase I
half life formula?T1/2 = 0.7 x Vd / (CL)
half life with discontinuing IV?50% --> 25% --> 12.5% --> 6.25%
half life with continuous IV?50% --> 75% --> 87.5% --> 94% --> 97%
low blood solubility meansrapid induction and recovery, lower AV gradient (this is the same as lower ionized form and blood/gas coefficient)
high lipid solubility meanshigher potency (lower MAC)
AV gradient reflectstissue solubility. higher AV gradient means slower induction (higher blood solubility)
NO islow lipid low blood --> low potency, rapid onset
halothane is high lipid high blood --> high potency, slow onset


Question Answer
blue-green color visionsildenafil
yellow color vision changedigxin
red-green color vision changeethambutol

Autonomic drugs - a functions-based approach

Question Answer
↑ vascular smooth muscle contractionα1, V1
↑ pupillary dilator muscle contraction (mydriasis)α1
↑ intestinal and bladder sphincter muscle contractionα1
↓ sympathetic outflowα2
↓ insulin releaseα2
↓ lipolysisα2
↑ platelet aggregationα2
↑ HRβ1, β2
↑ contractilityβ1, β2
↑ renin releaseβ1
↑ lipolysisβ1, β2
↓ uterine tone (tocolysis)β2
Ciliary muscle relaxationβ2
↑ aqueous humor productionβ2
CNS stimulationM1
Eneteric nervous system stimulationM1
↓ HRM2
↓ contractilityM2
↑ exocrine gland secretions (lacrimal, gastric acid)M3, H2 (gastric acid)
↑ gut peristalsisM3
↑ bladder contractionM3
BronchoconstrictionM3, H1
↑ pupillary sphincter muscle contraction (miosis)M3
Ciliary muscle contraction (accommodation)M3
Relaxes renal vascular smooth muscleD1
Modulates transmitter release, esp. in brainD2
↑ nasal and bronchial mucus productionH1
↑ H20 permeability/resorption in the collecting tubules of the kidneyV2


Question Answer
Gs does what?↑ AC --> ↑ cAMP --> ↑ PKA --> increase Ca++ concentration --> cardiac muscle contraction
Gi does what?↓ AC --> ↓ cAMP --> ↓ PKA --> inhibition of MLCK --> smooth muscle relax
what does Gq do?↑ PLC --> cleaves PiP2 --> ↑ IP3 and ↑ DAG
what does IP3 do?increase Ca++ concentration --> Ca++ - calmodulin --> smooth muscle contraction
what does DAG do?↑ PKC
high dose dopamine effect?increase Bp
low dose dopamine effect?increase RBF
isoproterenol effect?decrease Bp, increase HR
NE effect?increase Bp, decrease HR
Epi effect?increase HR
reversal of Epi?prazosin
dobutamine effect?increase HR and increase bp

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