Pharm (A/Q) Flashcards
(167 cards)
Measures the affinity of an enzyme for its substrate ( dec Km = inc affinity)
Km
Maximal velocity of an enzymatic reaction (proportional to enzyme concentration)
Vmax
Does not change Vmax (Lineweaver-Burke lines cross each other “competitively”)
Competitive inhibition
Decreases Vmax (Lineweaver-Burke lines do not cross each other)
Noncompetitive inhibition
Drug in body / plasma drug concentration (low Vd (4-8L: in blood)’ medium Vd (in extracellular space)’ High Vd (> body weight: in tissues))
Volume of Distribution (Vd)
Rate of elimination of drug / plasma drug concentration (OR Vd x Kc’ where Kc is the elimination constant)
Clearance (CL)
T1/2 = (0.7 x Vd) / CL
Half life (t1/2)
1:50%’ 2:75%’ 3:87.5%’ 4:93.75%
Concentration of a substance after X half lives (1’2’3’4)
”= Cp x (Vd / F); (Cp: target plasma conc., F: bioavailability, 1 if by IV)
Loading dose
”= Cp x (CL / F); (Cp: target plasma conc., F: bioavailability, 1 if by IV; a renal patient would have decreased clearance, so they would need a decreased maintenance dose)
Maintenance dose
PEA (phenytoin, ethanol, aspirin)
Common drugs that follow zero-order elimination
Will get trapped in a basic environment, treat with bicarbonate
Treating a weak acid overdose
Will get trapped in an acidic environment, treat with ammonium chloride
Treating a weak base overdose
(Cytochrome P450) 1. reduction, 2. oxidation, 3. hydrolysis (drugs became slightly polarized, may still be active)
Reactions involved in phase I drug metabolism
(Conjugation) 1. acetylation, 2. glucuronidation, 3. sulfonation (drugs become very polarized, are inactivated)
Reactions involved in phase II drug metabolism
Competitive antagonist shifts curve right, requires bigger dose of drug for effect (inc EC50); noncompetitive antagonist shortens curve, cannot reach same level of effect (dec efficacy)
Effect of competitive antagonists on efficacy curves versus noncompetitive antagonists
Partial agonists will have a lower maximal efficacy than full agonists (however potency is independent, they may still be more potent or less potent than a full agonist)
Effect of partial agonists versus full agnoists on efficacy curves
TILE: TI = LD50 / ED50 (median toxic dose / median effective dose; Safer drugs have HIGHER TI values)
Therapeutic index (TI)
Receptor location: NMJ; Function: skeletal muscle contraction; Mechanism: ion channel (Na influx)
Nm receptors
Receptor location: Ganglia; Function: stimulates sympathetics and parasympathetics; Mechanism: ion channel (Na influx);
Nn receptors
Receptor location: Nerve endings; Function: Gastric acid secretion; Mechanism: Gq protein;
M1 receptors
Receptor location: Heart; Function: Inhibitory, reduces heart rate; Mechanism: Gi protein;
M2 receptors
Receptor location: Smooth muscle, endothelium, glands; Function: bronchoconstriction, pupil constriction, accommodation, increases secretions; Mechanism: Gq proteins;
M3 receptors
Receptor location: Arterioles, glands; Function: vasoconstriction, pupillary dilation; Mechanism: Gq protein;
a1