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41 Cards in this Set
- Front
- Back
Km
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reflects the affinity of the enzyme for its substrate; lower Km corresponds with incr affinity
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Vmax is proportional to what
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the enzyme concentration
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the velocity of a reaction is dependent on which 3 things
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concentration of enzyme, substrate and product
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effects of competitive vs. noncompetitive inhibitors
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competitive: have no effect on Vmax and incr Km, the lines also cross on a graph; non-compet: decr Vmac, no change on Km, don't cross on a graph
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vol of distribution
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Vd= amount of drug in body/plasma drug concentration
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where do drugs with low, med and high Vd distribute
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low: blood; med: extracellular space, body water; high: tissues
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drug clearence
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relates the rate of elimination to the plasma concentration; CL = rate of elimination/plasma drug concentration = Vd X Ke (elimination constant)
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how many half lifes must a drug be infused at a constant rate to achieve 94% of steady state
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4
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half life equation
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t1/2 = (0.7xVd)/CL
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bioavailability
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fraction of an administered drug that reaches the systemic circulation in a chemically unchanged form
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loading dose
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LD=(Cp x Vd)/F Cp is target plasma concentration, F is bioavailability
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maintenence dose
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MD = (Cp x CL)/F Cp is target plasma concentration, F is bioavailability
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changes in maintenece or loading doses in pts with renal or hepatic function
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decr maintenece, same loading
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zero order elimination and 3 examples
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rate of elimination is constant, regardless of C (constant amount of drug eliminated per unit time); Ex: phenytoin, ethanol, aspirin
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phase I vs. phase II metablism
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phase I: P450, reduction, oxidation, hydrolysis, usually yields slightly polar water soluble metablites which are often active still, this is lost first in geriatric pts; phase II: (conjugation) acetylation, glucuronidation, sulfation, usually yields very polar inactive metabolites which are renally excreted
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efficacy vs. potency
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efficacy: max effect a drug can produce (decr by noncompet antagonist); potency: amount of drug needed for a given effect (decr by competitive antagonist)
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partial agonist
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has a lower maximal efficacy as a full agonist, can have incr, decr or equal potency (its independent)
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therapeutic index
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TI=LD50 (median toxic dose)/ED50 (median effective dose); safer drugs have higher TI values
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what type of receptors are preganglionic SNS
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ACh N, PNS and D1 also
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what type of receptors are NACh and MACh
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NACh: ligand gated Na/K channels; MACh: G-protein coupled
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which adrenergic receptor is responsible for incr renin release
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B1
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which histamine receptor is responsible for pruritis and vessel permeability
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H1
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phospholipase C
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is activated by Gq 2nd messangers, converts lipids into PIP2 which breaks down into IP3 (which incr Ca) and DAG (activtes PKC)
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protein kinase A
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is activated by incr levels of cAMP and vice versa
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nonselective B blockers (5)
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propanalol, timolol, naldolol, pindolol, labetelol
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B1 selective blockers (5)
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"A BEAM" acebutolol (partial agonist), betaxolol, esmolol, atenolol, metoprolol
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non selective a and b blockers (2)
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carvedilol, labetelol
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partial B agonsts (of b blockers), (2)
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pindolol, acebutalol
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findings in lead poisoning
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lead lines on gingivae and on epiphysis of long bones (only heavy metal that can deposit here), encephalopathy and cerebral edema (related to incr vessel permeability and ALA build up which is toxic to neurons), RBC basophilic stippling, abdominal coloc, sideroblastic anemia, wrist and foot drops (causes demyelination), N/V
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P450 inducers (8)
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"Bosten Red Soxs Gotta Play Quality Competitions" to go up: barbituates, rifampin, St Johns wart, griseosulvin, phenytoin/phenobarbital, quinidine, carbamezepine
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P450 inhibitors (8)
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"I C(see) KEGS" going down: INH, cimentidine/cipro, Ketoconzale, erythromycin, grapefruit, sulfonamides
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drugs that cause SLE like syndrome (4)
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Its not HIPP to have lupus: hydralazine, INH, phenytoin, procainamide
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drug that causes tendonitis/tendon rupture/cartilage damage
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fluroquinilones
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drugs that cause coronary vasospasm (2)
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cocaine, sumatriptan (migraines)
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which drugs cause cutaneous flushing (4)
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niacin, Ca channel blockers, adenosine, vanco
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which drugs cause agranulocytosis (5)
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C3: clozapine, carbamexepine, colchicine; plus propythiouriil and methimazole
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drugs that cause pulm fibrosis
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bleomycin, busulfan, amiodarone
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what drug causes acute cholestatic hepatitis
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macrolides
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which drugs cause gynecomastia (5)
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"some drugs cause awesome knockers": spironolactone, digitalis, cimentidine, alcohol (chronic use), ketoconazole
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what drugs cause interstitial nephritis (3)
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methicillin, NSAIDs, furosimide
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fomepizole
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inhibits alcohol dehydrogenase
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