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46 Cards in this Set
- Front
- Back
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potency
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how much of drug neweded to get effect
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efficacy
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ability of drug to activate receptor once bound
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non competitive antagonist does what to dose response
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DECREASES peak doesnt shift
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competitive antagonist shifts dose response curve
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right
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weak acids ____and become _____ ; weak bases_____ and become
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unionized,lipid soluble;ionized,not lipid soluble
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bioavailability
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fraction of drug getting into systemic circulation
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one compartment model
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iv bolus,drug injected directly into circulation then evenly distributed
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two compartment
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drug enters central hen goes into peripheral then excreted
more common |
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central volume
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blood
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peripheral volume
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everything besides blood
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Vd
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apparent volume of ditribution
Vd=amount of drug in body/plasma conc of drug |
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drug bound to protein
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high conc in blood therefore low apparent Vd
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drug bound to tissue
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low conc in blood therefore high apparent Vd
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phase 1 metabolism
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involves,oxidation,reduction,hydrolysis
involve CYP450 |
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phase 2 metabolism
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involves conjugation make water soluble
manly transferases |
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cyp450 made in
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hepatocyte smooth ER
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drug clearance
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ttoal elimination of drug from body amount /time
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ttoal body clearance=
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CL renal+CL liver+CL other
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takes how many half lives to eliminate
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4
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first order kinetics
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constant fraction of drug broken down /time
most drugs shpow this |
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zero order kinetics
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constant amount of drug broken down /time
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loading dose
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given during serious situations,huge dose
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pharmacokinetic tolerance
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decreased conc of drug at site of action
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pharmacodynamic tolernace
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decreased effect of drug
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behavioural tolerance
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decreased effect of drug due to conditioned response (subject counteract effect)
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innate
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genetic variabilty
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surmountable tolerance
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give more of drug get same effect
decreased postsynaptic receptors |
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insurmountable
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no matter how much drug you give dont get same effect
decrease presynaptic transmitter |
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cross tolerance
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substitution of different drug in same famil wont work
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differential tolerance
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drugs act in more than one location
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behavioural tolernace
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learned phenomenon not always conscious
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cyp2A6 activates
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procarcinogens
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muscarinic receptor
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g protein linked to K ion channel
choliergic |
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nicotinic recptor
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ligand gate ion channel
cholinergic 5 subunits each spannins membrane 4x allows sodium/calcium alpha or beta subunits Ach binds opens sodium channel channel desensitized with nicotine continuously desensiizes=long term inactivation act on PNS/CNS/ANS |
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major type of receptor in brain/ganglia is
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homomeric neuronal AchR
have 5 alpha7 subunits calcium channel |
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nicotine only binds to
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alpha unit
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need how many alpha subunits to function
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2
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heteromeric neuronal AchR
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sodium and calcium channels
(alpha4)2(beta2)3 |
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glutamate cells have what receptors
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alpha7,nicotine binds cause increase in excitaory glutamate that acts on dopamine cells
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GABA cells have what receptors
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non alpha 7 nAchR,nicotine binds cause gaba release that inhibits dopamine cell
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GABA A receptor
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ligand gated gated ion channel
chloride |
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adenosine receptors
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neuromodulators damp down other pathways
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A1 receptors
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adenosine recpetor gprotein coupled
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alpha 1 Gaba a receos acted on
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sedatives
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alpha 2 on Gaba a rweceptors acted on
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benzo
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GABA b recptor
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gprotein with K channel for muscle relaxants
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