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28 Cards in this Set
- Front
- Back
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LADME
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liberation, absorption, distribution, metabolism, elimination
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excipient
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fillers
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dose dumping
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premature and exaggerated release of a drug due to environmental factors
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depot formulations
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oily IM injections that slowly leach into circulation
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Why would a steak meal affect a parkinson's patient?
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AA transport of steak into brain will compete with L-dopa transport into brain
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What is bulk diffusion dictated by?
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henderson-hasselback equation
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bioequivalence
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same rate of absorption and availability
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drugs that influence brain first
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fat soluable because of disproportionate percent of blood perfused to brain
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receptors at CTZ
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serotonin and dopaminergic
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circumventricular organ
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hypothalamus and other parts unprotected by the BBB
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OTC antihistamines often have these other effects
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affinity for muscarinic receptor as antagonists;
this causes sedation |
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What mechanism causes increased sensitivity to pain?
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alterations of phosphorylation status of NT mediators
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What can cause pruning of presynaptic terminals?
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chronic drug treatment which causes down-regulation of tophic factors
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LTP
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long term potentiation; increased glu release as a result of NO retrograde diffusion
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excitotoxicity
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neuronal swelling due to excess NT ausing large influxes of Ca
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denervation hypersensitivity
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increase in receptor number when NT is less available
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pharmacological denervation hypersensitivity
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increase in receptor number when receptor antagonist is administered
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down regulation
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receptor number decreases due to chronically increased NT availability
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time required for NT receptor number adjustments
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10-14 days
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Changes in receptor number affect what?
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drug potency, not efficacy
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chronic treatment of morphine causes what?
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upregulation of alpha-1 NE receptors at amygdala to hypersensitize amygdala
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difference between pharmacodynamic and physiological tolerance
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pharmacodynamics is alteration of receptor number;
physiological tolerance is reduction of potency due to secondary action of drug (distal neuron) |
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tolerance mechanism responsible for withdrawl
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physiological tolerance
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autoinduction
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a drug that induces the P450 enzyme that affects itself
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What is cross-tolerance
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reduction in drug Y potency as a result of drug X exposure
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What is reverse tolderance
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sensitization where potency is increased as a result of drug exposure
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How does the presence of many pathways affect tolerance?
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the more pathways, the more the body can return to homeostasis; tolerance is more rapid
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what causes disinhibition release?
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depressants depress inhibitory CNS functions to cause an initial excitement
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