Term
| Types of pharmocokinetic drug interactions: |
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Definition
what our body does to the drug:
- absorption
- distribution
- metabolism
- excretion |
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Term
| types of pharacodynamic drug interactions: |
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Definition
what the drug does to our body:
- additive or synergistic
- antagonism of one drug by another |
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Term
| If one drug has the potential for adsorbing another drug, it should be taken __ hour before or __ to ___ hours after. |
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Definition
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Term
| Give examples of adsorbing drugs: |
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Definition
| - antacids bind (adsorb) digoxin |
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Term
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Definition
| tetracyline binds calcium, Fe+2, and other minerals and blocks absorption |
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Term
| pH altering drugs can also increase/decrease amount of another drug that is absorbed. example: |
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Definition
| proton pump blockers decrease ketoconazole concentrations |
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Term
| Drugs may increase/decrease gastric emptying which in turn increases/decreases drug absorption. Example: |
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Definition
| - antinausea meds increase gastric emptying so don't have time to absorb other drugs |
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Term
| pharamacokinetic drug interactions involving drug distribution: |
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Definition
- competition for plasma binding protein causes transient rise in plasma concentration when one drug is displaced off of proteins (phenylbutazone displacement of warfarin)
- displacement from tissue binding sites causes transient rise in plasma concentrations
- these are likely not super important |
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Term
| Pharmacokinetic drug interactions involving changes in absorption: |
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Definition
Adsorbing drugs: antacids bind digoxin, iron, azole antifungals, ASA, tetracycline, thyroxine
Chelating drugs: tetracycline binds Ca2+, Fe2+, and other minerals, which blocks its absorption (note: dairy products)
pH altering drugs: proton pump blockers decrease ketoconazole concentrations
Drugs affecting gastric emptying |
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Term
| P-glycoprotein is a ___ ___ ___. This is the major causes of resistance to ___ with ___. It was first discovered in ___ cells. |
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Definition
- multi-drug resistance protein
- chemotherapy with cancer
- cancer cells |
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Term
| P-glycoprotein is a ___ __that moves drugs __ of cells, and thus is involved with ___ of drugs. |
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Definition
- transport protein
- out
- excretion |
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Term
| P-glycoprotein is located in the ___ ____ ____ where it moves drugs out the brain and into the blood. If there was a blockade of Pglycoproteins here, you would ____ ___ concentrations. |
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Definition
- blood brain barrier
- increase CNS |
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Term
| Pglycoproteins are also in the ___ ___where they move drugs into the lumen of the intestine to be excreted. Blockading these proteins would cause ___ ____ concentration. |
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Definition
- GI tract
- increased plasma concentration |
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Term
| P-glycoproteins are also in the ___where they move drugs into the urine. Blocking these would lead to an ___ ___ concentration of drug. |
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Definition
- kidney
- increased plasma |
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Term
| summary of locations and roles of Pglycoproteins: |
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Definition
Transporter that moves drugs out of cells
Blood-brain-barrier: moves drugs out of brain and
into blood (blockade = increased CNS concentration)
GI tract: moves drugs into the lumen of the intestine
(blockade = increased plasma concentration)
Kidney: moves drugs into the urine
(blockade = increased plasma concentration) |
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Term
| P-glycoprotein transporter ____ secretes drug from cells. |
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Definition
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Term
| P-glycoproteins are important where? |
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Definition
Important at the blood brain barrier
In proximal renal tubule: responsible for secreting some
compounds, e.g., conjugated metabolites (Phase II) |
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Term
| P-glycoproteins are inhibited by many ___ ____. Give example. |
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Definition
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Term
| Ketoconazole is a ____ ____ thus it inhibits ______ and increases concentration of digoxin in the renal tubule by decreasing its excretion. |
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Definition
- CYP3A inhibitor
- P-glycoprotein |
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Term
Excretion Multi-Drug Resistance-associated Protein (MRP)
Probenecid inhibits MRP and reduces renal tubular secretion of penicillin =
increase in plasma concentration of penicillin |
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Definition
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Term
| Penicillin is substrate to MRP so if block MRP then you increase plasma level of penicillin |
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Definition
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Term
| Pharmocokinetic drug interactions involving metabolism: |
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Definition
- induction or inhibition of metabolism by P450
Ketoconazole and other azoles: inhibit CYP3A4: increased
concentrations of warfarin, benzodiazepines, cyclosporine,
amiodarone, phenytoin
Griseofulvin: enhances P450 enzymes, reduces warfarin
concentrations |
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Term
| ___ enhance their own metabolism. |
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Definition
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Term
| with pharmacodynamic interactions similar drugs may have ___ or ___ effects, opposing drugs may ____, and two drugs together may produce ___ or ___ effects. |
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Definition
- additive or synnergistic
- counterbalance
- additive or synnergistic |
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Term
| With chronic alcohol intake, there is ___ ___ and ___ ___ of drugs. |
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Definition
- enzyme induction
- enhanced metabolism |
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Term
| Acute alcohol intake has ___ actions with other ___ _____ which leads to increased ___ ___ effect on insulin. |
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Definition
- synergistic actions with other CNS depressants
- increased hypoglycemic effect of insulin |
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Term
| Disulfiram is ____ blocks alcohol dehyrogenase. so if you take this and drink get nausea and vomitting, headache, hypotension, malaise, flushing. |
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Definition
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Term
| Drug A inhibits enzyme that metabolizes Drug B. How does A affect the concentration of B? |
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Definition
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Term
| Drug A induces enzyme that metabolizes Drug B- how does a influence b concnetration? |
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Definition
| decreases B concentration |
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