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25 Cards in this Set
- Front
- Back
When two drugs interact the combined effect can be? (three possibilites) |
Additive – the combined effect is higher that either of the individual effects but not higher than the sum of the two individual effects Potentiated (potentiation) – the combined effect is higher than the sum of the two individual effects Antagonized – the combined effect is smaller than that of one of the individual effects |
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Name some drug types with small margins of safety. |
Anticoagulants Antiarrhythmic drugs Cytotoxic drugs Antiepileptic drugs Antidiabetic drugs Cardiac glycosides |
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Drug interactions that lead to increased effect of the drug are most dangerous when the drug has a certain property. What property? |
Drug interactions that lead to increased effect of the drug are most severe when the drug has a small margin of safety. |
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Drug interactions that lead to decreased effect of the drug are most dangerous when the disease the drug treats has a certain property. What property? |
Drug interactions that lead to decreased effect of the drug are most dangerous when the disease the drug treats is sensitive to undertreatment. |
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Name some conditions which are sensitive to undertreatment. |
Arrhythmias Epilepsy Serious infections |
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What properties do drugs which can displace other drugs from plasma proteins have? |
Drugs which are highly plasma protein bound but not very potent can effectively displace other drugs |
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What properties do drugs which can be displaced from plasma proteins by other drugs have? |
Drugs which are highly plasma protein bound but very potent cannot effectively displace other drugs, but they can themselves be displaced |
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Name some drugs which often displace other drugs from plasma proteins. |
Aspirin Sulphonamides Valproate |
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Name some drugs which are often displaced from plasma proteins by other drugs. |
Coumarins Phenytoin NSAIDs |
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What is the function of P-glycoprotein (Pgp)? |
P-glycoprotein (Pgp) is a transport protein which pumps drugs out from organs which require extra protection against foreign substances, like the brain, placenta and testicles. It’s also found in kidney tubules, the GI tract and in bile ducts, where it contributes to drug excretion. |
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Name some drugs which are substrates for Pgp.(often asked on exam) |
Colchicine, Cyclosporine, Digoxin, Fexofenadine, Morphine, Tacrolimus
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Name some drugs which inhibit Pgp. |
Amiodarone, Clarithromycin, Cyclosporine, Erythromycin, Ketoconazole, Quinidine, Verapamil |
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Name some drugs which induce Pgp. |
Rifampin, chlorpromazine, St. John's wort. |
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What is the result of induction of the enzyme which metabolizes a prodrug? |
More of the prodrug is converted into the active metabolite, so the pharmacological effect increases. |
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What is the result of induction of the enzyme which metabolizes an active drug (not a prodrug)? |
More of the drug is converted into an inactive metabolite, so the pharmacological effect decreases. |
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What is the result of inhibiton of the enzyme which metabolizes an active drug (not a prodrug)? |
Less of the drug is converted into an inactive metabolite, so the pharmacological effect increases. |
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What is the result of inhibition of the enzyme which metabolizes a prodrug? |
Less of the prodrug is converted into the active metabolite, so the pharmacological effect decreases. |
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Name some prodrugs. |
Codeine, tamoxifen, clopidogrel |
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Name some drugs which are typical enzyme inducers |
Phenytoin, carbamazepine, phenobarbital, rifampin, etc. |
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Name some drugs which are typical enzyme inhibitors. |
Ketoconazole, amiodarone, erythromycin, allopurinol, verapamil, cimetidine |
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Name some substrates for organic anion transporter (OAT) |
NSAIDs, penicillins, cephalosporins, thiazides, loop diuretics |
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Name some substrates for organic cation transporter (OCT) |
Metformin Cimetidine Amiloride |
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Administration of sodium bicarbonate makes the urine more basic. This increases the excretion of what types of drugs? |
Weak acids, like salicylates and phenobarbital
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Administration of ammonium chloride makes the urine more acidic. This increases the excretion of what types of drugs? |
Weak bases, like quinidine |
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How can drug interactions occur at the level of renal excretion? |
Drugs which are secreted into the tubules by the same transporter protein (OAT, OCT, Pgp) can compete with each other for secretion. |