Shared Flashcard Set

Details

Factors Affecting Drug Metabolism
N/A
52
Pharmacology
Graduate
09/20/2012

Additional Pharmacology Flashcards

 


 

Cards

Term
Benzopyrene
Definition
Enhances CYP metabolism of theophylline
Term
Carbamazepine
Definition
Enhances CYP metabolism of carbamazepine, clonazepam and itraconazole
Term
Chlorcyclizine
Definition
Enhances CYP metabolism of Steroid Hormones
Term
Ethchlorvynol
Definition
Sedative that Enhances CYP metabolism of warfarin
Term
Glutethimide
Definition
Enhances CYP metabolism of antipyrine, glutethimide, warfarin
Term
Griseofulvin
Definition
Antifungal Enhances CYP metabolism of warfarin
Term
Phenobarbital and other barbituates
Definition
Enhances CYP metabolism of barbituates, chloramphenical, chlorpomazine, cortisol, coumarin anticoagulants, desmethylimipramine, digitoxin, doxorubicin, estradiol, itraconazole, phenylbutazone, phenytoin, qunine, testosterone
Term
Phenylbutazone
Definition
Enhances CYP metabolism of Aminopyrine, cortisol, digitoxin
Term
Phenytoin
Definition
Anti Seizure medication Enhances CYP metabolism of cortisol, digitoxin, dexamethasone, itraconazole, theophylline
Term
Rifampin
Definition
Enhances CYP metabolism of Oral contraceptive, anticoagulants, digitoxin, glucocorticoids, itraconazole, methadone, metoprolol, prednisone, propanolol, quinidine, saquinavir
Term
Ritonavir
Definition
Enhances CYP metabolism of midazolam
Term
St. John's Wort
Definition
Enhances CYP metabolism of alprazolam, oral contraceptives, digoxin, warfarin, cyclosporine, indinavir, ritonavir, simvastatin, tacrolimus
Term
Warfarin Metabolism Inducers
Definition
Rifampin, barbituates, st. john's wort. If you discontinue the inducer, the plasma level will increase,
Term
Stron inhibitors of CYP3A4
Definition
Ketoconazole, erythromycin, itraconazole
Term
Implication of inhibition of CYP
Definition
Increased plasma levels of drugs and toxic effects as a result
Term
Terfenadine
Definition
Antihistamine which was a 3A4 inhibitor, caused fatal cardiac arrhytmias
Term
Cimetidine
Definition
Reduced metabolism of chlordiazepoxide causing increased plasma conc
Term
Grapefruit Juice
Definition
Suicide inhibitor of CYP 450. This inactivates the P450 and causes increases in plasma conc of drugs. Inhibit CYP3A4
Term
Young and old enzyme activity
Definition
Decreased
Term
Placenta' metabolism
Definition
semi permable barrier which carries out hydroxylation, N-dealkylation, demethylation.
Term
Fetal Drug metabolism
Definition
Drugs going to the fetus go through the 1st pass effect twice. It can inactivate most drugs but if the metabolite is toxic or it is a pro drug this can cause extra toxicity
Term
Metabolism in infant and children
Definition
Activiy of P450 is much lower. Glucoronide formation only starts aroudn 3-4 years. However if drugs are sulfated, the metabolism of toddlers may exceed adults
Term
Geriatric Drug metabolism
Definition
Some (not all drugs) have decreased metabolism. Most phase 1 reactions occur more slowly. Conjugative enzyme work at roughly the same pace. Age can also cause low blood flow or injury which affects metabolism
Term
Charbroiled Food+ Cruiciferous Vegetables
Definition
Induces CYP1A causing increased drug metabolism. Therefore increaed metabolism, shorter half life
Term
Starvation
Definition
Increases CYP2E1. Causes an increased metabolism of drug, therefore shorter half life
Term
Protein deficiency
Definition
Causes decreased P450 activity causing less metabolism of drugs and increased half life
Term
Fatty acid deficiency
Definition
Less membrane/CYP450 function leading to less metabolism and higher half lifes
Term
Cirrhosis
Definition
Leads to impairment of phase I metabolism
Term
Vitamin and mineral deficiencies
Definition
Lower P450 activity leading to less metabolism and increased half life
Term
Alcohol
Definition
Induces CYP2E1 causing high metabolism and decreased half life
Term
High Carbohydrate diet
Definition
Low P450 activity leading to decreased metabolism and increased half life
Term
Cats
Definition
Deficient in UDP glucuronosyl transferase, uses sulfate conjugation instead meaning that there will be lower clearance rates
Term
Species Differences
Definition
Because animals metabolize at such different rates, it is difficult to extrapolate data to humans. This makes animal studies less effective
Term
Acute or chronic liver disease
Definition
Alcoholic hepatitis, alcoholic or chronic hepatitis, viral or drug induced hepatitis, hemochromatosis. All of these increase half life of drugs.
Term
Heavy metal poisoning
Definition
Leads to impaired enzyme activity leading to less metabolism and increased half life
Term
Flow dependent elimination
Definition
Some drugs are metabolized rapidly by the liver so the limiting step is how fast the heart can pump the drug to it. Include alprenolol, amitriptyline, clomethiazole, labetalol, isoniazid, impramine, desipramine, lodocaine, meperidine, morphine, pentazocine, propoxyphene, propranolol, verapamil
Term
Lung Disease
Definition
Impairs hydrolysis of procaine, increased half life of antipyrine in lung cancer patients
Term
Infections
Definition
Release inflammatory mediators, inactivate p450 causing decreased metabolism and increased half life
Term
Hypothyroidism
Definition
Hypothyroidism leads to increased half life of antipyrine, digoxin, beta blockers
Term
Hyperthyroidism
Definition
leads to decreased half life of antipyrine, digoxin, beta blockers
Term
Testosterone
Definition
INcreased metabolism due to CYP450 leading to faster metabolism and shorter half lifes
Term
Pregnancy
Definition
Up regulation of 2C9 and 2D6, (40% of drug phase 1 metabolism)
Down regulation of 2C19.
Term
Intestinal bacteria
Definition
Deconjugate glucoronic acid, sulfates, glycine, leads to drugs be unconjugated and absorbed. Can vary based on antibiotics and diet
Term
Genetic polymorphism
Definition
Variation in more than 1 percent of population
Term
Genetics
Definition
Can impact drug distribution, metabolism and elimination. Can be the drug itself causing a variation
Term
Preabsorption
Definition
Physiochemical interactions can change drug availability.
Term
Cisplatin
Definition
Forms a black precipitate when exposed to aluminum
Term
Tetracycline
Definition
chelates with divalent cations (ca+2)
Term
Gentamicin + Pencicillin
Definition
Interfere with bacterial lysis
Term
Probenecid
Definition
Inhibits activate secretion of penicillin
Term
Alkalinization of urin
Definition
prevents drug reabsorption (increases excretion of weak acids
Term
Physiological agonists
Definition
Bind 2 seperate receptors by 2 seperate drugs results in additive effect (nitroglycerin + viagra) leads to hypotension
Supporting users have an ad free experience!