Fundamentals Of Pharmacology Flashcards
Cytochrome p450
Superfamily of enzymes involved in drug metabolism and bioactivation. It is a membrane associated protein that present in most tissues
Function of cytochrome p450
Plays important roles in hormone synthesis and breakdown, cholesterol synthesis, and vitamin D metabolism
P450 inhibitors
Drugs that decrease the activity of cytochrome p450
What happens if cytochrome p450 is inhibited
Drugs metabolized by p450 are metabolized at a decreased rate.
Example of p450 inhibitors
Cimetidine, ketoconazole, erythromycin, ciprofloxacin, Indinavir, acute alcohol use, isoniazid, grapefruit juice, quinidine, sulfonamides
Quinidine
Class I anti-arrhythmic agent that acts on fast inward currents
Ciproflaxin
A fluoroquinolone antibiotic that is commonly used for gram negative rod infections of the urinary and GI tracts. It works by interfering with topoisomerase II
Isoniazid
Decreases the synthesis of myopic acids, which is a key component of mycobacterium tuberculosis. It is the only agent used for mono therapy prophylaxis against TB
Grape fruit juice
Decreased activity of P450 system leading to toxicities caused by slow metabolism of other p450 drugs
Acute alcohol abuse
Inhibits -450 system bc p45- enzymes are saturated by the toxic metabolites of acute ingestion
Erythromycin (macrolide)
Antibiotic that is commonly used tor bordetalla pertusis, legionella pneumophilia and mycoplasma pneumoniae. It inhibits protein synthesis by binding to the 23s RNA of the 50s ribosomal subunit, thereby blocking translocation
Indinavir
HIW protease inhibitor that is used as a component of antiretroviral therapy in HIV AIDS
Cimetidine
histamine H2 receptor antagonist that is commonly used in the treatment of heartburn by decreasing stomach acid production
Sulfonamides
Have sulfonamide group (sulfa drugs) often interact with p450 system
Common sulfanoamides are antibiotics, diuretics, and dulfonylureas
Ketoconazole
For systemic mycoses. Acts by inhibiting fungal ergol sterol synthesis