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
Amiodarone
Is an antiarrhythmic which is a potent inhibitor of a number of cytochrome p450 enzymes
P45 inducer
Drugs that increase the activity of p450 causing drugs that are also metabolized by the p450 system to be metabolized at an increased rate
Examples of p450 inducer
Phenytoin, griseofulvin, St. John’s wort, carbamazepine, rifampin, barbiturates, chronic alcohol use
Griseofulvin
Orally administered antifungal drug Thor treatment of fungal infections of the skin and nails.
With does griseofulvin interfere with
Microtubule function and therefore disrupts mitosis of fungal organisms
Phenytoin
Antiepileptic drug Acts to suppress abnormal brain activities via blockade of sodium channels. Also a class 1B anti-arrhythmic
Carbamazepine
Anticonvulsant and mood stabilizing drug. It is commonly used for epilepsy and trigeminal neuralgia
Rifampin
Used mainly for the treatment of active mycobacterium tb. It acts by inhibiting the DNA dependent RNA polymerase
Barbiturates
Drugs that depress the CNS by increasing the duration of chloride channel opening and thus decreasing neuron firing. they are commonly used for anxiety, seizure, and insomnia
Chronic alcohol abuse
Causes the liver to increase transcription of p450 enzymes to metabolize the toxic byproducts of alcohol and induces the p450 system
St. John’s wort
Herbal treatment for mild depression
Induced or p450