General Pharma Flashcards
refers to the amount of a drug that reaches the systemic circulation
bioavailability
used to determine the safety and efficacy of generic drug
bioequivalence
measures the dose or concentration required to bring about 50% of the drug’s maximal effect
potency/ EC50
dose at which 50% of the individuals exhibit the specified quantal effect
ED50/ median effective dose
dose at which 50% of the animals manifest a particular toxic effect
TD50/ median toxic dose
transfer of drug from site of administration to bloodstream
absorption
refers the apparent volume into which the drug is able to distribute
volume of distribution
elimination of drug at a constant rate
zero order kinetics
elimination at a rate that is proportional to the serum concentration of the drug
first order kinetics
addition of a polar moiety (sulfate, acetate or glucuronate)
phase II metabolism
use of CYP 450 system oxidation, reduction or hydrolysis
phase I metabolism
describes the rate at which a specific drug is cleared from the system
clearance
refers to the amount of time required for the amount of the drug in the body to decrease to half of its value after the administration of the drug has been stopped
half life ( t 1/2)
defined as the single amount of drug that is needed achieve a desired plasma concentration quickly
loading dose
amount of drug that must be given over time to maintain desired plasma concentration
maintenance dose
used as a measure of drugs safety
therapeutic index
formula for therapeutic index
TD50/ED50
refers to the dosage range between the minimum effective therapeutic concentration or dose and minimum toxic concentration or dose
therapeutic window
substance that shifts the graded dose-response curve to the right
competitive antagonist
substance that does not produce the same maximum effect and is exhibited by a decrease in the Emax
partial antagonist
substance that depress the graded-dose response curve
noncompetitive antagonist
an antagonist that interacts directly with the agonist and not at all or only incidentally with the receptor
chemical antagonist
the action of the drug on the body
pharmacodynamics
the action of the body on the drug
pharmacokinetics
permeation that is governed by Fick’s Law
liquid diffusion aqueous diffusion
permeation that is saturable and inhibitable
carrier-mediated transport
adverse effect that is infrequently observed in most patients
idiosyncratic reactions
responsiveness diminishes rapidly after drug administration
tachyphylaxis
induction of developmental defects in the fetus
teratogenesis
induction of malignant characteristics in cells
carcinogenesis
induction of changes in the genetic material of animals of any age
mutagenesis
Cytochrome P450 INDUCERS
[Ethel Booba takes Phen-Phen and Refuses Greasy Carb Shakes]
Ethanol (chronic ingestion)
Barbiturates exc. Secobarbital - an inhibiot
Phenytoin
Rifampicin
Griseofulvin
Carbamazepine
St. John’s Work / Smoking
Others: Glytethimide, Phenylbutazone (induces the metabolism of Aminopyrine, Cortisol, Digitoxin), Ritonavir
Cytochrome P450 INHIBITORS
[Inhibitors Stop Cyber Kids from Eating GRApefruit QV] Isoniazid Sulfonamides Cimetidine Ketoconazole Erythromycin Grapefruit Juice Ritonavir (on acute ingestion) Amiodarone Quinidine Valproic Acid Others: Allopurinol, Chloramphenicol, Chlopromazine, Dicumarol, Disulfiram, Ethanol (acute toxicity), Itraconazole, Nortriptyline, oral contraceptives, Phenylbutazone (inhibits the metabolism of phenytoin and tolbutamide), Saquinavir, Secobarbital, Spironolactone, Troleandromycin
Narrow Therapeutic Index Drugs
[WALA na Cyang PaPa! VasTeD na! Warfarin Aminoglycosides Lithium Amphotericin B Carbamazepine Phenobarbital Phenytoin Vancomycin Theophylline Digoxin
Zero Order Kinetics Drugs
[WHAT PET] Warfarin Heparin Aspirin Tolbutamide Phenytoin Ethanol Theophylline
Drugs that cause Tachyphylaxis
[MED students Love to watch CNN in HD] Metoclopramide Ephedrine Dobutamine LSD Calcitonin Nitroglycerin Nicotin Hydralazine Desmopressin
Route of Drug Administration: 100% bioavailability
Intravenous
Route of Drug Administration: first pass effect
Oral
Route of Drug Administration: Partial avoidance of first pass effect
Rectal, SL
Route of Drug Administration: application to skin for local effect
Topical
Route of Drug Administration: Application to skin for systemic effect
Transdermal
Phase of drug studies with small number of normal volunteers
phase I
Phase of drug studies with post-marketing surveillance
phase IV
Phase of drug studies: “does it work in patients?”
phase II
Phase of drug studies with randomized, double-blind, controlled trials
phase III
a drug for rare disease
orphan drug
Volume of distribution formula
Vd= dose/TC
Steady state concentration (Css) formula
Css= infusion rate/clearance
vasoCONSTRICTors
“AVENU” Angiotensin II Vasopressin Endothelin Neuropeptide Y Uropeptides
vasoDILATors
“KVSCANN” Kinins VIP Substance P CGRP Adrenomedullin Natriuretic Peptide Neurotensin
Acetylcholinesterase inhibitors
Neostigmine, Pyridostigmine -myasthenia gravis
Physostigmine -glaucoma
Donepezil, rivastigmine, galantamine -Alzheimer disease
