General Principles Flashcards
Refers to the amount of drug that reaches the systemic circulation.
Bioavailability
Used to determine the safety and efficacy of generic drugs.
Bioequivalence
Measures the dosage 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 to the apparent volume into which 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 polar moiety (sulfate, acetate, or glucoronate)
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 drug in the body to decrease to half of its value after administration of the drug has been stopped.
Half life (t 1/2)
Defined as the single amount of drug that is needed to achieve a desired plasma concentration quickly.
Loading dose
Amount of drugs must be given overtime in order 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 in minimum toxic concentration or dose.
Therapeutic window
Substance that shifts the graded dose-response curve to the right.
Competitive agonist
Substance that does not produce the same maximum effect and is exhibited by a decrease in the Emax.
Partial agonist
Substance that depressed it graded dose-response curve.
Non-competitive agonist
An antagonist that interacts directly with the agonist and not 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.
Lipid diffusion
Aqueous diffusion
Permeation that is saturable and inhibitable.
Carrier-mediated transport
At first affect that is infrequently observed in most patients.
Idiosyncratic reactions
Responsiveness decreases a consequence of continued drug administration.
Tolerance
Responsiveness diminishes rapidly after a drug administration.
Tachyphylaxis
Induction of developmental defects in the fetus.
Teratogenesis
Induction of malignant characteristics in cells.
Carcinogenesis
Induction of changes in genetic material of animals of any age.
Mutagenesis
CY P450 Inducers
Ethel Booba INDUCES Phen-Phen & Refuses Greasy Carb Shakes
Ethanol Barbiturates Phenytoin Phrnobarbital Rifampicin Griesofulvin Carbamazepine St. Johns wort Smoking
All barbiturates are INDUCER except one.
SECOBARBITAL
-CY P450 INHIBITOR
CY P450 INHIBITORS
Inhibitors Stop Cyber Kids from Eating GRApefruit VQ
Iosoniazid Sulfonamides Cimetidine Ketoconazole Erythromycin Grapefruit Juice Ritonavir Amiodarone Valproic acid Quinidine
Narrow therapetic index
WALA na Cyang Pa Pa, VasTeD pa!
Warfarin
Aminoglycosides
Lithium
Amphotericin B
Carbamazepine Phenobarbital Phenytoin Vancomycin Theophylline Digoxin
Zero Order Kinetic
WHAT PET
Warfarin
Heparin
Aspirin
Tolbutamide
Phenytoin
Ethanol
Theophylline
Rectal artery responsible for FIRST PASS EFFECT on giving rectal suppository?
Superior Rectal Artery
Phases of Drug studies: for a RARE disease
Orphan Drug
Phases of Drug studies:
Normal volunteer, small number
Phase 1
Phases of Drug studies:
Post marketing
Phase 4
Phases of Drug studies:
Clinical trials
Phase 3
