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level: Level 3

Questions and Answers List

level questions: Level 3

Question	Answer
1 actions of drug on the body 2 actions of the body on the drug	1 Pharmacodynamics 2 Pharmacokinetics
LADMERS	• Liberation of an active ingredient from the dosage form • Absorption into systemic circulation • Distribution • Metabolism in the body • Excretion of the drug from the body • Response
the transfer of a drug from the site of administration to the bloodstream	Absorption
the drug moves from a region of high concentration to one of lower concentration - does not involve a carrier and not saturable - movement is along the concentration gradient	Passive Diffusion
• directly proportional to the concentrations, surface area and permeability coefficient • inversely proportional to the thickness of the membrane	Fick's Law of Diffusion
drugs enter the cell through specialized transmembrane carrier proteins that facilitate the passage of large molecules – movement is along concentration gradient – does not require energy & can be saturated – may be inhibited by compounds that compete for the carrier	Facilitated Diffusion
involves specific carrier proteins that span the membrane – energy-dependent & saturable – movement is against the concentration gradient – selective and may be competitively inhibited by other cotransported substances	Active Transport
engulfment of a drug by the cell membrane and transport into the cell by pinching off the drug-filled vesicle	Endocytosis
reverse of endocytosis	Exocytosis
Factors influencing absorption	1 Effect of pH on drug absorption 2 Blood flow to the absorption site 3 Total surface area available for absorption 4 Contact time at the absorption surface
Absorbs nutrients in the small intestine	microvilli
responsible for transporting various molecules, including drugs, across cell membranes - "pumps" drugs out of the cells - associated with multi-drug resistance	Expression of P-glycoprotein
• the fraction (F) of the administered dose that reaches the systemic circulation • determined by comparing plasma levels of drugs after a particular route of administration with levels achieved by IV administration	Bioavailability
Bioavailability is usually measured using __	Area Under the Curve (AUC)
1) 100% Bioavailability, most rapid onset 2) 5 to <100 Bioavailability, most convenient; may have significant First Pass Effect	1 Intravenous 2 Oral
Factors Influencing Bioavailability	1 First-pass Hepatic Metabolism 2 Solubility of the drug 3 Chemical instability 4 Nature of the drug formulation
Show comparable bioavailability and similar times to achieve peak blood concentrations	BIOEQUIVALENCE
Pharmaceutically equivalent with similar chemical and safety profiles	THERAPEUTIC EQUIVALENCE
if the drugs have the same dosage form, contain the same active ingredient, and use the same route of administration	Pharmaceutical Equivalence