Factors that affect drug absorption (Bioavailability) Flashcards
Factors that affect drug absorption (Bioavailability):
- Routes of drug administration
- First pass effect
- drug pH – alkaline is lipid soluble (uncharged form)
- liver metabolism
- higher dosage (mg) and drug concentration (% solution)
- solubility of preparation – increase in solution
- increase blood flow to the absorbing area – increase absorption
- wider absorbing surface – greater absorption
- half-life – time it takes for ½ of the drug to be eliminated at constant rate of 0.693 t ½
effect of GI secretions along with the action of gastric HCl which initially change drug molecules followed by liver metabolism
→ oral route
First Pass Effect
→ occurs whenever the drug is administered orally, enters the liver, and suffers extensive biotransformation to such an extent that the bioavailability is drastically reduced
First-pass metabolism or first-pass effect or pre-systemic metabolism
- amount of time required for plasma concentration of a drug to decrease by 50% after discontinuance of the drug
Half-Life
– reflects rapid decline in plasma concentration as the dose of drug is distributed throughout the body
distribution half-life (t ½ alpha)
– slower, reflecting metabolism and excretion of the drug
elimination half-life (t ½ beta)
when the response of a particular system is measured against increasing concentration of the drug
Graded Dose-Response Relationship
– when the dose required to produce a specified response are determined in each member of the population
Quantal Dose-Response Relationship
relative rate at which the drug reaches the general blood circulation
Bioavailability
Factors that affects Bioavailability:
- Solubility of the drug in the contents of the stomach
- Dietary Pattern
- Tablet Size
- Quality control in the manufacturing and Drug formulation
constant fraction of the drug reaches the blood circulation after any routes
except: IV, IA, IC
First Order Kinetic of Drug absorption
100% of the drug reaches the blood circulation after IV, IA, IC
Zero Order Kinetic of Drug Absorption