Pharmacokinetics Flashcards
(21 cards)
Action of the BODY on the drug
PHARMACOKINETICS
LADME Liberation Absorption Distribution Metabolism Excretion
Elimination
Metabolism + Excretion
Transfer of DRUG from its site of administration to the BLOODSTREAM
Absorption
MC route of drug administration
Significant 1st pass
Oral (Swallowed)
Direct absorption into the systemic venous circulation (bypasses the 1st pass effect)
Buccal and Sublingual
Instantaneous and complete absorption that BYPASSES 1st pass effect
Intravenous
Absorption is more complete than oral
anticoagulants CANNOT be given by this route - may cause HEMATOMA
Intramuscular
Bypasses the 1st pass effect
Slower absorption than IM
Subcutaneous
PARTIAL avoidance of 1st pass effect
Rectal suppository
Offers delivery closest to the respiratory tissues
VERY RAPID ABSORPTION with minimal systemic effects
Inhalational
Application to the skin or mucous membrane for LOCAL EFFECT
SLOWEST of drug administration
Topical
Application to the skin for SYSTEMIC effects
Transdermal
The fraction of ADMINISTERED DRUG that reaches SYSTEMIC CIRCULATION
Bioavailability
Safe range b/w the minimum effective concentration and the minimum toxic concentration of a drug
Therapeutic window
Process wherein drug REVRSIBLY leaves the bloodstream and enters the target organ
DISTRIBUTION
4 factors: size of the organ blood flow solubility protein binding
The dose required to achieve a specific plasma drug concentration with a single administration
Loading Dose
The dose required for regular administration to maintain a target plasma
Maintenance Dose
Process by which drugs are chemically altered in the body
METABOLISM
termination
activation
elimination without metabolism
Reactions the convert the parent to a MORE POLAR (WATER SOLUBLE) or more reactive product by unmasking or inserting a polar functional group
PHASE I - Biotransformation/Functionalization
Reactions the involve CONJUGATION of subgroups to -OH,-NH2, and -SH functions on the drug molecule
makes the drug MORE POLAR
PHASE 2 - Synthesis/Conjugation
Cytochrome P450 INDUCERS
Ethanol (chronic ingestion) Barbiturates (EXCEPT secobarbital) Phenytoin Rifampicin Griseofulvin Carbamazepine St. John's Wort/Smoking Glutethimide Phenylbutazone Ritonavir