Drug Action Flashcards
(36 cards)
Pharmaceutic phase
Drug becomes a solution so that it can cross the biologic membrane.
Disintegration
Breakdown of the tablet into smaller part
Dissolution
Is the dissolving of the smaller particles in the GI fluid before absorption
Rate limit
Is the time it takes the drug to disintegrate and dissolve to become available for the body to absorb it.
Passive absorption
Occurs mostly by diffusion ( movement from high concentration to low concentration) & it doesn’t required energy.
Active absorption.
Requires an enzyme or a protein to move the drug against concentration gradient. Energy is required.
Pinocytosis
Cells carry a drug across their membrane by engulfing the drug particles
First pass effect (hepatic first pass)
The process in which the drug passes to the liver first where is partially metabolized prior reaching the target.
Ex. Coumadin ( warfarin )
Morphine
Bioavailability
Subcategory of absorption.
It is the percentage of the administered drug dose that reaches the systematic circulation. Once it has been released from the protein bound.
Distribution
Is the process in which the drugs becomes available to body fluids and body tissues
Free drugs (drugs not bound to protein)
Are the drugs available to receptors and responsible for causing a. Pharmacological response.
Half life ( t1/2)
Is the time it takes for one half of the drug concentration to be eliminated.
Notes to remember.
Drugs that are lipid soluble and nonionized are absorbed faster than water soluble and ionized drugs.
Metabolism
It occurs in the GI and liver ,but the liver is the primary site.
The liver transform by hepatic enzymes to inactive metabolites and lipid soluble drugs to water soluble substance for renal excretion.
The urine ph influence in Excretion or elimination
Urine ph varies from 4.5-8.
Acidic urine promotes elimination of weak bases drugs.
Aspirin a weak acid is excreted rapidly in alkaline urine.
Creatinine clearance ( CLcr) test.
The most accurate test to determine renal function.
Creatinine is a metabolic by product of muscle excreted through the kidneys.
It compares the levels of creatinine in the urine with creatinine in the blood
Normal creatinine clearance
85-135 ml/ min
Older adults may have a creatinine clearance of 60 ml/ min due to a decrease on muscle mass.
Pharmacodynamics
The study of drug concentration and it’s effects on the body.
Dose response?
Is the relationship between the maximal versus minimal amount of drug dose needed to produce the desire drug response.
Onset of action
Is the time it takes to reach the minimum effective concentration (MEC) after the drug is administered.
Peak action.
Occurs when the drug reaches its highest blood or plasma concentration.
Duration of action.
Is the length of the time the drug has a pharmacological effect.
Receptors or drug binding sites.
Drug binding sites:
Proteins, glycoproteins,proteolipids, and enzymes
Receptor families:
Kinase linked receptors, ligand-gated receptors, G protein coupled receptor systems, nuclear receptors.
Ligand binding domain
Is the site on the receptor at which the drug binds.