Kategorier: Alle - pharmacokinetics

af Bradley Campbell 1 år siden

84

Drug dosing and elimination

When administering multiple doses of a drug, a plateau state is eventually reached, where additional doses do not increase the peak concentration. This steady state typically occurs after 3-5 half-lives of the drug.

Drug dosing and elimination

Drug dosing and elimination

Multiple dosing

Loading dose
Administering a larger initial dose followed by smaller maintenance dose
In instances where waiting for steady state is not reasonable
Maitinance dose
Practically, a steady state is reached after 3-5 half lives
Can be solved for if you have:

Max concentration

Drug swing
Peak dose minus trough dose when at plateau state
plateau state
After giving the same dose over the same interval for an amount of time, there will be a maximum dose that additional doses will not peak above
Dosing interval
a consistent time period between drug doses
adding additional dose before the origonal dose is excreted is cumulative and leads to a new peak of dose

compartment models

Multicompartment model
For many drugs 2 compartments is sufficient

Second compartment is the rest of the body

Can group together key organs

Used to account for distribution phase

modeling every organ is unrerasonable
One compartment model
Used for:

Aminoglycosides

Antibacterial drugs

Assumes drug is freely distributed and eliminated
A method of approximating drug distribution

Pharmacokinetics

Half life
Rate constant can be calculated for a drug
Does not apply to second order drugs
Plasma half life does not always equal pharmacological half life

Some things that can cause discrepency

DNA damaging drugs

Irreversible receptor binding

Amount of time for half of initial concentration to be cleared

Constant time irrespective of initial concentration

Zero order
Zero order drugs

Phenytoin

salicylate

Alcohol

Elimination of drug is constant

Some first order drugs at high concentrations function as zero order drugs

irrespective of drug concentration

First order
Drug elimination dependent on concentration

Constant percentage of drug eliminated

Accounts for most drugs

Bioavailability

Bioequivilence
Two drugs with varying concentration of the same therapeutic ingredient and different routes of administration, but same bioavailability
Can be used to compare drugs
Drugs with the same route of administration and mechanism can compare efficiency by bioavailability
Intravenous administration is 100% bioavailable
dependent upon routes of administration
Ammount of drug that reaches circulation