CPT Flashcards
(1448 cards)
Def: pharmacokinetics
Study of factors which determine the amount of drugs at their sites of biological effect at various times.
Includes
ADME
Absorption
Distribution
Metabolism
Excretion
Def: Pharmacodynamics
What the drug does to the body
Def: clearance
Volume of plasma cleared of a drug per unit time
Def: half-life
Time taken for drug concentration to decline to half its original valu
Depends on volume of distribution and clearance
Def: volume of distribution
Volume into which a drug appears to distribute
Theoretical volume that would be necessary to contain the total amount of a drug administered at the same concentration that it is observed in the blood plasma.
High for lipid-soluble drugs
Low for water-soluble drugs
What factors can increase the volume of distribution?
Higher Vd indicates a greater amount of tissue distribution.
High lipid solubility (non-polar drugs), low rates of ionisation or low plasma binding capabilities have higher volumes of ditribution than drugs which are more polar, more highly ionised or exhibit high plasma binding.
Vd may be increased by renal failure (due to fluid retention) and liver failure (due to altered body fluid)
Vd=
Total amount of drug in body/drug blood plasma concentration
What is first order kinetics?
Clearance of durg is always proportional to plasma concentration
Most drugs are in this category
What is zero order kinetics?
Clearance of drug is not always proportional to plasma concentration
Saturation of metabolism-> constant rate of elimination regardless of plasma levels
Give some examples of drugs with zero order kinetics
Phenytoin
Salicylates
Ethanol
What is bioavailability?
Percentage of the dose of a drug which reaches the systemic circulation
100% for IV administration
How long is ~ required for a drug to reach a steady state?
Around 5 half lifes
What does a loading dose do?
Reduces the time needed to reach a steady state, useful if long or short half life
What are some drugs that use loading doses?
Phenytoin
Digoxin
Amiodarone
Theophylline
What are the indications for therapeutic drug monitoring?
Ix lack of drug efficacy (possibility of poor compliance)
Suspected toxicity
Prevention of toxicity
What are three drugs that must have therapeutic drug monitoring?
Aminoglycosides
Vancomycin
Li
What are some dugs that have therapeutic monitoring?
Phenytoin
Carbamazepine
Digoxin
Ciclosporin
Does Warfarin undergo therapeutic drug monitoring?
Not monitored per se, it is the biological effect that is monitored rather than the plasma drug level
What is first pass metabolism?
Metabolism and inactivation of a drug before it reaches the systemic circulation
i.e. pre-systemic elimination
Occurs in gut wall and liver
Gives some examples of drugs that undergo FPM
Propranolol
Verapamil
Morphine
Nitrates
What are the pathways of drug metabolism and elimination?
Excreted unchanged by the kidney e.g. frusemide
Phase 1 metabolism and then renal excretion
Phase 2 metabolism and then renal excretion
What is phase 1 metabolism
Creation of reactive, polar functional groups.
Oxidation: usually by cytochrome P450 system
Reduction and hydrolysis
What is phase 2 metabolism?
Production of polar compounds for renal elimination
Either the drug or its phase 1 metabolite
Conjugation reactions: glucuronidation, sulfonation, acetylation, methylation
What is the principle method of elimination?
Renal, depends on GFR



