Pharmacokinetics Flashcards
Where are most drugs metabolised?
The liver
What is the purpose of metabolism?
To increase water solubility and aid excretion
What is the name given to the group of drugs that are activated follow metabolism?
Prodrugs
Give 2 examples of prodrugs
Codeine
Enalapril
What kind of metabolism can involve hydrolysis, oxidation or reduction?
Phase 1
How does phase 1 metabolism provide an active site for phase 2?
Increasing the polarity
Name the super family of metabolising enzymes?
Cytochrome P-450 enzymes
What does the isoform of the cytochrome P-450 determine?
Drug specificity
Name the three families of cytochrome P-450 that are important in oxidative drug metabolism
CYP1, CYP2, CYP3
Name the major constitutive enzyme in the human liver
CYP3A4
What can induce the enzyme CYP1A2?
Smoking
What does increased water solubility mean in phase 2 metabolism?
Enhanced excretion of the metabolised compound
What conjugation usually result in?
Inactivation
What happens to the drug’s effect when the the drug metabolising enzyme is induced?
Decreased drug effect
What are the most common enzyme inducers?
Alcohol and smoking
What does increased synthesis lead to in terms of enzymes?
Increased activity
What can drugs such as clarithromycin do?
Inhibit drug metabolising enzymes
Lack/decreased activity of an enzyme often results in what?
Increased drug toxicity
What can deficieny in renal function in young children lead to?
Metabolites rapidly building up to toxic levels
By what ages can children metabolise many drugs more rapidly than adults?
Two
Name the important process involved in eliminating drugs from the body?
Metabolism
What is the therapeutic process?
Producing the correct therapeutic effect
Name the four basic factors that determine drug pharmacokinetics?
Absorption
Distribution
Metabolism
Elimination
What is Tmax?
Time to peak concentration
What is Cmax?
The peak concentration
What is the range of when the drug is active?
Therapeutic range
What is the therapeutic index a measure of?
The range at which a drug is safe and active
What bioavailability does a drug given intravenously have?
100%
Most drugs are what kinds of acids?
Weak Acids
Small changes in pH will do what to the ionisation of a drug?
Will significantly influence it