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Lithium Digoxin
Carbamazepine Cyclosporin
Phenytoin Phenobarbitone
Theophylline Warfarin
(Aminophylline)
Pharmacodynamic Drug
Interactions
One drug causes a change in patient
response to another drug without
altering that drug’s pharmacokinetics
CYP2D6
Sub-Family Individual Gene
CYP 450 System
Definitions
• Substrate:
Drug is metabolised by the enzyme system
• Inducer:
Drug that will increase the synthesis of CYP450
enzymes
• Inhibitor
Drug that will decrease the metabolism of a
substrate
Enzyme Induction 1
• Leads to production of more enzyme,
usually after 3-4 days of exposure to
inducer
• Most CYPs are inducible but not
CYP2D6
• Time course of interaction depends on
half-life of inducer.
Enzyme Induction 2
• Rifampicin has short half-life and
induction apparent with 24 hours
Drug A Drug A
free free
• CYP2C9
PM 1-3% Caucasians
• CY2C19
PM- 3-5% Caucasians, 15-20% Asians
Enzyme Characteristics
Interindividual Enzyme
Content
• CYP3A4 x5
• CYP2D6 > 50
• CYP1A2 x 20
• CYP2C9 x5
• CYP2C19 ?
• CYP2E1 x 12
Interactions via Enterohepatic
Circulation (EHC)
Free drug
Liver
Conjugate
Bile