10 Questions
What is the primary carbamazepine metabolite that contributes to its efficacy and toxicity?
10, 11-epoxide
Which of the following isoenzymes is primarily responsible for catalyzing 10, 11-oxidation of carbamazepine in the human liver?
CYP3A4, CYP2C8, and CYP1A1
What is the timeframe for autoinduction of carbamazepine to occur in patients on a fixed dosing regimen?
3-5 weeks
How long does it take to assess therapeutic effect and steady-state carbamazepine serum concentrations after the final dosage increase?
2-3 weeks
What is the duration of holding doses for the effects of autoinduction to be reversible?
6 days
What is the consequence of carbamazepine inducing its own metabolism?
Complicated dosing regimen
Which isoenzyme is NOT responsible for catalyzing 10, 11-oxidation of carbamazepine in the human liver?
CYP2C9
What happens to carbamazepine clearance during gradual exposure?
It increases
How long does it take for liver enzyme induction to occur during gradual exposure?
3-5 weeks
What happens to the effects of autoinduction if doses are held for a short period?
They are reversed
Study Notes
Carbamazepine Metabolism
- The primary metabolite of carbamazepine is 10, 11-epoxide, which is active and contributes to the drug's efficacy and toxicity.
Enzymes Responsible for Carbamazepine Oxidation
- CYP3A4, CYP2C8, and CYP1A1 are the isoenzymes responsible for catalyzing 10, 11-oxidation of carbamazepine in the human liver.
Autoinduction of Carbamazepine
- Carbamazepine induces its own metabolism, complicating dosing regimens.
- Autoinduction occurs approximately 3-5 weeks after starting a fixed dosing regimen.
- Autoinduction continues when a dosage increase is required, even in stabilized patients.
- Gradual exposure to carbamazepine allows liver enzyme induction, increasing carbamazepine clearance.
Therapeutic Effect and Steady-State Concentrations
- Therapeutic effect and steady-state carbamazepine serum concentrations can be assessed 2-3 weeks after the final dosage increase.
Reversibility of Autoinduction
- The effects of autoinduction are reversible, even when doses are held for as few as 6 days.
Carbamazepine Metabolism
- The primary metabolite of carbamazepine is 10, 11-epoxide, which is active and contributes to the drug's efficacy and toxicity.
Enzymes Responsible for Carbamazepine Oxidation
- CYP3A4, CYP2C8, and CYP1A1 are the isoenzymes responsible for catalyzing 10, 11-oxidation of carbamazepine in the human liver.
Autoinduction of Carbamazepine
- Carbamazepine induces its own metabolism, complicating dosing regimens.
- Autoinduction occurs approximately 3-5 weeks after starting a fixed dosing regimen.
- Autoinduction continues when a dosage increase is required, even in stabilized patients.
- Gradual exposure to carbamazepine allows liver enzyme induction, increasing carbamazepine clearance.
Therapeutic Effect and Steady-State Concentrations
- Therapeutic effect and steady-state carbamazepine serum concentrations can be assessed 2-3 weeks after the final dosage increase.
Reversibility of Autoinduction
- The effects of autoinduction are reversible, even when doses are held for as few as 6 days.
Explore the metabolism of carbamazepine, including its active metabolite and the enzymes responsible for its oxidation. Learn about the autoinduction process and its impact on dosing.
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