Pharmacology Drug Metabolism & Pharmacokinetics Intermediate
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Cytochrome P450 Enzyme Inducers

CRAP
GPS
Classic mnemonic for agents that induce hepatic microsomal enzymes, accelerating metabolism of co-administered drugs.

Enzyme inducers upregulate transcriptional synthesis of CYP enzymes (primarily via PXR and CAR nuclear receptors). This accelerates drug clearance, leading to subtherapeutic plasma levels and clinical failure of oral contraceptives, warfarin, and immunosuppressants.

Systematic Breakdown

C

Carbamazepine

Powerful inducer of CYP3A4; also notable for auto-induction (induces its own metabolism over time).

R

Rifampin (Rifampicin)

The most potent CYP3A4/2C9 inducer known. Rapidly renders oral contraceptives and warfarin ineffective.

A

Alcohol (Chronic Use)

Chronic alcoholism induces CYP2E1, causing increased acetaminophen conversion to toxic NAPQI.

P

Phenytoin

Anticonvulsant that induces CYP3A4, 2C9, and 2C19.

G

Griseofulvin

Oral antifungal used for tinea capitis; induces hepatic cytochrome P450 system.

P

Phenobarbital

Barbiturate that powerfully upregulates transcription of multiple CYP isoenzymes.

S

St. John's Wort / Smoking

Herbal supplement that induces CYP3A4 and P-glycoprotein; aromatic hydrocarbons in cigarette smoke induce CYP1A2.

High-Yield Clinical Pearls & Exam Tips
  • Classic Board Scenario: A woman on oral contraceptive pills is started on Rifampin for latent TB (or St. John's Wort for depression) and becomes pregnant.
  • Organ Transplant Scenario: A patient on Cyclosporine or Tacrolimus starts St. John's Wort, experiences sharp drop in drug level, and suffers acute organ rejection.
Related Pharmaceuticals
Rifampin Carbamazepine Phenytoin Phenobarbital St. John's Wort
Related Clinical Conditions
Unintended Pregnancy Graft Rejection Subtherapeutic Anticoagulation
Authoritative Sources: Katzung Basic & Clinical Pharmacology 15e · First Aid USMLE Step 1

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