| 1. Accepted major perpetrators | 2. Rejected perpetrators | 3. Unclassifiable | 4. Full table |
valproate is a weak inducer of CYP1A2. valproate has not been evaluated in the literature showing its role of altering the activities of CYP3A.
- Weak inducers: < 2-fold decrease in AUC or < 50% increase in clearance of in vivo CYP probe.
- Not evaluated in the literature: drugs implicated as inhibitors and inducers of CYP enzymes without reported clinical PK interaction studies.
Footnotes and References
|a.||reported at Clinical Trials.gov ( http://clinicaltrials.gov/ct2/show/study/NCT00785486?sect=X701&view=results ).|
|b.||likely to be a major inhibitor based on subjective evaluation (≥ 2-fold AUC increase or ≥ 50% decrease in clearance of in vivo CYP probe).|
|1.||Wietholtz H, Zysset T, Kreiten K, Kohl D, Buchsel R, Matern S. Effect of phenytoin, carbamazepine, and valproic acid on caffeine metabolism. European Journal of Clinical Pharmacology 1989; 36: 401-06.[PubMed]|
|2.||Yeh RF, Gaver VE, Patterson KB, Rezk NL, Baxter-Meheux F, Blake MJ, Eron JJJ, Klein CE, Rublein JC, Kashuba ADM. Lopinavir/Ritonavir Induces the Hepatic Activity of Cytochrome P450 Enzymes CYP2C9, CYP2C19, and CYP1A2 But Inhibits the Hepatic and Intestinal Activity of CYP3A as Measured by a Phenotyping Drug Cocktail in Healthy Volunteers. Journal of Acquired Immune Deficiency Syndromes 2006; 42: 52-60.[PubMed]|
|3.||Malmstrom K, Schwartz J, Reiss TF, Sullivan TJ, Reese JH, Jauregui L, Miller K, Scott M, Shingo S, Peszek I, Larson P, Ebel D, Hunt TL, Huhn RD, Bachmann K. Effect of Montelukast on Single-Dose Theophylline Pharmacokinetics. American Journal of Therapeutics 1998; 5: 189-96.[PubMed]|
|4.||Saccar CL, Danish M, Ragni MC, Rocci ML, Greene J, Yaffe SJ, Mansmann HC. The effect of phenobarbital on theophylline disposition in children with asthma. Journal of Allergy and Clinical Immunology 1985; 75: 716-19.[PubMed]|
|5.||Backman JT, Schroder MT, Neuvonen PJ. Effects of gender and moderate smoking on the pharmacokinetics and effects of the CYP1A2 substrate tizanidine. European Journal of Clinical Pharmacology 2008; 64: 17-24.[PubMed]|
|6.||Shadle CR, Lee Y, Majumdar AK, Petty KJ, Gargano C, Bradstreet TE, Evans JK, Blu RA. Evaluation of potential inductive effects of aprepitant on cytochrome P450 3A4 and 2C9 activity. Journal of Clinical Pharmacology 2004; 44: 215-23.[PubMed]|
|7.||Dingemanse J, Schaarschmidt D, van Giersbergen PLM. Investigation of the mutual pharmacokinetic interactions between bosentan, a dual endothelin receptor antagonist, and simvastatin. Clinical Pharmacokinetics 2003; 42: 293-301.[PubMed]|
|8.||Villikka K, Kivisto KT, Neuvonen PJ. The effect of dexamethasone on the pharmacokinetics of triazolam. Pharmacol Toxicol 1998; 83: 135-38.[PubMed]|
|9.||Robertson SM, Davey RT, Voell J, Formentini E, Alfaro RM, Penzak SR. Effect of Ginkgo biloba extract on lopinavir, midazolarn and fexofenadine pharmacokinetics in healthy subjects. Current Medical Research and Opinion 2008; 24: 591-99.[PubMed]|
|10.||Ochs HR, Greenblatt DJ, Burstein ES. Lack of influence of cigarette smoking on triazolam pharmacokinetics. British Journal of Clinical Pharmacology 1987; 23: 759-63.[PubMed]|
|11.||Ahonen J, Olkkola KT, Neuvonen PJ. Effect of itraconazole and terbinafine on the pharmacokinetics and pharmacodynamics of midazolam in healthy volunteers. British Journal of Clinical Pharmacology 1995; 40: 270-72.[PubMed]|
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