| 1. Accepted major perpetrators | 2. Rejected perpetrators | 3. Unclassifiable | 4. Full table |
saquinavir/ritonavir is a strong inhibitor of CYP3A.
|Strong inhibitors||clarithromycin  |
grapefruit juice 
- Strong inhibitors: ≥ 5-fold increase in AUC or ≥ 80% decrease in clearance of in vivo CYP probe.
Footnotes and References
|a.||assessment based on product information accessed via the Therapeutic Goods Administration of Australia Product and Consumer Medicines Information website ( https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/PICMI?OpenForm&t=PI&q=&r=https://www.ebs.tga.gov.au/ ).|
|1.||Gorski JC, Jones DR, Haehner-Daniels BD, Hamman MA, O'Mara EM, Hall SD. The contribution of intestinal and hepatic CYP3A to the interaction between midazolam and clarithromycin. Clinical Pharmacology & Therapeutics 1998; 64: 133-43.[PubMed]|
|2.||Kivisto KT, Lamberg TS, Kantola T, Neuvonen PJ. Plasma buspirone concentrations are greatly increased by erythromycin and itraconazole. Clinical Pharmacology & Therapeutics 1997; 62: 348-54.[PubMed]|
|3.||Lilja JJ, Kivisto KT, Backman JT, Lamberg TS, Neuvonen PJ. Grapefruit juice substantially increases plasma concentrations of buspirone. Clinical Pharmacology & Therapeutics 1998; 64: 655-60.[PubMed]|
|4.||Olkkola KT, Backman JT, Neuvonen PJ. Midazolam should be avoided in patients receiving the systemic antimycotics ketoconazole or itraconazole. Clinical Pharmacology & Therapeutics 1994; 55: 481-85.[PubMed]|
|5.||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]|
|6.||Culm-Merdek KE, von Moltke LL, Gan L, Horan KA, Reynolds R, Harmatz JS, Court MH, Greenblatt DJ. Effect of extended exposure to grapefruit juice on cytochrome P450 3A activity in humans: Comparison with ritonavir. Clinical Pharmacology & Therapeutics 2006; 79: 243-54.[PubMed]|
|7.||Palkama VJ, Ahonen J, Neuvonen PJ, Olkkola KT. Effect of saquinavir on the pharmacokinetics and pharmacodynamics of oral and intravenous midazolam. Clinical Pharmacology & Therapeutics 1999; 66: 33-39.[PubMed]|
|8.||Abel S, Russell D, Taylor-Worth RJ, Ridgway CE, Muirhead GJ. Effects of CYP3A4 inhibitors on the pharmacokinetics of maraviroc in healthy volunteers. British Journal of Clinical Pharmacology 2008; 65: 27-37.[PubMed]|
|9.||Saari TI, Laine K, Leino K, Valtonen M, Neuvonen PJ, Olkkola KT. Effect of voriconazole on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Clinical Pharmacology & Therapeutics 2006; 79: 362-70.[PubMed]|
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