Interaction Checker
No Interaction Expected
_ZZNelfinavir#
Varenicline
Quality of Evidence: Very Low
Summary:
Description:
Based on varenicline characteristics and clinical experience to date, varenicline has no clinically meaningful drug interactions. No dosage adjustment of varneicline or co-administered medicinal products listed below is recommended. In vitro studies indicate that varenicline is unlikely to alter the pharmacokinetics of compounds that are primarily metabolised by cytochrome P450 enzymes. Furthermore since metabolism of varenicline represents less than 10% of its clearance, active substances known to affect the cytochrome P450 system are unlikely to alter the pharmacokinetics of varenicline and therefore a dose adjustment of varenicline would not be required. In vitro studies demonstrate that varenicline does not inhibit human renal transport proteins at therapeutic concentrations. Therefore, active substances that are cleared by renal secretion are unlikely to be affected by varenicline.
Champix Summary of Product Characteristics, Pfizer Ltd, August 2008.
No clinically meaningful pharmacokinetic drug-drug interactions have been identified. In vitro studies demonstrated that varenicline does not inhibit the following cytochrome P450 enzymes (IC50 >6400 ng/mL): 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4/5. Also, in human hepatocytes in vitro, varenicline does not induce the cytochrome P450 enzymes 1A2 and 3A4. In vitro studies demonstrated the active renal secretion of varenicline is mediated by the human organic cation transporter, OCT2. Co-administration with inhibitors of OCT2 may not require a dose adjustment of varenicline as the increase in systemic exposure to varenicline is not expected to be clinically meaningful. Furthermore, since metabolism of varenicline represents less than 10% of its clearance, drugs known to affect the cytochrome P450 system are unlikely to alter the pharmacokinetics of varenicline and therefore a dose adjustment of varenicline would not be required.
Chantix Prescribing Information, Pfizer Inc, May 2008.
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