"The U.S. Food and Drug Administration today approved Tivicay (dolutegravir), a new drug to treat HIV-1 infection.
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In a healthy volunteer repeat-dose pharmacokinetic study evaluating high-dose combinations of LEXIVA plus ritonavir, an increased frequency of Grade 2/3 ALT elevations (greater than 2.5 x ULN) was observed with LEXIVA 1,400 mg twice daily plus ritonavir 200 mg twice daily (4 of 25 subjects). Concurrent Grade ½ elevations in AST (greater than 1.25 x ULN) were noted in 3 of these 4 subjects. These transaminase elevations resolved following discontinuation of dosing.
There is no known antidote for LEXIVA. It is not known whether amprenavir can be removed by peritoneal dialysis or hemodialysis. If overdosage occurs, the patient should be monitored for evidence of toxicity and standard supportive treatment applied as necessary.
LEXIVA is contraindicated:
- in patients with previously demonstrated clinically significant hypersensitivity (e.g., Stevens-Johnson syndrome) to any of the components of this product or to amprenavir.
- when coadministered with drugs that are highly dependent on CYP3A4 for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events (Table 1).
Table 1: Drugs Contraindicated With LEXIVA (Information
in the table applies to LEXIVA with or without ritonavir, unless otherwise
|Drug Class/Drug Name||Clinical Comment|
|Alpha 1-adrenoreceptor antagonist: Alfuzosin||Potentially increased alfuzosin concentrations can result in hypotension|
|Antiarrhythmics: Flecainide, propafenone||POTENTIAL for serious and/or life-threatening reactions such as cardiac arrhythmias secondary to increases in plasma concentrations of antiarrhythmics if LEXIVA is co-prescribed with ritonavir.|
|Antimycobacterials: Rifampina||May lead to loss of virologic response and possible resistance to LEXIVA or to the class of protease inhibitors.|
|Ergot derivatives: Dihydroergotamine, ergonovine, ergotamine, methylergonovine||POTENTIAL for serious and/or life-threatening reactions such as acute ergot toxicity characterized by peripheral vasospasm and ischemia of the extremities and other tissues.|
|GI motility agents: Cisapride||POTENTIAL for serious and/or life-threatening reactions such as cardiac arrhythmias.|
|Herbal products: St. John's wort (Hypericum perforatum)||May lead to loss of virologic response and possible resistance to LEXIVA or to the class of protease inhibitors.|
|HMG co-reductase inhibitors: Lovastatin, simvastatin||POTENTIAL for serious reactions such as risk of myopathy including rhabdomyolysis.|
|Neuroleptic: Pimozide||POTENTIAL for serious and/or life-threatening reactions such as cardiac arrhythmias.|
|Non-nucleoside reverse transcriptase inhibitor: Delavirdinea||May lead to loss of virologic response and possible resistance to delavirdine.|
|PDE5 inhibitor: Sildenafil (REVATIO®) (for treatment of pulmonary arterial hypertension)||A safe and effective dose has not been established when used with LEXIVA. There is increased potential for sildenafil-associated adverse events (which include visual disturbances, hypotension, prolonged erection, and syncope).|
|Sedative/hypnotics: Midazolam, triazolam||POTENTIAL for serious and/or life-threatening reactions such as prolonged or increased sedation or respiratory depression.|
|a See CLINICAL PHARMACOLOGY Tables 10, 11, 12, or 13 for magnitude of interaction.|
when coadministered with ritonavir in patients receiving the antiarrhythmic agents flecainide and propafenone. If LEXIVA is coadministered with ritonavir, reference should be made to the full prescribing information for ritonavir for additional contraindications.
Last reviewed on RxList: 3/1/2013
This monograph has been modified to include the generic and brand name in many instances.
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