"The U.S. Food and Drug Administration today approved Tivicay (dolutegravir), a new drug to treat HIV-1 infection.
Tivicay is an integrase strand transfer inhibitor that interferes with one of the enzymes necessary for HIV to multiply. "...
No data are available on overdose of STRIBILD in patients. If overdose occurs the patient must be monitored for evidence of toxicity. Treatment of overdose with STRIBILD consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient.
Elvitegravir: Limited clinical experience is available at doses higher than the therapeutic dose of elvitegravir. In one study, boosted elvitegravir equivalent to 2 times the therapeutic dose of 150 mg once daily for 10 days was administered to 42 healthy subjects. No severe adverse reactions were reported. The effects of higher doses are not known. As elvitegravir is highly bound to plasma proteins, it is unlikely that it will be significantly removed by hemodialysis or peritoneal dialysis.
Cobicistat: Limited clinical experience is available at doses higher than the therapeutic dose of cobicistat. In two studies, a single dose of cobicistat 400 mg (2.7 times the dose in STRIBILD) was administered to a total of 60 healthy subjects. No severe adverse reactions were reported. The effects of higher doses are not known. As cobicistat is highly bound to plasma proteins, it is unlikely that it will be significantly removed by hemodialysis or peritoneal dialysis.
Emtricitabine: Limited clinical experience is available at doses higher than the therapeutic dose of EMTRIVA. In one clinical pharmacology study, single doses of emtricitabine 1200 mg (6 times the dose in STRIBILD) were administered to 11 subjects. No severe adverse reactions were reported. The effects of higher doses are not known.
Hemodialysis treatment removes approximately 30% of the emtricitabine dose over a 3 hour dialysis period starting within 1.5 hours of emtricitabine dosing (blood flow rate of 400 mL per minute and a dialysate flow rate of 600 mL per minute). It is not known whether emtricitabine can be removed by peritoneal dialysis.
Tenofovir DF: Limited clinical experience at doses higher than the therapeutic dose of VIREAD 300 mg is available. In one study, 600 mg tenofovir DF (2 times the dosage in STRIBILD) was administered to 8 subjects orally for 28 days, and no severe adverse reactions were reported. The effects of higher doses are not known. Tenofovir is efficiently removed by hemodialysis with an extraction coefficient of approximately 54%. Following a single 300 mg dose of VIREAD, a 4-hour hemodialysis session removed approximately 10% of the administered tenofovir dose.
Coadministration of STRIBILD is contraindicated with drugs that are highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events. These drugs and other contraindicated drugs (which may lead to reduced efficacy of STRIBILD and possible resistance) are listed in Table 1 [see DRUG INTERACTIONS, CLINICAL PHARMACOLOGY].
Table 1 : Drugs that are Contraindicated with STRIBILD
|Drug Class||Drugs within class that are contraindicated with STRIBILD||Clinical Comment|
|Alpha 1-Adrenoreceptor Antagonist||Alfuzosin||Potential for increased alfuzosin concentrations, which can result in hypotension.|
|Antimycobacterial||Rifampin||Rifampin is a potent inducer of CYP450 metabolism and may cause significant decrease in the plasma concentration of elvitegravir and cobicistat. This may result in loss of therapeutic effect to STRIBILD.|
|Ergot Derivatives||Dihydroergotamine Ergotamine Methylergonovine||Potential for serious and/or life-threatening events such as acute ergot toxicity characterized by peripheral vasospasm and ischemia of the extremities and other tissues.|
|GI Motility Agent||Cisapride||Potential for serious and/or life-threatening events such as cardiac arrhythmias.|
|Herbal Products||St. John’s wort (Hypericum perforatum)||Coadministration of products containing St. John’s wort and STRIBILD may result in reduced plasma concentrations of elvitegravir and cobicistat. This may result in loss of therapeutic effect and development of resistance.|
|HMG-CoA Reductase Inhibitors||Lovastatin Simvastatin||Potential for serious reactions such as myopathy, including rhabdomyolysis.|
|Neuroleptic||Pimozide||Potential for serious and/or life-threatening events such as cardiac arrhythmias.|
|Phosphodiesterase-5 (PDE5) Inhibitor||Sildenafila when dosed as REVATIO for the treatment of pulmonary arterial hypertension||There is increased potential for sildenafil-associated adverse events (which include visual disturbances, hypotension, priapism, and syncope).|
|Sedative/hypnotics||Triazolam Orally administered midazolamb||Triazolam and orally administered midazolam are extensively metabolized by CYP3A4. Coadministration of triazolam or orally administered midazolam with STRIBILD may cause large increases in the concentration of these benzodiazepines. The potential exists for serious and/or life threatening events such as prolonged or increased sedation or respiratory depression.|
|a See DRUG INTERACTIONS Table 6 for
sildenafil when dosed as VIAGRA for erectile dysfunction.
b See DRUG INTERACTIONS, Table 6 for parenterally administered midazolam.
Last reviewed on RxList: 1/2/2015
This monograph has been modified to include the generic and brand name in many instances.
Additional Stribild Information
- Stribild Drug Interactions Center: elvitegr-cobicist-emtric-tenof oral
- Stribild Side Effects Center
- Stribild FDA Approved Prescribing Information including Dosage
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
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