TIVICAY Dosage & Rx Info | Uses, Side Effects

Tivicay Generic Name & Formulations

Legal Class

General Description

Dolutegravir 50mg; tabs.

Pharmacological Class

HIV-1 integrase strand transfer inhibitor (INSTI).

How Supplied

Tabs—30; PD—60 (w. dosing cup + oral dosing syringe)

Manufacturer

ViiV Healthcare

Generic Availability

Mechanism of Action

Dolutegravir inhibits HIV integrase by binding to the integrase active site and blocking the strand transfer step of retroviral DNA integration which is essential for the HIV replication cycle.

Tivicay Indications

Indications

In combination with other antiretroviral agents for treatment of HIV-1 infection in adults (treatment-naïve or -experienced) and in pediatric patients (treatment-naïve or -experienced but integrase strand transfer inhibitor [INSTI]-naïve) aged ≥4weeks and weighing ≥3kg. In combination with rilpivirine as a complete regimen for treatment of HIV-1 infection in adults to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA <50 copies per mL) on a stable antiretroviral regimen for ≥6 months with no history of treatment failure or known substitutions associated with resistance to either antiretroviral agent.

Tivicay Dosage and Administration

Adult

Treatment-naïve or treatment-experienced INSTI-naïve or virologically suppressed adults switching to dolutegravir + rilpivirine: 50mg once daily. Treatment-naïve or treatment-experienced INSTI-naïve when concomitant with certain UDP-UGT1A or CYP3A inducers: 50mg twice daily. INSTI-experienced with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance: 50mg twice daily.

Children

See full labeling. <4weeks, <3kg, or INSTI-experienced with documented or clinically suspected resistance to other INSTIs (eg, raltegravir, elvitegravir): not established. ≥4weeks: (≥20kg): 50mg once daily. If concomitant with certain UGT1A or CYP3A inducers, increase weight-based dose to twice daily.

Tivicay Contraindications

Contraindications

Concomitant dofetilide.

Tivicay Boxed Warnings

Not Applicable

Tivicay Warnings/Precautions

Warnings/Precautions

Tabs and tabs for oral susp are not interchangeable on a mg per mg basis. Discontinue if hypersensitivity reactions develop. Increased risk for worsening/development of elevated transaminases in patients with underlying hepatitis B or C; monitor for hepatotoxicity. Severe hepatic impairment: not recommended. INSTI-experienced patients (with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance) with severe renal impairment: may result in loss of efficacy and development of resistance. Dialysis. Elderly. Pregnancy. Nursing mothers: see full labeling for potential risks in infants.

Tivicay Pharmacokinetics

Absorption

Peak plasma concentrations were observed 1–3 hours postdose. Steady state is achieved within ~5 days.

Distribution

Apparent volume of distribution: 17.4 L (after a 50mg once daily dose). Plasma protein bound: ≥98.9%.

Metabolism

UGT1A1 (primarily), CYP3A.

Elimination

Fecal (53%), renal (31%). Half-life: ~14 hours. Apparent clearance: 1.0 L/hr.

Tivicay Interactions

Interactions

Avoid concomitant nevirapine, oxcarbazepine, phenytoin, phenobarbital, St. John’s wort. Avoid etravirine unless coadministered with atazanavir/ritonavir, darunavir/ritonavir, or lopinavir/ritonavir. Concomitant efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, rifampin, or carbamazepine: adjust dose (see Adults, Children). May be affected by drugs that induce or inhibit UGT1A1, UGT1A3, UGT1A9, BCRP, and P-gp enzymes or transporters. May potentiate drugs eliminated via OCT2 or MATE1 (eg, dofetilide, dalfampridine, metformin). Concomitant cation-containing antacids, laxatives, sucralfate, buffered drugs, or oral iron/calcium supplements (also can give together with a meal): give dolutegravir 2hrs before or 6hrs after.

Tivicay Adverse Reactions

Adverse Reactions

Insomnia, fatigue, headache; hypersensitivity reactions, hepatotoxicity, immune reconstitution syndrome.

Tivicay Clinical Trials

See Literature

Tivicay Note

Notes

Tivicay Patient Counseling