Tivicay

Generic name: dolutegravir

Drug class: HIV integrase strand transfer inhibitors (HIV-1 INSTI)

Dosage form: Tablets (oral; 10 mg, 25 mg, 50 mg); PD Tablet for suspension (oral; 5 mg)

Route of administration: Oral

Dose:

• Adults and pediatric patients aged 12 years and older weighing at least 40 kg: 50 mg once daily
• Adults and pediatric patients aged 12 years and older weighing at least 40 kg when coadministered with certain UGT1A or CYP3A inducers (e.g., efavirenz, fosamprenavir/ritonavir, tipranavir/ritonavir, rifampin): 50 mg twice daily
• Adults and pediatric patients aged 12 years and older with certain INSTI-associated resistance substitutions or clinically suspected INSTI resistance: 50 mg twice daily
• Pediatric patients aged 4 weeks and older weighing at least 3 kg: 5 mg once daily (TIVICAY PD tablets for oral suspension)

Mechanism of action: Dolutegravir is an integrase strand transfer inhibitor that blocks the HIV integrase enzyme, preventing the integration of viral DNA into the host cell genome, thereby inhibiting HIV replication.

Drug usage cases:

• Treatment of HIV-1 infection in adults and pediatric patients aged at least 4 weeks and weighing at least 3 kg, in combination with other antiretroviral agents
• Replacement of the current antiretroviral regimen in adults who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) on a stable regimen for at least 6 months, with no history of treatment failure or known substitutions associated with resistance to either antiretroviral agent, in combination with rilpivirine

Drug contraindications:

• Previous hypersensitivity reaction to dolutegravir
• Coadministration with dofetilide

Side effects:

• Common: Nausea, diarrhea, headache, rash, itching, vomiting, stomach pain or discomfort, abnormal dreams, fatigue, flatulence, increase in liver enzymes, increase in creatine phosphokinase
• Serious: Hypersensitivity reactions characterized by rash, fever, fatigue, swelling (including of the face or mouth), muscle or joint aches, and liver injury
• Other: Insomnia, fatigue, dizziness, abdominal pain, and elevated liver enzymes

Warnings:

• Hypersensitivity reactions have been reported; discontinue dolutegravir and other suspect agents immediately if signs or symptoms develop
• Hepatotoxicity has been observed; monitor liver function during therapy, especially in patients with underlying hepatitis B or C
• Immune reconstitution syndrome may occur; monitor for signs and symptoms
• Not interchangeable with TIVICAY PD tablets for oral suspension; use appropriate formulation based on patient age and weight
• Use during pregnancy may increase the risk of neural tube defects; discuss potential risks and benefits with a healthcare provider

Use during pregnancy or breastfeeding:

Dolutegravir should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Studies have shown an increased risk of neural tube defects when dolutegravir is taken at the time of conception or during the first six weeks of pregnancy. Women of childbearing potential should discuss contraceptive options with their healthcare provider while taking dolutegravir. The safety of dolutegravir during breastfeeding is not well established; consult a healthcare provider before breastfeeding while on this medication.