Generic Dolutegravir

Introduction

Dolutegravir is an antiretroviral medication used primarily for the treatment of HIV-1 infection. It is available as a 50 mg oral tablet and belongs to the integrase strand transfer inhibitor (INSTI) class. The drug was developed by ViiV Healthcare and is marketed worldwide under brand names such as Tivicay and Dolutegravir-DTG. Its main indication is in combination regimens for adults with HIV-1, and it is also approved for use in certain pediatric populations. Secondary investigational uses have been explored, but they remain off-label.

What is Dolutegravir?

Dolutegravir is a synthetic small-molecule inhibitor of the HIV-1 integrase enzyme. The medication was approved by the U.S. Food and Drug Administration (FDA) in August 2013 and later by the European Medicines Agency (EMA). It is supplied as a film-coated 50 mg tablet for oral administration.

How Dolutegravir Works

Dolutegravir binds to the active site of the HIV-1 integrase enzyme and blocks the strand-transfer step required for viral DNA to integrate into the host genome. By preventing integration, the drug halts the production of new virus particles. The inhibition is potent, with a long intracellular half-life that supports once-daily dosing. After oral intake, peak plasma concentrations are reached within 2-3 hours; the drug is primarily eliminated unchanged in the feces, with a minority (~10 %) excreted renally.

Conditions Treated with Dolutegravir

• HIV-1 infection (adults) - Used in fixed-dose combinations (e.g., dolutegravir-lamivudine-abacavir) or as a single agent with two nucleos(t)ide reverse-transcriptase inhibitors (NRTIs).
• HIV-1 infection (treatment-naïve adults) - Recommended by the WHO and major guidelines as a first-line component because of its high barrier to resistance and favorable safety profile.

These indications are supported by large phase III trials (e.g., SPRING-2, SINGLE, and FLAMINGO) which demonstrated non-inferior or superior virologic suppression compared with earlier INSTIs or protease inhibitors.

Off-Label and Investigational Uses of Dolutegravir

• Pre-exposure prophylaxis (PrEP) for high-risk individuals - Small pilot studies have examined dolutegravir-based regimens as an alternative to tenofovir-emtricitabine; efficacy data are still emerging and the approach is not approved.
• HIV-2 infection - Limited case series suggest activity against HIV-2 integrase, but regulatory agencies have not granted formal approval.
• Potential role in latent reservoir reduction - Early-phase research investigates dolutegravir in combination with latency-reversing agents to target dormant HIV cells.

These applications are experimental. Patients should not use dolutegravir for any off-label purpose without direct supervision from a qualified healthcare professional.

Is Dolutegravir the Right Medication for You?

Dolutegravir is most appropriate for:

• Adults with confirmed HIV-1 infection who are starting antiretroviral therapy (ART) or switching from a failing regimen.
• Individuals who require a once-daily pill with a high genetic barrier to resistance.
• Patients without significant drug-drug interaction concerns (e.g., certain anticonvulsants, rifampicin).

Contraindications include known hypersensitivity to dolutegravir or any tablet excipients, and concurrent use of medicines that markedly reduce dolutegravir exposure without dose adjustment. Caution is advised in pregnant women (category B) and in patients with severe hepatic impairment (Child-Pugh C), where dosage modification may be required.

Risks, Side Effects, and Interactions

Common

• Headache
• Nausea or vomiting
• Diarrhea
• Insomnia
• Fatigue

Rare

• Increased serum creatinine (due to inhibition of renal tubular secretion)
• Elevated liver enzymes (ALT/AST)
• Rash (including mild maculopapular eruption)

Serious

• Severe hypersensitivity reactions (e.g., Stevens-Johnson syndrome)
• Neuropsychiatric events (e.g., depression, mood changes, suicidal ideation) - reported at low frequency but require prompt evaluation.

Drug-Drug Interactions

• Rifampicin: reduces dolutegravir levels; co-administration requires dolutegravir 50 mg twice daily.
• Anticonvulsants (e.g., carbamazepine, phenytoin, phenobarbital): lower dolutegravir exposure; alternative therapy or dose adjustment is needed.
• Metformin: dolutegravir can increase metformin plasma concentration; monitor for lactic acidosis.

Drug-Food Interactions

Dolutegravir may be taken with or without food. High-fat meals modestly increase exposure but do not affect efficacy. Caution with antacids or supplements containing polyvalent cations (e.g., calcium, magnesium) within 2 hours of dosing, as they can diminish absorption.

Use: Dosing, Missed Dose, Overdose

• Standard dosing: One 50 mg tablet taken orally once daily, with or without food.
• Special populations: For patients on rifampicin, the dose is increased to 50 mg twice daily. In severe hepatic impairment, a 25 mg daily dose may be considered under medical guidance.
• Missed dose: Take the missed tablet as soon as remembered unless the next scheduled dose is within 12 hours. In that case, skip the missed tablet and resume the regular schedule; do not double-dose.
• Overdose: No specific antidote exists. Supportive care and gastrointestinal decontamination (if within 1 hour) are recommended. Seek immediate medical attention.
• Practical precautions: Alcohol does not interact directly but excessive intake may worsen neuropsychiatric side effects. Operating machinery is permissible if the patient feels mentally clear; caution is advised if dizziness or insomnia occurs.

FAQ

• What should I do if I travel abroad with dolutegravir?   Carry the medication in its original packaging with a copy of the prescription. Store tablets at room temperature, away from direct sunlight, and keep them in your hand-luggage to avoid temperature extremes in checked baggage.

• Can dolutegravir be crushed or split?   The film coating is not essential for drug absorption, so tablets may be split if a lower dose is required, but they should not be crushed because this can affect taste and may increase the risk of accidental ingestion by children.

• How long does a dolutegravir tablet stay stable after opening the bottle?   Tablets remain chemically stable for up to 24 months from the manufacture date when stored in a dry, cool environment, provided the container is tightly closed.

• Are there any known differences in dolutegravir formulation between regions?   Yes. Some markets use tablet fillers such as lactose, while others use rice starch. Patients with specific allergies should review the excipient list on the packaging or ask the pharmacy for a detailed ingredient sheet.

• Is dolutegravir detectable on standard drug-screening tests?   Dolutegravir is not screened for in routine occupational or athletic drug tests because it is not a controlled substance and does not interfere with most immunoassays.

• Can I take dolutegravir with herbal supplements like St John’s wort?   St John’s wort induces enzymes that can lower dolutegravir concentrations, potentially reducing efficacy. Patients should discuss any herbal products with a qualified professional before combining them.

• What is the significance of the modest rise in serum creatinine seen with dolutegravir?   Dolutegravir inhibits renal tubular secretion of creatinine without affecting glomerular filtration, resulting in a harmless increase of about .1-.2 mg/dL. This does not indicate kidney damage but should be distinguished from true renal impairment.

• How does dolutegravir compare with earlier INSTIs like raltegravir?   Dolutegravir has a longer plasma half-life (≈14 hours) allowing once-daily dosing, and it possesses a higher genetic barrier to resistance, meaning mutations that confer resistance are less likely to develop compared with raltegravir.

• Is there any benefit to taking dolutegravir at night versus morning?   Pharmacokinetic data show similar exposure regardless of dosing time. Patients may choose the time that best fits their routine, as long as the schedule is consistent.

• What should I know about dolutegravir and pregnancy?   Clinical data from the DOBRA and Tsepamo studies suggest dolutegravir does not increase the risk of major congenital anomalies. However, it is still classified as a pregnancy category B medication, and treatment decisions should be individualized with obstetric input.

• Can dolutegravir cause weight changes?   Weight gain has been observed in some patients on dolutegravir-based regimens, particularly when combined with tenofovir alafenamide and emtricitabine. Monitoring body weight and metabolic parameters is recommended during routine follow-up.

Glossary

Integrase Strand Transfer Inhibitor (INSTI)

A class of antiretroviral drugs that block the HIV integrase enzyme, preventing viral DNA from integrating into the host cell’s genome.

Genetic Barrier to Resistance

The number and type of viral mutations required for a drug to lose effectiveness; a high barrier means resistance develops less readily.

Pharmacokinetics

The study of how a drug is absorbed, distributed, metabolized, and eliminated by the body.

Off-Label Use

Prescription of a medication for an indication, age group, dosage, or route of administration that has not received formal regulatory approval.

Buying Dolutegravir from Our Online Pharmacy

Dolutegravir can be obtained through our online pharmacy, a dedicated broker service that links patients with licensed overseas suppliers. The platform offers the generic 50 mg tablet at a price close to the manufacturer’s cost, providing a more affordable alternative to brand-name products. All shipments are sourced from verified, GMP-certified manufacturers, ensuring consistent quality and potency.

Customers benefit from discreet packaging and reliable delivery options, including express service (typically 7 days) and standard airmail (approximately 3 weeks). Because the service operates exclusively online, it reaches individuals in regions where local pharmacies may lack stock or where insurance coverage is limited. Privacy is a core principle; each order is processed with encrypted data handling and unmarked parcels to protect patient confidentiality.

Disclaimer

The material presented here on Dolutegravir is intended for informational purposes only and does not substitute for professional medical advice. Treatment decisions, including any off-label applications, must be made under the direct supervision of a qualified healthcare provider. Readers are presumed to be competent adults capable of informed health choices. Our online pharmacy supplies Dolutegravir to people who encounter restricted access through conventional pharmacies or insurance programs and who seek cost-effective generic options. Always discuss any medication changes with your clinician before initiating, modifying, or discontinuing therapy.