Generic Dolutegravir

Introduction

Dolutegravir is an antiretroviral medication used to treat human immunodeficiency virus (HIV) infection. It belongs to the integrase strand transfer inhibitor (INSTI) class, which blocks a key step in the HIV replication cycle. In the United Kingdom, dolutegravir is a cornerstone of modern combination therapy for both treatment‑naïve and treatment‑experienced adults. The active compound is dolutegravir, and the medication is listed under the HIV therapeutic group by the Medicines and Healthcare products Regulatory Agency (MHRA). Although its primary indication is HIV‑1 infection, dolutegravir is also incorporated in fixed‑dose combinations for pre‑exposure prophylaxis (PrEP) in clinical trials.

What is Dolutegravir?

Dolutegravir is the generic version of Tivicay®, the original brand developed by ViiV Healthcare. Both contain the same active compound, dolutegravir, and meet identical quality and bioequivalence standards set by the European Medicines Agency (EMA). Our online pharmacy provides this generic alternative as a cost‑effective treatment option for patients who require lifelong HIV management.

The drug is classified as an integrase strand transfer inhibitor (INSTI). It was first approved in the European Union in 2014 after extensive phase III trials demonstrated superior viral suppression compared with earlier regimens. Manufacturing is undertaken by several WHO‑prequalified firms under strict Good Manufacturing Practice (GMP) conditions.

How Dolutegravir Works

Dolutegravir targets the HIV integrase enzyme, which catalyzes the insertion of viral DNA into the host cell genome. By binding to the active site of integrase and chelating the essential magnesium ions, dolutegravir prevents strand transfer, thereby halting integration. Without integration, the proviral DNA cannot be transcribed into new viral particles, leading to a rapid decline in plasma HIV‑RNA levels.

Key pharmacokinetic features:

• Absorption: Oral tablets are absorbed with a bioavailability of ~78 % under fasting conditions; food increases exposure by ~30 % but does not require dose adjustment.
• Onset: Plasma concentrations reach steady state within 4–5 days of once‑daily dosing.
• Distribution: The drug exhibits a volume of distribution of ~120 L, indicating extensive tissue penetration, including the central nervous system.
• Elimination: Primarily hepatic metabolism via UGT1A1, with a minor contribution from CYP3A4. The terminal half‑life is approximately 14 hours, supporting once‑daily dosing.

Conditions Treated with Dolutegravir

• HIV‑1 infection (adults) – First‑line or part of salvage regimens, either as monotherapy (in selected cases) or in fixed‑dose combinations (e.g., dolutegravir/lamivudine, dolutegravir/abacavir/lamivudine).
• HIV‑2 infection (selected patients) – Limited data support use in combination therapy where resistance patterns allow.
• Pregnancy (as part of combination therapy) – Recommended by British HIV Association (BHIVA) guidelines for pregnant women with a high barrier to resistance.

In the UK, roughly 105,000 people are living with HIV, and national targets aim for ≥95 % viral suppression. Dolutegravir’s high potency and high genetic barrier to resistance make it instrumental in achieving these public‑health goals.

Who is Dolutegravir For?

Dolutegravir is appropriate for adult patients (≥18 years) who require an effective, once‑daily antiretroviral agent with a robust resistance profile. Typical clinical scenarios include:

• Treatment‑naïve individuals – Those starting therapy for the first time, regardless of baseline viral load, as recommended by BHIVA first‑line guidance.
• Treatment‑experienced patients – Individuals with documented resistance to older INSTIs (e.g., raltegravir, elvitegravir) but still susceptible to dolutegravir.
• Pregnant women – When the benefits of viral suppression outweigh potential teratogenic concerns; dolutegravir is now considered safe after the first trimester, with close monitoring.
• Patients with renal or hepatic impairment – Dolutegravir can be used without dose adjustment in mild to moderate impairment; severe hepatic dysfunction (Child‑Pugh C) requires specialist assessment.

Contra‑indications or cautionary use:

• Known hypersensitivity to dolutegravir or any tablet excipients.
• Co‑administration with potent UGT1A1 inducers (e.g., rifampicin) without dose adjustment, as they reduce drug exposure.
• Women of child‑bearing potential not using effective contraception during the first trimester, due to early‑pregnancy safety data concerns.

Risks, Side Effects, and Interactions

Common

• Headache – Usually mild and transient.
• Insomnia – Reported in up to 10 % of patients; timing of dose may be adjusted.
• Nausea and abdominal discomfort – Often resolve within the first two weeks.
• Fatigue – May be multifactorial; assess for anemia or concurrent infections.

Rare

• Elevated serum creatinine – Reflects inhibition of tubular secretion rather than true nephrotoxicity; monitor renal function.
• Skin rash – Typically maculopapular; discontinue if severe or accompanied by systemic symptoms.
• Depression or mood changes – Small incidence; patients with a history of psychiatric illness should be monitored.

Serious

• Severe hypersensitivity reactions – Includes Stevens‑Johnson syndrome or toxic epidermal necrolysis; immediate discontinuation required.
• Hepatic toxicity – Rare elevations in transaminases; consider alternative therapy if ALT/AST >5 × ULN.
• Immune reconstitution inflammatory syndrome (IRIS) – May occur after rapid viral suppression; manage with supportive care and, if needed, corticosteroids.

Drug–Drug Interactions

• Rifampicin – Requires dolutegravir 50 mg twice daily (or 100 mg once daily with boosted atazanavir).
• Anticonvulsants (e.g., carbamazepine, phenobarbital) – May lower dolutegravir levels; consider alternative antiretroviral or dose adjustment.
• Metformin – Dolutegravir increases metformin exposure; monitor for lactic acidosis and adjust metformin dose as needed.
• Hormonal contraceptives – No clinically significant interaction; however, adherence to dosing schedule is essential.

Patients should always provide a complete medication list to their prescriber to evaluate potential interactions.

Practical Use: Dosing, Missed Dose, Overdose

• Standard adult dose: 50 mg dolutegravir taken orally once daily, with or without food. In fixed‑dose combinations, the dosage is incorporated into the tablet.
• Renal or hepatic impairment: No adjustment needed for CrCl ≥ 30 mL/min or mild‑to‑moderate hepatic disease.
• Missed dose: If less than 12 hours have passed, take the missed tablet immediately and continue with the next scheduled dose. If more than 12 hours have elapsed, skip the missed dose and resume the regular schedule; do not double‑dose.
• Overdose: Symptoms may include nausea, vomiting, dizziness, or headache. Seek urgent medical advice; supportive care is the mainstay of treatment.

Precautions:

• Avoid concomitant use of strong UGT1A1 inducers without dose modification.
• Alcohol does not affect dolutegravir pharmacokinetics but may exacerbate hepatic side effects.
• Counsel patients on adherence; missed doses can lead to viral rebound and resistance development.

Buying Dolutegravir from Our Online Pharmacy

Dolutegravir can be purchased safely from our online pharmacy in the UK. Our service combines affordability with quality assurance:

• Near‑manufacturer pricing – We negotiate directly with WHO‑prequalified suppliers, passing savings on to the patient.
• Verified quality – All batches are sourced from licensed manufacturers that comply with GMP standards and are inspected by third‑party auditors.
• Discreet, reliable delivery – Orders are packaged in unmarked parcels and dispatched via a tracked service, typically arriving within 7 days for express or 2‑3 weeks for standard airmail.
• Online‑only access – For patients facing limited availability through traditional pharmacies or insurance schemes, our pharmacy broker model connects you with overseas licensed pharmacies that legally export the medication to the UK.

Our platform respects patient privacy, maintains strict data protection protocols, and offers a user‑friendly ordering interface. The service is intended for individuals seeking a cost‑effective, high‑quality generic alternative to brand‑name dolutegravir.

FAQ

• Is dolutegravir available in both brand‑name and generic forms in the UK?
  Yes. The original brand‑name product is Tivicay® produced by ViiV Healthcare, while multiple generic manufacturers supply dolutegravir tablets that contain the same active compound and meet the same regulatory standards.

• Does dolutegravir require refrigeration or special storage conditions?
  No. The tablets should be stored at controlled room temperature (15–30 °C), protected from excess moisture, heat, and direct sunlight. Refrigeration is not required.

• What does the dolutegravir tablet look like, and are there any distinguishing markings?
  Generic dolutegravir tablets are typically round, white to off‑white, and bear a score line for easy splitting. Imprint codes vary by manufacturer but are listed on the product packaging for verification.

• Can dolutegravir be taken with other antiretroviral drugs in a fixed‑dose combination?
  Yes. Dolutegravir is commonly co‑formulated with lamivudine (and optionally abacavir) in a single tablet taken once daily. Fixed‑dose combinations simplify regimens and improve adherence.

• Are there any specific warnings for people of Asian descent taking dolutegravir?
  Population‑specific data do not indicate a unique safety signal for Asian patients. However, genetic variations in UGT1A1 activity can affect drug metabolism, so clinicians may monitor liver function tests more closely in patients with known polymorphisms.

• How does dolutegravir compare to older INSTIs such as raltegravir?
  Dolutegravir has a higher genetic barrier to resistance, a longer half‑life allowing once‑daily dosing, and demonstrated superior viral suppression in head‑to‑head trials (e.g., FLAMINGO study). Raltegravir requires twice‑daily dosing and has a lower barrier to resistance.

• What are the travel considerations for carrying dolutegravir across international borders?
  Carry a copy of the prescription or a doctor’s letter, keep the medication in its original packaging, and declare it at customs if required. The UK’s Personal Importation Scheme permits up to 90 days’ supply for personal use, provided documentation is available.

• Does dolutegravir affect results of standard drug‑testing panels?
  No. Dolutegravir is not a substance screened for in typical workplace or sports drug‑testing panels, and it does not produce false‑positive results in standard immunoassays.

• Are there any known differences between dolutegravir formulations approved in the EU versus the US?
  The active ingredient and dosage are identical, but excipients may differ slightly (e.g., lactose content). These differences are generally clinically insignificant but may be relevant for patients with specific allergies or intolerances.

• What is the history behind the development of dolutegravir?
  Dolutegravir was discovered by ViiV Healthcare through a structure‑based design programme targeting the integrase enzyme. After pre‑clinical optimization, it entered Phase I trials in 2009, followed by pivotal Phase III studies (SPRING‑1, SINGLE, FLAMINGO) that demonstrated rapid viral load decline and a favorable safety profile, leading to its EMA approval in 2014.

Glossary

Integrase Strand Transfer Inhibitor (INSTI)

A class of antiretroviral drugs that block the HIV integrase enzyme, preventing insertion of viral DNA into the host genome.

Genetic Barrier to Resistance

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

Good Manufacturing Practice (GMP)

International quality standards that ensure medicines are consistently produced and controlled according to strict guidelines.

⚠️ Disclaimer

The information provided about Dolutegravir is for general knowledge only. It does not replace professional medical consultation. All treatment decisions should be made under the supervision of a qualified healthcare provider. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to Dolutegravir for individuals who may have limited availability through traditional pharmacies, prescription‑based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication.