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Dolutegravir

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Dolutegravir is an integrase strand transfer inhibitor (INSTI) used in combination with other medications to treat HIV infection. It works by blocking the enzyme needed for the virus to replicate. This helps adults maintain a lower viral load and strengthens the immune system's response.


Category
Availability
In Stock
Delivery Time
Airmail (14-21 days) | EMS trackable (5-9 days)
Product is shipped in a fully discreet envelope with no content disclosure, including all required documentation inside

Product Sheet

Active Ingredient(s)
Dolutegravir Sodium
Reference Brand
Tivicay
Product Form
Tablet, Dispersible tablet
Regulatory Classification
Rx
Primary Category
Antiviral
Product Category
Infective diseases, Antivirals for systemic use, Integrase inhibitor
Pharmacological Class
HIV integrase strand transfer inhibitor (INSTI)
Manufacturer Description
A powerful antiviral medication used as part of a combination therapy to manage HIV.
Mechanism of Action
Dolutegravir prevents the HIV virus from replicating by blocking integrase, an enzyme the virus needs to insert its DNA into the body's cells.
Route of Administration
Oral
Onset Time
Rapid reduction in viral load within weeks
Duration
24 hours
Contraindications
Use with dofetilide
Severe Adverse Events
Liver problems, Severe skin rash, Hypersensitivity reactions, Mood changes
Common Side Effects
Trouble sleeping, Headache, Diarrhea
Uncommon Side Effects
Nausea, Weight gain, Dizziness, Fatigue
Drug Interactions
Metformin, Antacids, Iron supplements, St John's Wort
Pregnancy Safety Warnings
Can be used; discuss with your HIV specialist.
Age Restrictions
Adults and children over 4 weeks (weight dependent)
Storage Guidelines
Store in the original container to protect from moisture.
Related Products
Raltegravir, Bictegravir

Dolutegravir FAQ

Can I take dolutegravir with my daily multivitamin?

Dolutegravir may interact with mineral supplements containing calcium, iron, magnesium, or zinc, reducing its absorption. To avoid this, separate the dosing by at least two hours-take the antiretroviral first, then the multivitamin later.

Will dolutegravir affect my birth control pill?

Dolutegravir does not significantly induce or inhibit the enzymes that metabolise hormonal contraceptives, so it is unlikely to reduce their effectiveness. Nonetheless, discuss all concurrent medicines with your clinician to ensure optimal protection.

Do I need to take dolutegravir on an empty stomach?

No. Dolutegravir can be taken with or without food. A high-fat meal may increase drug exposure modestly, but this does not require dose adjustment.

What should I do if I miss a dose while traveling abroad?

If you remember the missed dose within 12 hours, take it as soon as possible. If it is close to the time of your next scheduled dose, skip the missed tablet and continue with your regular schedule. Do not double-dose.

Is dolutegravir safe for people with hepatitis B or C?

Dolutegravir itself is not hepatotoxic, but patients co-infected with hepatitis B or C should have regular liver function monitoring. The drug can be part of a regimen that also treats hepatitis B when combined with appropriate agents.

Can dolutegravir cause weight gain?

Clinical observations have noted modest weight increases in some patients, particularly when dolutegravir is paired with tenofovir alafenamide. The mechanism is not fully understood, and the benefit of viral suppression generally outweighs this effect.

Will my blood tests for drug screening detect dolutegravir?

Dolutegravir is not typically screened for in standard workplace or sports drug tests. It is not classified as a performance-enhancing or prohibited substance.

Is there a generic version of dolutegravir available in the UK?

Yes. The active ingredient, dolutegravir sodium, is available as a generic medication in the same 50 mg tablet formulation, subject to the same prescribing regulations.

How long does it take for dolutegravir to suppress the virus?

Most patients achieve an undetectable viral load within 8-12 weeks of initiating a fully suppressive regimen that includes dolutegravir, provided adherence is good.

What should I do if I develop a rash while on dolutegravir?

A mild rash is often self-limiting. However, if you notice widespread redness, swelling, blistering, or difficulty breathing, seek immediate medical care as this could represent a serious allergic reaction.

What is Dolutegravir?

Dolutegravir is an antiretroviral medication used to treat Human Immunodeficiency Virus (HIV) infection.

  • Therapeutic class: Integrase strand transfer inhibitor (INSTI)
  • Active ingredient: Dolutegravir sodium
  • Formulation: Oral pill, available in a fixed 50 mg strength
  • Regulatory status in the UK: Prescription-only medicine (POM) authorised by the Medicines and Healthcare products Regulatory Agency (MHRA) and marketed by ViiV Healthcare

Dolutegravir is not a cure for HIV but a core component of combination antiretroviral therapy (cART) that suppresses viral replication, helps maintain immune function, and reduces the risk of HIV transmission.

How Dolutegravir Works in the Body

Dolutegravir inhibits the HIV integrase enzyme, which is essential for inserting viral DNA into the host’s genome. By binding to the active site of integrase, the drug prevents the strand-transfer step of integration, halting the establishment of new infection cycles.

  • Onset of action: Viral load reduction is typically observed within weeks of starting therapy.
  • Peak plasma concentration: Reached 2-3 hours after oral dosing.
  • Half-life: Approximately 14 hours, supporting once-daily dosing.
  • Metabolism: Primarily glucuronidated by UDP-glucuronosyltransferase 1A1 (UGT1A1); minor oxidation via cytochrome P450 3A4.
  • Excretion: Mostly in the feces (≈80 %) and urine (≈20 %).

Because dolutegravir does not rely heavily on CYP enzymes, it has a relatively low potential for drug-drug interactions compared with many other antiretrovirals.

Conditions Treated by Dolutegravir

In the United Kingdom, dolutegravir is approved as part of combination regimens for the following indications:

  • Initial treatment of HIV-1 infection in adults and adolescents (≥12 years) with fully active virus.
  • Switch therapy for patients who are already virologically suppressed on a stable regimen, provided resistance testing shows no integrase-site mutations that affect dolutegravir.

Dolutegravir is used together with other antiretrovirals (e.g., nucleoside reverse-transcriptase inhibitors like tenofovir disoproxil fumarate/emtricitabine) to build a complete three-drug regimen.

Off-Label and Investigational Applications

Current peer-reviewed evidence does not support routine off-label use of dolutegravir for conditions outside HIV infection. Investigational studies have explored its role in HIV pre-exposure prophylaxis (PrEP) and in long-acting injectable formulations, but these remain experimental and are not approved by the MHRA.

Disclaimer: Off-label use of any medication must be prescribed and monitored by a qualified HIV specialist, with a clear assessment of benefits and risks.

Who Should (and Should Not) Use Dolutegravir?

Ideal Candidates

  • Adults and adolescents (≥12 years) with confirmed HIV-1 infection who require a potent, once-daily integrase inhibitor.
  • Patients with normal or mildly impaired liver function (Child-Pugh A-B) and a creatinine clearance ≥ 30 mL/min.

Absolute Contra-indications

  • Known hypersensitivity to dolutegravir sodium or any of the tablet’s excipients.
  • Co-administration with dofetilide, quinidine, or amiodarone because dolutegravir can increase plasma concentrations of these antiarrhythmic agents, raising the risk of life-threatening QT prolongation.

Relative Contra-indications & Special Populations

  • Renal impairment: No dose adjustment for eGFR ≥ 30 mL/min; for severe renal impairment (eGFR < 30 mL/min) use should be overseen by a specialist.
  • Hepatic impairment: No adjustment for mild or moderate disease; severe hepatic dysfunction requires careful monitoring.
  • Pregnancy: Dolutegravir is approved for use in pregnancy when the therapeutic benefit outweighs potential risks. Observational data have suggested a small increase in neural-tube defects when exposure occurs in the first trimester; clinicians should discuss these findings with the patient.
  • Breast-feeding: Small amounts are excreted in breast milk; continuation is generally considered acceptable if the mother is receiving effective antiretroviral therapy.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Nausea (often mild and transient)
  • Headache
  • Fatigue or insomnia
  • Diarrhoea (usually mild)

These events typically improve within the first few weeks of therapy and rarely require discontinuation.

Serious Adverse Events

  • Neuropsychiatric effects: Rare cases of insomnia, anxiety, or depressive symptoms have been reported.
  • Weight gain: Modest increase in body weight has been observed, especially when dolutegravir is combined with tenofovir alafenamide.
  • Hepatotoxicity: Elevations in liver enzymes may occur; monitor patients with pre-existing liver disease.
  • Immune reconstitution inflammatory syndrome (IRIS): May emerge shortly after initiating therapy in patients with very low CD4 counts.

If any of the following occur, seek immediate medical attention: severe rash, signs of liver injury (jaundice, dark urine), or symptoms suggestive of an allergic reaction (swelling of face or throat).

Drug Interactions

  • Strong UGT1A1 inducers (e.g., rifampicin, carbamazepine) markedly reduce dolutegravir concentrations. The recommended adjustment is 50 mg twice daily while the inducer is co-administered.
  • Antacids or supplements containing aluminium, magnesium, calcium, iron, or zinc decrease absorption. Separate dosing by at least 2 hours (dolutegravir first, then the antacid).
  • Other integrase inhibitors (e.g., raltegravir) should not be combined because of overlapping mechanisms.

Food and Lifestyle Interactions

  • Dolutegravir can be taken with or without food; a high-fat meal may increase exposure by ~30 %, which is not clinically significant.
  • Moderate alcohol consumption does not affect dolutegravir levels, but excessive alcohol may worsen liver health and adherence.

How to Take Dolutegravir

  • Standard dose: One 50 mg tablet taken once daily, with or without food.
  • If co-administered with a strong UGT1A1 inducer (e.g., rifampicin): Two 50 mg tablets (total 100 mg) taken once daily (or 50 mg twice daily, as advised).
  • Renal or hepatic impairment: No routine dose change for eGFR ≥ 30 mL/min or mild-to-moderate liver disease; severe impairment should be assessed individually.
  • Missed dose: Take the missed tablet as soon as remembered unless it is near the time of the next scheduled dose. Do not double-dose.
  • Overdose: Symptoms may include nausea, vomiting, dizziness, or tremor. Seek urgent medical care; activated charcoal may be considered if presentation is early. No specific antidote exists.
  • Discontinuation: Dolutegravir does not require tapering. If therapy is stopped, it should be done under clinician guidance to avoid viral rebound.

Monitoring and Follow-Up

  • Baseline labs: HIV viral load, CD4 count, liver function tests (ALT, AST, bilirubin), renal function (creatinine, eGFR).
  • Follow-up schedule:
  • Viral load at 4-8 weeks after initiation, then every 3-6 months if suppressed.
  • Liver enzymes at baseline and periodically (especially if co-administered with hepatotoxic agents).
  • Renal function at baseline and annually, or more often if comorbid kidney disease exists.

Patients should be instructed to report new neurological symptoms, severe rash, or signs of liver injury promptly.

Storage and Handling

  • Store tablets at room temperature (15-25 °C), protected from moisture and direct sunlight.
  • Keep out of reach of children; use child-proof containers.
  • Do not use tablets after the expiry date printed on the packaging.
  • If a tablet becomes damaged or discoloured, discard it and obtain a replacement.

Medication-Specific Glossary

Integrase Strand Transfer Inhibitor (INSTI)
A class of antiretrovirals that block the HIV integrase enzyme, preventing viral DNA from inserting into host DNA.
Viral Load
The quantity of HIV RNA copies per millilitre of blood; a key marker of treatment efficacy.
UGT1A1 (Uridine-5′-diphospho-glucuronosyltransferase 1A1)
An enzyme that glucuronidates dolutegravir for elimination; its activity influences drug levels.
QT Prolongation
Extension of the heart’s electrical repolarisation interval, which can predispose to arrhythmias.
Immune Reconstitution Inflammatory Syndrome (IRIS)
An exaggerated inflammatory response that may occur after rapid immune recovery following antiretroviral initiation.

Medical Disclaimer

This article provides educational information about Dolutegravir and is not a substitute for professional medical advice. Treatment decisions, including the use of any medication for unapproved indications, must be made under the guidance of a qualified healthcare provider. The content is intended for informational purposes only and does not constitute medical recommendations. Always consult a physician before starting, stopping, or changing any medication regimen.

Information for Dolutegravir is sourced from established medical standards and updated frequently. It is provided for general guidance and should be confirmed with a healthcare professional before use.
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