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Isentress

8.58
An antiretroviral medicine used as part of combination therapy to manage HIV-1 infection in adults and children.


Ingredient
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In Stock
Delivery
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

Alternative/Local Brand
Isentress
Active Ingredient(s)
Raltegravir
Primary Category
HIV Treatment
Therapeutic Class
Antivirals for Systemic Use, Antivirals for Treatment of HIV Infections, Integrase inhibitors
Pharmacological Class
HIV Integrase Strand Transfer Inhibitor
Indications
HIV-1 Infection
Contraindications
Hypersensitivity to raltegravir
Minor Side Effects
Nausea, Headache, Tiredness, Difficulty sleeping
Moderate Side Effects
Dizziness, Flatulence, Abdominal bloating
Serious Side Effects
Severe skin reactions (Stevens-Johnson syndrome), Muscle breakdown (rhabdomyolysis), Liver failure, Depression or suicidal thoughts
Dosage Forms
Film-coated tablet, Chewable tablet, Sachets
Administration Route
Oral
Mechanism of Action
Raltegravir works by blocking integrase, an enzyme that the HIV virus needs to insert its genetic material into human cells. By blocking this process, the medication prevents the virus from multiplying and reduces the amount of HIV in the blood.
Prescription Status
Rx
Manufacturer
MSD (Merck & Co.)
Patient Summary
An antiretroviral medicine used as part of combination therapy to manage HIV-1 infection in adults and children.
Onset Time
Begins working quickly to reduce viral load over weeks
Duration
12 to 24 hours depending on formulation
Storage Instructions
Store in the original bottle at room temperature.
Drug Interactions
Rifampicin, Antacids containing magnesium or aluminium, Phenytoin
Age Restrictions
Suitable for infants, children, and adults.
Pregnancy Use
Can be used during pregnancy if prescribed by a specialist.
Alternative Drugs
Dolutegravir, Bictegravir, Elvitegravir

Isentress: Raltegravir Overview for HIV Management

Isentress is the brand name for the antiretroviral medication raltegravir, a key component of HIV therapy. It is available as a 400 mg tablet and is prescribed in Hong Kong under the guidance of the Department of Health. This article explains how raltegravir works, its approved uses, safety considerations, and practical information for patients taking Isentress.

How Raltegravir Works in the Body

  • Class: Raltegravir belongs to the integrase strand transfer inhibitor (INSTI) class of antiretrovirals.
  • Mechanism: HIV integrates its genetic material into host DNA using the viral enzyme integrase. Raltegravir binds to the active site of integrase, preventing the strand-transfer step required for viral DNA to insert into the host genome.
  • Effect: By blocking integration, the drug halts the production of new viral particles, reducing the amount of circulating virus (viral load).
  • Onset and Duration: Viral suppression can be observed within days of the first dose; the drug’s half-life is about 9 hours, supporting twice-daily dosing.

Approved Medical Uses

  • Treatment-naïve adults living with HIV-1, in combination with other antiretroviral agents.
  • Treatment-experienced adults who have documented resistance to other drug classes, provided that a suitable background regimen is used.
  • Pregnant women may receive raltegravir when the benefits outweigh potential risks, as recommended by the Hong Kong Department of Health.

These indications follow the approval status granted by the Hong Kong regulatory authority, which aligns with international standards such as those of the U.S. FDA and the EU EMA.

Off-Label and Investigational Applications

Current peer-reviewed evidence does not support routine off-label use of raltegravir for conditions other than HIV infection. Clinical trials investigating its role in preventing mother-to-child transmission and in post-exposure prophylaxis have been conducted, but these uses remain under study and should only be considered within a clinical trial or specialist-guided protocol.

Who Should Use Isentress? Contraindications and Special Populations

Absolute contraindications

  • Known hypersensitivity to raltegravir or any tablet excipients.

Relative contraindications / cautions

  • Pregnancy: Use only if prescribed by a qualified provider after risk-benefit analysis.
  • Breastfeeding: Limited data; discuss with a healthcare professional.
  • Severe hepatic impairment: No dose adjustment required, but monitoring is advisable.

Special populations

  • Elderly patients: No specific dose change, but consider comorbidities and other medications.
  • Renal impairment: No dosage adjustment needed for creatinine clearance ≥ 30 mL/min; for severe renal dysfunction, clinical judgment is required.

Safety Profile: Side Effects and Interactions

Common Side Effects

  • Nausea, diarrhea, and abdominal pain (typically mild and transient).
  • Headache and fatigue.
  • Mild elevations in liver enzymes (monitor if pre-existing liver disease).

Serious Adverse Events

  • Hepatotoxicity: Rare but may present as jaundice, dark urine, or elevated bilirubin; seek immediate medical attention.
  • Severe hypersensitivity reactions: Rash, fever, or angioedema-discontinue promptly.
  • Immune reconstitution inflammatory syndrome (IRIS): May occur after initiating therapy in severely immunocompromised patients.

Drug Interactions

  • Major interactions

  • Rifampin (a strong inducer of CYP3A4 and UGT1A1) reduces raltegravir exposure; avoid co-administration or adjust dosing under specialist guidance.

  • Moderate interactions

  • Anticonvulsants such as carbamazepine or phenytoin may modestly lower raltegravir levels.

  • Methadone may have reduced efficacy; monitor withdrawal symptoms.

  • Mechanism of interaction

  • Raltegravir is metabolized primarily by UGT1A1 glucuronidation; drugs that induce or inhibit this pathway can alter its plasma concentration.

Food and Lifestyle Interactions

  • Food: Raltegravir can be taken with or without meals; however, consistent timing with respect to meals may improve adherence.
  • Alcohol: No direct contraindication, but excessive drinking can worsen liver function and adherence.
  • Driving: No sedation effect reported; patients should still assess individual response before operating machinery.

How to Take Isentress

  • Standard dosing: 400 mg tablet taken twice daily (every 12 hours).
  • Administration: Swallow whole with water. Do not crush, split, or chew unless a health professional advises otherwise.
  • Missed dose: If a dose is missed within 8 hours, take it as soon as remembered; if it is close to the next scheduled dose, skip the missed one-do not double up.
  • Overdose: Symptoms may include nausea, vomiting, and abdominal pain. Seek emergency care; supportive treatment is the mainstay, as no specific antidote exists.
  • Discontinuation: Abrupt cessation can lead to viral rebound. Stopping should be done under medical supervision, often with a transition to an alternative regimen.

Monitoring and Follow-Up

  • Baseline labs: HIV viral load, CD4⁺ count, liver function tests, and renal function.
  • Routine checks: Viral load every 3-4 weeks after initiation, then every 3-6 months once suppressed.
  • Liver monitoring: Repeat liver enzymes if clinically indicated or if symptoms of hepatitis develop.

Storage and Handling

  • Store tablets at room temperature (20-25 °C), protected from moisture and direct sunlight.
  • Keep the container tightly closed and out of reach of children.
  • Do not use tablets past the expiration date printed on the label.

Medication-Specific Glossary

Integrase inhibitor
A drug class that blocks the HIV integrase enzyme, preventing viral DNA from integrating into host cells.
Viral load
The quantity of HIV RNA fragments per millilitre of blood; a key marker of treatment effectiveness.
CD4⁺ count
A measurement of immune system health, indicating the number of CD4-positive T-lymphocytes per microlitre of blood.
Resistance
The ability of HIV to mutate and continue replicating despite the presence of antiretroviral drugs.

Medical Disclaimer

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

Isentress FAQ

Can I take Isentress with my other HIV medicines?

Yes. Raltegravir is meant to be part of a combination antiretroviral regimen. Your prescriber will choose companion drugs that complement its activity and minimize interaction risk.

Do I need to take Isentress on an empty stomach?

No. Raltegravir can be taken with or without food. Consistency-taking it at the same times each day-helps maintain steady drug levels.

What do the imprint codes on the tablet look like?

The 400 mg tablet typically bears the imprint “R200” on one side and “400” on the other, helping pharmacists verify authenticity.

Will Isentress show up on a workplace drug test?

Raltegravir is not screened for in standard occupational drug testing panels, as it is not a substance of abuse.

Can I travel internationally with Isentress?

Yes, but carry the medication in its original pharmacy label, a copy of your prescription, and a brief physician letter if you need to cross customs with a controlled-substance declaration.

Is there a generic version of Raltegravir available in Hong Kong?

As of the latest regulatory updates, only the brand-name product Isentress is listed in Hong Kong’s pharmacopeia. Generic formulations may become available after patent expiry.

What should I do if I experience a rash while on Isentress?

A mild rash can be common, but if it spreads, becomes painful, or is accompanied by fever, seek medical attention promptly, as it may signal a serious hypersensitivity reaction.

How does Raltegravir compare with other INSTIs like dolutegravir?

Both inhibit HIV integrase, but dolutegravir has a longer half-life allowing once-daily dosing. Choice of agent depends on resistance patterns, tolerability, and clinician judgment.

Can I store Isentress in a bathroom cabinet?

It is best to keep tablets in a dry place away from heat and humidity. A bathroom cabinet may expose them to moisture; a bedroom drawer at room temperature is preferable.

Is it safe to use herbal supplements with Isentress?

Some herbs (e.g., St. John’s wort) can induce drug-metabolizing enzymes and lower raltegravir levels. Discuss any supplement use with your healthcare provider before adding it to your regimen.

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