Darunavir/Cobicistat｜HIV-1 infection｜HongKong DengYue

Darunavir/Cobicistat Application Scope

Is a fixed-dose combination antiretroviral medication used in the treatment of HIV-1 infection in adults and pediatric patients (typically aged ≥12 years and weighing ≥40 kg).

• Darunavir: A protease inhibitor (PI) that blocks HIV viral replication.
• Cobicistat: A pharmacokinetic enhancer (CYP3A4 inhibitor) that boosts darunavir levels.

Characteristics

Ingredients:

• Active: Darunavir ethanolate (equivalent to darunavir 800 mg) + cobicistat 150 mg per tablet.
• Inactive: May include microcrystalline cellulose, silicon dioxide, etc.

Properties:

• Appearance: Film-coated tablet (e.g., yellow, oval).
• Solubility: Poorly soluble in water.

Specification:

• Available as 800 mg darunavir/150 mg cobicistat per tablet.

Packaging Specification:

• Bottles of 30 tablets or blister packs.

Storage:

• Store below 30°C (86°F), protect from moisture.

Expiry Date:

• Typically 24 months from manufacture (check packaging).

Executive Standard:

• Complies with USP (United States Pharmacopeia) or EMA (European Medicines Agency) standards.

Approval Number:

• FDA: e.g., NDA 205395 (Prezista/cobicistat).
• EMA: EU/1/06/347/001 (check local regulations).

Date of Revision:

• Varies by manufacturer (e.g., latest label updates in 2023).

Manufacturer:

• Janssen Pharmaceuticals (Johnson & Johnson).

Guidelines for the Use 

Dosage and Administration:

• Adults: 1 tablet (800/150 mg) once daily with food.
• Pediatrics: Weight-based dosing (≥40 kg).
• Must be combined with other antiretrovirals .

Adverse Reactions:

• Common: Diarrhea, nausea, rash, headache.
• Serious: Severe skin reactions (e.g., Stevens-Johnson syndrome), hepatotoxicity, hyperglycemia.

Contraindications:

• Hypersensitivity to darunavir/cobicistat.
• Concurrent use with CYP3A substrates .

Precautions:

• Monitor liver function (risk of hepatitis B/C flare-up).
• May increase serum creatinine (cobicistat effect).
• Pregnancy: Use only if benefits outweigh risks (Category C).

Interactions

Drug Interactions:

• Contraindicated:
  • CYP3A inducers: Rifampin, carbamazepine.
  • Alpha-1-adrenergic antagonists: Alfuzosin (severe hypotension).
  • Herbal supplements: St. John’s wort.
• Require Dose Adjustment:
  • Statins: Avoid simvastatin/lovastatin; use atorvastatin with caution.
  • Anticoagulants: Monitor warfarin closely.
  • Anticonvulsants: Phenytoin, phenobarbital.

 

Note:

• If there is a new packaging for the drug, the new packaging shall prevail. The above information is sourced from DengYue Medicine.
• It is only for internal discussion among medical staff and does not serve as a basis for medication. For specific medication guidelines, please consult the attending physician.