Lupravir
Generic Name
Lopinavir/Ritonavir
Manufacturer
Square Pharmaceuticals Ltd.
Country
Bangladesh
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| lupravir 200 mg capsule | ৳ 50.00 | ৳ 250.00 |
Description
Overview of the medicine
Lupravir is a combination of Lopinavir and Ritonavir, used to treat Human Immunodeficiency Virus (HIV-1) infection in adults and children. Lopinavir is an HIV protease inhibitor, and Ritonavir is a potent inhibitor of cytochrome P450 3A (CYP3A) which boosts Lopinavir concentrations.
Uses & Indications
Dosage
Adults
400 mg Lopinavir/100 mg Ritonavir twice daily (two 200 mg/50 mg tablets) or 800 mg Lopinavir/200 mg Ritonavir once daily (four 200 mg/50 mg tablets) in selected patients.
Elderly
No specific dose adjustment required, but caution is advised due to potential age-related decrease in renal, hepatic, or cardiac function.
Renal_impairment
No dose adjustment is needed for patients with renal impairment.
Hepatic_impairment
Use with caution in patients with mild to moderate hepatic impairment. Contraindicated in severe hepatic impairment.
How to Take
Tablets can be taken with or without food. Oral solution should be taken with food. It is crucial to take the medicine exactly as prescribed by the doctor, without missing doses.
Mechanism of Action
Lopinavir is an HIV protease inhibitor that binds to the active site of the HIV protease enzyme, preventing the cleavage of Gag-Pol polyproteins, which are essential for the formation of mature infectious virus particles. Ritonavir inhibits the CYP3A enzyme, reducing the metabolism of lopinavir and thereby increasing its plasma concentrations and half-life, allowing for less frequent dosing.
Pharmacokinetics
Onset
Steady-state plasma concentrations are generally achieved within 2-3 days of dosing.
Excretion
Primarily eliminated via the feces (approximately 82% of an oral dose), with a small amount excreted in urine (approximately 10%).
Half life
Lopinavir's effective half-life is approximately 5 to 6 hours when co-administered with ritonavir.
Absorption
Lopinavir is well absorbed orally, and its absorption is enhanced when taken with food. Ritonavir significantly increases lopinavir plasma concentrations.
Metabolism
Primarily metabolized in the liver by the cytochrome P450 3A (CYP3A) enzyme system. Ritonavir is a potent inhibitor of CYP3A.
Side Effects
Contraindications
- Hypersensitivity to lopinavir, ritonavir, or any component of the formulation.
- Severe hepatic impairment.
- Concomitant use with drugs highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events (e.g., simvastatin, midazolam, pimozide, ergot derivatives).
Drug Interactions
Rifampin
Significantly decreases lopinavir/ritonavir plasma concentrations, potentially leading to loss of therapeutic effect and development of resistance. Concomitant use generally not recommended.
Warfarin
Altered anticoagulant effect; monitor INR closely.
Midazolam (oral)
Significantly increased plasma concentrations of midazolam due to CYP3A inhibition. Concomitant use is contraindicated. Use caution with parenteral midazolam.
Oral Contraceptives
Decreased efficacy of oral contraceptives; advise alternative or additional contraceptive methods.
Statins (e.g., Simvastatin, Lovastatin)
Increased risk of myopathy, including rhabdomyolysis, due to CYP3A inhibition by ritonavir. Concomitant use is contraindicated.
Storage
Store in a cool and dry place, below 30°C. Protect from light and moisture. Keep out of reach of children.
Overdose
Experience with acute overdose is limited. There is no specific antidote for Lupravir. Management should consist of general supportive measures, including monitoring vital signs and clinical status. Removal of unabsorbed drug may be considered.
Pregnancy & Lactation
Pregnancy Category B. Studies in animals have shown no evidence of teratogenicity. Limited data from pregnant women indicate no increased risk of major birth defects. Use during pregnancy should only be considered if the potential benefit justifies the potential risk to the fetus. It is recommended that HIV-infected mothers do not breastfeed to avoid transmitting HIV to the infant.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
24 months
Availability
Available in hospitals and pharmacies nationwide
Approval Status
FDA approved, DGDA approved in Bangladesh
Patent Status
Generic versions available, original patent expired
WHO Essential Medicine
YesClinical Trials
Lopinavir/Ritonavir has been extensively studied in numerous clinical trials for its efficacy and safety in treating HIV-1 infection across various patient populations, including adults, adolescents, and children.
Lab Monitoring
- Liver function tests (ALT, AST, bilirubin) at baseline and periodically during treatment.
- Lipid profile (total cholesterol, LDL, HDL, triglycerides) at baseline and periodically.
- Glucose levels, especially in patients with risk factors for diabetes.
- HIV viral load and CD4+ T-cell counts to assess treatment efficacy.
Doctor Notes
- Emphasize strict adherence to the dosing regimen to prevent viral resistance.
- Carefully review concomitant medications for potential drug interactions, especially those metabolized by CYP3A.
- Monitor for signs of hepatotoxicity, pancreatitis, and metabolic abnormalities (lipids, glucose) regularly.
Patient Guidelines
- Take Lupravir exactly as prescribed; do not miss doses or stop treatment without consulting your doctor.
- Lupravir is not a cure for HIV infection and does not prevent the transmission of HIV to others.
- Inform your doctor about all other medications, supplements, and herbal products you are taking.
- Report any severe side effects, such as persistent diarrhea, severe abdominal pain, or yellowing of the skin/eyes, immediately.
Missed Dose Advice
If a dose is missed, take it as soon as you remember. If it is almost time for the next dose, skip the missed dose and continue with your regular dosing schedule. Do not take a double dose to make up for a missed one.
Driving Precautions
Some patients may experience dizziness, lightheadedness, or other central nervous system effects. Patients should be advised to exercise caution when driving or operating machinery until they know how Lupravir affects them.
Lifestyle Advice
- Maintain a healthy diet and exercise regularly to manage potential metabolic side effects like dyslipidemia and glucose abnormalities.
- Avoid excessive alcohol consumption, which can exacerbate liver issues.
- Practice safe sex to prevent the transmission of HIV to others.
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