Lopinavir: Indication, Dosage, Side Effect, Precaution

This information is not country-specific. Please refer to the Malaysia prescribing information.

Generic Medicine Info

Indications and Dosage

Oral
HIV postexposure prophylaxis

Adult: 400 mg (with ritonavir 100 mg) bid, to be used with at least 2 other antiretrovirals. Treatment should be initiated as soon as possible (preferably within 72 hr) and continued for 28 days.

Oral
HIV infection

Adult: Lopinavir 400 mg (with ritonavir 100 mg) bid. In treatment naive patients: 800 mg (with ritonavir 200mg) once daily may be used. When taken with amprenavir, efavirenz, nevirapine or nelfinavir in treatment experienced patients, dose increases to 600 mg (with ritonavir 150 mg) bid (tablets) or 533 mg (with ritonavir 133 mg) bid (capsules and oral solution) may be required.
Child: >2 yr: Lopinavir 230 mg (with ritonavir 57.5 mg) /m² bid. When taken with amprenavir, efavirenz, nevirapine or nelfinavir, dose may be increased to 300 mg (with ritonavir 75 mg) /m² bid if required. Max dose 400 mg bid.

Administration

Should be taken with food.

Contraindications

Hypersensitivity; renal or hepatic failure; lactation; Concomitant use of drugs highly dependant on CYP3A for clearance and associated with serious toxicity.

Special Precautions

DM, haemophilia A and B, hepatitis; renal impairment; hyperlipidaemia or hypercholesterolaemia, monitor for signs of lipodystrophy. Always use with other antiretroviral agents in HIV treatment. Capsules and oral solution not interchangeable on a mg-per-mg basis. Pregnancy (oral solution CI). Monitor for propylene glycol-associated adverse effect when oral solution is administered.

Adverse Reactions

Diarrhoea, abdominal pain, asthenia, headache, dyspepsia, vomiting, myalgia, bronchitis, hypertension, palpitation, thrombophlebitis, vasculitis, agitation, anxiety, ataxia, hypertonia, confusion, depression, dyskinesia, peripheral neuritis; Cushing's syndrome; hypothyroidism, sexual dysfunction, lactic acidosis, arthralgia, abnormal vision, otitis media, tinnitus, acne, alopoecia, dry skin, skin discoloration, nail disorders, sweating.
Potentially Fatal: Pancreatitis.

Overdosage

Treat symptomatically with general supportive measures. Activated charcoal may aid in removal of unabsorbed drug.

Drug Interactions

Most interactions reported with lopinavir are due to its combination with the potent inhibitor of CYP3A4 ritonavir. Lopinavir levels may be decreased by CYP3A4 inducers such as efavirenz, nevirapine, amprenavir, nelfinavir, rifampicin, phenytoin. Lopinavir level are increased by CYP3A4 inhibitors such as valproate and rifabutin.
Potentially Fatal: Severe myelosuppression reported with paclitaxel.

Action

Description:
Mechanism of Action: Lopinavir is an antiretroviral agent which inhibits HIV protease, causing the enzyme incapable of processing the polyprotein precursor. This leads to the production of non-infectious and immature HIV particles. Lopinavir is used in combination with ritonavir, which increases the bioavailability to therapeutic levels.
Pharmacokinetics:
Absorption: Absorbed from the GI tract. Tablet formulation unaffected by food but liquid capsules and oral liquid have improved bioavailability when taken with food.
Distribution: Approx 98-99% plasma bound.
Metabolism: Metabolised hepatically by isoenzyme CYP3A.
Excretion: Eliminated via urine (10%) and faeces (83%).

Chemical Structure

Storage

Tablets: Store at 20-25°C in original container. Oral liquid and capsules: store at 2-8°C until dispensed then at ≤25°C for up to 2 mth.

MIMS Class

Antivirals

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