Lopinavir

Oral
HIV postexposure prophylaxis

Oral
HIV infection

Should be taken with food.

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

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.

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.

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

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.

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%).

Source: National Center for Biotechnology Information. PubChem Database. Lopinavir, CID=92727, https://pubchem.ncbi.nlm.nih.gov/compound/Lopinavir (accessed on Jan. 22, 2020)

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.

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