Lopinavir


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO HIV infection 400 mg (w/ ritonavir 100 mg) twice daily. In treatment-naive patients: 800mg (w/ ritonavir 200 mg) once daily. W/ amprenavir, efavirenz, nevirapine or nelfinavir in treatment experienced patients: 600 mg (w/ ritonavir 150 mg) twice daily (in tab) or 533 mg (w/ ritonavir 133 mg) twice daily (in cap and oral soln) may be required. HIV postexposure prophylaxis 400 mg (w/ ritonavir 100 mg) twice daily w/ at least 2 other antiretrovirals. Initiate treatment as soon as possible (preferably w/in 72 hr) and continue for 28 days.
Dosage Details
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: 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

Chemical Structure Image
Lopinavir

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

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
Disclaimer: This information is independently developed by MIMS based on Lopinavir from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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