Trade name : Lopimune
Active ingredient : Lopinavir & ritonavir
Strength availability : 200mg & 50mg
Manufactured by : Cipla
Package : 60 tablets in a container
Lopimune is a fixed dose combinational treatment which is also used with other HIV drugs. Lopimune tablets involves in anti-retroviral agent which includes Lopinavir & ritonavir as an active substances. Both are classified pharmacologically as protease inhibitors. Lopimune tablets are not a curable disease, Lopimune is a prescription drugs only under the guidance of physician.
Lopimune is primarily used to treat in patients suffering from HIV-1 infection by combining with other anti-retroviral drugs.
MECHANISM OF ACTION :
Lopinavir belongs to an inhibitor of the HIV-1 protease, inhibits cleavage of the Gag-Pol polyprotein, resulting in the formation of immature, non-infectious viral particles. Ritonavir prohibits the CYP3A-mediated metabolism of lopinavir, hence providing increased plasma levels of lopinavir.
In adults, the usual dose of Lopimune is 400mg/100mg that is 2 tablets of Lopimune
It should be administered orally as two times a day.
The dose prescribed as 800/200mg (given as 4 tablets of 200/50mg) once daily in patients with < 3 lopinavir resistance associated substitions
Lopimune is not recommended once daily in combination with anticonvulsant drugs,
Combination of Lopimune with Efavirenz, nevirapine or nelfinavir once daily is not recommended
Thereby dose increased for all patients is 500/125mg of Lopimune tablets in combination with Efavirenz, nevirapine or nelfinavir is given twice daily as two tablet of 200/50mg and one tablet of 100/25mg.
Lopimune should not administrated once daily in patients < 18 years of age the tablet
Based on BSA or Weight the Lopimune dose is calculated.
6 months to 18 years :
The patients administrated dose of 15 -25 kg or BSA < 0.9 m2 – lopinavir 200mg & Ritonavir 50mg twice a day orally >25 – 35 kg or BSA 0.9 to < 1.4 m2 – lopinavir 300mg & Ritonavir 75 mg twice daily orally. The patients administrated dose of greater than 35kg or BSA at least 1.4m2 – lopinavir 400mg & Ritonavir 100mg twice daily orally.
Concomitant Efavirenz, nelfinavir or nevirapine :
The dose administrated 15 -20kg or BSA 0.6 to < 0.8m2 – Lopinavir 200mg & Ritonavir 50mg orally. >20 – 30kg or BSA 0.8 <1.2m2 – lopinavir 300mg – Ritonavir 75mg orally twice a day. > 30 – 45 kg or BSA 1.2 to <1.7m2 – lopinavir 400mg – Ritonavir 100mg orally twice a day > 45kg or BSA at least 1.7m2: - Lopinavir 500mg & Ritonavir 125mg twice a day orally. Lopimune tablets should be administered with food or without food. Lopimune tablets should not be chewed, crushed or broke
Absorption: The time to peak plasma concentration of Lopinavir occurs at 4 hours approximately.
While taking Lopimune with or without food no alteration of pharmacokinetic effect occurs.
Distribution: Lopinavir & Ritonavir are heavily bound to human plasma protein with the range of 98 to 99%.
Lopinavir Mainly metabolized in hepatically, by using CYP3A isoenzymes. Ritonavir in circulation is produce as an unchanged form,. The primary metabolite of Ritonavir is Isopropylthiazole oxidation metabolite which is present as low level attaining anti-retroviral activity. CYP3A & CYP2D6 isoenzymes are main cytochrome enzyme required for metabolism of ritonavir.
Excretion: The Ritonavir half life period is 3 to 5 hours and Ritonavir metabolite should be eliminated through feces & urine. The Lopinavir half life period of is 12 hours after dosing with range of 5 to 6 hours The unchanged form of Lopinavir is encountered with the range of via urine 2.2% & feces 19.8%.
WARNING & PRECAUTION
QT prolongation: Stop the therapy.
Immune reconstitution syndrome: Discontinue the Lopimune treatment
Fat redistribution: Reaccumulation of fat occur which may results as obesity. In severe condition, discontinue the therapy. Diabetes mellitus: Patients blood glucose level should be maintained by checking the levels frequently. Take alcohol & propylene glycol from all the drugs should be given to infants for reducing thwe toxicity associated to the components.
Pancreatitis: Elevation of triglyceride levels may leads to cause pancreatitis. Pancreatitis is the major risk factor during the Lopimune treatment. Lipase and amylase value should be monitored periodically.
Liver toxicity: Due to elevation of AST, ALT & bilirubin, leads to cause liver injury this may concluds as liver damage or failure. Monitor liver function test periodically during or after completion of treatment. Drug interaction-CYP3A enzyme prohibition, causes increased plasma concentration of concurrent used drugs. Avoid the concomitant use. Toxicity occurs to neonates, potential risk may occur while using Lopimune in neonates.
Interaction of Lopimune with calcium channel blocker leads to cause elevating the effect of concentration of these drugs. Interaction of Lopimune is an inhibitor of CYP3A, may uplift the plasma concentration of agents that ate formerly metabolized by CYP3A. While Lopimune is a CYP3A substrate, when Lopimune is co administered with CYP3A inducers causes depletion of Lopinavir plasma concentration and leads to loss of effectiveness. Lopimune interaction with NNRTI like efavirenz or nevirapine causes decreasing the effect of concentration of Lopinavir. Lopimune interaction with tenofovir, causes increasing effect of concentration of tenofovir. Combination of Lopimune tablets with lipid lowering drugs or Immuno suppressants leads to cause increasing concentration of these drugs Concomitant use with abacavir, leads to decreasing the effect of concentration of abacavir. Interaction of Lopimune with anti-gout or anti-mycobacterials causes increasing effect of concentration of these drugs.
Drugs that are largely vulnerable on CYP3A for clearance & for which increased plasma concentration are related with severe life threatening conditions during concurrent use of Lopimune is contraindicated. Lopimune is contraindicated by using with strong CYP3A inducers, causes decreasing Lopinavir plasma concentration.
If missed dose occurs, patient should be following the instructions provided by medical adviser. Missed dose of Lopimune should be avoided.Regular dosing schedule should be maintained.
Lopimune drug should be stored at 20℃ to 25℃. Protect the drug from heat, moisture & light.
Common side effects :
GI effects: abdominal pain, nausea, vomiting, diarrhea, anorexia Common side effects Hyperaesthesia, pharyngitis, rash, pruritus, sweating, vasodilatation, wt loss, Asthenia , taste disorder, headache, numbness or tingling around the mouth or extremities, anxiety, insomnia, fever, dizziness, malaise, Allergic reactions : urticaria, bronchospasm, angioedema, mild skin eruptions, immune reconstitution syndrome, lipodystrophy, osteonecrosis, Metabolic abnormalities: hypertriglyceridaemia, hypercholesterolaemia, insulin resistance, hyperglycaemia, hyperlactataemia. Reduced levels of Hb, K, free and total thyroxine; increased eosinophil, liver enzymes, amylase and uric acid; reduced or increased WBC and neutrophil counts.
MAJOR SIDE EFFECTS
Pancreatitis, hepatic dysfunction, Stevens-Johnson syndrome. Rarely, anaphyla Post marketing: Fat redistribution Brady arrhythmias Toxic epidermal necrolysis, Stevens Johnson’s syndrome Erythema multiforme