Emletra (Lopinavir & Ritonavir)
Emletra tablets belongs to the type of anti-retroviral agent which includes Lopinavir & ritonavir as an active substances. The two component included in Emletra tablets are classified pharmacologically as protease inhibitors.
Emletra is notify as fixed dose combinational treatment which is also used with other HIV drugs. Emletra tablets are not a curable disease, Emletra is a prescription drugs that is used in adults and pediatric with 14 days of age or older by only under the guidance of physician.
Emletra is mainly indicated for treating in patients suffering from HIV-1 infection by combining with other anti-retroviral drugs.
MECHANISM OF ACTION
Emletra consist of protease inhibitor activity component, display an anti-retroviral activity. The two composition Lopinavir & Ritonavir are undergoes action by prohibiting the protease enzymes which is effective for separation of gag-pol polyproteins which is specific for viral group production. This process is inhibited by interfering with protease enzyme activity and finally concludes as end of production of virus. The production of immature non-infectious virus occurs.
After oral administration the peak plasma concentration of Lopinavir occurs at 4 hours approximately. While taking Emletra with or without food no alteration of pharmacokinetic effect occurs.
Lopinavir & Ritonavir are heavily bound to human plasma protein with the range of 98 to 99%.
Hepatically Lopinavir is metabolized, by using CYP3A isoenzymes. Ritonavir is available as an unchanged form, in circulation. 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.
The Lopinavir half life period of is 12 hours after dosing with range of 5 to 6 hours The Ritonavir half life period is 3 to 5 hours. The unchanged form of Lopinavir is encountered with the range of via urine 2.2% & feces 19.8%. Ritonavir metabolite should be eliminated through feces & urine.
DOSAGE REGIMENS AND ADMINISTRATION OF LOPIMUNE
In adults, the prescribed dose of Emletra is 400mg/100mg that is 2 tablets of Emletra It should be administered orally as two times a day.
PATIENT WITH LESSER THREE LOPINAVIR RESISTANCE RELATED SUBSTITUTIONS
The prescribed dose of Emletra tablets is 800mg/200mg given by 4 Emletra tablets should be administered orally as single dose. This 800mg/200mg dose should not be recommended for the patients with 3 or greater Lopinavir resistance related substitutions. Emletra should not be used as single dose for combined with carbamazepine, Phenobarbital or phenytoin Emletra should not be used as single dose therapy by combining with efavirenz, nevirapine, or Nelfinavir. During the combination of these drugs, the Emletra dose should be 500mg/125mg( 2 tablets of 200mg/50mg Emletra & one tablet of 100mg/25mg Lopimune) as twice a day In pediatrics: Emletra tablets as mono therapy should not be recommended in pediatric patients with the age of <18 years. Based up on the body weight or body surface area of pediatric patients, To avoid the problems like under dosing or over dosing.the dose should be calculated 6 months to 18 years:
WITHOUT COMBINING WITH EFAVIRENZ, NEVIRAPINE OR NELFINAVIR
The prescribed dose of Emletra is 2 tablets of 100mg/25mg Emletra tablets should be administered as two times a day for body weight of 15 to 25kg or ≥ 0.6 to <0.9 m2 The prescribed dose of Emletra is 3 tablets of 100mg/25mg Emletra tablets should be used as two times a day for >25 to 35kg or ≥0.9 to <14 m2 The prescribed dose is 4 tablets of 100mg/25mg of Emletra tablets or 2 tablets of 200mg/50mg Emletra tablets should be suggested as two times a day for body weight of >35kg or ≥ 1.4 m2
CONCOMITANT USE WITH EFAVIRENZ, NEVIRAPINE OR NELFINAVIR
2 tablets of 100mg/25mg Emletra should be administered as two times a day is given for patients weighing 15 to 20kg or ≥0.6 to <0.8m2 The prescribed dose is 3 tablets 100mg/25mg of Emletra should be administered as two times a day is given for patients weighing >20 to 30kg or ≥0.8 to <1.2 m2. The prescribed dose is 4 tablets 100mg/25mg of Emletra should be administered as two times a day is given for patients weighing >30 to 45kg or ≥1.2 to <1.7 m2 The prescribed dose is 5 tablets 100mg/25mg of Emletra should be administered as two times a day is given for patients weighing >45kg or ≥1.7 m2. Emletra tablets should be administered with food or without food. Emletra tablets should not be chewed, crushed or broke
EMLETRA CAUSED SIDE EFFECTS
The major adverse effects; PR interval extension, QT interval extension Drug interactions Pancreatitis Liver toxicity The most common side effects; Diarrhea Nausea Vomiting Abdominal pain Dyspepsia Flatulence Asthenia Bronchitis Loss of weight Anorexia Myalgia Headache Insomnia Depression Loss of libido Rash Vasodilatation Increased glucose levels Increased uric acid level Increased AST, ALT Elevation of cholesterol Elevation of amylase, lipase Depletion of creatinine clearance Neutropenia In pediatrics; Increased sodium levels Increased total bilirubin Increased AST, ALT increased amylase Decreased platelets count Decreased neutrophils Post marketing: Fat redistribution Brady arrhythmias Toxic epidermal necrolysis, Stevens Johnson’s syndrome
Diabetes mellitus: Patients blood glucose level should be maintained by checking the levels frequently. QT prolongation: Stop the therapy. Immune reconstitution syndrome: Discontinue the Emletra treatment Fat redistribution: Reaccumulation of fat occur which may results as obesity. In severe condition, discontinue the therapy. 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 Emletra in neonates. Take alcohol & propylene glycol from all the drugs should be given to infants for reducing thwe toxicity associated to the components.
Elevation of triglyceride levels may leads to cause pancreatitis. Pancreatitis is the major risk factor during the Emletra treatment. Lipase and amylase value should be monitored periodically.
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.
Interaction of Emletra is an inhibitor of CYP3A, may uplift the plasma concentration of agents that ate formerly metabolized by CYP3A. While Emletra is a CYP3A substrate, when Emletra is co administered with CYP3A inducers causes depletion of Lopinavir plasma concentration and leads to loss of effectiveness. Emletra interaction with NNRTI like efavirenz or nevirapine causes decreasing the effect of concentration of Lopinavir.
Interaction Emletra with delaveridine causes elevation of effect of concentration of Lopinavir. Emletra interaction with tenofovir, causes increasing effect of concentration of tenofovir. Interaction of Emletra with calcium channel blocker leads to cause elevating the effect of concentration of these drugs.
Emletra Interaction with dexamethasone decreases the concentration of Lopinavir. Combination of Emletra 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 Emletra 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 Emletra is contraindicated. Emletra is contraindicated by using with strong CYP3A inducers, causes decreasing Lopinavir plasma concentration.
PREGNANCY & LACTATION
Pregnancy category: C Emletra should not be used in both pregnancy and lactating period.
Emletra drug should be stored at 20°C to 25°C. Protect the drug from heat, moisture & light.
In case of missed dose, patient should be following the instructions provided by medical adviser. Missed dose of Emletra should be avoided. Regular dosing schedule should be maintained.