Emletra tablet which exhibits anti-retroviral property. Emletra tablet is a which contain combination of Lopinavir 200mg and Ritonavir 50mg Both peak active ingredients consist of anti-viral activity against human immunodeficiency virus (HIV) which is required for causing AIDS Emletra is preventing the progression of HIV virus from multiplication. Emletra tablet is used to reduce problem related to AIDS, it is not cure or prevent the disease. Emletra combination helps to postpone the symptoms caused by HIV/AIDS.
Lopinavir and Ritonavir
200mg & 50mg
Emletra is primarily indicated for;
HIV infection associated AIDS
Normally, Emletra is used as combination with other anti-retroviral medicines.
Emletra is used to suppress the progression of HIV virus in immune cells and increase T cell counts. The number of Lopinavir blockade associated substitutions affects the virologic action of Emletra
Mechanism of action
Emletra is an anti-viral medicine that has two prime compounds which are inhibitors of HIV protease and effective against retrovirus.
Retrovirus has capable of converting RNA into DNA with the help of reverse transcriptase enzyme.
Then the viral DNA incorporated into DNA of affected immune cells and then multiplied Anti-viral activity of Emletra is exhibited by Lopinavir; it is a virulent protease inhibitor which inhibits the separation of Gag-Pol polyprotein.
Gag-Pol polyprotein is most important protein in the augmentation of active virus. This viral protease enzyme breaks the Gag-Pol polyprotein at the last stage of multiplication, an active and grown virus released into infected immune cells. A Emletra tablet prohibits the proteases enzyme that leads to formation of premature, non-infectious viral particles.
After oral administration, ritonavir present in Emletra tablet inhibits the metabolism of Lopinavir; therefore, the plasma level of Lopinavir is elevated. The peak plasma concentration of the Lopinavir occurs only at 4 hours after administration The effect of food, there is no significant difference between fasted and fed condition. Emletra should be taken with or without food.
The drug Lopinavir is highly bound to the human plasma protein around 98-99%.
Lopinavir is undergoes oxidative metabolism, it is metabolized by CYP3A isoenzymes. Ritonavir is a potent CYP3A inhibitor, prohibits metabolism of Lopinavir and increased the plasma level of Lopinavir.
Emletra is highly excreted through urine and feces. Lopinavir is a potent protease inhibitor which is responsible for anti-viral activity. The terminal half-life period is approximately 2.33 hours in case of twice daily, 2.44 hours at once daily.
Emletra Dosage and administration
Emletra tablet should be taken with or without food. Emletra is available in fixed dose combination (Lopinavir 200mg + ritonavir 50mg)
Emletra 400mg/100mg should be given as 200mg/50mg as two tablets two times a day
Emletra 800mg/200mg should be taken as 200mg/50mg as four tablets once a day.
Emletra should not administered as a single dose, in case of combination with carbamazepine, Phenobarbital, or phenytoin.
Emletra should be combined with some other anti-viral medicines; Efavirenz Nevirapine Nelfinavir By combining with the above mentioned anti-viral medicines, the prescribed dose of Emletra is 500mg/125mg, it is taken as 200mg/50mg as two tablets & 100mg/25mg as one tablet at two times a day in concomitant with efavirenz, nevirapine, Nelfinavir
The dose of Emletra in children is recommended on the basis of; Body weight or Body surface area (BSA) Emletra is not given as single dose for pediatric patients who are under the age of <18 years
Emletra not combined with efavirenz, nevirapine, Nelfinavir
15kg to 25kg: The BSA should be ≥0.6 to <0.9, the prescribed dose of Emletra 100mg/25mg as two tablets two times a day
>25kg to 35kg: BSA- ≥0.9 to <1.4, the recommended dose of Emletra 100mg/25mg as three tablets two times a day
>35kg: BSA ≥1.4, the dose should be taken as Emletra 100mg/25mg tablets as four tablets or two Emletra 200mg/50mg tablets.
Emletra combined with efavirenz, nevirapine, Nelfinavir
15kg to 20kg: The BSA should be ≥0.6 to <0.8, the prescribed dose of Emletra 100mg/25mg as two tablets two times a day
>20kg to 30kg: BSA- ≥0.8 to <1.2, the recommended dose of Emletra 100mg/25mg as three tablets two times a day
>30kg to 45kg: BSA ≥1.2 to <1.7, the dose should be taken as Emletra 100mg/25mg tablets as four tablets or two Emletra 200mg/50mg tablets.
>45kg: BSA ≥1.7, Emletra 100mg/25mg taken as 5 tablets at twice daily
Blood and lymphatic system
Anemia, leucopenia, neutropenia, lymphadenopathy
Atherosclerosis such as myocardial infarction, atrioventricular block
Ear and labyrinth problems
Diarrhea, nausea, vomiting, abdominal pain, gastroenteritis, colitis, dyspepsia, pancreatitis, ulcers, dry mouth
AST, ALT and GGT elevation, hepatomegaly, cholangitis, hepatic steatosis
Hypersensitivity reaction like; urticaria and angioedema
Infections and infestation
Upper and lower respiratory tract infection, cellulitis, folliculitis and furuncle
Hypercholesterolemia, hyper triglycerides, weight decreased, loss of appetite
Arthralgia, back pain, Myalgia, rhabdomyolysis
Headache, insomnia, neuropathy, ageusia, convulsions
Renal failure, Hematuria, nephritis
Erectile dysfunction, amenorrhea, menorrhagia
Rashes, seborrheic dermatitis, night sweats, Pruritus, alopecia, capillaritis, vasculitis
Emletra precautions and warning
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 the 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.
Caution should be taken
Pregnancy women, Breastfeeding, Hepatic impairment, Geriatric patients