Efavirenz, Lamivudine And Tenofovir Disoproxil Fumarate 600/300/300
Efavirenz, Lamivudine And Tenofovir Disoproxil Fumarate 600/300/300 Uses, Dosage, Side Effects, Food Interaction and all others data.
Efavirenz, a synthetic antiretroviral agent, is a non- nucleoside reverse transcriptase inhibitor. While Efavirenz is pharmacologically related to other non nucleoside reverse transcriptase inhibitors, Efavirenz differs structurally from these drugs and also differs structurally from other currently available anti-retroviral agents.
Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with activity against HIV-1. It blocks the RNA- and DNA-dependent polymerase activities including HIV-1 replication.
Efavirenz (dideoxyinosine, ddI) is an oral non-nucleoside reverse transcriptase inhibitor (NNRTI). It is a synthetic purine derivative and, similar to zidovudine, zalcitabine, and stavudine. Efavirenz was originally approved specifically for the treatment of HIV infections in patients who failed therapy with zidovudine. Currently, the CDC recommends that Efavirenz be given as part of a three-drug regimen that includes another nucleoside reverse transcriptase inhibitor (e.g., lamivudine, stavudine, zidovudine) and a protease inhibitor or efavirenz when treating HIV infection.
Table Of contents
| Trade Name | Efavirenz, Lamivudine And Tenofovir Disoproxil Fumarate 600/300/300 |
| Generic | Efavirenz + Lamivudine And Tenofovir |
| Weight | 600mg, 300mg, 300mg |
| Type | Tablet |
| Therapeutic Class | |
| Manufacturer | Cipla Limited |
| Available Country | India, Nigeria |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Efavirenz in combination with other antiretroviral agents is used for the treatment of HIV-1 infection. This indication is based on analyses of plasma HIV- RNA levels and CD4 cell counts in controlled studies of up to 24 weeks in duration. At present, there are no results from controlled trials evaluating long term suppression of HIVRNA with Efavirenz.
Efavirenz, Lamivudine And Tenofovir Disoproxil Fumarate 600/300/300 is also used to associated treatment for these conditions: Human Immunodeficiency Virus Type 1 (HIV-1) Infection
How Efavirenz, Lamivudine And Tenofovir Disoproxil Fumarate 600/300/300 works
Similar to zidovudine, efavirenz inhibits the activity of viral RNA-directed DNA polymerase (i.e., reverse transcriptase). Antiviral activity of efavirenz is dependent on intracellular conversion to the active triphosphorylated form. The rate of efavirenz phosphorylation varies, depending on cell type. It is believed that inhibition of reverse transcriptase interferes with the generation of DNA copies of viral RNA, which, in turn, are necessary for synthesis of new virions. Intracellular enzymes subsequently eliminate the HIV particle that previously had been uncoated, and left unprotected, during entry into the host cell. Thus, reverse transcriptase inhibitors are virustatic and do not eliminate HIV from the body. Even though human DNA polymerase is less susceptible to the pharmacologic effects of triphosphorylated efavirenz, this action may nevertheless account for some of the drug's toxicity.
Dosage
Efavirenz, Lamivudine And Tenofovir Disoproxil Fumarate 600/300/300 dosage
It is recommended that Efavirenz be taken on an empty stomach, preferably at bedtime.
Adults: The recommended dosage of Efavirenz is 600 mg orally, once daily, in combination with a protease inhibitor and/or nucleoside analogue reverse transcriptase inhibitors (NRTIs).
Pediatric Patients: Following table describes the recommended dose of Efavirenz for pediatric patients 3 years of age or older and weighing between 10 and 40 kg. The recommended dosage of Efavirenz for pediatric patients weighing greater than 40 kg is 600 mg, once daily.
10 to <15 kg: 200 mg
15 to < 20 kg:250 mg
20 to < 25 kg: 300 mg
25 to < 32.5 kg:350 mg
32.5 to < 40 kg: 400 mg
40 kg: 600 mg
Side Effects
Rashes, psychiatric or CNS disturbances, amnesia, agitation, confusion, dizziness, vertigo, headache, euphoria, insomnia or somnolence, impaired concentration, abnormal thinking or dreaming, depersonalisation, convulsions, hallucinations, nausea, vomiting, diarrhoea, pancreatitis, fatigue, hepatic failure, photoallergic dermatitis; autoimmune disorders (e.g. Graves’ disease, polymyositis, Guillain-Barre syndrome), osteonecrosis. Accumulation or redistribution of body fat (lipodystrophy) including central obesity, peripheral and facial wasting, buffalo hump, breast enlargement, cushingoid appearance. Metabolic abnormalities e.g. hypercholesterolaemia, hyperglycaemia, hypertriglyceridaemia, hyperlactataemia, insulin resistance.
Precaution
Patient with history of seizures and psychiatric disorders; acute porphyria. Patients receiving voriconazole or rifampicin (weighing ≥50 kg). Discontinue if severe rash or fever develops. Moderate hepatic and severe renal impairment. Childn. Pregnancy.
Interaction
Additive CNS effects w/ psychoactive drugs. May alter plasma warfarin concentrations. May reduce plasma concentrations of HIV integrase inhibitors (e.g. dolutegravir), other HIV NNRTIs (e.g. etravirine), HMG-CoA reductase inhibitors (e.g. simvastatin). Plasma concentrations of efavirenz is increased and that of voriconazole is reduced when given concomitantly. Reduced plasma concentrations w/ rifampicin.
Half Life
40-55 hours
Elimination Route
Nearly all of the urinary excretion of the radiolabeled drug was in the form of metabolites.
Pregnancy & Breastfeeding use
Category D: There is positive evidence of human fetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Lactation: Efavirenz may pass through breast milk and cause serious harm to the baby. It should not be used during lactation.
Contraindication
Hypersensitivity. Severe hepatic impairment. Lactation. Concomitant admin with terfenadine, astemizole, cisapride, midazolam, triazolam, pimozide, bepridil, ergot alkaloids, St John’s wort.
Special Warning
Paediatric use: Efavirenz has not been studied in pediatric patients below 3 years of age or who weigh less than 10 kg.
Women taking hormone-based birth control: Women should not rely only on hormone-based birth control, such as pills, injections, or implants, because Efavirenz may make these contraceptives ineffective.
Acute Overdose
Symptoms: Increased adverse CNS effects including involuntary muscle contractions.
Management: Supportive and symptomatic treatment. May administer activated charcoal.
Storage Condition
Store at 25°C.
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