Emtricitabin
Emtricitabin Uses, Dosage, Side Effects, Food Interaction and all others data.
Emtricitabin is a nucleoside reverse transcriptase inhibitor (NRTI) indicated for the treatment of HIV infection in adults or combined with tenofovir alafenamide for the prevention of HIV-1 infection in high risk adolescents and adults. Emtricitabin is a cytidine analogue. The drug works by inhibiting HIV reverse transcriptase, preventing transcription of HIV RNA to DNA.
Emtricitabin was granted FDA approval on 2 July 2003.
Emtricitabin is a cytidine analog that competes with the natural substrate of HIV-1 reverse transcriptase to be incorporated into newly formed DNA, terminating its transcription. It is administered once daily so it has a long duration of action. Patients should be counselled regarding the risk of lactic acidosis and hepatomegaly with steatosis.
| Trade Name | Emtricitabin |
| Availability | Prescription only |
| Generic | Emtricitabine |
| Emtricitabine Other Names | Emtricitabin, Emtricitabina, Emtricitabine, Emtricitabinum |
| Related Drugs | Biktarvy, Truvada, tenofovir, ritonavir, zidovudine, abacavir, lamivudine, Complera, Atripla, Stribild |
| Type | |
| Formula | C8H10FN3O3S |
| Weight | Average: 247.247 Monoisotopic: 247.042690096 |
| Protein binding | Emtricitabine is 5 mainly serum albumin.[A19948] |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Emtricitabin is a nucleoside reverse transcriptase inhibitor used for the treatment and prophylaxis of HIV.
Emtricitabin is indicated in combination with other medications for the treatment of HIV-1 infections; treatment of HIV-1 infections in pediatric patients 25-35kg, treatment of HIV-1 infections in adult patients ≥35kg, for pre exposure prophylaxis of HIV-1 in adolescent and adult patients excluding those who have receptive vaginal sex; treatment of HIV-1 infections in pediatric and adult patients ≥17kg, pre exposure prophylaxis in adolescents and adults ≥35kg; treatment of HIV-1 in patients ≥12 years and ≥35kg; treatment of HIV-1 in patients weighing ≥35kg; treatment of HIV-1 in patients weighing ≥25kg; and treatment of HIV-1 in patients weighing ≥40kg.
Emtricitabin is also used to associated treatment for these conditions: HIV Transmission, Human Immunodeficiency Virus (HIV) Infections, Human Immunodeficiency Virus Type 1 (HIV-1), Human Immunodeficiency Virus Type 1 (HIV-1) Infection
How Emtricitabin works
Emtricitabin is a cytidine analog which, when phosphorylated to emtricitabine 5'-triphosphate, competes with deoxycytidine 5'-triphosphate for HIV-1 reverse transcriptase. As HIV-1 reverse transcriptase incorporates emtricitabine into forming DNA strands, new nucleotides are unable to be incorporated, leading to viral DNA chain termination. Inhibition of reverse transcriptase prevents transcription of viral RNA into DNA, therefore the virus is unable to incorporate its DNA into host DNA and replicate using host cell machinery. This reduces viral load.
Toxicity
The LD50 of emtricitabine is not readily available.[9019,L9818]
Symptoms of emtricitabine toxicity include hepatotoxicity with steatosis, as well as lactic acidosis. Treat overdose with symptomatic and supportive measures, including hemodialysis.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Emtricitabin Drug Interaction
Unknown: citalopram, citalopram, ethanol, ethanol, raltegravir, raltegravir, pregabalin, pregabalin, oxycodone, oxycodone, acetaminophen, acetaminophen, tramadol, tramadol, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol, olanzapine, olanzapine
Emtricitabin Disease Interaction
Volume of Distribution
The apparent central volume of distribution is 42.3L and the peripheral volume of distribution is 55.4L.
Elimination Route
Emtricitabin reaches a Cmax of 1.8±0.7µg/mL with a Tmax of 1-2 hours, and has an AUC of 10±3.1µg*hr/mL. The bioavailability of emtricitabine capsules is 93% and the bioavailability of the oral solution is 75%. Taking emtricitabine with food decreases the Cmax by 29%.[L9019
Half Life
The half life of emtricitabine is approximately 10 hours.
Clearance
Emtricitabin has an apparent elimination rate of 15.1L/h. This rate is closely linked to creatinine clearance.
Elimination Route
Emtricitabin is 86% recovered in the urine and 14% recovered in feces. 13% of the dose is recovered in the urine as metabolites; 9% as 3'-sulfoxide diastereomers and 4% as 2'-O-glucuronide.
Innovators Monograph
You find simplified version here Emtricitabin
