Adult: In combination with other antiretrovirals: As 10 mg/mL solution: 240 mg (24 mL) once daily. As cap: 200 mg once daily. Child: In combination with other antiretrovirals: 1-<3 months As 10 mg/mL solution: 3 mg/kg once daily; >3 months As 10 mg/mL solution: 6 mg/kg once daily. Max: 240 mg daily. In patient weighing >33 kg who are capable of swallowing whole capsules: As capsules: 200 mg once daily.
Renal Impairment
CrCl (mL/min)
Dosage
<15
200 mg as cap every 96 hours or 60 mg as solution (6 mL) every 24 hours.
15-29
200 mg as cap every 72 hours or 80 mg as solution (8 mL) every 24 hours.
30-49
200 mg as cap every 48 hours or 120 mg as solution (12 mL) every 24 hours.
Administration
May be taken with or without food.
Contraindications
Hypersensitivity.
Special Precautions
Patient with severe immune deficiency; chronic Hepatitis B. Renal impairment. Children. Pregnancy and lactation.
Adverse Reactions
Significant: Immune reconstitution syndrome, severe acute exacerbations of Hepatitis B, hyperpigmentation (children). Blood and lymphatic system disorders: Anaemia, neutropenia. Ear and labyrinth disorders: Otitis media. Gastrointestinal disorders: Diarrhoea, vomiting, nausea, abdominal pain, gastroenteritis, dyspepsia. General disorders and administration site conditions: Weakness, fever Immune system disorders: Allergic reaction. Infections and infestations: Infection. Investigations: Increased creatine phosphokinase, increased serum triglycerides, increased amylase, increased serum transaminases. Metabolism and nutrition disorders: Hyperglycaemia. Musculoskeletal and connective tissue disorders: Myalgia, arthralgia. Nervous system disorders: Dizziness, headache, paraesthesia. Psychiatric disorders: Depression, insomnia, abnormal dreams. Respiratory, thoracic and mediastinal disorders: Cough, rhinitis, pneumonia, sinusitis, upper respiratory tract infection, pharyngitis. Skin and subcutaneous tissue disorders: Rash. Potentially Fatal: Lactic acidosis, severe hepatomegaly with steatosis.
Monitor viral load, CD4, LFT, serum creatinine. Perform Hepatitis B testing prior to initiation of therapy.
Drug Interactions
Increased serum concentration of either emtricitabine or co-administered drugs that are eliminated by active tubular secretion. May enhance the adverse effect with lamivudine. May diminish therapeutic effect of cladribine. May decrease serum concentration with orlistat.
Action
Description: Mechanism of Action: Emtricitabine, a synthetic nucleoside analogue of cytidine, is phosphorated intracellularly to form emtricitabine 5’-triphosphate, which interferes with HIV viral RNA dependent DNA polymerase thereby inhibiting viral replication. Pharmacokinetics: Absorption: Rapidly and extensively absorbed from the gastrointestinal tract. Bioavailability: 93% (cap); 75% (solution). Time to peak plasma concentration: 1-2 hours. Distribution: Crosses placenta, enters breast milk. Plasma protein binding: <4%. Metabolism: Metabolised minimally via oxidation and glucuronide conjugation. Phosphorated intracellularly to emtricitabine 5’-triphosphate. Excretion: Via urine (86% as unchanged drug, 13% as metabolites, 9% as oxidative metabolite, 4% as glucuronide metabolite); faeces (14%). Elimination half-life: Approx 10 hours (emtricitabine). Intracellular half-life: 39 hours (emtricitabine 5’-triphosphate).
Chemical Structure
Emtricitabine Source: National Center for Biotechnology Information. PubChem Database. Emtricitabine, CID=60877, https://pubchem.ncbi.nlm.nih.gov/compound/Emtricitabine (accessed on Jan. 22, 2020)
Storage
Cap: Store at 25°C. Solution: Store between 2-8°C.
J05AF09 - emtricitabine ; Belongs to the class of nucleoside and nucleotide reverse transcriptase inhibitors. Used in the systemic treatment of viral infections.
References
Anon. Emtricitabine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/06/2020 .Buckingham R (ed). Emtricitabine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/06/2020.Emtriva 200 mg Hard Capsules (Gilead Sciences Ireland UC). European Medicines Agency [online]. Accessed 30/06/2020.Emtriva Capsule, Solution (Gilead Sciences, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 30/06/2020.Joint Formulary Committee. Emtricitabine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/06/2020 .
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