Emtricitabine Case Study

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Structure of Emtricitabine

b) Chemical Name / IUPAC Name: 4-amino-5-fluoro-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-1,2-dihydropyrimidin-2-one

c) Molecular Formula: C8H10FN3O3S

d) Molecular Weight: 247.248 g/mol

e) Description: white to off-white crystalline solid

f) Melting point: 136 °C to140 °C

g) Solubility: Freely soluble in methanol and in water; practically insoluble in methylene chloride.

h) pKa value: 2.65

i) Route of administration: Oral

j) Excretion: Renal (86%) and fecal (14%)

k) Metabolism: Hepatic oxidation and glucuronidation CYP system not involved

l) Storage: Store at 25 °C (77 °F); excursions permitted to 15 °C-30 °C (59 °F-86 °F)

m) Trade name: Emtriva, Truvada (a fixed-dose combination with Tenofovir), Atripla (A fixed-dose triple combination of Emtricitabine, Tenofovir and Efavirenz)

2.2.4 Drug profile of Tenofovir:
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It is used in combination with other antiretrovirals for the treatment of HIV/AIDS. Food and Drug Administration approved Tenofovir on 26th October 2001. It is an analogue of adenosine monophosphate. It inhibits the activity of HIV-1 reverse transcriptase enzyme that converts HIV RNA into viral DNA. NtRTIs stops this reverse transcription, thus interrupts HIV replication and prevents HIV from infecting human cells. Tenofovir is also used for the treatment of Hepatitis B. Market availability of Tenofovir is in the name of Viread. The recommended dosage of Tenofovir is 300 mg taken once daily with

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