Peringatan Keamanan

The LD₅₀ of emtricitabine is not readily available.9019,L9818

Symptoms of emtricitabine toxicity include hepatotoxicity with steatosis, as well as lactic acidosis.^L9019 Treat overdose with symptomatic and supportive measures, including hemodialysis.^L9019

Emtricitabine

DB00879

small molecule approved investigational

Deskripsi

Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) indicated for the treatment of HIV infection in adults^L9019 or combined with tenofovir alafenamide for the prevention of HIV-1 infection in high risk adolescents and adults.^L9010 Emtricitabine is a cytidine analogue.^L9019 The drug works by inhibiting HIV reverse transcriptase, preventing transcription of HIV RNA to DNA.^L9019

Emtricitabine was granted FDA approval on 2 July 2003.^L9019

Struktur Molekul 2D

Berat 247.247

Wujud solid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of emtricitabine is approximately 10 hours.[L9019]

Volume Distribusi The apparent central volume of distribution is 42.3L and the peripheral volume of distribution is 55.4L.[A187673]

Klirens (Clearance) Emtricitabine has an apparent elimination rate of 15.1L/h.[A187673] This rate is closely linked to creatinine clearance.[A187673]

Absorpsi

Emtricitabine reaches a C_max of 1.8±0.7µg/mL with a T_max of 1-2 hours, and has an AUC of 10±3.1µg\*hr/mL.^L9019 The bioavailability of emtricitabine capsules is 93% and the bioavailability of the oral solution is 75%.^L9019 Taking emtricitabine with food decreases the C_max by 29%.[L9019

Metabolisme

Emtricitabine is approximately 86% unmetabolized.^L9019 Approximately 9% of a dose is metabolized to 3'-sulfoxide diastereomers, 4% to the 2'-O-glucuronide, and a minor amount is converted to 5-fluorocytosine.A187643,L9019

Rute Eliminasi

Emtricitabine is 86% recovered in the urine and 14% recovered in feces.^L9019 13% of the dose is recovered in the urine as metabolites; 9% as 3'-sulfoxide diastereomers and 4% as 2'-O-glucuronide.^L9019

Interaksi Makanan

1 Data

1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

60 Data

Ribavirin	Ribavirin may increase the hepatotoxic activities of Emtricitabine.
Ganciclovir	The risk or severity of cytopenia can be increased when Ganciclovir is combined with Emtricitabine.
Valganciclovir	The risk or severity of cytopenia can be increased when Valganciclovir is combined with Emtricitabine.
Flecainide	The excretion of Flecainide can be decreased when combined with Emtricitabine.
Relebactam	The excretion of Relebactam can be decreased when combined with Emtricitabine.
Metformin	The excretion of Emtricitabine can be decreased when combined with Metformin.
Levofloxacin	The excretion of Levofloxacin can be decreased when combined with Emtricitabine.
Nadolol	The excretion of Nadolol can be decreased when combined with Emtricitabine.
Estrone sulfate	The excretion of Estrone sulfate can be decreased when combined with Emtricitabine.
N-methylnicotinamide	The excretion of N-methylnicotinamide can be decreased when combined with Emtricitabine.
Solriamfetol	The excretion of Solriamfetol can be decreased when combined with Emtricitabine.
Guanidine	The excretion of Emtricitabine can be decreased when combined with Guanidine.
Cephalexin	The excretion of Emtricitabine can be decreased when combined with Cephalexin.
Acyclovir	The excretion of Emtricitabine can be decreased when combined with Acyclovir.
Cefradine	The excretion of Cefradine can be decreased when combined with Emtricitabine.
Procainamide	The excretion of Procainamide can be decreased when combined with Emtricitabine.
Topotecan	The excretion of Topotecan can be decreased when combined with Emtricitabine.
Abemaciclib	The excretion of Abemaciclib can be decreased when combined with Emtricitabine.
Pyrimethamine	The excretion of Emtricitabine can be decreased when combined with Pyrimethamine.
Tafenoquine	The excretion of Emtricitabine can be decreased when combined with Tafenoquine.
Istradefylline	The excretion of Emtricitabine can be decreased when combined with Istradefylline.
Glasdegib	The excretion of Emtricitabine can be decreased when combined with Glasdegib.
Gilteritinib	The excretion of Emtricitabine can be decreased when combined with Gilteritinib.
Brigatinib	The excretion of Emtricitabine can be decreased when combined with Brigatinib.
Fedratinib	Fedratinib may decrease the excretion rate of Emtricitabine which could result in a higher serum level.
Pexidartinib	The excretion of Emtricitabine can be decreased when combined with Pexidartinib.
Tazemetostat	The excretion of Emtricitabine can be decreased when combined with Tazemetostat.
Cimetidine	The excretion of Emtricitabine can be decreased when combined with Cimetidine.
Ciprofloxacin	The excretion of Emtricitabine can be decreased when combined with Ciprofloxacin.
Lofexidine	The excretion of Emtricitabine can be decreased when combined with Lofexidine.
Tucatinib	The excretion of Emtricitabine can be decreased when combined with Tucatinib.
Methylene blue	The excretion of Emtricitabine can be decreased when combined with Methylene blue.
Capmatinib	The excretion of Emtricitabine can be decreased when combined with Capmatinib.
Selpercatinib	The excretion of Emtricitabine can be decreased when combined with Selpercatinib.
Ripretinib	The excretion of Emtricitabine can be decreased when combined with Ripretinib.
Pralsetinib	The excretion of Emtricitabine can be decreased when combined with Pralsetinib.
Remdesivir	The excretion of Emtricitabine can be decreased when combined with Remdesivir.
Famotidine	The excretion of Emtricitabine can be decreased when combined with Famotidine.
Plazomicin	The excretion of Emtricitabine can be decreased when combined with Plazomicin.
Trilaciclib	The excretion of Emtricitabine can be decreased when combined with Trilaciclib.
Ranolazine	The excretion of Emtricitabine can be decreased when combined with Ranolazine.
Trimethoprim	Trimethoprim may decrease the excretion rate of Emtricitabine which could result in a higher serum level.
Rubella virus vaccine	The therapeutic efficacy of Rubella virus vaccine can be decreased when used in combination with Emtricitabine.
Bacillus calmette-guerin substrain tice live antigen	The therapeutic efficacy of Bacillus calmette-guerin substrain tice live antigen can be decreased when used in combination with Emtricitabine.
Bacillus calmette-guerin substrain connaught live antigen	The therapeutic efficacy of Bacillus calmette-guerin substrain connaught live antigen can be decreased when used in combination with Emtricitabine.
Yellow fever vaccine	The therapeutic efficacy of Yellow fever vaccine can be decreased when used in combination with Emtricitabine.
Anthrax vaccine	The therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Emtricitabine.
Typhoid Vaccine Live	The therapeutic efficacy of Typhoid Vaccine Live can be decreased when used in combination with Emtricitabine.
BCG vaccine	The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Emtricitabine.
Human adenovirus e serotype 4 strain cl-68578 antigen	The therapeutic efficacy of Human adenovirus e serotype 4 strain cl-68578 antigen can be decreased when used in combination with Emtricitabine.
Vibrio cholerae CVD 103-HgR strain live antigen	The therapeutic efficacy of Vibrio cholerae CVD 103-HgR strain live antigen can be decreased when used in combination with Emtricitabine.
Adenovirus type 7 vaccine live	The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Emtricitabine.
Varicella zoster vaccine (live/attenuated)	The therapeutic efficacy of Varicella zoster vaccine (live/attenuated) can be decreased when used in combination with Emtricitabine.
Bacillus calmette-guerin substrain russian BCG-I live antigen	The therapeutic efficacy of Bacillus calmette-guerin substrain russian BCG-I live antigen can be decreased when used in combination with Emtricitabine.
Risdiplam	The serum concentration of Emtricitabine can be increased when it is combined with Risdiplam.
Fexinidazole	The excretion of Emtricitabine can be decreased when combined with Fexinidazole.
Levoketoconazole	The excretion of Emtricitabine can be decreased when combined with Levoketoconazole.
Capivasertib	The excretion of Emtricitabine can be decreased when combined with Capivasertib.
Chikungunya vaccine (live, attenuated)	The therapeutic efficacy of Chikungunya vaccine (live, attenuated) can be decreased when used in combination with Emtricitabine.
Smallpox (Vaccinia) Vaccine, Live	The therapeutic efficacy of Smallpox (Vaccinia) Vaccine, Live can be decreased when used in combination with Emtricitabine.

Target Protein

Reverse transcriptase/RNaseH pol

Gag-Pol polyprotein gag-pol

Referensi & Sumber

Artikel (PubMed)

PMID: 8868002
Shockcor JP, Wurm RM, Frick LW, Sanderson PN, Farrant RD, Sweatman BC, Lindon JC: Hplc-nmr identification of the human urinary metabolites of (-)-cis-5-fluoro-1-2-(hydroxymethyl)-1,3-oxathiolan-5-yl cytosine, a nucleoside analogue active against human immunodeficiency virus (HIV). Xenobiotica. 1996 Feb;26(2):189-99. doi: 10.3109/00498259609046699.
PMID: 24492366
Valade E, Treluyer JM, Bouazza N, Ghosn J, Foissac F, Benaboud S, Fauchet F, Viard JP, Urien S, Hirt D: Population pharmacokinetics of emtricitabine in HIV-1-infected adult patients. Antimicrob Agents Chemother. 2014;58(4):2256-61. doi: 10.1128/AAC.02058-13. Epub 2014 Feb 3.
PMID: 28737291
Orkin C, Llibre JM, Gallien S, Antinori A, Behrens G, Carr A: Nucleoside reverse transcriptase inhibitor-reducing strategies in HIV treatment: assessing the evidence. HIV Med. 2018 Jan;19(1):18-32. doi: 10.1111/hiv.12534. Epub 2017 Jul 24.
PMID: 15814459
Bocedi A, Notaril S, Narciso P, Bolli A, Fasano M, Ascenzi P: Binding of anti-HIV drugs to human serum albumin. IUBMB Life. 2004 Oct;56(10):609-14.

Link

Contoh Produk & Brand

Produk: 235 • International brands: 1

Produk

Ag-emtricitabine / Tenofovir Disoproxil Fumarate

Tablet • - • Oral • Canada • Generic • Approved
Apo-efavirenz-emtricitabine-tenofovir

Tablet • - • Oral • Canada • Generic • Approved
Apo-emtricitabine-tenofovir

Tablet • - • Oral • Canada • Generic • Approved
Atripla

Tablet, film coated • - • Oral • US • Approved
Atripla

Tablet, film coated • - • Oral • US • Approved
Atripla

Tablet, film coated • - • Oral • US • Approved
Atripla

Tablet, film coated • - • Oral • US • Approved
Atripla

Tablet, film coated • - • Oral • US • Approved

Menampilkan 8 dari 235 produk.

International Brands

Coviracil

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.