Peringatan Keamanan

Acute overdose: Inadvertent pediatric overdoses have occurred with doses up to 1.5 mg/kg zalcitabine. Chronic overdose: in an initial dose-finding study in which zalcitabine was administered at doses 25 times (0.25 mg/kg every 8 hours) the currently recommended dose, one patient discontinued zalcitabine after 1½ weeks of treatment subsequent to the development of a rash and fever.

Zalcitabine

DB00943

small molecule approved investigational

Deskripsi

A dideoxynucleoside compound in which the 3'-hydroxyl group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of 5' to 3' phosphodiester linkages, which are needed for the elongation of DNA chains, thus resulting in the termination of viral DNA growth. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy.

Struktur Molekul 2D

Berat 211.2178

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) 2 hours

Volume Distribusi * 0.304 to 0.734 L/kg

Klirens (Clearance) * 285 mL/min [HIV-infected patients receiving 1.5 mg IV infusion for 1 hour]

Absorpsi

Bioavailability is over 80% following oral administration.

Metabolisme

Zalcitabine is not reported to undergo significant hepatic metabolism; it is mainly phosphorylated intracellularly to zalcitabine triphosphate, the active substrate for HIV-reverse transcriptase. The concentration of zalcitabine triphosphate remains low for quantitative detection and measurement in the plasma following administration of therapeutic doses FDA Label.

Rute Eliminasi

Renal excretion of unchanged drug appears to be the primary route of elimination, accounting for approximately 80% of an intravenous dose and 60% of an orally administered dose within 24 hours after dosing (n=19). Renal clearance exceeds glomerular filtration rate suggesting renal tubular secretion contributes to the elimination of zalcitabine by the kidneys.

Interaksi Makanan

2 Data

1. Avoid multivalent ions. Magnesium and aluminum containing products can reduce the absorption of this medication.
2. Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.

Interaksi Obat

120 Data

Ribavirin	Ribavirin may increase the hepatotoxic activities of Zalcitabine.
Ganciclovir	The risk or severity of cytopenia can be increased when Ganciclovir is combined with Zalcitabine.
Valganciclovir	The risk or severity of cytopenia can be increased when Valganciclovir is combined with Zalcitabine.
Cyclosporine	The excretion of Zalcitabine can be decreased when combined with Cyclosporine.
Riboflavin	The excretion of Zalcitabine can be decreased when combined with Riboflavin.
Folic acid	The excretion of Zalcitabine can be decreased when combined with Folic acid.
Aspartame	The excretion of Zalcitabine can be decreased when combined with Aspartame.
Pravastatin	The excretion of Zalcitabine can be decreased when combined with Pravastatin.
Cefotiam	The excretion of Zalcitabine can be decreased when combined with Cefotiam.
Ethoxzolamide	The excretion of Zalcitabine can be decreased when combined with Ethoxzolamide.
Valproic acid	The excretion of Zalcitabine can be decreased when combined with Valproic acid.
Codeine	The excretion of Zalcitabine can be decreased when combined with Codeine.
Piperacillin	The excretion of Zalcitabine can be decreased when combined with Piperacillin.
Indomethacin	The excretion of Zalcitabine can be decreased when combined with Indomethacin.
Aminohippuric acid	The excretion of Zalcitabine can be decreased when combined with Aminohippuric acid.
Cidofovir	The excretion of Zalcitabine can be decreased when combined with Cidofovir.
Trifluridine	The excretion of Zalcitabine can be decreased when combined with Trifluridine.
Chloramphenicol	The excretion of Zalcitabine can be decreased when combined with Chloramphenicol.
Cefalotin	The excretion of Zalcitabine can be decreased when combined with Cefalotin.
Cefotaxime	The excretion of Zalcitabine can be decreased when combined with Cefotaxime.
Tolmetin	The excretion of Zalcitabine can be decreased when combined with Tolmetin.
Cimetidine	The excretion of Zalcitabine can be decreased when combined with Cimetidine.
Caspofungin	The excretion of Zalcitabine can be decreased when combined with Caspofungin.
Foscarnet	The excretion of Zalcitabine can be decreased when combined with Foscarnet.
Piroxicam	The excretion of Zalcitabine can be decreased when combined with Piroxicam.
Methotrexate	The excretion of Zalcitabine can be decreased when combined with Methotrexate.
Cephalexin	The excretion of Zalcitabine can be decreased when combined with Cephalexin.
Carbenicillin	The excretion of Zalcitabine can be decreased when combined with Carbenicillin.
Enalapril	The excretion of Zalcitabine can be decreased when combined with Enalapril.
Diclofenac	The excretion of Zalcitabine can be decreased when combined with Diclofenac.
Oxytetracycline	The excretion of Zalcitabine can be decreased when combined with Oxytetracycline.
Sulindac	The excretion of Zalcitabine can be decreased when combined with Sulindac.
Cyclothiazide	The excretion of Zalcitabine can be decreased when combined with Cyclothiazide.
Nafcillin	The excretion of Zalcitabine can be decreased when combined with Nafcillin.
Chlorpropamide	The excretion of Zalcitabine can be decreased when combined with Chlorpropamide.
Fluorescein	The excretion of Zalcitabine can be decreased when combined with Fluorescein.
Furosemide	The excretion of Zalcitabine can be decreased when combined with Furosemide.
Methazolamide	The excretion of Zalcitabine can be decreased when combined with Methazolamide.
Flurbiprofen	The excretion of Zalcitabine can be decreased when combined with Flurbiprofen.
Adefovir dipivoxil	The excretion of Zalcitabine can be decreased when combined with Adefovir dipivoxil.
Nateglinide	The excretion of Zalcitabine can be decreased when combined with Nateglinide.
Etodolac	The excretion of Zalcitabine can be decreased when combined with Etodolac.
Tetracycline	The excretion of Zalcitabine can be decreased when combined with Tetracycline.
Nalidixic acid	The excretion of Zalcitabine can be decreased when combined with Nalidixic acid.
Acyclovir	The excretion of Zalcitabine can be decreased when combined with Acyclovir.
Naproxen	The excretion of Zalcitabine can be decreased when combined with Naproxen.
Phenylbutazone	The excretion of Zalcitabine can be decreased when combined with Phenylbutazone.
Acetazolamide	The excretion of Zalcitabine can be decreased when combined with Acetazolamide.
Carprofen	The excretion of Zalcitabine can be decreased when combined with Carprofen.
Cinoxacin	The excretion of Zalcitabine can be decreased when combined with Cinoxacin.
Diflunisal	The excretion of Zalcitabine can be decreased when combined with Diflunisal.
Ranitidine	The excretion of Zalcitabine can be decreased when combined with Ranitidine.
Chlorothiazide	The excretion of Zalcitabine can be decreased when combined with Chlorothiazide.
Bumetanide	The excretion of Zalcitabine can be decreased when combined with Bumetanide.
Etacrynic acid	The excretion of Zalcitabine can be decreased when combined with Etacrynic acid.
Dinoprostone	The excretion of Zalcitabine can be decreased when combined with Dinoprostone.
Salicylic acid	The excretion of Zalcitabine can be decreased when combined with Salicylic acid.
Meclofenamic acid	The excretion of Zalcitabine can be decreased when combined with Meclofenamic acid.
Acetylsalicylic acid	The excretion of Zalcitabine can be decreased when combined with Acetylsalicylic acid.
Hydrochlorothiazide	The excretion of Zalcitabine can be decreased when combined with Hydrochlorothiazide.
Ketoprofen	The excretion of Zalcitabine can be decreased when combined with Ketoprofen.
Glyburide	The excretion of Zalcitabine can be decreased when combined with Glyburide.
Minocycline	The excretion of Zalcitabine can be decreased when combined with Minocycline.
Probenecid	The excretion of Zalcitabine can be decreased when combined with Probenecid.
Ibuprofen	The excretion of Zalcitabine can be decreased when combined with Ibuprofen.
Novobiocin	The excretion of Zalcitabine can be decreased when combined with Novobiocin.
Benzylpenicillin	The excretion of Zalcitabine can be decreased when combined with Benzylpenicillin.
Norfloxacin	The excretion of Zalcitabine can be decreased when combined with Norfloxacin.
Amoxicillin	The excretion of Zalcitabine can be decreased when combined with Amoxicillin.
Tolbutamide	The excretion of Zalcitabine can be decreased when combined with Tolbutamide.
Cefadroxil	The excretion of Zalcitabine can be decreased when combined with Cefadroxil.
Ofloxacin	The excretion of Zalcitabine can be decreased when combined with Ofloxacin.
Captopril	The excretion of Zalcitabine can be decreased when combined with Captopril.
Ceftriaxone	The excretion of Zalcitabine can be decreased when combined with Ceftriaxone.
Cefamandole	The excretion of Zalcitabine can be decreased when combined with Cefamandole.
Cefazolin	The excretion of Zalcitabine can be decreased when combined with Cefazolin.
Cefoperazone	The excretion of Zalcitabine can be decreased when combined with Cefoperazone.
Cefradine	The excretion of Zalcitabine can be decreased when combined with Cefradine.
Cefacetrile	The excretion of Zalcitabine can be decreased when combined with Cefacetrile.
Aminophenazone	The excretion of Zalcitabine can be decreased when combined with Aminophenazone.
Antipyrine	The excretion of Zalcitabine can be decreased when combined with Antipyrine.
Cilastatin	The excretion of Zalcitabine can be decreased when combined with Cilastatin.
Tazobactam	The excretion of Zalcitabine can be decreased when combined with Tazobactam.
Topiroxostat	The excretion of Zalcitabine can be decreased when combined with Topiroxostat.
Glutaric Acid	The excretion of Zalcitabine can be decreased when combined with Glutaric Acid.
Oxyphenbutazone	The excretion of Zalcitabine can be decreased when combined with Oxyphenbutazone.
Phenacetin	The excretion of Zalcitabine can be decreased when combined with Phenacetin.
Taurocholic acid	The excretion of Zalcitabine can be decreased when combined with Taurocholic acid.
Caprylic acid	The excretion of Zalcitabine can be decreased when combined with Caprylic acid.
Ataluren	The excretion of Zalcitabine can be decreased when combined with Ataluren.
Ellagic acid	The excretion of Zalcitabine can be decreased when combined with Ellagic acid.
Dabrafenib	The excretion of Zalcitabine can be decreased when combined with Dabrafenib.
Dolutegravir	The excretion of Zalcitabine can be decreased when combined with Dolutegravir.
Lenvatinib	The excretion of Zalcitabine can be decreased when combined with Lenvatinib.
Silibinin	The excretion of Zalcitabine can be decreased when combined with Silibinin.
Cabotegravir	The excretion of Zalcitabine can be decreased when combined with Cabotegravir.
Enasidenib	The excretion of Zalcitabine can be decreased when combined with Enasidenib.
Istradefylline	The excretion of Zalcitabine can be decreased when combined with Istradefylline.
Favipiravir	The excretion of Zalcitabine can be decreased when combined with Favipiravir.
Ceftizoxime	The excretion of Zalcitabine can be decreased when combined with Ceftizoxime.

Target Protein

Gag-Pol polyprotein gag-pol

Reverse transcriptase/RNaseH pol

Referensi & Sumber

Artikel (PubMed)

PMID: 8097417
Shelton MJ, O'Donnell AM, Morse GD: Zalcitabine. Ann Pharmacother. 1993 Apr;27(4):480-9.
PMID: 7614775
Devineni D, Gallo JM: Zalcitabine. Clinical pharmacokinetics and efficacy. Clin Pharmacokinet. 1995 May;28(5):351-60.

Contoh Produk & Brand

Produk: 5 • International brands: 0

Produk

Hivid

Tablet, film coated • 0.75 mg/1 • Oral • US • Approved
Hivid

Tablet, film coated • 0.375 mg/1 • Oral • US • Approved
Hivid

Tablet, film coated • 0.75 mg/1 • Oral • US • Approved
Hivid Tab 0.375mg

Tablet • .375 mg • Oral • Canada • Approved
Hivid Tab 0.75 mg

Tablet • .75 mg • Oral • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.