Peringatan Keamanan

LD50 100 mg/kg (Human, oral). Adverse reactions include rash, abnormal liver function tests, hepatitis, peripheral neuropathy, mild central nervous system (CNS) effects. In vivo, Isoniazid reacts with pyridoxal to form a hydrazone, and thus inhibits generation of pyridoxal phosphate. Isoniazid also combines with pyridoxal phosphate; high doses interfere with the coenzyme function of the latter.

Isoniazid

DB00951

small molecule approved investigational

Deskripsi

Antibacterial agent used primarily as a tuberculostatic. It remains the treatment of choice for tuberculosis.

Struktur Molekul 2D

Berat 137.1393
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Fast acetylators: 0.5 to 1.6 hours. Slow acetylators: 2 to 5 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Readily absorbed following oral administration; however, may undergo significant first pass metabolism. Absorption and bioavailability are reduced when isoniazid is administered with food.

Metabolisme

Primarily hepatic. Isoniazid is acetylated by N -acetyl transferase to N -acetylisoniazid; it is then biotransformed to isonicotinic acid and monoacetylhydrazine. Monoacetylhydrazine is associated with hepatotoxicity via formation of a reactive intermediate metabolite when N-hydroxylated by the cytochrome P450 mixed oxidase system. The rate of acetylation is genetically determined. Slow acetylators are characterized by a relative lack of hepatic N -acetyltransferase.

Rute Eliminasi

From 50 to 70 percent of a dose of isoniazid is excreted in the urine within 24 hours.

Farmakogenomik

1 Varian
CYP2E1 (None)

The presence of this genotype in CYP2E1 may be associated with an increased risk of drug-induced hepatotoxicity from isoniazid treatment.

Interaksi Makanan

8 Data
  • 1. Administer vitamin supplements. Vitamin B6 (pyridoxine) should be given with isoniazid to prevent deficiency.
  • 2. Avoid alcohol. Avoid drinking alcoholic beverages such as unpasteurized beer; unless approved by your physician, as they may contain tyramine. Consuming alcohol may also increase the risk of isoniazid induced hepatitis and neuropathy.
  • 3. Avoid chocolate. Chocolate contains caffeine, which should be limited during isoniazid therapy.
  • 4. Avoid histamine-containing foods and supplements. Histamine-containing foods (e.g., skipjack, tuna, other tropical fish) can cause headaches, sweating, palpitations, flushing, and hypotension.
  • 5. Avoid tyramine-containing foods and supplements. Tyramine-containing foods include cheese, red wine, fava beans, pickled food, cured food, and alcoholic beverages.
  • 6. Limit caffeine intake.
  • 7. Take on an empty stomach. Take at least 1 hour before or 2 hours after meals.
  • 8. Take separate from antacids. Taking this medication with antacids can reduce absorption.

Interaksi Obat

1791 Data
Cilostazol The serum concentration of Cilostazol can be increased when it is combined with Isoniazid.
Citalopram The serum concentration of Citalopram can be increased when it is combined with Isoniazid.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Isoniazid.
Clopidogrel The serum concentration of the active metabolites of Clopidogrel can be reduced when Clopidogrel is used in combination with Isoniazid resulting in a loss in efficacy.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Isoniazid.
Everolimus The metabolism of Everolimus can be decreased when combined with Isoniazid.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Isoniazid.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Isoniazid.
Ivabradine The metabolism of Ivabradine can be decreased when combined with Isoniazid.
Ivacaftor The metabolism of Ivacaftor can be decreased when combined with Isoniazid.
Lurasidone The metabolism of Lurasidone can be decreased when combined with Isoniazid.
Naloxegol The metabolism of Naloxegol can be decreased when combined with Isoniazid.
Olaparib The metabolism of Olaparib can be decreased when combined with Isoniazid.
Ranolazine The metabolism of Ranolazine can be decreased when combined with Isoniazid.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Isoniazid.
Avanafil The metabolism of Avanafil can be decreased when combined with Isoniazid.
Eplerenone The metabolism of Eplerenone can be decreased when combined with Isoniazid.
Colchicine The metabolism of Colchicine can be decreased when combined with Isoniazid.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Isoniazid.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Isoniazid.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Isoniazid.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Isoniazid.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Isoniazid.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Isoniazid.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Isoniazid.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Isoniazid.
Phenytoin The serum concentration of Phenytoin can be increased when it is combined with Isoniazid.
Fosphenytoin The serum concentration of Fosphenytoin can be increased when it is combined with Isoniazid.
Cycloserine The risk or severity of adverse effects can be increased when Isoniazid is combined with Cycloserine.
Caffeine The serum concentration of Caffeine can be increased when it is combined with Isoniazid.
Theophylline The serum concentration of Theophylline can be increased when it is combined with Isoniazid.
Dyphylline The serum concentration of Dyphylline can be increased when it is combined with Isoniazid.
Pentoxifylline The serum concentration of Pentoxifylline can be increased when it is combined with Isoniazid.
Mercaptopurine The serum concentration of Mercaptopurine can be increased when it is combined with Isoniazid.
Aminophylline The serum concentration of Aminophylline can be increased when it is combined with Isoniazid.
Oxtriphylline The serum concentration of Oxtriphylline can be increased when it is combined with Isoniazid.
Theobromine The serum concentration of Theobromine can be increased when it is combined with Isoniazid.
Fenethylline The serum concentration of Fenethylline can be increased when it is combined with Isoniazid.
8-azaguanine The serum concentration of 8-azaguanine can be increased when it is combined with Isoniazid.
7,9-Dimethylguanine The serum concentration of 7,9-Dimethylguanine can be increased when it is combined with Isoniazid.
Xanthine The serum concentration of Xanthine can be increased when it is combined with Isoniazid.
7-Deazaguanine The serum concentration of 7-Deazaguanine can be increased when it is combined with Isoniazid.
Guanine The serum concentration of Guanine can be increased when it is combined with Isoniazid.
9-Methylguanine The serum concentration of 9-Methylguanine can be increased when it is combined with Isoniazid.
Peldesine The serum concentration of Peldesine can be increased when it is combined with Isoniazid.
Hypoxanthine The serum concentration of Hypoxanthine can be increased when it is combined with Isoniazid.
9-Deazaguanine The serum concentration of 9-Deazaguanine can be increased when it is combined with Isoniazid.
Propentofylline The serum concentration of Propentofylline can be increased when it is combined with Isoniazid.
Valomaciclovir The serum concentration of Valomaciclovir can be increased when it is combined with Isoniazid.
3-isobutyl-1-methyl-7H-xanthine The serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Isoniazid.
Uric acid The serum concentration of Uric acid can be increased when it is combined with Isoniazid.
Doxofylline The serum concentration of Doxofylline can be increased when it is combined with Isoniazid.
6-O-benzylguanine The serum concentration of 6-O-benzylguanine can be increased when it is combined with Isoniazid.
Lisofylline The serum concentration of Lisofylline can be increased when it is combined with Isoniazid.
Lobucavir The serum concentration of Lobucavir can be increased when it is combined with Isoniazid.
Cafedrine The serum concentration of Cafedrine can be increased when it is combined with Isoniazid.
Theodrenaline The serum concentration of Theodrenaline can be increased when it is combined with Isoniazid.
Bamifylline The serum concentration of Bamifylline can be increased when it is combined with Isoniazid.
Proxyphylline The serum concentration of Proxyphylline can be increased when it is combined with Isoniazid.
Acefylline The serum concentration of Acefylline can be increased when it is combined with Isoniazid.
Etamiphylline The serum concentration of Etamiphylline can be increased when it is combined with Isoniazid.
Pentifylline The serum concentration of Pentifylline can be increased when it is combined with Isoniazid.
Bufylline The serum concentration of Bufylline can be increased when it is combined with Isoniazid.
Bromotheophylline The serum concentration of Bromotheophylline can be increased when it is combined with Isoniazid.
Furafylline The serum concentration of Furafylline can be increased when it is combined with Isoniazid.
8-chlorotheophylline The serum concentration of 8-chlorotheophylline can be increased when it is combined with Isoniazid.
PCS-499 The serum concentration of PCS-499 can be increased when it is combined with Isoniazid.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Isoniazid.
Acetaminophen Isoniazid may increase the hepatotoxic activities of Acetaminophen.
Propacetamol Isoniazid may increase the hepatotoxic activities of Propacetamol.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Isoniazid.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Isoniazid.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Isoniazid.
Carbamazepine The metabolism of Carbamazepine can be decreased when combined with Isoniazid.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Isoniazid.
Ethionamide The serum concentration of Isoniazid can be increased when it is combined with Ethionamide.
Rifabutin Rifabutin may increase the hepatotoxic activities of Isoniazid.
Rifapentine Rifapentine may increase the hepatotoxic activities of Isoniazid.
Rifaximin Rifaximin may increase the hepatotoxic activities of Isoniazid.
Rifamycin Rifamycin may increase the hepatotoxic activities of Isoniazid.
25-desacetylrifapentine 25-desacetylrifapentine may increase the hepatotoxic activities of Isoniazid.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Isoniazid.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Isoniazid.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Isoniazid.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Isoniazid.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Isoniazid.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Isoniazid.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Isoniazid.
Disulfiram The risk or severity of adverse effects can be increased when Disulfiram is combined with Isoniazid.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Isoniazid.
Itraconazole The serum concentration of Itraconazole can be decreased when it is combined with Isoniazid.
Levodopa The therapeutic efficacy of Levodopa can be decreased when used in combination with Isoniazid.
Ketoconazole The serum concentration of Ketoconazole can be decreased when it is combined with Isoniazid.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Isoniazid.
Mirtazapine Isoniazid may increase the serotonergic activities of Mirtazapine.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Isoniazid.
Methylene blue Isoniazid may increase the serotonergic activities of Methylene blue.
Pantoprazole The metabolism of Pantoprazole can be decreased when combined with Isoniazid.
Pentobarbital The metabolism of Pentobarbital can be decreased when combined with Isoniazid.
Methadone The metabolism of Methadone can be decreased when combined with Isoniazid.

Target Protein

Catalase-peroxidase katG
Enoyl-[acyl-carrier-protein] reductase [NADH] inhA
Cytochrome P450 2C8 CYP2C8
Cytochrome P450 1A2 CYP1A2
Cytochrome P450 3A4 CYP3A4
Cytochrome P450 2C19 CYP2C19
Dihydrofolate reductase folA

Referensi & Sumber

Synthesis reference: Costin Rentzea, Albrecht Harreus, Eberhard Ammermann, Gisela Lorenz, "Oxalyl hydrazide-hydroxamic acid derivatives, their preparation and their use as fungicides." U.S. Patent US5399589, issued November, 1969.

Contoh Produk & Brand

Produk: 112 • International brands: 7
Produk
  • Dom-isoniazid 300mg Tablets
    Tablet • 300 mg • Oral • Canada • Generic • Approved
  • IsonaRif
    Capsule • 50 mg/5mL • Oral • US • Generic • Approved
  • Isoniazid
    Tablet • 300 mg/1 • Oral • US • Generic • Approved
  • Isoniazid
    Tablet • 300 mg/1 • Oral • US • Generic • Approved
  • Isoniazid
    Tablet • 300 mg/1 • Oral • US • Generic • Approved
  • Isoniazid
    Tablet • 300 mg/1 • Oral • US • Generic • Approved
  • Isoniazid
    Tablet • 300 mg/1 • Oral • US • Generic • Approved
  • Isoniazid
    Tablet • 100 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 112 produk.
International Brands
  • Nicozid — Piam
  • Nidrazid — Zentiva
  • Nydrazid — Sandoz
  • Rimicid — Sopharma
  • Rimifon — Roche
  • Servizid — Novartis
  • Tibinide — Meda

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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