Peringatan Keamanan

LD50=6800 mg/kg (Orally in mice) L2806.

Sulfonamide-induced hypersensitivity reactions, although uncommon, can be severe. They can include rare life-threatening cutaneous reactions such as erythema multiform (Stevens-Johnson syndrome) and toxic epidermal necrolysis. Crystalluria may result in dysuria, renal colic, haematuria and acute renal obstruction L2803.

Other infrequent reactions include granulocytopenia, agranulocytosis, aplastic anemia, thrombocytopenic purpura and toxic hepatitis. Rarely, hemolysis may occur in individuals deficient in glucose-6-phosphate dehydrogenase L2803.

The severe or irreversible adverse effects of sulfisoxazole, which give rise to more complications which may include: nephrotoxicity, blood dyscrasias, interstitial nephritis, hematuria, crystalluria, oliguria, anuria, lumbar pain, and tubular necrosis L2803.

The symptomatic adverse reactions produced by sulfisoxazole are more or less tolerable and if severe, may be treated symptomatically, these include anorexia, diarrhea, rashes, pruritus, nausea and vomiting, hypersensitivity reactions, Photosensitivity reactions L2793.

Overdosage: Continuously forced diuresis may be beneficial and an alkaline urine should be initiated L2793.

Acetyl sulfisoxazole

DB14033

small molecule approved vet_approved

Deskripsi

Sulfisoxazole acetyl is an ester of sulfisoxazole, a broad-spectrum sulfanilamide and a synthetic analog of para-aminobenzoic acid (PABA) with antibacterial activity. Sulfisoxazole acetyl competes with PABA for the bacterial enzyme, dihydropteroate synthase, preventing the incorporation of PABA into dihydrofolic acid, which is the precursor of folic acid. This process causes an inhibition of bacterial folic acid synthesis and de novo synthesis of purines and pyrimidines, resulting in cell growth arrest and cell death L2788.

It is often combined with erythromycin to treat acute otitis media caused by the bacteria, haemophilus influenzae L2790.

Struktur Molekul 2D

Berat 309.34
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The serum half-life is 10 -12 hours [L2793].
Volume Distribusi The sulfonamides are widely distributed throughout all body tissues [L2793]. It readily crosses the placental barrier and enters into fetal circulation and also crosses the blood-brain barrier. In healthy subjects, cerebrospinal fluid concentrations of sulfisoxazole vary; in patients with meningitis, however, concentrations of free drug in cerebrospinal fluid as high as 94 mcg/mL have been reported [L2804]. In a pharmacokinetic study, the apparent volume of distribution for total drug was 10.9 +/- 2.0 liters and 136 +/- 36 liters for the unbound drug, indicating that sulfisoxazole is primarily distributed extracellularly [L2800].
Klirens (Clearance) The clearance of sulfisoxazole is 18.7 +/- 3.9 ml/min for total drug and 232 +/- 64 ml/min for the unbound drug [L2800].

Absorpsi

Readily absorbed from the gastrointestinal tract L2793. In a pharmacokinetic study, the adjustments for variable renal clearances between oral and intravenous administration and using the unbound plasma concentrations, the bioavailability for an oral dose of sulfisoxazole was found to be 0.95 +/- 0.04 L2800.

Metabolisme

Sulfisoxazole acetyl is a prodrug of sulfisoxazole. The acetyl group is added to make the drug poorly water-soluble and is hydrolyzed in vivo to the active drug L2804, L2807. N1-acetyl sulfisoxazole is metabolized to sulfisoxazole by digestive enzymes in the gastrointestinal tract and is absorbed as sulfisoxazole. This enzymatic splitting is thought to be responsible for slower absorption and lower peak blood concentrations are achieved after administration of an equal oral dose of sulfisoxazole. With sustained administration of acetyl sulfisoxazole, blood concentrations approximate those of sulfisoxazole. Following a single 4 gram dose of acetyl sulfisoxazole to healthy volunteers, maximum plasma concentrations of sulfisoxazole ranged from 122 to 282 mcg/mL (mean, 181 mcg/mL) for the pediatric suspension and occurred between 2 and 6 hours postadministration of sulfisoxazole, in a pharmacokinetic study L2804.

Rute Eliminasi

The mean urinary excretion recovery following oral administration of sulfisoxazole is 97% within 48 hours, of which 52% is the parent drug, and the remaining as the N4-acetylated metabolite. It is excreted in human milk L2793. Sulfisoxazole and its acetylated metabolites are excreted primarily by the kidneys through glomerular filtration L2804.

Interaksi Obat

351 Data
Nicotine The risk or severity of adverse effects can be increased when Acetyl sulfisoxazole is combined with Nicotine.
Mecamylamine The risk or severity of adverse effects can be increased when Acetyl sulfisoxazole is combined with Mecamylamine.
Pentolinium The risk or severity of adverse effects can be increased when Acetyl sulfisoxazole is combined with Pentolinium.
Trimethaphan The risk or severity of adverse effects can be increased when Acetyl sulfisoxazole is combined with Trimethaphan.
Hexamethonium The risk or severity of adverse effects can be increased when Acetyl sulfisoxazole is combined with Hexamethonium.
Cyclopentamine The risk or severity of adverse effects can be increased when Acetyl sulfisoxazole is combined with Cyclopentamine.
Methotrexate The protein binding of Methotrexate can be increased when combined with Acetyl sulfisoxazole.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Acetyl sulfisoxazole.
Dexketoprofen The risk or severity of adverse effects can be increased when Dexketoprofen is combined with Acetyl sulfisoxazole.
Ketoprofen The risk or severity of adverse effects can be increased when Ketoprofen is combined with Acetyl sulfisoxazole.
Cyclosporine The risk or severity of renal failure can be increased when Acetyl sulfisoxazole is combined with Cyclosporine.
Methenamine Methenamine can cause a decrease in the absorption of Acetyl sulfisoxazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Acetyl sulfisoxazole.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Acetyl sulfisoxazole.
Insulin human The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin human.
Insulin lispro The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin lispro.
Insulin glargine The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin glargine.
Insulin pork The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin pork.
Troglitazone The therapeutic efficacy of Troglitazone can be increased when used in combination with Acetyl sulfisoxazole.
Glimepiride The therapeutic efficacy of Glimepiride can be increased when used in combination with Acetyl sulfisoxazole.
Sulfisoxazole The therapeutic efficacy of Sulfisoxazole can be increased when used in combination with Acetyl sulfisoxazole.
Disopyramide The therapeutic efficacy of Disopyramide can be increased when used in combination with Acetyl sulfisoxazole.
Acarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Acetyl sulfisoxazole.
Metformin The therapeutic efficacy of Metformin can be increased when used in combination with Acetyl sulfisoxazole.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be increased when used in combination with Acetyl sulfisoxazole.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Acetyl sulfisoxazole.
Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Acetyl sulfisoxazole.
Quinine The therapeutic efficacy of Quinine can be increased when used in combination with Acetyl sulfisoxazole.
Miglitol The therapeutic efficacy of Miglitol can be increased when used in combination with Acetyl sulfisoxazole.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Acetyl sulfisoxazole.
Nateglinide The therapeutic efficacy of Nateglinide can be increased when used in combination with Acetyl sulfisoxazole.
Pentamidine The therapeutic efficacy of Pentamidine can be increased when used in combination with Acetyl sulfisoxazole.
Mifepristone The therapeutic efficacy of Mifepristone can be increased when used in combination with Acetyl sulfisoxazole.
Tolazamide The therapeutic efficacy of Tolazamide can be increased when used in combination with Acetyl sulfisoxazole.
Repaglinide The therapeutic efficacy of Repaglinide can be increased when used in combination with Acetyl sulfisoxazole.
Phenformin The therapeutic efficacy of Phenformin can be increased when used in combination with Acetyl sulfisoxazole.
Sulfamethoxazole The therapeutic efficacy of Sulfamethoxazole can be increased when used in combination with Acetyl sulfisoxazole.
Glyburide The therapeutic efficacy of Glyburide can be increased when used in combination with Acetyl sulfisoxazole.
Glipizide The therapeutic efficacy of Glipizide can be increased when used in combination with Acetyl sulfisoxazole.
Gliclazide The therapeutic efficacy of Gliclazide can be increased when used in combination with Acetyl sulfisoxazole.
Tolbutamide The therapeutic efficacy of Tolbutamide can be increased when used in combination with Acetyl sulfisoxazole.
Pioglitazone The therapeutic efficacy of Pioglitazone can be increased when used in combination with Acetyl sulfisoxazole.
Bromocriptine The therapeutic efficacy of Bromocriptine can be increased when used in combination with Acetyl sulfisoxazole.
Gliquidone The therapeutic efficacy of Gliquidone can be increased when used in combination with Acetyl sulfisoxazole.
Mitiglinide The therapeutic efficacy of Mitiglinide can be increased when used in combination with Acetyl sulfisoxazole.
Sitagliptin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Acetyl sulfisoxazole.
Sunitinib The therapeutic efficacy of Sunitinib can be increased when used in combination with Acetyl sulfisoxazole.
Exenatide The therapeutic efficacy of Exenatide can be increased when used in combination with Acetyl sulfisoxazole.
Mecasermin The therapeutic efficacy of Mecasermin can be increased when used in combination with Acetyl sulfisoxazole.
Pramlintide The therapeutic efficacy of Pramlintide can be increased when used in combination with Acetyl sulfisoxazole.
Glisoxepide The therapeutic efficacy of Glisoxepide can be increased when used in combination with Acetyl sulfisoxazole.
Insulin aspart The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin aspart.
Insulin detemir The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin detemir.
Insulin glulisine The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin glulisine.
Glymidine The therapeutic efficacy of Glymidine can be increased when used in combination with Acetyl sulfisoxazole.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be increased when used in combination with Acetyl sulfisoxazole.
Buformin The therapeutic efficacy of Buformin can be increased when used in combination with Acetyl sulfisoxazole.
Vildagliptin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Acetyl sulfisoxazole.
Voglibose The therapeutic efficacy of Voglibose can be increased when used in combination with Acetyl sulfisoxazole.
NN344 The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with NN344.
AMG-222 The therapeutic efficacy of AMG-222 can be increased when used in combination with Acetyl sulfisoxazole.
Bisegliptin The therapeutic efficacy of Bisegliptin can be increased when used in combination with Acetyl sulfisoxazole.
Alogliptin The therapeutic efficacy of Alogliptin can be increased when used in combination with Acetyl sulfisoxazole.
Dapagliflozin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Acetyl sulfisoxazole.
Saxagliptin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Acetyl sulfisoxazole.
Liraglutide The therapeutic efficacy of Liraglutide can be increased when used in combination with Acetyl sulfisoxazole.
Gosogliptin The therapeutic efficacy of Gosogliptin can be increased when used in combination with Acetyl sulfisoxazole.
Linagliptin The therapeutic efficacy of Linagliptin can be increased when used in combination with Acetyl sulfisoxazole.
Canagliflozin The therapeutic efficacy of Canagliflozin can be increased when used in combination with Acetyl sulfisoxazole.
Glibornuride The therapeutic efficacy of Glibornuride can be increased when used in combination with Acetyl sulfisoxazole.
Benfluorex The therapeutic efficacy of Benfluorex can be increased when used in combination with Acetyl sulfisoxazole.
Empagliflozin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Acetyl sulfisoxazole.
Albiglutide The therapeutic efficacy of Albiglutide can be increased when used in combination with Acetyl sulfisoxazole.
Dulaglutide The therapeutic efficacy of Dulaglutide can be increased when used in combination with Acetyl sulfisoxazole.
Lobeglitazone The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Acetyl sulfisoxazole.
Netoglitazone The therapeutic efficacy of Netoglitazone can be increased when used in combination with Acetyl sulfisoxazole.
Rivoglitazone The therapeutic efficacy of Rivoglitazone can be increased when used in combination with Acetyl sulfisoxazole.
Ciglitazone The therapeutic efficacy of Ciglitazone can be increased when used in combination with Acetyl sulfisoxazole.
Lixisenatide The therapeutic efficacy of Lixisenatide can be increased when used in combination with Acetyl sulfisoxazole.
Insulin beef The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin beef.
Insulin degludec The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin degludec.
Insulin peglispro The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin peglispro.
Insulin tregopil The risk or severity of hypoglycemia can be increased when Acetyl sulfisoxazole is combined with Insulin tregopil.
Ipragliflozin The therapeutic efficacy of Ipragliflozin can be increased when used in combination with Acetyl sulfisoxazole.
Dutogliptin The therapeutic efficacy of Dutogliptin can be increased when used in combination with Acetyl sulfisoxazole.
Allicin The therapeutic efficacy of Allicin can be increased when used in combination with Acetyl sulfisoxazole.
Tofogliflozin The therapeutic efficacy of Tofogliflozin can be increased when used in combination with Acetyl sulfisoxazole.
Ertugliflozin The therapeutic efficacy of Ertugliflozin can be increased when used in combination with Acetyl sulfisoxazole.
2,4-thiazolidinedione The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Acetyl sulfisoxazole.
Teneligliptin The therapeutic efficacy of Teneligliptin can be increased when used in combination with Acetyl sulfisoxazole.
Omarigliptin The therapeutic efficacy of Omarigliptin can be increased when used in combination with Acetyl sulfisoxazole.
Carmegliptin The therapeutic efficacy of Carmegliptin can be increased when used in combination with Acetyl sulfisoxazole.
Gemigliptin The therapeutic efficacy of Gemigliptin can be increased when used in combination with Acetyl sulfisoxazole.
Anagliptin The therapeutic efficacy of Anagliptin can be increased when used in combination with Acetyl sulfisoxazole.
Evogliptin The therapeutic efficacy of Evogliptin can be increased when used in combination with Acetyl sulfisoxazole.
Sotagliflozin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Acetyl sulfisoxazole.
Balaglitazone The therapeutic efficacy of Balaglitazone can be increased when used in combination with Acetyl sulfisoxazole.
Remogliflozin etabonate The therapeutic efficacy of Remogliflozin etabonate can be increased when used in combination with Acetyl sulfisoxazole.
Carbutamide The therapeutic efficacy of Carbutamide can be increased when used in combination with Acetyl sulfisoxazole.
Guar gum The therapeutic efficacy of Guar gum can be increased when used in combination with Acetyl sulfisoxazole.

Target Protein

Dihydropteroate synthase folP

Referensi & Sumber

Artikel (PubMed)
  • PMID: 6101167
    Suber RL, Lee C, Torosian G, Edds GT: Pharmacokinetics of sulfisoxazole compared in humans and two monogastric animal species. J Pharm Sci. 1981 Sep;70(9):981-4.

Contoh Produk & Brand

Produk: 6 • International brands: 0
Produk
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