Peringatan Keamanan

Mesalazine caused no increase in the incidence of neoplastic lesions over controls in a two-year study of Wistar rats fed up to 320 mg/kg/day of mesalazine admixed with diet (about 1.7 times the recommended human intra-rectal dose of CANASA, based on body
surface area). Mesalazine was not mutagenic in the Ames test, the mouse lymphoma cell (TK+/-) forward mutation test, or the mouse micronucleus test. No effects on fertility or reproductive performance of the male and female rats were observed at oral mesalamine doses up to 320 mg/kg/day (about 1.7 times the recommended human intra-rectal dose of mesalazine, based on body surface area).L36280

Mesalazine is an aminosalicylate, and symptoms of salicylate toxicity include nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe salicylate intoxication may lead to electrolyte and blood pH imbalance and potentially to other organ involvement (e.g., renal and liver). There is no specific antidote for mesalamine overdose; however, conventional therapy for salicylate toxicity may be beneficial in the event of acute
overdosage and may include gastrointestinal tract decontamination to prevent further absorption. Correct fluid and electrolyte imbalance by the administration of appropriate intravenous therapy and maintain adequate renal function.L36230

Mesalazine is known to be substantially excreted by the kidney, and the risk of adverse reactions may be greater in patients with impaired renal function. Evaluate renal function in all patients prior to initiation and periodically while on Asacol HD therapy. Monitor patients with known renal impairment or a history of renal disease or taking nephrotoxic drugs for decreased renal function and mesalamine-related adverse reactions.L36230

Mesalazine

DB00244

small molecule approved

Deskripsi

An anti-inflammatory agent, structurally related to the salicylates and non-steroidal anti-inflammatory drugs like acetylsalicylic acid, which is active in inflammatory bowel disease A174022. Although demonstrably effective in treating and maintaining remission for ulcerative colitis, mesalazine has historically faced a number of issues regarding its lack of stability as a pharmaceutical agent A174019. Throughout the late seventies and the eighties, important research initiatives developed stable mesalazine formulations like the eudragit-S coating of Asacol brand mesalazine and the Pentasa brand's encapsulation of mesalazine within microgranules A174019. In the present day, contemporary research regarding novel methods to stabilize mesalazine continues and interest in the agent's capacity to decrease inflammatory activity and subsequently potentially reduce the risk of colorectal cancer in conditions like ulcerative colitis is maintained.A174019,A174022

Struktur Molekul 2D

Berat 153.1354
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) For the delayed-release formulation, after intravenous administration, the elimination half-life of mesalamine is reported to be approximately 40 minutes. After oral dosing, the median terminal half life values for mesalamine are usually about 25 hours, but are variable, ranging from 1.5 to 296 hours. There is a large inter-subject and intra-subject variability in the plasma concentrations of mesalamine and N-acetyl-5-aminosalicylic acid and in their terminal half-lives following the administration of mesalazine.[L36275] For the extended-release formulation, following single and multiple doses of mesalazine, the mean half-lives were 9 to 10 hours for 5-ASA, and 12 to 14 hours for N-Ac-5-ASA.[L44196] The mean elimination half-life was 5 hours (CV=73%) for 5-ASA and 5 hours (CV=63%) for N-acetyl-5-ASA in patients taking 500 mg mesalazine as a rectal suppository every 8 hours for 6 days.[L36280] For the rectal enema suspension formulation, the elimination half-life was 0.5 to 1.5 hours for 5-ASA and 5 to 10 hours for N-acetyl-5-ASA.[L40978]
Volume Distribusi For the extended-release formulation, mesalazine has a Vd of 18 L, confirming minimal extravascular penetration of systemically available drug.[L44201] For the delayed-release formulation, the apparent volume of distribution was estimated to be 4.8 L.[L44206]
Klirens (Clearance) The mean (SD) renal clearance in L/h for mesalazine following the single dose administration of mesalazine delayed-release tablets 4.8g under fasting conditions to young and elderly subjects were documented as 2.05 ± 1.33 in young subjects aged 18 to 35 years old, 2.04 ± 1.16 in elderly subjects aged 65 to 75 years old and 2.13 ± 1.20 in elderly subjects older than 75 years.[L40848]

Absorpsi

Depending on the formulation administered, prescribing information for orally administered delayed-released tablets of 2.4g or 4.8g of mesalazine given once daily for 14 days to healthy volunteers was to found to be about 21% to 22% of the administered dose FDA Label while prescribing information for an orally administered controlled-release capsule formulation suggests 20% to 30% of the mesalazine in the formulation is absorbed.F3001 In contrast, when mesalamine is administered orally as an unformulated 1-g aqueous suspension, mesalazine is approximately 80% absorbed.F3001

Metabolisme

Mesalazine is metabolized both pre-systemically by the intestinal mucosa and systemically in the liver to N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA) principally by NAT-1. Some acetylation also occurs through the action of colonic bacteria.L5107,L44196

Rute Eliminasi

Elimination of mesalazine is mainly via the renal route following metabolism to N-acetyl-5-aminosalicylic acid (acetylation) L40848. However, there is also limited excretion of the parent mesalazine drug in the urine.L40848 After the oral administration of the extended-release formulation of mesalazine, of the approximately 21% to 22% of the drug absorbed, less than 8% of the dose was excreted unchanged in the urine after 24 hours, compared with greater than 13% for N-acetyl-5-aminosalicylic acid.L40848 When given the controlled-release formulation, about 130 mg free mesalazine was recovered in the feces following a single 1-g dose, which was comparable to the 140 mg of mesalazine recovered from the molar equivalent sulfasalazine tablet dose of 2.5 g F3001]. Elimination of free mesalazine and salicylates in feces increased proportionately with the dose given. N-acetylmesalazine was the primary compound excreted in the urine (19% to 30%) following the controlled-release dosing.F3001 In patients with ulcerative proctitis treated with mesalamine 500 mg as a rectal suppository every 8 hours for 6 days, 12% or less of the dose was eliminated in urine as unchanged 5-ASA and 8% to 77% was eliminated as N-acetyl-5-ASA following the initial dose. At steady state, 11% or less of the dose was eliminated in the urine as unchanged 5-ASA and 3% to 35% was eliminated as N-acetyl-5-ASA.L36280

Interaksi Makanan

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

Interaksi Obat

1513 Data
Amlodipine Mesalazine may decrease the antihypertensive activities of Amlodipine.
Phentermine The risk or severity of hypertension can be increased when Phentermine is combined with Mesalazine.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Mesalazine.
Eletriptan The risk or severity of hypertension can be increased when Eletriptan is combined with Mesalazine.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Mesalazine.
Ziprasidone The risk or severity of hypertension can be increased when Mesalazine is combined with Ziprasidone.
Methysergide The risk or severity of hypertension can be increased when Mesalazine is combined with Methysergide.
Cabergoline The risk or severity of hypertension can be increased when Mesalazine is combined with Cabergoline.
Zolmitriptan The risk or severity of hypertension can be increased when Mesalazine is combined with Zolmitriptan.
Dihydroergotamine The risk or severity of hypertension can be increased when Mesalazine is combined with Dihydroergotamine.
Methylergometrine The risk or severity of hypertension can be increased when Mesalazine is combined with Methylergometrine.
Norepinephrine The risk or severity of hypertension can be increased when Mesalazine is combined with Norepinephrine.
Mirtazapine The risk or severity of hypertension can be increased when Mesalazine is combined with Mirtazapine.
Phenylephrine The risk or severity of hypertension can be increased when Mesalazine is combined with Phenylephrine.
Phenylpropanolamine The risk or severity of hypertension can be increased when Mesalazine is combined with Phenylpropanolamine.
Promazine The risk or severity of hypertension can be increased when Mesalazine is combined with Promazine.
Droperidol The risk or severity of hypertension can be increased when Mesalazine is combined with Droperidol.
Doxapram The risk or severity of hypertension can be increased when Mesalazine is combined with Doxapram.
Atropine The risk or severity of hypertension can be increased when Mesalazine is combined with Atropine.
Lisuride The risk or severity of hypertension can be increased when Mesalazine is combined with Lisuride.
Linezolid The risk or severity of hypertension can be increased when Mesalazine is combined with Linezolid.
Metaraminol The risk or severity of hypertension can be increased when Mesalazine is combined with Metaraminol.
Furazolidone The risk or severity of hypertension can be increased when Mesalazine is combined with Furazolidone.
Epinephrine The risk or severity of hypertension can be increased when Mesalazine is combined with Epinephrine.
Thioridazine The risk or severity of hypertension can be increased when Mesalazine is combined with Thioridazine.
Ergotamine The risk or severity of hypertension can be increased when Mesalazine is combined with Ergotamine.
Nicergoline The risk or severity of hypertension can be increased when Mesalazine is combined with Nicergoline.
Sufentanil The risk or severity of hypertension can be increased when Mesalazine is combined with Sufentanil.
Methoxamine The risk or severity of hypertension can be increased when Mesalazine is combined with Methoxamine.
Risperidone The risk or severity of hypertension can be increased when Mesalazine is combined with Risperidone.
Tranylcypromine The risk or severity of hypertension can be increased when Mesalazine is combined with Tranylcypromine.
Isoflurane The risk or severity of hypertension can be increased when Mesalazine is combined with Isoflurane.
Propiomazine The risk or severity of hypertension can be increased when Mesalazine is combined with Propiomazine.
Alfentanil The risk or severity of hypertension can be increased when Mesalazine is combined with Alfentanil.
Minaprine The risk or severity of hypertension can be increased when Mesalazine is combined with Minaprine.
Orciprenaline The risk or severity of hypertension can be increased when Mesalazine is combined with Orciprenaline.
Propofol The risk or severity of hypertension can be increased when Mesalazine is combined with Propofol.
Phenmetrazine The risk or severity of hypertension can be increased when Mesalazine is combined with Phenmetrazine.
Trifluoperazine The risk or severity of hypertension can be increased when Mesalazine is combined with Trifluoperazine.
Pseudoephedrine The risk or severity of hypertension can be increased when Mesalazine is combined with Pseudoephedrine.
Benzphetamine The risk or severity of hypertension can be increased when Mesalazine is combined with Benzphetamine.
Ritodrine The risk or severity of hypertension can be increased when Mesalazine is combined with Ritodrine.
Flupentixol The risk or severity of hypertension can be increased when Mesalazine is combined with Flupentixol.
Remifentanil The risk or severity of hypertension can be increased when Mesalazine is combined with Remifentanil.
Bitolterol The risk or severity of hypertension can be increased when Mesalazine is combined with Bitolterol.
Oxymetazoline The risk or severity of hypertension can be increased when Mesalazine is combined with Oxymetazoline.
Diethylpropion The risk or severity of hypertension can be increased when Mesalazine is combined with Diethylpropion.
Salmeterol The risk or severity of hypertension can be increased when Mesalazine is combined with Salmeterol.
Naratriptan The risk or severity of hypertension can be increased when Mesalazine is combined with Naratriptan.
Formoterol The risk or severity of hypertension can be increased when Mesalazine is combined with Formoterol.
Frovatriptan The risk or severity of hypertension can be increased when Mesalazine is combined with Frovatriptan.
Methoxyflurane The risk or severity of hypertension can be increased when Mesalazine is combined with Methoxyflurane.
Selegiline The risk or severity of hypertension can be increased when Mesalazine is combined with Selegiline.
Ergoloid mesylate The risk or severity of hypertension can be increased when Mesalazine is combined with Ergoloid mesylate.
Isoprenaline The risk or severity of hypertension can be increased when Mesalazine is combined with Isoprenaline.
Arbutamine The risk or severity of hypertension can be increased when Mesalazine is combined with Arbutamine.
Dutasteride The risk or severity of hypertension can be increased when Mesalazine is combined with Dutasteride.
Halothane The risk or severity of hypertension can be increased when Mesalazine is combined with Halothane.
Moclobemide The risk or severity of hypertension can be increased when Mesalazine is combined with Moclobemide.
Pergolide The risk or severity of hypertension can be increased when Mesalazine is combined with Pergolide.
Desflurane The risk or severity of hypertension can be increased when Mesalazine is combined with Desflurane.
Finasteride The risk or severity of hypertension can be increased when Mesalazine is combined with Finasteride.
Aripiprazole The risk or severity of hypertension can be increased when Mesalazine is combined with Aripiprazole.
Isocarboxazid The risk or severity of hypertension can be increased when Mesalazine is combined with Isocarboxazid.
Ergometrine The risk or severity of hypertension can be increased when Mesalazine is combined with Ergometrine.
Lisdexamfetamine The risk or severity of hypertension can be increased when Mesalazine is combined with Lisdexamfetamine.
Fenoterol The risk or severity of hypertension can be increased when Mesalazine is combined with Fenoterol.
Pirbuterol The risk or severity of hypertension can be increased when Mesalazine is combined with Pirbuterol.
Ephedra sinica root The risk or severity of hypertension can be increased when Mesalazine is combined with Ephedra sinica root.
Ephedrine The risk or severity of hypertension can be increased when Mesalazine is combined with Ephedrine.
Mephentermine The risk or severity of hypertension can be increased when Mesalazine is combined with Mephentermine.
Procaterol The risk or severity of hypertension can be increased when Mesalazine is combined with Procaterol.
Yohimbine The risk or severity of hypertension can be increased when Mesalazine is combined with Yohimbine.
Methotrimeprazine The risk or severity of hypertension can be increased when Mesalazine is combined with Methotrimeprazine.
Clenbuterol The risk or severity of hypertension can be increased when Mesalazine is combined with Clenbuterol.
Bambuterol The risk or severity of hypertension can be increased when Mesalazine is combined with Bambuterol.
MMDA The risk or severity of hypertension can be increased when Mesalazine is combined with MMDA.
Midomafetamine The risk or severity of hypertension can be increased when Mesalazine is combined with Midomafetamine.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when Mesalazine is combined with 2,5-Dimethoxy-4-ethylamphetamine.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when Mesalazine is combined with 4-Methoxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when Mesalazine is combined with 4-Bromo-2,5-dimethoxyamphetamine.
Tenamfetamine The risk or severity of hypertension can be increased when Mesalazine is combined with Tenamfetamine.
Chlorphentermine The risk or severity of hypertension can be increased when Mesalazine is combined with Chlorphentermine.
Dextroamphetamine The risk or severity of hypertension can be increased when Mesalazine is combined with Dextroamphetamine.
Phendimetrazine The risk or severity of hypertension can be increased when Mesalazine is combined with Phendimetrazine.
Solifenacin The risk or severity of hypertension can be increased when Mesalazine is combined with Solifenacin.
Periciazine The risk or severity of hypertension can be increased when Mesalazine is combined with Periciazine.
Acepromazine The risk or severity of hypertension can be increased when Mesalazine is combined with Acepromazine.
Thioproperazine The risk or severity of hypertension can be increased when Mesalazine is combined with Thioproperazine.
Zuclopenthixol The risk or severity of hypertension can be increased when Mesalazine is combined with Zuclopenthixol.
Epicaptopril The risk or severity of hypertension can be increased when Mesalazine is combined with Epicaptopril.
Clorgiline The risk or severity of hypertension can be increased when Mesalazine is combined with Clorgiline.
1-benzylimidazole The risk or severity of hypertension can be increased when Mesalazine is combined with 1-benzylimidazole.
Iproniazid The risk or severity of hypertension can be increased when Mesalazine is combined with Iproniazid.
Nialamide The risk or severity of hypertension can be increased when Mesalazine is combined with Nialamide.
Lysergic acid diethylamide The risk or severity of hypertension can be increased when Mesalazine is combined with Lysergic acid diethylamide.
Dronedarone The risk or severity of hypertension can be increased when Mesalazine is combined with Dronedarone.
Flibanserin The risk or severity of hypertension can be increased when Mesalazine is combined with Flibanserin.
Iloperidone The risk or severity of hypertension can be increased when Mesalazine is combined with Iloperidone.
Indacaterol The risk or severity of hypertension can be increased when Mesalazine is combined with Indacaterol.

Target Protein

Prostaglandin G/H synthase 2 PTGS2
Prostaglandin G/H synthase 1 PTGS1
Polyunsaturated fatty acid 5-lipoxygenase ALOX5
Peroxisome proliferator-activated receptor gamma PPARG
Inhibitor of nuclear factor kappa-B kinase subunit alpha CHUK
Inhibitor of nuclear factor kappa-B kinase subunit beta IKBKB
Nitric oxide synthase, inducible NOS2

Referensi & Sumber

Synthesis reference: Thomas M. Parkinson, Joseph P. Brown, Robert E. Wingard, Jr., "Pharmaceutical preparations containing a polymeric agent for releasing 5-aminosalicylic acid or its salts into the gastrointestinal tract." U.S. Patent US4298595, issued January, 1975.
Artikel (PubMed)
  • PMID: 24369317
    Mayberry J: The history of 5-ASA compounds and their use in ulcerative colitis--trailblazing discoveries in gastroenterology. J Gastrointestin Liver Dis. 2013 Dec;22(4):375-7.
  • PMID: 24005861
    Stolfi C, De Simone V, Pallone F, Monteleone G: Mechanisms of action of non-steroidal anti-inflammatory drugs (NSAIDs) and mesalazine in the chemoprevention of colorectal cancer. Int J Mol Sci. 2013 Sep 3;14(9):17972-85. doi: 10.3390/ijms140917972.
  • PMID: 11151876
    Bantel H, Berg C, Vieth M, Stolte M, Kruis W, Schulze-Osthoff K: Mesalazine inhibits activation of transcription factor NF-kappaB in inflamed mucosa of patients with ulcerative colitis. Am J Gastroenterol. 2000 Dec;95(12):3452-7.
  • PMID: 12950415
    Allgayer H: Review article: mechanisms of action of mesalazine in preventing colorectal carcinoma in inflammatory bowel disease. Aliment Pharmacol Ther. 2003 Sep;18 Suppl 2:10-4.
  • PMID: 11054378
    Weber CK, Liptay S, Wirth T, Adler G, Schmid RM: Suppression of NF-kappaB activity by sulfasalazine is mediated by direct inhibition of IkappaB kinases alpha and beta. Gastroenterology. 2000 Nov;119(5):1209-18.
  • PMID: 18544567
    Schwab M, Reynders V, Loitsch S, Shastri YM, Steinhilber D, Schroder O, Stein J: PPARgamma is involved in mesalazine-mediated induction of apoptosis and inhibition of cell growth in colon cancer cells. Carcinogenesis. 2008 Jul;29(7):1407-14. doi: 10.1093/carcin/bgn118. Epub 2008 Jun 9.
  • PMID: 18077625
    Linard C, Gremy O, Benderitter M: Reduction of peroxisome proliferation-activated receptor gamma expression by gamma-irradiation as a mechanism contributing to inflammatory response in rat colon: modulation by the 5-aminosalicylic acid agonist. J Pharmacol Exp Ther. 2008 Mar;324(3):911-20. Epub 2007 Dec 12.
  • PMID: 16939423
    Desreumaux P, Ghosh S: Review article: mode of action and delivery of 5-aminosalicylic acid - new evidence. Aliment Pharmacol Ther. 2006 Sep;24 Suppl 1:2-9.
Menampilkan 8 dari 11 artikel.

Contoh Produk & Brand

Produk: 154 • International brands: 5
Produk
  • 5-asa
    Tablet, delayed release • 400 mg • Oral • Canada • Approved
  • Apriso
    Capsule, extended release • 375 mg/1 • Oral • US • Approved
  • Apriso
    Capsule, extended release • 375 mg/1 • Oral • US • Approved
  • Apriso
    Capsule, extended release • 375 mg/1 • Oral • US • Approved
  • Asacol
    Tablet, delayed release • 400 mg/1 • Oral • US • Approved
  • Asacol
    Tablet, delayed release • 400 mg/1 • Oral • US • Approved
  • Asacol
    Tablet, delayed release • 400 mg/1 • Oral • US • Approved
  • Asacol
    Tablet, delayed release • 400 mg/1 • Oral • US • Approved
Menampilkan 8 dari 154 produk.
International Brands
  • Asacolitin
  • Claversal
  • Fisalamine
  • Iialda
  • Lixacol

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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