Peringatan Keamanan

The pharmacological activity of acemetacin causes blockage of prostaglandin synthesis. Prostaglandin is one of the mediators of renal blood flow and glomerular filtration thus, acemetacin causes a decreased renal function, transient renal insufficiency, interstitial nephritis and papillary necrosis especially in elderly patients, patients with congestive heart failure, hepatic cirrhosis and impaired renal function.T53

Acemetacin

DB13783

small molecule approved investigational

Deskripsi

Acemetacin is a carboxymethyl ester of indometacin. It is a potent non-steroidal anti-inflammatory drug, derived from the indol-3-acetic acid, whose activity is thought to be mainly through its active metabolite indomethacin.A31352 In clinical trials, acemetacin exhibits a better gastric tolerability compared to its active metabolite indometacin.T50 It was developed by E. Merck and Company in Germany as an attempt to provide a safer drug but other than the amelioration on the gastrointestinal effects, the metabolism of acetamicin led to the formation of indomethacin and it kept the same side effects.T51

Struktur Molekul 2D

Berat 415.83
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of acemetacin after steady-state is 4.5 hours.[A31356]
Volume Distribusi The apparent volume of distribution of acemetacin is in a range of 0.5-0.7 L/kg.[T53]
Klirens (Clearance) Intravenous administration of acemetacin in healthy subjects reported a clearance rate of 4.59 ml min/kg.[A31357]

Absorpsi

After 8 days of oral administration twice daily of acemetacin there was an age-dependant Cmax of 276.8 ng/ml in elderly compared to 187 ng/ml for younger individuals. There was also a Tmax of 2.5 h and AUC in a range of 483-712 ng h/ml.A31355 The bioavailability of acemetacin after repeated doses is aproximately 66% in plasma and 64% in urine.A31356

Metabolisme

Acemetacin is highly metabolized and degraded by esterolytic cleavage to form its major and active metabolite indometacin. It presents other inactive metabolites made by reaction of O-demethylation, N-desacylation and part of them are also transformed by conjugation with glucuronic acid.T53

Rute Eliminasi

The elimination of acemetacin is divided in renal elimination that covers 40% of the complete administered dose and the restant 60% is excreted in feces.T53

Interaksi Obat

1444 Data
Amlodipine Acemetacin may decrease the antihypertensive activities of Amlodipine.
Phentermine The risk or severity of hypertension can be increased when Phentermine is combined with Acemetacin.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Acemetacin.
Eletriptan The risk or severity of hypertension can be increased when Eletriptan is combined with Acemetacin.
Isoetharine The risk or severity of hypertension can be increased when Isoetharine is combined with Acemetacin.
Ziprasidone The risk or severity of hypertension can be increased when Ziprasidone is combined with Acemetacin.
Methysergide The risk or severity of hypertension can be increased when Methysergide is combined with Acemetacin.
Cabergoline The risk or severity of hypertension can be increased when Cabergoline is combined with Acemetacin.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Acemetacin.
Dihydroergotamine The risk or severity of hypertension can be increased when Dihydroergotamine is combined with Acemetacin.
Methylergometrine The risk or severity of hypertension can be increased when Methylergometrine is combined with Acemetacin.
Norepinephrine The risk or severity of hypertension can be increased when Norepinephrine is combined with Acemetacin.
Mirtazapine The risk or severity of hypertension can be increased when Mirtazapine is combined with Acemetacin.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Acemetacin.
Phenylpropanolamine The risk or severity of hypertension can be increased when Phenylpropanolamine is combined with Acemetacin.
Promazine The risk or severity of hypertension can be increased when Promazine is combined with Acemetacin.
Droperidol The risk or severity of hypertension can be increased when Droperidol is combined with Acemetacin.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Acemetacin.
Atropine The risk or severity of hypertension can be increased when Atropine is combined with Acemetacin.
Lisuride The risk or severity of hypertension can be increased when Lisuride is combined with Acemetacin.
Linezolid The risk or severity of hypertension can be increased when Linezolid is combined with Acemetacin.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Acemetacin.
Furazolidone The risk or severity of hypertension can be increased when Furazolidone is combined with Acemetacin.
Epinephrine The risk or severity of hypertension can be increased when Epinephrine is combined with Acemetacin.
Thioridazine The risk or severity of hypertension can be increased when Thioridazine is combined with Acemetacin.
Ergotamine The risk or severity of hypertension can be increased when Ergotamine is combined with Acemetacin.
Nicergoline The risk or severity of hypertension can be increased when Nicergoline is combined with Acemetacin.
Sufentanil The risk or severity of hypertension can be increased when Sufentanil is combined with Acemetacin.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Acemetacin.
Risperidone The risk or severity of hypertension can be increased when Risperidone is combined with Acemetacin.
Tranylcypromine The risk or severity of hypertension can be increased when Tranylcypromine is combined with Acemetacin.
Isoflurane The risk or severity of hypertension can be increased when Isoflurane is combined with Acemetacin.
Propiomazine The risk or severity of hypertension can be increased when Propiomazine is combined with Acemetacin.
Alfentanil The risk or severity of hypertension can be increased when Alfentanil is combined with Acemetacin.
Minaprine The risk or severity of hypertension can be increased when Minaprine is combined with Acemetacin.
Orciprenaline The risk or severity of hypertension can be increased when Orciprenaline is combined with Acemetacin.
Propofol The risk or severity of hypertension can be increased when Propofol is combined with Acemetacin.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Acemetacin.
Trifluoperazine The risk or severity of hypertension can be increased when Trifluoperazine is combined with Acemetacin.
Pseudoephedrine The risk or severity of hypertension can be increased when Pseudoephedrine is combined with Acemetacin.
Benzphetamine The risk or severity of hypertension can be increased when Benzphetamine is combined with Acemetacin.
Ritodrine The risk or severity of hypertension can be increased when Ritodrine is combined with Acemetacin.
Flupentixol The risk or severity of hypertension can be increased when Flupentixol is combined with Acemetacin.
Remifentanil The risk or severity of hypertension can be increased when Remifentanil is combined with Acemetacin.
Bitolterol The risk or severity of hypertension can be increased when Bitolterol is combined with Acemetacin.
Oxymetazoline The risk or severity of hypertension can be increased when Oxymetazoline is combined with Acemetacin.
Diethylpropion The risk or severity of hypertension can be increased when Diethylpropion is combined with Acemetacin.
Salmeterol The risk or severity of hypertension can be increased when Salmeterol is combined with Acemetacin.
Naratriptan The risk or severity of hypertension can be increased when Naratriptan is combined with Acemetacin.
Formoterol The risk or severity of hypertension can be increased when Formoterol is combined with Acemetacin.
Frovatriptan The risk or severity of hypertension can be increased when Frovatriptan is combined with Acemetacin.
Methoxyflurane The risk or severity of hypertension can be increased when Methoxyflurane is combined with Acemetacin.
Selegiline The risk or severity of hypertension can be increased when Selegiline is combined with Acemetacin.
Ergoloid mesylate The risk or severity of hypertension can be increased when Ergoloid mesylate is combined with Acemetacin.
Isoprenaline The risk or severity of hypertension can be increased when Isoprenaline is combined with Acemetacin.
Arbutamine The risk or severity of hypertension can be increased when Arbutamine is combined with Acemetacin.
Dutasteride The risk or severity of hypertension can be increased when Dutasteride is combined with Acemetacin.
Halothane The risk or severity of hypertension can be increased when Halothane is combined with Acemetacin.
Moclobemide The risk or severity of hypertension can be increased when Moclobemide is combined with Acemetacin.
Pergolide The risk or severity of hypertension can be increased when Pergolide is combined with Acemetacin.
Desflurane The risk or severity of hypertension can be increased when Desflurane is combined with Acemetacin.
Bromocriptine The risk or severity of hypertension can be increased when Bromocriptine is combined with Acemetacin.
Finasteride The risk or severity of hypertension can be increased when Finasteride is combined with Acemetacin.
Aripiprazole The risk or severity of hypertension can be increased when Aripiprazole is combined with Acemetacin.
Isocarboxazid The risk or severity of hypertension can be increased when Isocarboxazid is combined with Acemetacin.
Ergometrine The risk or severity of hypertension can be increased when Ergometrine is combined with Acemetacin.
Lisdexamfetamine The risk or severity of hypertension can be increased when Lisdexamfetamine is combined with Acemetacin.
Fenoterol The risk or severity of hypertension can be increased when Fenoterol is combined with Acemetacin.
Pirbuterol The risk or severity of hypertension can be increased when Pirbuterol is combined with Acemetacin.
Ephedra sinica root The risk or severity of hypertension can be increased when Ephedra sinica root is combined with Acemetacin.
Ephedrine The risk or severity of hypertension can be increased when Ephedrine is combined with Acemetacin.
Mephentermine The risk or severity of hypertension can be increased when Mephentermine is combined with Acemetacin.
Procaterol The risk or severity of hypertension can be increased when Procaterol is combined with Acemetacin.
Yohimbine The risk or severity of hypertension can be increased when Yohimbine is combined with Acemetacin.
Methotrimeprazine The risk or severity of hypertension can be increased when Methotrimeprazine is combined with Acemetacin.
Clenbuterol The risk or severity of hypertension can be increased when Clenbuterol is combined with Acemetacin.
Bambuterol The risk or severity of hypertension can be increased when Bambuterol is combined with Acemetacin.
MMDA The risk or severity of hypertension can be increased when MMDA is combined with Acemetacin.
Midomafetamine The risk or severity of hypertension can be increased when Midomafetamine is combined with Acemetacin.
2,5-Dimethoxy-4-ethylamphetamine The risk or severity of hypertension can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Acemetacin.
4-Methoxyamphetamine The risk or severity of hypertension can be increased when 4-Methoxyamphetamine is combined with Acemetacin.
4-Bromo-2,5-dimethoxyamphetamine The risk or severity of hypertension can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Acemetacin.
Tenamfetamine The risk or severity of hypertension can be increased when Tenamfetamine is combined with Acemetacin.
Chlorphentermine The risk or severity of hypertension can be increased when Chlorphentermine is combined with Acemetacin.
Dextroamphetamine The risk or severity of hypertension can be increased when Dextroamphetamine is combined with Acemetacin.
Phendimetrazine The risk or severity of hypertension can be increased when Phendimetrazine is combined with Acemetacin.
Solifenacin The risk or severity of hypertension can be increased when Solifenacin is combined with Acemetacin.
Periciazine The risk or severity of hypertension can be increased when Periciazine is combined with Acemetacin.
Acepromazine The risk or severity of hypertension can be increased when Acepromazine is combined with Acemetacin.
Thioproperazine The risk or severity of hypertension can be increased when Thioproperazine is combined with Acemetacin.
Zuclopenthixol The risk or severity of hypertension can be increased when Zuclopenthixol is combined with Acemetacin.
Epicaptopril The risk or severity of hypertension can be increased when Epicaptopril is combined with Acemetacin.
Clorgiline The risk or severity of hypertension can be increased when Clorgiline is combined with Acemetacin.
1-benzylimidazole The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Acemetacin.
Iproniazid The risk or severity of hypertension can be increased when Iproniazid is combined with Acemetacin.
Nialamide The risk or severity of hypertension can be increased when Nialamide is combined with Acemetacin.
Lysergic acid diethylamide The risk or severity of hypertension can be increased when Lysergic acid diethylamide is combined with Acemetacin.
Dronedarone The risk or severity of hypertension can be increased when Dronedarone is combined with Acemetacin.
Flibanserin The risk or severity of hypertension can be increased when Flibanserin is combined with Acemetacin.
Iloperidone The risk or severity of hypertension can be increased when Iloperidone is combined with Acemetacin.

Target Protein

Prostaglandin G/H synthase 1 PTGS1
Prostaglandin G/H synthase 2 PTGS2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 6587139
    Wada Y, Nakamura M, Kogo H, Aizawa Y: Inhibitory effect of acemetacin, a prodrug of indomethacin, on prostaglandin E2 release from inflamed synovial tissue. Jpn J Pharmacol. 1984 Apr;34(4):468-70.
  • PMID: 6968219
    Jacobi H, Dell HD: On the pharmacodynamics of acemetacin (author's transl). Arzneimittelforschung. 1980;30(8A):1348-62.
  • PMID: 1888622
    Jones RW, Collins AJ, Notarianni LJ, Sedman E: The comparative pharmacokinetics of acemetacin in young subjects and elderly patients. Br J Clin Pharmacol. 1991 May;31(5):543-5.
  • PMID: 7191306
    Dell HD, Doersing M, Fischer W, Jacobi H, Kamp R, Kohler G, Schollnhammer G: Metabolism and pharmacokinetics of acemetacin in man (author's transl). Arzneimittelforschung. 1980;30(8A):1391-8.
  • PMID: 6193370
    Ochs HR, Schuppan U, Greenblatt DJ, Abernethy DR: Reduced distribution and clearance of acetaminophen in patients with congestive heart failure. J Cardiovasc Pharmacol. 1983 Jul-Aug;5(4):697-9.
Textbook
  • Acton A. (2011). Issues in Pharmacology, Pharmacy, Drug Research and Drug Innovation . ScholarlyEditions.
  • Sneader W. (2005). Drug discovery a history. Wiley.
  • Chian R., Nargund G. and Huang J. (2017). Development of In vitro maturation for human oocytes. Springer.
  • Seyffart G. (1992). Drug dosage in renal insufficiency (2nd ed.). Springer Science+Business Media Dordrecht.

Contoh Produk & Brand

Produk: 0 • International brands: 4
International Brands
  • Acemix — Bioprogress
  • Emflex — Merck Serono
  • Rantudil — Bayer or Bial
  • Solart — Bioindustria

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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