Peringatan Keamanan

The major toxic effects reported for arotinolol-like drugs are the presence of central nervous system depression.T90

Arotinolol

DB09204

small molecule investigational

Deskripsi

Arotinolol is an alpha- and beta-receptor blocker developed in Japan. It is a thiopropanolamine with a tertiary butyl moiety. It has been studied for its potential to be an antihypertensive therapy.T87 Artinolol is being developed by Sumitomo Pharmaceutical Co., Ltd. and it is currently under clinical trials.L1168

Struktur Molekul 2D

Berat 371.53
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported half-life of arotinolol is 7.2 hours.[T87]
Volume Distribusi The stereospecificity of arotinolol is very important for its pharmacokinetic characteristics. The S-enantiomer is highly retained in red blood cells. The distribution studies have shown that arotinolol is mainly distributed from the plasma to the liver followed by the lungs and lastly in the heart. The distribution in the liver was independent on the stereochemistry of the molecules.[T89]
Klirens (Clearance) -

Absorpsi

Arotinolol gets rapidly absorbed and distributed in the plasma. The plasma concentration peaks 2 hours after initial administration.A31639

Metabolisme

The stereospecificity of arotinolol is very important for its pharmacokinetic characteristics. The R-enantiomer remains unchanged and it is eliminated from the organism by urine in this form while the S-enantiomer is metabolized.T87

Rute Eliminasi

The stereospecificity of arotinolol is very important for its pharmacokinetic characteristics. Both of the enantiomers were found in urine, suggesting this as the major elimination pathway. It is possible to find arotinolol in urine 2-4 hours after initial administration.T87

Interaksi Obat

1626 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Arotinolol is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Arotinolol is combined with Levodopa.
Risperidone Arotinolol may increase the hypotensive activities of Risperidone.
Ceritinib Arotinolol may increase the bradycardic activities of Ceritinib.
Ivabradine Arotinolol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Arotinolol.
Amiodarone The therapeutic efficacy of Arotinolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Arotinolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Arotinolol.
Disopyramide Disopyramide may increase the bradycardic activities of Arotinolol.
Dronedarone Dronedarone may increase the bradycardic activities of Arotinolol.
Fingolimod Arotinolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Arotinolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Arotinolol.
Methacholine Arotinolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Arotinolol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Arotinolol.
Propafenone The risk or severity of adverse effects can be increased when Propafenone is combined with Arotinolol.
Regorafenib Regorafenib may increase the bradycardic activities of Arotinolol.
Reserpine Reserpine may increase the hypotensive activities of Arotinolol.
Deserpidine Deserpidine may increase the hypotensive activities of Arotinolol.
Guanethidine Guanethidine may increase the hypotensive activities of Arotinolol.
Rivastigmine Arotinolol may increase the bradycardic activities of Rivastigmine.
Mirabegron The serum concentration of Arotinolol can be increased when it is combined with Mirabegron.
Nicorandil Nicorandil may increase the hypotensive activities of Arotinolol.
Insulin argine Arotinolol may increase the hypoglycemic activities of Insulin argine.
Nicotine The risk or severity of adverse effects can be increased when Arotinolol is combined with Nicotine.
Carbamoylcholine The risk or severity of adverse effects can be increased when Arotinolol is combined with Carbamoylcholine.
Bethanechol The risk or severity of adverse effects can be increased when Arotinolol is combined with Bethanechol.
Pilocarpine The risk or severity of adverse effects can be increased when Arotinolol is combined with Pilocarpine.
Acetylcholine The risk or severity of adverse effects can be increased when Arotinolol is combined with Acetylcholine.
Arecoline The risk or severity of adverse effects can be increased when Arotinolol is combined with Arecoline.
Lobeline The risk or severity of adverse effects can be increased when Arotinolol is combined with Lobeline.
NGX267 The risk or severity of adverse effects can be increased when Arotinolol is combined with NGX267.
GTS-21 The risk or severity of adverse effects can be increased when Arotinolol is combined with GTS-21.
Epibatidine The risk or severity of adverse effects can be increased when Arotinolol is combined with Epibatidine.
Xanomeline The risk or severity of adverse effects can be increased when Arotinolol is combined with Xanomeline.
Cevimeline The risk or severity of adverse effects can be increased when Arotinolol is combined with Cevimeline.
Varenicline The risk or severity of adverse effects can be increased when Arotinolol is combined with Varenicline.
Thiethylperazine The serum concentration of Arotinolol can be increased when it is combined with Thiethylperazine.
Promazine The serum concentration of Arotinolol can be increased when it is combined with Promazine.
Prochlorperazine The serum concentration of Arotinolol can be increased when it is combined with Prochlorperazine.
Triflupromazine The serum concentration of Arotinolol can be increased when it is combined with Triflupromazine.
Fluphenazine The serum concentration of Arotinolol can be increased when it is combined with Fluphenazine.
Moricizine The serum concentration of Arotinolol can be increased when it is combined with Moricizine.
Trifluoperazine The serum concentration of Arotinolol can be increased when it is combined with Trifluoperazine.
Perphenazine The serum concentration of Arotinolol can be increased when it is combined with Perphenazine.
Mesoridazine The serum concentration of Arotinolol can be increased when it is combined with Mesoridazine.
Acetophenazine The serum concentration of Arotinolol can be increased when it is combined with Acetophenazine.
Promethazine The serum concentration of Arotinolol can be increased when it is combined with Promethazine.
Alimemazine The serum concentration of Arotinolol can be increased when it is combined with Alimemazine.
Periciazine The serum concentration of Arotinolol can be increased when it is combined with Periciazine.
Acepromazine The serum concentration of Arotinolol can be increased when it is combined with Acepromazine.
Aceprometazine The serum concentration of Arotinolol can be increased when it is combined with Aceprometazine.
Pipotiazine The serum concentration of Arotinolol can be increased when it is combined with Pipotiazine.
Thioproperazine The serum concentration of Arotinolol can be increased when it is combined with Thioproperazine.
BL-1020 The serum concentration of Arotinolol can be increased when it is combined with BL-1020.
Cyamemazine The serum concentration of Arotinolol can be increased when it is combined with Cyamemazine.
Methylene blue The serum concentration of Arotinolol can be increased when it is combined with Methylene blue.
Propiopromazine The serum concentration of Arotinolol can be increased when it is combined with Propiopromazine.
Perazine The serum concentration of Arotinolol can be increased when it is combined with Perazine.
Butaperazine The serum concentration of Arotinolol can be increased when it is combined with Butaperazine.
Chlorproethazine The serum concentration of Arotinolol can be increased when it is combined with Chlorproethazine.
Thiazinam The serum concentration of Arotinolol can be increased when it is combined with Thiazinam.
Dixyrazine The serum concentration of Arotinolol can be increased when it is combined with Dixyrazine.
Perphenazine enanthate The serum concentration of Arotinolol can be increased when it is combined with Perphenazine enanthate.
Acetyldigitoxin Arotinolol may increase the bradycardic activities of Acetyldigitoxin.
Deslanoside Arotinolol may increase the bradycardic activities of Deslanoside.
Ouabain Arotinolol may increase the bradycardic activities of Ouabain.
Digitoxin Arotinolol may increase the bradycardic activities of Digitoxin.
Oleandrin Arotinolol may increase the bradycardic activities of Oleandrin.
Cymarin Arotinolol may increase the bradycardic activities of Cymarin.
Proscillaridin Arotinolol may increase the bradycardic activities of Proscillaridin.
Metildigoxin Arotinolol may increase the bradycardic activities of Metildigoxin.
Lanatoside C Arotinolol may increase the bradycardic activities of Lanatoside C.
Gitoformate Arotinolol may increase the bradycardic activities of Gitoformate.
Acetyldigoxin Arotinolol may increase the bradycardic activities of Acetyldigoxin.
Peruvoside Arotinolol may increase the bradycardic activities of Peruvoside.
Lidocaine The serum concentration of Lidocaine can be increased when it is combined with Arotinolol.
Icosapent Icosapent may decrease the antihypertensive activities of Arotinolol.
Mesalazine The risk or severity of hyperkalemia can be increased when Mesalazine is combined with Arotinolol.
Indomethacin Indomethacin may decrease the antihypertensive activities of Arotinolol.
Nabumetone Nabumetone may decrease the antihypertensive activities of Arotinolol.
Ketorolac Ketorolac may decrease the antihypertensive activities of Arotinolol.
Tenoxicam Tenoxicam may decrease the antihypertensive activities of Arotinolol.
Celecoxib Celecoxib may decrease the antihypertensive activities of Arotinolol.
Tolmetin Tolmetin may decrease the antihypertensive activities of Arotinolol.
Rofecoxib Rofecoxib may decrease the antihypertensive activities of Arotinolol.
Piroxicam Piroxicam may decrease the antihypertensive activities of Arotinolol.
Fenoprofen Fenoprofen may decrease the antihypertensive activities of Arotinolol.
Valdecoxib Valdecoxib may decrease the antihypertensive activities of Arotinolol.
Diclofenac Diclofenac may decrease the antihypertensive activities of Arotinolol.
Sulindac Sulindac may decrease the antihypertensive activities of Arotinolol.
Flurbiprofen Flurbiprofen may decrease the antihypertensive activities of Arotinolol.
Etodolac Etodolac may decrease the antihypertensive activities of Arotinolol.
Mefenamic acid Mefenamic acid may decrease the antihypertensive activities of Arotinolol.
Naproxen Naproxen may decrease the antihypertensive activities of Arotinolol.
Sulfasalazine Sulfasalazine may decrease the antihypertensive activities of Arotinolol.
Phenylbutazone Phenylbutazone may decrease the antihypertensive activities of Arotinolol.
Meloxicam Meloxicam may decrease the antihypertensive activities of Arotinolol.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Alpha-1 adrenergic receptors ADRA1A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11478592
    Zhao J, Golozoubova V, Cannon B, Nedergaard J: Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes. Can J Physiol Pharmacol. 2001 Jul;79(7):585-93.
  • PMID: 12853233
    Lee KS, Kim JS, Kim JW, Lee WY, Jeon BS, Kim D: A multicenter randomized crossover multiple-dose comparison study of arotinolol and propranolol in essential tremor. Parkinsonism Relat Disord. 2003 Aug;9(6):341-7.
  • PMID: 11675958
    Wu H, Zhang Y, Huang J, Zhang Y, Liu G, Sun N, Yu Z, Zhou Y: Clinical trial of arotinolol in the treatment of hypertension: dippers vs. non-dippers. Hypertens Res. 2001 Sep;24(5):605-10.
  • PMID: 10554561
    Miyauchi E, Matsumoto M, Kimura Y, Hattori H, Tsukio Y, Tsuchiya H, Takasaki M, Munehira J, Yamada K, Iwai K, Kawanishi K, Hoshino T, Murai H: Clinical effect of arotinolol hydrochloride and its influence on renal function in elderly patients with essential hypertension. Nihon Ronen Igakkai Zasshi. 1999 Aug;36(8):542-6.
  • PMID: 2411566
    Nakashima M, Uematsu T, Takiguchi Y, Hashimoto H, Watanabe I, Morioka S, Hibino T: Effect of ophthalmic administration of S-596 (Arotinolol) on intraocular pressure and haemodynamics in health volunteers: comparison with timolol. Eur J Clin Pharmacol. 1985;28(4):391-6.
Textbook
  • Ganten D. and Mulrow P.J. (1990). Pharmacology of anti-hypertensive therapeutics (1st ed.). Springer .
  • Allen R. (1988). Annual reports in medicinal chemistry (23rd ed.). Academic press.
  • Kato R., Estabrook W. and Cayen M. (1988). Xenobiotic metabolism and disposition (2nd ed.). Taylor and Francis.
  • Pillay V.V. (2013). Modern medical toxicology (4th ed.). Jaypee Brothers.

Contoh Produk & Brand

Produk: 0 • International brands: 1
International Brands
  • Almarl

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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