Peringatan Keamanan

The oral LD50 for timolol maleate is 1028 mg/kg in the rat and 1137 mg/kg in the mouse.MSDS

Symptoms of timolol overdose may include dizziness, headache, shortness of breath, bradycardia, in addition to bronchospasm. Sometimes, an overdose may lead to cardiac arrest. An overdose of timolol can be reversed with dialysis, however, patients with renal failure may not respond as well to dialysis treatment.L6724

Timolol

DB00373

small molecule approved

Deskripsi

Timolol is a nonselective beta-adrenergic antagonist given in an eye drop solution to reduce intraocular pressure, or pressure in the eyes.L6724 It is also used in tablet form as a drug to treat hypertension.L6727 Timolol was first approved by the FDA in 1978.L6724 This drug is marketed by several manufacturers L6736 and is an effective agent for the management of conditions such as open-angle glaucoma and hypertension.

Struktur Molekul 2D

Berat 316.42
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Timolol half-life was measured at 2.9 ± 0.3 h hours in a clinical study of healthy volunteers.[A179560]
Volume Distribusi 1.3 - 1.7 L/kg [L6] Timolol is distributed to the following tissues: the conjunctiva, cornea, iris, sclera, aqueous humor, kidney, liver, and lung.[L6]
Klirens (Clearance) One pharmacokinetic study in healthy volunteers measured the total plasma clearance of timolol to be 557 ± 61 ml/min.[A179557] Another study determined the total clearance 751.5 ± 90.6 ml/min and renal clearance to be 97.2 ± 10.1 ml/min in healthy volunteers.[A179560]

Absorpsi

The systemic bioavailability of the ophthalmic eyedrop in one study of healthy volunteers was 78.0 ± 24.5% A179539, indicating that caution must be observed when this drug is administered, as it may be significantly absorbed and have various systemic effects. Another study measured the bioavailability of timolol eyedrops to be 60% in healthy volunteers.A179548 The peak concentration of ophthalmic timolol in plasma, Cmax was about 1.14 ng/ml in most subjects within 15 minutes following the administration of timolol by the ophthalmic route. The mean area under the curve (AUC) was about 6.46 ng/ml per hour after intravenous injection and about 4.78 ng/ml per hour following eyedrop administration.A179539

Metabolisme

Timolol is metabolized in the liver by the cytochrome P450 2D6 enzyme, with minor contributions from CYP2C19.A179551,L6724 15-20% of a dose undergoes first-pass metabolism.A179560 Despite its relatively low first pass metabolism, timolol is 90% metabolized.A179560 Four metabolites of timolol have been identified, with a hydroxy metabolite being the most predominant.A179551

Rute Eliminasi

Timolol and its metabolites are mainly found excreted in the urine.A179560

Interaksi Obat

1891 Data
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Timolol is combined with Levodopa.
Risperidone Timolol may increase the hypotensive activities of Risperidone.
Ceritinib Timolol may increase the bradycardic activities of Ceritinib.
Ivabradine Timolol may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Timolol.
Alfuzosin Alfuzosin may increase the hypotensive activities of Timolol.
Amifostine Timolol may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Timolol.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Timolol.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Timolol.
Obinutuzumab Timolol may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Timolol.
Rituximab Timolol may increase the hypotensive activities of Rituximab.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Timolol.
Doxapram Doxapram may decrease the antihypertensive activities of Timolol.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Timolol.
Naratriptan Naratriptan may decrease the antihypertensive activities of Timolol.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Timolol.
Dutasteride Dutasteride may decrease the antihypertensive activities of Timolol.
Finasteride Finasteride may decrease the antihypertensive activities of Timolol.
Epicaptopril Epicaptopril may decrease the antihypertensive activities of Timolol.
1-benzylimidazole 1-benzylimidazole may decrease the antihypertensive activities of Timolol.
Amineptine Amineptine may decrease the antihypertensive activities of Timolol.
Naluzotan Naluzotan may decrease the antihypertensive activities of Timolol.
Nitrous oxide Nitrous oxide may decrease the antihypertensive activities of Timolol.
Cinitapride Cinitapride may decrease the antihypertensive activities of Timolol.
Tyramine Tyramine may decrease the antihypertensive activities of Timolol.
Ifenprodil Ifenprodil may decrease the antihypertensive activities of Timolol.
Tianeptine Tianeptine may decrease the antihypertensive activities of Timolol.
Oxaprotiline Oxaprotiline may decrease the antihypertensive activities of Timolol.
Atipamezole Atipamezole may decrease the antihypertensive activities of Timolol.
Tetrahydrocannabivarin Tetrahydrocannabivarin may decrease the antihypertensive activities of Timolol.
Piclozotan Piclozotan may decrease the antihypertensive activities of Timolol.
Siponimod Siponimod may decrease the antihypertensive activities of Timolol.
Idazoxan Idazoxan may decrease the antihypertensive activities of Timolol.
Tramazoline Tramazoline may decrease the antihypertensive activities of Timolol.
Amitriptylinoxide Amitriptylinoxide may decrease the antihypertensive activities of Timolol.
Dibenzepin Dibenzepin may decrease the antihypertensive activities of Timolol.
Quinupramine Quinupramine may decrease the antihypertensive activities of Timolol.
Trichloroethylene Trichloroethylene may decrease the antihypertensive activities of Timolol.
Fenozolone Fenozolone may decrease the antihypertensive activities of Timolol.
Melitracen Melitracen may decrease the antihypertensive activities of Timolol.
Lofepramine Lofepramine may decrease the antihypertensive activities of Timolol.
Xenon Xenon may decrease the antihypertensive activities of Timolol.
Iprindole Iprindole may decrease the antihypertensive activities of Timolol.
Buflomedil Buflomedil may decrease the antihypertensive activities of Timolol.
Imipramine oxide Imipramine oxide may decrease the antihypertensive activities of Timolol.
Mefenorex Mefenorex may decrease the antihypertensive activities of Timolol.
5-methoxy-N,N-dimethyltryptamine 5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Timolol.
Quinoline Yellow WS Quinoline Yellow WS may decrease the antihypertensive activities of Timolol.
Sufentanil Sufentanil may decrease the antihypertensive activities of Timolol.
Remifentanil Remifentanil may decrease the antihypertensive activities of Timolol.
Halothane Halothane may decrease the antihypertensive activities of Timolol.
Alfentanil Alfentanil may decrease the antihypertensive activities of Timolol.
Flibanserin Flibanserin may decrease the antihypertensive activities of Timolol.
Diethyl ether Diethyl ether may decrease the antihypertensive activities of Timolol.
Fentanyl Fentanyl may decrease the antihypertensive activities of Timolol.
Dimetacrine Dimetacrine may decrease the antihypertensive activities of Timolol.
Opipramol Opipramol may decrease the antihypertensive activities of Timolol.
Selpercatinib Selpercatinib may decrease the antihypertensive activities of Timolol.
Naxitamab Naxitamab may decrease the antihypertensive activities of Timolol.
Cannabidiol The metabolism of Timolol can be decreased when combined with Cannabidiol.
Amiodarone The therapeutic efficacy of Timolol can be increased when used in combination with Amiodarone.
Bupivacaine The serum concentration of Bupivacaine can be increased when it is combined with Timolol.
Dipyridamole Dipyridamole may increase the bradycardic activities of Timolol.
Disopyramide Disopyramide may increase the bradycardic activities of Timolol.
Dronedarone Dronedarone may increase the bradycardic activities of Timolol.
Fingolimod Timolol may increase the bradycardic activities of Fingolimod.
Floctafenine The risk or severity of adverse effects can be increased when Timolol is combined with Floctafenine.
Mepivacaine The serum concentration of Mepivacaine can be increased when it is combined with Timolol.
Methacholine Timolol may increase the bronchoconstrictory activities of Methacholine.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Timolol.
Nifedipine The risk or severity of congestive heart failure and hypotension can be increased when Nifedipine is combined with Timolol.
Regorafenib Regorafenib may increase the bradycardic activities of Timolol.
Rivastigmine Timolol may increase the bradycardic activities of Rivastigmine.
Dabrafenib The serum concentration of Timolol can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Timolol can be increased when it is combined with Luliconazole.
Mirabegron The serum concentration of Timolol can be increased when it is combined with Mirabegron.
Nicorandil Nicorandil may increase the hypotensive activities of Timolol.
Molsidomine Molsidomine may increase the hypotensive activities of Timolol.
Insulin argine Timolol may increase the hypoglycemic activities of Insulin argine.
Dorzolamide Timolol may increase the hypotensive activities of Dorzolamide.
Bimatoprost Timolol may increase the hypotensive activities of Bimatoprost.
Unoprostone Timolol may increase the hypotensive activities of Unoprostone.
Minoxidil Minoxidil may increase the hypotensive activities of Timolol.
Remikiren Remikiren may increase the hypotensive activities of Timolol.
Guanadrel Guanadrel may increase the hypotensive activities of Timolol.
Bosentan Timolol may increase the hypotensive activities of Bosentan.
Candoxatril Timolol may increase the hypotensive activities of Candoxatril.
Nitroglycerin Timolol may increase the hypotensive activities of Nitroglycerin.
Metyrosine Timolol may increase the hypotensive activities of Metyrosine.
Cryptenamine Timolol may increase the hypotensive activities of Cryptenamine.
Pentolinium Timolol may increase the hypotensive activities of Pentolinium.
Trimethaphan Timolol may increase the hypotensive activities of Trimethaphan.
Diethylnorspermine Timolol may increase the hypotensive activities of Diethylnorspermine.
Pinacidil Timolol may increase the hypotensive activities of Pinacidil.
Riociguat Timolol may increase the hypotensive activities of Riociguat.
Hexamethonium Timolol may increase the hypotensive activities of Hexamethonium.
Rauwolfia serpentina root Timolol may increase the hypotensive activities of Rauwolfia serpentina root.
Angiotensin 1-7 Timolol may increase the hypotensive activities of Angiotensin 1-7.

Target Protein

Beta-1 adrenergic receptor ADRB1
Beta-2 adrenergic receptor ADRB2
Endolysin E

Referensi & Sumber

Synthesis reference: Markku Per alampi, "S-timolol hemihydrate composition and method of preparation therefor." U.S. Patent US5574035, issued October, 1986.
Artikel (PubMed)
  • PMID: 17366003
    Nieminen T, Lehtimaki T, Maenpaa J, Ropo A, Uusitalo H, Kahonen M: Ophthalmic timolol: plasma concentration and systemic cardiopulmonary effects. Scand J Clin Lab Invest. 2007;67(2):237-45. doi: 10.1080/00365510601034736.
  • PMID: 6765488
    Dunn FG, Frohlich ED: Pharmacokinetics, mechanisms of action, indications, and adverse effects of timolol maleate, a nonselective beta-adrenoreceptor blocking agent. Pharmacotherapy. 1981 Nov-Dec;1(3):188-200.
  • PMID: 6649055
    Obel AO: A comparison of timolol plus hydrochlorothiazide plus amiloride and methyldopa in essential hypertension in Black Africans. Trop Geogr Med. 1983 Sep;35(3):285-91.
  • PMID: 6314218
    Watanabe K, Chiou GC: Action mechanism of timolol to lower the intraocular pressure in rabbits. Ophthalmic Res. 1983;15(3):160-7. doi: 10.1159/000265251.
  • PMID: 27534869
    Maenpaa J, Pelkonen O: Cardiac safety of ophthalmic timolol. Expert Opin Drug Saf. 2016 Nov;15(11):1549-1561. doi: 10.1080/14740338.2016.1225718. Epub 2016 Aug 31.
  • PMID: 363400
    Laverty R: Catecholamines: role in health and disease. Drugs. 1978 Nov;16(5):418-40. doi: 10.2165/00003495-197816050-00003.
  • PMID: 3946944
    Leier CV, Baker ND, Weber PA: Cardiovascular effects of ophthalmic timolol. Ann Intern Med. 1986 Feb;104(2):197-9. doi: 10.7326/0003-4819-104-2-197.
  • PMID: 6370874
    Valvo E, Gammaro L, Tessitore N, Fabris A, Ortalda V, Bedogna V, Maschio G: Effects of timolol on blood pressure, systemic hemodynamics, plasma renin activity, and glomerular filtration rate in patients with essential hypertension. Int J Clin Pharmacol Ther Toxicol. 1984 Mar;22(3):156-61.
Menampilkan 8 dari 15 artikel.

Contoh Produk & Brand

Produk: 339 • International brands: 5
Produk
  • Act Dorzotimolol
    Solution • - • Ophthalmic • Canada • Approved
  • Act Latanoprost/timolol
    Solution • - • Ophthalmic • Canada • Approved
  • Ag-dorzolamide Timolol
    Solution • - • Ophthalmic • Canada • Generic • Approved
  • Apo-brimonidine-timop
    Solution • - • Ophthalmic • Canada • Generic • Approved
  • Apo-dorzo-timop
    Solution • - • Ophthalmic • Canada • Generic • Approved
  • Apo-latanoprost-timop
    Solution • - • Ophthalmic • Canada • Generic • Approved
  • Apo-timop
    Solution • 0.5 % • Ophthalmic • Canada • Generic • Approved
  • Apo-timop
    Solution • 0.25 % • Ophthalmic • Canada • Generic • Approved
Menampilkan 8 dari 339 produk.
International Brands
  • Proflax — Sidus
  • Tenopt — Sigma
  • Timacar Depot — MSD
  • Timacor — Gerda
  • Timoptol — Merck

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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