Peringatan Keamanan

No information is available at this time regarding bimatoprost overdose in humans. Provide supportive symptomatic treatment if an overdose occurs.L6877

Bimatoprost

DB00905

small molecule approved investigational

Deskripsi

Bimatoprost, also known as Latisse or Lumigan, belongs to a group of drugs called prostamides, which are synthetic structural analogs of prostaglandin. Bimatoprost, marketed by Allergan, is administered in both the ophthalmic solution and implant form. It has the ability to reduce ocular hypotension, proving effective in conditions such as ocular hypertension and glaucoma.L6877,L6892,L6898,L12069 Bimatoprost is also used to treat eyelash hypotrichosis, or sparse eyelash growth.L6910 It was initially approved by the FDA in 2001 for ocular hypertension and later approved for hypothrichosis in 2008, as eyelash growth became a desirable adverse effect for patients using this drug.L4894

Struktur Molekul 2D

Berat 415.5656
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 bimatoprost is approximately 45 minutes.[L6877,L6892]
Volume Distribusi The volume of distribution at steady state is 0.67 L/kg.[L6877,L6898]. It penetrates the human cornea and sclera.[L6898]
Klirens (Clearance) The clearance was measured to be 1.5 L/hr/kg in healthy subjects receiving IV administration of bimatoprost dosed at 3.12 ug/kg.[L6877,L6892]

Absorpsi

This drug is absorbed systemically when administered to the eye. A study was performed on 15 healthy volunteers and bimatoprost ophthalmic solution 0.03% was administered once daily for 14 days. The mean Cmax was approximately 0.08 ng/mL and AUC0-24hr was approximately 0.09 on days 7 and 14 of the study.L6877 By 10 minutes, peak blood concentration was achieved. Bimatoprost was not detectable at 1.5 hours after administration in most subjects. The maximum blood concentration in a study of 6 healthy volunteers was determined to be 12.2 ng/mL. Steady state was reached in the first week of dosing.L6877 One drug label mentions that onset of decreased intraocular pressure occurs approximately 4 hours after the first administration and the peak effect occurs in the range of 8-12 hours. Bimatoprost effects may last up to 24 hours.L6898

Metabolisme

Bimatoprost is hydrolyzed to its active form, bimatoprost acid, in the eye.L6913 Bimatoprost undergoes oxidation, N-deethylation, and glucuronidation after it is systemically absorbed, and this leads to the production of various metabolites.L6877 In vitro studies show that CYP3A4 is an enzyme that participates in the metabolism of bimatoprost. Despite this, many enzymes and pathways metabolize bimatoprost, therefore, no significant drug-drug interactions are likely to occur.L6892 Glucuronidated metabolites comprise most of the excreted drug product in the blood, urine, and feces in rats.L6892

Rute Eliminasi

One pharmacokinetic study of bimatoprost in 6 healthy volunteers determined that 67% of the administered dose was found to be excreted in the urine while 25% of the dose was recovered in the feces.L6877

Interaksi Obat

297 Data
Latanoprost The risk or severity of intraocular pressure can be increased when Latanoprost is combined with Bimatoprost.
Valsartan Valsartan may increase the hypotensive activities of Bimatoprost.
Ramipril Ramipril may increase the hypotensive activities of Bimatoprost.
Esmolol Esmolol may increase the hypotensive activities of Bimatoprost.
Betaxolol Betaxolol may increase the hypotensive activities of Bimatoprost.
Reserpine Reserpine may increase the hypotensive activities of Bimatoprost.
Remikiren Remikiren may increase the hypotensive activities of Bimatoprost.
Torasemide Torasemide may increase the hypotensive activities of Bimatoprost.
Bethanidine Bethanidine may increase the hypotensive activities of Bimatoprost.
Guanadrel Guanadrel may increase the hypotensive activities of Bimatoprost.
Metoprolol Metoprolol may increase the hypotensive activities of Bimatoprost.
Isradipine Isradipine may increase the hypotensive activities of Bimatoprost.
Olmesartan Olmesartan may increase the hypotensive activities of Bimatoprost.
Chlorthalidone Chlorthalidone may increase the hypotensive activities of Bimatoprost.
Nitroprusside Nitroprusside may increase the hypotensive activities of Bimatoprost.
Atenolol Atenolol may increase the hypotensive activities of Bimatoprost.
Diltiazem Diltiazem may increase the hypotensive activities of Bimatoprost.
Minoxidil Minoxidil may increase the hypotensive activities of Bimatoprost.
Timolol Timolol may increase the hypotensive activities of Bimatoprost.
Treprostinil Treprostinil may increase the hypotensive activities of Bimatoprost.
Amlodipine Amlodipine may increase the hypotensive activities of Bimatoprost.
Nimodipine Nimodipine may increase the hypotensive activities of Bimatoprost.
Nisoldipine Nisoldipine may increase the hypotensive activities of Bimatoprost.
Prazosin Prazosin may increase the hypotensive activities of Bimatoprost.
Fosinopril Fosinopril may increase the hypotensive activities of Bimatoprost.
Trandolapril Trandolapril may increase the hypotensive activities of Bimatoprost.
Carteolol Carteolol may increase the hypotensive activities of Bimatoprost.
Metolazone Metolazone may increase the hypotensive activities of Bimatoprost.
Lercanidipine Lercanidipine may increase the hypotensive activities of Bimatoprost.
Benazepril Benazepril may increase the hypotensive activities of Bimatoprost.
Bosentan Bosentan may increase the hypotensive activities of Bimatoprost.
Propranolol Propranolol may increase the hypotensive activities of Bimatoprost.
Clonidine Clonidine may increase the hypotensive activities of Bimatoprost.
Enalapril Enalapril may increase the hypotensive activities of Bimatoprost.
Doxazosin Doxazosin may increase the hypotensive activities of Bimatoprost.
Labetalol Labetalol may increase the hypotensive activities of Bimatoprost.
Bisoprolol Bisoprolol may increase the hypotensive activities of Bimatoprost.
Candoxatril Candoxatril may increase the hypotensive activities of Bimatoprost.
Nicardipine Nicardipine may increase the hypotensive activities of Bimatoprost.
Guanabenz Guanabenz may increase the hypotensive activities of Bimatoprost.
Mecamylamine Mecamylamine may increase the hypotensive activities of Bimatoprost.
Losartan Losartan may increase the hypotensive activities of Bimatoprost.
Moexipril Moexipril may increase the hypotensive activities of Bimatoprost.
Phentolamine Phentolamine may increase the hypotensive activities of Bimatoprost.
Eplerenone Eplerenone may increase the hypotensive activities of Bimatoprost.
Lisinopril Lisinopril may increase the hypotensive activities of Bimatoprost.
Nitroglycerin Nitroglycerin may increase the hypotensive activities of Bimatoprost.
Metyrosine Metyrosine may increase the hypotensive activities of Bimatoprost.
Cryptenamine Cryptenamine may increase the hypotensive activities of Bimatoprost.
Perindopril Perindopril may increase the hypotensive activities of Bimatoprost.
Candesartan cilexetil Candesartan cilexetil may increase the hypotensive activities of Bimatoprost.
Tolazoline Tolazoline may increase the hypotensive activities of Bimatoprost.
Fenoldopam Fenoldopam may increase the hypotensive activities of Bimatoprost.
Tadalafil Tadalafil may increase the hypotensive activities of Bimatoprost.
Alprenolol Alprenolol may increase the hypotensive activities of Bimatoprost.
Dorzolamide Dorzolamide may increase the hypotensive activities of Bimatoprost.
Eprosartan Eprosartan may increase the hypotensive activities of Bimatoprost.
Quinapril Quinapril may increase the hypotensive activities of Bimatoprost.
Omapatrilat Omapatrilat may increase the hypotensive activities of Bimatoprost.
Phenoxybenzamine Bimatoprost may increase the hypotensive activities of Phenoxybenzamine.
Pindolol Bimatoprost may increase the hypotensive activities of Pindolol.
Telmisartan Bimatoprost may increase the hypotensive activities of Telmisartan.
Methyldopa Bimatoprost may increase the hypotensive activities of Methyldopa.
Guanfacine Bimatoprost may increase the hypotensive activities of Guanfacine.
Felodipine Bimatoprost may increase the hypotensive activities of Felodipine.
Irbesartan Bimatoprost may increase the hypotensive activities of Irbesartan.
Nitrendipine Bimatoprost may increase the hypotensive activities of Nitrendipine.
Deserpidine Bimatoprost may increase the hypotensive activities of Deserpidine.
Pentolinium Bimatoprost may increase the hypotensive activities of Pentolinium.
Trimethaphan Bimatoprost may increase the hypotensive activities of Trimethaphan.
Diazoxide Bimatoprost may increase the hypotensive activities of Diazoxide.
Carvedilol Bimatoprost may increase the hypotensive activities of Carvedilol.
Bretylium Bimatoprost may increase the hypotensive activities of Bretylium.
Terazosin Bimatoprost may increase the hypotensive activities of Terazosin.
Guanethidine Bimatoprost may increase the hypotensive activities of Guanethidine.
Rescinnamine Bimatoprost may increase the hypotensive activities of Rescinnamine.
Acebutolol Bimatoprost may increase the hypotensive activities of Acebutolol.
Captopril Bimatoprost may increase the hypotensive activities of Captopril.
Nadolol Bimatoprost may increase the hypotensive activities of Nadolol.
Metipranolol Bimatoprost may increase the hypotensive activities of Metipranolol.
Epoprostenol Bimatoprost may increase the hypotensive activities of Epoprostenol.
Bepridil Bimatoprost may increase the hypotensive activities of Bepridil.
Hydralazine Bimatoprost may increase the hypotensive activities of Hydralazine.
Bevantolol Bimatoprost may increase the hypotensive activities of Bevantolol.
Practolol Bimatoprost may increase the hypotensive activities of Practolol.
Cilazapril Bimatoprost may increase the hypotensive activities of Cilazapril.
Saprisartan Bimatoprost may increase the hypotensive activities of Saprisartan.
Spirapril Bimatoprost may increase the hypotensive activities of Spirapril.
Penbutolol Bimatoprost may increase the hypotensive activities of Penbutolol.
Mibefradil Bimatoprost may increase the hypotensive activities of Mibefradil.
Oxprenolol Bimatoprost may increase the hypotensive activities of Oxprenolol.
Pargyline Bimatoprost may increase the hypotensive activities of Pargyline.
Dexpropranolol Bimatoprost may increase the hypotensive activities of Dexpropranolol.
Tienilic acid Bimatoprost may increase the hypotensive activities of Tienilic acid.
Debrisoquine Bimatoprost may increase the hypotensive activities of Debrisoquine.
Celiprolol Bimatoprost may increase the hypotensive activities of Celiprolol.
Nebivolol Bimatoprost may increase the hypotensive activities of Nebivolol.
Lofexidine Bimatoprost may increase the hypotensive activities of Lofexidine.
Sitaxentan Bimatoprost may increase the hypotensive activities of Sitaxentan.
Ambrisentan Bimatoprost may increase the hypotensive activities of Ambrisentan.

Target Protein

Prostaglandin F2-alpha receptor PTGFR
Prostaglandin E2 receptor EP1 subtype PTGER1
Prostaglandin E2 receptor EP3 subtype PTGER3

Referensi & Sumber

Synthesis reference: Jiang Xing Chen, "Process for the production of intermediates for making prostaglandin derivatives such as latanaprost, travaprost, and bimatoprost." U.S. Patent US20090287003, issued November 19, 2009.
Artikel (PubMed)
  • PMID: 16808680
    Chen MJ, Cheng CY, Chen YC, Chou CK, Hsu WM: Effects of bimatoprost 0.03% on ocular hemodynamics in normal tension glaucoma. J Ocul Pharmacol Ther. 2006 Jun;22(3):188-93.
  • PMID: 16804825
    Kruse P, Rieck P, Sherif Z, Liekfeld A: Cystoid macular edema in a pseudophakic patient after several glaucoma procedures. Is local therapy with bimatoprost the reason?. Klin Monbl Augenheilkd. 2006 Jun;223(6):534-7.
  • PMID: 16567279
    Steinhauser SL: Decreased high-density lipoprotein serum levels associated with topical bimatoprost therapy. Optometry. 2006 Apr;77(4):177-9.
  • PMID: 11434936
    Woodward DF, Krauss AH, Chen J, Lai RK, Spada CS, Burk RM, Andrews SW, Shi L, Liang Y, Kedzie KM, Chen R, Gil DW, Kharlamb A, Archeampong A, Ling J, Madhu C, Ni J, Rix P, Usansky J, Usansky H, Weber A, Welty D, Yang W, Tang-Liu DD, Garst ME, Brar B, Wheeler LA, Kaplan LJ: The pharmacology of bimatoprost (Lumigan). Surv Ophthalmol. 2001 May;45 Suppl 4:S337-45.
  • PMID: 18452763
    Lim KS, Nau CB, O'Byrne MM, Hodge DO, Toris CB, McLaren JW, Johnson DH: Mechanism of action of bimatoprost, latanoprost, and travoprost in healthy subjects. A crossover study. Ophthalmology. 2008 May;115(5):790-795.e4. doi: 10.1016/j.ophtha.2007.07.002.
  • PMID: 11434937
    Brubaker RF: Mechanism of action of bimatoprost (Lumigan). Surv Ophthalmol. 2001 May;45 Suppl 4:S347-51.
  • PMID: 15350319
    Christiansen GA, Nau CB, McLaren JW, Johnson DH: Mechanism of ocular hypotensive action of bimatoprost (Lumigan) in patients with ocular hypertension or glaucoma. Ophthalmology. 2004 Sep;111(9):1658-62.
  • PMID: 12027782
    Easthope SE, Perry CM: Topical bimatoprost: a review of its use in open-angle glaucoma and ocular hypertension. Drugs Aging. 2002;19(3):231-48.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 50 • International brands: 0
Produk
  • Apo-bimatoprost
    Solution • 0.03 % w/v • Ophthalmic • Canada • Generic • Approved
  • Apo-bimatoprost
    Solution • 0.03 % w/v • Topical • Canada • Generic • Approved
  • Bimatoprost
    Solution / drops • 0.3 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bimatoprost
    Solution • 3 ug/1mL • Topical • US • Generic • Approved
  • Bimatoprost
    Solution / drops • 0.3 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bimatoprost
    Solution / drops • 0.3 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bimatoprost
    Solution / drops • 0.3 mg/1mL • Ophthalmic • US • Generic • Approved
  • Bimatoprost
    Solution / drops • 0.3 mg/1mL • Ophthalmic • US • Generic • Approved
Menampilkan 8 dari 50 produk.

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