Peringatan Keamanan

The oral LD50 in rats is 3130 mg/kg.L11241

Symptoms of overdose are likely consistent with formoterol's adverse effect profile (i.e. consistent with excessive beta-adrenergic stimulation) and may include angina, hyper or hypotension, tachycardia, arrhythmia, nervousness, headache, tremor, seizures, dry mouth, etc. Patients may experience laboratory abnormalities including hypokalemia, hyperglycemia, and metabolic acidosis.L10986 Treatment of overdosage should consist of symptomatic and supportive therapy, with a particular focus on cardiac monitoring. Consider the use of a cardioselective beta-adrenergic blocker to oppose excessive adrenergic stimulation if clinically appropriate.L10986

Formoterol

DB00983

small molecule approved investigational

Deskripsi

Formoterol is an inhaled beta2-agonist used in the management of COPD and asthma that was first approved for use in the United States in 2001.L10986 It acts on bronchial smooth muscle to dilate and relax airways, and is administered as a racemic mixture of its active (R;R)- and inactive (S;S)-enantiomers.A189528 A major clinical advantage of formoterol over other inhaled beta-agonists is its rapid onset of action (2-3 minutes), which is at least as fast as salbutamol, combined with a long duration of action (12 hours) - for this reason, treatment guidelines for asthma recommend its use as both a reliever and maintenance medication.L11256 It is available as a single-entity product L10986,L11223 and in several formulations in combination with both inhaled corticosteroids L10995,L10619 and long-acting muscarinic antagonists.L10992,L10989

Struktur Molekul 2D

Berat 344.4049
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average terminal elimination half-life of formoterol following inhalation is 7-10 hours, depending on the formulation given.[L10986,L11223,A189537] The plasma half-life of formoterol has been estimated to be 3.4 hours following oral administration and 1.7-2.3 hours following inhalation.[A1533]
Volume Distribusi -
Klirens (Clearance) Renal clearance of formoterol following inhalation is approximately 157 mL/min.[L10986]

Absorpsi

The pulmonary bioavailability of formoterol has been estimated to be about 43% of the delivered dose, while the total systemic bioavailability is approximately 60% of the delivered dose (as systemic bioavailability accounts for absorption in the gut).L11223 Formoterol is rapidly absorbed into plasma following inhalation. In healthy adults, formoterol Tmax ranged from 0.167 to 0.5 hours.L10995 Following a single dose of 10 mcg, Cmax and AUC were 22 pmol/L and 81 pmol.h/L, respectively. In asthmatic adult patients, Tmax ranged from 0.58 to 1.97 hours.L10995 Following single-dose administration of 10mcg, Cmax and AUC0-12h were 22 pmol/L and 125 pmol.h/L, respectively; following multiple-dose administration of 10 mcg, Cmax and AUC0-12h were 41 pmol/L and 226 pmol.h/L, respectively. Absorption appears to be proportional to dose across standard dosing ranges.L10995,L10986

Metabolisme

Formoterol is metabolized primarily via direct glucuronidation of the parent drug and via O-demethylation of the parent drug followed by glucuronidation.L10986,A189606 Minor pathways include sulfate conjugation of the parent drug and deformylation of the parent drug followed by sulfate conjugation, though these minor pathways have not been fully characterized. The major pathway of formoterol metabolism is a direct glucuronidation of the parent drug at its phenolic hydroxyl group, while the second most prominent pathway involves O-demethylation following by glucuronidation at the phenolic hydroxyl group.L10986,A189606 In vitro studies of formoterol disposition indicate that O-demethylation of formoterol involves a number of cytochrome P450 isoenzymes (CYP2D6, CYP2C19, CYP2C9, and CYP2A6) and glucuronidation involves a number of UDP-glucuronosyltransferase isoenzymes (UGT1A1, UGT1A8, UGT1A9, UGT2B7, and UGT2B15), though specific roles for individual enzymes have not been elucidated.L10986

Rute Eliminasi

Elimination differs depending on the route and formulation administered. Following oral administration in 2 healthy subjects, approximately 59-62% and 32-34% of an administered dose was eliminated in the urine and feces, respectively.L10998 Another study which attempted to mimic inhalation via combined intravenous/oral administration noted approximately 62% of the administered dose in the urine and 24% in the feces.A189606 Following inhalation in patients with asthma, approximately 10% and 15-18% of the administered dose was excreted in urine as unchanged parent drug and direct formoterol glucuronides, respectively, and corresponding values in patients with COPD were 7% and 6-9%, respectively.L10998

Interaksi Obat

1425 Data
Loxapine The therapeutic efficacy of Formoterol can be decreased when used in combination with Loxapine.
Ramipril Formoterol may decrease the antihypertensive activities of Ramipril.
Remikiren Formoterol may decrease the antihypertensive activities of Remikiren.
Olmesartan Formoterol may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Formoterol may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Formoterol may decrease the antihypertensive activities of Minoxidil.
Nisoldipine Formoterol may decrease the antihypertensive activities of Nisoldipine.
Fosinopril Formoterol may decrease the antihypertensive activities of Fosinopril.
Trandolapril Formoterol may decrease the antihypertensive activities of Trandolapril.
Benazepril Formoterol may decrease the antihypertensive activities of Benazepril.
Enalapril Formoterol may decrease the antihypertensive activities of Enalapril.
Candoxatril Formoterol may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Formoterol may decrease the antihypertensive activities of Mecamylamine.
Eplerenone Formoterol may decrease the antihypertensive activities of Eplerenone.
Lisinopril Formoterol may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Formoterol may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Formoterol may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Formoterol may decrease the antihypertensive activities of Cryptenamine.
Perindopril Formoterol may decrease the antihypertensive activities of Perindopril.
Fenoldopam Formoterol may decrease the antihypertensive activities of Fenoldopam.
Tadalafil Formoterol may decrease the antihypertensive activities of Tadalafil.
Eprosartan Formoterol may decrease the antihypertensive activities of Eprosartan.
Quinapril Formoterol may decrease the antihypertensive activities of Quinapril.
Deserpidine Formoterol may decrease the antihypertensive activities of Deserpidine.
Pentolinium Formoterol may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Formoterol may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Formoterol may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Formoterol may decrease the antihypertensive activities of Epoprostenol.
Hydralazine Formoterol may decrease the antihypertensive activities of Hydralazine.
Cilazapril Formoterol may decrease the antihypertensive activities of Cilazapril.
Saprisartan Formoterol may decrease the antihypertensive activities of Saprisartan.
Spirapril Formoterol may decrease the antihypertensive activities of Spirapril.
Ambrisentan Formoterol may decrease the antihypertensive activities of Ambrisentan.
Diethylnorspermine Formoterol may decrease the antihypertensive activities of Diethylnorspermine.
Pinacidil Formoterol may decrease the antihypertensive activities of Pinacidil.
Temocapril Formoterol may decrease the antihypertensive activities of Temocapril.
Riociguat Formoterol may decrease the antihypertensive activities of Riociguat.
Macitentan Formoterol may decrease the antihypertensive activities of Macitentan.
Hexamethonium Formoterol may decrease the antihypertensive activities of Hexamethonium.
Aliskiren Formoterol may decrease the antihypertensive activities of Aliskiren.
Nicorandil Formoterol may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Formoterol may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Formoterol may decrease the antihypertensive activities of Enalaprilat.
Selexipag Formoterol may decrease the antihypertensive activities of Selexipag.
Angiotensin 1-7 Formoterol may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Formoterol may decrease the antihypertensive activities of Imidapril.
BQ-123 Formoterol may decrease the antihypertensive activities of BQ-123.
Dihydralazine Formoterol may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Formoterol may decrease the antihypertensive activities of Zofenopril.
Guanoxan Formoterol may decrease the antihypertensive activities of Guanoxan.
Delapril Formoterol may decrease the antihypertensive activities of Delapril.
Vincamine Formoterol may decrease the antihypertensive activities of Vincamine.
Linsidomine Formoterol may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Formoterol may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Formoterol may decrease the antihypertensive activities of Tolonidine.
Endralazine Formoterol may decrease the antihypertensive activities of Endralazine.
Cadralazine Formoterol may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Formoterol may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Formoterol may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Formoterol may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Formoterol may decrease the antihypertensive activities of Guanoclor.
Muzolimine Formoterol may decrease the antihypertensive activities of Muzolimine.
Xipamide Formoterol may decrease the antihypertensive activities of Xipamide.
Dexniguldipine Formoterol may decrease the antihypertensive activities of Dexniguldipine.
Tocopherylquinone Formoterol may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Formoterol may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Formoterol may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Formoterol may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Formoterol may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Formoterol may decrease the antihypertensive activities of Quinaprilat.
Captopril Formoterol may decrease the antihypertensive activities of Captopril.
Amlodipine The metabolism of Formoterol can be decreased when combined with Amlodipine.
Levamlodipine Formoterol may decrease the antihypertensive activities of Levamlodipine.
Lercanidipine Formoterol may decrease the antihypertensive activities of Lercanidipine.
Azilsartan medoxomil Formoterol may decrease the antihypertensive activities of Azilsartan medoxomil.
Dabrafenib The serum concentration of Formoterol can be decreased when it is combined with Dabrafenib.
Desmopressin The risk or severity of hypertension can be increased when Desmopressin is combined with Formoterol.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Formoterol.
Phentermine The risk or severity of hypertension can be increased when Phentermine is combined with Formoterol.
Mesalazine The risk or severity of hypertension can be increased when Mesalazine is combined with Formoterol.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Formoterol.
Methylphenidate The risk or severity of hypertension can be increased when Methylphenidate is combined with Formoterol.
Nabumetone The risk or severity of hypertension can be increased when Nabumetone is combined with Formoterol.
Ketorolac The risk or severity of hypertension can be increased when Ketorolac is combined with Formoterol.
Tolmetin The risk or severity of hypertension can be increased when Tolmetin is combined with Formoterol.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Formoterol.
Fenoprofen The risk or severity of hypertension can be increased when Fenoprofen is combined with Formoterol.
Sulindac The risk or severity of hypertension can be increased when Sulindac is combined with Formoterol.
Sumatriptan The risk or severity of hypertension can be increased when Sumatriptan is combined with Formoterol.
Sufentanil The risk or severity of hypertension can be increased when Sufentanil is combined with Formoterol.
Sulfasalazine The risk or severity of hypertension can be increased when Sulfasalazine is combined with Formoterol.
Alfentanil The risk or severity of hypertension can be increased when Alfentanil is combined with Formoterol.
Fentanyl The risk or severity of hypertension can be increased when Fentanyl is combined with Formoterol.
Carprofen The risk or severity of hypertension can be increased when Carprofen is combined with Formoterol.
Phenmetrazine The risk or severity of hypertension can be increased when Phenmetrazine is combined with Formoterol.
Omapatrilat Formoterol may decrease the antihypertensive activities of Omapatrilat.
Remifentanil The risk or severity of hypertension can be increased when Remifentanil is combined with Formoterol.
Diethylpropion The risk or severity of hypertension can be increased when Diethylpropion is combined with Formoterol.
Meclofenamic acid The risk or severity of hypertension can be increased when Meclofenamic acid is combined with Formoterol.
Acetylsalicylic acid The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with Formoterol.

Target Protein

Beta-2 adrenergic receptor ADRB2
Beta-1 adrenergic receptor ADRB1
Beta-3 adrenergic receptor ADRB3

Referensi & Sumber

Synthesis reference: Jan W. Trofast, Edib Jakupovic, Katarina L. Mansson, "Process for preparing formoterol and related compounds." U.S. Patent US5434304, issued August, 1992.
Artikel (PubMed)
  • PMID: 9506248
    Bartow RA, Brogden RN: Formoterol. An update of its pharmacological properties and therapeutic efficacy in the management of asthma. Drugs. 1998 Feb;55(2):303-22.
  • PMID: 12236843
    Zhang M, Fawcett JP, Shaw JP: Stereoselective urinary excretion of formoterol and its glucuronide conjugate in human. Br J Clin Pharmacol. 2002 Sep;54(3):246-50. doi: 10.1046/j.1365-2125.2002.01641.x.
  • PMID: 17627976
    Somers GI, Lindsay N, Lowdon BM, Jones AE, Freathy C, Ho S, Woodrooffe AJ, Bayliss MK, Manchee GR: A comparison of the expression and metabolizing activities of phase I and II enzymes in freshly isolated human lung parenchymal cells and cryopreserved human hepatocytes. Drug Metab Dispos. 2007 Oct;35(10):1797-805. Epub 2007 Jul 12.
  • PMID: 18974284
    Tronde A, Gillen M, Borgstrom L, Lotvall J, Ankerst J: Pharmacokinetics of budesonide and formoterol administered via 1 pressurized metered-dose inhaler in patients with asthma and COPD. J Clin Pharmacol. 2008 Nov;48(11):1300-8. doi: 10.1177/0091270008322122.
  • PMID: 25751092
    Salomon JJ, Hagos Y, Petzke S, Kuhne A, Gausterer JC, Hosoya K, Ehrhardt C: Beta-2 Adrenergic Agonists Are Substrates and Inhibitors of Human Organic Cation Transporter 1. Mol Pharm. 2015 Aug 3;12(8):2633-41. doi: 10.1021/mp500854e. Epub 2015 Mar 18.
  • PMID: 16917073
    Horvath G, Schmid N, Fragoso MA, Schmid A, Conner GE, Salathe M, Wanner A: Epithelial organic cation transporters ensure pH-dependent drug absorption in the airway. Am J Respir Cell Mol Biol. 2007 Jan;36(1):53-60. doi: 10.1165/rcmb.2006-0230OC. Epub 2006 Aug 17.
  • PMID: 10497135
    Rosenborg J, Larsson P, Tegner K, Hallstrom G: Mass balance and metabolism of (3)HFormoterol in healthy men after combined i.v. and oral administration-mimicking inhalation. Drug Metab Dispos. 1999 Oct;27(10):1104-16.
  • PMID: 8099696
    Anderson GP: Formoterol: pharmacology, molecular basis of agonism, and mechanism of long duration of a highly potent and selective beta 2-adrenoceptor agonist bronchodilator. Life Sci. 1993;52(26):2145-60. doi: 10.1016/0024-3205(93)90729-m.
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