Peringatan Keamanan

Patients experiencing an overdose have presented with metabolic acidosis, hyperlactatemia, anxiety, palpitations, chest pain, sinus tachycardia, ST depression, hypokalemia, hypophosphatemia.A190450 Though patients may also present with seizures, angina, hypertension or hypotension, arrhythmia, headache, tremor, muscle cramps, dry mouth, nausea, dizziness, fatigue, malaise, insomnia, and hyperglycemia.L11548 Patients should be given symptomatic and supportive treatment which may include intravenous fluids, potassium supplementation, a cardioselective beta-blocker, and cardiac monitoring.A190450,L11548

Data regarding the LD50 of salmeterol is not readily available.L11569

Salmeterol

DB00938

small molecule approved

Deskripsi

Salmeterol is a long-acting beta-2 adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD.L11545,L11548,L11551,L11554,L11557 It has a longer duration of action than the short-acting beta-2 adrenergic receptor agonist, salbutamol.A190459 Salmeterol was first described in the literature in 1988.A190477 Salmeterol's structure is similar to salbutamol's with an aralkyloxy-alkyl substitution on the amine.A183737

Salmeterol was granted FDA approval on 4 February 1994.L11542

Struktur Molekul 2D

Berat 415.5656
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of salmeterol is 5.5h.[A183737]
Volume Distribusi In asthmatic patients, the volume of distribution of the central compartment is 177L and the volume of distribution of the peripheral compartment is 3160L.[A190459]
Klirens (Clearance) The average clearance of salmeterol in a group of asthmatic patients was 392L/h.[A190459] Further data regarding the clearance of salmeterol is not readily available.[L11545,L11548,L11551,L11554,L11557]

Absorpsi

In asthmatic patients, a 50µg dose of inhaled salmeterol powder reaches a Cmax of 47.897pg/mL, with a Tmax of 0.240h, and an AUC of 156.041pg/mL/h.A190459

Metabolisme

Salmeterol is predominantly metabolized by CYP3A4 to alpha-hydroxysalmeterol,A183737 and minorly by an unknown mechanism to an O-dealkylated metabolite.A190438

Rute Eliminasi

Salmeterol is 57.4% eliminated in the fecesL11548 and 23% in the urine.A183737 Less than 5% of a dose is eliminated in the urine as unchanged salmeterol.A183737

Interaksi Obat

1365 Data
Loxapine The therapeutic efficacy of Salmeterol can be decreased when used in combination with Loxapine.
Valsartan Salmeterol may decrease the antihypertensive activities of Valsartan.
Ramipril Salmeterol may decrease the antihypertensive activities of Ramipril.
Remikiren Salmeterol may decrease the antihypertensive activities of Remikiren.
Olmesartan Salmeterol may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Salmeterol may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Salmeterol may decrease the antihypertensive activities of Minoxidil.
Fosinopril Salmeterol may decrease the antihypertensive activities of Fosinopril.
Trandolapril Salmeterol may decrease the antihypertensive activities of Trandolapril.
Benazepril Salmeterol may decrease the antihypertensive activities of Benazepril.
Candoxatril Salmeterol may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Salmeterol may decrease the antihypertensive activities of Mecamylamine.
Lisinopril Salmeterol may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Salmeterol may decrease the antihypertensive activities of Nitroglycerin.
Metyrosine Salmeterol may decrease the antihypertensive activities of Metyrosine.
Cryptenamine Salmeterol may decrease the antihypertensive activities of Cryptenamine.
Perindopril Salmeterol may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Salmeterol may decrease the antihypertensive activities of Candesartan cilexetil.
Fenoldopam Salmeterol may decrease the antihypertensive activities of Fenoldopam.
Quinapril Salmeterol may decrease the antihypertensive activities of Quinapril.
Telmisartan Salmeterol may decrease the antihypertensive activities of Telmisartan.
Deserpidine Salmeterol may decrease the antihypertensive activities of Deserpidine.
Pentolinium Salmeterol may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Salmeterol may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Salmeterol may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Salmeterol may decrease the antihypertensive activities of Epoprostenol.
Cilazapril Salmeterol may decrease the antihypertensive activities of Cilazapril.
Saprisartan Salmeterol may decrease the antihypertensive activities of Saprisartan.
Spirapril Salmeterol may decrease the antihypertensive activities of Spirapril.
Tienilic acid Salmeterol may decrease the antihypertensive activities of Tienilic acid.
Debrisoquine Salmeterol may decrease the antihypertensive activities of Debrisoquine.
Diethylnorspermine Salmeterol may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Salmeterol may decrease the antihypertensive activities of Temocapril.
Hexamethonium Salmeterol may decrease the antihypertensive activities of Hexamethonium.
Nicorandil Salmeterol may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Salmeterol may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Salmeterol may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Salmeterol may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Salmeterol may decrease the antihypertensive activities of Imidapril.
BQ-123 Salmeterol may decrease the antihypertensive activities of BQ-123.
Dihydralazine Salmeterol may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Salmeterol may decrease the antihypertensive activities of Zofenopril.
Guanoxan Salmeterol may decrease the antihypertensive activities of Guanoxan.
Delapril Salmeterol may decrease the antihypertensive activities of Delapril.
Vincamine Salmeterol may decrease the antihypertensive activities of Vincamine.
Linsidomine Salmeterol may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Salmeterol may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Salmeterol may decrease the antihypertensive activities of Tolonidine.
Endralazine Salmeterol may decrease the antihypertensive activities of Endralazine.
Cadralazine Salmeterol may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Salmeterol may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Salmeterol may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Salmeterol may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Salmeterol may decrease the antihypertensive activities of Guanoclor.
Muzolimine Salmeterol may decrease the antihypertensive activities of Muzolimine.
Xipamide Salmeterol may decrease the antihypertensive activities of Xipamide.
Candesartan Salmeterol may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Salmeterol may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Salmeterol may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Salmeterol may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Salmeterol may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Salmeterol may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Salmeterol may decrease the antihypertensive activities of Quinaprilat.
Bosentan Salmeterol may decrease the antihypertensive activities of Bosentan.
Hydralazine Salmeterol may decrease the antihypertensive activities of Hydralazine.
Sitaxentan Salmeterol may decrease the antihypertensive activities of Sitaxentan.
Pinacidil Salmeterol may decrease the antihypertensive activities of Pinacidil.
Macitentan Salmeterol may decrease the antihypertensive activities of Macitentan.
Aliskiren Salmeterol may decrease the antihypertensive activities of Aliskiren.
Manidipine Salmeterol may decrease the antihypertensive activities of Manidipine.
Naftopidil Salmeterol may decrease the antihypertensive activities of Naftopidil.
Dexniguldipine Salmeterol may decrease the antihypertensive activities of Dexniguldipine.
Amlodipine Salmeterol may decrease the antihypertensive activities of Amlodipine.
Azilsartan medoxomil Salmeterol may decrease the antihypertensive activities of Azilsartan medoxomil.
Desmopressin The risk or severity of hypertension can be increased when Desmopressin is combined with Salmeterol.
Icosapent The risk or severity of hypertension can be increased when Icosapent is combined with Salmeterol.
Amphetamine The risk or severity of hypertension can be increased when Amphetamine is combined with Salmeterol.
Midodrine The risk or severity of hypertension can be increased when Midodrine is combined with Salmeterol.
Bethanidine Salmeterol may decrease the antihypertensive activities of Bethanidine.
Mesalazine The risk or severity of hypertension can be increased when Mesalazine is combined with Salmeterol.
Etomidate The risk or severity of hypertension can be increased when Etomidate is combined with Salmeterol.
Zolmitriptan The risk or severity of hypertension can be increased when Zolmitriptan is combined with Salmeterol.
Indomethacin The risk or severity of hypertension can be increased when Indomethacin is combined with Salmeterol.
Phenylephrine The risk or severity of hypertension can be increased when Phenylephrine is combined with Salmeterol.
Methylphenidate The risk or severity of hypertension can be increased when Methylphenidate is combined with Salmeterol.
Nabumetone The risk or severity of hypertension can be increased when Nabumetone is combined with Salmeterol.
Tenoxicam The risk or severity of hypertension can be increased when Tenoxicam is combined with Salmeterol.
Tolmetin The risk or severity of hypertension can be increased when Tolmetin is combined with Salmeterol.
Doxapram The risk or severity of hypertension can be increased when Doxapram is combined with Salmeterol.
Fenoprofen The risk or severity of hypertension can be increased when Fenoprofen is combined with Salmeterol.
Sulindac The risk or severity of hypertension can be increased when Sulindac is combined with Salmeterol.
Metaraminol The risk or severity of hypertension can be increased when Metaraminol is combined with Salmeterol.
Guanabenz Salmeterol may decrease the antihypertensive activities of Guanabenz.
Dexmedetomidine The risk or severity of hypertension can be increased when Dexmedetomidine is combined with Salmeterol.
Sumatriptan The risk or severity of hypertension can be increased when Sumatriptan is combined with Salmeterol.
Flurbiprofen The risk or severity of hypertension can be increased when Flurbiprofen is combined with Salmeterol.
Methoxamine The risk or severity of hypertension can be increased when Methoxamine is combined with Salmeterol.
Etodolac The risk or severity of hypertension can be increased when Etodolac is combined with Salmeterol.
Sulfasalazine The risk or severity of hypertension can be increased when Sulfasalazine is combined with Salmeterol.
Carprofen The risk or severity of hypertension can be increased when Carprofen is combined with Salmeterol.

Target Protein

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

Referensi & Sumber

Synthesis reference: Panayiotis Procopiou, "Novel process for preparing salmeterol." U.S. Patent US20030162840, issued August 28, 2003.
Artikel (PubMed)
  • PMID: 11825095
    Cazzola M, Testi R, Matera MG: Clinical pharmacokinetics of salmeterol. Clin Pharmacokinet. 2002;41(1):19-30. doi: 10.2165/00003088-200241010-00003.
  • PMID: 7905380
    Manchee GR, Barrow A, Kulkarni S, Palmer E, Oxford J, Colthup PV, Maconochie JG, Tarbit MH: Disposition of salmeterol xinafoate in laboratory animals and humans. Drug Metab Dispos. 1993 Nov-Dec;21(6):1022-8.
  • PMID: -
    Prentice B, Jaffe A, Thomas P: Beta2 Receptor Agonists Parnham M. (eds) Compendium of Inflammatory Diseases.
  • PMID: 23131487
    Manara A, Hantson P, Vanpee D, Thys F: Lactic acidosis following intentional overdose by inhalation of salmeterol and fluticasone. CJEM. 2012 Nov;14(6):378-81. doi: 10.2310/8000.2012.110581.
  • PMID: 28374512
    Soulele K, Macheras P, Karalis V: Pharmacokinetic analysis of inhaled salmeterol in asthma patients: Evidence from two dry powder inhalers. Biopharm Drug Dispos. 2017 Oct;38(7):407-419. doi: 10.1002/bdd.2077. Epub 2017 Jul 12.
  • PMID: 2904183
    Ullman A, Svedmyr N: Salmeterol, a new long acting inhaled beta 2 adrenoceptor agonist: comparison with salbutamol in adult asthmatic patients. Thorax. 1988 Sep;43(9):674-8. doi: 10.1136/thx.43.9.674.

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