Peringatan Keamanan

The oral LD50 of spironolactone is greater than 1000 mg/kg in mice, rats, and rabbits.L44602

Acute overdosage of ALDACTONE may be manifested by drowsiness, mental confusion, maculopapular or erythematous rash, nausea, vomiting, dizziness, or diarrhea. Rarely, instances of hyponatremia, hyperkalemia,or hepatic coma may occur in patients with severe liver disease, but these are unlikely due to acute overdosage. Hyperkalemia may occur, especially in patients with impaired renal function. In case of an overdose, vomiting may be induced and gastric lavage may be instituted. As there is no specific antidote, treatment is supportive to maintain hydration, electrolyte balance, and vital functions. Patients who have renal impairment may develop hyperkalemia. In such cases, discontinue spironolactone.L44602

Spironolactone

DB00421

small molecule approved

Deskripsi

Spironolactone is a potassium-sparing diuretic. It binds to mineralocorticoid receptors and functions as aldosterone antagonists.A178192 It promotes sodium and water excretion and potassium retention.A11837 Spironolactone was originally developed purely for this ability before other pharmacodynamic properties of the drug were discovered.A11837, A178246 It is indicated to treat several conditions, including heart failure, edema, hyperaldosteronism, and hypertension.L44602 Off-label uses of spironolactone include hirsutism, female pattern hair loss, and adult acne vulgaris.A178135, A261025

Spironolactone was developed in 1957, marketed in 1959, and approved by the FDA on January 21, 1960.A178243, L6187

Struktur Molekul 2D

Berat 416.573
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean half-life of spironolactone is 1.4 hours. The mean half-life values of its metabolites, including canrenone, TMS, and HTMS are 16.5, 13.8, and 15 hours, respectively.[L44602]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The mean time to reach peak plasma concentration of spironolactone and the active metabolite, canrenone, in healthy volunteers is 2.6 and 4.3 hours, respectively. Food increased the bioavailability of spironolactone (as measured by AUC) by approximately 95.4%.L44602

Metabolisme

Spironolactone is rapidly and extensively metabolized to form different metabolites. A group of metabolites are formed when sulfur of spironolactone is removed, such as canrenone. Sulfur is retained in another group of metabolites, including 7-alpha (?)-thiomethylspironolactone (TMS) and 6-beta (ß)-hydroxy-7-alpha (?)-thiomethylspirolactone (HTMS).L44602 Spironolactone is firstly deacetylated to 7-?-thiospironolactone.A178069, A178072, A178165 7-?-thiospironolactone is S-methylated to TMS, which is the primary metabolite,A11837, A178207, A261030 or dethioacetylated to canrenone.A178069, A178072, A261030 TMS and HTMS can be further metabolized.A178069, A178072, A261030 In humans, the potencies of TMS and 7-?-thiospirolactone in reversing the effects of the synthetic mineralocorticoid, fludrocortisone, on urinary electrolyte composition were approximately a third relative to spironolactone. However, since the serum concentrations of these steroids were not determined, their incomplete absorption and/or first-pass metabolism could not be ruled out as a reason for their reduced in vivo activities.L44602

Rute Eliminasi

The metabolites are excreted primarily in the urine and secondarily in bile.L44602 Metabolites of spironolactone are excreted in urine (42-56%) and in the feces (14.2-14.6%). No unmetabolized spironolactone is present in the urine.A178165

Interaksi Makanan

2 Data
  • 1. Avoid potassium-containing products. Potassium products increase the risk of hyperkalemia.
  • 2. Take with or without food. Food increases the bioavailability of spironolactone by approximately 95.4%. It should be taken at a consistent time in regards to food.

Interaksi Obat

1293 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Spironolactone is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Spironolactone is combined with Levodopa.
Risperidone Spironolactone may increase the hypotensive activities of Risperidone.
Reserpine Reserpine may increase the hypotensive activities of Spironolactone.
Chlorpromazine Chlorpromazine may decrease the antihypertensive activities of Spironolactone.
Cimetidine Spironolactone may increase the excretion rate of Cimetidine which could result in a lower serum level and potentially a reduction in efficacy.
Bosentan Spironolactone may increase the hypotensive activities of Bosentan.
Ketoconazole The risk or severity of hyperkalemia can be increased when Ketoconazole is combined with Spironolactone.
Quinidine Quinidine may decrease the antihypertensive activities of Spironolactone.
Midodrine The therapeutic efficacy of Midodrine can be decreased when used in combination with Spironolactone.
Bethanidine The therapeutic efficacy of Bethanidine can be decreased when used in combination with Spironolactone.
Isoetharine The therapeutic efficacy of Isoetharine can be decreased when used in combination with Spironolactone.
Etomidate The therapeutic efficacy of Etomidate can be decreased when used in combination with Spironolactone.
Norepinephrine The therapeutic efficacy of Norepinephrine can be decreased when used in combination with Spironolactone.
Phenylephrine The therapeutic efficacy of Phenylephrine can be decreased when used in combination with Spironolactone.
Phenylpropanolamine The therapeutic efficacy of Phenylpropanolamine can be decreased when used in combination with Spironolactone.
Clonidine The risk or severity of hypotension can be increased when Clonidine is combined with Spironolactone.
Metaraminol The therapeutic efficacy of Metaraminol can be decreased when used in combination with Spironolactone.
Guanabenz The therapeutic efficacy of Guanabenz can be decreased when used in combination with Spironolactone.
Dexmedetomidine The therapeutic efficacy of Dexmedetomidine can be decreased when used in combination with Spironolactone.
Epinephrine The therapeutic efficacy of Epinephrine can be decreased when used in combination with Spironolactone.
Tizanidine The therapeutic efficacy of Tizanidine can be decreased when used in combination with Spironolactone.
Methoxamine The therapeutic efficacy of Methoxamine can be decreased when used in combination with Spironolactone.
Orciprenaline The therapeutic efficacy of Orciprenaline can be decreased when used in combination with Spironolactone.
Dobutamine The therapeutic efficacy of Dobutamine can be decreased when used in combination with Spironolactone.
Pseudoephedrine The therapeutic efficacy of Pseudoephedrine can be decreased when used in combination with Spironolactone.
Benzphetamine The therapeutic efficacy of Benzphetamine can be decreased when used in combination with Spironolactone.
Ritodrine The therapeutic efficacy of Ritodrine can be decreased when used in combination with Spironolactone.
Terbutaline The therapeutic efficacy of Terbutaline can be decreased when used in combination with Spironolactone.
Bitolterol The therapeutic efficacy of Bitolterol can be decreased when used in combination with Spironolactone.
Oxymetazoline The therapeutic efficacy of Spironolactone can be decreased when used in combination with Oxymetazoline.
Salmeterol The therapeutic efficacy of Salmeterol can be decreased when used in combination with Spironolactone.
Methyldopa The therapeutic efficacy of Methyldopa can be decreased when used in combination with Spironolactone.
Formoterol The therapeutic efficacy of Formoterol can be decreased when used in combination with Spironolactone.
Albuterol The therapeutic efficacy of Salbutamol can be decreased when used in combination with Spironolactone.
Guanfacine The therapeutic efficacy of Guanfacine can be decreased when used in combination with Spironolactone.
Isoprenaline The therapeutic efficacy of Isoprenaline can be decreased when used in combination with Spironolactone.
Arbutamine The therapeutic efficacy of Arbutamine can be decreased when used in combination with Spironolactone.
Pergolide The therapeutic efficacy of Pergolide can be decreased when used in combination with Spironolactone.
Bromocriptine The therapeutic efficacy of Bromocriptine can be decreased when used in combination with Spironolactone.
Ergometrine The therapeutic efficacy of Ergometrine can be decreased when used in combination with Spironolactone.
Arformoterol The therapeutic efficacy of Arformoterol can be decreased when used in combination with Spironolactone.
Fenoterol The therapeutic efficacy of Fenoterol can be decreased when used in combination with Spironolactone.
Pirbuterol The therapeutic efficacy of Pirbuterol can be decreased when used in combination with Spironolactone.
Ephedra sinica root The therapeutic efficacy of Ephedra sinica root can be decreased when used in combination with Spironolactone.
Ephedrine The therapeutic efficacy of Ephedrine can be decreased when used in combination with Spironolactone.
Mephentermine The therapeutic efficacy of Mephentermine can be decreased when used in combination with Spironolactone.
Procaterol The therapeutic efficacy of Procaterol can be decreased when used in combination with Spironolactone.
Clenbuterol The therapeutic efficacy of Clenbuterol can be decreased when used in combination with Spironolactone.
Bambuterol The therapeutic efficacy of Bambuterol can be decreased when used in combination with Spironolactone.
4-Methoxyamphetamine The therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Spironolactone.
4-Bromo-2,5-dimethoxyphenethylamine The therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be decreased when used in combination with Spironolactone.
Metamfetamine The therapeutic efficacy of Metamfetamine can be decreased when used in combination with Spironolactone.
Phendimetrazine The therapeutic efficacy of Phendimetrazine can be decreased when used in combination with Spironolactone.
Celiprolol The risk or severity of hyperkalemia can be increased when Celiprolol is combined with Spironolactone.
Nebivolol The risk or severity of hyperkalemia can be increased when Nebivolol is combined with Spironolactone.
Lofexidine The therapeutic efficacy of Lofexidine can be decreased when used in combination with Spironolactone.
Indacaterol The therapeutic efficacy of Indacaterol can be decreased when used in combination with Spironolactone.
Amibegron The therapeutic efficacy of Amibegron can be decreased when used in combination with Spironolactone.
Nylidrin The risk or severity of hyperkalemia can be increased when Nylidrin is combined with Spironolactone.
Solabegron The therapeutic efficacy of Solabegron can be decreased when used in combination with Spironolactone.
Droxidopa The therapeutic efficacy of Droxidopa can be decreased when used in combination with Spironolactone.
Xylometazoline The therapeutic efficacy of Xylometazoline can be decreased when used in combination with Spironolactone.
Isometheptene The therapeutic efficacy of Isometheptene can be decreased when used in combination with Spironolactone.
Levonordefrin The therapeutic efficacy of Levonordefrin can be decreased when used in combination with Spironolactone.
Naphazoline The therapeutic efficacy of Naphazoline can be decreased when used in combination with Spironolactone.
Tetryzoline The therapeutic efficacy of Tetryzoline can be decreased when used in combination with Spironolactone.
Protokylol The therapeutic efficacy of Protokylol can be decreased when used in combination with Spironolactone.
Mirabegron The therapeutic efficacy of Mirabegron can be decreased when used in combination with Spironolactone.
Adrafinil The therapeutic efficacy of Adrafinil can be decreased when used in combination with Spironolactone.
Isoxsuprine The therapeutic efficacy of Isoxsuprine can be decreased when used in combination with Spironolactone.
Hexoprenaline The therapeutic efficacy of Hexoprenaline can be decreased when used in combination with Spironolactone.
Etilefrine The therapeutic efficacy of Etilefrine can be decreased when used in combination with Spironolactone.
Olodaterol The therapeutic efficacy of Olodaterol can be decreased when used in combination with Spironolactone.
Vilanterol The therapeutic efficacy of Vilanterol can be decreased when used in combination with Spironolactone.
Cirazoline The therapeutic efficacy of Cirazoline can be decreased when used in combination with Spironolactone.
Synephrine The therapeutic efficacy of Synephrine can be decreased when used in combination with Spironolactone.
Moxonidine The therapeutic efficacy of Moxonidine can be decreased when used in combination with Spironolactone.
Doxofylline The therapeutic efficacy of Doxofylline can be decreased when used in combination with Spironolactone.
Racepinephrine The therapeutic efficacy of Racepinephrine can be decreased when used in combination with Spironolactone.
DL-Methylephedrine The therapeutic efficacy of DL-Methylephedrine can be decreased when used in combination with Spironolactone.
Amitraz The therapeutic efficacy of Amitraz can be decreased when used in combination with Spironolactone.
Medetomidine The therapeutic efficacy of Medetomidine can be decreased when used in combination with Spironolactone.
Xylazine The therapeutic efficacy of Xylazine can be decreased when used in combination with Spironolactone.
Ractopamine The therapeutic efficacy of Ractopamine can be decreased when used in combination with Spironolactone.
Romifidine The therapeutic efficacy of Romifidine can be decreased when used in combination with Spironolactone.
Detomidine The therapeutic efficacy of Detomidine can be decreased when used in combination with Spironolactone.
Etafedrine The therapeutic efficacy of Etafedrine can be decreased when used in combination with Spironolactone.
Rilmenidine The therapeutic efficacy of Rilmenidine can be decreased when used in combination with Spironolactone.
Anisodamine The risk or severity of hyperkalemia can be increased when Anisodamine is combined with Spironolactone.
PF-00610355 The therapeutic efficacy of PF-00610355 can be decreased when used in combination with Spironolactone.
Ritobegron The therapeutic efficacy of Ritobegron can be decreased when used in combination with Spironolactone.
Abediterol The therapeutic efficacy of Abediterol can be decreased when used in combination with Spironolactone.
Tulobuterol The therapeutic efficacy of Tulobuterol can be decreased when used in combination with Spironolactone.
Dopexamine The therapeutic efficacy of Dopexamine can be decreased when used in combination with Spironolactone.
Batefenterol The therapeutic efficacy of Batefenterol can be decreased when used in combination with Spironolactone.
Higenamine The therapeutic efficacy of Higenamine can be decreased when used in combination with Spironolactone.
Reproterol The therapeutic efficacy of Reproterol can be decreased when used in combination with Spironolactone.
Levosalbutamol The therapeutic efficacy of Levosalbutamol can be decreased when used in combination with Spironolactone.
Octopamine The therapeutic efficacy of Octopamine can be decreased when used in combination with Spironolactone.

Target Protein

Mineralocorticoid receptor NR3C2
Glucocorticoid receptor NR3C1
Androgen receptor AR
Progesterone receptor PGR
Estrogen receptor ESR1
Nuclear receptor subfamily 1 group I member 2 NR1I2
Voltage-dependent L-type calcium channel CACNA1C

Referensi & Sumber

Synthesis reference: Giuseppe Bernini, "Process for preparing micronized spironolactone." U.S. Patent US4332721, issued July, 1975.
Artikel (PubMed)
  • PMID: 9144743
    Takamura N, Maruyama T, Ahmed S, Suenaga A, Otagiri M: Interactions of aldosterone antagonist diuretics with human serum proteins. Pharm Res. 1997 Apr;14(4):522-6.
  • PMID: 3675606
    LaCagnin LB, Lutsie P, Colby HD: Conversion of spironolactone to 7 alpha-thiomethylspironolactone by hepatic and renal microsomes. Biochem Pharmacol. 1987 Oct 15;36(20):3439-44.
  • PMID: 7895608
    Los LE, Pitzenberger SM, Ramjit HG, Coddington AB, Colby HD: Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites. Drug Metab Dispos. 1994 Nov-Dec;22(6):903-8.
  • PMID: 22468178
    Kim GK, Del Rosso JQ: Oral Spironolactone in Post-teenage Female Patients with Acne Vulgaris: Practical Considerations for the Clinician Based on Current Data and Clinical Experience. J Clin Aesthet Dermatol. 2012 Mar;5(3):37-50.
  • PMID: 363379
    Karim A: Spironolactone: disposition, metabolism, pharmacodynamics, and bioavailability. Drug Metab Rev. 1978;8(1):151-88. doi: 10.3109/03602537808993782.
  • PMID: 28024992
    Carone L, Oxberry SG, Twycross R, Charlesworth S, Mihalyo M, Wilcock A: Spironolactone. J Pain Symptom Manage. 2017 Feb;53(2):288-292. doi: 10.1016/j.jpainsymman.2016.12.320. Epub 2016 Dec 23.
  • PMID: 15947888
    Sica DA: Pharmacokinetics and pharmacodynamics of mineralocorticoid blocking agents and their effects on potassium homeostasis. Heart Fail Rev. 2005 Jan;10(1):23-9. doi: 10.1007/s10741-005-2345-1.
  • PMID: 2723123
    Gardiner P, Schrode K, Quinlan D, Martin BK, Boreham DR, Rogers MS, Stubbs K, Smith M, Karim A: Spironolactone metabolism: steady-state serum levels of the sulfur-containing metabolites. J Clin Pharmacol. 1989 Apr;29(4):342-7.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 361 • International brands: 7
Produk
  • 011054 Niacinamide 4% / Spironolactone 5%
    Gel • - • Topical • US
  • 011218 Niacinamide 2% / Spironolactone 5% / Tretinoin 0.025%
    Gel • - • Topical • US
  • 011220 Niacinamide 2% / Spironolactone 5% / Tretinoin 0.05%
    Gel • - • Topical • US
  • 011503 Dapsone 6% / Niacinamide 2% / Spironolactone 5%
    Gel • - • Topical • US
  • Aldactazide
    Tablet, film coated • - • Oral • US • Approved
  • Aldactazide
    Tablet, film coated • - • Oral • US • Approved
  • Aldactazide 25
    Tablet • - • Oral • Canada • Approved
  • Aldactazide 50
    Tablet • - • Oral • Canada • Approved
Menampilkan 8 dari 361 produk.
International Brands
  • Osyrol
  • Spiresis
  • Spiretic
  • Spiroctan
  • Uractone
  • Verospiron
  • Xenalon

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul