1.What is Spironolactone?
Definition:
Spironolactone is a mineralocorticoid receptor blocker and a potassium-sparing diuretic (water pill) used to treat essential hypertension, congestive heart failure, hypokalemia, fluid retention (edema), and hyperaldosteronism. Also, its off-label uses include acne and hirsutism.
Spironolactone is a prescription drug and is available in the form of oral tablets and suspensions. It is safe, easy to use, and comes at an affordable price.
Spironolactone was developed in 1957 and approved by the U.S FDA in 1960. It is available in BP/IP/USP pharmaceutical grades.
Chemical & Physical Properties:
Chemical structure:
Molecular weight: 416.6
Molecular formula: C24H32O4S
CAS number:52-01-7
DrugBank accession number: DB00421
IUPAC Name: S-[(7R,8R,9S,10R,13S,14S,17R)-10,13-dimethyl-3,5'-dioxospiro[2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-17,2'-oxolane]-7-yl] ethanethioate
Color: White or yellowish-white powder.
Melting point: 134.5 °C
Boiling point: 201
Storage temperature: Below 77°F (25°C)
Solubility: Insoluble in water, soluble in most organic solvents.
Brand name:
Aldactone® (spironolactone tablets, USP)
2.Spironolactone Mechanism of action
Spironolactone is a competitive inhibitor of aldosterone activity and blocks its pathophysiologic effects. Blockage of aldosterone results in diuretic and antihypertensive effects via reduction of sodium-water retention in the distal convoluted tubule.
Additionally, spironolactone antagonizes the effects of androgen and progesterone receptors, which results in reduced sebum production.
3.Spironolactone forms and specifications
Spironolactone potassium
Spironolactone is a potassium-sparing diuretic that inhibits the exchange of sodium for potassium in the distal convoluted tubule and stops its excretion by the body; therefore, it is indicated to treat or prevent hypokalemia. Also, it prevents fluid retention, and it is prescribed to reduce swelling in nephrotic syndrome and liver conditions. It may be given alone or with other diuretics.
However, its levels should be monitored as hypokalemia may occur with a higher intake of food rich in it or its supplements.
Spironolactone prostaglandins
Concomitant use of spironolactone and non-steroidal anti-inflammatory drugs (NSAIDs) such as indomethacin and aspirin may attenuate the diuretic and antihypertensive effects of spironolactone. This is due to the inhibition of intrarenal prostaglandin synthesis.
Therefore, patients should be advised about the possible interaction when both medications are taken together, and kidney function should be monitored as well.
4.Spironolactone vs. Accutane
Accutane® is the brand name of isotretinoin, which is used for the treatment and prevention of acne. Likewise, one of spironolactone's off-label uses is the treatment of acne.
Both drugs have the same effects in acne treatment; however, the mechanism of action is different. Accutane is discontinued in the U.S, but generic formulations of the drug are still available.
5.Uses of Spironolactone
Spironolactone acne
Spironolactone off-label's uses include acne vulgaris because it blocks androgen and progesterone receptors and inhibits sebocyte proliferation. Therefore, it is currently used as a non-antibiotic alternative to classical acne treatments in women with persistent or late-onset acne.
Spironolactone for hair loss
Spironolactone off-labels and non-FDA approved uses include treatment of female pattern hair loss caused by androgenic alopecia, where hair loss is associated with overproduction in male sex hormones.
Spironolactone blocks the binding of dihydrotestosterone to its androgen receptors, reduces testosterone production, and increases its metabolic clearance rate.
Spironolactone for heart failure
Spironolactone is FDA approved for the treatment of heart failure with reduced ejection fraction (HFrEF) & preserved ejection fraction (HFpEF) with resistant hypertension, as it lowers high blood pressure levels, reduces fluid retention overload, and significantly reduces risks of mortality and morbidity in patients with severe heart failure.
Spironolactone is indicated in patients with congestive heart failure taking digitalis when other treatment strategies aren't suitable.
According to guidelines, spironolactone is recommended to be added to angiotensin-converting enzyme (ACE) inhibitors, as both work synergistically to provide further blockage of the renin-angiotensin-aldosterone system (RAAS).
6.Spironolactone Manufacturing process
According to the spironolactone's label, the inactive ingredients included in the oral tablet are calcium sulfate, corn starch, flavor, hypromellose, iron oxide, magnesium stearate, polyethylene glycol, povidone, and titanium dioxide.
7.Spironolactone dosage
Spironolactone oral tablets are available in 25 mg, 50 mg, or 100 mg strengths. Also, it is available as an oral suspension at a dose of 5 mg/mL, and dosage varies according to condition.
The maximum daily dosage depends on indication as follows:
50 mg for HFrEF
100 mg for resistant hypertension
400 mg for edema caused by liver cirrhosis/ 200 mg for edema caused by nephrotic syndrome
400 mg for primary hyperaldosteronism
200 mg for hirsutism and acne vulgaris
Dosage is adjusted according to indication and medical status (i.e., renal function disorders).
8.Spironolactone Side effects
The reported side effects include:
Diarrhea and abdominal cramping
Nausea and vomiting
Dizziness
Hyperkalemia
Menstrual irregularities
Breast complaints
9.Spironolactone Active Pharmaceutical Ingredients (API) bulk price
The average price is $331 (USD/kg)
10.Spironolactone Manufacturers in china
Below are some trustworthy Spironolactone Manufacturers in China who are professional in making active pharma ingredients.
Arshine Pharmaceutical Co., Ltd.
A leading manufacturer in life science raw material production based in China and with more than 2000 products in the health, human API, and pharmaceutical products. The company's business has developed into one of the major pharmaceuticals export enterprises in southern China and with a global main sales market in more than 100 countries in South America (e.g., the United States & Canada), Australia, Europe (e.g., the United Kingdom), South Asia (e.g., India), and Africa.
Contact number: +86-731-88503670
Address: lock 14, No.100, Luyun Road, Changsha 410205, China.
NINGBO NUOBAI PHARMACEUTICAL CO., LTD.
Nuobai Pharm is a supplier of health products, APIs, chemicals, intermediates, and pharmaceuticals-related businesses based in China. The company provides GMP consultant service, and their main sales market includes South America, Europe, Asia, and Africa.
Contact number: +86-574-87260242
Address：21 Jiangxia St., Ningbo 315000, Zhejiang, China
Business cooperation email：BD@nbpharm.com
Tianjin Harmony Technology Development company
A well-known manufacturer of Active Pharmaceutical Ingredients (APIs), pharmaceutical intermediates, and high-quality chemicals manufactured according to GMP criteria and export standards with a worldwide sales market that includes Asia, Europe, Africa, and Australia.
Contact number: +86-22-23697098
Address: ziyuanlu No.6 Nankai District, Tianjin, China
Shanghai Yst Pharma company
The company is a supplier of API, chemical intermediates, and pharmaceutical products based in China. The company focuses on the quality of products and services to fulfill customers' requirements in several countries worldwide.
11.FAQ
Does spironolactone affect weight?
There isn't much scientific evidence regarding the specific properties of spironolactone for weight loss; however, as a diuretic, it helps reducing weight associated with water retention. This effect is limited, and when fluids re-accumulate, the weight can back to normal.
Does spironolactone speed up your metabolism?
Animal studies showed that spironolactone improves glucose and lipid metabolism by ameliorating hepatic steatosis and inflammation, suppressing enhanced gluconeogenesis. Likewise, it enhances the secretion of insulin in metabolic syndrome.
How quickly does spironolactone work?
Spironolactone reaches peak plasma concentrations within 0.5-1.5 hours after oral administration, and the duration of action after multiple doses is 2-3 days.
References
https://pubchem.ncbi.nlm.nih.gov/compound/Spironolactone
https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/012151s062lbl.pdf
https://www.ncbi.nlm.nih.gov/books/NBK554421/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5440451/
https://www.drugs.com/spironolactone.html
https://go.drugbank.com/drugs/DB00421
https://www.rxlist.com/aldactone-drug.htm
https://www.rxlist.com/aldactone_vs_accutane/drugs-condition.htm
https://www.pharmasources.com/products/searchKey-Spironolactone
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4508078/
https://www.healthline.com/health/spironolactone-for-hair-loss
https://www.pharmacompass.com/price/spironolactone
https://www.pdr.net/drug-summary/Aldactone-spironolactone-978.2934
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