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spironolactone

 
Dictionary: spi·ro·no·lac·tone   (spī'rə-nō-lăk'tōn, spī-rō'-, spī-rŏn'ə-) pronunciation
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n.
A steroid derivative, C24H32O4S, that blocks the action of aldosterone, used as a diuretic primarily in the treatment of hypertension.

[Alteration of spirolactone : Latin spīra, coil; see spiral + LACTONE.]


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Dental Dictionary: spironolactone
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n

trade names: Aldactone, Spirozide; drug class: potassium-sparing diuretic; action: competes with aldosterone at receptor sites in distal tubule, resulting in excretion of sodium chloride and water and retention of potassium and phosphate; uses: treatment for edema, hypertension, diuretic-induced hypokalemia, and cirrhosis of the liver with ascites.

Drug Info: Spironolactone
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Brand names: Aldactone®Spirono™

Chemical formula:



Spironolactone Oral tablet

What is this medicine?

SPIRONOLACTONE is a diuretic. It helps you make more urine and to lose excess water from your body. This medicine is used to treat high blood pressure, and edema or swelling from heart, kidney, or liver disease. It is also used to treat patients who make too much aldosterone or have low potassium.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•high blood level of potassium
•kidney disease or trouble making urine
•liver disease
•an unusual or allergic reaction to spironolactone, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a drink of water. Follow the directions on your prescription label. You may take this medicine with or without food. If it upsets your stomach, take it with food or milk. Do not take your medicine more often than directed. Remember that you will need to pass more urine after taking this medicine. Do not take your doses at a time of day that will cause you problems. Do not take at bedtime.

Talk to your pediatrician regarding the use of this medicine in children. While this drug may be prescribed for selected conditions, precautions do apply.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•eplerenone

This medicine may also interact with the following medications:
•corticosteroids
•digoxin
•lithium
•medicines for high blood pressure like ACE inhibitors
•skeletal muscle relaxants like tubocurarine
•NSAIDs, medicines for pain and inflammation, like ibuprofen or naproxen
•potassium products like salt substitute or supplements
•pressor amines like norepinephrine
•some diuretics

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. Check your blood pressure as directed. Ask your doctor what your blood pressure should be, and when you should contact them.

You may need to be on a special diet while taking this medicine. Ask your doctor. Also, ask how many glasses of fluid you need to drink a day. You must not get dehydrated.

This medicine may make you feel confused, dizzy or lightheaded. Drinking alcohol and taking some medicines can make this worse. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not sit or stand up quickly.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions such as skin rash or itching, hives, swelling of the lips, mouth, tongue, or throat
•black or tarry stools
•fast, irregular heartbeat
•fever
•muscle pain, cramps
•numbness, tingling in hands or feet
•trouble breathing
•trouble passing urine
•unusual bleeding
•unusually weak or tired

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•change in voice or hair growth
•confusion
•dizzy, drowsy
•dry mouth, increased thirst
•enlarged or tender breasts
•headache
•irregular menstrual periods
•sexual difficulty, unable to have an erection
•stomach upset

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store below 25 degrees C (77 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

Veterinary Dictionary: spironolactone
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A competitive antagonist of aldosterone, used as a diuretic. It increases resorption of sodium in the distal renal tubules.

Wikipedia: Spironolactone
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Spironolactone
Systematic (IUPAC) name
7α-Acetylthio-3-oxo-17α-pregn-4-ene-21,17-carbolactone
OR
(1' S,2R,2' R,9' R,10' R,11' S,15' S)-9'-(acetylsulfanyl)-2',15'-dimethylspiro[oxolane-2,14'-tetracyclo[8.7.0.02,7.011,15]heptadecan]-6'-ene-5,5'-dione
Identifiers
CAS number 52-01-7
ATC code C03DA01
PubChem 5833
DrugBank APRD01234
ChemSpider 5628
Chemical data
Formula C24H32O4S 
Mol. mass 416.574 g/mol
SMILES eMolecules & PubChem
Synonyms Aldactone
Spirotone
Spirolactone
Pharmacokinetic data
Bioavailability  ?
Metabolism Hepatic
Half life 10 minutes
Excretion Urine, bile
Therapeutic considerations
Pregnancy cat.

B3(AU) C(US)
Legal status

POM(UK)
Routes Oral
 Y(what is this?)  (verify)

Spironolactone (marketed under the trade names Aldactone, Novo-Spiroton, Aldactazide, Spiractin, Spirotone, Verospiron or Berlactone) is a diuretic and is used as an antiandrogen.

It is a synthetic 17-lactone drug that is a renal competitive aldosterone antagonist in a class of pharmaceuticals called potassium-sparing diuretics, used primarily to treat heart failure, ascites in patients with liver disease, low-renin hypertension, hypokalemia, secondary hyperaldosteronism (such as occurs with hepatic cirrhosis), and Conn's syndrome (primary hyperaldosteronism). On its own, spironolactone is only a weak diuretic because its effects target the distal nephron (collecting tubule), where urine volume can only be slightly modified; but it can be combined with other diuretics to increase efficacy. About one person in one hundred with hypertension has elevated levels of aldosterone; in these persons, the antihypertensive effect of spironolactone may exceed that of complex combined regimens of other antihypertensives. Due to its antiandrogen effect, it can also be used to treat hirsutism, and it is a common component in hormone therapy for male-to-female transsexual and transgender people. It is also used for treating hair loss and acne in women, and can be used as a topical medication for treatment of male baldness. It is commonly used to treat symptoms of polycystic ovary syndrome (PCOS) such as excess facial hair and acne. It can also cause gynecomastia in males and should never be given with potassium supplementation for fear of the development of hyperkalemia.

Contents

Mechanism of action

Spironolactone inhibits the effect of aldosterone by competing for intracellular aldosterone receptors in the distal convoluted tubule cells (it actually works on aldosterone receptors in the collecting duct). This decreases the reabsorption of sodium and water, while decreasing the secretion of potassium. Spironolactone has a fairly slow onset of action, taking several days to develop, and, so, the effect diminishes slowly. This is because steroid pathways alter gene transcription, and it will take several days for the gene products to change (in this case the ENaC and ROMK channels will be decreased). Spironolactone has anti-androgen activity by binding to the androgen receptor and preventing it from interacting with dihydrotestosterone.[1]

Pharmacokinetics

Spironolactone is a synthetic steroid that acts as a competitive antagonist to aldosterone. Its onset and duration of action are determined by the kinetics of the aldosterone response in the target tissue. Substantial inactivation of spironolactone occurs in the liver and hepatitis or cirrhosis can lead to secondary aldosteronism, which is one indication for treatment. Overall, spironolactone has a rather slow onset of action, requiring several days before full therapeutic effect is achieved.

Mortality and morbidity benefit in severe heart failure

Spironolactone was shown to have a significant mortality and morbidity benefit in the Randomized Aldactone Evaluation Study (RALES), which studied people with severe congestive heart failure (New York Heart Association functional class III or IV).[2] Patients in the study arm of the trial (those receiving spironolactone) had a relative risk of death (when compared to the placebo group) equal to 0.70 or a 30% relative risk reduction. Patients in the study arm also had fewer symptoms of CHF and were hospitalized less frequently.

The mechanism of this effect is also mediated by inhibiting aldosterone, which in conjunction with heart failure leads to myocardial remodeling including fibrosis, sodium retention, and vascular dysfunction.

Adverse effects and interactions

Spironolactone is associated with an increased risk of bleeding from the stomach and duodenum, but a causal relationship between the two has not been established.[3] Because it also affects androgen receptors and other steroid receptors, it can cause gynecomastia, menstrual irregularities and testicular atrophy. Other side-effects include ataxia, erectile dysfunction, drowsiness, and rashes. A carcinogenic effect has been demonstrated in rats. Spironolactone has been shown to be immunosuppressive in the treatment of sarcoidosis.[4]

Spironolactone often increases serum potassium levels and can cause hyperkalemia, a very serious condition. Therefore, it is recommended that people using this drug avoid potassium supplements and salt substitutes containing potassium. [5] Doctors usually recommend periodic screening of serum potassium levels and some patients may be advised to limit dietary consumption of potassium.

Research has also shown that spironolactone can interfere with the effectiveness of antidepressant treatment. The drug is actually (among its other receptor interactions) a mineralocorticoid (MR) antagonist, and has been found to reduce the effectiveness of antidepressant drugs in the treatment of major depression, it is presumed by interfering with normalization of the hypothalamic-pituitary-adrenal axis in patients receiving antidepressant therapy. [6]

Carcinogenicity

Studies of spironolactone and the related compound potassium canrenoate (which, like spironolactone, metabolizes to canrenone) in rats for one- to two-year periods show an increase in carcinogenesis in the thyroid gland, testes, liver, breasts, and myelocytic leukocytes. Mammalian cells, depending on the presence of metabolic activation, show mixed results for mutagenicity in vitro.[7] Doses relative to body weight were 10 to 150 mg per kg, which is ten to 500 times higher than normal doses for treating humans. In light of this research, Sandoz has recommended that unnecessary use of spironolactone be avoided.

Other potential benefits

It has been suggested that spironolactone can reduce the risk of Alzheimer's disease. In one study [8], researchers observed a reduction in the risk of Alzheimer's specifically associated with potassium-sparing diuretics. Unpublished findings from other studies, including the Gothenberg Study have suggested that higher potassium levels may be associated with a lower risk of dementia.

See also

References

  1. ^ Berardesca, E; Gabba P, Ucci G, Borroni G, Rabbiosi G. (1988). "Topical spironolactone inhibits dihydrotestosterone receptors in human sebaceous glands: an autoradiographic study in subjects with acne vulgaris". Int J Tissue React. 10 (2): 115–119. PMID 2972662. http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2972662&dopt=Abstract. Retrieved 2007-03-15. 
  2. ^ Pitt B, Zannad F, Remme W, Cody R, Castaigne A, Perez A, Palensky J, Wittes J (1999). "The effect of spironolactone on morbidity and mortality in patients with severe heart failure. Randomized Aldactone Evaluation Study Investigators". N Engl J Med 341 (10): 709–17. doi:10.1056/NEJM199909023411001. PMID 10471456. http://content.nejm.org/cgi/content/full/341/10/709. 
  3. ^ Verhamme KMC, Mosis G, Dieleman JP, et al. (2006). "Spironolactone and risk of upper gastrointestinal events: population based case-control study". Brit Med J 333 (7563): 330–3. doi:10.1136/bmj.38883.479549.2F. PMID 16840442. 
  4. ^ Wandelt-Freerksen E. (1977). "Aldactone in the treatment of sarcoidosis of the lungs". JZ Erkr Atmungsorgane. 149(1): 156–9. PMID 607621. http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&dopt=AbstractPlus&list_uids=607621&query_hl=22&itool=pubmed_DocSum. Retrieved 2007-05-02. 
  5. ^ "Advisory Statement" (pdf). Klinge Chemicals / LoSalt. http://www.losalt.com/docs/lo_salt_web_advice.pdf. Retrieved 2007-03-15. 
  6. ^ Holsboer, F. The Rationale for Corticotropin-Releasing Hormone Receptor (CRH-R) Antagonists to Treat Depression and Anxiety. J. Psychiatr. Res. 33, 181–214 (1999)
  7. ^ "Spironolactone RX Monograph" (html). Sandoz Inc.. http://dailymed.nlm.nih.gov/dailymed/fdaDrugXsl.cfm?id=2479&type=display. Retrieved 2007-05-02. 
  8. ^ [Antihypertensive Medication Use and Incident Alzheimer Disease http://archneur.ama-assn.org/cgi/content/full/63.5/noc60013v1]

External links

v • d • e
Antihypertensives: diuretics (C03)
Sulfonamides
(except EA)
Thiazide-likes (primarily DCT)
Potassium-sparing (at CD)
Spironolactone# • Eplerenone • Potassium canrenoate • Canrenone
Osmotic diuretics (PT, DL)
VAs (DCT and CD)
Other
#WHO-EM. †Undergoing clinical trials, not FDA approved. ‡Withdrawn from market. §Development halted.
v • d • e
Sex hormones and related agents (primarily G03, also L02, H01C) – human endogenous in SMALL CAPS
#WHO-EM. †Undergoing clinical trials, not FDA approved. ‡Withdrawn from market. §Development halted.

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Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2009. Published by Houghton Mifflin Company. All rights reserved.  Read more
Dental Dictionary. Mosby's Dental Dictionary. Copyright © 2004 by Elsevier, Inc. All rights reserved.  Read more
Drug Info. Gold Standard. Copyright © 2008 by Gold Standard. All rights reserved.  Read more
Veterinary Dictionary. Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.  Read more
Wikipedia. This article is licensed under the Creative Commons Attribution/Share-Alike License. It uses material from the Wikipedia article "Spironolactone".  Read more