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Spironolactone
 
 
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Spironolactone (marketed under the trade names Aldactone, Novo-Spiroton, Spiractin, Spirotone, Verospiron or Berlactone) is a diuretic
Diuretic

A diuretic is any drug that elevates the rate of urination and thus provides a means of forced diuresis. There are several categories of diuretics....
 and is used as an antiandrogen
Antiandrogen

An antiandrogen, or androgen antagonist, is any of a group of hormone receptor antagonist compounds that are capable of preventing or inhibiting the biologic effects of androgens, male sex hormones, on normally responsive tissues in the body ....
.

It is a synthetic 17-lactone
Lactone

A lactone is a cyclic ester in organic chemistry . It is the condensation reaction product of an alcohol functional group and a carboxylic acid group in the same molecule....
 drug that is a renal competitive aldosterone antagonist
Aldosterone antagonist

Aldosterone antagonist refers to drugs which receptor antagonist the action of aldosterone at mineralocorticoid receptors. This group of drugs is often used as adjunctive therapy, in combination with other drugs, for the management of chronic heart failure....
 in a class of pharmaceuticals called potassium-sparing diuretic
Potassium-sparing diuretic

Potassium-sparing diuretics are diuretic drugs that do not promote the secretion of potassium into the urine.They are used as adjunctive therapy, together with other drugs, in the treatment of hypertension and management of congestive heart failure....
s, used primarily to treat heart failure, ascites
Ascites

In medicine , ascites is an accumulation of fluid in the peritoneal cavity. Although most commonly due to cirrhosis and severe liver disease, its presence can portend other significant medical problems....
 in patients with liver disease, low-renin
Renin

Renin , also known as Angiotensinogenase, is a circulating enzyme that participates in the body's renin-angiotensin system that mediates extracellular volume , and arterial vasoconstriction....
 hypertension
Hypertension

Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
, hypokalemia
Hypokalemia

Hypokalemia refers to the condition in which the concentration of potassium in the blood is low. The prefix hypo- means low . Kal refers to kalium, the Neo-Latin for potassium, and -emia means "in the blood."...
, and Conn's syndrome
Conn's syndrome

Primary aldosteronism, also known as primary hyperaldosteronism, is characterized by the overproduction of the mineralocorticoid hormone aldosterone by the adrenal glands....
 as well as high blood pressure.






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Encyclopedia


Spironolactone (marketed under the trade names Aldactone, Novo-Spiroton, Spiractin, Spirotone, Verospiron or Berlactone) is a diuretic
Diuretic

A diuretic is any drug that elevates the rate of urination and thus provides a means of forced diuresis. There are several categories of diuretics....
 and is used as an antiandrogen
Antiandrogen

An antiandrogen, or androgen antagonist, is any of a group of hormone receptor antagonist compounds that are capable of preventing or inhibiting the biologic effects of androgens, male sex hormones, on normally responsive tissues in the body ....
.

It is a synthetic 17-lactone
Lactone

A lactone is a cyclic ester in organic chemistry . It is the condensation reaction product of an alcohol functional group and a carboxylic acid group in the same molecule....
 drug that is a renal competitive aldosterone antagonist
Aldosterone antagonist

Aldosterone antagonist refers to drugs which receptor antagonist the action of aldosterone at mineralocorticoid receptors. This group of drugs is often used as adjunctive therapy, in combination with other drugs, for the management of chronic heart failure....
 in a class of pharmaceuticals called potassium-sparing diuretic
Potassium-sparing diuretic

Potassium-sparing diuretics are diuretic drugs that do not promote the secretion of potassium into the urine.They are used as adjunctive therapy, together with other drugs, in the treatment of hypertension and management of congestive heart failure....
s, used primarily to treat heart failure, ascites
Ascites

In medicine , ascites is an accumulation of fluid in the peritoneal cavity. Although most commonly due to cirrhosis and severe liver disease, its presence can portend other significant medical problems....
 in patients with liver disease, low-renin
Renin

Renin , also known as Angiotensinogenase, is a circulating enzyme that participates in the body's renin-angiotensin system that mediates extracellular volume , and arterial vasoconstriction....
 hypertension
Hypertension

Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the blood pressure is chronically elevated....
, hypokalemia
Hypokalemia

Hypokalemia refers to the condition in which the concentration of potassium in the blood is low. The prefix hypo- means low . Kal refers to kalium, the Neo-Latin for potassium, and -emia means "in the blood."...
, and Conn's syndrome
Conn's syndrome

Primary aldosteronism, also known as primary hyperaldosteronism, is characterized by the overproduction of the mineralocorticoid hormone aldosterone by the adrenal glands....
 as well as high blood pressure. On its own, spironolactone is only a weak diuretic, but it can be combined with other diuretics. 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 anti-androgen
Androgen

Androgen is the generic term for any natural or synthetic compound, usually a steroid hormone, that stimulates or controls the development and maintenance of masculine characteristics in vertebrates by binding to androgen receptors....
 effect, it can also be used to treat hirsutism
Hirsutism

Hirsutism or Frazonism or is defined as excessive and increased hair growth in women in locations where the occurrence of terminal hair normally is minimal or absent....
, and it is a common component in hormone therapy
Hormone replacement therapy (male-to-female)

Hormone replacement therapy for transgender and transsexual people replaces the hormones naturally occurring in their bodies with those of the other sex....
 for male-to-female transsexual
Transwoman

A transwoman is a male-to-female transsexual or transgender person and the term transwoman is preferred by many such individuals over various medical terms....
 and transgender
Transgender

Transgender is a general term applied to a variety of individuals, behaviors, and groups involving tendencies that diverge from the normative gender role commonly, but not always, assigned at birth, as well as the role traditionally held by society....
ed people. It is also used for treating hair loss
Alopecia

Alopecia or hair loss is the medical description of the loss of hair from the head or body, sometimes to the extent of baldness. Unlike the common cosmetic depilation of body hair, alopecia tends to be involuntary and unwelcome, e.g., androgenic alopecia....
 and acne
Acne

Acne is a group of skin rashes that have different causes.* Acne vulgaris - most commonly experienced around puberty, typically of the face and shoulders/chest...
 in women and can be used as a topical
Topical

In medicine, a topical medication is applied to body surface area such as the skin or mucous membranes, for example the vagina, anus, pharynx, eyes and ears....
 medication for treatment of male baldness
Baldness

Baldness involves the state of lacking hair where it often grows, especially on the head. The most common form of baldness is a progressive hair thinning condition called androgenic alopecia or "male pattern baldness" that occurs in adult male humans and other species....
.

Mechanism of action

Spironolactone inhibits the effect of aldosterone by competing for intracellular aldosterone receptors
Mineralocorticoid receptor

The mineralocorticoid receptor , also called aldosterone receptor, is officially labelled nuclear receptor subfamily 3, group C, member 2, and is a receptor with high affinity for mineralocorticoids....
 in the distal tubule
Distal convoluted tubule

The distal convoluted tubule is a portion of kidney nephron between the loop of Henle and the collecting duct system....
 cells (it actually works on aldosterone receptors in the collecting duct). This increases the excretion of water and sodium
Sodium

Sodium is an element which has the symbol Na , atomic number 11, atomic mass 23 amu , and a common oxidation number +1. Sodium is a soft, silvery white, highly reactive element and is a member of the alkali metals within "group 1" ....
, while decreasing the excretion of potassium. Spironolactone has a fairly slow onset of action, taking several days to develop, and similarly the effect diminishes slowly. Spironolactone has anti-androgen activity by binding to the androgen receptor
Androgen receptor

The androgen receptor , also known as NR3C4 , is a type of nuclear receptor which is activated by binding of either of the androgen hormones testosterone or dihydrotestosterone....
 and preventing it from interacting with dihydrotestosterone
Dihydrotestosterone

Dihydrotestosterone While DHT is best known for its roles in causing male pattern hair loss and prostate problems, it is crucial to virilization and is necessary to mitigate estrogen's effects in men....
.

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
Aldosterone

Aldosterone is a hormone that increases the reabsorption of sodium and water and the release of potassium in the kidneys. This increases the volume of fluid in the body, and drives blood pressure up....
 response in the target tissue. Substantial inactivation of spironolactone occurs in the liver. Over all, 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
Death

Death is the permanent termination of the biological functions that define a life organism. It refers to both a particular event and to the condition that results thereby....
 and morbidity benefit in the Randomized Aldactone Evaluation Study (RALES), which studied people with severe congestive heart failure (New York Heart Association functional class
New York Heart Association Functional Classification

The New York Heart Association Functional Classification provides a simple way of classifying the extent of Congestive heart failure. It places patients in one of four categories based on how much they are limited during physical activity; the limitations/symptoms are in regards to normal breathing and varying degrees in shortness of breath...
 III or IV). Patients in the study arm of the trial (those receiving spironolactone) had a relative risk
Relative risk

In statistics and mathematical epidemiology, relative risk is the risk of an event relative to exposure. Relative risk is a ratio of the probability of the event occurring in the exposed group versus a non-exposed group....
 of death (when compared to the placebo group) equal to 0.70 or a 30% relative risk reduction
Relative risk reduction

In epidemiolgy, the relative risk reduction is a measure calculated by dividing the absolute risk reduction by the control event rate.The relative risk reduction can be more useful than the absolute risk reduction in determining an appropriate treatment plan, because it accounts not only for the effectiveness of a proposed treatment, but al...
. 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 fibrosis, sodium retention, and vascular dysfunction.

Adverse effects and interactions

Spironolactone is associated with an increased risk of bleeding from the stomach
Stomach

In most mammals, the stomach is a hollow muscular organ of the gastrointestinal tract involved in the second phase of digestion, following mastication....
 and duodenum
Duodenum

The duodenum is the first section of the small intestine in most higher vertebrates, including mammals, reptiles, and birds. In fish, the divisions of the small intestine are not as clear and the terms anterior intestine or proximal intestine may be used instead of duodenum....
, but a causal relationship between the two has not been established. Because it also affects androgen receptor
Androgen receptor

The androgen receptor , also known as NR3C4 , is a type of nuclear receptor which is activated by binding of either of the androgen hormones testosterone or dihydrotestosterone....
s and other steroid receptors, it can cause gynecomastia
Gynecomastia

Gynecomastia, or gynaecomastia, is the development of abnormally large mammary glands in males resulting in breast enlargement, which can sometimes cause secretion of milk....
, menstrual irregularities and testicular atrophy. Other side effects include ataxia
Ataxia

Ataxia is a neurology sign and symptom consisting of gross lack of coordination of muscle movements. Ataxia is a non-specific clinical manifestation implying dysfunction of parts of the nervous system that coordinate movement, such as the cerebellum....
, erectile dysfunction
Erectile dysfunction

Erectile dysfunction is a sexual dysfunction characterized by the inability to develop or maintain an erection of the penis sufficient for satisfactory sexual performance....
, drowsiness and rash
Rash

A rash is a change of the skin which affects its color, appearance, or texture. A rash may be localized in one part of the body, or affect all the skin....
es. A carcinogen
Carcinogen

The term carcinogen refers to any substance, radionuclide or radiation that is an agent directly involved in the promotion of cancer or in the increase of its propagation....
ic effect has been demonstrated in rats. Spironolactone has been shown to be immunosuppressive
Immunosuppression

Immunosuppression involves an act that reduces the activation or efficacy of the immune system. Some portions of the immune system itself have immuno-suppressive effects on other parts of the immune system, and immunosuppression may occur as an adverse reaction to treatment of other conditions....
 in the treatment of sarcoidosis
Sarcoidosis

Sarcoidosis, also called sarcoid or Besnier-Boeck disease, is a multisystem disorder characterized by non-caseating granulomas . It most commonly arises in young adults....
.

Spironolactone often increases serum potassium
Potassium

Potassium is a chemical element. It has the symbol K , atomic number 19, and atomic mass 39.0983. Potassium was first isolated from potash, hence the name....
 levels and can cause hyperkalemia
Hyperkalemia

Hyperkalemia Hyperkalaemia is an elevated blood level of the electrolyte potassium. The prefix hyper- means high . The middle kal refers to kalium, which is neo-Latin for potassium....
, a potentially serious condition. Therefore, it is recommended that people using this drug avoid potassium supplements and salt substitutes containing potassium. 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
Antidepressant

An antidepressant is a psychiatric medication used for alleviating major depressive disorder or dysthymia. Drug groups known as MAOIs, tricyclics, and second-generation antidepressants such as SSRIs, and serotonin-norepinephrine reuptake inhibitors are particularly associated with the term....
 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, presumably by interfering with normalization of the hypothalamic-pituitary-adrenal axis
Hypothalamic-pituitary-adrenal axis

The hypothalamic-pituitary-adrenal axis , also known as thelimbic-hypothalamic-pituitary-adrenal axis , is a complex set of direct influences and feedback interactions among the hypothalamus , the pituitary gland , and the adrenal glands ....
 in patients receiving antidepressant therapy.

Carcinogenicity

Studies of spironolactone and the related compound potassium canrenoate
Potassium canrenoate

Potassium canrenoate or canrenoate potassium , the potassium salt of canrenoic acid, is an aldosterone antagonist.Like spironolactone, it is a prodrug, which is drug metabolism to canrenone in the body....
 (which, like spironolactone, metabolizes to canrenone
Canrenone

Canrenone is an aldosterone antagonist.The active form, and first metabolite of, Spironolactone....
) 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. 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
Alzheimer's disease

Alzheimer's disease , also called Alzheimer disease, Senile Dementia of the Alzheimer Type or simply Alzheimer's, is the most common form of dementia....
. In one study , 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
Dementia

Dementia is the progressive decline in cognition due to damage or disease in the body beyond what might be expected from normal aging. Although dementia is far more common in the geriatric population, it may occur in any stage of adulthood....
.

It is widely reported that most American
United States

The United States of America is a Federal government constitutional republic comprising U.S. state and a federal district. The country is situated mostly in central North America, where its Contiguous United States and Washington, D.C., the Capital districts and territories, lie between the Pacific Ocean and Atlantic Oceans, Borders of the U...
 diet
Diet

Diet, in relation to food, might mean:* Diet , the sum of the food consumed by an organism or group.* Dieting, the deliberate selection of food to control body weight or nutrient intake....
s contain more sodium
Sodium

Sodium is an element which has the symbol Na , atomic number 11, atomic mass 23 amu , and a common oxidation number +1. Sodium is a soft, silvery white, highly reactive element and is a member of the alkali metals within "group 1" ....
 than is necessary and lack the optimal daily intake of potassium. Therefore, spironolactone could theoretically counter the effects of the typical American diet as it tends to promote sodium excretion and potassium retention. However, there is no proof that it is beneficial for persons whose serum potassium and sodium levels are within the normal range. Few if any doctors would recommend using spironolactone in the absence of conditions for which it is normally indicated.

Spironolactone has also been shown to help prevent certain types of acne
Acne

Acne is a group of skin rashes that have different causes.* Acne vulgaris - most commonly experienced around puberty, typically of the face and shoulders/chest...
 in females when taken in combination with oral contraceptives.

See also

  • Baldness treatments
    Baldness treatments

    More than half of men are affected by male pattern baldness by age 50, and baldness treatments are estimated to be a US $1 billion per year industry....


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