Portal:Corticosteroids
Portal maintenance status: (October 2018)
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Introduction
Corticosteroids are a class of steroid hormones that are produced in the adrenal cortex of vertebrates, as well as the synthetic analogues of these hormones. Two main classes of corticosteroids, glucocorticoids and mineralocorticoids, are involved in a wide range of physiological processes, including stress response, immune response, and regulation of inflammation, carbohydrate metabolism, protein catabolism, blood electrolyte levels, and behavior.
Some common naturally occurring steroid hormones are cortisol (C
21H
30O
5), corticosterone (C
21H
30O
4), cortisone (C
21H
28O
5) and aldosterone (C
21H
28O
5). (Note that aldosterone and cortisone share the same chemical formula but the structures are different.) The main corticosteroids produced by the adrenal cortex are cortisol and aldosterone.
Selected general articles
Carbenoxolone (CBX) is a glycyrrhetinic acid derivative with a steroid-like structure, similar to substances found in the root of the licorice plant. Carbenoxolone is used for the treatment of peptic, esophageal and oral ulceration and inflammation. Electrolyte imbalance is a serious side effect of carbenoxolone when used systemically.
Carbenoxolone reversibly inhibits the conversion of cortisol to the inactive metabolite cortisone by blocking 11β-hydroxysteroid dehydrogenase (11β-HSD). 11β-HSD also reversibly catalyzes the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. Read more...
Corticosterone, also known as 17-deoxycortisol and 11β,21-dihydroxyprogesterone, is a 21-carbon steroid hormone of the corticosteroid type produced in the cortex of the adrenal glands. It is of minor importance in humans, except in the very rare case of congenital adrenal hyperplasia due to 17 alpha-hydroxylase deficiency. Read more...
Felodipine is a medication of the calcium channel blocker type which is used to treat high blood pressure. Read more...
Ketoconazole is an antifungal medication which is used primarily to treat fungal infections. Ketoconazole is sold commercially as a tablet for oral administration (although this use has been discontinued in a number of countries), and in a variety of formulations for topical administration, such as creams (used to treat tinea; cutaneous candidiasis, including candidal paronychia; and pityriasis versicolor) and shampoos (used primarily to treat dandruff – seborrhoeic dermatitis of the scalp).
In terms of chemical structure, ketoconazole is an imidazole. The less toxic and generally more effective triazole antifungal agents fluconazole and itraconazole are usually preferred for systemic use. In 2013 the European Medicines Agency's Committee on Medicinal Products for Human Use (CHMP) recommended that a ban be imposed on the use of oral ketoconazole for systemic use in humans throughout the European Union, after concluding that the risk of serious liver injury from systemic ketoconazole outweighs its benefits. The oral formulation of ketoconazole was discontinued in Australia in 2013 and in China in 2015. Read more...
Metyrapone, sold under the brand name Metopirone, is a medication which is used in the diagnosis of adrenal insufficiency and occasionally in the treatment of Cushing's syndrome (hypercortisolism). Read more...
Fludrocortisone, sold under the brand name Florinef among others, is a corticosteroid which is used to treat adrenogenital syndrome, postural hypotension, and adrenal insufficiency. In adrenal insufficiency it is generally taken together with hydrocortisone. It is taken by mouth. The medication is most commonly used in its acetate form.
Common side effects include high blood pressure, swelling, heart failure, and low blood potassium. Other serious side effects include low immune system function, cataracts, muscle weakness, and mood changes. It is unclear if use during pregnancy is safe for the baby. Fludrocortisone is mostly a mineralocorticoid; however, also has glucocorticoid effects. Read more...
Trilostane, sold under the brand names Desopan, Modrastane, and Modrenal among others, is a steroidogenesis inhibitor which is used in the treatment of Cushing's syndrome.
It was withdrawn from human use in the United States market in April 1994. The drug was previously available in the United Kingdom for use in humans under the brand name Modrenal for the treatment of Cushing's disease and for breast cancer. It was approved in the United States in 2008 for the treatment of Cushing's disease (hyperadrenocorticism) in dogs under the brand name Vetoryl. It was available by prescription in the UK under the Vetoryl brand name for some time before it was approved in the US. The drug is also used to treat the skin disorder Alopecia X in dogs.
It is also the first drug approved to treat both pituitary- and adrenal-dependent Cushing's in dogs. This prescription drug works by stopping the production of cortisol in the adrenal glands. In studies of the drug, the most common side effects were vomiting, lack of energy, diarrhea, and weight loss. Trilostane should not be given to a dog that:- has kidney or liver disease;
- takes certain medications used to treat heart disease;
- is pregnant, nursing or intended for breeding
The safety and effectiveness of trilostane were shown in several studies. Success was measured by improvements in both blood test results and physical symptoms (increased appetite and activity level, and decreased panting, thirst and urination). Read more...
Benidipine (INN), also known as Benidipinum or benidipine hydrochloride, is a dihydropyridine calcium channel blocker for the treatment of high blood pressure (hypertension). It is a triple L-, T-, and N-type calcium channel blocker. It is reno- and cardioprotective. Read more...
Nimodipine (sold under the brandname Nimotop) is a calcium channel blocker originally developed for the treatment of high blood pressure. It is not frequently used for this indication, but has shown good results in preventing a major complication of subarachnoid hemorrhage (a form of cerebral hemorrhage) termed vasospasm; this is now the main use of nimodipine. Read more...
Aldosterone, the main mineralocorticoid hormone, is a steroid hormone produced by the zona glomerulosa of the adrenal cortex in the adrenal gland. It is essential for sodium conservation in the kidney, salivary glands, sweat glands and colon. It plays a central role in the homeostatic regulation of blood pressure, plasma sodium (Na+), and potassium (K+) levels. It does so primarily by acting on the mineralocorticoid receptors in the distal tubules and collecting ducts of the nephron. It influences the reabsorption of sodium and excretion of potassium (from and into the tubular fluids, respectively) of the kidney, thereby indirectly influencing water retention or loss, blood pressure and blood volume. When dysregulated, aldosterone is pathogenic and contributes to the development and progression of cardiovascular and renal disease. Aldosterone has exactly the opposite function of the atrial natriuretic hormone secreted by the heart.
Aldosterone is part of the renin–angiotensin–aldosterone system. It has a plasma half-life of under 20 minutes. Drugs that interfere with the secretion or action of aldosterone are in use as antihypertensives, like lisinopril, which lowers blood pressure by blocking the angiotensin-converting enzyme (ACE), leading to lower aldosterone secretion. The net effect of these drugs is to reduce sodium and water retention but increase retention of potassium. In other words, these drugs stimulate the excretion of sodium and water in urine, while they block the excretion of potassium. Read more...
11-Deoxycorticosterone (DOC), or simply deoxycorticosterone, also known as 21-hydroxyprogesterone, as well as desoxycortone (INN), deoxycortone, and cortexone, is a steroid hormone produced by the adrenal gland that possesses mineralocorticoid activity and acts as a precursor to aldosterone. It is an active (Na+-retaining) mineralocorticoid. As its names indicate, 11-deoxycorticosterone can be understood as the 21-hydroxy-variant of progesterone or as the 11-deoxy-variant of corticosterone.
DOCA is the abbreviation for the ester 11-deoxycorticosterone acetate. Read more...
Nifedipine, sold under the brand name Adalat among others, is a medication used to manage angina, high blood pressure, Raynaud's phenomenon, and premature labor. It is one of the treatments of choice for Prinzmetal angina. It may be used to treat severe high blood pressure in pregnancy. Its use in preterm labor may allow more time for steroids to improve the baby's lung function and provide time for transfer of the mother to a well qualified medical facility before delivery. Nifedipine is taken by mouth and comes in fast and slow release formulations.
Common side effects include lightheadedness, headache, feeling tired, leg swelling, cough, and shortness of breath. Serious side effects may include low blood pressure and heart failure. There is tentative evidence that its use in pregnancy is safe; however, it is not recommended during breastfeeding. It is a calcium channel blocker of the dihydropyridine type. Read more...
11-Deoxycortisol, also known as cortodoxone (INN) or cortexolone, as well as 17α,21-dihydroxyprogesterone or 17α,21-dihydroxypregn-4-ene-3,20-dione, is a glucocorticoid steroid hormone. It was first synthesized by Tadeusz Reichstein, and has also been referred to as Reichstein's Substance.
On April 5, 1952, biochemist Durey Peterson and microbiologist Herbert Murray at Upjohn published the first report of a breakthrough fermentation process for the microbial 11α-oxygenation of steroids (e.g. progesterone) in a single step by common molds of the order Mucorales.
11α-oxygenation of Compound S produces 11α-hydrocortisone, which can be chemically oxidized to cortisone, or converted by further chemical steps to 11β-hydrocortisone (cortisol). Read more...
Cortisol is a steroid hormone, in the glucocorticoid class of hormones. When used as a medication, it is known as hydrocortisone.
It is produced in humans by the zona fasciculata of the adrenal cortex within the adrenal gland. It is released in response to stress and low blood-glucose concentration. It functions to increase blood sugar through gluconeogenesis, to suppress the immune system, and to aid in the metabolism of fat, protein, and carbohydrates. It also decreases bone formation. Read more...
Spironolactone, sold under the brand name Aldactone among others, is a medication that is primarily used to treat fluid build-up due to heart failure, liver scarring, or kidney disease. It is also used in the treatment of high blood pressure, low blood potassium that does not improve with supplementation, early puberty in boys, acne and excessive hair growth in women, and as a part of feminizing hormone therapy in transgender women. Spironolactone is taken by mouth.
Common side effects include electrolyte abnormalities, particularly high blood potassium, nausea, vomiting, headache, rashes, and a decreased desire for sex. In those with liver or kidney problems, extra care should be taken. Spironolactone has not been well studied in pregnancy and should not be used to treat high blood pressure of pregnancy. It is a steroid that blocks the effects of the hormones aldosterone and testosterone and has some estrogen-like effects. Spironolactone belongs to a class of medications known as potassium-sparing diuretics. Read more...
Gestodene, sold under the brand names Femodene and Minulet among others, is a progestin medication which is used in birth control pills for women. It is also used in menopausal hormone therapy. The medication is available almost exclusively in combination with an estrogen. It is taken by mouth.
Side effects of the combination of an estrogen and gestodene include menstrual irregularities, headaches, nausea, breast tenderness, mood changes, and others. Gestodene is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has weak androgenic activity, weak antimineralocorticoid activity, and weak glucocorticoid activity. Read more...
Fludrocortisone, sold under the brand name Florinef among others, is a corticosteroid which is used to treat adrenogenital syndrome, postural hypotension, and adrenal insufficiency. In adrenal insufficiency it is generally taken together with hydrocortisone. It is taken by mouth. The medication is most commonly used in its acetate form.
Common side effects include high blood pressure, swelling, heart failure, and low blood potassium. Other serious side effects include low immune system function, cataracts, muscle weakness, and mood changes. It is unclear if use during pregnancy is safe for the baby. Fludrocortisone is mostly a mineralocorticoid; however, also has glucocorticoid effects. Read more...
Canrenone, sold under the brand names Contaren, Luvion, Phanurane, and Spiroletan, is a steroidal antimineralocorticoid of the spirolactone group related to spironolactone which is used as a diuretic in Europe, including in Italy and Belgium. It is also an important active metabolite of spironolactone, and partially accounts for its therapeutic effects. Read more...
Eplerenone is a steroidal antimineralocorticoid of the spirolactone group that is used as an adjunct in the management of chronic heart failure. Classed as a selective aldosterone receptor antagonist (SARA), it is similar to the diuretic spironolactone, though it is much more selective for the mineralocorticoid receptor in comparison (i.e., does not possess any antiandrogen, progestogen, glucocorticoid, or estrogenic effects), and is specifically marketed for reducing cardiovascular risk in patients following myocardial infarction. Eplerenone is a potassium-sparing diuretic, meaning that it helps the body get rid of water but still keep potassium.
Eplerenone was developed by Pharmacia Corporation, which was acquired by Pfizer in 2002. It was marketed by Pfizer under the trade name Inspra. The US Food and Drug Administration (FDA) approved the drug for sale in the United States in 2002. Eplerenone is currently approved for sale in the US, EU, Netherlands and Japan. Eplerenone costs an estimated $2.93 per day when treating congestive heart failure and $5.86 per day when treating hypertension. Read more...
Amlodipine, sold under the brand name Norvasc among others, is a medication used to treat high blood pressure and coronary artery disease. While not typically recommended in heart failure, amlodipine may be used if other medications are not sufficient for high blood pressure or heart-related chest pain. Amlodipine is taken by mouth and has an effect for at least a day.
Common side effects include swelling, feeling tired, abdominal pain, and nausea. Serious side effects may include low blood pressure or a heart attack. Whether use is safe during pregnancy or breastfeeding is unclear. When used by people with liver problems, and in elderly individuals, doses should be decreased. Amlodipine works partly by increasing the size of arteries. It is a long-acting calcium channel blocker of the dihydropyridine (DHP) type. Read more...
Nitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary (essential) hypertension to decrease blood pressure and can reduce the cardiotoxicity of cocaine. Read more...
Finerenone (INN, USAN) (developmental code name BAY-94-8862) is a nonsteroidal antimineralocorticoid that is in phase III clinical trials for the treatment of chronic heart failure . It has less relative affinity to other steroid hormone receptors than currently available antimineralocorticoids such as eplerenone and spironolactone, which should result in fewer adverse effects like gynaecomastia, impotence, and low libido. Read more...
Enoxolone (INN, BAN; also known as glycyrrhetinic acid or glycyrrhetic acid) is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb liquorice. It is used in flavoring and it masks the bitter taste of drugs like aloe and quinine. It is effective in the treatment of peptic ulcer and also has expectorant (antitussive) properties. It has some additional pharmacological properties including antiviral, antifungal, antiprotozoal, and antibacterial activities. Read more...
Aminoglutethimide (AG), sold under the brand names Elipten, Cytadren, and Orimeten among others, is a medication which has been used in the treatment of seizures, Cushing's syndrome, breast cancer, and prostate cancer, among other indications. It has also been used by bodybuilders, athletes, and other men for muscle-building and performance- and physique-enhancing purposes. AG is taken by mouth three or four times per day.
Side effects of AG include lethargy, somnolence, dizziness, headache, appetite loss, skin rash, hypertension, liver damage, and adrenal insufficiency, among others. AG is both an anticonvulsant and a steroidogenesis inhibitor. In terms of the latter property, it inhibits enzymes such as cholesterol side-chain cleavage enzyme (CYP11A1, P450scc) and aromatase (CYP19A1), thereby inhibiting the conversion of cholesterol into steroid hormones and blocking the production of androgens, estrogens, and glucocorticoids, among other endogenous steroids. As such, AG is an aromatase inhibitor and adrenal steroidogenesis inhibitor, including both an androgen synthesis inhibitor and a corticosteroid synthesis inhibitor. Read more...
Drospirenone, sold under the brand names Yasmin and Angeliq among others, is a progestin medication which is used in birth control pills to prevent pregnancy and in menopausal hormone therapy, among other uses. It is available only in combination with an estrogen and is not available alone. The medication is taken by mouth.
Rare side effects of drospirenone may include high potassium levels and blood clots, among others. Drospirenone is a progestin, or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has additional antimineralocorticoid and antiandrogenic activity and no other important hormonal activity. Because of its antimineralocorticoid activity, drospirenone is said to more closely resemble bioidentical progesterone than other progestins. Read more...
Mitotane, sold under the brand name Lysodren, is a steroidogenesis inhibitor and cytostatic antineoplastic medication which is used in the treatment of adrenocortical carcinoma and Cushing's syndrome. It is a derivative of p,p'-DDT and an isomer of p,p'-DDD, and is also known as 1,1-(dichlorodiphenyl)-2,2-dichloroethane (o,p'-DDD). Read more...
Progesterone (P4) is an endogenous steroid and progestogen sex hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. It belongs to a group of steroid hormones called the progestogens, and is the major progestogen in the body. Progesterone has a variety of important functions in the body. It is also a crucial metabolic intermediate in the production of other endogenous steroids, including the sex hormones and the corticosteroids, and plays an important role in brain function as a neurosteroid.
In addition to its role as a natural hormone, progesterone is used as a medication, for instance in menopausal hormone therapy; for information on progesterone as a medication, see the progesterone (medication) article. Read more...
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Cortisol (hydrocortisone), a corticosteroid with both glucocorticoid and mineralocorticoid activity and effects.
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