Aromatase Inhibitors
18-Hydroxydesoxycorticosterone
Menopause
Androstenedione
Tamoxifen
Hydrocortisone
Sleep Stages
Dehydroepiandrosterone
A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.
Adrenergic Agents
Androstenediols
Estrone
An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women.
Adrenal Cortex
The outer layer of the adrenal gland. It is derived from MESODERM and comprised of three zones (outer ZONA GLOMERULOSA, middle ZONA FASCICULATA, and inner ZONA RETICULARIS) with each producing various steroids preferentially, such as ALDOSTERONE; HYDROCORTISONE; DEHYDROEPIANDROSTERONE; and ANDROSTENEDIONE. Adrenal cortex function is regulated by pituitary ADRENOCORTICOTROPIN.
Adrenocorticotropic Hormone
An anterior pituitary hormone that stimulates the ADRENAL CORTEX and its production of CORTICOSTEROIDS. ACTH is a 39-amino acid polypeptide of which the N-terminal 24-amino acid segment is identical in all species and contains the adrenocorticotrophic activity. Upon further tissue-specific processing, ACTH can yield ALPHA-MSH and corticotrophin-like intermediate lobe peptide (CLIP).
Metyrapone
Steroids
A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed)
Danazol
A synthetic steroid with antigonadotropic and anti-estrogenic activities that acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties. Danazol has been used in the treatment of endometriosis and some benign breast disorders.
Estrogens
Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds.
Cortisone
Neoplasms, Hormone-Dependent
Adrenal Glands
Aromatase
An enzyme that catalyzes the desaturation (aromatization) of the ring A of C19 androgens and converts them to C18 estrogens. In this process, the 19-methyl is removed. This enzyme is membrane-bound, located in the endoplasmic reticulum of estrogen-producing cells of ovaries, placenta, testes, adipose, and brain tissues. Aromatase is encoded by the CYP19 gene, and functions in complex with NADPH-FERRIHEMOPROTEIN REDUCTASE in the cytochrome P-450 system.
Nausea
Encyclopedias as Topic
Cushing Syndrome
A condition caused by prolonged exposure to excess levels of cortisol (HYDROCORTISONE) or other GLUCOCORTICOIDS from endogenous or exogenous sources. It is characterized by upper body OBESITY; OSTEOPOROSIS; HYPERTENSION; DIABETES MELLITUS; HIRSUTISM; AMENORRHEA; and excess body fluid. Endogenous Cushing syndrome or spontaneous hypercortisolism is divided into two groups, those due to an excess of ADRENOCORTICOTROPIN and those that are ACTH-independent.
Anabolic Agents
Hypothyroidism
Testosterone
A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.
Polygala
Puberty, Precocious
Development of SEXUAL MATURATION in boys and girls at a chronological age that is 2.5 standard deviations below the mean age at onset of PUBERTY in the population. This early maturation of the hypothalamic-pituitary-gonadal axis results in sexual precocity, elevated serum levels of GONADOTROPINS and GONADAL STEROID HORMONES such as ESTRADIOL and TESTOSTERONE.
Fibrous Dysplasia, Polyostotic
Paraganglioma, Extra-Adrenal
A relatively rare, usually benign neoplasm originating in the chemoreceptor tissue of the CAROTID BODY; GLOMUS JUGULARE; GLOMUS TYMPANICUM; AORTIC BODIES; and the female genital tract. It consists histologically of rounded or ovoid hyperchromatic cells that tend to be grouped in an alveolus-like pattern within a scant to moderate amount of fibrous stroma and a few large thin-walled vascular channels. (From Stedman, 27th ed)
Pregnenolone
Goiter
Enlargement of the THYROID GLAND that may increase from about 20 grams to hundreds of grams in human adults. Goiter is observed in individuals with normal thyroid function (euthyroidism), thyroid deficiency (HYPOTHYROIDISM), or hormone overproduction (HYPERTHYROIDISM). Goiter may be congenital or acquired, sporadic or endemic (GOITER, ENDEMIC).
Drug Overdose
Alcohol Drinking
Pregnancy
Meningitis, Fungal
Drug Contamination
Injections, Epidural
A proposed sequence of hormones controlling the induction of luteal 20alpha-hydroxy steroid dehydrogenase and progesterone withdrawal in the late-pregnant rat. (1/183)
1. The previously reported induction of luteal 20alpha-hydroxy steroid dehydrogenase by administration of aminoglutethimide to late-pregnant rats was shown to be unaffected by prior removal of the foetuses. Aminoglutethimide therefore does not act via the foetuses in this context. 2. The ability of injected oestrogen to prevent the above induction was lost by delaying the injection for 12h after aminoglutethimide, although the increase in enzyme activity begins only after 24h. 3. Induction of 20alpha-hydroxy steroid dehydrogenase by foetoplacental removal on day 18 of pregnancy was inhibited by human choriogonadotropin, lutropin (luteinizing hormone) and pregnant-mare serum gonadotropin, but not by somatotropin (growth hormone), thyrotropin or follitropin (follicle-stimulating hormone) 4. Indomethacin blocked the normal induction of 20alpha-hydroxy steroid dehydrogenase in late pregnancy and that caused by aminoglutethimide. It partially blocked that caused by human choriogonadotropin given on days 19-20 and that caused by 2-bromo-alpha-ergocryptine on days 5-6, but failed to block that caused by human choriogonadotropin on days 15-16 or by foetoplacental removal on day 18 of pregnancy. 5. These findings, and the control of progesterone synthesis in late pregnancy, are interpreted in terms of a sequence of hormonal or enzymic syntheses, each of which is inhibited by the product of the preceding synthesis. (+info)Product of side-chain cleavage of cholesterol, isocaproaldehyde, is an endogenous specific substrate of mouse vas deferens protein, an aldose reductase-like protein in adrenocortical cells. (2/183)
Mouse vas deferens protein (MVDP) is an aldose reductase-like protein that is highly expressed in the vas deferens and adrenal glands and whose physiological functions were unknown. We hereby describe the enzymatic characteristics of MVDP and its role in murine adrenocortical Y1 cells. The murine aldose reductase (AR) and MVDP cDNAs were expressed in bacteria to obtain recombinant proteins and to compare their enzymatic activities. Recombinant MVDP was functional and displayed kinetic properties distinct from those of murine AR toward various substrates, a preference for NADH, and insensitivity to AR inhibitors. For MVDP, isocaproaldehyde, a product of side-chain cleavage of cholesterol generated during steroidogenesis, is the best natural substrate identified so far. In Y1 cells, we found that NADH-linked isocaproaldehyde reductase (ICR) activity was much higher than NADPH-linked ICR activity and was not abolished by AR inhibitors. We demonstrate that in Y1 cells, forskolin-induced MVDP expression enhanced NADH-linked ICR activity by 5-6-fold, whereas no variation in ICR-linked NADPH activity was observed in the same experiment. In cells stably transfected with MVDP antisense cDNA, NADH-linked ICR activity was abolished even in the presence of forskolin, and the isocaproaldehyde toxicity was increased compared with that of intact Y1 cells, as measured by isocaproaldehyde LD(50). In Y1 cells transfected with MVDP antisense cDNA, forskolin-induced toxicity was abolished by aminoglutethimide. These results indicate that in adrenocortical cells, MVDP is responsible for detoxifying isocaproaldehyde generated by steroidogenesis. (+info)Decreased progesterone levels and progesterone receptor antagonists promote apoptotic cell death in bovine luteal cells. (3/183)
We tested the hypothesis that progesterone (P(4)) acts at a local level to inhibit luteal apoptosis. Initial experiments employed aminoglutethimide, a P450 cholesterol side-chain cleavage inhibitor, to inhibit steroid synthesis. Cultured bovine luteal cells were treated with aminoglutethimide (0.15 mM) +/- P(4) (500 ng/ml) for 48 h. Luteal cells were recovered and snap frozen for isolation and analysis of oligonucleosomal DNA fragmentation or fixed for morphological analysis. Medium was collected for analysis of P(4) levels by RIA. Aminoglutethimide inhibited P(4) synthesis by > 95% and increased the level of apoptosis as evidenced by (32)P-labeled oligonucleosomal DNA fragmentation (> 40%). P(4) supplementation inhibited the onset of apoptosis that was induced by aminoglutethimide. These data were further supported by morphological assessment of apoptotic cells utilizing a Hoechst staining technique and together strongly suggest that P(4) has anti-apoptotic capacity. Using reverse transcription-polymerase chain reaction, we were able to isolate a 380-base pair cDNA from the bovine corpus luteum (CL) that was 100% homologous to the progesterone receptor (PR) previously found in bovine oviductal tissue. Furthermore, PR transcripts were present in large and small luteal cells. Immunohistochemistry also revealed that PR protein was present in both large and small luteal cells. To determine whether the anti-apoptotic effect of P(4) was regulated at the receptor level, luteal cells were cultured in the presence of PR antagonists, RU-486 and onapristone, for 48 h. Both antagonists caused approximately a 40% increase in (32)P-labeled oligonucleosomal DNA fragmentation. Interestingly, there was no difference (P >/= 0.05) in P(4) levels after treatment with PR antagonists. These observations support the concept that P(4) represses the onset of apoptosis in the CL by a PR-dependent mechanism. (+info)Status of aromatase inhibitors in relation to other breast cancer treatment modalities. (4/183)
Aromatase is one of the key enzymes possibly linked with the perpetuation or even initiation of breast cancer. Modulation of its activity by the new generation inhibitors has resulted in increased responses and improved therapeutic ratio compared with those of parent aromatase inhibitors. More recent trials have shown promising results with regard to improved therapeutic ratio compared with what is seen with presently accepted second-line hormonal approaches. Present data and laboratory research indicate that new aromatase inhibitors have the potential to play an important role as adjuvants, and possibly in the prevention of human breast cancer. It is probable that it may be as adjuvants that their real therapeutic strength in terms of a beneficial impact on survival may be realized. The absence of estrogen agonist activity of new aromatase inhibitors on lipid and bone metabolism calls for more clinical studies having late mortality in breast cancer survivors as the ultimate outcome objective; in this regard, interaction of new aromatase inhibitors with new selective estrogen receptor modulators looks promising. Achievement of these outcomes, and understanding of interactions with other therapies, await the termination of present trials and the start of new initiatives. (+info)Use of aromatase inhibitors in breast carcinoma. (5/183)
Aromatase, a cytochrome P-450 enzyme that catalyzes the conversion of androgens to estrogens, is the major mechanism of estrogen synthesis in the post-menopausal woman. We review some of the recent scientific advances which shed light on the biologic significance, physiology, expression and regulation of aromatase in breast tissue. Inhibition of aromatase, the terminal step in estrogen biosynthesis, provides a way of treating hormone-dependent breast cancer in older patients. Aminoglutethimide was the first widely used aromatase inhibitor but had several clinical drawbacks. Newer agents are considerably more selective, more potent, less toxic and easier to use in the clinical setting. This article reviews the clinical data supporting the use of the potent, oral competitive aromatase inhibitors anastrozole, letrozole and vorozole and the irreversible inhibitors 4-OH androstenedione and exemestane. The more potent compounds inhibit both peripheral and intra-tumoral aromatase. We discuss the evidence supporting the notion that aromatase inhibitors lack cross-resistance with antiestrogens and suggest that the newer, more potent compounds may have a particular application in breast cancer treatment in a setting of adaptive hypersensitivity to estrogens. Currently available aromatase inhibitors are safe and effective in the management of hormone-dependent breast cancer in post-menopausal women failing antiestrogen therapy and should now be used before progestational agents. There is abundant evidence to support testing these compounds as first-line hormonal therapy for metastatic breast cancer as well as part of adjuvant regimens in older patients and quite possibly in chemoprevention trials of breast cancer. (+info)Lipoproteins regulate expression of the steroidogenic acute regulatory protein (StAR) in mouse adrenocortical cells. (6/183)
The steroidogenic acute regulatory protein (StAR) is required for the movement of cholesterol from the outer to the inner mitochondrial membrane, the site of cholesterol side chain cleavage. Here we describe a novel form of regulation of StAR gene expression in steroidogenic cells. Treatment of Y-1 BS1 adrenocortical cells with either low density lipoprotein (LDL) or high density lipoprotein (HDL) increases expression of endogenous StAR mRNA and protein in a dose-dependent manner. Induction of StAR mRNA by lipoprotein requires basal cAMP-dependent protein kinase, since the inhibitor, R(p)-8-Br-cAMP, inhibited induction of StAR protein by LDL. Likewise, basal StAR expression or LDL induction of StAR protein was not detectable in Y-1 kin-8 cells which are deficient in cAMP-dependent protein kinase. Aminoglutethimide and ketoconazole were used to determine if side chain cleavage of lipoprotein-derived cholesterol is required for induction of StAR mRNA. Treatment with either drug alone induced StAR mRNA expression 1.5-3-fold, while induction of StAR in cells treated with either drug plus LDL, was equal to, or greater than, induction seen with either agent alone, suggesting that lipoprotein does not regulate StAR via generation of an oxysterol intermediate. Both LDL and HDL increased expression of a mouse -966 StAR promoter-reporter construct 1.5-2.5-fold, indicating that regulation occurs at the level of transcription. In contrast, neither lipoprotein was able to induce transcription from a -966 StAR promoter in which the steroidogenic factor-1 site at -135 was abolished, indicating that regulation of StAR transcription by lipoproteins requires steroidogenic factor-1. The regulation of StAR gene expression by lipoproteins may represent a positive feedback circuit which links cholesterol availability with steroidogenic output. (+info)Contribution of progesterone, follicle stimulating hormone and glucocorticoids in survival of serum-free cultured granulosa cell explants. (7/183)
To investigate the role of progesterone (P4) as a survival factor in quail granulosa cell explants, P4 content was determined under various conditions and correlated with apoptotic indexes (AIs) evaluated by 2',6'-diamidino-2-phenylindole (DAPI)-staining. Analysis of serum-free cultures from 24 to 96 h shows decreased P4 levels in the medium paralleled by increasing AI. Inhibiting apoptosis by gonadotropic support (FSH, 100 ng/ml) stimulates a 3-fold increase of the P4 level in the medium (83.49+/-8.69 vs 26.31+/-1.61 ng/ml in serum-free controls) together with a significant decrease in AI from 8.81+/-1.06% in serum-free controls to 3.50+/-0.72%. Substantial evidence for P4 as an autocrine/paracrine survival factor can be inferred from experiments with aminoglutethimide (AG, 1 mM) and RU486 (20 microM). Blocking P4 synthesis by AG causes a 2-fold increase in apoptosis from 6.08+/-0.67% in serum-free controls to 12.53+/-1.60%. Blocking P4 receptors by RU486 causes a similar increase in AI (3.02+/-0.98% in serum-free controls to 17.07+/-3.20%) and about a 50% decrease in P4. The effect of RU486 could be attenuated by exogenous P4 but not by dexamethasone indicating selective binding of P4 to the progesterone receptor. Dexamethasone treatment promotes survival without affecting P4 levels. In further support of an autocrine/paracrine action for P4 in the granulosa cells, both the A and B form of the avian P4 receptor (PR) are identified in vivo and in vitro by Western blotting. Exogenous administration of P4 only affects survival when endogenous P4 synthesis is blocked or after 48 h of serum-free culture when endogenous P4 production is very low. Because FSH also affects survival when its stimulatory effect on P4 synthesis is blocked by AG (AI decrease from 6.08+/-0.67% in serum-free controls to 1.64+/-0.71% in FSH+AG treated) it is proposed that (1) P4 is an autocrine/paracrine survival factor in the preovulatory granulosa and (2) FSH mediates both P4-dependent and P4-independent survival pathways. (+info)Aromatase inhibition by an 11,13-dihydroderivative of a sesquiterpene lactone. (8/183)
Compounds that inhibit aromatase activity are used for the treatment of breast cancer. A group of sesquiterpene lactones inhibit aromatase activity and also exert cytotoxicity through their reactive alpha-methylene-gamma-lactone group. To synthesize sesquiterpene lactones with greater specificity for aromatase inhibition and lower cytotoxicity, we chemically reduced the alpha-methylene-gamma-lactone group in the active aromatase inhibitor 10-epi-8-deoxycumambrin B (compound 1), to obtain the new compound 11betaH,13-dihydro-10-epi-8-deoxycumambrin B (compound 2). Reduction of the alpha-methylene-gamma-lactone group abrogated the cytotoxic activity of compound 1 against the JEG-3, HeLa, and COS-7 cell lines. Compound 2 had higher aromatase inhibitory activity than compound 1 (IC(50) = 2 +/- 0.5 microM versus 7 +/- 0.5 microM, K(i) = 1.5 microM versus 4.0 microM) and was a more potent type II ligand to the heme iron present in the cytochrome P450(arom) active site. Compound 2 inhibited aromatase activity in JEG-3 cells in a comparable manner to the inhibitor aminoglutethimide (AG) used clinically for the treatment of breast cancer. Additionally, compound 2 inhibited androstenedione-induced uterine hypertrophy in sexually immature mice (41% of uterine weight suppression for compound 2 versus 51% for AG). We conclude that the anti-aromatase activity of sesquiterpene lactones does not depend on the presence of the highly reactive alpha-methylene-gamma-lactone group, whereas their cytotoxicity does. These findings may facilitate the development of safer agents for breast cancer therapy. (+info)
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Hormone replacement therapy
The Women's Health Initiative trials were conducted between 1991 and 2006 and were the first large, double-blind, placebo-controlled clinical trials of HRT in healthy women.[52] Their results were both positive and negative, suggesting that during the time of hormone therapy itself, there are increases in invasive breast cancer, stroke and lung clots. Other risks include increased endometrial cancer, gallbladder disease, and urinary incontinence, while benefits include decreased hip fractures, decreased incidence of diabetes, and improvement of vasomotor symptoms. There also is an increased risk of dementia with HRT in women over 65, though when given earlier it appears to be neuroprotective. After the cessation of HRT, the WHI continued observe its participants, and found that most of these risks and benefits dissipated, though some elevation in breast cancer risk did persist.[24] Other studies have also suggested an increased risk of ovarian cancer.[43] The arm of the WHI receiving combined ...
Norethisterone
Due to its weak androgenic activity, norethisterone can produce androgenic side effects such as acne, hirsutism, and voice changes of slight severity in some women at high dosages (e.g., 10 to 40 mg/day).[8] This is notably not the case with combined oral contraceptives that contain norethisterone and EE, however.[9] Such formulations contain low dosages of norethisterone (0.35 to 1 mg/day)[9] in combination with estrogen and are actually associated with improvement in acne symptoms.[25][26] In accordance, they are in fact approved by the FDA for the treatment of acne in women in the United States.[25][26] The improvement in acne symptoms is believed to be due to a 2- to 3-fold increase in sex hormone-binding globulin (SHBG) levels and a consequent decrease in free testosterone levels caused by EE, which results in an overall decrease in androgenic signaling in the body.[27] The sebaceous glands are highly androgen-sensitive and their size and activity are potential markers of androgenic ...
Promestriene
... (INN) (brand names Colpotrofin, Colpotrophine, Delipoderm), also known as estradiol 3-propyl 17β-methyl diether, is a synthetic steroidal estrogen which is used topically in a 1% cream formulation.[1][2][3][4] It is the 3-propyl and 17β-methyl diether of estradiol.[5] The drug is described as a tropic agent and antiseborrheic.[1] It has not been found to be effective in the treatment of androgenic alopecia or other conditions of cutaneous androgenization.[6][7] ...
Antiestrogen
First-generation: Aminoglutethimide. *Testolactone. *Second-generation: Fadrozole. *Formestane. *Third-generation: Anastrozole ...
Polyestradiol phosphate
PEP produces minimal undesirable effects on coagulation factors and is thought to increase the risk of blood clots little or not at all.[28][29] This is in spite of the fact that estradiol levels can reach high concentrations of as much as 700 pg/mL with high-dose (320 mg/month) PEP therapy.[30] It is also in contrast to oral synthetic estrogens such as diethylstilbestrol and ethinylestradiol, which produce marked increases in coagulation factors and high rates of blood clots at the high doses used to achieve castrate levels of testosterone in prostate cancer.[28][29][6] The difference between the two types of therapies is due to the bioidentical and parenteral nature of PEP and its minimal influence on liver protein synthesis.[28][29][6] PEP might actually reduce the risk of blood clots, due to decreases in levels of certain procoagulatory proteins.[28][29] Although PEP does not increase the hepatic production or levels of procoagulatory factors, it has been found to significantly decrease ...
8,9-Dehydroestrone
First-generation: Aminoglutethimide. *Testolactone. *Second-generation: Fadrozole. *Formestane. *Third-generation: Anastrozole ...
Lynestrenol
... itself does not bind to the progesterone receptor and is inactive as a progestogen.[7][8] It is a prodrug, and upon oral administration, is rapidly and almost completely converted into norethisterone, a potent progestogen, in the liver during first-pass metabolism.[7][8] No other metabolites besides norethisterone are formed from lynestrenol.[8] As such, its pharmacological activity is essentially identical to that of norethisterone.[9] The conversion of lynestrenol into norethisterone is catalyzed by CYP2C9 (28.0%), CYP2C19 (49.8%), and CYP3A4 (20.4%), while other cytochrome P450 enzymes are each responsible for no more than 1.0% of the total conversion.[8] It appears that lynestrenol first undergoes hydroxylation of the C3 position, forming etynodiol as an intermediate,[12] followed by oxygenation of the hydroxyl group to form norethisterone.[11] The peak blood levels are reached within 2 to 4 hours after oral administration, 97% of the administered dose being bound to plasma ...
Estrogen
... may play a role in suppressing binge eating. Hormone replacement therapy using estrogen may be a possible treatment for binge eating behaviors in females. Estrogen replacement has been shown to suppress binge eating behaviors in female mice.[53] The mechanism by which estrogen replacement inhibits binge-like eating involves the replacement of serotonin (5-HT) neurons. Women exhibiting binge eating behaviors are found to have increased brain uptake of neuron 5-HT, and therefore less of the neurotransmitter serotonin in the cerebrospinal fluid.[54] Estrogen works to activate 5-HT neurons, leading to suppression of binge like eating behaviors.[53] It is also suggested that there is an interaction between hormone levels and eating at different points in the female menstrual cycle. Research has predicted increased emotional eating during hormonal flux, which is characterized by high progesterone and estradiol levels that occur during the mid-luteal phase. It is hypothesized that these ...
Ethylestrenol
... , also known as ethyloestrenol or ethylnandrol and sold under the brand names Maxibolin and Orabolin among others, is an androgen and anabolic steroid (AAS) medication which has been used in the past for a variety of indications such as to promote weight gain and to treat anemia and osteoporosis but has been discontinued for use in humans.[1] It is still available for veterinary use in Australia and New Zealand however.[2] It is taken by mouth.[1] Side effects of ethylestrenol include symptoms of masculinization like acne, increased hair growth, voice changes, and increased sexual desire.[1] It can also cause liver damage.[1] The drug is a synthetic androgen and anabolic steroid and hence is an agonist of the androgen receptor (AR), the biological target of androgens like testosterone and dihydrotestosterone (DHT).[1][3] It has strong anabolic effects relative to its androgenic effects.[1] The drug also has strong progestogenic effects.[1] Ethylestrenol is a prodrug of ...
Estradiol acetate
... , sold under the brand names Femtrace, Femring, and Menoring, is an estrogen medication which is used in hormone therapy for the treatment of menopausal symptoms in women.[3][4][5][6] It is taken by mouth or given as a vaginal ring once every three months.[1] Side effects of estradiol acetate include breast tenderness, breast enlargement, nausea, headache, and fluid retention.[7][5][6] Estradiol acetate is a synthetic estrogen and hence is an agonist of the estrogen receptor (ER), the biological target of estrogens like estradiol.[8][9] It is an estrogen ester and a prodrug of estradiol in the body.[9][8] Because of this, it is considered to be a natural and bioidentical form of estrogen.[9] Estradiol acetate was introduced for medical use in 2001.[10] It is available in the United States and the United Kingdom.[10][3] The formulation for use by mouth has been discontinued in the United States.[11] .mw-parser-output .toclimit-2 .toclevel-1 ul,.mw-parser-output .toclimit-3 ...
Antiandrogen
These drugs include aminoglutethimide, ketoconazole,[115] and abiraterone acetate.[70][28][116] Aminoglutethimide inhibits ... Aminoglutethimide. Nonsteroidal. Androgen synthesis inhibitor. Cytadren, Orimeten. Oral. 1960. Availableb. 222,000 ... The androgen synthesis inhibitors aminoglutethimide and ketoconazole were first marketed in 1960 and 1977, respectively,[165][ ... inhibitor aminoglutethimide,[70] and the 5α-reductase inhibitors finasteride, dutasteride, epristeride, alfatradiol, and saw ...
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Cash, Ralph; Brough, A. Joseph; Margo, N.P.Cohen; Satoh, Paul S. (1967). "Aminoglutethimide as an inhibitor of adrenal ... Cohen, Margo P. (1968). "Aminoglutethimide inhibition of adrenal desmolase activity". Proc Soc Exp Biol Med. 127 (4): 1086-1090 ...
Glutethimide
Aminoglutethimide Piperidione Methyprylone Pyrithyldione Barceloux DG (2012). Medical Toxicology of Drug Abuse: Synthesized ...
Non steroidal aromatase inhibitors
Aminoglutethimide has an oral administration and a usual dosage range between 250-100 mg/day. The drug has good oral ... Aminoglutethimide is an NSAIs and therefore inhibits aromatase among other biosynthesis and is for example used to treat ... Aminoglutethimide has a good distribution around the body and is partly metabolized in the liver by acetylation. The ... In 1960 aminoglutethimide was marketed as an anticonvulsant. Later in 1963, a doctor at the Sinai Hospital in Detroit ...
Mitotane
Analogues of mitotane include aminoglutethimide, amphenone B, and metyrapone. Mitotane was introduced in 1960 for the treatment ...
Tamoxifen
The aromatase inhibitor aminoglutethimide induces the metabolism of tamoxifen. Conversely, the aromatase inhibitor letrozole ...
Metyrapone
Analogues of metyrapone include aminoglutethimide, amphenone B, and mitotane. Metyrapone has been found in early human trials ...
Sex hormone-binding globulin
Aminoglutethimide. Nonsteroidal. ,0.01. ,0.2. ,0.1. ,0.1 Androstanolone. Steroidal. 220. 5500. 1.3. 0.83 ...
N-acetyltransferase
... aminoglutethimide, and sulfamethazine. NAT2 is involved in the metabolism of xenobiotics, which can lead to both the ...
Management of prostate cancer
Ketoconazole can cause liver damage with prolonged use, and aminoglutethimide can cause skin rashes. When hormonal treatment is ... Medications that block the production of adrenal androgens such as DHEA include ketoconazole and aminoglutethimide. Because the ...
Rogletimide
This makes it potentially useful in the treatment of breast cancer, and with fewer side effects than aminoglutethimide, but its ... MacNeill FA, Jones AL, Jacobs S, Lønning PE, Powles TJ, Dowsett M (October 1992). "The influence of aminoglutethimide and its ... but instead has pharmacological activity as a selective aromatase inhibitor similar to the related drug aminoglutethimide and ...
Hormonal therapy (oncology)
Aminoglutethimide inhibits both aromatase and other enzymes critical for steroid hormone synthesis in the adrenal glands. It ...
Anticorticosteroid
They include: Antiglucocorticoids - e.g., mifepristone, ketoconazole, aminoglutethimide Antimineralocorticoids - e.g., ...
Antiandrogen
These drugs include aminoglutethimide, ketoconazole,[106] and abiraterone acetate.[61][62][107] Aminoglutethimide inhibits ... The androgen synthesis inhibitors aminoglutethimide and ketoconazole were first marketed in 1960 and 1977, respectively,[152][ ... inhibitor aminoglutethimide,[61] and the 5α-reductase inhibitors finasteride, dutasteride, epristeride, alfatradiol, and saw ... aminoglutethimide, and ketoconazole.[78] In contrast, spironolactone, enzalutamide,[79] and other antiandrogens are not ...
Aminoglwtethimid - Wicipedia
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Ketoconazole
Other steroidogenesis inhibitors besides ketoconazole and levoketoconazole include the nonsteroidal compound aminoglutethimide ...
Antiglucocorticoid
... and aminoglutethimide. They are used to treat Cushing's syndrome. Antiglucocorticoids could be effective antidepressants for a ...
Aminoglutethimide - Wikipedia
Aminoglutethimide is the generic name of the drug and its INN, USAN, and BAN, while aminoglutéthimide is its DCF and ... Aminoglutethimide (AG), sold under the brand names Elipten, Cytadren, and Orimeten among others, is a medication which has been ... ISBN 978-1-56363-429-1. Siraki AG, Bonini MG, Jiang J, Ehrenshaft M, Mason RP (July 2007). "Aminoglutethimide-induced protein ... 481-. ISBN 978-1-4613-3837-6. https://www.drugs.com/international/aminoglutethimide.html J.E. Castro (9 March 2013). The ...
Cytadren (Aminoglutethimide): Uses, Dosage, Side Effects, Interactions, Warning
Aminoglutethimide) may treat, side effects, dosage, drug interactions, warnings, patient labeling, reviews, and related ... aminoglutethimide) Tablets USP. DESCRIPTION. Cytadren, aminoglutethimide tablets USP, is an inhibitor of adrenocortical steroid ... aminoglutethimide) . In spite of an increase in TSH, Cytadren (aminoglutethimide) has not been associated with increased ... Aminoglutethimide USP is a fine, white or creamy white, crystalline powder. It is very slightly soluble in water, and readily ...
Aminoglutethimide - DrugBank
Aminoglutethimide has been used in the treatment of advanced breast and prostate cancer. It was formerly used for its weak ... Aminoglutethimide. ATC Codes. L02BG01 - Aminoglutethimide*L02BG - Aromatase inhibitors. *L02B - HORMONE ANTAGONISTS AND RELATED ... Aminoglutethimide has been used in the treatment of advanced breast and prostate cancer. It was formerly used for its weak ... Aminoglutethimide. Accession Number. DB00357 (APRD00592) Type. Small Molecule. Groups. Approved, Investigational. Description. ...
Aminoglutethimide - wikidoc
Aminoglutethimide, aminoglutethimide tablets USP, is an inhibitor of adrenocortical steroid synthesis, available as 250-mg ... Note: Aminoglutethimide was marketed previously as an anticonvulsant but was withdrawn from marketing for that indication in ... Aminoglutethimide diminishes the effect of coumarin and warfarin.. Use in Specific Populations. Pregnancy. Pregnancy Category ( ... There is no FDA guidance on usage of Aminoglutethimide in women who are pregnant. Pregnancy Category (AUS): There is no ...
Aminoglutethimide in the Treatment of Advanced Postmenopausal Breast Cancer | Cancer Research
Aminoglutethimide in the Treatment of Advanced Postmenopausal Breast Cancer. Adrian L. Harris, Trevor J. Powles and Ian E. ... Aminoglutethimide in the Treatment of Advanced Postmenopausal Breast Cancer. Adrian L. Harris, Trevor J. Powles and Ian E. ... Aminoglutethimide in the Treatment of Advanced Postmenopausal Breast Cancer. Adrian L. Harris, Trevor J. Powles and Ian E. ... Aminoglutethimide in the Treatment of Advanced Postmenopausal Breast Cancer Message Subject (Your Name) has forwarded a page to ...
Cytadren (Aminoglutethimide) - Regrowth. Your Source Of Hair News
Cytadren is a drug used to treat overactive adrenal cortexes. The adrenals produce female estrogens/estradiols, cortisol (used in your bodys reaction to stress) and some precursor hormones (DHEA). It is often used by weight lifters to suppress female hormones, increase male hormones and help build muscle. One person has emailed Regrowth.com saying he, his doctor, and another male friend had moderate to dense regrowth using this drug. He was using Proscar concurrently. Since this drug raises free testosterone levels, you would probably need to use this in conjunction with Proscar to prevent raised DHT levels. Since Cytadren can suppress DHEA levels, which appear to play a major role in female loss, this may be why it works in women. This drug MUST be used under the supervision of a doctor since it lowers cortisol. This hormone is vital for your body to function under stressful conditions, and without it, your body can have very severe reactions. Your doctor will need to monitor your cortisol and ...
AMINOGLUTETHIMIDE 125-84-8 - PROPOSITION 65
... p-Aminoglutethimide;Ba-16038;Elipten;2-(p-Aminophenyl)-2-ethylglutarimide;dl-Aminoglutethimide;Cytadren;3-Ethyl-3-(p- ... Aminoglutethimide testing. Laboratory testing for CAS number 125-84-8. 2,6-Piperidinedione, 3-(4-aminophenyl)-3-ethyl-; ... p-Aminoglutethimide;Ba-16038;Elipten;2-(p-Aminophenyl)-2-ethylglutarimide;dl-Aminoglutethimide;Cytadren;3-Ethyl-3-(p- ... 125-84-8 Aminoglutethimide. The Proposition 65 Chemical List information is provided for reference only and is subject to ...
A randomized trial comparing surgical adrenalectomy with aminoglutethimide plus hydrocortisone in women with advanced breast...
Chemoprevention of MNU-induced mammary tumorigenesis by hormone response modifiers: toremifene, RU 16117, tamoxifen,...
Combinations of aminoglutethimide, progesterone and/or a suboptimal dose of tamoxifen citrate also proved to be effective in ... Aminoglutethimide, RU 16117 and toremifene citrate, in addition to their effects on tumor multiplicity, caused significant ... Treatment with either RU 16117, progesterone or aminoglutethimide resulted in a significant decrease in cancer multiplicity [, ... The effects of structurally different antiestrogens, progesterone and the aromatase inhibitor aminoglutethimide, were evaluated ...
Aminoglutethimide: a 'side-effect' turned to therapeutic advantage | Postgraduate Medical Journal
Aminoglutethimide as Treatment of Postmenopausal Women with Advanced Breast Carcinoma | Annals of Internal Medicine | American...
Aminoglutethimide as Treatment of Postmenopausal Women with Advanced Breast Carcinoma RICHARD J. SANTEN, M.D.; THOMAS J. WORGUL ... Aminoglutethimide, a known inhibitor of steroid synthesis, is also a potent blocker of the aromatase enzyme and, thus, of ... Aminoglutethimide as Treatment of Postmenopausal Women with Advanced Breast Carcinoma. Ann Intern Med. 1982;96:94-101. doi: ... We developed an effective regimen to inhibit estrogen production in postmenopausal women using aminoglutethimide and ...
Aminoglutethimide - Side Effects, Uses, Dosage, Overdose, Pregnancy, Alcohol | RxWiki
Get up-to-date information on Aminoglutethimide side effects, uses, dosage, overdose, pregnancy, alcohol and more. Learn more ... Aminoglutethimide falls into category D:. It has been shown that use of Aminoglutethimide in pregnant women caused some babies ... How was your experience with Aminoglutethimide?. First, a little about yourself. Male Female ... The Aminoglutethimide dose your doctor recommends will be based on the following (use any or all that apply): ...
Aminoglutethimide-induced hematologic toxicity: Worldwide experience
- Penn State
Aminoglutethimide-induced hematologic toxicity: Worldwide experience. A. A. Messeih, Allan Lipton, R. J. Santen, Harold Harvey ... Aminoglutethimide-induced hematologic toxicity : Worldwide experience. / Messeih, A. A.; Lipton, Allan; Santen, R. J.; Harvey, ... Aminoglutethimide-induced hematologic toxicity: Worldwide experience. Cancer Treatment Reports. 1985 Dec 11;69(9):1003-1004. ... Blood cell counts recovered promptly upon cessation of aminoglutethimide in all but one patient, who died from septicemia and ...
Phenomenex HPLC Application #17667: Aminoglutethimide on Lux 5µ Cellulose-1 250 x 4.6mm in NP
Phenomenex HPLC Application #24497: Chiral Separation of Aminoglutethimide on Lux 5µm i-Amylose-1 in NP
RePub, Erasmus University Repository:
Effect of combination therapy with aminoglutethimide and hydrocortisone on prostate...
Aminoglutethimide, Androgen independent, Prostate cancer, Prostate-specific antigen Persistent URL dx.doi.org/10.1097/00001813- ... We conclude that aminoglutethimide is a valuable second-line therapy for patients with androgen-independent prostate cancer. ... Kruit, W.H.J, Stoter, G, & Klijn, J.G.M. (2004). Effect of combination therapy with aminoglutethimide and hydrocortisone on ... Thirty-five patients were treated with aminoglutethimide 1000 mg daily and hydrocortisone acetate 40 mg daily. PSA measurements ...
Cytadren (Aminoglutethimide) Oral: Uses, Dosage & Side Effects
Aminoglutethimide is the drug which acts on the adrenal cortex. Production of steroids is affected by its administration. ... Therapeutic dosage of Aminoglutethimide is 4.8 mg/kg of body weight which is administered 8 hourly in an adult to treat a ... Aminoglutethimide is prescribed to treat certain tumors that affect the adrenal cortex. This drug is also used to prevent over- ... Aminoglutethimide is the drug which acts on the adrenal cortex. Production of steroids is affected by its administration. ...
ISRCTN - ISRCTN44725655: Comparison of second-line hormonal agents medroxyprogesterone acetate and aminoglutethimide in...
2. Group B: Aminoglutethimide 250 mg twice daily plus hydrocortisone 20 mg twice daily until disease progression or failure of ... Comparison of second-line hormonal agents medroxyprogesterone acetate and aminoglutethimide in advanced breast cancer. ... Comparison of second-line hormonal agents medroxyprogesterone acetate and aminoglutethimide in advanced breast cancer ...
Low dose aminoglutethimide (125 mg twice daily) with hydrocortisone for the treatment of advanced postmenopausal breast cancer....
Aminoglutethimide 125 mg twice daily and hydrocortisone 20 mg twice daily was used to treat 76 postmenopausal women with ... Aminoglutethimide 125 mg twice daily and hydrocortisone 20 mg twice daily was used to treat 76 postmenopausal women with ... Low dose aminoglutethimide (125 mg twice daily) with hydrocortisone for the treatment of advanced postmenopausal breast cancer. ... Low dose aminoglutethimide (125 mg twice daily) with hydrocortisone for the treatment of advanced postmenopausal breast cancer. ...
Aminoglutethimide - Healthery
Aminoglutethimide is an adrenal anti-steroid drug that inhibits the productions of particular hormones. It is a synthetic ... Aminoglutethimide. Aminoglutethimide is used as a treatment for certain types of cancer that affect the adrenal cortex and is ... In the U.S. the brand name of aminoglutethimide is cytadren. Aminoglutethimide should only be prescribed by a doctor and is ... The following drugs may cause interactions with Aminoglutethimide:. *A combination of Docetaxel and Aminoglutethimide increase ...
AMINOGLUTETHIMIDE | SelfDecode | Genome Analysis
Aminoglutethimide has been used in the treatment of advanced breast and prostate cancer. It was formerly used for its weak ... Aminoglutethimide co-treated with 17-alpha-hydroxy-progesterone caproate] results in decreased expression of PGR protein. R ... Aminoglutethimide co-treated with Hydrogen Peroxide] results in increased oxidation of MPO protein. R ... Aminoglutethimide reduces the production of D5-pregnenolone and blocks several other steps in steroid synthesis, including the ...
Depo-Medrol (methylprednisolone acetate) for Inflammation, Allergies, Disease Flares: Uses, Dosage, Side Effects, Interactions,...
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Drug Information
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Buy Legal Anti Estrogen Steroids Powder Aminoglutethimide With No Side Effects 125 from Zhuhaishi Shaohui Technology Co.,ltd, ... Aminoglutethimide. Synonyms:. alpha-(p-Aminophenyl)-alpha-ethylglutarimide. CAS:. 125-84-8. EINECS:. 204-756-4. MF:. C13H16N2O2 ... Name:Aminoglutethimide Synonyms: 2-(p-aminophenyl)-2-ethyl-glutarimid;2-(p-Aminophenyl)-2-ethylglutarimide;. 2-(p-Aminophenyl)- ... Home,Products,Cancer Treatment Steroids,Legal Anti Estrogen Steroids Powder Aminoglutethimide With No Side Effects 125 ...
Medical adrenalectomy using aminoglutethimide and dexamethasone in advanced breast cancer<...
Medical adrenalectomy using aminoglutethimide and dexamethasone in advanced breast cancer. / Lipton, Allan; Santen, Richard J. ... Medical adrenalectomy using aminoglutethimide and dexamethasone in advanced breast cancer. Cancer. 1974 Feb;33(2):503-512. ... Twelve women with advanced breast carcinoma were given aminoglutethimide (up to 2 gm q.d. p.o.), in addition to dexamethasone ( ... Lipton, A., & Santen, R. J. (1974). Medical adrenalectomy using aminoglutethimide and dexamethasone in advanced breast cancer. ...
CytadrenPlus hydrocortisoneKetoconazoleWomen with Advanced Breast CarcinomaInhibitorDosage1000 mgEither aminoglutethimideDaily and hydrocortisoneMetabolism of dexamethasoneTestolactoneGlucocorticoidAdrenocorticalTamoxifenAdrenalectomyDosePostmenopausal womenInhibitionSynthesisMetastaticConversion of cholesterolSteroidsDecreaseTherapyAntineoplasticTumorMedicationOralProgesteroneCortisolProstate cancerTreatmentSimultaneousBreastPatients treatedSecretion
Cytadren9
- 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. (wikipedia.org)
- Cytadren, aminoglutethimide tablets USP, is an inhibitor of adrenocortical steroid synthesis, available as 250-mg tablets for oral administration. (rxlist.com)
- Cytadren (aminoglutethimide) is indicated for the suppression of adrenal function in selected patients with Cushing's syndrome . (rxlist.com)
- Because Cytadren (aminoglutethimide) does not affect the underlying disease process, it is used primarily as an interim measure until more definitive therapy such as surgery can be undertaken or in cases where such therapy is not appropriate. (rxlist.com)
- Cytadren (aminoglutethimide) should be used only in those patients who are responsive to treatment. (rxlist.com)
- Untoward effects have been reported in about 2 out of 3 patients with Cushing's syndrome who were treated for 4 or more weeks with Cytadren (aminoglutethimide) as the only adrenocortical suppressant. (rxlist.com)
- In the U.S. the brand name of aminoglutethimide is cytadren. (healthery.com)
- Cytadren, officially known as aminoglutethimide first hit the market in 1960 as an anticonvulsant and as an AI in 1967 under the Cytadren name manufactured by Ciba. (steroid.com)
- Be sure to mention aminoglutethimide (Cytadren). (medlineplus.gov)
Plus hydrocortisone4
- A randomized trial comparing surgical adrenalectomy with aminoglutethimide plus hydrocortisone in women with advanced breast cancer. (nih.gov)
- 2. Group B: Aminoglutethimide 250 mg twice daily plus hydrocortisone 20 mg twice daily until disease progression or failure of treatment. (isrctn.com)
- Monthly serum dehydroepiandrosterone sulfate, androstenedione, testosterone, dihydrotestosterone, and free testosterone levels were measured in 94 of 129 patients with castration resistant prostatic carcinoma treated on a clinical protocol with aminoglutethimide (1000 mg/day) plus hydrocortisone (40 mg/day) Base-line steroid levels were not found to be age related. (elsevier.com)
- Therapy with aminoglutethimide plus hydrocortisone as administered in this study may not uniformly achieve the objective of suppressing adrenal androgen production. (elsevier.com)
Ketoconazole6
- Median Range Karnofsky performance status 90 80 70 Site of metastatic disease Bone Lymph nodes Liver Bone marrow Soft tissue Lung Bladder Perirectal mass Prior therapy Orchiectomy Radiation to prostate Radiation to metastases Flutamide Leuprolide Hydrocortisone Megestrol acetate Diethylstilbestrol Ketoconazole Goserelin Aminoglutethimide Suramin Estramustine Tamoxifen. (tripod.com)
- Drugs such as aminoglutethimide or ketoconazole may stop the adrenal glands from producing hormones. (clinicaltrials.gov)
- Combining hydrocortisone with either aminoglutethimide or ketoconazole may be an effective treatment for prostate cancer. (clinicaltrials.gov)
- PURPOSE: Phase II trial to study the effectiveness of combining hydrocortisone with either aminoglutethimide or ketoconazole in treating patients who have localized stage IV prostate cancer. (clinicaltrials.gov)
- OBJECTIVES: I. Determine the Prostate-Specific Antigen (PSA) response proportion and duration of response of patients with localized stage IV (D0.5) adenocarcinoma of the prostate treated with early medical adrenalectomy using hydrocortisone combined with aminoglutethimide or ketoconazole after prior antiandrogen withdrawal. (clinicaltrials.gov)
- Patients undergo medical adrenalectomy using hydrocortisone combined with aminoglutethimide OR ketoconazole. (clinicaltrials.gov)
Women with Advanced Breast Carcinoma1
- Twelve women with advanced breast carcinoma were given aminoglutethimide (up to 2 gm q.d. p.o.), in addition to dexamethasone (1.0-3.0 mg daily) and Florinef (0.1 mg b.i.w.) in order to produce a medical adrenalectomy. (elsevier.com)
Inhibitor7
- Aminoglutethimide is an aromatase inhibitor that is FDA approved for the treatment of suppression of adrenal function in selected patients with Cushing's syndrome . (wikidoc.org)
- We randomized 96 postmenopausal women with metastatic breast carcinoma to receive surgical adrenalectomy or medical therapy with an adrenal inhibitor, aminoglutethimide (AG), plus replacement hydrocortisone. (nih.gov)
- The effects of structurally different antiestrogens, progesterone and the aromatase inhibitor aminoglutethimide, were evaluated for chemopreventive activity in the N-methyl-N-nitrosourea (MNU)-induced mammary carcinogenesis model. (nih.gov)
- Aminoglutethimide, a known inhibitor of steroid synthesis, is also a potent blocker of the aromatase enzyme and, thus, of estrogen production. (annals.org)
- A prospective study was performed to investigate the combination of the aromatase inhibitor aminoglutethimide and hydrocortisone in androgen-independent prostate cancer with changes in prostate-specific antigen (PSA) level as main determinant for response. (eur.nl)
- Aminoglutethimide is an aromatase (CYP19A1) and steroid 11β-hydroxylase (CYP11A1) inhibitor. (guidetopharmacology.org)
- An inhibitor of adrenal steroid biosynthesis, aminoglutethimide, was administered to seven patients with low renin essential hypertension, and the antihypertensive action of the drug was compared with its effects on adrenal steroid production. (utmb.edu)
Dosage2
- Therapeutic dosage of Aminoglutethimide is 4.8 mg/kg of body weight which is administered 8 hourly in an adult to treat a variety of health disorders including breast cancer and prostate cancer . (findatopdoc.com)
- Minor side effects attributable to aminoglutethimide (nystagmus, ataxia, lethargy, skin rash) were seen frequently but abated with reduction in dosage. (elsevier.com)
1000 mg1
- Thirty-five patients were treated with aminoglutethimide 1000 mg daily and hydrocortisone acetate 40 mg daily. (eur.nl)
Either aminoglutethimide1
- however, the combination regimen was no more effective than either aminoglutethimide or progesterone administered alone. (nih.gov)
Daily and hydrocortisone1
- Aminoglutethimide 125 mg twice daily and hydrocortisone 20 mg twice daily was used to treat 76 postmenopausal women with advanced breast cancer. (ox.ac.uk)
Metabolism of dexamethasone2
- Since aminoglutethimide increases the rate of metabolism of dexamethasone but not that of hydrocortisone, the latter is preferred as the adrenal glucocorticoid replacement. (drugbank.ca)
- Escape from blockade, when observed, was attributed to the rapid metabolism of dexamethasone induced by aminoglutethimide, demonstrated by determining the half‐life of 3 H‐dexamethasone before and during treatment. (elsevier.com)
Testolactone2
- We now report the results of studies which have examined the cytotoxicity, antiaromatase, and intrinsic estrogenic activities of aminoglutethimide, 1,2-dehydrotestolactone (testolactone), dihydrotestosterone, 4-hydroxy-4-androstene-3,17-dione, and 10-propargylestr-4-ene-3,17-dione within MCF-7 monolayer cultures. (aacrjournals.org)
- testolactone = aminoglutethimide). (aacrjournals.org)
Glucocorticoid2
- We developed an effective regimen to inhibit estrogen production in postmenopausal women using aminoglutethimide and replacement glucocorticoid. (annals.org)
- One hundred forty-seven women initially received aminoglutethimide and replacement glucocorticoid as treatment of metastatic breast carcinoma. (annals.org)
Adrenocortical2
- A decrease in adrenal secretion of cortisol is followed by an increased secretion of pituitary adrenocorticotropic hormone (ACTH), which will overcome the blockade of adrenocortical steroid synthesis by aminoglutethimide. (drugbank.ca)
- Aminoglutethimide may cause adrenocortical hypofunction, especially under conditions of stress , such as surgery , trauma , or acute illness. (wikidoc.org)
Tamoxifen4
- Chemoprevention of MNU-induced mammary tumorigenesis by hormone response modifiers: toremifene, RU 16117, tamoxifen, aminoglutethimide and progeste. (nih.gov)
- Eleven tamoxifen and 13 aminoglutethimide pa. (tripod.com)
- Modulatory influences of tamoxifen, tocopherol, retinyl acetate, aminoglutethimide, ergocryptine and selenium on DMBA-induced initiation of mammary carcinogenesis in rats. (bvsalud.org)
- Present study evaluates the chemopreventive actions of tamoxifen (10 mg/kg), retinyl acetate (50 mg/kg), tocopherol (200 mg/kg), aminoglutethimide (1 mg/kg), ergocryptine (5 mg/kg), and sodium selenite (1 mg/kg) when given singly/in combinations on the initiation of mammary carcinogenesis induced by 20 mg of DMBA in virgin female rats . (bvsalud.org)
Adrenalectomy1
- Lipton, A & Santen, RJ 1974, ' Medical adrenalectomy using aminoglutethimide and dexamethasone in advanced breast cancer ', Cancer , vol. 33, no. 2, pp. 503-512. (elsevier.com)
Dose1
- Low dose aminoglutethimide (125 mg twice daily) with hydrocortisone for the treatment of advanced postmenopausal breast cancer. (ox.ac.uk)
Postmenopausal women1
- A group of 213 unselected postmenopausal women with advanced breast cancer were treated with aminoglutethimide, 250 mg 4 times a day, and hydrocortisone, 20 mg 2 times a day. (aacrjournals.org)
Inhibition1
- Although aminoglutethimide inhibits the synthesis of thyroxine by the thyroid gland, the compensatory increase in thyroid-stimulating hormone (TSH) is frequently of sufficient magnitude to overcome the inhibition of thyroid synthesis due to aminoglutethimide. (drugbank.ca)
Synthesis1
- Aminoglutethimide reduces the production of D5-pregnenolone and blocks several other steps in steroid synthesis, including the C-11, C-18, and C-21 hydroxylations and the hydroxylations required for the aromatization of androgens to estrogens, mediated through the binding of aminoglutethimide to cytochrome P-450 complexes. (drugbank.ca)
Metastatic1
- Cancer treat rev 9-204, 198 7 lawrence bv, lipton a, harvey ha, et al: influence of estrogen receptor status on response of metastatic breast cancer to aminoglutethimide therapy. (tripod.com)
Conversion of cholesterol1
- Aminoglutethimide inhibits the enzymatic conversion of cholesterol to D5-pregnenolone, resulting in a decrease in the production of adrenal glucocorticoids, mineralocorticoids, estrogens, and androgens. (drugbank.ca)
Steroids1
- The observation that chronic administration of aminoglutethimide lowered blood pressure in these patients and elevated their plasma renin activity to the normal range without decreasing production of the adrenal steroids, deoxycorticosterone, 18-hydroxydeoxycorticosterone, and 16β-hydroxydehydroepiandrosterone, makes it unlikely that these steroids are responsible either for the decreased renin or the elevated blood pressure in patients with low renin essential hypertension. (utmb.edu)
Decrease4
- Acetyldigitoxin may decrease the cardiotoxic activities of Aminoglutethimide. (drugbank.ca)
- Acetyldigoxin may decrease the cardiotoxic activities of Aminoglutethimide. (drugbank.ca)
- The gradual lowering of blood pressure and body weight during aminoglutethimide therapy is consistent with the view that the antihypertensive effect of the drug is mediated through a reduction in the patients' extracellular fluid volume, probably secondary to the persistent decrease in aldosterone production. (utmb.edu)
- Aminoglutethimide is used to decrease the production of sex hormones (estrogen in women or testosterone in men) and suppress the growth of tumors that need sex hormones to grow. (cancer.gov)
Therapy5
- Thirty-eight % of patients responding to previous endocrine therapy responded to aminoglutethimide compared with 19% of patients who had progressed on previous endocrine therapy. (aacrjournals.org)
- Aminoglutethimide is an effective endocrine therapy in advanced postmenopausal breast cancer, particularly for bone deposits. (aacrjournals.org)
- We conclude that aminoglutethimide is a valuable second-line therapy for patients with androgen-independent prostate cancer. (eur.nl)
- Mean arterial pressure was reduced from a pretreatment value of 117±2 (mean±SE) mm Hg to 108±3 mm Hg after 4 days of aminoglutethimide therapy and further to 99±3 mm Hg when drug administration was stopped (usually 21 days). (utmb.edu)
- Plasma renin activity was not significantly increased after 4 days of treatment but had risen to the normal range by the termination of aminoglutethimide therapy. (utmb.edu)
Antineoplastic1
- aminoglutethimide, it is a hormone antineoplastic agent. (disqueenfrance.com)
Tumor1
- Aminoglutethimide, RU 16117 and toremifene citrate, in addition to their effects on tumor multiplicity, caused significant increases in the latency period for tumor development. (nih.gov)
Medication1
- Upon withdrawal of medication with aminoglutethimide, the capability of the adrenal glands to produce steroid returns within 72 hours. (healthery.com)
Oral1
- Oral aminoglutethimide is administered twice daily for 1 week and then 4 times daily during subsequent weeks. (clinicaltrials.gov)
Progesterone1
- Mean plasma concentrations of deoxycorticosterone and cortisol were unchanged during aminoglutethimide treatment whereas those of 18-hydroxydeoxycorticosterone, progesterone, 17α-hydroxyprogesterone, and 11-deoxycortisol were increased as compared to pretreatment values. (utmb.edu)
Cortisol1
- Aminoglutethimide has also been shown to modify the extra-adrenal metabolism of cortisol. (bmj.com)
Prostate cancer1
- Aminoglutethimide has been used in the treatment of advanced breast and prostate cancer. (drugbank.ca)
Treatment3
- Aminoglutethimide is used as a treatment for certain types of cancer that affect the adrenal cortex and is sometimes used in cases where the adrenal cortex is overactive but not cancerous. (healthery.com)
- In contrast, aminoglutethimide treatment reduced mean plasma aldosterone concentrations to about 30% of control values. (utmb.edu)
- Excretion rates of 16β-hydroxydehydroepiandrosterone, 16-oxo-androstenediol, 17-hydroxycorticosteroids and 17-ketosteroids, and the secretion rate of 16β-hydroxydehydroepiandrosterone were not significantly altered by aminoglutethimide treatment whereas the excretion rate of aldosterone was reduced from 3.62±0.5 (mean±SE) in the control period to 0.9±0.2 μg/24 h after 4 days and to 1.1±0.3 μg/24 h at the termination of aminoglutethimide treatment. (utmb.edu)
Simultaneous2
- A. M. ADAM, I. D. Bradbrook, H. J. Rogers: The simultaneous assay of aminoglutethimide and Its acetyl metabolite by high performance liquid chromatography. (ac.ke)
- A simple rapid high-performance liquid chromatographic assay for simultaneous estimation of aminoglutethimide and its acetylated metabolite acetylamidoglutethimide in plasma, saliva, and urine is described. (ac.ke)
Breast1
- Suppression of plasma 6-keto-prostaglandin F1 alpha and 13,14-dihydro-15-keto-prostaglandin F2 alpha by aminoglutethimide in advanced breast cancer. (ox.ac.uk)
Patients treated1
- Marked leukopenia and/or thrombocytopenia occurred in 12 of 1333 patients treated with aminoglutethimide (0.9% incidence). (elsevier.com)
Secretion1
- In spite of an increase in TSH, aminoglutethimide has not been associated with increased prolactin secretion. (drugbank.ca)