Drugs that inhibit 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE. They are commonly used to reduce the production of DIHYDROTESTOSTERONE.
Steroidal compounds in which one or more carbon atoms in the steroid ring system have been substituted with nitrogen atoms.
An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.
Inability to empty the URINARY BLADDER with voiding (URINATION).
Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both.
An enzyme that catalyzes the reduction of TESTOSTERONE to 5-ALPHA DIHYDROTESTOSTERONE.
An oxidoreductase that catalyzes the conversion of 3-oxo-delta4 steroids into their corresponding 5alpha form. It plays an important role in the conversion of TESTOSTERONE into DIHYDROTESTOSTERONE and PROGESTERONE into DIHYDROPROGESTERONE.
Compounds that inhibit HMG-CoA reductases. They have been shown to directly lower cholesterol synthesis.
A subclass of enzymes which includes all dehydrogenases acting on carbon-carbon bonds. This enzyme group includes all the enzymes that introduce double bonds into substrates by direct dehydrogenation of carbon-carbon single bonds.
An enzyme that catalyzes reversibly the oxidation of an aldose to an alditol. It possesses broad specificity for many aldoses. EC 1.1.1.21.
A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.
A fungal metabolite isolated from cultures of Aspergillus terreus. The compound is a potent anticholesteremic agent. It inhibits 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It also stimulates the production of low-density lipoprotein receptors in the liver.
An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES).
Enzymes that catalyze the reversible reduction of alpha-carboxyl group of 3-hydroxy-3-methylglutaryl-coenzyme A to yield MEVALONIC ACID.
7-carbon saturated monocarboxylic acids.
Compounds based on reduced IMIDAZOLINES which contain no double bonds in the ring.
Oxidoreductases that are specific for the reduction of NITRATES.
Azoles of one NITROGEN and two double bonds that have aromatic chemical properties.
Fatty acids which are unsaturated in only one position.
A polyhydric alcohol with about half the sweetness of sucrose. Sorbitol occurs naturally and is also produced synthetically from glucose. It was formerly used as a diuretic and may still be used as a laxative and in irrigating solutions for some surgical procedures. It is also used in many manufacturing processes, as a pharmaceutical aid, and in several research applications.
Reversibly catalyzes the oxidation of a hydroxyl group of sugar alcohols to form a keto sugar, aldehyde or lactone. Any acceptor except molecular oxygen is permitted. Includes EC 1.1.1.; EC 1.1.2. and EC 1.1.99.
Catalyzes the oxidation of GLUTATHIONE to GLUTATHIONE DISULFIDE in the presence of NADP+. Deficiency in the enzyme is associated with HEMOLYTIC ANEMIA. Formerly listed as EC 1.6.4.2.
A FLAVOPROTEIN oxidoreductase that occurs both as a soluble enzyme and a membrane-bound enzyme due to ALTERNATIVE SPLICING of a single mRNA. The soluble form is present mainly in ERYTHROCYTES and is involved in the reduction of METHEMOGLOBIN. The membrane-bound form of the enzyme is found primarily in the ENDOPLASMIC RETICULUM and outer mitochondrial membrane, where it participates in the desaturation of FATTY ACIDS; CHOLESTEROL biosynthesis and drug metabolism. A deficiency in the enzyme can result in METHEMOGLOBINEMIA.
A group of enzymes that oxidize diverse nitrogenous substances to yield nitrite. (Enzyme Nomenclature, 1992) EC 1.
The class of all enzymes catalyzing oxidoreduction reactions. The substrate that is oxidized is regarded as a hydrogen donor. The systematic name is based on donor:acceptor oxidoreductase. The recommended name will be dehydrogenase, wherever this is possible; as an alternative, reductase can be used. Oxidase is only used in cases where O2 is the acceptor. (Enzyme Nomenclature, 1992, p9)
An enzyme that utilizes NADH or NADPH to reduce FLAVINS. It is involved in a number of biological processes that require reduced flavin for their functions such as bacterial bioluminescence. Formerly listed as EC 1.6.8.1 and EC 1.5.1.29.
A FLAVOPROTEIN enzyme that catalyzes the oxidation of THIOREDOXINS to thioredoxin disulfide in the presence of NADP+. It was formerly listed as EC 1.6.4.5
Substances used to lower plasma CHOLESTEROL levels.
A flavoprotein that catalyzes the reduction of heme-thiolate-dependent monooxygenases and is part of the microsomal hydroxylating system. EC 1.6.2.4.

Mutagenicity tests on epristeride in vitro and in vivo. (1/197)

AIM: To evaluate the genetic effects of epristeride (Epr), a new prospective drug for treating benign prostatic hyperplasia. METHODS: 1) Assaying reverse mutation in histidine nutritional deficiency strain of Salmonella typhimurium 2) detecting chromosome aberrations in Chinese hamster lung cells (CHL); 3) micronucleus assays of mouse bone marrow; 4) counting sperm shape abnormalities 35 d after first ig Epr. RESULTS: 1) The reverse mutation happened at almost the same rate of the negative control. Epr did not induce bacterial mutation. 2) In vitro, the rates of aberration were all below 3%, thus Epr did not induce chromosome damage in CHL. 3) Micronucleated polychromatic erythroblasts (PCE) were not apparently more than those of sovent control, Epr did not induce the formation of micronuclei in PCE. 4) With Epr 818, 682, and 341 mg.kg-1, the head abnormalities of sperms were 5.3% +/- 2.7%, 5.3% +/- 1.9%, and 5.2% +/- 1.2%, respectively. CONCLUSION: No genetic toxicity of Epr was detected.  (+info)

Z-350, a novel compound with alpha 1-adrenoceptor antagonistic and steroid 5 alpha-reductase inhibitory actions: pharmacological properties in vivo. (2/197)

The alpha(1)-adrenoceptor-antagonistic and steroid 5alpha-reductase-inhibitory actions of Z-350 [(S)-4-{3-{4-{1-(4-methylphenyl)-3-[4-(2-methoxyphenyl)piperazine-1-y l]propoxy}benzoyl}indole-1-yl}butyric acid hydrochloride] were investigated in rabbits and rats in vivo. Z-350 (1-30 mg/kg), administered intraduodenally, dose-dependently inhibited phenylephrine-induced increases in prostatic urethral pressure with an ED(50) value of 3.8 mg/kg in anesthetized male rabbits, whereas the effects on mean blood pressure and orthostatic hypotensive response were weaker when compared with other alpha(1)-adrenoceptor antagonists, tamsulosin and prazosin. Z-350 (1-10 mg/kg p.o.) dose-dependently inhibited the prostatic steroid 5alpha-reductase activity in rats with an ED(50) value of 2.8 mg/kg. The daily oral administration of Z-350, at >==10 mg/kg for 7 days, significantly reduced the prostatic growth induced by testosterone in castrated rats, with no effect on dihydrotestosterone-induced prostatic growth. These results indicate that Z-350 exhibited alpha(1)-adrenoceptor-antagonistic and 5alpha-reductase inhibitory actions at almost equal doses in vivo, and was expected to improve the bladder outlet obstruction associated with benign prostatic hyperplasia with smaller cardiovascular adverse effect.  (+info)

Evaluation of the EDSTAC female pubertal assay in CD rats using 17beta-estradiol, steroid biosynthesis inhibitors, and a thyroid inhibitor. (3/197)

The Endocrine Disrupter Screening and Testing Advisory Committee has recommended the female pubertal onset assay as a Tier I test to detect potential endocrine-disrupting chemicals (EDs). We evaluated this assay's ability to detect EDs acting through various mechanisms. In two similar experiments, weanling female rats were dosed for 20 days by gavage with vehicle (0.5% methocel) or the following test compounds (mg/kg/day): 17beta-estradiol (E2; 0.1, 2, or 4), ketoconazole (KETO; 24, 50, or 100), finasteride (FIN; 20), testolactone (TL; 220), fadrozole (FAD; 0.6, 1.2, or 6.0) or 6-propylthiouracil (PTU; 240). In vehicle-treated females, mean age at pubertal onset, as evidenced by vaginal opening (VO), varied interexperimentally from 32.3+/-1.6 days to 33.5+/-1.8 days. At 0.1 mg/kg E2, age at VO was reduced slightly to 31.0+/-1.6 days, but not significantly (alpha=0.05). Higher E2 doses (2.0 and 4.0) reduced age at VO to 28 days. KETO delayed VO, but this delay was significant only at 100 mg/kg (39.7+/-2.4 days). FIN and TL had no effect on age at pubertal onset; however, FAD significantly delayed VO. PTU delayed VO to 34.2+/-1.1 days and altered thyroid weight, histology, and hormone levels. With each compound, significant changes in age at VO were accompanied by decreased uterine or ovarian weights. Thus, although this assay did not detect TL or lower doses of E2 (0.1 mg/kg) or KETO (< or = 50 mg/kg), it was capable of detecting EDs operating through a variety of mechanisms.  (+info)

Steroid 5alpha-reductase inhibitory activity and hair regrowth effects of an extract from Boehmeria nipononivea. (4/197)

The acetone extract of Boehmeria nipononivea showed both potent 5alpha-reductase inhibitory activity and hair regrowth promotion effects on mice. 5alpha-Reductase inhibitory activity-guided fractionation led to six active fatty acids: alpha-linolenic, linoleic, palmitic, elaidic, oleic and stearic acids. The extract of B. nipononivea, and alphalinolenic, elaidic and stearic acids exhibited a hair regrowth effect.  (+info)

Anti-tumour effects and pharmacokinetic profile of 17-(5'-isoxazolyl)androsta-4,16-dien-3-one (L-39) in mice: an inhibitor of androgen synthesis. (5/197)

17-(5'-Isoxazolyl)androsta-4,16-dien-3-one (L-39), a novel androstene derivative, was synthesized and evaluated in vitro and in vivo. L-39 showed potent and non-competitive inhibition of human testicular microsomal 17alpha-hydroxylase/C(17,20)-lyase with an IC50 value of 59 nM and Ki of 22 nM. L-39 also showed potent and competitive inhibition of 5alpha-reductase in human prostatic microsomes with IC50 and Ki values of 33 and 28 nM respectively. L-39 (5 microM) has also been shown to manifest anti-androgenic activity in cultures of human prostate cancer cell lines (LNCaP) by preventing the labelled synthetic androgen R1881 (5 nM) from binding to the androgen receptors. Androgen-dependent human prostate cancer xenografts (PC-82) were grown in nude mice and the effects of L-39 (50 mg kg(-1) day(-1)) on tumour growth and prostate-specific antigen (PSA) levels were determined after 28 days. L-39 significantly (P < 0.01) diminished tumour growth and wet weights to a similar extent as castration or flutamide treatment. L-39 also significantly (P < 0.01) reduced serum PSA levels by more than 80% in the mice bearing human prostate cancer xenografts. Pharmacokinetic studies were also conducted in male Balb/c mice. After subcutaneous administration of a single bolus dose, L-39 was rapidly absorbed into the systemic circulation. Peak plasma levels occurred at 0.75 h and then declined with a t(1/2) of 1.51 h. The bioavailability of L-39 after subcutaneous administration was 28.5%. These results demonstrate that L-39 is a potent inhibitor of androgen synthesis and is effective in reducing the growth of human prostate cancer xenografts in nude mice. Although improvements in the bioavailability are necessary, L-39 is a potential lead compound with this profile as an inhibitor of prostate cancer growth.  (+info)

Effects of a new steroidal aromatase inhibitor, TZA-2237, and/or chlormadinone acetate on hormone-induced and spontaneous canine benign prostatic hyperplasia. (6/197)

OBJECTIVE: It has been known for many years that human benign prostatic hyperplasia (BPH) is composed predominantly of hyperplastic stromal cells rather than epithelial cells. In the present study the effects of a new steroidal aromatase inhibitor on hormone-induced and spontaneous canine BPH were investigated. METHODS: (1) Effects of TZA-2237 on hormone-induced canine BPH. Ten castrated beagles were administered testosterone and androstenedione 6 days/week for 8 months, and divided randomly into three groups after 2 months of treatment as follows. Group I served as controls, Group II was given 0.5 and Group III was given 2.5 mg/kg/day TZA-2237 5 days/week for 6 months. (2) Effects of TZA-2237 on spontaneous canine BPH. Twenty aged beagles with BPH were divided into five groups, Group IV was untreated, Group V was treated with 1 and Group VI with 5mg/kg/day TZA-2237 5 days/week for 31 weeks. Group VII was treated with 5mg/kg/day Atamestane and Group VIII was treated with 0.3 mg/kg/day chlormadinone acetate (CMA) 5 days/week. (3) Effects of TZA-2237 combined with CMA on spontaneous canine BPH. Three aged beagles with BPH were treated with 1mg/kg/day TZA-2237 and 0.03 mg/kg/day CMA 5 days/week for 20 weeks (Group IX) and a further three aged beagles with BPH were treated with 0.3 mg/kg/day CMA alone 5 days/week (Group X). RESULTS: Hormone-induced prostatic growth was significantly suppressed in group III compared with that in other groups. In Group III, the intraprostatic aromatase activity, estradiol level and androgen receptor content decreased significantly in comparison with the values in Group I. The prostatic weights in Groups V, VI and VII increased significantly in comparison with the weight in Group IV. Serum LH and testosterone levels in Groups V, VI, and VII increased significantly in comparison with the level in Group IV. The prostatic weight in Group IX was decreased only slightly, but the smooth muscle component was decreased significantly. CONCLUSIONS: TZA-2237 is a new, unique and effective aromatase inhibitor that causes inhibition of both epithelial and stromal compartments in hormone-induced canine BPH. Dual inhibition of androgen and estrogen resulted in inhibition of smooth muscle growth, and should prove effective as a new method of treatment given the atrophic effects on not only the epithelium but also the stroma in human BPH.  (+info)

Increased levels of clusterin (SGP-2) mRNA and protein accompany rat ventral prostate involution following finasteride treatment. (7/197)

Finasteride is a well-known inhibitor of the prostatic enzyme 5 alpha-reductase type 2 which prevents conversion of testosterone into 5 alpha-dihydrotestosterone, the active intraprostatic androgen, which causes prostate involution through a combination of cell atrophy and cell death. The drug is widely used to improve symptoms of benign prostatic hyperplasia in man. Clusterin, a glycoprotein which is generally up-regulated under conditions inducing cell atrophy or organ involution, is produced at a high level in the regressing rat ventral prostate following androgen ablation. According to several authors, clusterin does not respond to finasteride treatment, suggesting a different action of testosterone and 5 alpha-dihydrotestosterone. We show here that, under our conditions, finasteride was capable of inducing production of both clusterin mRNA and protein in the rat ventral prostate. In fact, by using different and converging techniques, such as Northern hybridization, in situ hybridization histochemistry and immunohistochemistry, we were able to show a strong induction of the clusterin gene in the epithelial cell population of the gland. The response to finasteride, which was similar to that seen with castration, occurred with a delay of a few days. In situ and immunohistochemistry experiments indicated that both orchidectomy and finasteride administration resulted in increased transition of the epithelial cells from the columnar to the cuboidal (atrophic) shape, and this was accompanied by an increased intensity of the signal for clusterin. Thus, it appears that induction of clusterin is part of the molecular process leading to prostate involution caused by either orchidectomy or finasteride administration.  (+info)

Antiandrogenic effects of novel androgen synthesis inhibitors on hormone-dependent prostate cancer. (8/197)

We have found that in addition to being potent inhibitors of 17alpha-hydroxylase/C17,20-lyase and/or 5alpha-reductase, some of our novel androgen synthesis inhibitors also interact with the mutated androgen receptor (AR) expressed in LNCaP prostate cancer cells and the wild-type AR expressed in hormone-dependent prostatic carcinomas. The effects of these compounds on the proliferation of hormone-dependent human prostatic cancer cells were determined in vitro and in vivo. L-2 and L-10 are delta4-3-one-pregnane derivatives. L-35 and L-37 are delta5-3beta-ol-androstane derivatives, and L-36 and L-39 are delta4-3-one-androstane-derived compounds. L-2, L-10, and L-36 (L-36 at low concentrations) stimulated the growth of LNCaP cells, indicating that they were interacting agonistically with the mutated AR expressed in LNCaP cells. L-35, L-37, and L-39 acted as LNCaP AR antagonists. To determine whether the growth modulatory effects of our novel compounds were specific for the mutated LNCaP AR, competitive binding studies were performed with LNCaP cells and PC-3 cells stably transfected with the wild-type AR (designated PC-3AR). Regardless of AR receptor type, all of our novel compounds were effective at preventing binding of the synthetic androgen methyl-trienolone[17alpha-methyl-(3H)-R1881 to both the LNCaP AR and the wildtype AR. L-36, L-37, and L-39 (5.0 microM) prevented binding by >90%, whereas L-35 inhibited binding by 30%. To determine whether the compounds were acting as agonists or antagonists, LNCaP cells and PC-3AR cells were transfected with the pMAMneoLUC reporter gene. When luciferase activity was induced by dihydrotestosterone, all of the compounds were found to be potent inhibitors of transcriptional activity, and the pattern of inhibition was similar for both receptor types. However, L-2, L-10, and L-36 were determined to be AR agonists, and L-35, L-37, and L-39 were wild-type AR antagonists. When tested in vivo, L-39 was the only AR antagonist that proved to be effective at inhibiting the growth of LNCaP prostate tumor growth. L-39 slowed tumor growth rate in LNCaP tumors grown in male SCID mice to the same level as orchidectomy, significantly reduced tumor weights (P < 0.05), significantly lowered serum levels of prostate-specific antigen (P < 0.02), and significanty lowered serum levels of testosterone (P < 0.05). L-39 also proved to be effective when tested against the PC-82 prostate cancer xenograft that expresses wild-type AR. These results show that some of our compounds initially developed to be inhibitors of androgen synthesis also interact with the human AR and modulate the proliferation of hormone-dependent prostatic cancer cells. Therefore, compounds such as L-39, which have multifunctional activities, hold promise for the treatment of androgen-dependent prostate tumors.  (+info)

1. Benign Prostatic Hyperplasia (BPH): The enlargement of the prostate gland can put pressure on the urethra and bladder, making it difficult to urinate.
2. Prostatitis: Inflammation of the prostate gland can cause urinary retention.
3. Bladder Outlet Obstruction: A blockage in the muscles of the bladder neck or urethra can prevent urine from flowing freely.
4. Neurological Disorders: Conditions such as multiple sclerosis, Parkinson's disease, and spinal cord injuries can disrupt the nerve signals that control urination, leading to urinary retention.
5. Medications: Certain medications, such as antidepressants, antipsychotics, and anesthetics, can cause urinary retention as a side effect.
6. Urinary Tract Infections (UTIs): UTIs can cause inflammation and scarring in the bladder or urethra, leading to urinary retention.
7. Impacted Stone: Kidney stones that are too large to pass can cause urinary retention if they become lodged in the ureter or bladder.
8. Bladder Cancer: Tumors in the bladder can grow and block the flow of urine, leading to urinary retention.
9. Urethral Stricture: A narrowing of the urethra can cause urinary retention by restricting the flow of urine.

Symptoms of urinary retention may include:

1. Difficulty starting to urinate
2. Weak or interrupted urine stream
3. Painful urination
4. Inability to fully empty the bladder
5. Frequent urination
6. Leaking of urine (incontinence)
7. Blood in the urine

Treatment for urinary retention depends on the underlying cause and may include medications, catheterization, or surgery. It is important to seek medical attention if symptoms persist or worsen over time, as untreated urinary retention can lead to complications such as kidney damage or sepsis.

Treatment options include medications such as alpha-blockers and 5-alpha-reductase inhibitors, minimally invasive therapies such as transurethral microwave therapy or laser therapy, and surgical intervention such as a transurethral resection of the prostate (TURP) or robotic-assisted laparoscopic surgery.

There are also lifestyle changes that can help manage Prostatic Hyperplasia, including limiting fluid intake before bedtime, avoiding caffeine and alcohol, and following a healthy diet. It is important to consult with a healthcare professional for proper diagnosis and treatment of this condition.

In simpler terms, Prostatic Hyperplasia is an enlargement of the prostate gland which can cause urinary problems and discomfort. Treatment options include medication, minimally invasive therapies, and surgery, and lifestyle changes can also help manage the condition.

"Synthesis and evaluation of novel steroidal oxime inhibitors of P450 17 (17 alpha-hydroxylase/C17-20-lyase) and 5 alpha- ... "Inhibitors of 5alpha -reductase type I in LNCaP cells from the roots of Angelica koreana". Planta Medica. 68 (2): 162-3. doi: ... a novel dual type I and II 5alpha-reductase inhibitor". The Journal of Steroid Biochemistry and Molecular Biology. 64 (3-4): ... Meaning the 5a-reductase inhibition activity of 1mg finasteride is equal to 18000mg saw palmetto. Spore of Japanese climbing ...
However, it can only decrease circulating DHT levels by about 25 to 54%. Alfatradiol (brand names Ell-Cranell Alpha, Pantostin ... Reductase Inhibitor Finasteride". CNS Drug Reviews. 12 (1): 53-76. doi:10.1111/j.1527-3458.2006.00053.x. PMC 6741762. PMID ... "A new look at the 5alpha-reductase inhibitor finasteride". CNS Drug Reviews. 12 (1): 53-76. doi:10.1111/j.1527-3458.2006.00053. ... McConnell J. D.; Wilson J. D.; George F. W.; Geller J.; Pappas F.; Stoner E. (1992). "Finasteride, an inhibitor of 5α-reductase ...
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It acts as a selective inhibitor of 5α-reductase type 2. The drug has been found to decrease circulating dihydrotestosterone ... 16-androstadien-3-one and MK-434 on the kinetics of pig testis microsomal testosterone-4-ene-5alpha-reductase activity". J. ... 60 (5-6): 353-9. doi:10.1016/s0960-0760(96)00223-3. PMID 9219928. S2CID 25760027. MK-434 - AdisInsight v t e v t e (Articles ... List of 5α-reductase inhibitors "MK 434 - AdisInsight". Van Hecken A, Depré M, Schwartz JI, Tjandramaga TB, Winchell GA, De ...
Wilt TJ, MacDonald R, Hagerty K, Schellhammer P, Kramer BS (April 2008). Wilt TJ (ed.). "Five-alpha-reductase Inhibitors for ... Also in trials for CRPC are : checkpoint inhibitor ipilimumab, CYP17 inhibitor galeterone (TOK-001), and immunotherapy PROSTVAC ... X-linked inhibitor of apoptosis (XIAP) is hypothesized to promote cancer cell survival and growth, the Macrophage inhibitory ... Watanabe S, Miyata Y, Kanda S, Iwata T, Hayashi T, Kanetake H, Sakai H (May 2010). "Expression of X-linked inhibitor of ...
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CPA has antiandrogenic activity, progestogenic activity, weak partial glucocorticoid activity, weak steroidogenesis inhibitor ... CPA alone has been found to suppress ovulation in 3 of 5 women at a dose of 0.5 mg/day and in 5 of 5 women at a dose of 1 mg/ ... CPA has been found to decrease inflammatory acne lesions in males by about 15% at 5 mg/day, by 45% at 25 mg/day, and by 73% at ... 15 (5): 579-88. doi:10.1016/0010-7824(77)90108-1. PMID 880829. Hümpel M, Wendt H, Dogs G, Weiss C, Rietz S, Speck U (1977). " ...
However, this was not the case in another study with a similar design that used the aromatase inhibitor testolactone. Men with ... alpha] in the ventromedial nucleus of the hypothalamus but not in the amygdala". Neuroendocrinology. 91 (2): 142-154. doi: ... role of 3 alpha- and 3 beta-androstanediols". Biol. Reprod. 51 (3): 562-71. doi:10.1095/biolreprod51.3.562. PMID 7803627. ... with or without the aromatase inhibitor anastrozole, showed that prevention of the conversion of testosterone into estradiol ...
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A substance known as torilin can be extracted from the plant and has been shown to be a potent inhibitor of 5 alpha-reductase, ... May 2003). "Torilin from Torilis japonica, as a new inhibitor of testosterone 5 alpha-reductase". Planta Med. 69 (5): 459-61. ...
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... therapy can be withdrawn in the majority of men following initial combination therapy with the dual 5alpha-reductase inhibitor ... Selective alpha-1 blockers are similar in effectiveness but have slightly different side effect profiles. Alpha blockers relax ... Effects may take longer to appear than alpha blockers, but they persist for many years. When used together with alpha blockers ... Non-selective alpha blockers such as terazosin and doxazosin may also require slow dose adjustments as they can lower blood ...
... such as alpha-1 receptor blockers, 5-alpha-reductase inhibitors, or phosphodiesterase-5 enzyme inhibitors. Those with severe/ ... 74 (5): 542-50. doi:10.1111/j.1464-410x.1994.tb09181.x. PMID 7530115. Traish AM, Hassani J, Guay AT, Zitzmann M, Hansen ML ( ... The guidewire allows a 4 to 5 French sheath to be inserted into the artery.8 Contrast material is injected through the sheath ... For example, sexual dysfunction and orthostatic hypotension are side effects of 5-alpha-reductase inhibitors. Prostatic artery ...
... indicating that lack of mane may at one time have had an alpha correlation. Although primates do not go bald, their hairlines ... "Androgenic correlates of genetic variation in the gene encoding 5alpha-reductase type 1". Journal of Human Genetics. 50 (10): ... placebo-controlled trial to determine the effectiveness of botanically derived inhibitors of 5-alpha-reductase in the treatment ... 5-alpha-reductase converts free testosterone into DHT, and is highest in the scalp and prostate gland. DHT is most commonly ...
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Wilt TJ, MacDonald R, Hagerty K, Schellhammer P, Kramer BS (April 2008). Wilt TJ (ed.). "Five-alpha-reductase Inhibitors for ... Aspirin has been found to reduce the risk of death from cancer by about 7%. COX-2 inhibitors may decrease the rate of polyp ... Angiogenesis inhibitors were once incorrectly thought to have potential as a "silver bullet" treatment applicable to many types ... Angiogenesis inhibitors and other cancer therapeutics are used in combination to reduce cancer morbidity and mortality. ...
Wilt TJ, MacDonald R, Hagerty K, Schellhammer P, Kramer BS (2008). Wilt TJ (ed.). "Five-alpha-reductase Inhibitors for prostate ... Aspirin has been found to reduce the risk of death from cancer by about 7%. COX-2 inhibitor may decrease the rate of polyp ... "Nonsteroidal anti-inflammatory drugs and cyclooxygenase-2 inhibitors for primary prevention of colorectal cancer: a systematic ... 132 (5): 1740-5. doi:10.1053/j.gastro.2007.03.044. PMID 17484871. Zheng W, Lee SA (2009). "Well-done meat intake, heterocyclic ...
Aromatase inhibitors can help to prevent the estrogenic activity of testosterone enanthate in the body. Testosterone enanthate ... 5 (4): 301-311. doi:10.1016/S2213-8587(16)00036-X. PMID 27084565. Becker KL (2001). Principles and Practice of Endocrinology ... 25 (5): 381-8. PMID 7486812. Hoeh MP, Levine LA (March 2015). "Management of Recurrent Ischemic Priapism 2014: A Complex ... Retrieved December 5, 2018. "Testosterone cypionate profile and most popular brands in USA". Anabolic Steroids Ratings and ...
Nonsteroidal inhibitors can be categorized due to their structure. Many have been obtained from azasteroid inhibitors by taking ... quinolonone Piperidones Carboxylic acids Nonsteroidal inhibitors are thought to act as competitive inhibitors on the 5α- ... reductase isozymes, except for epristeride analogues (carboxylic acids), which are noncompetitive inhibitors. Bexlosteride ... Dutasteride, however, is a so-called dual inhibitor with both 5α-R1 and 5α-R2 inhibition. IC50 for 5α-R1 is 7 nM but 6 nM for 5 ...
Fluid production can be decreased by beta blockers, alpha2-agonists, and carbonic anhydrase inhibitors. Structures of the eye ... 57 (5): 291-7. PMID 11764684.{{cite journal}}: CS1 maint: multiple names: authors list (link) Weinstein, B. I.; Kandalaft, N.; ... 5 alpha-dihydrocortisol, an enzyme inhibited by 5-alpha reductase inhibitors, may be involved in production of aqueous humour. ... Ritch, R.; Camras, C. B.; Morris, D. J.; Latif, S. A.; Vecsei, P.; Vittek, J.; Gordon, G. G.; Southren, A. L. (1991). "5 alpha- ...
This is done through alpha antagonists such as tamsulosin, or 5-alpha-reductase inhibitors such as finasteride and dutasteride ... 50 (5): 969-79, discussion 980. doi:10.1016/j.eururo.2005.12.042. PMID 16469429. Özdal OL, Özden C, Benli K, Gökkaya S, Bulut S ... 50 (5): 969-79, discussion 980. doi:10.1016/j.eururo.2005.12.042. PMID 16469429. Jensen V (January 1991). "The TURP syndrome". ... 50 (5): 969-79, discussion 980. doi:10.1016/j.eururo.2005.12.042. PMID 16469429. "Transurethral resection of the prostate (TURP ...
... selective inhibitor of the human type 1 5alpha-reductase". J. Steroid Biochem. Mol. Biol. 58 (4): 377-84. doi:10.1016/0960-0760 ... an inhibitor of 5alpha-reductase type 1, reduces dihydrotestosterone concentrations in serum and sebum without affecting ... It is a 4-azasteroid and a potent and selective inhibitor of 5α-reductase type I and shows high selectivity for inhibition of ... 67-. Machetti, Fabrizio; Guarna, Antonio (2005). "Novel inhibitors of 5α-reductase". Expert Opinion on Therapeutic Patents. 12 ...
December 2006). "The importance of dual 5alpha-reductase inhibition in the treatment of male pattern hair loss: results of a ... and alpha-Linolenic acid (ALA) The scalp must be cleaned from sebum, sweat, and dirt, prior to topical application, for agents ... Choi GS, Kim JH, Oh SY, Park JM, Hong JS, Lee YS, Lee WS (August 2016). "Safety and Tolerability of the Dual 5-Alpha Reductase ... Inhibitor Dutasteride in the Treatment of Androgenetic Alopecia". Annals of Dermatology. 28 (4): 444-450. doi:10.5021/ad. ...
Alpha reductase inhibitors in androgenetic alopecia: Shifting paradigms, current concepts, comparative efficacy, and safety". ... Frye SV (2006). "Discovery and clinical development of dutasteride, a potent dual 5alpha-reductase inhibitor". Current Topics ... Since dutasteride is an inhibitor of both type 1 and 2 5α-reductases, it could theoretically be a more effective therapy for ... inhibitor of all three isoforms of 5α-reductase, types I, II, and III (IC50 values are 3.9 nM for type I and 1.8 nM for type II ...
... (developmental code name LY-320,236) is a selective inhibitor of the 5α-reductase, with dual effects on both the ... The scheme used to produce a somewhat more complex 5-a-reductase inhibitor relies on a chiral auxiliary to yield the final ... 5α-Reductase inhibitor List of 5α-reductase inhibitors Chang C (2002). Androgens and androgen receptor : mechanisms, functions ... US 5622962, Audia JR, McQuaid LA, Neubauer BL, Rocco VP, "5-alpha-reductase inhibitors", issued 22 April 1997, assigned to Eli ...
HMG-CoA reductase inhibitors (statins) for lowering LDL cholesterol inhibitors: hypolipidaemic agents. Drugs affecting the ... selective alpha-1 blockers, sildenafils, fertility medications. Hormonal contraception. Ormeloxifene. Spermicide. NSAIDs, ... Anti-allergy: mast cell inhibitors. Anti-glaucoma: adrenergic agonists, beta-blockers, carbonic anhydrase inhibitors/ ... Cytotoxic drugs, therapeutic antibodies, sex hormones, aromatase inhibitors, somatostatin inhibitors, recombinant interleukins ...
BPH may respond to alpha blocker and 5-alpha-reductase inhibitor therapy, or surgically with prostatectomy or transurethral ... Medications: Anticholinergics and medications with anticholinergic properties, alpha-adrenergic agonists, opiates, nonsteroidal ... "The role of alpha blockers prior to removal of urethral catheter for acute urinary retention in men". The Cochrane Database of ... resection of the prostate (TURP).[citation needed] Use of alpha-blockers can provide relief of urinary retention following de- ...
Some individuals do not produce any pre-ejaculate fluid, while others emit as much as 5 ml (0.18 imp fl oz; 0.17 US fl oz). The ... 28 (3): 374-5. doi:10.2164/jandrol.107.002576. PMID 17251594. Chughtai B, Sawas A, O'Malley RL, Naik RR, Ali Khan S, Pentyala S ... A few case reports have indicated satisfactory results when such individuals are treated with a 5-alpha-reductase inhibitor, ...
This reduced form of the coenzyme is then a substrate for any of the reductases in the cell that need to transfer hydrogen ... Nonessensial amino acid synthesis depends on the formation of the appropriate alpha-keto acid, which is then transaminated to ... The enzymes that catalyze these chemical reactions can then be purified and their kinetics and responses to inhibitors ... 31 (5): 284-91. doi:10.1016/j.tibs.2006.03.007. PMID 16616498. Duarte NC, Becker SA, Jamshidi N, Thiele I, Mo ML, Vo TD, et al ...
... also called alpha-C). In this process, the alcohol group of the alpha-carbon is deprotonated and the resulting lone pair of ... showed that such high concentrations of D-2HG could act as a direct inhibitor of lactate dehydrogenase in mouse T cells. ... oxalosuccinate reductase as an ancestral form of isocitrate dehydrogenase". Journal of Bacteriology. 190 (6): 2050-2055. doi: ... in the Mn2+ isocitrate porcine IDH complex to deprotonate the alcohol off the alpha-carbon atom. The oxidation of the alpha-C ...
... alpha K_{m}+\alpha ^{\prime }[S]}}={\frac {(1/\alpha ^{\prime })V_{max}[S]}{(\alpha /\alpha ^{\prime })K_{m}+[S]}}} where the ... Inhibitors of dihydrofolate reductase (DHFR) are prominent examples. Other examples of these substrate mimics are the protease ... reverse-transcriptase inhibitors targeting HIV/AIDS, neuraminidase inhibitors targeting influenza, and terminase inhibitors ... For example, an inhibitor might compete with substrate A for the first binding site, but be a non-competitive inhibitor with ...
A 2007 Cochrane review of aldose reductase inhibitors for the treatment of the pain deriving from diabetic polyneuropathy found ... "Review of Diabetic Polyneuropathy: Pathogenesis, Diagnosis A". Bartkoski, Scott; Day, Margaret (2016-05-01). "Alpha-Lipoic Acid ... Chalk C, Benstead TJ, Moore F (October 2007). "Aldose reductase inhibitors for the treatment of diabetic polyneuropathy". The ... imapramine, and desipramine,) serotonin-norepinephrine reuptake inhibitor (SNRI) medications (duloxetine, venlafaxine, and ...
... in the 5alpha-reductase type 2 gene in a boy with 5alpha-reductase deficiency: genotype-phenotype correlations". Am. J. Med. ... The enzyme is active at acidic pH and is sensitive to the 4-azasteroid inhibitor finasteride. Deficiencies in 5αR2 activity of ... Chávez B, Valdez E, Vilchis F (2000). "Uniparental disomy in steroid 5alpha-reductase 2 deficiency". J. Clin. Endocrinol. Metab ... 2002). "A novel homozygous disruptive mutation in the SRD5A2-gene in a partially virilized patient with 5alpha-reductase ...
The alpha carbon of the resulting acetyl-ACP is linked to C3 of the polyketide chain by MupH. This intermediate is dehydrated ... It does not contain an enoyl reductase (ER) domain, which would be required for the complete reduction to the nine-carbon fatty ... A proposed mode of action of pseudomonic acid as an inhibitor of isoleucyl-tRNA synthetase". J. Biol. Chem. 269 (39): 24304-9. ... 195 (1): 244-5. doi:10.1016/0005-2787(69)90621-2. PMID 4982424. El-Sayed AK, Hothersall J, Cooper SM, Stephens E, Simpson TJ, ...
... alpha 2(6p21.3) CYP21A2: cytochrome P450, family 21, subfamily A, polypeptide 2 (6p21.33) DHX16: DEAH-box helicase 16 (6p21.33 ... quinone reductase 2 (6p25.2) NRSN1: neurensin 1 (6p22.3) NUDT3: nudix hydrolase 3 (6p21.31) PFDN6: prefoldin subunit 6 (6p21.32 ... cAMP-dependent protein kinase inhibitor beta (6p22.31) PLAGL1: (6q24.2) RCD1: retinal cone dystrophy 1 RFPL4B: Ret finger ... mannosidase alpha class 1A member 1 (6q22.31) MB21D1: encoding protein Mab-21 domain containing 1 MCDR1: macular dystrophy, ...
Bicalutamide, as well as enzalutamide, have been found to act as inhibitors of P-glycoprotein efflux and ATPase activity. This ... role of 3 alpha- and 3 beta-androstanediols". Biology of Reproduction. 51 (3): 562-71. doi:10.1095/biolreprod51.3.562. PMID ... In fact, estradiol is a much stronger inhibitor of gonadotropin secretion than is testosterone, and even though circulating ... Bicalutamide has been identified as a strong CYP27A1 (cholesterol 27-hydroxylase) inhibitor in vitro. CYP27A1 converts ...
Istvan, Eva S.; Deisenhofer, Johann (2001-05-11). "Structural Mechanism for Statin Inhibition of HMG-CoA Reductase". Science. ... Sabatine, Marc S. (March 2019). "PCSK9 inhibitors: clinical evidence and implementation". Nature Reviews Cardiology. 16 (3): ... of fibrates is due to their ability to activate a nuclear receptor called peroxisome proliferator activated receptor alpha. ... Statins competitively inhibit hydroxymethylglutaryl (HMG) CoA reductase which is used in the biosynthesis of cholesterol and ...
... eplerenone HMG-CoA reductase inhibitors: lovastatin, simvastatin ergot alkaloids: ergotamine, dihydroergotamine, ergometrine, ... 7α-Hydroxylase inhibitors, 11β-Hydroxylase inhibitors, 21-Hydroxylase inhibitors, Acetamides, Aldosterone synthase inhibitors, ... Cholesterol side-chain cleavage enzyme inhibitors, CYP17A1 inhibitors, Dioxolanes, Disulfiram-like drugs, Endocrine disruptors ... Oral ketoconazole has been used clinically as a steroidogenesis inhibitor in men, women, and children at dosages of 200 to ...
GTP activates the alpha subunit of the G protein, causing it to dissociate from the G protein and act as a downstream effector ... Ribonucleotide reductase (RNR) is the enzyme responsible for converting NTPs to dNTPs. Given that dNTPs are used in DNA ... Menéndez-Arias L (June 2008). "Mechanisms of resistance to nucleoside analogue inhibitors of HIV-1 reverse transcriptase". ... Kolberg M, Strand KR, Graff P, Andersson KK (June 2004). "Structure, function, and mechanism of ribonucleotide reductases". ...
Co-administration of alpha-1 inhibitor can cause hypotension. Since alpha-1 blockers may cause orthostatic hypotension, co- ... Alpha-1 blockers have no effect on renin release or cardio output. Alpha-1 blocker, blocks alpha receptors and it relaxes the ... Alpha-1 blockers (also called alpha-adrenergic blocking agents or alpha-1 antagonists) constitute a variety of drugs that block ... Wikimedia Commons has media related to Alpha-1 blockers. DrugDigest - Alpha blockers RxList.com - Tamsulosin alpha-Adrenergic+ ...
The strands are connected by turns and a single alpha-helical insertion. A single-atom copper binding site is located about 7 Å ... P53 also activates the expression of cell-cycle inhibitors, preventing tumor cells from progressing beyond the G1 or S phase. ... When expressed in nitrogen-fixing organisms, azurin serves as the electron donor to nitrite reductase, an enzyme in the ... as well as an alpha-helical segment outside the barrel linking beta-sheets 4 and 5. Although the Cu(I)/Cu(II) redox potential ...
RAG1 Alpha-2-plasmin inhibitor deficiency; 262850; PLI Alpha-ketoglutarate dehydrogenase deficiency; 203740; OGDH Alpha- ... CBG Cortisone reductase deficiency; 604931; H6PD Cortisone reductase deficiency; 604931; HSD11B1 Costello syndrome; 218040; ... NLRP3 Mucolipidosis II alpha/beta; 252500; GNPTAB Mucolipidosis III alpha/beta; 252600; GNPTAB Mucolipidosis III gamma; 252605 ... methylacetoacetic aciduria; 203750; ACAT1 Alpha-thalassemia myelodysplasia syndrome, somatic; 300448; ATRX Alpha-thalassemia ...
HMG CoA Reductase is an important enzyme in lipid and cholesterol metabolism, but it is not the only one. The statins act by ... and CETP inhibitors: meta-analysis of randomised controlled trials including 117,411 patients". BMJ. 349: g4379. doi:10.1136/ ... "Effects of peroxisome proliferator-activated receptor alpha/delta agonists on HDL-cholesterol in vervet monkeys". J Lipid Res. ... 46 (5): 1009-16. doi:10.1194/jlr.M500002-JLR200. PMID 15716581. Hwang JS, Ham SA, Yoo T, Lee WJ, Paek KS, Lee CH, Seo HG (2016 ...
Aldose reductase inhibitor Alpha cell one of the types of cell in the pancreas (in areas called the Islets of Langerhans). ... See ACE inhibitor). Arteriosclerosis Hardening of the blood vessels. It causes inflexibility of the arterial walls, so they are ... ACE inhibitor Angiotensin conversion enzyme. A class of drugs used to decrease hypertension, mainly by interfering with the ... There are currently five known types of cells in an islet: beta cells, which make insulin and C-peptide; alpha cells, which ...
Studies on the metabolism of 17-alpha-hydroxy-19-norprogesterone caproate by humans in vivo and of 17-alpha-hydroxy-19- ... 493-. ISBN 978-0-203-30415-0. Aubrey DA, Khosla T (September 1971). "The effect of 17-alpha-hydroxy-19-norprogesterone caproate ... Rodriguez-Restrepo, R. (1969). 17-alpha-hydroxy 19 norprogesterone capronate as a prolonged-action injectable contraceptive ... 59 (5): 963-9. doi:10.1210/jcem-59-5-963. PMID 6237116. Jacobi GH, Altwein JE, Kurth KH, Basting R, Hohenfellner R (1980). " ...
Another enzyme, Vitamin K epoxide reductase (VKORC), reduces vitamin K back to its active form. Vitamin K epoxide reductase is ... The activation of FX (to form FXa) by TF-FVIIa is almost immediately inhibited by tissue factor pathway inhibitor (TFPI). FXa ... deficient alpha granules), and delta storage pool deficiency (deficient dense granules). Most are rare. They predispose to ... A newer class of drugs, the direct thrombin inhibitors, is under development; some members are already in clinical use (such as ...
P-glycoprotein inhibitors Methylprednisolone is shown to be a substrate of P-glycoprotein; its inhibition is thought to ... Hepatic metabolism is mediated by 11 beta-hydroxysteroid dehydrogenases (11[beta]-HSD) and 20-ketosteroid reductases. ... alpha]-hydroxymethylprednisolone. As stated previously, the primary use of methylprednisolone is to suppress inflammatory and ... Cox1 inhibitors Methylprednisolone may increase rate of elimination with chronic high dose aspirin. Patient's are susceptible ...
CYP17A1 inhibitors, Enzyme inhibitors, Fluoroarenes, Synthetic estrogens, All stub articles, Antineoplastic and ... ISBN 978-0-89925-374-9. Barrie SE, Rowlands MG, Foster AB, Jarman M (December 1989). "Inhibition of 17 alpha-hydroxylase/C17- ... Bifluranol has also been found to act as a 17α-hydroxylase/17,20 lyase inhibitor, though with less potency than ketoconazole, ... Jarman M, Smith HJ, Nicholls PJ, Simons C (October 1998). "Inhibitors of enzymes of androgen biosynthesis: cytochrome P450(17) ...
This dose, however, is less in those with lowered gastric acidity (for instance those using proton pump inhibitors). Children ... allowing it to permanently ribosylate the Gs alpha subunit of the heterotrimeric G protein. This results in constitutive cAMP ... and formation of periplasmic nitrate reductase complexes were induced just before defecation. These induced characteristics ... 66 (5): 432-8. doi:10.1016/j.jinf.2012.11.013. PMC 3677557. PMID 23201968. King AA, Ionides EL, Pascual M, Bouma MJ (August ...
3β-Hydroxysteroid dehydrogenase inhibitors, Androgens and anabolic steroids, Androstanes, Hepatotoxins, Ketones, Synthetic ... 5 (4): 415-8. doi:10.1002/art.1780050411. PMID 13879693. Matusow PD (1962). "If - Then; C.A.M.S.I.; In the future" (PDF). ... Like other AAS, oxymetholone is an agonist of the androgen receptor (AR). It is not a substrate for 5α-reductase (as it is ... Oxymetholone has very low affinity for human serum sex hormone-binding globulin (SHBG), less than 5% of that of testosterone ...
HMG-CoA reductase inhibitor This type of categorisation of drugs is from a biological perspective and categorises them by the ... cyclooxygenase inhibitor Proton-pump inhibitor Renin inhibitor Selective glucocorticoid receptor modulator Serotonergic Statin ... Enzyme target mechanisms include activator or inhibitor. Ion channel modulators include opener or blocker. The following are ... 5 (10): 821-34. doi:10.1038/nrd2132. PMID 17016423. S2CID 8872470. Buer JK (Oct 2014). "Origins and impact of the term 'NSAID ...
... alpha 1-antichymotrypsin MeSH D12.776.377.715.085.085 - alpha 1-antitrypsin MeSH D12.776.377.715.085.100 - alpha-macroglobulins ... cyclin-dependent kinase inhibitor p27 MeSH D12.776.624.776.355.700 - cyclin-dependent kinase inhibitor p57 See List of MeSH ... nitrate reductase (nad(p)h) MeSH D12.776.556.579.374.375.988 - nitrate reductase (nadph) MeSH D12.776.556.579.374.450 - ... alpha-crystallin a chain MeSH D12.776.306.366.100.300 - alpha-crystallin b chain MeSH D12.776.306.366.300.100 - beta-crystallin ...
Aggarwal S, Thareja S, Verma A, Bhardwaj TR, Kumar M (February 2010). "An overview on 5alpha-reductase inhibitors". Steroids. ... Frye SV (2006). "Discovery and clinical development of dutasteride, a potent dual 5alpha-reductase inhibitor". Curr Top Med ... 402-. ISBN 978-0-323-08619-6. Robaire B, Henderson NA (May 2006). "Actions of 5alpha-reductase inhibitors on the epididymis". ... "A new look at the 5alpha-reductase inhibitor finasteride". CNS Drug Reviews. 12 (1): 53-76. doi:10.1111/j.1527-3458.2006.00053. ...
SEARCH RESULTS for: 5-alpha Reductase Inhibitors [Drug Class] (123 results) *Share : JavaScript needed for Sharing tools. ...
The 5-alpha reductase inhibitors are a family of agents used to treat benign prostatic hypertrophy. They act by inhibiting the ... steroid 5-alpha reductase which catalyzes the conversion of testosterone to dihydrotestosterone. Dihydrotestosterone is an ... Alpha Reductase Inhibitors No authors listed In: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [ ... and androgen receptor signaling response to steroid 5α-reductase inhibitors. Wu Y, Godoy A, Azzouni F, Wilton JH, Ip C, Mohler ...
The 5-alpha reductase inhibitors are a family of agents used to treat benign prostatic hypertrophy. They act by inhibiting the ... steroid 5-alpha reductase which catalyzes the conversion of testosterone to dihydrotestosterone. Dihydrotestosterone is an ... Alpha Reductase Inhibitors No authors listed In: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [ ... The rationale for inhibiting 5alpha-reductase isoenzymes in the prevention and treatment of prostate cancer. Tindall DJ, ...
5 p.m.. ET, Monday - Friday Email: [email protected] Phone: +1-800-860-8747 TTY: +711 Chat. Live Chat Available. 8:30 a. ... Dictionary Definition: 5-alpha reductase inhibitors. 5-alpha reductase inhibitors. A class of medicines that shrinks the ...
Lists the various brand names available for medicines containing finasteride. Find information on finasteride use, treatment, drug class and molecular formula.
Five-alpha-reductase Inhibitors for prostate cancer prevention. Cochrane Database Syst Rev. 2008 Apr 16. CD007091. [QxMD ... 254] It should be noted that the aromatase inhibitors were not studied specifically in individuals known to have genetic risk ... Some data suggest that eradication of H pylori infection through regimens of antibiotics and proton pump inhibitors may be ... specific antigen for the detection of prostate cancer is preserved in men receiving the dual 5alpha-reductase inhibitor ...
Type 2 alpha 5 reductase operates below neutral in our scalps. So by raising our bodily pH we can directly reduce the amount of ... Amazingly this is a method thats far more effective at inhibiting alpha 5 reductase from creating DHT in the scalp, than any ... Type 2 alpha 5 reductase is an enzyme that converts testosterone to dihydroxytestosterone. ... 5 alpha reductase is an enzyme in the body that converts testosterone into DHT which then goes on to cause hair loss in men ...
1. 5alpha-reductase inhibitors.. Rittmaster RS. J Androl; 1997; 18(6):582-7. PubMed ID: 9432130. [No Abstract] [Full Text] [ ... 9. 5alpha-reductase inhibitors in benign prostatic hyperplasia and prostate cancer risk reduction.. Rittmaster RS. Best Pract ... 5alpha-Reductase inhibitor treatment of prostatic diseases: background and practical implications.. Dörsam J; Altwein J. ... 6. An overview on 5alpha-reductase inhibitors.. Aggarwal S; Thareja S; Verma A; Bhardwaj TR; Kumar M. Steroids; 2010 Feb; 75(2 ...
Participants will have 5 radiation treatments. They will lie on a table while a machine delivers the treatment. The machine ... Use of 5 alpha reductase inhibitors (e.g. Finasteride or Dutasteride) within 3 months of screening. - Prostate volume more than ... Estimated life expectancy ,5 years. - Patients must have adequate organ and marrow function as defined below: --Leukocytes ,= ... NCCN high risk prostate cancer due to Gleason Grade 4 or 5 AND refuses to receive systemic ADT, OR -- NCCN high risk prostate ...
5-alpha Reductase Inhibitor. Yes 2002. In Use. NA. Finasteride Proscar. 5mg. Ancillary Therapy Protective Agent. 5-alpha ... Reductase Inhibitor. Yes 1992. In Use. J8655. Netupitant/palonostron Akynzeo. 300mg/0.5 mg. Ancillary Therapy Antiemetic. 5HT3 ...
Dutasteride is in a class of medications called 5-alpha reductase inhibitors. It works by blocking the production of a natural ...
A phase II randomized trial of metastasis-directed therapy with alpha emitter radium-223 in men with oligometastatic castration ... 5-alpha reductase inhibitors and MRI prostates: actively reducing prostate sizes and ambiguity ... a study in 316 inguinal basins with a mean follow-up of 5 years ...
Evidence for atrophy and apoptosis in the ventral prostate of rats given the 5alpha-reductase inhibitor finasteride. ... Inhibitors of 5α-reductases, enzymes involved in intraprostatic conversion of testosterone to its biologically active form ... Atrophy and apoptosis in ventral prostate of rats induced by 5 alpha-reductase inhibitor epristeride. Acta Pharmacol Sin 22:399 ... Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5α-reductase inhibitor ...
... one is an blocker of alpha-1 adrenoceptors and the other is an inhibitor of 5-alpha-reductase. These drugs treat different, ... 5. To implement procedures for and evaluate compliance to drug therapy. 6. To allow the study participants to better estimate ... This information should be included in the form PHS 398 in Sections 1-4 of the Research Plan AND summarized in Section 5, Human ... 5. External Advisory Committee An External Advisory Committee composed of experts in relevant medical, statistical, and ...
Bhasin and colleagues hypothesized that the effects of these inhibitors on the prostate depend on baseline testosterone levels. ... Bhasin and his colleagues found that administration of testosterone and an ornithine decarboxylase inhibitor in a testosterone- ... Within this partnership, PCORI has committed up to $30 million toward a 5-year study for prevention of fall injuries in older ... In a randomized trial in which men received testosterone with placebo or a 5-alpha reductase inhibitor, Dr. Bhasin and his ...
NOTE: If the alpha reductase inhibitor is stopped prior to randomization the patient is eligible ... PSA > 20 ng/mL prior to starting ADT Note: Patients receiving a 5-alpha reductase inhibitor (ex. finasteride) at the time of ... The baseline PSA value should be doubled for PSAs taken while on 5-alpha reductase inhibitors and the medication should be ...
Enzyme Inhibitors [D27.505.519.389] * Steroid Synthesis Inhibitors [D27.505.519.389.870] * 14-alpha Demethylase Inhibitors [ ... Steroid Synthesis Inhibitors [D27.505.696.399.450.855] * 14-alpha Demethylase Inhibitors [D27.505.696.399.450.855.100] ... inhibitors (1976-2010). Public MeSH Note. 2011. History Note. 2011. Date Established. 2011/01/01. Date of Entry. 2010/06/25. ... 3-Oxo-5-alpha-Steroid 4-Dehydrogenase Inhibitors Term UI T768874. Date04/07/2010. LexicalTag NON. ThesaurusID NLM (2011). ...
Some studies suggest that taking 5-alpha reductase inhibitors, including finasteride (Propecia, Proscar) and dutasteride ( ...
The highest risk was observed in patients exposed to alpha blocker therapy alone. ... Nonselective alpha blocker treatment had an 8% higher risk of cardiac failure than selective alpha blocker therapy, according ... "Secondly, the alpha blockers (maybe specifically nonselective alpha blockers) have a higher association with new cardiac ... Alpha blocker] association with cardiac failure, on the other hand, may be linked to their vasodilatory effects and blood ...
Poly(ADP-ribose) Polymerase Inhibitors. Enzyme Inhibitors. Molecular Mechanisms of Pharmacological Action. Antineoplastic ... Any previous treatment with a PARP inhibitor, including rucaparib.. *Resting ECG with QTc , 480 msec on 2 or more time points ... Prior oral anti-androgen (e.g. bicalutamide, nilutamide, enzalutamide, apalutamide), or androgen synthesis inhibitor (e.g. ... 5-alpha reductase inhibitor therapy (e.g. finasteride, dutasteride) is allowed, as long as subject has been stable on ...
Vitamin K Epoxide Reductase Inhibitors,N0000000164, Pituitary Hormone Receptor Agonists,N0000000165, alpha Glucosidase ... 14-alpha demethylase Inhibitors,N0000020025, Phosphodiesterase 5 Inhibitors,N0000020026, Glucan Synthase Inhibitors,N0000020027 ... VEGFR1 Inhibitors,N0000020031, VEGFR2 Inhibitors,N0000020032, VEGFR3 Inhibitors,N0000020033, Stem Cell Factor (KIT) Inhibitors, ... Epidermal Growth Factor Inhibitor,N0000020006, HER-2/Neu/cerbB2 Inhibitor,N0000020008, HER-1 Inhibitor,N0000020010, HER-3 ...
... those taking alpha blockers or 5ARIs may have higher risks of heart failure, according to a study. ... The risk for new heart failure among men taking medications for benign prostatic hyperplasia was highest in users of alpha ... Heart failure risk is increased among men taking an alpha blocker (AB) or 5-alpha reductase inhibitor (5ARI) for benign ...
SEARCH RESULTS for: 5-alpha Reductase Inhibitors [Drug Class] (123 results) *Share : JavaScript needed for Sharing tools. ...
Basil M Hantash, MD, PhD, MBA is a member of the following medical societies: Alpha Omega Alpha, American Academy of ... Eflornithine cream is a prescription topical cream that acts as a growth inhibitor, not a depilatory. It inhibits ornithine ... Finasteride, a 5-alpha reductase inhibitor approved for use in benign prostatic hypertrophy and in male-pattern alopecia, ...
... such as alpha blockers and 5 alpha reductase inhibitors) and minimally invasive surgical techniques (such as stents, lasers, ...
... inhibitor#Herbs_and_other_inhibitors ... 5 The Effectiveness of Medical Treatments for Prostate Cancer. ... The use of 5-alpha-reductase inhibitors are controversial as a treatment for prostate cancer. Ultrasound Right now, some ... A past study from 2005 indicated that a stronger single dose of radiation (8 Gy) is as effective as 20 Gy for 5 treatments or ... Even advanced forms of the cancer have a long-term survival rate that lasts 5 years or more. However, if prostate cancer ...
... and/or alpha-adrenergic blockers such as tamsulosin (Flomax). Unfortunately, these medications often produce insufficient ... Men with mild BPH symptoms are often treated with medications including 5-alpha-reductase inhibitors such as finasteride ( ...
  • The 5-alpha reductase inhibitors in clinical use in the United States include two agents of similar chemical structure (azasteroids) and activity: finasteride (Proscar: 1992) and dutasteride (Avodart: 2001). (nih.gov)
  • 5-alpha reductase inhibitors include finasteride which primarily blocks the type II form of the enzyme and dutasteride which blocks both type I and II forms). (nih.gov)
  • Amazingly this is a method that's far more effective at inhibiting alpha 5 reductase from creating DHT in the scalp, than any synthetic drug like finasteride . (syromonoed.com)
  • Finasteride is a 5-alpha-reductase inhibitor, which is applied in the treatment of BHP and male baldness. (nih.gov)
  • In the doses used finasteride acts mainly by inhibiting the 5-alpha-reductase type 2, thereby reducing the serum level of DHT by approximately 70% and by about 85-90% in the prostate. (nih.gov)
  • 14. Comparative study of human steroid 5alpha-reductase isoforms in prostate and female breast skin tissues: sensitivity to inhibition by finasteride and epristeride. (nih.gov)
  • 16. Finasteride, an inhibitor of 5 alpha-reductase, suppresses prostatic dihydrotestosterone in men with benign prostatic hyperplasia. (nih.gov)
  • 20. Pharmacokinetic parameters and mechanisms of inhibition of rat type 1 and 2 steroid 5alpha-reductases: determinants for different in vivo activities of GI198745 and finasteride in the rat. (nih.gov)
  • Inhibitors of 5α-reductases, enzymes involved in intraprostatic conversion of testosterone to its biologically active form dihydrotestosterone, such as finasteride and epristeride, are known to induce atrophy of prostate. (nih.gov)
  • 2004. Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5α-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: New approach for benign prostate hyperplasia. (nih.gov)
  • Evidence for atrophy and apoptosis in the ventral prostate of rats given the 5alpha-reductase inhibitor finasteride. (nih.gov)
  • Men with mild BPH symptoms are often treated with medications including 5-alpha-reductase inhibitors such as finasteride (Proscar) and/or alpha-adrenergic blockers such as tamsulosin (Flomax). (uclahealth.org)
  • Other medications like 5- alpha reductase inhibitor (eg: Finasteride or Dutasteride) can also be used in combination with alpha- blocker or alone. (ndtv.com)
  • Like finasteride (the active ingredient in Propecia), dutasteride is an inhibitor of the enzyme 5 alpha-reductase which converts testosterone to DHT (dihydrotestosterone), the hormone responsible for genetic hair loss. (bernsteinmedical.com)
  • As important, the half-life of dutasteride is significantly longer than finasteride (5-6 weeks vs. 6-8 hours). (bernsteinmedical.com)
  • You may be familiar with finasteride (Proscar) and dutasteride (Avodart) as drugs used to treat benign prostatic hyperplasia (BPH), but studies have also looked at whether these two 5-alpha-reductase inhibitors could help prevent prostate cancer. (prostate.net)
  • Dihydrotestosterone and the concept of 5alpha-reductase inhibition in human benign prostatic hyperplasia. (nih.gov)
  • Adherence to 5-alpha reductase inhibitor therapy for benign prostatic hyperplasia: clinical and economic outcomes. (bvsalud.org)
  • Our goal was to quantify relationships between adherence to 5-alpha reductase inhibitors (5-ARIs), the risk of acute urinary retention (AUR) and prostate surgery , and medical costs related to patients with benign prostatic hyperplasia (BPH). (bvsalud.org)
  • 3. [Dihydrotestosterone and the role of 5 alpha-reductase inhibitors in benign prostatic hyperplasia]. (nih.gov)
  • 4. Marked suppression of dihydrotestosterone in men with benign prostatic hyperplasia by dutasteride, a dual 5alpha-reductase inhibitor. (nih.gov)
  • 5. Dihydrotestosterone and the prostate: the scientific rationale for 5alpha-reductase inhibitors in the treatment of benign prostatic hyperplasia. (nih.gov)
  • 7. Dutasteride: a potent dual inhibitor of 5-alpha-reductase for benign prostatic hyperplasia. (nih.gov)
  • 11. Dutasteride: a novel dual inhibitor of 5alpha-reductase for benign prostatic hyperplasia. (nih.gov)
  • 15. 5alpha-reductase inhibitors in benign prostatic hyperplasia and prostate cancer risk reduction. (nih.gov)
  • 18. A review on steroidal 5α-reductase inhibitors for treatment of benign prostatic hyperplasia. (nih.gov)
  • They act by inhibiting the steroid 5-alpha reductase which catalyzes the conversion of testosterone to dihydrotestosterone. (nih.gov)
  • 5 alpha reductase is an enzyme in the body that converts testosterone into DHT which then goes on to cause hair loss in men affected with androgenic alopecia. (syromonoed.com)
  • Type 2 alpha 5 reductase is an enzyme that converts testosterone to dihydroxytestosterone. (syromonoed.com)
  • DHT is formed by the reduction of testosterone by the enzyme 5-alpha-reductase, which has two isoenzymes. (nih.gov)
  • Potential mechanisms for the associations between cardiac failure and [5-alpha reductase inhibitors] include the deleterious impact on metabolic disorders and cardiac function through their antiandrogen effect and blockage of serum testosterone conversion to dihydrotestosterone," wrote the authors of the current study. (urologytimes.com)
  • In some clinical studies, patients taking dutasteride with another drug called alpha-blocker (such as tamsulosin) were more likely to have heart failure than patients taking only dutasteride or an alpha-blocker. (thefamilyrx.com)
  • If you have significant voiding symptoms which are bothersome then you may need medications like alpha-blockers (eg: Tamsulosin). (ndtv.com)
  • 8. The rationale for inhibiting 5alpha-reductase isoenzymes in the prevention and treatment of prostate cancer. (nih.gov)
  • 19. New steroidal 17β-carboxy derivatives present anti-5α-reductase activity and anti-proliferative effects in a human androgen-responsive prostate cancer cell line. (nih.gov)
  • Abiraterone (Zytiga), a hormone therapy drug approved for treatment of metastatic prostate cancer, may also help eliminate localized high-risk prostate cancer, according to researchers who will present their findings at the American Society of Clinical Oncology meeting in Chicago June 1-5, 2012. (prostate.net)
  • Dutasteride is in a class of medications called 5-alpha reductase inhibitors. (medlineplus.gov)
  • Dutasteride (Avodart) is a prescribed medicine classified under the group of drugs known as 5-alpha reductase inhibitors. (thefamilyrx.com)
  • Dutasteride, a new 5-α-reductase inhibitor, has shown a specific action in medical research by decreasing the volume of the transition zone in contact with the prostatic urethra. (thefamilyrx.com)
  • It is important to note that compared to the Type II form of the 5 alpha-reductase enzyme, the Type I variety is present in many different organs of the body, including the brain, which accounts for the increased potential side effects. (bernsteinmedical.com)
  • The mechanisms usually evoked to explain the effect of "5-ARI" on hematuria related to BPH and on TURP hemorrhage are related to the reduction of microvasculature density of prostatic epithelium and regulating the activity of growth factors of androgen-controlled angiogenesis. (thefamilyrx.com)
  • Published online 2023 Mar 5. (nih.gov)
  • In patients with BPH who received 5-ARI therapy , greater adherence and persistence were associated with significantly reduced risks of AUR and prostate surgery and with significantly lower medical costs . (bvsalud.org)
  • 20 ng/mL prior to starting ADT Note: Patients receiving a 5-alpha reductase inhibitor (ex. (urotoday.com)
  • The highest risk was observed in patients exposed to alpha blocker therapy alone. (urologytimes.com)
  • The highest risk for cardiac failure was among BPH patients taking alpha blockers alone or in combination, according to the study published in The Journal of Urology . (urologytimes.com)
  • The data set Siemens and colleagues studied included 8339 BPH patients exposed to 5-alpha reductase inhibitors, 55,383 exposed to alpha blockers, and 41,491 who had taken a combination. (urologytimes.com)
  • Consider 5-alpha-reductase inhibitors, which shrink the prostate, for patients who have predominantly irritative symptoms (urgency and frequency). (consultant360.com)
  • The era of medical therapy for BPH dawned in the mid 1970s with the use of nonselective alpha-blockers such as phenoxybenzamine. (medscape.com)
  • The medical therapeutic options for BPH have evolved significantly since then, with the development of receptor-specific alpha-blockers that comprise current first-line therapy, as well as the approval of 5-alpha-reductase inhibitors. (medscape.com)
  • An approximately 4- to 6-point improvement is expected in IPSS/AUA-SI scores when alpha-blockers are used. (medscape.com)
  • Selective long-acting alpha-1 blockers - Terazosin, doxazosin, slow-release (SR) alfuzosin. (medscape.com)
  • Investigators studied data on more than 175,200 men with BPH treated with 5-alpha reductase inhibitors, alpha blockers, or a combination. (urologytimes.com)
  • Secondly, the alpha blockers (maybe specifically nonselective alpha blockers) have a higher association with new cardiac failure. (urologytimes.com)
  • The issue of cardiac failure and alpha blockers arose almost 20 years ago in the ALLHAT trial (NCT00000542), among the first studies to highlight a possible link between alpha blockers and hypertension. (urologytimes.com)
  • Although it hasn't changed my practice that much-I still of course use alpha blockers-it has made me more diligent in assessing cardiovascular health," Siemens said. (urologytimes.com)
  • The evidence also makes Siemens discuss the choice of his primary care colleagues' use of nonselective alpha blockers when they are being prescribed for lower urinary tract symptoms. (urologytimes.com)
  • Over the last decade significant advances have been made in characterizing this abnormality and treating it with medical therapy (such as alpha blockers and 5 alpha reductase inhibitors) and minimally invasive surgical techniques (such as stents, lasers, hyperthermia and others). (nih.gov)
  • Medical treatment of benign prostatic hypertrophy can use three types of medications: plant extracts, alphablockers which have an essentially symptomatic effect, and inhibitors of 5-α-reductase ("5-ARI") which, through their hormonal action, reduces the volume of the prostate gland, and therefore, can improve clinical symptomatology and reduce the risk of long-term complications. (thefamilyrx.com)
  • Isotretinoin is both a serotonin reuptake inhibitor and a 5-alpha reductase inhibitor (5ARI), so it could give rise to PSSD or PFS, or all three conditions may have something else in common. (rxisk.org)
  • While serotonin and 5-alpha reductase may be where these problems start, they seem to go beyond this. (rxisk.org)
  • Interestingly, alpha-blocker therapy has not been shown to reduce the overall long-term risk for acute urinary retention (AUR) or need for BPH-related surgery. (medscape.com)
  • and 9% higher among men exposed to 5-alpha reductase inhibitor therapy alone. (urologytimes.com)
  • Nonselective alpha blocker treatment had an 8% higher risk of cardiac failure than selective alpha blocker therapy, according to the paper. (urologytimes.com)
  • Here's the top 4 natural compounds that inhibit 5 alpha reductase. (syromonoed.com)
  • Green tea contains two important compounds for inhibiting 5 alpha reductase scientists found. (syromonoed.com)
  • 17. Potency of a novel saw palmetto ethanol extract, SPET-085, for inhibition of 5alpha-reductase II. (nih.gov)
  • The first line of treatment for mild to moderate symptoms usually consists of alpha-blocking agents because of the rapid onset of their therapeutic effect. (consultant360.com)
  • This portion of the meeting was closed to the public, in accordance with the determination that it concerned matters exempt from mandatory disclosure under Sections 552(b)(c)(4) and 552(b)(c)(6), Title 5, U.S. Code and Section 10(d) of the Federal Advisory Committee Act, as amended (5 U.S.C. Appendix). (nih.gov)
  • Because of the availability of more alpha-1-receptor-specific agents, phenoxybenzamine is no longer often used for the treatment of BPH. (medscape.com)
  • However, the circulating and intraprostatic DHT could be further reduced by a more effective dual 5-alpha-reductase inhibitor, which would be efficacious in the treatment of benign prostate hyperplasia and other DHT-related disorders. (nih.gov)
  • It's not as well known yet but initial trials are promising as a 5 alpha reductase inhibitor. (syromonoed.com)
  • The baseline PSA value should be doubled for PSAs taken while on 5-alpha reductase inhibitors and the medication should be discontinued prior to randomization but a washout period is not required. (urotoday.com)
  • Alklaizing the bloodstream by consuming foods that have a net alkaline effect on the body can significantly reduce the amount of type 2 alpha 5 reductase in the scalp. (syromonoed.com)
  • Participants will have 5 radiation treatments. (nih.gov)
  • A past study from 2005 indicated that a stronger single dose of radiation (8 Gy) is as effective as 20 Gy for 5 treatments or 30Gy over 10 treatments. (progressivehealth.com)
  • Type 2 alpha 5 reductase operates below neutral in our scalps. (syromonoed.com)
  • The 5-alpha-reductase type 2 is the predominant isoenzyme in genital tissue and thus also in the prostate. (nih.gov)
  • It is nonselective, antagonizing both the alpha 1- and alpha 2-adrenergic receptors, which results in a higher incidence of adverse effects. (medscape.com)
  • Oral ingestion is the least effective way you can benefit from saw palmettos inhibiting effect on 5-alpha-reductase because it's diluted throughout the entire body. (syromonoed.com)
  • Alkalizing the bloodstream is in my experience the most effective and long term solution for inhibiting 5 alpha reductase and can have a dramatic effect on preventing further hair loss. (syromonoed.com)
  • therefore, alpha-adrenergic receptor-blocking agents should theoretically decrease resistance along the bladder neck, prostate, and urethra by relaxing the smooth muscle, thus allowing easier passage of urine. (medscape.com)
  • The 5-alpha reductase inhibitors are a family of agents used to treat benign prostatic hypertrophy. (nih.gov)
  • In accordance with the provisions of Public Law 92-463, the meeting was closed to the public on Tuesday, September 17, from 3 to 5 p.m. for the review, discussion, and evaluation of grant applications in accordance with the provisions set forth in Sections 552(b)(c)(4) and 552(b)(c)(6), Title 5, U.S. Code and Section 10(d) of the Public Law 92-463. (nih.gov)
  • Even advanced forms of the cancer have a long-term survival rate that lasts 5 years or more. (progressivehealth.com)
  • Saw palmetto is probably the most well-known and also controversial 5 alpha reductase inhibitor, due to the variation in results and side effects associated with high oral dosages. (syromonoed.com)
  • Alpha blocker] association with cardiac failure, on the other hand, may be linked to their vasodilatory effects and blood pressure variability. (urologytimes.com)
  • Neither of the 5-alpha reductase inhibitors in current use has been linked to clinically apparent acute liver injury. (nih.gov)
  • The 5-alpha reductase inhibitors used for benign prostatic hypertrophy are discussed individually, with references on their hepatotoxicity given together at the end of this introductory section. (nih.gov)