Avodart® (dutasteride) Reductase Inhibitors DHT blockers

akn · Jul 4, 2014

<!--[if gte mso 9]><xml> <w:WordDocument> <w:View>Normal</w:View> <w:Zoom>0</w:Zoom> <w:TrackMoves/> <w:TrackFormatting/> <w

unctuationKerning/> <w:ValidateAgainstSchemas/> <w:SaveIfXMLInvalid>false</w:SaveIfXMLInvalid> <w:IgnoreMixedContent>false</w:IgnoreMixedContent> <w:AlwaysShowPlaceholderText>false</w:AlwaysShowPlaceholderText> <w

oNotPromoteQF/> <w:LidThemeOther>EN-US</w:LidThemeOther> <w:LidThemeAsian>X-NONE</w:LidThemeAsian> <w:LidThemeComplexScript>X-NONE</w:LidThemeComplexScript> <w:Compatibility> <w:BreakWrappedTables/> <w:SnapToGridInCell/> <w:WrapTextWithPunct/> <w:UseAsianBreakRules/> <w

ontGrowAutofit/> <w:SplitPgBreakAndParaMark/> <w

ontVertAlignCellWithSp/> <w

ontBreakConstrainedForcedTables/> <w

ontVertAlignInTxbx/> <w:Word11KerningPairs/> <w:CachedColBalance/> <w:UseFELayout/> </w:Compatibility> <w

oNotOptimizeForBrowser/> <m:mathPr> <m:mathFont m:val="Cambria Math"/> <m:brkBin m:val="before"/> <m:brkBinSub m:val="--"/> <m:smallFrac m:val="off"/> <m:dispDef/> <m:lMargin m:val="0"/> <m:rMargin m:val="0"/> <m:defJc m:val="centerGroup"/> <m:wrapIndent m:val="1440"/> <m:intLim m:val="subSup"/> <m:naryLim m:val="undOvr"/> </m:mathPr></w:WordDocument> </xml><![endif]--> [FONT=&quot]Description:[/FONT]
[FONT=&quot]Dutasteride is an inhibitor of the 5-alpha reductase enzyme.[/FONT]
[FONT=&quot]Reductase inhibitors are designed to prevent the conversion[/FONT]
[FONT=&quot]of testosterone to its more androgenic counterpart DHT[/FONT]
[FONT=&quot](dihydrotestosterone). DHT is implicated in a number of[/FONT]
[FONT=&quot]disorders in men including male pattern hair loss and benign[/FONT]
[FONT=&quot]prostate enlargement. Dutasteride is specifically approved[/FONT]
[FONT=&quot]for the treatment of symptomatic benign prostate hyperplasia[/FONT]
[FONT=&quot](BPH). While dutasteride is similar in structure and action to[/FONT]
[FONT=&quot]finasteride, it differs from the first generation reductase[/FONT]
[FONT=&quot]inhibitor in its tissue selectivity. Finasteride inhibits the[/FONT]
[FONT=&quot]type-2 isozyme of the 5- alpha reductase enzyme, found[/FONT]
[FONT=&quot]prominently in the scalp and prostate. Dutasteride is nonspecific[/FONT]
[FONT=&quot]for isotype, and inhibits both type-1 and type-2[/FONT]
[FONT=&quot]reductase. As such, it inhibits DHT conversion in all tissues[/FONT]
[FONT=&quot]including the scalp, liver, prostate, and skin. Because of this[/FONT]
[FONT=&quot]it also lowers systemic levels of DHT much more effectively[/FONT]
[FONT=&quot]than finasteride.[/FONT]
[FONT=&quot]The DHT inhibiting effects of dutasteride make this drug of[/FONT]
[FONT=&quot]some interest to bodybuilders and athletes, particularly those[/FONT]
[FONT=&quot]concerned with the androgenic component of testosteronebased[/FONT]
[FONT=&quot]steroids. Dutasteride is capable of reducing the[/FONT]
[FONT=&quot]androgenic side effects produced by DHT conversion,[/FONT]
[FONT=&quot]changing the profile of testosterone drugs measurably.[/FONT]
[FONT=&quot]Provided moderate doses of testosterone are being used, the[/FONT]
[FONT=&quot]result can be a substantial reduction in the occurrence of oily[/FONT]
[FONT=&quot]skin and acne. For those prone to male pattern hair loss,[/FONT]
[FONT=&quot]dutasteride may also reduce the harsh impact of testosterone[/FONT]
[FONT=&quot]on the hairline. Note that as a selective type-2 inhibitor,[/FONT]
[FONT=&quot]finasteride is also effective at lowering DHT levels in the[/FONT]
[FONT=&quot]scalp (and reducing hairline impact of testosterone use), but[/FONT]
[FONT=&quot]does not work as well for reducing oily skin and acne.[/FONT]
[FONT=&quot]In terms of overall potency, a study published in the Journal[/FONT]
[FONT=&quot]of Clinical Endocrinology and Metabolism [/FONT][FONT=&quot](May 2004)[/FONT]
[FONT=&quot]directly compared dutasteride to its closest pharmaceutical[/FONT]
[FONT=&quot]counterpart, finasteride.765 In this investigation 399 males[/FONT]
[FONT=&quot]suffering from benign prostatic hypertrophy were assembled[/FONT]
[FONT=&quot]and separated into three general groups, each receiving[/FONT]
[FONT=&quot]dutasteride (subdivided by doses of .01, .05, .5, 2.5, or 5.0[/FONT]
[FONT=&quot]mg daily), finasteride (.5 mg daily) or placebo, for a period[/FONT]
[FONT=&quot]of 24 weeks. Over the 24- week period, the dutasteride[/FONT]
[FONT=&quot]group noted the strongest level of DHT inhibition. The[/FONT]
[FONT=&quot]beneficial effects of this drug also occurred over a wide[/FONT]
[FONT=&quot]range of dosages. For example, a 5 mg daily amount caused[/FONT]
[FONT=&quot]98.4% inhibition in DHT levels, while 1/10th of this amount[/FONT]
[FONT=&quot](.5 mg daily, the adopted therapeutic dose) lowered levels[/FONT]
[FONT=&quot]by an average of 94.7%.[/FONT]
[FONT=&quot]This was in great contrast to the 5 mg finasteride group,[/FONT]
[FONT=&quot]which noticed only 70.8% inhibition. Researchers also noted[/FONT]
[FONT=&quot]that there was significantly more of a variation in the results[/FONT]
[FONT=&quot]of the finasteride group, with some patients noting DHT[/FONT]
[FONT=&quot]suppression in the range of only 50-55%.[/FONT]
[FONT=&quot]Just as there can be benefits to lowering 5-alpha reductase[/FONT]
[FONT=&quot]activity by way of less androgenic side effects, there can also[/FONT]
[FONT=&quot]be some drawbacks. For one, a strong androgen like DHT[/FONT]
[FONT=&quot]helps with neuromuscular interaction, fostering strength and[/FONT]
[FONT=&quot]muscle gain. Users of reductase inhibitors often report a drop[/FONT]
[FONT=&quot]in their maximum lifts soon after the drug is initiated. Libido[/FONT]
[FONT=&quot]may also decline as DHT concentrations are lowered. A[/FONT]
[FONT=&quot]small percentage of men even find the need to keep Viagra on[/FONT]
[FONT=&quot]hand, as dutasteride renders them otherwise impotent.[/FONT]
[FONT=&quot]Dihydrotestosterone also serves as a potent endogenous antiestrogen,[/FONT]
[FONT=&quot]as this non-aromatizable steroid competes with[/FONT]
[FONT=&quot]other substrates (like testosterone, which aromatizes) to bind[/FONT]
[FONT=&quot]with the aromatase enzyme. Gynecomastia or other[/FONT]
[FONT=&quot]estrogenic side effects may occur when this competition is[/FONT]
[FONT=&quot]absent. Gynecomastia is listed in the warnings for this[/FONT]
[FONT=&quot]product, although the frequency of this in testing was very[/FONT]
[FONT=&quot]low (1.1% of users).[/FONT]
[FONT=&quot]History:[/FONT]
[FONT=&quot]Dutasteride was first described in 1997.766 It was developed[/FONT]
[FONT=&quot]by the U.S. based pharmaceutical company GlaxoSmithKline.[/FONT]
[FONT=&quot]It was approved by the FDA in November 2001, and[/FONT]
[FONT=&quot]introduced to market the following year by Glaxo under the[/FONT]
[FONT=&quot]Avodart trade name. GlaxoSmithKline also markets the drug[/FONT]
[FONT=&quot]in a number of other countries in Europe and South America[/FONT]
[FONT=&quot]under the same trade name.[/FONT]
[FONT=&quot]How Supplied:[/FONT]
[FONT=&quot]Dutasteride is supplied in soft gelatin capsules containing .5[/FONT]
[FONT=&quot]mg each.[/FONT]
[FONT=&quot]Structural Characteristics:[/FONT]
[FONT=&quot]Dutasteride is a synthetic 4-azasteroid. It has the chemical[/FONT]
[FONT=&quot]designation (5·,17‚)-N-{2,5 bis(trifluoromethyl)phenyl}-3-[/FONT]
[FONT=&quot]oxo-4-azaandrost-1-ene-17-carboxamide.[/FONT]
[FONT=&quot]Warnings (Pregnancy):[/FONT]
[FONT=&quot]This drug must never be taken during pregnancy. Be aware[/FONT]
[FONT=&quot]that dutasteride can be absorbed through the skin. Women[/FONT]
[FONT=&quot]who are, or might become pregnant, should never handle[/FONT]
[FONT=&quot]dutasteride capsules. The DHT blocking action of dutasteride[/FONT]
[FONT=&quot]can cause severe developmental problems to an unborn male[/FONT]
[FONT=&quot]fetus, even in very small amounts. Unaltered dutasteride can[/FONT]
[FONT=&quot]also be recovered in the semen. It is unknown if the drug can[/FONT]
[FONT=&quot]be absorbed during sexual intercourse enough to harm a[/FONT]
[FONT=&quot]developing male fetus. The use of condoms or abstinence is[/FONT]
[FONT=&quot]recommended during therapy.[/FONT]
[FONT=&quot]Side Effects:[/FONT]
[FONT=&quot]The most common adverse reactions to dutasteride therapy[/FONT]
[FONT=&quot]are impotence, reduced libido, and difficulty ejaculating.[/FONT]
[FONT=&quot]Gynecomastia was also noted during clinical trials, but[/FONT]
[FONT=&quot]occurred in less than 1% of patients. Some patients have also[/FONT]
[FONT=&quot]developed allergic reactions to the drug, including rash,[/FONT]
[FONT=&quot]itching, edema, and hives.[/FONT]
[FONT=&quot]Administration (General Considerations):[/FONT]
[FONT=&quot]Reductase inhibitors cannot completely protect against[/FONT]
[FONT=&quot]androgenic side effects such as steroid-induced hair loss,[/FONT]
[FONT=&quot]oily skin, and acne. Reductase inhibitors lessen these side[/FONT]
[FONT=&quot]effects by reducing, not eliminating, the level of androgenic[/FONT]
[FONT=&quot]activity in the skin and scalp. Androgenic and anabolic[/FONT]
[FONT=&quot]effects are both mediated by the same receptor, and there is[/FONT]
[FONT=&quot]presently no way known to completely separate these two[/FONT]
[FONT=&quot]properties. Dihydrotestosterone is also not unique in its[/FONT]
[FONT=&quot]ability to facilitate androgenetic alopecia (male pattern hair[/FONT]
[FONT=&quot]loss). DHT inhibition, therefore, does not offer complete[/FONT]
[FONT=&quot]protection against this side effect.[/FONT]
[FONT=&quot]Reductase inhibitors are only applicable with testosterone,[/FONT]
[FONT=&quot]methyltestosterone, and fluoxymesterone. These three drugs[/FONT]
[FONT=&quot]are converted to stronger “dihydro” derivatives by the[/FONT]
[FONT=&quot]reductase enzyme. Nandrolone and some of its derivatives[/FONT]
[FONT=&quot]become weaker upon interaction with this enzyme, as their[/FONT]
[FONT=&quot]“dihydro” metabolites bind the androgen receptor very[/FONT]
[FONT=&quot]poorly. Reductase inhibition may intensify their androgenic[/FONT]
[FONT=&quot]side effects. Methandrostenolone and boldenone undergo[/FONT]
[FONT=&quot]conversion to stronger 5-alpha reduced metabolites, but at[/FONT]
[FONT=&quot]such small levels that reductase inhibitors have little effect[/FONT]
[FONT=&quot]on their androgenicity. Most other synthetic anabolic steroids[/FONT]
[FONT=&quot]are unaffected by the reductase enzyme and reductase[/FONT]
[FONT=&quot]inhibitors.[/FONT]
[FONT=&quot]Administration:[/FONT]
[FONT=&quot]When used medically for the treatment of symptomatic benign[/FONT]
[FONT=&quot]prostatic hyperplasia (BPH), dutasteride is taken in a dosage[/FONT]
[FONT=&quot]of .5 mg (1 capsule) per day. When used by bodybuilders and[/FONT]
[FONT=&quot]athletes to reduce the androgenicity of testosterone,[/FONT]
[FONT=&quot]methyltestosterone, or fluoxymesterone, dutasteride is[/FONT]
[FONT=&quot]commonly taken in a dosage of .5 mg (1 capsule) once every[/FONT]
[FONT=&quot]1-2 days. The drug is typically administered for as long as[/FONT]
[FONT=&quot]the offending steroids are also taken.[/FONT]
[FONT=&quot]Availability:[/FONT]
[FONT=&quot]GlaxoSmithKline distributes this drug in the U.S., Europe,[/FONT]
[FONT=&quot]and South America under the Avodart trade name.[/FONT]
[FONT=&quot]Additionally, a number of other brands can be found in[/FONT]
[FONT=&quot]different markets including Austria (Avolve, Zyfetor),[/FONT]
[FONT=&quot]Greece (Duagen), India (Duprost), Netherlands (Duagen),[/FONT]
[FONT=&quot]Portugal (Duagen), and Spain (Duagen).

By WL
[/FONT][FONT=&quot][/FONT]

Avodart® (dutasteride) Reductase Inhibitors DHT blockers

akn

Musclechemistry Member

Similar threads