Meridia® (sibutramine hydrochloride) Fat Loss Agent - Sympathomimetics profile

akn

Musclechemistry Member
<!--[if gte mso 9]><xml> <w:WordDocument> <w:View>Normal</w:View> <w:Zoom>0</w:Zoom> <w:TrackMoves/> <w:TrackFormatting/> <w:punctuationKerning/> <w:ValidateAgainstSchemas/> <w:SaveIfXMLInvalid>false</w:SaveIfXMLInvalid> <w:IgnoreMixedContent>false</w:IgnoreMixedContent> <w:AlwaysShowPlaceholderText>false</w:AlwaysShowPlaceholderText> <w:DoNotPromoteQF/> <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:DontGrowAutofit/> <w:SplitPgBreakAndParaMark/> <w:DontVertAlignCellWithSp/> <w:DontBreakConstrainedForcedTables/> <w:DontVertAlignInTxbx/> <w:Word11KerningPairs/> <w:CachedColBalance/> <w:UseFELayout/> </w:Compatibility> <w:DoNotOptimizeForBrowser/> <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]--> Description:
Phentermine hydrochloride is a sympathomimetic stimulant
of the amphetamine family. Like other amphetamine
derivatives, it is categorized as an anorectic (appetite
suppressing) agent. Phentermine is commonly prescribed as a
weight loss aid in obese patients. It is typically used for short
periods of time (less than 12 weeks), and as an adjunct to
support an ongoing exercise and dieting regimen.The main
focus is to curb the desire to eat, thereby reducing the total
caloric intake. Although the data seems to vary from trial to
trial, much of it supports at least a modest additional loss of
fat mass with the use of phentermine hydrochloride.886
Athletes and bodybuilders use phentermine hydrochloride for
the same purpose, typically when weight loss is required for
physique remodeling or competition.
History:
Phentermine hydrochloride was first introduced to the U.S.
drug market in the 1970s. Base phentermine was available in
the U.S. as far back as 1959. Phentermine had long been used
as an appetite suppressant, although the most notable
attention to it came in the early 1990s, when the drug was
successfully paired with fenfluramine during diet studies.
Investigators had shown that this type of drug combination
was actually more effective at promoting weight loss than
diet and exercise, results that quickly catapulted Fen-Phen
into top place in the prescription weight loss drug market. By
1997, however, it had become apparent that a very high
percentage of Fen-Phen users were noticing heart valve
defects as a result of the drugs. Fenfluramine was identified
as the principle cause, and was withdrawn from the U.S.
market that same year. Phentermine remains available in the
U.S. and many nations abroad today. Popular trade names
include Adipex, Ionamin, Anoxine, Phentrol, and Obenix.
Note that as an amphetamine derivative, this medication has
a tendency to be habit forming. For this reason it has been
added to the U.S. controlled substances list as a schedule IV
medication.
How Supplied:
Phentermine hydrochloride is most commonly supplied in
tablets and capsules of 18.75 mg and 37.5 mg each.
Structural Characteristics:
Phentermine hydrochloride is a central stimulant and
indirect-acting sympathomimetic of the amphetamine family.
It has the chemical designation 2-methyl-1- phenylpropan-2-
amine (2-methyl-amphetamine).
Side Effects:
Common side effects associated with phentermine
hydrochloride include insomnia, increased blood pressure,
irritability, nervousness, and euphoria. Less common side
effects include vision disturbances, reduced libido,
confusion, diarrhea, dizziness, dry mouth, headache, irregular
heartbeat, nausea, vomiting, rash, and tiredness. Phentermine
is a CNS stimulant with potential for fatal overdose. Signs of
overdose may include rapid breathing, fever, hallucinations,
blood pressure irregularities, irregular heartbeat,
unconsciousness, trembling, shaking, panic, extreme
restlessness, and severe nausea, vomiting, or diarrhea.
Administration:
For optimal effectiveness, phentermine hydrochloride should
not be taken with food. The usual adult dose is one capsule
or tablet (37.5 mg) daily, administered before or 1- 2 hours
after breakfast. For some patients a half of a tablet (18.75
mg) daily may be adequate, while in other cases it may be
advisable to give a half of a tablet (18.75 mg) twice
daily.When taken more than once per day, the second dose
should never be taken within 4-6 hours of sleep. The drug is
typically used for 3-4 weeks at a time, with longer durations
of therapy rarely exceeding 12 weeks. Bodybuilders and
athletes typically use the prescribed amount of drug in a
similar short-term fashion,due to the high likelihood of side
effects as the dose escalates beyond the normal therapeutic
range.
Availability:
Phentermine hydrochloride is available in a number of
different countries. It is not widely counterfeited. U.S.
residents would not be advised to order the drug from
overseas, however, since phentermine is a schedule IV
controlled substance and carries similar legal restrictions as
Valium and anabolic steroids. Many U.S. doctors who
specialize in weight loss medications will readily dispense
phentermine for controlled periods of weight loss.

activation. With the use of this drug, we are specifically
seeing a strong increase in brown adipose tissue
thermogenesis (BAT), which is accompanied by body
temperature increases of .5 – 1 degree Celsius.690 Elevated
body temperature is a good indicator that thermogenesis is
being triggered, which you may recall as one of the key
things we are looking for when taking clenbuterol.
To get a better idea of exactly how well sibutramine
hydrochloride works, we refer to some of the clinical studies
on this agent.One investigation was conducted at the Kansas
Foundation for Clinical Pharmacology in 2001. Here, a
group of 322 obese patients were given either 20 mg of
sibutramine or placebo once daily for 24 weeks. By the
conclusion of this study, 42% of patients in the sibutramine
group lost 5% or more of their initial body weight, while
12% noticed a 10% or greater loss in body weight.
Sibutramine was also associated with significant
improvements in serum triglyceride and HDL cholesterol
levels, which were displaying poor values at the onset of the
study. Another detailed investigation was completed in China
by the Department of Endocrinology for Rui-jin Hospital this
same year, and involved giving only 10 mg per day of
sibutramine to a group of 120 men and women.691 This
investigation also faired extremely well, with patients losing
an average of 15 pounds by the 24th week of use
History:
Sibutramine hydrochloride received Food and Drug
Administration approval for sale as a prescription weightloss
agent in 1998. It was developed and marketed by Abbott
Laboratories, which sold the drug on the U.S. market under
the brand name Meridia. The company also sold the drug in
many international markets under the name Reductil.
Sibutramine enjoyed only a limited period of sales in the
U.S., as it was removed from the market in October 2010
under FDA pressure, citing an increased incidence of
adverse cardiovascular events. Abbott has since also
withdrawn sibutramine from many markets worldwide. Note
that sibutramine remains classified as a schedule IV
controlled substance in the United States.
How Supplied:
Sibutramine hydrochloride is most commonly supplied in
capsules of 5 mg, 10 mg, and 15 mg.
Structural Characteristics:
Sibutramine hydrochloride is a centrally-acting serotoninnorepinephrine
reuptake inhibitor structurally related to
amphetamine. It is chemically a racemic mixture of (+) and (-
) enantiomers of 1-(4-chlorophenyl)-N,N-dimethyl-a-(2-
methylpropyl)-cyclobutanemethanamine.
Side Effects:
The most common side effect with sibutramine is an increase
in blood pressure, a trait that contraindicates its use in
patents with high blood pressure or other cardiovascular
issues. Other common side effects include dry mouth,
sleeplessness, irritability, back pain, stomach upset, and
constipation, all of which tend to become reduced in
magnitude as the user becomes accustomed to the drug.
Sibutramine hydrochloride should be discontinued
immediately if any of the more serious side effects or
symptoms of toxicity occur, including excitement,
restlessness, loss of consciousness, confusion, agitation,
weakness, shivering, clumsiness, rapid heartbeat, large
pupils, vomiting, difficulty breathing, chest pains, swelling of
feet, ankles or legs, fainting, disorientation, depression, high
fever, eye pain, tremor, or excessive sweating. Note that
increased incidence of cardiovascular events has prompted
the removal of this product from most markets. It is no longer
considered a safe product by many standards.
Administration:
Sibutramine hydrochloride is used for the management of
obesity, including weight loss and maintenance, and should
be used in conjunction with a reduced-calorie diet. This drug
has been used with patients who have additional weightrelated
risk factors including controlled hypertension,
diabetes, and dyslipidemia (high cholesterol). The
recommended starting dosage for most patients is 10 mg once
daily, which is to be adjusted upwards to 15 mg after 4
weeks if weight loss has not been sufficiently initiated.
Higher doses are usually not recommended.
Availability:
This drug is subject to limited availability following an FDA
supported recall in the United States, and subsequently its
removal from many other international markets for safety
reasons.
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