Glucophage (metformin hydrochloride) Hypoglycemics profile and use in bodybuilding

akn · Jun 11, 2014

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Metformin hydrochloride is an oral antihyperglycemic
medication. It is prescribed for the management of Type-II
diabetes, sometimes also referred to as mature onset diabetes
since it tends to develop later in life. The drug is typically
utilized when dietary management and exercise alone have
not been able to control the progress of the disease, yet
injectable insulin is not an appropriate option. While the
main activity of metformin HCL is the increased utilization of
glucose, it does not directly mimic the action of insulin.
While its precise mode of action is unknown, it is understood
to reduce the output of glucose by the liver, decrease the
intestinal absorption of glucose, and increase insulin
sensitivity in certain organs and peripheral tissues. Use of
this agent will lower the patient’s blood sugar, though its
activity makes it less likely to cause a dangerous state of
hypoglycemia if the dosage is accidentally misjudged (a
concern with injectable insulin).
Insulin manipulation is common in sports due to the
biological actions of this hormone. Insulin is involved in
nutrient storage, helping to transport amino acids, fatty acids,
and carbohydrates (glucose) into various cells. In the case of
muscle cells, insulin also facilitates cellular anabolic
(protein synthesizing) and anti-catabolic (protein sparing)
actions. This hormone also directs nutrient storage to adipose
cells, however, thus its manipulation has the potential to
increase fat mass. Bodybuilders have found, however, that
with intense weight training, insulin can show a much greater
affinity for protein and carbohydrate storage in muscle cells.
By manipulating insulin levels (or insulin sensitivity) under
these conditions, muscle growth with minimal fat gain is
possible. Injectable insulin can be risky however, as a
mistake in dosage or carbohydrate intake has the potential to
cause life-threatening hypoglycemia (low blood sugar).
Since this effect is rare with metformin, it is considered by
some athletes to be an introduction to insulin manipulation.
History:
Metformin has a long and fairly complicated history in
medicine. This drug was first synthesized in 1929 along with
a series of other biguanides. Although some of its beneficial
properties were elucidated at the time, it was not initially
subject to human trials.729 It sat idle in the research books for
nearly three decades after its creation. The first clinical study
investigating its therapeutic potential as a glucose lowering
medication was finally initiated in 1956.730These trials were
very successful, and metformin was selected for clinical
development. It was given the trade name Glucophage, which
translates to “glucose eater”. This, of course, refers to its
ability to help the body dispose of blood glucose.
Glucophage went on to be the most recognized trade name
for metformin HCL. This trade name is still being used to
market the drug today, presently by the Bristol-Myers Squibb
Company.
Metformin was not initially the glucose-lowering agent of
choice among clinicians. During the 1950s, it had been
studied alongside phenformin and buformin, which had also
been selected for commercial development. Metformin was
initially pushed aside in favor of these two drugs, both of
which had proven to be significantly more potent at lowering
blood sugar levels. These drugs would remain the dominant
biguanides for approximately 20 years. By the 1970s,
however, it was being reported that phenformin and buformin
were producing unacceptably high incidences of lactic
acidosis, an often-fatal metabolic disorder characterized by a
rapid drop in pH. By the close of the 1970s, most
governments had determined that these drugs were too risky
to continue using. Phenformin and buformin were
subsequently removed from most pharmaceutical markets
worldwide.
The structural and pharmacological similarity of metformin
to phenformin and buformin held back its clinical potential
for many years. Researchers were widely concerned that this
agent would also present unfavorable risks.While lactic
acidosis is a legitimate concern, it occurs much less
frequently than with the other biguanides (approximately 1 in
33,000 patients). Following much evaluation of its benefitrisk
ratio, metformin eventually came to be regarded as the
safest drug of the biguanide class. It was widely pushed back
into clinical medicine during the mid-1990s. It was
introduced to the United States in 1995, where it was an
immediate success. In the years to follow, metformin
continued to grab a stronger share of the global diabetes
medication market. Today, it is estimated that metformin
HCL is the most widely prescribed medication for the
treatment of type-2 diabetes.
How Supplied:
Metformin hydrochloride is most commonly supplied in oral
tablets of 500, 850, and 1000 mg each.
Structural Characteristics:
Metformin is a synthetic derivative of the natural antidiabetic
agent guanide. It is specifically the 1,1- dimethylated
biguanide variant.
Warnings:
In rare cases, the use of metformin HCL is associated with
lactic acidosis, an often-fatal metabolic disorder involving
(among other factors) an increase in lactate levels (lactic)
and a pronounced decrease in blood pH (acidosis). This risk
increases with conditions such as sepsis, dehydration, excess
alcohol intake, hepatic insufficiency, renal impairment, and
acute congestive heart failure. Symptoms of lactic acidosis
include malaise, muscle pain, respiratory distress,
drowsiness, and abdominal distress. Laboratory
abnormalities include low pH,increased anion, and elevated
blood lactate. If lactic acidosis is suspected, metformin HCL
should be discontinued and the individual should seek
immediate medical attention.
Side Effects:
Common side effects of metformin HCL therapy include
diarrhea (53.2%), nausea/vomiting (25.5%), flatulence
(12.1%), weakness (9.2%), indigestion (7.1%), abdominal
discomfort (6.4%), and headache (5.7%).731 Metformin must
be used with caution in patients with renal dysfunction, and
impaired creatinine clearance. A serum creatinine
concentration above 1.5 mg/dL (men) or 1.4 mg/dL (women)
is considered a contraindication to treatment. Metformin may
also impair the absorption of vitamin B12. Hypoglycemia is
uncommon with the use of metformin, though is sometimes
noted when caloric intake is deficient, or when strenuous
exercise is not compensated by caloric supplementation.
Minor side effects often subside over time, or with use of a
lower metformin HCL dosage. Lactic acidosis has been
reported in approximately 32% of metformin HCL overdose
cases
Administration:
The oral absorption rate of metformin HCL is slow, with the
body taking approximately six hours to absorb and distribute
each dose. Extended release (XR) formulations are also
made, which further delay the absorption of metformin HCL.
Extended release tablets should be taken whole, and not
crushed. In a clinical setting, the drug is given in divided
doses with meals, except for extended release formulations,
which are administered once daily with the evening meal.
There is no set adult clinical dose, and the drug must be
tailored to and the drug must be tailored to the individual
needs of the patient. It is typically initiated at a low daily
dosage, and slowly escalated by 500 mg each week or 850
mg every two weeks until the minimum daily dose required
for adequate glycemic control has been established. The
maximum recommended daily dose for type-2 diabetic
patients in 2550 mg per day. Fasting plasma glucose is used
to determine the therapeutic response to metformin HCL, and
glycosylated hemoglobin levels are measured every three
months. The goal of therapy is to decrease fasting plasma
glucose and glycosylated hemoglobin levels to normal or
near normal levels using the lowest effective dose of
metformin HCL, either alone or in combination with another
antihyperglycemic drug (sulfonylurea or insulin).
When used for physique or performance-enhancing purposes,
the typical protocol is to take 850 mg once or twice per day.
If a single application is desired, it is typically taken 1-2
hours before exercise, so that the drug can have its peak
effect during the early stages of recovery. It is highly
common to utilize a carbohydrate supplement during the
hours metformin is active in the body, especially during the
crucial 2-3 hour “nutrient uptake” window following intense
training. The result of metformin treatment is typically not as
dramatic as insulin, but the drug still does have a notable
anabolic effect for many users. Most bodybuilders/athletes
opt to use this drug for a limited duration, with cycles lasting
6-8 weeks in length. This would be followed by an equally
long break (at a minimum) before metformin, insulin, or any
other antihyperglycemic agent is used for physique or
performance-enhancing purposes.
Availability Trends:
Metformin is readily available given its widespread use in
clinical medicine. It is sold under many brand names, as both
a standalone and combination medication. Bodybuilders and
athletes tend to limit their use to preparations containing only
metformin.While the drug is not the subject of much interest
by steroid counterfeiting or underground manufacturing
operations, it is the target of many other general drug
counterfeits given the ease in which it can be sold. As such,
it should not be assumed that all packaged drug products
labeled as metformin are legitimate. Care should be taken to
ensure that all products bearing this ingredient have been
acquired through legitimate pharmaceutical channels

Presser · Sep 1, 2018

Bumping metformin to the top, reminde to fix the run on sentences and seperate paragraphs

Glucophage (metformin hydrochloride) Hypoglycemics profile and use in bodybuilding

akn

Musclechemistry Member

Presser

Admin

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