Dyrenium® (triamterene) Diuretic profile , administration and side effects

akn · Jun 18, 2014

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Triamterene is an oral diuretic used medically to treat
edema. Edema may occur without known cause (idiopathic
edema), or be associated with liver or kidney disease,
congestive heart failure, corticosteroid/progestin use, or the
overproduction of aldosterone. Triamterene is classified as a
potassium sparing diuretic, increasing the rate of water and
sodium excretion but preserving potassium levels. As the
name suggests, this drug produces a pronounced diuretic
effect without the potassium loss associated with
thiazides/loop diuretics. The need for potassium
supplementation is, therefore, eliminated with this agent. The
diuretic activity following a single dose of triamterene is
usually evident within 2 to 4 hours, reaching peak effect at
approximately 3 hours in most cases. Its diuretic effect lasts
for a total of 7-9 hours following administration.
Triamterene is utilized (off-label) by bodybuilders and
athletes to shed subcutaneous water prior to a bodybuilding
competition, or to make weight class adjustments in certain
competitive sports. Bodybuilders in particular rely heavily
on the increased definition that can result when wa
retention is reduced. The highly defined “shredded” physique
common to bodybuilding today is nearly impossible to
achieve without the use of diuretics. At the same time,
diuretics are the reason weight class competitors like
wrestlers and boxers often appear much heavier during an
event than they do at the weigh-in. A considerable amount of
bodyweight (in the form of water) can be removed with
diuretic use, often resulting in a drop of one or more weight
categories. This practice is very common in sports where the
user is not drug tested and has ample time to rehydrate
following a weigh-in, resulting in the athlete competing at a
significantly heavier weight than his or her weight class
would dictate.
History:
Triamterene first saw extensive clinical use during the
1960s. It was used largely as a standalone agent at first, but
went on to become a widely used agent in clinical medicine
in combination products with other diuretic drugs. Today this
usually includes other, more potent diuretics like thiazides
and loop agents. Here, the potassium loss of the stronger
diuretic is balanced to some degree by the potassium sparing
triamterene, which often results in a reduced or even
eliminated need for potassium supplementation during
therapy. Single ingredient preparations of triamterene are
still sold, however, and can be found in several countries
including Belgium (Dytac), United Kingdom (Dytac), and the
United States (Dyrenium).
How Supplied:
Triamterene is most commonly supplied in capsules of 50 mg
and 100 mg.
Structural Characteristics:
Triamterene is a potassium-sparing diuretic. It has the
chemical designation 2,4,7-triamino-6-phenyl-pteridine.
Warnings (Dehydration, Death):
The misuse of diuretic drug(s) for physique- or performanceenhancing
purposes is characterized as a high-risk practice.
Diuretics may produce a life-threatening level of dehydration
and electrolyte imbalance when administered without proper
medical supervision. Many deaths have been associated with
the misuse of these drugs. It is also important to note that the
supplementation of potassium, either through pharmaceuticals
or a diet rich in potassium, is generally not advised while
taking a potassium-sparing diuretic like triamterene.
Excessive potassium intake may cause hyperkalemia, which
may lead to cardiac irregularities and possibly death.
Side Effects:
Triamterene use may be associated with electrolyte
imbalance, including elevated or decreased potassium
levels. Signs of electrolyte imbalance include dry mouth,
thirst, weakness, lethargy, drowsiness, restlessness, muscle
pain, muscle cramping, seizures, reduced urine volume, low
blood pressure, and gastrointestinal disturbances. Other side
effects may include nausea, vomiting, jaundice, blood
platelet deficiency, anemia, azotemia (buildup of metabolic
waste products in the blood), renal stones, and other kidney
disturbances. Additionally, some rare side effects
characterized as hypersensitivity reactions have been
reported including skin rash, photosensitivity, and
anaphylaxis (an extreme and potentially life threatening
allergic reaction).
Administration:
When used medically to treat hypertension, the usual initial
dosage in adults is 100 mg twice daily after meals (200 mg
per day). This may be increased, but should never exceed
300 mg per day in total. Among bodybuilders, this drug is
commonly used for only a few days prior to a competition,
adjusting the dosage over the course to elicit the best level of
diuretic effect. Since it has a long lasting action, it is
generally administered once per day. One capsule (100 mg)
is usually taken the first thing in the morning with a meal, and
the effect judged over the next several hours. The dosage is
usually increased by one capsule per day for 2-3 days at
most, until the user is noticing the proper water loss for
competition. When looking for a stronger diuretic effect,
many bodybuilders and athletes will opt to combine
triamterene with another stronger diuretic such as
hydrochlorthiazide or furosemide. The dosage of both agents
would be adjusted downward to compensate for their
combined effects. The goal here is usually to increase shortterm
diuresis, without causing the extreme potassium loss
that can be associated with the use of thiazides or loop
diuretics alone at higher doses.
Availability:
Triamterene is widely sold throughout the developed world.
Although single-ingredient preparations containing
triamterene are available, this drug is most commonly sold in
multi-ingredient preparations targeting edema and/or high
blood pressure. Low cost, modest demand, and high
availability make this drug a low-profit target for
counterfeiting.

By WL

Dyrenium® (triamterene) Diuretic profile , administration and side effects

akn

Musclechemistry Member

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