Aranesp® (darbepoetin alfa) Endurance/Erythropoietic Drugs Profile

akn · Jun 19, 2014

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Darbepoetin alfa is a synthetic derivative of the human
erythropoietin protein. It also has the same pharmacological
action as recombinant human erythropoietin (epoetin alfa). In
the body, erythropoietin is normally released by the kidneys
in response to hypoxia (low blood oxygen levels). This in
turn triggers bone marrow to increase red blood cell
production. As such, this hormone is vital to the regulation of
normal red blood cell concentrations in humans. With a
similar mode of action to recombinant erythropoietin,
darbepoetin alfa can be used to augment erythropoiesis when
the body is not maintaining adequate red blood cell levels on
its own. It is FDA approved for the treatment of anemia (low
red blood cell count) associated with chronic renal failure or
chemotherapy.
Darbepoetin alfa differs from recombinant human
erythropoietin (epoetin alfa) mainly in its duration of
activity. This new protein maintains its levels in the blood
for approximately three times longer, causing it to have a
much longer therapeutic window. This means that with
darbepoetin alfa patients are required to administer the
product much less frequently than they would epoetin alfa.
While epoetin alfa is usually injected on a schedule of three
times per week, darbepoetin alfa requires only one injection
in the same time frame. This may enhance patient comfort
considerably, especially when the patient is visiting the
physician for routine drug administration.
Endurance athletes are highly attracted to darbepoetin alfa
for the effect it has on red blood cell production. It is no
secret that the practice of blood doping has been popular
with endurance sports. This procedure involves removing,
concentrating, and storing a quantity of red blood cells from
your own body to be transfused later. By adding the stored
cells before an event (by then the body has restored the lost
blood volume), the athlete has a much greater concentration
of red blood cells. The blood should, likewise, transport
oxygen more efficiently, and the athlete may be given a
significant endurance boost. This procedure can be quite
risky, however, as blood products can be difficult to store
and administer correctly. Darbepoetin alfa is a drug that
basically equates to chemical blood doping, and can achieve
the same end result (higher red cell concentrations) with the
use of a simple medication.
History:
Darbeopetin alfa was developed as a prescription drug by
Amgen. The U.S.Food & Drug Administration first approved
it for sale in 2001. Amgen is the world’s largest
biotechnologies company, and the same firm that first brought
recombinant erythropoietin (epoetin alfa) to the U.S. market
in 1984. The main focus with darbepoetin alfa appears to
have been the development of a much longer acting
erythropoietic protein in comparison to their earlier
recombinant erythropoietin, which is commonly injected on a
schedule of three times per week. The prescribing guidelines
for darbepoetin alfa recommend a once per week schedule,
which seems to offer strong comfort advantages to epoetin
alfa for patients that do not like receiving frequent injections.
Darbepoetin alfa has not yet reached the level of market
success that has been noted with epoetin alfa preparations,
but has been a strong selling drug for Amgen ever since its
release.
How Supplied:
Darbepoetin alfa is most commonly found in single-dose
vials and prefilled syringes containing 25, 40, 60, 100, 150,
200, 300, or 500 mcg of drug.
Structural Characteristics:
Darbepoetin alfa is a 165-amino acid protein that differs
from human erythropoietin by the substitution of amino acids
on the erythropoietin peptide backbone, which allows the
addition of two additional N-linked oligosaccharide chains.
Warnings (Death, Viral Disease):
The misuse of darbepoetin alfa for physique- or
performance-enhancing purposes is characterized as a highrisk
practice. Like traditional blood doping methods,
darbepoetin alfa can produce an abnormally high
concentration of hemoglobin in the blood (polycythemia),
which may result in heart attack, stroke, seizure, or death.
Some forms of darbepoetin alfa contain albumin, a purified
human blood product. Although effective donor screening
and product manufacturing procedures are in place, it still
carries a risk, though extremely remote, for transmission of
viral disease.
Side Effects:
Side effects associated with the use of darbepoetin alfa may
include flu-like symptoms such as fever, chills, headache
muscle pain, weakness, or dizziness. Such effects tend to be
more pronounced at the initiation of therapy. Other adverse
reactions may include infection, rash, swelling of the skin,
nausea, vomiting, diarrhea, high blood pressure, low blood
pressure, cough, bronchitis, or edema. In some instances
darbepoetin alfa has been associated with thromboembolism,
deep-vein thrombosis, pulmonary embolism, heart attack, and
cerebrovascular accidents.
Administration:
Darbepoetin alfa is indicated for the treatment of anemia
associated with chronic renal failure (CRF) and
chemotherapy. The recommended starting dose for the
treatment of anemia in adult CRF patients is .45 mcg/kg body
weight, administered once per week as a single IV or SC
injection. The dosage is subsequently adjusted based on
changes in hematocrit. Healthy athletes using darbepoetin
alfa for performance-enhancing purposes generally start on
the very low end of the therapeutic spectrum, and adjust
according to changes in hematocrit. This may entail initiating
therapy with as little as .05 mcg/kg of body weight once per
week. Note that it is considered very important to monitor
blood cell counts closely during the entire intake of
darbepoetin alfa to help ensure hematocrit is not allowed to
increase to an unhealthy level.
Availability:
Darbepoetin alfa is not widely sold on the black market. Yet
because of the high cost for erythropoiesis stimulating agents
like darbepoetin alfa, it is a high profile target for counterfeit
drug manufacturing operations. Counterfeit drugs of this class
have even infiltrated legitimate pharmaceutical distribution
channels, suggesting that care should be taken when
purchasing this and similar drug products.

By WL

Aranesp® (darbepoetin alfa) Endurance/Erythropoietic Drugs Profile

akn

Musclechemistry Member

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