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by Anthony Roberts - Ketotifen Fumarate is
an H1-antihistamine that is available in two versions
oral and ophthalmic. In the ophthalmic (for use
in the eye) form, it is used to treat conjunctivitis
(pink eye), or the itchy red eyes caused by allergies.
It is used orally as a medication to aid in the
prevention of asthma attacks, and has also been
used by many as a sleeping aid and appetite stimulant.
Background
Ketotifen fumurate is sold under the brand name
Zaditor. It is also available from many underground
labs, typically for use with
clenbuterol or sometimes
mixed with it.
Action
Ketotifen is an antihistimine that inhibits down
regulation of beta receptors, which are often degraded
by fat-burners such as Albuterol
and Clenbuterol.
It can be used in combination with these other
drugs in order to keep feeling their fat-burning
effects for longer periods of time with out the
need for periods of on and off cycling. Side effects
can include drowsiness, irritability, nosebleeds
and dry mouth. Ketoifen increases appetite; therefore
another side effect is typically weight gain. Ketotifen
also (potentially) improves insulin sensitivity
within muscle tissue.
Technical Data
Because Ketotifen has the ability to stimulate
the appetite, it has been studied for use with wasting
conditions. In the most commonly referenced study
examining this property, 22 AIDS patients who were
administered Ketotifen and
Oxymetholone, 18 gained an average of 11.4 pounds
after just under 4 weeks (1). Further research proved
Ketotifen to be a TNF-alpha blocker. TNF-alpha lowers
testosterone and IGF-1 levels
immensely (2,3) while strenuous exercise raises
TNF-alpha levels (4). TNF-alpha has also been found
to inhibit the muscle's ability to uptake glucose,
(which is known as insulin resistance). It has recently
been discovered that
hypogonadism and low testosterone are also associated
with elevated TNF-alpha (5).
This would seem to indicate a potential use for
Ketotifen in Post-Cycle Therapy.
User Notes
Ketotifen was first introduced to the bodybuilding
world by Dan Duchaine, who proposed its use for
upregulation of Beta – Receptors. Several years
after his passing I figured out that Benadryl would
work for the same purpose, and Ketotifen was largely
abandoned for the more commonly available Benadryl.
It is, however, due to the late Karl Hoffman
that we owe the use of Ketotifen for reducing TNF-a
and for possible use in PCT. He pioneered this idea
(though it didn’t really catch on, per se), and
it would seem to be very beneficial as an anti-catabolic,
though it’s cost would make it prohibitive for use
in up-regulating Beta-Receptors.
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| Trivial
Name |
Ketotifen fumarate |
| Systematic
Name |
4,9-dihydro-4-(1-methyl-4-piperidinylidene)-
10H-benzocyclohepta[1,2-b]thiopen-10-one |
| CAS Number |
34580-14-8 |
| Merck Index
Number |
5144 |
| Chemical
Formula |
C19H19NOS
· C4H4O4 |
| Molecular
Weight |
425.50 g/mol |
| Bioavailability |
60% |
| Metabolism |
Hepatic |
| Elimination
Half Life |
21 Hours |
| Excretion |
Urinary |
| Legal Status |
Prescription |
| Route of
Administration |
Oral |
References
- Smart T. GMHC Treat Issues. 1995 May;9(5):7-8,
12.
- Mauduit C, et.al Endocrinology 1998 Jun;139(6):2863-8
- Lang CH et.al Growth Horm IGF Res 2001 Aug;11(4):250-60
- Pedersen BK et. al. Exerc Immunol Rev 2001;7:18-31
- Malkin CJ et.al. J Clin Endocrinol Metab.
2004 Jul;89(7):3313-8.
(Assistance on this profile provided by Rosanne
Clemente)
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