Ketotifen

[JayDiesel Senior Member Find all posts View Profile Close JayDiesel]

Ketotifen and Clen
Clenbuterol is a beta 2 agonist which has a limited anabolic effect during its first few days of use and afterward is normally used to fight fat. At higher doses, however, it can be catabolic to muscle and it must be cycled on a 2 week on, 2 week of basis or the beta 2 receptors that clen binds to become saturated and down regulate.

Ketotifen's magic is that it upregulates the beta-receptors including the beta 2s that clen uses. As long as you are taking ketotifen, it will continue to clean these receptors, never allowing them to downregulate, even while on a heavy clen cycle. That means you can continue to take clen indefinitely without having to cycle off to regenerate the receptors. 2-3mg ED can upregulate even severely shut down receptors within a week.

It also means that you don't need as much clen to get the same benefits. It seems u can take about 30-40% less clen and it be equally effective. FONZ posted that it also increases the number of receptor sites on the surface of the cell, allowing more clen to attach and perhaps this is the reason for the increased efficacy. Ketotifen also seems to lessen the sides of clen including the jitters.

Ketotifen and ECA
Perhaps an even better use for ketotifen is taking it with the ECA stack. While the thermogenic effect of ephedrine is not as potent as clen because it doesn't have a high receptor affinity, and it is not limited to beta-2 receptors. In fact it seems to have a good effect on beta 3 receptors as well, which act as a type of thermogenic messenger and over half of ephedrine effect is from beta-3 stimulation. Clen has almost no effect on beta 3 however. So by keeping the beta 2 receptors up, ketotifen can allow the benefits of continuous beta 2 and beta 3 stimulation from ephedrine.

[JayDiesel Senior Member Find all posts View Profile Close JayDiesel]

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.





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.

[JayDiesel Senior Member Find all posts View Profile Close JayDiesel]

Ketotifen
Ketotifen was made popular by its ability to inhibit the down regulation of beta receptors caused by drugs like clenbuterol. Clenbuterol, albuterol, and Ephedrine used to be cycled on and off because they desensitize the various receptors they act on to produce their lipolytic effect. Ketotifen would therefore allow the use of these fat burning drugs for much longer periods.

If youve read my writings on Clenbuterol, you already know that Benadryl (the anti-histimine) can also be used for this same purpose, and is 10x cheaper and infinitely more available to most people. So why am I bothering to write about Ketotifen at all?

Ketotifen, in medical circles, is also recognized for its ability to lower levels of the cytokine Tumor Necrosis Factor-alpha (TNF-alpha), which is a catabolic hormone, and this is a property that Benadryl does not have to my knowledge. TNF-alpha lowers both testosterone and IGF-1 levels (3) (4), and strenuous exercise elevates TNF-alpha levels (5). TNF-alpha has also been shown to increase insulin resistance,, which we certainly dont want.

Ketotifen and Weigh Loss
Ketotifen is used by people suffering from wasting diseases partially caused by TNF-alpha. I think, however, its ability to lower TNF-alpha is going to be overshadowed by anabolic effects produced by anabolic steroids. In one study involving AIDS patients, combining Ketotifen and Oxymetholone (Anadrol 50) showed that the Ketotifen didnt add much to the Oxymetholone induced weight gain (1). Hence, you are reading this profile in the "Ancilliaries" portion of this book, and not the "Fat - Burning" part, even though Ketotifen is typically used as part of a fat burning cycle including clen. Benadryl is simply too much cheaper and readily available to use Ketotifen in its place with Clen. However, for Post-Cycle-Therapy, Ketotifen and its ability to lower TNF-alpha, is a very valuable tool. You see, Hypogonadism (low testosterone) often accompanies elevated TNF-alpha levels (6), and after a cycle of anabolic steroids, you are going to be in a hypogonadal state, with elevated TNF-alpha. Thus, taking Ketotifen with your PCT is probably a very good idea. I recommend 1-3mgs/day before bed because this stuff will make you pretty drowsy.

References:




Oxymetholone promotes weight gain in patients with advanced human immunodeficiency virus (HIV-1) infection. Br J Nutr. 1996 Jan;75(1):129-38.
Smart T. GMHC Treat Issues. 1995 May;9(5):7-8, 12.
Mauduit C, et.al Endocrinology 1998 Jun;139(6):2863-.
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.

[JayDiesel Senior Member Find all posts View Profile Close JayDiesel]

Description:
Ketotifen is an antihistamine drug that is used for the treatment of general allergy symptoms, certain allergic conditions (including conjunctivitis), and the management of asthma. When used for asthma, the drug is not regarded as effective for treating an immediate attack (it is not a rapid bronchodilator). Instead, over time its use is associated with a reduction in the frequency, duration, and severity of attacks. It is usually prescribed as a way to increase the efficacy of other asthma medications. Likewise, ketotifen fumarate will usually supplement an existing asthma medication program, and not replace the prescribing of immediate rescue devices such as an asthma inhaler or nebuliser.
Ketotifen fumarate alleviates allergy symptoms by blocking histamine Hl receptors, a property that is common to drugs of the antihistamine class. Its second and very unique mode of action, however, makes it useful in the treatment asthma. Ketotifen fumarate increases the concentration of beta-adrenergic receptors in the body (especially beta-2 receptors). Drugs that stimulate beta-2 receptors are commonly prescribed as bronchodilators, used to increase airflow to the lungs and counter the constriction caused by asthma.. While potentially efficacious alone, one key therapeutic effect of ketotifen fumarate is to increase the sensitivity of the body to drugs ofthe beta agonist class.
The beta-2 receptor upregulating properties of ketotifen fumarate make this drug of interest to the bodybuilding and athletic communities. This is due to the strong role of the beta-2 receptor in supporting fat loss. Although not a strong fat loss compound by itself, when taken with a beta2 agonist thermogenic like clenbuterol, ketotifen fumarate may increase thermogenic potency and noticeably extend the window of active lipolysis. Clenbuterol and other beta2 agonists normally have a limited duration of usefulness here because beta-2-adrenergic receptors decrease in number with regular stimulation. Within several weeks of initiating therapy with such a drug, it usually begins to diminish in effectiveness. Ketotifen may extend this time period considerably.
The ability of ketotifen to potentiate the effects of beta-2 agonist drugs has been demonstrated in a number of clinical studies. For example, one study published in 1990 demonstrated that when ketotifen and clenbuterol were taken together, there was a significant increase in betaadrenergic receptor density compared to the use of clenbuterol alone, which again decreases beta adrenoceptor density fairly quickly.872 Other studies with salbutamol (also referred to generically as albuterol) showed that beta adrenoceptor downregulation caused by long-term use of this beta-adrenergic agent could be rapidly reversed with as little as 2mg of ketotifen fumarate per day.

History:
Ketotifen was globalized as a prescription medication by Novartis. It is presently prescribed for allergies, allergic conditions, and (most commonly) the management of asthma in more than three-dozen countries around the world. The most widely available brand name is Novartis'
Zaditen, which is sold throughout most parts of Europe and Asia. In addition to generic forms of the medication, dozens of other brand names can be found in many different markets as well. Ketotifen fumarate is approved for sale in the United States, but currently only as an ophthalmic anti-allergy solution (Zaditor), not an oral allergy/asthma medication. The dosage of ketotifen fumarate in this product is also too low for it to be ?considered useful for any other (off label) purpose. Given the ready availability of ketotifen fumarate in other countries, the drug is easily diverted for black market sale. As of now, it is not extremely popular with bodybuilders and athletes.
The UK guidelines on the clinical management of asthma consider ketotifen to be ineffective for the management of this disease. There is admittedly conflicting data on the potential usefulness of ketotifen fumarate for this purpose, with some studies reporting positive results and others showing an insignificant effect. A thorough review of the data published on the Cochrane Database of systematic Reviews in 2004 concluded that it appeared to have some usefulness in controlling asthma and wheezing in many children, but the variability of the disease and response to the drug meant that these positive results could not be generalized for all asthma patients.

How Supplied:
Ketotifen fumarate is most commonly supplied in tablets of 1mg. This dosage is usually expressed in terms of the base, so each tablet actually contains 1.38mg of ketotifen fumarate.

Structural Characteristics:
Ketotifen fumarate is selective histamine Hl antagonist, anti-allergic, and anti-asthmatic agent. It has the chemical designation 4-(1-Methyl-4-piperidylidene-4Hbenzo[4,5]cycl0 hepta[1 ,2-b]thiphene-l-(9H)-one fumarate.

Side Effects:
Common side effects include dry mouth, appetite stimulation, weight gain, dizziness, CNS stimulation, and drowsiness. These side effects are all commonly associated with strong antihistamine compounds. In rare cases severe allergic reaction on the skin or a urinary bladder inflammation called cystitis may occur.

Administration:
When used to reduce the frequency, duration, and severity of asthma attacks, ketotifen fumarate is usually initiated at a dosage of 1mg twice per day (2mg total). If necessary, this may be increased to a maximum dosage of 2mg twice per day (4mg total). Bodybuilders and athletes will commonly use a dosage of 1mg twice per day (2mg total) for the (off-label) use of preventing receptor downregulation with clenbuterol or other beta-agonists. This may allow an individual to obtain a strong thermogenic effect from, and run longer cycles with, beta2 agonist drugs. Note that given its ability to increase drug sensitivity, the dosage of beta-2 agonist medications may need to be reduced upon ketotifen fumarate administration.



Reference:
Llewellyn’s W. (2009). Anabolics (9th ed), Zaditen? ketotifen fumarate (pp. 525-527): Jupiter, FL: Molecular Nutrition

[beatricia2 Senior Member Find all posts View Profile Close beatricia2]

I take it in every cutting cycle

[RonnyT Senior Member Find all posts View Profile Close RonnyT]

Explain, bro, you are extremely ripped on stage, so educate our members on doses and stacks if you want..

[beatricia2 Senior Member Find all posts View Profile Close beatricia2]

no more that 80 grams carbohydrate never cardio,
ece every time whit ketotifen after 8 weeks every nigth.
only fish the dinner for 12 weeks
dont take fat out of contest fat under skin not in eating
gh 3 to 5 ui every morning
tren all ce cycle masteron 8 weeeks winstrol tabs the same first testosterone enanthate after sustanon 6 last weeks propionate no more 300 mg weeks, cut proprio 2 weeks before contest.
the same training all th year.
grenn tea and cafeine and ginkgo, taurine, calcium magnesium ect

[beatricia2 Senior Member Find all posts View Profile Close beatricia2]

ace not ece sorry

[player Senior Member Find all posts View Profile Close player]

thanx the info bea!

[BeauBody38 Member Find all posts View Profile Close BeauBody38]

Make sure to consider these side effects:

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using ketotifen ophthalmic and call your doctor at once if you have any of these serious side effects:

redness, drainage, eyelid swelling, or other signs of infection;
eye pain;
vision changes; or
severe itching of the eyes worse than before using the medication.
Less serious side effects may include:

mild burning, stinging, or eye irritation;
dryness of the eyes; or
increased sensitivity to light.
This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

[BeauBody38 Member Find all posts View Profile Close BeauBody38]

Make sure to consider these side effects:

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using ketotifen ophthalmic and call your doctor at once if you have any of these serious side effects:

redness, drainage, eyelid swelling, or other signs of infection;
eye pain;
vision changes; or
severe itching of the eyes worse than before using the medication.
Less serious side effects may include:

mild burning, stinging, or eye irritation;
dryness of the eyes; or
increased sensitivity to light.
This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

[beatricia2 Senior Member Find all posts View Profile Close beatricia2]

I take 3 mg every day before bed and it is magic for me, after the contest a little clen with it and I stay clean

[PartyHard Member Find all posts View Profile Close PartyHard]

Often adding ketotifen after two weeks of using clenover, helps a lot, no need to go on two weeks without clen.

[zetisuasa Junior Member Find all posts View Profile Close zetisuasa]

With this influence comes great responsibility, as they must paper io strive to present information accurately and objectively, without succumbing paper io2 to biases or sensationalism.

[kalyl Junior Member Find all posts View Profile Close kalyl]

The use of Clenbuterol and other substances for weight loss among us online or performance enhancement purposes can have side effects and may not be suitable for everyone. These substances may affect the cardiovascular system, nervous system, and metabolism, and their use should be carefully monitored.