View Full Version : Zaditen®~ketotifen fumarate

12-23-2010, 08:26 PM
Zaditen® (ketotifen fumarate)


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.


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.


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.

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

12-23-2010, 08:27 PM

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 you´ve 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 don´t 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 didn´t 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 it´s 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.

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.