Ketotifen Fumarate 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 is Ketotifen Fumarate 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 of Ketotifen Fumarate
Ketotifen fumarate is selective histamine H1 antagonist, anti-allergic, and anti-asthmatic agent. It has the chemical designation 4-(1-Methyl-4-piperidylidene-4Hbenzo [4,5]cyclohepta[1,2-b]thiphene-1-(9H)-one fumarate.
Ketotifen Fumarate Side Effects
Common side effects include dry mouth, appetite stimulation, weight gain, dizziness, CNS 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.
Ketotifen Fumarate 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, beta-2 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.
Ketotifen Fumarate Availability
Ketotifen fumarate is widely available, and is sold under numerous brand names in many countries. Large scale counterfeiting of this medication is currently not known to be a problem.
Wlliam Llewellyn (2011) - Anabolics