Zaditen® (ketotifen fumarate) profile and use in sports

akn · Aug 29, 2014

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oNotOptimizeForBrowser/> <m:mathPr> <m:mathFont m:val="Cambria Math"/> <m:brkBin m:val="before"/> <m:brkBinSub m:val="--"/> <m:smallFrac m:val="off"/> <m:dispDef/> <m:lMargin m:val="0"/> <m:rMargin m:val="0"/> <m:defJc m:val="centerGroup"/> <m:wrapIndent m:val="1440"/> <m:intLim m:val="subSup"/> <m:naryLim m:val="undOvr"/> </m:mathPr></w:WordDocument> </xml><![endif]--> [FONT=&quot]Description:[/FONT]
[FONT=&quot]Ketotifen is an antihistamine drug that is used for the[/FONT]
[FONT=&quot]treatment of general allergy symptoms, certain allergic[/FONT]
[FONT=&quot]conditions (including conjunctivitis), and the management of[/FONT]
[FONT=&quot]asthma. When used for asthma, the drug is not regarded as[/FONT]
[FONT=&quot]effective for treating an immediate attack (it is not a rapid[/FONT]
[FONT=&quot]bronchodilator). Instead, over time its use is associated with[/FONT]
[FONT=&quot]a reduction in the frequency, duration, and severity of attacks.[/FONT]
[FONT=&quot]It is usually prescribed as a way to increase the efficacy of[/FONT]
[FONT=&quot]other asthma medications. Likewise, ketotifen fumarate will[/FONT]
[FONT=&quot]usually supplement an existing asthma medication program,[/FONT]
[FONT=&quot]and not replace the prescribing of immediate rescue devices[/FONT]
[FONT=&quot]such as an asthma inhaler or nebuliser.[/FONT]
[FONT=&quot]Ketotifen fumarate alleviates allergy symptoms by blocking[/FONT]
[FONT=&quot]histamine H1 receptors, a property that is common to drugs[/FONT]
[FONT=&quot]of the antihistamine class. Its second and very unique mode[/FONT]
[FONT=&quot]of action, however, makes it useful in the treatment asthma.[/FONT]
[FONT=&quot]Ketotifen fumarate increases the concentration of betaadrenergic[/FONT]
[FONT=&quot]receptors in the body (especially beta-2[/FONT]
[FONT=&quot]receptors). Drugs that stimulate beta-2 receptors are[/FONT]
[FONT=&quot]commonly prescribed as bronchodilators, used to increase[/FONT]
[FONT=&quot]airflow to the lungs and counter the constriction caused by[/FONT]
[FONT=&quot]asthma. While potentially efficacious alone, one key[/FONT]
[FONT=&quot]therapeutic effect of ketotifen fumarate is to increase the[/FONT]
[FONT=&quot]sensitivity of the body to drugs of the beta agonist class.[/FONT]
[FONT=&quot]The beta-2 receptor upregulating properties of ketotifen[/FONT]
[FONT=&quot]fumarate make this drug of interest to the bodybuilding and[/FONT]
[FONT=&quot]athletic communities. This is due to the strong role of the[/FONT]
[FONT=&quot]beta-2 receptor in supporting fat loss. Although not a strong[/FONT]
[FONT=&quot]fat loss compound by itself, when taken with a beta-2 agonist[/FONT]
[FONT=&quot]thermogenic like clenbuterol, ketotifen fumarate may increase[/FONT]
[FONT=&quot]thermogenic potency and noticeably extend the window of[/FONT]
[FONT=&quot]active lipolysis. Clenbuterol and other beta-2 agonists[/FONT]
[FONT=&quot]normally have a limited duration of usefulness here because[/FONT]
[FONT=&quot]beta-2-adrenergic receptors decrease in number with regular[/FONT]
[FONT=&quot]stimulation. Within several weeks of initiating therapy with[/FONT]
[FONT=&quot]such a drug, it usually begins to diminish in effectiveness.[/FONT]
[FONT=&quot]Ketotifen may extend this time period considerably.[/FONT]
[FONT=&quot]The ability of ketotifen to potentiate the effects of beta-2[/FONT]
[FONT=&quot]agonist drugs has been demonstrated in a number of clinical[/FONT]
[FONT=&quot]studies. For example, one study published in 1990[/FONT]
[FONT=&quot]demonstrated that when ketotifen and clenbuterol were taken[/FONT]
[FONT=&quot]together, there was a significant increase in betaa-drenergic[/FONT]
[FONT=&quot]receptor density compared to the use of clenbuterol alone,[/FONT]
[FONT=&quot]which again decreases beta adrenoceptor density fairly[/FONT]
[FONT=&quot]quickly.692 Other studies with salbutamol (also referred to[/FONT]
[FONT=&quot]generically as albuterol) showed that beta adrenoceptor[/FONT]
[FONT=&quot]down regulation caused by long-term use of this betaadrenergic[/FONT]
[FONT=&quot]agent could be rapidly reversed with as little as[/FONT]
[FONT=&quot]2mg of ketotifen fumarate per day.693[/FONT]
[FONT=&quot]History:[/FONT]
[FONT=&quot]Ketotifen was globalized as a prescription medication by[/FONT]
[FONT=&quot]Novartis. It is presently prescribed for allergies, allergic[/FONT]
[FONT=&quot]conditions, and (most commonly) the management of asthma[/FONT]
[FONT=&quot]in more than three-dozen countries around the world. The[/FONT]
[FONT=&quot]most widely available brand name is Novartis’ Zaditen,[/FONT]
[FONT=&quot]which is sold throughout most parts of Europe and Asia. In[/FONT]
[FONT=&quot]addition to generic forms of the medication, dozens of other[/FONT]
[FONT=&quot]brand names can be found in many different markets as well.[/FONT]
[FONT=&quot]Ketotifen fumarate is approved for sale in the United States,[/FONT]
[FONT=&quot]but currently only as an ophthalmic anti-allergy solution[/FONT]
[FONT=&quot](Zaditor), not an oral allergy/asthma medication. The dosage[/FONT]
[FONT=&quot]of ketotifen fumarate in this product is also too low for it to[/FONT]
[FONT=&quot]be considered useful for any other (off label) purpose. Given[/FONT]
[FONT=&quot]the ready availability of ketotifen fumarate in other countries,[/FONT]
[FONT=&quot]the drug is easily diverted for black market sale. As of now,[/FONT]
[FONT=&quot]it is not extremely popular with bodybuilders and athletes.[/FONT]
[FONT=&quot]The UK guidelines on the clinical management of asthma[/FONT]
[FONT=&quot]consider ketotifen to be ineffective for the management of[/FONT]
[FONT=&quot]this disease. There is admittedly conflicting data on the[/FONT]
[FONT=&quot]potential usefulness of ketotifen fumarate for this purpose,[/FONT]
[FONT=&quot]with some studies reporting positive results and others[/FONT]
[FONT=&quot]showing an insignificant effect. A thorough review of the[/FONT]
[FONT=&quot]data published on the Cochrane Database of systematic[/FONT]
[FONT=&quot]Reviews in 2004 concluded that it appeared to have some[/FONT]
[FONT=&quot]usefulness in controlling asthma and wheezing in many[/FONT]
[FONT=&quot]children, but the variability of the disease and response to the[/FONT]
[FONT=&quot]drug meant that these positive results could not be[/FONT]
[FONT=&quot]generalized for all asthma patients.694[/FONT]
[FONT=&quot]How Supplied:[/FONT]
[FONT=&quot]Ketotifen fumarate is most commonly supplied in tablets of[/FONT]
[FONT=&quot]1mg. This dosage is usually expressed in terms of the base,[/FONT]
[FONT=&quot]so each tablet actually contains 1.38mg of ketotifen fumarate.[/FONT]
[FONT=&quot]Structural Characteristics:[/FONT]
[FONT=&quot]Ketotifen fumarate is selective histamine H1 antagonist, antiallergic,[/FONT]
[FONT=&quot]and anti-asthmatic agent. It has the chemical[/FONT]
[FONT=&quot]designation 4-(1-Methyl-4-piperidylidene-4Hbenzo[/FONT]
[FONT=&quot][4,5]cyclohepta[1,2-b]thiphene-1-(9H)-one fumarate.[/FONT]
[FONT=&quot]Side Effects:[/FONT]
[FONT=&quot]Common side effects include dry mouth, appetite stimulation,[/FONT]
[FONT=&quot]weight gain, dizziness, CNS stimulation, and drowsiness.[/FONT]
[FONT=&quot]These side effects are all commonly associated with strong[/FONT]
[FONT=&quot]antihistamine compounds. In rare cases severe allergic[/FONT]
[FONT=&quot]reaction on the skin or a urinary bladder inflammation called[/FONT]
[FONT=&quot]cystitis may occur.[/FONT]
[FONT=&quot]Administration:[/FONT]
[FONT=&quot]When used to reduce the frequency, duration, and severity of[/FONT]
[FONT=&quot]asthma attacks, ketotifen fumarate is usually initiated at a[/FONT]
[FONT=&quot]dosage of 1mg twice per day (2mg total). If necessary, this[/FONT]
[FONT=&quot]may be increased to a maximum dosage of 2mg twice per day[/FONT]
[FONT=&quot](4mg total). Bodybuilders and athletes will commonly use a[/FONT]
[FONT=&quot]dosage of 1mg twice per day (2mg total) for the (off-label)[/FONT]
[FONT=&quot]use of preventing receptor down regulation with clenbuterol[/FONT]
[FONT=&quot]or other beta-agonists. This may allow an individual to[/FONT]
[FONT=&quot]obtain a strong thermogenic effect from, and run longer[/FONT]
[FONT=&quot]cycles with, beta-2 agonist drugs. Note that given its ability[/FONT]
[FONT=&quot]to increase drug sensitivity,the dosage of beta-2 agonist[/FONT]
[FONT=&quot]medications may need to be reduced upon ketotifen fumarate[/FONT]
[FONT=&quot]administration.[/FONT]
[FONT=&quot]Availability:[/FONT]
[FONT=&quot]Ketotifen fumarate is widely available, and is sold under[/FONT]
[FONT=&quot]numerous brand names in many countries. Large scale[/FONT]
[FONT=&quot]counterfeiting of this medication is currently not known to be[/FONT]
[FONT=&quot]a problem.[/FONT]

Presser · Aug 20, 2016

has anyone here used this Ketotifen ? and if so how did you like it? The CNS stimulation sounds great

Dean Destructo · Aug 20, 2016

Interesting.

Zaditen® (ketotifen fumarate) profile and use in sports

akn

Musclechemistry Member

Presser

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Dean Destructo

New member

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