Cyproheptadine hydrochloride is a first-generation prescription histamine and serotonin antagonist. This drug is most often given in the U.S. for the treatment of allergy-related symptoms, including hay fever, runny nose, irritated eyes, hives, and swelling. It is also FDA approved for the treatment of anaphylactic reactions caused by allergens, often as an adjunct to injectable epinephrine (adrenalin). The serotonin inhibiting effect of this drug also gives it a unique ability to increase appetite. This has led to a considerable amount of off-label use as a weight-gain medication, particularly with patients who are suffering from a lean tissue wasting associated with AIDS infection, cancer, or other debilitating diseases. Cyproheptadine hydrochloride is also used on occasion as an adjunct to growth hormone therapy in children, to foster greater nutrient uptake and increases in linear growth beyond what is normally achieved with rHGH alone. Bodybuilders and athletes use the drug on occasion to help increase caloric intake, usually during periods of bulking training where increased mass is desired, and often used in conjunction with anabolic/androgenic steroids. Although this is a controversial use of the drug, references to the appetite stimulating properties of cyproheptadine hydrochloride are abundant in the medical literature. One of the more detailed papers compares the appetite increasing effects of cyproheptadine hydrochloride to megestrol acetate668 in a group of 14 men with weight loss associated with HIV infection. The other agent, megestrol, is a progestin that was approved by the FDA in 1993 for the treatment of anorexia, cachexia, or weight loss in patients with AIDS. In this investigation, cyproheptadine hydrochloride was shown to have a similar level of benefit to FDA approved agent megestrol, with patients consuming about 500 extra calories per day, and gaining a moderate amount of weight with either medications. While the benefits were similar, the side effects were not. The investigators reported that more than 50% of the patients taking megestrol suffered impotence during the investigation, while the cyproheptadine hydrochloride group had no such side effects. Cyproheptadine hydrochloride may offer an effective alternative to megestrol therapy for many patients, especially those prone to negative side effects associated with this type of hormone manipulation.
|Brand name||Periactin, Cyproheptadine hydrochloride|
Cyproheptadine Hydrochloride History
Cyproheptadine hydrochloride is an early anti-histamine drug, and has been sold as a prescription medication in most developed nations for decades. It was introduced to the U.S. in 1961 under the Periactin brand name by Merck & Co. This brand of cyproheptadine hydrochloride was sold for many years in the U.S, but was voluntarily discontinued by Merck in 2003 (in both the U.S. and Canada). While Merck & Co. has withdrawn Periactin from a number of other nations (likely due to low financial interest), the brand is still sold in more than one dozen countries including Australia, Austria, Belgium, Ireland, Italy, Netherlands, New Zealand, South Africa, Spain, Sweden, Thailand, and the United Kingdom. It is also sold under dozens of other brand names around the world, in both singleand multi-ingredient preparations. A number of generic products are still sold in both the U.S. and Canada as well. Subsequent to studies questioning the long-term weight gaining value of cyproheptadine hydrochloride therapy, in 1994 the World Health Organization warned against using the drug for this purpose. Regardless of this report, many still support the value of cyproheptadine hydrochloride as a short-term appetite stimulant.
How is Cyproheptadine Hydrochloride Supplied
Cyproheptadine hydrochloride is most commonly supplied in tablets of 4 mg.
Structural Characteristics of Cyproheptadine Hydrochloride
Cyproheptadine hydrochloride is antihistaminic and antiserotonergic agent with the chemical designation 4- ( 5H - dibenzo [a,d] cyclohepten - 5 - ylidene) - 1 - methylpiperidine hydrochloride sesquihydrate.
Cyproheptadine Hydrochloride Side Effects
As a first-generation anti-histamine, cyproheptadine hydrochloride may be prone to producing a number of side effects in its users. The most common of which is sedation or the classic “anti-histamine lethargy”, which is common to these types of drugs. For some users, the tiredness that cyproheptadine hydrochloride will produce will outweigh any potential as a weightgaining/performance-enhancing agent. For most, this side effect of cyproheptadine hydrochloride is not very noticeable, and perhaps a nuisance (not strong enough to an ingredient. necessitate discontinuation) at best. Other less common side effects of concern include, but are not limited to, dizziness, disturbed coordination, muscular weakness, nausea, vomiting, diarrhea, constipation, dryness of the mouth, difficulty urinating, vertigo, blurred vision, tightness of the chest, wheezing, stuffed nose, sweating, early period, headaches, and faintness. Any strong incidence of unwelcome side effects would immediately warrant discontinuing the drug, or even seeking immediate medical attention if severe.
Cyproheptadine Hydrochloride Administration
The dosage required for medical purposes may vary depending on the individual and their particular needs. The established therapeutic range for cyproheptadine hydrochloride is 4 mg to 20 mg per day, with most adults requiring 12 mg to 16 mg daily. The total daily dosage is usually divided into three separate applications. When used (off-label) as an appetite stimulant, a dosage of 4mg is commonly taken 2-3 times per day (8-12 mg). Above this level, side effects may become more noticeable (most notably sleepiness), often interfering with the benefit of the drug.
This may be used during a steroid cycle focused on bulking, with the intake of cyproheptadine hydrochloride usually lasting no more than 4-8 weeks. For those who tolerate this anti-histamine’s side effects (mainly tiredness), cyproheptadine hydrochloride is often reported to offer significant value as an appetite stimulant during weight gaining cycles. This is especially so in individuals that have trouble eating enough food to meet the high calorie/protein requirements for optimal muscle growth.
Cyproheptadine Hydrochloride Availability
Cyproheptadine hydrochloride is produced in a wide number of countries. Although it is not commonly traded on the black market, high supply and the relatively benign nature of this drug (loose controls) make it easily diverted for sale when needed. Given its low demand, counterfeiting of cyproheptadine hydrochloride preparations is not common.
It is interesting to also note that the Dominican steroid product, Anabolex, actually includes 1.5 mg of cyproheptadine hydrochloride in each 3 mg methandrostenolone tablet, which was added by its developers to facilitate increased caloric intake and weight gain during anabolic therapy. The 2:1 ratio provided is optimal for a daily dose of 24 mg Dianabol (a very common amount), as it would provide 12 mg of cyproheptadine hydrochloride (the maximum common daily dose). This is the only common anabolic steroid product that includes cyproheptadine hydrochloride as an ingredient.
Wlliam Llewellyn (2011) - Anabolics