Cyproheptadine Hydrochloride/Periactin Profile
Pharmaceutical Name: Cyproheptadine Hydrochloride
Drug Classification: Piperidine Antihistamine
Active Life: 16-24 hours
Cyproheptadine hydrochloride is an antihistamine most often medically prescribed for symptoms of hay fever and other allergies that may include such things as hives, nasal inflammation, and irritated eyes among others. However one of its less frequently utilized medical uses can be beneficial for bodybuilders and strength athletes. This is namely its ability to stimulate the appetite of users. For those athletes, and others, that want to or need to put out body weight but have difficulty ingesting enough calories to do so cyproheptadine hydrochloride could be beneficial.
Cyproheptadine affects the appetite of a user via its antierotonergic effect on 5-HT2 receptors in the brain (1). These receptors are responsible for numerous mechanisms in various tissues of the body but it is believed that it is the mechanism that causes these receptors to interact with serotonin (2), dopamine and possibly leptin (1) that is responsible for the ability of this drug to dramatically increase the appetite of some users. Medically it is prescribed to some that are considered underweight but its effects as an appetite stimulant appear not to be limited to those that suffer from a disease or abnormal hormone levels. For example cyproheptadine hydrochloride has been prescribed to patients suffering from such ailments as various forms of cancer (3), anorexia (4), cystic fibrosis (5, 6) and others. Seemingly the drug used the same mechanism to stimulate appetite in patients with these various diseases with no need for a special mechanism to exist as it relates to a disease and therefore cyproheptadine hydrochloride should elicit the same effects on healthy individuals as well.
Unlike other antihistamines, such as ketotifen, the benefits of cyproheptadine hydrochloride for bodybuilders and strength athletes are basically limited to those looking for something to stimulate their appetite. There is some indication that the drug may help assist those who suffer from exercise induced breathing difficulty (7) but this assists primarily only those that already have pre-existing conditions. However for the sole purpose of inducing weight gain via appetite stimulation cyproheptadine hydrochloride is well suited.
The duration with which a user can administer cyproheptadine hydrochloride is relatively limitless due to the lack of toxicity related to the drug, as discussed below in greater detail in the Risks/Side Effects section of this profile. The primary limiting factor however is that the user will begin to build a tolerance to the drug and will need to increase his or her dosages to continue achieving the same intensity of effect if they so desire. This will likely limit the amount of time that one will want to continuously administer the drug. As well, in practical terms, a user will also be limited by the time that he or she will actually want to stimulate their appetite artificially in an attempt to induce large gains in body weight. So for most purposes the practical concerns will usually invoke a discontinuation of the drug prior to any medical/physiological reasons to do so would arise.
The version of the drug that will be available to most users is the oral; however an intravenous version is produced. Most users will have no reason to pursue the use of the intravenous version of the drug due to it seemingly having no greater effect. In at least one study there was no difference in the efficacy of cyproheptadine hydrochloride in producing gains in both overall body mass as well as lean mass whether the drug was administered orally or intravenously (6). Of course using the intravenous version would result in a much larger percentage of the drug becoming active in the system of the user then when administered orally but this greater percentage is not enough to make a significant difference in the results achieved.
As for dosages regularly used, commonly users administer orally doses in the range of between four to twenty milligrams per day. Often one will want to gage their tolerance for the drug with lower doses prior to increasing them. However once one has begun administering the drug for a period of time they may be inclined to increase their dosage of the drug as they begin to tolerate the lower doses. As well, some users will and have experimented with doses exceeding twenty milligrams per day. This is a rather low-risk venture due to the lack of serious side effects associated with cyproheptadine hydrochloride but should not be necessary for the majority of users, assuming any present negative side effects are tolerated by the user.
Due to the active life of the drug a single dose per day would be all that would be required to reap the benefits of the drug, however many users will want to spread their dosage of the drug throughout the day to not only avoid a spike in hunger that slowly dissipates but also so that the side effects do not become too severe. This may be counterproductive for some however who become extremely drowsy while using cyproheptadine hydrochloride. For this reason some users may choose to administer their entire dosage prior to going to sleep. This way the drug will not inhibit their energy levels as much during their waking hours.
As indicated earlier, the most prevalent and often reported side effect with use of cyproheptadine hydrochloride is drowsiness and lethargy. This is a common occurrence with many antihistamines. There are little countermeasures that users can take to combat this effect, with some users being affected more severely then others. Timing of the administration of the drug can help with this side effect but will not negate it of course.
While some antihistamines, primarily those of later drug generations and non-sedative, have been shown to sometimes cause various forms of toxicity including cardio-toxicity (8), there is no indication that any toxicity issues will arise with the normal use of cyproheptadine hydrochloride. No specific precautions need to be taken to prevent such occurrences with this drug.
Other sporadically reported side effects associated with cyproheptadine hydrochloride include an early onset of menstrual cycles in females, constipation, dry mouth, stomach upset, excessive sweating, blurred vision, low blood pressure and a sensitivity to light among others. However these listed side effects are relatively uncommon for most users and will only afflict an extremely small percentage of users.
1. Calka O, Metin A, Dulger H, Erkoc R. Effect of cyproheptadine on serum leptin levels. Adv Ther. 2005 Sep-Oct;22(5):424-8.
2. Kang YM, Chen JY, Ouyang W, Qiao JT, Reyes-Vazquez C, Dafny N. Serotonin modulates hypothalamic neuronal activity. Int J Neurosci. 2004 Mar;114(3):299-319.
3. Mattox TW. Treatment of unintentional weight loss in patients with cancer. Nutr Clin Pract. 2005 Aug;20(4):400-10.
4. Powers PS, Santana C. Available pharmacological treatments for anorexia nervosa. Expert Opin Pharmacother. 2004 Nov;5(11):2287-92.
5. Homnick DN, Marks JH, Hare KL, Bonnema SK. Long-term trial of cyproheptadine as an appetite stimulant in cystic fibrosis. Pediatr Pulmonol. 2005 Sep;40(3):251-6.
6. Homnick DN, Homnick BD, Reeves AJ, Marks JH, Pimentel RS, Bonnema SK. Cyproheptadine is an effective appetite stimulant in cystic fibrosis. Pediatr Pulmonol. 2004 Aug;38(2):129-34.
7. Hallstrand TS, Moody MW, Wurfel MM, Schwartz LB, Henderson WR Jr, Aitken ML. Inflammatory basis of exercise-induced bronchoconstriction. Am J Respir Crit Care Med. 2005 Sep 15;172(6):679-86.
8. Paakkari I. Cardiotoxicity of new antihistamines and cisapride. Toxicol Lett. 2002 Feb 28;127(1-3):279-84.