2832 Cyproheptadine Cyproheptadine is only found in individuals that have used or taken this drug. It is a serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc. Cyproheptadine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite. 129-03-3 2913 C21H21N 287.167400 White powder. 112.3-113.3°C Soluble Well absorbed after oral administration. Cyproheptadine competes with free histamine for binding at HA-receptor sites. This antagonizes the effects of histamine on HA-receptors, leading to a reduction of the negative symptoms brought on by histamine HA-receptor binding. Cyproheptadine also competes with serotonin at receptor sites in smooth muscle in the intestines and other locations. Antagonism of serotonin on the appetite center of the hypothalamus may account for Cyproheptadine's ability to stimulate appetite. Hepatic (cytochrome P-450 system) and some renal. Route of Elimination: After a single 4 mg oral dose of14C-labelled cyproheptadine HCl in normal subjects, given as tablets 2% to 20% of the radioactivity was excreted in the stools. At least 40% of the administered radioactivity was excreted in the urine. No indication of carcinogenicity to humans (not listed by IARC). Used as an antihistaminic/anticholinergic and antiserotonergic agent. For treatment of perennial and seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis due to inhalant allergens and foods, mild uncomplicated allergic skin manifestations of urticaria and angioedema, amelioration of allergic reactions to blood or plasma, cold urticaria, dermatographism, and as therapy for anaphylactic reactions adjunctive to epinephrine. Drowsiness, epigastric distress (dysphagia), nausea, vomiting, (it is noted that these side effects are much more common in people with neuromuscular disorders). [Wikipedia] If vomiting has not occurred spontaneously the patient should be induced to vomit with syrup of ipecac. If the patient is unable to vomit, perform gastric lavage followed by activated charcoal. Isotonic or 1/2 isotonic saline is the lavage of choice. Precautions against aspiration must be taken especially in infants and children. When life threatening CNS signs and symptoms are present, intravenous physostigmine salicylate may be considered. Dosage and frequency of administration are dependent on age, clinical response, and recurrence after response. (See package circulars for physostigmine products.) Saline cathartics, as milk of magnesia, by osmosis draw water into the bowel and, therefore, are valuable for their action in rapid dilution of bowel content. Stimulants should not be used. Vasopressors may be used to treat hypotension. (L1712) 2009-07-21T20:26:53Z 2014-12-24T20:25:51Z Cyproheptadine C06935 4046 Cyproheptadine DB00434 true CN1CCC(CC1)=C1C2=CC=CC=C2C=CC2=CC=CC=C12 C21H21N InChI=1S/C21H21N/c1-22-14-12-18(13-15-22)21-19-8-4-2-6-16(19)10-11-17-7-3-5-9-20(17)21/h2-11H,12-15H2,1H3 InChIKey=JJCFRYNCJDLXIK-UHFFFAOYSA-N 287.3981 287.167399677 Exogenous Solid 4.69 HMDB14578 CHEMBL516 2810 <p>Engelhardt, E.L.; U S . Patent 3,014,911; December 26, 1961; assigned to Merck &amp; Co., Inc.</p>