Cyproheptadine

Mechanism-of-action classes: Histamine H1 Receptor Antagonists; Monoamine Oxidase Inhibitors; Serotonin Antagonists.

• Perennial and seasonal allergic rhinitis, Vasomotor rhinitis, Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema.ICD-10: H10.9, J30.9

• Newborn or Premature Infants: This drug should not be used in newborn or premature infants. Nursing Mothers: Because of the higher risk of antihistamines for infants generally, and for newborns and prematures in particular, antihistamine therapy is contraindicated in nursing mothers.contraindicated

DOSAGE SHOULD BE INDIVIDUALIZED ACCORDING TO THE NEEDS AND THE RESPONSE OF THE PATIENT. Children: The total daily dosage for children may be calculated on the basis of body weight or body area using approximately 0.25 mg/kg/day (0.11 mg/lb/day) or 8 mg per square meter of body surface (8 mg/m 2 ). In small children for whom the calculation of the dosage based upon body size is important, it may be necessary to use cyproheptadine syrup to permit accurate dosage. Age 2 to 6 years: The usual dose is 2 mg (1/2 tablet) two or three times a day, adjusted as necessary to the size and response of the patient. The dose is not to exceed 12 mg a day. Age 7 to 14 years: The usual dose is 4 mg (1 tablet) two or three times a day, adjusted as necessary to the size and response of the patient. The dose is not to exceed 16 mg a day. Adults: The total daily dose for adults should not exceed 0.5 mg/kg/day (0.23 mg/lb/day). The therapeutic range is 4 to 20 mg a day, with the majority of patients requiring 12 to 16 mg, a day. An occasional patient may require as much as 32 mg a day for adequate relief. It is suggested that dosage be initiated with 4 mg (1 tablet) three times a day and adjusted according to the size and response of the patient.

Children - Overdosage of antihistamines, particularly in infants and children, may produce hallucinations, central nervous system depression, convulsions, and death. Antihistamines may diminish mental alertness conversely particularly in the young child they may occasionally produce excitation. CNS Depressants - Antihistamines may have additive effects with alcohol and other CNS depressants, e.g., hypnotics, sedatives, tranquilizers, antianxiety agents. Activities Requiring Mental Alertness - Patients should be warned about engaging in activities requiring mental alertness and motor coordination, such as driving a car or operating machinery. Antihistamines are more likely to cause dizziness, sedation and hypotension in elderly patients.

Adverse reactions which have been reported with the use of antihistamines are as follows: Central Nervous System: Sedation and sleepiness (often transient), dizziness, disturbed coordination, confusion, restlessness, excitation, nervousness, tremor, irritability, insomnia, paresthesias, neuritis, convulsions, euphoria, hallucinations, hysteria, faintness. Integumentary: Allergic manifestation of rash and edema, excessive perspiration, urticaria, photosensitivity. Special Senses: Acute labyrinthitis, blurred vision, diplopia, vertigo, tinnitus. Cardiovascular: Hypotension, palpitation, tachycardia, extrasystoles, anaphylactic shock. Hematologic: Hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia. Digestive System: Dryness of mouth, epigastric distress, anorexia, nausea, vomiting, diarrhea, constipation, jaundice. Genitourinary: Urinary frequency, difficult urination, urinary retention, early menses. Respiratory: Dryness of nose and throat, thickening of bronchial secretions, tightness of chest and wheezing, nasal stuffiness. Miscellaneous: Fatigue, chills, headache, increased appetite/weight gain.

PREGNANCY Pregnancy Category B: Reproduction studies have been performed in rabbits, mice, and rats at oral or subcutaneous doses up to 32 times the maximum recommended human oral dose and have revealed no evidence of impaired fertility or harm to the fetus due to cyproheptadine. Cyproheptadine has been shown to be fetotoxic in rats when given by intraperitoneal injection in doses four times the maximum recommended human oral dose. Two studies in pregnant women, however, have not shown that cyproheptadine increases the risk of abnormalities when administered during the first, second and third trimesters of pregnancy. No teratogenic effects were observed in any of the newborns. Nevertheless, because the studies in humans cannot rule out the possibility of harm, cyproheptadine should be used during pregnancy only if clearly needed. Nursing Mothers: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, and because of the potential for serious adverse reactions in nursing infants from cyproheptadine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother (see CONTRAINDICATIONS ). Pediatric Use: Safety and effectiveness in children below the age of two years have not been established.

Antihistamine overdosage reactions may vary from central nervous system depression to stimulation, especially in children. Also, atropine-like signs and symptoms (dry mouth; fixed, dilated pupils; flushing, etc.) as well as gastrointestinal symptoms may occur. If vomiting has not occurred spontaneously, the patient should be induced to vomit with syrup of ipecac. If 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. The oral LD 50 of cyproheptadine is 123 mg/kg, and 295 mg/kg in the mouse and rat, respectively.

• May 26, 1983ANDAANDA088212Chartwell Rx
• Sep 30, 2003ANDAANDA040537Mountain
• Jun 28, 2006ANDAANDA040668Rising
• Sep 23, 2015ANDAANDA205087Ingenus Pharms Llc
• Nov 29, 2016ANDAANDA206553Appco
• Jan 31, 2017ANDAANDA207555Rising
• May 19, 2017ANDAANDA208938Zydus Pharms
• Jul 13, 2017ANDAANDA203191Chartwell Molecular

1. 1Off Label Use3237.5%
2. 2Drug Ineffective2926.8%
3. 3Diarrhoea2425.6%
4. 4Vomiting2325.4%
5. 5Nausea2295.3%
6. 6Fatigue2255.2%
7. 7Pneumonia2014.7%
8. 8Headache1934.5%
9. 9Anxiety1884.4%
10. 10Serotonin Syndrome1844.3%
11. 11Weight Decreased1724.0%
12. 12Decreased Appetite1683.9%
13. 13Pyrexia1583.7%
14. 14Pain1503.5%
15. 15Abdominal Pain1483.4%

Recent PubMed references pinned to Cyproheptadine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Spectral residual augmented classical least squares for simultaneous green determination of cetirizine, fexofenadine and loratadine by UV spectrophotometry in pharmaceuticals and environmental samples.
  Scientific reports · 2026 · Alqahtani A, Alqahtani T, Alshehri A, et al.
  PMID 42236886DOI 10.1038/s41598-026-56246-6
• Synthesis of desloratadine analogues as potent antifungal agents: in vitro and in vivo efficacy, and structure-activity relationship studies.
  Bioorganic chemistry · 2026 · Wali S, Ghazal F, Atia-Tul-Wahab, et al.
  PMID 42013599DOI 10.1016/j.bioorg.2026.109848
• A Cu-based metal-organic framework based on desloratadine and siHIF-1α for achievement of genes/drugs/CDT combination therapy in hepatocellular carcinoma.
  Journal of nanobiotechnology · 2026 · Ding D, Huang Z, Wang L, et al.
  PMID 42010649DOI 10.1186/s12951-026-04334-0
• Orodispersible tablets as delivery platform for oral administration of drug-loaded nanoparticles to paediatric patients.
  European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2026 · Cornilă A, Iurian S, Tefas LR, et al.
  PMID 41866000DOI 10.1016/j.ejpb.2026.115061
• Combinatorial Anti-Mitotic Activity of Loratadine/5-Fluorouracil Loaded Zein Tannic Acid Nanoparticles in Breast Cancer Therapy: In silico, in vitro and Cell Studies.
  International journal of nanomedicine · 2026 · Hamdi M, Al-Tabakha MM, Ali IH, et al.
  PMID 41858579DOI 10.2147/IJN.S564050
• 'Oral isotretinoin plus desloratadine for acne vulgaris: an updated global meta-analysis of efficacy, safety, and patient-centered outcomes'.
  The Journal of dermatological treatment · 2026 · Alrubaiaan MT, Bajamaan R, Altuwaijri AM, et al.
  PMID 41840862DOI 10.1080/09546634.2026.2644003
• Investigation of the impacts of second-generation antihistamines on free-living marine nematodes and their interaction with ZnS nanoparticles: Mechanistic insights from community and population approaches and molecular interactions modeling.
  Marine environmental research · 2026 · Ghannem S, Labiadh H, Ishak S, et al.
  PMID 41797016DOI 10.1016/j.marenvres.2026.107969
• Repurposing loratadine to reverse colistin resistance in Klebsiella pneumoniae through targeting lipid A modification.
  Emerging microbes & infections · 2026 · Wu X, Ge Z, Zhan H, et al.
  PMID 41678146DOI 10.1080/22221751.2026.2623697

The 10 most recently updated of 102 ClinicalTrials.gov registrations naming Cyproheptadine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• The Use of Cyproheptadine in Pediatric Feeding Disorders
  Completed · Phase 4 · Interventional · 18 enrolled · University of Miami
  NCT06751290updated 2026-06-04
• Loratadine for the Reduction of G-CSF Induced Bone Pain in Patients With Multiple Myeloma Undergoing Stem Cell Mobilization
  Recruiting · Early phase 1 · Interventional · 70 enrolled · Rutgers, The State University of New Jersey
  NCT04211259updated 2026-05-29
• Rivastigmine as an Antidote for Clozapine and Other Anticholinergic-Induced CNS Depression and Delirium: A Study of 100 Cases
  Completed · Phase 4 · Interventional · 100 enrolled · Alexandria University
  NCT07545382updated 2026-05-19
• Efficacy of Auricular Acupressure Combined With Antihistamines in Patients With Wind-Heat Type Urticaria.
  Not yet recruiting · Interventional · 66 enrolled · University of Medicine and Pharmacy at Ho Chi Minh City
  NCT07575464updated 2026-05-08
• Noninvasive Markers of Functional Nausea in Children
  Completed · Early phase 1 · Interventional · 42 enrolled · Vanderbilt University Medical Center
  NCT03593811updated 2026-04-22
• Comparison of Antihistamine and Antileukotriene Add-On Therapy to Intranasal Corticosteroid in Allergic Rhinitis
  Not yet recruiting · Phase 4 · Interventional · 32 enrolled · Liaquat National Hospital & Medical College
  NCT07532993updated 2026-04-16
• Altering Activation Patterns Post-stroke
  Completed · Interventional · 96 enrolled · Shirley Ryan AbilityLab
  NCT02418949updated 2026-03-31
• I-SPY COVID-19 TRIAL: An Adaptive Platform Trial for Critically Ill Patients
  Active not recruiting · Phase 2 · Interventional · 1,500 enrolled · QuantumLeap Healthcare Collaborative
  NCT04488081updated 2026-03-16
• Evaluating Premedication Regimens (Methylprednisolone vs Dexamethasone-based) for the Prevention of Systemic and Injection Site Reactions to Motixafortide in Patients With Multiple Myeloma Undergoing Stem Cell Mobilization, PARADE Trial
  Recruiting · Phase 4 · Interventional · 94 enrolled · Emory University
  NCT07101445updated 2026-02-10
• Loratadine for the Prevention of G-CSF-related Bone Pain
  Recruiting · Phase 2 · Interventional · 78 enrolled · AHS Cancer Control Alberta
  NCT05421416updated 2026-02-05

Frequently asked questions

How does Cyproheptadine work?

Mechanism-of-action classes: Histamine H1 Receptor Antagonists; Monoamine Oxidase Inhibitors; Serotonin Antagonists.

What is Cyproheptadine used for?

According to FDA labeling, Cyproheptadine carries indications including: Perennial and seasonal allergic rhinitis, Vasomotor rhinitis, Allergic conjunctivitis due to inhalant allergens and foods. Mild, uncomplicated allergic skin manifestations of urticaria and angioedema.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Cyproheptadine?

Cyproheptadine is classified as Other antihistamines for systemic use, Histamine H1 Receptor Antagonists, Monoamine Oxidase Inhibitors, Serotonin Antagonists, Decreased Histamine Activity, Decreased Serotonin Activity.

What are the contraindications for Cyproheptadine?

Cyproheptadine labeling lists contraindications including: Newborn or Premature Infants: This drug should not be used in newborn or premature infants. Nursing Mothers: Because of the higher risk of antihistamines for infants generally, and for newborns and prematures in particular, antihistamine therapy is contraindicated in nursing mothers.. Always consult the full prescribing information and a clinician.