Skip to content
← Drug library
Drug reference

Cyproheptadine

Sedating H1 antihistamine · Oral tablets and syrup

A prescription oral histamine/serotonin antagonist for selected allergic conditions. This profile follows current 4 mg tablets and 2 mg/5 mL syrup labels, including anticholinergic restrictions, child dose limits and lactation contraindication. Appetite stimulation and serotonin-syndrome treatment are not labeled indications here.

Therapeutic class
Sedating H1 / serotonin antagonist
Selected strengths
4 mg tablet; 2 mg/5 mL syrup
Major cautions
Sedation, anticholinergic effects and pediatric overdose
Essential safety

Sedation and anticholinergic toxicity can be severe.

Avoid alcohol and other CNS depressants; impairment or paradoxical excitation can occur. Newborn/premature infants and nursing mothers are contraindicated under selected labeling. Suspected overdose, seizures, severe confusion or respiratory compromise need immediate emergency/Poison Control assessment.

Warnings and precautions
01

Indications

Labeled relief of selected allergic conditions.

Approved label scope

Perennial/seasonal allergic rhinitis, vasomotor rhinitis, allergic conjunctivitis from inhalant/food allergens, mild uncomplicated urticaria/angioedema, blood/plasma allergic reactions, cold urticaria and dermatographism. Anaphylactic reactions: adjunct to epinephrine and standard measures only after acute manifestations are controlled. It is not initial rescue or a substitute for epinephrine.

Off-label boundary

Increased appetite/weight gain is reported as an adverse effect, not a labeled appetite-stimulation indication. No independent weight-gain, migraine or serotonin-syndrome dose algorithm supplied. Different clinical uses require diagnosis-specific professional review; do not use sedating medication to delay emergency care.

02

Dosage and administration

Individualize total daily dose and respect age limits.

Selected labeled regimens

PopulationOral dose and limit
Age 2–6 years2 mg two or three times daily; maximum 12 mg/day. Selected syrup:5 mL/dose; tablet:half 4 mg tablet.
Age 7–14 years4 mg two or three times daily; maximum 16 mg/day. Selected syrup:10 mL/dose.
Pediatric total-dose basisApproximately 0.25 mg/kg/day or 8 mg/m²/day described, with individualized response and age maximums. This is total daily dose, not per dose; do not stack formulas.
AdultsStart 4 mg three times daily; usual therapeutic range 4–20 mg/day, most 12–16 mg/day. Occasional 32 mg/day may be needed, but total must never exceed 0.5 mg/kg/day.
Age 15–17 gapSelected tables name child bands through 14 and Adults without explicitly assigning 15–17. Obtain exact prescriber dose review; no automatic adult regimen.
Below 2 / neonatalSafety/effectiveness below 2 unestablished; newborn/premature infant use contraindicated. No infant dose inferred.

Administration and adjustment limits

Use a calibrated oral device for syrup mL; household spoons are unsuitable. Tablet is scored, but confirm exact dispensed product for half-tablet dosing. Renal insufficiency reduces elimination, yet labels give no validated numeric renal/hepatic or dialysis adjustment; clinician individualization is required. No independent missed-dose doubling or off-label escalation.

03

Safety

Sedation, paradoxical excitation and anticholinergic effects.

Warnings and precautions

  • Sedation, impaired coordination and dizziness can affect driving/machinery. Young children may instead become excited; overdose can cause hallucinations, convulsions, respiratory/cardiac arrest or death.
  • Avoid alcohol and review hypnotics, sedatives, tranquilizers and other CNS depressants; effects may add. Selected syrup already contains 5% alcohol.
  • Atropine-like effects require caution with bronchial asthma history, raised intraocular pressure, hyperthyroidism, cardiovascular disease or hypertension.
  • Older adults are more susceptible to dizziness, sedation and hypotension. The contraindication list includes elderly, debilitated patients; a geriatric low-start paragraph does not override that restriction.
  • Reported severe reactions include allergy, blood-cell disorders, urinary retention and liver injury. New jaundice, severe rash, inability to urinate or major neurologic symptoms require assessment.

Contraindications

Newborn/premature infants; nursing mothers; hypersensitivity to cyproheptadine or structurally similar drugs; MAO-inhibitor therapy; angle-closure glaucoma; stenosing peptic ulcer; symptomatic prostatic hypertrophy; bladder-neck or pyloroduodenal obstruction; the label’s elderly, debilitated patients category. Below 2 is unestablished, distinct from explicit neonatal contraindication.

Boxed warning / status

No boxed warning appears in selected oral labels. Prescription status and explicit neonatal/lactation/MAO/obstruction restrictions remain applicable. No blanket pediatric, frail-older-adult or pregnancy safety claim.

Adverse reactions and overdose

Sleepiness, dizziness, dry mouth, constipation, blurred vision and weight gain/increased appetite are reported; excitation, hallucinations, seizures, hypotension, palpitations, urinary retention, photosensitivity and blood abnormalities also occur. Tablet label reports cholestasis, hepatitis/hepatic failure. Overdose may cause CNS depression or stimulation and anticholinergic signs; seek emergency/Poison Control advice. Legacy labels include ipecac/lavage/physostigmine directions; they are not a home treatment protocol and are not propagated as an automatic modern management algorithm.

04

Drug interactions

MAO inhibitors are prohibited and CNS depression can add.

MAO inhibitors

Contraindicated during MAO-inhibitor therapy because anticholinergic antihistamine effects can be prolonged/intensified. Labels do not give a validated universal post-stop washout interval; recent MAO therapy needs pharmacist/prescriber review before dosing.

Alcohol and CNS depressants

Alcohol, hypnotics, sedatives, tranquilizers and antianxiety agents may add impairment. Review other antihistamines/anticholinergic products to avoid duplicate exposure; no quantified dose-reduction formula is supplied. The selected syrup’s 5% alcohol is formulation-specific and not assumed for every oral solution.

05

Use in specific populations

Child safety, frailty and nursing status change suitability.

Children and older adults

Below 2 safety/effectiveness are unestablished; newborn/premature use is prohibited. Children need supervision for sedation/excitation and overdose prevention. Ages 15–17 lack an explicit dose-table row. Older adult trial evidence is limited and adverse sensitivity greater; respect the explicit elderly, debilitated contraindication before considering any cautious starting dose.

Renal and hepatic considerations

Renal insufficiency diminishes elimination. No numerical renal/hepatic adjustment or dialysis supplement is supplied; assess organ function and clinical response rather than infer standard safety. Tablet postmarketing hepatic injury reports make jaundice/liver symptoms clinically relevant, but do not establish a universal liver-test schedule.

Pregnancy and lactation

Limited human studies did not show increased malformations but cannot exclude harm; use in pregnancy only if clearly needed after benefit/risk review. Selected contraindications prohibit use while nursing because serious infant effects are possible; the later lactation paragraph advises choosing discontinuation of nursing or drug. Human milk excretion is unknown. No legacy category-based pregnancy guarantee or automatic breastfeeding permission.

06

Clinical pharmacology

Histamine/serotonin antagonism accompanies anticholinergic sedation.

Mechanism

Competes at histamine and serotonin receptor sites, with sedative and atropine-like effects. These explain allergic symptom relief and many adverse effects; they do not establish the drug as emergency anaphylaxis rescue or approve appetite treatment.

Pharmacokinetics

After a single radiolabeled 4 mg dose, at least 40% of radioactivity was recovered in urine and 2–20% in stool; parent was not detected in urine during chronic dosing. Main urinary metabolite is a quaternary ammonium glucuronide conjugate. Elimination diminishes with renal insufficiency. Selected labels supply no validated plasma elimination half-life, CYP dosing algorithm or therapeutic concentration target.

07

Monitoring and counseling

Assess indication, dose, alertness and urinary/visual effects.

Monitoring priorities

Review allergy diagnosis/severity, exact age/weight, nursing status, organ disease, glaucoma/obstruction/frailty and MAO/CNS-depressant exposure. Follow benefit, sedation/excitation, BP-related symptoms, visual/urinary effects and weight/appetite change. Relevant liver/blood symptoms require evaluation; no routine serum level or universal lab interval asserted.

Counseling

Use exact tablet/syrup regimen and calibrated mL measurement; never double or treat a young child from an adult bottle without instructions. Avoid alcohol, unsafe activities and duplicate sedating products; supervise children. Epinephrine/emergency services remain primary for acute anaphylaxis. Report urinary retention, severe confusion, jaundice or rash. Suspected excess ingestion needs immediate Poison Control/emergency assessment; no induced vomiting at home.

08

Product identification

Selected generic appearance and syrup excipients are not universal.

Representative 4 mg tablet

Appearance
White/off-white round flat-faced tablet; B137 one side, score on other.
Selected packages
PD-Rx Pharmaceuticals bottles 30 or 100; NDC 72789-102-30/-01.
Status
Prescription oral product; other generic imprints require exact package verification.

Dosage forms and strengths

Tablet
4 mg cyproheptadine HCl per tablet; selected ingredients include lactose.
Selected syrup
2 mg/5 mL(0.4 mg/mL), yellow mint-flavored 473 mL bottle; NDC 64980-504-48.
Excipients
Selected Rising/Lyne syrup contains alcohol 5%, sucrose and sorbic acid 0.1%; no universal sugar-free/alcohol-free claim.
Route scope
Oral tablets/syrup; no unverified injection, compounded concentration or weight-gain supplement approval.

Storage and handling

Tablets 20–25°C in well-closed child-resistant container. Selected syrup 20–25°C with 15–30°C excursions, tight light-resistant container. Keep securely away from children, use actual expiration and calibrated device; no universal compounded or after-opening stability interval supplied.

09

References

Original sources for the clinical and product information.

  1. DailyMed / official U.S. product labelingCyproheptadine 4 mg tablet · PD-Rx Pharmaceuticals full label

    Current full label; no separate formal clinical revision printed in retained text; SPL v 13 effective 20260216; API publication Feb 18, 2026. Clinical revision is distinct from publication. Checked October 1, 2026.

  2. DailyMed / official U.S. product labelingCyproheptadine 2 mg/5 mL syrup · Rising/Lyne

    Clinical PI revised February 2025; selected syrup contains alcohol 5%; SPL v 9 effective 20250326; API publication Apr 02, 2025. Clinical revision is distinct from publication. Checked October 1, 2026.

LearnOpen tools