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 precautionsIndications
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.
Dosage and administration
Individualize total daily dose and respect age limits.
Selected labeled regimens
| Population | Oral dose and limit |
|---|---|
| Age 2–6 years | 2 mg two or three times daily; maximum 12 mg/day. Selected syrup:5 mL/dose; tablet:half 4 mg tablet. |
| Age 7–14 years | 4 mg two or three times daily; maximum 16 mg/day. Selected syrup:10 mL/dose. |
| Pediatric total-dose basis | Approximately 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. |
| Adults | Start 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 gap | Selected tables name child bands through 14 and Adults without explicitly assigning 15–17. Obtain exact prescriber dose review; no automatic adult regimen. |
| Below 2 / neonatal | Safety/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.
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.
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.
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.
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.
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.
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.
References
Original sources for the clinical and product information.
- 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.
- 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.