Cyproheptadine is a first-generation piperidine antihistamine with potent serotonin (5-HT2) and histamine (H1) receptor antagonist activity. It is widely used in India for its appetite-stimulating effects, management of allergic conditions, and as a prophylactic agent for migraine headaches. Its anticholinergic and sedative properties are significant.
Adult: For Allergies: 4 mg three times daily (12 mg/day). Initial dose often 2 mg. For Appetite: 2 mg three times daily (6 mg/day), may increase to 4 mg three times daily (12 mg/day). For Migraine Prophylaxis: 4 mg three to four times daily (12-16 mg/day).
Note: Administer orally with or without food. For appetite stimulation, best taken 30 minutes before meals. Tablet can be crushed if needed. Avoid alcohol and CNS depressants. Maintain adequate hydration.
Cyproheptadine competitively and reversibly blocks histamine at H1-receptor sites, preventing histamine-mediated allergic responses. It also acts as a potent antagonist at serotonin (5-HT2) receptors. Its appetite-stimulating effect is attributed to antagonism of hypothalamic serotonin receptors, which are involved in satiety signaling. Anticholinergic effects are due to muscarinic receptor blockade.
Pregnancy: Category B (US FDA). Animal studies show no risk, but no adequate human studies. Use only if clearly needed and benefit outweighs risk. Not recommended for routine use.
Driving: NOT ADVISABLE, especially during initial therapy or dose escalation. Can impair alertness, reaction time, and motor coordination. Warn patients.
| Alcohol, Benzodiazepines, Opioids | Potentiates CNS depression, sedation, and impaired psychomotor performance. | Major |
| Monoamine Oxidase Inhibitors (MAOIs) e.g., Phenelzine | Risk of severe anticholinergic crisis, hyperpyrexia, convulsions, hypertensive crisis. | Contraindicated |
| Other Anticholinergics (e.g., Atropine, TCAs, Antipsychotics) | Additive anticholinergic effects (dry mouth, constipation, urinary retention, confusion). | Major |
| CNS Stimulants (e.g., Amphetamines) | Cyproheptadine may antagonize the stimulant effect. | Moderate |
| Serotonergic Drugs (SSRIs, SNRIs, Tramadol) | Cyproheptadine's antiserotonergic effect may theoretically reduce efficacy of these drugs. | Moderate |