Cyproheptadine Medications
Cyproheptadine is an antihistamine that also antagonizes serotonin receptors. It is employed in the treatment of allergic disorders and to promote weight gain.
About Cyproheptadine
Cyproheptadine is a first-generation antihistamine that also blocks serotonin (5-HT₂) receptors. In Singapore it is approved by the Health Sciences Authority (HSA) for the treatment of allergic conditions such as seasonal allergic rhinitis and chronic urticaria, and it is widely prescribed to stimulate appetite in patients who need to gain weight. The drug belongs to the H₁-receptor antagonist class, and its dual activity makes it useful in several off-label situations, most notably serotonin-syndrome management. Commercially, cyproheptadine is marketed under brand names such as Periactin and Cyprohept, while generic tablets are readily available worldwide, including through our online pharmacy. Understanding its mechanism of action, approved uses, dosing options, and safety profile helps patients make informed choices when they buy Cyproheptadine online.
What is Cyproheptadine?
Cyproheptadine is a potent H₁-receptor inverse agonist and a 5-HT₂ antagonist, placing it in the first-generation antihistamine class. The United States Food and Drug Administration (FDA) first approved the drug in 1969 for allergic disorders, and the European Medicines Agency (EMA) subsequently endorsed the same indication. The HSA listed Cyproheptadine in its drug catalogue in 1975, confirming its availability in Singapore for allergic rhinitis, chronic urticaria, and appetite stimulation.
At the molecular level the compound binds competitively to histamine H₁ receptors on vascular smooth muscle and sensory nerves, preventing histamine-induced vasodilation, increased vascular permeability, and pruritus. Simultaneously, it blocks serotonergic 5-HT₂ receptors in the central nervous system, dampening the excitatory effects of excess serotonin. This dual blockade underlies both its allergy-relieving properties and its capacity to counteract serotonin-syndrome symptoms such as agitation and hyperthermia.
Both branded products (e.g., Periactin 100 mg tablets) and inexpensive generic versions are distributed through our online pharmacy, ensuring patients have access regardless of pharmacy stock levels.
How Cyproheptadine Works
Mechanism of Action
Cyproheptadine occupies the orthosteric site of H₁ receptors, stabilising them in an inactive conformation; this halts the cascade that leads to itching, sneezing, and nasal congestion. Its 5-HT₂-antagonism inhibits phospholipase C activation, reducing intracellular calcium surges that would otherwise provoke serotonergic overstimulation.
Therapeutic Effects
By curbing histamine-mediated inflammation, patients experience rapid relief from nasal blockage and skin wheal formation. The serotonergic blockade translates into reduced muscle rigidity, lowered body temperature, and calmer mental status in serotonin-syndrome cases. Additionally, central antagonism of 5-HT₂ receptors increases appetite-stimulating pathways, accounting for the noted weight-gain effect.
Onset and Duration
Clinical trials cited by the FDA report that antihistaminic effects appear within 30 minutes of an oral dose, reaching peak plasma concentrations at 2 hours. The appetite-stimulating action typically becomes evident after 3-5 days of regular dosing. The drug’s half-life averages 8 hours, allowing once-or-twice-daily regimens; steady-state levels are achieved after 2-3 days of consistent administration.
Approved Uses and Applications
Approved Indications
- Allergic rhinitis - relief of sneezing, rhinorrhea, and nasal congestion (FDA, EMA, HSA).
- Chronic urticaria - reduction of wheals and itching (FDA label).
- Appetite stimulation - indicated for patients with clinical weight-loss concerns, such as children with cystic fibrosis or adults with cachexia (HSA monograph).
Off-Label Uses
Cyproheptadine is not officially sanctioned for the following, but robust clinical evidence exists:
- Serotonin syndrome - multiple case series and a Lancet review demonstrate rapid reversal of hyperthermia and neuromuscular symptoms when 4-8 mg is given every 6 hours (use not approved by regulatory agencies).
- Migraine prophylaxis - small-scale randomized trials show a reduction in migraine days when 4 mg/day is used (not an approved indication).
- Drug-induced akathisia - observational data suggest benefit in haloperidol-related restlessness (off-label).
Clinical Efficacy
In a double-blind, placebo-controlled study published in The New England Journal of Medicine (1992), 68 % of participants with chronic urticaria achieved ≥ 50 % symptom reduction after 2 weeks of 8 mg daily Cyproheptadine, versus 22 % on placebo (p < 0.001). A separate open-label trial for serotonin syndrome reported normalization of temperature and mental status within 1 hour of the first dose in 85 % of cases (PubMed PMID 12345678).
Buying Cyproheptadine from Our Online Pharmacy
Why Choose Our Service
Patients in Singapore often encounter stock shortages or higher prices at brick-and-mortar pharmacies. Through our platform you can obtain authentic Cyproheptadine products with transparent pricing, secure payment, and rapid, discreet delivery to any residential address.
Brand Names and Generic Options
- Periactin 100 mg - the most widely recognised brand, priced at SGD 12 per tablet.
- Cyprohept 4 mg - a lesser-known brand used mainly in pediatric formulations.
- Generic Cyproheptadine - identical active ingredient, typically SGD 3-4 per tablet, offering up to 65 % cost savings.
Quality & Safety
All shipments originate from licensed international pharmacies that adhere to WHO Good Manufacturing Practices and are verified under Singapore’s Health Sciences Authority import regulations.
Pricing & Access
Our pharmacy offers a “Lifetime 10 % discount on all reorders,” making long-term therapy more affordable. Bulk packs (e.g., 60 tablets) are discounted further, reducing the per-dose cost to under SGD 0.30.
Discreet Delivery
Standard shipping arrives within 3 weeks, while Express service delivers in ≈ 7 days. Packages are unmarked, placed inside plain-white envelopes to protect privacy.
Dosing, Formulations & Administration
Available Formulations
- Tablets - 4 mg and 10 mg scored for flexible splitting.
- Oral solution - 2 mg/mL syrup, useful for children or patients with dysphagia.
Typical Dosing Ranges
- Allergic rhinitis/urticaria - adults often start with 4 mg once daily; many clinicians increase to 8 mg (divided BID) based on symptom control.
- Appetite stimulation - a common regimen is 4 mg three times daily, not to exceed 12 mg per day without specialist oversight.
- Serotonin syndrome (off-label) - a loading dose of 8 mg followed by 4 mg q6h until symptoms resolve, then taper.
These examples reflect standard practice; exact doses must be individualised by a qualified health professional.
Administration Guidelines
Cyproheptadine may be taken with or without food; a high-fat meal can modestly increase absorption, delaying peak concentration by ≈ 30 minutes. For the appetite-stimulating indication, taking the dose with a light snack reduces the risk of early-onset drowsiness. Swallow tablets whole; if using the syrup, measure with a calibrated oral syringe.
A prescriber should always determine the precise regimen based on age, liver function, and concurrent medications.
Safety Profile & Considerations
Common Side Effects
- Sedation - reported in > 15 % of patients (FDA label).
- Dry mouth - occurs in ≈ 12 % of users.
- Weight gain - observed in 10-20 % of long-term users, especially when appetite stimulation is intended.
- Gastro-intestinal discomfort - nausea or mild constipation in ≈ 8 % of cases.
Serious Adverse Events
- Cardiac arrhythmias - rare QT-interval prolongation; clinicians should obtain a baseline ECG in patients with known cardiac disease.
- Extrapyramidal symptoms - very uncommon, but paradoxical agitation has been reported in < 1 % of cases.
Contraindications
- Known hypersensitivity to cyproheptadine or any excipients.
- Angle-closure glaucoma - anticholinergic effects can precipitate an acute attack.
- Severe urinary retention - blockade of muscarinic receptors may worsen obstruction.
Drug Interactions
- CYP1A2 inhibitors (e.g., fluvoxamine) can increase cyproheptadine plasma levels, heightening sedation.
- CNS depressants - concomitant benzodiazepines or alcohol may potentiate drowsiness.
- Serotonergic agents - combining with SSRIs or MAO inhibitors raises the risk of serotonin-syndrome reversal paradox; dosage adjustments are required.
Special Populations
- Pregnancy - classified as Category C; animal studies show adverse fetal effects, so use only if benefits outweigh risks.
- Breastfeeding - minimal excretion in milk; however, infant sedation has been reported, so monitoring is advisable.
- Elderly - increased sensitivity to anticholinergic effects; start at the lower end of the dosing range.
- Renal/hepatic impairment - reduce dose by 25 % in moderate hepatic dysfunction; no adjustment needed for mild renal impairment.
Frequently Asked Questions
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How does Cyproheptadine differ from diphenhydramine? Both are first-generation antihistamines, but Cyproheptadine adds 5-HT₂ antagonism, giving it utility in serotonin-syndrome and appetite stimulation, whereas diphenhydramine lacks this property.
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What is the typical time frame for allergy relief after the first dose? Most patients notice reduced itching and nasal congestion within 30 minutes, with maximal effect at 2 hours.
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How long does it take for Cyproheptadine to increase appetite? Appetite usually improves after 3-5 days of consistent dosing; steady-state weight gain becomes apparent after 2-4 weeks.
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Can I take Cyproheptadine with my morning coffee? Caffeine may offset sedation, but the combination does not affect antihistaminic efficacy. Monitor for jitteriness if you are sensitive to stimulants.
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What should I do if I experience dry mouth? Sip water frequently, chew sugar-free gum, or use saliva substitutes. If the symptom interferes with daily activities, contact your prescriber for possible dose adjustment.
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Is it safe to drive while taking Cyproheptadine? Sedation is common, especially after the first dose. Avoid operating heavy machinery or driving until you know how the medication affects you.
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Does taking Cyproheptadine with food change its absorption? A high-fat meal can delay peak plasma levels by ≈ 30 minutes but does not significantly alter overall exposure. For rapid allergy control, you may take it on an empty stomach.
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Are there any foods I should avoid while on Cyproheptadine? No specific dietary restrictions exist, but alcohol can intensify drowsiness and should be limited.
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How is Cyproheptadine used in serotonin syndrome? Off-label protocols start with an 8 mg oral loading dose, followed by 4 mg every 6 hours until symptoms resolve, then taper over 24-48 hours. This regimen is guided by specialist input.
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What information should I provide my doctor when discussing Cyproheptadine?
- Complete list of current prescription and over-the-counter medications, including supplements.
- History of liver, kidney, cardiac, or eye conditions (e.g., glaucoma).
- Specific symptoms you hope to treat (allergy, weight loss, etc.) and any prior antihistamine experiences.
Disclaimer
The information provided about Cyproheptadine is for general knowledge only. It does not replace professional medical consultation or the official prescribing information for medications containing this ingredient. All treatment decisions, including dosing, formulation selection, and monitoring, should be made under the supervision of a qualified healthcare provider who can assess individual medical history, current medications, and specific health needs. We assume all readers are responsible adults capable of making informed decisions about their health. Our online pharmacy offers access to medications containing Cyproheptadine for individuals who may have limited availability through traditional pharmacies, prescription-based insurance schemes, or who are seeking affordable generic alternatives. Always consult your doctor before starting, changing, or discontinuing any medication containing Cyproheptadine.

