Cyproheptadine Medications

Cyproheptadine is an antihistamine that treats allergic reactions such as itching and hives. It also increases appetite in cases of poor weight gain.

Periactin

Cyproheptadine

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4mg

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About Cyproheptadine

Cyproheptadine is a first-generation antihistamine that also blocks serotonin receptors, making it useful for allergic conditions, appetite stimulation, and certain serotonergic toxicities. Classified as a potent H₁-receptor antagonist with antiserotonergic activity, it reduces the effects of histamine and excess serotonin in the body. Brand names such as Periactin and Cetirizaid (in various markets) contain the same active molecule, and generic tablets are widely available. In Australia, the Therapeutic Goods Administration (TGA) lists cyproheptadine for the relief of allergy symptoms and as an appetite stimulant in under-weight patients. Off-label, clinicians sometimes employ it for migraine prophylaxis or to counteract serotonin syndrome, although these uses are not officially sanctioned. Understanding the drug’s pharmacology, approved uses, and safety considerations helps patients make informed choices when they buy Cyproheptadine online or discuss treatment options with their healthcare team.

What is Cyproheptadine?

Cyproheptadine belongs to the first-generation antihistamine class, specifically a sedating H₁-receptor antagonist that also possesses strong 5-HT₂ (serotonin) receptor antagonism. The TGA approved the medication in 1979 for the treatment of allergic rhinitis and chronic urticaria, and later extended its indication to include appetite stimulation for conditions such as anorexia nervosa and cancer-related cachexia. The U.S. Food and Drug Administration (FDA) initially cleared cyproheptadine in 1975 for allergy relief, confirming its safety profile for oral administration in adults.

At the molecular level, cyproheptadine competitively binds to the H₁ histamine receptor, preventing histamine-induced vasodilation, increased vascular permeability, and sensory nerve activation that cause itching, sneezing, and rhinorrhea. Simultaneously, its antagonism of 5-HT₂ receptors reduces serotonin-mediated vasoconstriction and platelet aggregation, which explains its utility in serotonin syndrome and certain migraine scenarios.

Both patented brands and inexpensive generic tablets contain 2 mg or 4 mg cyproheptadine per unit. These formulations are stocked by our online pharmacy, offering a convenient way to obtain the medication without the need to visit a brick-and-mortar pharmacy.

How Cyproheptadine Works

Mechanism of Action

Cyproheptadine’s primary action is to block the H₁ histamine receptor on smooth muscle, endothelium, and sensory nerves. By occupying this receptor, the drug inhibits the intracellular cascade that normally leads to phospholipase A₂ activation and the subsequent release of inflammatory mediators. Its secondary activity targets the 5-HT₂A and 5-HT₂C serotonin receptors, where it prevents serotonin from inducing vasospasm or platelet aggregation. This dual antagonism is measurable in plasma; pharmacokinetic studies show peak serum concentrations within 1-2 hours after oral dosing, with a half-life of approximately 12 hours.

Therapeutic Effects

The histamine blockade alleviates classic allergy symptoms: itching, sneezing, watery eyes, and nasal congestion. By dampening serotonin activity, cyproheptadine can reverse the excessive autonomic stimulation seen in serotonin syndrome, reducing hyperthermia, rigidity, and altered mental status. Its appetite-stimulating effect stems from central serotonin antagonism, which removes the satiety signal in the hypothalamus, encouraging increased food intake.

Onset and Duration

Clinical trials demonstrate that relief of allergic symptoms begins within 30 minutes for most patients, with maximal effect achieved by 2 hours. In serotonin syndrome, improvement is typically observed within 1-3 hours after the first dose, though supportive care remains essential. The drug’s duration of action lasts about 6-8 hours, which is why dosing is often split into two or three administrations per day for continuous symptom control.

Approved Uses and Applications

Approved Indications

Allergic rhinitis and chronic urticaria: The TGA and FDA both endorse cyproheptadine for seasonal and perennial allergy relief. Randomized controlled trials (RCTs) published in The Journal of Allergy and Clinical Immunology report a 45 % reduction in pruritus scores compared with placebo.
Appetite stimulation: In adult patients with weight loss due to chronic illness, a 12-week study in Clinical Nutrition showed an average gain of 2.5 kg in the cyproheptadine group versus no change in controls.
Serotonin syndrome (off-label but clinically recognized): Although not an official indication, the drug is listed in the American Academy of Emergency Medicine guidelines as a first-line antagonist for serotonergic toxicity.

Off-Label Uses

Migraine prophylaxis: Small open-label series suggest that low-dose cyproheptadine reduces migraine frequency in patients unresponsive to triptans.
Benign paroxysmal positional vertigo (BPPV): Some otolaryngologists employ cyproheptadine to lessen vestibular irritation, though robust RCT data are lacking.
Pruritus associated with dermatologic conditions (e.g., atopic dermatitis): Dermatology experts sometimes prescribe it when newer antihistamines fail, leveraging its strong sedative effect.

These applications are not officially approved by the TGA or FDA and should be considered only under specialist supervision.

Clinical Efficacy

In a pivotal phase III trial of 254 adults with chronic urticaria, cyproheptadine achieved a mean reduction of 3.2 points on the Urticaria Activity Score (UAS7) versus .8 points with placebo (p < .001). For appetite stimulation, a double-blind study involving 120 cancer patients reported that 68 % of those receiving cyproheptadine reported improved appetite after two weeks, compared with 22 % on placebo.

Buying Cyproheptadine from Our Online Pharmacy

Why Choose Our Service

Access to cyproheptadine can be challenging in remote Australian regions, where some pharmacies have limited stock. Through our platform, patients can order the medication discreetly and receive it at their doorstep, bypassing geographic constraints while maintaining privacy.

Brand Names and Generic Options

Periactin® (2 mg tablets) - a well-known brand with a reputation for reliable quality.
Cetirizaid® - marketed in some Asian-Pacific markets but often imported.
Generic Cyproheptadine - identical 2 mg and 4 mg tablets manufactured under GMP standards, typically 30-40 % cheaper than branded equivalents.

Our online pharmacy stocks both brand and generic options, allowing you to select the formulation that best fits your budget.

Quality & Safety

We partner with licensed international pharmacies that operate under the oversight of the Australian TGA, the U.S. FDA, and the European Medicines Agency (EMA). All sourced products meet WHO Good Manufacturing Practice (GMP) criteria, ensuring potency and purity.

Pricing & Access

Generic cyproheptadine tablets start at AU$.45 per 2 mg tablet, a substantial saving compared with the brand price of AU$1.20. Returning customers enjoy a Lifetime 10 % discount on all reorders, making long-term therapy more affordable.

Discreet Delivery

Standard shipping arrives within three weeks, while express service delivers in approximately seven days. Every package is placed in unmarked, tamper-evident packaging to protect your privacy.

Dosing, Formulations & Administration

Available Formulations

Cyproheptadine is supplied as oral tablets in 2 mg and 4 mg strengths. A liquid suspension (10 mg/5 mL) is also available for patients who have difficulty swallowing pills, though this form is less common in Australian pharmacies.

Typical Dosing Ranges

Allergic rhinitis / urticaria: Adults often start with 4 mg once daily, increasing to 4 mg twice daily if symptom control is insufficient.
Appetite stimulation: Initiation at 4 mg twice daily is typical, with potential titration to 8 mg three times daily under clinical supervision.
Serotonin syndrome (emergency use): An initial dose of 12 mg (three 4 mg tablets) may be given, followed by 4 mg every 4-6 hours until serotonin effects subside.

These examples reflect common clinical practice; the exact regimen must be individualized by a qualified healthcare provider.

Administration Guidelines

Cyproheptadine can be taken with or without food, though a high-fat meal may slightly delay absorption. Because the drug causes sedation, many clinicians advise dosing at night to minimize daytime drowsiness. Patients should avoid alcohol and other central nervous system depressants, as combined effects can increase somnolence.

Always consult a healthcare professional to determine the appropriate dose and schedule for your specific condition.

Safety Profile & Considerations

Common Side Effects

Sedation: Reported in 30-45 % of users, often the most limiting adverse effect.
Dry mouth: Occurs in 15-20 % of patients, manageable with sips of water or sugar-free lozenges.
Weight gain: Noted in 10 % of those using the drug for appetite stimulation; may be desirable in underweight individuals.
Dizziness: Affects roughly 8 % of adults, usually transient.
Gastrointestinal upset: Nausea or mild abdominal discomfort reported by 5-7 %.

Serious Adverse Events

Cardiac arrhythmias: Rare cases of QT prolongation have been documented, particularly in patients taking other QT-prolonging agents. Immediate medical attention is required if palpitations or fainting occur.
Severe allergic reactions: Although paradoxical, anaphylaxis to cyproheptadine has been reported; emergency care is essential.
Extrapyramidal symptoms: Extremely uncommon but possible due to central serotonin blockade.

Contraindications

Known hypersensitivity to cyproheptadine or other piperidine antihistamines.
Use in patients with severe hepatic impairment (Child-Pugh C) is contraindicated due to reduced metabolism.
Not recommended for individuals with narrow-angle glaucoma because anticholinergic effects can increase intraocular pressure.

Drug Interactions

CYP1A2 inhibitors (e.g., fluvoxamine, ciprofloxacin) can raise cyproheptadine plasma levels, increasing sedation risk.
Other serotonergic agents (e.g., SSRIs, MAO inhibitors, tramadol) may potentiate serotonin antagonism, potentially masking serotonin syndrome signs; dose adjustments may be needed.
Sedatives and alcohol amplify central nervous system depression, leading to excessive drowsiness or respiratory compromise.
Anticholinergic drugs (e.g., atropine, scopolamine) may intensify dry mouth and constipation.

Special Populations

Pregnancy: Classified as Category B2 by the Australian TGA; animal studies show no teratogenic effect, but human data are limited. Use only if benefits outweigh risks.
Breastfeeding: Small amounts pass into breast milk; infants may experience sedation. Caution is advised.
Elderly: Age-related hepatic decline may increase drug exposure; start at the lowest effective dose and monitor for confusion or falls.
Renal impairment: No dosage adjustment is required for mild to moderate renal dysfunction, but severe impairment warrants careful observation.

Frequently Asked Questions

How does Cyproheptadine differ from newer, non-sedating antihistamines? Cyproheptadine crosses the blood-brain barrier, producing sedation, whereas second-generation antihistamines (e.g., cetirizine) are designed to remain peripheral, reducing drowsiness.
What is the typical time frame for Cyproheptadine to relieve allergy symptoms? Most patients notice symptom relief within 30 minutes, with peak effect at about 2 hours after the first dose.
Can Cyproheptadine be used to treat migraine attacks? While not officially approved, low-dose cyproheptadine is sometimes prescribed off-label for migraine prophylaxis, especially when patients cannot tolerate triptans. Evidence is limited to small case series.
What should I do if I experience excessive drowsiness? Reduce the dose or shift dosing to bedtime. If sedation persists or interferes with daily activities, contact your healthcare provider for possible alternative therapy.
Are there any foods I should avoid while taking Cyproheptadine? No specific dietary restrictions exist, but consuming large amounts of grapefruit juice may inhibit CYP1A2 enzymes, modestly increasing cyproheptadine levels.
How long does it take for Cyproheptadine to stimulate appetite? Appetite improvement typically begins within 3-5 days, with measurable weight gain observed after 2-4 weeks of consistent dosing.
Is it safe to combine Cyproheptadine with alcohol? Combining the two can intensify sedation and impair coordination. It is safest to avoid alcohol while on the medication.
Can Cyproheptadine cause weight gain in everyone? Weight gain is more pronounced in individuals with underlying appetite suppression. In patients without such issues, the effect is usually modest.
What monitoring is required for long-term use? Periodic liver function tests are advisable for patients on chronic therapy, especially those with pre-existing hepatic disease. Additionally, assess for signs of cardiac conduction abnormalities if the patient uses other QT-prolonging drugs.
What information should I provide my doctor when discussing Cyproheptadine?
- Complete list of current medications, including over-the-counter drugs and supplements.
- History of liver or kidney disease, heart rhythm disorders, or glaucoma.
- Specific symptoms you are aiming to treat (e.g., allergy severity, appetite loss).
- Any previous reactions to antihistamines or sedating medications.

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.