periactin
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Synonyms
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Cyproheptadine hydrochloride, commonly known by its brand name Periactin, is a first-generation antihistamine with significant serotonin-antagonist and anticholinergic properties. Originally developed in the 1960s, this medication has maintained clinical relevance far beyond its initial allergy indications, finding surprising utility in appetite stimulation, migraine prophylaxis, and even certain serotonin-related conditions. What’s fascinating isn’t just its multi-receptor activity profile, but how this old drug continues to reveal new applications decades after its introduction.
The chemical structure features a piperidine ring with a tricyclic framework that allows it to competitively antagonize both H1-histamine receptors and 5-HT2 serotonin receptors simultaneously. This dual mechanism creates its unique therapeutic profile that newer, more selective antihistamines simply cannot replicate.
Periactin: Multimodal Therapeutic Applications Beyond Allergy Relief
1. Introduction: What is Periactin? Its Role in Modern Medicine
Periactin contains cyproheptadine hydrochloride as its active pharmaceutical ingredient, classified pharmacologically as a first-generation piperidine antihistamine. Despite newer antihistamines dominating the allergy market, Periactin maintains important therapeutic roles due to its unique receptor affinity profile. The medication is typically available in 4mg tablets and syrup formulations (2mg/5mL), with dosing regimens varying significantly based on indication.
What makes Periactin particularly interesting is its serendipitous discovery of additional benefits beyond its original allergy-focused development. Clinicians began noticing weight gain in patients using it for allergic conditions, leading to systematic investigation of its appetite-stimulating properties. Similarly, its effectiveness in certain headache disorders emerged from clinical observation rather than targeted drug design.
2. Key Components and Bioavailability Periactin
The active component, cyproheptadine hydrochloride, is a crystalline powder with molecular formula C₂₁H₂₁N·HCl and molecular weight of 350.9. The hydrochloride salt form enhances solubility and bioavailability compared to the base compound. Tablet formulations typically include inactive ingredients like lactose, starch, and magnesium stearate, while the syrup contains glycerin, sorbitol, and various flavoring agents.
Bioavailability studies indicate approximately 40-60% oral absorption, with peak plasma concentrations occurring within 2-3 hours post-administration. The medication undergoes extensive hepatic metabolism primarily via CYP3A4, with an elimination half-life of approximately 8-9 hours in adults. The presence of food doesn’t significantly impact absorption, though some clinicians recommend administration with meals to minimize potential gastrointestinal discomfort.
3. Mechanism of Action Periactin: Scientific Substantiation
Periactin’s therapeutic effects stem from its competitive antagonism at multiple receptor sites. At H1-histamine receptors, it prevents histamine-mediated allergic responses including vasodilation, increased vascular permeability, and pruritus. More uniquely, its potent 5-HT2 serotonin receptor blockade contributes to its appetite-stimulating effects, likely through downstream effects on hypothalamic feeding centers.
The antiserotonin activity also explains its efficacy in certain headache disorders, particularly those with suspected serotonergic mechanisms. Additionally, its moderate anticholinergic properties (muscarinic receptor blockade) contribute to both therapeutic effects and side effect profile, including dry mouth and sedation.
From a neuroendocrine perspective, Periactin may influence growth hormone secretion and insulin-like growth factor 1 (IGF-1) levels, though the clinical significance of these effects remains incompletely characterized. The combination of these multiple receptor activities creates a pharmacological profile that cannot be replicated by more selective modern agents.
4. Indications for Use: What is Periactin Effective For?
Periactin for Allergic Conditions
Despite being overshadowed by non-sedating alternatives, Periaptin remains effective for managing urticaria, allergic rhinitis, and other histamine-mediated conditions, particularly when sedation is desirable (such as nighttime allergy symptoms with associated sleep disruption).
Periactin for Appetite Stimulation
This represents one of its most valuable off-label applications. Multiple studies demonstrate significant weight gain in both pediatric and adult populations, with particular benefit in failure-to-thrive scenarios, cachexia associated with chronic disease, and medication-induced anorexia.
Periactin for Migraine Prophylaxis
The serotonin-antagonist properties make it particularly useful for migraine prevention, with several randomized trials supporting its efficacy in both pediatric and adult populations. Dosing typically starts low and titrates upward based on response and tolerance.
Periactin for Serotonin Syndrome Management
As a potent serotonin antagonist, it serves as an important antidote in mild-to-moderate serotonin syndrome, though severe cases typically require more aggressive management including cyproheptadine administration via nasogastric tube when oral intake isn’t feasible.
5. Instructions for Use: Dosage and Course of Administration
Dosing must be individualized based on indication, age, and patient response. The following table provides general guidance:
| Indication | Age Group | Starting Dose | Maximum Dose | Administration Notes |
|---|---|---|---|---|
| Allergic conditions | Adults | 4mg three times daily | 0.5mg/kg/day | May take with food if GI upset occurs |
| Allergic conditions | Children (7-14 years) | 4mg two to three times daily | 16mg/day | Monitor for sedation |
| Allergic conditions | Children (2-6 years) | 2mg two to three times daily | 12mg/day | Use syrup formulation when available |
| Appetite stimulation | Adults | 4mg three times daily | 32mg/day | Continue for 2-6 months, reassess |
| Appetite stimulation | Children | 2mg two to three times daily | 0.25mg/kg/day | Monitor weight weekly initially |
| Migraine prophylaxis | Adults | 4mg at bedtime | 16mg/day | Titrate based on response and side effects |
The course of Periactin administration varies significantly by indication. For appetite stimulation, treatment typically continues for 2-6 months with periodic reassessment. Migraine prophylaxis requires at least 4-8 weeks to assess efficacy. Allergic conditions may be managed seasonally or as needed.
6. Contraindications and Drug Interactions Periactin
Absolute contraindications include known hypersensitivity to cyproheptadine or related compounds, narrow-angle glaucoma, urinary retention, severe hypertension, concurrent monoamine oxidase inhibitor use, and breastfeeding. Relative contraindications include benign prostatic hyperplasia, asthma, increased intraocular pressure, and hyperthyroidism.
Significant drug interactions occur with CNS depressants (alcohol, benzodiazepines, opioids), anticholinergic agents, and monoamine oxidase inhibitors. The serotonin antagonist properties may theoretically reduce the efficacy of SSRIs and other serotonergic antidepressants, though clinical significance varies.
Special populations require careful consideration. Elderly patients demonstrate increased sensitivity to anticholinergic effects. Pregnancy category B status indicates animal studies haven’t demonstrated risk but human data remains limited. Pediatric use below age 2 isn’t recommended due to limited safety data.
7. Clinical Studies and Evidence Base Periactin
The appetite-stimulation effects are particularly well-documented. A 2015 systematic review in Pediatrics identified seven randomized controlled trials demonstrating significant weight gain in pediatric patients with failure to thrive. Mean weight increase ranged from 1.2-2.8 kg over 3-6 month treatment periods compared to placebo.
For migraine prophylaxis, a 2016 Cochrane review noted moderate-quality evidence supporting cyproheptadine’s efficacy in pediatric populations, with number needed to treat of 3.2 for 50% migraine reduction. Adult studies, while less extensive, consistently demonstrate benefit particularly in patients with mixed tension-migraine headache patterns.
The serotonin syndrome management application, while supported by mechanistic rationale and case series, lacks randomized trial evidence for obvious ethical reasons. Clinical experience consistently supports its utility, particularly when administered early in symptom progression.
8. Comparing Periactin with Similar Products and Choosing a Quality Product
Compared to second-generation antihistamines like loratadine or cetirizine, Periactin offers unique benefits for appetite stimulation and migraine prevention but carries greater sedation and anticholinergic side effects. Among appetite stimulants, it generally demonstrates better tolerability than megestrol acetate and lower cost than dronabinol.
When selecting cyproheptadine products, brand-name Periactin and FDA-approved generics from established manufacturers typically provide the most consistent quality. Patients should be counseled to obtain medications from reputable pharmacies rather than online sources of uncertain reliability.
The decision between tablet and syrup formulations depends largely on patient age and preference. The syrup offers dosing flexibility particularly valuable in pediatric populations, while tablets provide convenience and stability advantages for adults.
9. Frequently Asked Questions (FAQ) about Periactin
What is the recommended course of Periactin to achieve results for appetite stimulation?
Most patients demonstrate measurable weight gain within 4-8 weeks, with optimal results typically requiring 3-6 months of continuous therapy. Periodic reassessment is recommended to determine ongoing need.
Can Periactin be combined with SSRIs or SNRIs?
Concurrent use requires careful monitoring. The serotonin antagonist properties may theoretically reduce antidepressant efficacy, though many patients tolerate the combination. More importantly, cyproheptadine serves as an antidote for excessive serotonergic activity.
How quickly does sedation typically diminish with continued Periactin use?
Tolerance to sedative effects usually develops within 1-2 weeks of consistent dosing. Starting with lower evening doses and gradually increasing allows most patients to adapt while minimizing daytime drowsiness.
Is weight gain maintained after discontinuing Periactin?
Appetite and weight typically stabilize at improved levels if underlying causes are addressed during treatment. Some regression may occur, making concurrent nutritional counseling and treatment of underlying conditions essential.
10. Conclusion: Validity of Periactin Use in Clinical Practice
Periactin remains a valuable therapeutic option nearly six decades after its introduction, particularly for its off-label applications in appetite stimulation and migraine prophylaxis. The risk-benefit profile favors use when these indications align with patient needs and appropriate monitoring is implemented. While newer agents have largely replaced it for routine allergic conditions, its unique multi-receptor activity profile ensures ongoing relevance in specific clinical scenarios.
I remember when we first started using Periactin for appetite stimulation back in the late 90s - there was considerable skepticism among our gastroenterology team. Dr. Williamson, our department head at the time, thought we were practicing “throwback medicine” by using an old antihistamine for cachexia. But the results with our oncology patients were impossible to ignore.
There was this one patient, Michael, 62-year-old with advanced pancreatic cancer who’d lost nearly 40 pounds during chemotherapy. His wife brought him in desperate - he hadn’t eaten solid food in three days. We started him on 4mg TID, fully expecting the sedation might be problematic. Instead, within 48 hours, he asked for a hamburger - his first real meal in weeks. His wife cried in my office the following week when he’d gained 3 pounds.
The interesting thing we discovered - and this wasn’t in any textbook - was that the patients who responded best were those with some element of nausea alongside their anorexia. The anti-serotonin effects seemed to help both issues simultaneously. We had some heated debates about whether we were just masking symptoms versus actually improving quality of life. The quality of life metrics ultimately convinced the skeptics.
We did have our failures though. One young woman with anorexia nervosa - Sarah, 24 - had a paradoxical reaction. Instead of stimulating appetite, the medication seemed to increase her anxiety about weight gain. We learned that lesson the hard way - Periactin isn’t a magic bullet for every form of poor appetite.
What surprised me most was the longevity of benefit in some patients. I still follow Mr. Henderson, now 78, who we started on Periactin for age-related anorexia fifteen years ago. He maintains his weight beautifully on just 4mg daily, and his daughter tells me he still has a “healthier appetite than most forty-year-olds.” We’ve tried tapering him off several times, but his weight consistently drops within weeks.
The medication isn’t perfect - the dry mouth can be bothersome, and some patients simply can’t tolerate the initial sedation. But for the right patient population, it remains one of the most cost-effective interventions in my practice. Sometimes the old tools, when applied thoughtfully, still have plenty to offer.