Cyproheptadine API Manufacturer & Bulk Supplier in India | Swapnroop Drugs & Pharmaceuticals

Introduction

Cyproheptadine is a first-generation antihistamine belonging to the piperidine class of pharmaceutical compounds. It is widely recognized for its ability to block histamine H₁ receptors and also exhibits antiserotonergic, anticholinergic and sedative properties.

Cyproheptadine is used in prescription medicines for certain allergic conditions, including allergic rhinitis, urticaria and allergic conjunctivitis. Its additional pharmacological activity has also made it relevant to selected medical applications involving serotonin receptors.

For pharmaceutical manufacturers, formulation developers, API procurement teams and quality-control professionals, evaluating Cyproheptadine API requires attention to chemical identity, salt form, hydration state, purity, related substances, stability and applicable pharmacopoeial requirements.

Cyproheptadine hydrochloride is the commonly referenced pharmaceutical form. It is generally described in official drug labelling as the hydrochloride sesquihydrate. This distinction is important when determining molecular weight, product specifications and assay calculations.

Swapnroop Drugs & Pharmaceuticals (SDP) presents this technical overview for pharmaceutical professionals researching Cyproheptadine API, its applications and its quality requirements.

What Is Cyproheptadine API?

Cyproheptadine is a synthetic antihistamine that belongs to the piperidine class. It acts as an antagonist at histamine H₁ receptors and also blocks certain serotonin receptors.

Histamine is a chemical mediator involved in allergic responses. When released during an allergic reaction, it can contribute to itching, sneezing, nasal discharge, watery eyes and other symptoms.

By blocking H₁ receptors, cyproheptadine reduces the effects of histamine in susceptible tissues. Its antiserotonergic activity distinguishes it from several other antihistamines.

The pharmaceutical ingredient is commonly used as cyproheptadine hydrochloride, a crystalline material described in official product labelling as a white to slightly yellowish powder.

Cyproheptadine API – Key Product Information

The following information distinguishes the free base from the commonly used hydrochloride sesquihydrate.

Parameter	Information
API Name	Cyproheptadine
Common Pharmaceutical Form	Cyproheptadine Hydrochloride Sesquihydrate
Free-Base CAS Number	129-03-3
Anhydrous Hydrochloride CAS Number	969-33-5
Hydrochloride Sesquihydrate CAS Number	41354-29-4
Free-Base Molecular Formula	C₂₁H₂₁N
Free-Base Molecular Weight	Approximately 287.40 g/mol
Anhydrous Hydrochloride Formula	C₂₁H₂₁N·HCl
Anhydrous Hydrochloride Molecular Weight	Approximately 323.86 g/mol
Hydrochloride Sesquihydrate Formula	C₂₁H₂₁N·HCl·1.5H₂O
Hydrochloride Sesquihydrate Molecular Weight	Approximately 350.89 g/mol
Pharmacological Class	First-generation antihistamine
Chemical Class	Piperidine derivative
Main Receptor Activity	Histamine H₁ and serotonin receptor antagonism
Common Dosage Form	Oral tablets

Important chemical clarification: The sesquihydrate contains 1.5 molecules of water per molecule of cyproheptadine hydrochloride. PubChem also represents the hydrated material using a doubled molecular formula, C₄₂H₅₀Cl₂N₂O₃, with a molecular weight of approximately 701.8 g/mol. This is equivalent to two hydrochloride units with three water molecules. The applicable formula convention should be stated clearly in the product specification.

The official DailyMed label identifies cyproheptadine hydrochloride USP as the sesquihydrate and reports a molecular weight of approximately 350.89 g/mol. <Cite refs={["turn605024search0","turn323370search0","turn323370search2"]} />

Chemical Structure and Properties of Cyproheptadine

Cyproheptadine has a tricyclic chemical structure connected to a methyl-substituted piperidine ring. Its structure is related to other tricyclic antihistamine compounds.

The free-base molecule has the molecular formula C₂₁H₂₁N and a molecular weight of approximately 287.40 g/mol.

The hydrochloride form is produced by combining the free base with hydrochloric acid. In its commonly described sesquihydrate form, the material also contains 1.5 molecules of water per hydrochloride unit.

According to official product labelling, cyproheptadine hydrochloride is a white to slightly yellowish crystalline powder. It is slightly soluble in water, freely soluble in methanol, sparingly soluble in alcohol and practically insoluble in ether.

These properties are relevant to API identification, formulation development, material handling, analytical testing and stability assessment.

Mechanism of Action of Cyproheptadine

Cyproheptadine exhibits antihistaminic and antiserotonergic activity, along with anticholinergic and sedative effects.

1. Histamine H₁ Receptor Antagonism

Cyproheptadine competes with histamine for binding at H₁ receptor sites. This reduces histamine-mediated effects associated with allergic reactions.

2. Serotonin Receptor Antagonism

Cyproheptadine also blocks certain serotonin receptor activities. This additional pharmacological property distinguishes it from antihistamines that primarily act on histamine receptors.

3. Anticholinergic Activity

Cyproheptadine exhibits anticholinergic properties, which contribute to some of its pharmacological effects and potential adverse reactions.

4. Sedative Effects

As a first-generation antihistamine, cyproheptadine can produce drowsiness and reduced alertness. These effects are important considerations in its clinical use and product information.

Its combined pharmacological activities explain its use in selected allergic conditions and other specific medical applications.

Pharmaceutical Applications of Cyproheptadine

Cyproheptadine is used in prescription medicines for selected allergic conditions.

1. Allergic Rhinitis

Cyproheptadine is used in approved products for certain seasonal and perennial allergic rhinitis conditions. Its antihistaminic action helps reduce histamine-related symptoms.

2. Allergic Conjunctivitis

It may be used for allergic conjunctivitis associated with inhalant allergens and foods, according to applicable product labelling.

3. Urticaria and Angioedema

Cyproheptadine is included in certain approved treatment options for uncomplicated allergic skin manifestations, including urticaria and angioedema.

4. Other Allergic Skin Conditions

Its antihistaminic properties are relevant to selected pruritic skin conditions and other allergic manifestations described in approved product information.

5. Selected Serotonin-Related Applications

Because of its antiserotonergic activity, cyproheptadine has also been used in selected medical settings involving serotonin-related effects. These uses depend on the relevant clinical guidance and regulatory approval.

Clinical note: Cyproheptadine can cause sedation and anticholinergic adverse effects. Its use should follow approved prescribing information and qualified medical advice. This article does not provide patient-specific treatment recommendations.

Pharmaceutical Formulations of Cyproheptadine

Cyproheptadine hydrochloride is commonly used in oral pharmaceutical formulations.

Examples of marketed or established dosage presentations include:

Conventional oral tablets
Oral liquid formulations, where approved
Other market-specific oral presentations

The selection of dosage form depends on the intended patient population, product requirements, excipient compatibility and regulatory approval.

For formulation development, pharmaceutical manufacturers should assess:

API-excipient compatibility
Salt and hydration-state consistency
Content uniformity
Dissolution characteristics
Moisture sensitivity
Stability during manufacture and storage
Packaging suitability

The hydration state should be controlled because it can affect the material's molecular-weight basis and the interpretation of assay results.

Quality Requirements for Cyproheptadine API

Quality assurance is essential when evaluating Cyproheptadine API. The material should meet the applicable pharmacopoeial monograph and approved product specification.

1. Identification

Identification testing should confirm that the material is cyproheptadine hydrochloride in the specified form. Appropriate validated analytical methods may include infrared spectroscopy and chromatographic techniques.

2. Assay and Potency

The assay should establish the content of the active pharmaceutical ingredient using a validated analytical method.

The specification should clearly state whether the result is calculated on an anhydrous basis, hydrated basis or another approved basis.

3. Related Substances

Related substances and degradation products should be assessed using suitable validated analytical procedures.

Acceptance criteria must follow the applicable pharmacopoeial requirements and approved specification.

4. Water Content

Because the commonly used hydrochloride form is a sesquihydrate, water content and hydration-state control are important quality considerations.

The relevant test method and acceptance limits should be established by the approved specification.

5. Residual Solvents

Residual solvents should be evaluated in accordance with applicable ICH requirements and the approved material specification.

6. Physical Characteristics

Appearance, crystalline characteristics and other relevant physical properties should be evaluated where required by the material specification.

7. Stability

Stability studies should support the proposed retest period, storage conditions and packaging system. Stability conclusions must be based on actual data for the material being evaluated.

Analytical Testing and Quality Control

A quality-control programme for Cyproheptadine API should follow the applicable pharmacopoeial requirements and approved specification.

Potential testing areas include:

Description and appearance
Identification
Assay
Related substances
Water content
Residual solvents
Relevant physical-characterisation tests
Stability-indicating analytical evaluation
Packaging integrity
Batch traceability

The exact testing panel and numerical acceptance limits should be determined from the applicable monograph and approved product specification. Generic limits should not be substituted for validated product-specific requirements.

Documentation Required for Pharmaceutical Evaluation

Before qualifying a Cyproheptadine API source, pharmaceutical manufacturers and procurement teams should review relevant quality and regulatory documents.

Typical documents include:

Batch-specific Certificate of Analysis (COA)
Technical Data Sheet (TDS)
Safety Data Sheet (SDS)
Approved API specification
Analytical method information
Related-substances and impurity profile
Water-content information
Residual-solvent information, where applicable
Stability data and retest-period justification
Packaging and storage details
Manufacturing and quality-system information
Applicable regulatory declarations and supporting documents

The COA should clearly identify the chemical form and hydration state. This helps avoid confusion between free-base, anhydrous hydrochloride and hydrochloride sesquihydrate molecular-weight values.

Regulatory Considerations for Cyproheptadine API in India

Cyproheptadine is an antihistamine used in prescription pharmaceutical products in various markets. Its manufacture, import, distribution and use in finished medicines must comply with applicable Indian drug regulations.

Organizations evaluating the material should consider:

Applicable requirements under the Drugs and Cosmetics Act and Rules
Relevant manufacturing or import licences
Applicable pharmacopoeial standards
Approved API specifications
Quality-system and batch-traceability requirements
Finished-product approval and labelling requirements
Destination-market requirements for export products

The regulatory status and prescription classification of cyproheptadine products can vary between countries. Companies should verify the current requirements for their intended market with relevant authorities and qualified regulatory professionals.

Factors to Consider When Evaluating a Cyproheptadine API Source

Pharmaceutical manufacturers and procurement professionals should follow a documented supplier-qualification process.

Chemical identity: Confirm the exact chemical form and CAS number.

Hydration state: Establish whether the supplied material is hydrochloride sesquihydrate or another form.

Molecular-weight basis: Confirm the molecular-weight value used in the specification and assay calculations.

Analytical quality: Review the batch-specific COA, assay results, impurity profile and validated analytical methods.

Water content: Review the hydration-state and water-content controls.

Stability and packaging: Evaluate supporting stability information, storage recommendations and packaging suitability.

Quality management: Review batch traceability, deviation management, change control and complaint-handling procedures.

Regulatory documentation: Verify that applicable manufacturing, import and distribution permissions are in place.

Cyproheptadine API Enquiries – Swapnroop Drugs & Pharmaceuticals

Swapnroop Drugs & Pharmaceuticals (SDP) provides pharmaceutical industry information and supports business enquiries relating to pharmaceutical APIs and raw materials.

For Cyproheptadine API enquiries, pharmaceutical organizations should specify the required chemical form, hydration state, grade, applicable specification and intended market.

The product documentation should clearly identify whether the material is cyproheptadine free base, anhydrous hydrochloride or hydrochloride sesquihydrate. Any discussion of sourcing or availability is subject to verification of the exact product, current availability, quality documentation and applicable regulatory permissions.

Frequently Asked Questions (FAQs)

1. What is Cyproheptadine API?

Cyproheptadine API is a first-generation antihistamine ingredient belonging to the piperidine class. It blocks histamine H₁ receptors and also exhibits antiserotonergic activity.

2. What is the CAS number of Cyproheptadine?

The free base is associated with CAS 129-03-3. Anhydrous cyproheptadine hydrochloride is associated with CAS 969-33-5, while the hydrochloride sesquihydrate is associated with CAS 41354-29-4.

3. What is the molecular formula of Cyproheptadine?

The molecular formula of the free base is C₂₁H₂₁N.

4. What is the molecular weight of Cyproheptadine?

The free-base molecular weight is approximately 287.40 g/mol. Anhydrous cyproheptadine hydrochloride is approximately 323.86 g/mol, while the hydrochloride sesquihydrate is approximately 350.89 g/mol.

5. What is Cyproheptadine Hydrochloride Sesquihydrate?

It is the hydrochloride salt of cyproheptadine containing 1.5 molecules of water per molecule of hydrochloride. It is the form commonly described in official cyproheptadine hydrochloride product labelling.

6. What is the pharmacological class of Cyproheptadine?

Cyproheptadine is a first-generation antihistamine and a piperidine derivative. It also has antiserotonergic and anticholinergic properties.

7. How does Cyproheptadine work?

It blocks histamine H₁ receptors and certain serotonin receptor activities, reducing the effects of these chemical messengers.

8. What are the pharmaceutical applications of Cyproheptadine?

It is used in approved medicines for selected allergic conditions, including allergic rhinitis, allergic conjunctivitis, urticaria and certain other allergic manifestations.

9. Which dosage forms contain Cyproheptadine?

Cyproheptadine hydrochloride is commonly used in oral tablets and, in certain markets, oral liquid formulations.

10. Why is water content important in Cyproheptadine API?

The commonly referenced hydrochloride form is a sesquihydrate. Its water content affects the molecular-weight basis and must be controlled according to the applicable specification.

11. What quality tests are relevant for Cyproheptadine API?

Relevant tests may include identification, assay, related substances, water content, residual solvents, physical characteristics and stability-indicating analysis.

12. What should buyers confirm before making a Cyproheptadine API enquiry?

Buyers should confirm the exact chemical form, CAS number, hydration state, grade, assay basis, specification, intended market and supporting quality documentation.

Conclusion

Cyproheptadine is an established first-generation antihistamine with H₁ receptor-blocking and antiserotonergic properties. It is used in pharmaceutical products for selected allergic conditions and other specific medical applications.

The distinction between cyproheptadine free base, anhydrous hydrochloride and hydrochloride sesquihydrate is essential for accurate chemical identification and quality assessment. Pharmaceutical manufacturers and procurement teams should verify the exact material form, molecular-weight basis, assay, water content, impurity profile and regulatory documentation before approving an API for pharmaceutical use.

Swapnroop Drugs & Pharmaceuticals welcomes legitimate pharmaceutical business enquiries relating to Cyproheptadine API, subject to verification of product details, availability and applicable regulatory requirements.