Kofen

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Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Kofen

Kofen represents the medicinal entity Ketotifen Fumarate, a synthetic compound used for the long-term, prophylactic management of allergic manifestations. It is categorized as a single-ingredient product.

Property Description
Active Ingredient Ketotifen Fumarate
Common Forms Oral (Tablet, Solution), Ophthalmic Solution (Eye drops)
Pharmacological Class Mast Cell Stabilizer, Non-competitive H1-Receptor Antagonist (Antiallergic Agent)
General Purpose Prophylactic management of allergic manifestations
Origin Synthetic Benzocycloheptathiophene Derivative

Definition and Composition: Ketotifen Fumarate

The core of Kofen is the active ingredient, Ketotifen Fumarate, which is a manufactured benzocycloheptathiophene derivative. This formulation is utilized as a fumarate salt to ensure stability and reliable absorption of the active base, Ketotifen.

Pharmacological Type: Dual-Action Antiallergic Agent

Ketotifen Fumarate is classified as an antiallergic agent, distinguished by its dual mechanism of action: it functions as a mast cell stabilizer and a non-competitive H1-receptor antagonist. This dual role is a defining characteristic of its pharmacological type.

Ketotifen functions as a long-acting mast cell stabilizer for preventative therapy. This mechanism aims to diminish the severity and frequency of recurring allergic manifestations, positioning the drug for maintenance therapy rather than immediate, acute relief.

Available Forms: Systemic versus Local

Kofen is supplied in multiple dosage forms, including oral preparations (tablets and solutions) and a local ophthalmic solution (eye drops). The oral preparations are systemic agents, meaning the Ketotifen circulates throughout the body. Conversely, the ophthalmic solution acts as a local agent, concentrating its effect on the surface of the eye to manage localized allergic conjunctivitis, thereby limiting systemic exposure.

What side effects are possible with Kofen?

Kofen (Ketotifen) is generally well-tolerated, but like all medications, it can cause side effects. Patients should be aware of both common and rare, but more serious, potential effects.

Common Side Effects

Side effects that often occur, particularly at the beginning of treatment, include:

  • Drowsiness or Sedation: This is a frequent initial side effect. Patients should avoid driving or operating machinery until they know how the medication affects them.
  • Dry Mouth
  • Slight Dizziness
  • Increased Appetite and Weight Gain
  • Central Nervous System Effects in Children: This may include excitability, irritability, or sleep disturbances.

These common side effects often lessen or disappear spontaneously after the first few days of treatment.


Important Safety Information and Warnings

Discontinue Kofen and seek immediate medical attention if you experience any signs of a severe allergic reaction, such as difficulty breathing, swelling of the face, tongue, or throat, or a generalized rash.

Interactions: Kofen may potentiate the effects of alcohol, sedatives, hypnotics, and other antihistamines. Concurrent use of alcohol should be avoided.

Medical Conditions: Kofen should be used with caution in individuals with a history of epilepsy or seizures, as it may potentially increase the risk. Additionally, a reversible decrease in platelet count has been observed in some patients taking Kofen with oral antidiabetic agents; this combination should be avoided or closely monitored. Always inform your healthcare provider of all existing medical conditions and all medications you are currently taking.

Overdose and Emergency Response

Overdose and When to Seek Help

Official regulatory documents define the potential manifestations of an acute Kofen (Ketotifen Fumarate) overdose and outline the required emergency actions.

Documented Overdose Manifestations

Overdosage primarily affects the Central Nervous System (CNS) and Cardiovascular System. Presentations may range from drowsiness, confusion, disorientation, or severe sedation to more serious outcomes like convulsions and reversible coma.

Cardiovascular effects, such as tachycardia (rapid heartbeat) and hypotension (low blood pressure), are also documented in regulatory prescribing information.

Population-Specific Note: Official labeling specifically highlights convulsions and hyperexcitability as symptoms of acute overdosage, particularly in children.

Required Emergency Actions

Immediate medical help is required in the event of an overdose. If the product is swallowed, official instructions mandate that you get medical help or contact a Poison Control Center right away.

Management is primarily symptomatic and supportive, as no specific antidote is listed in the official prescribing information. Depending on the time of ingestion, procedures such as gastric lavage or administration of activated charcoal may be considered. Short-acting barbiturates or benzodiazepines may be used if convulsions or excitation develop.

Therapeutic Uses of Kofen

Kofen is used in the management of symptomatic discomfort across key allergic axes, helping patients cope more steadily with difficult episodes. It is commonly used to help with conditions presenting with systemic or localized discomfort.

Kofen is applied across therapeutic domains where short-term symptomatic assistance is appropriate, including supporting the long-term management of allergic asthma, easing symptoms of allergic rhinitis (hay fever), and addressing signs of allergic conjunctivitis and urticaria (hives). It is particularly helpful in situations where multiple symptoms occur together and create noticeable functional strain. The support provided helps ease the overall symptom burden, particularly during flare-ups.

This medication supports the patient during difficult episodes by easing distress and is generally used when symptoms intensify and supportive relief is needed. It helps address symptom clusters that may become intense or disruptive, contributing to improved day-to-day comfort during periods of heightened symptoms.


Quick Fact: Relief for Itching Kofen is considered relevant for easing intense itching (pruritus) associated with allergic skin reactions like hives.

Regulatory References

  1. NIH MedlinePlus overview

Eligibility and Restrictions for Use

Kofen (Ketotifen) is typically prescribed to help manage and prevent symptoms associated with allergic conditions, such as bronchial asthma (as a prophylactic add-on therapy), allergic rhinitis, and allergic conjunctivitis.

Who Can Use Kofen?

This medication is generally intended for adults and children aged three years and older for the prophylactic treatment of asthma and other allergic indications, as determined by a healthcare provider. Dosage adjustments may be necessary for elderly patients or individuals with pre-existing conditions.

Who Should Not Use Kofen? (Contraindications)

Kofen is not suitable for everyone. Do not use this medication if you:

  • Have a known allergy or severe hypersensitivity reaction to Ketotifen or any other ingredient in the formulation.
  • Are currently taking oral antidiabetic agents, as there is a risk of a reversible fall in platelet count (thrombocytopenia). Consultation with a doctor is essential.

Additionally, caution is advised for certain groups due to a lack of sufficient data or potential risks:

  • Pregnant or breastfeeding individuals: Use during these periods is generally not recommended unless the potential benefits outweigh the possible risks.
  • Acute asthma attacks: Kofen is a prophylactic drug and is not effective for the prevention or treatment of sudden, acute asthma attacks.
  • Patients with epilepsy: Use may increase the risk of convulsions (seizures).

Always consult a healthcare professional to determine if Kofen is appropriate for your specific health situation.

What should I know about interactions with other medicines?

Kofen Interactions with other medicines and products

Official regulatory information indicates that co-administration of Kofen may alter the effects of certain other medicinal products through distinct mechanistic pathways, including alterations to drug effects and a potential increase in specific adverse risks.


Documented Interacting Categories and Products

Kofen has documented interactions with several classes of drugs, including Oral Antidiabetic Agents, Sympathomimetic Agents, and Anticholinergic Agents. Specific medicinal products explicitly listed in regulatory labeling include Metformin, Glipizide, Linagliptin, Amphetamine, Dextroamphetamine, Hyoscyamine, and Betahistine.

Mechanistic and Outcome Summary

Interacting Product Category Documented Interaction Mechanism or Outcome
Oral Antidiabetic Agents (e.g., Metformin, SGLT2 inhibitors) Increased risk or severity of thrombocytopenia (low platelet count).
Sympathomimetic Agents (e.g., Amphetamine, Ephedrine) May decrease the sedative activities of sympathomimetics; can increase the therapeutic efficacy of certain adrenergic agents (e.g., Epinephrine).
Anticholinergic Agents (e.g., Hyoscyamine) May increase the anticholinergic activities of these agents.
Betahistine May decrease the therapeutic efficacy of Betahistine.

This structure reflects official labeling, focusing on specific risks and documented changes in efficacy or toxicity. Individuals are strongly advised to discuss all current medications and supplements with a healthcare professional, as only a full medical review can confirm the relevance of these interactions.

Mechanism of Action

How Kofen Works: Pharmacodynamic Mechanism

Kofen (Ketotifen) modulates biological activity through a dual pharmacodynamic mechanism that influences the histamine signaling pathway and inflammatory mediator secretion.

Direct Antagonism of Histamine H1 Receptors

Kofen functions as a direct antagonist at the Histamine H1 receptors, transmembrane proteins expressed on various peripheral cell types. This molecular interaction blocks the binding of endogenous histamine, a key inflammatory mediator. Antagonism of the H1 receptor contributes to reduced signaling that triggers vascular permeability changes and sensory nerve stimulation.


Inhibition of Inflammatory Mediator Release

The molecule also acts to inhibit the cellular processes of mast cells and basophils. This upstream mechanism involves blocking the inflow of calcium ions ( Ca^2+) necessary for regulated secretion (degranulation). Inhibition limits the availability of pre-formed mediators, including histamine and leukotrienes, to activate downstream pathways. This action contributes to a reduction in mediator-driven cellular activation, which modulates sustained inflammation-related signaling in the affected tissues.

Dosage and Administration Information

Kofen (ketotifen) is an anti-allergic medication and mast cell stabilizer used for the prophylactic treatment of bronchial asthma and the symptomatic management of allergic conditions, such as allergic rhinitis and conjunctivitis. It is important to understand that Kofen is not intended to treat or stop an acute asthma attack that has already started.

General Administration

Kofen should be taken orally as prescribed by a healthcare provider. It is generally advised to take the medication twice daily, once in the morning and once in the evening, and with food to minimize potential side effects, such as gastrointestinal upset.

If you are taking Kofen for asthma, it is crucial to continue your current asthma treatments (e.g., systemic corticosteroids, bronchodilators) for at least two weeks after starting Kofen, unless otherwise instructed by your doctor, to prevent a potential exacerbation of asthma.

Dosage Guidelines

Dosages may vary based on age, severity of the condition, and formulation. Always follow the specific instructions from your prescribing physician. The typical initial daily doses are:

Patient Group Recommended Dosage Notes
Adults 1 mg twice daily May be increased up to 2 mg twice daily in severe cases.
Children over 3 years 1 mg twice daily In some children, a lower initial dose of 0.5 mg to 1 mg at night may be used for the first few days to address potential sedation.

Missed Dose and Precautions

If you miss a dose, take it as soon as you remember. If it is nearly time for your next scheduled dose, skip the missed one and continue with your regular dosing schedule. Do not double the dose to make up for a missed one.

Because Kofen can cause drowsiness or dizziness, especially at the start of treatment, caution should be exercised when driving or operating machinery until you know how the drug affects you. The effects of other central nervous system depressants, including alcohol, may be potentiated by Kofen, and concurrent use should be avoided.

Recent Clinical Evidence

Kofen is a brand name for the drug Ketotifen (oral and ophthalmic formulations) or Caffeine Citrate (parenteral/oral solution). The clinical evidence summarized below focuses on the primary indications for these active ingredients.


Ketotifen (Oral and Ophthalmic)

Recent clinical studies confirm Ketotifen's role as an anti-allergic and mast cell stabilizer, primarily in treating bronchial asthma and allergic conjunctivitis/rhinitis. For the prophylactic management of asthma, trials—including long-term studies—have shown that Ketotifen can reduce the number, severity, and duration of asthma attacks. This may also allow for a reduction in the requirement for concomitant corticosteroids and/or bronchodilators in some patients.

In the treatment of seasonal and perennial allergic rhinitis and allergic conjunctivitis, evidence supports Ketotifen's efficacy in relieving associated symptoms like sneezing, nasal discharge, nasal obstruction, and ocular itching, with one study showing superiority over a comparator antihistamine in rhinitis treatment.

Primary Indication Key Clinical Finding Patient Population
Asthma Prophylaxis Reduced attack frequency, severity, and duration. Adults and children (typically age 3+)
Allergic Conjunctivitis/Rhinitis Effective relief of symptoms (e.g., itching, sneezing). Adults and children (ocular: age 3+, oral: age 2+/3+)

Caffeine Citrate (Neonatal Apnea of Prematurity)

When Kofen refers to the active ingredient Caffeine Citrate, the focus of clinical evidence is on its use in apnea of prematurity (AOP) in preterm infants. The landmark Caffeine for Apnea of Prematurity (CAP) trial and subsequent follow-up studies established its significant benefits and safety profile, leading to its status as the preferred pharmacological treatment over other methylxanthines.

Key findings from high-quality clinical trials include:

  • Respiratory Benefits: Caffeine therapy significantly reduces the incidence of Bronchopulmonary Dysplasia (BPD) and facilitates earlier successful extubation from mechanical ventilation.
  • Neurodevelopmental Outcomes: Neonatal caffeine treatment is associated with improved survival without neurodevelopmental disability at 18–21 months of age. Long-term follow-up has also indicated lasting positive effects on motor function into middle childhood (up to 11 years of age), without adversely affecting general intelligence or behavior.

Frequently Asked Questions (FAQ)

Common questions about Kofen (FAQ)

Q: How long will it take for Kofen to start working for my asthma?

Kofen is indicated for the long-term, prophylactic (preventative) management of asthma, meaning it is not intended for immediate relief. Clinical reviews indicate that the full protective effect of the oral formulation in reducing asthma attack frequency is typically not seen right away. Regulatory reviews suggest that it may require approximately 6 to 12 weeks of continuous administration to reach the full therapeutic effect. Individual results may vary.


Q: What are the key differences between the oral tablet form and the eye drop form of Kofen?

Kofen is available in both an oral tablet (or solution) and an ophthalmic (eye drop) solution. Official product information states that the oral form is used for systemic conditions, such as the prophylactic treatment of bronchial asthma and generalized allergic conditions. In contrast, the eye drop solution is used locally for the temporary prevention of eye itching due to allergic conjunctivitis, acting directly on the surface of the eye.


Q: What is the recommended maximum daily dose for an adult?

Official product information describes the usual starting dose for adults. The maximum daily intake is determined by the healthcare provider based on the individual's needs and condition severity. Regulatory labeling indicates that the dose may be increased in severe cases, up to the highest specified limit, which is twice the standard starting amount. A healthcare professional should always be consulted for specific dosing.


Q: Is Kofen safe to take long-term?

Kofen is indicated for the long-term, preventative management of allergic manifestations, and clinical trials for the oral formulation have been conducted for extended periods of administration. Official information notes that common side effects, such as initial sedation, often lessen or disappear spontaneously after the first few days of continuous use, but individual responses should be monitored by a healthcare professional.

How should Kofen be stored and disposed of?

How to Store and Dispose of Kofen (Ketotifen Fumarate)

Storage and disposal must strictly adhere to instructions provided in the official regulatory labeling to ensure product quality and safety.


Official Storage Requirements

Kofen must be stored within regulated environmental limits:

  • Temperature: Oral forms (tablets/syrup) require storage at controlled room temperature (typically 20 C to 25 C), and must be kept from freezing. The ophthalmic solution may be stored at room temperature or refrigerated.
  • Protection: The medicine must be kept away from heat, moisture, and direct light. The container must be kept tightly closed; for eye drops, the cap must be replaced after each use to prevent contamination.
  • Child Safety: Kofen must be stored out of the sight and reach of children.

Disposal Requirements

Unused or expired Kofen should not be disposed of in household waste or emptied into drains. Disposal must follow procedures in accordance with local requirements, typically involving return to a pharmacist or approved pharmaceutical waste collection center.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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