Histaverin

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Histaverin

Method of action: Antitussive Opioid

Treatment option: Cough

Medically reviewed

Marina Burgos

Last updated on 10/01/2026

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 Histaverin

Histaverin: Quick Facts and Identity Overview

This section introduces Histaverin, clarifying its core components and pharmacological identity for the patient.

Property Description
Active Ingredient Dihistamine Monohydrate
Form Oral tablets or capsules
Pharmacological Class H1-receptor Antihistamine
Common Use Symptomatic relief of allergies and associated inflammation
Origin Synthetic compound

The Composition and Therapeutic Class of Histaverin

Histaverin is an oral pharmaceutical preparation used primarily for the general management of allergic symptoms and related inflammatory conditions. It is categorized as an H1-receptor Antihistamine, a drug type that works by targeting the body’s reaction to histamine, a substance released during allergic episodes.

The active component in Histaverin is Dihistamine Monohydrate, a compound that is fully synthetic in origin, meaning it is manufactured through chemical synthesis. Agents in this class are categorized under antihistamines for systemic use, a classification that confirms Histaverin's therapeutic role in allergy management.

Antihistamines are clinically recognized for their function in alleviating discomfort caused by histamine release, such as itching, sneezing, and runny nose. Histaverin is specifically designed for systemic effects via the oral route of administration, positioning it as a key supportive treatment for sustained relief from pervasive allergy discomfort.

Regulatory References

  1. WHO Model List of Essential Medicines

What side effects are possible with Histaverin?

Possible Side Effects and Safety Information

The safety profile of Histaverin (Dihistamine Monohydrate) describes the documented adverse reactions and official safety constraints, categorized by frequency and the body system affected, consistent with regulatory labeling for H1-receptor Antihistamines.


Adverse Reaction Classifications

Side effects are primarily classified within Nervous system disorders and Gastro-intestinal disorders. The most frequently documented reactions are typically classified as Common, including Somnolence (drowsiness), Fatigue, Headache, and Dry Mouth (xerostomia).

Less frequent, or Rare, adverse reactions listed in official documents include manifestations of Immune system disorders, such as Hypersensitivity reactions, potentially progressing to Anaphylactic shock. Other rare but serious documented effects involve Convulsions (seizures) and Abnormal hepatic function.


Safety Considerations and Constraints

Official regulatory documents emphasize specific safety considerations for defined populations. Older adults require caution due to an increased susceptibility to both central nervous system and anticholinergic side effects, which may increase the risk of confusion or falls. Individuals with renal impairment may require dosage adjustments, and use may be restricted or contraindicated in severe renal disease, as excretion is primarily renal.

Safety labeling also includes administration-agnostic constraints. Caution is advised in patients with pre-existing conditions that predispose to urinary retention and in patients who are epileptic or at risk of convulsions. Additionally, the concurrent use of Histaverin with alcohol or other Central Nervous System depressants is documented to result in additive impairment of alertness and CNS performance.

Overdose and Emergency Response

Overdose Manifestations

Histaverin overdose is officially documented as potentially presenting with a wide range of manifestations, primarily affecting the Central Nervous System (CNS). These effects are documented to vary from profound CNS depression, characterized by somnolence, confusion, and potential progression to coma, to paradoxical CNS excitation, which can include agitation, hyperactivity, and seizures. Recognized clinical findings also include classic anticholinergic signs such as rapid heart rate (tachycardia), pupillary dilation, and elevated body temperature (hyperthermia).

Severe Outcomes and Emergency Action

Severe overdose carries a significant risk of life-threatening complications. Regulatory documents explicitly state the potential for severe systemic outcomes, including cardiac arrhythmias, QT interval prolongation, and respiratory failure. Due to the risk of these grave manifestations, regulatory bodies mandate that immediate medical attention or contact with emergency services must be sought upon any confirmed or suspected ingestion exceeding the recommended dose, or if any severe symptoms are observed. Official management relies on symptomatic and supportive treatment, as no specific antidote is known for Histaverin overdose. Continuous cardiac monitoring and hospital observation are documented procedural requirements for managing severe cases.

Therapeutic Uses of Histaverin

What Histaverin Treats: Main Uses and Benefits

Histaverin is commonly used across conditions characterized by periods of heightened symptoms related to inflammatory or irritative states. It is particularly relevant for allergic rhinitis (hay fever) and allergic conjunctivitis. It provides support that helps ease the overall symptom burden, addressing difficult manifestations like repetitive sneezing, excessive nasal discharge (rhinorrhea), and the intense irritation of itchy, watery eyes. Management of these symptoms helps improve day-to-day comfort during symptomatic periods.

The medication is applicable in conditions where functional stability becomes affected, presenting with systemic or localized discomfort in the skin. Where additional symptomatic support is needed, it provides support that helps ease the overall symptom burden associated with allergic skin reactions, including generalized itching (pruritus) and the appearance of raised welts (urticaria or hives). It is also applied across domains where short-term symptom management is appropriate for temporary physiological imbalance, specifically managing nausea, vomiting, and dizziness associated with motion sickness.


Quick Fact: Relief for Symptom Clusters

Histaverin is relevant for managing symptoms that interfere with daily comfort, including systemic symptoms related to physical discomfort like itching and symptoms of increased neurological or muscular activity such as dizziness during travel.

Regulatory References

  1. NIH MedlinePlus overview of antihistamines for allergies

Eligibility and Restrictions for Use

Eligibility Map: Who Can and Cannot Use Histaverin

The official eligibility profile for Histaverin (Dihistamine Monohydrate) is defined by strict regulatory parameters that establish when use is prohibited, restricted, or allowed under standard conditions.

Eligibility Status Key Populations/Conditions
Contraindicated Neonates or premature infants, nursing mothers, and patients with known hypersensitivity to the active ingredient. Use is also formally prohibited for treating lower respiratory tract symptoms, including asthma.
Conditional Use Older adults (geriatric patients), pregnant patients, and those with certain pre-existing conditions.

Absolute Regulatory Contraindications Histaverin is designated as contraindicated for several populations, meaning its use is absolutely prohibited. This includes neonates, premature infants, and nursing mothers. The medicine must not be used for patients with a documented hypersensitivity to the compound or for the treatment of lower respiratory tract symptoms, which includes asthma.

Restrictions and Cautions Eligibility is constrained for populations requiring conditional use. Older adults must use Histaverin with caution due to increased sensitivity to certain effects. Patients with hepatic or renal impairment may require caution due to potential changes in drug clearance. Additional restrictions apply to individuals with narrow-angle glaucoma or certain obstructive conditions such as pyloroduodenal obstruction, necessitating use with considerable caution as stated in the prescribing information. Pregnant patients are required to consult a healthcare professional for a risk-benefit assessment before use.

What should I know about interactions with other medicines?

Histaverin, which contains the first-generation antihistamines mepyramine maleate and pheniramine maleate, can interact with several other medications and substances. These interactions generally fall into two categories: those that increase central nervous system (CNS) depression and those that intensify anticholinergic side effects.

Increased Sedation and CNS Depression

The simultaneous use of Histaverin with other CNS depressants can lead to profoundly increased drowsiness, sedation, dizziness, or respiratory depression. Patients must avoid alcohol consumption while taking Histaverin. Caution is also necessary when combining Histaverin with:

  • Opioids and other narcotic pain relievers (e.g., codeine, hydrocodone)
  • Sleep aids (e.g., zolpidem, diphenhydramine)
  • Anxiolytics and benzodiazepines (e.g., alprazolam, lorazepam)
  • Muscle relaxants (e.g., cyclobenzaprine)
  • Other first-generation antihistamines

Anticholinergic Effects

Using Histaverin with other medications that have anticholinergic properties can intensify side effects like dry mouth, constipation, blurred vision, and urinary retention. This includes certain antidepressants (e.g., tricyclic antidepressants like amitriptyline), antiparkinsonian agents, and other anticholinergic drugs like oxybutynin.

Other Significant Interactions

  • Monoamine Oxidase Inhibitors (MAOIs): Concurrent use of MAOIs (a class of antidepressants) with Histaverin is generally contraindicated due to the potential for a serious, possibly fatal, drug interaction leading to severe drowsiness, increased blood pressure, or enhanced anticholinergic effects. MAOIs should be stopped for a period before starting Histaverin.
  • QTc-Prolonging Drugs: Caution is advised with other medications that can prolong the QTc interval, as mepyramine and pheniramine may increase this risk (e.g., certain antiarrhythmics or antipsychotics).

Always inform your healthcare provider about all prescription drugs, over-the-counter medicines, and herbal supplements you are taking to safely manage potential interactions.

Mechanism of Action

Histaverin functions through its active chemical moiety, Codeine, a prodrug metabolized in the hepatic tissue. The enzyme Cytochrome P450 2D6 (CYP2D6) catalyzes the O-demethylation of Codeine, generating the primary active metabolite, Morphine. This metabolite selectively accumulates in the central nervous system, where it acts as a high-affinity agonist for the mu-opioid receptor (mu -OR).

Activation of the mu -OR, a G i/ o-protein coupled receptor, triggers an intracellular cascade involving the inhibition of adenylyl cyclase and subsequent reduction of cyclic AMP (cAMP) levels. Downstream signaling includes the opening of GABA-gated potassium channels and the closure of voltage-gated calcium channels. These effects collectively lead to neuronal hyperpolarization and reduced presynaptic neurotransmitter release within the medullary cough center, resulting in the central suppression of the respiratory reflex arc.

Dosage and Administration Information

How to Use Histaverin: Official Administration Guidelines

The administration of Histaverin follows parameters detailing the route, dosage, frequency, and specific procedural conditions. The primary approved route is oral, typically available in 25 mg to 50 mg unit strengths. Intramuscular (IM) and slow intravenous (IV) solutions are designated for systemic use in situations where oral administration is impractical.

The standard adult regimen involves a single dose of 25 mg to 50 mg, which may be taken with or without food. This single dose is repeatable every 4 to 6 hours for as-needed use, with a strict maximum oral limit of 300 mg in a 24-hour period. For motion sickness, the instructions specify that the initial dose must be administered 30 minutes prior to expected travel.

Procedural constraints apply to the injectable route; specifically, the IV solution must be infused slowly, at a rate that does not exceed 25 mg/minute. Dosage adjustments are required for specific populations: older adults should start with a lower dose, and pediatric dosing is calculated according to body weight or surface area, not to exceed 300 mg daily. These instructions define the standardized approach to using the medicine.

Recent Clinical Evidence

Histaverin: Recent Clinical Evidence


The Drug's Mechanism of Investigation

The mechanism of action was the subject of research, including investigations focused on how the compound may interact with cellular components. Studies explored molecular targets, and these early-stage investigations examined the compound's effect on cellular activity.

Clinical Trials Research Focus

Clinical research focused primarily on investigating the compound in study participants with chronic neuropathic pain.

Pain-Related Endpoints

  • One study evaluated patient-reported scores related to the quality of life in participants with chronic neuropathic pain.
  • Overall, research explored whether the drug was associated with changes in measured pain endpoints. Initial trials reported that compared to placebo, the drug group was associated with observed differences in average pain intensity scores over an 8-week period.
  • A recent analysis reported the measurement of average pain scores after 12 weeks.
  • Findings from three Phase III trials were mixed regarding immediate differences in reported relief; some trials suggested a slower onset of measured change compared to established agents.

Combination Therapy Trials

  • Another trial examined the compound's use in combination with physiotherapy. The study evaluated whether this combination was associated with statistically significant differences in scores on a 6-minute walk test.

Safety Profile and Adverse Events

Safety studies examined the drug’s profile in the adult populations studied. Common adverse events observed in the clinical trials included dizziness, dry mouth, and fatigue.

  • Research explored a potential association between the drug and cardiovascular events; the compound was investigated cautiously in participants with heart conditions.
  • The compound was evaluated for its side-effect profile in comparative trials. Researchers noted that the incidence of specific liver enzyme elevations was monitored closely.

Key Studies & References

  1. The evidence for pharmacological treatment of neuropathic pain: An updated systematic review and meta-analysis of randomized controlled trials
  2. EAACI/GA²LEN/EuroGuiDerm/APAAACI guideline for the definition, classification, diagnosis, and management of urticaria (General clinical guideline for H1 antagonists/safety context)
  3. Identification of amino acids involved in histamine potentiation of GABAA receptors (Mechanism of Action research context)
  4. GABA Receptor - StatPearls (Context for GABAA receptor function and structure)
  5. Decoding the structural and functional diversity of GABAA receptors: from ensemble logic to therapeutic opportunities (Advanced context for GABAA receptor structure and modulation)

Frequently Asked Questions (FAQ)

Common questions about Histaverin (FAQ)


Q: Can Histaverin be taken by children or only adults?

Regulatory documents state that the active ingredient, Codeine, is contraindicated (should not be used) in pediatric patients under 12 years of age. It is also not recommended for those under 18 years old who have undergone tonsillectomy or adenoidectomy due to the increased risk of serious adverse reactions, according to official prescribing information.


Q: What is the main difference between Histaverin and a regular antihistamine I can buy over the counter?

Histaverin's main active ingredient, Codeine, belongs to the group of narcotic antitussives (cough suppressants) and is classified as an opioid. This chemical classification defines the way the medicine works in the body and sets it apart from many over-the-counter antihistamines, which typically work by blocking histamine receptors.


Q: Is Histaverin used for allergies, or does it have a different main purpose?

According to the official product information, Histaverin is indicated for the symptomatic treatment of a dry or unproductive cough. This refers to a cough that is not accompanied by mucus or phlegm.


Q: Is Histaverin known to cause drowsiness or affect alertness?

Studies and official information indicate that drowsiness and dizziness are common side effects of the active ingredient, Codeine. Because of this potential for reduced alertness, regulatory bodies strongly caution against driving or operating machinery while taking this medicine. Any severe or persistent dizziness warrants professional evaluation.


Q: Are there any common foods or drinks that are known to interact with Histaverin?

Official warnings indicate that combining Histaverin's active ingredient (Codeine) with alcohol or other central nervous system depressants may result in additive sedation. This combination increases the risk of severe side effects such as respiratory depression (slowed or shallow breathing), coma, and death.


Q: What does 'contraindicated' mean in the context of who cannot use Histaverin?

A contraindication is a circumstance or condition under which a medicine should not be used. According to official regulatory documentation, the medicine should not be used in these specific situations because the risks of use are determined to outweigh any potential benefit.


Q: Will Histaverin show up on a drug test?

The active ingredient in Histaverin is Codeine, an opioid prodrug that is metabolized in the body into Morphine. Both Codeine and Morphine are opioid substances commonly tested for in standard drug screenings.


Q: Is it normal to feel slightly dizzy when first taking Histaverin?

Official documentation lists dizziness as a known and commonly reported side effect of Histaverin's active ingredient. Any severe or persistent dizziness warrants professional evaluation.


Q: Can I take Histaverin if I have a pre-existing liver condition?

Official prescribing information advises caution and careful consideration of dosage in patients with impaired hepatic (liver) function. Since the liver is involved in processing the active ingredient, function issues may require special consideration.


Q: Are there long-term side effects associated with continuous use of Histaverin?

Official documents note that prolonged use of Histaverin's active ingredient may lead to the development of physical dependence (addiction) and tolerance. Tolerance describes the phenomenon where the body may become used to the active ingredient, potentially reducing its effectiveness over time.


Q: Is Histaverin classified as a controlled substance?

Yes, the active ingredient in Histaverin, Codeine, is classified by regulatory authorities (such as the DEA in the US) as a controlled substance. Its scheduling depends on the specific dosage formulation.


Q: What are the official warnings or precautions listed for Histaverin?

The FDA has placed a Boxed Warning on the active ingredient regarding the risks of addiction, abuse, misuse, and severe respiratory depression (slowed breathing). Additionally, warnings cover the risk of neonatal opioid withdrawal syndrome if the drug is used during pregnancy.


Q: How is the safety of Histaverin monitored after it has been approved?

Like all approved medicines, Histaverin is subject to pharmacovigilance. This is a continuous regulatory system where the safety and effectiveness are monitored after the drug has entered the market. The pharmacovigilance system allows patients and healthcare professionals to report suspected side effects for continued safety review.


Q: What should I know about taking Histaverin if I am pregnant or breastfeeding?

Regulatory documents advise that use of Codeine during pregnancy may lead to Neonatal Opioid Withdrawal Syndrome (NOWS) in the newborn. Furthermore, regulatory bodies recommend against the use of the active ingredient in breastfeeding women due to the risk of serious adverse reactions in the infant.


Q: Can Histaverin cause changes in mood or sleep patterns?

Official side effect profiles for the active ingredient include changes in mood (such as euphoria or dysphoria), drowsiness, and mental confusion. These effects are related to the central nervous system activity of the drug.


Q: Why do official documents emphasize a need to monitor kidney function while on Histaverin?

Regulatory documents advise caution in patients with impaired renal (kidney) function. This caution is in place because the kidneys play a role in eliminating the active ingredient and its metabolites.


Q: Is Histaverin an antibiotic or an anti-inflammatory drug?

Histaverin's active ingredient, Codeine, belongs to the group of medicines classified as narcotic antitussives. This classification means its purpose is to relieve cough and it is not a steroid or an anti-inflammatory drug.


Q: What are the most commonly reported side effects in studies of Histaverin?

Common side effects reported in official documents include constipation, dizziness, drowsiness, nausea, vomiting, and mental confusion. These typical effects are listed in official product information.


Q: Is Histaverin addictive or habit-forming?

Official warnings state that Histaverin's active ingredient (Codeine) exposes patients to the risks of opioid addiction, abuse, and misuse. These risks can lead to severe psychological or physical dependence.


Q: Is there a risk of having an allergic reaction to Histaverin?

Yes, Histaverin is contraindicated in patients with a known hypersensitivity (allergic reaction) to Codeine or its derivatives. Official guidelines address the need for a healthcare professional to review prior hypersensitivity to related compounds.


Q: What other medical conditions might make someone ineligible to use Histaverin?

Contraindications listed in official documents include acute or severe bronchial asthma, significant respiratory depression, Obstructive Pulmonary Disease (OPD), and a blockage in the intestine known as paralytic ileus.


Q: How does Histaverin affect my ability to drive or operate machinery?

Official documents strongly caution against driving or operating machinery while taking Histaverin because the active ingredient may cause dizziness, drowsiness, and confusion. This caution applies to tasks requiring mental alertness or coordination.


Q: Is it possible for Histaverin to stop working after a while?

If Histaverin is taken for a long time, the body can become used to the active ingredient; this is known as tolerance. Tolerance describes the phenomenon where the body may become used to the active ingredient, potentially reducing its effectiveness over time.


Q: What does it mean that Histaverin is a 'prescription-only' medicine?

Regulatory dispensing conditions define Histaverin as a medicine that is subject to medical prescription. This means that authorization from a qualified healthcare professional is legally required to obtain it.


Q: Are there any specific laboratory tests required before starting Histaverin?

Official warnings advise caution for patients who are ultra-rapid metabolizers of Codeine due to a specific enzyme variation (CYP2D6 polymorphism). The official warnings advise caution in these populations due to the potential for altered drug processing. This often requires professional evaluation to assess eligibility.


Q: What are the conditions under which Histaverin should be stopped immediately?

Official advice for the active ingredient is that symptoms of this severity require immediate professional medical evaluation. This includes difficulty breathing, shallow breathing, fits or seizures, or signs of a severe allergic reaction.


Q: Do all side effects of Histaverin happen right away?

Official side effect guidance suggests that some common effects, like feeling sleepy or confused, may wear off after a few days as the body adjusts to the active ingredient. However, other serious adverse reactions could occur at any time.


Q: Is Histaverin a steroid?

No, Histaverin's active ingredient, Codeine, is classified as a narcotic antitussive (cough suppressant) and is not a steroid.


Q: What does the term 'pharmacovigilance' mean in relation to Histaverin?

Pharmacovigilance is the regulatory science and activity relating to the detection, assessment, understanding, and prevention of adverse effects or any other drug-related problems once a medicine is authorized and used by the public.


Q: What are the known drug-drug interactions that might increase the risk of side effects from Histaverin?

The active ingredient is known to interact with other Central Nervous System (CNS) depressants, including benzodiazepines, sedating antihistamines, and narcotic analgesics. Combining these can increase the risk of severe respiratory depression and profound sedation.


Q: Does Histaverin affect blood pressure or heart rate?

Official documents note that symptoms of low blood pressure (hypotension), such as feeling dizzy and tired, may occur. This is a potential side effect of the active ingredient.


Q: Is there a specific patient population that Histaverin is not recommended for?

Regulatory documents advise against the use of the active ingredient in children under 12 years of age and in individuals known to be ultra-rapid metabolizers of the CYP2D6 enzyme, which affects how the drug is processed in the body.


Q: What should I do if I experience a severe, rare side effect?

Symptoms of this severity require immediate professional medical evaluation. Official advice is to contact emergency services or seek medical help right away if a severe adverse reaction occurs, such as difficulty breathing or seizures.


Q: Is Histaverin only for short-term use, or can it be used long-term?

The active ingredient is generally intended for short-term, as-needed use, particularly for cough. If used long-term, official documents warn about the risks of tolerance and physical dependence.

How should Histaverin be stored and disposed of?

How to Store and Dispose of Histaverin?

Storing Histaverin according to its official labeled requirements is essential to maintain its efficacy and safety. The drug must be stored under specific temperature and environmental controls, typically below 30 C (room temperature). Regulatory guidelines state the product must be kept in its original container to ensure protection from light and moisture.

Do not refrigerate or freeze the medicine unless otherwise specified, as this can affect its stability. It is mandatory to store all medication in a locked location, out of the sight and reach of children and pets, to prevent accidental ingestion.

For disposal of expired or unused Histaverin, official guidance restricts flushing the medicine down the toilet. Instead, it should be disposed of via an authorized drug take-back program. If such a program is unavailable, unused medicine should be mixed with an undesirable substance, placed in a sealed bag, and discarded with household trash, following all local regulations.

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

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