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Betahistine (Betaserc)

Betahistine, marketed under the brand name Betaserc, is a medication primarily used to treat symptoms of Ménière’s disease, a disorder of the inner ear characterized by vertigo, tinnitus, and hearing loss. It is a histamine analog that improves blood flow in the inner ear and reduces pressure in the endolymphatic system. This article provides a detailed overview of betahistine (Betaserc), referencing authoritative sources such as the British National Formulary (BNF)Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology. We will explore its mechanism of action, uses, dosage, side effects, precautions, drug interactions, and generic names in pharmacy.

Betahistine exerts its therapeutic effects through multiple mechanisms:

  1. Histamine H1 Receptor Agonism:
    • Stimulates H1 receptors in the inner ear, leading to vasodilation and improved microcirculation in the cochlea and vestibular system (BNF).
  2. Histamine H3 Receptor Antagonism:
    • Blocks H3 receptors, increasing the release of endogenous histamine and further enhancing blood flow (Lippincott).
  3. Reduction of Endolymphatic Pressure:
    • Improves fluid drainage in the endolymphatic sac, reducing pressure and alleviating symptoms like vertigo and tinnitus (Lange).
  4. Central Vestibular Compensation:
    • Enhances the brain’s ability to adapt to vestibular imbalances, improving balance and reducing dizziness (Lippincott).

Betahistine is primarily indicated for:

  1. Ménière’s Disease:
    • Reduces the frequency and severity of vertigo attacks.
    • Alleviates tinnitus and hearing loss associated with the condition.
  2. Other Vestibular Disorders:
    • Used off-label for vertigo and dizziness caused by other inner ear conditions, such as vestibular neuritis or labyrinthitis.
  3. Symptomatic Relief:
    • Improves balance and reduces nausea in patients with chronic vestibular dysfunction.

The dosage of betahistine varies depending on the condition being treated. Always follow the prescribing physician’s instructions.

Adults:

  • Ménière’s Disease: 16–48 mg daily in divided doses (BNF).
    • Typical starting dose: 8 mg 3 times daily, adjusted based on response.

Elderly Patients:

  • Use lower doses initially, as they may be more sensitive to side effects.

Administration Tips:

  • Take with or after meals to minimize gastrointestinal side effects.
  • Do not crush or chew the tablets; swallow them whole with water.

Betahistine is generally well-tolerated, but some patients may experience side effects:

Common:

  • Gastrointestinal: Nausea, indigestion, bloating.
  • Headache or dizziness.
  • Mild skin rash or itching.

Rare but Serious:

  • Severe allergic reactions (anaphylaxis).
  • Worsening of asthma or peptic ulcer disease (due to histamine-like effects).

Before using betahistine, inform your healthcare provider if you have:

  • A history of peptic ulcers or gastrointestinal bleeding.
  • Asthma or other respiratory conditions.
  • Pheochromocytoma (a rare adrenal gland tumor).
  • Allergies to betahistine or any component of the formulation.

Special Populations:

  • Pregnancy: Use only if benefits outweigh risks (BNF Category: Not formally established; caution advised).
  • Breastfeeding: Limited data; avoid unless essential.
  • Elderly Patients: Monitor for dizziness or gastrointestinal side effects.

Betahistine may interact with other medications, altering their effects:

  1. Antihistamines:
    • May reduce the efficacy of betahistine by blocking H1 receptors.
  2. Monoamine Oxidase Inhibitors (MAOIs):
    • Concurrent use may increase the risk of hypertensive crises.
  3. Anticholinergics:
    • May counteract the vestibular benefits of betahistine.
  4. Antihypertensives:
    • Betahistine’s vasodilatory effects may enhance blood pressure-lowering effects.

Generic Names in Pharmacy

  • Betahistine dihydrochloride (active ingredient)

Common brand names: Betaserc®, Serc®, Vasomotal®

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