Does Vertin (betahistine) affect prolactin levels?

Betahistine (Vertin) Does Not Affect Prolactin Levels

Based on the available evidence, betahistine (Vertin) does not appear to affect prolactin levels. The literature does not indicate any relationship between betahistine and prolactin secretion or metabolism.

Mechanism of Action of Betahistine

• Betahistine is a structural analogue of histamine with weak histamine H1 receptor agonist and more potent H3 receptor antagonist properties 1
• It primarily acts on the vestibular system through three main mechanisms:
  • Increases cochlear and vestibular blood flow through H1 receptors 1, 2
  • Enhances histamine synthesis and release in the central nervous system through antagonism of H3 autoreceptors 1
  • Decreases peripheral vestibular input through H3/H4 receptors 2

Clinical Applications and Effects

• Betahistine is primarily used for vestibular disorders such as Ménière's disease and for symptomatic treatment of vertigo 3, 2
• The American Academy of Otolaryngology-Head and Neck Surgery notes that betahistine has shown no significant difference from placebo in reducing vertigo attacks in Ménière's disease patients over a 9-month treatment period 4
• While betahistine affects various physiological systems, there is no evidence in the provided literature suggesting it influences prolactin secretion or metabolism 3, 1, 2

Contraindications and Side Effects

• Betahistine is completely contraindicated in patients with pheochromocytoma 5
• It should be used with caution in patients with asthma and history of peptic ulcer disease 5
• Common side effects include:
  • Cutaneous hypersensitivity reactions (rash, pruritus, urticaria) 3
  • Gastrointestinal complaints (nausea, vomiting, abdominal pain) 3
  • Headache and nasopharyngitis 4
• No adverse effects related to hormonal systems, including prolactin, have been reported in extensive post-marketing surveillance 3

Prolactin Regulation and Medications That Affect It

• Dopamine agonists are the primary medications that reduce prolactin levels, with cabergoline being the dopamine agonist of choice due to its superior effectiveness and lower adverse effect profile 6
• Dopamine agonists normalize prolactin levels in 60-70% of patients with prolactinomas 6
• Betahistine does not have dopamine agonist or antagonist properties that would affect prolactin secretion 1, 2

Important Clinical Considerations

• When evaluating medications for potential effects on prolactin, focus should be on drugs with dopaminergic activity, as dopamine is the primary inhibitor of prolactin secretion 6
• Betahistine's safety profile has been well-established through more than 35 years of worldwide post-marketing surveillance with no reports of prolactin-related effects 3
• If prolactin abnormalities are a concern, medications with known effects on the dopaminergic system should be considered first 6