Betahistine is a medication primarily prescribed to treat vertigo, Meniere's disease, and other inner ear conditions. It is known for its ability to reduce dizziness, nausea, vomiting, and symptoms related to changes in inner ear pressure. While betahistine is not primarily intended for weight management, its effects on histaminergic pathways have led to investigations into its potential role in appetite regulation and weight control, particularly in the context of antipsychotic-induced weight gain.
Understanding Betahistine
Betahistine hydrochloride acts as both a histamine receptor H1 (HRH1) agonist and a histamine receptor H3 (HRH3) antagonist. The histaminergic neuronal system plays a role in appetite regulation. HRH1 is a postsynaptic receptor observed in the periventricular nucleus and the ventromedial hypothalamus. HRH3 is an inhibitory autoreceptor believed to regulate the secretion of histamine and other neurotransmitters.
Betahistine and Appetite Regulation: Clinical Studies
Several studies have explored the effects of betahistine on appetite and food intake.
Study Design and Methodology
One study was a proof-of-concept, randomized, double-blinded, placebo-controlled, dose-ranging study performed to examine the effects of betahistine in women with class I or II obesity [body mass index (BMI; in kg/m2) of 30-39.99]. After a 24-h placebo run-in period, subjects received a placebo (n = 19) or 48 (n = 19), 96 (n = 17), or 144 (n = 21) mg betahistine/d for 24 h. Treatment was followed by a buffet test meal to assess energy intake. Hunger, satiety, and desire to eat were measured after consuming the meal by using visual analog scales. Data were analyzed by using regression models with the assumption that there would be an increasing effect of betahistine doses.
Results and Findings
The results of the study indicated that betahistine did not produce a significant effect on food intake or appetite in the studied group of obese women. Specifically, the betahistine dose did not significantly change intakes from those observed during the run-in period of the buffet test meal (P = 0.78). The study involved 79 obese women with a mean age of 42 ± 11 years and a BMI of 35 ± 3, with 76 completing the study. The conclusion drawn was that more potent histaminergic modulators may be required to elucidate the possible role of histaminergic pathways in human obesity.
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Implications
Despite some evidence from animal models suggesting that betahistine could reduce food intake, the clinical study did not find a similar effect in humans. This suggests that the histaminergic pathways involved in appetite regulation may be more complex than initially understood, and that betahistine, at the tested doses, may not be potent enough to produce a significant effect on appetite and food intake in obese women.
Betahistine and Weight Gain Associated with Antipsychotic Medications
Weight gain is a common side effect of certain antipsychotic medications, particularly second-generation antipsychotics like olanzapine and clozapine. These medications can lead to decreases in histaminergic transmission in the brain, which may contribute to weight gain. Betahistine has been investigated as a potential adjunctive treatment to mitigate this weight gain.
Clinical Trial
A double-blind, placebo-controlled study evaluated the effects of 12 weeks of treatment with betahistine (N = 29) or placebo (N = 22) in adolescents and adults on anthropomorphically measured weight-related parameters, appetite, and fasting glucose-lipid and leptin levels in 51 patients treated with first and/or second-generation antipsychotics who had gained weight during treatment or had high body-mass-index (BMI).
Outcomes
In a subgroup of patients being treated with olanzapine or clozapine (n = 26), betahistine was significantly (P < .05) better than placebo in preventing increases in weight (3.1 kg less weight gain than placebo), BMI, and waist circumference. However, betahistine did not decrease weight or BMI in patients treated with other antipsychotics, nor did it have a significant effect on preventing weight or BMI gain in the total combined sample of all subjects. Additionally, betahistine did not significantly improve appetite or glucose-lipid measures in either subgroup.
Conclusion
The results suggest that betahistine may be a useful adjunctive drug for decreasing weight gain in patients treated with antipsychotics that are potent histamine antagonists, such as olanzapine or clozapine, but may not be useful for this purpose in patients on other antipsychotic medications.
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Side Effects of Betahistine
While betahistine is generally well-tolerated, it can cause side effects in some individuals.
Common Side Effects
Some of the common side effects of betahistine include:
- Migraines
- Gas formation
- Bloating
- Acid reflux
- Nausea
- Vomiting
Most of these side effects are minor and tend to resolve on their own.
Less Common and Acute Side Effects
In rare cases, betahistine may cause allergic reactions or more severe side effects, such as:
- Skin rashes
- Irritation or itchiness on the skin
- Abdominal pain
- Swelling of oral parts (e.g., tongue, gums, lips)
Precautions and Contraindications
Certain individuals should exercise caution or avoid taking betahistine. These include:
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- People with breathing conditions or respiratory problems (e.g., asthma, bronchitis, COPD)
- Pregnant or breastfeeding women
- People with hepatic problems or liver conditions (e.g., hepatitis, cirrhosis)
It is crucial to inform your doctor about your complete medical history, including any prior illnesses or conditions, before starting betahistine.
Betahistine: Dosage and Administration
Betahistine is typically taken orally, and the dosage varies depending on the individual and the condition being treated. It is essential to follow the doctor's instructions regarding dosage and administration.
Betahistine and Vertigo
Vertigo is a condition characterized by extreme dizziness, loss of balance, and unsteadiness. It can be caused by changes in inner ear pressure, deposits of crystals in the inner ear, or other factors. Betahistine is often prescribed to alleviate the symptoms of vertigo by improving blood flow to the inner ear and reducing pressure.
Clinical studies indicate that the main causes for the incidence of vertigo can be (1) a significant change in the pressure levels inside your ears, (2) deposit of crystals inside the otolith area of your ears and (3) a few other reasons such as scaling / climbing tall structures, etc. In most cases of vertigo, changes in pressure stands out as a lead cause for adverse signs such as feeling dizzy, ringing in ears (or, tinnitus), a marked decrease in your ability to hear ambient sounds, etc. However, the incidence of vertigo owing to other causes cannot be ruled out. In a few instances, deposits of inner-ear crystals may get dislodged and may get inside the deeper canals of your ear. You can make these crystals get resorbed through a set of movements. These are essentially manoeuvres of head / body and neck. These movements have the backing of the academy of neuro sciences, a nodal agency based in the US.
Important Considerations
- Prescription Requirement: Betahistine is typically available only with a prescription from a doctor.
- Self-Medication: It is dangerous to take betahistine without consulting a healthcare professional.
- Medical Supervision: Betahistine should always be taken under the guidance of a doctor.
- Weight Management: Betahistine is not be used as an anti-obesity medication.