Betaserc

Betaserc 16 mg is a round, biconvex, scored, white to almost white tablet with beveled edges. On the one side, the tablet is scored and the number 267 is engraved on either side of the score line. This tablet is for oral administration (to be taken by mouth) and contains 16 mg of betahistine dihydrochloride. The tablet can be divided into equal halves to create two doses of 8 mg each.
Betaserc 24 mg is a round, biconvex, scored, white to almost white tablet with beveled edges. On the one side, the tablet is scored and the number 289 is engraved on either side of the score line. This tablet is for oral administration (to be taken by mouth) and contains 24 mg of betahistine dihydrochloride.
The purpose of the scoreline is only to facilitate breaking for ease of swallowing and does not divide the tablet into equal doses.
Excipients/Inactive Ingredients: Microcrystalline cellulose, mannitol (E421), citric acid monohydrate, colloidal anhydrous silica and talc.

Pharmacotherapeutic group: Anti-vertigo preparations.
Pharmacology: Pharmacodynamics: The following is detailed description of how the active ingredients of Betaserc work. For further explanations, patients must be advised to consult the doctor.
The mechanism of action of betahistine is only partly understood. There are several plausible hypotheses that are supported by animal studies and human data: Betahistine affects the histaminergic system: Betahistine acts both as a partial histamine H₁-receptor agonist and histamine H₃-receptor antagonist also in neuronal tissue, and has negligible H₂-receptor activity.
Betahistine increases histamine turnover and release by blocking presynaptic H₃-receptors and inducing H₃-receptor downregulation.
Betahistine may increase blood flow to the cochlear region as well as to the whole brain: Pharmacological testing in animals has shown that the blood circulation in the striae vascularis of the inner ear improves, probably by means of a relaxation of the precapillary sphincters of the microcirculation of the inner ear. Betahistine was also shown to increase cerebral blood flow in humans.
Betahistine facilitates vestibular compensation: Betahistine accelerates the vestibular recovery after unilateral neurectomy in animals, by promoting and facilitating central vestibular compensation; this effect, characterized by an up-regulation of histamine turnover and release, is mediated through H₃-receptor antagonism. In human subjects, recovery time after vestibular neurectomy was also reduced when treated with betahistine.
Betahistine alters neuronal firing in the vestibular nuclei: Betahistine was also found to have a dose dependent inhibiting effect on spike generation of neurons in lateral and medial vestibular nuclei.
The pharmacodynamic properties as demonstrated in animals may contribute to the therapeutic benefit of betahistine in the vestibular system.
The efficacy of betahistine was shown in studies in patients with vestibular vertigo and with Ménière's disease as was demonstrated by improvements in severity and frequency of vertigo attacks.
Pharmacokinetics: The following is a detailed description of how the active ingredients of Betaserc are metabolized by the body. For further explanations, patients must be advised to consult the doctor.
Absorption: Orally administered betahistine is readily and almost completely absorbed from all parts of the gastrointestinal tract. After absorption, the drug is rapidly and almost completely metabolized into 2-pyridylacetic acid. Plasma levels of betahistine are very low.
Pharmacokinetic analyses are therefore based on 2-PAA measurements in plasma and urine.
Under fed conditions C_max is lower compared to fasted conditions. However, total absorption of betahistine is similar under both conditions, indicating that food intake only slows down the absorption of betahistine.
Distribution: The percentage of betahistine that is bound by blood plasma proteins is less than 5%.
Biotransformation: After absorption, betahistine is rapidly and almost completely metabolized into 2-PAA (which has no pharmacological activity). After oral administration of betahistine, the plasma (and urinary) concentration of 2-PAA reaches its maximum 1 hour after intake and declines with a half-life of about 3.5 hours.
Excretion: 2-PAA is readily excreted in the urine. In the dose range between 8 and 48 mg, about 85% of the original dose is recovered in the urine. Renal or fecal excretion of betahistine itself is of minor importance.
Linearity: Recovery rates are constant over the oral dose range of 8-48 mg indicating that the pharmacokinetics of betahistine are linear, and suggesting that the involved metabolic pathway is not saturated.

Ménière's syndrome as defined by the following triad of core symptoms: vertigo (with nausea/vomiting); hearing loss (hardness of hearing); tinnitus.
Symptomatic treatment of vestibular vertigo.

The dosage for adults is 24-48 mg divided over the day.
Swallow the tablets whole with some liquid during or after meals.
The dosage should be individually adapted according to the response. Improvement can sometimes only be observed after a couple of weeks of treatment. The best results are sometimes obtained after a few months.
There are indications that treatment from the onset of the disease prevents the progression of the disease and/or the loss of hearing in later phases of the disease.
Children and adolescents: Betahistine is not recommended for the treatment of children and adolescents in the age range 0-18 years. No studies are available on efficacy and safety in this age group.
Elderly population: Only limited data from clinical studies are available for this patient group. Betahistine should be used with caution in this patient group.
Renal insufficiency: There are no specific clinical studies for this patient group. Dose adjustment cannot therefore be recommended for these patients.
Hepatic insufficiency: There are no specific clinical studies for this patient group. Dose adjustment cannot therefore be recommended for these patients.

Symptoms of overdose: A few overdose cases have been reported. Some patients experienced mild to moderate symptoms such as nausea, sleepiness and abdominal pain with doses up to 640 mg. More serious complications including convulsions, and lung and heart complications were observed in cases of intentional overdose of Betaserc, especially when taken in combination with other overdosed drugs.
Treatment of overdose: No specific antidote is known. Treatment of overdose should include standard supportive measures.

Betaserc should not be taken if the patient is allergic (hypersensitive) to the active substance or to any of the excipients or if the patient suffers from an adrenal gland tumor known as a phaeochromocytoma.

If the patient suffers from bronchial asthma or has a history of stomach (peptic ulcer), the patient will need to be monitored carefully while taking this medication.
Effect on ability to drive and use machines: According to clinical trials, Betahistine has no or negligible effect on the ability to drive or use tools or machinery.
However, remember that the disease for which the patient is treated with Betaserc (Morbus Meniere or vertigo) can make the patient feel dizzy or sick, and can affect the ability to drive and use machines.

Patients must be advised by the doctor or pharmacist before taking any medicine during pregnancy.
Pregnancy: Not enough information is available with regard to the use of Betaserc in pregnant women. Animal studies are also insufficient with respect to effects on pregnancy, embryonal/foetal development, giving birth and postnatal development. The potential risk for humans in this regard is unknown. The patient should not take betahistine during pregnancy unless it is deemed clearly necessary by the doctor.
Lactation: It is not known whether betahistine is excreted in human milk. There are no animal studies on the excretion of betahistine in milk. The patient should not take Betaserc if she is nursing unless advised by the doctor. For further information, she must be advised to talk to the doctor regarding the importance of this medicine, the benefits of nursing and the potential risks to the child.
Fertility: Animal studies did not show effects on fertility on rats.

Like all medicines, Betaserc may have side effects. If the patient notices any side effects not mentioned in this monograph, or if any of the side effects get serious, they must be advised to inform the doctor or pharmacist.
The following undesirable effects have been experienced with the following indicated frequencies in Betaserc-treated patients in placebo-controlled clinical trials: common (between 1 and 10 cases in 100 treated patients).
Gastrointestinal disorders: Common: nausea and indigestion (dyspepsia).
Nervous system disorders: Common: headache.
In addition to those events reported during clinical trials, the following undesirable effects have been reported spontaneously during postmarketing use and in scientific literature. A frequency cannot be estimated from the available data and is therefore classified as "not known".
Immune system disorders: Allergic (hypersensitivity) reactions, including a serious allergic reaction (anaphylaxis) which can cause: a red or lumpy skin rash or inflamed itchy skin; swelling of face, lips, tongue or neck; a drop in blood pressure; loss of consciousness; difficulty breathing.
Gastrointestinal disorders: Mild gastric complaints (e.g., vomiting, gastrointestinal pain, abdominal distension and bloating). These can normally be dealt with by taking the dose during meals or by lowering the dose.
Skin and subcutaneous tissue disorders: Allergic reactions of the skin or tissues under the skin, in particular a sudden onset of face, neck or limb swelling (angioneurotic oedema), hives (urticaria), rash and itchiness (pruritus).
If any of the side effects get serious, or if the patient notices any side effects not listed in this monograph, they must be advised to inform the doctor or pharmacist.

Patients must be advised to inform the doctor or pharmacist if they are taking or have recently taken any other medicines including medicines obtained without a prescription.
No interaction studies on living subjects (in vivo) have been performed. Based on laboratory (in vitro) data, no inhibition of Cytochrome P450 enzymes is expected in living subjects.
If the patient is taking monoamine-oxidase inhibitors [MAOIs, including MAO subtype B (e.g., selegiline)], which are used to treat depression or Parkinson's disease, they must be advised to inform the physician, as these medicines may increase the exposure of Betaserc.
As betahistine is similar in structure to histamine, interaction of betahistine with antihistamines may affect the efficacy of one of these drugs. Patients must be advised to inform the doctor if they are taking an antihistamine before taking Betaserc.

Incompatibilities: Not applicable.
Any unused product or waste material should be disposed of in accordance with local requirements.
The information in this monograph is limited. For further information, patients must be advised to contact the doctor or pharmacist.

Store in the original package in order to protect from light.

Antivertigo Drugs / Peripheral Vasodilators & Cerebral Activators

N07CA01 - betahistine ; Belongs to the class of antivertigo preparations.

P₁S₁S₃