Moxonidine

Moxonidine belongs to a group of drugs called anti-hypertensives that lower blood pressure. Moxonidine is used to treat high blood pressure.

In different animal models, Moxonidine has been shown to be a relatively potent antihypertensive agent. Available experimental data suggest that the site of the antihypertensive action of Moxonidine is the central nervous system (CNS). Moxonidine has been shown to bind to I1 imidazoline receptors and to a lesser extent a2-adrenoreceptors. The therapeutic action of Moxonidine appears to result from interaction with I1 receptors located within the rostral ventrolateral medulla, leading to a reduced activity of sympathetic nerves. Moxonidine differs from other available centrally acting antihypertensives by exhibiting only low affinity to central a2-adrenoceptors compared to I1 imidazoline receptors; a2-adrenoceptors are considered the molecular target via which sedation and dry mouth, the most common side effects of centrally acting antihypertensives, are mediated. In humans, Moxonidine leads to a reduction of systemic vascular resistance and consequently in arterial blood pressure.

Treatment should be started with 200 micrograms in the morning. The dose may be titrated after three weeks to 400 micrograms given as single dose or as divided daily doses (morning and evening) until a satisfactory response is achieved. If the response is still unsatisfactory after a further 3 weeks treatment, the dosage can be increased up to a maximum of 600 micrograms in divided doses (morning and evening). A single dose of 400 micrograms and a daily dose of 600 micrograms of Moxonidine should not be exceeded. Moxonidine may be taken with or without food.

Concurrent administration of moxonidine and other antihypertensive agents enhances the hypotensive effect of Moxonidine. The sedative effect of tricyclic antidepressants, tranquilizers, alcohol, sedatives, hypnotics and benzodiazepines can be potentiated by Moxonidine. Moxonidine moderately augmented the impaired performance in cognitive functions in subjects receiving lorazepam. Since tricyclic antidepressants may reduce the effectiveness of centrally acting antihypertensive agents, it is not recommended that tricyclic antidepressants be co-administered with Moxonidine. Moxonidine is excreted through tubular excretion. Interaction with other agents that are excreted through tubular excretion cannot be excluded.

• Hypersensitivity to any component
• Sick sinus syndrome
• Bradycardia (resting heart rate <50 beats/minute)
• AV-block 2nd and 3rd degree
• Cardiac insufficiency

• Asthenia, Headache, Pain, Abdominal Pain
• Back Pain
• Dizziness, Dry mouth, Somnolence, Vertigo

Pregnancy Category: B3. There is inadequate data for use of moxonidine in pregnant women. Embryotoxicological effects have shown in animals that moxonidine should not be used during pregnancy unless the benefit clearly justifies the possible risks to the foetus. Moxonidine is secreted in breast-milk and should therefore not be used during breast-feeding. Breast-feeding should be stopped if therapy with Moxonidine is considered necessary.

Cessation of combination therapy with beta-blockers: Abrupt cessation of combination therapy with Moxonidine and a beta-blocker may result in rebound hypertension. If combination therapy with Moxonidine and a beta-blocker is to be ceased, the beta-blocker should be stopped first and then Moxonidine stopped after a few days. During cessation of therapy blood pressure should be regularly monitored.

Atrioventricular block: Cases of varying degrees of AV block have been reported in the post-marketing setting in patients undergoing Moxonidine treatment. Based on these case reports, the causative role of Moxonidine in delaying atrioventricular conduction cannot be completely ruled out. Therefore, caution is recommended when treating patients with a possible predisposition to developing an AV block. When Moxonidine is used in patients with 1st degree AV block, special care should be exercised to avoid bradycardia. Moxonidine must not be used in higher degree AV blocks.

Caution is advised in the administration of moxonidine to patients with renal impairment as moxonidine is excreted primarily via kidney. Careful titration of the dose is recommended in patients with renal impairment, specially at the start of therapy.

Patients with rare hereditary problems of galactose intolerance, total lactose deficiency or glucose galactose malabsorption should not take this medicinal product.

Anti-hypertensive

Do not store above 25°C temperature. Keep away from light and wet place. Keep out of reach of children.