Moxonidine belongs to a class of medicines called antihypertensives, which are used to lower blood pressure. It is indicated for the treatment of high blood pressure (hypertension).
Moxonidine
Generic MedicinePharmacology
In animal studies, Moxonidine has been shown to be a relatively potent antihypertensive agent. Experimental data suggest that its primary site of action is the central nervous system (CNS). It selectively binds to I1 imidazoline receptors and to a lesser extent to α2-adrenoceptors. Its antihypertensive effect is mainly due to stimulation of I1 receptors in the rostral ventrolateral medulla, which reduces sympathetic nervous system activity. Unlike other centrally acting antihypertensives, Moxonidine has a low affinity for α2-adrenoceptors, which are mainly responsible for side effects such as sedation and dry mouth. In humans, it reduces systemic vascular resistance, leading to a decrease in arterial blood pressure.
Dosage Administration
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.
Interactions
Concomitant use of Moxonidine with other antihypertensive drugs may enhance its blood pressure–lowering effect. The sedative effects of tricyclic antidepressants, tranquilizers, alcohol, sedatives, hypnotics, and benzodiazepines may be increased when used with Moxonidine. It may also moderately impair cognitive function when taken with lorazepam. Since tricyclic antidepressants may reduce the effect of centrally acting antihypertensives, co-administration with Moxonidine is not recommended. Moxonidine is excreted via tubular secretion; therefore, interactions with other drugs eliminated by the same pathway cannot be ruled out.
Contraindications
- Hypersensitivity to any component of the product.
- Sick sinus syndrome.
- Bradycardia (resting heart rate <50 beats/min).
- Second- and third-degree AV block.
- Cardiac insufficiency.
Side Effects
- Asthenia, headache, pain, abdominal pain,
- back pain,
- dizziness, dry mouth, somnolence, vertigo.
Pregnancy & Lactation
Pregnancy Category B3. There is insufficient data in pregnant women. Animal studies have shown embryotoxic effects; therefore, Moxonidine should not be used during pregnancy unless the potential benefit clearly outweighs the risk to the fetus. It is excreted in breast milk, so it should not be used during breastfeeding. Breastfeeding should be discontinued if treatment is necessary.
Precautions & Warnings
Abrupt discontinuation of combination therapy with beta-blockers may cause rebound hypertension. In such cases, the beta-blocker should be withdrawn first, followed by Moxonidine after a few days. Blood pressure should be monitored during withdrawal.
Cases of AV block have been reported; caution is required in patients with possible risk. It should not be used in higher-degree AV block. In first-degree AV block, careful monitoring is needed to avoid bradycardia.
Use with caution in renal impairment as the drug is primarily excreted by the kidneys; dose adjustment is required. Patients with rare hereditary problems of galactose intolerance, lactose deficiency, or glucose-galactose malabsorption should avoid this medicine.
Therapeutic Class
Anti-hypertensive
Storage Conditions
Do not store above 25°C. Keep away from light and moisture. Keep out of reach of children.
Common Questions
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Can Moxonidine be taken during pregnancy?