MOXONIDINE-WGR

What it is

APO-MOXONIDINE tablets are immediate release film-coated tablets for oral use containing 0.2 mg or 0.4 mg moxonidine. The 0.2 mg tablets are pink round biconvex film coated tablets 5 mm in diameter, and the 0.4 mg tablets are pink round biconvex film coated tablets 7 mm in diameter. The site of the antihypertensive action of moxonidine is the central nervous system. Moxonidine binds to I1-imidazoline receptors and to a lesser extent α2-adrenoreceptors, with its therapeutic action resulting from interaction with I₁ and α2-receptors located within the rostral ventrolateral medulla, leading to reduced activity of sympathetic nerves.

Approved indications

— Treatment of hypertension.

Dosing overview

Treatment should be started with 0.2 mg in the morning. The dose may be titrated after two weeks to 0.4 mg given as one dose or as divided doses (morning and evening) until a satisfactory response is achieved. If the response is still unsatisfactory after a further 2 weeks treatment, the dosage can be increased up to a maximum of 0.6 mg in divided doses (morning and evening). A single daily dose of 0.4 mg and a divided daily dose of 0.6 mg should not be exceeded. In patients with moderate renal impairment (GFR 30–60 mL/min), the single dose should not exceed 0.2 mg and the daily dose should not exceed 0.4 mg.

Key safety warnings

Abrupt cessation of combination therapy with moxonidine and a beta-blocker may result in rebound hypertension. If combination therapy is to be ceased, the beta-blocker should be stopped first and then moxonidine stopped after a few days have elapsed. Cases of varying degrees of atrioventricular block have been reported in the post-marketing setting in patients undergoing moxonidine treatment. Based on case reports, the causative role of moxonidine in delaying atrioventricular conduction cannot be completely ruled out. Caution is recommended when treating patients with a possible predisposition to developing an AV block. Moxonidine should be used with caution in patients with a history of angioneurotic oedema and in patients with severe coronary artery disease and unstable angina. Moxonidine should not be used in cases of intermittent claudication, Raynaud's disease, Parkinson's disease, epileptic disorders, glaucoma, and depression. Due to lack of therapeutic experience, the use of moxonidine concomitantly with alcohol or tricyclic antidepressants should be avoided.

Contraindications

Moxonidine is contraindicated in patients with hypersensitivity to any of the ingredients, heart failure (NYHA Class I–IV), age 75 years or older, bradycardia (HR < 50 beats/minute) or severe bradyarrhythmia including sick sinus syndrome or second or third degree atrioventricular block, malignant arrhythmias, and severe renal impairment (GFR < 30 mL/min, serum creatinine concentration >160 µmol/L).

Regulatory history

MOXONIDINE-WGR was first listed on the ARTG on 2 July 2019, with registrations for both the 0.2 microgram and 0.4 microgram tablet strengths.