TOPRELOC-XL

What it is

TOPRELOC-XL is a modified release tablet containing metoprolol succinate, available in strengths of 23.75 mg, 47.5 mg, 95 mg and 190 mg. TOPRELOC-XL is recommended for once daily treatment and is preferably taken together with the morning meal.

Approved indications

— Stable, chronic heart failure as an adjunct to other heart failure therapy.

Dosing overview

The dose of TOPRELOC-XL should be individually adjusted in patients with chronic heart failure stabilised on other heart failure treatment, with patients titrated from an initial low dose. Patients typically start with TOPRELOC-XL 23.75 mg (half or one tablet daily for two weeks), then TOPRELOC-XL 47.5 mg once daily for two weeks, then TOPRELOC-XL 95 mg once daily for two weeks. During long term treatment the aim should be to reach TOPRELOC-XL 190 mg once daily (or the highest tolerated dose). Patients with moderate to severe heart failure (NYHA III-IV) should start treatment with half a TOPRELOC-XL 23.75 mg tablet once daily for one week, then take a full TOPRELOC-XL 23.75 mg tablet once daily for the second week. Dose adjustment is not needed in the elderly.

Key safety warnings

TOPRELOC-XL should not be ceased abruptly due to the risk of rebound hypertension and tachycardia, and if treatment is to be discontinued, it should be reduced gradually. If there is a need to discontinue treatment with TOPRELOC-XL, this should be done gradually over at least two weeks with the dose reduced by half in each step, down to a final dose of half a 23.75 mg tablet, and the final dose should be taken for at least four days before discontinuation. Some patients may experience an initial, usually transient, worsening of the symptoms and signs of heart failure when starting treatment with TOPRELOC-XL, and if this occurs, the patient should be monitored very closely and the dose of TOPRELOC-XL should be reduced if symptoms continue to worsen. Beta-blockers are contraindicated in any patient with a history of airways obstruction or a tendency to bronchospasm. TOPRELOC-XL should be used with caution in patients with diabetes mellitus, especially those receiving insulin or oral hypoglycaemic agents, as beta-blockers affect glucose metabolism and may mask some important premonitory signs of acute hypoglycaemia such as tachycardia, and the dose of insulin or oral hypoglycaemic agent may need to be adjusted.

Contraindications

Beta-blockers are contraindicated in any patient with a history of airways obstruction or a tendency to bronchospasm, as beta-adrenergic blockade may result in increased airways resistance, and even cardioselective beta-blockers can result in severe bronchospasm. Contraindications include allergic disorders (including allergic rhinitis) which may suggest a predisposition to bronchospasm, right ventricular failure secondary to pulmonary hypertension, significant right ventricular hypertrophy, second and third degree atrioventricular block, shock (including cardiogenic and hypovolaemic shock), and unstable decompensated congestive heart failure (pulmonary oedema, hypoperfusion or hypotension). Continuous or intermittent inotropic therapy acting through beta-receptor agonism, clinically relevant sinus bradycardia (less than 45–50 beats/minute), and non-compensated congestive heart failure are contraindicated. Sick-sinus syndrome (unless a permanent appropriately functioning pacemaker is in place), severe peripheral arterial circulatory disorders, suspected acute myocardial infarction with specific haemodynamic parameters, hypotension, and untreated phaeochromocytoma are contraindicated. Hypersensitivity to any component of TOPRELOC-XL and related derivatives is contraindicated.

Regulatory history

TOPRELOC-XL was first registered on the ARTG on 4 March 2022, with all four strengths (23.75 mg, 47.5 mg, 95 mg and 190 mg modified release tablets) listed simultaneously.