VALOID

What it is

Valoid is a cyclizine lactate injection containing 50 mg cyclizine lactate per 1 mL ampoule. Valoid injection is a clear, colourless solution for injection. Cyclizine is a histamine H1 receptor antagonist of the piperazine class. It possesses anticholinergic and antiemetic properties.

Approved indications

— Prevention of nausea and vomiting in the post-operative period.

Dosing overview

The adult dose is 50 mg intravenously up to three times daily. For the prevention of postoperative nausea and vomiting, administer the first dose by slow intravenous injection 20 minutes before the anticipated end of surgery. Treatment with Valoid should commence within the first 24 hours of surgery and should not continue beyond 48 hours. When used intravenously, Valoid should be injected slowly into the bloodstream, with only minimal withdrawal of blood into the syringe.

Key safety warnings

Cyclizine has anticholinergic effects and may precipitate pre-existing conditions that are likely to be exacerbated by anticholinergic activity, such as urinary retention or obstruction, hepatic disease, phaeochromocytoma, hypertension, epilepsy, prostatic hypertrophy, angle-closure glaucoma, untreated intraocular hypertension, or uncontrolled primary open-angle glaucoma. Cyclizine should be administered cautiously in patients with asthma or chronic obstructive pulmonary disease. Nervous system side effects of cyclizine have included drowsiness and sedation in many patients, motor skills may be impaired, and cyclizine may also cause restlessness, excitation, nervousness and insomnia. Extrapyramidal effects may occur and dystonic reactions have been reported after single doses of cyclizine. There have been case reports of paralysis occurring in patients using intravenous cyclizine, some of whom had an underlying neuromuscular disorder. Thus intravenous cyclizine should be used with caution in all patients in general, and in patients with underlying neuromuscular disorders in particular.

Contraindications

Valoid should not be given to individuals with known hypersensitivity to cyclizine or to any of the excipients. Valoid should not be given to patients who have severe heart failure or acute myocardial infarction, as in such patients cyclizine may cause a fall in cardiac output associated with increases in heart rate, mean arterial pressure and pulmonary wedge pressure. Valoid should not be given to patients who have acute alcohol intoxication, as the anti-emetic properties of cyclizine may increase the toxicity of alcohol.

Regulatory history

Valoid was approved by the TGA on 13 June 2012 and registered on the ARTG on 19 June 2012. The TGA approved Valoid injection for the prevention of nausea and vomiting in the post-operative period for intravenous administration only, with intramuscular use not recommended due to insufficient biopharmaceutic data. The TGA approved Valoid injection as a new chemical entity for intravenous use, noting that initial quality concerns regarding product monitoring and stability were resolved, and while nonclinical studies were not robust by current standards, the extensive clinical history of cyclizine was considered.