Source: Pharmaceutical Benefits Scheme (AU) Revision Year: 2020 Publisher: Johnson & Johnson Pacific, AUSTRALIA NEW ZEALAND, 45 Jones Street, Ultimo NSW 2007, Registered Trademark Consumer Care Centre Australia: 1800 029 979, New Zealand: 0800 446 147, Overseas Customers: +61 ...
ZYRTEC eye drops contain levocabastine, a potent, fast-acting and highly selective histamine H1-antagonist with a sustained duration of action. After topical application to the eyes, it almost immediately and for several hours relieves the typical symptoms of allergic conjunctivitis (itching, redness, chemosis, eyelid swelling, tearing).
ZYRTEC nasal spray contains levocabastine, a potent, fast-acting and highly selective histamine H1-antagonist with a sustained duration of action. After topical application to the nose, it almost immediately and for several hours relieves the typical symptoms of allergic rhinitis (sneezing, itchy nose, rhinorrhoea).
Clinical studies have shown that ZYRTEC eye drops and nasal spray are effective for the indications listed above. The duration of treatment with the eye drops alone was generally 2-4 weeks but lasted up to 3 months in two studies and 4 months in one study. Duration of treatment with the nasal spray alone was also generally 2-4 weeks, but lasted up to 10 weeks in some instances. The duration of treatment in studies using a combination of the eye drops and nasal spray was 8 weeks.
After intranasal and ocular application, the absorption of levocabastine is incomplete with a systemic bioavailability ranging from 60 to 80% for the nasal spray and from 30 to 60% for the eye drops. However, as the amount of levocabastine applied intranasally and ocularly is small, the levocabastine plasma concentrations achieved are very low. Steady-state concentrations of levocabastine are attained within 7 to 10 days following multiple dosage and are predictable from single-dose pharmacokinetics
After single intravenous dosing, levocabastine is rapidly distributed over the tissues, and the terminal half-life is 33 h. The total steady-state volume of distribution is 82 L (1.14 L/kg) with a total plasma clearance of 30 mL/min.
The plasma protein binding of levocabastine is 55% with albumin being the main binding protein.
Levocabastine undergoes minimal hepatic metabolism, i.e. ester glucuronidation, and is predominantly cleared by the kidneys. 70% of the parent drug is recovered unchanged in the urine, and 10% of the dose is excreted in the urine as the acylglucuronide of levocabastine. The remaining 20% is excreted unchanged in the faeces.
No data available
In female mice, dietary administration of levocabastine for 20 months stimulated the development of pituitary adenomas and mammary adenocarcinomas. The no-effect dose level for the pituitary tumours was 3 mg/kg/day, but a no-effect dose level has not been established for the mammary tumours. In female rats, there was an equivocal increase in the incidence of mammary tumours at the highest dose level of 34 mg/kg/day administered in the diet for 24 months. There was no evidence of carcinogenic activity in male rats or mice. The mechanism of the carcinogenic effects of levocabastine in female mice (and possibly rats) may involve antagonism of dopamine D2-receptors in the pituitary gland and subsequent elevation of serum prolactin levels.
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