Consumer medicine information

Notes

Distributed by Alphapharm Pty Limited

1 Name of Medicine

Rabeprazole sodium.

2 Qualitative and Quantitative Composition

Each enteric coated (EC) tablet contains 10 mg rabeprazole sodium (equivalent to 9.42 mg rabeprazole) or 20 mg rabeprazole sodium (equivalent to 18.85 mg rabeprazole), as the active ingredient.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Rabeprazole Mylan 10 mg are pink, round, biconvex delayed release tablets plain on both sides.
Rabeprazole Mylan 20 mg are yellow, round, biconvex delayed release tablets, plain on both sides.

4 Clinical Particulars

4.9 Overdose

Symptoms. Experience to date with deliberate or accidental overdose is limited. The maximum established exposure has not exceeded 60 mg twice daily, or 160 mg once daily. Effects are generally minimal, representative of the known adverse event profile, and reversible without further medical intervention.
Treatment. No specific antidote is known. Rabeprazole sodium is extensively protein bound and is therefore not readily dialysable. As in any case of overdose, treatment should be symptomatic and general supportive measures should be used.
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Note. In the following section, the relative exposure levels in animals have been calculated using a human dose of 20 mg/day, the maximum recommended rabeprazole dose for the treatment of GORD and active gastro-duodenal ulcers. For H pylori eradication, the recommended dose of rabeprazole is 40 mg/day (20 mg b.i.d.) for one week; this should be taken into account when reviewing exposure figures.
Genotoxicity. Rabeprazole was positive in assays for gene mutations (the AMES test, forward gene mutation tests in Chinese hamster ovary cells (CHO/HGPRT) and mouse lymphoma cells (L5178Y/TK+/-)). Its demethylated-metabolite was also positive in the AMES test. Rabeprazole was negative in assays for chromosomal damage (the in vitro Chinese hamster lung cell chromosome aberration test, the in vivo mouse micronucleus test), and in vitro and ex vivo rat hepatocyte unscheduled DNA synthesis (UDS) tests.
Carcinogenicity. In an 88/104 week carcinogenicity study in CD-1 mice, rabeprazole at oral doses up to 100 mg/kg/day did not produce any increased tumour occurrence. The highest tested dose produced a systemic exposure to rabeprazole (AUC) of 1.40 microgram.hr/mL which is 1.6 times the human exposure at the recommended dose for GORD (20 mg/day).
In a 104-week carcinogenicity study in SD rats, males were treated with oral doses of 5, 15, 30 and 60 mg/kg/day and females with 5, 15, 30, 60 and 120 mg/kg/day. Rabeprazole produced gastric enterochromaffin-like (ECL) cell hyperplasia in male and female rats and ECL cell carcinoid tumours in female rats at all doses. The lowest dose (5 mg/kg/day) produced a systemic exposure to rabeprazole (AUC) of about 0.1 microgram.hr/mL which is about 0.1 times the human exposure at 20 mg/day. In male rats, no treatment-related tumours were observed at doses up to 60 mg/kg/day producing a rabeprazole plasma exposure (AUC) of about 0.2 microgram.hr/mL (0.2 times the human exposure at 20 mg/day).

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Rabeprazole sodium is a substituted benzimidazole and belongs to the class of proton pump inhibitors. Its solubility in water is pH dependent, being very soluble in water at pH 9 to 11, and only slightly soluble in water at pH 8. It is very soluble in methanol, freely soluble in dichloromethane and practically insoluble in hexane. Rabeprazole has one chiral centre and is a racemate of two enantiomers.
Chemical structure.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSRABSOD.gif Chemical name: (±) 2-[{4-(3-methoxypropoxy)-3-methylpyridin-2-yl}-methylsulphinyl]-1H-benzimidazole sodium.
Molecular formula: C₁₈H₂₀N₃NaO₃S.
Molecular weight: 381.43.
CAS number. CAS-117976-89-3 (rabeprazole); CAS-117976-90-6 (rabeprazole sodium).

7 Medicine Schedule (Poisons Standard)

S4 - Prescription Only Medicine.

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/RABMYLST.gif