Consumer medicine information

1. Why am I using VARENAPIX?

VARENAPIX contains the active ingredient varenicline tartrate. VARENAPIX is used to help adults stop smoking. For more information, see Section 1. Why am I using VARENAPIX? in the full CMI.

2. What should I know before I use VARENAPIX?

Do not use if you have ever had an allergic reaction to varenicline tartrate or any of the ingredients listed at the end of the CMI.
Talk to your doctor if you have any other medical conditions, take any other medicines, or are pregnant or plan to become pregnant or are breastfeeding.
For more information, see Section 2. What should I know before I use VARENAPIX? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with VARENAPIX and affect how it works. Furthermore, the effects of changes in your body resulting from stopping smoking, with or without VARENAPIX, may alter the way some medicines work.
A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use VARENAPIX?

Your doctor will decide with you on how to use VARENAPIX to quit smoking. There are 3 ways to quit smoking with VARENAPIX. To take VARENAPIX, you start with the white 0.5 mg tablet and then increase the dose up to the blue 1 mg tablet. More instructions can be found in Section 4. How do I use VARENAPIX? in the full CMI.

5. What should I know while using VARENAPIX?

6. Are there any side effects?

Common side effects of VARENAPIX include: stomach or bowel problems (e.g. nausea), dry mouth, toothache, headache, dizziness, sleep problems, signs and symptoms of a cold, change in appetite, weight gain, changes in taste, muscle or joint pain. Other serious side effects have also been reported: convulsions, vision problems or pain in eyes, blood in stools or vomit, stomach pain, excessive thirst, dry mouth and skin, passing large amounts of urine, changes in behaviour, thinking or mood, severe skin issues, allergic reactions, heart related issues.
For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

1 Name of Medicine

Varenicline tartrate.

2 Qualitative and Quantitative Composition

Each 0.5 mg film coated tablet contains 0.855 mg varenicline tartrate, equivalent to 0.5 mg varenicline.
Each 1 mg film coated tablet contains 1.71 mg varenicline tartrate, equivalent to 1 mg varenicline.
For the full list of excipients see Section 6.1 List of Excipients.

3 Pharmaceutical Form

1 mg tablets. Blue coloured, modified capsule-shaped, biconvex, film coated tablets, engraved with "APO" on one side and "VAR" over "1" on the other side.
0.5 mg tablets. White coloured, modified capsule-shaped, biconvex, film coated tablets, engraved with "APO" on one side and "VAR" over "0.5" on the other side.

4 Clinical Particulars

4.9 Overdose

No cases of overdose were reported in pre-marketing clinical trials.
In case of overdose, standard supportive measures should be instituted as required.
Varenicline has been shown to be dialysed in patients with end stage renal disease (see Section 5.2 Pharmacokinetic Properties); however, there is no experience in dialysis following overdose.
For information on the management of overdose, contact the Poisons Information Centre on 131 126 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Varenicline had no genotoxic effects, with or without metabolic activation, based on the following assays: Ames bacterial mutation assay; mammalian CHO/HGPRT assay; and tests for cytogenic aberrations in vivo in rat bone marrow and in vitro in human lymphocytes.
Carcinogenicity. Carcinogenicity studies were performed in mice and rats at respective oral doses of varenicline up to 20 mg/kg/day and 15 mg/kg/day for 2 years, with respective systemic drug exposure (C_max) up to 130 and 50 times the human plasma C_max at the maximal recommended dose of 1 mg twice daily. There was no evidence of carcinogenicity in mice or female rats. Male rats showed increased incidences of hibernoma (a rare tumour of brown fat) at systemic exposures of 25 times the human C_max (incidence 1/65 rats) and 50 times the human C_max (incidence 2/65 rats); the no effect exposure was 10 times the human C_max. The clinical relevance of this finding has not been established.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Varenicline tartrate powder is a white to off-white to slightly yellow solid. It is highly soluble in water. The pKa (ionisation constant) for varenicline is 9.2. The octanol-water partition coefficient (Log D) of varenicline tartrate is -1.23 at pH 5, -0.817 at pH 7 and 0.758 at pH 9.
Chemical structure. Structural formula:
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSVARTAR.gif Chemical name: 7,8,9,10-tetrahydro-6,10-methano-6H-pyrazino [2,3-h] [3] benzazepine, (2R,3R)-2,3-dihydroxybutanedioate (1:1).
Molecular formula: C₁₃H₁₃N₃.C₄H₆O₆. Molecular weight: 361.35 Daltons.
CAS number. 375815-87-5.

7 Medicine Schedule (Poisons Standard)

S4 - Prescription Only Medicine.

Summary Table of Changes

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