Consumer medicine information

1 Name of Medicine

Modafinil.

2 Qualitative and Quantitative Composition

Modafinil-WGR (modafinil) is a wakefulness-promoting agent for oral administration.
Modafinil-WGR (modafinil) tablet contains 100 mg of modafinil.
Excipients with known effect. Contains sugars as lactose.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Modafinil-WGR tablet is white to off-white colour, capsule shape, biconvex, uncoated tablets with 'L233' debossed on one side and plain on other side.

4 Clinical Particulars

4.9 Overdose

Symptoms. A small number of individuals have each taken modafinil at doses of 1000 mg/day (2.5 times the maximum recommended daily dose of 400 mg) or more. The adverse experiences observed were limited, expected and non-life threatening, and the patients recovered fully by the following day. The adverse experiences included excitation or agitation, insomnia and slight or moderate elevations in haemodynamic parameters. No specific organ toxicities were observed. Other observed high dose effects in clinical studies have included anxiety, irritability, aggressiveness, confusion, nervousness, tremor, palpitations, sleep disturbances, nausea, diarrhoea and decreased prothrombin time.
Death has occurred with modafinil overdose alone or in combination with other drugs.
Symptoms accompanying modafinil overdose, alone or in combination with other drugs, have included: insomnia; central nervous system symptoms such as restlessness, disorientation, confusion, agitation, anxiety, excitation and hallucination; digestive changes such as nausea and diarrhea; and cardiovascular changes such as tachycardia, bradycardia, hypertension and chest pain.
Management. Management of overdosage is primarily symptomatic, as no specific antidote to the toxic effects of modafinil overdose has been identified. Overdoses should be managed empirically, with supportive care, including cardiovascular monitoring.
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

Genotoxicity. There was no consistent evidence for genotoxic activity of modafinil in in vitro assays of gene mutation (reverse mutation in S. typhimurium and E. coli, forward mutation in Chinese hamster V79 fibroblasts) or in the chromosomal damage assay (human lymphocytes in vitro, Chinese hamster bone marrow cells in vivo, mouse micronucleus assay). Modafinil did not increase unscheduled DNA synthesis in rat hepatocytes. In a cell transformation assay in BALB/3T3 mouse embryo cells, modafinil did not cause an increase in the frequency of transformed foci in the presence or absence of metabolic activation.
Carcinogenicity. Carcinogenicity studies were conducted in which modafinil was administered in the diet to mice for 78 weeks and to rats for 104 weeks at doses up to 60 mg/kg/day. The highest dose studied in these studies would have achieved systemic exposure levels less than human exposure at the maximum recommended dose. There was no evidence of tumourigenesis associated with modafinil administration in these studies; however, the carcinogenic potential of modafinil has not been fully evaluated.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Modafinil is a racemic compound and the chemical name is 2-[(diphenylmethyl)sulfinyl] acetamide. The molecular formula is C₁₅H₁₅NO₂S and the molecular weight is 273.35.
Modafinil is a white to off-white, crystalline powder that is practically insoluble in water and cyclohexane. It is sparingly to slightly soluble in ethanol and acetone.
Chemical structure.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSMODEFI.gif CAS number. 68693-11-8.

7 Medicine Schedule (Poisons Standard)

Prescription Only Medicine (S4).

Summary Table of Changes

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