1,2,4-Trioxolane

Arthromir is used in the treatment of:
Acute and chronic rheumatoid arthritis, osteoarthritis, inflammatory polyarthritis and other forms of arthropathies; Systemic lupus erythematosus;
Arthromir is also used in promoting micro-capillary blood circulation.

Dosage and administration
Arthromir is for both oropharyngeal and topical use depending on the condition for which it is applied.
For oropharyngeal use, the product should be administered as a buccal (sublingual) dose of 50mg contained in 250ul (or 10 drops containing a total of 50mg of 1,2,4-trioxolane), four times a day. Retain the product within the oropharyngeal area for at least five minutes after which it may be swallowed. Avoid taking anything else by mouth for at least 30 minutes following administration. Because one of the principal modes of action of Arthromir is through receptor activation at the oropharyngeal area, the dosage is not directly related to body weight but, rather, to surface area on which the product is acting. Hence, the adult dose is similar to that of children above the age of five years.
For topical use, the product should be applied to the affected area, four times a day. Do not wash the affected area for at least 30 minutes after applying. There is no age restriction for topical use of Arthromir. The product is well tolerated.
In cases of localized topical manifestations or swellings, it is possible to apply the topical preparation on the affected areas and use oropharyngeal preparation simultaneously without inducing toxicity or overdose, and without loss of efficacy.

Contraindications and special precautions
There are no known hypersensitivity reactions to the active substance or to any of the excipients. Unlike other non-steroidal anti-inflammatory products (NSAIDs), Arthromir is safe for use in patients with allergies. In case itching or any other undesirable effect occurs, withdraw the product temporarily (for about 2 days) and thereafter, resume treatment.

Overdose
The window of safety for Arthromir is wide; hence, there is little likelihood of the product inadvertently causing recognized toxicity due to overdose. However, caution should be taken (by taking the recommended dose) in order to limit loss of efficacy that may occur as a result of higher doses than recommended.

Pharmacodynamics and pharmacokinetics
1,2,4-Trioxolane is an endoperoxide derivative of an unsaturated fatty acid. It is metabolized in vivo by cleavage of the endoperoxide ring followed by beta-oxidation of the resulting short chain aliphatic molecules. The molecule is sufficiently lipophilic to be able to cross cell membranes. But due to its ready inactivation in tissues, its site of action is near the site of administration, i.e. the oropharyngeal areas (the buccal cavity) or the skin. The relative ease of inactivation of the molecule confers on it the unique safety margin during its use in therapy.
The therapeutic regimen of 1,2,4-trioxolane represents a special concept in pharmacodynamics whereby small amounts of the agent is administered to initiate a biological response modification which then develops a cascade of reactions through molecular signalling. The pharmacokinetic behaviour of such an agent would not be expected to provide significant levels of the compound and its metabolites in body fluids for detection and especially due to its rapid rate of metabolism and its non-parenteral mode of administration. This is a novel concept in modern pharmacotherapy.

Storage requirements
Arthromir is stable at ambient temperatures (150C-300C). However, the activity progressively reduces as ambient temperatures increase. It is, therefore, recommended to keep the product in a cool dry place, and it is better if refrigerated. It should not be frozen. Keep free from moisture.

Packaging
For oropharyngeal use, Arthromir is presented as 15ml liquid preparation in a squeezable bottle for a 2-week supply. The topical preparation is presented as 60ml unit pack in a squeezable bottle.

Note:
Like all other medications, Arthromir should be kept out of reach of children.

Molecular Technologies Ltd