Artoxan (Suppositories rectal)

(Tenoxicam)

 

CONTENT:

Rectal suppositories containing tenoxicam 20 mg. 

 

PHARMACOLOGICAL PROPERTIES:

PHARMACODYNAMICS. Artoxan is effective non-steroid anti-inflammatory drug (NSAID) with potent anti-inflammatory, analgesic and less expressed antipyretic action. Properties of the preparation are determined by inhibition of both cyclooxygenase enzyme isoforms that leads to decrease in metabolism of the arachidonic acid and blockade of prostaglandin synthesis.

The anti-inflammatory effect is determined by reduction of capillaries permeability (limits exudation), stabilization of lysosomal membranes (prevents the exit of lysosomes enzymes, causing tissue damage), suppression of synthesis or inactivation of inflammation mediators (prostaglandins, histamine, bradykinin, lymphokins, comlement factors). It reduces the quantity of free radicals in the center of inflammation, supresses chemotaxis and phagocytosis. Inhibits the proliferative phase of inflammation, reduces post-inflammatory sclerosis of tissues; renders chondroprotective action. The preparation reduces painful sensitivity in the center of inflammation and has the effect on thalamic centers of pain, possesses desensitizing action (at long application). At rheumatic diseases weakens the pain in joints at rest and at movement, reduces morning constraint and swelling of joints, improves functions and increases volume of movements of joints.

 

PHARMACOKINETICS. 

Bioavailability in case of rectal administration is 80 %. Cmax is reached within 2 hours. İn single administration of 20-40 mg maximal plasma concentrations of 2-4 mg/l are reached. Plasma concentrations in steady state is 11 mg/l, it is reached 10-12 days following everyday application of 20 mg tenoxicam once daily. 

Distribution volume is 0.15 l/kg, half-life period is 60-75 hours. 

Tenoxicam easily penetrates into synovial fluid of osteoarthritis or  rheumatoid

arthritis patients. İt is transformed in liver with formation of non-active metabolites. 2/3 of administered dose is excreted with urine, 1/3 with faeces.

 

THERAPEUTIC INDICATIONS:

Inflammatory-degenerative diseases of the musculoskeletal system, accompanied by pain syndrome:

-  articular syndrome in gout, rheumatoid arthritis, osteoartritis, ankylosing spondylitis, osteochondrosis, articular rheumatism (tendinitis, bursitis, myositis); - back pain, neuralgia, myalgia, ishalgia; - algodysmenorea.

CONTRAINDICATIONS:

-  Hypersensitivity to tenoxicam or other NSAID;

-  Erosive or ulcerative lesions of GIT;

-  Gastroenteric bleedings;

-  significant renal or hepatic disturbances;

-  diabetes mellitus;

-  arterial hypertension, heart failure, oedema; - pregnancy, lactation.

 

SIDE EFFECTS:

From digestive system: dyspepsia (nausea, vomiting, epigastric burning, diarrhea, flatulence),  pains and unpleasant feelings in stomach, stomatitis, anorexia, in long-term administration and in excessive dosage – erosive and ulcerative damages of gastrointestinal tract.

 

From nervous system and sense organs: headache, dizziness, depression, nervousness.

Allergic reactions: itching, urticaria, erythema, syndromes of Stevens-Johnson's and Lyell's.

Others: hepatic dysfunction, increase of creatinine, nitrogen, bilirubin and urea concentration in plasma, increase of "hepatic" transaminases activity, CT prolongation, local irritation.

DOSAGE AND ADMINISTRATION:

For rectal administration. 

It is usually prescribed in the dose of 20 mg once a day, in one and the same time of the day. In acute gouty arthritis – 40 mg once daily during 2 days, then 20 mg once daily during 5 days.

 

PACKAGING:

5 rectal suppositories in a strip. 

1 strip with a leaflet in a carton box.