MOBITIL
Ampoules for I.M. Injection
Anti·lnflammatory, Anti·rheumatlc, Analgesic
COMPOSITION:
Each ampoule (1.5 ml) contains 15 mg meloxicam.
CHEMICAL STRUCTURE:
4·hydroxy·2-methyl-N·(5·methyl·2·thiazolyl)·2H·1,2·benzothiazine·3 carboxamide·1,1·dioxide.
DESCRIPTION:
MOBITIL is a new potent nonsteroidal anti-inflarnmatory drug, belonging to the enolic acid group. It acts through the preferential inhibition of cyclo-oxygenase-Z (COX·2), with polentially high anfi-inflarnrnatory and analgesic actions.
PHARMACOLOGY:
Nonsteroidal anti-inflammatory drugs (NSAIDs) are potent anti-inflammatory agents that act through the inhibition of the cyclo-oxyqenase (COX) enzyme and the subsequent inhibition of prostaglandin synlhesis at the site of inflammation. Recently two isoforms ofthe COX enzyme have been identified; 1· COX·1, which is constitutively (naturally) expressed in many cells and tissues including the gastric mucosa, where the inhibition of COX-1 is responsible forthe toxicity associated with the clinically active NSAIDs. 2· COX·2, which is induced by the proinflammatory cytokines at the site of inflammation, where Ihe anti- inflammatory properties of NSAIDs are caused by the inhibition of inducible COX-2. MOBITIL preferentially inhibits COX·2 enzyme.
PHARMACOKINETICS:
sorptionTts complete after intramuscular administration.
Distribution:
– Plasma protein binding: 99 %.
– Steady state plasma concentration: Achieved within 3-5 days with a 15 mg single daily dose.
Metabolism:
Meloxicam is extensively metabolized in the liver, with only traces of the drug appearing unchanged in the urine and feces. The main metabolites are formed by hydroxylation and further oxidation of the methyl group ofthe thiazolyl moiety.
Excretion:
Meloxicam is excreted through both renal and hepatic pathways. The excretion of a single dose is complele in 5 days .
– Elimination half life (t 11,): 17·20 hours .
– Total plasma ciearance (CL): 0.42· 0.481iter I hour.
The pharmacokinetic parameters of meloxicam are Iinearoverthe dose range of 7.5·30 mg. Neither moderate hepatic insufficiency nor moderate renal dysfunction has any relevant effects on the pharmacokinetics of meloxicam.ln terminal renal failure, the volume of distribution is increased and a daily dose of7.5 mg must not be exceeded.
INDICATIONS:
* Symptomatic treatment of acute exacerbations of inflammatory and degenerative rheumatic diseases, such as
rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis.
* Post-traumatic and post-operative pain, inflammation and swelling.
* Painful syndromes of the vertebral column.
Painful and/or inflammatory conditions in gynecology such as primary dysmenorrhea or adnexitis. Painful and/or inflammatory conditions in dentistry.
CONTRAINDICATIONS AND PRECAUTIONS:
* Hypersensitivily to the oxicam group ofNSAIDs.
* Use with caution in patients known to be hypersensitive to other NSAIDs or aspirin as there is a probability for cross sensitivity. Active peptic ulcer.
* Severe hepatic insufficiency.
* Severe, non-dialyzed renal insufficiency.
* Pregnancy and breast·feeding.
ADVERSE REACTIONS:
The following adverse reactions were infrequently reported:
* CNS: Headache, drowsiness, tinnitus.
* GIT: Dyspepsia, nausea, flatulence, diarrhea or constipation.
* Cardiovascular: Peripheral edema.
* Dermatological: Pruritus, skin rash.
DOSAGE AND ADMINISTRATION:
* One 15 mg injection once a day. The injections must be administered slowly by deep intramuscular injection in the upper outer quadrant of the buttock. In case of repeated administration, it is recommended to altemate left and right side. In case of hip prosthesis, the injection should be performed on the other side.
* In dialysis patients with severe renal failure: the dose should not exceed 7.5 mg per day (half an 1.5 ml ampoule).
HOWSUPPLIED:
Box containing three 1.5 ml-ampoUfesOfl5 mg meloxicao
OTHER DOSAGE FORMS AVAILABLE:
MOBITIL Tablets: Box containing 10 tablets of either 7.5 mg or 15 mg meloxicam.
MOBITIL Suppositories: Box containing 6 suppositories of 15 mg meloxicam.
Keep out of reach of children. To be used under medical supervision.
PRODUCT OF:
Medical Union Pharmaceuticals,
Abu-Sultan, Ismailia, Egypt
