Overview

Atmoxicam-TH comprises of Lornoxicam and Thiocolchicoside is used in pain and relax the muscle due to muscle spasm. Lornoxicam is a new non steroidal anti-inflammatory medication of the oxicam class with analgesic and antipyretic properties which works by blocking the release of certain chemical messengers that cause pain and inflammation (redness and swelling). Thiocolchicoside is a GABA-A antagonist,semi-synthetic colchicoside(natural compound) derivative, A centrally acting muscle relaxant. It works on the centres in the brain and spinal cord to relieve muscle stiffness or spasm and to improve pain and movement of muscles.

Indications

• Muscle pain and Mu sculo skeletal pain.
• Low back pain.
• Post operative pain
• Arthritis. [Osteo & Rhumatoid Arthritis].
• Ankylosing spondylitis.
• Acute Sciatica.

Pharmacology

PHARMACODYNAMIC PROPERTIES OF LORNOXICAM

LORNOXICAM inhibits prostaglandin biosynthesis by blocking the enzyme Cyclo- oxygenase. It inhibits both isoforms in the same concentration range,that is, Balanced COX-1 Inhibition & COX-2 inhibition through that it's a safest pain killer. It is distinguished from established oxicams by a relatively short elimination half-life (3 to 5 hours), which may be advantageous from a tolerability standpoint. The absolute bioavailability of Lornoxicam is 90-100% and no firstpass effect was observed.

PHARMACODYNAMIC OF THIOCOLCHICOSIDE

Thiocolchicoside is usually classified along with nonsteroidal anti-inflammatory drugs (NSAID), Like all drugs of this class, its main mechanism of action is the inhibition of Cyclo oxygenase (COX). Thiocholchicoside is a muscle relaxing agent that works through selective binding to the GABA-A receptor. It prevents muscle contractions by activating the GABA inhibitory motor pathway. It acts as a competitive GABA receptor antagonist and inhibits glycine receptors with similar potency as nicotinic acetylcholine receptors

PHARMACOKINETICS PROPERTIES OF LORNOXICAM

Bioavailability : 90-100%
Distribution : 99% bound to plasma proteins.
Metabolism : Metabolism by Cytochrome P450
Biological half-life : 3-4 hours
Excretion: 2/3 hepatic, 1/3 renal

PHARMACOKINETICS OF THIOCOLCHICOSIDE

Absorption: Well absorbed.
Distribution:The binding of thiocolchicoside to human serum proteins is low (13%) and serum albumin is mainly involved in serum protein binding.
Metabolism: It is metabolized in the 3 main metabolites. Firstly, in the intestines to 3-demethylcolchicine (inactive metabolite). This product is further metabolized in circulation by either conjugation to 3-O-glucurono-demethylcolchicine (active metabolite) or demethylated to didemethylcolchicine (inactive metabolite).
Excretion: It is mainly excreted in feces (79%) while urinary excretion represents only 20%.

Side Effects

Nausea

Diarrhoea

Discomfort

Allergy

Contraindications

This is contraindicated in patients with peptic ulceration, salicylate sensitivity, gastrointestinal bleeding, severe renal and liver impairment; pregnancy and lactation.

Drug Interactions

Increased Lornoxicam blood concentration was observed when given concomitantly with cimetidine. Enhanced effects of anticoagulants, sulfonylureas, methotrexate, ciclosporin, digoxin. Decreased effects of diuretics, ACE inhibitors.

Precautions

PREGNANT AND LACTATING WOMEN: Pregnant and lactating women should take this medication only under the prescription of the physician.