LOCAM MR

Indications

• Osteoarthritis
• Rheumatoid arthritis
• Acute pain
• Postoperative pain
• Musculoskeletal disorders

Dosage

Children: Refer to the BNF for Children for specific dosage recommendations for paediatric patients.

Adults: Refer to the BNF for specific dosage recommendations for adults, considering individual patient needs and clinical circumstances.

Mechanism of action

Lornoxicam's anti-inflammatory and analgesic activity is related to its inhibitory action on prostaglandin and thromboxane synthesis through the inhibition of both COX-1 and COX-2. This inhibition leads to a reduction in inflammation, pain, fever, and swelling, mediated by prostaglandins. However, the precise mechanism of lornoxicam has not been fully elucidated.

Pharmacodynamics

Lornoxicam is a potent inhibitor of the cyclooxygenase enzymes (COX-1 and COX-2), which catalyze the formation of prostaglandins and thromboxanes from arachidonic acid. Unlike some other NSAIDs, lornoxicam does not increase leukotriene formation, thus minimizing the risk of adverse events related to the 5-lipoxygenase pathway. Its pharmacodynamic properties allow for effective pain management and reduction of inflammation without significant increases in certain side effects.

Pharmacokinetics

Lornoxicam is absorbed well following oral administration, with peak plasma concentrations typically reached within 2 hours. It has a half-life of approximately 3 to 5 hours, allowing for dosing flexibility. Lornoxicam is metabolized in the liver primarily through conjugation with glucuronic acid. The drug is excreted mainly via the urine, with both unchanged drug and metabolites present in the excreted material.

Adverse effects

• Gastrointestinal ulceration
• Gastrointestinal bleeding
• Nausea
• Vomiting
• Dizziness
• Headache
• Rash
• Renal impairment

Interactions

• Increased risk of gastrointestinal toxicity when used with other NSAIDs or corticosteroids
• May enhance the effects of anticoagulants
• Potential for increased nephrotoxicity when combined with other renal-affecting drugs

Precautions

• Use with caution in patients with a history of peptic ulcer disease
• Monitor renal function in patients with renal impairment
• Caution in patients with cardiovascular disease due to potential fluid retention

Pregnancy

Lornoxicam should be avoided in pregnancy, especially during the third trimester, as it may affect fetal cardiovascular function and prolong gestation.

Breast-feeding

Limited data suggest that lornoxicam is excreted in breast milk; caution is advised when administering to nursing mothers.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Tablets
• Injection

Indications

• Muscle spasms
• Musculoskeletal pain
• Osteoarthritis
• Cervical spondylosis
• Lower back pain

Dosage

Children: Refer to the BNF for Children for specific dosing guidance.

Adults: Refer to the BNF for specific dosing guidance.

Mechanism of action

Thiocholchicoside acts as a muscle relaxant primarily through its central action on the spinal cord and brain, inhibiting the release of excitatory neurotransmitters and modulating the activity of gamma-aminobutyric acid (GABA) receptors. This results in reduced muscle tone and relaxation of spastic muscles.

Pharmacodynamics

The pharmacodynamic effects of thiocholchicoside include muscle relaxation, reduction of spasticity, and analgesic effects. It is believed to exert its effects through the modulation of neural pathways involved in muscle contraction and relaxation, thus providing symptomatic relief from muscle spasms and associated pain.

Pharmacokinetics

Thiocholchicoside is well-absorbed from the gastrointestinal tract and reaches peak plasma concentrations within a few hours after oral administration. It is metabolized in the liver, and its elimination half-life is variable, depending on individual metabolic rates. The drug is primarily excreted in urine, both as unchanged compound and metabolites.

Contra-indications

• Hypersensitivity to thiocholchicoside or any of its excipients
• Severe renal impairment
• Pregnancy

Adverse effects

• Drowsiness
• Dizziness
• Gastrointestinal disturbances
• Allergic reactions
• Muscle weakness

Interactions

• CNS depressants may enhance the sedative effects of thiocholchicoside
• Care should be taken when combining with other muscle relaxants

Precautions

• Use with caution in patients with a history of peptic ulcers
• Monitor patients for signs of respiratory depression
• Caution in elderly patients and those with hepatic impairment

Pregnancy

Thiocholchicoside is contraindicated during pregnancy due to potential risks to the fetus.

Breast-feeding

Thiocholchicoside should be used with caution during breastfeeding, as it is not well studied in lactating women.

Storage

Store in a cool, dry place, away from direct sunlight and moisture.

Formulations

• Oral tablets
• Oral syrup

Mechanism of action

Like other NSAIDS, lornoxicam's anti-inflammatory and analgesic activity is related to its inhibitory action on prostaglandin and thromboxane synthesis through the inhibition of both COX-1 and COX-2. This leads to the reduction of inflammation, pain, fever, and swelling, which are mediated by prostaglandins. However, the exact mechanism of lornoxicam, like that of the other NSAIDs, has not been fully determined.

Pharmacodynamics

Lornoxicam is a non-steroidal anti-inflammatory drug (NSAID) that belongs to the oxicam class. As with other NSAIDS, lornoxicam is a potent inhibitor of the cyclooxgenase enzymes, which are responsible for catalyzing the formation of prostaglandins (act as messenger molecules in the process of inflammation) and thromboxane from arachidonic acid. Unlike some NSAIDS, lornoxicam's inhibition of cyclooxygenase does not lead to an increase in leukotriene formation, meaning that arachidonic acid is not moved to the 5-lipoxygenase cascade, resulting in the minimization of the risk of adverse events.