Diclofenac / Thiocolchicoside

BRANDS

Dynapar MR, Troikaa Pharmaceuticals Ltd


Thiocolchicoside Chemical Structure: Thiocolchicoside in Kenya
Thiocolchicoside Chemical Structure
Diclofenac in Kenya
Diclofenac Chemical Structure

MODE OF ACTION

Diclofenac is a non-steroidal anti-inflammatory drug (NSAID)that exhibits antiinflammatory, analgesic, and antipyretic activities.
The mechanism of action of diclofenac, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetase inhibition.

Thiocolchicoside is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive GABAA receptor antagonist and also glycine receptor antagonist with similar potency and nicotinic acetylcholine receptors to a much lesser extent.

INDICATIONS

Painful musculoskeletal conditions associated with muscle spasm like lumbar and sciatic pain, persistent torticollis, post-traumatic pain, etc

CONTRAINDICATIONS

Diclofenac
Diclofenac is contraindicated in patients with known hypersensitivity to diclofenac.

Diclofenac should not be given to patients who have experienced asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions have been reported in such patients

Diclofenac is contraindicated for the treatment of post-operative pain in the setting of coronary artery bypass graft (CABG) surgery.

Thiocolchicoside.

Flaccid paralysis, muscle hypotonus, confirmed individual Hypersensitivity to Thiocolchicoside.

DRUG INTERACTIONS

Diclofenac

Aspirin :
When diclofenac is administered with aspirin, its protein binding is reduced. The clinical significance of this interaction is not known; however, as with other NSAIDs, concomitant administration of diclofenac and aspirin is not generally recommended because of the potential of increased adverse effects.

Methotrexate :

NSAIDs could enhance the toxicity of methotrexate. Caution should be used when NSAIDs are administered concomitantly with methotrexate.

Cyclosporine :
Diclofenac, like other NSAIDs, may affect renal prostaglandins and increase the toxicity of certain drugs. Therefore, concomitant therapy with diclofenac may increase cyclosporine’s nephrotoxicity. Caution should be used when diclofenac is administered concomitantly with cyclosporine.

ACE Inhibitors :
Reports suggest that NSAIDs may diminish the antihypertensive effect of ACE inhibitors. This interaction should be considered in patients taking NSAIDs concomitantly with ACE inhibitors.

Furosemide :
Diclofenac can reduce the natriuretic effect of furosemide and thiazides in some patients. This response has been attributed to inhibition at renal prostaglandin synthesis. During concomitant therapy With NSAIDs, the patient should be observed closely for signs of renal failure, as well as to assure diuretic efficacy.

Lithium :
NSAIDs have produced an elevation of plasma lithium levels and a reduction in renal lithium clearance. The mean minimum lithium concentration increased by 15% and the renal clearance was decreased by approximately 20%. These effects have been attributed to inhibition of renal prostaglandin synthesis by the NSAID. Thus, when NSAIDs and lithium are administered concurrently, subjects should be observed for signs of lithium toxicity.

Warfarin :
The effects of warfarin and NSAIDs on GI bleeding are synergistic, such that users of both drugs together have a risk of serious GI bleeding higher than users of either drug alone.

Thiocolchicoside

None known

ADVERSE EFFECTS :

Diclofenac

In patients taking diclofenac, or other NSAIDs, the most frequently reported adverse experiences occurring in approximately 1 %-10% of patients are :

Gastrointestinal experiences including abdominal pain, constipation, diarrhea, dyspepsia, flatulence, gross bleeding/perforation, heartburn, nausea, GI ulcers (gastric/ duodenal), and vomiting.

Abnormal renal function, anemia, dizziness, edema, elevated liver enzymes, headaches, increased bleeding time, pruritus, rashes, and tinnitus.

Additional adverse experiences reported occasionally include:

Body as a Whole: fever, infection, sepsis

Cardiovascular System: congestive heart failure, hypertension, tachycardia, syncope

Digestive System: dry mouth, esophagitis, gastric/peptic ulcers, gastritis, gastrointestinal bleeding, glossitis, hematemesis, hepatitis, jaundice

Hemic and Lymphatic System :
ecchymosis, eosinophilia, leukopenia, melena, purpura, rectal bleeding, stomatitis, thrombocytopenia

Metabolic and Nutritional :
weight changes

Nervous System :
anxiety, asthenia, confusion, depression, dream abnormalities, drowsiness, insomnia, malaise. nervousness, paresthesia, somnolence, tremors, vertigo

Respiratory System :
asthma, dyspnea

Skin and Appendages :
alopecia, photosensitivity, sweating
increased

Special Senses :
blurred vision

Urogenital System: cystitis, dysuria, hematuria, interstitial nephritis, 0liguria/polyuria, proteinuria, renal failure

Other adverse reactions, which occur rarely are:

Body as a whole:
anaphylactic reactions, appetite changes, death

Cardiovascular System :
arrhythmia, hypotensive, myocardial infarction, palpitations, vasculitis
Digestive System: colitis, eructation, liver failure, pancreatitis

Hemic and Lymphatic System: agranulocytosis, hemolytic anemia, aplastic anemia, lymphadenopathy, pancytopenia

Metabolic and Nutritional: hyperglycemia

Nervous System: convulsions, coma, hallucinations. meningitis Respiratory System: respiratory depression, pneumonia

Skin and Appendages: angioedema, toxic epidermal necrolysis, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, urticaria

Special Senses: conjunctivitis. hearing impairment

Thiocolchicoside

In rare cases, diarrhea, gastric pain, and heartburn have been reported after oral administration. Although rarely, a decrease in blood pressure, temporary loss of consciousness (blurred conscious), or excitation can be seen. Infrequent cases of skin rash or erythema have been reported.

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