Brands of Diclofenac / Paracetamol / Chlorzoxazone Combination in Kenya
Admol MR, Troikaa Pharmaceuticals Limited
Dafenac MR, Dawa Limited
Diclosara-MR ,Krishna Chemists Ltd
Doloact-MR ,Ochoa Laboratories Ltd
Flamacor MR , Coral Laboratories Ltd
Flamcheck MR, Indoco Remedies Limited
Flamoryl-S, Household Pharmaceuticals Ltd
Lobak, Geno Pharmaceuticals Pvt. Ltd
Lofnac MR, Bliss GVS Pharma Ltd.
Mobyle-SP, Lincoln Pharmaceuticals Ltd
Powergesic MR, Jenburkt Pharmaceuticals Ltd
Track-MR, National Pharmacy Ltd
Trifast MR, PSM Pharmaceuticals Ltd
Diclofenac is a non-steroidal compound, a phenylacetic acid derivative, with analgesic antipyretic and anti-inflammatory effects. Diclofenac inhibits the biosynthesis and release of prostaglandins, which are known to be implicated in the pathogenesis of inflammation, pain, and fever. Absorption occurs in the gastrointestinal tract to give peak plasma concentrations approximately 2 hours after ingestion There is at least 99% binding to plasma proteins and excretion of metabolites is mainly in the urine.
Paracetamol has analgesic and antipyretic effects similar to those of Aspirin. However, it has no anti-inflammatory effect and does not share the antirheumatic properties of the salicylates. It is rapidly and practically completely absorbed from the gastrointestinal tract. The concentration in plasma reaches a peak in 30 to 60 minutes and the plasma half-life is about 2 hours after therapeutic doses. It is distributed into most body tissues. It crosses the placenta and is present in breast milk.
Chlorzoxazone is a centrally acting muscle relaxant. Chlorzoxazone acts primarily at the level of the spinal cord and subcortical areas of the brain where it inhibits multisynaptic reflex arcs involved In producing and maintaining skeletal muscle spasm of varied etiology. Chlorzoxazone is rapidly absorbed from the gastrointestinal tract, It is metabolized to 6-hydroxychlorzoxazone and then eliminated in the urine.
For the relief of rheumatism, rheumatoid arthritis. ankylosing spondylitis. osteoarthritis. painful postoperative and post-traumatic Inflammation and swelling and dysmenorrhoea and as an adjunct to physical therapy in the treatment of partial musculoskeletal disorders.
Sensitivity to any of the ingredients.
It is s contra-indicated in patients with known hypersensitivity to diclofenac and in patients who respond to aspirin and aspirin-type drugs with sensitivity reactions like asthma, acute rhinitis, and urticaria.
Diclofenac is contraindicated in patients with peptic ulceration or a history of such ulceration and should be used with caution in patients with renal or hepatic insufficiency.
Dosage over those (recommended by the Physician may cause liver damage. Patients suffering from liver or kidney disease should take Paracetamol only under medical supervision. Consult your doctor If no relief is obtained from the recommended dosage.
Do not use continuously for more than 10 days without consulting your doctor.
DOSAGE AND DIRECTIONS FOR USE:
Usual Adult Dose:0ne tablet three times daily, with or after meals or as directed by the Physician.
For muscle spasm: one tablet 3 or 4 times daily. The initial dosage for severe muscle spasm should be 2 tablets three or four times daily.
SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Diclofenac: Gastro-intestinal disorders including epigastric pain. eructation, nausea, and vomiting may occur. Peptic ulceration and gastrointestinal bleeding have been reported.
Other side effects include vertigo. headache, skin rashes pruritis, tinnitus, depression, drowsiness, nervousness. insomnia, irritability, agitation, minor hearing disorder, edema, palpitations blurred vision and other ocular reactions
Hypersensitivity reactions may occur and include fever and rashes.
Diclofenac may cause cystitis and haematuria as well as acute renal failure, interstitial nephritis, and nephrotic syndrome.
Other adverse effects include anemia. thrombocytopenia, neutropenia, eosinophilia, agranulocytosis, and abnormalities in liver function tests. Patients with congestive heart failure, cirrhosis, diuretic-induced volume depletion, or renal insufficiency are at greater risk of developing renal dysfunction.
Skin rashes and other allergic reactions may occur occasionally. The rash is usually erythematous or urticarial but sometimes more serious and may be accompanied by drug fever and mucosal lesions.
In a few cases, the use of Paracetamol has been associated with the occurrence of thrombocytopenia, neutropenia. pancytopenia. leucopenia and agranulocytosis. The dose should be reduced in renal functional impairment.
Paracetamol should also be given with care to patients taking other drugs that affect the liver such as the barbiturates.
The absorption of Acetaminophen (Paracetamol) may be accelerated by Metoclopramide. Excretion may be affected and plasma concentrations altered when administered with Probenecid.
Prolonged excessive use may cause irreversible kidney damage.
Occasional patients may develop gastrointestinal disturbances. It is possible, in rare instances. that chlorzoxazone may have been associated with gastrointestinal bleeding.
Drowsiness,nausea,dizziness. lightheadedness, malaise, or overstimulation may be noted by an occasional patient. Rarely, allergic-type skin rashes, petechiae, or ecchymoses may develop during treatment. Angioneurotic edema and anaphylactic reactions are extremely rare.
Rarely, a patient may note discoloration of the urine resulting from a phenolic metabolite of chlorzoxazone.
It should be used with caution in patients with known allergies or with a history of allergic reactions to medicines. If a sensitivity reaction occurs such as urticaria, redness, or itching of the skin. the medicines should be stopped.
If any signs or symptoms suggestive of liver dysfunction are observed the medicine should be discontinued.
Plasma concentrations are significantly decreased by the concomitant administration of therapeutic doses of Aspirin.
When given together with preparations containing lithium or digoxin, Diclofenac may raise their plasma concentrations.
Concomitant administration of glucocorticoids or other non-steroidal anti-inflammatory agents may aggravate gastro-intestinal Side effects.
Concurrent administration with two or more non-steroidal anti-inflammatory agents may promote the occurrence of side effects.
Should be used with caution in patients with asthma.
Use with care in elderly patients.
KNOWN SYMPTOMS 0F OVERDOSAGE AND PARTICULARS OF ITS TREATMENT
Treatment of overdose should be symptomatic and supportive and may include the following
1. Induce vomiting or perform gastric lavage.
2. Administer activated charcoal.
3. Antacids may relieve adverse gastrointestinal effects.
4. Nephritis or nephrotic syndrome, thrombocytopenia, hemolytic anemia, and severe cutaneous or other hypersensitivity reactions may respond to glucocorticoid administration.
5. Administer as required: plasma volume expanders for severe hypotension; diazepam or benzodiazepine for convulsions; vitamin K1 for hypoprothrombinemia; and/or dopamine plus dobutamine intravenously to prevent or reverse early indications of renal failure
6. Hypotension may be counteracted by the use of dextran plasma, concentrated albumin or vasopressor agents such as noradrenaline
Clinical | Pharmacokinetic data
Pregnancy Category: C
Routes of Administration: Oral
Bioavailability: Not Available
Protein Binding: Not Available
Metabolosim: Not Available
Onset of Action: Not Available
Elimination Half life: Not Available
Excretion: Not Available
Legal Status | Dosage forms & Strengths
Prescription only Medicine (POM) , ℞-only
Narcotic Drugs and Psychotropic Substances (Control ) Act Schedule:
This drug is not a controlled substance under Narcotic Drugs and Psychotropic Substances (Control ) Act
Dosage Forms | Strengths:
- Conney, A. H., and J. J. Burns. “Physiological disposition and metabolic fate of chlorzoxazone (Paraflex) in man.” Journal of Pharmacology and Experimental Therapeutics 128.4 (1960): 340-343.
- O’Shea, Diamuird, et al. “Effect of fasting and obesity in humans on the 6‐hydroxylation of chlorzoxazone: a putative probe of CYP2E1 activity.” Clinical Pharmacology & Therapeutics 56.4 (1994): 359-367.
- Kramer, Iza, et al. “Comparison of chlorzoxazone one-sample methods to estimate CYP2E1 activity in humans.” European journal of clinical pharmacology 59.10 (2003): 775-778.