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- Pharmacology For Nimesulide + Diclofenac Sodium
Nimesulide + Diclofenac Sodium Pharmacology
Nimesulide + Diclofenac SodiumAbout Nimesulide + Diclofenac SodiumN/AMechanism of Action of Nimesulide + Diclofenac SodiumN/APharmacokinets of Nimesulide + Diclofenac SodiumN/AOnset of Action for Nimesulide + Diclofenac SodiumN/ADuration of Action for Nimesulide + Diclofenac SodiumN/AHalf Life of Nimesulide + Diclofenac SodiumN/ASide Effects of Nimesulide + Diclofenac SodiumN/AContra-indications of Nimesulide + Diclofenac SodiumN/ASpecial Precautions while taking Nimesulide + Diclofenac SodiumN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Nimesulide + Diclofenac SodiumN/AInteractions for Nimesulide + Diclofenac SodiumN/ATypical Dosage for Nimesulide + Diclofenac SodiumN/ASchedule of Nimesulide + Diclofenac SodiumN/AStorage Requirements for Nimesulide + Diclofenac SodiumN/AEffects of Missed Dosage of Nimesulide + Diclofenac SodiumN/AEffects of Overdose of Nimesulide + Diclofenac SodiumN/A
NimesulideAbout NimesulideCOX-2 selective NSAID, Analgesic,antipyretic.Mechanism of Action of NimesulideThis Non Steroidal Anti Inflammatory Drug reduces prostaglandin synthesis by the inhibition of cyclo oxygenase enzyme2 selectively. This is a weaker inhibition .So it produces weaker analgesic property. Its potent anti-inflammatory activity is due to its action on various stages of inflammation. This leads to the inhibition of super oxide anion formation invitro by activated neutrophil, inhibition of histamine release from tissue mast cells and basophiles. Additionally it also prevents platelet activating factor synthesis and metalloproteinase synthesis thus prevents the breakdown of osteoarthritic human cartilage. It also prevent tumor necrosis factor alpha and thus reduce the formation of cytokines. This drug can activate glucocorticoid receptors in the body.Pharmacokinets of NimesulideAbsorption-Completely absorbed after oral administration.
Distribution-Widely distributed in the body and extensively bind to the plasma proteins i.e.99%.
Metabolism-It is metabolized in liver to its metabolites.4-hydroxyl derivative is its one active metabolite.
Excretion - Excreted via urine and bile.
Onset of Action for Nimesulide30 to 60 minutesDuration of Action for Nimesulide8-10 hoursHalf Life of NimesulideIts plasma half life is long-nearly 2daysSide Effects of Nimesulide1. Nausea
4. Heart burn
5. Epigastric pain
7. Skin rash
Contra-indications of Nimesulide1. Hypersensitivity to this drug
2. Active peptic ulcer
3. Hepatic impairment
Special Precautions while taking Nimesulide1. Renal impairment
2. Heart failure
3. Alcohol abuse
5. Crohns disease
7. Gastric ulcer
8. Diabetis mellitus
10. Hepatic failure
11. Rectal irritation or bleeding
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Nimesulide1. Painful inflammatory conditions associated with -
Musculoskeletal system, Dysmenorrhea, Thrombophlebitis, Gout
2. Dental pain
3. ENT infection
5. Rheumatoid arthritis
6. Gynecological disorder
7. Low back pain
8. Post operative pain
Interactions for NimesulideFenofibrate, Salicyclic acid, Valproic acid and Tolbutamide: These drugs displace nimesulide from the plasma binding sites.
Methotrexate and Frusemide: These drugs may be displaced from plasma proteins by nimesulide.
Warfarin: Exercise caution since efficacy may be increased.
Theophylline: Efficacy of slow release theophylline preparations reduced. Typical Dosage for NimesulideOral-
Adults - 100 mg two times daily.
Children - 5mg/kg/day divided in 2 or 3 doses.
Schedule of NimesulideHStorage Requirements for NimesulideStore in cool, dark, dry placeEffects of Missed Dosage of NimesulideTake the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose
Effects of Overdose of NimesulideEmpty the stomach if necessary. Symptomatic treatment should be given
Diclofenac SodiumAbout Diclofenac SodiumN/AMechanism of Action of Diclofenac SodiumDiclofenac possess analgesic, anti-inflammatory and antipyretic action. It inhibits the enzyme cyclo-oxygenase and there by inhibits the synthesis of Prostaglandins (PGs). It is more potent against cyclo-oxygenase-2 enzyme as compared to other NSAIDs like Indomethacin, Naproxen etc. It reduces intracellular concentrations of free arachidonic acid in leukocyte by altering its release or uptake. .Pharmacokinets of Diclofenac SodiumAbsorption: Diclofenac sodium is rapidly absorbed after oral administration. It undergoes first pass metabolism and its bioavailability is 50 % only. Distribution: It is distributed in highly protein bound form. Metabolism: Diclofenac sodium is metabolised in the liver. Excretion: Drug and metabolites are primarily excreted in urine and some amount in the bile.Onset of Action for Diclofenac Sodium1- 4.5 hoursDuration of Action for Diclofenac SodiumHoursHalf Life of Diclofenac Sodium2 hoursSide Effects of Diclofenac Sodium1.Nausea
9.Ulceration of the stomach or intestine
Contra-indications of Diclofenac Sodium1.Hypersensitivity to Indomethacin and other Non steroidal anti inflammatory drugs(NSAID)
Special Precautions while taking Diclofenac Sodium1.Hepatic impairment
4.Blood clotting disorders
8.Cautioned against driving, operating or activities requiring concentration
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with caution
CHILDREN below 14: contraindicatedIndications for Diclofenac Sodium1.Ankylosing spondylitis
3.Joint disorders e.g. inflammatory disease in joints, crystal deposition in the joints
5.For the relief of pain and inflammation in dental minor surgery and orthopedic
7.Juvenile chronic arthritis
Interactions for Diclofenac SodiumLithium & Digoxin : Blood levels of lithium and digoxin increased leading to enhanced efficacy and posible toxicity.
Diuretics : Inhibits diuretics but efficacy of potassium sparing diuretics enhanced.
Methotrexate : Toxicity enhanced.
Salicylates : Efficacy of salicylates reduced.
Cyclosporine : Increases nephrotoxicity of both agents.
Hydantoins : Increases serum levels resulting in toxicity.
Typical Dosage for Diclofenac SodiumAdult: 100 - 150 mg / day in 2 - 3 divided doses.
For the relief of pain, Migraine, Dysmenorrhoea: 150 mg / day in 3 divided doses.
Osteoarthritis: 50 mg 2 - 3 times daily
Rheumatoid arthritis: 150 - 200 mg / day in 3 - 4 divided doses.
Ankylosing spondylitis: 25 mg 4 times daily give an extra dose of 25 mg at bed time if necessary.
Children Juvenile rheumatoid arthritis: 0.5 - 2 mg / kg body weight / day in divided doses.
Maximum dose: 3 mg / kg body weight / day in divided doses
Schedule of Diclofenac SodiumHStorage Requirements for Diclofenac SodiumStore Diclofenac sodium at room temperature in a tightly closed light resistant container.Effects of Missed Dosage of Diclofenac SodiumTake the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.Effects of Overdose of Diclofenac SodiumGive supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage or by inducing emesis. Absorption of the drug can be reduced by administration of activated charcoal.
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