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- Pharmacology For Diclofenac Sodium + Paracetamol + Chlorzoxazone
Diclofenac Sodium + Paracetamol + Chlorzoxazone Pharmacology
Diclofenac Sodium + Paracetamol + ChlorzoxazoneAbout Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/AMechanism of Action of Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/APharmacokinets of Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/AOnset of Action for Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/ADuration of Action for Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/AHalf Life of Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/ASide Effects of Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/AContra-indications of Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/ASpecial Precautions while taking Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/AInteractions for Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/ATypical Dosage for Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/ASchedule of Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/AStorage Requirements for Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/AEffects of Missed Dosage of Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/AEffects of Overdose of Diclofenac Sodium + Paracetamol + ChlorzoxazoneN/A
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.
ParacetamolAbout ParacetamolAcetanilide derivative, Non narcotic Analgesic,Antipyretic.Mechanism of Action of ParacetamolParacetamol has analgesic and antipyretic action.
It is more active on cyclo-oxygenase enzyme in brain. Peripherally it is a poor inhibitor of prostaglandin synthesis.
Analgesic action: Paracetamol raises the pain threshold and produces analgesic effect.
Antipyretic action: Paracetamol lowers fever by direct action on the thermoregulatory centre in the Hypothalamus and block the effects of endogenous pyrogen.
Pharmacokinets of ParacetamolAbsorption: Paracetamol is rapidly and completely absorbed after oral administration.
Distribution: It is distributed mostly in the body in unbound form.
Metabolism: It is extensively metabolised in the liver.
Excretion: Excreted in the urine.
Onset of Action for Paracetamol30 - 60 minutesDuration of Action for Paracetamol6 hoursHalf Life of Paracetamol1-4 hoursSide Effects of Paracetamol1. Nausea
2. Abdominal distress
3. Allergic reactions
Contra-indications of Paracetamol1. Hypersensitivity to ParacetamolSpecial Precautions while taking Paracetamol1. Hepatic impairment
2. Renal impairment
Pregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationUse with caution
NEONATES : Contraindicated
Indications for Paracetamol1. To relieve pain and fever
2. Acute gout
Interactions for ParacetamolCholestyramine: Reduces absorption of paracetamol.
Charcoal: Activated, administered immediately reduces absorption of paracetamol.
Domperidone and metochlopramide: Enhance absorption of paracetamol.
Alcohol: Chronic excessive ingestion of alcohol potentiates hepatotoxicity of paracetamol.
Zidovudine: Effects zidovudine may be decreased.Typical Dosage for ParacetamolAdult:
500 - 1000 mg in 3 times daily
Maximum dose: 4 g / day
For migraine: 500 mg to be taken at the first sign of migraine attack and repeated 4 - 6 hourly until suppress mild attacks.
60 mg / kg body weight /day in 4 divided doses.
Schedule of ParacetamolHStorage Requirements for ParacetamolStore at 15-30 degree C in a tightly closed container. Protect from heat and moisture. Keep out of the reach of children.Effects of Missed Dosage of ParacetamolTake 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 ParacetamolGive 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. N-acetylcysteine is the specific antidote for Paracetamol poisoning. Dose: 150 mg /kg body weight as IV infusion over 15 minutes followed by same dose over 20 hours.
Maintenance dose: 75 mg / kg orally every 4 - 6 hours for 2 - 3 days. Haemodialysis can be done in emergency conditions.
ChlorzoxazoneAbout ChlorzoxazoneA benzoxazolone derivative, Centrally acting Muscle relaxant and mild sedative.Mechanism of Action of ChlorzoxazoneThis muscle relaxant works by blocking nerve impulses (or pain sensations) that are sent to your brain. It inhibits degranulation of mast cells, subsequently preventing the release of histamine and slow-reacting substance of anaphylaxis (SRS-A), mediators of type I allergic reactions. It may also reduce the release of inflammatory leukotrienes. Chlorzoxazone may act by inhibiting calcium influx.Pharmacokinets of ChlorzoxazoneAbsorption- Rapidly and completely absorbed after oral administration.
Distribution- Widely distributed in the body.
Metabolism- It is metabolized in the liver to its metabolites by glucoronide conjugation.
Excretion- It is excreted through urine.
Onset of Action for Chlorzoxazone1 hr after oral administrationDuration of Action for Chlorzoxazone3 to 4 hrsHalf Life of ChlorzoxazoneN/ASide Effects of Chlorzoxazone1. Difficulty breathing
2. Closing of your throat
3. Swelling of your lips, tongue, or face
4. Liver damage
5. Yellowing of the skin or eyes
6. Abdominal pain or discomfort
7. Unusual bleeding or bruising
8. Severe fatigue
9. Stomach damage
13. Discolored urine
Contra-indications of Chlorzoxazone1. Hypersensitivity to the drugSpecial Precautions while taking Chlorzoxazone1. Liver problems
2. Stomach problems
3. Intestinal problems
4. Any drug allergies
5. Any work which require mental alertness such as driving and machines operating
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationUse with cautionIndications for Chlorzoxazone1. Painful skeletal muscle spasmsInteractions for ChlorzoxazoneAlcohol or other CNS depressants: Additive effect if used concomitantly.Typical Dosage for ChlorzoxazoneAdults: 250 mg-750 mg 3-4 times daily.
Children: 125 mg -500 mg 3-4 times daily.
Schedule of ChlorzoxazoneHStorage Requirements for ChlorzoxazoneStore at room temperature away from moisture and heat.Effects of Missed Dosage of ChlorzoxazoneTake the missed dose as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and take only your next regularly scheduled dose. Do not take a double dose of this medication.Effects of Overdose of ChlorzoxazoneGive symptomatic and supportive treatment. Induce emesis or gastric lavage. Administer activated charcoal to avoid further absorption of drug.
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