Diclofenac Potassium + Paracetamol + Chlorzoxazone Pharmacology

Diclofenac Potassium + Paracetamol + Chlorzoxazone

About Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Mechanism of Action of Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Pharmacokinets of Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Onset of Action for Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Duration of Action for Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Half Life of Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Side Effects of Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Contra-indications of Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Special Precautions while taking Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Interactions for Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Typical Dosage for Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Schedule of Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Storage Requirements for Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Effects of Missed Dosage of Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Effects of Overdose of Diclofenac Potassium + Paracetamol + Chlorzoxazone
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Diclofenac Potassium

About Diclofenac Potassium
NSAID, anti-inflammatory ,antipyretic and analgesic.
Mechanism of Action of Diclofenac Potassium
Diclofenac 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 Potassium
Absorption: Diclofenac potassium is rapidly absorbed after oral administration. It undergoes first pass metabolism. Distribution: It is distributed in highly protein bound form. Metabolism: Diclofenac potassium is metabolised in the liver to mainly 4 hydroxy Diclofenac. Excretion: Drug and metabolites are primarily excreted in urine and some amount in the bile.
Onset of Action for Diclofenac Potassium
Analgesic action: with in 60 minutes and Antirheumatic action with in 2 weeks
Duration of Action for Diclofenac Potassium
12hours
Half Life of Diclofenac Potassium
1-2 hours
Side Effects of Diclofenac Potassium
1.Nausea
2.Vomiting
3.Anorexia
4.Diarrhoea
5.Gastrointestinal bleeding
6.Abdominal distress
7.Constipation
8.Flatulence
9.Ulceration of the stomach or intestine
10.Dyspepsia
11.Headache
12.Dizziness
13.Rash
Contra-indications of Diclofenac Potassium
1.Hypersensitivity to Diclofenac and other Non steroidal anti inflammatory drugs(((NSAID)))
2.Peptic ulcer
3.Asthma
Special Precautions while taking Diclofenac Potassium
1.Hepatic impairment
2.Renal impairment
3.Hypertension
4.Blood clotting disorders
5.Gastrointestinal diseases
6.Proctitis
7.Asthma
8.Cautioned against driving, operating or activities requiring concentration
9.Avoid alcohol
10.Heart failure
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
CHILDREN below 14: contraindicated
Indications for Diclofenac Potassium
1.Rheumatoid arthritis
2.Ankylosing spondylitis
3.Acute gout
4.Joint disorders e.g. inflammatory disease in joints, crystal deposition in the joints
5.Osteoarthritis
6.For the relief of pain and inflammation in dental minor surgery and orthopedic
7.Dysmenorrhoea
8.Migraine
Interactions for Diclofenac Potassium
N/A
Typical Dosage for Diclofenac Potassium
Adult: 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.
Schedule of Diclofenac Potassium
H
Storage Requirements for Diclofenac Potassium
Store Diclofenac potassium at room temperature in a tightly closed light resistant container.
Effects of Missed Dosage of Diclofenac Potassium
Take 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 Potassium
Give 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.

Paracetamol

About Paracetamol
Acetanilide derivative, Non narcotic Analgesic,Antipyretic.
Mechanism of Action of Paracetamol
Paracetamol 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 Paracetamol
Absorption: 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 Paracetamol
30 - 60 minutes
Duration of Action for Paracetamol
6 hours
Half Life of Paracetamol
1-4 hours
Side Effects of Paracetamol
1. Nausea
2. Abdominal distress
3. Allergic reactions
4. Rash
Contra-indications of Paracetamol
1. Hypersensitivity to Paracetamol
Special Precautions while taking Paracetamol
1. Hepatic impairment
2. Renal impairment
3. Hypertension
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
NEONATES : Contraindicated
Indications for Paracetamol
1. To relieve pain and fever
2. Acute gout
3. Migraine
Interactions for Paracetamol
Cholestyramine: 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 Paracetamol
Adult:
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.
Children:
60 mg / kg body weight /day in 4 divided doses.
Schedule of Paracetamol
H
Storage Requirements for Paracetamol
Store 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 Paracetamol
Take 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 Paracetamol
Give 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.

Chlorzoxazone

About Chlorzoxazone
A benzoxazolone derivative, Centrally acting Muscle relaxant and mild sedative.
Mechanism of Action of Chlorzoxazone
This 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 Chlorzoxazone
Absorption- 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 Chlorzoxazone
1 hr after oral administration
Duration of Action for Chlorzoxazone
3 to 4 hrs
Half Life of Chlorzoxazone
N/A
Side Effects of Chlorzoxazone
1. 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
5. Nausea
6. Abdominal pain or discomfort
7. Unusual bleeding or bruising
8. Severe fatigue
9. Stomach damage
10. Drowsiness
11. Dizziness
12. Lightheadedness
13. Discolored urine
14. Rash
Contra-indications of Chlorzoxazone
1. Hypersensitivity to the drug
Special Precautions while taking Chlorzoxazone
1. 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 Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
Indications for Chlorzoxazone
1. Painful skeletal muscle spasms
Interactions for Chlorzoxazone
Alcohol or other CNS depressants: Additive effect if used concomitantly.
Typical Dosage for Chlorzoxazone
Adults: 250 mg-750 mg 3-4 times daily.
Children: 125 mg -500 mg 3-4 times daily.
Schedule of Chlorzoxazone
H
Storage Requirements for Chlorzoxazone
Store at room temperature away from moisture and heat.
Effects of Missed Dosage of Chlorzoxazone
Take 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 Chlorzoxazone
Give symptomatic and supportive treatment. Induce emesis or gastric lavage. Administer activated charcoal to avoid further absorption of drug.

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