Methocarbamol + Diclofenac Sodium + Paracetamol Pharmacology

Methocarbamol + Diclofenac Sodium + Paracetamol

About Methocarbamol + Diclofenac Sodium + Paracetamol
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Mechanism of Action of Methocarbamol + Diclofenac Sodium + Paracetamol
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Pharmacokinets of Methocarbamol + Diclofenac Sodium + Paracetamol
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Onset of Action for Methocarbamol + Diclofenac Sodium + Paracetamol
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Duration of Action for Methocarbamol + Diclofenac Sodium + Paracetamol
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Half Life of Methocarbamol + Diclofenac Sodium + Paracetamol
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Side Effects of Methocarbamol + Diclofenac Sodium + Paracetamol
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Contra-indications of Methocarbamol + Diclofenac Sodium + Paracetamol
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Special Precautions while taking Methocarbamol + Diclofenac Sodium + Paracetamol
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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 Methocarbamol + Diclofenac Sodium + Paracetamol
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Interactions for Methocarbamol + Diclofenac Sodium + Paracetamol
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Typical Dosage for Methocarbamol + Diclofenac Sodium + Paracetamol
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Schedule of Methocarbamol + Diclofenac Sodium + Paracetamol
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Storage Requirements for Methocarbamol + Diclofenac Sodium + Paracetamol
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Effects of Missed Dosage of Methocarbamol + Diclofenac Sodium + Paracetamol
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Effects of Overdose of Methocarbamol + Diclofenac Sodium + Paracetamol
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Methocarbamol

About Methocarbamol
A centrally acting skeletal muscle relaxant, Carbamate derivative, Skeletal muscle relaxant.
Mechanism of Action of Methocarbamol
This skeletal muscle relaxant depresses central nervous system by the preferential blockade of spinal and supraspinal polysynaptic reflexes. This leads to sedation and a reduction in skeletal muscle spasms. These effects are accompanied by relief of pain and an increase in the mobility of the affected muscles. Pain relief is postulated to be due to alterations in the perception of pain.
Pharmacokinets of Methocarbamol
Absorption- Rapidly and completely absorbed after administration
Distribution- Widely distributed throughout the body. It crosses the placenta
Metabolism- Extensively metabolized in the liver to its metabolites, by dealkylation and hydroxylation
Excretion- Drug and its metabolites are excreted rapidly and completely in urine
Onset of Action for Methocarbamol
30 minutes after oral administration
Immediate after IV administration
Duration of Action for Methocarbamol
4-6 hours
Half Life of Methocarbamol
0.9 to 2.2 hours
Side Effects of Methocarbamol
1. Drowsiness
2. Dizziness
3. Upset stomach
4. Blurred vision
5. Fever
6. Rash
7. Itching
8. Dyspepsia
9. Jaundice
10. Nausea
11. Vomiting
12. Leucopenia
Contra-indications of Methocarbamol
1. Hypersensitive to methocarbamol or to any of the tablet components
2. Epilepsy
3. Coma or pre-coma
4. Myasthenia gravis
Special Precautions while taking Methocarbamol
1. Alcohol abuse
2. CNS depressants therapy
3. Impairment of hepatic function
4. Renal impairment
5. Any work which require mental alertness such as driving or operating machine
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
Indications for Methocarbamol
1. Skeletal muscle spasm
2. Surgery
3. Orthopedic procedure
4. Neurological diseases
5. Tetanus
Interactions for Methocarbamol
Alcohol and other CNS depressant drugs: CNS depressant effect potentiated.
Anorectics and anticholinergics: Efficacy increased by methocarbamol.
Lab tests: Causes colour interference in certain screening tests for 5-hydroxy-indoleacetic acid (5-HIAA) and Vanillyl mandelic acid (VMA).
Typical Dosage for Methocarbamol
Adults-
Oral-
500 mg -initial dosage, 3 tablets 4 times daily
Maintenance dosage- 2 tablets 4 times daily
750 mg - initial dosage, 2 tablets 4 times daily
Maintenance dosage, 1 tablet q.4 h, or 2 tablets 3 times daily
Intravenous-
Tetanus-
2-3g over 10-15 minutes
Then 2g ampules every 6 hours until oral therapy can be started by dose of 18-40 tablets of 500mg daily in divided doses, 4-6 hourly by nasogastric tube.
Children-
Initial dose -15mg / kg. Repeat every 6 hours.
Schedule of Methocarbamol
H
Storage Requirements for Methocarbamol
Store at room temperature away from heat and direct light. Keep out of the reach of children.
Effects of Missed Dosage of Methocarbamol
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 Methocarbamol
Give symptomatic and supportive treatment. Induce emesis or gastric lavage. Monitor urine output and vital signs regularly

Diclofenac Sodium

About Diclofenac Sodium
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Mechanism of Action of Diclofenac Sodium
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 Sodium
Absorption: 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 Sodium
1- 4.5 hours
Duration of Action for Diclofenac Sodium
Hours
Half Life of Diclofenac Sodium
2 hours
Side Effects of Diclofenac Sodium
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 Sodium
1.Hypersensitivity to Indomethacin and other Non steroidal anti inflammatory drugs(NSAID)
2.Peptic ulcer
3.Asthma
Special Precautions while taking Diclofenac Sodium
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 Sodium
1.Ankylosing spondylitis
2.Acute gout
3.Joint disorders e.g. inflammatory disease in joints, crystal deposition in the joints
4.Osteoarthritis
5.For the relief of pain and inflammation in dental minor surgery and orthopedic
6.Dysmenorrhoea
7.Juvenile chronic arthritis
8.Migraine
Interactions for Diclofenac Sodium
Lithium & 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 Sodium
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.
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 Sodium
H
Storage Requirements for Diclofenac Sodium
Store Diclofenac sodium at room temperature in a tightly closed light resistant container.
Effects of Missed Dosage of Diclofenac Sodium
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 Sodium
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.

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