Diclofenac Sodium + Rabeprazole Pharmacology

Diclofenac Sodium + Rabeprazole

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

Rabeprazole

About Rabeprazole
Benzimidazole derivative, Proton Pump Inhibitor, Antiulcer.
Mechanism of Action of Rabeprazole
Rabeprazole sodium is a proton pump inhibitor. It is a prodrug. After administration it diffuses in to the parietal cell of the stomach and accumulates in the secretory canaliculi. In the acidic medium Rabeprazole is converted to sulfenamide. This sulfenamide covalently interacts with sulfhydryl (SH) group in the proton pump (H+ K+ATPase) and inhibits the exchange of extracellular K+ for intracellular H+ ion. Rabeprazole sodium irreversibly inhibits proton pumps activity and decreases gastric acid secretion. Rabeprazole produces fastest acid suppression and helps in mucin synthesis.
Pharmacokinets of Rabeprazole
Absorption: Rabeprazole sodium is well absorbed after oral administration and its bioavailability is about 50% since it undergoes first pass metabolism. Distribution: It is widely distributed in the body in protein bound form. Metabolism: Rabeprazole sodium is extensively metabolised in the liver. Excretion: It is excreted mainly in the urine and small amount in faeces.
Onset of Action for Rabeprazole
1hour
Duration of Action for Rabeprazole
1 day
Half Life of Rabeprazole
1 - 2 hours
Side Effects of Rabeprazole
1. Diarrhoea
2. Nausea
3. Headache
4. Vomiting
5. Abdominal pain
6. Dizziness
7. Flatulence
8. Constipation
9. Dyspepsia
10. Flu like syndrome
11. Insomnia
12. Back pain
13. Cough
14. Rhinitis
15. Pharyngitis
16. Rash

Contra-indications of Rabeprazole
1. Hypersensitivity to Rabeprazole sodium
Special Precautions while taking Rabeprazole
1. Hepatic impairment
2. Monitor gastric malignancy

Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Contraindicated
NEONATES: Contraindicated
Indications for Rabeprazole
1. Active Duodenal ulcer
2. Benign Gastric ulcer
3. Zollinger- Ellison syndrome
4. Erosive Gastroesophageal reflux disease
Interactions for Rabeprazole
Ketoconazole : Coadministration of rabeprazole sodium results in a 33% decrease in ketoconazole levels.
Digoxin : Increase in trough digoxin levels in normal subjects.
Typical Dosage for Rabeprazole
Oral
Adult: 10 - 20 mg / day drug to be taken before breakfast.
Duodenal ulcer: 20 mg / day in the morning for 1 month if needed dose can be continuing for 1more month.
Benign Gastric ulcer: 20 mg / day in the morning for 6 weeks if needed dose can be continuing for 6 more weeks.
Zollinger- Ellison syndrome: Initial dose: 60 mg / day if needed increase the dose up to 120 mg / day in 2 divided doses.
Erosive Gastroesophageal reflux disease: 20mg / day for 1-2 months.
Gastroesophageal reflux disease long term management: 10-20 mg once daily before breakfast for 1 year

Children: not recommended
Schedule of Rabeprazole
H
Storage Requirements for Rabeprazole
Store at 15 - 30 degree C in a tightly closed container. Protect from light.
Effects of Missed Dosage of Rabeprazole
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 Rabeprazole
Give supportive measures and symptomatic treatment.

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