Paracetamol + Diclofenac Sodium + Famotidine Pharmacology

Paracetamol + Diclofenac Sodium + Famotidine

About Paracetamol + Diclofenac Sodium + Famotidine
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Mechanism of Action of Paracetamol + Diclofenac Sodium + Famotidine
Diclofenac is a NSAID (NSAID). Paracetamol is an analgesic and antipyretic. When used together, the actions of paracetamol set in earlier and provides pain relief before the effects of diclofenac Na set in.Famotidine is added to reduce gastric irritation.

Pharmacokinets of Paracetamol + Diclofenac Sodium + Famotidine
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Onset of Action for Paracetamol + Diclofenac Sodium + Famotidine
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Duration of Action for Paracetamol + Diclofenac Sodium + Famotidine
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Half Life of Paracetamol + Diclofenac Sodium + Famotidine
N/A
Side Effects of Paracetamol + Diclofenac Sodium + Famotidine
1.GI disturbances
2.Nephrotic syndrome
3.Epigastric pain
4.Nausea
5.Vomiting
6.Diarrhea
7.Hepatitis
8.Rash
9.Pruritus
10.Wheezing
11.Bronchospasm
12.Prolonged bleeding time
13.Dangerous: Bleeding or perforation through peptic ulcer, rarely blood dyscrasia or anaphylaxis, acute renal failure.
Contra-indications of Paracetamol + Diclofenac Sodium + Famotidine
1.Hypersensitivity
2.Active peptic ulcer or GI bleeding
3.History of allergic responses to aspirin or other nsaids
4.Acute porphyria
Special Precautions while taking Paracetamol + Diclofenac Sodium + Famotidine
1.Analgesic nephropathy
2.Renal or hepatic impairment
3.Hypertension
4.Cardiac failure
5.Bronchospasm
6.Patients taking diuretics
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 Paracetamol + Diclofenac Sodium + Famotidine
Pain and inflammation associated with musculoskeletal and joint disorders.
Interactions for Paracetamol + Diclofenac Sodium + Famotidine
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Typical Dosage for Paracetamol + Diclofenac Sodium + Famotidine
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Schedule of Paracetamol + Diclofenac Sodium + Famotidine
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Storage Requirements for Paracetamol + Diclofenac Sodium + Famotidine
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Effects of Missed Dosage of Paracetamol + Diclofenac Sodium + Famotidine
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Effects of Overdose of Paracetamol + Diclofenac Sodium + Famotidine
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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.

Diclofenac Sodium

About Diclofenac Sodium
N/A
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.

Famotidine

About Famotidine
Guanidine:Thiazole derivative,a histamine H2-receptor antagonist, Anti-secretory,Antiulcer.
Mechanism of Action of Famotidine
Famotidine is a H2 (Histamine) receptor antagonist. Histamine is the most potent stimulus of acid secretion and acts as the common mediator. H2 receptor is a G-protein coupled receptor. It induces adenylate cyclase which converts ATP to cyclic AMP. This cyclic AMP acts on proton pump and exchange extracellular potassium ion for intracellular hydrogen ion across the parietal cell membrane. Famotidine reversibly competes with Histamine for binding to H2 receptors on the parietal cells and predominantly inhibits basal acid secretion.
Anaesthetic adjuncts: It is used in patients undergoing prolonged operations, caesarian section; obese patients are at increased risk of gastric regurgitation and aspiration pneumonia. It raises pH of gastric juice and also reduces its volume and thus chances of regurgitation. It is now routinely used before prolonged surgery.
Pharmacokinets of Famotidine
Absorption: Famotidine is 40 - 45 % absorbed after oral administration. Distribution: Distributed mainly in unbound form. Metabolism: Famotidine undergoes metabolism in the liver. Excretion: It is excreted mainly in urine and in the faeces.
Onset of Action for Famotidine
60 minutes
Duration of Action for Famotidine
2.5-3.5 hours
Half Life of Famotidine
2.5 - 3.5 hours
Side Effects of Famotidine
1.Headache
2.Dizziness
3.Constipation
4.Diarrhoea
5.Nausea
6.Vertigo
7.Confusion
8.Rash
9.Thrombocytopenia
10.Leukopenia
Contra-indications of Famotidine
1. Hypersensitivity to Famotidine
Special Precautions while taking Famotidine
1.Hepatic impairment
2.Renal impairment
3.Acute Porphyria
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 Famotidine
1.Duodenal ulcer
2.Benign gastric ulcer
3.Zollinger- Ellison syndrome
4.Gastroesophageal reflux diseases
5.Acid indigestion
6.Heart burn
7.Sour stomach
8.Preanaesthetic medication (PAM)
Interactions for Famotidine
Antacids: Bioavailability of Famotidine slightly decreased, hence antacids in small doses can be given concomitantly.
Typical Dosage for Famotidine
Adult: 40mg / day
Duodenal ulcer, benign gastric ulcer: 40 mg /day as single dose at bed time or in 2 divided dose (morning and bed time) for 1 - 2 months. Maintenance dose: 20 mg / day at bed time.
Zollinger- Ellison syndrome: 80mg / day in 4 divided doses; dose can be increased if necessary to a maximum up to 800 mg / day
Gastroesophageal reflux disease: 40 mg / day as single dose at bed time or in 2 divided doses (morning and bed time) for maximum 2-3 months, dose can be increased to 80 mg / day in 2 divided doses if needed.
Acid indigestion, Heart burn, Sour stomach: Dose: 20mg/day in 2 divided doses.
PAM: 20mg given night before and in the morning before surgical procedure.
Schedule of Famotidine
H
Storage Requirements for Famotidine
Store at 15 - 30 degree C in a tightly closed container. Protect from light.
Effects of Missed Dosage of Famotidine
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 Famotidine
Give supportive measures and symptomatic treatment. Drug can be removed from the body by inducing emesis and or by gastric lavage. Activated charcoal is given to reduce the absorption of the drug. Haemodialysis can be done if necessary.

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