Diclofenac Sodium + Paracetamol + Dextropropoxyphene Pharmacology

Diclofenac Sodium + Paracetamol + Dextropropoxyphene

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

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.

Dextropropoxyphene

About Dextropropoxyphene
A synthetic morphine derivative,Opioid-like agonist,optical isomer of Levopropoxyphene, Narcotic Analgesic, anti-tussive and local anesthetic.
Mechanism of Action of Dextropropoxyphene
It acts on the CNS Opioid receptors. It has agonist action on mu Opioid receptors. It primarily binds to the mu Opioid receptors and produce analgesia. Its CNS effects are same as morphine. It gives in combination with other Non Steroidal Anti Inflammatory Drugs or other analgesics usually.
Pharmacokinets of Dextropropoxyphene
Absorption-Orally absorbed; primarily to the upper small intestine.
Distribution-Widely distributed in the body. Enters the cerebrospinal fluid and cross the placenta.
Metabolism-In liver it is metabolized by N-demethylation. Norpropoxyphene is its active metabolite. It has more half life than parent drug. It causes toxicity at sometime due to its metabolites accumulation in the body.
Excretion-It is excreted through urine.
Onset of Action for Dextropropoxyphene
30 to 60 min. after oral administration
Duration of Action for Dextropropoxyphene
4 to 6 hrs
Half Life of Dextropropoxyphene
Plasma half life is 6 to 12 hrs
Side Effects of Dextropropoxyphene
1. Nausea
2. Vomiting
3. Epigastric distress
4. Sedation
5. Dizziness
6. Urticaria
7. Visual disturbances
8. Physiological dependence
Contra-indications of Dextropropoxyphene
1. Hypersensitivity to this drug
2. Respiratory depression
3. Children below 12 years
Special Precautions while taking Dextropropoxyphene
1. In patients with hepatic failure or renal failure used cautiously
2. Patient can not drive or operate machinery after the drug administration. So the care should be taken
3. Use cautiously in patients with suicidal mentality
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
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Indications for Dextropropoxyphene
1. Relieve moderate to severe pain in various conditions
2. Opioid withdrawal
Interactions for Dextropropoxyphene
Barbiturate anaesthetics: May increase respiratory and CNS depressive effects of propoxyphene.
Warfarin: Potentiation of hypoprothrombinemic effect.
Carbamazipine: May increase serum carbamzipine levels with resultant toxicity.
Typical Dosage for Dextropropoxyphene
Oral-
Adults - 65mg 3 to 4 times daily.
Schedule of Dextropropoxyphene
H
Storage Requirements for Dextropropoxyphene
Store controlled room temperature i.e. between 15 and 30 degree Celsius
Effects of Missed Dosage of Dextropropoxyphene
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 Dextropropoxyphene
Provide supportive and symptomatic treatment. Establish artificial respiratory exchange. In the case of respiratory or cardiovascular depression administer a narcotic antagonist i.e. naloxone.Induce emesis or gastric lavage if the patient shows symptoms within 2hrs after drug administration. Avoid the risk of aspiration. For the further removal of drug, administer activated charcoal via nasogastric tube. Continue the supportive treatment and closely monitor the laboratory parameters, vital signs, neurological status closely. In some cases dialysis may be helpful for the treatment.

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