Phenylbutazone + Paracetamol Pharmacology

Phenylbutazone + Paracetamol

About Phenylbutazone + Paracetamol
N/A
Mechanism of Action of Phenylbutazone + Paracetamol
This peripherally acting NSAID binds to and inactivates prostaglandin H synthase and prostacyclin synthase through peroxide (H2O2) mediated deactivation i.e. by inhibiting COX1 and COX2 isoenzymes. The reduced production of prostaglandin leads to reduced inflammation of the surrounding tissues.
Pharmacokinets of Phenylbutazone + Paracetamol
Absorption- Readily absorbed after oral administration.
Distribution- 98% bound to the plasma proteins.
Metabolism- Metabolized in the liver by oxidation and glucoronide conjugation.
Excretion- Excreted through urine.


Onset of Action for Phenylbutazone + Paracetamol
Analgesic action: 2 hrs after oral administration
Antirheumatic action: 3 to 4 days after oral administration
Duration of Action for Phenylbutazone + Paracetamol
3 to 4 days
Half Life of Phenylbutazone + Paracetamol
N/A
Side Effects of Phenylbutazone + Paracetamol
1. Nausea
2. Epigastric distress
3. Aplastic anemia
4. Vomiting
5. Diarrhoea
6. Peptic ulcer
7. Depression
8. Neutropenia
9. Hypothyroidism
10. Skin rash
11. Urticaria
12. Oedema


Contra-indications of Phenylbutazone + Paracetamol
1. Hypersensitivity to the drug
2. Peptic ulcer
3. Hypertension
4. Congestive heart failure
5. Impairment of liver
6. Kidney dysfunction
7. Blood dyscrasias
8. Thyroid disease


Special Precautions while taking Phenylbutazone + Paracetamol
1. Check blood cell count regularly
2. Patients with Cardiac insufficiency


Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Contraindicated
Indications for Phenylbutazone + Paracetamol
1. Rheumatoid arthritis
2. Ankylosing spondylitis
3. Gouty arthritis
4. Osteoarthritis
6. Tendinitis
7. Sprains
8. Strains
9. Menstrual cramps
10. Bursitis
Interactions for Phenylbutazone + Paracetamol
Alcohol: May impair psychomotor skills.
Anti-inflammatory agents, Oral anticoagulants, Oral antidiabetics, Sulfonamides, Sodium valproate and Phenytoin: Duration of effect and toxicity of these drugs may be increased.
Barbiturates, Promethazine, Chlorpheniramine, Rifampicin and Corticosteroids: Decrease half life of phenylbutazone.
Cholestyramine: Enteral absorption of phenylbutazone reduced.
Coumarin-type anticoagulants: Hypo-prothrombonemic effects are increased by phenylbutazone.
Dicoumarol, Digoxin and Cortisone: May induce microsomal metabolism of phenylbutazone.
Phenytoin: Serum levels and toxicity of phenytoin increased.
Methotrexate, Insulin, Lithium: Effects of these drugs may be increased.
Lab tests: Reduces iodine uptake by thyroid and may interfere with laboratory tests of thyroid function.

Typical Dosage for Phenylbutazone + Paracetamol
Oral:
Adults:
Initial dose- 200mg 2-3 times daily for 2 days.
Maintenance dose-100 mg 2-3 times daily.
Schedule of Phenylbutazone + Paracetamol
H
Storage Requirements for Phenylbutazone + Paracetamol
Store at room temperature in a sealed container.Keep away from moisture.
Effects of Missed Dosage of Phenylbutazone + 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 Phenylbutazone + Paracetamol
Give symptomatic and supportive treatment.

Phenylbutazone

About Phenylbutazone
NSAID, a synthetic Pyrazolone derivative, Analgesic ,antipyretic,anti inflammatory.
Mechanism of Action of Phenylbutazone
This peripherally acting NSAID binds to and inactivates prostaglandin H synthase and prostacyclin synthase through peroxide (H2O2) mediated deactivation i.e. by inhibiting COX1 and COX2 isoenzymes. The reduced production of prostaglandin leads to reduced inflammation of the surrounding tissues.
Pharmacokinets of Phenylbutazone
Absorption- Readily absorbed after oral administration
Distribution- 98% bound to the plasma proteins
Metabolism- Metabolized in the liver to its metabolites by oxidation and glucoronide conjugation
Excretion- Excreted through urine
Onset of Action for Phenylbutazone
Analgesic action- 2 hrs after oral administration
Antirheumatic action -3 to 4 days after oral administration
Duration of Action for Phenylbutazone
3 to 4 days
Half Life of Phenylbutazone
Its plasma half life is 60 hrs
Side Effects of Phenylbutazone
1. Nausea
2. Epigastric distress
3. Aplastic anemia
4. Vomiting
5. Diarrhoea
6. Peptic ulcer
7. Depression
8. Neutropenia
9. Hypothyroidism
10. Skin rash
11. Urticaria
12. Oedema.
Contra-indications of Phenylbutazone
1. Hypersensitivity to the drug
2. Peptic ulcer
3. Hypertension
4. Congestive heart failure
5. Impairment of liver
6. Kidney dysfunction
7. Blood dyscriasis
8. Thyroid disease
Special Precautions while taking Phenylbutazone
Check blood cell count regularly
Use with caution in patients with Cardiac insufficiency
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Contraindicated
Indications for Phenylbutazone
1. Rheumatoid arthritis
2. Ankylosing spondylitis
3. Gouty arthritis
4. Osteoarthritis.
6. Tendinitis
7. Sprains
8.Strains
9. Menstrual cramps
10 Bursitis
Interactions for Phenylbutazone
N/A
Typical Dosage for Phenylbutazone
Oral-
Adults (General dose) -
Initial dose- 200mg 2-3 times daily for 2 days
Maintenance dose-100 mg 2 - 3 times daily
Schedule of Phenylbutazone
H
Storage Requirements for Phenylbutazone
Store at room temperature in a tightly closed container.
Effects of Missed Dosage of Phenylbutazone
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 Phenylbutazone
Give supportive measures and symptomatic treatment.

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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