Pentazocine + Paracetamol Pharmacology

Pentazocine + Paracetamol

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

About Pentazocine
Benzomorphan derivative, Opioid Analgesic(centrally acting analgesic).
Mechanism of Action of Pentazocine
It is morphine like Opioid analgesic. Its analgesic action is due to the agonistic action at kappa Opioid receptors. At mu receptors it has weak agonistic and partial antagonistic action. It produces more dysphoria than euphoria because of the activation at supraspinal kappa receptors. Its psycho mimetic activity is due to the action at sigma Opioid receptors. On respiratory depression it has a ceiling effect i.e. by increasing the dose there is no increase of respiratory depression. Symptoms of withdrawal are less in this drug than morphine.
Pharmacokinets of Pentazocine
Absorption. Orally well absorbed but its bioavailability is low due to first pass metabolism. In patients with hepatic dysfunction can absorb 60-70% of the drug.It is rapidly absorbed after intra venous, intramuscular and subcutaneous administration.
Distribution:-Widely distributed in the body.
Metabolism -It undergoes metabolism by oxidation and glucoronidation in liver.
Excretion-It is excreted via urine and a small amount through faeces.
Onset of Action for Pentazocine
Oral. 15-30min
Intravenous. 2 - 3min
Intramuscular and Subcutaneous. 10 - 20min
Duration of Action for Pentazocine
2 - 3 hrs
Half Life of Pentazocine
2 - 3 hrs
Side Effects of Pentazocine
1. Sedation
2. Light headedness
3. Euphoria
4. Psychomimetic effect
5. Shock
6. Hypertension
7. Hypotension
8. Constipation
9. Nausea
10. Vomiting
11. Urine retention
12. Respiratory depression
13. Dyspnea
14. Apnea
15. Sclerosis of injection site
16. Pruritis
17. Psychological dependence
Contra-indications of Pentazocine
1. Hypersensitivity to the drug
2. Myocardial infarction
3. Hypertension
4. Pregnancy
6. Increased intracranial pressure
7. Respiratory failure
8. Narcotic dependence
Special Precautions while taking Pentazocine
1. Labour
2. Elderly patients
3. Patients with head injury
4. Respiratory depression
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
N/A
Children Related Information
Use with caution
Indications for Pentazocine
1. Pain in -Trauma, Surgery, Burns, Labour, Cancer
2. Pre- anaesthetic medication
Interactions for Pentazocine
Alcohol : Increased CNS depressant effects.
Barbiturate anaesthetics : May increase respiratory & CNS depression effects of pentazocine.
Typical Dosage for Pentazocine
Oral :
Adults -50 to 100 mg every 3-4 times.
Intravenous,Intramuscular and Subcutaneous - 30 to 60mg every 3-4 times.
Labour patient-30mg i.v or 20 mg i.m in 2 to 3 hour interval.
Rectal :50mg suppository 4 times daily.
Oral:
Children: 25mg every 3-4 times.
Schedule of Pentazocine
H
Storage Requirements for Pentazocine
Store at room temperature.
Effects of Missed Dosage of Pentazocine
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 Pentazocine
Take all supportive measures. Give mechanical ventilation. If respiratory depression occurs give an antagonistic parenterally e.g.Naloxone.

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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