Paracetamol + Promethazine Pharmacology

Paracetamol + Promethazine

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

Promethazine

About Promethazine
A first-generation H1 antagonist, a phenothiazine derivative, Antihistamine,antiemetic,sedative.
Mechanism of Action of Promethazine
Antiallergic actions: Promethazine mainly acts on H1 receptor. It competes with Histamine for H1 receptor. It does not affect the release of Histamine. It blocks the Histamine actions on smooth muscles (GIT, uterus, blood vessel & bronchi) and reduces Histamine induced excess salivary secretion. It has anticholinergic actions. Promethazine produces sedation by inhibiting the stimuli to the brain stem reticular system.
Antiemetic and Antivertigo actions: The central antimuscarinic actions of antihistamines are responsible for their antivertigo and antiemetic effects. They suppress end organ receptors or inhibit central cholinergic action. It also acts on Chemoreceptor trigger zone.
Migraine: Promethazine is used in migraine due to its sedative as well as antiemetic actions.
Anaesthetic adjuncts: Promethazine is used as anaesthetic adjunct due to its sedative, antiemetic and anticholinergic properties.

Pharmacokinets of Promethazine
Absorption: It is well absorbed after oral administration. Distribution: It is distributed widely in the body. Metabolism: It is metabolised in the liver .Excretion: It is excreted mainly through urine. Small amount of drug is excreted through faeces and breast milk.
Onset of Action for Promethazine
15 - 60 minutes
Duration of Action for Promethazine
12 hours
Half Life of Promethazine
10 - 15 hours
Side Effects of Promethazine
1. Tardive dyskinesia
2. Extrapyramidal reactions
3. Drowsiness
4. Sedation
5. Dizzines
6. Hypotension
7. Dry mouth
8. Constipation
9 .Blurred vision
10. Agranulocytosis
11. Photosensitivity
12. Insomnia
13. Weight gain
14. Cholestatic jaundice
Contra-indications of Promethazine
1.Hypersensitivity to Promethazine
2.Comatose
3.Blood dyscrasias
4.Patient taking antidepressants
5.Liver damage
Special Precautions while taking Promethazine
1. Renal impairment
2. Hepatic impairment
3. Cardiovascular disease
4. Pheochromocytoma
5. Hypocalcaemia
6. Epilepsy
7. Cholestatic jaundice
8. Patient exposed to extreme heat or cold or phosphorus insecticides
9. Ceribrovascular disorder
10. Patient on ECT
11. Reaction to Insulin
12. Prostatic hyperplasia
13. Glaucoma
14. Peptic ulcer
15. Slowly withdraw the drug with caution
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
CHILDREN (below 2 years): Contraindicated
NEONATES: Contraindicated
Indications for Promethazine
1. Motion sickness
2. Nausea
3. Sedation
4. Allergy
5. Migraine
6. Vertigo
7. Anticough ingredient
8. Anaesthetic adjuncts
Interactions for Promethazine
Alcohol: CNS depression, extrapyramidal reactions.
Aluminium salts: Decrease efficacy.
Antacids should be given 1 hour before or 2 hours after promethazine.
Anticholinergics: Decrease efficacy and increase the anticholinergic side-effects of promethazine.
Barbiturates: Decrease efficacy.
Barbiturate anaesthetics: Increase frequency and severity of neuromuscular excitation and hypotension.
Bromocriptine: Efficacy decreased by promethazine.
Charcoal: Prevents absorption of promethazine.
Lithium: Disorientation, unconsciousness and extrapyramidal symptoms.
Meperidine: Excessive sedation and hypotension.
TCAs: Serum concentration increased by promethazine.
Propranolol: Increased plasma levels of both drugs.
MAOIs: Additive orthostatic hypotensive effect.
Lab tests: Pregnancy tests: False positive results.
Plasma bound iodine (PBI): Increase in PBI occurs.
Typical Dosage for Promethazine
Adult:
Motion sickness: 50 mg / day in 2 divided dose
Allergy: 25 mg at bed time
Nausea: 12.5 - 25 mg / day
Sedation: 25 - 50 mg at bed time
Children:
Motion sickness: 12.5 - 25 mg / day
Allergy: 6.25 - 12. 5 mg 3 times a day
Sedation: 12.5 - 25 mg at bed time
Schedule of Promethazine
G
Storage Requirements for Promethazine
The drug should be kept at 15 - 25 degree C in a tightly closed container. Protect from heat and light. Keep out of the reach of children
Effects of Missed Dosage of Promethazine
Take the missed dose as soon s noticed and if it is the time to take the next dose then skip the missed dose.
Effects of Overdose of Promethazine
Give supportive measures and treatment. Gastric lavage has to be done. Hypotension can be treated with IV fluids, seizure with Diazepam or Barbiturates, arrhythmia with Phenytoin and excretion of drug can be increased by acidification of urine.

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