Paracetamol + Metoclopramide Pharmacology
Paracetamol + Metoclopramide
Paracetamol
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.
Distribution: It is distributed mostly in the body in unbound form.
Metabolism: It is extensively metabolised in the liver.
Excretion: Excreted in the urine.
2. Abdominal distress
3. Allergic reactions
4. Rash
2. Renal impairment
3. Hypertension
NEONATES : Contraindicated
2. Acute gout
3. Migraine
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.
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.
Maintenance dose: 75 mg / kg orally every 4 - 6 hours for 2 - 3 days. Haemodialysis can be done in emergency conditions.
Metoclopramide
Antiemetic action: Metoclopramide inhibits Dopamine receptor in the chemoreceptor trigger zone and produces antiemetic action.
Intestinal motility modifying action: The binding of Metoclopramide on 5HT4 receptor will activate interneuron and enhance the release of acetylcholine innervating the smooth muscles. This produces gastric emptying and enhances lower esophageal sphincter tone.
Migraine: Metoclopramide is used in migraine to relieve nausea and vomiting
Anaesthetic adjuncts: It is used preoperatively in order to reduce the post operative vomiting.
Metabolism: Only a small amount undergoes hepatic metabolism. Excretion: It is excreted mainly in urine and faeces.
IM: 10 - 15 minutes
IV: 1 - 3 minutes
2.Confusion
3.Constipation
4.Muscle spasm
5.Tremor
6.Bronchospasm
7.Bradycardia
8.Fatigue
9.Headache
10.Dizziness
11.Nervousness
12.Sedation
13.Nausea
14.Rash
2.Gastrointestinal haemorrhage
3.Mechanical obstruction
4.Pheochromocytoma
5.Epilepsy
6.Parkinsonism
7.Pyloric stenosis
8.Previous history of dystonia
2. Depression
3. Renal impairment
4. Hepatic impairment
5. Use with caution while driving vehicles, operating machines and people involving any other dangerous activities
NEONATES: contraindicated
a)associated with various gastrointestinal disorders and migraine
b) Nausea and vomiting associated with cytotoxic chemotherapy or radiotherapy.
c) Post operative nausea and vomiting
2. Treatment of delayed gastric motility
3. Gastroesophageal reflux
4. Diagnostic procedure in gastroenterology
Alcohol, sedatives, hypnotics, narcotics or tranquilizers: Additive sedative effect may occur.
Digoxin, Cimetidine: Absorption of these drugs decreased.
Acetaminophen, Aspirin: The absorption of these agents increased.
Phenothiazines, Butyrophenone, Lithium and Thioxanthine drugs: May potentiate extrapyramidal effects.
Bromocriptine: Antagonism of hypoprolactinaemic effect of bromocryptine.
Cyclosporine: May lead to increased cyclosporine absorption, possibly increasing immunosupressive and toxic effect.
Succinylcholine: Metoclopramide may increase the neuromuscular blocking effects of succinylcholine.
ORAL: 15 - 30 mg / day in 3 divided doses.
Treatment of delayed gastric motility: 10 mg to be taken 30 minutes before each meal and at bed time for3 months. Drug is given depending upon the symptom being treated and clinical response.
Gastroesophageal reflux: 10 - 15 mg 4 times a day, drug to be taken half an hour before each meal and at bed time.
INJECTION:
Post operative nausea and vomiting: 10 - 20 mg IM at the end of surgical procedure and repeat the dose every 4 - 6 hours if needed
Nausea and vomiting associated with cytotoxic chemotherapy or radiotherapy: 2 - 4 mg / kg as IV infusion over 15 - 30 minutes.
Maintenance dose: 3 - 5 mg / kg given over 8 hours
Maximum dose: 10 mg / kg / day.
Children:
ORAL: 0.4 mg / kg / day in 4 divided doses.
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