Metoclopramide Pharmacology

Metoclopramide

About Metoclopramide
It is a dopamine antagonist - antiemetic gastroprokinetic agent.
Mechanism of Action of Metoclopramide
Metoclopramide acts through both serotonergic and dopaminergic receptors. Metoclopramide binds to Serotonin (5 HT3 &5HT4) and Dopamine (D2) receptor.
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.
Pharmacokinets of Metoclopramide
Absorption: Metoclopramide is rapidly and well absorbed after oral administration. Distribution: It is extensively distributed to tissues and fluids, brain.
Metabolism: Only a small amount undergoes hepatic metabolism. Excretion: It is excreted mainly in urine and faeces.
Onset of Action for Metoclopramide
Oral: ? - 1 hour.
IM: 10 - 15 minutes
IV: 1 - 3 minutes
Duration of Action for Metoclopramide
1-2 hours.
Half Life of Metoclopramide
3 - 6 hour.
Side Effects of Metoclopramide
1.Drowsiness
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
Contra-indications of Metoclopramide
1.Hypersensitivity to Metoclopramide
2.Gastrointestinal haemorrhage
3.Mechanical obstruction
4.Pheochromocytoma
5.Epilepsy
6.Parkinsonism
7.Pyloric stenosis
8.Previous history of dystonia
Special Precautions while taking Metoclopramide
1. Hypertension
2. Depression
3. Renal impairment
4. Hepatic impairment
5. Use with caution while driving vehicles, operating machines and people involving any other dangerous activities
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
NEONATES: contraindicated
Indications for Metoclopramide
1. Nausea and vomiting (except motion sickness)
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

Interactions for Metoclopramide
Anticholinergic drugs and narcotic analgesics: Effects on GI motility are antagonised by these drugs.
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.
Typical Dosage for Metoclopramide
Adult:
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.
Schedule of Metoclopramide
H
Storage Requirements for Metoclopramide
Store at 15 - 30 degree C in a tightly closed container. Protect from heat and light.
Effects of Missed Dosage of Metoclopramide
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 Metoclopramide
Give supportive measures and symptomatic treatment. Extrapyramidal effects may be controlled by administration of antimuscarinic or antiparkinsonian agents or antihistamine with antimuscarinic activity

Home Delivery for Metoclopramide in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including metoclopramide.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for metoclopramide and other medicines and health products. Home delivery services for metoclopramide may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take metoclopramide only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for metoclopramide before they complete the sale. You can get this information while placing the order for metoclopramide with the pharmacy.

Metoclopramide is a generic medicine name and there are several brands available for it. Some of the brands for metoclopramide might be better known than metoclopramide itself. If the pharmacy that's willing to deliver medicines to your home doesn't have metoclopramide in stock, you can ask for one of the branded alternatives for metoclopramide.