Metoclopramide - Uses, Side Effects, Dosage, Precautions, and Interactions

Overview:

Metoclopramide is a Food and Drug Administration (FDA) - approved medication for nausea and vomiting associated with various gastrointestinal disorders and post-operative procedures. The drug works by increasing muscle contractions in the upper digestive tract and speeding up gastric emptying.

Drug Group:

Metoclopramide is a prokinetic agent stimulating gastrointestinal tract muscles. It is a procainamide derivative, a peripheral cholinergic agonist, and a central dopamine receptor antagonist.

Uses of Metoclopramide:

Metoclopramide is an antiemetic usually used to stop nausea and vomiting after radiotherapy or chemotherapy. The drug may also be used to treat sickness associated with migraine.

The anti-sickness medication is often prescribed to treat gastroesophageal reflux disease (GERD), which may cause symptoms like nausea and vomiting. Metoclopramide helps to relieve heartburn and heal esophageal sores. It may be used to reduce symptoms of nausea, vomiting, loss of appetite, and feeling of fullness, often associated with diabetic gastroparesis. Metoclopramide may be used to treat hyperemesis gravidarum in pregnant women.

How Does Metoclopramide Work?

• Antiemetic Effect - Metoclopramide inhibits dopamine D2 and serotonin 5-HT3 receptors in the chemoreceptor trigger zone located posterior of the brain. This enhances the release of acetylcholine, causing increased lower esophageal sphincter and gastric tone and accelerating gastric emptying.

• For Migraine - Metoclopramide antagonizes the dopamine D2 receptor and reduces nausea and vomiting in acute migraines.

• Post-radiotherapy - The antiemetic is used to reduce nausea and vomiting after radiotherapy or chemotherapy (treatment after cancer).

What Is the Onset of Action of Metoclopramide?

The onset of action of Metoclopramide may take one to three minutes following an intravenous dose. The medication may take up to 10 to 15 minutes following an intramuscular administration. Metoclopramide starts to act after 30 to 60 minutes when given orally. Metoclopramide is rapidly and well absorbed in the gastrointestinal tract, with an absorption rate of 84 %. The bioavailability of oral Metoclopramide is 40 %, and it has a high tissue distribution level. Cytochrome P450 enzymes metabolize the drug in the liver. About 85 % of the orally administered dose is eliminated in the urine. The mean elimination half-life of Metoclopramide ranges from five to six hours.

Habit-Forming:

Metoclopramide is an addictive drug and may cause withdrawal symptoms like dizziness, nervousness, or headache when stopped suddenly.

Expiry Date:

Avoid taking this medicine after it expires. Check for the expiry on the back of the medicine pack.

What Is the Dosage of Metoclopramide?

How to Use Metoclopramide?

Metoclopramide is available as a tablet, an orally disintegrating tablet, and a solution. The antiemetic is usually prescribed to be taken 30 minutes before meals, at bedtime, or on an empty stomach. The dosage of the tablet and solution is generally 5 to 10 mg.

The disintegrating tablets must be allowed to melt in the mouth. Metoclopramide must not be used longer than 12 weeks. The medicines must be stored at room temperature, away from heat, moisture, and direct sunlight.

Missed Dose:

In case of a missed dose of Metoclopramide, take it soon after you remember. However, do not take two tablets together at once, as it may cause adverse reactions.

What Are the Drug Warnings and Precautions?

Metoclopramide has a black box warning from the U.S. Food and Drug Administration (FDA) as it can cause serious drug effects that may be dangerous. Long-term treatment and an increased dose of Metoclopramide can cause a severe irreversible condition called Tardive dyskinesia (TD), which is caused by long-term use of psychiatric drugs.

• Pregnancy and Breastfeeding - Metoclopramide may cause a risk of side effects to the fetus. Metoclopramide passes into the human breast milk and may cause side effects to the child.

• Elderly - It is advised to start therapy with Metoclopramide at a low dose. In people older than 65, there is a greater risk of symptoms like uncontrolled arms and legs or face movements.

• Children - Metoclopramide is not advised in children below 18.

• Allergy - Metoclopramide can cause severe allergic reactions and should not be taken if you have ever had an allergic reaction.

• High Blood Pressure - Therapy with Metoclopramide should be administered cautiously in patients with hypertension as it may increase blood pressure.

• Renal Dysfunction - Therapy with Metoclopramide should be administered cautiously in patients with impaired renal function.

What Are the Common Side Effects of Metoclopramide?

Some of the common side effects of Metoclopramide can include

• Headache.

• Confusion.

• Trouble sleeping.

• Dizziness.

• Restlessness.

• Exhaustion.

What Are the Serious Side Effects of Metoclopramide?

Metoclopramide interferes with the brain's chemical dopamine and can cause serious side effects that can include

Depression and Suicide - Symptoms such as sadness, lack of motivation, or thoughts of self-harm.

Neuroleptic Malignant Syndrome - Symptoms may include

• Fever.

• Stiff muscles.

• Trouble thinking.

• Irregular heart rate.

• Increased sweating.

Tardive Dyskinesia - Symptoms may include

• Uncontrolled movements in the face, such as blinking, grimacing, or sticking out the tongue.

• Jerky movements of the arms and legs.

Parkinsonism - Symptoms may include

• Shaking.

• Body stiffness.

• Slow movements.

• Trouble keeping balance.

• Blank stares with an open mouth.

Allergic Reaction - Symptoms may include,

• Rash.

• Hives.

• Trouble breathing.

• Swelling of the tongue, lips, or throat.

Hyperprolactinemia - Symptoms may include,

• Menstrual problems or vaginal dryness in women.

• Erectile dysfunction.

• Decreased body hair.

• Decreased body muscle mass.

• Increased breast size in men.

• Hallucinations.

What Are the Drug Interactions of Metoclopramide?

Metoclopramide oral tablets may interact with other medicines, vitamins, or herbs, preventing the drug from working effectively or increasing the risk of side effects.

Interaction with Drugs:

Sedatives, hypnotics, narcotics, antihistamines, and tranquilizers include

• Diazepam.

• Lorazepam.

• Phenobarbital.

• Promethazine.

• Temazepam.

• Zaleplon.

• Meperidine.

• Propofol.

• Meprobamate.

• Hydroxyzine.

• Monoamine oxidase inhibitors may include

• Isocarboxazid.

• Phenelzine.

• Rasagiline.

• Selegiline.

• Tranylcypromine.

Certain drugs may increase or decrease Metoclopramide's effectiveness or side effects,

Increase the Risk of Side Effects -

• Tetracycline.

• Cyclosporine.

• Insulin.

Reduce the Risk of Side Effects -

• Anticholinergics - These drugs include Atropine, Hyoscyamine, Scopolamine, and Methscopolamine.

• Narcotics - These drugs include Codeine, Fentanyl, Hydro codeine, Meperidine, and Morphine.

Interaction with Food:

• Alcohol - Drinking alcohol while taking Metoclopramide can increase side effects like drowsiness, dizziness, and impaired thinking and judgment and should be avoided.

Interaction with Disease:

• Depression - Therapy with Metoclopramide in patients with a history of mental depression should be administered cautiously as it may cause symptoms like suicidal ideation.

• Gastrointestinal Disorders - Metoclopramide is contraindicated in patients with bowel obstruction, perforation, or gastrointestinal bleeding.

• Neuroleptic Malignant Syndrome - Metoclopramide therapy must not be initiated in patients with the active neuroleptic malignant syndrome.

• Pheochromocytoma - Metoclopramide is contraindicated in patients with pheochromocytoma as it may cause a hypertension crisis.

• Seizures - Metoclopramide is contraindicated in patients with seizure disorders.

• Tardive Dyskinesia - Chronic administration of Metoclopramide may precipitate symptoms of tardive dyskinesia, especially in elderly patients and women.

• Fluid Retention - Metoclopramide can increase the risk of fluid retention in patients with cirrhosis or congestive heart failure and should be administered cautiously.

• Parkinsonism - Initiation of Metoclopramide therapy may cause Parkinson's-like symptoms and should be administered with caution.

Different Brands of Metoclopramide:

1. Tablet Perinorm 5 mg.

2. Syrup Clomet 450 ml.

3. Tablet Emenil 10 mg.

4. Injection Emenorm 5 mg.

5. Injection Maxeron 10 ml.

6. Syrup Maxolon 30 ml.

7. Capsule Metocontin.

8. Syrup Reggi 30 ml.

9. Syrup Reglan 30 ml.

10. Tablet Rivnorm 10 mg.