Motilon1 mg/ml

Gastroesophageal Reflux Disease (GERD)

Motilon is an established short-term (up to 12 weeks) treatment for symptomatic GERD in adults who have not responded adequately to other therapy, used to relieve heartburn and related symptoms by increasing gastric emptying and lower esophageal sphincter tone.

Diabetic Gastroparesis

Motilon is FDA-approved for the relief of symptoms associated with acute and recurrent diabetic gastroparesis, including nausea, vomiting, early satiety, bloating, and abdominal pain related to delayed gastric emptying. Because of the risk of tardive dyskinesia, treatment with Motilon for this indication is generally limited to 12 weeks or less.

Nausea and Vomiting

Motilon is an established antiemetic used to prevent and treat nausea and vomiting associated with chemotherapy (often as part of a combination antiemetic regimen for highly or moderately emetogenic chemotherapy), postoperative nausea and vomiting, and other causes of nausea and vomiting when other measures are inadequate.

Facilitation of Small Bowel Intubation and Radiologic Examination

Motilon is used, as a single intravenous dose, to stimulate gastric and small bowel motility to facilitate intubation of the small bowel when the tube does not pass the pylorus with conventional maneuvers, and to accelerate gastric emptying and small bowel transit when a barium examination of the stomach or small intestine is delayed.

Off-Label Use

Motilon is used off-label by some clinicians to support lactation (as a galactagogue) in mothers with low milk supply; this use is not FDA-approved, is supported only by limited evidence, and carries the same tardive dyskinesia and other risks as approved uses, so it should only be considered under close medical supervision.

Each tablet contains Metoclopramide Hydrochloride equivalent to 10 mg of metoclopramide base. Metoclopramide Hydrochloride is also available as an oral solution and as an injectable solution for intramuscular or intravenous use, in strengths determined by the manufacturer.

Motilon is a prokinetic and antiemetic medicine that works by blocking dopamine D2 receptors, primarily in the gastrointestinal tract and in the chemoreceptor trigger zone of the brain. Motilon increases the tone and strength of stomach contractions, relaxes the pyloric sphincter, and increases peristalsis of the upper small intestine, which together speed up gastric emptying and transit time without stimulating gastric, biliary, or pancreatic secretions. Motilon also has central antiemetic activity, which is why it is used both for gastrointestinal motility disorders and for the prevention and treatment of nausea and vomiting. Motilon carries an FDA boxed warning for tardive dyskinesia with prolonged or high-dose use, so treatment with Motilon is generally kept as short and at as low a dose as clinically possible, and should always be taken exactly as prescribed by a qualified healthcare professional.

Prokinetic agent / Antiemetic (Dopamine D2-receptor antagonist)

Metoclopramide Hydrochloride is a dopamine D2-receptor antagonist that also has weak serotonin 5-HT3-receptor antagonist and 5-HT4-receptor agonist activity at higher doses, contributing to its combined prokinetic and antiemetic effects. Peripherally, Metoclopramide Hydrochloride sensitizes gastrointestinal smooth muscle to the effects of acetylcholine, increasing lower esophageal sphincter tone, stimulating antral and duodenal contractions, and relaxing the pyloric sphincter, which accelerates gastric emptying and reduces reflux without increasing gastric acid secretion. Centrally, Metoclopramide Hydrochloride crosses the blood-brain barrier and blocks dopamine receptors in the chemoreceptor trigger zone of the medulla, producing its antiemetic effect; this same central dopamine blockade is responsible for the extrapyramidal side effects and tardive dyskinesia risk associated with Metoclopramide Hydrochloride. After oral administration, Metoclopramide Hydrochloride is rapidly absorbed, with onset of action within 30-60 minutes orally, 10-15 minutes intramuscularly, and 1-3 minutes intravenously; the plasma half-life of Metoclopramide Hydrochloride is approximately 5-6 hours, and Metoclopramide Hydrochloride is eliminated primarily by the kidneys, largely as unchanged drug and conjugates, so dose reduction is required in significant renal impairment.

• Take oral Motilon exactly as directed, typically 30 minutes before meals and at bedtime, unless your doctor advises otherwise.
• Motilon may be given by injection (intramuscular or intravenous) in a hospital or clinic setting by a qualified healthcare professional; intravenous doses of Motilon are given slowly.
• Do not increase the dose or frequency of Motilon on your own, and do not use Motilon for longer than your doctor has prescribed, because of the risk of tardive dyskinesia with prolonged use.
• If you miss a dose of Motilon, take it as soon as you remember unless it is close to the time of your next dose; do not double the dose.
• Avoid alcohol while taking Motilon, as it can increase drowsiness.
• Inform your doctor immediately if you notice any unusual or uncontrollable movements of the face, tongue, or limbs while taking Motilon.

• Dopaminergic drugs (levodopa, dopamine agonists): Motilon antagonizes the effect of dopaminergic drugs and may reduce their efficacy in Parkinson's disease; concurrent use is generally avoided.
• Antipsychotics and other drugs causing extrapyramidal reactions: concurrent use with Motilon increases the risk of extrapyramidal symptoms and tardive dyskinesia; combined use should be avoided where possible or monitored closely.
• CNS depressants (sedatives, hypnotics, opioids) and alcohol: Motilon can cause drowsiness that is additive with these agents, increasing sedation and impairing mental alertness.
• Monoamine oxidase inhibitors (MAOIs): Motilon may provoke hypertensive reactions in patients taking MAOIs due to release of catecholamines; concurrent use should be avoided.
• Serotonergic drugs (SSRIs, SNRIs, triptans, other serotonergic agents): Motilon has serotonergic activity and, combined with these drugs, has been associated with a risk of serotonin syndrome; monitor patients for agitation, tremor, hyperreflexia, and autonomic instability.
• Drugs affected by altered gastrointestinal motility (e.g., digoxin): by accelerating gastric emptying, Motilon may reduce the absorption of drugs such as digoxin that depend on slow gastric transit; conversely, Motilon may increase the rate and extent of absorption of drugs typically absorbed in the small bowel (e.g., cyclosporine, certain oral anticoagulants), so monitoring and dose adjustment may be needed.
• Succinylcholine: Motilon inhibits plasma cholinesterase and may prolong the neuromuscular blocking effect of succinylcholine.

Common Side Effects

• Drowsiness and fatigue
• Restlessness or nervousness
• Headache
• Diarrhea or bowel changes
• Nausea

Serious Side Effects (Seek Medical Attention)

• Acute dystonic reactions (involuntary muscle spasms of the face, neck, tongue, or eyes), akathisia (severe restlessness), and parkinsonian symptoms (tremor, rigidity) — these extrapyramidal symptoms occur more often in children, young adults, and with higher doses; see Precautions and Warnings.
• Tardive dyskinesia — involuntary, repetitive movements of the face, tongue, or limbs, which may be irreversible and is associated with prolonged use or higher cumulative doses of Motilon; see Precautions and Warnings for details.
• Symptoms of hyperprolactinemia, such as breast tenderness or enlargement, unexpected milk production (galactorrhea), or menstrual irregularities.
• Signs of neuroleptic malignant syndrome (high fever, severe muscle rigidity, altered consciousness, unstable blood pressure) — a rare but life-threatening reaction.
• Signs of an allergic reaction, such as rash, swelling of the face or throat, or difficulty breathing.
• Depression, suicidal ideation, or significant mood changes.
• Methemoglobinemia (unusual bluish discoloration of the skin, shortness of breath) — rare, reported particularly in neonates and infants given excessive doses.

Pregnancy

Motilon crosses the placenta. Available data have not shown a clear increased risk of major birth defects with Motilon use in pregnancy, but data remain limited, and animal reproduction studies do not always predict human response. Motilon should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus, and only under the direction of a qualified healthcare professional; it is not recommended for routine or non-essential use such as ordinary morning sickness unless other measures have failed.

Breastfeeding

Motilon passes into breast milk, generally in concentrations higher than in maternal plasma, and infant exposure through milk is possible. Motilon should be used with caution during breastfeeding, and only if clearly needed, with the infant monitored for drowsiness or unusual symptoms; consult a physician before using Motilon while breastfeeding.

Tardive Dyskinesia (Boxed Warning)

Treatment with Motilon can cause tardive dyskinesia, a syndrome of potentially irreversible, involuntary, repetitive movements, most often of the face, tongue, or limbs. The risk of developing tardive dyskinesia with Motilon increases with the duration of treatment and the total cumulative dose. Treatment with Motilon should be avoided for periods exceeding 12 weeks except in rare cases where therapeutic benefit is judged by the physician to outweigh the risk of developing tardive dyskinesia. There is no known treatment for tardive dyskinesia once it develops; Motilon should be discontinued immediately if signs or symptoms appear.

Extrapyramidal Symptoms

Motilon can cause acute dystonic reactions, akathisia, and parkinsonian symptoms, which occur most often within the first 24-48 hours of treatment and are more common in children, young adults, and with higher doses of Motilon. Seek prompt medical attention if involuntary muscle movements occur.

Neuroleptic Malignant Syndrome (NMS)

A potentially fatal symptom complex, NMS, has been reported with Motilon, particularly when used with other dopamine-blocking or neuroleptic agents. Discontinue Motilon immediately and seek emergency care if hyperthermia, muscle rigidity, altered mental status, or autonomic instability develop.

Depression and Suicidal Ideation

Motilon has been associated with depression, sometimes severe, including suicidal ideation and suicide, in patients with and without a prior history of depression; use with caution in patients with a history of depression and monitor for mood changes.

Hypertension in Pheochromocytoma

Motilon may cause a hypertensive crisis in patients with pheochromocytoma; see Contraindications.

Seizures

Motilon may increase the frequency and severity of seizures in patients with pre-existing seizure disorders; see Contraindications.

Fluid Overload (Injectable Use)

Formulations of Motilon containing sodium should be used with caution in patients with conditions where sodium retention is a concern, such as heart failure or cirrhosis with fluid retention.

Symptoms of Motilon overdose may include drowsiness, disorientation, extrapyramidal reactions (such as dystonic reactions, tremor, or muscle rigidity), and, in severe cases, seizures or changes in consciousness. There is no specific antidote for Motilon overdose. If overdose of Motilon is suspected, seek immediate medical attention or contact a poison control center right away; treatment is supportive and symptomatic, and extrapyramidal symptoms may be managed under medical supervision with anticholinergic, antihistaminic, or antiparkinsonian agents as directed by a physician. Do not attempt to manage a suspected overdose of Motilon at home without professional medical guidance.

Store at room temperature (below 30°C), protected from light and moisture. Keep out of reach and sight of children. Do not use beyond the expiry date printed on the pack.

Children

Motilon is associated with a higher risk of extrapyramidal reactions, including dystonic reactions, in children and young adults than in older adults, particularly at higher doses. Use of Motilon in children should be limited to situations where the potential benefit is judged by a pediatrician to outweigh this risk, at the lowest effective dose, and safety and efficacy for chronic or non-essential use in children have not been well established.

Elderly

Elderly patients, particularly those with renal impairment, may be more sensitive to the sedative and extrapyramidal effects of Motilon and may be at greater risk of developing tardive dyskinesia, particularly with prolonged treatment; use the lowest effective dose for the shortest necessary duration and monitor closely.

Renal Impairment

Dose reduction of Motilon is recommended in moderate to severe renal impairment, as clearance is reduced; see Dosage and Administration.

Hepatic Impairment

Motilon should be used with caution and with dose adjustment in patients with hepatic cirrhosis; see Dosage and Administration.

Pregnant and Breastfeeding Women

See Pregnancy and Lactation above for detailed guidance on the use of Motilon in this population.

The duration of treatment with Motilon depends on the indication: single-dose use for facilitation of small bowel intubation or radiologic examination, short courses (typically days) for postoperative or chemotherapy-related nausea and vomiting, and up to a maximum of 12 weeks for GERD or diabetic gastroparesis because of the boxed-warning risk of tardive dyskinesia with prolonged use. Treatment with Motilon beyond 12 weeks should only occur in rare cases where a physician determines the benefit clearly outweighs this risk, with regular reassessment. Do not continue Motilon longer than prescribed without consulting your doctor.

Dopamine D2-receptor antagonist; Prokinetic agent; Antiemetic

Metoclopramide Hydrochloride works mainly by blocking dopamine D2 receptors both peripherally, in the gastrointestinal tract, and centrally, in the chemoreceptor trigger zone of the brainstem. In the gastrointestinal tract, this dopamine blockade (combined with sensitization of smooth muscle to acetylcholine) increases lower esophageal sphincter tone, strengthens antral contractions, relaxes the pylorus, and increases duodenal and jejunal peristalsis, which together speed up gastric emptying and reduce gastroesophageal reflux. In the brain, blockade of dopamine receptors in the chemoreceptor trigger zone raises the threshold for triggering nausea and vomiting, producing the antiemetic effect of Metoclopramide Hydrochloride; at higher doses, Metoclopramide Hydrochloride also has some 5-HT3 receptor antagonist activity that contributes to its antiemetic effect, particularly against chemotherapy-induced nausea and vomiting. This same central dopamine blockade is responsible for the extrapyramidal effects and tardive dyskinesia risk associated with Metoclopramide Hydrochloride.

Category B (FDA legacy pregnancy category)

Motilon may be used in children under close medical supervision for indications such as prevention of chemotherapy-induced nausea and vomiting or facilitation of small bowel intubation, but children and young adults have a substantially higher risk of extrapyramidal reactions, including acute dystonic reactions, with Motilon than adults, particularly at higher doses. Safety and efficacy of Motilon for chronic use (such as GERD or gastroparesis) in children have not been well established, and such use is generally avoided. When Motilon is used in children, the lowest effective dose should be used for the shortest necessary duration, and caregivers should be advised to seek prompt medical attention if involuntary movements or muscle spasms develop. Use of Motilon in neonates and infants requires particular caution given case reports of methemoglobinemia with excessive dosing in this age group.