Reglan 10 mg Tablets

Brand Name

The medication is marketed under the brand name Reglan, a well-established label in the field of gastrointestinal motility and symptom management.

International Nonproprietary Name (INN)

The active ingredient in this product is identified globally as metoclopramide, a name standardized for consistency across international pharmacological practices.

Form of Release

Reglan is available as oral tablets, orally disintegrating tablets, oral solution, and an injectable solution. Tablets come in strengths of 5 mg and 10 mg, disintegrating tablets match these doses, the oral solution provides 5 mg per 5 mL, and the injectable form offers 5 mg per mL, typically in vials or ampules.

Composition

Each tablet or disintegrating tablet of Reglan contains metoclopramide hydrochloride as the primary active substance, with dosages of 5 mg or 10 mg (equivalent to metoclopramide base). The formulation includes several inactive ingredients, such as microcrystalline cellulose, which provides structural support, and lactose monohydrate, acting as a filler. Additional excipients like magnesium stearate serve as lubricants, while the disintegrating form includes mannitol and aspartame for rapid dissolution and taste. The oral solution contains sodium benzoate as a preservative and citric acid for pH adjustment, and the injectable solution includes sodium chloride for isotonicity, ensuring stability across all forms.

Pharmacologic Properties

Pharmacodynamics

Reglan functions as a dopamine D2 receptor antagonist and a 5-HT4 receptor agonist, exerting its effects by enhancing gastrointestinal motility and reducing nausea. Its D2 antagonism in the chemoreceptor trigger zone of the medulla suppresses nausea and vomiting, while its 5-HT4 agonism stimulates acetylcholine release in the myenteric plexus, increasing gastric emptying and intestinal peristalsis. This dual action accelerates the movement of food through the stomach and upper intestine, alleviating symptoms of delayed gastric emptying.

The medication also exhibits mild 5-HT3 receptor antagonism, contributing to its antiemetic effect, particularly in chemotherapy-induced nausea. Clinical studies demonstrate its ability to reduce vomiting episodes by 50–70% within 1–2 hours and improve gastric emptying time by 30–50% in gastroparesis. It does not alter acid secretion or mucosal integrity directly, focusing on motility and symptom relief. This multifaceted mechanism supports its efficacy in managing nausea and motility disorders.

Pharmacokinetics

Following oral administration, Reglan is absorbed rapidly from the gastrointestinal tract, with peak plasma concentrations reached within 1 to 2 hours. Bioavailability ranges from 60–80%, reduced by first-pass metabolism, and food slightly delays absorption without altering extent. The drug binds to plasma proteins at approximately 30%, distributing widely to tissues, including the brain, gastrointestinal tract, and kidneys.

Metabolism occurs in the liver via cytochrome P450 enzymes CYP2D6 and CYP1A2, converting metoclopramide into inactive conjugates like glucuronide and sulfate forms. The half-life ranges from 4 to 6 hours, supporting dosing every 6–8 hours. Elimination is predominantly renal, with 85% excreted in urine as unchanged drug (20–30%) and metabolites, with minor fecal clearance via bile.

Indications for Use

Reglan is prescribed for the short-term treatment of gastroesophageal reflux disease (GERD) in adults unresponsive to conventional therapies, relieving heartburn by enhancing gastric emptying. It is also indicated for diabetic gastroparesis, improving symptoms like nausea, bloating, and vomiting by accelerating stomach motility. The medication manages acute and recurrent nausea and vomiting, including postoperative or chemotherapy-induced cases, via oral or injectable routes.

Intravenous use is indicated for severe nausea in hospitalized patients or to facilitate small bowel intubation by enhancing peristalsis. It may be used off-label for hiccups or migraine-associated nausea, though efficacy varies. These applications highlight its role as a versatile prokinetic and antiemetic agent for acute gastrointestinal and nausea-related conditions.

Contraindications

Reglan is contraindicated in patients with known hypersensitivity to metoclopramide or any formulation component, such as aspartame in disintegrating tablets, where reactions could range from rash to anaphylaxis. It is also prohibited in those with pheochromocytoma, as its dopamine antagonism may trigger a hypertensive crisis.

Use is restricted in patients with a history of tardive dyskinesia, epilepsy, or Parkinson’s disease, as it may exacerbate movement disorders or seizures. Gastrointestinal obstruction, perforation, or hemorrhage preclude its use due to risks of worsening these conditions. Severe depression or a history of neuroleptic malignant syndrome also contraindicate it, as do children under 1 year for injectable forms due to heightened risk of extrapyramidal symptoms.

Method of Administration and Dosage

Administration Guidelines

The tablets should be taken orally, swallowed whole with water, ideally 30 minutes before meals and at bedtime to optimize motility effects. Disintegrating tablets dissolve on the tongue without water, and the oral solution requires measuring with a provided device. Intravenous or intramuscular injections are administered by healthcare professionals over 1–2 minutes or 15 minutes for infusions. Timing aligns with meal schedules or symptom onset for best results.

Dosage for Adults and Children

For adults with GERD or gastroparesis, the typical dose of Reglan is 10 mg four times daily (before meals and bedtime) for 2–8 weeks, not exceeding 12 weeks. Nausea and vomiting use 10 mg every 6–8 hours as needed, up to 40 mg daily, with intravenous dosing at 10 mg every 6–8 hours. Children aged 1–14 with GERD or nausea receive 0.1–0.2 mg/kg per dose, up to 10 mg, every 6–8 hours, not exceeding 0.8 mg/kg daily; those under 1 year are limited to supervised injectable use at 0.1 mg/kg per dose. Duration is typically limited to 5 days for acute nausea.

Dose Adjustment in Specific Conditions

In moderate to severe renal impairment (creatinine clearance below 60 mL/min), doses are reduced by 50% (e.g., 5 mg four times daily) to prevent accumulation. Mild to moderate liver dysfunction allows standard dosing, but severe cases require similar reduction due to prolonged clearance. Elderly patients or those with movement disorder risks may start at 5 mg per dose, adjusted by tolerance. Use beyond 12 weeks is discouraged unless benefits outweigh risks.

Side Effects

Reglan may cause a variety of side effects, though many patients experience only mild reactions with short-term use. Common issues include drowsiness, fatigue, or restlessness, reflecting its central dopamine effects. Nausea, diarrhea, or headache are also reported, often resolving without intervention.

Less frequent effects include extrapyramidal symptoms (e.g., tremors, rigidity), particularly with higher doses or prolonged use, and mild hypotension or tachycardia. Rare but serious reactions, such as tardive dyskinesia, neuroleptic malignant syndrome, or severe depression, require immediate cessation and medical attention. Akathisia or dystonia may occur, especially in children or the elderly. Monitoring during initial use helps manage these risks effectively.

Overdose

Symptoms of Overdose

Excessive intake of Reglan may lead to drowsiness, confusion, or extrapyramidal symptoms like muscle spasms or tremors, with higher doses causing disorientation, seizures, or hypotension. Doses exceeding 100 mg have shown no consistent lethal pattern, but symptoms reflect exaggerated dopamine antagonism.

First Aid Measures

In case of overdose, medical consultation is urgent, with antihistamines or anticholinergics (e.g., diphenhydramine) considered to reverse extrapyramidal effects under supervision. Treatment focuses on supportive care, such as fluids for hypotension or monitoring neurological status. Activated charcoal may limit absorption if given within 1 hour, with recovery typically within 24 hours.

Drug Interactions

Effects on Other Medications

Reglan enhances absorption of drugs like levodopa or cyclosporine by increasing gastric emptying, potentially raising levels, while it delays absorption of digoxin or cimetidine by slowing release. It antagonizes dopamine agonists (e.g., levodopa in Parkinson’s), reducing efficacy, and potentiates sedatives or alcohol, increasing drowsiness. Co-use with serotonergic drugs (e.g., SSRIs) may heighten extrapyramidal risk.

Drugs like cyclosporine or tacrolimus may have altered bioavailability, requiring monitoring. Patients should report all medications to their healthcare provider to manage these interactions, especially in short-term use.

Compatibility with Alcohol and Food

Alcohol enhances sedation and should be avoided during therapy to prevent excessive drowsiness or hypotension. Food does not significantly affect bioavailability, allowing administration before or after meals, though pre-meal dosing optimizes motility effects.

Special Precautions

Use During Pregnancy and Breastfeeding

Reglan is Category B in pregnancy, with no clear fetal harm in limited data, used cautiously if benefits outweigh risks, typically for severe nausea. It passes into breast milk, potentially causing sedation or motility changes in infants, so short-term use requires monitoring, guided by medical advice.

Women of childbearing age should confirm non-pregnant status before starting and discuss risks with their provider during therapy planning.

Impact on Driving and Operating Machinery

The medication may cause drowsiness or restlessness, prohibiting driving or machinery use during therapy until effects clear, typically 4–6 hours post-dose. Patients should avoid such activities if affected, with caution advised even after single doses.

Considerations for Elderly and Pediatric Populations

Elderly patients are at higher risk for tardive dyskinesia or sedation, requiring lower doses (e.g., 5 mg) and monitoring for movement disorders. Children over 1 year can use weight-adjusted dosing safely, while those under 1 are limited to supervised injectable use due to extrapyramidal risks.