Get your patient on Metoclopramide - Metoclopramide Hydrochloride injection, Solution (Metoclopramide Hydrochloride)
Metoclopramide - Metoclopramide Hydrochloride injection, Solution prescribing information
WARNING: TARDIVE DYSKINESIA
- Metoclopramide, including metoclopramide injection, can cause tardive dyskinesia (TD), a potentially irreversible serious movement disorder. In patients treated with metoclopramide, including metoclopramide injection, the risk of developing tardive dyskinesia increases with duration of treatment and total cumulative dosage.
- Metoclopramide injection, is contraindicated in patients with a history of TD.
- Immediately discontinue metoclopramide injection in patients who develop signs or symptoms of TD.
- In patients with diabetic gastroparesis, avoid a total duration of treatment with metoclopramide products, including metoclopramide injection, for longer than 12 weeks. If longer-term use is unavoidable, routinely monitor for signs and symptoms of TD.
See WARNINGS .
INDICATIONS AND USAGE
Diabetic Gastroparesis
Metoclopramide injection (metoclopramide hydrochloride, USP) is indicated for the relief of symptoms associated with acute and recurrent diabetic gastroparesis in adults.
The Prevention of Nausea and Vomiting Associated with Emetogenic Cancer Chemotherapy
Metoclopramide injection is indicated for the prophylaxis of vomiting associated with emetogenic cancer chemotherapy in adults.
The Prevention of Postoperative Nausea and Vomiting
Metoclopramide injection is indicated for the prophylaxis of postoperative nausea and vomiting in those circumstances where nasogastric suction is undesirable in adults.
Small Bowel Intubation
Metoclopramide injection is indicated to facilitate small bowel intubation in adult and pediatric patients in whom the tube does not pass the pylorus with conventional maneuvers.
Radiological Examination
Metoclopramide injection is indicated to stimulate gastric emptying and intestinal transit of barium where delayed emptying interferes with radiological examination of the stomach and/or small intestine in adults.
DOSAGE AND ADMINISTRATION
For the Relief of Symptoms Associated with Diabetic Gastroparesis
If only the earliest manifestations of diabetic gastroparesis are present, oral administration of metoclopramide may be initiated. However, if severe symptoms are present, the recommended dosage of metoclopramide injection in adults is 10 mg administered intramuscularly or intravenously over at least 1 - to 2 - minutes.
Administration of metoclopramide injection up to 10 days may be required before symptoms subside, at which time oral administration of metoclopramide may be instituted.
Avoid a total duration of treatment with metoclopramide products, including metoclopramide injection, for longer than 12 weeks. If longer-term use us unavoidable, routinely monitor for signs and symptoms of TD (see WARNINGS – Tardive Dyskinesia ).
For the Prevention of Nausea and Vomiting Associated with Emetogenic Cancer Chemotherapy
The recommended dosage of metoclopramide injection in adults is 2 mg/kg, with highly emetogenic drugs (e.g., cisplatin or dacarbazine) alone or in combination, and 1 mg/kg, with less emetogenic drugs, infused intravenously over at least 15 minutes, 30 minutes before beginning cancer chemotherapy and repeated every 2 hours for two doses, then every 3 hours for three doses.
For doses in excess of 10 mg, metoclopramide injection should be diluted in 50 mL of a parenteral solution. The preferred parenteral solution is Sodium Chloride Injection (normal saline), which when combined with metoclopramide injection, can be stored frozen for up to 4 weeks. Metoclopramide injection is degraded when admixed and frozen with Dextrose-5% in Water. Metoclopramide injection diluted in Sodium Chloride Injection, Dextrose-5% in Water, Dextrose-5% in 0.45% Sodium Chloride, Ringer's Injection, or Lactated Ringer's Injection may be stored up to 48 hours (without freezing) after preparation if protected from light. All dilutions may be stored unprotected from light under normal light conditions up to 24 hours after preparation.
If acute dystonic reactions should occur, inject 50 mg Benadryl ® (diphenhydramine hydrochloride) intramuscularly, and the symptoms usually will subside.
For the Prevention of Postoperative Nausea and Vomiting
The recommended dosage of metoclopramide injection in adults is 10 mg or 20 mg as a single intramuscular injection near the end of surgery.
To Facilitate Small Bowel Intubation
In adult and pediatric patients undergoing small bowel intubation, in whom the tube has not passed the pylorus with conventional maneuvers after 10 minutes, the recommended dosage of metoclopramide injection is a single dose administered (undiluted) by the intravenous route over at least 1 to 2 minutes:
- Adults and pediatric patients above 14 years of age : 10 mg
- Pediatric patients 6 to 14 years of age : 2.5 to 5 mg
- Pediatric patients less than 6 years of age : 0.1 mg/kg
To Aid in Radiological Examinations
In adult patients where delayed gastric emptying interferes with radiological examination of the stomach and/or small intestine, the recommended dosage of metoclopramide injection is a single 10 mg dose administered (undiluted) by the intravenous route over at least 1- to 2 - minutes.
Use in Patients with Renal Impairment
The clearance of metoclopramide is decreased, and the systemic exposure is increased in patients with moderate to severe renal impairment compared to patients with normal renal function, which may increase the risk of adverse reactions.
There is no dosage adjustment for patients with mild renal impairment (creatinine clearance greater than 60 mL/minute).
For patients with moderate or severe renal impairment (creatinine clearance less than or equal to 60 mL/minute), who are receiving more than a single dose of metoclopramide injection, reduce the metoclopramide injection dosage to one-half the dosage recommended for patients with normal renal function.
For patients with End-Stage Renal Disease (ESRD) including those treated with hemodialysis or continuous ambulatory peritoneal dialysis, who are receiving more than a single dose of metoclopramide injection, reduce the metoclopramide injection dosage to one-fourth the dosage recommended for patients with normal renal function.
See OVERDOSAGE section for information regarding dialysis.
Use in Patients with Hepatic Impairment
Patients with severe hepatic impairment (Child-Pugh C) have reduced systemic metoclopramide clearance (by approximately 50%) following intravenous administration compared to patients with normal hepatic function. The resulting increase in metoclopramide blood concentrations increases the risk of adverse reactions. There is no pharmacokinetic data in patients with moderate hepatic impairment (Child-Pugh B).
There is no dosage adjustment required for patients with mild hepatic impairment (Child-Pugh A). For patients with moderate and severe hepatic impairment (Child-Pugh B or C), who are receiving more than a single dose of metoclopramide injection, reduce the metoclopramide injection dosage to one-half the dosage recommended for patients with normal hepatic function.
NOTE: Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.
CONTRAINDICATIONS
Metoclopramide injection is contraindicated:
- in patients with a history of tardive dyskinesia (TD) or a dystonic reaction to metoclopramide. See WARNINGS .
- whenever stimulation of gastrointestinal motility might be dangerous, e.g., in the presence of gastrointestinal hemorrhage, mechanical obstruction, or perforation.
- in patients with pheochromocytoma or other catecholamine-releasing paragangliomas. Metoclopramide may cause a hypertensive/pheochromocytoma crisis, probably due to release of catecholamines from the tumor.
- in patients with known sensitivity or intolerance to metoclopramide.
- in patients with epilepsy. Metoclopramide injection may increase the frequency and severity of seizures.
ADVERSE REACTIONS
In general, the incidence of adverse reactions correlates with the dose and duration of metoclopramide administration. The following reactions have been reported, although in most instances, data do not permit an estimate of frequency.
CNS Effects
Restlessness, drowsiness, fatigue, and lassitude may occur in patients receiving the recommended prescribed dosage of metoclopramide injection. Insomnia, headache, confusion, dizziness, or mental depression with suicidal ideation also may occur (see WARNINGS ). In cancer chemotherapy patients being treated with 1-2 mg/kg per dose, incidence of drowsiness is about 70%. There are isolated reports of convulsive seizures without clear-cut relationship to metoclopramide. Rarely, hallucinations have been reported.
Extrapyramidal Reactions (EPS)
Acute dystonic reactions, the most common type of EPS associated with metoclopramide, occur in approximately 0.2% of patients (1 in 500) treated with 30 to 40 mg of metoclopramide per day. In cancer chemotherapy patients receiving 1-2 mg/kg per dose, the incidence is 2% in patients over the ages of 30-35, and 25% or higher in pediatric patients and adult patients less than 30 years of age who have not had prophylactic administration of diphenhydramine. Symptoms include involuntary movements of limbs, facial grimacing, torticollis, oculogyric crisis, rhythmic protrusion of tongue, bulbar type of speech, trismus, opisthotonus (tetanus-like reactions), and, rarely, stridor and dyspnea possibly due to laryngospasm; ordinarily these symptoms are readily reversed by diphenhydramine (see WARNINGS ).
Parkinsonian-like symptoms may include bradykinesia, tremor, cogwheel rigidity, mask-like facies (see WARNINGS ).
Tardive dyskinesia most frequently is characterized by involuntary movements of the tongue, face, mouth, or jaw, and sometimes by involuntary movements of the trunk and/or extremities; movements may be choreoathetotic in appearance (see WARNINGS ).
Motor restlessness (akathisia) may consist of feelings of anxiety, agitation, jitteriness, and insomnia, as well as inability to sit still, pacing, foot tapping. These symptoms may disappear spontaneously or respond to a reduction in dosage.
Neuroleptic Malignant Syndrome
Rare occurrences of neuroleptic malignant syndrome (NMS) have been reported. This potentially fatal syndrome is comprised of the symptom complex of hyperthermia, muscular rigidity, altered consciousness, and autonomic instability (see WARNINGS ).
Endocrine Disturbances
Galactorrhea, amenorrhea, gynecomastia, impotence secondary to hyperprolactinemia (see PRECAUTIONS ). Fluid retention secondary to transient elevation of aldosterone (see CLINICAL PHARMACOLOGY ).
Cardiovascular
Hypotension, hypertension, supraventricular tachycardia, bradycardia, fluid retention, acute congestive heart failure and possible atrioventricular (AV) block (see CONTRAINDICATIONS and PRECAUTIONS ).
Gastrointestinal
Nausea and bowel disturbances, primarily diarrhea.
Hepatic
Rarely, cases of hepatotoxicity, characterized by such findings as jaundice and altered liver function tests, when metoclopramide was administered with other drugs with known hepatotoxic potential.
Renal
Urinary frequency and incontinence.
Hematologic
A few cases of neutropenia, leukopenia, or agranulocytosis, generally without clear-cut relationship to metoclopramide. Methemoglobinemia in adults and especially with overdosage in neonates (see OVERDOSAGE ). Sulfhemoglobinemia in adults.
Allergic Reactions
A few cases of rash, urticaria, or bronchospasm, especially in patients with a history of asthma. Rarely, angioneurotic edema, including glossal or laryngeal edema.
Miscellaneous
Visual disturbances. Porphyria.
Transient flushing of the face and upper body, without alterations in vital signs, following high doses intravenously.
To report SUSPECTED ADVERSE REACTIONS, contact Avenacy at 1-855-283-6229 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
Drug Interactions
Effects of Other Drugs on Metoclopramide
Table 3 displays the effects of other drugs on metoclopramide.
| Antipsychotics | |
| Clinical Impact | Potential for additive effects, including increased frequency and severity of tardive dyskinesia (TD), other extrapyramidal symptoms (EPS), and neuroleptic malignant syndrome (NMS). |
| Intervention | Avoid concomitant use. |
| Strong CYP2D6 Inhibitors, not Included in Antipsychotic Category Above | |
| Clinical Impact | Increased plasma concentrations of metoclopramide; risk of exacerbation of extrapyramidal symptoms. |
| Intervention | Avoid metoclopramide injection. If use is unavoidable, monitor for adverse reactions |
| Examples | quinidine, bupropion, fluoxetine, and paroxetine |
| Monoamine Oxidase Inhibitors | |
| Clinical Impact | Increased risk of hypertension. |
| Intervention | Avoid concomitant use. |
| Central Nervous System (CNS) Depressants | |
| Clinical Impact | Increased risk of CNS depression. |
| Intervention | Avoid metoclopramide injection or the interacting drug, depending on the importance of the drug to the patient |
| Examples | alcohol, sedatives, hypnotics, opiates and anxiolytics |
| Drugs that Impair Gastrointestinal Motility | |
| Clinical Impact | Decreased systemic absorption of metoclopramide. |
| Intervention | Monitor for reduced therapeutic effect. |
| Examples | antiperistaltic antidiarrheal drugs, anticholinergic drugs, and opiates |
| Dopaminergic Agonists and Other Drugs that Increase Dopamine Concentrations | |
| Clinical Impact | Decreased therapeutic effect of metoclopramide due to opposing effects on dopamine. |
| Intervention | Monitor for reduced therapeutic effect. |
| Examples | apomorphine, bromocriptine, cabergoline, levodopa, pramipexole, ropinirole, and rotigotine |
Effects of Metoclopramide on Other Drugs
Table 4 displays the effects of metoclopramide on other drugs.
•Interaction does not apply to posaconazole delayed-release tablets | |
| Dopaminergic Agonists and Drugs Increasing Dopamine Concentrations | |
| Clinical Impact | Opposing effects of metoclopramide and the interacting drug on dopamine. Potential exacerbation of symptoms (e.g., parkinsonian symptoms). |
| Intervention | Avoid concomitant use. |
| Examples | Apomorphine, bromocriptine, cabergoline, levodopa, pramipexole, ropinirole, rotigotine |
| Succinylcholine, Mivacurium | |
| Clinical Impact | Metoclopramide inhibits plasma cholinesterase leading to enhanced neuromuscular blockade. |
| Intervention | Monitor for signs and symptoms of prolonged neuromuscular blockade |
| Drugs with Absorption Altered due to Increased Gastrointestinal Motility | |
| Clinical Impact | The effect of metoclopramide on other drugs is variable. Increased gastrointestinal (GI) motility by metoclopramide may impact absorption of other drugs leading to decreased or increased drug exposure. |
| Intervention | Drugs with Decreased Absorption (e.g., digoxin, atovaquone, posaconazole oral suspension•, fosfomycin) : Monitor for reduced therapeutic effect of the interacting drug. For digoxin monitor therapeutic drug concentrations and increase the digoxin dose as needed (see prescribing information for digoxin). Drugs with Increased Absorption (e.g., sirolimus, tacrolimus, cyclosporine) : Monitor therapeutic drug concentrations and adjust the dose as needed. See prescribing information for the interacting drug. |
| Insulin | |
| Clinical Impact | Increased GI motility by metoclopramide may increase delivery of food to the intestines and increase blood glucose. |
| Intervention | Monitor blood glucose and adjust insulin dosage regimen as needed. |
DESCRIPTION
Metoclopramide hydrochloride is a white crystalline, odorless substance, freely soluble in water. Chemically, it is 4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-methoxy benzamide monohydrochloride monohydrate. Molecular weight: 354.3.
 |
C 14 H 22 ClN 3 O 2 •HCl•H 2 O |
Metoclopramide Injection, USP is a clear, colorless, sterile solution with a pH of 2.5 to 6.5 for intravenous (IV) or intramuscular (IM) administration.
This product is light sensitive. It should be inspected before use and discarded if either color or particulate is observed.
Metoclopramide Injection, USP is supplied in 2 mL single-dose vials.
Each 1 mL contains: Metoclopramide base 5 mg (as the monohydrochloride monohydrate), Sodium Chloride, USP 8.5 mg, Water for Injection, USP q.s. pH adjusted, when necessary, with hydrochloric acid and/or sodium hydroxide.
CLINICAL PHARMACOLOGY
Metoclopramide stimulates motility of the upper gastrointestinal tract without stimulating gastric, biliary, or pancreatic secretions. Its mode of action is unclear. It seems to sensitize tissues to the action of acetylcholine. The effect of metoclopramide on motility is not dependent on intact vagal innervation, but it can be abolished by anticholinergic drugs.
Metoclopramide increases the tone and amplitude of gastric (especially antral) contractions, relaxes the pyloric sphincter and the duodenal bulb, and increases peristalsis of the duodenum and jejunum resulting in accelerated gastric emptying and intestinal transit. It increases the resting tone of the lower esophageal sphincter. It has little, if any, effect on the motility of the colon or gallbladder.
In patients with gastroesophageal reflux and low LESP (lower esophageal sphincter pressure), single oral doses of metoclopramide produce dose-related increases in LESP. Effects begin at about 5 mg and increase through 20 mg (the largest dose tested). The increase in LESP from a 5 mg dose lasts about 45 minutes and that of 20 mg lasts between 2 and 3 hours. Increased rate of stomach emptying has been observed with single oral doses of 10 mg.
The antiemetic properties of metoclopramide appear to be a result of its antagonism of central and peripheral dopamine receptors. Dopamine produces nausea and vomiting by stimulation of the medullary chemoreceptor trigger zone (CTZ), and metoclopramide blocks stimulation of the CTZ by agents like l-dopa or apomorphine which are known to increase dopamine levels or to possess dopamine-like effects. Metoclopramide also abolishes the slowing of gastric emptying caused by apomorphine.
Like the phenothiazines and related drugs, which are also dopamine antagonists, metoclopramide produces sedation and may produce extrapyramidal reactions, although these are comparatively rare (see WARNINGS ). Metoclopramide inhibits the central and peripheral effects of apomorphine, induces release of prolactin and causes a transient increase in circulating aldosterone levels, which may be associated with transient fluid retention.
The onset of pharmacological action of metoclopramide is 1 to 3 minutes following an intravenous dose, 10 to 15 minutes following intramuscular administration, and 30 to 60 minutes following an oral dose; pharmacological effects persist for 1 to 2 hours.
Pharmacokinetics
Metoclopramide is rapidly and well absorbed. Relative to an intravenous dose of 20 mg, the absolute oral bioavailability of metoclopramide is 80% ± 15.5% as demonstrated in a crossover study of 18 subjects. Peak plasma concentrations occur at about 1-2 hr after a single oral dose. Similar time to peak is observed after individual doses at steady state.
In a single dose study of 12 subjects, the area under the drug concentration-time curve increases linearly with doses from 20 to 100 mg. Peak concentrations increase linearly with dose; time to peak concentrations remains the same; whole body clearance is unchanged; and the elimination rate remains the same. The average elimination half-life in individuals with normal renal function is 5-6 hr. Linear kinetic processes adequately describe the absorption and elimination of metoclopramide.
Approximately 85% of the radioactivity of an orally administered dose appears in the urine within 72 hr. Of the 85% eliminated in the urine, about half is present as free or conjugated metoclopramide.
The drug is not extensively bound to plasma proteins (about 30%). The whole body volume of distribution is high (about 3.5 L/kg) which suggests extensive distribution of drug to the tissues (see Table 1 ).
| Parameter | Value |
| Vd (L/kg) | ~ 3.5 |
| Plasma Protein Binding | ~ 30% |
| t 1/2 (hr) | 5 to 6 |
| Oral Bioavailability | 80%±15.5% |
Patients with Renal Impairment
In a study of 24 patients with varying degrees of renal impairment (moderate, severe, and end-stage renal disease (ESRD) requiring dialysis), the systemic exposure (AUC) of metoclopramide following intravenous administration in patients with moderate to severe renal impairment was about 2-fold the AUC in subjects with normal renal function. The AUC of metoclopramide in patients with ESRD in dialysis was about 3.5-fold the AUC in subjects with normal renal function.
Patients with Hepatic Impairment
In a group of 8 patients with severe hepatic impairment (Child-Pugh C) administered intravenous metoclopramide, the average metoclopramide clearance was reduced by approximately 50% compared to patients with normal hepatic function.
Effect of CYP2D6 Inhibitors on Metoclopramide
In healthy subjects, 20 mg of oral metoclopramide and 60 mg of fluoxetine (a strong CYP2D6 inhibitor) were administered, following prior exposure to 60 mg fluoxetine orally for 8 days. The patients who received concomitant metoclopramide and fluoxetine had a 40% and 90% increase in metoclopramide C max and AUC 0-∞ , respectively, compared to patients who received metoclopramide alone (see Table 2 ).
| Parameter | Metoclopramide alone (mean ±SD) | Metoclopramide with fluoxetine (mean ±SD) |
| C max (ng/mL) | 44±15 | 62.7±9.2 |
| AUC 0-∞ (ng∙h/mL) | 313±113 | 591±140 |
| T 1/2 (h) | 5.5±1.1 | 8.5±2.2 |
Pediatric Patients
In pediatric patients, the pharmacodynamics of metoclopramide following oral and intravenous administration are highly variable and a concentration-effect relationship has not been established.
There are insufficient reliable data to conclude whether the pharmacokinetics of metoclopramide in adults and the pediatric population are similar.
HOW SUPPLIED
Metoclopramide Injection, USP, 5 mg per mL metoclopramide base (as the monohydrochloride monohydrate) is supplied as follows:
| NDC | Metoclopramide Injection, USP (5 mg per mL) | Package Factor |
| 83634-779-02 | 10 mg per 2 mL Single-Dose Vial | 25 vials per carton |
Storage Conditions
Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° and 30°C (59° and 86°F). [See USP Controlled Room Temperature.]
Retain in carton until time of use. Do not store open single dose vials for later use, as they contain no preservative.
This product is light sensitive. It should be inspected before use and discarded if either color or particulate is observed.
Dilutions may be stored unprotected from light under normal light conditions up to 24 hours after preparation.
Discard unused portion.
Dispense with Medication Guide.
Sterile, Nonpyrogenic, Preservative-free.
The container closure is not made with natural rubber latex.
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AVENACY
Mfd. for Avenacy Schaumburg, IL 60173 (USA) Made in India ©2026 Avenacy
Revised: April 2026
