metoclopramide intranasal (Rx)

Brand and Other Names:Gimoti
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

intranasal solution

  • 15mg/actuation
  • Each bottle contains 9.8 mL

Gastroparesis

Indicated for symptomatic relief in adults with acute and recurrent diabetic gastroparesis

<65 years

  • 1 spray (15 mg) in 1 nostril, 30 min before each meal and at bedtime (up to 4x/day) for 2-8 weeks, depending on symptomatic response

Dosage Modifications

Renal impairment

  • Mild (CrCl ≥60 mL/min): No dosage adjustment necessary
  • Moderate-to-severe (CrCl <60 mL/min) and patients on hemodialysis or peritoneal dialysis: Not recommended

Hepatic impairment

  • Mild (Child-Pugh A): No dosage adjustment necessary
  • Moderate-to-severe (Child-Pugh B or C): Not recommended

Dosing Considerations

Use not recommended

  • Glucose-6-phosphate dehydrogenase (G6PD) deficiency with metoclopramide-induced methemoglobinemia treated with methylene blue
  • CYP2D6 poor metabolizers
  • Coadministration with strong CYP2D6 inhibitors

Use not recommended owing to risk of developing tardive dyskinesia and other extrapyramidal symptoms, as well as the risk of methemoglobinemia in neonates

Gastroparesis

Indicated for symptomatic relief in adults with acute and recurrent diabetic gastroparesis

≥65 years

  • Geriatric patients may be more sensitive to the adverse effects of metoclopramide and require a lower initial dose
  • Not recommended as initial therapy
  • If receiving an alternative metoclopramide product at a stable dose of 10 mg QID, may be switched to metoclopramide intranasal 1 spray (15 mg) in 1 nostril, 30 min before each meal and at bedtime (up to 4x/day) for 2-8 weeks, depending on symptomatic response
  • Avoid treatment with metoclopramide (all dosage forms and routes of administration) for >12 weeks because of the increased risk of developing tardive dyskinesia with longer-term use

Dosage Modifications

Renal impairment

  • Mild (CrCl ≥60 mL/min): No dosage adjustment necessary
  • Moderate-to-severe (CrCl <60 mL/min) and patients on hemodialysis or peritoneal dialysis: Not recommended

Hepatic impairment

  • Mild (Child-Pugh A): No dosage adjustment necessary
  • Moderate-to-severe (Child-Pugh B or C): Not recommended

Dosing Considerations

Use not recommended

  • Glucose-6-phosphate dehydrogenase (G6PD) deficiency with metoclopramide-induced methemoglobinemia treated with methylene blue
  • CYP2D6 poor metabolizers
  • Coadministration with strong CYP2D6 inhibitors
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Interactions

Interaction Checker

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            Adverse Effects

            ~10%

            Restlessness

            Drowsiness

            Fatigue

            Lassitude

            Frequency Not Defined

            CNS disorders: Tardive dyskinesia, acute dystonic reactions, drug-induced parkinsonism, akathisia, other extrapyramidal symptoms, convulsive seizure, hallucinations, neuroleptic malignant syndrome, serotonin syndrome (in combination with serotonergic agents)

            Endocrine disorders: Fluid retention secondary to transient elevation of aldosterone, galactorrhea, amenorrhea, gynecomastia, impotence secondary to hyperprolactinemia

            Cardiovascular disorders: Acute congestive heart failure, possible atrioventricular block, hypotension, hypertension, supraventricular tachycardia, bradycardia, fluid retention

            GI disorders: Nausea, bowel disturbances (primarily diarrhea)

            Hepatic disorders: Hepatotoxicity

            Renal and urinary disorders: Urinary frequency, urinary incontinence

            Hematologic disorders: Agranulocytosis, neutropenia, leukopenia, methemoglobinemia, sulfhemoglobinemia

            Hypersensitivity reactions: Bronchospasm (especially in patients with a history of asthma), urticaria, rash, angioedema (including glossal or laryngeal edema)

            Eye disorders: Visual disturbances

            Metabolism disorders: Porphyria

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            Warnings

            Black Box Warnings

            Tardive dyskinesia

            • Metoclopramide can cause tardive dyskinesia (TD), a serious movement disorder that is often irreversible; the risk of developing TD increases with duration of treatment and total cumulative dosage
            • Discontinue treatment in patients who develop signs or symptoms of TD; symptoms may lessen or resolve after metoclopramide is stopped
            • Avoid treatment (all dosage forms and routes of administration) for >12 weeks because of the increased risk of developing TD with longer-term use

            Contraindications

            History of TD or dystonic reaction to metoclopramide

            When stimulation of GI motility might be dangerous (eg, GI hemorrhage, mechanical obstruction, perforation)

            Pheochromocytoma or other catecholamine-releasing paragangliomas

            Epilepsy

            Hypersensitivity to metoclopramide

            Cautions

            Can cause TD, a syndrome of potentially irreversible and disfiguring involuntary movements of the face or tongue, and sometimes of the trunk and/or extremities

            In addition to TD, may cause other extrapyramidal symptoms (EPSs), parkinsonian symptoms, and motor restlessness; advise patients to seek immediate medical attention if such symptoms occur and to discontinue treatment

            Depression has occurred with and without a history of depression; avoid use with a history of depression

            May produce transient increases in plasma aldosterone and increased risk for fluid retention and volume; caution in patients at risk of fluid overload (heart failure or cirrhosis); discontinue if any of these adverse reactions occur

            Mental and/or physical abilities required for the performance of hazardous tasks (eg, operating machinery, driving a motor vehicle) may be impaired

            Not recommended with moderate or severe renal or hepatic impairment, patients who are CYP2D6 poor metabolizers, or coadministration with strong CYP2D6 inhibitors; increased exposure to metoclopramide due to reduced metabolism or excretion may lead to increased adverse reactions, including TD

            Neuroleptic malignant syndrome

            • Neuroleptic malignant syndrome (NMS) has been reported in association with metoclopramide overdosage and concomitant treatment with another drug associated with NMS
            • Avoid in patients receiving other drugs associated with NMS, including typical and atypical antipsychotics
            • Management of NMS includes
              • Immediately discontinue other drugs not essential to concurrent therapy
              • Intensive symptomatic treatment and medical monitoring
              • Treatment of any concomitant serious medical problems for which specific treatments are available

            Hypertension

            • May elevate blood pressure
            • Hypertensive crises also reported in patients with undiagnosed pheochromocytoma
            • Contraindicated in patients with pheochromocytoma or other catecholamine-releasing paragangliomas
            • Discontinue treatment in any patient with a rapid rise in blood pressure

            Hyperprolactinemia

            • May elevate prolactin levels
            • Hyperprolactinemia may suppress hypothalamic gonadotropin-releasing hormone and eventually may inhibit reproductive function by impairing gonadal steroidogenesis in both females and males
            • Galactorrhea, amenorrhea, gynecomastia, and impotence reported with prolactin-elevating drugs

            Drug interaction overview

            • Metoclopramide is a CYP2D6 substrate
            • Strong CYP2D6 inhibitors
              • Not recommended
              • Coadministration with CYP2D6 inhibitors may increase plasma concentrations of metoclopramide
            • CNS depressants
              • Avoid use of metoclopramide intranasal or interacting drug, depending on importance of drug to patient
              • Coadministration with CNS depressants may increase effects of CNS depression
            • Antipsychotics
              • Avoid coadministration
              • Coadministration with antipsychotics may enhance the frequency and severity of TD, other EPSs, and NMS
            • Monoamine oxidase inhibitors (MAOIs)
              • Avoid coadministration
              • Coadministration of MAOIs may increase risk of hypertension
            • Drugs that may impair GI motility
              • Coadministration may decrease systemic absorption of metoclopramide
              • Monitor for reduced therapeutic effect
            • Dopamine agonists and other drugs that increase dopamine concentrations
              • Avoid use
              • Coadministration may have opposing effects on each other
            • Succinylcholine or mivacurium
              • Metoclopramide may enhance the neuromuscular-blocking effect of succinylcholine or mivacurium; monitor for signs and symptoms of prolonged neuromuscular blockade
            • Drugs with absorption altered due to increased GI motility
              • Increased GI motility by metoclopramide may impact absorption of other drugs, leading to decreased or increased drug exposure
              • Monitor therapeutic effect of the drugs with altered absorption
            • Insulin
              • Increased GI motility by metoclopramide may increase delivery of food to the intestines and increase blood glucose
              • Monitor blood glucose and adjust insulin dosage regimen as needed
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            Pregnancy & Lactation

            Pregnancy

            Published studies do not report a consistent pattern or a consistently increased risk of adverse pregnancy-related outcomes with oral use of metoclopramide during pregnancy

            However, available data from a case report of use in pregnancy are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes

            There are potential risks to the neonate following exposure in utero to metoclopramide during delivery

            Animal data

            • No adverse developmental effects were observed with oral administration of metoclopramide to pregnant rats and rabbits at exposures about 6 and 12x the maximum recommended human dose

            Clinical considerations

            • Metoclopramide crosses the placental barrier and may cause extrapyramidal signs and methemoglobinemia in neonates with maternal administration during delivery
            • Monitor neonates for extrapyramidal signs

            Lactation

            No data available on the presence in human milk following nasal administration

            However, published data report presence in human milk in variable amounts following oral administration

            Breastfed infants exposed to metoclopramide have experienced GI adverse reactions, including intestinal discomfort and increased intestinal gas formation

            Clinical considerations

            • Monitor breastfeeding neonates because metoclopramide may cause extrapyramidal signs (eg, dystonias) and methemoglobinemia

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Metoclopramide stimulates motility of the upper GI tract without stimulating gastric, biliary, or pancreatic secretions

            Exact mechanism of action of metoclopramide has not been fully established

            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

            Absorption

            Peak plasma concentration: 41 ng/mL

            Peak plasma time: 1.25 hr

            AUC: 349 ng⋅hr/mL

            Distribution

            Protein bound: ~30%

            Vd: ~3.5 L/kg

            Metabolism

            Primarily metabolized by CYP2D6, which forms monodeethylmetoclopramide (a major oxidative metabolite)

            Elimination

            Half-life: 8.1 hr

            Excretion: Urine (~85% within 72 hr; 18-20% of free metoclopramide within 36 hr)

            Pharmacogenomics

            NADH-Cytochrome b5 Reductase Deficiency

            • Metoclopramide-treated patients with NADH-cytochrome b5 reductase deficiency are at an increased risk of developing methemoglobinemia and/or sulfhemoglobinemia
            • For patients with G6PD deficiency with metoclopramide-induced methemoglobinemia, methylene blue treatment is not recommended
            • Methylene blue may cause hemolytic anemia in patients with G6PD deficiency, which may be fatal

            CYP2D6 poor metabolizers

            • Elimination of metoclopramide may be slowed in patients who are CYP2D6 poor metabolizers, possibly increasing the risk of dystonic and other adverse reactions to metoclopramide
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            Administration

            Intranasal Administration

            Avoid treatment with metoclopramide (all dosage forms and routes of administration) for >12 weeks because of the increased risk of developing tardive dyskinesia with longer-term use

            1 spray in 1 nostril administers the appropriate dose

            Before administering first dose, prime pump by releasing 10 sprays in the air

            Place nozzle tip under 1 nostril and lean the head slightly forward

            Close other nostril with the other index finger; move spray pump upwards so the tip of the nozzle is in the nostril

            To ensure a full dose, hold bottle upright while pressing down firmly on finger flange and release while inhaling slowly through the open nostril

            Remove nozzle tip from nostril and exhale slowly through the mouth

            Wipe spray nozzle with a clean tissue

            Missed or incomplete doses

            • If uncertain that the spray entered the nose, do not repeat the dose; take the next dose at the scheduled time
            • Missed dose: Take the next dose at the regularly scheduled time; do not make up for the missed dose or double the next dose

            Storage

            Unused bottle

            • Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

            Open bottle

            • Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
            • Discard 4 weeks after opening even if bottle contains unused drug
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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.