Names and pronunciation
(met-oh-kloe-pra′mide) Gimoti, Maxeran , Metonia , Reglan
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Drug reference
(met-oh-kloe-pra′mide) Gimoti, Maxeran , Metonia , Reglan
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Func. class.: Cholinergic, antiemetic, GI stimulant
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Chem. class.: Central dopamine receptor antagonist
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Do not confuse: metoclopramide/metOLazone
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ACTION: Enhances response to ace- tylcholine of tissue in upper GI tract, which causes the contraction of gastric muscle; relaxes pyloric, duodenal seg- ments; increases peristalsis without stimulating secretions; blocks DOPamine in chemoreceptor trigger zone of CNS
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USES: Prevention of nausea, vomiting induced by chemotherapy, radiation, delayed gastric emptying, gastroesophageal reflux
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CONTRAINDICATIONS: Hyper- sensitivity to this product, procaine, or procainamide; seizure disorder, pheo- chromocytoma, GI obstruction, hemor- rhage/perforation, child <1 yr Precautions: Pregnancy, breastfeeding, Parkinson’s disease, breast cancer (pro- lactin dependent), abrupt discontinua- tion, cardiac disease, children, depres- sion, diabetes mellitus, G6PD deficiency, geriatrics, heart failure, hypertension, infertility, malignant hyperthermia, met- hemoglobinemia, procainamide/paraben hypersensitivity, renal impairment
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Black Box Warning: Tardive dyskinesia Black Box Warning: EPS, tardive dys- kinesia; more likely to occur in treatment >3 mo, geriatric patients and may be ir- reversible; assess for involuntary move- ments often; avoid using phenothiazines, haloperidol • Neuroleptic malignant syndrome: hyperthermia, change in B/P, pulse, tachy- cardia, sweating, rigidity, altered con- sciousness (rare) • Mental status: depression, anxiety, ir- ritability • GI complaints: nausea, vomiting, an- orexia, constipation; assess bowel sounds • Pregnancy/breastfeeding: use only if clearly needed; no studies in preg- nancy; do not breastfeed, appears in breast milk • Beers: avoid in older adults unless for gastroparesis; can cause extrapyramidal effects; monitor for EPS frequently Black Box Warning: Symptoms of EPS, tardive dyskinesia; to report to prescriber • How to use oral disintegrating product
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SIDE EFFECTS CNS: Sedation, fatigue, restlessness, headache, sleeplessness, dystonia, dizzi- ness, drowsiness, suicidal ideation, seizures, EPS, neuroleptic malignant syndrome; tar- dive dyskinesia (>3 mo, high doses) CV: Hypotension, supraventricular tachycardia GI: Dry mouth, constipation, nausea, anorexia, vomiting, diarrhea GU: Decreased libido, prolactin secre- tion, amenorrhea, galactorrhea HEMA: Neutropenia, leukopenia, agranulocytosis INTEG: Urticaria, rash
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INTERACTIONS • Avoid use with MAOIs; may increase hypertension Increase: sedation—alcohol, other CNS depressants; avoid concurrent use Increase: risk for EPS—haloperidol, phenothiazines; assess for EPS Decrease: action—anticholinergics, opi- ates; avoid using together or assess carefully Drug/Lab Test Increase: prolactin, aldosterone, thyrotropin
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DOSAGE AND ROUTES Nausea/vomiting (chemotherapy) • Adult: IV 1-2 mg/kg 30 min before administration of chemotherapy, then q2hr × 2 doses, then q3hr × 3 doses • Child (unlabeled): IV 1-2 mg/kg/dose Facilitate small-bowel intubation for radiologic exams • Adult and child >14 yr: IV 10 mg over 1-2 min • Child <6 yr: IV 0.1 mg/kg • Child 6-14 yr: IV 2.5-5 mg Diabetic gastroparesis • Adult: PO 10 mg 30 min before meals, at bedtime × 2-8 wk; Nasal Spray: Adult <65 yr: 1 spray (15 mg) in 1 nos- tril, 30 min before meals and bedtime × 2-8 wk (max 4 sprays/day; >65 yr not recommended • Geriatric: PO 5 mg 30 min before meals, at bedtime, increase to 10 mg if needed Gastroesophageal reflux • Adult: PO 10-15 mg qid 30 min before meals and at bedtime • Child: PO 0.4-0.8 mg/kg/day in 4 di- vided doses Renal dose • Adult: PO CCr <60 mL/min, 5 mg qid, max 20 mg/day, or CCr 10-15 mL/min give 75% of normal dose; CCr <10 mL/min give 50% of normal dose
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Available forms: Tabs 5, 10 mg; syr 1 mg/mL , solution for inj 5 mg/mL, 10 mg/2 mL; oral sol 5 mg/5 mL, 10 mg/10 mL; orally disintegrating tab 5, 10 mg; nasal spray 15 mg/actuation
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Administer: • Total daily dose, max 0.5 mg/kg except in platinum-based chemotherapy PO route • ½-1 hr before meals and at bedtime for better absorption • Gum, hard candy, frequent rinsing of mouth for dry oral cavity • Oral disintegrating: place on tongue, al- low to dissolve, swallow; remove from blis- ter immediately before use; give ≥30 min before meals and at bedtime; do not use if tablet breaks Nasal Spray • Prime before first use, use 10 sprays • Lean head slightly forward to use, close other nostril with finger, press firmly, while inhaling, wipe tip when done IM route • Give for postoperative nausea, vomit- ing before end of surgery Direct IV route • DiphenhydrAMINE IV or benztropine IM for EPS • Undiluted if dose ≤10 mg; give by slow injection over 2 min Intermittent IV INFUSION route • 10-mL and 30-mL vials (50 mg and 150 mg, respectively, in 5 mg/mL) are used for IV infusion with dilu- tion: Dilute calculated amount in ≥50 mL D5W, NaCl, given over ≥15 min • Max 5 mg/min infusion route • Infusions are stable at room tempera- ture for 24 hr • Discard unused portions Y-site compatibilities: Acetaminophen, alfentanil, amifostine, amikacin, aminoph ylline, ascorbic acid, atracurium, atropine, azaTHIOprine, aztreonam, bivalirudin, bleomycin, bumetanide, buprenorphine, butorphanol, calcium chloride/gluco- nate, CARBOplatin, caspofungin, ceFAZo- lin, cefonicid, cefoperazone, cefotaxime, cefoTEtan, cefOXitin, cefTAZidime, cef tizoxime, cefTRIAXone, cefuroxime, chloramphenicol, chlorproMAZINE, ci- metidine, ciprofloxacin, cisatracurium, CISplatin, cladribine, clindamycin, cya- nocobalamin, cyclophosphamide, cyclo- SPORINE, cytarabine, DACTINomycin, DAPTOmycin, dexamethasone, dexme- detomidine, digoxin, diltiaZEM, diphen- hydrAMINE, DOBUTamine, DOCEtaxel, DOPamine, doripenem, doxapram, DOXOrubicin hydrochloride, doxycy- cline, droperidol, enalaprilat, ePHED- rine, EPINEPHrine, epiRUBicin, epoetin M alfa, ertapenem, erythromycin, esmolol, etoposide, etoposide phosphate, famotidine, fenoldopam, fentaNYL, filgrastim, flucon- azole, fludarabine, folic acid, foscarnet, gallium nitrate, gemcitabine, gentamicin, glycopyrrolate, granisetron, heparin, hydrocortisone, HYDROmorphone, IDA rubicin, ifosfamide, imipenem/cilastatin, indomethacin, insulin, isoproterenol, ketorolac, labetalol, leucovorin, levo- FLOXacin, lidocaine, linezolid, LORaze- pam, magnesium sulfate, mannitol, mechlorethamine, melphalan, meperi- dine, meropenem, metaraminol, meth adone, methotrexate, methoxamine, methyldopate, methylPREDNISolone, metoprolol, metroNIDAZOLE, miconazole, midazolam, milrinone, minocycline, mito- MYcin, morphine, moxalactam, multiple vitamins, nafcillin, nalbuphine, naloxone, nesiritide, nitroglycerin, nitroprusside, norepinephrine, octreotide, ondanse- tron, oxaliplatin, oxytocin, PACLitaxel, palonosetron, pantoprazole, papaverine, PEMEtrexed, penicillin G, pentamidine, pentazocine, PENTobarbital, PHENobarbi- tal, phentolamine, phenylephrine, phytona dione, piperacillin/tazobactam, potassium chloride, procainamide, prochlorperazine, promethazine, propranolol, protamine, pyridoxine, quinupristin/dalfopristin, raNITIdine, remifentanil, riTUXimab, ro- curonium, sargramostim, sodium acetate/ bicarbonate, succinylcholine, SUFentanil, tacrolimus, teniposide, theophylline, thi- amine, thiotepa, ticarcillin/clavulanate, tigecycline, tirofiban, tobramycin, tolazo- line, topotecan, trastuzumab, trimethaphan, urokinase, vancomycin, vasopressin, ve- curonium, verapamil, vinBLAStine, vinCRIS- tine, vinorelbine, voriconazole, zidovudine
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Assess:
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Evaluate: • Therapeutic response: absence of nau- sea, vomiting, anorexia, fullness; de- creased GERD
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To avoid driving, other hazardous ac- tivities until stabilized on product • To avoid alcohol, other CNS depres- sants that will enhance sedating proper- ties of this product
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PHARMACOKINETICS Metabolized by liver, excreted in urine, half-life 2½-6 hr PO: Onset ½-1 hr, duration 1-2 hr IM: Onset 10-15 min, duration 1-2 hr IV: Onset 1-3 min, duration 1-2 hr
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• Adult: IV 1-2 mg/kg 30 min before administration of chemotherapy, then q2hr × 2 doses, then q3hr × 3 doses
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• Child (unlabeled): IV 1-2 mg/kg/dose Facilitate small-bowel intubation for radiologic exams
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• Adult and child >14 yr: IV 10 mg over 1-2 min
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• Child <6 yr: IV 0.1 mg/kg
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• Child 6-14 yr: IV 2.5-5 mg Diabetic gastroparesis
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• Adult: PO 10 mg 30 min before meals, at bedtime × 2-8 wk; Nasal Spray: Adult <65 yr: 1 spray (15 mg) in 1 nos- tril, 30 min before meals and bedtime × 2-8 wk (max 4 sprays/day; >65 yr not recommended
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• Geriatric: PO 5 mg 30 min before meals, at bedtime, increase to 10 mg if needed Gastroesophageal reflux
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• Adult: PO 10-15 mg qid 30 min before meals and at bedtime
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• Child: PO 0.4-0.8 mg/kg/day in 4 di- vided doses Renal dose
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• Adult: PO CCr <60 mL/min, 5 mg qid, max 20 mg/day, or CCr 10-15 mL/min give 75% of normal dose; CCr <10 mL/min give 50% of normal dose
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