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Anti-Emetics:
Aprepitant (Emend®)
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Mechanism of Action: Prevents acute
and delayed vomiting by selectively inhibiting the substance P/neurokinin
1 (NK1) receptor. Dosage: Adults: (Prevention of acute and delayed nausea and vomiting associated with highly-emetogenic chemotherapy in combination with a corticosteroid and 5-HT3 receptor antagonist): 125 mg on day 1, followed by 80 mg on days 2 and 3; should be used in combination with a corticosteroid and 5-HT3 receptor antagonist. In clinical trials, the following regimen was used: Aprepitant: Oral: 125 mg day 1, followed by 80 mg on days 2 and 3. Dexamethasone: Oral: 12 mg on day 1, followed 8 mg on days 2, 3, and 4. Ondansetron: I.V.: 32 mg on day 1. Supplied: 80 mg, 125 mg capsule |
dolasetron (Anzemet ®):
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Nausea (chemotherapy): 1.8 mg/kg up to 100mg IV/orally
x 1. Post-op: 12.5 mg IV x 1. Prevention: 100mg orally 2 hours preop. Mechanism of Action: Selective serotonin receptor (5-HT3) antagonist, blocking serotonin both peripherally (primary site of action) and centrally at the chemoreceptor trigger zone. Dosage: Nausea and vomiting prophylaxis, chemotherapy-induced (including initial and repeat courses): Children 2-16 years: Oral: 1.8 mg/kg within 1 hour before chemotherapy; maximum: 100 mg/dose. I.V.: 1.8 mg/kg ~30 minutes before chemotherapy; maximum: 100 mg/dose. Adults: Oral: 200 mg single dose I.V.: 0.6-5 mg/kg as a single dose. 50 mg 1-2 minute bolus. 2.4 to 3 mg/kg 20-minute infusion. Prevention of postoperative nausea and vomiting: Children 2-16 years: Oral: 1.2 mg/kg within 2 hours before surgery; maximum: 100 mg/dose. I.V.: 0.35 mg/kg (maximum: 12.5 mg) ~15 minutes before stopping anesthesia. Adults: Oral: 100 mg within 2 hours before surgery I.V.: 12.5 mg ~15 minutes before stopping anesthesia Treatment of postoperative nausea and vomiting: I.V. (only): Children: 0.35 mg/kg (maximum: 12.5 mg) as soon as needed Adults: 12.5 mg as soon as needed Administration I.V. injection may be given either undiluted IVP over 30 seconds or infused over 15 minutes. Dolasetron injection may be diluted in apple or apple-grape juice and taken orally. Supplied Injection, solution, as mesylate: 20 mg/mL (0.625 mL, 5 mL) [single-use ampuls and vial]; 20 mg/mL (25 mL) [multidose vial] Tablet, as mesylate: 50 mg, 100 mg |
droperidol (Inapsine ®):
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Mechanism of Action: Droperidol
is a butyrophenone antipsychotic; antiemetic effect is a result of
blockade of dopamine stimulation of the chemoreceptor trigger zone.
Other effects include alpha-adrenergic blockade, peripheral vascular
dilation, and reduction of the pressor effect of epinephrine resulting
in hypotension and decreased peripheral vascular resistance; may also
reduce pulmonary artery pressure Dosage - Adults: Nausea and vomiting: I.M., I.V.: Initial: 2.5 mg; additional doses of 1.25 mg may be administered to achieve desired effect; administer additional doses with caution Administration Administer I.M. or I.V.; I.V. should be administered as a rapid IVP (over 30-60 seconds); for I.V. infusion, dilute in 50-100 mL NS or D5W. ECG monitoring for 2-3 hours after administration is recommended. Supplied Injection, solution: 2.5 mg/mL (1 mL, 2 mL) |
granisetron (Kytril ®):
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Mechanism of Action: Selective
5-HT3-receptor antagonist, blocking serotonin, both peripherally on
vagal nerve terminals and centrally in the chemoreceptor trigger zone Dosage Oral: Adults: Prophylaxis of chemotherapy-related emesis: 2 mg once daily up to 1 hour before chemotherapy or 1 mg twice daily; the first 1 mg dose should be given up to 1 hour before chemotherapy. Prophylaxis of radiation therapy-associated emesis: 2 mg once daily given 1 hour before radiation therapy. I.V.: Children >/= 2 years and Adults: Prophylaxis of chemotherapy-related emesis: 10 mcg/kg/dose (or 1 mg/dose) administered IVPB over 5 minutes given within 30 minutes of chemotherapy: for some drugs (eg, carboplatin, cyclophosphamide) with a later onset of emetic action, 10 mcg/kg every 12 hours may be necessary. Breakthrough: Repeat the dose 2-3 times within the first 24 hours as necessary (not based on controlled trials, or generally recommended) Adults: PONV: Prevention: 1 mg given undiluted over 30 seconds; administer before induction of anesthesia or before reversal of anesthesia Treatment: 1 mg given undiluted over 30 seconds Supplied Injection, solution: 1 mg/mL (4 mL) [contains benzyl alcohol] Injection, solution [preservative free]: 0.1 mg/mL (1 mL); 1 mg/mL (1 mL) Solution, oral: 2 mg/10 mL (30 mL) [contains sodium benzoate; orange flavor] Tablet: 1 mg |
metoclopramide (Reglan ®):
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Mechanism of Action: Blocks
dopamine receptors and (when given in higher doses) also blocks
serotonin receptors in chemoreceptor trigger zone of the CNS; enhances
the response to acetylcholine of tissue in upper GI tract causing
enhanced motility and accelerated gastric emptying without stimulating
gastric, biliary, or pancreatic secretions; increases lower esophageal
sphincter tone Dosage - Children: Gastroesophageal reflux: Oral: 0.1-0.2 mg/kg/dose up to 4 times/day; efficacy of continuing metoclopramide beyond 12 weeks in reflux has not been determined; total daily dose should not exceed 0.5 mg/kg/day Gastrointestinal hypomotility (gastroparesis): Oral, I.M., I.V.: 0.1 mg/kg/dose up to 4 times/day, not to exceed 0.5 mg/kg/day Antiemetic (chemotherapy-induced emesis) (unlabeled): I.V.: 1-2 mg/kg 30 minutes before chemotherapy and every 2-4 hours, for a total of 5 doses (5-10 mg/kg) daily Post-pyloric feeding tube placement (unlabeled): I.V.: <6 years: 0.1 mg/kg. 6-14 years: 2.5-5 mg. Dosage - Adults: Gastroesophageal reflux: Oral: 10-15 mg/dose up to 4 times/day 30 minutes before meals or food and at bedtime; single doses of 20 mg are occasionally needed for provoking situations Gastrointestinal hypomotility (gastroparesis): Oral: 10 mg 30 minutes before each meal and at bedtime for 2-8 weeks. I.V. (for severe symptoms): 10 mg over 1-2 minutes; 10 days of I.V. therapy may be necessary for best response Antiemetic (chemotherapy-induced emesis) (unlabeled): I.V.: 1-2 mg/kg 30 minutes before chemotherapy and every 2-4 hours, for a total of 5 doses (5-10 mg/kg) daily Postoperative nausea and vomiting (unlabeled): I.M., I.V.: 10 mg near end of surgery; 20 mg doses may be used Post-pyloric feeding tube placement (unlabeled): I.M., I.V.: 10 mg Elderly: Gastroesophageal reflux: Oral: 5 mg 4 times/day (30 minutes before meals and at bedtime); increase dose to 10 mg 4 times/day if no response at lower dose Gastrointestinal hypomotility: Oral: Initial: 5 mg 30 minutes before meals and at bedtime for 2-8 weeks; increase if necessary to 10 mg doses. I.V.: Initiate at 5 mg over 1-2 minutes; increase to 10 mg if necessary Postoperative nausea and vomiting (unlabeled): I.M.: 5 mg near end of surgery; may repeat dose if necessary Dosing adjustment in renal impairment: Clcr 10-40 mL/minute: Administer at 50% of normal dose Clcr<10 mL/minute: Administer at 25% of normal dose Hemodialysis: Not dialyzable (0% to 5%); supplemental dose is not necessary Supplied Injection, solution, as hydrochloride (Reglan®): 5 mg/mL (2 mL, 10 mL, 30 mL). Syrup, as hydrochloride: 5 mg/5 mL (10 mL, 480 mL) [some products contain sodium benzoate; sugar free] Tablet, as hydrochloride (Reglan®): 5 mg, 10 mg |
ondansetron (Zofran ®):
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Mechanism of Action: Selective
5-HT3-receptor antagonist, blocking serotonin, both peripherally on
vagal nerve terminals and centrally in the chemoreceptor trigger zone ------------------------------------------------------- Children: I.V.: Chemotherapy-induced emesis: 4-18 years: 0.15 mg/kg/dose administered 30 minutes prior to chemotherapy, 4 and 8 hours after the first dose or 0.45 mg/kg/day as a single dose Postoperative nausea and vomiting: 2-12 years: </= 40 kg: 0.1 mg/kg >40 kg: 4 mg Oral: Chemotherapy-induced emesis: 4-11 years: 4 mg 30 minutes before chemotherapy; repeat 4 and 8 hours after initial dose, then 4 mg every 8 hours for 1-2 days after chemotherapy completed >/= 12 years: Refer to adult dosing. ------------------------------------------------------- Adults: I.V.: Chemotherapy-induced emesis: 0.15 mg/kg 3 times/day beginning 30 minutes prior to chemotherapy or 0.45 mg/kg once daily or 8-10 mg 1-2 times/day or 24 mg or 32 mg once daily I.M., I.V.: Postoperative nausea and vomiting: 4 mg as a single dose approximately 30 minutes before the end of anesthesia, or as treatment if vomiting occurs after surgery Oral: Chemotherapy-induced emesis: Highly-emetogenic agents/single-day therapy: 24 mg given 30 minutes prior to the start of therapy. Moderately-emetogenic agents: 8 mg every 12 hours beginning 30 minutes before chemotherapy, continuously for 1-2 days after chemotherapy completed. Total body irradiation: 8 mg 1-2 hours before daily each fraction of radiotherapy Single high-dose fraction radiotherapy to abdomen: 8 mg 1-2 hours before irradiation, then 8 mg every 8 hours after first dose for 1-2 days after completion of radiotherapy Postoperative nausea and vomiting: 16 mg given 1 hour prior to induction of anesthesia ------------------------------------------------------- Elderly: No dosing adjustment required Dosage adjustment in renal impairment: No dosing adjustment required. Dosage adjustment in hepatic impairment: Maximum daily dose: 8 mg in patients with severe liver disease (Child-Pugh score >/= 10) Supplied: Infusion [premixed in D5W] (Zofran®): 32 mg (50 mL). Injection solution (Zofran®): 2 mg/mL (2 mL, 20 mL). Oral Soln (Zofran®): 4 mg/5 mL (50 mL) . Tablet (Zofran®): 4 mg, 8 mg, 24 mg Tablet, orally-disintegrating (Zofran® ODT): 4 mg, 8 mg. |
prochlorperazine (Compazine ®):
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IMechanism of Action:
Prochlorperazine is a piperazine phenothiazine antipsychotic which
blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the
brain, including the medullary chemoreceptor trigger zone; exhibits a
strong alpha-adrenergic and anticholinergic blocking effect and
depresses the release of hypothalamic and hypophyseal hormones; believed
to depress the reticular activating system, thus affecting basal
metabolism, body temperature, wakefulness, vasomotor tone and emesis Antiemetic: Adults: Oral: 5-10 mg 3-4 times/day; usual maximum: 40 mg/day. I.M.: 5-10 mg every 3-4 hours; usual maximum: 40 mg/day I.V.: 2.5-10 mg; maximum 10 mg/dose or 40 mg/day; may repeat dose every 3-4 hours as needed Rectal: 25 mg twice daily Surgical nausea/vomiting: Adults: I.M.: 5-10 mg 1-2 hours before induction; may repeat once if necessary. I.V.: 5-10 mg 15-30 minutes before induction; may repeat once if necessary. Antipsychotic: Adults: Oral: 5-10 mg 3-4 times/day; doses up to 150 mg/day may be required in some patients for treatment of severe disturbances I.M.: 10-20 mg every 4-6 hours may be required in some patients for treatment of severe disturbances; change to oral as soon as possible Nonpsychotic anxiety: Oral: Adults: Usual dose: 15-20 mg/day in divided doses; do not give doses >20 mg/day or for longer than 12 weeks Elderly: Behavioral symptoms associated with dementia (unlabeled use): Initial: 2.5-5 mg 1-2 times/day; increase dose at 4- to 7-day intervals by 2.5-5 mg/day; increase dosing intervals (twice daily, 3 times/day, etc) as necessary to control response or side effects; maximum daily dose should probably not exceed 75 mg in elderly; gradual increases (titration) may prevent some side effects or decrease their severity Hemodialysis: Not dialyzable (0% to 5%) Administration----------------------------------------------------------- May be administered orally, I.M., or I.V.: I.V. doses should be given as a short (~30 minute) infusion or by slow (5-10 minutes) IVP to avoid orthostatic hypotension. To Control Severe Nausea and Vomiting Adjust dosage to the response of the individual. Begin with the lowest recommended dosage. I.M. Dosage Initially 5 to 10 mg (1 to 2 mL) injected deeply into the upper outer quadrant of the buttock. If necessary, repeat every 3 or 4 hours. Total I.M. dosage should not exceed 40 mg per day. I.V. Dosage 2½ to 10 mg (½ to 2 mL) by slow I.V. injection or infusion at a rate not to exceed 5 mg per minute. Compazine Injection may be administered either undiluted or diluted in isotonic solution. A single dose of the drug should not exceed 10 mg; total I.V. dosage should not exceed 40 mg per day. When administered I.V., do not use bolus injection. Hypotension is a possibility if the drug is given by I.V. injection or infusion. Subcutaneous administration is not advisable because of local irritation. Supplied Injection, solution, as edisylate: 5 mg/mL (2 mL, 10 mL) [contains benzyl alcohol] Suppository, rectal: 2.5 mg (12s), 5 mg (12s), 25 mg (12s) [may contain coconut and palm oil] Tablet, as maleate: 5 mg, 10 mg |
scopolamine:
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Mechanism of Action Blocks the action of acetylcholine at parasympathetic sites in smooth muscle, secretory glands and the CNS; increases cardiac output, dries secretions, antagonizes histamine and serotonin Scopolamine hydrobromide: Preoperative: Adults: I.M., I.V., SubQ: 0.3 to 0.65 mg; may be repeated every 4 to 6 hours Transdermal patch: Apply 2.5 cm 2 patch to hairless area behind ear the night before surgery or 1 hour prior to cesarean section (the patch should be applied no sooner than 1 hour before surgery for best results and removed 24 hours after surgery) Motion sickness: Transdermal: Adults: Apply 1 disc behind the ear at least 4 hours prior to exposure and every 3 days as needed; effective if applied as soon as 2-3 hours before anticipated need, best if 12 hours before Supplied Injection, solution, as hydrobromide: 0.4 mg/mL (1 mL) Transdermal system (Transderm Scop®): 1.5 mg (4s) [releases ~1 mg over 72 hours] |
trimethobenzamide (Tigan ®):
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Oral: 250 mg orally every 6 to 8 hours IM / Rectal: 200mg IM or rectally every 6 to 8 hours. |
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GlobalRPH does not directly or indirectly practice medicine or provide
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any diagnosis or treatment made in reliance thereon. David F. McAuley, Pharm.D., R.Ph. GlobalRPh Inc. |
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