methotrimeprazine

Contraindicated in:

Hypersensitivity to methotrimeprazine, phenothiazines, or sulfites;
Blood dyscrasias;
Hepatic impairment;
Patients in coma or those who have overdosed on CNS depressants, including alcohol, analgesics, opioids, or sedative/hypnotics;
OB: Pregnancy.

Use Cautiously in:

History of seizures;
History of glaucoma or prostatic hypertrophy (↑ risk of anticholinergic adverse reactions);
Bradycardia, electrolyte abnormalities, congenital/acquired prolonged QT interval, or concurrent use of drugs that may prolong QT interval (↑ risk of serious arrhythmias);
Underlying cardiovascular disease, including stroke, arteriosclerosis, or thromboembolism (↑ risk of adverse cardiovascular effects);
Lactation: Safety and effectiveness not established in breastfeeding;
Geri: ↑risk of stroke, cognitive decline, and mortality in older adults with dementia.

Adv. Reactions/Side Effects ⬆ ⬇

CV: orthostatic hypotension, bradycardia, palpitations, tachycardia

EENT: nasal congestion

Endo: hyperglycemia, hyperprolactinemia

GI: constipation, abdominal discomfort, dry mouth, nausea, vomiting

GU: difficulty in urination

Hemat: blood dyscrasias

Local: pain at injection site

Neuro: amnesia, drowsiness, sedation, disorientation, euphoria, extrapyramidal reactions, headache, NEUROLEPTIC MALIGNANT SYNDROME (NMS), SEIZURES, slurred speech, tardive dyskinesia, weakness.

Misc: chills

Interactions ⬆ ⬇

Drug-drug:

↑CNS depression with other CNS depressants, including alcohol, antihistamines, antidepressants, opioids, or sedative/hypnotics; ↓ dose of these agents by 50% initially.
↑anticholinergic effects with antihistamines, antidepressants, phenothiazines, quinidine, disopyramide, atropine, or scopolamine; ↓ doses of atropine or scopolamine.
Reverses vasopressor effects of epinephrine; avoid concurrent use; if vasopressor required, use phenylephrine or norepinephrine.
↑risk of hypotension with acute ingestion of alcohol, nitrates, MAO inhibitors, or antihypertensives.
Succinylcholine may result in tachycardia, hypotension, CNS stimulation, delirium, and ↑ extrapyramidal symptoms.

Drug-Natural Products:

kava, skullcap, valerian, chamomile, or hops may ↑ risk of CNS depression.

Availability ⬆ ⬇

Tablets: 2 mg; 5 mg; 25 mg; 50 mg
Solution for injection: 25 mg/mL

Route/Dosage ⬆ ⬇

PO (Adults ): Minor conditions: 6–25 mg/day in 3 divided doses (if sedation occurs, use smaller daytime doses and a larger dose at bedtime); Nighttime sedative: 10–25 mg as a single bedtime dose; Psychoses/intense pain: 50–75 mg/day in 2–3 divided doses; may ↑ dose to desired effect (doses of ≥1 g/day have been used; if dose exceeds 100–200 mg/day, administer in divided doses and keep patient on bedrest).
PO (Children ): 0.25 mg/kg/day in 2–3 divided doses (not to exceed 40 mg/day in children <12 yr).
IM (Adults ): Postoperative analgesic adjunct: 10–25 mg every 8 hr; if given with opioids, ↓ opioid dose by 50%.
IM (Children ): Analgesia: 62.5–125 mcg (0.0625–0.125 mg)/kg/day single dose or divided doses; change to oral medication as soon as possible.
IV (Children ): Palliative care setting: 62.5 mcg (0.0625 mg)/kg/day as a slow infusion.

Action ⬆ ⬇

Antagonizes dopamine receptors; also antagonizes alpha-1, alpha-2, serotonin, and muscarinic receptors.

Therapeutic effects:

Decreased manifestations of psychotic disturbances.
Reduction in severity of pain.
Reduction in nausea/vomiting.

Classifications ⬆ ⬇

Therapeutic Classification: antipsychotics, nonopioid analgesics

Pharmacologic Classification: phenothiazines

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed after oral and IM administration. IV administration results in complete bioavailability.

Distribution: Enters CSF.

Metabolism/Excretion: Mostly metabolized by the liver. Some metabolites are active; 1% excreted unchanged by the kidneys.

Half-Life: 15–30 hr.

Canadian Brand Names ⬆ ⬇

Methoprazine, Nozinan

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO (plasma concentrations)	unknown	2.7–2.9 hr	8–12 hr
IM (analgesia)	unknown	20–40 min	8 hr (up to 24 hr in children)

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Advise to take medication as directed. Take missed doses as soon as remembered unless almost time for next dose; do not double dose.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Advise patient on how and when to ask for pain medication.
Advise patients to make position changes slowly and to remain recumbent for 6–12 hr after administration to minimize orthostatic hypotension.
May cause drowsiness. Caution patient to request assistance with ambulation and transfer and to avoid driving or other activities requiring alertness until response to the medication is known.
Advise patient to avoid taking alcohol or other CNS depressants concurrently with this medication.
Advise patient to use sunscreen and protective clothing when exposed to the sun. Extremes of temperature should also be avoided because this drug impairs body temperature regulation.
Advise patient to use frequent mouth rinses, good oral hygiene, and sugarless gum or candy to minimize dry mouth.
Advise patient to notify health care provider promptly if sore throat, fever, unusual bleeding or bruising, rash, weakness, tremors, dark-colored urine, clay-colored stools, or signs of blood clots (swelling, pain, and redness in an arm or leg that can be warm to touch; sudden chest pain; difficulty breathing; heart palpitations) occur.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding. Use should be avoided during 3rd trimester because of ↑ risk of agitation, hypotonia, tremor, somnolence, respiratory distress, and feeding disturbances in newborn.

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Indications ⬇

Contraind./Precautions ⬆ ⬇