methotrimeprazine

REMS

Management of psychotic disturbances.
Management of conditions associated with anxiety/tension.
As an analgesic and adjunct in pain due to cancer, zona, trigeminal neuralgia, intercostal neuralgia, phantom limb pain, and muscular discomforts.
Used as a preoperative sedative.
As an antiemetic.
As a sedative in the treatment of insomnia.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Blood dyscrasias;
Hepatic impairment;
Hypersensitivity to methotrimeprazine, phenothiazines or sulfites;
Comatose patients or those who have overdosed on CNS depressants including alcohol, analgesics, opioids, or sedative/hypnotics;
OB: Third-trimester use may result in agitation, hypotonia, tremor, somnolence, respiratory distress, and feeding disturbances in newborn and should be avoided.

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);
Geri: Initial dosage ↓ recommended, ↑ risk of death in elderly patients with dementia;
Lactation: Safety not established;
Pedi: Safety not established.

Adv. Reactions/Side Effects ⬆ ⬇

CNS: amnesia, drowsiness, excess sedation, disorientation, euphoria, extrapyramidal reactions, headache, NEUROLEPTIC MALIGNANT SYNDROME, SEIZURES, slurred speech, tardive dyskinesia, weakness.

EENT: nasal congestion

CV: orthostatic hypotension, bradycardia, palpitations, tachycardia

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

GU: difficulty in urination

Endo: hyperglycemia, hyperprolactinemia

Hemat: blood dyscrasias

Local: pain at injection site

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 concurrent 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.
Concurrent use with succinylcholine may result in tachycardia, hypotension, CNS stimulation, delirium, and ↑ extrapyramidal symptoms.

Drug-Natural Products:

Concomitant use of kava, valerian, skullcap, chamomile, or hops↑ 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); Night time sedative: 10–25 mg as a single bedtime dose; Psychoses/intense pain: 50–75 mg/day in 2–3 divided doses, dose may be titrated upward to desired effect (doses of 1 g/day have been used, if daily dose exceeds 100–200 mg, administer in divided doses and keep patient at 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 in 250 mL of 5% dextrose solution as a slow infusion (20–40 drops/min).

Action ⬆ ⬇

Sedation.

Therapeutic effects:

Reduction in severity of pain.

Classifications ⬆ ⬇

Therapeutic Classification: antipsychotics, nonopioid analgesics

Pharmacologic Classification: phenothiazines

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed after PO/IM administration. IV administration results in complete bioavailability.

Distribution: Enters CSF and crosses the placenta. Minimal amounts enter breast milk.

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 (blood levels)	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 ⬆ ⬇

Instruct patient on how and when to ask for pain medication.
Instruct patient 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 read Patient Information leaflet prior to starting therapy and with each Rx refill in case of changes.
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 notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Caution 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.
Instruct patient to use frequent mouth rinses, good oral hygiene, and sugarless gum or candy to minimize dry mouth.
Instruct patient to notify health care professional promptly if sore throat, fever, unusual bleeding or bruising, rash, weakness, tremors, dark-colored urine, or 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.

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Indications ⬇