No

Analgesic, Non-narcotic

Relief of moderate to severe pain in nonambulatory patients; for analgesia and sedation when respiratory depression is to be avoided, as in obstetrics; preanesthetic for producing sedation, somnolence and relief of apprehension and anxiety

C

Severe cardiac, renal, or hepatic disease; history of convulsive disorders; concurrent use of MAO inhibitors; significant hypotension; children <12 years of age; hypersensitivity to methotrimeprazine or phenothiazines, sulfite sensitivity

>10%:

Cardiovascular: Hypotension, orthostatic hypotension

Central nervous system: Pseudoparkinsonism, akathisia, dystonias, dizziness

Gastrointestinal: Constipation

Neuromuscular & skeletal: Tardive dyskinesia

Ocular: Pigmentary retinopathy

Respiratory: Nasal congestion

Miscellaneous: Decreased diaphoresis

1% to 10%:

Central nervous system: Dizziness

Dermatologic: Increased sensitivity to sun, skin rash

Endocrine & metabolic: Changes in menstrual cycle, ejaculatory disturbances, changes in libido, pain in breasts

Gastrointestinal: Weight gain, nausea, vomiting, stomach pain

Genitourinary: Dysuria

Neuromuscular & skeletal: Trembling of fingers

Increased toxicity: Additive effects with other CNS-depressants

Methotrimeprazine is a phenothiazine with sites of action thought to be in the thalamus, hypothalamus, reticular and limbic systems, producing suppression of sensory impulses. This results with sedation, an elevated pain threshold, and induction of amnesia. The analgesic effect of methotrimeprazine is comparable to meperidine and morphine without the respiratory suppression. This agent also has antihistamine, anticholinergic, and antiepinephrine effects.

Peak effect: Within 20-40 minutes

Duration: 4 hours

Serum half-life, elimination: 20 hours

Time to peak serum concentration: Within 0.5-1.5 hours

Adults: I.M.:

Preoperative medication: 2-20 mg, 45 minutes to 3 hours before surgery

Postoperative analgesia: 2.5-7.5 mg every 4-6 hours is suggested as necessary since residual effects of anesthetic may be present

Pre- and postoperative hypotension: I.M.: 5-10 mg

Dosing adjustment/comments in renal or hepatic impairment: Administer cautiously although no specific guidelines are available

Is a phenothiazine; dizziness and extrapyramidal symptoms are common; may rarely cause neuroleptic malignant syndrome

Contraindicated with MAOIs and patient with hypersensitivity to phenothiazines; may rarely cause agranulocytosis; use caution with clozapine and carbamazepine

No information available to require special precautions

Anticholinergic side effects can cause a reduction of saliva production or secretion contributes to discomfort and dental disease (ie, caries, oral candidiasis and periodontal disease); phenothiazines can cause extrapyramidal reactions which may appear as muscle twitching or increased motor activity of the face, neck or head

May cause drowsiness, rise slowly after sitting or lying after administration

May cause drowsiness, rise slowly after sitting or lying after administration

Injection, as hydrochloride: 20 mg/mL (10 mL)