No

Antipsychotic Agent, Phenothazine, Piperidine

Schizophrenia; behavioral problems in mental deficiency and chronic brain syndrome; alcoholism (acute and chronic); psychoneurotic manifestations (anxiety, tension)

C

Hypersensitivity to mesoridazine or any component (cross reactivity between phenothiazines may occur); severe CNS depression and coma

May cause hypotension, particularly with I.M. administration. Highly sedating, use with caution in disorders where CNS depression is a feature. Use with caution in Parkinson's disease. Caution in patients with hemodynamic instability; bone marrow suppression; predisposition to seizures; subcortical brain damage; severe cardiac, hepatic, renal, or respiratory disease. Esophageal dysmotility and aspiration have been associated with antipsychotic use - use with caution in patients at risk of pneumonia (ie, Alzheimer's disease). Caution in breast cancer or other prolactin-dependent tumors (may elevate prolactin levels). May alter temperature regulation or mask toxicity of other drugs due to antiemetic effects. May alter cardiac conduction; life-threatening arrhythmias have occurred with therapeutic doses of phenothiazines. May cause orthostatic hypotension - use with caution in patients at risk of this effect or those who would tolerate transient hypotensive episodes (cerebrovascular disease, cardiovascular disease, or other medications which may predispose).

May cause extrapyramidal reactions, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia (risk of these reactions is low relative to other neuroleptics). May be associated with neuroleptic malignant syndrome (NMS) or pigmentary retinopathy (particularly at doses >1 g/day).

Cardiovascular: Hypotension, orthostatic hypotension, tachycardia, QT prolongation, syncope, edema

Central nervous system: Pseudoparkinsonism, akathisia, dystonias, tardive dyskinesia, dizziness, drowsiness, restlessness, ataxia, slurred speech, neuroleptic malignant syndrome (NMS), impairment of temperature regulation, lowering of seizure threshold

Dermatologic: Increased sensitivity to sun, rash, itching, angioneurotic edema, dermatitis, discoloration of skin (blue-gray)

Endocrine & metabolic: Changes in menstrual cycle, changes in libido, gynecomastia, lactation, galactorrhea

Gastrointestinal: Constipation, xerostomia, weight gain, nausea, vomiting, stomach pain

Genitourinary: Difficulty in urination, ejaculatory disturbances, impotence, enuresis, incontinence, priapism, urinary retention

Hematologic: Agranulocytosis, leukopenia, eosinophilia, thrombocytopenia, anemia, aplastic anemia

Hepatic: Cholestatic jaundice, hepatotoxicity

Neuromuscular & skeletal: Weakness, tremor, rigidity

Ocular: Pigmentary retinopathy, photophobia, blurred vision, cornea and lens changes

Respiratory: Nasal congestion

Miscellaneous: Diaphoresis (decreased)

Symptoms of overdose include deep sleep, coma, extrapyramidal symptoms, abnormal involuntary muscle movements, hypotension

Following initiation of essential overdose management, toxic symptom treatment and supportive treatment should be initiated; hypotension usually responds to I.V. fluids or Trendelenburg positioning. If unresponsive to these measures, the use of a parenteral inotrope may be required. Seizures commonly respond to diazepam (I.V. 5-10 mg bolus in adults every 15 minutes if needed up to a total of 30 mg; I.V. 0.25-0.4 mg/kg/dose up to a total of 10 mg in children) or to phenytoin or phenobarbital. Critical cardiac arrhythmias often respond to I.V. phenytoin (15 mg/kg up to 1 g), while other antiarrhythmics can be used. Extrapyramidal symptoms (eg, dystonic reactions) can be managed with benztropine mesylate I.V. 1-2 mg (adults).

Phenothiazines inhibit the ability of bromocriptine to lower serum prolactin concentrations

Benztropine (and other anticholinergics) may inhibit the therapeutic response to mesoridazine and excess anticholinergic effects may occur

Chloroquine may increase mesoridazine concentrations

Cigarette smoking may enhance the hepatic metabolism of mesoridazine. Larger doses may be required compared to a nonsmoker.

Concurrent use of mesoridazine with an antihypertensive may produce additive hypotensive effects

Antihypertensive effects of guanethidine and guanadrel may be inhibited by mesoridazine

Concurrent use with TCA may produce increased toxicity or altered therapeutic response

Mesoridazine may inhibit the antiparkinsonian effect of levodopa; avoid this combination

Mesoridazine plus lithium may rarely produce neurotoxicity

Barbiturates may reduce mesoridazine concentrations

Propranolol may increase mesoridazine concentrations

Sulfadoxine-pyrimethamine may increase mesoridazine concentrations

Mesoridazine and possibly other low potency antipsychotics may reverse the pressor effects of epinephrine

Mesoridazine and CNS depressants (ethanol, narcotics) may produce additive CNS depressant effects

Mesoridazine and trazodone may produce additive hypotensive effects

Protect all dosage forms from light; clear or slightly yellow solutions may be used; should be dispensed in amber or opaque vials/bottles. Solutions may be diluted or mixed with fruit juices or other liquids but must be administered immediately after mixing; do not prepare bulk dilutions or store bulk dilutions.

Blockade of postsynaptic CNS dopamine₂ receptors in the mesolimbic and mesocortical areas

Duration of action: 4-6 hours

Absorption: Very erratic with oral tablet; oral liquids much more dependable

Protein binding: 91% to 99%

Half-life: 24-48 hours

Time to peak serum concentration: 2-4 hours

Time to steady-state serum: 4-7 days

Elimination: In urine

Concentrate may be diluted just prior to administration with distilled water, acidified tap water, orange or grape juice; do not prepare and store bulk dilutions

Oral: 25-50 mg 3 times/day; maximum: 100-400 mg/day

I.M.: Initial: 25 mg, repeat in 30-60 minutes as needed; optimal dosage range: 25-200 mg/day

Hemodialysis: Not dialyzable (0% to 5%)

Alcohol: Additive CNS effect, avoid use

cholesterol (S), glucose; uric acid (S)

No information available to require special precautions

No effects or complications reported

Use exactly as directed (do not increase dose or frequency); may cause physical and/or psychological dependence. It may take 2-3 weeks to achieve desired results; do not discontinue without consulting prescriber. Dilute oral concentration with water, orange or grape juice. Do not take within 2 hours of any antacid. Avoid excess alcohol or caffeine and other prescription or OTC medications not approved by prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Avoid skin contact with medication; may cause contact dermatitis (wash immediately with warm, soapy water). You may experience excess drowsiness, restlessness, dizziness, or blurred vision (use caution driving or when engaging in tasks requiring alertness until response to drug is known); dry mouth, nausea, vomiting (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); constipation (increased exercise, fluids, or dietary fruit and fiber may help); postural hypotension (use caution climbing stairs or when changing position from lying or sitting to standing); urinary retention (void before taking medication); photosensitivity (use sunscreen, wear protective clothing and eyewear, and avoid direct sunlight); decreased perspiration (avoid strenuous exercise in hot environments); or changes in menstrual cycle, libido, ejaculation (will resolve when medication is discontinued). Report persistent CNS effects (eg, trembling fingers, altered gait or balance, excessive sedation, seizures, unusual movements, anxiety, abnormal thoughts, confusion, personality changes); chest pain, palpitations, rapid heartbeat, severe dizziness; unresolved urinary retention or changes in urinary pattern; menstrual pattern, change in libido, swelling or pain in breasts (male or female); vision changes; skin rash or yellowing of skin; difficulty breathing; or worsening of condition. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed.

Dilute oral concentrate with water or juice before administration; avoid skin contact with oral suspension or solution; may cause contact dermatitis; monitor orthostatic blood pressures 3-5 days after initiation of therapy or a dose increase

Monitor orthostatic blood pressures; tremors, gait changes, abnormal movement in trunk, neck, buccal area or extremities; monitor target behaviors for which the agent is administered; monitor hepatic function (especially if fever with flu-like symptoms); watch for hypotension when administering I.M. or I.V.

Injection, as besylate: 25 mg/mL (1 mL)

Liquid, oral, as besylate: 25 mg/mL (118 mL)

Tablet, as besylate: 10 mg, 25 mg, 50 mg, 100 mg

Marrs-Simon PA, Zell-Kanter M, Kendzierski DL, et al, "Cardiotoxic Manifestations of Mesoridazine Overdose," Ann Emerg Med, 1988, 17(10):1074-8.

Peabody CA, Warner MD, Whiteford HA, et al, "Neuroleptics and the Elderly," J Am Geriatr Soc, 1987, 35(3):233-8.

Risse SC and Barnes R, "Pharmacologic Treatment of Agitation Associated With Dementia," J Am Geriatr Soc, 1986, 34(5):368-76.

Saltz BL, Woerner MG, Kane JM, et al, "Prospective Study of Tardive Dyskinesia Incidence in the Elderly," JAMA, 1991, 266(17):2402-6.

Samet J and Surawicz B, "Cardiac Function in Patients Treated With Phenothiazines Comparison With Quinidine," J Clin Pharmacol, 1974, 14(11-12):588-96.

Seifert RD, "Therapeutic Drug Monitoring: Psychotropic Drugs," J Pharm Pract, 1984, 6:403-16.