prochlorperazine (Rx)

<1%

Insomnia

Restlessness (immediate restlessness or agitation may be treated with diphenhydramine 25 mg IV push)

Dizziness

Anxiety

Euphoria

Agitation

Depression

Weakness

Headache

Cerebral edema

Poikilothermia

Orthostatic hypotension (after IM injection)

Tachycardia

ECG changes

Anorexia

Dyspepsia

Constipation

Diarrhea

Ileus

Blood dyscrasia

Galactorrhea

Gynecomastia

Ejaculatory disorder

Lens opacities (with prolonged use)

Photosensitivity

Pruritus

Frequency Not Defined

Akathisia

Sedation

Anticholinergic effects

Weight gain

Oligomenorrhea or amenorrhea

Erectile dysfunction

Extrapyramidal symptoms (muscle stiffness, dystonia, parkinsonism, tardive dyskinesia)

Neuroleptic malignant syndrome (infrequent but serious)

Seizure

Decreased gag reflex

Confusion

Hypotension

Hypertension

Leukopenia

Agranulocytosis

Cholestatic jaundice

Photosensitivity reaction

Priapism

Hepatotoxicity

Contraindications

Documented hypersensitivity to phenothiazines

Coma, severe CNS depression, concurrent use of large amounts of CNS depressants, poorly controlled seizure disorder, subcortical brain damage

Postoperative management of nausea/vomiting following pediatric surgery

Children <2 years or weighing <9 kg

Cautions

Avoid using in children with suspected Reye syndrome

Use caution in evere hypertension, severe cardiovascular disease

Use with caution in glaucoma, prostatic hypertrophy, stenosing peptic ulcer disease, history of neuroleptic malignant syndrome, Parkinson disease, hypocalcemia, renal/hepatic impairment, history of severe reactions to insulin or electroconvulsive therapy, history of seizures, asthma, respiratory tract infections, cardiovascular disease, myelosuppression

Blood dyscrasias including neutropenia, agranulocytosis, and leukopenia reported with use; discontinue therapy at first sign of blood dyscrasias

Risk of extrapyramidal symptoms, neuroleptic malignant syndrome, hypotension (may be particularly severe in patients with pheochromocytoma or mitral insufficiency)

Esophageal dysmotility/aspiration may occur; use with caution in patients at risk of pneumonia

Depresses hypothalamic thermoregulatory mechanism; exposure to extreme temperatures may cause hypo- or hyperthermia

May alter cardiac conduction; life-threatening arrhythmias reported with therapeutic doses

May cause anticholinergic effects (constipation, xerostomia, urinary retention, blurred vision); use caution in patients with decreased gastrointestinal motility, paralytic ileus, urinary retention, BPH, xerostomia, visual problems

May cause pigmentary retinopathy and lenticular and corneal deposits, espcially in prolonged therapy

May cause sedation and impair ability to perform tasks which require mental alertness, including operating heavy machinery

Use associated with increased prolactin levels

In case of severe hypotension, use norepinephrine or phenylepinephrine; do not use epinephrine or dopamine

Do not crush extended-release product

Avoid SC administration (may cause irritation)

Antiemetic effect may obscure toxicity of chemotherapeutic drugs

Use may be associated with neuroleptic malignant syndrome; monitor muscle ritidity, mental status changes, fever, autonomic instability

May need anticholinergic antiparkinsonian agent to counter extrapyramidal symptoms

May impair core body temperature regulation

FDA warning regarding off-label use for dementia in elderly

Pregnancy category: C

Lactation: Phenothiazines may be excreted in breast milk; do not nurse

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Antiemetic: Antidopaminergic effect, blocking dopamine receptors in the brain, blocking vagus nerve in GI tract

Antipsychotic: Blocking mesolimbic dopamine receptors, and blocking alpha-adrenergic receptors (D1 and D2) in brain

Absorption

Bioavailability: 12.5%

Onset: 10-20 min (IM); 30-40 min (PO); 60 min (PR)

Duration: 3-4 hr (PO); 3-12hr (PR); extended-release, 10-12 hr

Distribution

Vd: 1400-1548 L

Metabolism

Metabolized by liver

Metabolites: N-desmethyl prochlorperazine (active)

Elimination

Half-life: 6.8-9 hr (PO); 6-10 hr (IV)

Dialyzable: No

Excretion: Feces (primarily)

IV Compatibilities

Solution: Compatible with most common solvents

Additive: Amikacin, ascorbic acid injection, dexamethasone, dimenhydrinate, erythromycin, ethacrynate, lidocaine, nafcillin, penicillin G potassium (incompatible at higher concentrations), sodium bicarbonate, vitamins B and C

Syringe (partial list): Atropine, chlorpromazine, cimetidine, diphenhydramine, fentanyl, glycopyrrolate, hydroxyzine, meperidine, metoclopramide, morphine sulfate (incompatible if phenol present)(?)

Y-site (partial list): Calcium gluconate, cisplatin, cladribine, clarithromycin, cyclophosphamide, cytarabine, docetaxel, doxorubicin, doxorubicin liposomal, heparin, linezolid, melphalan, methotrexate, potassium chloride, propofol, teniposide, thiotepa, topotecan, vitamins B and C

IV Incompatibilities

Additive: Aminophylline, amphotericin B, ampicillin, calcium gluconate(?), chloramphenicol, chlorothiazide, floxacillin, furosemide, hydrocortisone, methohexital, penicillin G sodium, phenobarbital, thiopental

Syringe: Dimenhydrinate, hydromorphone(?), ketorolac, midazolam, morphine tartate, pentobarbital, thiopental

Y-site: Aldesleukin, allopurinol, amifostine, amphotericin B, aztreonam, bivalirudin, cefepime, etoposide phosphate, fenoldopam, filgrastim, fludarabine, foscarnet, gemcitabine, piperacillin/tazobactam

IV Administration

Avoid bolus

IV push rate should not exceed 5 mg/min

For infusion, dilute 20 mg in 1 L of compatible solution; may infuse over 30 minutes

Storage

Store at room temperature, and protect from light

Solution is clear or slightly yellow