Orap

O·rap (ôrp)

A trademark for the drug pimozide.

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Orap,

trademark for an oral neuroleptic drug (pimozide).

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pimozide

Orap

Pharmacologic class: Diphenylbutylpiperidine

Therapeutic class: Antipsychotic

Pregnancy risk category C

Action

Unclear. Thought to relieve tics by blocking dopaminergic receptors on neurons in CNS.

Availability

Tablets: 1 mg, 2 mg

⊘Indications and dosages

➣ Motor and phonic tics in Tourette's syndrome

Adults: Initially, 1 to 2 mg P.O. daily in divided doses, increased every other day p.r.n. For maintenance, 0.2 mg/kg/day or 10 mg/day (whichever is smaller).

Contraindications

• Hypersensitivity to drug
• Severe toxic CNS depression
• Congenital long-QT syndrome
• History of arrhythmias
• Concurrent use of itraconazole, ketoconazole, macrolide antibiotics, protease inhibitors, nefazodone, or other drugs that prolong QT interval or cause motor and phonic tics
• Simple tics or tics other than those associated with Tourette syndrome

Precautions

Use cautiously in:
• history of seizures, cardiovascular disorders, hepatic or renal dysfunction, ECG abnormalities
• disorders that could be aggravated by adverse anticholinergic effects
• pregnant or breastfeeding patients
• children younger than age 12.

Administration

• Give with or without food.
• To minimize daytime sedation, give entire daily dose at bedtime.

Route	Onset	Peak	Duration
P.O.	Unknown	6-8 hr	Unknown

Adverse reactions

CNS: drowsiness, headache, dizziness, insomnia, akathisia, rigidity, speech disorder, handwriting changes, sedation, depression, excitement, nervousness, abnormal dreams, hyperkinesia, tardive dyskinesia, parkinsonian-like symptoms, tremor, neuroleptic malignant syndrome

CV: abnormal ECG, hypotension, orthostatic hypotension, hypertension, palpitations, chest pain, tachycardia, prolonged QT interval

EENT: visual disturbance, perception of spots before eyes, decreased visual accommodation

GI: nausea, vomiting, diarrhea, constipation, eructation, dysphagia, excessive salivation, dry mouth

GU: urinary frequency, menstrual disorder, breast secretions, erectile dysfunction, libido loss

Musculoskeletal: muscle cramps or tightness, stooped posture, torticollis

Skin: rash, skin irritation, sweating, photosensitivity

Other: taste changes, thirst, appetite changes, weight gain or loss

Interactions

Drug-drug. Amphetamines, methylphenidate, pemoline: tics

Antiarrhythmics, azole antifungals, macrolide antibiotics, phenothiazines, protease inhibitors, tricyclic antidepressants: ECG abnormalities

Anticholinergics: increased anticholinergic effects

CNS depressants: additive CNS depression

Drug-diagnostic tests. ECG: abnormalities

Drug-food. Grapefruit juice: inhibited pimozide metabolism

Drug-behaviors. Alcohol use: increased CNS depression

Patient monitoring

☞ Assess neurologic status, especially for signs and symptoms of neuroleptic malignant syndrome (high fever, stupor, sweating, unstable blood pressure, muscle rigidity, and autonomic dysfunction) and parkinsonian-like symptoms.
• Monitor for tardive dyskinesia, even after drug therapy ends.
• Assess vital signs and ECG. Stay alert for prolonged QT interval, hypertension, or orthostatic hypotension.

Patient teaching

• Tell patient he may take with or without food but not with grapefruit juice.
• Caution patient not to stop taking suddenly. Dosage must be tapered.
☞ Teach patient to recognize and immediately report signs and symptoms of neuroleptic malignant syndrome and tardive dyskinesia. Tell patient tardive dyskinesia may develop long after drug therapy ends.
• Instruct patient to rise slowly and carefully, because blood pressure may drop if he stands up suddenly.
• Advise patient that drug may cause erectile dysfunction and libido loss. Encourage him to discuss these problems with prescriber.
• Tell patient drug may cause appetite changes. Encourage good nutrition.
• Inform patient that drug may cause vision changes and photosensitivity, which he should report.
• Instruct patient not to drink alcohol or grapefruit juice while taking drug.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, vision, and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and behaviors mentioned above.