Inapsine

>10%

Restlessness

Anxiety

Extrapyramidal Symptoms

Dystonic reactions

Pseudoparkinsonian signs and symptoms

Tardive dyskinesia

Seizure

Altered central temperature regulation

Sedation

Drowsiness

Prolonged QT interval (dose dependent)

Swelling of breasts

Weight gain

Constipation

1-10%

Hallucinations

Persistent tardive dyskinesia

Akathisia

Orthostatic hypotension

Tachycardia

ECG: abnormal T waves

Hypertension

Nausea

Vomiting

Dysuria

Frequency Not Defined

Serious, potentially fatal cardiac effects: prolonged QT interval, torsades de pointes, cardiac arrest, ventricular tachycardia

Black Box Warnings

Patients with dementia-related psychosis who are treated with antipsychotic drugs are at an increased risk of death as shown in short-term controlled trials. The deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature

This drug is not approved for the treatment of patients with dementia-related psychosis

Contraindications

Hypersensitivity

Known or suspected prolonged QT interval; QTc interval >450 msec in females or 400 msec in males

Cautions

May cause potentially fatal QT interval prolongation/torsades de pointes at or below recommended doses; should be used only in patients who have failed to respond to other drugs

Use as sedative or anesthesia adjunct no longer recommended

Shares the toxic potentials of phenothiazines

Risk factors for prolonged QT interval

• Use with extreme cautions in patients at risk for development of prolonged QT syndrome
• CHF, bradycardia, diuretic use, hypokalemia, hypomagnesemia, cardiac hypertrophy
• Use of drug known to cause prolonged QT interval: class I or III antiarrhythmias, some antihistamines, antimalarials, calcium channel blockers, neuroleptics, antidepressants or drugs which may induce hypokalemia or hypomagnesemia
• >65 years, alcohol abuse, concomitant use of benzodiazepines or IV opiates, impaired hepatic/renal function

• Akorn, Inc.

• Janssen Pharmaceutical Products, L.P.

• Taylor Pharmaceuticals

Since this medicine is given by a healthcare professional in a medical setting, an overdose is unlikely to occur.

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Tell your caregiver right away if you have:

• headache with chest pain and severe dizziness, fainting, fast or pounding heartbeats;

• a light-headed feeling, like you might pass out;

• numbness or tingly feeling;

• confusion, hallucinations;

• bronchospasm (wheezing, chest tightness, trouble breathing);

• twitching or uncontrollable movements of your eyes, tongue, jaw, or neck; or

• severe nervous system reaction--very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors.

Common side effects include:

• drowsiness, dizziness; or

• feeling restless or anxious.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Absorption

Onset

Onset occurs within 3–10 minutes following IM or IV administration, but peak effects may not be apparent until 30 minutes.114

Duration

Following IM or IV administration, sedative and tranquilizing effects generally persist for 2–4 hours; alteration of consciousness may persist for up to 12 hours.114

Distribution

Extent

Reportedly crosses the blood-brain barrier and is distributed into the CSF.a

Reportedly crosses the placenta; not known whether droperidol is distributed into milk.a

Elimination

Metabolism

Metabolized in the liver.a

Elimination Route

Droperidol and its metabolites are excreted in urine (10% as unchanged drug) and feces.a

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses or alcohol use.114

• Importance of avoiding alcohol during therapy due to risk of additive effects.114

• Importance of women informing clinicians if they are or plan to become pregnant or to breast-feed.114

• Importance of informing patients of other important precautionary information.114 (See Cautions.)

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor or nurse immediately if any of the following side effects occur:

• Blurred vision
• confusion
• dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
• sweating
• unusual tiredness or weakness

• Chills
• cough
• difficulty with breathing
• difficulty with swallowing
• dizziness
• fast heartbeat
• noisy breathing
• puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
• skin rash, hives, or itching
• tightness in the chest

• Chest pain or discomfort
• fainting
• fast, pounding, or irregular heartbeat or pulse
• irregular or slow heart rate
• low blood pressure or pulse
• severe confusion or loss of consciousness

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

• Anxiety
• drowsiness
• restlessness
• trouble sitting still

• Difficulty with speaking
• drooling
• loss of balance control
• muscle trembling, jerking, or stiffness
• seeing, hearing, or feeling things that are not there
• shuffling walk
• stiffness of the limbs
• twisting movements of the body
• uncontrolled movements, especially of the face, neck, and back

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

QT interval prolongation, torsade de pointes, cardiac arrest, and ventricular tachycardia have been reported in patients treated with Inapsine. Some of these cases were associated with death. Some cases occurred in patients with no known risk factors, and some were associated with droperidol doses at or below recommended doses.

Physicians should be alert to palpitations, syncope, or other symptoms suggestive of episodes of irregular cardiac rhythm in patients taking Inapsine and promptly evaluate such cases (see WARNINGS, Effects on Cardiac Conduction).

The most common somatic adverse reactions reported to occur with Inapsine (droperidol) are mild to moderate hypotension and tachycardia, but these effects usually subside without treatment. If hypotension occurs and is severe or persists, the possibility of hypovolemia should be considered and managed with appropriate parenteral fluid therapy.

The most common behavioral adverse effects of Inapsine (droperidol) include dysphoria, postoperative drowsiness, restlessness, hyperactivity and anxiety, which can either be the result of an inadequate dosage (lack of adequate treatment effect) or of an adverse drug reaction (part of the symptom complex of akathisia).

Care should be taken to search for extrapyramidal signs and symptoms (dystonia, akathisia, oculogyric crisis) to differentiate these different clinical conditions. When extrapyramidal symptoms are the cause, they can usually be controlled with anticholinergic agents.

Postoperative hallucinatory episodes (sometimes associated with transient periods of mental depression) have also been reported.

Other less common reported adverse reactions include anaphylaxis, dizziness, chills and/or shivering, laryngospasm, and bronchospasm.

Elevated blood pressure, with or without pre-existing hypertension, has been reported following administration of Inapsine combined with SUBLIMAZE (fentanyl citrate) or other parenteral analgesics. This might be due to unexplained alterations in sympathetic activity following large doses: however, it is also frequently attributed to anesthetic or surgical stimulation during light anesthesia.