Droperidol

(droe per i dol)

PCaution when used during lactation : Caution when used during pregnancy

LCaution when used during lactation : Caution when used during lactation

Molecule Info

| See TERMINOLOGY & ABBREVIATIONS |

WARNING

 

Cases of QT prolongation and/or torsade de pointes have been reported in patients receiving droperidol at doses at or below recommended doses. Some cases have occurred in patients with no known risk factors for QT prolongation and some cases have been fatal.

Due to its potential for serious proarrhythmic effects and death, droperidol should be reserved for use in the treatment of patients who fail to show an acceptable response to other adequate treatments, either because of insufficient effectiveness or the inability to achieve an effective dose due to intolerable adverse effects from those drugs.

Cases of QT prolongation and serious arrhythmias (e.g., torsade de pointes) have been reported in patients treated with droperidol. Based on these reports, all patients should undergo a 12-lead ECG prior to administration of droperidol to determine if a prolonged QT interval (i.e., QTc greater than 440 msec for males or 450 msec for females) is present. If there is a prolonged QT interval, droperidol should NOT be administered. For patients in whom the potential benefit of droperidol treatment is felt to outweigh the risks of potentially serious arrhythmias, ECG monitoring should be performed prior to treatment and continued for 2-3 hours after completing treatment to monitor for arrhythmias.

Droperidol is contraindicated in patients with known or suspected QT prolongation, including patients with congenital long QT syndrome. Droperidol should be administered with extreme caution to patients who may be at risk for development of prolonged QT syndrome (e.g., congestive heart failure, bradycardia, use of a diuretic, cardiac hypertrophy, hypokalemia, hypomagnesemia, or administration of other drugs known to increase the QT interval). Other risk factors may include age over 65 years, alcohol abuse, and use of agents such as benzodiazepines, volatile anesthetics, and I.V. opiates. Droperidol should be initiated at a low dose and adjusted upward, with caution, as needed to achieve the desired effect.

Indication(s) & Dosage

- Prevention and treatment of post-operative nausea and vomiting in adults and, as second line, in children and adolescents.

- Prevention of nausea and vomiting induced by morphine derivates during post-operative patient controlled analgesia (PCA) in adults.

Parenteral route

Postoperative nausea and vomiting  Adult: Max initial dose: 2. 5 mg, may be given via IM/IV admin.  Additional doses of 1. 25 mg may be given if necessary. Child: 2-12 yr: Max initial dose of 100 mcg//kg, may be given via IV/IM admin. Elderly: Dose reduction may be necessary.

Special Populations: Elderly and debilitated patients: Reduced dosage, generally ½ adult dose.

Overdosage

Symptoms may include QT prolongation and serious arrhythmias.  In the presence of hypoventilation or apnea, oxygen may be used and respiration should be assisted or controlled as needed.  Maintain a patent airway.  The patient should be under careful observation for 24 hr; ensure adequate body warmth and fluid intake.  Hypotension may occur as a result of hypovolemia, may be managed with appropriate parenteral fluid therapy.

Contraindications

Droperidol is contraindicated in patients with:

- Hypersensitivity to droperidol or to any of the excipients;

- Hypersensitivity to butyrophenones;

- Known or suspected prolonged QT interval (QTc of > 450 msec in females and > 440 msec in males). This includes patients with congenitally long QT interval, patients who have a family history of congenital QT prolongation and those treated with medicinal products known to prolong the QT interval;

- Hypokalaemia or hypomagnesaemia;

- Bradycardia (< 55 heartbeats per minute);

- Known concomitant treatment leading to bradycardia;

- Phaeochromocytoma;

- Comatose states;

- Parkinson's Disease;

- Severe depression.

Special Precautions

Central Nervous System

Droperidol may enhance CNS depression produced by other CNS-depressant drugs. Any patient subjected to anaesthesia and receiving potent CNS depressant medicinal products or showing symptoms of CNS depression should be monitored closely.

Concomitant use of metoclopramide and other neuroleptics may lead to an increase in extrapyramidal symptoms and should be avoided.

Use with caution in patients with epilepsy (or a history of epilepsy) and conditions predisposing to epilepsy or convulsions.

Cardiovascular

Mild to moderate hypotension and occasionally (reflex) tachycardia have been observed following the administration of droperidol. This reaction usually subsides spontaneously. However, should hypotension persist, the possibility of hypovolaemia should be considered and appropriate fluid replacement administered.

Patients with, or suspected of having, the following risk factors for cardiac arrhythmia should be carefully evaluated prior to administration of droperidol:

- a history of significant cardiac disease including serious ventricular arrhythmia, second or third degree atrio-ventricular block, sinus node dysfunction, congestive heart failure, ischemic heart disease and left ventricular hypertrophy;

- family history of sudden death;

- renal failure (particularly when on chronic dialysis);

- significant chronic obstructive pulmonary disease and respiratory failure;

- risk factors for electrolyte disturbances, as seen in patients taking laxatives, glucocorticoids, potassium-wasting diuretics, in association with the administration of insulin in acute settings, or in patients with prolonged vomiting and/or diarrhoea.

Patients at risk for cardiac arrhythmia should have serum electrolytes and creatinine levels assessed and the presence of QT prolongation excluded prior to administration of droperidol.

Continuous pulse oximetry should be performed in patients with identified or suspected risk of ventricular arrhythmia and should continue for 30 minutes following single i.v. administration.

General

To prevent QT prolongation, caution is necessary when patients are taking medicinal products likely to induce electrolyte imbalance (hypokalaemia and/or hypomagnesaemia) e.g. potassium-wasting diuretics, laxatives and glucocorticoids.

Substances inhibiting the activity of cytochrome P450 iso-enzymes (CYP) CYP1A2, CYP3A4 or both could decrease the rate at which droperidol is metabolised and prolong its pharmacological action. Hence, caution is advised if droperidol is given concomitantly with strong CYP1A2 and CYP3A4 inhibitors.

Patients who have, or are suspected of having, a history of alcohol abuse or recent high intakes, should be thoroughly assessed before droperidol is administered.

In case of unexplained hyperthermia, it is essential to discontinue treatment, since this sign may be one of the elements of malignant syndrome reported with neuroleptics.

The dose should be reduced in the elderly and those with impaired renal and hepatic function.

This medicinal product contains less than 1 mmol sodium (23 mg) per 1 ml, i.e. essentially 'sodium-free'.

Adverse Drug Reaction(s)

Dry mouth, constipation, micturition difficulty, blurred vision, mydriasis, delirium, agitation, catatonic-like states, insomnia, nightmares, depression, miosis, convulsions, nasal congestion.  CV effects; hypersensitivity reactions, haematological disorders, extrapyramidal dysfunction.  Amenorrhoea, galactorrhoea, gynaecomastia, weight gain and hyperglycaemia, and altered glucose tolerance.  Pain and irritation at the Inj site.  Post-op drowsiness.

Drug Interactions

Avoid concurrent use with drugs that may prolong QT interval e. g.  certain antihistamines, antimalarials, calcium-channel blockers and antidepressants.  May potentiate the action of other CNS depressants e. g.  barbiturates, alcohol.  Caution when using with drugs that may induce hypokalaemia or hypomagnesemia.

Lab Interference

Minor abnormalities in liver function tests.

Pregnancy Category (FDA)

Category C: Either studies in animals have revealed adverse effects on the foetus and there are no controlled studies in women or studies in women and animals are not available.  Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Storage

Parenteral: Store at 15 - 25°C.

Pharmacology

Droperidol acts mainly at the subcortical levels and exhibits strong sedative effects.  It inhibits sympathetic postganglionic alpha-adrenergic receptor binding sites.  It also exhibits antiemetic but has no analgesic effects. Onset: 3-10 min. Duration: 2-4 hr.

ATC Classification

N01AX01 - droperidol; Belongs to the class of other general anesthetics.  N05AD08 - droperidol; Belongs to the class of butyrophenone derivatives antipsychotics.

 

Search Google: Droperidol

Brand/Product Info


Total Products : 0
Brand Name Manufacturer/Marketer Composition Dosage Form Pack Size & Price
| See Brand Manufacturer's Prescribing Information |
| Latest mph edition: Dec 2013 |  | Back to top |