Perflutren

Pronunciation: per-FLOO-tren
Class: Radiopaque agent

Trade Names

Definity
- Injection, suspension, lipid-based up to 1.2 × 10 10 /mL (after activation)

Optison
- Injection, suspension, protein-based 0.22 ± 0.11 mg/mL

Pharmacology

Perflutren, lipid-based

Provides contrast enhancement of the left ventricular chamber and aids delineation of the left ventricular endocardial borders during echocardiography.

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Perflutren, protein-based

Creates an echogenic contrast effect in the blood.

Pharmacokinetics

Distribution

Protein binding expected to be minimal.

Metabolism

Not metabolized.

Elimination

96% eliminated through the lungs; pulmonary elimination half-life is 1.3 min (lipid-based).

Special Populations

Renal Function Impairment

No data available.

Hepatic Function Impairment

The pharmacokinetics of perflutren have not been studied in subjects with hepatic disease.

Elderly

The pharmacokinetics of perflutren in elderly patients have not been studied.

Indications and Usage

To opacify the left ventricular chamber and to improve delineation of the left ventricular endocardial borders in patients with suboptimal echocardiograms.

Contraindications

Known or suspected right-to-left, bidirectional, or transient right-to-left cardiac shunts; known or suspected hypersensitivity to perflutren or any component; intra-arterial injection; hypersensitivity to blood, blood products, or albumin (protein-based only).

Dosage and Administration

Perflutren, lipid-based
Adults

IV bolus 10 mcL/kg of the activated product within 30 to 60 sec, followed by a 10 mL saline flush. May repeat 30 min after first injection, if needed.

IV infusion 1.3 mL of activated product added to 50 mL of preservative-free saline, initiated at a rate of 4 mL/min. Titrate as necessary to achieve optimal image enhancement, not to exceed 10 mL/min.

Perflutren, protein-based
Adults

IV 0.5 mL injected into a peripheral vein. Additional doses of 0.5 mL, up to 5 mL cumulatively in a 10-min period, may be injected, up to a maximum total dose of 8.7 mL in any one patient study.

General Advice

  • Do not inject air into the vial when withdrawing a dose.
  • Perflutren, lipid-based
  • Administer only after activation in the Vialmix apparatus. Before injection, this product must be activated and prepared according to the manufacturer's instructions.
  • Administer by IV bolus or infusion only. For IV bolus, administer over 30 to 60 sec and follow with a 10 mL saline flush. For IV infusion, administer at a rate of 4 to 10 mL/min.
  • If the product is not used within 5 min of Vialmix activation, resuspend the microspheres by 10 sec of hand agitation by inverting the vial. The activated perflutren may be used for up to 12 h after Vialmix , but only after the microspheres are resuspended by hand agitation.
  • Use the product immediately after withdrawing from the vial; do not allow to stand in the syringe.
  • After baseline noncontrast echocardiography, the mechanical index for the ultrasound device should be set at 0.8 or below. Inject activated perflutren and begin ultrasound imaging immediately.
  • Perflutren, protein-based
  • Administer in a peripheral vein only, at a rate of no more than 1 mL/sec.
  • Follow injection with a flush of dextrose 5% or sodium chloride 0.9%.
  • Invert vial and gently rotate to resuspend microspheres.
  • Do not use if the solution appears clear rather than milky white after resuspension.
  • Vent vial with a sterile vent spike or a sterile 18-gauge needle before withdrawing product from the vial.
  • If more than 1 min has passed after withdrawing contents of the vial into a syringe, resuspend the microspheres by gently rotating and inverting the syringe.
  • Do not aspirate blood back into the syringe before administration; this may lead to formation of a blood clot within the syringe.

Storage/Stability

Store between 36° and 46°F. Do not freeze. Discard unused product properly.

Drug Interactions

Drugs that prolong the QT interval (eg, antiarrhythmic agents [eg, amiodarone, bretylium, disopyramide, dofetilide, procainamide, quinidine, sotalol], arsenic trioxide, chlorpromazine, cisapride, dolasetron, droperidol, mefloquine, mesoridazine, moxifloxacin, pentamidine, pimozide, tacrolimus, thioridazine, ziprasidone)

An additive effect of perflutren with other drugs that prolong the QT interval, increasing the risk of life-threatening cardiac arrhythmias (including torsades de pointes), cannot be excluded.

Adverse Reactions

Cardiovascular

Chest pain, extracardiac vascular disorders (1%); cardiac arrest, hypertension, hypotension, shock, syncope, symptomatic arrhythmias (atrial fibrillation, tachycardia, bradycardia, supraventricular tachycardia, transient ischemic attack, ventricular fibrillation, ventricular tachycardia) (postmarketing).

CNS

Headache (5%); warm sensation/flushing (4%); dizziness (3%); malaise/weakness/fatigue (1%); agitation, coma, convulsions, fatigue, loss of consciousness, tremor (postmarketing).

EENT

Altered taste (2%); vision blurred (postmarketing).

GI

Nausea and/or vomiting (4%).

Hypersensitivity

Anaphylactic/anaphylactoid reaction, anaphylactic shock, angioedema, bronchospasm, edema (pharyngeal, palatal, mouth, peripheral, localized), erythema, facial hypoesthesia, flushing, hypersensitivity, pruritus, rash, swelling (face, lips, tongue, eye, upper airway), throat tightness, urticaria.

Local

Erythema, injection-site discomfort/disorders (1%).

Respiratory

Dyspnea (1%); decreased oxygenation, hypoxia, respiratory arrest or distress, stridor, wheezing (postmarketing).

Miscellaneous

Back/renal pain, chills/fever, flu-like symptoms (1%).

Precautions

Warnings

Cardiopulmonary reactions

Serious cardiopulmonary reactions, including fatalities, have occurred during or following perflutren administration. Assess all patients for conditions that preclude perflutren use. Monitor vital signs, ECG, and cutaneous oxygen saturation during and for at least 30 min after administration of perflutren in patients with pulmonary hypertension or unstable cardiopulmonary conditions. Ensure that resuscitation equipment and trained personnel are readily available.


Monitor

Monitor vital sign measurements, electrocardiography, and cutaneous oxygen saturation in patients with pulmonary hypertension or unstable cardiopulmonary conditions during and for 30 min following perflutren administration. Closely observe all patients during and following perflutren administration. Monitor all patients for signs and symptoms of anaphylactoid reactions.


Pregnancy

Category B (lipid-based); Category C (protein-based).

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hypersensitivity

Reports of acute and/or serious anaphylactoid reactions (eg, angioedema, bronchospasm, edema [pharyngeal, palatal, mouth, peripheral, localized], facial hypoesthesia, flushing, erythema, hypersensitivity, loss of consciousness, pruritus, rash, shock, swelling [face, eye, lip, tongue, upper airway], throat tightness, urticaria) have occurred in patients with no prior exposure to perflutren.

Embolization

Perflutren may bypass the pulmonary particle-filtering mechanism and directly enter the arterial circulation in patients with right-to-left, bidirectional, or transient right-to-left cardiac shunts, resulting in occlusion and ischemia.

QTc prolongation

Has occurred in patients receiving doses of lipid-based perflutren of up to 10 mcL/kg.

Ventricular arrhythmias

End-systolic triggering with high ultrasound mechanical indices may lead to ventricular arrhythmias.

Transmission of infectious agents

Perflutren protein-based contains albumin; there is a theoretical risk of transmission of Creutzfeldt-Jakob disease and viral diseases.

Overdosage

Symptoms

No data available.

Patient Information

  • Advise patients to inform their health care provider if they may be pregnant or are breast-feeding an infant.
  • Instruct patients to inform their health care provider if they have ever had an allergic or hypersensitivity reaction to blood, blood products, or albumin (perflutren protein-based only).
  • Advise patients to inform their health care provider if they have a congenital heart defect or recent worsening of heart or lung conditions.

Copyright © 2009 Wolters Kluwer Health.

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