OctreoScan

Name: OctreoScan

Uses of OctreoScan

  • It is used with a test to check for tumors.

How do I store and/or throw out OctreoScan?

  • If you need to store OctreoScan at home, talk with your doctor, nurse, or pharmacist about how to store it.

OctreoScan Description

OctreoScan™ is a kit for the preparation of indium In-111 pentetreotide, a diagnostic radiopharmaceutical. It is a kit consisting of two components:

1)     A 10-mL OctreoScan Reaction Vial which contains a lyophilized mixture of:

(i) 10 μg pentetreotide [N-(diethylenetriamine-N,N,N',N”-tetraacetic acid-N”-acetyl)-D-phenylalanyl-L-hemicystyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-L-hemicystyl-L-threoninol cyclic (2→7) disulfide], (also known as octreotide DTPA),
(ii) 2.0 mg gentisic acid [2, 5-dihydroxybenzoic acid],
(iii) 4.9 mg trisodium citrate, anhydrous,
(iv) 0.37 mg citric acid, anhydrous, and
(v) 10.0 mg inositol.

Pentetreotide has the following structural formula:

 

Prior to lyophilization, sodium hydroxide or hydrochloric acid may have been added for pH adjustment. The vial contents are sterile and nonpyrogenic. No bacteriostatic preservative is present.

2)     A 10-mL vial of Indium In-111 Chloride Sterile Solution, which contains: 1.1 mL or 111 MBq/mL (3.0 mCi/mL) indium In-111 chloride in 0.02N HCl at time of calibration. The vial also contains ferric chloride at a concentration of 3.5 μg/mL (ferric ion, 1.2 μg/mL). The vial contents are sterile and nonpyrogenic. No bacteriostatic preservative is present.

Indium In-111 pentetreotide is prepared by combining the two kit components (see INSTRUCTIONS FOR THE PREPARATION OF INDIUM In-111 PENTETREOTIDE). Indium In-111 reacts with the diethylenetriaminetetraacetic acid portion of the pentetreotide molecule to form indium In 111 pentetreotide. The pH of the resultant indium In-111 pentetreotide solution is between 3.8 and 4.3. No bacteriostatic preservative is present.

The indium In-111 pentetreotide solution is suitable for intravenous administration as is, or it may be diluted to a maximum volume of 3.0 mL with 0.9% Sodium Chloride Injection, U.S.P., immediately before intravenous administration. In either case, the labeling yield of indium In-111 pentetreotide should be determined before administration to the patient. A method recommended for determining the labeling yield is presented at the end of this package insert.

OctreoScan - Clinical Pharmacology

General

Pentetreotide is a DTPA conjugate of octreotide, which is a long-acting analog of the human hormone, somatostatin. Indium In-111 pentetreotide binds to somatostatin receptors on cell surfaces throughout the body. Within an hour of injection, most of the dose of indium In-111 pentetreotide distributes from plasma to extravascular body tissues and concentrates in tumors containing a high density of somatostatin receptors. After background clearance, visualization of somatostatin receptor-rich tissue is achieved. In addition to somatostatin receptor-rich tumors, the normal pituitary gland, thyroid gland, liver, spleen and urinary bladder also are visualized in most patients, as is the bowel, to a lesser extent. Excretion is almost exclusively via the kidneys.

Pharmacokinetics

Radioactivity leaves the plasma rapidly; one third of the radioactive injected dose remains in the blood pool at 10 minutes after administration. Plasma levels continue to decline so that by 20 hours post-injection, about 1% of the radioactive dose is found in the blood pool. The biological half-life of indium In-111 pentetreotide is 6 hours.

Half of the injected dose is recoverable in urine within six hours after injection, 85% is recovered in the first 24 hours, and over 90% is recovered in urine by two days.

Hepatobiliary excretion represents a minor route of elimination, and less than 2% of the injected dose is recovered in feces within three days after injection.

Metabolism

For several hours after administration, plasma radioactivity is predominantly in parent form. Ten percent of the radioactivity excreted is nonpeptide-bound.

Pharmacodynamics

Indium In-111 pentetreotide binds to cell surface receptors for somatostatin. In nonclinical pharmacologic studies, the hormonal effect of OctreoScan in vitro is one-tenth that of octreotide. Since diagnostic imaging doses of indium In-111 pentetreotide are lower than the therapeutic doses of octreotide, indium In-111 pentetreotide is not expected to exert clinically significant somatostatin effects.

Indium In-111 pentetreotide is cleared from the body primarily by renal excretion. Indium In-111 pentetreotide elimination has not been studied in anephric patients or in those with poorly functioning kidneys. It is not known whether indium In-111 pentetreotide can be removed by dialysis. Dosage adjustments in patients with decreased renal function have not been studied.

Contraindications

None known.

Warnings

DO NOT ADMINISTER IN TOTAL PARENTERAL NUTRITION (TPN) ADMIXTURES OR INJECT INTO TPN INTRAVENOUS ADMINISTRATION LINES; IN THESE SOLUTIONS, A COMPLEX GLYCOSYL OCTREOTIDE CONJUGATE MAY FORM.

The sensitivity of scintigraphy with indium In-111 pentetreotide may be reduced in patients concurrently receiving therapeutic doses of octreotide acetate. Consideration should be given to temporarily suspending octreotide acetate therapy before the administration of indium In-111 pentetreotide and to monitoring the patient for any signs of withdrawal.

Adverse Reactions

The following adverse effects were observed in clinical trials at a frequency of less than 1% of 538 patients: dizziness, fever, flush, headache, hypotension, changes in liver enzymes, joint pain, nausea, sweating, and weakness. These adverse effects were transient. Also in clinical trials, there was one reported case of bradycardia and one case of decreased hematocrit and hemoglobin.

Pentetreotide is derived from octreotide which is used as a therapeutic agent to control symptoms from certain tumors. The usual dose for indium In-111 pentetreotide is approximately 5 to 20 times less than for octreotide and is subtherapeutic. The following adverse reactions have been associated with octreotide in 3% to 10% of patients: nausea, injection site pain, diarrhea, abdominal pain/discomfort, loose stools, and vomiting. Hypertension and hyper- and hypoglycemia have also been reported with the use of octreotide.

Principal display panel - a050v0

OctreoScan™ Reaction Vial

Sterile, non-pyrogenic. For intravenous use after drug preparation. See package insert for directions for use.

Vial contains:
10 µg Pentetreotide
2.0 mg Gentisic Acid
4.9 mg Sodium Citrate, Anhydrous
0.37 mg Citric Acid, Anhydrous
10.0 mg Inositol

Prior to lyophilization, sodium hydroxide or hydrochloric acid may be added for pH adjustment. The pH of the reconstituted drug is between 3.8 and 4.3. Contents are sealed under nitrogen.

Manufactured by:
Mallinckrodt Nuclear Medicine LLC
Maryland Heights, MO 63043

Made in USA

Store refrigerated at 2° to 8°C (36°-46°F). Protect from light.

Use only with Indium In 111 Chloride Sterile Solution.

Rx only

Mallinckrodt™
Pharmaceuticals


A050V0
R10/2015

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