Sandostatin injection

Recommended dosage and monitoring requirements Sandostatin injectable solution is usually administered subcutaneously in initial doses of 50 to 100 pg two or three times daily. Upward dose titration is frequently required. Sandostatin LAR Depot injectable suspension should never be administered intravenously or subcutaneously. Patients not currently receiving octreotide acetate should begin therapy with subcutaneous injections and then can be switched to the depot injection of 20mg intragluteally at 4-week intervals for 3 months. 

Octreotide (Sandostatin) injection is commercially available in the United States for subcutaneous or intravenous administration. A long-acting intramuscular formulation of octreotide (Sandostatin EAR) is also available for monthly administration. In addition to the treatment of acromegaly, octreotide has many other therapeutic uses, including the treatment of carcinoid tumors, vasoactive intestinal peptide tumors (VIPomas), gastrointestinal fistulas, variceal bleeding, diarrheal states, and irritable bowel syndrome. 

Many drugs are administered as parenterals for speed of action because the patient is unable to take oral medication or because the drug is a macromolecule such as a protein that is unable to be orally absorbed intact due to stability and permeability issues. The U.S. Pharmacopoeia defines parenteral articles as preparations intended for injection through the skin or other external boundary tissue, rather than through the alimentary canal. They include intravenous, intramuscular, or subcutaneous injections. Intravenous injections are classified as small volume (<100 mL per container) or large volume (>100 mL per container) injections. The majority of parenteral dosage forms are supplied as ready-to-use solutions or reconstituted into solutions prior to administration. Suspension formulations may also be used,101 although their use is more limited to a subcutaneous (i.e., Novolin Penfill NOVO Nordisk) or intramuscular (i.e., Sandostatin LAR Depot Novartis) injection. Intravenous use of disperse systems is possible but limited (i.e., Doxil Injection Ortho Biotec). 

Somatostatin has a very brief half-life in serum and is not useful clinically. An 8-amino acid analogue with 2 D-amino acids substituted for the naturally occurring L-amino acids is more stable, and monthly injections of a depot form of this analogue (octreotide, Sandostatin LAR) have several uses. Long-acting octreotide is used to treat acromegaly, as described earlier. It is also used to counteract unpleasant effects caused by overproduction of secreted bioactive substances produced by neuroendocrine tumors, including hyperinsulinemia from insulinomas and secretions from carcinoid tumors that cause severe diarrhea. Octreotide may also control severe diarrhea associated with AIDS that has not responded to other treatments. 

Parenteral 10 mg/mL for subcutaneous injection Octreotide (generic, Sandostatin)... 

Parenteral depot injection (Sandostatin LAR Depot) 10, 20, 30 mg powder in single-use vials to reconstitute for IM injection... 

Rideout DJ, Graham MM. Buttock granulomas a consequence of intramuscular injection of Sandostatin detected by In-111 octreoscan. Clin Nucl Med 2001 26(7) 650. 

Octreotide acetate injectable suspension (octreotide long-acting release Sandostatin LAR) is a slow-release formulation in which octreotide is incorporated into microspheres. It is instituted only after a brief course of shorter-acting octreotide has been demonstrated to be effective and tolerated. The microspheres must be carefully put into suspension and immediately injected into a gluteal muscle. Injections into alternate gluteal muscles are repeated at 4-week intervals in doses of 20-40 mg. Octreotide is extremely costly. 

Fig. 2 The influence of Sandostatin LAR biodegradable depot formulation on the mean plasma growth hormone concentrations in humans. Plasma concentrations are shown over a 24 hour period 28 days after administration of a second monthly 20mg dose of Sandostatin LAR, . For comparison, plasma concentrations are provided for untreated controls, , and for patients receiving multiple daily subcutaneous octreotide injections, A. (From Refs. ° ° l)...

FIG. 4.10. Biodistribution patterns in healthy W lstar rats injected with 100 pL of cold octreotide (Sandostatin, Novartis) 15 min prior to injection with I-DOTATATE (control group) and in untreated rats (problem group) at (a) 30 min, (b) 4 h and (c) 24h post-injection of - I-DO l A l A ll. . 

The tumour bearing rats from group (d) were injected intravenously with 0.2 mL of 50 gCi of Lu-DOTATATE or l-DOTATATE, corresponding to approximately 0.68 gg of DOTATATE and 150 gg of Sandostatin as a blocking agent. After 1 h, the tumours and tissues expressing somatostatin receptors were removed and weighed, and the radioactivity was determined. 

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