Octreotide

Category: peptide

Aliases: SMS 201-995, Sandostatin, Sandostatin LAR

Pharmacological Mechanism

Cyclic octapeptide with a disulfide bridge (Cys-2 – Cys-7) and D-Phe, D-Trp, Thr-ol modifications — producing 30× longer t½ than native somatostatin (1.5 h vs 2 min) and SSTR2 > SSTR5 selectivity. Suppresses GH + IGF-1 (acromegaly), inhibits hormone release from functional neuroendocrine tumours (carcinoid, VIPoma, glucagonoma), and reduces portal pressure acutely (variceal bleeding). LAR formulation: biodegradable PLGA microspheres release drug over ~4 weeks.

Half-Life (t½)

SC: 1.5h, IV: 1.5h, IM: 1.5h

Dosing Guidelines

Target Organ Systems