Sandostatin LAR (microencapsulated octreotide acetate) in acromegaly: pharmacokinetic and pharmacodynamic relationships.
Double-blind, single-dose studies of 120 acromegalic patients given 10, 20, and 30 mg Sandostatin LAR (Sandoz Pharma Ltd, Basel, Switzerland) established the drug's pharmacokinetic profile. Patients then entered open-labeled extension phases, with Sandostatin LAR intramuscular (IM) injections every 4 weeks. These produced broadly constant octreotide concentrations with dose proportionality. Area fluctuations were minimal. Steady-state conditions were generally reached after the second to third injection. There was no evidence of downregulation with Sandostatin LAR over 1 year of study. Based on the pharmacokinetic/pharmacodynamic relationship of octreotide, a starting dose of 20 mg Sandostatin LAR and administrations every 4 weeks provide growth hormone (GH) control comparable to the thrice-daily subcutaneous (SC) injection regimen, which is commonly 0.3 to 0.6 mg/d. The reduction from the burden of two to three SC injections per day is a particular advantage of Sandostatin LAR, which is an attractive alternative to the approved Sandostatin injection.
Grass
P
P
Sandoz Pharma Ltd, Basel, Switzerland.
Marbach
P
P
Bruns
C
C
Lancranjan
I
I
D000172:Acromegaly / Q000188:drug therapy* / Q000378:metabolism; D002214:Capsules; D003692:Delayed-Action Preparations; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D013006:Growth Hormone / Q000097:blood; D006801:Humans; D007273:Injections, Intramuscular; D015282:Octreotide / Q000008:administration & dosage* / Q000097:blood / Q000627:therapeutic use; D013997:Time Factors
D002214:Capsules; D003692:Delayed-Action Preparations; D013006:Growth Hormone; D015282:Octreotide