A randomized comparison of intranasal and injectable octreotide administration in patients with acromegaly
| Autor: | Hans Ørskov, P. Illum, Jørgen Weeke, M. Mau Pedersen, Andreas Kaal, S. E. Christensen, A. G. Harris |
|---|---|
| Rok vydání: | 1992 |
| Předmět: |
Adult
Blood Glucose Male medicine.medical_specialty Injections Subcutaneous Endocrinology Diabetes and Metabolism Clinical Biochemistry Octreotide Mucous membrane of nose Biochemistry Route of administration Endocrinology Acoustic rhinometry Pharmacokinetics Internal medicine Acromegaly medicine Humans Insulin Administration Intranasal Aged business.industry Biochemistry (medical) Middle Aged medicine.disease Somatostatin Growth Hormone Female Nasal administration business medicine.drug |
| Zdroj: | The Journal of Clinical Endocrinology & Metabolism. 75:163-169 |
| ISSN: | 1945-7197 0021-972X |
| Popis: | Fifteen acromegalic patients received four single doses of octreotide in random order (500 micrograms, 1000 micrograms, and 2000 micrograms applied intranasally and 100 micrograms given sc). Serum octreotide and GH data were subjected to pharmacokinetic analyses, and local nasal effects were evaluated by acoustic rhinometry. Average areas (+/- SEM) under the serum octreotide curves were: 2000 micrograms: 4597 +/- 536; 1000 micrograms: 1923 +/- 439; 500 micrograms: 957 +/- 168; and 100 micrograms sc: 896 +/- 81 micrograms.L-1.min (n = 13). The calculated relative availability was 27% +/- 0.03; 22% +/- 0.05; 22% +/- 0.03, respectively, for the three nasal doses. The rate of absorption after intranasally administered octreotide was greater than after sc application: t1/2 ka: 7.1 +/- 1.6; 7.9 +/- 1.6; 11.3 +/- 1.9, respectively, vs. 24.1 +/- 2.5 min, whereas the rates of disappearance were similar. GH suppression started immediately after application and reached minimum levels 1-2 h later. The average intervals during which serum GH was below 50% of preadministration values were: 2000 micrograms: 544 +/- 47; 1000 micrograms: 423 +/- 56; 500 micrograms: 289 +/- 52 vs. 351 +/- 34 min after sc injection of 100 micrograms. With 2000 micrograms intranasally all but one of the 15 patients attained constant suppression of serum GH below 5 micrograms/L for 273 to 680 min. Pharmacokinetic analysis demonstrated that 100 micrograms sc and 1000 micrograms intranasally induced the same GH suppressive effect and that 2000 micrograms intranasally approximately doubled the duration of action. Acoustic rhinometry was performed after nasal application of the largest dose of 2000 micrograms and after carrier (n = 9). A highly significant tumescence of the nasal mucosa was maximal after 10 min and gradually receded over the next 2 h. However, this was felt by the patients to be acceptable. The effect was caused by octreotide per se and was probably due to vasodilation. |
| Databáze: | OpenAIRE |
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