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Cited by 160Growth Hormone and Insulin-like Growth FactorsPituitary Gland Disorders and TreatmentsHypothalamic control of reproductive hormones

Oral Octreotide Absorption in Human Subjects: Comparable Pharmacokinetics to Parenteral Octreotide and Effective Growth Hormone Suppression

Tuvia, S., Atsmon, J., Teichman, S. L., Katz, S., Salama, P., Pelled, D., Landau, I., Karmeli, I. +5 more·2012·The Journal of Clinical Endocrinology & Metabolism
DOI 10.1210/jc.2012-1179
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Abstract

CONTEXT: Oral administration of a novel octreotide formulation enabled its absorption to the systemic circulation, exhibiting blood concentrations comparable to those observed with injected octreotide and maintaining its biological activity. OBJECTIVES: The aim of the study was to determine oral octreotide absorption and effects on pituitary GH secretion compared to sc octreotide injection. DESIGN: Four single-dose studies were conducted in 75 healthy volunteers. INTERVENTION: Oral doses of 3, 10, or 20 mg octreotide and a single sc injection of 100 μg octreotide were administered. MAIN OUTCOME MEASURE: We measured the pharmacokinetic profile of orally administrated octreotide and the effect of octreotide on basal and stimulated GH secretion. RESULTS: Both oral and sc treatments were well tolerated. Oral octreotide absorption to the circulation was apparent within 1 h after dose administration. Escalating oral octreotide doses resulted in dose-dependent increased plasma octreotide concentrations, with an observed rate of plasma decay similar to parenteral administration. Both 20 mg oral octreotide and injection of 0.1 mg sc octreotide resulted in equivalent pharmacokinetic parameters [mean peak plasma concentration, 3.77 ± 0.25 vs. 3.97 ± 0.19 ng/ml; mean area under the curve, 16.2 ± 1.25 vs. 12.1 ± 0.45 h × ng/ml); and median time ≥ 0.5 ng/ml, 7.67 vs. 5.88 h, respectively). A single dose of 20 mg oral octreotide resulted in basal (P < 0.05) and GHRH-stimulated (P < 0.001) mean GH levels suppressed by 49 and 80%, respectively. CONCLUSIONS: The results support an oral octreotide alternative to parenteral octreotide treatment for patients with acromegaly.

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Crossref · 10.1210/jc.2012-1179

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  • Octreotide can reduce orthostatic tachycardia in POTS patients to a similar extent as midodrine, but it lacks a widely available oral dosage form and must be administered subcutaneously.

    “While it can reduce orthostatic tachycardia in POTS patients to a similar extent as midodrine, it lacks a widely available oral dosage form and must be administered subcutaneously (60, 61).”

    From Postural orthostatic tachycardia syndrome: mechanisms and new therapies (2020) · cites this paper as [61]

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Authors
Tuvia, S., Atsmon, J., Teichman, S. L., Katz, S., Salama, P., Pelled, D., Landau, I., Karmeli, I., Bidlingmaier, M., Strasburger, C. J., Kleinberg, D. L., Melmed, S., & Mamluk, R.
Affiliations
  • Tel Aviv University (IL)
  • LMU Klinikum (DE)
  • Stiftung Charité (DE)
  • New York University (US)
  • Cedars-Sinai Medical Center (US)
Corresponding author
Mamluk, R.
ORCID
Venue
The Journal of Clinical Endocrinology & Metabolism
Publisher
The Endocrine Society
Published
2012-07
Volume
97
Issue
7
Pages
2362-2369
ISSN
  • 0021-972X (ISSN-L)
  • 1945-7197
DOI
10.1210/jc.2012-1179
OpenAlex
W2017466268
Cited by
160
References
29
Citations by year
2026: 9 · 2025: 11 · 2024: 14 · 2023: 9 · 2022: 13 · 2021: 28 · 2020: 11 · 2019: 5 · 2018: 3 · 2017: 5 · 2016: 17 · 2015: 10 · 2014: 17 · 2013: 6 · 2012: 2
FWCI
8.99
Type
journal article
Language
en
Open access
closed
Locations
  • The Journal of Clinical Endocrinology & Metabolism (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Growth Hormone and Insulin-like Growth Factors
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Pituitary Gland Disorders and Treatments
  • Health Sciences › Medicine › Reproductive Medicine › Hypothalamic control of reproductive hormones
Keywords
octreotide, pharmacokinetics, growth hormone suppression, acromegaly, GHRH stimulation, oral drug absorption, growth hormone secretion
MeSH terms
Absorption, Administration, Oral, Adolescent, Adult, Dose-Response Relationship, Drug, Female, Humans, Infusions, Parenteral, Male, Middle Aged, Octreotide, Treatment Outcome, Cross-Over Studies, Antineoplastic Agents, Hormonal, Human Growth Hormone, Research Subjects, Infusions, Subcutaneous, Young Adult

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