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Transdermal versus subcutaneous leuprolide: A comparison of acute pharmacodynamic effect
Author(s) -
Robert Meyer B,
Kreis Willi,
Eschbach James,
O'Mara Vivian,
Rosen Sanford,
Sibalis Dan
Publication year - 1990
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1990.161
Subject(s) - transdermal , medicine , pharmacodynamics , adverse effect , subcutaneous injection , agonist , pharmacokinetics , route of administration , area under the curve , anesthesia , pharmacology , receptor
Transdermal administration of peptides has been limited by the barrier properties of the skin. We compared the acute luteinizing hormone (LH) response to subcutaneous and transdermal administration of an LH‐releasing hormone agonist (leuprolide). Eighteen volunteers received 5 mg leuprolide added to electrically powered patches delivering a current of 0.22 μA (transdermally). One week later, they received a 5 mg subcutaneous dose. LH response was measured. The area under the curve for LH response, maximum LH response, and time to maximum LH response were similar. Time to first response was shorter (147 ± 108 minutes [transdermally] and 73 ± 74 minutes [subcutaneously]; p < 0.05), and the area under the curve for the first 150 minutes was greater (3655 ± 2246 mIU · min/ml [transdermally] and 8666 ± 4067 mIU · min/ml [subcutaneously]; p < 0.05) for subcutaneous delivery. No major adverse effects were seen. This electrically powered transdermal technique merits further study. Clinical Pharmacology and Therapeutics (1990) 48, 340–345; doi: 10.1038/clpt.1990.161