Diazoxide
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| Non-proprietary name | Diazoxide | ||||||||||||||||||
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| Molecular formula | C 8 H 7 ClN 2 O 2 S | ||||||||||||||||||
| Brief description |
White to almost white, fine or crystalline powder |
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| Molar mass | 230.67 g · mol -1 | ||||||||||||||||||
| Physical state |
firmly |
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| Melting point |
330.5 ° C |
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| pK s value |
8.74 |
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | |||||||||||||||||||
Diazoxide is a benzothiadiazine - derivative which no diuretic has effect. It is lipophilic and at a physiological pH value is only about 10% as an anion. It is an orally effective selective potassium channel opener used as a hyperglycemic drug. By inhibiting the secretion of insulin in the islets of Langerhans, it causes a rapid and temporary, dose-dependent increase in blood sugar levels , generally over a period of less than eight hours.
Indications
The drug diazoxide is in hypoglycemia administered various origins orally, as in congenital leucine - hypersensitivity , with some congenital defects of the K ATP duct work in nesidioblastosis in pancreatic and extrapancreatic insulin-producing tumors, refractory malignant hypertension in renal insufficiency , and in glycogen storage disease .
Contraindications and undesirable effects
Treatment with diazoxide is contraindicated in cases of hypersensitivity to the active ingredient, allergy to benzothiadiazines, coronary artery disease and heart failure , diabetes mellitus , pheochromocytoma , azo dye and analgesic intolerance. There are no data on use in pregnant women. Embryotoxicity was found in animal studies . During the pregnancy , the drug should not be used, unless it is absolutely necessary. Since it is not known whether diazoxide is excreted in breast milk and since there is a risk of potentially serious side effects to the infant, women who require treatment while breastfeeding should stop breastfeeding.
The main undesirable effects of diazoxide are Na + and water retention, hyperuricemia , hypertrichosis (especially in children), leukopenia and thrombopenia , headache, dizziness. With long-term treatment, extrapyramidal symptoms may occur. Orally administered diazoxide has only a minor effect on blood pressure.
Commercial preparations
Proglicem (D, CH), Eudemine (GB), Proglycem (USA)
literature
- W. Forth, D. Henschler, W. Rummel: General and special pharmacology and toxicology . 9th edition. Urban & Fischer, Munich 2005, ISBN 3-437-42521-8 .
Individual evidence
- ↑ a b c European Pharmacopoeia Commission (Ed.): EUROPÄISCHE PHARMACOPÖE 5th EDITION . tape 5.0-5.7 , 2006.
- ↑ a b c d e Entry on diazoxide in the ChemIDplus database of the United States National Library of Medicine (NLM)
- ↑ a b Diazoxide data sheet from Sigma-Aldrich , accessed on March 24, 2011 ( PDF ).
- ↑ a b Claus-Jürgen Estler, Harald Schmidt: Pharmacology and toxicology for study and practice. 6th edition, 2007, Schattauer Verlag, ISBN 978-3-7945-2295-8 , p. 698, limited preview in the Google book search.
- ↑ a b Technical information from the Swiss drug compendium for Proglicem capsules from Essex Chemie, as of July 2004.
- ↑ Red List online, as of October 2009.
- ↑ AM comp. d. Switzerland, as of October 2009.
