Diltiazem
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Non-proprietary name | Diltiazem | |||||||||||||||||||||
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Molecular formula | C 22 H 26 N 2 O 4 S | |||||||||||||||||||||
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Molar mass | 414.52 g · mol -1 | |||||||||||||||||||||
Physical state |
firmly |
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Melting point |
207–212 ° C (diltiazem hydrochloride) |
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As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . |
Diltiazem is a drug from the group of calcium antagonists or calcium channel blockers, which has a vasodilator and conduction delay in the AV node of the heart . Diltiazem is one of the benzothiazepines . In Germany it is sold as Dilzem by the Pfizer company and by numerous other providers under the generic name.
history
Diltiazem ( Dilzem ) was first developed in Japan in the early 1970s . Masanori Sato examined this for pharmacological properties. The calcium antagonistic effect was discovered in 1975 by Nakajima.
application
In patients with coronary artery disease , diltiazem is used for stable angina pectoris , for unstable angina pectoris and especially for vasospastic angina pectoris ( Prinzmetal's angina ).
As an antiarrhythmic for the treatment of cardiac arrhythmias , diltiazem can be prescribed as a preventive measure against paroxysmal supraventricular tachycardias and in patients without WPW syndrome to slow the pulse rate in atrial fibrillation and atrial flutter .
In the treatment of high blood pressure , diltiazem is used to lower blood pressure .
It is used locally to treat anal fissures , for example as an ointment or cream.
Diltiazem is also used in the treatment of diffuse esophageal spasms. Here it leads to a relaxation of the smooth muscles of the esophagus.
Contraindications and warnings
Diltiazem may be used with SA block II. And III. Degree and during pregnancy . Intravenous administration is also contraindicated in bradycardia (pulse <55 beats per minute) .
Careful monitoring is required in Grade I SA block, in elderly patients, in severely impaired renal function, and in concurrent therapy with beta-blockers .
Even if the baby has not been known to harm it, it should not be taken during breastfeeding , as it passes into breast milk .
Side effects
Increase in liver enzymes Gamma-GT and LDH , lymph node swelling , vomiting , heartburn , diarrhea , SA block , weakness, edema . Allergic skin symptoms, syncope , heart failure , insomnia , hallucinations and depressive moods and erectile dysfunction are rare . In diabetics can hyperglycaemia occur.
Trade names
Coridil (CH), Dilsal (July 7, 1993 TAD Pharma GmbH, DE), Dil-Sanorania (D), Diltaretard (D), Diltiagamma (D), Dilzem (February 2, 1978 Pfizer GmbH D, A, CH), Tildiem (CH), various generics (D, A, CH)
Individual evidence
- ^ The Merck Index : An Encyclopedia of Chemicals, Drugs, and Biologicals, 14th Edition (Merck & Co., Inc.), Whitehouse Station, NJ, USA, 2006; P. 543, ISBN 978-0-911910-00-1 .
- ↑ a b Data sheet (+) - cis-Diltiazem hydrochloride from Sigma-Aldrich , accessed on March 25, 2011 ( PDF ).
- ↑ Entry on Diltiazem. In: Römpp Online . Georg Thieme Verlag, accessed on October 1, 2014.
- ^ Wolf-Dieter Müller-Jahncke , Christoph Friedrich , Ulrich Meyer: Medicinal history . 2., revised. and exp. Ed. Wiss. Verl.-Ges, Stuttgart 2005, ISBN 978-3-8047-2113-5 , pp. 174 .
- ^ Franz Bader, Hans-Peter Bruch, Oliver Schwandner: Topical diltiazem for the treatment of chronic anal fissures. In: Coloproctology . Volume 28, Number 6, pp. 309-313; doi : 10.1007 / s00053-006-6020-3 .
- ↑ Red List 2017.
- ↑ AM comp. d. Switzerland, as of September 2009.
- ↑ AGES-PharmMed, as of September 2009.