Dimenhydrinate

(2- Benzhydryloxyethyl ) dimethyl -8 -chloro- 1, 3 - dimethyl- 3 ,7- dihydropurin -2 ,6- dione

R06AA02

Antihistamine, antiemetic

Competitive antagonism to histamine on the H1 receptor.

Attention

1320 mg · kg -1 ( LD50, rat, oral)

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Dimenhydrinate is a salt of diphenhydramine 8- chlorotheophylline and, thus a combination of two active ingredients. Diphenhydramine is an H1 receptor antagonist, an antihistamine, and thus the first generation. It is used mainly as an antiemetic and sedative. Chlorotheophylline is a mild stimulant and has been added to reduce the fatigue.

Mechanism of Action

The drug acts on the central nervous system, where it competitively blocks H1 receptors in the vomiting center.

Areas of application

Dimenhydrinate may in accordance with German approval for the prevention and symptomatic treatment of nausea and vomiting of various causes, in particular applied by motion sickness. However, dimenhydrinate is not suitable due to chemotherapy for the sole treatment of nausea and vomiting.

Contraindications

For dimenhydrinate for intravenous injection (trade name Vomex A) following absolute contraindications are listed in the product information:

Vomex A may not be used in

  • Hypersensitivity / allergy to dimenhydrinate, other antihistamines, or any other component of the drug,
  • Acute asthma attack,
  • Narrow-angle glaucoma,
  • Pheochromocytoma,
  • Porphyria,
  • Prostatic hyperplasia with residual urine,
  • Seizures (epilepsy, eclampsia ).
  • Hepatic function,
  • Cardiac arrhythmia,
  • Hypokalemia, hypomagnesemia,
  • Bradycardia,
  • Congenital long QT syndrome or other clinically significant cardiac disorders (especially coronary heart disease, conduction disturbances, arrhythmias ),
  • Simultaneous use of drugs that also prolong the QT interval (eg Class IA or III antiarrhythmics, antibiotics, antimalarials, antihistamines, antipsychotics ) or hypokalemia lead,
  • Chronic respiratory symptoms and asthma,
  • Pyloric stenosis

Side effects

During the chewing of dimenhydrinate preparations a temporary numbness of the oral mucosa may occur. Depending on the individual sensitivity and the ingested dose of dimenhydrinate may result, inter alia, to drowsiness and dizziness. As so-called cholinergic side effects dry mouth, increased heart beat sequence, feeling a stuffy nose, blurred vision, increased intraocular pressure and interference may occur when urinating. Patients with congenital long QT syndrome should refrain from taking, as the QT interval of the ECG by dimenhydrinate may be extended dangerous in predisposed.

Since dimenhydrinate is 8-chloro- theophylline degraded in the body to diphenhydramine and it can hallucinogen from a dose of 400 mg and act delirious. In the drug scene, it is referred to as DMH. However, it is hardly used, in particular due to the more effective diphenhydramine.

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Dangerous Substances Directive (67/548/EEC)
290395
de