Atracurium besilate

  • IUPAC: 5 - [3 - [ 1 - [( 3,4- dimethoxyphenyl ) methyl] - 6,7- dimethoxy -2-methyl -3 ,4- dihydro-1H- isoquinolin- 2-yl] propanoyloxy ] pentyl -3 - [1 - [( 3,4- dimethoxyphenyl) methyl] - 6,7- dimethoxy -2-methyl -3 ,4- dihydro-1H- isoquinolin- 2-yl] propanoate
  • Atracurium besylate
  • 64228-79-1
  • 64228-81-5 ( atracurium besilate · )

M03AC04

Muscle relaxants

  • 929.15 g.mol -1
  • 1243.48 g · mol -1 ( atracurium besilate · )

Besilate

> 50 mg · kg -1 ( LD50, Rat, oral, besilate )

Template: Infobox chemical / molecular formula search available

Atracurium is a drug from the group of muscle relaxants, which is used during surgery and in intensive care.

  • 2.1 Mechanism of action ( pharmacodynamics )
  • 2.2 metabolism
  • 3.1 Chemical Information
  • 3.2 History

Clinical information

Areas of application (indications )

Atracurium is used to obtain a muscular relaxation ( muscle relaxation ) for surgery or other medical procedures, such as mechanical ventilation.

Interactions with other drugs

A prolonged duration of action or gain at co-administered with aminoglycosides, loop diuretics, magnesium, lithium, succinylcholine or volatile anesthetics is possible.

Adverse effects (side effects)

By histamine release, it may lead to skin redness, cardiac arrhythmias, hypotension and bronchospasm. The cis isomer does not, in contrast to cisatracurium atracurium to histamine release. The metabolite laudanosine is attributed to trigger seizures.

Pharmacological properties

Mechanism of action ( pharmacodynamics )

Atracurium as a peripherally acting muscle relaxant binds competitively to the acetylcholine receptor of the neuromuscular junction without causing depolarization. The effect of acetylcholine is blocked by it.

Metabolism

1/3 of atracurium spontaneously breaks ( Hofmann elimination ), 2/ 3 are non-specific esterases in blood plasma by split ( ester hydrolysis ). As degradation products arising Pentametyldiacrylat, laudanosine, quaternary acids and alcohol.

Other Information

Chemical information

The Benzylisochinolinderivat atracurium belongs chemically to the esters, tetrahydropyridine derivatives and phenol ethers. It is a mixture of ten different stereoisomers.

History

Atracurium was synthesized by John B. Stenlake 1974. In Germany atracurium in 1987 was approved.

Trade names

Tracrium (D, A, CH ), various generics (D)

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Dangerous Substances Directive (67/548/EEC) Active ingredient Intensive care medicine Blood pressure Saponification
86872
de