Pindolol

  • (±)- pindolol
  • ( RS)- pindolol
  • Rac- pindolol
  • DL- pindolol
  • (±) -1 - (1H-indol -4- yloxy ) -3 - ( 1 - methylethylamino ) propan- 2-ol

C07AA03

Beta blocker

167-171 ° C

Water: 7880 mg · l-1 at 25 ° C

Attention

263 mg · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

Pindolol is a drug from the group of beta blockers and including the treatment of hypertension (high blood pressure) is used. It may also be used in the rescue medicine for the treatment of supraventricular tachycardia, which may occur after the administration of nitroglycerin.

  • 2.1 pharmacokinetics
  • 3.1 stereochemistry

Clinical information

Pindolol belongs to the group of non-selective beta-blockers, since it does not specifically bind to the β1 -adrenoceptors. The relative potency compared to 5 is pindolol propranolol has an intrinsic sympathomimetic activity (ISA) in, as well as the beta-blockers acebutolol and oxprenolol. Unlike beta-blockers without ISA Beta -blockers with ISA have no beneficial effect in myocardial infarction. Beta-blockers with ISA are frequently lead to insomnia, as beta-blockers without ISA.

Responsiveness

Even in proper ingestion ability to react may be so far reduced that an active participation in the driving or operating machinery is not recommended.

Pharmacological properties

Pharmacokinetics

The fat-soluble pindolol is well absorbed after oral administration and has a plasma half -life of 3 to 6 hours. It undergoes less first-pass effect than propranolol, the bioavailability is highly variable and ranges from 40 % to 90 %. The plasma protein binding of pindolol is 60%. The pindolol is excreted in the kidney to 40%.

Other Information

Stereochemistry

The significance of the enantiomeric purity of the active compounds synthetically produced is increasingly given attention, for the two enantiomers of a chiral drug almost always show a different pharmacology and pharmacokinetics. This was previously often ignored due to ignorance of stereochemical relationships. In this respect, it is worth mentioning that pindolol is used as a racemate. The active stereoisomer ( eutomer ) is the (S)- form of pindolol.

Trade names

Glauco - Stulln (D), Viskaldix (D, CH), Visken (D, A, CH)

Viskenit (A)

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Dangerous Substances Directive (67/548/EEC) Active ingredient European Journal of Clinical Pharmacology
650815
de