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trimetazidine

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EntityQ674703· pop 21· linked from 221 articles

trimetazidine

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Also known as 1-(2,3,4-trimethoxybenzyl)piperazine, 1-[(2,3,4-trimethoxyphenyl)methyl]piperazine

Trimetazidine (IUPAC: 1-(2,3,4-trimethoxybenzyl)piperazine) is a drug used in the treatment of angina pectoris, a condition characterized by chest pain due to reduced blood flow to the heart. Developed and first marketed by Laboratoires Servier (France), it is described as the first cytoprotective anti-ischemic agent. Trimetazidine is an antianginal metabolic drug of the fatty acid oxidation inhibitor class; it shifts cardiac energy metabolism from fatty acid utilization toward glucose oxidation, thereby improving the efficiency of energy production in ischemic conditions.

Key facts

Drug.C
14
Drug.H
22
Drug.N
2
Drug.O
3
Drug.Verifiedfields
changed
Drug.verifiedrevid
470615044
Drug.IUPAC_name
1-(2,3,4-trimethoxybenzyl)piperazine
Drug.image
Trimetazidine.svg
Drug.image_class
skin-invert-image
Drug.tradename
Angintriz
Drug.legal_UK
CD
Drug.routes_of_administration
Oral
Drug.bioavailability
completely absorbed at around 5 hours, steady state is reached by 60th hour
Drug.protein_bound
low (16%)
Drug.metabolism
minimal
Drug.elimination_half life
7 to 12 hours
Drug.excretion
mainly renal (unchanged), exposure is increased in renal impairment – on average by four-fold in subjects with severe renal impairment (CrCl <30 ml/min)
Drug.CAS_number
5011-34-7

via Wikipedia infobox

Chemical data

Formula
C14H22N2O3
Molecular weight
266.34 g/mol
IUPAC name
1-[(2,3,4-trimethoxyphenyl)methyl]piperazine
SMILES
COC1=C(C(=C(C=C1)CN2CCNCC2)OC)OC
InChIKey
UHWVSEOVJBQKBE-UHFFFAOYSA-N
XLogP
1
Polar surface area
43 Ų
H-bond donors
1
H-bond acceptors
5
Formal charge
0

via PubChem

Research

1,410 papers

via PubMed

~10 min read

Encyclopedic overview

6 sections
Contents
  • Medical uses
  • Use as a performance-enhancing drug
  • Scientific criticism
  • Adverse effects
  • Mechanism of action
  • References

Trimetazidine (IUPAC: 1-(2,3,4-trimethoxybenzyl)piperazine) is a drug used in the treatment of angina pectoris, a condition characterized by chest pain due to reduced blood flow to the heart. Developed and first marketed by Laboratoires Servier (France), it is described as the first cytoprotective anti-ischemic agent. Trimetazidine is an antianginal metabolic drug of the fatty acid oxidation inhibitor class; it shifts cardiac energy metabolism from fatty acid utilization toward glucose oxidation, thereby improving the efficiency of energy production in ischemic conditions.

The drug has also become controversial as a performance-enhancing drug, with multiple doping scandals linked to its use at successive Olympic Games.

Excerpted from Wikipedia’s “trimetazidine” article, available under the CC BY-SA 4.0 licence.