Trimetazidine is a drug for angina pectoris, sometimes referred to by the brand name
Vastarel MR. Each tablet contains 35 mg of trimetazidine.
Trimetazidine is an anti-ischemic (anti-anginal) metabolic agent, which improves myocardial glucose utilization through stopping of
fatty acid metabolismFatty acids are an important source of energy for many organisms. Excess glucose can be stored efficiently as fat. Triglycerides yield more than twice as much energy for the same mass as do carbohydrates or proteins. All cell membranes are built up of phospholipids, each of which contains two fatty...
.
By preserving the energy metabolism in cells exposed to
hypoxiaHypoxia is a pathological condition in which the body as a whole or a region of the body is deprived of adequate oxygen supply. Variations in arterial oxygen concentrations can be part of the normal physiology, for example, during strenuous physical exercise...
or
ischemiaIn medicine, ischemia is a restriction in blood supply, generally due to factors in the blood vessels, with resultant damage or dysfunction of tissue...
, trimetazidine prevents a decrease in intracellular
adenosine triphosphateAdenosine-5'-triphosphate is a multifunctional nucleotide that plays an important role in cell biology as a coenzyme, that is, the "molecular unit of currency" of intracellular energy transfer. ATP transports chemical energy within cells for metabolism...
levels, thereby ensuring the proper functioning of ionic pumps and transmembranous sodium-potassium flow whilst maintaining cellular
homeostasisHomeostasis is the property of a system, either open or closed, that regulates its internal environment and tends to maintain a stable, constant condition...
.
Trimetazidine is a drug for angina pectoris, sometimes referred to by the brand name
Vastarel MR. Each tablet contains 35 mg of trimetazidine.
Trimetazidine is an anti-ischemic (anti-anginal) metabolic agent, which improves myocardial glucose utilization through stopping of
fatty acid metabolismFatty acids are an important source of energy for many organisms. Excess glucose can be stored efficiently as fat. Triglycerides yield more than twice as much energy for the same mass as do carbohydrates or proteins. All cell membranes are built up of phospholipids, each of which contains two fatty...
.
By preserving the energy metabolism in cells exposed to
hypoxiaHypoxia is a pathological condition in which the body as a whole or a region of the body is deprived of adequate oxygen supply. Variations in arterial oxygen concentrations can be part of the normal physiology, for example, during strenuous physical exercise...
or
ischemiaIn medicine, ischemia is a restriction in blood supply, generally due to factors in the blood vessels, with resultant damage or dysfunction of tissue...
, trimetazidine prevents a decrease in intracellular
adenosine triphosphateAdenosine-5'-triphosphate is a multifunctional nucleotide that plays an important role in cell biology as a coenzyme, that is, the "molecular unit of currency" of intracellular energy transfer. ATP transports chemical energy within cells for metabolism...
levels, thereby ensuring the proper functioning of ionic pumps and transmembranous sodium-potassium flow whilst maintaining cellular
homeostasisHomeostasis is the property of a system, either open or closed, that regulates its internal environment and tends to maintain a stable, constant condition...
. It also inhibits oxidation of fatty acid in blood vessels.
Controlled studies in angina patients have shown that trimetazidine increases coronary flow reserve, thereby delaying the onset of ischemia associated with exercise, limits rapid swings in
blood pressureBlood pressure is the pressure exerted by circulating blood on the walls of blood vessels, and is one of the principal vital signs. During each heartbeat, BP varies between a maximum and a minimum pressure...
without any significant variations in
heart rateHeart rate is determined by the number of heartbeats per unit of time, typically expressed as beats per minute , it can vary with as the body's need for oxygen changes, such as during exercise or sleep. The measurement of heart rate is used by medical professionals to assist in the diagnosis and...
, significantly decreases the frequency of angina attacks, and leads to a significant decrease in the use of
nitratesGlyceryl trinitrate is an alternate name for the chemical nitroglycerine, which has been used to treat angina and heart failure since at least 1870. Despite this, the mechanism of nitric oxide generation from GTN and the metabolic consequences of this bioactivation are still not entirely understood...
.
It improves
left ventricular functionThe left ventricle is one of four chambers in the human heart. It receives oxygenated blood from the left atrium via the mitral valve, and pumps it into the aorta via the aortic valve.-Shape:...
in diabetic patients with
coronary heart diseaseCoronary artery disease is the end result of the accumulation of atheromatous plaques within the walls of the coronary arteries that supply the myocardium with oxygen and nutrients...
. Recently, it has been shown to be effective in patients with heart failure of different etiologies (5-6).
Trimetazidine is described as the first cytoprotective anti-ischemic agent. It acts by directly counteracting all the major metabolic disorders occurring within the ischemic cell. The actions of trimetazidine include limitation of intracellular
acidosisAcidosis is an increased acidity . If not further qualified, it usually refers to acidity of the blood plasma....
, correction of disturbances of transmembrane ion exchanges, and prevention of excessive production of
free radicalIn chemistry, radicals are atoms, molecules, or ions with unpaired electrons on an otherwise open shell configuration. These unpaired electrons are usually highly reactive, so radicals are likely to take part in chemical reactions...
s.
Trimetazidine is usually prescribed as a long-term treatment of angina pectoris, and in some countries (including France) for
tinnitusTinnitus is the perception of sound within the human ear in the absence of corresponding external sound....
and dizziness. It is taken twice a day.
Trimetazidine has high safety and tolerability profile. It has no known drug interactions.
Reservations
There is scarce information about trimetazidine's effect on mortality, cardiovascular events or quality of life. Long term trials comparing trimetazidine against standard anti-anginal agents, using clinically important outcomes would be justifiable.
http://www.cochrane.org/reviews/en/ab003614.html
Brand names
Distributed as: Vastarel 35 mg, Vastarel 20 mg, Vastarel LM, Vastarel LP, Preductal MR, Flavedon MR, Flavedon 20 mg, Cardaptan, Idaptan, Carvidon MR and Trizedon MR. In the Philippines, a local brand is called
Vestar.
External links
http://www.cochrane.org/reviews/en/ab003614.html