Trimetazidine
Encyclopedia
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 inhibition of fatty acid metabolism
, also known as fatty acid oxidation inhibitor.
By preserving the energy metabolism in cells exposed to hypoxia
or ischemia
, trimetazidine prevents a decrease in intracellular adenosine triphosphate
levels, thereby ensuring the proper functioning of ionic pumps and transmembranous sodium-potassium flow whilst maintaining cellular homeostasis
. 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 pressure
without any significant variations in heart rate
, significantly decreases the frequency of angina attacks, and leads to a significant decrease in the use of nitrates.
It improves left ventricular function
in diabetic patients with coronary heart disease
. 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 developed and marketed by Les Laboratoires Servier (France). It acts by directly counteracting all the major metabolic disorders occurring within the ischemic cell. The actions of trimetazidine include limitation of intracellular acidosis
, correction of disturbances of transmembrane ion exchanges, and prevention of excessive production of free radical
s.
Trimetazidine is usually prescribed as a long-term treatment of angina pectoris, and in some countries (including France) for tinnitus
and dizziness. It is taken twice a day.
Trimetazidine has high safety and tolerability profile. It has no known drug interactions.
Trimetazidine is an anti-ischemic (anti-anginal) metabolic agent, which improves myocardial glucose utilization through inhibition of fatty acid metabolism
Fatty acid metabolism
Fatty acids are an important source of energy and adenosine triphosphate for many cellular organisms. Excess fatty acids, glucose, and other nutrients 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...
, also known as fatty acid oxidation inhibitor.
By preserving the energy metabolism in cells exposed to hypoxia
Hypoxia (medical)
Hypoxia, or hypoxiation, 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 ischemia
Ischemia
In medicine, ischemia is a restriction in blood supply, generally due to factors in the blood vessels, with resultant damage or dysfunction of tissue. It may also be spelled ischaemia or ischæmia...
, trimetazidine prevents a decrease in intracellular adenosine triphosphate
Adenosine triphosphate
Adenosine-5'-triphosphate is a multifunctional nucleoside triphosphate used in cells as a coenzyme. It is often called 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 homeostasis
Homeostasis
Homeostasis is the property of a system that regulates its internal environment and tends to maintain a stable, constant condition of properties like temperature or pH...
. It also inhibits oxidation of fatty acid in blood vessels.
Controlled studies in angina patients have shown that trimetazidine increases coronary flow reserve
Coronary flow reserve
Coronary flow reserve ' is the maximum increase in blood flow through the coronary arteries above the normal resting volume. Its measurement is often used in medicine to assist in the treatment of conditions affecting the coronary arteries and to determine the efficacy of treatments...
, thereby delaying the onset of ischemia associated with exercise, limits rapid swings in blood pressure
Blood pressure
Blood pressure is the pressure exerted by circulating blood upon the walls of blood vessels, and is one of the principal vital signs. When used without further specification, "blood pressure" usually refers to the arterial pressure of the systemic circulation. During each heartbeat, BP varies...
without any significant variations in heart rate
Heart rate
Heart rate is the number of heartbeats per unit of time, typically expressed as beats per minute . Heart rate can vary as the body's need to absorb oxygen and excrete carbon dioxide changes, such as during exercise or sleep....
, significantly decreases the frequency of angina attacks, and leads to a significant decrease in the use of nitrates.
It improves left ventricular function
Left ventricle
The 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 disease
Coronary heart disease
Coronary 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. It is sometimes also called coronary heart disease...
. 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 developed and marketed by Les Laboratoires Servier (France). It acts by directly counteracting all the major metabolic disorders occurring within the ischemic cell. The actions of trimetazidine include limitation of intracellular acidosis
Acidosis
Acidosis is an increased acidity in the blood and other body tissue . 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 radical
Radical (chemistry)
Radicals are atoms, molecules, or ions with unpaired electrons on an open shell configuration. Free radicals may have positive, negative, or zero charge...
s.
Trimetazidine is usually prescribed as a long-term treatment of angina pectoris, and in some countries (including France) for tinnitus
Tinnitus
Tinnitus |ringing]]") is the perception of sound within the human ear in the absence of corresponding external sound.Tinnitus is not a disease, but a symptom that can result from a wide range of underlying causes: abnormally loud sounds in the ear canal for even the briefest period , ear...
and dizziness. It is taken twice a day.
Trimetazidine has high safety and tolerability profile. It has no known drug interactions.