Vastinol
Vastinol Uses, Dosage, Side Effects, Food Interaction and all others data.
Vastinol is an anti-ischemic (anti-anginal) metabolic agent, which improves myocardial glucose utilization through inhibition of long-chain 3-ketoacyl CoA thiolase activity, which results in a reduction in fatty acid oxidation and a stimulation of glucose oxidation. High fatty acid oxidation rates are detrimental during ischemia due to an inhibition of glucose oxidation leading to uncoupling of glycolysis and an increase in proton production, which has the potential to accelerate sodium and calcium overload in the heart. This leads to an exacerbation of ischemic injury and decreased cardiac efficiency during reperfusion.
Vastinol is indicated for the symptomatic treatment of stable angina pectoris in patients inadequately controlled or intolerant to first line therapies. Patients should be counselled regarding the risk of use with reduced renal or hepatic function, worsening of extrapyramidal symptoms or other movement disorders, and risk of falls.
| Trade Name | Vastinol |
| Generic | Trimetazidine |
| Trimetazidine Other Names | Trimetazidina, Trimetazidine |
| Type | |
| Formula | C14H22N2O3 |
| Weight | Average: 266.341 Monoisotopic: 266.163042576 |
| Protein binding | Trimetazidine is 15% protein bound in plasma. Trimetazidine can bind to human serum albumin. |
| Groups | Approved, Investigational |
| Therapeutic Class | Other Anti-anginal & Anti-ischaemic drugs |
| Manufacturer | |
| Available Country | Thailand |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Long-term treatment of Ischaemic heart disease (angina pectoris, sequelae of infarction).
Vastinol is also used to associated treatment for these conditions: Angina Pectoris, Chronic Stable Angina Pectoris, Dizziness, Tinnitus, Decreased visual acuity caused by Vascular Disorders
How Vastinol works
During myocardial ischemia, anaerobic metabolism takes over, increasing levels of lactic acid. The decreased intracellular pH and increased concentration of protons activates sodium-hydrogen and sodium-calcium antiport systems, raising intracellular calcium concentrations, finally leading to decreased contractility.
This injury to the myocardium raises concentrations of catecholamines, which activate hormone sensitive lipase, and increasing fatty acid concentrations in plasma. When the myocardium is repurfused, fatty acid oxidation becomes the dominant form of ATP production, maintaining an acidic pH, and further exacerbating the injury.
The mechanism of action of trimetazidine is not fully understood. Vastinol may inhibit mitochondrial 3-ketoacyl coenzyme A thiolase, decreasing long chain fatty acid β-oxidation but not glycolysis in the myocardium. The decreased long chain fatty acid β-oxidation is compensated for by increased use of glucose, preventing a lowered myocardial pH, and further decreases in contractility. However, another study suggests that 3-ketoacyl coenzyme A thiolase may not be trimetazidine's target, and that this mechanism may be incorrect.
Dosage
Vastinol dosage
One 20 mg tablet thrice daily after meals. No dosage adjustments are required in patients with impaired renal and hepatic function.
One 35 mg modified release tablet twice daily at mealtimes in the morning and evening.
Side Effects
Vastinol is safe and well tolerated. The most commonly encountered side effects are gastric discomfort, nausea, headache and vertigo. However, the side effects are mild and non-specific.
Toxicity
Data regarding overdoses of trimetazidine are not readily available. Treat overdoses with symptomatic and supportive therapy.
The oral LD50 in rats is 1700 mg/kg, and in mice is 1550 mg/kg. The subcutaneous LD50 in rats is 1500 mg/kg, and in mice is 410 mg/kg.
Interaction
No drug interactions have so far been reported. In particular, no interactions of Vastinol with beta-blockers, calcium antagonists, nitrates, heparin, hypolipidemic agents or digitalis have been reported.
Food Interaction
- Take with food. Take during a meal.
- Take with plain water. Take with a glass of water.
Volume of Distribution
The volume of distribution of trimetazidine is 4.8 L/kg.
Elimination Route
In elderly patients, a 35 mg oral modified release tablet reaches a mean Cmax of 115 µg/L, with a Tmax of 2.0-5.0 hours, and a mean AUC0-12 of 1104 h*µg/L. In young, healthy patients, the same dose reaches a mean Cmax of 91.2 µg/L, with a Tmax of 2.0-6.0 hours, and an AUC0-12h 720 h*µg/L.
Half Life
In young, healthy subjects, the half life of trimetazidine is 7.81 hours. In patients over 65, the half life increases to 11.7 hours.
Clearance
Vastinol clearance is strongly correlated with creatinine clearance. In eldery patients with a creatinine clearance of 72 ± 8 mL/min, trimetazidine clearance was 15.69 L/h. In young, healthy patients with a creatinine clearance of 134 ± 18 mL/min, trimetazidine clearance was 25.2 L/h.
Elimination Route
Vastinol is 79-84% eliminated in the urine, with 60% as the unchanged parent compound. In a study of 4 healthy subjects, individual metabolites made up 0.01-1.4% of the dose recovered in urine. In the urine, 2-desmethyltrimetazidine made up 0-1.4% of the recovered dose, 3- and 4-desmethyltrimetazidine made up 0.039-0.071% each, N-methyltrimetazidine made up 0.015-0.11%, trimetazidine ketopiperazine made up 0.011-0.4%, N-formyltrimetazidine made up 0.035-0.42%, N-acetyltrimetazidine made up 0.016-0.19%, desmethyl trimetazidine O-sulphate made up 0.01-0.65%, and an unknown metabolite made up0.026-0.67%.
Pregnancy & Breastfeeding use
Pregnancy: Studies in animals have not demonstrated a teratogenic effect. However, in the absence of clinical data and for safety reasons, prescription should be avoided during pregnancy.
Nursing Mothers: There is no information on the secretion of Vastinol into breast milk. However, breast feeding should be discontinued if the use of Vastinol is considered essential.
Contraindication
Hypersensitivity to Vastinol Dihydrochloride.
Storage Condition
Store in a cool and dry place, protect from light and moisture. Keep out of the reach of children.
Innovators Monograph
You find simplified version here Vastinol
Vastinol contains Trimetazidine see full prescribing information from innovator Vastinol Monograph, Vastinol MSDS, Vastinol FDA label
FAQ
What is Vastinol used for?
Vastinol used to prevent and treat the symptoms of angina (chest pain).
How safe is Vastinol?
Vastinol has been generally very well tolerated in clinical trials and usually only isolated cases of adverse events were observed during Vastinol treatment.
What are the common side effects of Vastinol?
The most common side effects are include nausea, vomiting, fatigue, dizziness, and myalgia. The drug can induce or increase parkinsonian symptoms: extrapyramidal rigidity, bradykinesia, and tremor.
Is Vastinol safe during pregnancy?
The potential risk for humans is unknown.Vastinol should not be taken during pregnancy unless clearly necessary.
Is Vastinol safe during breastfeeding?
This medicinal product is generally not recommended during breastfeeding.Lactation It is unknown whether Vastinol is excreted in human or animal breast milk.
Does Vastinol effect my kidney?
Vastinol is contraindicated in patients with severe renal impairment.
When should I take Vastinol?
The recommended dose of Vastinol is one tablet to be taken two times a day during meals in the morning and evening.For patients with moderate renal impairment and the elderly, the dose should be reduced.
Is Vastinol good for the heart?
Vastinol improves cardiac function by improving hemodynamics.
Can I take Vastinol once a day?
Vastinol is taken twice, or three times, each day. A new altered form of Vastinol, which can be taken once a day, may improve patient-satisfaction.
Does Vastinol lower heart rate?
The dose of Vastinol does not affect hemodynamic stability, heart rate, blood pressure and speed-pressure multiplication, and it exerts no negative inotropic effect.
How long can I take Vastinol?
Vastinol usual treatment for up to 18 months was well tolerated and induced a functional improvement in patients with dilated cardiomyopathy.
Can I stop taking Vastinol?
Vastinol must be taken regularly for it to be effective. Continue taking this medicine even when you feel better. Do not stop taking it unless instructed by the doctor.
What happens if you stop taking Vastinol?
Discontinuing Vastinol treatment in people with Parkinson's disease may lessen their motor and non-motor symptoms and improve their quality of life, a study has found.
What is the benefit of taking Vastinol?
the benefit of taking Vastinol helps to maintain the energy metabolism of heart muscle cells, protecting them from the effects of reduced oxygen supply.
What happen if I miss Vastinol?
If you forget to take a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose. Then take your next dose at the usual time. Do not take two doses to make up for the missed dose.
Does Vastinol lower heart rate?
The dose of Vastinol does not affect hemodynamic stability, heart rate, blood pressure and speed-pressure multiplication, and it exerts no negative inotropic effect.
Can Vastinol cause drowsiness?
Vastinol does not have haemodynamic effects in clinical studies, however cases of dizziness and drowsiness have been observed in post-marketing experienc.
