Ranolazine is a piperazine derivative belonging to the anti-anginal class of drugs. It is mainly used for the management of stable angina pectoris. Chronic angina leads to ongoing chest pain or pressure, which is felt when the heart does not receive enough oxygen. Ranolazine may be prescribed for the treatment of heart-related chest pain either alone or in combination with another medicine. It should be taken orally with or without food and is contraindicated for hepatic cirrhosis patients. Ranolazine is not intended for use in case of an acute attack of angina.
Ranolazine was approved in the US by the FDA in 2006 and is sold under the brand name Ranexa. It is also sold as a generic by the name of Ranolazine ER, Rolazin, Ranx, Corvela, and Caroza among various others. It comes in an extended-release (ER) formulation, meaning long-acting or prolonged release. ‘Prolonged release’ means that ranolazine is released slowly from the tablet, over a few hours. Ranolazine tablets should be taken whole and not broken, chewed, or crushed for administration.
Chemical features:
Molecular formula: C24H33N3O4
Molecular structure:
Chemical Name: N-(2,6-Dimethylphenyl)-4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazineacetamide
CAS number: 95636-55-5
Weight: 427.5 g/mol
Color: White to off-white solid
Uses of ranolazine
Chronic angina is a common cardiovascular condition and affects millions of people worldwide causing significant disability, as well as interferes with daily activities. Ranolazine is a well-tolerated medicine used to treat heart-related chest pain in chronic stable angina patients, offering relief from uncomfortable and debilitating symptoms. The medicine helps to decrease the number of times a patient may experience chest pain. Relieving symptoms of angina also helps patients to increase their ability to exercise and perform strenuous work.
Mechanism of action
Ranolazine's mechanism of action accounting for its anti-ischemic effects is yet to be fully explained. It is believed that it is a selective late-sodium current inhibitor i.e., it works by reducing the flow of the sodium ions into the heart muscle cells. Thus, interfering with the activity of special channels on the cell surface known as ‘sodium-dependent calcium channels’ through which calcium ions normally enter the cells. This process reduces the number of calcium ions entering the cells. Calcium ions cause the heart muscles to contract and by reducing the flow of calcium into the cells, ranolazine is believed to help the heart relax. Subsequently, it improves the blood flow to the heart muscle and relieves the symptoms of angina pectoris
Some clinical studies have also identified ranolazine as a partial fatty acid oxidation inhibitor (pFOX). It shifts cardiac energy metabolism from fatty acid oxidation to glucose oxidation. As the oxidation of glucose requires less oxygen than the oxidation of fatty acids, ranolazine helps maintain myocardial function in times of ischemia.
Overall, it can be said that ranolazine works by a different mechanism than traditional anti-anginal drugs to decrease the diastolic tension during ischemia. Its mechanism of action is distinct from either beta-blockers or calcium channels which act on the oxygen supply-demand balance. Ranolazine may be concomitantly used with β-blockers, ACE inhibitors, angiotensin receptor blockers, calcium channel blockers, nitrates, antiplatelet therapy, and lipid-lowering therapy
Side effects of ranolazine:
Like most medications, ranolazine also shows some side effects, such as
Nausea
Constipation
Headache
Dizziness
However, some side effects can be serious. You should call your doctor immediately if you experience any of the following serious side effects, such as
Pounding, fast, or irregular heartbeat
Difficulty in breathing
Fainting
Ranolazine should be taken in the exact dose as prescribed. In case you miss a dose, you should not take a double dose to make up for the missed dose. You can skip the missed dose and continue with the next planned dose as normal. In case of an overdose, the following symptoms may occur:
Nausea
Vomiting
Dizziness or confusion
Pain, burning, numbness, or tingling sensation in any part of the body
Double vision
Fainting
Uncontrollable shaking (of a part of the body)
Difficulty with speaking
Seeing things, or hearing voices that do not exist
Ranolazine powder manufacturers and purchase
Various manufacturers around the globe follow cGMP guidelines for producing ranolazine. Some key manufacturers from China are:
Zhejiang Huahai Pharmaceutical Co., Ltd.: Huahai Pharmaceutical was founded in 1989 and is headquartered in the Zhejiang province of China. It has more than 40 branches and subsidiaries around the world, including the US, Japan, Germany, Russia, Spain, and India. Its main business covers chemical, biological medicines, pharmaceutical packaging, and trading. Zhejiang Huahai Pharmaceutical is one of the leading global manufacturers of cardiovascular and central nervous system products. As a leading Chinese pharmaceutical manufacturer, the company has also established an international platform to increase global trade for active pharmaceutical ingredients (API).
Zhejiang Haizhou Pharmaceutical Co., Ltd.: Zhejiang Haizhou Pharmaceutical was established in 1997. It focuses on specialized pharmaceuticals and fine chemicals. The company is located in Yanhai Industrial Park in China. Haizhou Pharmaceutical offers a global portfolio of products and services. It includes API, Intermediates, fine chemicals, and Custom manufacturing services. Haizhou Pharmaceuticals is ISO9001/14001 and OHSAS18001 approved. It also complies with the cGMP standard and is approved by SFDA (China FDA), USFDA and EDQM respectively.
You can also purchase ranolazine in bulk from PharmaSources.com. PharmaSources.com is one of the leading and trustworthy vertical e-commerce online pharmaceutical marketplaces. It provides information on quality pharmaceutical products and suppliers for its customers and delivers services to 90,000+ active members. You could find reliable active pharmaceutical ingredients manufacturers, medical equipment manufacturers, and Medical Equipment manufacturers in PharmaSources. The services are provided globally, across 211 countries and regions. PharmaSources.com sells over 1,600,000 products in 30 major pharmaceutical categories across the supply chain.
Ranolazine manufacturing process
Ranolazine dihydrochloride is the same as ranolazine with two additional molecules of HCl.
Ranolazine is manufactured using a three-step synthetic process, further followed by purification, drying, and
milling. The starting materials are:
Piperazine dihydrochloride
2,6-dimethylaniline (2,6-DMA)
Chloroacetyl chloride (CAC)
Guaiacol glicydil ether (GGE)
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