|
Enalapril maleate with the brand name of Epaned is an angiotensin-converting enzyme inhibitor which was recently approved by the USFDA in August 2013, to treat hypertension inadults and children older than one month. It is the first FDA approved oral solution for treatment of pediatric hypertension. Epaned was developed by Silvergate Pharmaceuticals Inc, a company which focuses on development and commercialization of innovative and safe medicines for pediatric use. Hypertension, also called as arterial hypertension is one of the leading causes of cardiovascular diseases, end-stage renal disease, and cerebrovascular accidents.It is a chronic medical condition that occurs due to raise in arterial blood pressure. This makes the heart work harder than normal to circulate blood through the blood vessels. Blood pressure is generally summarized by 2 parameters, systolic and diastolic, which depend on whether the heart muscle is contracting or relaxing between the beats. The normal range of blood pressure is within 100 140mmHg for systolic and 60-90mmHg for diastolic.High blood pressure ranges from 140mm Hg systolic and 90mm Hg diastolic or above. Hypertension is usually classified into two major types, primary hypertension and secondary hypertension.Primary hypertension is the most common type with no underlying medical cause where as secondary hypertension can be causedby other conditions that affect the kidneys, arteries, heartor endocrine system. In children,the severity of hypertension ranges from mild to moderate andis most commonly asymptomatic but may be associated with subtle changes in behaviour or school performance.They also tend to have other medical problems, such as obesity, high levels of lipid in blood and/or diabetes mellitus. Enalapril is a prodrug that is hydrolyzed in the bodytoenalapril maleate.Enalapril, the active pharmaceutical ingredient (API), is a poorly absorbed substance by the body and therefore not suitable to be taken orally. To overcome this, enalapril is reacted with maleic acid to formenalapril maleate salt. Enalapril maleate has good absorbance in the body compared to enalapril. Once enalapril maleate is absorbed into body it dissociates from maleic acid to give the API enalapril. Epaned is available as a combination of powdered enalapril maleate salt (150mg) and 150 mL solvent (alcohol free syrup) in a bottle. When mixed together they give a 1 mg/mL epaned oral solution. The designed formulation enables accurate dosing and has a taste compliance that appeals to children. Adults who have trouble to swallow tablets may also get benefited with this oral formulation. Epaned prevents the conversion of angiotensin I to angiotensin II through competitive inhibition of angiotensin-converting enzyme resulting in decreased plasma angiotensin II concentrations.Angiotensin II is a potent vasoconstrictor (causes the blood vessels to constrict), thus lowlevels of angiotensin II will cause the blood vessels to relax and this results in lowering of blood pressure which in turn increases the supply of blood and oxygen to the hearttherebyreducingthe risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. Many patients will require more than one dosing to achieve normal blood pressure. The recommended initial dose of epaned in adults is 5 mg/kg/day which can be titrated upward to a maximum of 40 mg/kg/day as needed to achieve a normal blood pressure. The dose may be divided and administered twice daily if the antihypertensive effect diminishes at the end of the dosing interval.The recommended initial dose in children older than 1 month is 0.08 mg/kg/daywhich can be titrated upward to 4 mg/kg/day. Dosage should be adjusted according to the blood pressure responses. The side effects of Enalapril maleate include liver, kidney, or heart damage in some patients. Symptoms like a rapid heart rate, fainting, a sensation of pounding in the chest, change in urine color, extreme body swelling, and yellowing of the skin and eyes are also common. Rarely, the drug can cause rhabdomyolysis, where the body starts breaking down muscle tissuethat result in overloading of kidneys with proteins. Severe muscle pain and weakness can be indicators of this dangerous side effect. Pregnant women or people with angioedema or a history of organ damage, especially from ACE inhibitors, should not use enalapril maleate. Epaned is one of the most promising and exciting new option for pediatric hypertension with taste compliance. As the drug is available in oral solution formulation it enables accurate dosing and is found to be effective in reducing the risk of fatal and non-fatal cardiovascular events. Clinnovo is a clinical innovation company. It is pioneer CRO industry in India. Clinnovo offers professional Clinical Research Course, clinical data management course , SAS and imaging training. Clinnovo has been serving different bio-pharma industries across the world with excellence and high quality. For more information contact at +91 9912868928, 040 64635501
Related Articles -
Paediatric Hypertension, oral hypertensive drug, Clinical Research, Clinical Data Management, SAS, Imaging Trials, evolution of enalapril maleate,
|
