© On 24th July 2015, the U.S. Food and Drug Administration approved Alirocumab (Praluent) injection to treat high cholesterol.
© Alirocumab is the first PCSK9 (Proprotein Convertase Subtilisin Kexin type9) inhibitor.
© Alirocumab(Praluent) is approved to treat adult patients …
Ø With Heterozygous familial hypercholesterolemia (HeFH)
Ø Who require additional lowering of LDL cholesterol (i.e Whose cholesterol is not controlled by diet and Statin treatment)
© The usual starting dose of Alirocumab is 75 mg/2 weeks.
Mechanism of Action:
© Alirocumab (Praluent) binds to a protein called Proprotein Convertase Subtilisin Kexin type 9 (PCSK9) and inhibits its binding to low density lipoprotein receptors (LDLR) at the surface of hepatocytes. When PCSK9 binds to cell surface LDLR, lysosomal degradation of LDLR occurs. But, inhibition of PCSK9 binding to LDLR by Alirocumab prevents the lysosomal degradation and increases the number of LDLR available to clear LDL particles leading to lowering of LDL cholesterol.
Adverse Drug Reactions:
© The most common ADRs noted in the clinical trial participants being treated with Alirocumab, include Nasopharyngitis, Itching, swelling, pain, or bruising at injection site, Flu like symptoms, Urinary tract infection, Diarrhea, Bronchitis, Myalgia, Muscle spasms, Sinusitis, Cough and Allergic reactions.
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