FDA approves Alirocumab (Praluent) to treat high cholesterol:

More Presentations from Naina Mohamed Pakkir Maideen

©  On 24^th 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.

FDA approves Entresto (A new Heart Failure Drug):

More Presentations from Naina Mohamed Pakkir Maideen

©  On 07^th July 2015, the U.S. Food and Drug Administration approved Entresto tablets for the treatment of heart failure.

©  Entresto is a crystalline complex composed of 2 molecular moieties…

Ø Sacubitril (Neprilysin inhibitor )

Ø Valsartan (Angiotensin Receptor Blocker)     

Mechanism of Action:

©  Sacubitril blocks the degradation of endogenous vasoactive peptides (ANP, BNP, bradykinin, and Adrenomedullin), by inhibiting Neprilysin enzyme.

©  Valsartan decreases vasoconstriction and sodium retention by blocking the binding of Angiotensin II to the AT 1 receptors (Vascular smooth muscle and the adrenal gland).

Adverse Drug Reactions:

©  The most common ADRs noted in the clinical trial participants being treated with Entresto include Hypotension, Hyperkalemia, Cough, Dizziness and Renal Impairment.

Contraindications:

©  Entresto is contraindicated in patients taking Aliskiren and ACEIs and in patients with a history of angioedema related to previous ACE inhibitor or ARB therapy.

Drug Interactions:

©  Entresto may interact significantly with drugs such asACE Inhibitors, Aliskiren, ARB, Potassium-sparing diuretics, NSAIDsandLithium.

Pregnancy:

©  Use of Entresto should be discontinued as soon as possible, if pregnancy is detected.

Lactation:

©  Use of Entresto or Breastfeeding should be discontinued.