FDA approves first rosuvastin powder for patients with difficulty in swallowing

Written by Dr. Kamal Kant Kohli Kohli Published On 2019-07-18T09:00:45+05:30 | Updated On 18 July 2019 9:00 AM IST

FDA approves first and only rosuvastin powder for patients with difficulty in swallowing.

The Food and Drug Administration (FDA) has approved a new sprinkle formulation of rosuvastatin, an HMG Co-A reductase inhibitor for patients who have difficulty in swallowing.

Ezallor Sprinkle (Rosuvastatin) has been launched in the US which is the first and only Food and Drug Administration

(FDA) approved sprinkle formulation of rosuvastatin extended-release-coated granules designed to facilitate once-daily administration especially for the 30-35% of long term care residents who have difficulty swallowing.

Ezallor Sprinkle™(rosuvastatin) capsules is indicated for three types of lipid disorders in conjunction with diet in adults.

These include hypertriglyceridemia, as an adjunct to diet for the treatment of adult patients with primary dysbetalipoproteinemia (type III hyperlipoproteinemia), and as an adjunct to other lipid-lowering treatments (e.g., LDL apheresis) or as monotherapy if such treatments are unavailable, to reduce LDL-C,

total cholesterol, and ApoB in adult patients with homozygous familial hypercholesterolemia.

Homozygous familial hypercholesterolemia (HoFH) is the most severe form of familial hypercholesterolemia, an autosomal dominant (a pattern of inheritance in which a child inherits one copy of a mutated [changed] gene from one parentvi) disorder that causes severe elevations in total cholesterol and LDL-C.The disorder results in aggressive atherosclerosis (narrowing and blockage of the arteries). If left untreated, HoFH can lead to heart attack and sudden death in childhood and adulthood.

HoFH is a rare disease, estimated to affect up to 1 in 160,000 individuals around the world.

Ezallor Sprinkle is indicated as an adjunct to diet for the treatment of adult patients with Ezallor Sprinkle has not been studied in Fredrickson type I and V dyslipidemias.

“With the introduction of Ezallor Sprinkle, Sun Pharma continues our commitment of providing a portfolio

of alternative formulation products to address the needs of people who have difficulty swallowing, which is

especially prevalent among residents in long-term care facilities,” said Abhay Gandhi, CEO, North America, Sun Pharma. “These patients often encounter more medication errors and challenges with medication administration as compared to long-term care residents who do not have difficulty in swallowing.”

“The risk of medication errors increases when people have difficulty swallowing, due to crushing of medicines that shouldn’t be crushed, or from residual medication left over in crushing devices,” said Dr.Chris Chappel, certified Medical Director, Chappel Senior Care and Chappel Group Research. “This

formulation will help in administering medication for patients with common types of elevated lipid disorders, especially in the geriatric population.”

Ezallor Sprinkle is formulated as extended-release-coated pellets that may be sprinkled over soft food such as applesauce, can be swallowed whole, or administered via a nasogastric tube to facilitate long term, once-daily administration. Ezallor Sprinkle joins Kapspargo Sprinkle™ (metoprolol succinate) extended-release capsules as the second product in the Sun Pharma portfolio designed for individuals in

long-term care.

Ezallor Sprinkle is contraindicated in patients with any known hypersensitivity to rosuvastatin, which may include rash, pruritus, urticaria, and angioedema; patients with active liver disease, which may include unexplained persistent elevations of hepatic transaminase levels, and females who are pregnant or breastfeeding. In the controlled clinical trials database, the most common adverse reactions with

rosuvastatin were headache, myalgia, abdominal pain, asthenia, and nausea..

Ezallor Sprinkle (rosuvastatin) capsules, for oral use, is an HMG Co-A reductase inhibitor (“statin”) indicated as

• An adjunct to diet for the treatment of adult patients with hypertriglyceridemia

• An adjunct to diet for the treatment of adult patients with primary dysbetalipoproteinemia (type III

hyperlipoproteinemia)

• An adjunct to other lipid-lowering treatments (e.g., LDL apheresis), or as monotherapy if such

treatments are unavailable, to reduce LDL-C, total cholesterol, and ApoB in adult patients with homozygous familial hypercholesterolemia.

Ezallor Sprinkle capsules are available in 5-mg, 10-mg, 20-mg, and 40-mg dose strengths. The dose

range is 5 mg to 40 mg once daily; the 40-mg dose is only for patients not reaching their LDL-C goal with a 20-mg dose. The product can be taken with or without food, at any time of day.

Limitations and Use

Ezallor Sprinkle has not been studied in Fredrickson type I and V dyslipidemias. Ezallor Sprinkle is

indicated only for use in patients aged 18 years and older.

IMPORTANT SAFETY INFORMATION

Contraindications

• Patients with a known hypersensitivity to any component of this product. Hypersensitivity reactions

including rash, pruritus, urticaria, and angioedema have been reported with rosuvastatin.

• Patients with active liver disease, which may include unexplained persistent elevations of hepatic

transaminase levels.

• Pregnancy: advise females of reproductive potential to use effective contraception during treatment

with Ezallor Sprinkle.

• Lactation: limited data indicate that rosuvastatin is present in human milk. Because statins have the

potential for serious adverse reactions in nursing infants, women who require Ezallor Sprinkle treatment

should not breastfeed their infants.

Warnings & Precautions

• Skeletal Muscle Effects: Cases of myopathy and rhabdomyolysis with acute renal failure secondary to

myoglobinuria have been reported with HMG-CoA reductase inhibitors, including rosuvastatin. These

risks can occur at any dose level, but are increased at the highest dose (40 mg). Ezallor Sprinkle should

be prescribed with caution in patients with predisposing factors for myopathy (e.g., aged ≥65 years,

inadequately treated hypothyroidism, renal impairment). The risk of myopathy during treatment with Ezallor Sprinkle may be increased with concurrent administration of some other lipid-lowering therapies (fibrates or niacin), gemfibrozil, cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir, or simeprevir.

Ezallor Sprinkle therapy should be discontinued if markedly elevated creatine kinase (CK) levels occur

or myopathy is diagnosed or suspected. There have been rare reports of immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy associated with statin use. All patients should be advised to promptly report unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever, and if muscle signs and symptoms persist after discontinuing Ezallor Sprinkle.

• Liver Enzyme Abnormalities: It is recommended that liver enzyme tests be performed before the

initiation of Ezallor Sprinkle, and if signs or symptoms of liver injury occur. There have been rare postmarketing reports of fatal and non-fatal hepatic failure in patients taking statins, including

rosuvastatin. If serious liver injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs

during treatment with Ezallor Sprinkle, promptly interrupt therapy. If an alternate etiology is not found,do not restart Ezallor Sprinkle. Ezallor Sprinkle should be used with caution in patients who consume substantial quantities of alcohol and/or have a history of chronic liver disease. Active liver disease,

which may include unexplained persistent transaminase elevations, is a contraindication to the use of

Ezallor Sprinkle.

• Concomitant Coumarin Anticoagulants: Caution should be exercised when anticoagulants are

given in conjunction with Ezallor Sprinkle because of its potentiation of the effect of coumarin-type

anticoagulants in prolonging the prothrombin time/international normalized ratio (INR). In patients

taking coumarin anticoagulants and Ezallor Sprinkle concomitantly, INR should be determined before

starting Ezallor Sprinkle and frequently enough during early therapy to ensure that no significant alteration of INR occurs.

• Proteinuria and Hematuria: Dipstick-positive proteinuria and microscopic hematuria were observed

among patients treated with CRESTOR. These findings were more frequent in patients taking rosuvastatin 40 mg, though it was generally transient and was not associated with worsening renal

function. Although the clinical significance of this finding is unknown, dose reduction should be

considered for patients on Ezallor Sprinkle therapy with unexplained persistent proteinuria and/or

hematuria during routine urinalysis testing.

• Endocrine Effects: Increases in HbA1c and fasting serum glucose levels have been reported with statins, including rosuvastatin. Based on clinical trial data with rosuvastatin, in some instances these increasesmay exceed the threshold for the diagnosis of diabetes mellitus.

ADVERSE REACTIONS

In the controlled clinical trials database, the most common adverse reactions were headache, myalgia,

abdominal pain, asthenia, and nausea. There have been rare reports of immune-mediated myopathy associated with statin use. There have been rare postmarketing reports of cognitive impairment (e.g.,

memory loss, forgetfulness, amnesia, memory impairment, and confusion) associated with statin use.

These cognitive issues have been reported for all statins. The reports are generally nonserious, and reversible upon statin discontinuation, with variable times to symptom onset (1 day to years) and symptom resolution (median of 3 weeks).

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Dr. Kamal Kant Kohli Kohli