MUDr. Dana Maňasková

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Repatha

Repatha (evolocumab)

  • Injectable drug from Amgen
  • Second in a new class of drugs called PCSK9 inhibitors
  • Approximate molecular weight (MW) of 144 kDa
  • Produced in genetically engineered mammalian (Chinese hamster ovary) cells.
  • Sterile, preservative-free
  • Clear to opalescent
  • Colorless to pale yellow solution for subcutaneous administration
  • Each 1 mL single-use prefilled syringe and single-use prefilled SureClick® autoinjector contains
    • 140 mg evolocumab, acetate (1.2 mg)
    • Polysorbate 80 (0.1 mg)
    • proline (25 mg) in Water for Injection, USP
    • Sodium hydroxide may be used to adjust to a pH of 5.0 [2]
  • Each single-use Pushtronex® system (on-body infusor with prefilled cartridge)
    • Delivers a 3.5 mL solution containing
      • 420 mg evolocumab, acetate (4.2 mg)
      • Polysorbate 80 (0.35 mg)
      • proline (89 mg) in Water for Injection, USP [2]

Mechanismus účinku

  • Evolocumab is a human monoclonal immunoglobulin G2 (IgG2) directed against human proprotein convertase subtilisin kexin 9 (PCSK9)
  • Evolocumab binds to PCSK9 and inhibits circulating PCSK9
    • From binding to the low-density lipoprotein (LDL) receptor (LDLR)
      • Preventing PCSK9-mediated LDLR degradation
        • Permitting LDLR to recycle back to the liver cell surface [2]
  • By inhibiting the binding of PCSK9 to LDLR
    • Evolocumab increases the number of LDLRs available to clear LDL from the blood
      • Thereby lowering LDL-C levels [2]

Indikace

  • Approved for patients to reduce low-density lipoprotein cholesterol (LDL-C).
    • Heterozygous or homozygous familial hypercholesterolemia
    • HeFh or HoFh
    • Inherited condition that causes high LDL cholesterol levels
  • Approved for patients who have had a heart attack or stroke.
  • Patients who aren't responding to currently available medications or who can't take them because they experience side effects

Primary Hyperlipidemia

  • Including Heterozygous Familial Hypercholesterolemia [2]

Homozygous Familial Hypercholesterolemia - HoFH


Kombinace

  • Diet, alone or in combination with other lipid-lowering therapies
  • Statins
  • Ezetimibe
  • LDL apheresis [2]


Dávkování

  • Can be self-administered through a prefilled auto-injector pen or syringe [1]

Adults with established cardiovascular disease or primary hyperlipidemia - incl. heterozygous familial hypercholesterolemia - HeFH

    • 140 mg every 2 weeks
    • OR 420 mg once monthly
    • Based on patient preference for dosing frequency and injection volume [2]

HoFH

  • 420 mg once monthly
  • Measure LDL-C levels 4 to 8 weeks after starting Repatha
    • Response to therapy will depend on the degree of LDL-receptor function.
      • LDL-C for patients receiving Repatha 420 mg once monthly, LDL-C can vary considerably during the dosing interval in some patients [2]

If a dose is missed

  • Instruct the patient to administer Repatha within 7 days from the missed dose and resume the patient’s original schedule.
  • If an every-2-week dose is not administered within 7 days
    • Instruct the patient to wait until the next dose on the original schedule.
  • If a once-monthly dose is not administered within 7 days
    • Instruct the patient to administer the dose and start a new schedule based on this date [2]

Most common side effects

  • Inflammation in the nasal or throat passages
  • Upper respiratory tract infections
  • Flu and black pain
  • Injection site reactions including
    • Redness, pain and bruising
  • Hives have also been reported
  • Most common adverse reaction that led to Repatha treatment discontinuation and occurred at a rate greater than placebo was myalgia
    • 0.3% versus 0% for Repatha and placebo [2]
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[2]

Imunogenicita

  • In a pool of placebo- and active-controlled clinical trials, 0.3% (48 out of 17,992) of patients treated with at least one dose of Repatha tested positive for the development of binding antibodies.
  • Patients whose sera tested positive for binding antibodies were further evaluated for neutralizing antibodies;
    • None of the patients tested positive for neutralizing antibodies. [2]
  • Allergic reactions: Angioedema
  • Influenza-like illness

Metabolism and Elimination

  • Two elimination phases were observed for Repatha
  • At low concentrations
    • Elimination is predominately through saturable binding to target (PCSK9)
  • Higher concentrations
    • Elimination of Repatha is largely through a non-saturable proteolytic pathway
  • Repatha was estimated to have an effective half-life of 11 to 17 days. [2]
Literatura

[1] cholesterol-drug-repatha/index.html">edition.cnn.com/2015/08/27/health/fda-new-cholesterol-drug-repatha/index.html
[2] www.drugs.com/pro/repatha.html#s-34067-9
O úroveň výše

Poslední aktualizace: 16. 6. 2019 17:25:12
© Dana Maňasková, metabalance.cz
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