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    Ivabradine

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    pasha
    This document discusses the use of ivabradine for treating angina and heart failure. It summarizes the drug's mechanism of action as blocking the If current in the sinus node, leading to reduced heart rate without effects on contractility. It outlines ivabradine's clinical uses, pharmacokinetics, contraindications and interactions. Key points include ivabradine being effective and safe for patients with conditions like renal dysfunction or hypotension, initiating at 5 mg bid and uptitrating if tolerated.

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    Ivabradine

    Uploaded by

    pasha
    245 views33 pages
    This document discusses the use of ivabradine for treating angina and heart failure. It summarizes the drug's mechanism of action as blocking the If current in the sinus node, leading to reduced heart rate without effects on contractility. It outlines ivabradine's clinical uses, pharmacokinetics, contraindications and interactions. Key points include ivabradine being effective and safe for patients with conditions like renal dysfunction or hypotension, initiating at 5 mg bid and uptitrating if tolerated.

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    ivabradine.ppt

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    This document discusses the use of ivabradine for treating angina and heart failure. It summarizes the drug's mechanism of action as blocking the If current in the sinus node, leading to reduced heart rate without effects on contractility. It outlines ivabradine's clinical uses, pharmacokinetics, contraindications and interactions. Key points include ivabradine being effective and safe for patients with conditions like renal dysfunction or hypotension, initiating at 5 mg bid and uptitrating if tolerated.

    Copyright:

    © All Rights Reserved
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    245 views33 pages

    Ivabradine

    Uploaded by

    pasha
    This document discusses the use of ivabradine for treating angina and heart failure. It summarizes the drug's mechanism of action as blocking the If current in the sinus node, leading to reduced heart rate without effects on contractility. It outlines ivabradine's clinical uses, pharmacokinetics, contraindications and interactions. Key points include ivabradine being effective and safe for patients with conditions like renal dysfunction or hypotension, initiating at 5 mg bid and uptitrating if tolerated.

    Copyright:

    © All Rights Reserved
    Download as PPT, PDF, TXT or read online from Scribd
    Download as ppt, pdf, or txt
    of 33

    Presentation by

    Dr Muhammad Burhan Pasha


    Topics to be covered
     Electrical System of Heart and
    Conduction of cardiac impulse

     Action Potential of SA node

     Ivabradine
    CONDUCTION OF CARDIAC IMPULSE
    SA node Atrial muscles

    Internodal pathways

    AV node

    Common bundle HIS

    Right and left bundle branches

    Purkinje fibers Ventricular muscles


    1

    4
    SA node is the pacemaker of Heart
    IONIC BASIS OF ACTION
    POTENTIAL IN SA NODE
    RMP (-55 to -60mV)

    + + + + + + + + ++ + + + + + + + + + + + + + + + + + + + + +

    - - - - - - - - - - - - - - - - - - - - - - - - - - - - - -- - -- - - - - - - - - - - - - - - - - - - -

    K+
    - - - - - - - - - - - - - - - - - --- - -- -- ---- - - - - - - - - - - - - - - - - - - - - - - - - - - -

    +++++++++++++++++++++++++++++++++++

    Na+ Ca++
     an outward K+ current (iK)

     an inward Na current induced by


    hyperpolarization

     an inward Ca++ current (ICa)


    CHANNELS IN SA NODE MUSCLE FIBRES

    1. SLOW / LEAK Na+ + K CHANNELS

    2. SHORT LASTING VOLTAGE GATED Ca++ CHANNELS


    ( T- TYPE CALCIUM CHANNELS)

    3. LONG LASTING VOLTAGE GATED Ca++ CHANNELS


    ( L- TYPE CALCIUM CHANNELS)

    4. VOLTAGE GATED K+ CHANNELS


    SEQUENCE OF EVENTS

    RAPID &

    RAPID
    LONG Ca++ K+ EFFLUX
    INFLUX

    SLOW

    K+EFFLUX

    SLOW Na+ INFLUX SLOW Ca++ INFLUX


    IVABRADINE
    Mechanism of Action

     Blocks the hyperpolarization-activated cyclic


    nucleotide-gated (HCN) channel responsible for the
    cardiac pacemaker I(f) ‘funny’ current, which
    regulates heart rate

     the cardiac effects most pronounced in the sinoatrial


    (SA) node

     No effect on ventricular repolarization and no effects


    on myocardial contractility
    AnginaPactoris
    Angina Pectoris

    Unique mechanism of action

    If Channel

    Control RR
    Coralan 0.3 µM

    0 mV

    -40 mV

    -70 mV
    Delay of diastolic depolarization
    in the sinus node

    DiFrancesco D, Camm JA. Drugs. 2004;64:1757-1765.


    AnginaPactoris
    Angina Pectoris

    Unique pharmacological properties

     Negative chronotropic effect

     No impact on the inotropism and dromotropism of the hea

     No coronary constriction

     Increases stroke volume

     Preserves cardiac output


    Clinical Uses
     heart failure with reduced ejection
    fraction

     Ivabradine is a second-line drug for


    systolic heart failure and chronic
    stable angina (after BB or when BB
    are contraindicated)
     for the treatment of inappropriate
    sinus tachycardia
    Pharmacokinetics
     Food delays absorption by ~1 hr and
    increases plasma exposure by 20-40% so
    should be taken with meals

     Protein bound: 70%

     Extensively metabolized in the liver by


    CYP3A4-mediated oxidation

     Major metabolite: N-desmethylated


    derivative (S 18982), which is equipotent to
    ivabradine
    Elimination

     Distribution half-life: 2 hr
     Effective half-life: ~6 hr
     Excretion: 4% unchanged in urine;
    excretion of metabolites occurs to a
    similar extent via feces and urine
    The MOST tested antianginal
    agent

    Coralan1-3

    1. Werdan K. et al. Clin Res Cardiol. 2012;101:365-373. 2. Amosova E et al. Cardiovasc Drugs Ther. 2011;25:531-537. 3. Fox
    K et al. Eur Heart J. 2009;30:2337-2345. 4. Wei J et al. Int J Cardiol. 2011;146(1):4-12. 5. Ezekowitz MD, Hossack K, Mehta
    JL, et al. Amlodipine in chronic stable angina: results of a multicenter double-blind crossover trial. Am Heart J. 1995;129:527-
    535. 6. Nissen SE et al. JAMA. 2004;292:2217-2225. 7. Poole-Wilson PA et al. Lancet. 2004;364:849-857. 8. Stone PH et al. J
    Am Coll Cardiol. 2006;48(3):566-575. 9. Chaitman BR et al. JAMA. 2004;291(3):309-316. 10. Morrow DA et al. JAMA.
    Heart Failure

    Effective and safe


    for patients with associated conditions
    RIGHT PATIENT ACEi / ARB β-Blocker MRA Ivabradine
    &
    RIGHT TREATMENT1-2

    Renal dysfunction

    Hypotension

    Asthma/COPD

    Hyperkalemia

    Bradycardia
    1. Maggioni AP et al. Are hospitalized or ambulatory patients with heart failure treated in accordance with ESC
    guidelines? Evidence from ESC Heart Failure Long-Term Registry.
    Eur J Heart Fail. 2013;15(7):1173-1184. 2. Coralan Summary of Product Characteristics (European Medicines Agency -
    Contraindications

     Ac.MI, USA
     Cardiogenic shock, hypotension
     congenital LQT
     HR<70
     Ac. CVA
     PPM dependent AV blocks
     SSS (severe)
     Unstable or acute HF
     A.Fib
     Pregnancy
     Severe renal failure
    Adverse Effects
     Severe bradycardia, hypotension,
    syncope

     Atrial Fibrillation

     Hypertension

     Visual brightness/ visual impairment


    Drug Interactions overview

     Coadministration of verapamil or
    diltiazem increases ivabradine systemic
    exposure and should be avoided

     Concomitant use with negative


    chronotropes (eg, digoxin, amiodarone,
    beta-blockers) may increase the risk of
    bradycardia
    For angina and heart failure patients

    INITIATE UPTITRATE

    *2.5 mg bid for patients over 75 years old

    1. Coralan Summary of Product Characteristics (European Medicines Agency - latest update of December 2013)

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