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    Sildanafl

    Pharmacologic Category

    Phosphodiesterase-5 Enzyme Inhibitor

    Mechanism of Action

    Sildenafil enhances the effect of NO by inhibiting phosphodiesterase type 5 (PDE-5) !hich is

    responsible for degradation of c"#P $ inhibition of PDE-5 by sildenafil ca%ses increased le&els of

    c"#P$

    Increased c"#P concentration res%lts &asodilation

    Pharmacodynamics and Pharmacokinetics

    Onset of action' * min%tes D%ration' +-, ho%rs

    bsorption' .apid/ slo!er !ith a high-fat meal

    Distrib%tion' 0dss' 1*5 2

    Protein binding plasma' 34

    #etabolism' epatic &ia 67P8, (ma9or) and 67P+63 (minor ro%te)/ forms N-desmethyl

    metabolite (acti&e)

    :ioa&ailability' ,14 (+54 to 84)

    alf-life elimination' , ho%rs/ the elderly and those !ith se&ere renal impairment ha&e red%ced

    clearance of sildenafil and its acti&e N-desmethyl metabolite

    ;ime to peaeces (?*4)/ %rine (184)

    Use

    Pulmonary arterial hypertension

    Erectile dysfunction:0iagra' ;reatment of erectile dysf%nction (ED)

    Use: Off-Label

    chalasia@Esophageal motility disorders/ Persistent p%lmonary hypertension after recent left

    &entric%lar assist de&ice placement/ Se=%al dysf%nction (antidepressant@antipsychotic-ind%ced)

    Aderse !eactions "ignificant

    :ased %pon normal doses for either indication or ro%te$ (d&erse effects s%ch as fl%shing diarrheamyalgia and &is%al dist%rbances may be increased !ith ad%lt doses A1** mg@+, ho%rs$)

    6ardio&asc%lar' >l%shing (1*4 to 134)

    6entral ner&o%s system' eadache (14 to ,4)

    "astrointestinal' Dyspepsia (84 to 1B4/ dose related)

    Ophthalmic' 0is%al dist%rbance (+4 to 114/ incl%ding &ision color changes bl%rred &ision and

    photophobia/ dose related)

    .espiratory' Epista=is (34 to 184)

    +4 to 1*4'

    6entral ner&o%s system' Insomnia (CB4) dizziness (+4 to ,4) paresthesia (C84)

    Dermatologic' Erythema (4) s

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    epatic' Increased li&er enzymes (+4 to 1*4)

    Ne%rom%sc%lar s

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    high dose sildenafil prod%ced significantly greater impro&ement in P0O+ hemodynamics and f%nctional

    class than placebo$ 2o!-dose therapy sho!ed no benefit$ No serio%s ad&erse effects !ere reported$