Upload
tanuj-verma
View
227
Download
0
Embed Size (px)
Citation preview
7/24/2019 Sil Dana Fil
1/3
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$)
6ardio&asc%lar' >l%shing (1*4 to 134)
6entral ner&o%s system' eadache (14 to ,4)
"astrointestinal' Dyspepsia (84 to 1B4/ dose related)
Ophthalmic' 0is%al dist%rbance (+4 to 114/ incl%ding &ision color changes bl%rred &ision and
photophobia/ dose related)
.espiratory' Epista=is (34 to 184)
+4 to 1*4'
6entral ner&o%s system' Insomnia (CB4) dizziness (+4 to ,4) paresthesia (C84)
Dermatologic' Erythema (4) s
7/24/2019 Sil Dana Fil
2/3
epatic' Increased li&er enzymes (+4 to 1*4)
Ne%rom%sc%lar s
7/24/2019 Sil Dana Fil
3/3
high dose sildenafil prod%ced significantly greater impro&ement in P0O+ hemodynamics and f%nctional
class than placebo$ 2o!-dose therapy sho!ed no benefit$ No serio%s ad&erse effects !ere reported$