BRETYLIUM GUANITHIDINE

Bretylium
Bretylium(alsobretyliumtosylate)isanantiarrhythmic
agent.
Itblocksthereleaseofnoradrenalinefromnerveterminals.
Ineffect,itdecreasesoutputfromtheperipheral
sympatheticnervoussystem.
ItalsoactsbyblockingK+channelsandisconsideredaclass
IIIantiarrhythmic.
Thedoseis510mg/kgandsideeffectsare
highbloodpressurefollowedbylowbloodpressureand
ventricularectopy.

Guanithedine
Guanethidineisanantihypertensivedrugthat
reducesthereleaseofcatecholamines,suchas
norepinephrine.

Guanethidineistransportedacrossthe
sympatheticnervemembranebythesame
mechanismthattransportsnorepinephrineitself
(NET,uptake1),anduptakeisessentialforthe
drug'saction.
Onceguanethidinehasenteredthenerve,itis
concentratedintransmittervesicles,whereit
replacesnorepinephrine.
Itmayalsoinhibitthereleaseofgranulesby
decreasingnorepinephrine.

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