phentolamine酚妥拉明prazosinpharma-chapter 9 adrenoceptor antagonists制药章拮抗剂.pdfVIP

❖Defination:bindtoadrenoceptors,but

affinityandnointrinsicactivity

❖Classification

❖1.α-blockers:phenoxybenzamine,

phentolamine酚妥拉明,prazosin,

doxazosin,terazosin.

❖2.β-blockers:acebutolol,atenolol,

labetalol,metoprolol,nadolol,pindolol

心得乐,propranolol心得安,timolol.

❖3.Drugsaffectingneurotransmitter

uptakeorrelease:e,

guanethidine胍乙啶,reserpine利血平.

Section1.

α-Rantagonists

Theblockadeofαreceptorsreducesthe

sympathetictoneofthebloodvessels,

resultingindecreasedperipheralvascular

resistanceandbloodpressure.Thisinduces

areflextachycardiaresultingfromthe

loweredbloodpressure.

Classificationofα-blockers

❖(1)short-termacting:

phentolamine酚妥拉明;tolazoline

苄唑啉(competitiveα-R

antagonists,reversibly);

❖(2)long-termacting:

phentoxybenzamine酚苄明(petitive

α-Rantagonists,irreversibly).

❖(3)Subtypes:α1-Rantagonists

prazosine(哌唑嗪);α2-Rantagonists

yohimbine(.

Adrenalinereversal

Phenoxybenzamine(酚苄明)

❖Pharmacokinetics

❖onlyiv,highliposolubility(enterlipotissue),

releaseandexcreteslowly,3-4d.

❖characteristics

❖

covalentlytobothα-postsynapticandα-

12

presynapticreceptors.

❖(2)Theblockisirreversibleand

petitive;linkcovalently

❖(3)theonlymechanismthebody

hastoetheblockistosynthesize

newadrenoceptors,whichrequires

adayormore.

PharmacologicalActions

❖1.Cardiovasculareffects:By

blockingαreceptors,

phenoxybenzamineprevents

vasoconstrictionofperipheralblood

vesselsbyendogenous

catecholamines.

❖Thedecreasedperipheralresistance

provokesareflextachycardia.Furthermore,

theabilitytoblock