chapter_024 - antihypertensive

7/24/2019 Chapter_024 - Antihypertensive

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Mosby items and derived items 2005, 2002 by

CHAPTER 2

Anti!y"ertensive A#ents

$%E& 2' A ( P!armaco)o#y I

E)i*a Rivera+Mit, R$, M-$


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)ood "ressre / C -R

C / cardiac ot"t

-R / systemic vasc)ar resistance


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Hy"ertension / !i#! b)ood "ressre


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Seventh Report of the JointNational Committee on

Prevention, Detection,

Evaluation, and Treatment ofHigh Blood Pressure 4$C+67

May 2003


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$C+6

8or sta#es, based on P measrements

$orma)

Pre!y"ertension

-ta#e 1 !y"ertension

-ta#e 2 !y"ertension


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Tab)e 2+1 C)assi9ication and Mana#ement o9 )ood Pressre


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C)assi9ication o9 P

Hy"ertension can a)so be de9ined by its

case

:n;no o9 t!e cases


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8i#re 2+1 $orma) re#)ation o9 b)ood "ressre and corres"ondin#

mec!anisms.


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Com"e))in# Indications

Post+MI Hi#! cardiovasc)ar ris;

Heart 9ai)re %iabetes me))its C!ronic ;idney disease

Cerebrovasc)ar disease


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$C+6 -i#ni9icant C!an#es

Hi#! diasto)ic P 4%P7 is no )on#er

considered to be more dan#eros t!an

!i#! systo)ic P 4-P7 -tdies !ave s!o


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4contBd7 8or t!ose o)der t!an a#e 50, -P is a

more im"ortant ris; 9actor 9or

cardiovasc)ar disease 4C%7 t!an%P

Pre!y"ertensiveD Ps are no )on#er

considered !i#! norma)D and reire)i9esty)e modi9ications to "revent C%


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4contBd7 T!ia*ide+ty"e diretics s!o)d be t!e

initia) dr# t!era"y 9or most "atients


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C)tra) Considerations

eta+b)oc;ers and ACE in!ibitors !ave

been 9ond to be more e99ective in

Cacasian "atients t!an A9ricanAmerican "atients

CCs 4Ca)cim C!anne) )oc;ers7 and

diretics !ave been s!o


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Anti!y"ertensive A#ents + Medications

sed to treat !y"ertension

Cate#ories Adrener#ic a#ents

An#iotensin convertin# en*yme 4ACE7in!ibitors

An#iotensin II rece"tor b)oc;ers 4ARs7

Ca)cim c!anne) b)oc;ers 4CCs7 %iretics

asodi)ators


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Adrener#ic A#ents

( Centra))y and "eri"!era))y actin#

adrener#ic neron b)oc;ers

( Centra))y actin# a)"!a2+rece"tor a#onists( Peri"!era))y actin# a)"!a1+rece"tor

a#onists


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Adrener#ic A#ents 4contBd7

( Peri"!era))y actin# beta+rece"tor b)oc;ers

4beta+b)oc;ers7Fbot! cardiose)ective

4beta1+rece"tors7 and nonse)ective 4bot!beta1+ and beta2+ rece"tors7

( Peri"!era))y actin# da) a)"!a1+ and beta+

rece"tor b)oc;ers


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Adrener#ic A#ents

Mec!anism o9 Action Centra))y and "eri"!era))y actin#

adrener#ic neron b)oc;er

( %e")etes nore"ine"!rine stores innerotransmitter stora#e vesic)es

( -$- is not stim)ated 4beta+rece"tors in

t!e !eart and a)"!a1+rece"tors in b)oodvesse)s7

Res)t decreased b)ood "ressre


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Centra))y and Peri"!era))y Actin#

$eron )oc;er Reser"ine

( T!e on)y centra))y and "eri"!era))y actin#

neron b)oc;er sti)) avai)ab)e in t!e :nited-tates


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Adrener#ic A#ents

Mec!anism o9 Action Centra))y actin# a)"!a2+rece"tor a#onists

( -tim)ate a)"!a2+adrener#ic rece"tors in

t!e brain( -ym"at!etic ot9)o< 9rom t!e C$- is

decreased

( $ore"ine"!rine "rodction is decreased Res)t decreased b)ood "ressre


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Adrener#ic A#ents Centrally

Actin# A)"!a2+Rece"tor A#onists c)onidine 4Cata"res7

#an9acine 4TeneG7

met!y)do"a 4A)domet7

( %r# o9 c!oice 9or !y"ertension in

"re#nancy


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Adrener#ic A#ents

Mec!anism o9 ActionPeri"!era))y actin# a)"!a1+rece"tor

anta#onists

)oc; t!e a)"!a1+adrener#ic rece"tors

T!e -$- is notstim)ated

Res)t decreasedb)ood "ressre


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Adrener#ic A#ents

Mec!anism o9 Action 4contBd7 -tim)ation o9 a)"!a1+adrener#ic

rece"tors cases hpertension

)oc;in# a)"!a1+adrener#ic rece"tors

cases decreased b)ood "ressre


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Adrener#ic A#ents Peripherally

Actin# A)"!a1+Rece"tor A#onists doGa*osin 4Cardra7

"ra*osin 4Mini"ress7

tera*osin 4Hytrin7


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Adrener#ic A#ents

Indications

Adrener#ic nerona) b)oc;ers 4centra))y and

"eri"!era))y actin# neron b)oc;er7( Treatment o9 !y"ertension, eit!er a)one or


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Adrener#ic A#ents

Indications 4contBd7

Centra))y actin# a)"!a2+rece"tor a#onists

( Treatment o9 !y"ertension, eit!er a)one or


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Adrener#ic A#ents


Centra))y actin# a)"!a2+rece"tor a#onists

(A)so may be sed 9or treatment o9 severedysmenorr!ea, meno"asa) 9)s!in#,

#)acoma

( Clonidineis se9) in t!e mana#ement o9


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Peri"!era))y actin# a)"!a1+rece"tor a#onists

( Treatment o9 !y"ertension

( Re)ie9 o9 sym"toms o9 PH

( Mana#ement o9 o9 severe H8


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Adrener#ic A#ents

-ide E99ects

Most common %ry mot! %ro


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Adrener#ic A#ents

eta+b)oc;ers

(Act in t!e "eri"!ery

( Redce !eart rate de to beta1+b)oc;ade

( EGam")es "ro"rano)o) 4Indera)7, ateno)o)

4Tenormin7


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%a) a)"!a1+ and beta+rece"tor b)oc;ers

(Act in t!e "eri"!ery at !eart and b)ood

vesse)s( Redce !eart rate 4beta1+rece"tor

b)oc;ade7

( Case vasodi)ation 4a)"!a1+rece"tor

b)oc;ade7( EGam")es )abeta)o) 4$ormodyne7,

carvedi)o) 4Core#7


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An#iotensin Convertin#

En*yme In!ibitors 4ACE in!ibitors, or ACEIs7

ar#e #ro" o9 sa9e and e99ective dr#s

9ten sed as 9irst+)ine a#ents 9or H8

and !y"ertension

May be combined


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ACE In!ibitors

Mec!anism o9 ActionRAA- renin an#iotensin+a)dosterone system

J!en t!e en*yme an#iotensin I is converted

to an#iotensin II, t!e res)t is "otentvasoconstriction and stim)ation o9a)dosterone

Res)t o9 vasoconstriction increased

systemic vasc)ar resistance and increaseda9ter)oad

Res)t increased P


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ACE In!ibitors

Mec!anism o9 Action 4contBd7 A)dosterone stim)ates


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ACE In!ibitors

Mec!anism o9 Action 4contBd7 ACE in!ibitors b)oc; t!e an#iotensin

convertin# en*yme, t!s "reventin# t!e

9ormation o9 an#iotensin II A)so "revent t!e brea;do


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ACE In!ibitors

Indications Hy"ertension

H8 4eit!er a)one or in combination


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ACE In!ibitors 4contBd7

ca"to"ri) 4Ca"oten7( ery s!ort !a)9+)i9e, not a "rodr#

ena)a"ri) 4asotec7(Avai)ab)e in ora) and "arentera) 9orms

)isino"ri) 4Prinivi) and Kestri)7 andina"ri) 4Acc"ri)7

( $e


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ACE In!ibitors

-ide E99ects8ati#e %i**iness

Headac!e Mood c!an#es

Im"aired taste Possib)e !y"er;a)emiaDry, nonproductive cough, which reverses

when therapy is stopped

N!TE 8irst+dose !y"otensive e99ect may occrL


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An#iotensin II Rece"tor )oc;ers

4A II b)oc;ers, or ARs7

$e


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Mec!anism o9 Action A))o< an#iotensin I to be converted to

an#iotensin II, bt b)oc; t!e rece"tors

t!at receive an#iotensin II )oc; vasoconstriction and re)ease o9

a)dosterone


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)osartan 4Co*aar, Hy*aar7

va)sartan 4%iovan7


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An#iotensin II Rece"tor

)oc;ers Indications Hy"ertension

Adnctive a#ents 9or t!e treatment o9

H8

May be sed a)one or to)erate ACE in!ibitors


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An#iotensin II Rece"tor

)oc;ers -ide E99ects :""er res"iratory in9ections

Headac!e

May case occasiona) di**iness,

inabi)ity to s)ee", diarr!ea, dys"nea,

!eartbrn, nasa) con#estion, bac; "ain,

9ati#e Hy"er;a)emia mc! )ess )i;e)y to occr


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Ca)cim C!anne) )oc;ers

Mec!anism o9 Action Case smoot! msc)e re)aGation by

b)oc;in# t!e bindin# o9 ca)cim to its

rece"tors, "reventin# msc)e contraction T!is cases decreased "eri"!era)

smoot! msc)e tone and decreased

systemic vasc)ar resistance Res)t decreased b)ood "ressre


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en*ot!ia*e"ines( di)tia*em 4Cardi*em, %i)acor7

P!eny)a);amines

( vera"ami) 4Ca)an, Iso"tin7

%i!ydro"yridines( am)odi"ine 4$orvasc7, be"ridi) 4ascor7,

nicardi"ine 4Cardene7( ni9edi"ine 4Procardia7, nimodi"ine

4$imoto"7


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4contBd7Indications

An#ina

Hy"ertension

%ysr!yt!mias

Mi#raine !eadac!es

RaynadNs disease


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-ide E99ects Cardiovasc)ar

( Hy"otension, "a)"itations, tac!ycardia

&astrointestina)( Consti"ation, nasea

t!er

( Ras!, 9)s!in#, "eri"!era) edema,dermatitis


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%iretics

%ecrease t!e ")asma and eGtrace)))ar 9)id

vo)mes

Res)ts %ecreased "re)oad%ecreased cardiac ot"t %ecreased tota)

"eri"!era) resistance

vera)) e99ect %ecreased


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asodi)ators

Mec!anism o9 Action %irect)y re)aG arterio)ar smoot! msc)e

Res)t decreased systemic vasc)ar

res"onse, decreased a9ter)oad, andperipheral vasodilation


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Anti!y"ertensive A#ents

asodi)ators dia*oGide 4Hy"erstat7

!ydra)a*ine HC) 4A"reso)ine7

minoGidi) 4oniten, Ro#aine7

sodim nitro"rsside 4$i"ride, $itro"ress7


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asodi)ators Indications

Treatment o9 !y"ertension

May be sed in combination


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asodi)ators -ide E99ects

Hydra)a*ine

( %i**iness, !eadac!e, anGiety, tac!ycardia,

nasea and vomitin#, diarr!ea, anemia,

dys"nea, edema, nasa) con#estion

-odim nitro"rsside

( radycardia, !y"otension, "ossib)e cyanide

toGicity


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$rsin# Im")ications

e9ore be#innin# t!era"y, obtain a

t!oro#! !ea)t! !istory and !ead+to+toe

"!ysica) eGamination Assess 9or contraindications to s"eci9ic

anti!y"ertensive a#ents

Assess 9or conditions t!at reirecatios se o9 t!ese a#ents


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$rsin# Im")ications Edcate "atients abot t!e im"ortance o9 not

missin# a dose and ta;in# t!e medications

eGact)y as "rescribed

Patients s!o)d never dob)e " on doses i9 adose is missedO c!ec;


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$rsin# Im")ications

Instrct "atients t!at t!ese dr#s s!o)dnot be sto""ed abr"t)y becase t!is maycase a rebond !y"ertensive crisis, and

"er!a"s )ead to stro;e ra) 9orms s!o)d be #iven


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$rsin# Im")ications

Remind "atients t!at medication is on)y "art o9

t!era"y. Encora#e "atients to


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$rsin# Im")ications

Instrct "atients to c!an#e "ositions s)o


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$rsin# Im")ications

Men ta;in# t!ese a#ents may not bea


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$rsin# Im")ications

Hot tbs, s!o


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$rsin# Im")ications

Edcate abot )i9esty)e c!an#es t!at

may be needed

( Jei#!t )oss( -tress mana#ement

( -"ervised eGercise


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$rsin# Im")ications

Monitor 9or sideadverse e99ects4di**iness, ort!ostatic !y"otension, 9ati#e7

and 9or toGic e99ects

Monitor 9or t!era"etic e99ects( )ood "ressre s!o)d be maintained at )ess

t!an 10=0 mm H#

( I9 a "atient

chapter_024 - antihypertensive

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