OBAT OBA T ANTA ANTANGNA NGNA
!ama S" Bra#awikal$a% &"%S'"% A$t
Bagian Farmakologi Fakultas Kedokteran Universitas Swadaya Gunung Jati
ANGINA •
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Angina pectoris is the principle symptom of ischemic heart disease The condition is characterized by sudden, severe substernal pain or pressure The primary cause of angina is an imbalance between myocardial oxygen demand and oxygen supplied by coronary vessels •
This imbalance imbalance may be due to: •
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a decrease in myocardial oxygen delivery an increase in myocardial oxygen demand or both ! "TA#$% ANGINA &! 'N"T 'N "TA#$% A#$% ANGINA
ANGINA "TA#$% •
"table angina is also (nown as: • • •
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Typical or classic Typical classic angina Angina of e)ort *physical activity+ Atherosclerotic angina
The underlying pathology is usually atherosclerosis *reduced *reduced oxygen delivery + giving rise to ischemia under conditions where the wor( load on the heart increases *increased * increased oxygen demand++ demand Anginal episodes can be precipitated by exercise, cold, stress, emotion, or eating Therapeutic goals: Increase myocardial blood ow by dilating coronary arteries and arterioles *increase oxygen delivery +, +, decrease cardiac load *preload and afterloaddecrease oxygen demand+, demand +, decrease heart rate *decrease * decrease oxygen demand+, demand +, .alter myocardial metabolism/0
ANGINA 'N"TA#$% •
'nstable angina is also (nown as: • • •
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1reinfarction angina 2rescendo angina *occurs suddenly+ Angina at rest
Associated with a change in the character, fre3uency, and duration of angina in patients with stable angina, and episodes of angina at rest 2aused by recurrent episodes of small platelet clots at the site of a ruptured atherosclerotic pla3ue which can also precipitate local vasospasm 4ay be associated with myocardial infarction Therapeutic rationale: Inhibit platelet aggregation and thrombus formation *increase oxygen delivery +, decrease cardiac load *decrease oxygen demand+, and vasodilate coronary arteries *increase oxygen delivery
Arteri (oronaria
1roses 1embentu(an 1la3ue
5bat ANTIANGINA ut(
mengobati angina pectoris *nyeri 6antung mendada( a(ibat tida( cu(upnya aliran darah (rn adanya sumbatan pd arteri (oroner yg menu6u 6antung+
4acam& Angina: ! "table Angina7(lasi( &! 'nstable Angina7pra infar( 8! 1rinz 4etal7 varian
1enyempitan7 sumbatan a! (oroner vasospasme
$ong acting interval 9; hours
Isosorbid 4ononitrat
Nitrogliserin mengalami frst past eek diberi(an scr sublingual
mg atau 7?= grain stlh mengalami nyeri 6antung, diulang setiap ? mnt sampai 8 dosis
#entu( lain: ointment, patch transdermal dan I@
arma(o(ineti( B farma(odinami( C5NTDAIN
INT%DAC"I
Jipotensi yg 6elas, pe K te(! Intra(ranial, anemia berat, fase I4 a(ut
5bat: efe( adi(tif dg al(ohol, penghambat beta, penghambat (alsium, obat& antihipertensi
NTG: AD4AC5 mnt -$: &=8= mnt Nitrogliserin, isosorbid: 15: 4ula:&=9= mnt Absorbsi "$: F?H 1: & 6am - $: ;& "aluran GI: ?=9=H 6am "alep: 4ula: &=9= mnt "alep B pacth: %%C T%DA1%'TIC $: 8; 6am transdermal NTG: 4e (ebut! 5(sigen 1acth: 4ula: 8=9= mnt diabsorbsi dg lambat 1: & 6am- $: &=>= 6am mio(ard I@ : F=H I@ : 4ula: 8 mnt - $: 4e preload dg dilatasi mnt 4e afterload dg dilatasi 6am %leminasi: hati arteri,shg te(!tahanan 15: 4ula: &=>= mnt 1: 8=>? mnt -$: >9 6am ber D%AC"I LG 4%D'GICAN %%C "A41ING Jipotensi ortostati( smp hipotensi berat, ta(i(ardia, "a(it (epala, pusing, bingung, pucat, lemah, ruam ingin pingsan, mual (ulit
Cunci: 15 : per oral- t7&: wa(tu paruh- 11: pengi(atan pd protein- I@: intravena- 1: w(tu
Menis 22# •
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berasal dari mole(ul (i)ydro$yridine dihydropyridine dan dapat menurun(an resistensi sistemi( vas(uler dan te(anan arteri!
Non (i)ydro$yridine"
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4e(anisme Cer6a •
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me (ontra(tilitas 6antung *efe( inotropi( negatif+ dan beban (er6a 6antung 4e (ebut! 5& mio(ard angina (lasi( 4erela(sasi(an a! (oroner angina 1rintz metal
4e(anisme A(si
%fe( Antagonis Calsium •
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"a(it Cepala Jipotensi *$bh "ring pd nifedipin dan lbh 6arang pd diltiazem+ 1using lushing 1ada Culit Dee(si ta(i(ardia dpt ter6adi a(ibat hipotensi 1erubahan& fungsi hati, gin6al dan enzim hati dlm serum
%)ects of 2alcium 2hannel #loc(ers *adapted from Goodman B Gilman, th ed!+ Compound
@erapamil
Coronary vasodilation
Suppression of cardiac contractility
= = =
Suppression of SA node
Suppression of AV node
Tabel 1enghambat rantai (alsium u7 angina
OBAT
(OSS
*+&AKAAN (AN *+!T&BANGAN
@erapamil *2alan+
<: 15: >=&= mg dlm, t!i!d! I@: ?= mg selama & mnt
'ntu( angina!
Nifedipin *1rocardia+
<: 15: =8= mg, setiap 9; 6am, tida( melebihi ;= mg7hr
'ntu( angina! Te(anan darah harus dipantau dengan (etat, terutama 6i(a (lien mema(ai nitrat atau penghambat beta! 4erupa(an penghambat (alsium yg (uat!
<: 15: 8=9= mg, 3!i!d "D: 9=&= mg, setiap & 6am
'ntu( angina! Dfe( hipotensi tida( seberat pada nifedipin! ungsi gin6al harus dipantau!
Ni(ardipin *2ardene+
<: 15: &= mg, t!i!d!
'ntu( angina! 4emperbai(i curah 6antung
4e(anisme 4nghambat
reseptor #eta me denyut 6antung B (ontra(tilitas mio(ard 't( obat antiangina, antidisritmia, antihipertensi 4acam&nya:
1enghamat beta tida( sele(tif *mOhmbt beta dan beta&+ ex: propanolol*Inderal+, nadolol*2ogard+, pindolol*@i(sen+ 1Ohmbt beta *6antung+ sele(tif mOhmbt beta ex: atenolol *Tenormin+, metoprolol *$opresor+
p!o
diabsorbsi dg bai(- (apsul sustained"release lambat %": pe JD dan T<, bron(ospasme, respons psi(oti(7 ting(ah la(u, impoten *pd pema(aian Inderal+ 1d penghentian pema(aian, dosis hrs diturun(an bertahap selama & mgg ut( mencegah efe( rebound *ree(s ta(i(ardia dan vaso(onstri(si+
