OBAT-OBAT UNTUK

ANGINA PECTORIS

TJOKORDA ALIT KAMAR ADNYANA

Coronary artery disease (CAD) is the leading cause of
death for men and women in the United States 1 . Acute
Coronary Syndromes (ACS) is a term used for clinical
symptoms consistent with myocardial ischemia. ACS
includes acute myocardial infarction (AMI), which is both
ST elevation myocardial infarction (STEMI) and non-ST
elevation myocardial infarction (NSTEMI), along with
unstable angina (UA). UA/NSTEMI is usually caused by
atherosclerotic disease, which is associated with an
increased risk for cardiac death and myocardial infarction
(MI). The pathological process of UA/NSTEMI is plaque
rupture and thrombosis in the coronary arteries, which
diminish the blood flow to the myocardium causing
myocardial ischemia.
Angina is pain or discomfort, most often in the
chest, that happens when some region of the heart
does not receive enough oxygen from the blood.
It is usually a symptom of coronary artery disease,
which occurs when the vessels that carry blood to
the heart become narrowed and blocked due to
atherosclerosis.
Angina can feel like a squeezing pain, pressure, or
tightness usually in the chest under the
breastbone, but sometimes in the shoulders, arms,
neck, jaw, or back. Angina is most commonly felt
after physical exertion. It is also triggered by stress,
extreme cold or heat, heavy meals, alcohol, and
cigarette smoking.
Risk Factors:
High Cholesterol and Low-Density Lipoprotein (LDL) in t
he blood
Low level of High-Density Lipoprotein (HDL) in the bloo
d
High Blood Pressure
Tobacco Smoke
Diabetes Mellitus
Obesity
Inactive Lifestyle
Age
Family History of Heart Disease
ANGINA PECTORIS
 Nyeri seperti tertekan di daerah substernal
(kadang-kadang di leher, bahu, atau
epigastrium) akibat cardiac ischemia

 Tidak ada keseimbangan antara suplai oksigen

oleh a. coroner dgn keperluan oksigen miokard

 Tipe: atherosclerotic (classic angina),

vasospastic (rest angina), dan unstable angina
(acute coronary syndrome)
STRATEGI TERAPI
 MENINGKATKAN SUPLAI OKSIGEN
(NITRATES, CALCIUM BLOCKERS)

 MENGURANGI KEPERLUAN AKAN OKSIGEN

(CALCIUM BLOCKERS, BETA BLOCKERS)

 MENINGKATKAN EFISIENSI PENGGUNAAN

OKSIGEN (ENERGI DARI FATTY ACIDS 
GLUCOSE) Ranolazine dan Trimetazidine—
partial fatty acid oxidation inhibitor (pFOX
inhibitor)
 Myocardial revascularization – bypass or
angioplasty
NITRATES
• Nitroglycerin (glyceryl trinitrate; s.l. transdermal,
p.o)  glyceryl dinitrate  glyceryl mononitrate
First-pass effect sekitar 90% (p.o)

• Isosorbide dinitrate (s.l., p.o)isosorbide

mononitrate

• Isosorbide mononitrate (p.o.)

• Amyl nitrite (inhaled): volatile and rapidly acting

vasodilator
• Mekanisme kerja: Denitrasi dari nitrate
menghasilkan NO yg akan menstimulir
guanylyl cyclase  ↑ cGMP smooth muscle
relaxation
• Efek pada organ:
– Cardiovascular: peripheral venodilation  ↓cardiac
size & cardiac output; ↓ peripheral resistance &
blood pressure;  ↓ O2 consumption
– Relaksasi otot polos bronchi, g.i., g.u.tract
– Nitroglycerin i.v. (kadang2 utk unstable angina) 
↓ platelet aggregation
• Duration of action:
– Sublingual (10-20 menit), oral (4-6 jam),
sustained release oral (> lama), transdermal (24
jam). Tolerance setelah 8-10 jam
• Toksisitas:
– Tachycardia, orthostatic hypotension, and
throbbing headache
• Interaksi nitrate dg sildenafil  menghambat
PDE 5  prolonged erection
• Nitrite  methemoglobinemia
GTP

Guanylyl cyclase + Nitrate

cGMP Smooth Muscle Erectile tissue

Relaxation Blood vessels

Phosphodiesterase 5 - Sildenafil, verdenafil,

tadalafil

GMP
DRUG DOSE DURATION
OF ACTION
Short Acting :
Nitroglycerin, subling. 10-30’
Isosorbide dinitrate, subling 0.15-1.2 mg 10-60’
Amyl nitrite, inhalant 2.5-5 mg 3-5’
0.18-0.3 mL
Long acting:
Nitroglycerin, oral-sustained-action 6.5-13 mg/ 6-8 6-8 jam
Nitroglycerin, 2% ointment jam 3-6 jam
Nitroglycerin, slow-release, buccal 1-1.5 inch/ 4 jam 3-6 jam
Nitroglycerin, slow-release, transderm 1-2 mg/ 4 jam 8-10 jam
Isosorbide dinitrate, sublingual 10-25 mg/ 24 jam 1.5-2 jam
Isosorbide dinitrate, oral 2.5-10 mg/ 2 jam 4-6 jam
Isosorbide dinitrate, chewable 10-60 mg/ 4-6 jam 2-3 jam
Isosorbide mononitrate 5-10 mg/ 2-4 jam 6-10 jam
20 mg/ 12 jam
CALCIUM CHANNEL-BLOCKING
DRUGS
 Nifedipine, Diltiazem, Verapamil
 Aktif secara oral, T1/2: 3-6 jam
 Nimodipine  u/stroke krn perdarahan
subarachnoid
 Bepridil (mirip verapamil): masa kerja
>lama, toksisitas pd cardiovascular >
 Mekanisme kerja: block voltage-gated
“L-type” calcium channel ↓ muscle
contractility
 Efek: relaksasi pd pembuluh darah
(sedikit pd uterus, bronchi, dan usus);
menurunkan tekanan darah, dan heart
rate & tek. drh sistole
 Penggunaan klinik: profilaksis pada
atherosclerotic dan vasospastic angina
 Toksisitas: konstipasi, pretibial edema,
nausea, flushing, dan dizziness; heart
failure, AV block
DRUG PLASMA USUAL TOXICITY
T ½ (jam) DOSAGE
Nifedipine 4 3-10 ug/kg IV; 20- Hypotension, dizziness,
40 mg/ 8 jam (oral) flushing, nausea, constipation,
dependent edema
Nimodipine 1-2 60 mg/4 jam (oral) Headache, diarrhea

Diltiazem 3-4 75-150 ug/kg IV; Hypotension, dizziness,

30-80 mg/ 6 jam flushing, bradycardia
oral
Verapamil 6 75-150 ug/kg IV; Hypotension, myocardial
80-160 mg/8 jam depression, constipation,
oral dependent edema

Biperidil 24-40 200-400 mg/hari Arrhythmias, dizziness, nausea

oral
 BETA-BLOCKING DRUGS
• Semua beta-blocker efektif utk profilaksis
atherosclerotic angina
• Efek: ↓ heart rate, COP, tek. drh; ↑heart size,
ejection period
• Penggunaan klinik: hanya utk terapi profilaksis thd
angina; baik digabung dg nitrate
• Toksisitas: bradycardia, AV block, CHF; sedasi,
lelah, gangguan pada tidur.
Preparat:

• Atenolol (Tenormin): 25, 50, 100 mg tablet; 5mg/10 mL IV

• Metoprolol (Lopressor): 50, 100 mg tablet; 50, 100, 200 mg extended-

release tablet; 1 mg/mL IV

• Nadolol (Corgard): 20, 40, 80, 120, 160 mg tablet

• Propranolol (Inderal): 10, 20, 40, 60, 80, 90 mg tablet; 60, 80, 120, 160 mg
capsul sustained-release; 1 mg/mL IV
Medications: •Angiotensin Converting Enzyme (ACE)
Inhibitors
•Anticoagulants
•Aspirin
•Beta Blockers
•Bile Acid Sequestrants
•Calcium Channel Blockers
•Ezetimibe
•Fibrates
•Glycoprotein IIb/IIIa Receptor
Inhibitors
•Niacin (Nicotinic Acid)
•Nitrates
•Platelet Inhibitors
•Statins
•Thrombolytics