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Antianginal Drugs in Eng
Antianginal Drugs in Eng
Non-
Invasive
method
ECG
Stress
Test:
Recordings
Iopramide Invasive
method
(Ultravist )
®
in a. femoralis
X-ray
a. femoralis
Antianginal drugs increase oxygen supply
by improving coronary blood flow or reduce
oxygen demand by decreasing cardiac work.
Glyceryl-
3-nitrate
Isosorbide
dinitrate
Organic nitrates are vasodilators which
relax vascular smooth muscle.
They connect with thiol groups (SH)
and release nitric oxide (NO).
NO combines with thiol groups in
vascular endothelium to form nitrosothiol
(RSNO). Nitrosothiol activates guanylate
cyclase which raises the concentration of
cyclic GMP. This reduces the availability
of intracellular calcium and produces
vasodilation in three main vascular beds.
Endothelium Smooth muscle
Organic
nitrate
(R-ONO2)
Ca2+
(–)
AP
Ca2+
(–)
Receptor
Cell
wall VDCC ROCC
Ca2+
Ca2+
Sarcoplasmatic
reticulum
AP – action potential, NA – noradrenaline
VDCC – voltage-dependent calcium channels
ROCC – receptor operating calcium channels
Calcium antagonists
cause a reduction
in coronary and
peripheral resistance,
lower the blood pressure
and oxygen demand.
Dihydropyridine derivatives
(e.g. amlodipine, felodipine, nifedipine,
nisoldipine) have no negative
chronotropic effect and do not impair
myocardial contractility.
(Tipathy, 2003)
Calcium antagonists Amlodipine
normal frequently dihydropyridine
t1/2 31–47 h, 55–91% p.o. bioavailability
5–10 mg/24 h p.o. (once daily)
Nifedipine (tachycardic dihydropyridine)
– effective in vasospastic angina
Diltiazem (in SR dosage forms)
Verapamil (Isoptin SR® – tabl. 120 mg)
(22% p.o. bioаvailability, first pass effect –
extensive liver metabolism)
ADRs of calcium antagonists
•Arterial dilation: headache, flush, dizziness,
ankle swelling (resistant to treatment with
diuretics but not with ACE inhibitors).
•Bradycardia and AV block (verapamil).
•Verapamil + beta-blockers: potentiate
cardiodepression.
•Tachycardia (nifedipine, nisoldipine).
•Constipation
(verapamil 8%, nifedipine 3%)
•Haemorrhagic gingivitis
(inhibition of collagen synthesis)
4. Metabolic cardioprotective agents
Trimetazidine (Preductal MR®) has prolonged
concentration plateau lasting up to 11 h.
It increases ATP synthesis and decreases acidosis
in ischemic tissues.
Trimetazidine supplies energy for the Na+/K+
transmembrane pump, but can cause parkinsonism.
parkinsonism
Angiotensinogen 5. ACE inhibitors:
Enalapril, Lisinopril
Ramipril, Trandolapril …
Angiotensin I
() Enalapril
ACE
PGs: vasodilation
Angiotensin II
Kinins ACE
AT 1- AT 2- (kininase II)
receptor receptor
6. If-blockers
ANGIOGENESIS
ANGIOGENESIS
(-)
TNF-
Regenerative
medicine
•Smoking
•Lipid status
2/3
Risk factors for CVD
of the