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Clinical Pharmacology of Antianginal Drugs

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Presentation on theme: "Clinical Pharmacology of Antianginal Drugs"— Presentation transcript:

1 Clinical Pharmacology of Antianginal Drugs

2 ISCHEMIC HEART DISEASE
There are 35 risk factors for development of IHD The most important risk factors for coronary artery disease Smoking Hypertension Hyperlipidaemia Diabetes mellitus 95 % of patients with IHD are observed to have aterosclerotic changes in coronary arteries

3 Angina pectoris

4 Life-threatning symptoms: chest pain +
sweating, weakness, faintness, numbness or tingling, nausea Pain that does not go away after a few minutes Pain that is of concern in any way

5 Most cases of coronary heart disease are caused by atherosclerosis (hardening of the arteries).
Atherosclerosis is a condition in which a fatty substance/cholesterol builds up inside the blood vessels. These buildups are called plaques, and they can block blood flow through the vessels partially or completely. Multiple risk factors: diabetes, high blood pressure, smoking, high cholesterol, and genetic predisposition may accelerate this build up.

6 Angina Pectoris Symptoms
Angina itself is a symptom (or set of symptoms), not a disease. Any of the following may signal angina: An uncomfortable pressure, fullness, squeezing, or pain in the center of the chest It may also feel like tightness, burning, or a heavy weight. The pain may spread to the shoulders, neck, or arms. It may be located in the upper abdomen, back, or jaw. The pain may be of any intensity from mild to severe.

7

8 ANTIANGINAL (CORONARY ACTIVE) DRUGS
І. Nitrates and sidnonims ІІ. Beta-adrenoblockers ІІІ. Calcium channel blockers ІУ. Activators of potassium channels

9 NITRATES

10 isosorbid-5-mononitrate
NITRATES Glyceryl trinitrate isosorbid dinitrate isosorbid-5-mononitrate INDICATIONS Treatment and prevention of angina. Treatment of acute left ventricular failure.

11 Nitrates mechanism of action

12 NITRATES

13 Nitroglycerine Unique transdermal system in a form of plaster

14 Contraindications for nitroglycerine use

15 Iso Mak Retard 20mg Iso Mak Retard 40mg Isomak Retard 60mg (isosorbid dinitrate)

16 Molsidomine – corvaton - sydnopharm
SYDNONIMINS Molsidomine – corvaton - sydnopharm is metabolized in liver forming a substance – SIN-1a which contains free NО group (doesn’t need previous interaction with SH-groups) nitrogen oxide stimulates guanilatecyclase that activates synthesis of cGMP cGMP causes dilation of vessels 2 mg of molsidomine= 0,5 mg of nitroglycerine

17 Beta-adrenoceptor antagonists

18 Nebivolol beta-blocker that also causes vasodilation by stimulating the release of nitric oxide

19 Calcium channel blockers classification

20 Calcium channel blockers
1. Phenyalkylamines(verapamil) 2. Benzthiazepines(dilthiazem) 3. Derivatives of Dihydropyridine (nifedipine, amlodipine, nimodipine)

21 Indications

22 Common side effects of calcium channel blockers include:
headache, constipation, rash, nausea, flushing, edema (fluid accumulation in tissues), drowsiness, low blood pressure, and dizziness. Sexual dysfunction, overgrowth of gums, and liver dysfunction also have been associated with calcium channel blockers. Verapamil (Covera-HS, Verelan PM, Calan) and diltiazem (Cardizem LA, Tiazac) worsen heart failure because they reduce the ability of the heart to contract and pump blood.

23 Usage of calcium channel antagonists
Disease Drugs Hypertension Verapamil Dylthiazem Nifedipin Felodipin Amlodipin Stenocardia Verapamil Dylthiazem Nifedipin Amlodipin Supraventricular tachy-arrhythmia Verapamil Dylthiazem Possible combination with β-blockers Dylthiazem Nifedipin Felodipin Amlodipin -recommended drug --should be used carefully

24 Nifedipin (Са2+ ions antagonist of dyhydropyrydine series)

25 Nicorandil Potassium channel activator

26 Adjunctive Antianginal Drugs Acetylsalicylic acid

27 Adjunctive Antianginal Drugs Antihypertensives
.

28 Amiodarone Antiarrhythmic drug acting on atrial and ventricular tissues

29 Amiodarone Treatment by mouth Treatment by intravenous infusion
200 mg 3 times daily for 1 week reduced to 200 mg twice daily for a further week. Maintenance dose, usually 200 mg daily or the minimum required to control the arrhythmia. Treatment by intravenous infusion Via a central line, 5 mg/kg over minutes with ECG monitoring; maximum 1.2 g in 24 hours. Emergency treatment during cardiopulmonary resuscitation VF or pulseless VT, 300 mg by intravenous injection over at least 3 minutes (pre-filled syringe).

30 Common types of cholesterol-lowering drugs include:
statins resins nicotinic acid (niacin) gemfibrozil clofibrate Reason for Medication Used to lower LDL ("bad") cholesterol, raise HDL ("good") cholesterol and lower triglyceride levels

31 Cholesterol-lowering drugs

32 Choose good nutrition Reduce blood cholesterol Lower high blood pressure Be physically active every day Aim for a healthy weight Manage diabetes Reduce stress Limit alcohol Stop smoking


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