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Clinical Pharmacology of Antianginal Drugs

Clinical Pharmacology of Antianginal Drugs. ISCHEMIC HEART DISEASE. There are 35 risk factors for development of IHD – The most important r isk factors for coronary artery disease Smoking Hypertension Hyperlipidaemia Diabetes mellitus

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Clinical Pharmacology of Antianginal Drugs

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

  8. NITRATES

  9. NITRATES Glyceryl trinitrate isosorbiddinitrate isosorbid-5-mononitrate INDICATIONS • Treatment and prevention of angina. • Treatment of acute left ventricular failure.

  10. Nitrates mechanism of action

  11. NITRATES

  12. NitroglycerineUnique transdermal system in a form of plaster

  13. Contraindications for nitroglycerine use

  14. Iso MakRetard 20mgIso Mak Retard 40mg IsomakRetard 60mg(isosorbid dinitrate)

  15. SYDNONIMINS Molsidomine –corvaton -sydnopharm is metabolized in liver forming a substance – SIN-1awhich contains freeNОgroup (doesn’t need previous interaction withSH-groups) • nitrogen oxide stimulates guanilatecyclase that activates synthesis ofcGMP • cGMP causes dilation of vessels 2 mg of molsidomine=0,5 mg of nitroglycerine

  16. Beta-adrenoceptor antagonists

  17. Nebivololbeta-blocker that also causes vasodilation by stimulating the release of nitric oxide

  18. Calcium channel blockers classification

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

  20. Indications

  21. 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.

  22. Usage of calcium channel antagonists Disease Drugs -recommended drug --should be used carefully

  23. Nifedipin(Са2+ions antagonist of dyhydropyrydine series)

  24. NicorandilPotassium channel activator

  25. Adjunctive Antianginal DrugsAcetylsalicylic acid

  26. Adjunctive Antianginal DrugsAntihypertensives • .

  27. AmiodaroneAntiarrhythmic drug acting on atrial and ventricular tissues

  28. Amiodarone • Treatment by mouth • 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 20-120 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).

  29. 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

  30. Cholesterol-lowering drugs

  31. Choose good nutritionReduce blood cholesterolLower high blood pressureBe physically active every dayAim for a healthy weightManage diabetesReduce stressLimit alcoholStop smoking

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