clinical pharmacology of antianginal drugs. ischemic heart disease there are 35 risk factors for...
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Clinical Pharmacology of Clinical Pharmacology of Antianginal DrugsAntianginal Drugs
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ISCHEMIC HEART DISEASEISCHEMIC 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
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Angina pectoris
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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
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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.
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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.
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ANTIANGINAL (CORONARY ACTIVE) DRUGS
І. Nitrates and sidnonims
ІІ. Beta-adrenoblockers
ІІІ. Calcium channel blockers
ІУ. Activators of potassium channels
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NITRATES
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NITRATES Glyceryl trinitrate
isosorbid dinitrate isosorbid-5-mononitrate
INDICATIONS Treatment and prevention of angina. Treatment of acute left ventricular failure.
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Nitrates mechanism of action
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NITRATES
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NitroglycerineUnique transdermal system in a form of plaster
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Contraindications for nitroglycerine use
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Iso Mak Retard 20mgIso Mak Retard 40mg Isomak Retard 60mg(isosorbid dinitrate)
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SYDNONIMINSSYDNONIMINS
MolsidomineMolsidomine – – corvatoncorvaton - - sydnopharmsydnopharm
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
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Beta-adrenoceptor antagonists
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NebivololNebivololbeta-blocker that also causes vasodilation by stimulating the beta-blocker that also causes vasodilation by stimulating the
release of nitric oxiderelease of nitric oxide
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Calcium channel blockers classification
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Calcium channel blockers1. Phenyalkylamines(verapamil)
2. Benzthiazepines(dilthiazem)
3. Derivatives of Dihydropyridine (nifedipine, amlodipine, nimodipine)
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Indications
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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.
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Hypertension
Verapamil Dylthiazem Nifedipin Felodipin Amlodipin
Stenocardia Dylthiazem
Nifedipin Amlodipin Verapamil
Supraventricular tachy-arrhythmia
Verapamil Dylthiazem
Possible combination with β-blockers
Dylthiazem Nifedipin Amlodipin
-recommended drug --should be used carefully
Usage of calcium channel antagonistsUsage of calcium channel antagonists
Disease Drugs
Felodipin
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Nifedipin (Са2+ ions antagonist of dyhydropyrydine series)
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NicorandilPotassium channel activator
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Adjunctive Antianginal Drugs Acetylsalicylic acid
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Adjunctive Antianginal Drugs Antihypertensives .
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AmiodaroneAntiarrhythmic drug acting on atrial and ventricular tissues
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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).
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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
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Cholesterol-lowering drugs
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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