Cardiovascular Drug Agents

Cardiovascular Drug Agents
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Contents Cardiac glycosides Antidysrhythmic agents Anti-anginal drugs
Anti-hypertensive drugs Anti-lipemic agents Anti-coagulants Anti-platelets

Cardiac glycosides Cardiac glycosides are drugs that increase the rate at which the heart beats is known as positive inotropic effects. Cardiac glycosides used to solve the problems of congestive heart failure (CHF). In patients with congestive heart failure occurs when the ejection fraction compared with the total amount of blood in the ventricle is decreased.

Continue Cardiac glycosides are one of the oldest and most effective groups of drugs. They were originally obtained from either digitalis purpurea or digitalis lanata plants both commonly referred to as foxglove. The cardiac glycosides have been the mainstay of therapy for CHF for more than 200 years and they continue to be one of the most frequently used positive inotropic agents.

Drugs 1.Digoxin: is the most prescribed drug in this group, it has less side effects. 2. Digitoxin: not frequently used because of it is side effects.

Mechanism of action The primary beneficial effect of digitalis is thought to be an increase in myocardial contractility. By doing this cellular sodium concentration and calcium concentration increases.

Digoxin Digoxin is the most commonly prescribed digitalis glycoside.
It is highly effective agent in the treatment of CHF. May also used clinically to improve myocardial contractility and thus reverse Cardiogenic shock.

Continue Digoxin is contraindicated in patients who have shown in:
Hypersensitivity Tachycardia Digoxin is available in: 50microgram elixir, 50,100, 200 microgram liquid filled capsule, 125, 250, 500 microgram tablet and 100, 200 microgram per mal injection.

Continue Adult dosage is 1-1.5mg/day, 0.125-0.5 mg.
Premature dosage is mg/kg.

Side-effects Anorexia Nausea Vomiting Confusion Colored vision
Headache Fatigue

Toxicity and management overdose
Discontinue the drug. Determine digoxin and electrolyte level. Administer potassium supplements for hypokalemia. Start ECG monitoring. Administer digibind for severe overdose.

Anti-dysrhythmic Agents
A dysrhythmia is any deviation from the normal rhythm of the heart, thus the more accurate term for an irregular heart rhythm is dysrhythmia. There are many conditions in which dysrhythmia can develop: Myocardial infraction Cardiac surgery as a result of coronary disease.

Continue There are numerous drug available to treat dysrhytmias and these are classified based on where and how they affect cardiac cells. The most commonly used system is the Vaughan Williams classification.

Classification of Drugs
Class one Class 1A Disopyramide Procainamide Quinidine

Continue Class 1B Lidocaine Phenytoin Tocainide Mexiletine

Continue Class 1C Propafenone Flecainide Entainide Class Two
Propranaolol Esmolol sotalol

Continue Class three Amiodarone Bretylium Class four Adenosine
Verpamil Diltiazem

Side-Effects Hypersensitivity Nausea Vomiting Diarrhoe Dizziness
Headache Blurred vision

Toxicity management of overdose
The main toxic affects of the anti- dysrhythmics involve: Heart Circulation CNS Speacific antidotes are not available and the management of an overdose involves maintaining adequate circulation and respiration.

Quinidine Quinidine has both direct action on the electrical activity of the heart and indirect (ant cholinergic) effect. It is ant cholinergic results in inhibition of the parasympathetic nervous system.

Continue Significant adverse effects of the agent include
Cardiac asystole Arterial embolism Ventricular ectopic beats Contraindicated Hypersensitivity AV block Abnormal rhyths

Continue Quinidine is available in 324mg quinidine gluconate tablets, 275 mg quinidine polygalacturonate tablets, 300mg quinidine sulfate tablets. Parentrally quinidine gluconate comes as an 80mg/ml injection. Adult dosage is 324 – 648 mg q8h-q12h, IM 600mg followed by 400mg q2h.

Procainamide It is similar to that of Quinidine but it differs from Quinidine in that it is indirect effect (anticholinergic is weaker). Procainamide is useful in the management of atrial and ventricular tachydysrhymias. It is a pregnancy category C drug.

Continue Available 250, 375, 500mg capsules, 500, 750, 1000mg film coated tablets and 100, 500mg/ml injection

Disopyramide Disopyramide is used primarily for the treatment of ventricular dysrhymias. It can produce significant side-effects including: Anticholinergic effects Cardiovascular depression For these reasons it is use is limited, especially in patients with poor left ventricular function.

Continue Significance adverse reactions from it are hypotension and widening of the QRS interval on ECG. It is available orally in mg capsules Adult dosage is 150mg q6h.

Lidocaine (1B) It is one of the most effective drugs for the treatment of ventricular dysrhytmias. It can only administer intravenously because it has extensive first pass effect, that is when taken orally, the liver metabolizes most of it. It is accomplished by blockade of sodium channels.

Continue Lidocaine is the drug of choice for treating the acute ventricular dysrhymias. Available 100mg/ml IM injection, 10, 20, 40, 100, 200mg/ml IV injection.

Propafenone( 1C) Propafenone reduces sodium current in purkinje fibers and to lesser extent in myocardial fibers. Propafenone has a mild beta-blocking effects. It is also believed to have calcium channel blocking effects, which contributes to propafenone mild negative inotropic effects.

Continue It should be used with causion in patients with congestive heart failure, because of it is beta-blocking agents and it is mild inotropic effects. The most frequently reported adverse reaction is dizziness.

Continue Patients may also complain Metallic taste Constipation
Headache Nausea

Continue Propafenone is contraindicated: Bradycardia Hypersensitivity
Bronchial asthma Hypotension Available orally as 150, 300mg, and the adult dosage is 150mg q8h.

Quinidine Case Study ID/CC: A 56 year old male comes to the cardiology unit for evaluation of ringing in his ears (Tinnitus), dizziness, GI distress (nausea, vomiting, diarrhea), and headaches. HPI: He also complains of blurred vision and impaired hearing. The patient had a myocardial infarction one year ago and has been receiving oral Quinidine antiarrhythmic therapy. Labs: CBC: normal, widening QRS.

Continue Treatment: Monitor ECG and vital signs, discontinue the drug, change to different antiarrhythmic drug. Treat cardio toxic effects with sodium lactate.

Continue Discussion: Quinidine, Procainamide, and Disopyramide are class 1A antiarrhythmic that acts by blocking sodium channels, increasing the effective refractory period. They are used for both atrial and ventricular arrhythmias. All these agents have low therapeutic toxic ratios and may produce severe adverse reactions. Cinchonism is commonly produced by drugs that are cinchona derivatives, such as Quinidine and quinine. The effects may occur with only one dose.

Atenalol (Tenormin) class II
It is a cardio-selective beta blocker that means it blocks the beta one adrenergic receptor. Atenalol also activates beta two in the lungs and could therefore exacerbate a pre-existing case of asthma or COPD. It is also useful in the treatment of hypertension and angina pectoris. It is available orally 25, 50, 100mg tablets, 0.5mg/ml IV injection.

Propranolol (class II)
Propranolol is one of the first beta blockers introduced into clinical practice and this occurred in 1967. It was then primarily used in the treatment of dysrhymias. Propranolol is a non-speacific blocker that blocks both beta one and beta two adrenergic receptor in the heart and the lungs.

Continue Propranolol is the oldest of this class of drugs, there are now many indications of It is use: Hypertension Angina pectoris Dysarrythemia

Continue Available as 10, 20, 40, 60, 80, 90 mg tablets, 60, 80, 120, 160 mg capsules, 20, 40, mg/5ml oral solution, 1mg/ml injection.

Amiodarone Amiodarone markedly prolongs the APD (action potential duration) and ERP (effective refractory period). Amiodarone also known to block both the alpha and beta adrenergic receptors. Amiodarone is a very lipophilic, there fore it may cause un wanted effects.

Continue Amiodarone can cause Hypothyrodism Hyperthyrodism
Amoidarone is contraindicated in patients Hypersensitivity Severe bradycardia Second or third degree of heart block.

Continue Amiodarone is available 200mg orally tablets.
Amiodarone is a pregnancy category C agent.

Diltiazem Diltiazem is primarily indicated for the temporary control of a rapid ventricular response in a patient with atrial fibrillation. It is a pregnancy category C drug. It is available both orally and parenterally, 30, 90, 120 mg tablets and 5mg/ml injection.

Verpamil Verpamil inhibits calcium ion influx across the slow calcium channels in cardiac conduction tissue. Usually decreases the heart beat at least 20 percent. Verpamil is also used to treat: Angina pectoris Hypertension

Continue It is available 40, 80, 120mg tablets, and 2.5 mg/ml injection parenterally. It is a pregnancy category C.

Adenosine It is an unclassified antidysarhythmic drug.
It is naturally occuring nucleoside that slows the electrical conduction rate. It is contraindicated in patients with second and third heart block. It is extremely short half life of less than 10 seconds, for this reason it is only administered by IV.

Continue It is available parenterally as a 3mg/ml injection.
It is a pregnancy category C.

Verpamil Case Study ID/CC: A 73 year old widow visits her cardiologist complaining of difficulty moving her bowels for the past week, she also reports facial flushing. HPI: She had been regular until she began taking verapamil for an irregular heart beat one month ago. PE: Mild lower leg edema, constipation. Labs: CBC: normal

Continue Treatment: increase fluids in diet, regular exercise, fruits high bulk foods or laxatives. If persistent, change to another calcium channel blocker.

Continue Discussion: Verapamil is one of the agents that block voltage dependant calcium channels, consequently reducing muscle contractility. Verapamil acts more specifically on myocardial fibers than on arteriolar smooth muscle. It is widely used for as an antihypertensive, as antiarrhythmic, and for the treatment of angina pectoris. Constipation is common side-effect, other side-effect include dizziness, facial flushing and peripheral edema.

Amiodarone Case Study ID/CC: A 45 year old female who works as a preschool teacher complains of fatigue, headache, dizziness, dry cough, shortness of breath and constipation. HPI: She has been receiving Amiodarone for 1 year for treatment for chronic palpitation that arose spontaneously, with tachycardia that reaches 220 beats per minute and increase when she drinks coffee, is under stress or smoking. PE: Bradycardia, well hydrated, conscious, wheezes in both lungs. Labs: prolonged QT interval. Imaging: CXR, pulmonary fibrosis

Continue Treatment Discontinue the drug Continues monitor of ECG
Supportive therapy Sodium bicarbonate

Continue Discussion: Amiodarone is a class 1A and class III anti-arrhythmic drug. Adverse reactions require careful monitoring and include thyroid dysfunction, constipation and pulmonary fibrosis, which may be fatal. It may also produce bradycardia, and heart block in susceptible individuals. Amiodarone has a long half life.

Angina Pectoris Angina pectoris is a pain syndrome due to induction of an adverse oxygen supply/ demand situation in a portion of the myocardium. Two principal forms are recognized: 1. Classical angina (stable): is the most common one and attacks are predictably provoked by exercise, eating. The underlying pathology is severe arteriosclerotic affliction of larger coronary arteries.

Continue 2. variant/prinzmetals/unstable angina: is an uncommon form and attacks occur at rest or during sleep and are unpredictable. They are due to recurrent localized (occasionally diffuse) coronary vasospasm which may be superimposed on arteriosclerotic coronary artery disease.

Anti-anginal Drugs The three main classes of drugs used to treat angina pectoris are: Nitrates Beta-blockers Calcium channel blockers Potassium channel blockers e.g Nicorandil. Others. E.g Dipyradimole, Trimetazidane, Ranolazine and oxyphedrine.

Continue There are three main therapeutic objectives of anti-anginal drug therapy: It must minimize the frequency of attacks and decrease the duration of the anginal pain. Improve the patients functional capacity with as few side-effects Prevent the worst outcome, myocardial infarction.

Nitrates/Nitrites Organic nitrates were introduced into medicine in the 19th century, de-nitrition in the smooth muscle cell releases nitric oxide which is the main physiological vasodilator. Nitrates, in particular nitroglycerin have long been the mainstay of both the prophylaxis and treatment of angina. This class of anti-anginal agents was first discovered by sir Thomas lauder brunton in England who noted that amyl nitrate was just effective as venesection in the management of angina.

Continue Few years later, a chemically related substance glyceryl trinitrate (nitroglycerin) was successfully isolated. They are available in a wide variety of preparations including: Sublingual Bucal Chewable tablets

Continue Oral tablets Capsules Ointments Patches Inhalable sprays
Intravenous solutions

Nitrates can be classified into: Rapid acting agents Amyl nitrate Nitroglycerin 2. Long acting agents Erythrityl tetra nitrate Isosorbide dinitrate Isosorbide mononitrate

Mechanism of Action The nitrates dilate all blood vessels, but they primarily affect the blood vessels of the venous circulation. This venodilation is the result of relaxation of the smooth muscle that surrounds veins. Nitrates also have a potent dilating effect on the coronary arteries. Activation of nitric oxide, stimulates guanosine mono-phosphate, and this results relaxation then vasodilation.

Nitroglycerin Nitroglycerin has traditionally been the most important drug used in the symptomatic treatment of ischemic heart conditions such as angina. it has classified pregnancy category C agent. Nitroglycerin is administered many other routes to pass first pass effect.

Continue Available sublingual 0.3, 0.4, 0.6 mg tablets, 0.4mg/metred dose aerosol, 5mg/ml IV, 2.6mg, 6.5mg tablets, 2.5, 6.5, 9, 13mg capsules, 2% ointment and 0.1, 0.2, 0.3, 0.4 mg patches. Adult dosage is mg q8h-q12h, sublingual mg Prn, transdermal, apply one patch q24h.

Isosorbide Dinitrate Isosorbide is an organic nitrate and therefore a powerful explosive. When Isosorbide dinitrate is metabolized in the liver, it is broken down into two active metabolites. It is used for the acute relief of angina pectoris and for prophylaxis.

Continue It is a pregnancy category C drug agent.
Available orally 40mg capsules, 5, 10, 20, 30, 40mg tablets and 2.5, 5, 10mg sublingual tablets. Adult dose is sublingual mg Prn and 5-30mg q8h-q12h.

Nadolol Nadolol is a non-selective beta-blocker indicated for the prophylactic treatment of angina and hypertension. It is the most hydrophilic of all beta blockers which may be a beneficial characteristic in elderly patients because as we age we lose muscle mass and gain fat.

Continue Water soluble drugs such as nadolol will have more consistent and reliable effect. It is a pregnancy category C agent. It is only available orally as 20, 40, 80, 120, 160mg tablets. Adult dosage is mg/day as a single dose.

Nifedipine Nifedipine is a calcium channel blocker drug.
It is given by sublingually. It is a pregnancy category C agent. Available 10, 20mg capsules, 30, 60, 90mg tablets. Adult dosage is 10mg Tid.

Nitroglycerin Case Study
ID/CC: A 58 year old man comes to see his cardiologist because of an increased need for nitroglycerin patches in order to control his oppressive exercise induced chest pain (Angina). HPI: In the past, taking one tablet five minutes before physical activity controlled his symptoms, now he has to take two tablets.

Continue The patient has continued to smoke two packs of cigarettes each day and is concerned that his cardiac condition is worsening because of his increased need for medication. PE: Obese male, BP: normal Labs: CBC: elevated hematocrit, elevated glucose and hypercholestremia. Imaging: CXR: normal

Continue Treatment: adjust timing of nitrate administration in order to have an 8 hour period free of nitroglycerin. Consider alternating with beta-blockers, calcium channel blocking agents, beta-blockers or other coronary vasodilators.

Discussion Tolerance is manifested as a poor response to a previously effective dose of nitroglycerin. Increasing the dosage does not yield relief of symptoms. The use of other agents, shorter acting nitroglycerin formulations or intervals free of nitroglycerin dosing can be tried in an attempt to regain sensitivity to the nitrate. Tolerance and headaches are the main drawbacks of nitrate use for the treatment of angina. Progression of coronary artery disease must always be considered with increasing nitroglycerin requirements.

Anti-hypertensive Agents
The anti-hypertensive drugs are classified based on their mechanism of action Adrenergic agents Vasodilators Diuretics ACEI Calcium channel blockers

Adrenergic Agents Centrally acting drugs Clonidine Guanabenz
Guanfacine Methyldopa

Continue Peripherally acting drugs Guanadrel Guanethidine Reserpine

Mechanism of action The centrally acting adrenergic agents decrease blood pressure by stimulating the alpha 2 receptors. The peripherally acting adrenergic agents decrease blood pressure by blocking alpha 1 adrenergic receptors.

Side-effets Dry mouth Drowsiness Sedation Constipation Headache
Sleep disorders Nausea Rash

Clonidine Clonidine is primarily used for it is ability to decrease blood pressure. It is also useful in the management of Opiod withdrawal. It has better safety profile than the other centrally acting adrenergics and has the advantage of being available in several dosage forms.

Continue It is a pregnancy category C agent.
Contraindicated in a patients who have shown hypersensitivity. Available 0.1, 0.2, 0.3 mg as patch, 0.1, 0.2, 0.3mg tablets orally. Adult dosage is mg/day divided dose.

Reserpine Reserpine is derived from rauwolfia alkaloids.
Reserpine promote sodium and water resorption and their anti-hypertensive effects my diminish. Reserpine, always it is combined with diuretics. Reserpine classified pregnancy category D.

Continue Contraindicated in patients who have: Mental illness
Peptic ulcer Hypersensitivity Available in 0.1, 0.25mg tablets. Adult dose is mg/day divided or single dose.

Prazosin It is the oldest of the alpha 1 blockers.
It reduces both peripheral vascular resistance and blood pressure by dilating both arterial and venous blood vessels. It is shown beneficial in the treatment of hypertension. It is classified in pregnancy category C. Available 1, 2, 5 mg capsules.

Angiotensin converting enzyme inhibitors (ACEI)
ACEI represent a large group of anti- hypertensive agents. There are currently more than seven agents available for clinical use. ACEI are beneficial in the treatment of CHF, because they prevent sodium and water resorption by inhibiting aldosterone secretion.

Side-Effects Dizziness Mood changes Headache Dry cough

The most pronounced symptom of overdose of ACEI is hypotension. Treatment is symptomatic and supportive: Administering IV fluids Hemodialysis is effective for the removal of Captopril and lisinopril.

Captopril Captopril was the first ACEI to became available in this group. It is given to a hospitalized patients because of it is short half life. Available 12.5, 25, 50, 100mg tablets. Adult dosage is mg 2-3 times aday.

Enalapril Enalapril is the only currently available ACEI that is available in both oral and parentral preparations. Parentral formulation offers the hemo- dynamic benefit of inhibiting ACE activity in an acutely ill patient who cannot tolerate oral medications.

Continue Enalapril differs from Captopril in that it is a prodrug and relies on a functioning liver to be converted to it is active form. Although it is half life is slightly longer that of captopril, it may in some instances still have to be given twice daily. Available 2.5, 5, 10, 20mg tablets and 1.25mg/ml injection.

Hydralazine Hcl It is a pregnancy category C agent.
It is contraindicated in patients with known hypersensitivity. Adult dosage is 10mg Qid 2-4 days followed by 25mg Qid for balance of week.

Minoxidil It is a pregnancy category C agent.
Available topical 2% minoxidil solution used to treat hair loss. Adult dosage is 10-40mg per day or divided dose. It is contraindicated into a hypersensitive patients.

Sodium Nitroprusside It is a pregnancy category C agent.
It is contraindicated with a known hypersensitivity patients. This drug use is limited to the management of the hypertensive emergencies. Peadtric dosage is mg/kg

Diuretics Diuretics are drugs, which increase renal excretion of salt and water: are principally used to remove excessive extracellular fluid from the body. In order to understand the action of diuretics it is important to have some knowledge of the basic processes that take place in the nephron (unit structure of kidney.

Continue Approximately 180 liters of fluid is filtered from the glomerulus into the nephron per day. The normal urine out put is 1-5 liters per day. The remaining is reabsorbed in different areas of nephron.

Continue There are three mechanisms involved in urine formation:
a) Glomerular filtration b) Tubular reabsorption c) Tubular secretion. These processes normally maintain the fluid volume, electrolyte concentration and PH of the body fluids.

Classification of Diuretics
Most of the diuretics used therapeutically act by interfering with sodium reabsorption by the tubules. The major groups are: I. Thiazides and related diuretics: e.g. Hydrochlorothiazide , chlorthalidone, bendrofluazide. II. Loop diuretics. furosemide, ethacrynic acid

Continue III. Potassium sparing diuretics. a. triamterene,
b. amiloride, c. spironolactone. IV. Carbonic anhydrase inhibitors. a. acetazolamide V. Osmotic diuretics. Mannitol glycerol

Loop Diuretics Loop diuretics like furosemide inhibit Na+- K – 2Cl symporter in the ascending limb. Adverse effects: Hypokalemia, nausea, anorexia, vomiting epigastric distress, fatigue weakness muscle cramps, drowsiness, Dizziness, hearing impairment and deafness are usually reversible. Therapeutic uses: acute pulmonary edema, edema of cardiac, hepatic and renal disease. Hypertension, cerebral edema, in drug overdose it can be used to produce forced diuresis to facilitate more rapid elimination of drug.

Potassium Sparing Diuretics
Potassium sparing diuretics mechanism of action: Potassium sparing diuretics (spironolactone, triamterene, amiloride) are mild diuretics causing diuresis by increasing the excretion of sodium, calcium and bicarbonate but decrease the excretion of potassium.

Continue Adverse effects: G.I. disturbances, dry mouth, rashes confusion, orthostatic hypotension, hyperkalaemia, Hyponatraemia . Therapeutic uses: used with conjunction with thiazides or loop diuretics in edema due to, cardiac failure nephrotic syndrome and hepatic disease.

Carbonic anhydrase Inhibitors
IV. Carbonic anhydrase inhibitors: these drugs like acetazolamide inhibit the enzyme carbonic anhydrase in renal tubular cells and lead to increased excretion of bicarbonate, sodium and potassium ions in urine. In eye it results in decrease information of aqueous humor. Therefore these are used in treatment of acute angle glaucoma. Main adverse effects of these agents are drowsiness, hypokalemia, metabolic acidosis and epigastric distress.

Osmotic Diuretics Osmotic diuretics: these drugs like mannitol and glycerine (glycerol) are freely filtered at the glomerulus and are relatively inert pharmacologically and undergo limited reabsorption by renal tubule. These are administered to increase significantly the osmolality of plasma and tubular fluid. Some times they produce nausea, vomiting, electrolyte imbalances. They are used in cerebral edema and management of poisoning.

Anti-lipemic Agents Anti-lipemic agents are drugs used to lower the rate of cholesterol and triglycerides. Anti-lipemic drugs can be classified based on their mechanism of actions: Bile acid sequestrants Statins Gemfibrotic acid

Classification Statins
e.g, lovastatin, simvastatin, pravastatin, atorvastatin and rosuvastatin. 2. Bile acid sequestrants (Resins) e.g, cholestyramine, colestipol. 3. Activate lipoprotein lipase (fibric acid derivatives) e.g, clofibrate, gemfibrozil, bezafibrate and fenofibrate. 4. Inhibit Triglyceride Synthesis. E.g nicotine.

Bile acid sequestrants
Bile acid sequestrants also called bile acid binding resins and ion exchange resins. Cholestyramine and colestipol are prime examples of these group. Both these agents have been used widely for more than 20 years and have been evaluated extensively in well controlled clinical trials. Generally these drugs lower plasma concentration of LDL cholesterol.

Mechanism of action The bile acid resins bind bile and this prevents the resorption of the bile acids from the small intestine. Decrease LDL 15-30% and Triglyceride is not affected (effects).

Side-effects Constipation Heart burn Nausea Belching Bloating

Note It is important to initiate the therapy with low doses and instruct patients to take the drugs with meals to reduce the side-effects.

Because of bile acid sequestrants are not absorbed, an overdose could cause obstruction of the GIT, therefore treatment of an overdose involves restoring gut motility.

Drug-Drug interactions
All drugs should be taken at least 1 hour before or 4-6 hours after the administration of the ion exchange resins. High dose of bile acid sequestrant will decrease the absorption of fat soluble vitamins. E.g vit A, D, E, K.

Cholestyramine It is a prescription only drug.
It is a pregnancy category C agent. It may interfere distribution of the proper amounts of fat soluble vitamins to the fetus or pregnant women taking these agents. It is only available 4-9 gram packets of powder to be taken as an oral suspension.

Lovastatin Lovastatin was the first agent in this drug class to be approved for use and this occurred in 1987. It is indicated primarily for the treatment of type 2A, and 2B hyperlipidemias. Effective in lowering the LDL cholesterol level and to some degree the triglyceride levels. Recommended daily dose is 20-80mg/day PO. It is a pregnancy category X agent.

Effect on lipids Decrease LDL 20-55% and Triglyceride %.

Gemfibrozil Gemfibrozil is a fibric acid derivative that lowers VLDL level. It is highly effective for lowering the plasma triglyceride levels. It is indicated for the treatment of type 4 and 5 hyperlipidemias and in some cases of the type 2B form. Available as 600mg orally tablet It is a pregnancy category B agent

Effects of lipids Decrease LDL 5-20% and Triglyceride %.

Nicotinic Acid Nicotinic acid is also known niacin, very unique lipid lowering agent. Nicotinic acid is a vitamin B3 drug. It is an effective and inexpensive medication. Niacin is often given in combination with other anti-lipemic drugs to enhance the lipid lowering effects. It is a pregnancy category A agent.

Continue Niacin is contraindicated in: Hypersensitivity Peptic ulcer
Hepatic diseases Hemorrhage Lactating women Severe hypotension

Continue Available as an over the counter drug.
Available 25, 50, 100, 250, 500, 750mg tablets. It is commonly given in 2-4 divided doses of g per day.

Effect on lipids Decrease LDL 15-20% AND Triglyceride %.

Introduction Coagulants are substances which promote coagulation, and are indicated in hemorrhagic states. Fresh whole blood or plasma provide all the factors needed for coagulation and are the best therapy for deficiency of any clotting factor; also they act immediately.

Drug profiles Vitamin K. E.g, vit k1 (phytonadione), vit k3 (menadione, acetomenaphtone). Vit k can be water soluble or fat soluble. 1929 dam produced bleeding disorder in chicken by feeding deficient diet. This was later found to be due to decreased concentration of prothrombin in blood. In 1939, alfalfa grass isolated- vit k1, while sardine (sea fish) is isolated-vitk2, and synthetic compounds have been produced by vit k3.

Uses Dietary deficiencies. Prolonged antimicrobial therapy.
Obstructive jaundice Liver disease (viral hepatitis) Newborn Overdose of anticoagulant Prolonged high dose of Salicylates.

Anti-coagulants Drugs that prevent the formation of a clot by inhibiting certain clotting factors are called anti-coagulants. These agents are only given prophylactically because they have no direct effect on a blood clot. There uses vary from preventing clot formation to preventing the extension of preformed clot or a thrombus.

Continue Once a clot forms on the wall of a blood vessel, it may dislodge and travel through the blood stream. If it goes to the brain, it causes stroke. If it goes to the lungs, it causes pulmonary emboli. If it goes to the veins in the lungs, it causes deep vein thrombosis.

Continue Anti-coagulants can prevent all of these from occurring, if used the correct manner. There are both orally and parenterally administered anti-coagulants.

1. Heparin 2. Warfarin 3. Phenindione 4. Hydroxy coumarin

Uses Deep vein thrombosis Myocardial infarction Unstable angina
Rheumatic heart disease. E.g Warfarin is effective in this case. Cerebrovascular disease. Vascular surgery.

Side-effects Nausea Vomiting Bleeding Abdominal cramp
Hypoaldosteronism

Toxicity management Symptoms that may be attributed to toxicity or an overdose of anti-coagulants are: Hematuria Melena (black tarry feces) Mucous membrane bleeding

Continue Steps of toxicity management: Discontinue the drug
If there is blood loss, replacement of packed red cells. Give protamine sulphate (obtained by sperm fish), 1mg of protamine sulphate can reverse the effects of 100 units of heparin.

Anti-platelet These are drugs which interfere with platelet function and are useful in the prophylaxis of thromboembolic disorders. The clinically important antiplatelt drugs are: Aspirin Dipyridamole Ticlopidine Clopidogrel Abciximab

Aspirin It inhibits the enzyme COX 1 & TX-synthase- inactivating them irreversibly. Aspirin induced prolongation of bleeding time lasts for 5-7 days. Maximal inhibition of platelet function occurs at 160mg aspirin per day. It is available 75mg, 80mg, 300mg, 360mg, and 600mg.

Warfarin case study ID/CC: A 32 year old with a prosthetic heart valve complains to his family doctor of black tarry stools. HPI: He had been receiving oral Warfarin to prevent thrombus formation. Two years ago, he had an aortic valve replacement due to destruction of the valve secondary to bacterial endocarditis.

Continue PE: BP is normal, hemorrhage, bleeding gums, generalized bleeding. Labs: hematuria, markedly elevated PT (Prothrombin Time)

Continue Discussion: This patient has generalized bleeding, including GI tract bleeding secondary to Warfarin treatment. Warfarin compounds inhibit epoxide reductase and hepatic production of the vitamin K- dependant clotting factors (2, 7, 9, & 10). Effects of Warfarin last between 5 to 7 days. Warfarin crosses the placenta and is thus contraindicated in pregnant women.

Continue Treatment: If significant bleeding and volume depletion have occurred, consider fresh frozen plasma and transfusions. Vitamin K may be required.

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