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Drugs for Disease. By L. Saarmann, RN, EdD. Antianginal Agents. Antianginal Agents. Therapeutic Objectives Increase blood flow to ischemic heart muscle Decrease myocardial oxygen demand Vasodilation of coronary arteries increases blood flow to heart muscle
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Drugs for Disease By L. Saarmann, RN, EdD
AntianginalAgents Therapeutic Objectives • Increase blood flow to ischemic heart muscle • Decrease myocardial oxygen demand Vasodilation of coronary arteries increases blood flow to heart muscle increases myocardial oxygen supply which decreases myocardial oxygen demand
Antianginal Agents: Nitrates • Cause vasodilation d/t relaxation of smooth muscles • Potent dilating effect on coronary arteries • Used for prophylaxis and treatment of angina
Antianginal Agents: Nitrates Nitroglycerin • Prototypical nitrate • Large first-pass effect with PO forms • Give Sublingual(SL) when they feel angina starting • Can be used prophylacticaly but not in SL form • Used for symptomatic treatment of ischemic heart conditions (angina) • IV form used for BP control in perioperative hypertension, treatment of CHF, ischemic pain, and pulmonary edema associated with acute MI
Antianginal Agents: Nitrates Side Effects • Headache • Usually diminish in intensity & frequency with continued use • Flushing of face • Tachycardia • d/t vasodialated vessels > BP drop > incr. HR • Postural hypotension • Tolerance may develop with patch forms
Interactions • With other Antianginal Agents • with Ca++ channel blockers & beta blockers • d/t additive effect so leads to much lower BP drop • ETOH • Viagra • may fatal hypotension
Nitroglycerin • Nursing • Care of SL pills • Heat is bad for them • Teach how to take Nitroglycerin • Creams & patches • Remove at bedtime to stave off development of intolerance • Take old patch off 1st before putting on new one • Put cream/patch anywhere not hairy • Doesn’t need to be over heart • Orthostatic hypotension care • NTG IV tubing is special
Other Antianginal Agents: Nitrates • isosorbidedinitrate(Isordil, Sorbitrate, Dilatrate SR) • isosorbidemononitrate(Imdur, Monoket, ISMO) Used for: • Acute relief of angina • Prophylaxis in situations that may provoke angina • Long-term prophylaxis of angina • Isosorbide may be given PO • no need to wait for angina to take it ?????. • Isosorbide may be given PO
Antianginal Agents: Beta Blockers • neginotropic (contractility) = weaker contraction • neg. chronotropic (HR) = slows HR • helps to conserve energy or decrease demand Mechanism of Action • Decrease the HR, resulting in decreased myocardial oxygen demand & increased oxygen delivery to the heart • neginotropic (contractility) = weaker contraction • neg. chronotropic (HR) = slows HR • Decreased myocardial contractility • helps to conserve energy or decrease demand • Suppress ang/renin system
Antianginal Agents: Beta Blockers Therapeutic Uses • Antianginalimmediately after MI is best • ELDERLY least likely to be started on B-blockers • Antihypertensive • Cardioprotective effects, especially after MI
Antianginal Agents: Beta Blockers Side Effects Body SystemEffects Cardiovascular bradycardia (negchronotropic), hypotension second- or third-degree heart block (longer time of QRS), heart failure Metabolic Altered glucose and lipid metabolism CNS dizziness, fatigue, mental depression, lethargy, drowsiness, unusual dreams Other impotence, wheezing, dyspnea, Asthma
Antianginal Agents: Beta Blockers • Interactions: • Diuretics • Antihypertensives additive • Phenothiazines • Anticholinergics • Insulin & oral hypoglycemics • Sx of hypoglycemia are obscured by B-blockers
Antianginal Agents: Beta Blockers-lol • atenolol (Tenormin) • metoprolol (Lopressor) • propranolol (Inderal) • Can be too effective on asians • nadolol (Corgard)
Antianginal Agents: Beta Blockers beta II in lungs and beta I in heart • Nursing • Monitor HR (apical pulse) & BP • Safety • Blood sugar • Lung sounds • Taper to stop • Contraindications • COPD, asthma, decompensated HF, arrhythmias • Benefits to heart may outweigh risks to asthma
Antianginal Agents: Calcium Channel Blockers Mechanism of Action • Cause peripheral arterial vasodilation • Reduce myocardial contractility (negative inotropic action) • Depress SA & AV nodes • Result: decreased myocardial oxygen demand • d/t weaker contractions
Calcium Channel Blocker Classes-dipine • Dihydropyridines • Uses: - • Tx HTN & angina • Prevent angina • Drugs • nifedipine [adalat, Procardia] – po • amlodipine [Norvasc] • isradipine [DdynaCirc] – most potent • nicardipine [Cardene] • nisoldipine [Nisocor]
CCBs • Does not cause bronchoconstriction so good for asthma pts • SE: • Flushing, HA, hypotension, peripheral edema • Interactions: • Beta-blockers additive • Digoxin lead to increased serum digoxin in blood • Grapefruit juice makes it longer acting
CCB Classes Nondihydropyridines • Inhibit Ca channels also • Diff is they have an interaction with statins • Different ending -zzzz • Uses: • HTN, angina • Dysrhythmias • Drugs • Diltiazem [Cardizem] • Verapamil [Calan, Isoptin]
CCBs • SE • Flushing, HA, dizziness, peripheral edema • Constipation • Dysrhythmias • Confusion, drowsiness, mood changes • Interactions • Dig lead to increased serum digoxin in blood • Antihypertensives additive • Statins myopathy (breakdown of skeletal muscle) • Grapefruit juice juice makes it longer acting
CCBs • Nursing • Vital Signs • Not for acute angina attacks • Prophylaxis only
Nitratesdecr. myocardial contractility (-inotrope) • Relaxes smooth vasc. muscle=>vasodilation=>incr. myo O2 supply=decr O2 demand • Nitroglycerin • isosorbidedinitrate (Isordil, Sorbitrate, Dilatrate SR) • isosorbidemononitrate (Imdur, Monoket, ISMO) • Vasodilation d/t relaxation of smooth muscles => BP drop > incr. HR • Beta blockers -lol • Decr. HR(- chronotrope) ANDdecr. myocardial contractility (-inotrope) • atenolol (Tenormin) • metoprolol(Lopressor) • propranolol (Inderal) • nadolol (Corgard) • Calcium channel blockers -dipine • periph arteriole vasodilation ANDdecr. myo contractility ANDdecr. HR • weaker contractions=>decr. myocardial oxygen demand • Dihydropyridines • nifedipine[adalat, Procardia] – po • amlodipine[Norvasc] • isradipine [DdynaCirc] – most potent • nicardipine [Cardene] • nisoldipine [Nisocor] • Dihydropyridines • Diltiazem [Cardizem] • Verapamil [Calan, Isoptin] neginotropic (contractility) = weaker contraction neg. chronotropic (HR) = slows HR -lol -dipine neginotropic (contractility) = weaker contraction neg. chronotropic (HR) = slows HR
Antilipemic Classes • Bile acid sequestrants • Form insoluble complexes w/ bile acids in the gut=>can’t be absorbed=> pooped out=>Liver synthesize more bile=>uses up your cholesterol • cholestyramine [Questran] • colestipol [Colestid] • colesevelam [Welchol] • HMG-CoA reductase inhibitors (HMGs or statins) • Inhibit HMG-CoA reductase, used by the liver to produce cholesterol • Fibric acid derivatives • Niacin (nicotinic acid)
Antilipemic Classes • Bile acid sequestrants • HMG-CoA reductase inhibitors (HMGs or statins) • Fibric acid derivatives • Niacin (nicotinic acid)
Antilipemics: Bile Acid Sequestrants Mechanism of Action • Form insoluble complexes w/ bile acids in the gut that can’t be absorbed and is pooped out • This makes the Liver synthesizes more bile acids • Bile acids are made from cholesterol so this uses up your cholesterol
Antilipemics: Bile Acid Sequestrants Therapeutic Uses • Treat hyperlipoproteinemia • Treat hypercholesterolemia • Relief of pruritus (itching) associated with partial biliary obstruction (cholestyramine) • Can be used by kids and pregnant women • Because not absorbed and don’t affect liver
Antilipemics: Bile Acid Sequestrants Side Effects • Constipation • Heartburn, nausea, • Belching, bloating, flatulence These adverse effects tend to disappear over time
Antilipemics: Bile Acid Sequestrants • Interactions • Interferes with absorption of Lipid soluble drugs & vitamins because you are taking the bile acids out of the picture and they are needed to absorb lipid soluble things • Dig & Coumadin Just pass thru you • Drugs • cholestyramine [Questran] • colestipol [Colestid] • colesevelam [Welchol]
Antilipemics: Bile Acid Sequestrants • Nursing • Basline labs to see if chol. is lowered • Mix w/ apple juice or applesauce no one know why • Watch for Vitamin deficiency • Force Fluids • Exercise • If on coumadin, monitor coagulation levels because coumadin will not be as effective • Night blindness, rickets, enlarged liver/spleen, sweating
Antilipemics: HMG-CoA Reductase Inhibitors AKA cholesterol synthesis inhibitors AKA statins Mechanism of Action • Inhibit HMG-CoA reductase, which is used by the liver to produce cholesterol • Lowers the rate of cholesterol production
Antilipemics: HMG-CoA Reductase Inhibitors Therapeutic Uses • Treatment of type IIa and IIbhyperlipidemias • Reduce LDL levels by 30 to 40% • Increase HDL levels by 2 to 15% • Reduce triglycerides by 10 to 30% • Also Primary & secondary prevention of CAD • anti inflammatory by decr. # of macrophages in plaque • Stabilize vessel walls • Possibly immune supressive • Lower BP • Slow development of DM II • May help prevent dementias
Antilipemics: HMG-CoA Reductase Inhibitors • anti inflammatory by decr. # of macrophages in plaque • May reduce incidence of bone fractures in 50 + yo • May reduce macular degeneration
Antilipemics: HMG-CoAReductase Inhibitors (HMGs or statins) • lovastatin (Mevacor) Pro drug • Take on empty stomach • Taking with food increases bioavailability and will give a much greater effect than you want • pravastatin (Pravachol) • atorvastatin (Lipitor) • fluvastatin (Lescol) • Rosuvastatin [Crestor] • simvastatin (Zocor) Pro Drug
Antilipemics: HMG-CoAReductase Inhibitors Side Effects • Mild, transient GI disturbances • Rash • Headache • Rhabdomyolysis • See next slide • Elevations in liver enzymes • (not a good choice for liver disease) • Prolonged QT interval
Antilipemics: HMG-CoAReductase Inhibitors • Interactions: • Interacts with Erythromycin, gemfibrozil, niacin to give you Rhabdomyolysis • Grapefruit juice • Nursing • Red-brown urine is the cardinal sign • Can lead to kidney damage so must flush myoglobin out of kidneys by drinking lots of fluids • Baseline labs • q6weeks • Avoid pregnancy while on statins • wait 6 mos after statins to get pregnant • Teratogenic
Antilipemics: Fibric Acid Derivatives Mechanism of Action • Believed to work by activating lipoprotein lipase, which breaks down cholesterol • May suppress release of FFA from the adipose tissue, inhibit synthesis of triglycerides, and increase the secretion of cholesterol in the bile • Uses • Decrease triglyceride levels
Antilipemics: Fibric Acid Derivatives • gemfibrozil (Lopid) • fenofibrate [Antara, Tricor] • SE: • GI stuff • Inc risk of gallstones • HA, peripheral neuropathy 9tingling /numbness) • Dec. libido • allergy
Antilipemics: Fibric Acid Derivatives • Interactions: • MORE Anticoagulantions • Decreased H&H, WBC • Increased liver enzymes • Nursing • Monitor labs • Monitor INR • Look for GI signs
Antilipemics: Niacin (Nicotinic Acid) Mechanism of Action • Thought to increase activity of lipase, which breaks down lipids • Reduces the metabolism or catabolism of cholesterol and triglycerides
Antilipemics: Niacin (Nicotinic Acid) • Known as Vitamin B3 • Lipid-lowering properties require much higher doses than when used as a vitamin • Effective, inexpensive, often used in combination with other lipid-lowering agents • Simcor = niacin + simvastatin combo drug
Antilipemics: Niacin (Nicotinic Acid) Side Effects • Flushing (due to histamine release) • Aspirin or nsaid decreases flushing • Pruritus • GI distress • Inc. liver enzymes • Hyperglycemia • Hyperuricemia too much uric acid leads to gout
Thrombolytics • Mechanism of Action • Activate conversion of plasminogen to plasmin • Plasmin lyses clots • To do something quickly (w/in 6 hours) before tissue dies
Thrombolytics • Therapeutic Uses • Acute MI • CVA • Deep vein thrombosis • Arterial thrombosis • Pulmonary embolism • Used in small doses to break up Occlusion of shunts and catheters
ThrombolyticsGood for MI too • streptokinase [Streptase] • Produced by streptococci • Some people can have an alergic rxn to this • Can occur way later and last up to a year • Does not work for CVA • alteplase [Activase] • Made with recombinate DNA • Mimics a naturally occuring =ase • works for CVA • Ttenecteplase – TNK-tPA • works for CVA
Thrombolytics • SE • Bleeding breaks up good clots too • Allergy • N/V • Hypotension • Interactions • Anticoagulants • Platelet inhibitors (Aspirin or NSAID)
Thrombolytics • Nursing • Check for bleeding • Tx is blood transfusion • Assess chest pain • May be new clot • Leave sheaths in place • No needle sticks for 24 hrs. • d/t bleeding
Hemostaticsto stop bleeding • AKA antifibrinolytics • Prevent breakup of clots • Can’t give if you JUST gave thrombolytic • Action: prevent dissolution of fibrin • Uses: - • stop bleeding • Aplastic anemia • Hemophilia pre dental • SE: - mild. Nasal stuffiness, anorexia, diarrhea • Drugs • aminocaproic acid [Amicar] • desmopressin [DDAVP] • thrombin topical