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Home , Local anesthetic

11/23/2015

CARDIOVASCULAR

CARDIOVASCULAR DRUGS

 include that affect the an vessels as well as and antiplatelet agents that prevent clotting  cardiac glycosides  antiarrhythmic agents  antihypertensives  vasodilators  antilipemic agents  inhibitors  thrombolytics  hematopoietic agents

1 11/23/2015

CARDIAC GLYCOSIDES (Digoxin)  occur widely in nature or can be prepared synthetically  act directly on the myocardium to increase the force of myocardial contractions  primary treatment of heart failure in patients with symptoms that persist after optimization of treatment with an ACE inhibitor, a beta- adrenergic blocker and/or a  sometimes used alone / in conjunction with other meds (calcium channel blockers) to slow the ventricular response in patient with atrial fibrillation / flutter

 heart failure – heart fails to adequately pump nutrients and O2 to the body tissues

 body attempts to compensate by retaining salt and fluid – may result in pulmonary and peripheral edema  heart increases in size to compensate for the increased work load  symptoms of heart failure – fatigue, weakness, dyspnea, , increased heart rate, cough and pitting edema

 small % of pts develop atrial fibrillation  complications include ischemic stroke and systemic embolism

2 11/23/2015

 https://media.giphy.com/media/HkwWUJfE9R6fu/giphy.gif

normal sinus rhythm

tachycardia

bradycardia

 in pts with heart failure – cardiac glycosides act by increasing the force of the cardiac contractions without increasing cardiac output

(O2 consumption)  cardiac glycosides also ↓ norepinephrine levels (elevated in heart failure and toxic to the heart)  glycosides produce ↑ heart efficiency - heart beats slower, heart size shrinks and concurrent diuretic therapy ↓ edema

 most commonly used cardiac glycosides – digitalis products  digoxin (Lanoxin) only product marketed for clinical use – can be admin orally and parenterally with an intermediate duration of action

3 11/23/2015

 digoxin – narrow margin between effective therapy and toxicity  careful of heart rate and rhythm monitoring (ECG – electrocardiograms), cardiac function, side effects and serum digoxin levels required to determine therapeutic maintenance dose  check apical pulse before admin of - <60 bpm consult physician  modification of dosage is based on individual requirements and response as determined by general condition, renal fxn, cardiac fxn  dosage adjustments required when changing from tabs or IM therapy to elixir or IV therapy

toxic side effects (common / important in blue) • anorexia, nausea, vomiting (early signs) – abdominal cramping, distention and diarrhea • headache, fatigue, lethargy and muscle weakness • vertigo, restlessness, irritability, tremors and • visual disturbances (blurring, diplopia (double vision) or halos) • cardiac (bradycardia <60 pbm) • electrolyte imbalance – potassium (hyperkalemia / hypokalemia cause arrhythmias) • insomnia, confusion, and mental disorders (↑ older adults)

4 11/23/2015

treatment of toxicity • discontinue drug immediately • monitor electrolytes (hyper/hypokalemia (K+), hypomagnesemia (Mg2+), and hypercalcemia (Ca2+) • atropine for symptomatic bradycardia • DigiFab (digoxin specific Fab fragments) as in life- threatening situations

precautions / contraindications • severe pulmonary disease • hypothyroidism • acute MI, acute myocarditis, severe heart failure • impaired renal fxn; hypokalemia / hypomagesemia • arrhythmias not caused by heart failure • pregnancy / lactation • ↑ doses in older adults

interactions of digoxin may occur with • , cholestryramine, and rifampin (↓ absorption digoxin – admin far apart) • , calcium, (↑ chance arrhythmias) • macrolide / antiarrhythmics (quinidne / verapamil – potentiate digoxin toxicity) • adrenergics (epinephrine, ephedrine, isoproterenol - ↑ risk of arrhythmias)

5 11/23/2015

PATIENT EDUCATION

Patients taking digoxin should be instructed regarding:

• recognition and immediate reporting of side effects • hold (stop taking) if any side effects occur – consult physician • check heart rate (pulse) on regular basis • avoid taking other meds at same time without physician approval • avoid taking OTC meds (antacids / cold remedies) • avoid abrupt withdrawal after prolonged use – dose decreased gradually under physician supervision

ANTIARRHYTHMIC AGENTS

– any change from the normal sequence of the electrical impulses of the heart – too fast (tachycardia), too slow (bradycardia) or erratically (fibrillation)

 antiarrhythmic agents – variety of drugs that act in different ways to suppress various types of cardiac arrhythmias (atrial / ventricular tachicardias, atrial fibrillation / flutter, and arrhythmias that occur with digoxin toxicity, during surgery and

 choice of agent is based on the careful assessment of many factors – type and frequency of arrhythmia; cardiac, renal or other pathologic condition; current signs and symptoms

6 11/23/2015

7 11/23/2015

 the role of the healthcare provider is critical when evaluating cardiac arrhythmias– accurate and timely reporting of vital signs, pertinent observations regarding effectiveness of meds and adverse side effects, modification of precipitating causes  adequate knowledge of drug action and effects, along with good judgment essential

 most drugs given to counteract arrhythmias have potential to lower BP and slow heart beat – look for signs of and bradycardia which can lead to  antiarrhythmic agents can worsen existing arrhythmias or cause new arrhythmias – careful monitoring essential

 arrhythmia detection / monitoring can include ECG rhythm strips and 24h Holter monitoring as indicted  electrolyte monitoring – potassium / magnesium  non-drug therapy can include a pacemaker or automatic implantable cardioverter-defibrillator (AICD – most effective treatment for pts with life-threatening ventricular tachycardia / fibrillation and pts who have survived cardiac arrest)

8 11/23/2015

Adenosine (Adenocard)  injectable with multiple electrophysiological activities – complicate its placement into a single category  restores normal sinus rhythm in paroxysmal supraventricular tachycardia (PSVT - a faster than normal heart rate beginning above the heart's two lower chambers) by slowing the conduction time through the atrioventricular (AV) node  also has vasodilatory, antiadrenergic, and negative chronotropic ( rate) properties –

 act to  cardiac O2 demand

 adenosine is equal in effectiveness to diltiazem / verapamil in converting PSVT but less likely to cause hypotension  common side effects - flushing, lightheadedness, headache, dyspnea, and chest pressure  contraindicated in pts with 2nd / 3rd degree heart block or synptomatic bradycardia (unless functioning artificial pacemaker present)

9 11/23/2015

Amiodarone (Cordarone)  oral and injectable antiarrhythmic – approved for the treatment of refractory life-threatening ventricular arrhythmias  despite problematic organ toxicity profile (black box warning) – widely used for preventing recurrence of atrial fibrillation  considered broad spectrum antiarrhythmic with multiple and complex electrophysiological effects  Amiodarone also relaxes both smooth and cardiac muscle -  coronary and peripheral vascular resistance and systolic BP

side effects ( with lower doses 200-400mg/d) (common / important in blue)

 nausea / vomiting, constipation, anorexia  cardiac arrhythmias, induction / worsening heart failure, hypotension  neurotoxicity (tremor, , parasthesia (numbness / tingling in extremities)  hyper / hypothyroidism  visual disturbances (optic neuropathy /  blindness)  dermatological rxns (photosensitivity)  hepatits (rare)

10 11/23/2015

precautions / contraindications apply to  pts with 2nd / 3rd degree heart block marked with sinus bradycardia (severe sinus node dysfunction) and when bradycardia has caused syncope (loss of consciousness due to BP) – cardiogenic shock  pts with thyroid disease (large amnt of iodine in amiodarone)  iodine hypersensitivity  older adults (susceptible to thyrotoxic and neurotoxic effects)

interactions with amiodarone – numerous and significant  warfarin (can cause serious, fatal if warfarin not reduced – effects may persist for months after d/c)  certain fluoroquinolones, macrolide , systemic azole (QT wave prolongation)  certain antiarrhythmics, digoxin, phenytoin (amiodarone  serum concentrations of drugs)  protease inhibitors and grapefruit juice ( amiodarone conc); beta- blockers, calcium channel blockers, (additive adverse cardiac effects)  cholestyramine, pheytoin, rifampin ( amiodarone conc -  pharmacologic effects

11 11/23/2015

Beta-adrenergic blockers ( / Inderal)  antiarrhythmetics that inhibit adrenergic (sympathetic - excite) nerve receptors  action is complx – results can include membrane stabilization effect on the heart

 Inderal (propranolol) – non-selective beta-blocker – management of some cardiac arrhythmias and treatment of (HTN) and some forms of chronic angina

 Block beta2 receptors in the lungs – can lead to bronchospasms

 Lopressor (metoprolol) – selective beta1-agonist – may be used with caution in pts with lung conditions that cause bronchospasm

note:

 β1 receptors – found primarily in heart – when stimulated cause an ↑ in rate and force of contraction

 Β2 receptors – found primarily in the lungs (when stimulated cause relaxation / bronchodilation of airways) and blood vessels (when stimulated cause )

 selective beta-blockers ↓ rate and force of contraction of the heart  non-selective beta-blockers may also cause bronchospasm and mild of blood vessels

12 11/23/2015

side effects (especially pts >60 / more common with IV admin) (common / important in blue)

• hypotension with vertigo and syncope • bradycardia (rarely heart block / cardiac arrest) • CNS symptoms (long term treatment / high doses) – dizziness, irritability, confusion, nightmares, insomnia, visual disturbances, weakness, sleepiness, lassitude (lack of energy), fatigue • GI symptoms – nausea, vomiting, diarrhea, constipation • rash / hematological effects • bronchospasm (especially hx asthma) • hypoglycemia

precautions / contraindications apply to • withdrawal after prolonged use (should be gradual) • withdrawal before surgery (weigh risks / benefits) • diabetes (may cause hypoglycemia and mask tachycardic response) • renal and hepatic impariment • asthma / allergic rhinitis • bradycardia, heart block, CHF (congestive heart failure) • COPD (chronic obstructive pulmonary disease) • pediatric use / pregnancy and lactation interactions – antagonism of β-blockers • adrenergics (epinephrine and isoproterenol) • NSAID’s and salicylates • tricyclic

13 11/23/2015

potentiation of hypotensive effect of propranolol occurs with • diuretics / antihypertensives (calcium channel blockers) • MAOI’s; phenothiazine / other tranquilizers • Tagamet (cimetidine) – slows of the drug • some antiarrhythmic drugs (adenosine, digoxin, quinidine) – may potentiate toxic effects • , muscle relaxants, – may precipitate hypotension, dizziness, confusion,

Calcium Channel Blockers  Calan (verapamil) / Cardizem (diltiazem) possess significant antiarrhythmic activity  indicated for the treatment of atrial fib / flutter and PSVT  counteract arrhythmias by slowing AV nodal conduction

 calcium channel blockers also used in treatment of angina / hypertension note: grapefruit juice may side effects (common / important in blue) potentiate adverse effects of certain calcium • hypotension with vertigo and headache channel blockers (do not • bradycardia with heart block take) • edema • constipation, nausea, abdominal discomfort

14 11/23/2015

precautions / contraindications apply to • heart block, heart failure, angina • hepatic and renal failure • hypotension • certain arrhythmias and severe heart failure • pregnancy and children interactions of Ca-channel blockers with other cardiac drugs (digoxin) can potentiate good and adverse effects antagonistic effects include • barbiturates, cimetidine, phenytoin, ranitidine, rifampin • hypotensive effect potentiated with diuretics, ACE inhibitors, β- blockers and quinidine

Lidocaine  local are administered for antiarrhythmic effects and membrane stabilizing action  lidocaine – second-line antiarrhythmic agent for acute, life- threatening ventricular arrhythmias side effects (short in duration, dose related) (common / important in blue) • CNS symptoms – tremors, seizures, dizziness, confusion and blurred vision • hypotension, bradycardia, heart block • dyspnea, respiratory depression and arrest • ECG monitoring and resuscitative equipment necessary during IV admin of lidocaine

15 11/23/2015

precautions / contraindications with lidocaine • pts hypersensitive to local (amide type) • heart block and respiratory depression • pregnancy, lactation, children interactions of lidocaine with other cardiac drugs – additive or antagonistic and may potentiate adverse effects • lidocaine usually titrated to achieve clinical response (minimal interactions)

Procainamide  procainamide, quinidine, disopryamide (Norpace) (antiarrhythmic)  act by ↓ myocardial excitability, inhibiting conduction, and may depress myocardial contractility  possess anticholinergic properties  used orally – prophylactic therapy to maintain normal rhythm after conversion by other methods

 IV procainamide – potential treatment alternative (to amiodarone) for treatment of ventricular tachycardia during CPR

16 11/23/2015

side effects (numerous and may necessitate cessation of treatment) (common / important in blue)

• diarrhea, anorexia, nausea / vomiting and abdominal (common) • tachycardia, QT prolongation, hypotension, syncope • anticholinergic effects – dry mouth, blurred vision, confusion, constipation, urinary retention • vascular collapse and with IV admin • dermatological effects – rash, pruritus, uritcaria

• vision abnormalities / hearing disturbances (quinidine) • blood dyscrasias – anemia, clotting deficiencies, leukopenia (relatively rare) • hepatic disorders

precautions / contraindications apply to • AV block and conduction defects • electrolyte imbalance • digoxin toxicity • heart failure and hypotension • hepatic and renal disorders • pregnancy, lactation, children

• hypersensitivity to “ester-type” local anesthetics (procainamide) • systemic lupus erythematosus – SLE (procainamide)

17 11/23/2015

interactions with ↑ possibility of toxicity may occur with • muscle relaxants and neuromuscular blockers • anticholinergics, tricyclic , phenothiazines • other cardiac drugs (digoxin / antihypertensives) interactions with ↑ possibility of quinidine toxicity may occur with • antiretroviral protease inhibitors • antacids / bicarbonate • (phenytoin and phenobarbital – cause ↓ serum levels) • anticoagulants (action can be potentiated by quinidine)

Propafenone (Rythmol)  oral antiarrhythmic used to treat symptomatic supraventricular arrhythmias or severe, life-threatening ventricular arrhythmias  useful in converting artrial fibrillation to sinus rhythm / maintaining it  has effects, direct stabilizing actin on myocardial membranes and β-adrenergic blocking properties side effects • dizziness / blurred vision • nausea, vomiting, unusual taste, constipation • angina, heart failure, palpitations, arrhythmia, dyspnea • fatigue, weakness, headache • rash

18 11/23/2015

precautions / contraindications • asthma / acute bronchospam • 2nd / 3rd degree heart block (in absence of pacemaker), cardiogenic shock, heart failure and bradycardia • marked hypotension and electrolyte imbalance interactions of propafenone may occur with • quinidine, ritonavir, certain SSRI’s (may ↑ serum levels of propafenone) • β-blockers, digoxin and theophylline (may ↑ serum levels)

PATIENT EDUCATION

Patients taking antiarrhythmics should be instructed regarding:

• immediate reporting of adverse side effects (palpitations, irregular or slow heart beat, faintness, dizziness, weakness, respiratory distress and visual disturbances) • hold medication if side effects – consult with physician • rise slowly from a reclined position

19 11/23/2015

ANTIHYPERTENSIVES  hypertension – widespread epidemic – 1 billion people world wide / 65 million adults in US  hypertension (HTN) – systolic BP >140 or diastolic BP >90  strong correlation b/t BP and the risk of cardiovascular disease (CVD)  high BP ↑ risk of angina, MI, heart failure, stroke, retinopathy, peripheral arterial disease, kidney disease – requires aggressive treatment

 37% adults in US are considered to have prehypertension (SBP 120-139 / DBP 80-89) - at higher cardiovascular risk  want to encourage pts to initiate healthy life style (weight reduction, healthy eating plan, dietary Na reduction, ↑ physical activity, modified alcohol use, smoking cessation) vs starting therapy

 antihypertensives do not cure hypertension – only control it  after withdrawal of drug, BP will return to levels similar to those before treatment with meds if all other factors remain the same  if treatment is terminated, ↓ dose gradually - abrupt withdrawal can cause rebound hypertension

 drugs to ↓ BP act in various ways  drug of choice varies according to stage of HTN (one/two), other physiological factors (cardiac / renal complications) and effectiveness of therapy  frequently prescribed on a trial basis – dosage may be changed or meds combined to ↑ effectiveness and ↓ side effects  health care practitioner must be observant of vital signs and side effects – assist physician in determining effective treatment

20 11/23/2015

side effects are common • hypotension (postural) • bradycardia (hydralazine may cause tachycardia)

1. thiazide diuretics (chapter 15 for more info) • pts meeting HTN criteria for therapy should be started on thiazide- type diuretics (alone or in combo with a drug from another class – ACE inhibitor, angiotensin receptor blockers, β-blockers, calcium channel blockers) • appear to be as effective as other HTN meds - inexpensive

2. β-adrenergic and calcium channel blockers

• β-adrenergic blockers (end in “lol”) • work by blocking the effects of the hormone epinephrine () - heart beats more slowly and with less force, thereby ↓ BP • Coreg (carvedilol) and Lopressor/Toprol XL (metoprolol) – generally well tolerated and suitable for initial therapy in some pts with angina, post MI, ischemic heart disease, heart failure and certain arrhythmias • bisoprolol, carvedilol, metoprolol ER (extended release) – proven to reduce mortality when used in pts with heart failure • atenolol should not be used to treat HTN b/c no effect in reducing cardiovascular events / mortality

21 11/23/2015

calcium channel blockers • Cardizem (diltaiazem) and Procardia (nifedipine) – initial therapy option for HTN pts with diabetes or high coronary disease risk • more effective in treating African-American, older adults and pts with higher pretreatment BP • may be preferred in pts with obstructive airway disease • short-term Ca-channel blockers should never be used to manage hypertensive crisis - ↑ MI and mortality

• b/c of , verapamil and diltiazen may be used to treat some arrhythmias

3. angiotensin-converting enzyme inhibitors (ACEI’s) • end in “pril” – lisinopril / enalapril • inhibition of antiotensin-converting enz (ACE) ↓ BP by ↓ vasoconstriction - no significant changes in HR or cardiac output • 1st / 2nd line in treatment of HTN – excellent alone – also effective and synergistic in combo with other antihypertensives (diuretics, calcium- channel blockers)

• good for pts who have other serious conditions (heart failure, following MI, high CAD risks, diabetes, renal disease and cerebrovascular disease) • more effective in younger, caucasian populations than black (unless given in higher doses or in combo with diuretic)

22 11/23/2015

side effects (more serious / common in blue) • severe hypotension • hyperkalemia (monitor serum K levels periodically) • rash / photosensitivity • chronic dry cough / nasal congestion • loss of taste / metallic taste • blood dyscrasias • renal impairment

precautions / contraindications apply to • collagen disease (Lupus / scleroderma) • heart failure • angioedema • pregnancy / lactation and children

Interactions with ACE inhibitors • diuretics (potentiate hypotension – watch BP closely) • vasodilators (watch BP closely) • potassium-sparing diuretics and K+ supplements (hyperkalemia) • NSAIS’s and salicylates (antagonize effects of ACE inhibitors and ↑ deterioration of renal fxn in pts with compromised renal fxn) • antacids ↓ absorption • digoxin (possible digitalis toxicity) • lithium (risk of lithium toxicity)

23 11/23/2015

angiotensin receptor blockers (ARB’s)  similar to ACE inhibitors – generally used as alternatives  block the angiotensin receptor that causes vasoconstriction when stimulated by angiontensin II  Cozar (losartan) and Diovan (valsartan) block the effects of angiotensin II -  BP without marked change to HR

 compared to ACEI’s – ARB’s are associated with lower incidence of drug induced cough, rash and/or taste disturbances – used in pts that cannot tolerate ACEI’s  African American pts - smaller antihypertensive response than other ethnic groups  addition of a low-dose thiazide diuretic significantly improves efficacy  ARB’s are good choice for pts with other serious conditions (heart failure, diabetes and renal disease)

side effects are relatively uncommon – include dizziness, orthostatic hypotension, upper respiratory tract and hyperkalemia precautions / contraindications  renal impairment  pregnancy / lactation and children

Interactions with ARB’s – similar to those with ACEI’s

24 11/23/2015

antiadrenergic agents  central-acting α-adrenergic agent (Clonidine / catapres) – used mainly in the treatment of HTN  available as oral, transdermal and (epidural) formulations  Clonidine – also used successfully in other conditions – ADHD, nicotine / withdrawal, vascular head aches, glaucoma. ulcerative colitis, Tourette’s syndrome, and treatment of severe pain in cancer pts

 peripheral acting α-adrenergic agent (Prazosin / minipress) – used primarily to treat HTN  other agents in this class – used to treat HTN and benign prostatic hyperplasia (BPH)-  risk of  HTN should not be managed with α-blocker alone

peripheral vasodilator  Hydralazine – sometimes used in treatment of mod-severe HTN (especially pts with CHF -  HR and cardiac output)  generally used in conjuction with a diuretic and another hypotensive agent (β-blocker) side effects (common / severe in blue)  tachycardia and palpitations  headache and flushing  orthostatic hypotension  GI effects (nausea, vomiting, diarrhea, constipation  edema and weight gain  blood abnormalities

25 11/23/2015

precautions / contraindications  systemic lupus erythematosus (SLE)  renal disease  CAD and rheumatic heart disease  pregnancy

PATIENT EDUCATION

Patients taking antihypertensives should be instructed regarding:

 monitor BP at home – keep a log and share with physician  immediately report adverse effects (slow / irregular heart beat, dizziness, weakness, difficulty breathing, gastric distress, numbness and swelling in extremities  take meds on time – do not skip a dose / double dose – do not discontinue meds unless directed by physician  rise slowly from reclined position ( lightheadedness)  take care when driving / operating machinery – medication may cause drowsiness  potentiation of adverse effects by alcohol (dizziness, weakness, sleepiness and confusion)  Reduction / cessation of smoking to help BP

26 11/23/2015

PATIENT EDUCATION

 importance of life-style modifications (exercise, smoking cessation, limit alcohol consumption, healthy diet)  avoid hot tubs and hot showers – may cause weakness / fainting  mild exercise on regular basis (approved by physician)  always swallow extended-release tabs intact (quick release of meds into system can cause BP to drop suddenly – loss of consciousness and shock  avoid grapefruit juice with calcium channel blockers ( risk of hypotension / other adverse cardiac effects)

CORONARY VASODILATORS  used in the treatment of angina – insufficient blood supply to part of the heart (ischemia) causing acute pain  most common form of angina – angina petoris – chest pain resulting from  blood supply to heart muscle (obstruction / constriction of the coronary arteries – supply the heart with oxygenated blood)

 vasodilators admin to dilate vessels ( myocardial O2 supply) and stop attacks of angina ( frequency when admin prophylactically)  vasodilators used: nitrates, β-blockers and calcium channel blockers

27 11/23/2015

nitrates  most commonly used for angina pectoris and long-term prophylactic management – nitroglycerine and isosorbide (Isordil, Imdur)  nitroglycerine available in several forms  sublingual (tabs or spray) – for acute angina – if no relief 5min after a dose, call EMS – unrelieved chest pain may indicate acute MI  timed-release caps / tabs (store in glass containers only, with a tight fitting metal screw cap, away from heat – plastic can absorb medication and air, heat or moisture causes loss of potency) – loss of potency can be detected by pt if there is loss of tingling under the tongue upon admin

 transdermal – long-term prophylactic treatment of angina pectoris –   Nitro-Bid ointment - ointment is spread lightly over hairless skin area and applicator paper is taped in place – care must be taken not to touch ointment during application as accidental absorption can cause headache – if d/c dose must be decreased gradually to prevent withrawal rxns  Nitro-Dur transdermal – longer acting than ointment – skin patch applied every 24h (on in am and off 12h later in pm) to upper arm or body – sites rotated to avoid skin irritation

28 11/23/2015

side effects (blue are common / adverse)  headache (diminishes over time – for relief)  postural hypotension (dizziness, weakness, syncope) – pts should be sitting during admin of fast-acting nitrates  transient flushing  rash and skin irritation (transdermal)  blurred vision and dry mouth (d/c drug with these symptoms)  hypersensitivity rxns (enhanced by alcohol – nausea, vomiting, diarrhea, cold sweats, tachycardia, syncope)

precautions / contraindications  glaucoma  GI hypermotility / malabsorption (timed-release forms)  intracranial pressure  severe anemia  hypotension

 interaction of nitrates may occur with  alcohol – potentiates hypotensive effects  phosphodiesterase (PDE) inhibitors (Viagra – erectile dysfunction) – two drugs interact causing a dangerous drop in BP

 for long-term prophylactic treatment of angina pectoris, β- blockers (Lopressor) and calcium channel blockers (Cardizem / Calan) are frequently used

29 11/23/2015

PATIENT EDUCATION

Patients taking coronary vasodilators (nitrates)should be instructed regarding:

• admin fast-acting preps (sublingual tabs / spray) while sitting down – pt may become lightheaded  rise slowly from a reclined position  do not drink alcohol or take PDE inhibitors while taking nitrates – cause a dangerous drop in BP  use time-released tabs to prevent attacks (work too slowly once an attack starts)  nitrates taken for chronic angina may require periods of drug- free intervals – avoid development of nitrate tolerance ( effects

PATIENT EDUCATION

• taking timed-released caps/tabs on an empty stomach with a full glass of water • Allow sublingual tabs to dissolve under the tongue / in cheek pouch – do not chew or swallow • repeat sublingual tabs / spray in 5-10 min for a max of 3x (if no relief / worsening symptoms after first dose – call EMS) • do not d/c medication suddenly id admin for several weeks (dosage must be reduced gradually) • sensations to be expected – facial flushing, headache for a short time, lightheadedness upon rising too suddenly (if sensations persist or symptoms of irregular heart beat / blurred vision notify physician immediately) • prevent attack by admin sublingual tabs /spray before exertion or emotional stress

30 11/23/2015

ANTILIPEMIC AGENTS • estimated that nearly 50% Americans have elevated total blood cholesterol levels (hypercholesterolemia) (200mg/dL) – key risk factor for coronary heart disease (CHD) • cardiovascular disease – leading killer of men and women in US (more deaths than cancer, diabetes, accidents and chronic lung disease combined) • high cholesterol can lead to arterial blockage, hardening of the arteries, blood clots, heart attack or stroke – may have a role in

 lipoproteins – transport cholesterol and other fats through the blood stream  low-density lipoproteins (LDL’s – bad cholesterol) carry the largest amount of cholesterol in the blood and are responsible for transporting and depositing it in the arterial walls  very low-density lipoproteins (VLDL’s – triglycerides) are precursors of LDL and compose the largest proportion of lipids in the diet, adipose tissue, and blood  triglycerides (TG) are source of energy – excess dieatary calories are converted to TG and stored as fat in adipose tissue for future energy needs  excess TG (>150) can be an independent risk factor leading to atherosclerosis, CHD and pancreatitis

31 11/23/2015

 high-density lipoproteins (HDL’s – good cholesterol) help transport LDL cholesterol from the walls of the arteries through the bloodstream to the liver for excretion  HDL <40mg/dL is low – each 1mg/dL ↑ is associated with a 6% lower risk of cardiovascular disease

 LDL cholesterol is the primary target of treatment in clinical lipid management  therapeutic life-style changes including LDL lowering dietary management (restriction of saturated and trans fats / cholesterol intake), weight control, appropriate exercise, limited alcohol intake, and smoking cessation – should achieve therapeutic goal in most pts  life-style changes inadequate – drug therapy may be added  drug therapy aimed at ↓ cholesterol levels by reducing hepatic production or intestinal absorption of cholesterol

 Six categories of antilipemic agents  HMG-CoA reductase inhibitors ()  Bile acid sequestrants  Nicotinic acid (niacin)  Fibric acid derivatives  Cholesterol absorption inhibitor  Omega-3 fatty acids

32 11/23/2015

Statins (HMG-CoA reductase inhibitors)

• inhibit the enzyme for cholesterol synthesis • most potent lipid-lowering meds available for monotherapy • first choice in managing high cholesterol • generally well tolerated • most active at night when dietary intake is low – generally given at bedtime in order to provide optimal ↓ LDL levels

• Lipitor (atorvastatin) and Zocor (simvastatin) – very effective in ↓LDL levels (up to 60%) and modestly effective in ↓TG levels and ↑ HDL levels - ↓ cardiovascular morbidity and mortality

side effects (common / serious in blue) • mild GI disturbances • myalgia / muscle weakness (try switching to different if problematic) • rhabdomyolysis (destruction of muscle tissue leading to renal failure) –rare • elevated liver enzymes (monitor if clinically indicated) • ↑ risk (9-13%) of new-onset diabetes mellitus with high dose statin use (benefits of statin therapy outweigh the risk of induced diabetes – monitor pt)

33 11/23/2015

precautions / contraindications • hepatic or renal disease • existing myalgia or muscle weakness • pregnancy / lactation and children • gemfibrozil, HIV and HepC protease inhibitors (↑ risk myopathy and rhabdomyolysis)

Interactions of certain statins with amiodarone, dronedarone, immunoseuppressinve drugc, erythromycin, azole antifungals, diltiazem, verapamil, grapefruits fuice or other antilipemic drugs ( and niacin) ↑ risk of myopathy and renal failure

bile acid sequestrants • cholestyramine (Questran) and colesevelam (WelChol) – not absorbed from the GI tract – bind bile acids in the intestine which interrupts the process by which bile acids are returned to the liver for reuse • bile acids are formed from cholesterol – sequestrants ↓ total body cholesterol • can be used as monotherapy when moderate ↓ in LDL levels are required,

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