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Running head: PERSONAL DRUGS1

PERSONAL DRUGS68

Personal Drugs

Ashley Peczkowski

Wright State University

First Diagnosis: Left Ventricular Heart Failure in a Renal Patient

A 45 year old male presents as a new patient to your cardiology practice. He has not seen a cardiologist since he was hospitalized three years ago for acute myocardial infarction (MI). The patient has expressed concern for increased leg swelling over the past week and a weight gain of three pounds. His history includes diabetes, end stage chronic kidney disease requiring hemodialysis, and MI. An in office echocardiogram shows a dilated left ventricle with a 40% ejection fracture (EF). Upon completion of history and physical his diagnosis is left ventricular heart failure (LVHF) with fluid overload. Laboratory tests have been ordered, including lipid panel, basic metabolic panel, complete blood count, B-type natriuretic peptide (BNP), and a urinalysis. Results are pending. Other tests ordered include an electrocardiogram (ECG) and chest x-ray. An in office blood glucose test was 152, blood pressure was 167/93 and his weight and height are 167 pounds (75.9 kilograms), five foot nine inches. Finally, he is set up to receive an additional hemodialysis treatment today for removal of excess fluid.

I. Definition of Diagnosis

Heart failure is defined by the Heart Failure Society of America (2013) as a syndrome, not a diagnosis, which can be caused by cardiac impairment. This can result from myocardial muscle dysfunction or destruction and is represented by either left ventricular dilation or hypertrophy or both (Albert et al., 2010). According to the 2009 heart failure guidelines, there are four different stages of heart failure. The first two stages (A and B) are not considered heart failure but rather at risk patients and include those with a history of hypertension (HTN), pervious MI, diabetes (DM), left ventricular (LV) remodeling and other pre heart failure (HF) diseases. The final two stages (C and D) are for those patients who have diagnosed heart failure. Stage C includes those with known structural cardiac deficits, shortness of breath (SOB), fatigue, and reduced tolerance for exercise. The final stage, stage D, are for patients who have maxed out on medical therapy and need specialized interventions such as hospice, heart transplant, or permanent mechanical support (Abraham et al., 2009).

Diagnosis criteria are not exact and can depend on a variety of findings or symptoms. An echocardiogram is the most common tool used to diagnosis HF. A comprehensive 2-dimensional echocardiogram with Doppler flow studies can determine EF, structural abnormalities, ventricular wall thickness, wall motion, valvular abnormalities, and pericardial abnormalities (Abraham et al., 2009). The typical findings of a HF patient are an EF of 40 percent or less; however, the patient may still have HF with a higher EF (Heart Failure Society of America, 2002). Left ventricular dilation, hypertrophy, reduced EF, and symptoms such as fatigue, SOB, fluid retention, reduced exercise tolerance, palpations, and cough are all evaluated when diagnosing LVHF.

II. Therapeutic Objectives

Treatment objectives for patients with LVHF include life style changes, risk factor management, starting ACE inhibitors, Beta blockers, and insertion of a pacemaker/ defibrillator for appropriate patients. Life style changes such as smoking cessation, regular exercise, reduced alcohol use, and illicit drug use should be encouraged. The treatment goals according to the Heart Failure Practice Guidelines for 2010 are: HTN patients with renal insufficiency and ≤ one g/day of proteinuria need to sustain a blood pressure of 130/85, have a limited sodium diet, reduced BMI to < 30(Albert et al., 2010), and obtain management of hyperlipidemia (HDL > 50mg/dL and LDL < 100mg/dL) and diabetes (A1C < 7%) (American Diabetes Association, 2011).

While HF is considered a progressive disease, it is important to stabilize myocardial dysfunction and improve remodeling. These outcomes are obtained by medication therapy through ACE inhibitors, beta-blockers, and diuretics. ACE inhibitors are given to those with increased risk of developing HF such as those with coronary artery disease, diabetes, peripheral vascular disease, or stroke. Beta blockers are given for those individuals who have suffered from a previous MI and diuretics are given to those with fluid overload and functioning kidneys (Albert et al., 2010). For those individuals with severe kidney impairment requiring hemodialysis, fluid overload should be treated with dialysis and ACE inhibitors should be avoided (Abraham et al., 2009).

An implantable cardioverter-defibrillator (ICD) should be considered for those patients with sustained ventricular arrhythmias, cardiac arrest, or unexplained syncope to prevent sudden death. An ICD is contraindicated in those individuals with progressive decompensated HF because death is expected. Only in cases of planned cardiac transplant should the ICD then be considered (Abraham et al., 2009).

III. Inventory of Effective Drug Groups: Oral

Drug

Efficacy

Safety

Suitability

Angiotensin II Receptor Blockers (ARBs)

Candesartan (Atacand®), Eprosartan (Teventen®), Irbesartan (Avapro®), Losartan (Cozaar®), Olmesartan (Benicar®), Telmisartan (Micardis®), Valsartan (Diovan®) (Lexi-comp, 2013)

Pharmacodynamics:

ARBs selective inhibition of angiotensin II by competitive antagonism of receptors. Displacement of angiotensin II from angiotensin I receptor to produce vasodilation, prohibit aldosterone release, catecholamine release, arginine vasopressin release, water intake and reduce hypertrophic response (Barraras & Gurk-Turner, 2003).

Pharmacokinetics

Absorption: Rapid

Metabolism: Absorption via ester hydrolysis with intestinal wall, hepatic CYP2C9 and 3A4. Extensive first pass effect

Excretion: Urine and feces (Clinical Pharmacology, 2013)

Side effects:

Common:

Hyperkalemia, hypotension, dizziness, headache, drowsiness, diarrhea, metallic taste, and rash.

Rare:

Kidney impairment, hepatic impairment, angioedema, and leukocytosis (Lexi-comp, 2013).

Monitor: Supine BP, CNS changes, hyperglycemia, electrolytes, serum creatinine, BUN, urinalysis, hypotension, tachycardia, and CBC (Lexi-comp, 2013).

Substrate CYP2C9 (minor), Inhibits CYP2C8 (moderate), (weak), CYP2C19 (weak), CYP2D6 (weak), CYP3A4 (weak), CYP2C9 (weak), (moderate) and SLCO1B1 (Lexi-comp, 2013).

This medication can be given with or without food. Avoid alcohol use (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to ARBs or formulary components. Concomitant use of aliskiren in diabetic patients (Lexi-comp, 2013).

Use Caution:

May not be effective in African-American patients. Use with caution in Aortic/Mitral stenosis. Reduce dose in hepatic impairment, and use with caution in renal impairment, Bilateral renal artery stenosis, aortic/mitral stenosis, oral airway surgery, or history of angioedema. Watch for hyperkalemia in renal impairment, potassium-sparring diuretics, potassium supplements, and potassium salts. Watch for hypotension in volume depletion. May cause further renal dysfunction. May cause worsening Heart failure. Diabetics should monitor glucose closely (Access Medicine, 2013; Lexi-comp, 2013).

Angiotensin-Converting Enzyme (ACE) Inhibitors

Benazepril (Lotensin®), Captopril (Capoten®), Enalapril (Vasotec®, Renitec®), Fosinopril (Monopril®), Lisinopril (Lisodur®, Lopril®, Novatec®, Prinivil®, Zestril®), Perindopril (Cpversy®, Aceon®), Quinapril (Accupril®), Ramipril (Altace®, Tritace®, Ramace®, Ramwin®), Trandolapril (Mavik®) (Lexi-comp, 2013)

Pharmacodynamics:

Prevents conversion of angiotensin I to angiotensin II which in turn dilates arterioles and promotes excretion of sodium and water. (Song & White, 2002).

Pharmacokinetics:

Absorption: Moderately in gastrointestinal (GI) tract

Metabolism: Rapid and extensive hepatic via enzymatic hydrolysis, 50%; Extensive first pass effect. Some drugs not metabolized

Excretion: Urine (unchanged) and hepatic depending on drug (Lexi-comp, 2013).

Side effects:

Common: Orthostatic effects, hypotension, headache, dizziness, cough, rash, hyperkalemia, weakness, and metallic taste

Under certain conditions:

Prolonged QT interval, gout, and bradycardia

Rare: Kidney failure, neutropenia, angioedema, and Steven-Johnson syndrome (Access Medicine, 2013; Lexi-comp, 2013).

Monitor:

BUN, Serum creatinine, Renal function, Lithium levels, White blood count, Potassium, and CBC with differential in renal impairment or collagen diseases

Substrate CYP2D6 (major) (Lexi-comp, 2013).

Take on empty stomach one hour before or two hours before meal. Long term use can alter taste due to zinc deficiency. Avoid potassium rich diet (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to ACE inhibitors, previous angioedema, and concomitant use of aliskiren in diabetic patients (Lexi-comp, 2013).

Use Caution:

Use caution with aortic stenosis, African Americans with angioedema history, cholestatic jaundice, cough, cardiovascular disease, collagen vascular diseases, hypertrophic cardiomyopathy, hyperkalemia, hypersensitivity reactions, hepatic impairment, neutropenia, agranulocytosis, renal artery stenosis, and renal impairment. Dose adjustment may be needed in renal impairment. Con-committed use with ARBs and renin inhibitors may cause hypotension, hyperkalemia, and increased renal impairment. (Clinical Pharmacology, 2013; Lexi-comp, 2013)

Beta Blockers

Acebutolol (Sectral®), Atenolol (Tenormin®), Betaxolol (Kerlone®, Betoptic®), Bisoprolol (Zebeta®), Carvedilol (Coreg®, Coreg CR®), Esmolol (Brevibloc®), Labetalol (Trandate®), Metoprolol (Lopressor®, Toprol-XL®), Nadolol (Corgard®), Nebivolol (Bystolic®), Penbutolol (Levatol®), Pindolol (Visken®), Propranolol (Inderal®, Inderal LA®, InnoPran XL®), Sotalol (Betapace®, Sorine®), Timolol (Betimol®, Blocadren®, Istalol®, Timoptic®) (Lexi-comp, 2013)

Pharmacodynamics:

Beta adrenoreceptor blocker or beta adrenoreceptor and alpha adrenergic blocker causing reduced cardiac output, exercise tachycardia, reduced reflex orthostatic tachycardia, vasodilation, lower peripheral vascular resistance, lower renal resistance, reduced plasma renin activity, increased atrial natriuretic peptide and in heart failure patients it reduced pulmonary wedge pressure, lower pulmonary artery pressure, increase stroke volume, and decrease right atrial pressure (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Rapid and extensive

Metabolism: Hepatic through CYP2c9, 2D6, 3A4, and 2C19. Three active metabolites. Extensive first pass effect. Plasma concentration in elderly and hepatic impaired are 50% and 4-7 times higher.

Excretion: primary feces (2-60%), some urine (30-80%) (Lexi-comp, 2013).

Side Effects:

Common:

Fatigue, cold hands, headache, GI distress, constipation, diarrhea, and dizziness.

Rare:

Shortness of breath, insomnia, decreased libido, and depression (Lexi-comp, 2013).

Monitor:

Blood pressure, heart rate, fluid balance, and glucose

Substrate CYP2C19 (minor) and CYP2D6 (major). Inhibits CYP2D6 (weak) (Lexi-comp, 2013).

This drug should be given with meals to reduce orthostatic hypotension. Do not crush or chew. Bradycardia may be more severe in elderly (Lexi-comp, 2013).

Contraindication:

Hypersensitivity to Beta blockers, Decompensated cardiac failure requiring intravenous inotropic therapy, Bronchial asthma, Bronchospastic conditions, Av block, Sick sinus syndrome, Sinus node dysfunction, Pregnancy, Severe bradycardia without pacemakers, Cardiogenic Shock, Severe hepatic impairment

Use Caution:

Bronchospatic disease, Conduction abnormality, Diabetes, Heart failure, Hepatic impairment, Mesenteric Vascular Disease, Myasthenia gravis, Peripheral vascular disease, Pheochromocytoma, Psoriasis, Psychiatric Disease, Renal impairment, and Thyroid disease. Use caution when taking verapamil, diltiazem, digoxin, or inhaled anesthetics (Lexi-comp, 2013).

Avoid:

Dental epinephrine (Lexi-comp, 2013).

Diuretic/

Anhydrase Diuretic

Acetazolamide (Lexi-comp, 2013)

Pharmacodynamics:

Reverses inhibition of carbonic anhydrase causing reduced hydrogen ion secretion at renal tubule and increase excretion of sodium, potassium, bicarbonate, and water. Decreased aqueous humor and inhibits carbonic anhydrase in CNS to retard abnormal and excessive discharge (Clinical Pharmacology, 2013; Lexi-comp, 2013).

Pharmacokinetics:

Onset of Action: Two hours

Peak Effect: Eight -18 hours

Duration: 18-24 hours

Time to Peak: three-six hours

Excretion: Urine (70-100% Unchanged) (Lexi-comp, 2013).

Side Effects:

Common:

Taste alterations, nausea, vomiting, diarrhea, polyuria, drowsiness, and dehydration

Under Certain Condition:

Numbness in extremities, blurred vision, and kidney stones

Rare:

Acidosis and confusion (Lexi-comp, 2013).

Monitor:

Intraocular pressure, serum electrolytes, CBC with differential, growth, and glucose in diabetics.

Inhibits CTYP3A4 (weak) (Lexi-comp, 2013).

Give with food to decrease GI upset. Can cause metallic taste (Access Medicine, 2013).

Contraindications:

Hypersensitivity to acetazolamide, sulfonamides, or any component. Hepatic disease or insufficiency. Decreased sodium/ potassium levels. Adrenocortical insufficiency. Cirrhosis, hyperchloremic acidosis. Severe renal disease. Long term use in non-congestive angle-closure glaucoma (Lexi-comp, 2013)

Use Caution:

Impairment of mental alertness, sulfa allergy, diabetes, hepatic impairment, and respiratory acidosis (Access Medicine, 2013).

Avoid:

High dose Aspirin (Lexi-comp, 2013).

Diuretic/

Loop Diuretics

Bumetanide (Bumex®), Ethacrynate (Edecrin®), Furosemide (Lasix®), Torsemide (Demadex®) (Lexi-comp, 2013)

Pharmacodynamics:

Inhibits reabsorption of sodium and chloride in ascending loop of Henle, distal tubules, and proximal renal tubule. Causes excretion of water, sodium, chloride, magnesium, phosphate, and calcium (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Extensively

Metabolism: Partially hepatic via CYP

Half-life: 0.5- 3.5 hours

Excretion: Urine (50-81%; 20-45% unchanged) and feces (2%) (Lexi-comp, 2013).

Side Effects:

Common:

Hypokalemia, dizziness, headache, fatigue, constipation, abdominal pain, nausea, tinnitus, and hyperglycemia.

Rare: Abnormal heart rhythms (Lexi-comp, 2013).

Monitor:

Weight, I&O, blood pressure, orthostasis, serum electrolytes, renal function, and hearing (Clinical Pharmacology, 2013).

May decrease levels if taken with food. Some patients may need potassium supplements (Lexi-comp, 2013).

Contraindicated:

Anuria, Hepatic come, hypersensitivity to loop diuretics or any component, history of severe watery diarrhea caused by drug and severe electrolyte depletion (Access Medicine, 2013).

Use Caution:

Cirrhosis, ascites, fluid/ electrolyte loss, diabetes, prostatic hyperplasia, urinary stricture, SLE hypersensitivity reactions, hyperuricemia, nephrotoxicity, ototoxicity, photosensitivity, sulfa allergy, digoxin, and with other antihypertensive (Lexi-comp, 2013)

Diuretics/

Potassium Sparing Diuretic

Amiloride Hydrochloride, Spironolactone (Aldactone®), Triamterene (Dyrenium®) (Lexi-comp, 2013)

Pharmacodynamics:

Blocks sodium channels in late distal convoluted tubule and collecting duct. This causes reduced intracellular sodium decreasing Na+/K+ATPase, leading to potassium retention and excretion of calcium, magnesium, and hydrogen ions (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: 15-25%

Metabolism: Hepatic, multiple metabolites

Half-life: 78 minutes to 23 hours

Excretion: Urine and feces (Lexi-comp, 2013).

Side Effects:

Common:

Dizziness, nausea, rash, decreased libido, constipation, lethargy, and vomiting.

Rare:

Macromastia, confusion, Steven-Johnsons syndrome, and breast cancer (Lexi-comp, 2013).

Monitor:

Blood pressure, serum electrolytes, renal function, I&O, CNS changes, ECG changes, rash, dehydration, and daily weight (Lexi-comp, 2013).

Avoid alcohol, licorice, and potassium rich foods. Do not use salt substitutes. May be taken with food if GI upset (Lexi-comp, 2013).

Contraindications:

Anuria, acute renal insufficiency, severe hepatic disease, hypersensitivity to potassium sparing diuretics or any component, diabetic nephropathy, and hyperkalemia (Lexi-comp, 2013).

Use caution:

Fluid or electrolyte loss, hyperkalemia, diabetes, photosensitivity, kidney stones, acidosis, gynecomastia, tumorigenic, adrenal vein catheterization, cirrhosis, heart failure, and taking potassium supplements (Lexi-comp, 2013).

Diuretics/

Thiazide Diuretics

Chlorothiazide (Diuril®) Chlorthalidone (Hygroton®), Hydrochlorothiazide (Hydrodiuril®, Microzide®), Indapamide (Lozol®), Methyclothiazide (Enduron®), Metolazone (Zaroxolyn®, Diulo®, Mykrox®) (Lexi-comp, 2013).

Pharmacodynamics:

Inhibits sodium and chloride reabsorption in distal tubules, Proximal segment of the distal tubule of the nephron, and cortical-diluting segment of the ascending loop of Henle causing excretion of sodium, chloride, and water. Product of mechanism results in diuresis. Also causes potassium, hydrogen ions, magnesium, phosphate, and bicarbonate loss (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Poor

Metabolism: Not metabolized

Half-life: 45 minutes -60 hours.

Excretion: Urine (10-15%) (Clinical Pharmacology, 2013; Lexi-comp, 2013).

Side effects:

Common:

Hypokalemia, dizziness, nausea, and xerostomia

Rare:

Urinary retention, sudden vision changes, eye pain, or rash (Lexi-comp, 2013)

Monitor:

Serum electrolytes, renal function, blood pressure, weight, and I&O (Lexi-comp, 2013).

Take dose in am or early day to avoid night time urinary frequency. If taking oral hypoglycemic, watch glucose closely. Decrease dietary sodium and calcium and increase dietary potassium, zinc, magnesium, and riboflavin (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to Thiazide diuretics or any component, Sulfonamide-derived drugs, and anuria (Lexi-comp, 2013).

Use Caution:

Use caution with patients who have: Asthma, electrolyte imbalance, hypersensitivity reactions, ocular effects, photosensitivity, sulfa allergy, diabetes, gout, hepatic impairment, hypercalcemia,

hypercholesterolemia, renal impairment, parathyroid disease, and systemic lupus erythematosus (Access Medicine, 2013; Lexi-comp, 2013).

Digoxin

(Lanoxin®) (Lexi-comp, 2013)

Pharmacodynamics:

Inhibits sodium/potassium APTase pump in myocardial cells causing increased intracellular sodium, promoting calcium influx creating increased contractility (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Passive diffusion in upper small intestine

Metabolism: Sugar hydrolysis in stomach or reduced lactone ring in intestinal bacteria

Excretion: Urine (50-70% unchanged) (Lexi-comp, 2013).

Side Effects:

Common:

Dizziness, dyspepsia, nausea, diarrhea, tachycardia, or bradycardia

Rare:

Confusion, weight gain, vision changes, anorexia, asthenia, rash, or abnormal heart conductions (Access Medicine, 2013)

Monitor:

Heart rate, Apical pulse, Rhythm, Periodic ECGs, Baseline and periodic serum creatinine, serum potassium, magnesium, and

Calcium. Monitor for signs of toxicity including confusion and depression. Draw digoxin level 12-14 hours after initial dose or 3-5 days, and then every 5-7 days until at steady state then 7-14 days (Lexi-comp, 2013).

Substrate of CYP3A4 (minor) (Lexicomp, 2013).

End stage renal disease requires 50% reduce in loading dose. Needs potassium rich diet (Lexi-comp, 2013).

Contraindication:

Hypersensitivity to digoxin, digitalis forms, or any component. Ventricular fibrillation (Lexi-comp, 2013).

Use caution:

Proarrhythmic effects, Accessory bypass tract, Wolff-Parkinson-White syndrome, Acute MI (6 months or less), Atrioventricular block, Beri beri heart disease, electrolyte imbalance, Heart failure, Low EF, Cardiomyopathy, Constrictive pericarditis, Amyloid heart disease, Sinus rhythm, No HF symptoms, Hypermetabolic states, Hypertrophic Cardiomyopathy, Renal impairment, Sinus nodal disease, and Thyroid disease. Reduce digoxin with Amiodarone, propafenone, quinidine, and verapamil (Clinical Pharmacology, 2013).

Nitrates

Isosorbide Dinitrate, Isosorbide Mononitrate (Imdur®, Monoket®), Nitroglycerin (Nitro-Dur®) (Lexi-comp, 2013)

Pharmacodynamics:

Stimulation of cyclic-GMP causing vascular smooth muscle relaxation. More prominent in veins. Decreases preload thus reducing cardiac oxygen demand and reduced afterload. Also improves coronary artery dilation. Nitroglycerin form free radical nitric oxide which works on the smooth muscle and increases guanosine 3’5’ monophosphate causing smooth muscle relaxation, reduces cardiac oxygen demand, decreased preload, reduced afterload, dilates coronary arteries, and improves collateral flow (Clinical Pharmacology, 2013)

Pharmacokinetics:

Absorption: 50% through mucous membranes in GI tract

Metabolism: Extensive hepatic via liver reductase enzyme. Extensive first pass effect. Nonhepatic metabolism via red blood cells and vascular walls.

Excretion: urine and feces (Lexi-comp, 2013).

Side effects:

Common:

Headache, flushing, dizziness, upset stomach, vomiting, hypotension, and arrhythmias

Rare:

Fainting, restlessness, blurry vision, dry mouth, and rash (Access Medicine, 2013).

Monitor:

Blood pressure, heart rate, GI disturbances, volume depletion, hypotension, right ventricular infarction, and tolerance (Lexi-comp, 2013).

Substrate CYP3A4 (major) (Lexi-comp, 2013).

Allow for nitrate free intervals. Dose alternate timing. Alcohol can exacerbate hypotension (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to Nitrates or any component, Organic nitrates, and Concurrent use of phosphodiesterase-5 inhibitors. Severe pericardial effusion, Severe anemia, increased Intracranial pressure, Hypotension, Extreme Bradycardia, Tachycardia in the absence of heart failure, and Right ventricular infarction (Lexi-comp, 2013).

Use caution:

Hypotension, Bradycardia, Inferior wall MI, Intracranial pressure increase, Hypertrophic cardiomyopathy, PDE-5 inhibitors, Extended release: Acute MI or Acute HF, Sublingual: acute anginal episode, and Tolerance: Overcome by short nitrate absence (Lexi-comp, 2013).

IV. Effective Drug Classification: Beta Blocker Oral

Drug Name

Efficacy

Safety

Suitability

Cost

Beta Blockers

Acebutolol (Sectral®) (Lexi-comp, 2013)

Onset: One to two hours


Absorption: Oral 40%

Protein binding: ~26%%

Metabolism: Extensive first pass effect to equipotent and cardio-selective diacetolol metabolite.

Bioavailability: 40%

Half-life: Parent drug: Three to four hours; Metabolite: Eight to 13 hours

Peak time: Two to four hours

Excretion: primary feces (50- 60%), some urine (30-40%) (Clinical Pharmacology, 2013; Lexi-comp, 2013).

Drug interactions:

Floctafenine, and Methacholine (Lexi-comp, 2013).

Increase Effect/Toxicity:

Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensives, Antipsychotic agents, Aripiprazole, Bupivacaine, Cardiac glycosides, Cholinergic agonists,

Ergot derivatives, Fingolimod, Hypotensive agents, Insulin, Lidocaine,

Mepivacaine, Methacholine, Midodrine, RiTuximab, and Sulfonylureas (Lexi-comp, 2013).

Decrease Effect/Toxicity:

Beta2-agnosits and Theophylline derviatives (Lexi-comp, 2013).

Avoid:

Beta2-angonist, Dong quai, Yohimbe, Ginseng, Bosutinib, Floctafenine, Methacholine, Pomalidomide, Topotecan, and VinCRIStine (Lexi-comp, 2013).

Weak inhibitor of CYP2D6 substrates (Lexi-comp, 2013).

-Teach diabetics about possible altered glucose.

-Taper over two weeks when discontinuing.

-Serum levels slightly increased with food intake.

-Check pulse prior to taking drug.

-Bradycardia may be more severe in elderly.

-Geriatrics may need reduced dose.

-Do not stop drug abruptly.

-Do not stop prior to surgery.

-Avoid herbs with hypertensive properties and hypotensive properties (Access Medicine, 2013; Lexi-comp, 2013).

Acebutolol HCL oral: 200mg (100): $100.73

400mg (100): $133.97

Sectral ® oral: 200mg (100)L $399.19

400mg (100) $530.75 (Lexi-comp, 2013)

Beta Blockers

Atenolol (Tenormin®) (Lexi-comp, 2013)

Onset: One to two hours

Peak effect: 2-4 hours


Absorption: Rapid and incomplete

Distribution: Does not cross blood brain barrier

Protein binding: 6-16%

Metabolism: Limited hepatic

Peak time: 2-4 hours

Excretion: Feces (50%) and Urine (40%) (Lexi-comp, 2013).

Drug interactions:

Floctafenine, and Methacholine (Lexi-comp, 2013)

Increased Effect/Toxicity:

Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensives, Bupivacaine, Cardiac glycosides, Cholinergic agonists,


Mepivacaine, Methacholine, Midodrine, RiTuximab and Sulfonylureas (Lexi-comp, 2013).

Decreased Effect/Toxicity:

Beta2-agnosits and Theophylline derviatives (Lexi-comp, 2013)

Avoid:

Dong quai, Ephedra, Yohimbe, Ginseng and Garlic (Lexi-comp, 2013).

-Teach diabetics about possible altered glucose.

-Taper over two weeks when discontinuing.

-May decrease concentration when taken with food.

-Check pulse prior to taking drug.

-Geriatrics may need reduced dose.

-Do not stop drug abruptly.

-Do not stop prior to surgery.

-Decreased HDL levels.

-Avoid herbs with hypertensive properties and hypotensive properties (Access Medicine, 2013; Lexi-comp, 2013).

Atenolol oral: 25mg (100): $81.75

50mg (100): $84.60

100mg (30): $42.62

Tenormin® oral: 25mg (100): $184.99

50mg (30): $41.06

100mg (30): $92.07 (Lexi-comp, 2013)

Beta Blockers

Betaxolol (Kerlone®, Betoptic) (Lexi-comp, 2013)

Onset: 1-1.5 hours

Absorption: ~100%

Metabolism: Hepatic to multiple metabolism

Protein Binding: ~50%


Half-life: 14-22 hours, prolonged with hepatic or renal disease

Peak time:1.5-6 hours

Excretion: Urine (Lexi-comp, 2013).

Drug interactions:

Floctafenine, and Methacholine (Clinical Pharmacology, 2013).


Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensives, Antipsychotic agents, Aripiprazole, Bupivacaine, Cardiac glycosides, Cholinergic agonists,




Beta2-agonists and theophylline derivatives (Lexi-comp, 2013).

Avoid:

Herbs with antihypertensive effects (Lexi-comp, 2013).

Increases metabolism of CYP1A2 (major) and CYP2D6 (minor) substrates. Inhibits CYP2D6 weak affect (Lexi-comp, 2013).

-Geriatrics may bradycardia more frequently.

-Taper down over two week when stopping drug.

-Do not stop for surgery.

-May take with meals.

-Diabetics should watch glucose closely.

-Do not abruptly stop. Can cause tachycardia and hypertension.

-Do not stop for surgery (Access Medicine, 2013).

Betaxolol HCL oral: 10mg (100): $123.00

20mg (100): $186.00

Kerlone® oral: 10mg (100): $156.89

20mg (100): $235.25 (Lexi-comp, 2013)

Beta Blockers

Bisoprolol (Zebeta®) (Lexi-comp, 2013)

Onset: 1-2 hours

Absorption: Rapid and almost complete

Distribution: Widely; heart, liver, lungs and saliva; does cross the blood-brain barrier

Protein binding: ~30%

Metabolism: Hepatic Extensive first pass effect.

Bioavailability: ~80%

Half-life: 9-36 hours depending on renal and liver function


Excretion: Urine (50% unchanged drug), and feces (2%) (Lexi-comp, 2013).

Drug interactions:

Floctafenine, Conivaptan, and Methacholine (Lexi-comp, 2013)

Increased Effect/Toxicity: Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensive, Antipsychotic agents, Bupivacaine, Cardiac glycosides, Cholinergic agonists,



Drug may decrease:


Avoid:

Herbs with antihypertensive properties (Lexi-comp, 2013).

Increases metabolism of substrate CYP2D6 (minor) and CYP3A4 (major) (Lexi-comp, 2013).

-Treatment for anaphylaxis may be ineffective or have undesirable effects.

-Do not abruptly stop.

-Do not stop prior to non-cardiac surgery.

-Can be given without regard to meals.

-Watch glucose in diabetic patients.

-Teach patients to monitor orthostatic hypotension (Access Medicine, 2013).

Bisoprolol Fumarate oral: 5mg (30): $36.59

10mg (30): $36.59

Zebeta® oral: 5mg (30): $117.78

10mg (30): $144.60 (Lexi-comp, 2013)

Beta Blockers

Carvedilol (Coreg, Coreg CR) (Lexi-comp, 2013)

Onset: 1-2 hours

Peak: ~1-2 hours

Absorption: Rapid and extensive

Protein binding: >98 to albumin

Metabolism: Extensively hepatic via CYP2C9, 2D6, 3A4, and 2C19 in to three different metabolites; First pass effect; Plasma concentration in geriatrics and cirrhotic patient

Bioavailability: Immediate release: 25-35%; Extended release: 85%


Peak time: 5 hours

Excretion: Primarily feces (Lexi-comp, 2013).

Drug interactions:

Beta2-Agonists, Bosutinib, Floctafenine, Methacholine, pomalidomide, topotecan, and vincristine (Lexi-comp, 2013).

Increased Effect/Toxicity: Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensives, Antipsychotic agents, bosutinib, Bupivacaine, Cardiac glycosides, Cholinergic agonists, cholchine, cyclosporine, daigatran, etexilate, digoxin,

Ergot derivatives, everolimus, Fingolimod, Hypotensive agents, Insulin, Lidocaine,

Mepivacaine, Methacholine, Midodrine, p-glycoprotein/ABCB1 substrates, pomalidamide, prucalapride, RiTuximab, rivaroxaban, Sulfonylureas, topotencan, and vincristine (Lexi-comp, 2013).

Drug may decrease:


Avoid:

Herbs with antihypertensive properties or hypotensive properties (Lexi comp, 2013).

Increases metabolism of substrate CYP1A2 (minor), CYP2C9 (minor), CYP2D6 (major), CYP2E1 (minor), CYP3A4 (minor), and P-glycoprotein. Inhibits metabolism of P-glycoprotein. (Lexi-comp, 2013).

-given with food to prevent orthostatic hypotension.





-Teach patients to monitor orthostatic hypotension.

-Assess blood pressure and pulse rate before giving (Access Medicine, 2013).

Coreg CR® oral:

10mg (30): $175.36

20mg (30): $174.76

40mg (30): $175.36

80mg (30): $174.76

Carvedilol oral:

3.125mg (100): $213.40

6.25mg (100): $213.40

12.5mg (100): $213.40

25mg (100): $213.40

Coreg® oral:

3.125mg 930): $96.21

6.25mg (30): $89.71

12.5mg (30): $91.75

25mg (30)L $89.11 (Lexi-comp, 2013)

Beta Blockers

Labetalol (Trandate®) (Lexi-comp, 2013)

Onset: 20 minutes- 2 hours

Peak: 1-4 hours

Absorption: Complete

Distribution: Can cross the blood-brain barrier

Protein binding: 50%

Metabolism: Hepatic primarily via glucuronide conjugation; extensive first pass effect

Bioavailability: 25%; increased in elderly, hepatic impairment, and cimetidine use

Half-life: 6-8 hours



Drug interactions:

Beta2-agonists, Floctafenine, and Methacholine (Lexi-comp, 2013).

Increased Effect/Toxicity: Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensives, Antipsychotic agents, Bupivacaine, Cardiac glycosides, Cholinergic agonists,



Drug may decrease:


Avoid:





-Serum levels increased with food intake.



-Not removed by dialysis.

-Bradycardia more common in elderly (Access, Medicine, 2013).

Labetalol HCL oral: 100mg (100): $51.31

200mg (100): $72.79

300mg (100): $96.83

Trandate® oral:

100mg (100): $64.87

200mg (100): $126.14

300mg (100): $127.78 (Lexi-comp, 2013).

Beta Blockers

Metoprolol (Lopressor, Toprol-XL) (Lexi-comp, 2013)

Onset: 1-2 hours

Duration: Variable depending on dose

Absorption: Rapid and complete

Protein binding: ~10% to albumin

Metabolism: Extensively hepatic via CYP2D6; Extensive first pass effect.




Drug interactions:


Increased Effect/Toxicity: Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensives, Antipsychotic agents, aripiprazole, Bupivacaine, Cardiac glycosides, Cholinergic agonists,


Mepivacaine, Methacholine, Midodrine, RiTuximab, and Sulfonylureas Lexi-comp, 2013).

Drug may decrease:


Avoid:


Increases metabolism of substrate CYP2C19 (minor) and CYP2D6 (major). Inhibits metabolism of CYP2D6 (weak) (Lexi-comp, 2013).




-Food can increased absorption. Give immediate release with food. Regular release can be given without regard to meals.

-Watch glucose in diabetic patients

-Teach patients to monitor orthostatic hypotension

-May need to dose down in elderly due to bradycardia (Access Medicine, 2013).

Metoprolol Succinate ER oral: 25mg (100): $105.38

50mg (100): $105.38

100mg (100): $158.35

200mg (100): $251.95

Toprol XL® oral: 25mg (100): $143.46

50mg (30): $44.39

100mg (30): $66.13

200mg (30): $97.96

Lopressor® oral: 50mg (30): $43.02

100mg (30): $63.29

Metoprolol Tartrate oral:

25mg (100): $24.25

50mg (100): $55.50

100mg (100): $80.10 (Lexi-comp, 2013).

Beta Blockers

Nadolol (Corgard®) (Lexi-comp, 2013).

Duration: 17-24 hour

Absorption: 30-40%


Metabolism: Not metabolized



Excretion: Urine (unchanged drug) (Lexi-comp, 2013).

Drug interactions:

Beta2-agonists Floctafenine, and Methacholine (Lexi-comp, 2013).

Increased Effect/Toxicity: Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensives, Bupivacaine, Cardiac glycosides, Cholinergic agonists,



Drug may decrease:


Avoid:


Increases metabolism of substrate P-glycoprotein (Lexi-comp, 2013).




-Bradycardia may be seen more in elderly.




Corgard® oral:

20mg (100): $384.04

40mg (30): $78.48

80mg (100): $617.29

Nadolol oral:

20mg (100): $92.49

40mg (100): $108.15

80mg (100): $142.30 (Lexi-comp, 2013).

Beta Blockers

Nebivolol (Bystolic®) (Lexi-comp, 2013)

Absorption: Rapid

Protein binding: ~98% mostly to albumin

Metabolism: Hepatic via glucuronidation and CYP2D6; Extensive first pass effect.



Peak time: 1.5-4 hours

Excretion: Urine (38%), and feces (44%) (Lexi-comp, 2013).

Drug interactions:





Drug may decrease:


Avoid:


Increases metabolism of substrate CYP2D6 (minor) (Lexi-comp, 2013).







-Watch bradycardia in geriatrics (Access Medicine, 2013).

Bystolic® oral:

2.5mg (100): $267.44

5mg (100): $267.44

10mg (100): $267.44

20mg (30): $81.49 (Lexi-comp, 2013).

Beta Blockers

Penbutolol (Levatol®) (Lexi-comp, 2013)

Onset: 1.3-3 hours

Duration: >20 hours

Absorption: ~100%

Protein binding: 80-98%

Metabolism: Hepatic –oxidation and conjugation


Half-life: 5 hours



Drug interactions:

Beta2-agonists, Floctafenine, and Methacholine (Lexi-comp, 2013).




Drug may decrease:

Beta2-agnosits and Theophylline derviatives.

(Lexi-comp, 2013).






Levatol® oral: 20mg (100): $406.80 (Lexi-comp, 2013).

Beta Blockers

Pindolol (Visken®) (Lexi-comp, 2013)

Absorption: Rapid; 50-95%


Metabolism: Hepatic 60-65% to conjugates


Peak time: ~1hour

Excretion: Urine (35-40% unchanged drug), and feces (6-9%) (Lexi-comp, 2013).

Drug interactions:

Bet2-agonists, Floctafenine, and Methacholine (Lexi-comp, 2013).

Increased Effect/Toxicity: Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensives, Antipsychotic agents, aripirazole, Bupivacaine, Cardiac glycosides, Cholinergic agonists,



Drug may decrease:


Avoid:


Increases metabolism of substrate CYP2D6 (minor). Inhibits metabolism of CYP2D6 (weak) (Lexi-comp, 2013).







-Half-life is ten time longer in cirrhosis patients (Access Medicine, 2013).

Pindolol oral:

5mg (100): $103.75

10mg (100): $141.36 (Lexi-comp, 2013).

Beta Blockers

Propranolol (Inderal®, Inderal LA®, InnoPran XL®) (Lexi-comp, 2013)

Onset: 1-2 hours

Duration:6-12 hours Absorption: Rapid and complete

Protein binding: ~90%

Metabolism: Hepatic via CYP2D6 and CYP1A2 to 4-hydroxypropranolol and inactive compounds; Extensive first pass effect.




Excretion: Urine (Lexicomp, 2013).

Drug interactions:

Beta2-agonists, bosutinib, Floctafenine, Methacholine, pomalidomide, topotecan, and vincristine (Lexi-comp, 2013).

Increased Effect/Toxicity: Alpha/Beta-agonists, Alpha1-blockers, Alpha2-agnosist, Amifostine, Antihypertensives, Antipsychotic agents, aripiprazole, bosutinib, Bupivacaine, Cardiac glycosides, Cholinergic agonists,

Dabigatran, etexilate, Ergot derivatives, everolimus, Fingolimod, Hypotensive agents, Insulin, Lidocaine,

Mepivacaine, Methacholine, Midodrine, p-glycoprotein/ABCB1 substrates, pomalidomide, prucalopride, RiTuximab, rizatriptan, Sulfonylureas, topotecan, vincristine, and zolmitriptan (Lexi-comp, 2013).

Drug may decrease:

Beta2-agnosits, lacidipina, and Theophylline derviatives (Lexi-comp, 2013).

Avoid:


Increases metabolism of substrate Cyp1A2 (major), CYP2C19 (minor) CYP2D6 (major) and CYP3A4 (major). Inhibits metabolism of CYP1A2 (weak) (Lexi-comp, 2013).





-Not dialyzable.

-Bradycardia seen in hepatic impairment patients.

-Smoking decreases serum plasma levels.

-Alcohol can increase or decrease plasma levels.

-Give medication on empty stomach (Access Medicine, 2013).

Inderal LA® oral:

60mg (30): $56.35

80 mg (30): $65.39

120 mg (100): $247.03

160 mg (100): $322.78

InnoPran XL® oral:

80 mg (30): $80.00

120 mg (30): $80.00

Propranolol HCL ER oral:

60 mg (100): $132.59

80 mg (100): $154.89

120 mg (100): $192.09

160 mg (100): $251.47

Propranolol HCL oral:

10mg (100): $33.53

20mg (100): $36.30

40mg (100): $60.07

60mg (100):

$121.83

80mg (100): $63.39 (Lexi-comp, 2013).

Beta Blockers

Sotalol (Betapace®, Sorine®) (Lexi-comp, 2013).

Onset: 1-2 hours

Duration:8-16 hours

Absorption: Decreased 20-30% when given with meals

Protein binding: none

Metabolism: none

Bioavailability: 90-100%

Half-life: 12 hours

Peak time: 2.5-4 hours


Drug interactions:

Beta2-agonists, Floctafenine, floctafenine, QT prolonging agents, ivabradine, Methacholine, mifepristone, and propafenone (Lexi-comp, 2013).


Ergot derivatives, Fingolimod, QT prolonging agents, Hypotensive agents, Insulin, Lidocaine,


Drug may decrease:


Avoid:

Ephedra (Lexi-comp, 2013).




-Do not give with meals.



-Dialysis removes drug. Give dose post dialysis.

-Closely monitor QT intervals.

-Do not give to elderly (BEERS criteria) (Lexi-comp, 2013)

Betapace AF® oral: 80mg (60): $259.50

120mg (60): $346.25

160mg (60): $433.07

Betapace® oral:

80mg (100): $473.45

120mg (100): $631.76

160mg (100): $789.65

Sorine® oral:

80mg (100): $260.89

120mg (100): $346.39

160mg (100): $430.98

240mg (100): $559.97

Sotalol HCL oral:

80mg (100): $234.72

120mg (100): $322.35

160mg (100): $403.00

240mg (100): $55.59 (Lexi-comp, 2013).

Beta Blockers

Timolol (Betimol, Blocadren, Istalol, Timoptic) (Lexi-comp, 2013)

Onset: 15-45minutes

Duration:~4 hours Absorption: Rapid and almost complete


Metabolism: Hepatic via CYP2D6; Extensive first pass effect.


Half-life: 2-2.7 hours



Drug interactions:

Beta2-agonists, Floctafenine, and Methacholine (Lexi-comp, 2013)




Drug may decrease:


Increases metabolism of substrate CYP2D6 (major).inhibits metabolism of CYP2D6 (weak) (Lexi-comp, 2013).




-Can be given without regard to meals (Access Medicine, 2013).

Timolol Maleate oral:

5mg (100): $63.66

10mg (100):

$78.75

20mg (100): $145.30 (Lexi-comp, 2013).

V. Drug of Choice: Carvedilol

The recommended therapy for treating HTN and controlling HF in hemodialysis patient is the use of beta blockers (Abbott, Agodoa, Bakris, Taylor, & Trespalacios, 2004). There are several different beta blockers for use of HF but only Carvedilol was mentioned by name by the American Heart Association (AHA, 2008). Carvedilol is unique compared to the other beta blockers because it is beta blocker and an alpha blocker. This drug has a slight inverse agonist action and has a reduced negative chronotropic and inotropic effect. Carvedilol has shown to improve EF, reduce HF symptoms, increase stroke volume, stroke work, cardiac output, improved insulin sensitivity and adrenergic activity. The overall effect of Carvedilol is a reduction in mortality from all causes (DiNicolantonio, Fares, Lavie, Menezes, & O’Keefe, 2012).

An Advanced Nurse Practitioner (APN) with a current certificate to prescribe (CTP) can prescribe Carvedilol according to the Ohio Board of Nursing Formulary (Ohio Board of Nursing, 2013). When giving a beta blocker, such as Carvedilol, close initial monitoring and follow up are necessary. While guidelines encourage an ACE inhibitor and a beta blocker for HF patients, those with severe renal impairment are only given beta blockers (Abbott et al., 2004). Carvedilol is given as 3.125 mg twice daily for two weeks and then increased to 6.25 mg twice daily if tolerated. Every two weeks the dose should be double as tolerated until the highest dose with the maximal benefit is reached. For this patient the recommended maximum dose is 25 mg twice daily. This medication should be given with food to help reduce the risk of hypotension. Close monitoring of the patients heart rate and blood pressure are needed to find optimum therapy dosage until goal is achieved. Blood test including renal studies, BUN, and liver function tests should be performed before each dose increase and then yearly when optimum dose is found. Carvedilol should be taken every day for the rest of the patient’s life unless hospice or change in diagnosis is made. This drug has a slight risk for increasing renal impairment. Carvedilol is metabolized in the liver and should not be given to those with liver impairment. This drug costs from $14.99 to $25.99 for 30 tablets depending on strength (Access Medicine, 2013).

Second Diagnosis: Acute Clavicle Fracture

A 23 year old Caucasian male presents to the emergency department complaining of right clavicle pain after falling off a stage. He states he was moving the stage set when he backed up into the curtain and fell off the stage catching himself with his right arm. He is in good health. He is a college student at the local community college and is majoring in stage manager assistant. After history and physical assessment and X-rays of the right shoulder, he is diagnosed with acute right clavicle fracture non-displaced.


Acute clavicle fracture is one of the most common fractures seen in young active adults, accounting for 2.6% to 4% of all total fractures (Andriolo, Belloti, Faloppa, Gomes dos Santos, & Lenza, 2010). The Allman’s method classifies clavicle fractures into three sub groups which are: Group I- mid shaft fractures, Group II- Lateral fractures, and Group III- medial fractures. Group I (midshaft factures) account for up to 81% of all clavicle fractures and are usually displaced resulting in the need for surgery (Farsetti, Gumina, Postacchini, & Postacchini, 2010). Clavicle fractures results from a fall with an out stretched hand or from direct trauma. For non-displaced factures conservative treatment is best (Andriolo et al., 2010).

II. Therapeutic Objectives

The choice of treatment for a non-displaced clavicle fracture is placement of the arm in a sling or placing the back in a figure eight bandage. One or both of these treatments can be used to achieve stabilization of the fracture. It is recommended that the patient be immobilized for two to six weeks for adequate healing. Some patients may need arm stretching exercises after, however, this incident is low (Adriolol et al., 2010).

The second focused treatment should be pain control. Only 28-85% of all patients with a facture receive analgesic prescription and of that only 17-64% received an opioid. This statistic leaves a large number of patients who have an acute painful injury without or with poorly controlled pain management (Castelluccio et al., 2010). Patients without proper pain control and immobilization are generally more dissatisfied with their care (Farsetti, Gumina, Postacchini, & Postacchini, 2010).

III. Inventory of Effective Drug Groups Oral

Drug

Efficacy

Safety

Suitability

Non-Steroidal Anti-Inflammatory Drugs/

Acetic Acid Derivatives

Indomethacin, Tolmetin, Sulindac, Etodolac, Ketorolac, Diclofenac (Valtaren®), Nabumetone (Lexi-comp, 2013)

Pharmacodynamics:

Inhibits cyclooxygenase 1 and 2 enzyme causing decreased prostaglandin precursors. This causes an antipyretic, analgesic, and anti-inflammatory effect (Clincial Pharmacology, 2013).

Pharmacokinetics:

Absorption: Immediate release

Metabolism: Hepatic

Excretion: Urine (60-80%) and feces (9-33%) (Lexi-comp, 2013).

Side Effects:

Common:

Dyspepsia, stomach ulcers, anemia, and GI bleeding

Rare:

MI, heart failure, and hypertension

Very Rare:

Kidney and liver impairment (Lexi-comp, 2013).

Monitor:

Pain response, inflammation, weight, edema, renal function, confusion, GI effects, CBC, Liver function, and bruising (Access Medicine, 2013).

Substrate: CYP1A2 (minor), CYP2B6 (minor), CYP2C19 (minor), CYP2C8 (minor), CYP2C9 (minor), CYP2D6 (minor). Inhibits: CYP1A2 (weak) CYP2C19 (weak), CYP2E1 (weak), CYP3A4 (weak), CYP2C9 (weak), UGT1A6 (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to NSAIDs or any component, perioperative setting for CABG, advanced renal impairment, and history of proctitis or rectal bleeding (Lexi-comp, 2013).

Use Caution:

Anaphylactoid reactions, cardiovascular events, CNS effects, GI events, hematologic effects, hyperkalemia, skin reactions, visual impairments, asthma, CABG, depression, hepatic impairment, hypertension, parkinsonism, photosensitivity reaction, and renal impairment (Lexi-comp, 2013).


Cox-2 Selective

Celecoxib (Celebrex) (Lexi-comp, 2013)

Pharmacodynamics:

Inhibits prostaglandin synthesis by decreasing enzyme cyclooxygenase-2. This causes an antipyretic, analgesic, and anti-inflammatory effect (Clinical Pharmacology, 2013; Lexicomp, 2013).

Pharmacokinetics:

Absorption: Not reported

Metabolism: Hepatic via CYP2C9

Excretion: Feces (60%), urine (30%) (Lexi-comp, 2013).

Side Effects:

Common:

GI upset, diarrhea, gas, dizziness, nervousness, headache, runny nose, sore throat, and skin rash

Rare:

Chest pain, weakness, SOB, vision problems, melena, coughing up blood, weight gain, oliguria, nausea, stomach pain, anorexia, jaundice, sever skin reaction, and ecchymosis (Lexi-comp, 2013).

Monitor:

CBC, occult blood loss, liver function, renal function, pain response, blood pressure, weight gain, bruising, and GI effects (Clinical Pharmacology, 2013).

Substrate: CYP 2C9 (major), CYP3A4 (monitor). Inhibits: CYP2C8 (moderate), CYP2D6 (moderate) (Lexi-comp, 2013).

Contraindications:

Advanced renal disease, hypersensitivity to celecoxib, sulfonamides, aspirin, NSAIDs, or any component, and perioperative CABG surgery (Lexi-comp, 2013)

Use Caution:

Anaphylactiod reactions, cardiovascular events, GI events, hematologic events, skin reactions, asthma, CABG, corticosteroid-dependent disease, cytochrome P450 isoenzyme 2C9 deficiency, hepatic impairment, and renal impairment (Lexi-comp, 2013).


Enolic Acid (Oxicam) Derivatives

Piroxicam, Meloxicam (Mobic®) (Lexi-comp, 2013).

Pharmacodynamics:

Inhibits cyclooxygenase 1 and 2 enzymes which cause decreased prostaglandin precursors. This causes antipyretic, analgesic, and anti-inflammatory response (Lexi-comp, 2013).

Pharmacokinetics:

Protein Binding: 99%

Metabolism: Heptaic via CYP2C9

Half-life: 50 hours

Peak Time: Three to five hours

Excretion: Urine and feces (Lexi-comp, 2013).

Side Effects:

Common:

GI upset, diarrhea, bloating, flatulence, dizziness, nervousness, headache, rhinitis, sore throat, and skin rash

Rare:

Chest pain, weakness, headache, pruritus, severe rash, anorexia, bleeding, constipation, confusion, anxiety, depression, somnolence, perforation, vomiting, anemia, increased bleeding time, tinnitus, micturition, flu-like symptoms, falls, and angina (Clinical Pharmacology, 2013).

Monitor:

Periodic: Occult blood loss, CBC, BMP, liver function tests, and eye exams (Access Medicine, 2013).

Substrate: CYP3A4 (minor), CYP2C9 (major). Inhibits: CYP2C9 (weak) (Lexi-comp, 2013).

Contraindications:

Severe renal impairment, severe hepatic impairment, hypersensitivity or asthma reaction to piroxicam, aspirin, NSAIDs, or any component, perioperative CABG surgery, and severe heart failure (Access Medicine, 2013).

Use Caution:

Anaphylactiod reactions, cardiovascular events, CNS events, GI events, hematologic events, skin reactions, hyperkalemia, serum sickness, asthma, CABG, hepatic impairment, hypertension, and renal impairment (Lexi-comp, 2013).


Fenamic Acid Derivatives (Fenamates)

Mefenamic acid (Ponstel®), Meclofenamate (Lexi-comp, 2013)

Pharmacodynamics:

Inhibits cyclooxygenase 1 and 2 enzymes which cause decreased prostaglandin precursors. This causes antipyretic, analgesic, and anti-inflammatory response (Clinical Pharmacology, 2013; Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Rapid

Metabolism: Hepatic via CYP2C9

Excretion: Urine (52-70%) and feces (20-30%) (Lexi-comp, 2013).

Side Effects:

Common:

Headache, dizziness, itching, abdominal cramps, heartburn, nausea, vomiting, diarrhea, constipation, dyspepsia, gastritis, and bleeding

Rare:

Nervousness, itching, fluid retention, LFTs increase, and tinnitus (Lexi-comp, 2013)

Monitor:

Renal function and dehydration (Lexi-comp, 2013).

Substrate: CYP2C9 (minor). Inhibits: CYP2C9 (weak) (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to mefenamic acid, aspirin, NSAIDs, or other components, perioperative CABG surgery, GI ulcerations, and renal disease (Lexi-comp, 2013).

Use Caution:

Anaphylactoid reactions, cardiovascular effects, CNS effects, GI events, hematologic effects, hyperkalemia, skin reactions, asthma, hepatic impairment, hypertension, and renal impairment (Lexi-comp, 2013).


Propionic Acid Derivatives

Ibuprofen (Motrin®) (Children’s Motrin®), Naproxen (Aleve®, Midol®), Oxaprozin (Daypro®), Fenoprofen (Nalfon®), Ketoprofen, Nuprin, Flurbiprofen (Lexi-comp, 2013)

Pharmacodynamics:

Inhibits cyclooxygenase 1 and 2 enzymes which cause decreased prostaglandin precursors. This causes antipyretic, analgesic, and anti-inflammatory response (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Rapid

Metabolism: hepatic via oxidation

Excretion: Urine, some feces (Lexi-comp, 2013).

Side Effects:

Common:

dizziness, headache, rash, itching, heartburn, nausea, abdominal pain, anorexia, and constipation

Rare:

Edema, nervousness, fluid retention, dyspepsia, vomiting, weakness, tremor, and tinnitus (Access Medicine, 2013).

Monitor:

CBC, chemistry profile, occult blood loss, liver function tests, pain response, inflammation, weight gain, edema, bleeding, GI effects, confusion, blood pressure, urine output, and eye exams (Access Medicine, 2013).

Substrate: CYP1A2 (minor), CYP2C19 (minor), CYP2C9 (minor). Inhibits CYP2C9 (weak) (Lexi-comp, 2013).

Contraindications:

Severe hepatic impairment, anuria, oliguria, hypersensitivity to NAIDS or any component, asthma, urticarial, allergic type response, and perioperative CABG surgery (Lexi-comp, 2013)

Use Caution:

Anaphylactoid reaction, cardiovascular events, CNS effects, GI events, hematologic effects, hyperkalemia, ophthalmic events, skin reactions, aseptic meningitis, asthma, CABG surgery, hepatic impairment, hypertension, and renal impairment (Lexi-comp, 2013).


Salicylates

Acetylsalicylic acid (Aspirin®), Choline Magnesium Salicylate, Sulfasalazine, Diflunisal, Salsalate (Lexi-comp, 2013)

Pharmacodynamics:

Irreversibly inhibits cyclooxygenase 1 and 2 enzymes by acetylation causing decreased prostaglandin precursors (thromboxane A2). This causes an antipyretic, analgesic, and anti-inflammatory effect (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Rapid, stomach and small intestines

Metabolism: hydrolyzed in GI mucosa, red blood cells, synovial fluid, and blood. Hepatic conjunction.


Side Effects:

Common:

Diarrhea, headache, abdominal pain, nausea, and rhinitis

Rare:

Hypotension, tachycardia, dysrhythmias, edema, rash, angioedema, urticarial, acidosis, gastric erosions, bleeding, hepatitis, weakness, asthma, bronchospasm, and Reye’s syndrome (Access Medicine, 2013).

Monitor:

Bleeding disorders, dehydration, GI diseases, asthma, renal function, and hepatic function (Lexi-comp, 2013).

Substrate: CYP2C9 (minor) (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to salicylate, NSAIDs, or any component, asthma, rhinitis, nasal polyps, bleeding disorders, and children less than 26 years of age (Lexi-comp, 2013)

Use Caution:

Salicylate sensitivity, tinnitus, upper GI events, bleeding disorders, dehydration, ethanol use, hepatic impairment, renal impairment, alteplase, NSAIDs, elderly, children, and surgery patients (Lexi-comp, 2013).

Opioids/

Esters of Morphine

Dihydrocodeine (Synalgos®) (Lexi-comp, 2013)

Pharmacodynamics:

Bind to opiate receptors in CNS, inhibiting ascending pain pathways altering pain response. Suppresses cough by direct action in medulla (Lexi-comp, 2013).

Pharmacokinetics:


Metabolism: Hepatic

Excretion: Urine unchanged

(Lexi-comp, 2013).

Side Effects:

Common:

Lightheadedness, dizziness, drowsiness, sedation, puritus, skin reactions, nausea, vomiting, constipation, hypotension, and respiratory depression.

Rare:

Palpitations, bradycardia, increased ICP, biliary tract spasm, urinary tract spasm, and miosis (Lexi-comp, 2013).

Monitor:

Respiratory and CNS effects (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to dihsrdocodeine or any component, and pregnancy (Access Medicine, 2013).

Use Caution:

CNS depression, phenanthrene hypersensitivity, salicylate sensitivity, tinnitus, abdominal conditions, adrenal insufficiency, biliary tract impairment, bleeding disorders, CNS depression/ coma, drug abuse, ethanol use, GI diseases, head trauma, hepatic impairment, prostatic hyperplasia, renal impairment, respiratory diseases, and thyroid dysfunction (Lexi-comp, 2013).

Opioids/

Opioid Alkaloids

Codeine , Morphine (Kadian®, MS Contin®) (Lexi-comp, 2013)

Pharmacodynamics:

Bind to opiate receptors in CNS, inhibiting ascending pain pathways altering pain response. Suppresses cough by direct action in medulla (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: GI 50% Metabolism: Hepatic via UGT2B7, UGT2B4, CYP2D6,and CYP3A4; conjugated with glucuronic acid

Excretion: Urine (90%) and feces (Lexi-comp, 2013).

Side Effects:

Common:

Weight loss, constipation, diarrhea, nausea, vomiting, abdominal pain, anorexia, flushing, headache, dizziness confusion, insomnia, and abnormal dreams

Rare:

Apnea, bradycardia, stiffness, seizure, clammy skin, confusion, weakness, SOB, tachycardia, and bleeding (Access Medicine, 2013).

Monitor:

Pain relief, respiratory and mental status, blood pressure, and heart rate (Clinical Pharmacology, 2013).

Substrate: CYP2D6 (major) (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to codeine or any component, respiratory depression, acute/severe asthma, hypercarbia, or paralytic ileus (Lexi-comp, 2013)

Use Caution:

CNS depression, constipation, hypotension, phenanthrene hypersensitivity, respiratory depression, abdominal conditions, adrenal insufficiency, biliary tract impairment, CND depression/coma, drug abuse, GI obstruction, head trauma, hepatic impairment, obesity, prostatic hyperplasia, renal impairment, respiratory disease, seizure disorder, and thyroid dysfunction (Lexi-comp, 2013).

Opioids/

Semisynthetic Opioids:

Hydrocodone (Lortab®, Vicodin®, Lorcet®), Hydromorphone (Dilaudid®), Oxycodone (Oxycontin®, Roxicodone®), Oxymorphone (Opana®) (Lexi-comp, 2013)

Pharmacodynamics:

Blocks pain reception in the cerebral cortex by binding to receptor molecules in the synapses preventing pain impulses to higher centers in the brain. Mu and Kapa are two of the receptor sites that are bound (Lexi-comp, 2013).

Pharmacokinetics:


Metabolism: Hepatic: O-demethyation via CYP2D6 to hydromorphone; N-demethylation via CYP3A4 to norhydrocodone; and 40% other non-CYP pathways; via glucuronidation


Side Effects:

Common;

Hypotension, drowsiness, faint feeling, dizziness, weakness, and ill feeling

Infrequent:

Bradycardia, bronchospasm, tachycardia, SOB, confusion, vision problems, dry mouth, nervous ness, anxious, and addiction

Rare:

Depression, tinnitus, hypertension, hepatitis, itching, hallucinations, rash, thrombocytopenia, nightmares, and insomnia (Lexi-comp, 2013)

Monitor:

Pain relief, respiratory and mental status, blood pressure, liver disease, ethanol abuse, falls, and withdrawal (Access Medicine, 2013).

Substrates: CYP2D6 (minor), CYP3A4 (major) (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to semisynthetic opioids, acetaminophen, or any component, CNS depression, GI obstruction, and severe respiratory depression (Lexi-comp, 2013)

Use Caution:

CNS depression, hepatotoxicity, hypersensitivity/anaphylactic reactions, constipation, hypotension, phenanthrene hypersensitivity, respiratory depression, abdominal conditions, adrenal insufficiency, biliary tract impairment, G6PD deficiency, CYP3A4 inhibitors, CNS depression/coma, delirium tremens, drug abuse, GI obstruction, head trauma, hepatic impairment, ethanol use, obesity, prostatic hyperplasia, psychosis, renal impairment, respiratory disease, seizure disorder, and thyroid dysfunction (Lexi-comp, 2013).

Opioids/

Synthetic Opioids/

Anilidopiperidines

Fentanyl- Lozenge (Lexi-comp, 2013)

Pharmacodynamics:

Increased pain threshold, alters pain reception, and inhibits ascending pain pathways by blocking many receptor cites (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: rapid buccal, 50% saliva, and slow GI

Metabolism: Hepatic via CYP3A4

Excretion: Urine (75%), Feces (9%) (Lexi-comp, 2013).

Side Effects:

Common:

Bradycardia, CNS depression, confusion, fatigue, headache, sedation, constipation, nausea, vomiting, weakness, dyspnea, and diaphoresis.

Rare:

Edema, xerstomia, and miosis (Access Medicine, 2013).

Monitor:

Respiratory and cardiovascular status, blood pressure, pain relief, heart rate, signs of misuse, abuse, or addiction (Access Medicine, 2013).

Substrate: CYP3A4 (major). Inhibits: CTP3A4 (weak) (Lexi-comp, 2013).

Contraindications:

Severe renal or hepatic impairment and hypersensitivity to fentanyl or any component (Lexi-comp, 2013)

Use Caution:

CNS depression, opioid agonist toxicities, respiratory depression, allergic rhinitis, bradycardia, drug abuse, head trauma, hepatic impairment, oral mucositis, renal impairment, respiratory disease, CNS depressants, CYP3A4 inhibitors, and MOA inhibitors (Lexi-comp, 2013).

Opioids/

Synthetic Opioids/

Diphenylpropylamine deriveratives

Methadone (Dolophine®) (Lexi-comp, 2013)

Pharmacodynamics:

Binds to receptor sites preventing ascending pain pathways and altering pain perception (Lexi-comp, 2013)

Pharmacokinetics:

Absorption: Rapid in stomach

Metabolism: Hepatic via CYP3A4, CPY2B6, and CYP2C19


Side Effects:

Common:

Hypotension, dizziness drowsiness, dysphoria and weakness

Rare:

Arrhythmias, bradycardia, agitation, confusion, rash, decreased libido, anorxia, constipation, impotence, thrombocytopenia, vision problems, respiratory depression, and death (Lexi-comp, 2013)

Monitor:

Dependence need, QT, blood pressure, CNS and respiratory status, sedation, and falls (Access Medicine, 2013).

Substrate: CYP2B6 (major), CYP2C19 (minor), CYP2C9 (minor), CYP2D6 (minor), CYP3A4 (major). Inhibits: CYP2D6 (moderate), CYP3A4 (weak) (Lexi-comp, 2013).

Contraindications:

Severe liver disease, hypersensitivity to methadone or any component, respiratory depression, asthma, hypercarbia, paralytic ileus, or selegiline use (Lexi-comp, 2013)

Use Caution:

CNS depression, hypotension, QT prolongation, respiratory depression, abdominal conditions, anxiety disorders, adreal insufficiency, drug abuse, depression, head injury, renal impairment, and seizure disorder (Lexi-comp, 2013).

Opioids/

Synthetic Opioids/

Others

Tramadol (Ultram®), Tapentadol (Nucynta®) (Lexi-comp, 2013)

Pharmacodynamics:

Inhibits reuptake of norepinephrine and serotonin modifying ascending pain pathways while binding to u-opiate receptors blocking ascending pain pathways which alters response to pain (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Rapid and complete

Metabolism: Hepatic via CYP3A4 and CYP2B6, glucuronidation, and sulfation


Side Effects:

Common:

Flushing, dizziness, headache, insomnia, constipation, nausea, vomiting, weakness, and hypotension

Rare:

Chest pain, anxiety, confusion, and vertigo (Lexi-comp, 2013).

Monitor:

Pain relief, respiratory rate, blood pressure, pulse, sings of tolerance, abuse, or suicide (Access Medicine, 2013).

Substrates: CYP2B6 (minor), CYP2D6 (major), CYP3A4 (major), CYP2C9 (minor) (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to tramadol, opioids, or any component, intoxication, hypnotics, analgesics, opioids, psychotropic drugs, asthma, hypercapnia, and respiratory depression (Lexi-comp, 2013).

Use Caution:

Anaphylactoid reactions, CNS depression, seizures, abdominal conditions, drug abuse, ethanol use, head trauma, hepatic or renal impairment, respiratory disease, or suicide risk (Lexi-comp, 2013).

Opioids/

Synthetic Opioids/

Morphinan Derivatives

Levorphanol (Lexi-comp, 2013)

Pharmacodynamics:

Alters perception of pain by interacting with opioid receptors in the CNs and other tissues (Lexi-comp, 2013).

Pharmacokinetics:


Metabolism: Hepatic


Side Effects:

Common:

Hypotension, CNS depression, drowsiness, nausea, vomiting, constipation, and weakness

Rare:

Palpitation, bradycardia, shock, nervousness, headache, anorexia, coma, convulsion, hallucinations, diplopia, apnea, cyanosis, and dependence (Lexi-comp, 2013).

Monitor:

Pain relief, respiratory and mental status, and blood pressure (Lexi-comp, 2013).

Reduce dose with renal or hepatic impairment.

Contraindications:

Hypersensitivity to levorphanol or any component (Lexi-comp, 2013).

Use Caution:

CNS depression, hypotension, phenanthrene hypersensitivity, abdominal conditions, adrenal insufficiency, biliary tract impairment, drug abuse, head trauma, obesity, respiratory disease, or thyroid disease (Lexi-comp, 2013).

Opioids/

Synthetic Opioids/

Phenylpiperdine

Meperidine (Demerol®) (Lexi-comp, 2013)

Pharmacodynamics:

Binds to opioid receptors in the ascending pathways altering perception of pain and depressing the CNS (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Erratic and highly variable

Metabolism: Hepatic; hydrolyzed


Side Effects:

Common:

Pre-syncope, fatigue, blurred vision, confusion, vertigo, nausea, and constipation

Rare:

Bradycardia, arrest, hypotension, shock, delirium, anorexia, ileus, dyspnea, and dependence (Lexi-comp, 2013)

Monitor:

Pain relief, respiratory and metal status, blood pressure, CNS depression, seizure, and respiratory depression (Lexi-comp, 2013)

Contraindications:

Hypersensitivity to meperidine or any component, respiratory depression, and the use of a MAO inhibitor within the last 14 days (Access Medicine, 2013).

Use Caution:

CNS depression, CNS events, hypotension, abdominal conditions, adrenal insufficiency, biliary tract impairment, coma, delirium, drug abuse, head trauma, hepatic impairment, obesity, pheochromocytoma, prostatic hyperplasia, psychoses, renal impairment, respiratory depression, sickle-cell disease, tachycardia, and thyroid dysfunction (Lexi-comp, 2013)

Acetaminophen

(Tylenol®) (Lexi-comp, 2013)

Pharmacodynamics:

Inhibit synthesis of prostaglandins in the CNS. In the peripheral it blocks pain impulse generation. Inhibits hypothalamus heat-regulating center to produce antipyresis (Lexi-comp, 2013).

Pharmacokinetics:

Absorption: Variable; Primarily in small intestine

Metabolism: Primarily hepatic to sulfate and glucuronide conjugates; small amount by CYP2E1


Side Effects:

Common:

Nausea, confusion, dyspepsia, jaundice, anorexia, asthenia, and rash

Rare:

Anemia, neutropenia, ammonia increase, nephropathy, and hypersensitivity (Clinical Pharmacology, 2013; Lexi-comp, 2013)

Monitor:

Serum APAP levels, liver function tests, pain relief, and temperature (Lexi-comp, 2013).

Substrate: CYP1A2 (minor), CYP2A6 (minor), CYP2C9 (minor), CYP2D6 (minor), CYP2E1 (minor), CYP3A4 (minor). Inhibits: CYP3A4 (weak) (Lexi-comp, 2013).

Contraindications:

Hypersensitivity to acetaminophen or any component, severe hepatic impairment, and liver disease (Lexi-comp, 2013).

Use Caution:

Hepatotoxicity, anaphylactic reactions, ethanol use, G6PD deficiency, hepatic impairment, hypovolemia, and renal impairment (Lexi-comp, 2013).

IV. Effective Drug Classification: Opioid/Semisynthetic Opioids Oral

Drug Name

Efficacy

Safety

Suitability

Cost

Opioids/

Semisynthetic Opioids

Hydrocodone (Lortab®, Vicodin®, Lorcet®) (Lexi-comp, 2013)

Hydrocodone:

Onset of Action: Ten to 20 minutes

Duration: Four to eight hours

Metabolism: Hepatic: O-demethyation via CYP2D6 to hydromorphone; N-demethylation via CYP3A4 to norhydrocodone; N-demethylation via CYP#A$ to norhydrocodone and ~40% other non-CYP pathways including 6-ketosteroid reduction to 6-alpha-hydrocol and 6-beta-hydrocol

Half-life: 3.3 -4.4 hours


Acetaminophen:

Onset of action: less than one hour

Duration: Four to six hours

Absorption: Primarily small intestine; varies by dose

Protein binding: Ten to 25%

Metabolism: Hepatic to sulfate and glucuronide conjugates; small amount CYP2E1: substrate of CYP1A2 (minor), CYP2A6 (minor), CYP2C9 (minor), CYP2D6 (minor), CYP2E1 (minor), CYP3A4 (minor); inhibits CYP3A4 (weak).

Half-life: ~2 hours

Peak Time: Immediate

Excretion: Urine

(Lexi-comp, 2013).

Drug Interactions:

Azelastine, conivptan, paraldehyde, MAO inhibitors, and pimozide (Lexi-comp, 2013).

Increased Effect/ Toxicity:

Alcohol, alvimopan, aripiprazole, azelastine, busulfan, CNS depressants, dasatinib, desmopressin, imatinib, lomitapide, metyrosine, mipomersen, mirtazapine, paraldehyde, pimozide, pramipexole, prilocaine, ropinirole, rotigotine, SSRIs, sorafenib, thiazide diuretics, vitamin K antagonists, and zolpidem (Lexi-comp, 2013).

Decrease Effect/ Toxicty:

Pegvisomant, Ammonium chloride, anticonvulsants, barbiturates, carbamazepine, cholestyrmine resin, mixed agonist/ antagonist opioids, peginterferon alfa-2b, rifampin, St Johns wort, tocilizumab, and quinidine (Lexi-comp, 2013).

Avoid:

More than three alcoholic beverages, MAO inhibitors, other sedatives, and herbs (valerian, St John’s wort, SAMe, and kava kava) (Lexi-comp, 2013).

-CYP2D6 poor or extensive metabolizers may have varied effects and toxicity.

-Do not abruptly stop in chronic use. May cause withdrawal.

-High potential of abuse.

-Avoid fatty meals.

-Take one before eating or two hours after eating.

-May cause constipation.

(Access Medicine, 2013; Lexi-comp, 2013).

Hydrogesic® oral (capsules): 5-500mg (100): $25.00

Lortab® oral (elixir) 7.5-500mg/15ml: (473ml): $220.50

Hycet® oral (solution): 7.5-325/15ml (473ml): $227.77

Hydrocodone-acetaminophen oral (solution): 7.5-325mg/5ml (473ml): $139.77

7.5-500mg/15ml (471ml): %58.12

Liquicet® oral (solution): 10-500mg/15ml (473ml): $201.03

Zamicet® oral (solution) 10-325mg/15ml (473ml): $173.12

Zolivt® oral (solution): 10-300mg/15ml (473ml): $92.40

Co-Gesic® oral (tablets): 5-500mg (100): $137.58

Hydrocodone-acetaminophen oral (tablets): 2.5-500mg (40): $21.28

5-300mg (100): $191.04

5-325mg (100): $54.22

5-500mg (30): $26.65

5-500mg (30): $26.65

7.5-300mg (100): $214.27

7.5-325mg (100): $61.85

7.5-500mg (100): $57.21

7.5-650mg (100): $69.50

7.5-750mg (100): $48.92

10-300mg (100): $276.44

10-325mg (100): $83.00

10-500mg (100): $70.10

10-650mg (60): $713.80

10-660mg (100): $71.50

10-750mg : (100): $11.55

Lorcet® 10/650 (tablets): 10-650mg (20): $45.12

Lorcet® plus oral (tablets): 7.5-650mg (100): $130.45

Lortab® oral (tablets):

5-500mg (100): $103.45

7.5-500mg (12): $13.32

10-500mg (100): $138.80

Maxidone® oral:10-750mg (100): $216.85

Norco® oral (tablets):

5-325mg (15): $33.00

7.5-325mg (30): $70.56

10-325mg (30): $59.53

(Lexi-comp, 2013).

Opioids/


Hydromorphone (Dilaudid®) (Lexi-comp, 2013)

Onset of Action: 15 to 30 minutes

Duration: Three to 13 hours

Absorption: Delayed and variable

Protein Binding: Eight to 19%

Metabolism: Hepatic: via glucuronidation

Half-life: Two -11 hours

Peak Time: Less than an hour to 16 hours


Drug Interactions:

Azelastine, paraldehyde, and MAO inhibitors (Access Medicine, 2013).

Increase Effect/ Toxicity:

Alcohol, alvimopan, azelastine, CNS depressants, desmopressin, metyrosine, mirtazapine, paraldehyde, pramipexole, ropinirole, rotigotine, SSRIs, sorafenib, thiazide diuretics, zolpidem,

Amphetamines, antipsychotic agents, droperidol, hydroxyzine, magnesium sulfate, MAO inhibitors, perampanel, probenecid, sodium oxybate, and succinylcholine (Access Medicine, 2013).


Pegvisomant, Ammonium chloride, and mixed agonist/ antagonist opioids (Access Medicine, 2013).

Avoid:

MAO inhibitors, other sedatives, and herbs (valerian, gotu kola, and kava kava) (Lexi-comp, 2013).

-Do not crush, chew, dissolve or inject medication.

-May be taken with or without food.

-Alcohol can increase,

-Does not have a histamine reaction.

-Do not abruptly stop in chronic use.

-High potential of abuse. (Lexi-comp, 2013).

Dilaudid-5® oral (liquid): 1mg/ml (473ml): $239.66

Hydromorphone HCL oral (liquid): 1mg/ml (473ml): $189.12

Hydromorphone HCL rectal (suppository): 3mg (6): $73.60

Exaglo® oral (24 hour tablet): 8mg (100): $1154.06

Dilaudid® oral (tablets):

2mf (100): $109.27

4mg (100): $178.38

8mg (100): $132.00

(Lexi-comp, 2013).

Opioids/


Oxycodone (Oxycontin®, Roxicodone®) (Lexi-comp, 2013)

Onset of Action: ten to 15 minutes

Peak Effect: 0.5-1 hour

Duration: Three to 12 hours

Protein Binding: ~45%

Metabolism: Hepatic: via CYP3A4 to noroxycodone, noromorphone, and apla/beta-noroxycodol. CYP2D6 to oxymorphone, alpha/beta-oxymorphol. Substrates of CTP2D6 (minor) and CYP3A4 (major)

Half-life: Two -~ five hours


Drug Interactions:

Azelastine, conivptan, and paraldehyde (Lexi-comp, 2013).


Alcohol, alvimopan, azelastine, CNS depressants, desmopressin, metyrosine, mirtazapine, paraldehyde, pramipexole, ropinirole, rotigotine, SSRIs, thiazide diuretics, zolpidem,

Amphetamines, antipsychotic agents, conivaptan, dasatinib, droperidol, hydroxyzine, magnesium sulfate, perampanel, sodium oxybate, and succinylcholine (Lexi-comp, 2013).


Pegvisomant, Ammonium chloride, mixed agonist/ antagonist opioids, rifampin, St Johns Wort, and tocilizumab (Lexi-comp, 2013).

Avoid:

MAO inhibitors, other sedatives, and herbs (valerian, St John’s wort, and kava kava) (Lexi-comp, 2013).

-Use of CYP3A4 inhibitors with oxycodone can result in increased effects.

-Do not moisten, dissolve, cut, crush, break, or chew.

-Drink full glass of water with pills.

-Laxatives should be given to avoid constipation.


-High potential of abuse.

(Lexi-comp, 2013).

Oxycodone HCL oral (capsules):

5mg (60): $48.99

Oxycodone HCL oral (concentrate):

20mg/ml (30ml): $221.88

Oxycontin® oral (12 hour tablet):

10mg (20): $61.95

15mg (60): $209.46

20mg (20): $100.42

30mg 960): $407.50

40mg (30): $280.43

60mg (30): $395.91

80mg (60): $1022.37

Oxecta® oral (tablets):

5mg (100): $320.40

7.5mg (100): $320.40

Oxycodone HCL oral (tablets):

5mg (100): $47.94

10mg (100): $62.50

15mg (100): $75.79

20mg (90): $99.00

30mg (100): $143.90

Roxicodone® oral (tablets): 15mg (100): $175.10

30mg (90): $278.65

(Lexi-comp, 2013).

Opioids/


Oxymorphone (Opana®) (Lexi-comp, 2013)

Onset of Action: Five to ten minutes

Duration: Three to six hours

Protein Binding: ten to 12 %

Metabolism: Hepatic: via glucuronidation

Half-life: Seven to 11hours


Drug Interactions:

Azelastine, paraldehyde, and MAO inhibitors (Lexi-comp, 2013).


Alcohol, alvimopan, azelastine, CNS depressants, desmopressin, metyrosine, mipomersen, paraldehyde, pramipexole, ropinirole, rotigotine, SSRIs, sorafenib, thiazide diuretics, zolpidem,

Amphetamines, antipsychotic agents, droperidol, hydroxyzine, magnesium sulfate, MAO inhibitors, perampanel, sodium oxybate, and succinylcholine (Lexi-comp, 2013).

Deceased Effect/Toxicity:

Pegvisomant, Ammonium chloride, and, mixed agonist/ antagonist opioids (Lexi-comp, 2013).

Avoid:

Alcoholic beverages, MAO inhibitors, other sedatives, and herbs (valerian, St John’s Wort, and kava kava) (Lexi-comp, 2013).


-High potential of abuse. –Do not break, crush, dissolve, or chew.

-Use safety measures to prevent falls.

-Use laxatives to prevent constipation.

-Avoid fatty meals.

-Take one before eating or two hours after eating.

(Lexi-comp, 2013).

Opana® ER oral (12 hour tablet):

5mg (60): $143.56

7.5.mg (60): $209.60

10mg (60): $275.66

15mg (600: $382.28

20mg (60): $488.93

30mg (60): $703.73

40mg (60): $918.54

Oxymorphone HCL ER oral (tablets):

7.5mg (100): $283.52

15mg (60): $565.00

Opana® oral (tablets):

5mg (56): $215.14

10mg (100): $534.93

Oxymorphone HCL oral (tablets):

5mg (100): $294.61

10mg (100): $534.93

(Lexi-comp, 2013).

V. Drug of Choice: Hydrocodone-Acetaminophen Oral

Hydrocodone-Acetaminophen is the drug of choice for many emergency departments for treating simple acute clavicle fractures in young healthy adults. Opioids such as hydrocodone act in preventing the transmission of the pain receptive neurons by blocking the mu receptors. Among the opioids the most common prescribed are oxycodone and hydrocodone. When compared to each other, both have the same pain control effectiveness and similar side effects. Only hydrocodone showed an increase in constipation and therefore should not be given to the elderly or those with constipation difficulties. A stool softener should be prescribed in combination with the hydrocodone (Black, Buderer, Marco, Plewa, & Roberts, 2008).

Hydrocodone-acetaminophen is a relatively safe opioid for the treatment of moderate to severe pain. Thorough review of the patient’s history and physical is needed because this drug has the potential for abuse. This drug is most commonly dosed as hydrocodone 5mg and acetaminophen 500mg, one to two tablets by mouth every four to six hours as needed for pain for a maximum of seven days. Hydrocodone is a cheap medicine only costing $11.99 for thirty pills in generic form. The patient should be well educated on the proper use of taking this medication such as , do not take while driving, use with alcohol or other sedatives, and do not take with other forms of Tylenol as this may cause the patient to exceed their daily limit. Side effects of this medication are vast and should be discussed with the patient. Have the patient follow up in two weeks to ensure adequate healing (Access Medicine, 2013). An Advance Practice Nurse can prescribe this medication only with a valid Certificate to Prescribe (CPT) and they can only write for a seven day maximum in the hospital setting (Ohio Board of Nursing, 2013).

Third Diagnosis: New on Set of Epilepsy after an Subdural Hematoma

A 32 year old man develops new onset of tonic-clonic seizures one month after suffering a stable subdural hematoma (SDH) from a fall. He was witnessed to have seizure like activity this morning while getting dressed for work. He is an otherwise healthy individual who works as an accountant. While being admitted to the hospital, staff witnessed a tonic-clonic seizure. Head computed tomography (CT) showed a resolving subdural hematoma without any ischemia. After a through history and physical he is diagnosed with new onset of generalized tonic-clonic seizures after a stable SDH.


A subdural hematoma is caused by tearing of a vein in minor head injuries. It is associated with a low risk a seizure development and therefore patients are not routinely placed on anti-convulsant afterward. The seizure itself is caused by abnormal excessive or synchronous neuronal activity in the brain. A generalized tonic-clonic seizure is defined by being bilaterally distributed across both hemispheres causing loss of consciousness with ridged motor movement. The seizure is abrupt, without warning, and absent of any aura. The tonic-clonic seizure, characterized by its name, has two parts with tonic being sustained

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