NAPLEX Review 2013

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Based on the Kaplan 2013-2014 Review Book

HTN definition

SBP >140
DBP >90

What drugs can cause HTN?

NSAIDs, steroids, cyclosporine, tacrolimus, sibutramine, estrogens, EPO, venlafaxine, sympathomimetics, cocaine

Pre-HTN is....

SBP 120-139
DBP 80-89

Stage I HTN is...

SBP 140-159
DBP 90-99

Stage II HTN is...

SBP >equal 160
DBP >equal 100

Uncomplicated HTN Goal

<140/90

DM, CKD, CAD, stable/unstable angina or MI HTN Goal

<130/80

HF HTN Goal

<120/80

HF anti-HTN drug therapy

diuretic
ACEI or ARB
BB (carvedilol, metoprolol or bisoprolol)
ARA
hydralazine/isosorbide dinatrate (for AAs)

Post-MI anti-HTN drug therapy

BB
ACEI or ARB
ARA

High coronary disease risk anti-HTN drug therapy

BB
ACEI
diuretic
CCB

DM anti-HTN drug therapy

ACEI or ARB
diuretic
BB
CCB

CKD anti-HTN drug therapy

ACEI or ARB

Recurrent stroke prevent anti-HTN drug therapy

ACEI
diuretic

Thiazide Diuretics

MOA - inhibit Na reabsorption in DCT
Chlorothiazide (Diuriil), Chlorthalidone (Thalitone), HCTZ (Microzide), Indapamide (no brand), Metolazone (Zaroxolyn)

Loop Diuretics

MOA - inhibit Na reabsorption in the ascending limb of loop of Henle (only used for HTN in patients w/ renal insufficiency)
Bumetanide (Bumex), Furosemide (Lasix), Torsemide (Demadex)
Use in severe edema or HF

K-Sparing Diuretics

MOA - inhibit Na reacsorption in collecting ducts
Amiloride (no brand), Triamterene (Dyrenium)
Not used often as monotherapy
Often used w/ HCTZ to increase K loss

Aldosterone Receptor Antagonists (ARAs)

MOA - block effects of aldosterone which decreases remodeling and Na/water retention
Spironolactone (Aldactone), Eplerenone (Inspra)
Eplerenone = selective ARA so NOT endorcrine SEs!
NOT used for HTN often

Cardioselective BBs

B1 > B2 at low doses
Less likely to cause bronchoconstriction/vasoconstriction at low doses
Safer to use in pts w/ asthma, COPD, PAD, or DM
Acebutolol (Sectral), Atenolol (Tenormin), Betaxolol (Kerlone), Bisoprolol (Zebeta), Metoprolol (Tartrate is Lopressor and Succinate is Toprol XL) = BAMBA

Non-Selective BBs

Carvedilol (Coreg), Labetalol (Trandate), Nadolol (Corgard), Pindolol (no brand), Propranolol (Inderal), Timolol (Blocadren)

Intrinsic Sympathomimetic Activity BBs

Partial B-receptor AGONIST activity
Carteolol, Acebutolol, Pindolol, Penbutolol = CAPP

Lipophillic BBs

Propranolol, Metoprolol, Carvedilol, Labetalol, Pindolol
Cause CNS SEs

Hydrophillic BBs

Atenolol
Non-CNS SEs

ACEIs

MOA - inhibit ACE and prevent conversion of angiotensin I to angiotensin II which causes vasodilation and decreases aldosterone production
Inhibits degradation of BK too
-ends w/ "pril"
Benazepril (Lotensin), Captopril (Capoten), Enalapril (Vasotec), Fosinopril (Monopril), Lisinopril (Zestril/Prinivil), Moexipril (Univasc), Perindopril (Aceon), Quinapril (Accupril), Ramipril (Altace), Trandolapril (Mavik)
Decrease mortality
Decrease preload and afterload

ARBs

MOA - inhibit binding of angiotensin II to angiotensin type I receptor which causes vasodilation, decreases aldosterone production
NO EFFECT on BK
-ends w/ "sartan"
Azilsartan (Edarbi), Candesartan (Atacadan), Eprosartan (Teveten), Irbesartan (Avapro), Losartan (Cozaar), Olmesartan (Benicar), Telmisartan (Micardis), Valsartan (Diovan)

Renin Inhibitor

MOA - inhibits renin and prevents the conversion of angiotensinogen to angiotensin I which decreases production of angiotensin II
Aliskiren (Tekturna)

DHP CCBs

MOA - bind to L-type channel in heart and coronary/peripheral arteries to block inward mvmnt of Ca which causes vasodilation
Amlodipine (Norvasc), Felodipine (Plendil), Isradipine (DynaCirc CR), Nicardipine (Cardene), Nifedipine (Adalat, Afeditab, Nifediac, Nifedical, Procardia), Nisoldipine (Sular)
All have negative inotropic effects (decreased contractility) EXCEPT amlodipine and felodipine
MORE selective to vasculature than non-DHP
MORE potent vasodilators
NO EFFECT on cardiac conduction

Non-DHP CCBs

MOA - bind to L-type channel in heart and coronary/peripheral arteries to block inward mvmnt of Ca which causes vasodilation
Diltiazem (Cardizem, Cartia, Dilacor, Taztia, Tiazac), Verapamil (Calan, Covera, Isoptin, Verelan)
All have negative inotropic effects (decreased contractility) EXCEPT amlodipine and felodipine
Cause LESS PERIPHERAL vasodilation than DHP
Have NEGATIVE CHRONOTRIC properties (decreased HR)

Alpha-1 Receptor Blocks

MOA - block alpha1 receptor on PERIPHERAL bloodvessels causing arterial and venous vasodilation
Doxazosin (Cardura), prazosin (Minipress), terazosin (Hytrin)
ALLHAT trial --> 25% increase in CV events w/ doxazosin

Central alpha-2 Receptor Agonists

MOA - stimulate alpha2 receptors in BRAIN causing decreased sympathetic outflow (release of NE) which decreases BP and HR
Clonidine (Catapres), methyldopa (DOC in pregnancy - but causes liver dz in pts) (Aldomet brand name)

Direct Vasodilators

MOA - increase cGMP causing arterial vasodilation
Hydralazine (Apresoline), Minoxidil (Loniten)
Minoxidil is usually absolutely LAST line

What counseling information should you give to a patient on a diuretic?

Wear sunscreen/protective clothing (sulfa compound)
If muscle cramps occur, possible ssx of hypoK or hypoMg

When should alpha1 receptor antagonists be taken?

At bedtime - to minimize orthostatic hypotension risk

Alpha1 receptor antagonists, alpha2 receptor agonists and direct vasodilators can all cause.... as a side effect?

Orthostatic hypotension
Rise slowly from seated position to prevent

What HTN agents can be used safely in pregnancy?

Methyldopa, Labetalol, CCB

What drugs can cause increased lipids?

BBs, diuretics, steroids, isotretinoin, protease inhibitors, cyclosporine, and estrogens

What are the normal levels of TC? HDL? LDL? TG?

TC - <200
HDL - >40 or >50
LDL - <100
TG - <150
Fasting lipid profiles start at 20 yo and q5yr after

What are 5 major RISK FACTORS for CHD (coronary heart disease)?

>45 for males and >55 for females
cigarette smoking
HTN
HDL <40
Family hx of premature CHD

What is the LDL goal for someone w/ 0-1 risk factors? 2 or more risk factors? CHD or CHD-risk equivalent?

0-1 risk factors = <160
2 or more = <130
CHD or risk equiv = <100
<70 if pt has CHD, PAD, artherosclerotic aortic dz, stroke/TIA, or DM

What classes are best at lowering LDL?

Bile acid resins (15-30)
Statins (18-55)
Cholesterol absorption inhibitors (15-20)

What classes have most effect on HDL?

Niacin (15-35)
Fibric acid derivatives (10-20)

What classes have most effect on TG?

Niacin (20-50)
Fibric acid derivatives (20-50)

Bile Acid Resins

MOA - bind to bile acids in intestine --> forming insoluble complex that is excreted in feces --> decreased bile acids cause liver to convert cholesterol into bile, which decreases cholesterol stores, which increases demand for cholesterol in liver, which causes upregulation of LDL receptors, which then increases LDL clearance from blood
Cholestyramine (Prevalite, Questran), colesevelam (Welchol), colestipol (Colestid)
Admin w/ meals - place in applesauce, pudding, oatmeal, jellO, etc, but NOT in carbonated beverages
Give other meds 1 hour PRIOR or 4 hours AFTER
CI - complete biliary obstruction
cause GI SEs = give w/ fiber/fiber supplements to decrease

Fibric Acid Derivatives

MOA - increase activity of lipoprotein lipase which increases catablism of VLDL which decreases TG
Fenofibrate (Tricor), gemfibrozil (Lopid)
Admin w/ meals to decrease GI SEs

Statins

MOA - inhibits HMG-CoA reductase which prevents the conversion of HMG CoA to mevalonate (RLS in cholesterol synthesis)
Atorvastatin (Lipitor), fluvastatin (Lescol), lovastatin (Altoprev, Mevacor), pitavastatin (Livalo), pravastatin (Pravachol), simvastatin (Zocor), rosuvastatin (Crestor)
Dose HS usually but atorvastatin, rosuvastatin and pitavastatin dose anytime
Pitavastatin = lower max dose when used w/ erythromycin or rifampin and adjust dose if CrCl 15-59
rosuvastatin > atorvastatin > simvastatin > pravastatin = lovastatin = pitavastatin > fluvastatin

Systolic HF

Pumping function/contractility impaired
LVEF <40%

Diastolic HF

Impaired ability to relax --> leads to underfilling
Normal LVEF (>40%)

Left-sided HF

Pulmonary congestion
Ssx - dyspnea, cough, rales, pulmonary edema

Right-sided HF

Systemic congestion
Ssx - ascites, peripheral edema, NV, bloating

Non-pharm tx for HF

physical activity, decrease Na (< 3g/day), decrease fluid intake (< 2L/day), weight loss (if obese), EtOH restriction, and smoking cessation

What are the tx for the different stages of HF?

A/Class I - modify risk factors + control HTN, DM, CAD, and dyslipidemia --> ACEI/ARB in pts w/ risk factors for vascular dz
B/Class II - ACEI + BB
C/Class III - ACEI + BB + diuretic (may consider adding ARA if needed or digoxin) - use Bidil only if pt intolerant to ACEI or ARB
D/Class IV - chronic + inotrope therapy w/ dobutamine, milrinone, etc, heart transplant, end of life care

What are 6 IV drugs used to treat ADHF?

1. NTG - vasodilator - decreases PREload - great for pts w/ myocardial ischemia
2. Nitroprusside - vasodilator - decreases PREload and AFTERload - avoid in renal dysfx pts
3. Nesiritide (Natrecor) - vasodilator - decreases PREload and AFTERload
4. Dopamine - positive inotrope - stimulates Da, B1, and alpha1 receptors - AVOID in myocardial ischemia pts
5. Dobutamine - positive inotrope - stimulates B1 and B2 receptors - AVOID in myocardial ischemia pts and in pts w/ chronic BB therapy
6. Milrinone - positive inotrope - PDE III inhibitor which increases CO and vasodilation - good for pts on chronic BB therapy

Counseling points on diuretics (4 points)

1. Wear sunscreen/protective clothing
2. Report any muscle cramps (ssx of hypoK or hypoMg)
3. If more than once daily, last dose at 5pm to decrease nocturia
4. Weight daily and call MD if 3-5 lb weight gain/week

Class IA Antiarrhythmics

MOA - Na channel blockers - slow conduction and decrease automaticity
Disopyramide (Norpace) - A or V arrythrmias - adjust in renal dysfx
Procainamide (Pronestyl) - A or V arrhythmias - adjust in renal dysfx
Quinidine (Quinidex, Quinaglute) - A or V arrhythmias
Increase risk of TdP (Torsades) w/ other drugs that cause QT prolongation
AVOID all Class IA in pts w/ STRUCTURAL heart dz

Class IB Antiarrhythmics

MOA - Na channel blockers - little effect on conduction - decrease automaticity
Lidocaine (Xylocaine) - V arrhythmias ONLY
Mexiletine (Mexitil) - V arrhythmias ONLY
Do NOT cause TdP

Class IC Antiarrhythmics

MOA - Na channel blockers (MOST potent) - markedly slow conduction, decrease automaticity
Flecainide (Tambocor) - A and V arrhythmias - adjust in renal dysfx
Propafenone (Rythmol) - A and V arrhythmias - also NS BB properties
AVOID all Class IC in pts w/ STRUCTURAL heart dz
Do NOT cause TdP

Class II Antiarrhytmics

BBs

Class III Antiarrythmics

MOA - K channel blockers - no effect on conduction or automaticity
Amiodarone (Cordarone, Pacerone) - A and V arrhythmias - also have Na channel blocking, BB, and CCB properties - CXR performed annually, TFT and LFT q6 mo, pulmonary fx tests if pt complains of sx, eye exam if vision changes
Dronedarone (Multaq) - A arrhythmias ONLY - also have Na channel blocking, BB, and CCB properties - NOT use in severe HF
Dofetilide (Tikosyn) - A arrhythmias ONLY - adjust in renal dysfx
Ibutilide (Corvert) - A arrhythmias ONLY
Sotalol (Betapace, Sorine) - A and V arrhythmias - also have NS BB properties - adjust in renal dysfx
Amiodarone and Dronedarone are DOCs for AF pts who have HF

Class IV Antiarrhytmics

CCBs

Ischemic Heart Disease (IHD)

Lack of O2 and inadequate perfusion of the myocardium
Often due to narrowing/blockage in coronary artery

Acute Coronary Syndrome (ACS)

Caused by rupture of an atherosclerotic plaque --> forms thrombus at site of plaque rupture
Should be suspected if ischemic-like chest pain persists for >20 minutes

NSTEMI

Thrombus contains more PLATELETS than fibrin ("white clot") and does NOT completely occlude vessel
Non-ST segment elevation MI
Cardiac enzymes (+)
ECG changes = ST depression, T wave inversion, or no changes

STEMI

Thrombus contains more FIBRIN than platelets ("red clot") and OCCLUDES the vessel
ST segment elevation MI
Cardiac enzymes (+)
ECG changes = ST elevation

Unstable Angina

Cardiac enzymes (-)
ECG changes = ST depression, T wave inversion, or no changes

What is the acute management of UA/NSTEMI as well as STEMI?

1. Morphine - for chest discomfort
2. NTG - for ongoing chest discomfort - give IV NTG w/in initial 48 hours if pt continues to have ischemia or if they present w/ HF or are hypotensive
3. BBs - give w/in 1st 24 hours to pts who DO NOT have ssx of HF, risk factors for developing cardiogenic shock, 2nd or 3rd degree heart block or severe reactive airway dz
4. CCBs - non-DHP CCB is an alternative for a pt w/ a CI to BB
5. ACEI - give w/in 1st 24 hours to pts w/ pulmonary congestion or LVEF <40%
6. ASA - all pts should chew and swallow a non-EC 162-325mg ASA at ONSET of chest pain - if pt has UA or NSTEMI at any point in life..... indefinite ASA tx is a must
7. Clopidogrel - prodrug converted via CYP2C19 - give w/ ASA to pts w/ PCI or conservative tx for UA/NSTEMI - If BMS or DES (at least 12 mo of tx) and if No stent (at least 1 mo of tx) - D/C 5 days before CABG
8. Prasugrel (Effient) - achieves faster inhibitor of platelet aggregation than clopidogrel, but NOT recommended for patients 75 yo or greater - D/C 7 days before CABG
9. Ticagrelor (Brilinta) - D/C 5 days before CABG
10. Glycoprotein IIb/IIIa receptor blockers like eptifibatide or tirofiban
11. If PCI planned, give EFH or enoxaparin
12. If conservative therapy planned, give enoxaparin or fondaparinux

If STEMI, fibrolyntic therapy should be given w/in 90 minutes if unable to perform PCI w/in that time - All other meds are the same

What are some secondary prevention methods for MI?

1. ASA - indefinitely
2. Clopidogrel, prasugrel, or ticagrelor
3. BB - continue indefinitely
4. ACEI - give and continued indefinitely
5. ARAs - give if LVEF <40% and already on ACEI and BB w/ DM or HF
6. Statins - give and continued indefinitely

Glycoprotein IIb/IIIa Receptor Blockers

MOA - block glycoprotein IIb/IIIa receptor on platelets to prevent vinding of fibrinogen --> inhibits platelet aggregation
Abiciximab (ReoPro) - preferred over others in NSTEMI if significant delay to PCI
Eptifibatide (Integrilin)
Tirofiban (Aggrastat)

Anticoagulants

UFH - potentiates action of antithrombin III --> inactivates clotting factors, IIa, IXa, Xa, XIa --> ultimately prevents conversion of fibrinogen to fibrin
If platelets <100,000 or decrease by 50% once UFH started... test for HIT and d/c heparin and start direct thrombin inhibitor
LMWH - enoxaparin (lovenox) or dalteparin (fragmin) - similar MOA to UFH but mainly inhibitor factor Xa
Fondaparinux (Arixtra) - selective inhibitor of facto Xa
Bivalirudin (Angiomax) - direct thrombin inhibitor

Fibrinolytic Agents

MOA - activate and convert plasminogen into plasmin --> degrades fibrin and lyses the clot
Used ONLY if STEMI
Reteplase (rPA or Retavase)
Tenecteplase (TNK or TNKase)
Tissue plasminogen activator (tPA or Alteplase)

Which drug classes decrease mortality in pts?

ACEIs
BBs
ARAs
hydralazine/isosorbide dinitrate

Abx tx for Acute Uncomplicated Cystitis

1st line - Nitrofurantoin x 5d
2nd line - TMP/SMX DS x3d
3rd line - Fosfomycin X1 dose
Alt: FQ x3d (only when other agents can't be used) or B-lactam x3-7d (avoid unless must use)

Abx tx for Acute Pyelonephritis (Inpatient and Outpatient)

Outpatient:
1st line - Cipro 500mg BID x7d or Cipro XR 1g daily x7d or Levoflx 750mg daily x5d
2nd line - TMP/SMX DS BID x14d
3rd line - oral B-lactam x10-14d PLUS one-time dose of rocephin 1g IV or gent 5-7mg/kg IV
1st and 2nd line can also be +/- rocephin 1g IV x1dose or gent 5-7mg/kg IV x1 dose
Inpatient:
IV FQ
AMG +/- IV ampicillin
IV extended-spec ceph or PCN +/- AMG
IV carbapenem

Tx for Complicated UTI

Same abx just x10-14d

Tx for CAP (outpatient and inpatient)

Outpatient:
Macrolide or Doxy x5 or more day
If comorbidities... Macrolide (or doxy) PLUS high dose amoxicillin, augmentin, or ceph (ceftriaxone, cefuroxime, cefpodoxime)
Inpatient:
Moderate CAP --> FQ or macrolide (or doxy) PLUS ampicillin, ceftriaxone, or cefotaxime x5 or more days
Severe CAP --> FQ or azithro PLUS amp/sulbactam, ceftriaxone, or cefotaxime x5 or more days

Tx for HAP

Hospitalized <5 days:
3rd gen ceph, FQ, amp/sulb, or ertapenem x8 days (14 if pseudomonas
Hospitalized >5 days:
FQ or AMG PLUS ceftazidime or cefepime, imipenem/cilastin or meropenem, or pip/tazo x8 days (14 if pseudomonas)

Empiric Tx for Meningitis in <1 mo, 1-23 mo, 2-50 yo, and >50 yo

<1 mo = amp + AMG or amp + cefotaxime
1-23 mo = 3rd gen ceph + vanc
2-50 yo = 3rd gen ceph + vanc
>50 = 3rd gen ceph + vanc + amp
Dexamethasone may be considered for adjunctive therapy
Infants and children - usually H. influ
Adults - usually S. pneumo

Tx for Chlamydia, Gonorrhea, and Syphilis

Chlamydia = azithro 1g PO x1 dose or doxy 100mg PO q12h x7d
Gonorrhea = ceftriaxone 250mg IM x1 dose or cefixime 400mg PO x1 dose PLUS tx for chlamydia if not ruled out
Syphillis =
1, 2, or early latent syphilis (<1 yr in duration) = benzathine pen G 2.5 million units IM x1 dose
Late latent syphilis (>1 yr in duration), late syphilis of unknown duration, or 3 syphilis = benzathine pen G 2.4 million units IM once weekly x3 weeks
Neurosphyilis = aq. PCN G 3-4 million units IV or as cont infusion q4h x10-14 days

When are HIV + patients at risk for OIs?

CD4 <200

NNRTIs

MOA - bind to allosteric site on reverse transcriptase that results in a conformational change to the enzyme's active site
Efavirenz
Nevirapine
Etravirine
Rilpivirine
SE - rash and increased LFTs

Protease Inhibitors

MOA - inhibits HIV protease enzyme from processing the gag-pol polyprotein precursor, thereby preventing development and maturation of new HIV particles
Darunavir
Atazanavir
Ritonavir
-end in "navir"
SE - dyslipidemia, hepatotoxicity, GI upset

Integrase Inhibitor

MOA - inhibits integration of proviral DNA into host CD4 T-cell genome
Raltegravir
SE - increased CPK, rhabdo

Fusion Inhibitor

MOA - block conformational change in gp41 on surface of HIV that is required for HIV fusion w/ CD4
Enfuvirtide
SE - local injection site rxns (only HIV injectable drug)

CCR5 Inhibitor

MOA - acts as antagonist for CCR5 receptor (which would normally help HIV entry into CD4 cell)
Maraviroc
SE - dizziness, orthostatic hypotension

NRTIs

MOA - triPO4 moiety competes w/ natural substrates for incorporation into proviral DNA that is developed by reverse transcriptase
Tenofovir
Emtricitabine
Abacavir
Lamivudine
Zidovudine
SE - all over the place

When should HIV + pts START therapy

CD4 <500
AIDS-defining illness or hx of OI
HIV-associated nephropathy
Hep B co-infx that requires tx
Pregnancy

What are 4 preferred antiviral regimens for starting therapy in tx naïve HIV + patients?

1. Tenofovir/Emtricitabine/Efavirenz (Atripla)
2. Tenofovir/Emtricitabine/Raltegravir
3. Tenofovir/Emtricitabine/Darunavir/Ritonavir
4. Tenofovir/Emtricitabine/Atazanavir/Ritonavir

What are the initial combo regimens for antiretroviral naïve patients?

NNRTI-based regimen --> 1 NNRTI + 2 NRTIs
PI-based --> PI (plus if boosted w/ ritonavir) + 2 NRTIs
Integrase-based --> Integrase inhibitor + 2 NRTIs
CCR5-based --> CCR5 inhibitor + 2 NRTIs

What is a TB + test result on a PPD?

>5 mm = if HIV +, recent contact w/ TB dz, organ transplant pt, immunosuppressed pts, etc
>10 mm = if recent immigrant from TB infected country, injection drug users, kids <4 yo, high-risk personnel/employees, etc
>15 mm = + for anyone

After a +PPD, diagnostic test must be performed...
Confirmatory test - chest radiographs and micro exam of sputum (total of 3 samples)

What are the 4 typical TB abx tx?

Isoniazid - 9 mo duration (daily or BIW) - DOC
Isoniazid - 6 mo duration (daily or BIW) - DOC
Isoniazid + Rifapentine - 3 mo duration (once weekly)
Rifampin - 4 mo duration (daily)

Isoniazid -
MOA: inhibit mycolic acid synthesis resulting in disruption of bacterial cell wall
NO drinking EtOH - protect from light

Ethambutol SE - causes decreased red-green color perception
Used more for drug-resistant TB (or could use streptomycin - maintain adequate hydration)

Rifabutin - used in place of rifampin in HIV pts

Rifampin - if any tingling/numbness in hands/feet --> D/C and call MD

Could also use pyrazinamide, ethambutol, streptomycin, or rifabutin

Natural PCNs

MOA - inhibit bacterial cell wall synthesis
Bactericidal
Pen G (pfizerpen), Pen G benzathine (Bicillin LA), Pen G procaine (Wycillin), Pen VK (Veetids)
Pen VK - 1 hr prior or 2 hr after meals

Penicillinase-Resistant PCNs

Dicloxacillin (no brand)
Nafcillin (no brand)
Oxacillin (no brand)

Amino-PCNs

Amoxicillin (Moxatag, Amoxil)
Ampicillin (Principen)

Amino-PCNs + B-lactamase inhibitors

Amoxicillin-clavulanate (Augmentin)
Ampicillin-sulbactam (Unasyn)

Covers anaerobes too

Antipseudomonal PCNs + B-lactamase inhibitors

Piperacillin-tazobactam (Zosyn)
Ticarcillin-clavulanic acid (Timentin)

Cephalosporins

MOA - inhibit bacterial cell wall synthesis
Bactericidal
1st --> 4th, increased activity against Gram - and decreased activity against Gram +

1st = cefadroxil (Duricef), cefazolin (Ancef), Cephalexin (Keflex)

2nd = Cefaclor (Raniclor), cefotetan (cefotan), cefoxitin (mefoxin), cefprozil (cefzil), cefuroxime (ceftin or zinacef),

3rd = cefdinir (omnicef), cefixime (suprax), cefoperazone (cefobid), cefpodoxime (vantin), cefotaxime (claforan), ceftazidime (fortaz or tazicef) - covers pseudomonas, ceftibuten (cedax), ceftriaxone (rocephin)

4th = cefepime (maxipime) - pseudomonas

5th = ceftaroline (teflaro) - MRSA too

Carbapenems

MOA - Inhibit bacterial cell wall synthesis
Bactericidal
+, -, anaerobes, and pseudomonas (not ertapenem tho)
Doripenem (Doribax)
Ertapenem (Invanz)
Imipenem-cilastin (Primaxin)
Meropenem (Merrem)
SE - seizures

Aztreonam

Monobactam B-lactam
Brand - Azactam, Cayston
MOA - inhibit bacterial cell wall synthesis
Bactericidal
Gram - and pseudomonas

AMG

MOA - inhibit bacterial protein synthesis by binding to 30S ribosome
Bactericidal
CONCENTRATION dependent killing
Amikacin (amikin) - Peak 20-30; Trough <6
Gentamicin (Gentak) - Peak 4-10; Trough <1
Kanamycin (Kantrex)
Neomycin (Neo-Fradin, Neo-Rx)
Streptomycin (no brand)
Tobramycin (AKTob, TOBI) - Trough <1
Covers - mainly
Synergistic w/ PCNs and vanc
Amikacin and strep active against mycobacteria
SE - nephrotoxicity, ototoxicity

Macrolides and Ketolides

MOA - inhibit bacterial protein synthesis by binding to 50S ribosome
Bacteriostatic
Azithromycin (Zithromax, Zmax)
Clarithromycin (Biaxin)
Erythromycin (EES, EryPed, Ery-Tab, Erythrocin, PCE)
Telithromycin (Ketek)
Covers +, -, atypicals
CI - QT prolongation
Take w/ food to decrease GI SEs

Tetracyclines

MOA - inhibit bacterial protein synthesis by binding to 30S ribosome
Bacteriostatic
Demeclocycline (Declomycin) - for SIADH
Doxycycline (Doryx, Vibramycin) - acne
Minocycline (Dynacin, Minocin) - acne
Tetracycline (Sumycin) - acne
Covers +, -, and atypicals
CI - kids <8 yo

Glycylcyclines

MOA - inhibits bacterial protein synthesis by binding to 30S ribosome
Bacteriostatic
Tigecycline (Tygacil)
Covers +, MRSA
Think SE, CI, and DDI like tetracycline

Oxazolidinones

MOA - inhibits bacterial protein synthesis by binding to 23S ribosome
Bacteriostatic
Linezolid (Zyvox)
Covers +, VREF, MRSA
Monitor CBC if >2w therapy (myelosuppression)
MAOI properties - caution cheeses, wines, smoked meats, etc

Synercid

Quinupristin-dalfopristin
Class - streptogramin
MOA - inhibits protein synthesis by binding to 50S ribosome
Bactericidal
Covers +
Caution 3A4 DDI

FQ

MOA - inhibit bacterial DNA topoisomerase and gyrase --> inhibit bacterial DNA replication
Bactericidal
Ciprofloxacin (Cetraxal, Cipro)
Gemifloxacin (Factive)
Levofloxacin (Iquix, Levaquin, Quixin)
Moxifloxacin (Avelox, Moxeza, vigamox)
Ofloxacin (Floxin, Ocuflox)
Covers +, -, atypicals, cipro covers pseudomonas
CI - kids <18
SE - QT prolongation, photosensitivity, tendon rupture, seizures, hypo/hyperglycemia
Absorption decreased w/ antacids, dairy products, vitamins, etc

Sulfonamides

MOA - inhibit incorporation of PABA into DNA --> inhibits folic acid production and bacterial growth
Bacteriostatic
Sulfadiazine (only generic) - tx toxoplasmosis
TMP/SMX
Covers +, -, MRSA

Daptomycin

Brand - Cubicin
Cyclic Lipopeptide
MOA - bind to bacterial cell membranes and cause rapid depolarization --> inhibit protein, DNA, and RNA synthesis
Bactericidal
Covers +, MRSA, and VRE
CI - none
SE - N, D, infusion site rxn, muscle pain/weakness
DDI - increase myopathy w/ statins
Monitor CK weekly
Adjust dose in renal dysfx

Chloramphenicol

Brand - none
MOA - inhibits bacterial protein synthesis by binding to 50S ribosome
Bacteriostatic
Covers +, -, and VRE
CI - neonates
SE - myelosuppression, NVD, gray-baby syndrome, optic neuritis
DDI - warfarin effects increased, phenytoin effects increased, phenobarb and/or rifampin effects decreased
ONLY use for life-threatening infx
Monitor CBC frequently
Peak = 15-25
Trough 5-10

Metronidazole

Brand - Flagyl, metrogel, noritate, vandazole
MOA - interferes w/ bacterial DNA synthesis
Bactericidal
Covers anaerobes
CI - 1st trimester
SE - N, D, confusion, dizziness, peripheral neuropathy, metallic taste
DDI - disulfiram like rxn w/ EtOH
Used in 4 drug regimen for H. pylori
DOC for C. diff

Telavancin

Brand - Vibativ
MOA - inhibits bacterial cell wall synthesis
Bactericidal
Covers +, MRSA
CI - preggers
SE - QT prolongation, red-man syndrome

Vancomycin

Brand - Vancocin
MOA - inhibits bacterial cell wall synthesis
Bactericidal
Covers +, MRSA, C. diff
CI - none
SE - red-man, nephrotoxicity, ototoxicity
Bactericidal effect is TIME dependent
Trough 15-20

Azole Antifungals

MOA - inhibit synthesis of ergosterol
Fluconazole (diflucan), Itraconazole (Sporanox), Ketoconazole (Nizoral), Posaconazole (Noxafil), Voriconazole (Vfend)
Imidazoles --> butoconazole, clotrimazole, econazole, ketoconazole, miconazole, oxiconazole, sulconazole, tioconazole
Triazoles --> fluconazole, itraconazole, terconazole, posaconazole, voriconazole
SE - increased LFTs, prolonged QT interval
DDI - many CYP intx like 3A4, 2C9, 2C19, etc

Echinocandins

MOA - inhibit synthesis of 1,2-beta-d-glucan (essential to fungal cell wall)
Anidulafungin (eraxis), capsofungin (cancidas), Micafungin (mycamine)
Covers candida and aspergillus
CI - none
SE - hypoK, phlebitis, increased LFTs, etc

Amphotericin B

MOA - bind to ergosterol in cell membrane --> produce a channel in cell membrane --> allow K and Mg to leak out causing cell death (lysis)
ampho B desoxycholate (fungizone), ampho B lipid complex (Abelcet), liposomal ampho B (AmBisome), amph B colloidal dispersion (Amphotec)
Covers most all fungi
SE - nephrotoxic
Pre-med w/ APAP, NSAIDs, etc

Flucytosine

Brand - Ancobon
MOA - enters fungal cell wall --> converted into 5-FU which interferes w/ fungal RNA and protein synthesis
Covers candida and Cryptococcus
NOT for monotherapy

Griseofulvin

Brand - Grifulvin V, Gris-PEG, Fulvicin
MOA - inhibits fungal cell mitosis
Covers trichophyton
No EtOH - disulfiram like rxn
Admin w/ high-fat meal to increase absorption

HSV and Varicella-Zoster anti-viral txs

MOA - inhibit viral DNA polymerase --> inhibit replication of viral DNA
Acyclovir (zovirax), famciclovir (famvir), penciclovir (denavir), valacyclovir (Valtrex)
SE - seizures, NVD, etc
Adjust in renal dysfx

Tx for CMV (4 tx)

MOA - inhibit replication of viral DNA
Cidofovir (Vistide)
Foscarnet (Foscavir) - tx HSV too
Ganciclovir (Cytovene, Vitrasert, Zirgan)
Valganciclovir (Valcyte) - prodrug of ganciclovir
SE - nephrotoxicity, seizures, etc

Tx for Influenza (2 txs)

MOA - inhibit the enzyme (neuraminidase) responsible for releasing the newly formed mature virus from the host cell
Osteltamavir (Tamiflu) - start w/in 2 days for prophy/tx - only decreases flu severity/duration by ~1 day
Zanamivir (Relenza) - start w/in 1.5-5 days for prophy and 2 days for tx - decreases flu severity/duration by ~1 days
Tx influenza A, B, H1N1
SE - neuropsych events, HA
DDI - none

What abx cover MRSA?

Vanc
Linezolid
Tigecycline
Daptomycin
Telavancin
Ceftaroline

What abx cover Pseudomonas?

Pip/Tazo
Ticar/Clav
Aztreonam
AMG
Cipro
Ceftazidime
Cefepime
Carbapenems (except ertapenem)

What abx cover anaerobes?

Metronidazole
Clindamycin
Pip/tazo
Ticar/clav
Cefoxitin
Cefotetan
Carbapenems

What abx cause nephrotoxicity?

Streptomycin
AMGs
Vancomycin
Telavancin
Ampho B
Cidofovir
Foscarnet
Ganciclovir
Valganciclovir

What abx cause QT prolongation?

Macrolides
FQ
Telavancin
Azole antifungals

What abx cause myelosupression?

Linezolid
Chloramphenicol
Flucytosine (antifungal)
Ganciclovir
Valganciclovir

What abx are associated w/ disulfiram-like rxn?

Cefotetan (2nd gen)
Cefoperrazone (3rd gen)
Metronidazole
Griseofulvin

What abx should avoid w/ antacids or products containing di/tri-valent cations?

Ethambutol
Cefdinir (3rd gen)
Cefpodoxime (3rd gen)
Tetracyclines
FQ

What abx cause photosensitivity?

Tetracyclines
Tigecycline
FQ
Sulfonamides
Voriconazole
Griseofulvin

Hallmark features of asthma

airflow obstruction
bronchial hyperresponsiveness
airway inflammation

Inhaled steroids

DOC in asthma --> prevent remodeling, improve sx, and prevent exacerbations
Fluticasone (Flovent), Budesonide (Pulmicort), Mometasone (Asmanex), Beclomethasone (QVAR), Flunisolide (AeroBid), Triamcinolone (Azmacort), Ciclesonide (Alvesco)

Inhaled LABA

Salmeterol (Serevent - asthma), Formoterol (Foradil - asthma, Performist - COPD), Indacaterol (Arcapta - COPD)), Aformoterol (Brovana - COPD)
MOA - relaxes bronchial smooth muscles
CI - presence of tachyarrhythmias
Use in adjunct w/ corticosteroids
BBW for aformoterol - more asthma related deaths

Cromolyn and Nedocromil

Brand - cromolyn is Intal; Nedocromil is Tilade
MOA - prevents mass cells from releasing histamine and leukotrienes
Takes 4-6 weeks for full benefit

Omalizumab

Brand - Xolair
MOA - IgG mab which inhibits IgE receptor on mast cells and basophils
SQ injection

Selective leukotriene antagonists

Singulair (montelukast) and Accolate (Zariflukast)
Zariflukast must be taken on an empty stomach

Zileuton

Brand - Zyflo
MOA - 5-lipooxygenase inhibitor limits neutrophil and monocyte aggregation
CI - acute liver dz
SE - elevations in LFTs
Monitoring - LFTs baseline and q2mo, peak flow
DDI - 1A2 drugs
QID dosing is a disadvantage

Theophylline and Aminophylline

Brand - Theo-24 or Uniphyl (Theophylline) and aminophylline is available only in generic form
MOA - methylxanthine causes bronchodilation by increasing tissue concentrations of cyclic adenine monophosphate
CI - sensitivity
SE - tachycardia, N, V, CNS stimulation, theophylline toxicity
Monitoring - serum range of 5-15
DDI - 1A2 nd 3A4
Aminophylline is available only IV
Theophylline is incompatible w/ phenytoin

Inhaled SABAs

Albuterol (Ventoline, Proventil, ProAir), Levalbuterol (Xopenex), Pirbuterol (MaxAir)
MOA - relaxes bronchial smooth muscle by acting on beta-2 receptors
CI - tachyarrhythmias
SE - dose dependent

What do MDIs require?

Hand coordination and proper technique

What do DPIs require?

Requires less coordination since they are breath-actuated

What are the defining characteristics of COPD?

Persistent and largely irreversible airflow obstruction
Does NOT fluctuate like asthma
Generally progressive and associated w/ abnormal inflammatory responses
Chronic bronchitis affects the LARGER airways (BLUE BLOATER) while emphysema affects the SMALLER airways like alveolar sacs (PINK PUFFER)
Noctural sx are unusual
Stage I - mild COPD - ssx w/o airflow limitation for many years
Stage II - moderate COPD - interferes w/ daily avtivities
Stage III - severe COPD - respiratory failure, right heart failure, arterial hypoxemia
Stage IV - very severe COPD - chronic respiratory failure
Spirometry should be used to diagnose COPD
Need inhaled glucocorticoids if pt has repeated acute exacerbations
Long-acting O2 therapy is needed if pt is hypoxemic

Smoking cessation nicotine supplements

5 A's --> Ask, Advise, Assess, Assist, Arrange
Nicotene - Commit, NicoDerm, Nicorette
MOA - supplements nicotine which exhibits primary effects via autonomic ganglia stimulation
Gum - max 24 pieces/day
Inhaler - max 16 cartridges/day - protect from light
Patch - max 1 patch/day
Lozenge - max 9/day
Spray - max 80 sprays/day
CI - smoking or chewing tobacco, post-MI, life-threatening arrhythmias, worsening angina
SE - HA, mouth/throat irritation, dyspepsia, cough
Monitoring - HR, BP, nicotine toxicity
DDI - 2A4 and 2E1
Antidepressant meds may increase suicidal behavior in young adults

Roflumilast

Brand - Daliresp
MOA - inhibits PDE4 leading to an accumulation of cAMP
CI - hepatic impairment
SE - D, wt loss, N
Monitoring - liver fx, weight
DDI - Cimetidine, 3A4 inducers, ciprofloxacin, rifampin
Not for acute bronchospasms or monotherapy of COPD

Pre-diabetic fasting glucose

100-125

A1C diagonistic of DM

6.5%
ADA goals:
A1C: <7%
BG: 80-120
LDL: <100, TG <200
Exercise improve insulin sensitivity

Insulin products

Rapid Acting - aspart (Novolog), lispro (Humalog), and glulisine (Apridra) - give at time of meal
Short Acting - regular insulin (Humulin R which is OTC) - give 30 min before meal
Intermediate Acting - NPH (Humulin N which is OTC)
Long Acting - glargine (lantus), detemir (levemir)
Premixed - 75% lispro protamine/25% lispro (Humalog mix 75/25; 50% lispro protamine/50% lispro (Humalog mix 50/50); 50% aspart protamine/50% aspart (Novolog Mix 50/50); 70% aspart protamine/30% aspart (Novolog Mix 70/30); 70% NPH/30% regular (70/30 which is OTC)

Sulfonylureas

1st gen - tolbutamide (Apo-tolbutamide, orinase), Acetohexamide (Dymelor), tolazamide (tolinase), chlorpropamide (Diabinese)
2nd gen - glyburide (micronas, diabeta), glipizide (Glucotrol, Glucotrol xl), glimperide (diabenese)

Nateglinide

Brand - Starlix
MOA - stimulates insulin release from pancreatic beta cells
Amino acid derivative

Alpha-glucosidase inhibitors

Acarbose (Precose) and Miglitol (Glyset)
MOA - inhibit pancreatic alpha-amylase and alpha-glucosidases, block carbohydrate hydrolysis to glucose
CI - cirrhosis, IBD, intestinal obstruction
SE - GI issues
Monitoring - acarbose --> LFTs - both drugs measures post prandial BG and A1C
DDI - hypoglycemia w/ sulfonylulreas or insulin
Must tx hypoglycemia w/ SIMPLE CARB such as glucose

Pramlintide

Brand - Symlin
MOA - amylin cosecreted w/ insulin reduces postprandial blood sugars, prolonging gastric emptying, reducing postprandial glucagon secretion, and caloric intake thru centrally mediated appetite suppression
Amylinomimetic class
CI - gastroparesis, hypoglycemia unawareness
SE - severe hypoglycemia, N
Monitoring - hypoglycemia, BG, A1C
May delay absorption of other drugs due to increased gastric emptying time
Must reduce dose of insulin by 50% when starting Pramlintide
Administer meds 1 hour prior to use of pramlintide and exanatide

GLP-1 inhibitors

Exenatide (Byetta), Liraglutide (Victoza)
MOA - glucagon like peptide which increases insulin secretion, increases beta-cell growth/replication, slows gastric emptying, decreases food intake

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