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345 terms

NAPLEX Review 2013

Based on the Kaplan 2013-2014 Review Book
STUDY
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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
DPP-4 inhibitors
Sitagliptin (Januvia), Saxagliptin (Onglyza)
MOA - prolong the active incretin levels of GLP and GIP
Insulin storage facts
Unopened vials should be stored in fridge
If not refrigerated, use w/in 28 days - protect from heat/light
Once opened or in use, store in fridge or at room temp for 28 days
Rotate injection sites
Clear then cloudy (like regular then NPH)
NEVER mix detemir or glargine w/ anything!!!!!
Hypothyroidism
Due to an actual dz of the thyroid itself
Hashimoto's is most common or Addison's dz
TSH >20
SSx - cold intolerance, fatigue, somnolence, poor memory, depression
Tx w/ levothyroxine, liothyronine (T3 - cytomel), dessicated thyroid, or liotrix (Thyrolar - T4:T3 ratio of 4:1)
Hyperthyroidism
Grave's dz is most common cause, esp in young pts - may cause exophthalmos, plaques on skin, etc
Toxic multinodular goiter is also common cause
May be drug-induced
TSH <0.1
SSx - heat intolerance, insomnia, wt loss, weakness, palpitations, and anxiety, fine tremor, eyelid lag
Tx by either surgical intervention, anti-thyroid drugs, and/or radioactive iodine
Drugs:
MOA - inhibits synthesis of thyroid hormones by blocking oxidation of iodine in thyroid gland
Propylthiouracil (PTU) and methimazole (MMI)
Many SEs such as rashes, aplasic anemia, leukopenia, etc
PTU is preferred in pregnancy (MMI is category D)
PTU is error PRONE abbreviation - do not use on rx pads, verbally, etc
Thyroid storm
Acute life-threatening exaggeration of usual hyperthyroid sx
Polycystic Ovarian Syndrome (PCOS)
involving infertility, hirsutism, obesity, and amenorrhea
Tx anovulation + amenorrhea by combo OC (regulate/restore irregular/absent menses), wt reduction, progestin (induce menses), and insulin-sensitizing agents (metformin, to reduce insulin resistance)
Tx ovulation induction via clomiphene citrate (Clomid brand name for up to 6 mo - inhibit normal estrogen negative feedback) or w/ insulin sensitizing agents
Tx hirsutism w/ OC, antiandrogens (spironolactone, flutamide - Eulexin brand name), and insulin sensitizing agents, and eflorinthine - vaniqa brand name - cream for facial hair)
If a woman of child bearing age is placed on an insulin sensitizer.... what should we warn her about?
At increased risk for ovulation since insulin sensitizers do this
Multiple Sclerosis
Inflammation w/in brain and spinal cord that results in areas of plaque formation and sclerosis --> leads to neuro ssx
Demyelinization of sheath surrounding neurons in CNS
Disease-modifying drugs (DMDs) - should be started as soon as possible after diagnosis - must be continued indefinitely except in cases of intolerable SEs, lack of benefits, or new therapy coniderations
Acute exacerbations --> IV corticosteroids
Altering dz progression --> DMDs like interferon B1a (Avonex and Rebif), interferon B1b (Betaseron and Extavia), glatiramer acetate (Copaxone), natalizumab (Tsabri), mitoxantrone (Novantrone), fingolimod (Gilenya), and dalfampridine (Ampyra)
Refrigeration req'd - interferon agents, glatiramer acetate, natalizumab, and mitoxantrone
Interferon products and glatiramer acetate come in prefilled syringes - can also be self-administered
What are the 1st line DMDs for MS?
Interferon agents (APA and NSAIDs can decrease flu-like sx)and glatiramer acetate
Natalizumab --> reserved for those who do not respond to these therapies -- TOUCH program -- IV infusion only
Mitoxantrone --> approved to tx worsening relapsing-remitting MS and progressive MS -- BBW for cardiac risks and need for frequent LVEF monitoring -- IV infusion only
Tx w/ ONE DMD at a time
Apply ice to injection site prior to injection
Allow med to reach room temp prior to injection and rotate injection sites
Epilepsy
Partial seizures - one hemi of brain - ssx asymmetrical
Generalized seizures - both hemis - ssx symmetrical
Simple - no LOC
Complex - LOC
Absence - spacing out
Tonic-clonic - sharp muscle contractions - often preceded by an aura
MONOtherapy is preferred
What are 5 1st line agents for partial seizures?
CBZ, phenytoin, lamotrigine, valproic acid, and OxCBZ
What are 2 1st line agents for absence seizures?
Valproic acid and
ethosuximide (Zarontin) - depresses motor cortex and elevates threshold of CNS to convulsive stimuli - used ONLY for absence seizures
What are 3 1st line agents for tonic-clonic seizures
CBZ, phenytoin, and valproic acid
What is newly req'd on all AED prescribing info?
A BBW for increased suicidal ideation
Name 6 Voltage gated Na inhibitors (AEDs)
CBZ (Tegretol) - voltage gated Na channels
OxCBZ (Trileptal) - voltage sensitive Na channels
Felbamate (Felbatol) - voltage sensitive Na channels
Lamotrigine (Lamictal) - voltage sensitive Na channels
Lacosamide (Vimpat) - voltage sensitive Na channels
Topiramate (Topamax) - voltage dependent Na channels & augments GABA
Zonisamide (Zonegran) - voltage dependent Na channels - adjunct therapy
What 5 AEDs MOA involve GABA?
Gabapentin (Neurontin)
Phenobarbital (Solfoton, Luminal) - serum conc 10-40 - DOC for neonatal seizures - otherwise adjunct therapy - freq SEs limit use
Primidone (Mysoline) - serum conc 5-10 - metab to phenobarbital
Tiagabine (Gabitril) - adjunct therapy
Vigabatrin (Sabril) - irrev inhib of GABA-T - used as adjunct for refractory complex-partial seizures - BBW for ocular effects - must get thru SHARE program
When taking AEDs, what SE should be reported to MDs right away?
Any rash - due to risk for SJS
Stop taking med immediately
Parkinson's Disease (PD)
Due to depletion of DA neurons in substantia nigra of basal ganglia
SSx - tremor, rigidity, bradykinesia, postural instability, malaise, fatigue
Generally unilateral and occurring at rest = tremor
65 or great w/ signif disability - take Carbidopa/levodopa
<65, DA agonist as initial therapy
COMT inhibitors may be added to ongoing levodopa therapy, as well as amantadine or anticholinergics if needed
Caution anticholinergic agents in elderly pts w/ pre-existing cognitive impairment
DA agonist - SE of hallucinations, delusions, psych SE in general
What are the typical drugs used to manage PD?
Amantadine (Symmetrel) - antiviral agent
Selegiline (Elepryl, Emsam, Zelapar) - MAOI
Carb/Levo
L-Dopa (Larodopa) - only used to help supplement pts in need of large carb/levo therapy
Bromocriptine (Parlodel) - caution <3 SE - DA agonist
Pramipexole (Mirapex, Mirapex ER) - DA agonist
Ropinirole (Requip) - DA agonist
Rotigotine (Neupro) - patch system - DA agonist
Tolcapone (Tasmar) - COMT inhibitor - 3rd line therapy
Entacapone (Comtan) - COMT inhibitor - 3rd line therapy
Benztropine (Cogentin) - anticholinergic
Trihexyphenidyl (Artane) - anticholinergic
Rasagiline (Azilect) - MAOI
Migraines
Pain usually unilateral and pulsating
Abortive tx - analgesics (Excedrin, Fiorinal/Fioricet, Midrin), ergotamine or DHE, serotonin agonists (zolmitriptan or zomig, Naratriptan or Amerge, Rizatriptan or Maxalt, Amotriptan or Axert, Eletriptan or Relpax, or Frovatriptan or Frova), butorphanol
Serotonin agonists are DOCs - may respond to one in class, but not another so keep trying diff serotonin agonists
Prophylactic tx if two or more HA/week or >8 HA/month
What are some prophylactic migraine treatments?
HTN meds - propranolol, atenolol, metoprolol
Antidepressants - amitriptyline, paroxetine, fluoxetine, sertraline
Anticonvulsants - VPA, gabapentin, tiagabine, topiramate
All of these doses are lower than for other typical uses
Peptic Ulcer Dz (PUD)
Development of duodenal or gastric ulcers caused by either H. pylori or use of NSAIDs (or stress)
H. pylori associated --> tx w/ PPI + 2 abx (usually clarithyromycin + amoxicillin) x10-14 days
If this fails, use PPI + bismuth + metronidazole + tetracycline x 14 days
NSAID ulcer induced --> 1st line is PPI x6-8 weeks, if this fails then 2nd lines is misoprostol or H2RA
GERD
Tx w/ lifestyle modifications like dietary sx
Step 1 - antacids and OTC H2RAs... if ssx persists over 2 weeks then proceed to step 2 or contact MD
Step 2 - PPI or H2RA (at higher rx doses)
Promotility agent can be used as adj therapy
Magnesium containing OTC items can cause...?
Diarrhea
Aluminum containing OTC items can cause...?
Constipation
Ca containing OTC items too
Name 4 H2RAs
Cimetidine (Tagamet)
Famotidine (Pepcid)
Ranitidine (Zantac)
Nizatidine (Axid)
Metoclopramide
Brand - Reglan or Metozolv ODT
MOA - DA antagonists, increases LES pressure and accelerates gastric emptying
CI - seizures
SE - dizziness, sedation, D, extrapyramidal sx (EPS)
Monitoring - ssx, EPS
DDI - antipsychotic use + metoclopramide may increase risk fo EPS
Can also be used for diabetic gastroparesis (erythromycin is an alternative)
Decrease dose in renal dysfx
Misoprostol
Brand - Cytotec
MOA - prostaglandin E1 analog - replaces protective PG inhibited by NSAID therapy
ABORTIFACIENT!!!
Need preggers test before starting therapy
May be used for medical termination of pregnancy
When should a pt take PPIs?
15-30 minutes before breakfast
Ulcerative Colitis (UC)
SUPERFICIAL mucosal lesions localized to COLON and RECTUM
Can cause toxic megacolon
At risk for colorectal cancer
CONTINUOUS pattern of inflammation
Mild: >4 stools/day - no systemic signs of toxicity
Moderate: > 4 stools/day - minimal signs of toxicity
Severe: > 6 stools/day w/ blood - evidence of toxicity
Chron's Disease (CD)
TRANSMURAL lesions that can occur anywhere along the GI tract
May have abdominal mass, or fistulas/strictures
SEGMENTED (cobblestone) pattern of inflammation
Mild-Moderate: able to tolerate PO
Mod-Severe: Fail to respond to tx, significant wt loss, abdom mass/tenderness
Severe/fulminant: Persistant sx despite initiation of tx, evidence of intestinal obstruction
What are the typical tx of UC?
Mild/mod distal dz:
Active dz - topical mesalamine (enema or sup), oral aminosalicylate, topical corticosteroid
Maintenance of remisson - topical mesalamine or oral aminosalicylate

Mild/mod extensive dz:
Active dz - 1st line is PO aminosalicylate, PO steroids, azathioprine, 6-MP, infliximab
Maintenance - same (except no PO steroids)

Severe dz - infliximab, IV steroids, IV cyclosporine
What are the typical tx of CD?
Mild/mod active dz:
1st line - PO aminosalicylate, budesonide
2nd line - metronidazole or cipro

Mod/Severe dz:
1st line - prednisone
2nd line - infliximab, adalimumab, certolizumab pegol, natalizumab, MTX IM or SC

Severe/fulminant dz:
1st line - IV steroids
2nd line - IV cyclosporine or IV tacrolimus

Maintenance therapy:
1st line - azathioprine, 6-MP, MTX, infliximab, adalimumab, certolizumab pegol, or natalizumab
Names of aminosalicylates often used in CD and UC
Sulfasalazine (Azulfidine) - Tabs, and EC tabs - caution sulfa allergy - also give folic acid supplements - wear sunscreen/protective clothing - take w/ meals (GI upset) - cause orange discoloration of body fluids
Mesalamine (Apriso, Asacol, Canasa, Lialda, Pentasa, Rowasa) - CR caps, DR tabs, rectal enema, rectal suppository - admin HS so direct contact of drug w/ rectal mucosa for at least 8 hours
Olsalazine (Dipentum) - caps
Balsalazide (Colazal) - caps
Immunosuppresants and Biological Agents used in CD and UC
Azathioprine (Imuran)
6-MP (Purinethol) - active metabolite of azathioprine
Cyclosporine (Sandimmune) - only use in severe CD or UC x7-10 days
MTX (Rhematrex)
Adlimumab (Humira) - PPD should be done before starting tx - only approved for mod-severe active CD who have not responded to other tx
Certolizumab pegol (Cimzia) - PPD should be done before starting tx - only approved for mod-severe active CD who have not responded to other tx
Infliximab (Remicade) - delayed hypersensitivity rxn may occur 3-10 days after admin (pre-tx w/ antihistamines, APAP, and/or steroids) - PPD must be done before starting tx - approved for mod-severe active CD who have not responded to other tx or in UC pts who are steroid-refractory or steroid-dependent despite conventional therapy
Natalizumab (Tysabri) - TOUCH program - must be monotherapy - CD only - *associated w/ PML
Rituximab
Brand - Rituxan
Targets CD20
Also used for RA
Alemtuzumab
Brand - Campath
Targets CD52
Imatinib, Nilotinib, or Dasatinib
Tyrosine Kinase Inhibitors
Target bcr-abl fusion gene (Philadelphia chromosome)
Dasatinib brand name is Sprycel
Imatinib brand name is Gleevec
Erlotinib
Brand - Tarceva
Targets EGFR mutation
Crizotinib
Targets ALK +
Bevacizumab
Brand - Avastin
Targets VEGF
Cetuximab
Brand - Erbitux
Targets EGFR
Panitumumab
Targets EGFR
Trastuzumab
Brand - Herceptin
Targets HER2/neu and EGFR
Lapatinib
Brand - Tykerb
Targets HER2/neu and EGFR
What chemo agents cause cardiotoxicity?
Doxorubicin
Daunorubicin
Idarubicin
Mitoxantrone
Trastuzumab
What chemo agents cause severe N/V?
Cisplatin
Carboplatin
Cytarabine
Doxorubicin
Cyclophosphamide
**Give an aprepitant
What chemo agents cause mucositis?
Cytarabine
Cyclophosphamide
5-FU
MTX
What chemo agents cause neuropathy?
Vincristine
Vinblastine
Oxaliplatin
Paclitaxel
What agents cause renal dysfx?
Cisplatin
Cyclophosphamide
Ifosfamide
What agents cause pulmonary fibrosis?
Bleomycin
Busulfan
What agents cause infusion rxns?
All mabs
Paclitaxel
Ibritumomab tiuxetan
Brand - Zevalin
Targets CD-20
Contain radioactive isotope**
Tositumumab
Brand - Bexxar
Targets CD-20
Contain radioactive isotope**
Sunitinib
Brand - Sutent
Targets VEGF
Sorafenib
Brand - Nexavar
Targets VEGF
ANC
Normal: 3000-7000
Mild neutropenia: 500-1000
Moderate: 100-500
Severe: <100
May give a CSF like filgrastim to shorten duration of neutropenia
Antiemetic Drugs used in chemo
Ondansetron (Zofran), Granisetron (Kytril), Dolasetron (Anzemet), Palonosetron (Aloxi) - 5HT3 antagonists
Aprepitant (Emend) - NK-1 antagonists
Dexamethasone (Decadron), Methylprednisolone (Solumedrol) - steroids - help 5HT3 antagonists
Metoclopramide (Reglan) - DA-2 antagonists
Leucovorin is a rescue agent for pts receiving what drug?
MTX
Enhances effects of 5-FU
What are 1st line agents for depression?
SSRI
Req 6-8 weeks for adequate trial
What SSRI has lower incidence of sexual SEs?
Bupropion
What must ALL antidepressants have on the labeling?
BBW - suicidality
TCAs
Amitripytline (Elavil), Amoxapine (Ascendin), Comipramine (Anafranil), Desipramine (Norpramin), Doxepin (Sinequan, Prudoxin, Zonalon), Imipramine (Tofranil), Nortiptyline (Pamelor or Aventyl), Protriptyline (Vivactil), Trimipramine (Surmontil)
Avoid dispensing large quantities b/c very dangerous in OD situations!!!
MAOIs
MOA - increase EPI, NE, DA, and serotonin
Isocarboxazid (Marplan), Phenelzine (Nardil), Tranylcypromine (Parnate), Selegiline (Emsam)
Used infreq due to LOTS of SEs
What are some 1st line tx for acute manic episodes?
Lithium, valproate, aripiprazole, queitapine, risperidone, ziprasidone, olanzapine, or CBZ
What are some 1st line tx for acute depressive episodes?
Lamotrigine monotherapy or lamotrigine + antimania tx
Name some atypical antipsychotics
Risperidone (Risperdal), ziprasidone (Geodon), lurasidone (Latuda), clozapine (Cloazril or FazaClo)
Name some typical antipsychotics and MOA
Phenothiazines: MOA - block postsynaptic mesolimbic DA receptors in brain
Chlorpromazine (Thorazine) - false + on preggers possible
fluphenazine (Prolixin)
Perphenazine (none)
Trifluperazine (none) - false + on preggers possible Prochlorperazine (Compazine or Compro supp) - false + on preggers possible
Thioridazine (none) - BBW for altered <3 fx

Haloperidal (Haldol, Haldol deconade inj): MOA - not well known, blocks DA brain receptors

Pimozide (orap): MOA - potent, centrally acting DA antagonist - FDA labeled for Tourette's

Loxapine (loxitane): MOA - blocks postsynaptic mesolimbic D1 and D2 brain receptors and blocks serotonin activity - false + in preggers possible - use w/ EXTREME caution in thyroid dz

Molindone (Moban): MOA - effects ascending reticular activating system

Thiothixen (Navane): MOA - black postsynaptic DA receptors - may cause false + preggers

MOA: mixed and varied D2/serotonin antagonist activity
aripiprazole (abilify), olanzapine (zyprexa), paliperidone (invega), quetiapine (Seroquel), iloperidone (fanapt), asenapine (saphris)

Atypical:
Lurasideon (Latuda) - MOA: mixed D2 and serotonin antagonist
Why are atypical antipsych better than typicals?
Fewer EPS
Have greater metabolic side effect risks though like wt gain, high BG, HLD
Alzheimer's Disease (AD)
Dementia of progressive nature that affects cognition and eventually behavior and functional status
Pathophys not fully understood

Mild-Mod Tx: Cholinesterase inhibitors
Donepezil (Aricept), Galantamine (Razadyne) - lots of fluids and w/ food, Rivastigmine (Exelon)
Mod-Severe Tx: NMDA receptor agonist (Memantine)
Osteoarthritis (OA)
Dz of cartilage destruction and formation w/ subsequent bony proliferation w/in joint

1st line tx: Scheduled APAP w/ max of 4g/day

2nd line tx: NSAIDs
ASA, salsalate , diflunisal, etodolac, diclofenac, indomethacin (Indocin - good for gout), ketorolac (toradol), nabumetone (Relafen), fenoprofen (Nalfon), Flurbiprofen (Ansaid), IBU, Ketoprofen (Orudis, Oruvail, Rhodis, Apo-Keto-E), naproxen, oxaprozin (daypro), meclofenamate, piroxicam (feldene), meloxicam (Mobic)

3rd line tx: Narcotics or hyaluronate injs
Vicodin, Tylenol #3, Morphine, Percocet
Hyaluronate inj (Synvisc or Synvisc-One) - IA injections

Adjunctive therapy: Topical capsaicin cream (used reg x2w for max effect) or glucosamine
Rheumatoid Arthritis (RA)
Autoimmune dz
Chronic inflammation of the synovial tissue lining the joint capsule
DMARDs should be initiated w/in 3 mo of dx --> examples are Leflunomide (arava) - PO DMARD w/ low risk of bone marrow toxicity - highly teratogenic
sulfasalazine (azulfidine) - serious warfarin DDI so monitor INR closely
hydroxychloroquine (plaquenil) - eye SEs,
MTX

Steroids are adjunctive agents

Biologic agents are used when initial DMARD has been demonstrated as ineffective as monotherapy
etanercept (Enbrel) - refregierate prior to use, self-admin OK, d/c temp if infx occurs, used alone or +MTX - prefilled syringe via SC
infliximab (remicade) - ALWAYS +MTX, IV infusion
adalimumab (humira) - caution in HF pts, d/c during serious infx, used along or +MTX, prefilled syringe via SC
Anakinra (Kineret) - alone or +MTX, prefilled syringe via SC
Tocilizumab (Actmera) - d/c if serious infx, NOT live vaccines, along or +MTX, used in pts that have failed 1 or more TNF agents (adalimumab, infliximab, etanercept, golimumab), IV infusion
Golimumab (simponi) - SC q month, +MTX, caution in HF pts, refrigerate, prefilled syringe via SC
Abatacept (Orencia) - NOT to be given w/ TNF antagonists or live vaccines, d/c if serious infx, along or +MTX, infx likely in COPD pts so caution, IV infusion
Which RA agents should be refrigerated?
MTX inj, etanercept, infliximab, adalimumab, anakinra, golimumab
Osteoporosis
Low bone mass - increased fragility of bone and subsequent increased risk of fracture
T-score > -1 = normal
-1 to -2.5 = osteopenia
< -2.5 = osteoporosis

Need to be on PO calcium + Vit D

1st line tx - bisphosphonates
alendronate, risedronate, ibandronate, zoledronic acid (reclast) - IV infusion once a year and refrigerate prior to use
PO bisphosphonate use should be shared w/ dentist due to low risk for osteonecrosis of jaw

If CI to bisphosphonates - take raloxifene

3rd line tx - calcitonin (not great evidence supporting use) - brand name miacalcin nasal spray or SC or IM- refrigerate b4 use then keep at room temp while in use and discard after 30 days of 1st spray

Teraparatide (forteo)- PTH agonist - tx of osteoporosis if pts w/ hx of fracture secondary to osteoporosis and have multiple risk factors for fracture OR if pt intolerant to bisphosphonate tx - prefilled syringe should be refrigerated - discard after 28 days of use

Denosumab (prolia) - 2nd line therapy in Postmenopausal females at high risk for fracture - refrigerate - inj by healthcare professional - once at room temp for inj discard after 14 days
Gout
Deposits of monosodium urate crystals in the synovial fluid and/or tissues and is most often associated w/ hyperuricemia

1st line - NSAIDs
Indomethacin (Indocin) most common

CI to NSAID
Acute tx (gout ssx <48 hours) - colchicine
NEVER use allopurinol or febuxostat in acute tx - only for chronic prophylactic tx

Chronic tx (>48 hours) - steroids
When starting prophylactic therapy, start colchicine w/ allopurinol/febuxostat/sulfinpyrazone/probenecid x3-6 mo to avoid causing an exacerbation

Refractory chronic gout - use pegloticase (krystexxa) w/ pre-tx w/ antihistamines and steroids
Glaucoma
Damage to an area of optic nerve (optic disk) --> results in loss of visual sensitivity and field
Open-angle - most common - due to genetics, trauma, surgery, or meds
Closed-angle - increased intraocular pressure (IOP)
Ssx - blind spots, reduced peripheral vision, changes in color perception

1st line - BBs as follows...
Betaxolol (betopic), carteolol, levobunolol (AKBeta, Betagan), Metipranolol (OptiPranolol), Timolol (Timoptic, Betimol, Isatol)
or PG analogs...
Bimatoprost (lumagin), latanoprost (xalantan), tafluprost (zioptan), travoprost (travatan Z)

2nd line - alpha2 agonists...
apraclonidine (iopidine), brimonidine (alphagan P)
OR topical carbonic anhydrase inhibitors...
brinzolamide (azopt), dorzolamide (trusopt)

3rd line - cholinergic agents (increased SEs)
carbachol (isopto carbachol), pilocarpine (isopto carpine or pilopine HS)
Laser or surgical procedures may be considered
What is the generic name for Combigan? Cosopt?
Combigan - timolol/brimonidine
Cosopt - timolol/dorzolamide
Counseling info if pt is on more than 1 eye drop?
Separate drops by 10 minutes
What type of eye drop class causes pigmentation changes in iris, eyelid, and eyelashes?
PG analogs
Carbonic anhydrase inhibitors should NOT be used if patient has ________ allergy?
Sulfa
Iron Deficiency Anemia (IDA)
Aka microcytic anemia
Usually caused by some form of blood loss

PO iron supplement is 1st line therapy - may take up to 4 months for iron stores to return to normal
GI absorption of elemental iron is enhanced in presence of an acidic gastric environment --> take w/ ascorbic acid
Take iron 2 hours BEFORE or 4 hours AFTER antacids
Iron can be constipating so pt may need laxatives, stool softener, adequate fluids

Pts sometimes exhibit pica
A transfusion should be given if Hgb is less than _____? When should a patient receive IV?
<10

chronic uncorrectable bleeding, intestinal malabsorption, intolerance to PO iron, Hgb <6
Anemia of CKD
Due to decreased endogenous EPO production (kidneys aren't working properly)
Esp if CrCl <50

EPO stimulating agents may be given and are the DOC
Epoetin alfa (Procrit), Darbepoetin alga (Aranesp)
Store in fridge, stable for 1w at room temp
Admin by IV infusion or inj
Avoid EtOH and check BP frequently

Hgb should NOT be >13 due to the all-case mortality and adverse <3 events in pts w/ CKD
Pernicious Anemia
Type of megaloblastic anemia - RBC larger than normal
Decrease in RBC when body cannot properly absorb Vitamin B12 from the GI tract
B12 is necessary for the formation of RBCs

Tx w/ Vitamin B12 IM injections and then move to PO injections
Cyanocobalamin folate (B12) - daily inj x1w then monthly - IN spray must be refrigerated
or folic acid (folate)

Often requires tx for life
Long-term Metformin therapy can decrease the absorption of what Vitamin?
B12 --> causing pernicious anemia
Acne Vulgaris
1st line -
mild-mod: topical benzoyl peroxide
mod: topical abx and topical retinoids
mod-severe: topical therapy + PO abx
severe, inflammatory: PO abx, topical therapy, and often PO isotretinoin therapy

2nd line -
mild-mod: topical abx and topical retinoids
Isotretinoin
Brand - Accutane
Females must agree to at least TWO forms of contraception during therapy
Tx of severe, inflammatory acne

iPLEDGE program - pts, pharmacies, MDs, and wholesalers
Psoriasis
Chronic inflame skin dz associated w/ silvery scalelike lesions
Sharp, demarcated, erythematous papules and plaques
Psoriatic arthritis refers to secondary joint inflame in pts w/ psoriasis

1st line - topical agents such as emollients and keratolytics (salicylic acid or sulfur), coal tar, anthralin, calcipotrien, or retinoids

Systemic therapy is 1st line in SEVERE cases or is 2nd line in pts not responding to topical - antimetabolite therapy (MTX, cyclosporine, tacrolimus), PO steroids, psoralens, immunosuppressants or retinoids
What are the antidotes for opioid toxicity?
Naloxone (Narcan)
Nalmefene (Revex)
Naltrexone (Trexan) - stored in fridge, kept at room temp <7 days prior to use is OK
What is the antidote for BZD toxicity?
Flumazenil (Romazicon)
What is the antidote for EtOH, methanol or ethylene glycol poisoning?
Fomepizole (Antizol)
If soln becomes solid in vial, warm carefully by running warm H2O over vial
What is the antidote for anticholinergic toxicity?
Physostigmine (Eserine)
What is the antidote for digoxin toxicity?
Digoxin Immune Fab (Digibind)
Refrigerated
What is the antidote for isophosphamide or cyclophosphamide toxicity?
Mesna (Mesnex)
What is the antidote for doxorubicin toxicity?
Dexrazoxane (Zinecard)
What is the antidote for cisplatin toxicity?
Amifostine (Ethyol)
What is the antidote for heparin toxicity/OD?
Protamine
Refrigerate, stable x2 weeks at room temp
NOT interchangeable w/ Vitamin K
What is the antidote for warfarin OD/toxicity?
Vitamin K or phytonadione (Mephyton)
Avoid IM route due to hematoma formation
NOT interchangeable w/ protamine
What is the antidote for MTX toxicity?
Leucovorin
What is the antidote for leflunomide toxicity?
Cholestyramine resin (binds to toxic agent)
What is the antidote for APAP toxicity?
Acetylcysteine (Acetadote, Mucomyst)
What is the antidote for cholinergic toxicity?
Atropine (AtroPen)
What do we give in an anaphylactic rxn?
Epinephrine (Adrenalin, EpiPen, Twiniject)
What do we give to reverse severe hypoglycemia?
Glucagon (GlycaGen)
Then give IV dextrose as soon as available
Estrogen
Suppresses FSH and prevents development of viable follicle
Progestin
Produces thick cervical mucus and the involution of the endometrium and blocks ovulation

Safe in...
breastfeeding, >35 yo, have lupus, or have intolerable estrogen related SEs

STRICT compliance is a MUST
Higher incidence of breakthrough bleeding
Need back up contraception w/ ANY missed pill
What are the available OC therapies?
Estrogen + Progestin
Monophasic (high dose estrogen, low dose estrogen)
Multiphasic (Biphasic, Triphasic, Four-phasic)

Progestin Only
Emergency Contraception
Start w/in 72 hours
OTC for >18 yo

Plan B - 2 tabs of 0.75mg levonorgestrel (taken q12h x2 doses)

Preven - 0.25mg levonorgestrel, 0.05mg ethinyl estradiol (taken q12h x2 doses)

Plan B One Step - 1 tab, levonorgestrel 1.5mg

Ella (RX only) - uliprastal acetate 30mg by mouth w/in 120 hours
What are the monophasic, high-dose estrogen OCs?
Ethinyl estradiol/norgestrel (Ovral, Ogestrel)

EE/ethynodiol diacetate (Demulen, Zovia)

mestranol/NE (Ortho-Novum, Necon, Norinyl)

All have 50mcg of estrogen
What are the monophasic, low-dose estrogen OCs?
EE/levonorgestrel (Alesse, Avaine, Lessina, Levlite) - 20mcg estrogen

EE/levonorgestrel (Levlen, Levora, Nordette, Portia, Seasonale, Lo Ovral, Low-Ogestrel) - 30mcg estrogen

EE/drospirenone (Yasmin, Yaz, Beyaz, Safyral) - 30mcg estrogen

EE/norgestrel (Apri, Deogen, Ortho-Cept) - 30 mcg estrogen

EE/norethindrone acetate (Loestrin, Microgestin, Lo Loestrin) - 10 to 20 mcg estrogen

EE/norethindrone (Ovcon, Brevicon, Modicon, Neocon, Nortrel, Norinyl, Ortho-Novum) - 35 mcg estrogen

EE/desogestrel (Kariva, Mircette) - 10 to 20 mcg estrogen

EE/norgestimate (Ortho cyclen, sprintec, mononessa, previfem) - 35 mcg estrogen
What are the biphasic OCs?
EE/norethindrone (Ortho-Novum 10/11 and Necon 10/11)
35 mcg estrogen
Created to decrease overall hormone exposure - high breakthrough bleeding SE
What are the triphasic OCs?
EE/norethindrone (Tri-Norinyl, Necon 777, Ortho Novum 777, Esrostep) - 35 mcg estrogen

EE/desogestrel (Cyclessa) - 35 mcg estrogen

EE/norgestimate (Trinessa, Ortho TriCyclen, Ortho TriCyclen Lo - 35 mcg estrogen

EE/levonorgestrel (Enpresse, Tri-Levlen, Triphasil, Trivora) - 35 mcg estrogen
What are the four-phasic OCs?
estradiol valerate/dienogest (Natazia)
ONLY 4 phasic option available
Increased efficacy for heavy menstrual bleeding
What are the progestin-only OCs?
Norethindrone (Ortho Micronor, Errin, Nor-QD, Nora-BE, Camila) - 0.35mg progestin

Norgestrel (Overette) - 0.075mg progestin

Medroxyprogesterone (Depo-Provera) - IM q12 w - 150mg/mL progestin
What are the implantable/intrauterine contraception options?
Levonorgestrel (Norplant) - not available as new therapy - upper arm
Levonorgestrel (Mirena) - Intrauterine
Progesterone (Progestasert) - Intrauterine
Etonorgestrel (Implanon) - upper arm
Missed OC pills.....
1?
2 (during 1st two weeks)?
2 (during 3rd week)?
3 or more?
1 pill - take missed dose immediately and next dose at regular time

2 (1st two weeks) - take 2 doses daily for next 2 days, then resume normal

2 (3rd week) and 3 or more - Take one dose until Sunday (start day), dispose of current pack, then begin next pack w/o placebo pills - BUM req x7 days
What is the primary indication for HRT?
hot flashes and night sweats

If only vaginal sx, local vaginal therapy is OK (lubricants)
Women receiving HRT with an intact uterus, should be on what?
PROGESTIN!!!!!
PDE5 inhibitor use is CI when taking.....?
Nitrates!
Due to significant, dangerous hypotension
In ED, if a PDE5 inhibitor PO does not work.... what's the next option?
Alprostadil intra-urethral (Muse) or Alprostadil intra-cavernosal (Caverject, Edex)
Stress Incontinence
Urethral underactivity
Tx w/ topical estrogen, alpha agonsits (PSE or PE), or TCA
Urge Incontinence
Bladder overactivity
Tx w/ anticholinergics (oxybutynin, tolterodine, darifenacin, solifenacin, fesoterodine) or imipramine (TCA)
Overflow Incontinence
Urethral overactivity or Bladder underactivity

If 2nd to BPH - tx w/ alpha antagonist
NS are doxazosin, terazosin, prazosin while selective alpha 1A are tamsulosin, alfuzosin, silodosin
OR 5alpha reductase inhibitor (finasteride, dutasteride) - reserved for pts w/ severely enlarged prostates
When should alpha blockers be taken?
HS - to avoid SEs of syncope and orthostasis while awake
Make sure to rise slowly from seated/laying position
What are the adverse effects of estrogen excess? deficiency?
EXCESS - breast tenderness, cyclic wt gain, edema, bloating, HTN, migraine, N

DEFICIENCY - hot flashes, spotting, decreased libido
What are the adverse effects of progestin excess? deficiency?
EXCESS - decreased libido, depression, fatigue, wt gain, acne, hypomenorrhea, vaginal candidiasis

DEFICIENCY - heavy bleeding, wt loss, delayed menses, spotting
What are the therapeutic concentrations of AMG? Vancomycin?
Gent, Tobra: peak 5-10 and trough <2
Amikacin: peak 15-30 and trough <10
Vanc: peak 20-40 and trough 5-10
What are the therapeutic concentrations of Phenytoin? CBZ? VPA? Phenobarbital/Primidone? Ethosuximide? Lithium?
Phenytoin: 10-20 (correct if hypoAlb)
CBZ: 4-12
VPA: 50-100
Phenobarb: 15-40
Ethosux: 40-100
Lithium: 0.6-1.4
What are the therapeutic concentrations of Digoxin? Cyclosporine? Theophylline?
Dig: 0.5-1.5 for inotropic effects or 0.8-2.0 for chronotropic effects
Cyclo: 150-400
Theophy: 10-20
Saw Palmetto
BPH
CoEnzyme Q10
CV dz
May help w/ myalgias due to statin therapy
Black Cohosh
Women's health problems like menospause or painful periods
Ginseng
DM
Help decrease mental/physical stress (suppose to)
What are some CI for decongestant use?
Fever >101.5
Chest pain
SOB
HTN, arrhythmias, insomnia, anxiety
Worsening sx after self-tx
Concurrent underlying chronic cardiopulm dz
AIDs or chronic immunosupp therapy
Frail pts of advanced age
Kids <2 yo
Current MAOI and/or TCA
How long is it OK to use topical decongestants?
3-5 days only
Otherwise may get rebound congestion

Ex. oxymetazoline (Afrin) or Naphazoline (Naphcon)
What are he different histamine receptors and what does each do?
H1 - produces sneezing, pruritus, and mucus production

H2 - stomach acid production

H3 - control synthesis and release of histamine
Are 1st or 2nd gen antihistamines more sedating? Why?
1st gen - cross the BBB so cause sedative effect

1st gen ex --> clemastine, chlorphenirmine, brompheniramine, diphenhydramine, doxylamine, fexofenadine (caution QT prolongation in allergra)

2nd gen ex --> loraatadine, cetirizine, azelastine
Contact dermatitis
Mild soap + H2O
Tx - topical tx w/ hydrocortisone, bicarb pastes, and antihistamines
Athlete's Foot
Apply thin layer x2 weeks even after ssx disappear
Butenafine (Lotrimin Ultra or Mentax) and Terbinafine (Lamisil)
Clotimazole (Lotrimin) and Miconazole (Micatin) - plus candida coverage
Tolnaftate (Tinactin)
Undecylenic Acid (Cruex, Fungi-Nail, Blis-To-Sol) - plus candida coverage
What are some common meds that cause constipation?
Anticholinergics, analgesics, BZD, sucralafate, CCB

Also occur due to menopause, dehydration, psych conditions, depression, etc
Ionized Drug
MORE soluble
Can NOT cross body membranes
Unionized Drug
Less soluble
CROSS body membranes OK
pH > pKa then an acid is ____ and base is _____.
Acid - more ionized
Base - more UN ionized
pH < pKa then acid is _____ and base is ______.
Acid - more UN ionized
Base - more ionized
Forms of Weak ACIDS
Na, Ca, K, or other cationic salts
Forms of Weak BASES
HCl, or other anionic salts
Hydrolysis
Presence of H2O
Oxidation
Presence of O2
Results in insoluble precipitates or colored cmpds
Photochemical Decompensation
Occurs due to light exposure
Results in colored cmpds
Crystalline Solids
Definite melting points
Less soluble
Solids tend to revert to this state on storage
Amorphous Solids
Melt over a range of temps
MORE soluble
Liniments
Alcoholic soln used to IRRITATE skin and relieve more deep seated pain or discomfort
Apply by rubbing and are NOT suitable for app to bruised or broken skin
Collodions
Contain pyroxylin in an alcohol/ether base that evaporates, leaving an occlusive film on the skin
Holds edges of wounds together
5 Ointment Bases
1. hydrocarbon/oleaginous - greasy, petroleum based (Vaseline)
2. anhydrous - greasy product that form W/O emulsion - used to incorporate soln into otherwise lipophilic bases
3. W/O emulsion - contain some H2O (Lanolin, cold cream)
4. O/W emulsion (water removable) - creamy emulsions that are easily washed from skin
5. Water-soluble - greaseless, water washable bases - Can NOT add large amts of H2O or will soften too much
Creams
Emulsion Bases
Soft, cosmetically acceptable topical products
Pastes
Very thick
Gels
Jelly-like
Water soluble, water washable, and greaseless
Nebulizers
Allow drug to be delivered directly to lung in HIGH concentrations and w/o use or propellant
Useful for uncoordinated or unabled pts
Protein drugs can be given via what routes?
Inj or pulmonary routes ONLY
_____, ______ drugs DISSOLVE more readily while _____, ______ drugs are ABSORBED more easily.
Dissolve - ionized, hydrophilic

Absorbed - uninonized, lipophilic
Volume of Distribution
Vd = IV bolus dose/peak concentration
or
Vd = (CL x t 1/2) / 0.693

SMALL Vd - drug mostly in blood and liver/kidneys only clear drug - shorter t 1/2

LARGE Vd - drug is in extravasc tissues too - longer t 1/2
Phase I reactions
Oxidation
Reduction
Hydrolysis
Phase II reactions
Glucuronidation
Sulfation
Amino acid conjugation
Acetylation
Methylation
Glutathion conjugation
1A2 drugs
Caffeine
Theophylline
3A4 drugs
Macrolides
CCB
BZD - alpraz, midaz, triaz
HIV protease inhibitors
2C9 drugs
Glipizide
Warfarin
Phenytoin
2C19 drugs
Omeprazole
Diazepam
2D6 drugs
Some opioids
Fluoxetine
Haloperidol
TCAs
Name a drug that causes auto-induction.
CBZ
Name some drugs that INHIBIT enzyme metabolism.
CCB
Macrolides
Quinolones
Azoles
Metronidazole
Cimeditine
Name some drugs that INDUCE enzyme metabolism.
Seizure meds
TB meds - rifampin, INH
Prednisone
Dissolution Test
Intended to reflect absorption of drug
Weight Variation Test and Content Uniformity Test
Asses distribution of active ingredient across the tables and ensure that each dose is appx the same weight
Disintegration Test
Evaluates how quickly/slowly a tablet disintegrates
Friability Test
Determines how well tablets will hold up handling/shipping
One-Compartment Model vs. Two-Compartment Model
One-Compartment:
only central compartment and drug distributes rapidly and uniformly into this compartment
lnC = lnCo - kt
k = 0.693/t 1/2 or (lnC1 - lnC2)/t2 - t1

Two-Compartment:
central compartment PLUS highly perfused organs like liver and kidneys
slow distribution of drug into the peripheral compartment of poorly perfused tissue (muscles/connective tissue)
What are TWO factors that can decrease the bioavailable fraction of a drug?
Incomplete absorption
1st pass metabolism

F = 1st pass metabl x absorption
(F = ffp x fa)
Hepatic Extraction Ratio (E)
ffp = (1-E)
HIGH E drugs - extensively metab by liver
LOW E drugs - metab by sluggish enzymes
What is the CLEARANCE equation?
CL = hepatic Cl + renal Cl
IBW
Males - 50 + [2.3 (inches over 60)]
Females - 45 + [2.3 (inches over 60)]
Css - Steady State Concentration
Rate of drug ENTERING the body = Rate of drug LEAVING the body

90% of Css is attained after 3 t1/2
97% of Css is attained after 5 t1/2

Css = LD/Vd
What 2 things affect drug accumulation?
Elimination half-life
Dosing interval

Dosing interval < t 1/2 - Css will be higher than conc after 1st dose
Dosing interval = t 1/2 - Css will be 2x high as conc after 1st dose
Dosing interval > t 1/2 - Css will be similar to conc after 1st dose
Infusion Rate (R)
R = (CS x Cl) / S
Increasing infusion rate will lead to HIGHER Css, but drug will not reach Css any faster
Non-linear PK
Occur when 1 or more enzyme(s) are SATURATED

So drug Cl is no longer necessarily constant and doubling a dose does not necessarily mean concentration and AUC will double as well
How many oz are in 1 cup?
1 pint?
1 qt?
1 gallon?
cup = 8 oz - 240 ml
pint = 16 oz - 473 ml
qt = 32 oz
gallon = 128 oz
How many mg is in 1 grain?
grams in 1 ounce?
grams in 1 pound?
grain = 65 mg
ounce = 28.4 g
pound = 454 g
Specific Gravity
Density of a substance relative to a reference substance (usually water)
SG of H2O is 1g/ml
Numeric data in Gaussian distribution- which tests?
Non-Gaussian distribution?
ANOVA (Gaussian)
T-tests (Gaussian)

Non-parametric tests like Mann-Whitney U (non-Gaussian) - also good for ordinal data
Nominal data - which test?
Chi-square
AHFS (hosp form service) Drug Info
FDA approved and off-label uses
Drug monographs
USP Drug Info
Volume I - General DI

Volume II - Patient Counseling Info

Volume III - Therapeutic Equivalence (FDA Orange Book; Labeling, storage, and packaging req; Pharmacy Law
Physicians' Desk Reference
FDA approved package insert info (not for unlabeled uses tho)
Colored insert for Drug ID and manufacturer info
Red Book
Cost Data
NDC numbers
Formulations available
DI colored inserts
Manufacturer info
Merck Index
Chemical and pharm info on drugs to help compound and/or for pharmaceutic reference
Remington: The Science and Practice of Pharmacy
For compounding and pharmaceutics resource
Provides info on numerous issues concerning pharmacy practice
Formula to calculate ANC
WBC x (%segs + %bands)