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					                      NAPLEX

                      ANTIMICROBIAL
                      AGENTS




PG 52




           Selecting Appropriate Antimicrobial Agents

       
          Empiric therapy
       
          Identify the causative organism
       
          Test the sensitivity of the organism to
           antimicrobial drugs
       
          Identify important host factors:
             Site of infection-CNS, bone, prostate, UTI
            

             Susceptibility to toxicity
            

             Patient allergies
            



PG 52




        Mechanisms of Action of Antimicrobial Agents

   
       Interference with cell wall synthesis
           
              penicillins, cephalosporins

   
       Inhibition of protein synthesis
           
              macrolides, clindamycin, tetracyclines, quinolones

   Interference with enzyme
                                            unique to bacterial cell
           
              sulfonamides

   Interference with the permeability of microbial cell
   
   membranes
           
              amphotericin B

PG 52
        Sulfonamides
   PABA
   PABA               dihydrofolic acid (DHFA)
                      dihydrofolic acid (DHFA)           tetrahydrolfolic acid (THFA)
                                                         tetrahydrolfolic acid (THFA)


              Sulfa




PG 53




        General considerations - Sulfonamides
    Mechanism of action : competitive antagonism of PABA in enzyme
    Mechanism of action : competitive antagonism of PABA in enzyme
    system essential for bacteria growth.
    system essential for bacteria growth.


    For ophthalmic use, sulfa sodium salt solutions are very alkaline (i.e.,
    For ophthalmic use, sulfa sodium salt solutions are very alkaline (i.e.,
    pH 10+). The only sodium salt suitable for ophthalmic use is
    pH 10+). The only sodium salt suitable for ophthalmic use is
    sulfacetamide sodium (solutions have pH of about 7.4).
    sulfacetamide sodium (solutions have pH of about 7.4).


    Sulfas are eliminated renally unchanged. Makes them good for UTIs.
    Sulfas are eliminated renally unchanged. Makes them good for UTIs.


    Sulfas are less soluble in acid urine. This is one cause of crystalluria.
    Sulfas are less soluble in acid urine. This is one cause of crystalluria.


    Stevens-Johnson syndrome is associated with sulfa use.
    Stevens-Johnson syndrome is associated with sulfa use.



PG 53




  General considerations – Sulfonamides (cont’d)
   Combinations of sulfamethoxazole and trimethoprim (Bactrim, Septra, etc.)
   Combinations of sulfamethoxazole and trimethoprim (Bactrim, Septra, etc.)
   are less likely to result in bacterial resistance.
   are less likely to result in bacterial resistance.


   Sulfasalazine (Azulfidine) is used in treating inflammatory bowel disease
   Sulfasalazine (Azulfidine) is used in treating inflammatory bowel disease
   and RA. Watch for sulfa allergy, salicylate allergy, and urine discoloration.
   and RA. Watch for sulfa allergy, salicylate allergy, and urine discoloration.
   - GI side effects, dose is titrated upward slowly, monitor blood counts – dyscrasias
   - GI side effects, dose is titrated upward slowly, monitor blood counts – dyscrasias
   If a patient cannot use sulfasalazine because of sulfa sensitivity, use
   If a patient cannot use sulfasalazine because of sulfa sensitivity, use
   mesalamine products, i.e., Asacol, Pentasa, Rowasa. – various dosage
   mesalamine products, i.e., Asacol, Pentasa, Rowasa. – various dosage
   forms
   forms
   Remember that silver sulfadiazine (Silvadene) and mafenide (Sulfamylon)
   Remember that silver sulfadiazine (Silvadene) and mafenide (Sulfamylon)
   are used topically for treatment of serious burns.
   are used topically for treatment of serious burns.




PG 53
  Penicillins




PG 54




  General Considerations – Penicillins
    Mechanism of action: interfere with bacterial cell-wall
    synthesis (bactericidal)


    Note that all penicillins have a beta lactam ring and
    thiazolidine ring.


    Possible cross-sensitivity with other beta lactam
    antimicrobials (e.g., cephalosporins).
           - percent cross-sensitive ranges from 5-7%




PG 54




   Structure Activity Relationships:
          
             AMino penicillins – AMpicillin, AMoxicillin, bacAMpicillin
          
             NOX penicillins – penicillinase (beta lactamase) resistant
              penicillins: Nafcillin, OXacillin, clOXacillin (PO),
                           Nafcillin,
              diclOXacillin(PO)----MSSA (vanco alternative)
          
             MEZPCT penicillins – antipseudomonal penicillins: MEZlocillin,
                                      antipseudomonal penicillins: MEZlocillin,
              Piperacillin, Carbenicillin, Ticarcillin (combo with
              aminoglycosides, not in the same IV)

        Therapy problems with penicillins:
          
             Acid Resistance
          
             Beta-lactamase (penicillinase) resistance (combo products;
              Zosyn, Timentin, Augmentin)
          
             Hypersensitivity
PG 55
         Which of the following is an adverse
         effect associated with use of
         aminopenicillins?
           a. polydipsia
           b. hemolytic anemia
           c. cholelithiasis
           d. tardive dyskinesia
           e. angina




         Which of the following is an adverse
         effect associated with use of
         aminopenicillins?
           a. polydipsia
           b. hemolytic anemia
           c. cholelithiasis
           d. tardive dyskinesia
           e. angina




        Cephalosporins




PG 56
        General considerations
        Contains beta-lactam ring. Therefore, may have cross-sensitivity with
        Contains beta-lactam ring. Therefore, may have cross-sensitivity with
        penicillins.
        penicillins.


        As you go from 1st generation to 4th generation, you get:
        As you go from 1st generation to 4th generation, you get:
            
                 increased gram-negative activity
                  increased gram-negative activity
            
                 decreased gram-positive activity
                  decreased gram-positive activity
            
                 increased resistance to beta-lactamase destruction
                  increased resistance to beta-lactamase destruction
            
                 increased ability to enter cerebrospinal fluid
                  increased ability to enter cerebrospinal fluid




PG 56




          Which of the following antimicrobial
          agents has effective coverage of streptococcus
          pneumoniae?
                I. amoxicillin
                II. doxycycline
                III. gentamicin


                a. I only
                b. III only
                c. I and II only
                d. II and III only
                e. I, II, and III




          Which of the following antimicrobial
          agents has effective coverage of streptococcus
          pneumoniae?
                I. amoxicillin
                II. doxycycline
                                                      Gram +
                III. gentamicin
                                                      Non-
                                                      Non-DRSP

                a. I only
                b. III only
                c. I and II only
                d. II and III only
                e. I, II, and III
        General considerations (cont’d)
        First generation (generally start with CEPH):
        First generation (generally start with CEPH):
            
               Good for surgical prophylaxis
                Good for surgical prophylaxis
        Second generation (generally start with CEF):
        Second generation (generally start with CEF):
            
               Good for otitis, sinusitis and respiratory tract infections
                Good for otitis, sinusitis and respiratory tract infections
        Third generation (generally end with IME or ONE):
        Third generation (generally end with IME or ONE):
            ●
            ●   Good for meningitis, CAP, gram-negative bacilli, gonorrhea,
                Good for meningitis, CAP, gram-negative bacilli, gonorrhea,
                Proteus, Salmonella, Klebsiella
                Proteus, Salmonella, Klebsiella
            ●
            ●   Cefixime (suprax), cefotaxime (claforan), ceftriaxone (rocephin)
                Cefixime (suprax), cefotaxime (claforan), ceftriaxone (rocephin)
        Fourth generation (cefepime) Maxipime:
        Fourth generation (cefepime) Maxipime:
            ●
            ●   Good antipseudomonal activity
                Good antipseudomonal activity




PG 57




        Tetracyclines




PG 58




        General Considerations
        Products:
        Products:
            
               Tetracycline HCI (Achromycin V, Sumycin, Robitet, Panmycin)
                Tetracycline HCI (Achromycin V, Sumycin, Robitet, Panmycin)
            
               Minocycline (Minocin)
                Minocycline (Minocin)
            
               Doxycycline (Vibramycin, Doxy 100, Doxychel, Vibra-Tabs)
                Doxycycline (Vibramycin, Doxy 100, Doxychel, Vibra-Tabs)
            
               Tigecycline (Tygacil) – IV for skin/soft tissue and Intra-
                Tigecycline (Tygacil) – IV for skin/soft tissue and Intra-abdominal
                                                                    Intra-abdominal
                infections
                infections
        These are bacteriostatic antimicrobials. They interfere with protein
        These are bacteriostatic antimicrobials. They interfere with protein
        synthesis.
        synthesis.
        Broad spectrum antimicrobials. Work against many gram-positive
        Broad spectrum antimicrobials. Work against many gram-positive
        and gram-negative organisms.
        and gram-negative organisms.
                 - also effective against atypical organisms mycoplasma and
                 - also effective against atypical organisms mycoplasma and
        chlamydia pneumoniae, useful for patients allergic to penicillin b/c gram +
        chlamydia pneumoniae, useful for patients allergic to penicillin b/c gram +
        coverage
        coverage

PG 58
        General Considerations
        Not for use in children under age 8. May cause discoloration of
        developing tooth enamel.

        Not for pregnant women. May adversely affect fetal
        development.

        Most have the potential for causing phototoxicity.
                      potential for causing phototoxicity.

        Drug interaction with divalent (Mg, Ca, Fe) or trivalent (Al)
        compounds and tetracyclines may result in complexation and
        impaired absorption. Do not use together.

        Broad spectrum activity can lead to thrush or vaginal candidias




PG 58




    Macrolides
    General Considerations:
               Bacteriostatic – inhibit protein synthesis
               May be good for patients who are
                                   beta-
                 hypersensitive to beta-lactam
                 antimicrobials.

               Good respiratory coverage.

                    CAP caused by S.pneumo, M.cat, H.flu or atypicals
                   (mycoplasma, legionella, and chlamydia)


PG 59




 Erythromycin
   Oral Products

                     (E-       Ery-
   Erythromycin base (E-Mycin, Ery-Tab, PCE, Eryc)
       Coating used on most products
       Administer on an empty stomach


   Erythromycin esolate (Ilosone)
   Associated with cholestatic hepatitis
    Better absorbed than erythromycin base


   Erythromycin ethylsuccinate (eryPed, E.E.S.)
         Most well absrobed
         Available in liquid form
         400 mg of EES = 250 mg of erythromycin base

PG 59
   Erythromycin (cont’d)

    Parenteral Products
    Erythromycin lactobionate


    Other Products
    Erythromycin for acne (Benzamycin, Eryderm, Erygel)
                          (Benzamycin,
    Erythromycin for ophthalmic use (Romycin)




    Drug Interactions: Mainly due to enzyme inhibition of erythromycin – (3A4)




PG 59




    Clarithromycin (Biaxin)


    Usually used BID. XL form used once daily.


    Prodrug: May be given with or without meals


    Used in combination with a proton pump inhibitor for H.
    pylori treatment.


    Metallic taste




PG 60




    Azithromycin (Zithromax)
           gram-
    More gram-negative activity than erythromycin or
    clarithromycin
    Once-
    Once-daily dosing, usually for five days for otitis media
           Z-
    (e.g., Z-Pack)
    Available as suspension, tablets, IV
    Suspension should not be taken with food or antacids.


    Telithromycin (Ketek)
    Not a macrolide
    Good strep pneumo coverage
    Contraindicated with myasthenia gravis
    Once-
    Once-daily dosing

PG 60
    Lincosamides
    General considerations
    Watch for pseudomembranous enterocolitis (Clostridium
    difficile).
           •Treat clostridium with metronidazole (Flagyl) or oral
           vancomycin.
                                      gram-
    Good in gram positive (staph) and gram-negative infections,
    particularly anaerobes

        Lincomycin (Lincocin, Lincorex)
        Morbilliform rash possible; D/C drug if it happens

        Clindamycin (Cleocin)
        Available in topical form for acne



PG 61




        Which of the following antibiotics has
           bacteriostatic activity?
            a. amoxicillin
            b. ciprofloxacin
            c. erythromycin
            d. penicillin
            e. cephalexin




        Which of the following antibiotics has
           bacteriostatic activity?
            a. amoxicillin (cell wall)
            b. ciprofloxacin (inhibits DNA gyrase)
            c. erythromycin (protein synthesis)
            d. penicillin (cell wall)
            e. cephalexin (cell wall)
    Aminoglycosides
    General Considerations
    Glycosides – poorly absorbed from the GI tract
    Bactericidal
                     gram-
    Good for serious gram-negative pathogens (pseudomonas,
    proteus, etc.)
                                 extended-
    Frequently administered with extended-action penicillin (IV
                                                            (IV
    incompatible)
    incompatible) - dosed q8h or q24h (conc. dependant kill)
    Eliminated by glomerular filtration; Watch for ototoxicity
    Monitor peaks and troughs – peaks 30 min after infusion, trough 30
                                       4-                   0.5-
    minutes before next dose. peak = 4-10ug/ml trough = 0.5-2, adjust
    dose if CrCl < 60ml/min. hearing test if prolonged therapy


PG 61




        Which of the following antimicrobial
        agents is available for parenteral use only?
          I. cefaclor
          II. tobramycin
          III. ticarcillin

           a. I only
           b. III only
           c. I and II only
           d. II and III only
           e. I, II, and III




        Which of the following antimicrobial
        agents is available for parenteral use only?
          I. cefaclor
          II. tobramycin
          III. ticarcillin

           a. I only
           b. III only
           c. I and II only
           d. II and III only
           e. I, II, and III
    Parenteral use

                                      Reference Peak Range

    Streptomycin sulfate
    Kanamycin sulfate (Kantrex)
    Gentamicin sulfate (Garamycin      (4mcg-
                                       (4mcg-10mcg/ml)

    Tobramycin sulfate (Nebcin)        (4mcg-
                                       (4mcg-10mcg/ml)

    Amikacin sulfate (Amikin)          (15mcg-
                                       (15mcg-25mcg/ml)

    Netilmicin sulfate (Netromycin)




PG 61




        Which of the following antibiotics
        requires monitoring of serum levels?

           a. penicillin
           b. ceftazidime
           c. azithromycin
           d. gentamicin
           e. cephalexin




        Which of the following antibiotics
        requires monitoring of serum levels?

           a. penicillin
           b. ceftazidime
           c. azithromycin
           d. gentamicin
           e. cephalexin
    Oral use
    Not for systemic action


    Neomycin sulfate (Mycifradin) - Used for bowel prep prior to
    surgery , treat diarrhea caused by e.coli, neomycin also binds
    ammonia, use in patients w/hepatic encephalopathy, watch for
    absorption interactions


    Tobramycin (TOBI) – inhaled product for CF patients




PG 62




    Fluoroquinolones
                                      DNA-
    General Considerations - Inhibits DNA-Gyrase
    May cause phototoxicity
    Not for patients under 18 – affects growth
                      2-
    Do not use within 2-4 hours of antacids; iron – also inhibits
                                   antacids;
    CYP1A2 (increased levels of theophylline and caffeine)
    Generally useful for UTI, lower respiratory infections,
    gonorrhea, prostatitis – older agents have more gram -,
    less gram + coverage, newer agents have broader gram +
     moxifloxacin, gatifloxacin]
    [moxifloxacin, gatifloxacin]
    All end in -oxacin


PG 62




    Names
    Second generation
        Norfloxacin (Noroxin) – high urine levels - UTIs
                      (Cipro)-
        Ciprofloxacin (Cipro)- renal elimination: reduce dose
        Ofloxacin (Floxin)

    Third generation
        Levofloxacin (Levaquin) – renal elimination: reduce dose
        Sparfloxacin (Zagam) – reports of prolongation of QT interval (D/C)
        Gemifloxacin (Factive) – renal elimination: reduce dose, skin rash
        Gatifloxacin (Zymar) – ophthalmic use only

    Fourth generation
        Moxifloxacin (Avelox) – Multi-drug resistant Streptococcus pneumonia
                                Multi-
        (MDRSP)
PG 62
     MISCELLANEOUS ANTIMICROBIAL AGENTS
     Antibacterials


     Mupirocin (Bactroban) – topical use for impetigo, intranasal for staph


     Vancomycin (Vancocin) – associated with red man syndrome (must be
                                                           serious/resistant
     infused slowly, over min of 30 minutes); reserved for serious/resistant
     gram + infections (MRSA, enterococcus)
              – rapid drop in BP accompanied by rash in neck or chest area
              - Monitoring – 1 hour before and 1 hour after
                       25-                  5-
              - Peak – 25-40mcg/dl & Trough 5-12mcg/dl


                                             gram-
     Metronidazole (Flagyl) – active against gram-negative organisms and
     protozoa, (anaerobes) Avoid alcohol. May darken urine. Metallic taste
PG 63




                                        (cont’
     MISCELLANEOUS ANTIMICROBIAL AGENTS (cont’d)
     Carbapenems
                                                  +/–
         •broad spectrum; used for resistant gram +/– organisms, pseudomonas,
                 enterococcus,
         MRSA, enterococcus, anaerobes
                                 (cross-
         •similar to penicillins (cross-sensitivity) but b-lactamase resistant
         •Risk of seizures and renal adjustment

                          Primaxin)
     Imipenem/cilastatin (Primaxin) – cilastatin is a renal dipeptidase
     inhibitor
                Merrem)---lacks
     Meropenem (Merrem)---lacks good pseudomonas coverage
                Doribax)
     Doripenem (Doribax)
                Invanz)
     Ertapenem (Invanz)
     ----Aztreonam Azactam)---monobactam,
     ----Aztreonam (Azactam)---monobactam, ok with PCN allergy



PG 63




            Which of the following antibiotic is
            classified as a macrolide?

               a. vibramycin
               b. tobramycin
               c. azithromycin
               d. doxycycline
               e. kanamycin
            Which of the following antibiotic is
            classified as a macrolide?

               a. vibramycin
               b. tobramycin
               c. azithromycin
               d. doxycycline
               e. kanamycin




                                         (cont’
      MISCELLANEOUS ANTIMICROBIAL AGENTS (cont’d)


      VRE and MRSA drugs
      Quinupristin / dalfopristin (Synercid) –
                         ……oral
      Linezolid (Zyvox) –……oral dosing available
      Tigecycline (Tygacil) – tetracycline derivative




      Chloramphenicol (Chloromycetin) – for typhoid fever; may cause
      aplastic anemia and gray baby syndrome




PG 63-64




                            Pneumonia
  
     Organisms:




  
     Treatment:
                                                         --Comorbidities:
                                                         --Comorbidities:
                                                         Chronic obstructive
                                                         pulmonary disease
                                                         (COPD), diabetes,
                                                         chronic renal failure,
                                                         chronic liver failure,
                                                         heart failure (HF),
                                                         cancer, asplenia,
                                                         immunosuppressed
                     Pneumonia

   Treatment:




                                  --Risk
                                  --Risk factors for
                                  MDR organisms:
                                  recent antibiotic
                                  therapy (in last 90
                                  days), hospitalized ≥
                                  5 days,  resistance
                                  in environment,
                                  nursing home
                                  resident, chronic
                                  dialysis, home
                                  infusion therapy,
                                  immunosuppressed




                     Meningitis
    
       Organisms:




    
       Treatment:




            Urinary Tract Infection
    
       Organisms:




    
       Treatment:
                                     STDs
    
       Organisms:




    
       Treatment:




                 Antitubercular Drugs


               R         rifampin
               I         isoniazid
               P         pyrazinamide
               E         ethambutol
               S         streptomycin


PG 64




   Antitubercular Drugs
   Isoniazid (Nydrazid, Laniazid)
        May cause B6 deficiency – supplement malnourished, alcoholics, kids
                                                                      disease
        Used for prophylaxis or in combo with other drugs for active disease
                                                                           with
             6 months of prophylaxis if +PPD; For treatment used in combo with
               rifampin for at least 6 months
        Metabolized by acetylation (slow versus rapid acetylators)
             monitor for hepatoxicity
   Rifampin (Rifadin, Rimactane)
                                                                      drugs)
        Potent enzyme inducer (potential drug interactions with many drugs)
        Potentially hepatotoxic;
                                                                      (urine
        Use may result in discoloration of virtually all body fluids (urine and
        tears----watch
        tears----watch contact lenses)



PG 64
  Antitubercular Drugs (cont.)

                                                    drug-
  Ethambutol (Myambutal) – for treatment of MAC and drug-resistant Tb
  as part of combination therapy
         - optic neuritis is a rare but serious side effect
         - monitor with eye exams
  Pyrazinamide – used in combination therapy; potentially hepatotoxic

         - may increase uric acid levels
  Steptomycin- can be used as fourth drug in regimen instead of
  pyrazinamide




PG 65




   Antimalarials
   Quinine sulfate (Quinamm) – also used for muscle cramps;
   no longer used due to hematologic adverse effects


   Doxycycline – tetracycline; possible phototoxicity and
   binding interactions


   Melfoquine HCl (Lariam) – may cause neuropsychiatric
                    once-
   adverse effects; once- weekly dosing


   Atovaquone/proguanil (Malarone) – newer product; once
   daily; do not use if renally impaired
PG 65




   Antimalarials
   Chloroquine (Aralen) – may worsen psoriasis symptoms


   Hydroxychloroquine sulfate (Plaquenil Sulfate) – may
   worsen psoriasis symptoms
           - also used as a DMARD for RA; phototoxicity,
            hematological side effects, ocular and ototoxicity
   Primaquine phosphate – take with food to reduce GI upset;
   may be used for PCP




PG 66
          HIV Antiretroviral Therapy
    
       Therapy initiated based on CD4 count,
        viral load and presence of symptoms
          Initial regimen in treatment naive patients:
         
           • NNRTI + 2 NRTIs
           • PI + 2 NRTIs


       Learn drug class representatives and
        major toxicities


PG 68




        Which HIV drug is correctly matched
          with its mechanism of action?

  a. Lamivudine - nucleoside reverse
    transcriptase inhibitor
  b. Enfuvirtide - protease inhibitor
  c. Stavudine - binds to human CCR5
    receptor
  d. Didanosine – protease inhibitor
  e. Indinavir – blocks virus entry into human
    cells and subsequent viral replication




        Which HIV drug is correctly matched
          with its mechanism of action?

  a. Lamivudine - nucleoside reverse
    transcriptase inhibitor
  b. Enfuvirtide - protease inhibitor
  c. Stavudine - binds to human CCR5
    receptor
  d. Didanosine – protease inhibitor
  e. Indinavir – blocks virus entry into human
    cells and subsequent viral replication
                       NNRTIs
        non-
        non-nucleoside reverse transcriptase
        non-nucleoside
           inhibitors (vir in the middle)

    
        Delavirdine (rescriptor)
           rash, LFTs
          
    
        Efavirenz (Sustiva)
           Drug of choice
          
           Category X, vivid dreams
          
    
        Nevirapine (Viramune)
           Rash (Steven Johnson Syndrome)
          
           Liver metabolism
          
    
        Entravirine (Intelence)
           Rash (Steven Johnson Syndrome)
          




PG 71




                 PIs
  Protease inhibitors (vir at the end)
                                                                         (NRTI)
   Exception – tenofovir (NRTI), raltegravir (Integrase Inhib), abacavir (NRTI)

   Metabolized through the liver (commonly 3A4)
        • potential for significant drug interactions
   Low dose of ritonavir frequently used to enhance
   the concentrations of coadministered PIs
   Adverse effects: GI intolerance, hyperglycemia,
   dyslipidemia, lipodystrophy, LFT alterations


PG 72




                                 NRTIs
      nucleoside reverse transcriptase
              inhibitors (all the others)
  Exception – maraviroc ( CCR5 entry inhibitor)

                    abacavir)              renally;
  All NRTIs (except abacavir) are excreted renally; require
  dose adjustment but few drug interactions


  Most common ADRs – GI intolerance, typically subsides in
  first couple of weeks
          - High risk for perpheral neuropathy


  Black Box warning: Risk of lactic acidosis with hepatic
  steatosis
PG 69
        AIDS – Opportunistic Infections
    
       PCP / PJP (pneumocystis carninii pneumonia)
                  (pneumocystis carninii pneumonia)
        
           trimethoprim-sulfamethoxazole
    
       CMV retinitis
        
           Ganciclovir
    
       MAC / MAI (mycobacterium avium complex)
                  (mycobacterium avium complex)
        
           Macrolide + ethambutol
    
       Cryptococcus neuformans meningitis
        
           Amphotericin B +/- flucytosine
        
           Fluconazole used for maintenance


PG 74




   Drugs for influenza


   M2 inhibitors
            Amantadine, rimantidine
            Effective for influenza A virus only
                                                        2-
            Begin within 48h of symptom onset; continue 2-5 days


   Neuroaminidase inhibitors
            Oseltamivir (Tamiflu)
            Zanamivir (Relenza)
            Effective for influenza A and B viruses
            Begin with 48h of symptoms onset; continue 5 days


PG 74




   Drugs for herpes simplex and herpes zoster (shingles)
   Acyclovir (Zovirax) – for herpes simplex types 1 and 2
   - dosed 5x/day for 10 days, 5 days if recurrence
   Penciclovir (Denavir) – topical treatment for herpes labialis
   (cold sores)
   Valacyclovir HCl (Valtrex) – for herpes simplex and herpes
   zoster; acyclovir prodrug
   Famcyclovir (Famvir) for herpes simplex and herpes zoster
   (shingles); penciclovir prodrug
   - begin therapy as soon as first sign of lesion
             (OTC-
   Docosanol (OTC-Abreva) topical cream

PG 75
   Anthelmintic drugs of choice
   Nematodes (roundworm)
                        (Vermox)—
           Mebendazole (Vermox)—do not use in pregnancy – blocks glucose uptake
           Albendazole (Albenza) – degeneration of cytoplasmic microtubules intestinal cells
           of helminths

           Piperazine citrate Preg B – blocks affect of ACH
           Pyrantel pamoate (Antiminth)


   Trichuriasis (whipworm)
           Mebendazole (do not use in pregnancy)


   Hookworm – mebendazole (do not use in pregnancy)



PG 75




    Which of the following medication(s) can cause
      nephrotoxicity?

    I.
    I.       Ganciclovir
    II.
    II.      Foscarnet
    III.
    III.     Gentamicin

                  a. I only
                  b. III only
                  c. I and II only
                  d. II and III only
                  e. I, II, and III




    Which of the following medication(s) can cause
      nephrotoxicity?

    I.
    I.       Ganciclovir
    II.
    II.      Foscarnet
    III.
    III.     Gentamicin

                  a. I only
                  b. III only
                  c. I and II only
                  d. II and III only
                  e. I, II, and III
    Which of the following agents inhibits the
       HIV enzyme reverse transcriptase?
            I. zanamivir
            II. ritonivir
            III. didanosine

            a. I only
            b. III only
            c. I and II only
            d. II and III only
            e. I, II, and III




    Which of the following agents inhibits the
       HIV enzyme reverse transcriptase?
            I. zanamivir ((Neuroaminidase inhibitors)
                              Neuroaminidase inhibitors)
            II. ritonivir (protease inhibitor)
                          (protease inhibitor)
            III. didanosine ((nucleoside reverse transcriptase inhibitors)
                                nucleoside reverse transcriptase inhibitors)


            a. I only
            b. III only
            c. I and II only
            d. II and III only
            e. I, II, and III




         DERMATOLOGIC STUDY OUTLINE
         Acne
         Pathophysiology—
         Pathophysiology— abnormal keratinization
         leads to obstruction of the follicle and
         accumulation of sebum to form a closed
                     white- head”
         comedo or “white-head”


         Goal of therapy is to unblock follicles



PG 149
   Dermatologic Study Outline
         Isotretinoin (Accutane)
          Effective therapy option for the treatment of severe,
         inflammatory acne, or more moderate forms that have been
         refractory to other treatment options
          pregnancy category X
          two forms of contrception, iPLEDGE program


         Oral Antimicrobials
               • Tetracycline
               • Erythromycin
               • Clindamycin


PG 146




   Dermatologic Study Outline




      Which of the following psoriasis
    medications is not pregnancy category
                      X?
    I. Dovonex
    II. Methotrexate
    III. Soriatane

          A.
          A.      I only
          B.
          B.      III only
          C.
          C.      I and II only
          D.
          D.      II and III only
          E.
          E.      I, II and III
  Which of the following psoriasis
medications is not pregnancy category
                  X?
I. Dovonex
II. Methotrexate
III. Soriatane

  A.
  A.   I only
  B.
  B.   III only
  C.
  C.   I and II only
  D.
  D.   II and III only
  E.
  E.   I, II and III




   A patient presents to the pharmacy
  with obvious mild acne, which of the
   following cannot be recommended
         without a prescription?

   a. Benzoyl peroxide 2.5% cream
   b. Sulfur soap
   c. Benzamycin gel
   d. Salicylic acid wash
   e. Benzoyl peroxide 10% lotion




   A patient presents to the pharmacy
  with obvious mild acne, which of the
   following cannot be recommended
         without a prescription?

   a. Benzoyl peroxide 2.5% cream
   b. Sulfur soap
   c. Benzamycin gel
   d. Salicylic acid wash
   e. Benzoyl peroxide 10% lotion
                          Fungal Infections

    
        Tinea corporis – body surface
    
        Tinea capitis – scalp
    
        Tinea cruris – groin (“jock itch”)
    
        Tinea pedis – feet (“athlete’s foot”)
    
        Onychomycosis – nails




PG 67-68 and 150




    Therapy
         Prophylaxis. Keep skin dry; frequent changes and thorough cleaning of
         clothing; and avoid likely areas of contamination.
         Active:
         Dusting powders (medicated versus nonmedicated), wet compresses
         Topical drug therapy
             • Fatty acids (undecylenic acid)        • Tolnaftate (Tinactin, Aftate)
                            (Femstat-
             • Butoconazole (Femstat-3)              • Miconazole (Micatin,Monistat)
             • Clotrimazole (Lotrimin)               • Oxiconazole (Oxistat)
             • Sulconazole (Exelderm)                • Butenafine (Mentax)

             Nystatin (Mycostatin, Nilstat) – good for superficial candida (thrush)


         Systemic drug therapy for topical fungal disorders
             • Griseofulvin (microsized versus ultramicrosized)
             • Terbinafine (Lamisil)
             • Avoid corticosteroids

PG 150




                         (cont’
        Antifungal Drugs (cont’d)
                                         broad-
        Miconazole (Monistat, Micatin) – broad-spectrum antifungal
        agent available as powder, aerosol, cream, and
        suppository; may be used topically or vaginally
                                            broad-
        Clotrimazole (Lotrimin, Mycelex) – broad-spectrum
        antifungal available as cream, lotion, suppositories, and
        troches (OTC use for 2 weeks after infection clears)
        Ketoconazole (Nizoral) – for superficial and systemic fungal
        infections; also available as OTC shampoo for dandruff;
        enzyme inhibitor
        Itraconazole (Sporanox) – for oral or topical treatment of
        superficial or systemic fungal disorders; enzyme inhibitor.
                   - hepatotoxicity; take w/ food and avoid antacids
PG 68
                     (cont’
    Antifungal Drugs (cont’d)
                     (cont’d)

   
       Terbinafine (Lamisil) – used orally for
        onychomycosis of fingernail or toenail. Used
        topically for superficial tinea infections (OTC
        use for 1 week). Monitor for hepatoxicity with
        oral use.

   
       Ciclopriox (Penlac) – applied topically once
        daily for treatment of onychomycosis. –
                   long-
        requires long-term therapy
                   long-term


PG 67




                     (cont’
    Antifungal Drugs (cont’d)
                     (cont’d)

   
       Griseofulvin (Grisactin, Grifulvin V, Fulvicin)
         For tinea only
        

         Duration of therapy
        
                                          2-                 4-
             • depends on type: corporis: 2-4 wks.; capitis: 4-6 wks.,
                                          2-4                4-6
                      4-
               pedis: 4-8 wk
                      4-8
        
           Regular versus microsized versus
            ultramicrosized
             • ultra is better absorbed; take w/ fatty meal
                                                 fatty meal
             • causes induction interactions




PG 67




                             (cont’
            Antifungal Drugs (cont’d)
                             (cont’d)
    
        Other Azoles
          Posaconazole (Noxafil)
          
          Voriconazole (Vfend)
          
              • Reserved for severe invasive fungal infections (asperigillosis)
              • Reserved for severe invasive fungal infections (asperigillosis)
    
        Echinocandins (less DI, but monitor LFTs)
           Anidulafungin (Eraxis)
          
           Caspofungin (Cancidas)
          
           Micafungin (Mycamine)
          
    
        Ampho B and related Lipid products
           nephrotoxicity
          




PG 68
        NAPLEX


        Sample Questions




Which of the following antibiotics does
not have a significant drug interaction
            with warfarin?

  A.
  A.   ciprofloxacin
  B.
  B.   azithromycin
  C.
  C.   TMP-SMZ
  D.
  D.   Metronidazole
  E.
  E.   Nafcillin




Which of the following antibiotics does
not have a significant drug interaction
            with warfarin?

  A.
  A.   ciprofloxacin
  B.
  B.   azithromycin
  C.
  C.   TMP-SMZ
  D.
  D.   Metronidazole
  E.
  E.   Nafcillin
  Which of the following medications is
     the best treatment option for an
  uncomplicated urinary tract infection?
       A.
       A.   penicillin
       B.
       B.   cefuroxime
       C.
       C.   levofloxacin
       D.
       D.   gentamicin
       E.
       E.   clarithromycin




  Which of the following medications is
     the best treatment option for an
  uncomplicated urinary tract infection?
       A.
       A.   penicillin
       B.
       B.   cefuroxime
       C.
       C.   levofloxacin
       D.
       D.   gentamicin
       E.
       E.   clarithromycin




      Which of the following antimicrobial
      agents is available for parenteral use
                      only?
I.
I.        piperacillin
II.
II.       aztreonam
III.
III.      rifampin
       A.
       A.     I only
       B.
       B.     III only
       C.
       C.     I and II only
       D.
       D.     II and III only
       E.
       E.     I, II and III
      Which of the following antimicrobial
      agents is available for parenteral use
                      only?
I.
I.        piperacillin
II.
II.       aztreonam
III.
III.      rifampin
       A.
       A.     I only
       B.
       B.     III only
       C.
       C.     I and II only
       D.
       D.     II and III only
       E.
       E.     I, II and III




Which of the following agents is a
      non-nucleoside reverse
      transcriptase inhibitor?

       A.
       A.   didanosine
       B.
       B.   delavirdine
       C.
       C.   stavudine
       D.
       D.   zidovudine
       E.
       E.   lamivudine




Which of the following agents is a
      non-nucleoside reverse
      transcriptase inhibitor?

       A.
       A.   didanosine
       B.
       B.   delavirdine
       C.
       C.   stavudine
       D.
       D.   zidovudine
       E.
       E.   lamivudine
Which of the following agents may be
 utilized in combination with other
medications for H. pylori eradication?


  A.
  A.   tetracycline
  B.
  B.   azithromycin
  C.
  C.   penicillin
  D.
  D.   fluconazole
  E.
  E.   cefuroxime




Which of the following agents may be
 utilized in combination with other
medications for H. pylori eradication?


  A.
  A.   tetracycline
  B.
  B.   azithromycin
  C.
  C.   penicillin
  D.
  D.   fluconazole
  E.
  E.   cefuroxime




 Peripheral neuropathy is associated
with which one of the following agents:


  A.
  A.   nevirapine
  B.
  B.   delavirdine
  C.
  C.   Saquinavir
  D.
  D.   Stavudine
  E.
  E.   tenofovir
 Peripheral neuropathy is associated
with which one of the following agents:


  A.
  A.        Nevirapine (NNRTI)
  B.
  B.        Delavirdine (NNRTI)
  C.
  C.        Saquinavir (PI)
  D.
  D.        Stavudine (NRTI) do not use with AZT (zidovudine)
  E.
  E.        Tenofovir (NRTI)




Administration of calcium or iron must
  be separated by at least 2 hours if
   antibiotics in this category are
             prescribed:

       I.
       I.        Macrolides
       II.
       II.       Tetracyclines
       III.
       III.      Fluroquinolones
              A.
              A.    I only
              B.
              B.    III only
              C.
              C.    I and II only
              D.
              D.    II and III only
              E.
              E.    I, II and III




Administration of calcium or iron must
  be separated by at least 2 hours if
   antibiotics in this category are
             prescribed:

       I.
       I.        Macrolides
       II.
       II.       Tetracyclines
       III.
       III.      Fluroquinolones
              A.
              A.    I only
              B.
              B.    III only
              C.
              C.    I and II only
              D.
              D.    II and III only
              E.
              E.    I, II and III
Which of the following antimicrobial
  agents has effective coverage for
           M. pneumoniae?
A.
A.   amoxicillin
B.
B.   erythromycin
C.
C.   metronidazole
D.
D.   ceftriaxone
E.
E.   clindamycin




Which of the following antimicrobial
  agents has effective coverage for
           M. pneumoniae?
A.
A.   amoxicillin
B.
B.   erythromycin
C.
C.   metronidazole
D.
D.   ceftriaxone
E.
E.   clindamycin




Which of the following regimens is
 most appropriate for C. difficile
           eradication?

A.
A.   Clarithromycin 500 mg PO q 12 hours
B.
B.   Clindamycin 300 mg IV q 6 hours
C.
C.   Vancomycin 125 mg PO q 6 hours
D.
D.   Doxycycline 100 mg PO q 12 hours
E.
E.   Vancomycin 1000 mg IV q 12 hours
       Which of the following regimens is
        most appropriate for C. difficile
                  eradication?

       A.
       A.   Clarithromycin 500 mg PO q 12 hours
       B.
       B.   Clindamycin 300 mg IV q 6 hours
       C.
       C.   Vancomycin 125 mg PO q 6 hours
       D.
       D.   Doxycycline 100 mg PO q 12 hours
       E.
       E.   Vancomycin 1000 mg IV q 12 hours




       Which agent is available in both a
        topical and an oral product for the
                treatment of acne?
I.
I.        clindamycin
II.
II.       erythromycin
III.
III.      doxycycline
       A.
       A.     I only
       B.
       B.     III only
       C.
       C.     I and II only
       D.
       D.     II and III only
       E.
       E.     I, II and III




       Which agent is available in both a
        topical and an oral product for the
                treatment of acne?
I.
I.        clindamycin
II.
II.       erythromycin
III.
III.      doxycycline
       A.
       A.     I only
       B.
       B.     III only
       C.
       C.     I and II only
       D.
       D.     II and III only
       E.
       E.     I, II and III
     Which of the following drugs
represents first (primary) agents in the
          treatment of TB?

  A.
  A.   Ethambutol + PASA
  B.
  B.   Ciprofloxacin + PASA
  C.
  C.   Isoniazid + rifampin
  D.
  D.   Cycloserine + streptomycin
  E.
  E.   Penicillin + Benemid




     Which of the following drugs
represents first (primary) agents in the
          treatment of TB?

  A.
  A.   Ethambutol + PASA
  B.
  B.   Ciprofloxacin + PASA
  C.
  C.   Isoniazid + rifampin
  D.
  D.   Cycloserine + streptomycin
  E.
  E.   Penicillin + Benemid




 Which of the following antibiotics is
 considered first line treatment for a
       gonorrhea infection?

  A.
  A.   Ampicillin
  B.
  B.   Ciprofloxacin
  C.
  C.   Doxycycline
  D.
  D.   Penicillin
  E.
  E.   Tetracycline
       Which of the following antibiotics is
       considered first line treatment for a
             gonorrhea infection?

       A.
       A.   Ampicillin
       B.
       B.   Ciprofloxacin (also..ceftriaxone, cefixime)
       C.
       C.   Doxycycline (chlamydia)
       D.
       D.   Penicillin
       E.
       E.   Tetracycline




        Which of the following groups of
         antibiotics may be prescribed for a
           gravid patient with gonorrhea?
I.
I.        cephalosporins
II.
II.       fluoroquinolones
III.
III.      tetracyclines
       A.
       A.     I only
       B.
       B.     III only
       C.
       C.     I and II only
       D.
       D.     II and III only
       E.
       E.     I, II and III




        Which of the following groups of
         antibiotics may be prescribed for a
           gravid patient with gonorrhea?
I.
I.        cephalosporins
II.
II.       fluoroquinolones
III.
III.      tetracyclines
       A.
       A.     I only
       B.
       B.     III only
       C.
       C.     I and II only
       D.
       D.     II and III only
       E.
       E.     I, II and III
  A gravid patient with a Chlamydia
  infection is likely to be prescribed
  which of the following antibiotics?

  A.
  A.   Ampicillin
  B.
  B.   Levofloxacin
  C.
  C.   Doxycycline
  D.
  D.   Erythromycin
  E.
  E.   Penicillin




  A gravid patient with a Chlamydia
  infection is likely to be prescribed
  which of the following antibiotics?

  A.
  A.   Ampicillin
  B.
  B.   Levofloxacin
  C.
  C.   Doxycycline
  D.
  D.   Erythromycin
  E.
  E.   Penicillin




Which of the following is the BEST
    treatment for a patient with
          herpes zoster?
  A.
  A.   Cidofovir
  B.
  B.   Famciclovir
  C.
  C.   Ganciclovir
  D.
  D.   Penciclovir
  E.
  E.   Tenofovir
Which of the following is the BEST
    treatment for a patient with
          herpes zoster?
     A.
     A.   Cidofovir
     B.
     B.   Famciclovir
     C.
     C.   Ganciclovir
     D.
     D.   Penciclovir
     E.
     E.   Tenofovir




     Which of the following medications
        would be appropriate for the
         treatment of Pseudomonas
                 aeruginosa?
a.
a.   Ampicillin
b.
b.   Cefepime
c.
c.   Ceftriaxone
d.
d.   Erythromycin
e.
e.   Clindamycin




     Which of the following medications
        would be appropriate for the
         treatment of Pseudomonas
                 aeruginosa?
a.
a.   Ampicillin
b.
b.   Cefepime
c.
c.   Ceftriaxone
d.
d.   Erythromycin
e.
e.   Clindamycin