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Pharmacology Tests > Test #2 > Flashcards

Test #2 Flashcards

1
Q

Macrolides

A
  • Erythromycin, azithromycin, clarithromycin, fidaxomicin
  • Lincosamide: Clindamycin
  • MOA: Inhibit protein synthesis (50s)
  • Spectrum : Gram + and Gram -
  • Uses: AOM (in PCN allergic pts), Strep pharyngitis (in PCN allergic patients), CAP outpatient (first-line), atypical pneumonia, legionella pneumonia, acute exacerbations of chronic bronchitis, chlamydia, pertussis, diphtheria, campylobacter, H. pylori, mycobacteria, rheumatic fever prophylaxis
  • ADRs: N/V/D, liver problems, long QT syndrome
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2
Q

Erythromycin

A
  • Macrolide
  • Natural product: Streptomyces erythreus
  • Usually bacteriostatic
  • Degraded by stomach acid (enteric-coated tablet)
  • Uses: diphtheria (FIRST-LINE), chlamydia if patient is pregnant, pertussis, , campylobacter gastroenteritis (second-line), rheumatic fever prophylaxis
  • Contraindications: hypersensitivity (rash, hives, anaphylaxis, SJS, TEN), liver disease, heart problems
  • Drug Interactions: Pimozide (life-threatening)
  • Drug Interactions: P450!
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3
Q

Stevens-Johnson Syndrome

A
  • Erythema multiforme major
  • Erythromycin, telithromycin
  • Penicillins
  • Sulfonamides
  • Affects skin and mucous membranes
  • Can be fatal
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4
Q

Clarithromycin

A
  • Macrolide
  • More acid-stable than erythro, better oral absorption
  • Spectrum: better than erythro, includes MAC and H. flu
  • Uses: pertussis (FIRST-LINE), AOM (second-line for PCN allergy), pharyngitis/tonsillitis, legionnaire’s dz, Bartonella (cat scratch fever), Lyme dz, toxoplasmosis, cryptosporidiosis
  • CYP 3A4
  • Distributes into CSF
  • Absorption improved with food
  • Preg. category C
  • ADRs: generally mild, N/V/D, dysgeusia
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5
Q

Azithromycin

A
  • Macrolide
  • Uses: COPD exacerbations, CAP, strep pharyngitis/tonsillitis in PCN-allergic pts, uncomplicated skin and skin structure infections, chlamydia, genital ulcer dz in men
  • Little enters CSF
  • Preg. category B (low breast milk levels)
  • Warnings: hypersensitivity (SJS/TEN), CDAD, long QT, not for use in severe pneumonia
  • ADRs: N/V/D, abd. pain (less than erytho, claritho), rare: angioedema, cholestatic jaundice
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6
Q

Fidaxomicin

A
  • Macrolide
  • CDAD tx in adults (compared to vancomycin)
  • ADRs: hypersensitivity rxns, N/V, abd. pain, GI hemmorrhage, anemia, neutropenia
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7
Q

Clindamycin

A
  • Lincosamide abx
  • MOA: inhibits protein synthesis (50s)
  • Administered as inactive salts; activated by hydrolysis
  • Spectrum: Gram + and - aerobes, anaerobes
  • Active against Plasmodium (malaria)
  • Erythromycin resistance often leads to clindamyin resistance (D test)
  • Indications: AOM, pharyngitis, tonsilitis, infxns, SSTI, septicemia, malaria, etc.
  • ADRs: CDAD, diarrhea, N/V, abd. pain, rash, jaundice, increased LFTs, leukopenia, eosinophilia
  • “Diarrhea in a pill”
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8
Q

Tetracyclines

A
  • Tetracycline, doxycycline, demeclocycline, minocycline, tigecycline
  • Bacteriostatic
  • MOA: inhibit protein synthesis (30s)
  • Indications: URI, lower respiratory tract infections, SSTI, rickettsia infxns (RMSF)
  • When PCN is contraindicated, these are alternative drugs in certain infxns
  • Food and milk decrease absorption 50%
  • Do not take with Al, Mg, Ca, Fe (1-2 hrs before, 4 hrs after)
  • ADRs: photosensitivity, discolored teeth (limited use in peds), N/V/D, abd. pain, candidal infxn, hepatotoxicity, Jarisch-Herxheimer rxn
  • Pregnancy category D (enters breast milk)
  • Different dosing for renal insufficiency
  • Hepatic insufficiency - avoid use
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9
Q

Jarish-Herxheimer Rxn

A
  • often seen after tx of syphilis with PCN
  • Can be seen in tx of lyme dz, leptospirosis, with tetracyclines
  • Mild fever, chills, HA, malaise 8 hrs after tx
  • can progress to seizure, but usually self-limited
  • Due to inflammation after large # of organisms die
  • Tx with ASA or other anti-inflammatory
  • Steroids not beneficial
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10
Q

Doxycycline

A
  • Tetracycline
  • 5x more lipid soluble than tetracycline
  • Indications: RMSF (FIRST-LINE), Lyme dz (FIRST-LINE), Vibrio (FIRST-LINE), chlamydial infxns, acne, bites, gonorrhea, syphilis (PCN allergic)
  • Take with meals to decrease GI upset
  • Take with water and sit up for 30 minutes
  • ADRs: discoloration of teeth, diarrhea, rash, photosensitivity, urticaria, black tongue, elevated LFTs, Jarisch-Herxheimer rxn
  • Preg. category D (will only use for pregnancy with RMSF)
  • Drug interactions: PCN, digoxin, anticoagulents, Al, Ca, Mg, Fe, barbituates
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11
Q

Minocycline

A
  • Tetracycline
  • Similar to doxycycline
  • More lipid soluble
  • Excellent CSF penetration
  • Causes vestibular probs. in some pts (vertigo, ataxia)
  • 100% bio availability
  • ADRs: GI, N/V, teeth discoloration/deformity, hepatotoxicity, skin hyperpigmentation with long-term use
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12
Q

Democlocyline

A
  • Tetracycline
  • Similar indications to tetracyclines
  • Used primarily for SIADH
  • Decreases collecting tubule response to ADH, increases water secretion
  • Expensive
  • Avoid in renal insufficiency
  • Similar ADRs and drug interactions
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13
Q

Fluoroquinolones

A
  • Ciprofloxacin, ofloxacin, levofloxacin, moxifloxacin, gemifloxacin
  • MOA: Inhibits DNA synthesis (DNA gyrase and topoisomerase IV)
  • Bactericidal
  • Post abx effect (1-2 hrs)
  • Broad spectrum
  • Indications: inpatient CAP (FIRST-LINE), outpt. CAP with comorbidities (FIRST-LINE), acute pyelonephritis (FIRST-LINE)
  • Conc > serum: lung, kidneys, prostate tissue
  • Conc < serum: prostatic tissue fluid, bone, CSF
  • Respiratory FQs: levofloxacin, moxifloxacin
  • Not recommended in kids < 16 y/o (joint cart. injury)
  • Pregnancy cat. C
  • Renal dose adjustment
  • Long QT
  • CDAD
  • Drug Interactions: Al, Mg, Ca antacids, CYP450 interactions
  • ADRs: N/V, HA, dizziness, confusion, insomnia, delirius, hallucinations, Torsades depointes, arthralgias, tendinitis, polyneuropathy (rare), blood sugar abnormalities (rare)
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14
Q

Ciprofloxacin (Cipro)

A
  • Fluoroquinolone
  • Greatest potency for gram - rods
  • Poor activity against MSSA and Strep pneumoniae
  • Indications: UTI, bone/join infxns, diarrhea, SSTI, etc.
  • Administer w/ or w/o food, but avoid dairy
  • ADRs: N/D, HA, malaise, insomnia, candidal vaginitis, CDAD
  • Rare ADRs: QTC prolongation, torsades de pointes, arrhythmias, tendinopathy/rupture, interstitial nephritis
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15
Q

Levofloxacin (Levaquin)

A
  • Fluoroquinolone
  • Gram -, gram +
  • Indications: chronic bronchitis, CAP, HAP, SSTIs, intra-abdominal infxns
  • Oral bioavailabiity 99%
  • Renal dosing adjustment
  • ADRs: dysglycemias, QTC prolongation, torsades de pointes, arrhythmias, N/D, institial nephritis, photosensitivity
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16
Q

Moxifloxacin (Avelox)

A
  • Fluoroquinolone
  • Gram -, Gram +, MRSA, S pneumonia
  • best FQ activity against enteric pathogens
  • Indications: intra-abdominal infxns, SSTI, anthrax, plague, chronic bronchitis, CAP, bacterial conjunctivitis, sinusitis
  • Safety/efficacy not est. in < 18 y/o
  • ADRs: dysglycemias, QTC prolongation, torsades de pointes, arrhythmias, N/V, interstitial nephritis, HA, peripheral neuropathy, photosensitivity
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17
Q

Gatifloxacin (Zymaxid)

A
  • Fluoroquinolone
  • Indicated for bacterial conjunct. in pts > 1 y/o
  • ADRs: worsening conjunctivitis, dysguesia, eye irritation and pain
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18
Q

Sulfonamides

A
  • Sulfadiazine, sulfamethoxazole, sulfacetamide, sulfasalazine
  • Structural analogs of PABA - block folate production
  • Bacteriostatic
  • Increasing problems with resistance
  • Pseudomonas is resistant, poor anaerobe activity
  • Combined with trimethoprim
  • Distributes into CSF and crosses placenta
  • Dependent on renal function
  • Indications: UTI, MRSA, nocardiosis, toxoplasmosis, PCP pneumonia, traveler’s diarrhea, AOM, acute exac. of chronic bronchitis, shigellosis
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19
Q

Sulfamethoxazole/Trimethoprim

Cotrimoxazole

A
  • Sulfonamide
  • Trimethoprim: dihydrofolate reductase inhib.
  • Inhibits bacterial nucleic acids and proteins
  • Makes SMZ bactericidal
  • Contraindications: megaloblastic anemia, pregnancy (can cause kernicterus), lactation
  • Renal adjustment
  • ADRs: generally well tolerated, fever, HA, dizziness, rash, allergic rxn, GI intolerance, photosensitivity, hepatitis, bone marrow suppression, hemolytic anemia (G6PD deficiency), crystalluria
  • Rare ADRs: SJS, TEN, serum sickness, fever, aseptic meningitis
  • Drug Interactions: cyclosporine, PABA derivatives, phenytoin, sulfonylureas, warfarin, ACEI/ARB, age 66+
    (may cause sudden death)
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20
Q

Silver Sulfadiazine

A
  • Sulfonamide
  • Topical
  • Inhibits growth of nearly all bacteria and fungi
  • Used for prevention of bacterial growth in burns
  • NOT used for established infxn
  • Contraindications: pregnancy, premature babies, newborns
  • ADRs: well tolerated, burning, rash, itching
  • Transient leukopenia - WBC count decreases
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21
Q

Sulfacetamide (Bleph-10, Bephamide)

A
  • Sulfonamide
  • Indicated for conjunctivitis
  • Also used in creams, lotions, gels for seborrheic dermatitis, acne
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22
Q

Sulfasalazine (Azulfidine)

A
  • Sulfonamide

- Used for ulcerative colitis

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23
Q

Aminoglycosides

A
  • Gentamicin, tobramycin, amikacin, streptomycin, neomycin
  • MOA: inhibit protein synthesis (30s)
  • Bactericidal
  • Primarily gram - coverage, some gram +
  • Tissue penetration not good (esp. adipose)
  • Eliminated entirely by glomerular filtration
  • Burn and cystic fibrosis patients require higher dosing
  • Extended interval dosing
  • Indications: pyelonephritis, UTI w/ resistant organisms, ophthalmic/otic infxns, osteomyelitis (abx beads)
  • Tobramycin given via inhalation to cystic fibrosis pts
  • Ototoxicity: vestibular and auditory dysfunction, can result in permanent hearing loss and balance issues, tinnitus, more common with amikacin and neomycin
  • ADRs: vertigo, ataxia, HA, N/V, positive Romberg test
  • Nephrotoxicity: damage to kidney tubules, usually reversible (neomycin greatest risk)
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24
Q

Fosfomycin (Monurol)

A
  • UTI drug
  • Broad spectrum
  • Bactericidal
  • Indicated for tx of uncomplicated UTI due to E. coli and E. faecalis
  • ADRs: CDAD, N/D, vaginitis, HA, rhinitis
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25
Q

Nitrofurantoin (Macrodantin, Macrobid)

A
  • UTI drug
  • Prodrug
  • Disrupts ribosomal RNA, DNA
  • Bactericidal, particularly in urine
  • Used for uncomplicated UTI
  • Spectrum: enterococcus, E. coli, proteus, pseudomonas
  • ADRs: N/V/D, hypersensitivity rxns
  • Rare ADRs: chronic hepatitis, neurologic manifestations, institial pulmonary fibrosis in long-term use
  • OK for pregnancy
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26
Q

Phenazopyridine (Pyridium)

A
  • UTI drug
  • NOT an abx (urinary tract analgesic)
  • Relieves burning, dysuria, frequency, urgency
  • Turns urine orange/red
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27
Q

IDSA Guidelines for Pyelonephritis

A

Ciprofloxacin, Levofloxacin, or SMX-TMP

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28
Q

Vancomycin (Vancocin)

A
  • MRSA Med
  • Inhibits bacterial cell wall synthesis
  • Bactericidal, except enterococcus
  • Active against gram +
  • Indications: bone/joint infxns, pneumonia, septicemia, endocarditis for PCN allergic pts, CDAD (second-line after metronidazole)
  • ADRs: Red man syndrome (flushing of chest/face, hypotension, pruritus), phlebitis, renal toxicity
  • Rare ADRs: drug rush, ototoxicity, blood dyscrasias
  • Therapeutic drug monitoring (peak and trough levels)
  • Dose with actual body weight
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29
Q

Linezolid (Zyvox)

A
  • MRSA Med
  • Oxazolidinone
  • Inhibits protein synthesis (50s)
  • Activity against Gram + (Streph, strep, MRSA, VRE, VRSA)
  • Indications: HAP, CAP, VRE, SSTI
  • Lots of off-label uses
  • 100% bioavailability
  • Eliminated in urine
  • ADRs: N/V/D, pancytopenia, HA, lactic acidosis
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30
Q

Tedizolid (Sivextro)

A
  • MRSA Med
  • Oxazolidinone
  • Same MOA as linezolid
  • Indications: SSTIs caused by Staph, Strep and enterococcus
  • Warnings: neutropenia, CDAD
  • ADRs: N/V/D, HA, dizziness
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31
Q

Lipoglycopeptides

A
  • Class of MRSA Meds
  • Includes Oritavancin and Dalbavancin
  • MOA: interferes with cross-linking of peptidoglycan
  • Indications: ABSSSI, MRSA, Strep, enterococcus
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32
Q

ABSSSI

A
  • Acute Bacterial Skin and Skin Structure Infxn
  • Lesion > 75 cm squared in area
  • Cellulitis, wound infxn, abscess
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33
Q

Oritavancin (Orbactiv)

A
  • MRSA Med
  • Lipoglycopeptide
  • Injectable
  • Warnings: hypersensitivity, CDAD, osteomyelitis, infusion rxns (pruritus, urticaria, flushing)
  • Drug Interactions: warfarin, heparin
  • ADRs: HA, N/V/D, abscesses
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34
Q

Dalbavancin (Dalvance)

A
  • MRSA Med
  • Lipoglycopeptide
  • Injectable
  • Warnings: severe hypersensitivity rxns (rxn to fast infusion), CDAD, elevated LFTs
  • ADRs: N/D, HA
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35
Q

Mupirocin (Bactroban)

A
  • Miscellaneous MRSA drug
  • MOA: inhibits bacterial protein synthesis
  • Active against gram + (incl. MRSA) and gram -
  • Topical (cream and ointment)
  • Indications: impetigo, intranasal MRSA
  • ADRs: stinging, irritation, itching, tingling, burning, soreness, facial pain over maxillae, postnasal drip, sinusitis, rhinitis and conjunctivitis
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36
Q

Quinupristin-Dalfopristin (Synercid)

A
  • Miscellaneous MRSA drug
  • Streptogramin abx
  • Bactericidal
  • MOA: inhibits protein synthesis
  • Indications: serious or life-threatening VRE, complicated SSTI (MSSA, strep pyogenes)
  • does not cover E. faecalis
  • CYP 3A4 inhibitor
  • ADRs: arthalgias/myalgias, hyperbilirubinemia, CDAD
  • very expensive
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37
Q

Bezlotoxumab (Zinplava)

A
  • New C. Diff Med

- Indicated to reduce C. diff recurrence in adults receiving treatment and at risk for recurrence

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38
Q

Colistin (Polymyxin E)

A
  • Miscellaneous drug
  • Last line of defense for pandrug resistant organisms
  • Gram - coverage
  • Stopped using due to renal toxicity
  • MOA: increases cell membrane permeability
  • ADRs: neurotoxicity, hypersensitivity, urticaria, CDAD, itching, rash, fever, mild GI upset
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39
Q

Antifungal Drug Classes

A
  • Polyenes (amphotericin B and nystatin)
  • Imidazoles (ketoconazole, fluconazole, miconazole, clotrimazole)
  • Antimetabolite (flucytosine)
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40
Q

Amphotericin B

A
  • Antifungal Polyene
  • Broadest spectrum of action
  • MOA: binds ergosterol
  • Indications: progressive, potentially life-threatening fungal infxns, Candida infxns, leishmaniasis (second-line)
  • Pregnancy cat. B
  • Concentration dependent
  • Excreted slowly by kidneys (weeks - months)
  • Not advised during breast-feeding
  • Med errors (liposomal dosing diff.)
  • Do not exceed daily 1.5 mg/kg
  • Infusion rxns (give small dose first)
  • Nephrotoxicity (can be permanent), frequent monitoring recommended
  • Anaphylaxis, leukoencephalopathy
  • ADRs: hypotension, tachypnea, fever, chills, HA, anorexia, N/V/D, heartburn, anemia, generalized/muscle/joint pain, pain at injection site
    Drug Interactions: nephrotoxic agents, chemotherapy, aminoglycosides, cyclosporine, pentamidine, steroids, digoxin, flucytosine, imidazoles
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41
Q

Nystatin (Mycostatin)

A
  • Antifungal Polyene
  • Binds ergosterol
  • Little GI absorption
  • Fungistatic/fungicidal
  • Preg. category C
  • Indications: oral candidiasis, vulvovaginal candidiasis, diaper dermatitis, intestinal candidiasis
  • Contraindication: hypersensitivity
  • PO ADRs: N/V/D, stomach cramps, rash, urticaria (rare), SJS (rare), blistering, skin peeling
  • Vag ADRs: rash, burning sensation
  • abstain from sexual intercourse until tx completed
  • avoid tampons, tight diapers, etc.
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42
Q

Azole Antifungals

A
  • Fluconazole, itraconazole, voriconazole, posaconazole, terconazole, isavuconazium sulfate, ketoconazole
  • Widely used antifungal agents
  • MOA: inhibit conversion of lanosterol to ergosterol
  • Fungistatic to candida species
  • Voriconazole fungicidal for Aspergillus
  • Associated with QT prolongation and arrhythmias
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43
Q

Fluconazole (Diflucan)

A
  • Azole Antifungal
  • Yeasts
  • Indications: candidiasis, uncomplicated systemic infxns, skin infxns, prevention of candidiasis, cryptococcal meningitis
  • Contraindication: hypersensitivity, CYP 3A4 drugs that prolong QT interval
  • Distributes into CSF, eye, etc.
  • Renal adjustment
  • ADRs w/ single dose: generally mild, HA, N/D, abd. pain, dyspepsia, taste perversion
  • ADRs w/ multiple doses: N/V/D, HA, abd. pain
  • Rare ADRs: serious hepatic rxns, elevated LFTs, hepatic failure
  • Association with QT prolongation
  • Long half life (30 hrs)
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44
Q

Itraconazole (Sporanox)

A
  • Azole Antifungal
  • Broader spectrum of activity than fluconazole
  • Indications: blastomycosis, histoplasmosis, aspergillosis, onychomycosis, candidiasis (oropharyngeal and esophageal)
  • Contraindications: P450 3A4 inhibitors, triazolam or midazolam, ventricular dysfunction, breast feeding
  • Warnings: rare hepatic failure, neuropathy, hearing loss, CSF, COPD, renal disease
  • Gastric acid suppression decreases absorption (take with soda)
  • ADRs: N/V, rash, hearing loss, gynecomastia (rare)
  • Preg cat. C
  • Inhibits CYP 3A4
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45
Q

Vorizonazole (Vfend)

A
  • Azole Antifungal
  • Broad spectrum
  • Enhanced activity against Aspergillus species
  • Indications: aspergilliosis, candidal infxns
  • Preg. category D
  • IV form can be nephrotoxic in renal insufficiency
  • Metabolized by P450
  • Monitor liver fxn during tx
  • ADRs: visual disturbances, fever, N/V, rash, chills, HA, abnormal LFTs, tachycardia, hallucinations, galactose intolerance, infusion rxns, SJS, TEN, photosensitivity
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46
Q

Posiconazole (Noxafil)

A
  • Azole Antifungal
  • Broadest spectrum
  • Uses: prophylaxis of aspergillus and candidias infxns in immunocompromised (FIRST-LINE)
  • Poor bioavailability (must be taken w/ food)
  • ADRs: fever, N/V/D, HA, elevated LFTs
  • Strong inhibitor of CYP 3A4
  • Preg. cat C
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47
Q

Ketoconazole

A
  • Azole Antifungal
  • Endemic mycoses, Candida
  • Largely replaced by itraconazole due to fewer side effects
  • Preg. cat C
  • ADRs: N/V/D, abd. pain, HA, nervousness, dizziness, somnolence, suicidal tendencies, severe depression, photophobia, impotence , thrombocytopenia, hemolytic anemia, leukopenia, fetal hepatoxicity, hyperlipidemia, pruritus, association with long QT syndrome
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48
Q

Isavuconazium sulfate (Cresemba)

A
  • Azole antifungal
  • Prodrug
  • Indications: invasive aspergillosis and mucormycosis
  • Inhibitor of CYP 3A4 (contraindicated w/ 3A4 inhibitors)
  • ADRs: LFT elevations, infusion rxns, SJS/TEN, N/V/D, peripheral edema, hypokalemia
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49
Q

Efinaconazole (Jublia)

A
  • Azole antifungal
  • 10% topical solution
  • Indication: onychomycosis
  • 48 wk tx
  • ADRs: ingrown toenails, application site dermatitis, application site vesicles, and application site pain
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50
Q

Allylamine Antifungals

A

Terbinafine, Naftifine, Butenafine

51
Q

Terbinafine (Lamisil)

A
  • Allylamine Antifungal
  • Fungicidal
  • Inhibits production of lanosterol
  • Half-life: 12 hrs
  • Steady state half life - 200-400 hrs
  • Indications: onychomycosis, tineae cruris, pedias, corporis
  • Oral ADRs: diarrhea, dyspepsia, abd. pain, LFT abnormalities, rash, pruritus, dysgeusia, SJS, TEN
52
Q

Naftifine (Naftin)

Butenafine (Lotrimin)

A
  • Allylamine Antifungals
  • Topicals for tinea infxns
  • ADRs: burning, stinging, itching, rash
53
Q

Flucytosine (Ancobon)

A
  • Misc. antifungal
  • MOA: - inhibits fungal protein/DNA synthesis
  • Indications: severe fungal infxns, candida species (septicemia, endocarditis, UTI, pulmonary infxns), cryptococcus infxns (meningitis)
  • Can be used with ampho B (increases therapeutic action and toxicity)
  • Preg cat C
  • Renal adjustment
  • ADRs: leukopenia and thrombocytopenia, rash, N/V/D, elevated LFTs (reversible)
  • Use w/ extreme caution in hepatic/renal pts or bone marrow suppression
  • Monitor blood, liver, and renal function
54
Q

Echinocandins

A
  • Misc. antifungal
  • Caspofungin, Anidulafungin, Micafungin
  • MOA: inhibit beta-glucan synthesis, causes cell lysis
  • Indications: severe invasis fungal infxns (candida, aspergillus)
  • No P450 interaction
  • ADRs: N/V/D, infusion rxns, hepatotoxicity (rare)
55
Q

Griseofulvin

A
  • Misc. antifungal
  • MOA: inhibits fungal cell mitosis
  • No activity against Candida
  • Indicated for tinea infxns
  • Tinea capitis - FIRST LINE
  • ADRs: HA, neuropathy, insomnia, fatigue, rash, hepatotoxicity
  • May be 3A4 inhibitor
  • Contraindications: P450 substrates, oral contraceptives, alcohol
56
Q

Ciclopirox (Loprox, Penlac)

A
  • Misc. antifungal
  • Indications: dermatophyte infxns, tinea, onychomycosis, and candida
  • Fungicidal - inhibits growth
  • Lotion, cream, nail lacquer, shampoo
  • ADRs: burning, itching, irritation
  • Preg. cat B
57
Q

Tavoborole (Kerydin)

A
  • Misc. antifungal
  • Oxaborole antifungal
  • Inhibits fungal protein synthesis
  • Topical (48 wks)
  • ADRs: application site exfoliation, erythema, dermatitis, ingrown toenail
58
Q

Antimalarials

A
  • Chloroquine, atovaquone-proguanil, artemisinin derivatives, mefloquine, quinine and quinidine, sulfa combination drugs, halofantrine
  • Chloroquine is drug of choice depending on where infxn acquired
59
Q

Chloroquine (Aralen)

A
  • Antimalarial
  • Drug of choice if infxn from: C. America west of Panama Canal, Haiti, D.R., and most of Middle East
  • Also used to treat lupus
  • Acts on asexual intraerythrocytic forms
  • Useful for tx or prophylaxis
  • Limited efficacy against P. falciparum
  • Resistant strains of P. vivax emerging
  • Safe in children and pregnancy
  • ADRs: N/V, abd. pain, HA, blurred vision, pruritus
  • Pruritus major side effect (more common in dark-skinned) - offer antihistamines, continue use
60
Q

Atovaquone and Proguanil (Malarone)

A
  • Antimalarial
  • Inhibits DNA synthesis
  • Effective against asexual intraerythrocytic stages
  • Use in adult and peds tx and prophylaxis
  • First line for CQ resistance
  • Take with food
  • ADRs: N/V/D, abd. pain, HA, rash
  • Drug interactions: highly protein-bound, rifampin (P450 inducer), tetracycline
61
Q

Artemisinins

A
  • Class of antimalarial drugs
  • Artemether, artesunate
  • Artemether/lumefantrine (Coartem)
  • First line alternative
  • ADRs: neurological changes, decreased neutrophil counts, increased liver enzymes, hypersensitivity
  • Not recommended for preg or kids < 5 kg
62
Q

Primaquine

A
  • Antimalarial
  • Acts on gametocytes, hypnozoites
  • Weak against asexual blood stage parasites
  • Primarily used as post-exposure prophylaxis and radical cure for P. vivax and P. ovale
  • Contraindicated in G6PD deficiency and pregnancy
  • Use in P. vivax and P. ovale infxns
  • Check G6PD level (can cause hemolysis in deficient pts)
  • Partial resistance in Oceania and Southeast Asia (double dose)
  • If pregnant, use CQ weekly until delivery or until end of breast-feeding, then switch to primaquine
63
Q

Quinine

A
  • Antimalarial
  • Acts against asexual erythrocytic stages
  • Used for treatment of all 4 species
  • Narrow therapeutic window (2.8 g fatal dose)
  • ADRs: cinchonism (tinnitus, visual disturbances, HA, dysphoria, N/V, postural hypotension), hypoglycemia, hypotension, GI, CV (long QT), skin manifestations
  • Antagonizes myasthenia gravis symptoms
  • Off-label use: leg cramps
64
Q

Mefloquine (Lariam)

A
  • Antimalarial
  • Acts on asexual intraerythrocytic forms
  • Effective prophylaxis against CRPF
  • Start 2 wks before travel, weekly through 4 weeks after
  • Not indicated for use in pregnancy and < 5 kg
  • ADRs: neuropsychiatric rxns, cardiac dysrhythmias, vomiting in children
  • Resistance is limited to SE Asia
65
Q

Antimalarial Chemoprophylaxis

A
  • Prevents disease, not infxn
  • Appropriate for non-immune travelers
  • Practical only for some populations in endemic areas
  • Consider: immune status, intensity/duration of exposure, parasite drug resistance, resources for dx and tx
66
Q

Atovaquone (Mepron)

A
  • Antiparasite
  • Use: for tx or prevention of mild to moderate Pneumocystis jiroveci pneumonia in pts. who cannot tolerate TMP-SMX
  • Preg cat C
  • Drug interactions: rifampin
  • ADRs: N/V/D, rash, HA, hypoglycemia, hypotension, pancytopenia
67
Q

Miltefosine (Impavido)

A
  • Leishmaniasis
  • Orphan drug destination
  • Also used for Naegleria fowler primary amoebic meningoencephalitis
  • Contraindications: pregnancy (use contraception if taking)
  • ADRs: N/V/D, HA, decreased appetite, dizziness, abd. pain, itching, drowsiness, elevated LFTs and sCr
68
Q

Metronidazole (Flagyl)

A
  • Nitroimidazole
  • Antiprotozoal and antibacterial
  • Use: CDAD (FIRST LINE), amebiasis, giardiasis, trichomoniasis, rosacea, bacterial vaginosis, serious infxns
  • MOA: bactericidal, forms free radicals inside cells
  • PK: crosses BBB, liver metabolism, no renal adjustment
  • Contraindications: first trimester of pregnancy with trichomoniasis, hypersensitivity
  • Warnings: CNS effects, seizures, encephalopathy, neuropathy, aseptic meningitis, plasma clearance decreased in elderly and patients with liver disease
  • Dose adjust with severe hepatic impairment
  • ADRs: CNS effects, N/V/D, abd. cramps, HA, anorexia, dysgeusia, black hairy tongue, candidiasis, leukopenia
  • Drug interactions: alcohol, disulifiram, warfarin, lithium, phenobarbital
69
Q

Tinidazole (Tindamax)

A
  • Nitroimidazole
  • Antiparasite
  • Indications: trichomoniasis, bacterial vaginosis, amebiasis, giardasis
  • Off-label: H pylori eradication (not first-line)
  • Disulfiram rxn, neuropathy, seizures, metallic taste, nausea, weakness, fatigue
70
Q

Antihelmintics

A
  • Mebendazole
  • Abendazole
  • Praziquantel
71
Q

Mebendazole (Vermex)

A
  • Antihelmintic
  • Effective for hookworms, roundworms, pinworms, and whipworms
  • Inhibits formation of worm microtubules
  • Prevents uptake of glucose
  • Only 10% absorbed systemically (improved w/ fatty food)
  • Eliminated in urine as inactive metabolites
  • Monitor liver function and CBC during tx (rare neutropenia and agranulocytosis)
  • ADRs: abd. pain, diarrhea, rash, urticaria, angioedema in allergic rxns
  • Rare ADRs: seizures, hepatitis, elevation of LFTs
  • Preg cat. C (found in breast milk but ok)
72
Q

Albendazole (Albenza)

A
  • Antihelmintic
  • Effective for tapeworms
  • Inhibits formation of worm microtubules
  • Poorly absorbed systemically (improved w/ fatty food)
  • Eliminated in urine as inactive metabolites
  • ADRs: abd. pain, N/V, HA, dizziness, vertigo, alopecia, fever, elevation of LFTs
  • Rare ADRs: fatal agrunlocytosis, pancytopenia (greater risk in pts with liver dz), increased bone marrow suppression
  • Monitor CBC (baseline and q 2 wks)
  • Eye exam prior to tx to rule out retinal involvement
  • Death of parasites may cause inflammatory reaction
  • Preg. cat. C (pts should avoid preg until 1 mo after tx)
  • Found in breast milk
  • Drug interactions: dexamethasone, praziquantel
73
Q

Praziquantel (Biltricide)

A
  • Antihelmintic
  • Cysticidal: affects parasite cell membrane permeability
  • Indicated for cysticercosis (caution if infection in brain)
  • Drug of choice: schistosomiasis, noninvasive tapeworm
  • Metabolized by CYP 3A4
  • Contraindications: rifampin, inhibited by grapefruit juice
  • Preg cat B
  • Appears in breast milk but ok
74
Q

Hepatitis B Agents

A 
Entecavir
Tenofovir
Adefovir
Lamivudine/Emtricitabine
Interferon alfa-2b/-n3/-2a
Peginterferon alfa-2a/-2b
75
Q

Entecavir (Baraclude)

A
  • Hepatitis B NRTI
  • Deoxyguanosine analogue
  • Inhibits base priming, reverse transcription, and synthesis of DNA
  • Available orally only (100% bioavailability)
  • Take on empty stomach
  • More potent than lamivudine and adefovir
  • Recommended for Hep B in patients 2-11 y/o
  • ADRs: generally well tolerated, rash, HA, fatigue, dizziness, N/V/D, cough, myalgia, risk of lactic acidosis (usually in pts w/ hepatotoxicity)
76
Q

Adefovir Dipivoxil (Hepsera)

A
  • Hepatitis B NRTI
  • Phosphonate nucleotide analog
  • Inhibits viral DNA polymerase and reverse transciptase
  • Available orally only
  • Activity includes HBV resistant to lamivudine and entecavir, HIV, pox, HSV
  • ADRs: well tolerated, asthenia, HA, diarrhea, abd. pain, nephrotoxicity at higher doses
  • Warnings: some risk of acute hepatitis when tx stopped, nephrotoxicity, lactic acidosis and hepatosteatosis, HIV resistance
77
Q

Interferon Alfa

A
  • Hepatitis B drug
  • MOA: not directly virucidl or virustatic
  • Induces changes in infected cells to promote resistance to virus
  • Induces enzyme activities
  • Indications: HBV, HCV
  • ADRs: flu-like syndrome (fevers/chills, HA, malaise, myalgia/arthalgia, N/V/D)
  • neuropsychiatric disturbances (depression, anxiety, somnolence, behavioral disturbances)
  • Local rxns, bone marrow suppression, thyroid dysfunction, seizures, cardiotoxicity, pulmonary toxicity
  • Monitoring: CDC, TSH, autoimmune concerns, ischemia, neuropsych issues, infxn
78
Q

Hepatitis C Agents

A
  • Elbasvir/grazoprevir
  • Ledipasvir/sofosbuvir
  • Simeprevir
  • Telaprevir
  • Ombitasvir/paritaprevir/ritonavir/dasabuvir
  • Ribavirin
  • Pegylated interferon
79
Q

Ribavirin

A
  • Hepatitis C Agent
  • Purine nucleoside analog
  • MOA: causes alterations to cellular nucleotide pools, inhibits RNA synthesis
  • ADRs: hemolytic anemia (major one), respiratory deterioration, depression, suicidal ideation, bacterial infxns, psychiatric effects, anxiety, fatigue, dizziness
80
Q

Sofosbuvir (Sovaldi)

A
  • Hepatitis C Agent
  • Nucleotide analogue hep C polymerase inhibitor
  • Cure rate: 80-90%
  • ADRs: well-tolerated, fatigue, HA
  • Drug Interactions: P450 inducers
81
Q

Ledipasvir-sofosbuvir (Harvoni)

A
  • Hep C Agent
  • Ledipasir: viral phosphoprotein inhibitor
  • Eliminates interferon and ribavirin from tx
  • well tolerated
  • interaction with amiodarone
  • first-line for genotype 1
82
Q

Elbasvir/Grazoprevir (Zepatier)

A
  • Indicated for Hep C genotypes 1 and 4
  • Breakthrough designation for use in patients on dialysis
  • ADRs: fatigue, HA, and nausea
  • Caution for elevated liver enzymes (contraindicated for liver impairment)
  • Drug interactions: phenytoin, carbamazepine, rifampin, St. John’s wort, efavirenz, some HIV meds, cyclosporine
83
Q

Daclatasvir (Daklinza)

A
  • Indications: Hep C genotype 3
  • combo with sofosbuvir
  • P450 substrate (interactions with inhibitors/inducers)
  • ADRs: HA, fatigue, N/D
  • Associated with symptomatic bradycardia when given with sofosbuvir and amiodarone
84
Q

Paritaprevir/ritonavir/ombitasvir/dasabuvir/ribavirin (Viekira Pak)

A
  • Hep C Agent
  • For genotype 1
  • Contraindicated in hepatic decompensation
  • Contraindicated with P450 drugs
  • FDA Warning: severe liver injury in pts with cirrhosis
  • ADRs: fatigue, nausea, pruritus, insomnia, asthenia, skin rxns, elevated LFTs with oral contraceptives
85
Q

Sofosbuvir/Velpatasvir (Epclusa)

A
  • Hep C Agent
  • First single tablet regimen for all genotypes (pan-genotypic)
  • ADRs: HA and fatigue, anemia, N/D, insomnia
  • Drug interactions: P450
86
Q

Influenza Antiviral Agents

A

Neuraminidase Inhibitors:
Oseltamivir (Tamiflu)
Zanamivir (Relenza)
Peramivir (Rapivab)

87
Q

Neuraminidase Inhibitors

A
  • Influenza Antiviral Class
  • Spectrum: Influenza A and B in both children and adults
  • Includes avian influenza and H5N1 dz
  • Indicated for both tx and prevention of influenza
  • Reduces flu duration by 1 day
  • Reduces severe clinical outcomes in hospitalized adults
  • PEP best within 48 hours of exposure (treat 10 days)
  • Best prevention is vaccine
88
Q

Oseltamivir (Tamiflu)

A
  • Influenza Med
  • ADRs: N/V, neuropsych
  • Preg. cat C
  • Renal adjustment
89
Q

Zanamivir (Relenza)

A
  • Influenza Med
  • Given via inhalation
  • ADRs: bronchospasm (can be fatal), hypersensitivity, oropharyngeal edema, rash, anaphylaxis, N/V/D, sinusitis, nasal and throat discomfort, bronchitis
  • Preg Cat. C
90
Q

Peramivir (Rapivab)

A
  • Influenza med
  • IV neuraminidase inhibitor
  • Renal adjustment
  • ADRs: diarrhea, skin rxns (SJS), neuropsych (hallucinations, delirium, abnormal behavior)
91
Q

Herpes Antivirals (HSV/VZV)

A
  • Oral Agents: Acyclovir, Valacyclovir, Famciclovir
  • Topical Agents: Acyclovir, Docosanol, Penciclovir
  • Ophthalmic: Trifluridine
92
Q

Acyclovir (Zovirax)

A
  • Herpes Antiviral
  • MOA: inhibits viral DNA synthesis and replication
  • Topical, oral and IV formulations
  • Spectrum: Herpes simplex 1 and 2, VZV, possibly EBV
  • Tx of choice for visceral, disseminated or CNS involvement
  • Preg. cat B (distributes into breast milk, crosses placenta)
  • Dependent on renan fxn
  • ADRs: phlebitis (IV), reversible renal toxicity, neuro symptoms (encephalopathic changes such as somnolence, hallucinations, confusion coma), diarrhea, vertigo, arthralgia, rash, HA, TTP/HUS, photosensitivity, anemia
93
Q

Valacyclovir (Valtrex)

A
  • Herpes Antiviral
  • Prodrug of acyclovir
  • Rapidly and almost completely converted to acyclovir
  • Available orally only
  • Spectrum: similar to acyclovir
  • ADRs: nausea, HA, weakness, dizziness, confusion
94
Q

Famciclovir (Famvir)

A
  • Herpes Antiviral
  • Converted to penciclovir in the liver and intestines
  • Available orally only
  • Spectrum: HSV 1 and 2, VZV, to a lesser extent, EBV in vitro activity to HBV
  • ADRs: HA, GI, abnormal LFTs
95
Q

Acyclovir Resistance

A
  • Mostly occurs in immunocompromised host
  • Three basic resistance mechanisms exist:
    1. Reduced or absent thymidine kinase
    2. Altered TK substrate specificity
    3. Alterations in DNA polymerase
  • Cross resistance to famciclovir and valacyclovir
96
Q

Penciclovir (Denavir)

A
  • Topical Herpes Antiviral

- Orolabial herpes

97
Q

Docosanol (Abreva)

A
  • Topical Herpes Antiviral
  • Orolabial herpes
  • MOA: interferes with viral fusion to host cell
98
Q

Trifluridine (Viroptic)

A
  • Topical Herpes Antiviral

- HSV Keratoconjunctivitis

99
Q

Anti-CMV Agents

A
  • Ganciclovir
  • Valganciclovir
  • Foscarnet
  • Cidofovir
100
Q

Ganciclovir (Cytovene, Vitraset)

A
  • Anti-CMV Agent
  • Spectrum: CMV, EBV, HSV/VZV
  • MOA: completely inhibits DNA polymerases; incorporated into viral DNA
  • ADRs: reversible pancytopenia (most common), fever, diarrhea, rash, phlebitis, confusion, renal dysfunction, psychiatric disturbances, seizures
  • Monitor CDC and renal function weekly
  • Drug interactions: Zidovudine, imipenem-cilastatin
101
Q

Valganciclovir (Valcyte)

A
  • Anti-CMV Agent
  • Drug of choice for most cases of CMV retinitis
  • Prodrug of ganciclovir
  • Available orally only
  • Spectrum: similar to ganciclovir
  • ADRs: similar to ganciclovir
102
Q

Foscarnet (Foscavir)

A
  • Anti-CMV Agent
  • MOA: selective inhibition at the pyrophosphate binding site on virus-specific DNA polymerase
  • IV only
  • ADRs: renal dysfunction (common), N/V, anemia, CNS disturbances, electrolyte abnormalities, seizures, arrhythmias, neutropenias
  • Renal adjustments
  • Monitor electrolytes, CBC, renal function wkly
103
Q

Cidofovir (Vistide)

A
  • Anti-CMV Agent
  • Selective inhibition of CMV DNA polymerase
  • Spectrum: CMV including acyclovir and foscarnet resistant strains, HSV 1 and 2, EBV
  • Also has activity against DNA viruses (papilloma, poxvirus, adenovirus, etc.)
  • Indicated for CMV retinitis in patients with AIDS
  • Rarely used due to nephrotoxicity
104
Q

HPV Papillomavirus Options

A
  • Imiquimod
  • Podofilox
  • Trichloroacetic Acid
  • Podophyllin
  • Cryotherapy
105
Q

Imiquimod (Aldara)

A
  • HPV Agent
  • immunomodulator
  • Topical tx
  • FIRST LINE for HPV external and perianal genital warts
  • Also indicated for BCC and actinic keratosis
  • ADRs: site rxns (pain, erythema, scarring, pruritus)
106
Q

Podofilox (Condylox)

A
  • HPV Agent
  • Topical tx
  • First-line alternative to imiquimod
  • ADRs: localized pain, burning, inflammation and erosion
  • systemic effects not reported
107
Q

Sinecatechins (Veregen)

A
  • Green tea extract
  • Clears anogenital warts after 10-16 wks of tx
  • ADRs: mild skin runs, hypersensitivity, narrowing of foreskin in uncircumcised males
108
Q

Trichloroacetic Acid (Tri-Chlor)

A
  • HPV Agent
  • Topical tx
  • Not approved by FDA
  • CDC recommends only if applied by provider
  • ADRs: severe burning, inflammation or tenderness
  • Can neutralize with soap or bicarb
109
Q

Antiretroviral Medications (HIV)

A 
NRTI
NNRTI
PI
Integrase Inhibitors
Fusion Inhibitors
CCR5 Antagonists
110
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTI)

A
  • Abacavir, tenofovir, emtricitabine
  • Competitive inhibitors of HIV reverse transcriptase
  • Uses: tx and prophylaxis of HIV
  • ADRs: lactic acidosis, hepatic steatosis, lipodystrophy (lipohypertrophy, lipoatrophy)
111
Q

Abacavir ADRs

A
  • Hypersensitivity rxns
  • Rash
  • Possible increased risk of MI
112
Q

Tenofovir ADRs

A
  • Renal impairment
  • Decrease in bone-mineral density
  • HA
  • GI introlerance
113
Q

NNRTI

A
  • “vir in the middle” (Efavirenz)

- ADRs: hepatoxicity, rash (inclu. SJS), drug interactions

114
Q

Integrase Inhibitors

A
  • “-gravir” (Elvitegravir)
  • ADRs:
    Dolutegravir - HA, insomnia, rash, hypersensitivity rxns
    Evitegravir - decrease CrCl, nephrotoxicity, N/D
    Raltegravir - N/D, rash, HA, CPK elevation
115
Q

Protease Inhibitors

A
  • “-navir”

- ADRs: hyperlipidemia, lipodystrophy, hepatotoxicity, GI intolerance, drug interactions

116
Q

Fusion Inhibitors

A

Enfuvirtide

  • Binds HIV envelope glycoprotein
  • Prevents viral fusion with target membrane
  • ADRs: injection-site rxn, hypersensitivity, rxns, increased risk of bacterial pneumonia
117
Q

CCR5 Antagonist

A

Maraviroc

  • binds CCR5 protein on human cell membrane, blocking HIV-1 from cell entry
  • ADRs: drug-drug interaction, rash, abd. pain, URI, cough, hepatotoxicity, musculoskeletal symptoms, orthostasis
118
Q

Pharmacokinetic Boosters

A

Ritonavir, Cobicistat
- Boost blood levels of other ARV meds
- Inhibit P450 3A4 enzymes
- ADRs:
Ritonavir: GI upset, hyperlipidemia, hyperglycemia, hepatitis
Cobicistat: GI upset, increased serum creatinine

119
Q

HIV Treatment Goals

A
  1. Reduce HIV-related morbidity
  2. Prolong duration and quality of survival
  3. Restore and/or preserve immunologic function
  4. Maximally and durably suppress HIV viral load
  5. Prevent HIV transmission
120
Q

HIV Testing

A
  1. CD4 counts
  2. HIV Viral Load
  3. Medication resistance testing
  4. Specific Testing (HLA*B701, CCR5)
121
Q

When HIV Tx is Strong Indicated:

A 
Pregnancy
Low CD4 counts (< 200 cell/mcl)
High viral load ( >100K copies/ml)
Concomitant hepatitis
AIDS-related symptoms
122
Q

Truvada

A

Tenofovir

Emtricitabine

123
Q

Atripla

A

Tenofovir
Emtricitabine
Efavirenz

124
Q

Stribild

A

Tenofovir
Emtricitabine
Cobicistat
Elvitegravir

Pharmacology Tests (1 decks)

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