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1
Q

Penicillin G

A

1) Gram-positive organisms (S. pneumoniae, S. pyogenes, Actinomyces) & syphillis; Bactericidal for gram-positive cocci, gram-positive rods, gram-negative cocci, & spirochetes; Not penicillinase resistant 2) IV Penicillin (Prototype Beta-lactam abx;Non-penicillinase resistant); Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes 3) Hypersensitivity rxns; Hemolytic anemia 4) Resistance: Beta-lactamases cleave Beta-lactam ring

2
Q

Penicillin V

A

1) Gram-positive organisms (S. pneumoniae, S. pyogenes, Actinomyces) & syphillis; Bactericidal for gram-positive cocci, gram-positive rods, gram-negative cocci, & spirochetes; Not penicillinase resistant 2) PO Penicillin (Prototype Beta-lactam abx;Non-penicillinase resistant); Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes 3) Hypersensitivity rxns; Hemolytic anemia 4) Resistance: Beta-lactamases cleave Beta-lactam ring

3
Q

Methicillin

A

1) S. aureua (except MRSA; resistant d/t altered PNC-binding protein target site) 2) PNC-Resistant PNCs; Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC). Narrow spectrum; Penicillinase resistant b/c of bulkier R-group 3) Hypersensitivity rxns; Interstitial nephritis (Methicillin specific)

4
Q

Nafcillin

A

1) S. aureua (except MRSA; resistant d/t altered PNC-binding protein target site) 2) PNC-Resistant PNCs; Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC). Narrow spectrum; Penicillinase resistant b/c of bulkier R-group 3) Hypersensitivity rxns 4) Use naf for staph!

5
Q

Dicloxacillin

A

1) S. aureua (except MRSA; resistant d/t altered PNC-binding protein target site) 2) PNC-Resistant; Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC). Narrow spectrum; Penicillinase resistant b/c of bulkier R-group 3) Hypersensitivity rxns

6
Q

Ampicillin

A

1) Extended-spectrum PNC–Haemophilus influenza, E. Coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella, enterococci (HELPSS kill enterococci) 2) AminoPNCs; Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC). Wider spectrum; Penicillinase sensitive. Also combine w/ clavulonic acid to protect against Beta-lactamase. 3) Hypersensitivity rxs; Ampicillin rash; Pseudomemranous colitis 4) Resistance: Beta-lactamases cleave Beta-lactam ring

7
Q

Amoxicillin

A

1) Extended-spectrum PNC–Haemophilus influenza, E. Coli, Listeria monocytogenes, Proteus mirabilis, Salmonella, Shigella, enterococci (HELPSS kill enterococci) 2) AminoPNCs; Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC). Wider spectrum; Penicillinase sensitive. Also combine w/ clavulonic acid to protect against Beta-lactamase. 3) Hypersensitivity rxs; Ampicillin rash; Pseudomemranous colitis 4) Resistance: Beta-lactamases cleave Beta-lactam ring; AmOxicillin has greater Oral bioavailability vs Ampicillin

8
Q

Ticarcillin

A

1) Pseudomonas spp. & gram-negative rods; Susceptible to penicillinase; Use w/ Clavulonic acid (to protect against Beta-lactamase) 2) Antipseudomonals; Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC). Extended spectrum 3) Hypersensitivity rxns 4) TCP (Ticarcillin, Carbenicillin, & Piperacillin)–Takes Care of Pseudomonas

9
Q

Carbenicillin

A

1) Pseudomonas spp. & gram-negative rods; Susceptible to penicillinase; Use w/ Clavulonic acid (to protect against Beta-lactamase) 2) Antipseudomonals; Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC). Extended spectrum 3) Hypersensitivity rxns 4) TCP (Ticarcillin, Carbenicillin, & Piperacillin)–Takes Care of Pseudomonas

10
Q

Piperacillin

A

1) Pseudomonas spp. & gram-negative rods; Susceptible to penicillinase; Use w/ Clavulonic acid (to protect against Beta-lactamase) 2) Antipseudomonals; Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC). Extended spectrum 3) Hypersensitivity rxns 4) TCP (Ticarcillin, Carbenicillin, & Piperacillin)–Takes Care of Pseudomonas

11
Q

Clavulonic Acid

A

1) Often added to PNC abxs to protect the abx from destruction by Beta-lactamase (penicillinase) 2) Beta-lactamase inhibitor 3) – 4) CAST (Clavulonic Acid, Sulbactam, & Tazobactam)

12
Q

Sulbactam

A

1) Often added to PNC abxs to protect the abx from destruction by Beta-lactamase (penicillinase) 2) Beta-lactamase inhibitor 3) – 4) CAST (Clavulonic Acid, Sulbactam, & Tazobactam)

13
Q

Tazobactam

A

1) Often added to PNC abxs to protect the abx from destruction by Beta-lactamase (penicillinase) 2) Beta-lactamase inhibitor 3) – 4) CAST (Clavulonic Acid, Sulbactam, & Tazobactam)

14
Q

Cefazolin

A

1) Gram-positive cocci, Proteus mirabilis, E. Coli, Klebsiella pneumoniae. **Cefazolin–used prior to surgery to prevent S. aureus wound infections. 2) Beta-lactam, 1st Generation Cephalosporins; Beta-lactam rx that inhibits cell wall synthesis but are less susceptible to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Orgs covered by 1st Generation=PEcK–Proteus mirabilis, E. Coli, Klebsiella pneumoniae; Orgs typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

15
Q

Cephalexin

A

1) Gram-positive cocci, Proteus mirabilis, E. Coli, Klebsiella pneumoniae 2) Beta-lactam, 1st Generation Cephalosporins; Beta-lactam rx that inhibits cell wall synthesis but are less susceptible to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Orgs covered by 1st Generation=PEcK–Proteus mirabilis, E. Coli, Klebsiella pneumoniae; Organisms typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

16
Q

Cefoxitin

A

1) Gram-positive cocci, Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. Coli, Klebsiella pneumoniae, Serratia marcescens 2) Beta-lactam, 2nd Generation Cephalosporins; Beta-lactam rx that inhibits cell wall synthesis but are less susceptibl to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Orgs covered by 2nd Generation=HEN PEcKS–Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. Coli, Klebsiella pneumoniae, Serratia marcescens; Organisms typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

17
Q

Cefaclor

A

1) Gram-positive cocci, Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. Coli, Klebsiella pneumoniae, Serratia marcescens 2) Beta-lactam, 2nd Generation Cephalosporins; Beta-lactam rx that inhibits cell wall synthesis but are less susceptibl to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Orgs covered by 2nd Generation=HEN PEcKS–Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. Coli, Klebsiella pneumoniae, Serratia marcescens; Organisms typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

18
Q

Cefuroxime

A

1) Gram-positive cocci, Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. Coli, Klebsiella pneumoniae, Serratia marcescens 2) Beta-lactam, 2nd Generation Cephalosporins; Beta-lactam rx that inhibits cell wall synthesis but are less susceptibl to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Orgs covered by 2nd Generation=HEN PEcKS–Haemophilus influenzae, Enterobacter aerogenes, Neisseria spp., Proteus mirabilis, E. Coli, Klebsiella pneumoniae, Serratia marcescens; Organisms typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

19
Q

Ceftriaxone

A

1) Serious gram-negative infections resistant to other Beta-lactams; **Ceftriaxone–meningitis & gonorrhea 2) Beta-lactam, 3rd Generation Cephalosporins; Beta-lactam rx that inhibits cell wall synthesis but are less susceptibl to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Organisms typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

20
Q

Cefotaxime

A

1) Serious gram-negative infections resistant to other Beta-lactams 2) Beta-lactam, 3rd Generation Cephalosporins; Beta-lactam rx that inhibits cell wall synthesis but are less susceptibl to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Organisms typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

21
Q

Ceftazidime

A

1) Serious gram-negative infections resistant to other Beta-lactams; **Ceftazidime–Pseudomonas. 2) Beta-lactam, 3rd Generation Cephalosporins; Beta-lactam rx that inhibits cell wall synthesis but are less susceptibl to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Organisms typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

22
Q

Cefepime

A

1) Increase activity against Pseudomonas & gram-positive orgs 2) Beta-lactam, 4th Generation Cephalosporins; Beta-lactam rx that inhibits cell wall synthesis but are less susceptibl to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Organisms typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

23
Q

Ceftaroline

A

1) **Only Cephalosporin that covers MRSA 2) Beta-lactam, **Newest Generation Cephalosporin; Beta-lactam rx that inhibits cell wall synthesis but are less susceptibl to penicillinases. Bactericidal 3) Hypersensitivity rxns, Vit K deficiency. Low cross-reactivity w/ Penicillins. Increased nephrotoxicity of Aminoglycosides. 4) Organisms typically not covered by Cephalosporins are LAME: Listeria, Atypicals (Chlamydia, Mycoplasma), MRSA & Enterococci. (Exception= Ceftaroline-covers MRSA)

24
Q

Aztreonam

A

1) Gram-negative rods only–No activity against gram-positives or anaerobes. For penicllin-allergic pts & those w/ renal insufficiency who cannot tolerate aminoglycosides 2) Beta-lactam, Monobactam; Resistant to Beta-lactamases. Prevents peptidoglycan cross-linking by binding to PBP3. Synergistic w/ Aminoglycosides. No cross-allergenicity w/ Penicillins. 3) Usually nontoxic; Occasional GI upset

25
Q

Meropenem

A

1) Gram-positive cocci, gram-negative rods, & anaerobes. Wide spectrum, but the significant side effects limit use to life-threatening infections, or after other drugs have failed. **Meropenem, however, has a reduced risk of seizures & is stable to dehydropeptidase I. 2) Beta-lactam, Carbapenem; Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC) 3) GI distress, Skin rash, & CNS toxicity (seizures) at high plasma levels

26
Q

Imipenem (w/ Cilastatin)

A

1) Gram-positive cocci, gram-negative rods, & anaerobes. Wide spectrum, but the significant side effects limit use to life-threatening infections, or after other drugs have failed. *Meropenem, however, has a reduced risk of seizures & is stable to dehydropeptidase I. 2) Beta-lactam, Carbapenem; *Imipenem–broad-spectrum, Beta-lactamase-resistant carbapenem. Bind PNC-binding proteins; Block transpeptidase cross-linking of peptidoglycan; Activates autolytic enzymes (=Same MOA as PNC). **Always administered w/ Cilastatin (inhib of renal dehydropeptidase I) to decrease inactivation of drug in renal tubules. 3) GI distress, Skin rash, & CNS toxicity (seizures) at high plasma level

27
Q

Vancomycin

A

1) Gram-positive only–serious, amultidrug-resistant orgs, including MRSA, enterococci, & C. difficile (oral dose for pseudomembranous colitis) 2) Antimicrobial; Inhib cell wall peptidoglycan formation by binding D-ala D-ala portion of cell wall precursors. Bactericidal. 3) Nephrotoxicity, Ototoxicity, Thrombophlebitis, diffuse flushing–red man syndrome (can largely prevent by pretreatment w/ antihistamines & slow infusion rate). Well tolerated in general (–does NOT have many problems) 4) Resistance: Occurs w/ amino acid change of D-ala D-ala to D-ala D-lac. [“Pay back 2 D-alas (dollars) for VANdalizing (VANcomycin)]

28
Q

Streptomycin

A

1) Severe gram-negative rod infections. Synergistic w/ Beta-lactam Abs. 2) Aminoglycoside; Bactericidal. Inhibits formation of initiation complex & cause misreading of mRNA. Also block translocation. Req O2 for uptake; therefore, ineffective against anaerobes. (A “initiates” the Alphabet) 3) Nephrotoxicity (esp when used w/ Cephalosporins), Neuromuscular blockade, Ototoxicity (esp when used w/ Loop diuretics). Teratogen. 4) Resistance: Transferase enzymes that inactivate the drug by acetylation, phosphorylation, or adenylation. 4) Aminoglycoside Rxs & ADES: “MEAN”=(aMINoglycosides) GNATS caNNOT kill anaerobes–Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin, Nephrotox, Neuromuscular blockade, Ototoxicity, Teratogen

29
Q

Tobramycin

A

1) Severe gram-negative rod infections. Synergistic w/ Beta-lactam Abs. 2) Aminoglycoside; Bactericidal. Inhibits formation of initiation complex & cause misreading of mRNA. Also block translocation. Req O2 for uptake; therefore, ineffective against anaerobes. (A “initiates” the Alphabet) 3) Nephrotoxicity (esp when used w/ Cephalosporins), Neuromuscular blockade, Ototoxicity (esp when used w/ Loop diuretics). Teratogen. 4) Resistance: Transferase enzymes that inactivate the drug by acetylation, phosphorylation, or adenylation. 4) Aminoglycoside Rxs & ADES: “MEAN”=(aMINoglycosides) GNATS caNNOT kill anaerobes–Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin, Nephrotox, Neuromuscular blockade, Ototoxicity, Teratogen

30
Q

Amikacin

A

1) Severe gram-negative rod infections. Synergistic w/ Beta-lactam Abs. 2) Aminoglycoside; Bactericidal. Inhibits formation of initiation complex & cause misreading of mRNA. Also block translocation. Req O2 for uptake; therefore, ineffective against anaerobes. (A “initiates” the Alphabet) 3) Nephrotoxicity (esp when used w/ Cephalosporins), Neuromuscular blockade, Ototoxicity (esp when used w/ Loop diuretics). Teratogen. 4) Resistance: Transferase enzymes that inactivate the drug by acetylation, phosphorylation, or adenylation. 4) Aminoglycoside Rxs & ADES: “MEAN”=(aMINoglycosides) GNATS caNNOT kill anaerobes–Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin, Nephrotox, Neuromuscular blockade, Ototoxicity, Teratogen

31
Q

Neomycin

A

1) Severe gram-negative rod infections. Synergistic w/ Beta-lactam Abs.; *Neomycin–for bowel surgery 2) Aminoglycoside; Bactericidal. Inhibits formation of initiation complex & cause misreading of mRNA. Also block translocation. Req O2 for uptake; therefore, ineffective against anaerobes. (A “initiates” the Alphabet) 3) Nephrotoxicity (esp when used w/ Cephalosporins), Neuromuscular blockade, Ototoxicity (esp when used w/ Loop diuretics). Teratogen. 4) Resistance: Transferase enzymes that inactivate the drug by acetylation, phosphorylation, or adenylation. 4) Aminoglycoside Rxs & ADES: “MEAN”=(aMINoglycosides) GNATS caNNOT kill anaerobes–Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin, Nephrotox, Neuromuscular blockade, Ototoxicity, Teratogen

32
Q

Gentamicin

A

1) Severe gram-negative rod infections. Synergistic w/ Beta-lactam Abs. 2) Aminoglycoside; Bactericidal. Inhibits formation of initiation complex & cause misreading of mRNA. Also block translocation. Req O2 for uptake; therefore, ineffective against anaerobes. (A “initiates” the Alphabet) 3) Nephrotoxicity (esp when used w/ Cephalosporins), Neuromuscular blockade, Ototoxicity (esp when used w/ Loop diuretics). Teratogen. 4) Resistance: Transferase enzymes that inactivate the drug by acetylation, phosphorylation, or adenylation. 4) Aminoglycoside Rxs & ADES: “MEAN”=(aMINoglycosides) GNATS caNNOT kill anaerobes–Gentamicin, Neomycin, Amikacin, Tobramycin, Streptomycin, Nephrotox, Neuromuscular blockade, Ototoxicity, Teratogen

33
Q

Minocycline

A

1) Borrelia burgdorferi, M. pneumoniae. Drug’s ability to accumulate intracellularly makes it very effective against Rickettsia & Chlamydia. 2) Tetracycline; Bacteriostatic. Bind to 30S & present attachment of aminoacyl-tRNA; Limited CNS penetration. Do not take w/ milk, antacids, or iron-containing preparations b/c divalent cations inhib its absorption in the gut 3) GI distress, Discoloration of teeth & inhib of bone growth in children, Photosensitivity. Contraindicated in pregnancy. 4) Resistance: Decreased uptake into cells or Increased efflus of cell by plasmid-encoded transport pumps.

34
Q

Demeclocycline

A

1) Acts as diuretic in SIADH; *Rarely used as antibiotic (Role of abx= Borrelia burgdorferi, M. pneumoniae. Drug’s ability to accumulate intracellularly makes it very effective against Rickettsia & Chlamydia.) 2) Tetracycline; MOA in SIADH tx=ADH antagonist; MOA as abx=Bacteriostatic. Bind to 30S & present attachment of aminoacyl-tRNA; Limited CNS penetration. Do not take w/ milk, antacids, or iron-containing preparations b/c divalent cations inhib its absorption in the gut 3) GI distress, Discoloration of teeth & inhib of bone growth in children, Photosensitivity. Contraindicated in pregnancy. 4) Resistance: Decreased uptake into cells or Increased efflus of cell by plasmid-encoded transport pumps.

35
Q

Doxycycline

A

1) Borrelia burgdorferi, M. pneumoniae. Drug’s ability to accumulate intracellularly makes it very effective against Rickettsia & Chlamydia. 2) Tetracycline; Bacteriostatic. Bind to 30S & present attachment of aminoacyl-tRNA; Limited CNS penetration. *Doxycycline is fecally eliminated & can be used in pts w/ renal failure. Do not take w/ milk, antacids, or iron-containing preparations b/c divalent cations inhib its absorption in the gut 3) GI distress, Discoloration of teeth & inhib of bone growth in children, Photosensitivity. Contraindicated in pregnancy. 4) Resistance: Decreased uptake into cells or Increased efflus of cell by plasmid-encoded transport pumps.

36
Q

Tetracycline

A

1) Borrelia burgdorferi, M. pneumoniae. Drug’s ability to accumulate intracellularly makes it very effective against Rickettsia & Chlamydia. 2) Tetracycline; Bacteriostatic. Bind to 30S & present attachment of aminoacyl-tRNA; Limited CNS penetration. Do not take w/ milk, antacids, or iron-containing preparations b/c divalent cations inhib its absorption in the gut 3) GI distress, Discoloration of teeth & inhib of bone growth in children, Photosensitivity. Contraindicated in pregnancy. 4) Resistance: Decreased uptake into cells or Increased efflus of cell by plasmid-encoded transport pumps.

37
Q

Erythromycin

A

1) Atypical pneumonias (Mycoplasma, Chlamydia, Legionella), STDs (for Chlamydia), & gram-positive cocci (Strep infections in pts allergic to penicillins) 2) Macrolide; Inhib protein synth by blocking translocation; Bind to 23S rRNA of 50S ribosomal subunit. Bacteriostatic. 3) Motility issues, Arrhythmia caused by prolonged QT, acute Cholecstatic hepatitis, Rash, eOsiniphilia (=MACRO). Increases serum concentration of theophyllines, oral anticoagulants. 4) Resistance: Methylation of 23S rRNA binding site.

38
Q

Clarithromycin

A

1) Atypical pneumonias (Mycoplasma, Chlamydia, Legionella), STDs (for Chlamydia), & gram-positive cocci (Strep infections in pts allergic to penicillins) 2) Macrolide; Inhib protein synth by blocking translocation; Bind to 23S rRNA of 50S ribosomal subunit. Bacteriostatic. 3) Motility issues, Arrhythmia caused by prolonged QT, acute Cholecstatic hepatitis, Rash, eOsiniphilia (=MACRO). Increases serum concentration of theophyllines, oral anticoagulants. 4) Resistance: Methylation of 23S rRNA binding site.

39
Q

Azithromycin

A

1) Atypical pneumonias (Mycoplasma, Chlamydia, Legionella), STDs (for Chlamydia), & gram-positive cocci (Strep infections in pts allergic to penicillins) 2) Macrolide; Inhib protein synth by blocking translocation; Bind to 23S rRNA of 50S ribosomal subunit. Bacteriostatic. 3) Motility issues, Arrhythmia caused by prolonged QT, acute Cholecstatic hepatitis, Rash, eOsiniphilia (=MACRO). Increases serum concentration of theophyllines, oral anticoagulants. 4) Resistance: Methylation of 23S rRNA binding site.

40
Q

Chloramphenicol

A

1) Meningitis (Haemophius influenzae, Neisseria meningitidis, Streptococcus pneumoniae). Conservative use d/t toxicities but often still used in developing countries b/c of low cost 2) Protein Synthesis Inhib; Blocks peptidyltransfease at 50s ribosomal subunit. Bacteriostatic 3) Anemia (dose dep), Aplastic aneima (dose dep), Gray baby syndrome (in premature infants b/c lack liver UDP-glucuronyl transferase) 4) Resistance: Plasmid-encoded acetyltransferase that inactivates drug

41
Q

Clindamycin

A

1) Anaerobic infections (e.g., Bacteroides fragilis, Clostridium perfringens) in aspiration pneumonia or lung abscesses. Also oroal infections w/ mouth anaerobes. 2) Protein Synthesis Inhib; Block peptide transfer (transpeptidation at 50s ribosomal subunit. Bacteriostatic. 3) Pseudomembranous colitis (C. dificile overgrowth), fever, diarrhea. 4) Clindamycin tx anaerobes ABOVE the diaphragm vs Metronidazole (which tx anaerobes BELOW the diaphragm)

42
Q

Sulfadiazine

A

1) Gram-positive, gram-negative, Nocardia, Chlamydia. Triple sulfas or SMX for simple UTI. 2) Sulfonamides; PABA antimetabolites inhib dihydropteroate synthase. Bacteriostatic. 3) Hypersensitivity rxns, Hemolysis if G6PD deficient, Nephrotoxicity (tubulointerstitial nephritis), Photosensitivity, Kernicterus in infants, Displace other drugs from albumin (e.g. Warfarin) 4) Resistance: Altered enzyme (bacterial dihydropteroate synthase), Decreased uptake, or Increased PABA synthesis

43
Q

Sulfisoxazole

A

1) Gram-positive, gram-negative, Nocardia, Chlamydia. Triple sulfas or SMX for simple UTI. 2) Sulfonamides; PABA antimetabolites inhib dihydropteroate synthase. Bacteriostatic. 3) Hypersensitivity rxns, Hemolysis if G6PD deficient, Nephrotoxicity (tubulointerstitial nephritis), Photosensitivity, Kernicterus in infants, Displace other drugs from albumin (e.g. Warfarin) 4) Resistance: Altered enzyme (bacterial dihydropteroate synthase), Decreased uptake, or Increased PABA synthesis

44
Q

Sulfamethoxazole (SMX)

A

1) Gram-positive, gram-negative, Nocardia, Chlamydia. Triple sulfas or SMX for simple UTI. 2) Sulfonamides; PABA antimetabolites inhib dihydropteroate synthase. Bacteriostatic. 3) Hypersensitivity rxns, Hemolysis if G6PD deficient, Nephrotoxicity (tubulointerstitial nephritis), Photosensitivity, Kernicterus in infants, Displace other drugs from albumin (e.g. Warfarin) 4) Resistance: Altered enzyme (bacterial dihydropteroate synthase), Decreased uptake, or Increased PABA synthesis

45
Q

Trimethoprim (TMP)

A

1) Used in combo w/ sulfonamides [trimethoprim-sulfamethoxazole (TMP-SMX)], causing sequential block of folate synth. This combination is used to tx: UTIs, Shigella, Salmonella, Pneumocystic jirovecii pneumonia (tx & prophylaxis) 2) Inhib bacterial dihydrofolate reductase. Bacteriostatic 3) Megaloblastic anemia, leukopenia, granulocytopenia. [May alleviate w/ supplemental folinic acid (=Leucovorin rescue)] 4) TMP–Treats Marrow Poorly

46
Q

Ciprofloxacin

A

1) Gram-negative rods of urinary & GI tracts (including Pseudomonas), Neisseria, some gram-positive orgs 2) Fluoroquinolone; Inhib DNA gyrase (topoisomerase II) & topoisomerase IV. Bacterocidal. Must not be taken w/ antacids. 3) GI upset, Super infections, Skin rashes, HA, Dizziness. Less comonly–tendonitis, tendon rupture, leg cramps, & myalgias. Contraindicated in–pregnant women & children b/c animal studies show damage to cartilage. Some may cause prolonged QT interal. May cause tendon rupture in ppl >60 yo & in pts taking Prednisone. 4) Resistance: Chromosome-encodede mut in DNA gyrase, plasmid-mediated resistance, efflux pumps

47
Q

Norfloxacin

A

1) Gram-negative rods of urinary & GI tracts (including Pseudomonas), Neisseria, some gram-positive orgs 2) Fluoroquinolone; Inhib DNA gyrase (topoisomerase II) & topoisomerase IV. Bacterocidal. Must not be taken w/ antacids. 3) GI upset, Super infections, Skin rashes, HA, Dizziness. Less comonly–tendonitis, tendon rupture, leg cramps, & myalgias. Contraindicated in–pregnant women & children b/c animal studies show damage to cartilage. Some may cause prolonged QT interal. May cause tendon rupture in ppl >60 yo & in pts taking Prednisone. 4) Resistance: Chromosome-encodede mut in DNA gyrase, plasmid-mediated resistance, efflux pumps

48
Q

Levofloxacin

A

1) Gram-negative rods of urinary & GI tracts (including Pseudomonas), Neisseria, some gram-positive orgs 2) Fluoroquinolone; Inhib DNA gyrase (topoisomerase II) & topoisomerase IV. Bacterocidal. Must not be taken w/ antacids. 3) GI upset, Super infections, Skin rashes, HA, Dizziness. Less comonly–tendonitis, tendon rupture, leg cramps, & myalgias. Contraindicated in–pregnant women & children b/c animal studies show damage to cartilage. Some may cause prolonged QT interal. May cause tendon rupture in ppl >60 yo & in pts taking Prednisone. 4) Resistance: Chromosome-encodede mut in DNA gyrase, plasmid-mediated resistance, efflux pumps

49
Q

Ofloxacin

A

1) Gram-negative rods of urinary & GI tracts (including Pseudomonas), Neisseria, some gram-positive orgs 2) Fluoroquinolone; Inhib DNA gyrase (topoisomerase II) & topoisomerase IV. Bacterocidal. Must not be taken w/ antacids. 3) GI upset, Super infections, Skin rashes, HA, Dizziness. Less comonly–tendonitis, tendon rupture, leg cramps, & myalgias. Contraindicated in–pregnant women & children b/c animal studies show damage to cartilage. Some may cause prolonged QT interal. May cause tendon rupture in ppl >60 yo & in pts taking Prednisone. 4) Resistance: Chromosome-encodede mut in DNA gyrase, plasmid-mediated resistance, efflux pumps

50
Q

Sparfloxacin

A

1) Gram-negative rods of urinary & GI tracts (including Pseudomonas), Neisseria, some gram-positive orgs 2) Fluoroquinolone; Inhib DNA gyrase (topoisomerase II) & topoisomerase IV. Bacterocidal. Must not be taken w/ antacids. 3) GI upset, Super infections, Skin rashes, HA, Dizziness. Less comonly–tendonitis, tendon rupture, leg cramps, & myalgias. Contraindicated in–pregnant women & children b/c animal studies show damage to cartilage. Some may cause prolonged QT interal. May cause tendon rupture in ppl >60 yo & in pts taking Prednisone. 4) Resistance: Chromosome-encodede mut in DNA gyrase, plasmid-mediated resistance, efflux pumps

51
Q

Moxifloxacin

A

1) Gram-negative rods of urinary & GI tracts (including Pseudomonas), Neisseria, some gram-positive orgs 2) Fluoroquinolone; Inhib DNA gyrase (topoisomerase II) & topoisomerase IV. Bacterocidal. Must not be taken w/ antacids. 3) GI upset, Super infections, Skin rashes, HA, Dizziness. Less comonly–tendonitis, tendon rupture, leg cramps, & myalgias. Contraindicated in–pregnant women & children b/c animal studies show damage to cartilage. Some may cause prolonged QT interal. May cause tendon rupture in ppl >60 yo & in pts taking Prednisone. 4) Resistance: Chromosome-encodede mut in DNA gyrase, plasmid-mediated resistance, efflux pumps

52
Q

Gatifloxacin

A

1) Gram-negative rods of urinary & GI tracts (including Pseudomonas), Neisseria, some gram-positive orgs 2) Fluoroquinolone; Inhib DNA gyrase (topoisomerase II) & topoisomerase IV. Bacterocidal. Must not be taken w/ antacids. 3) GI upset, Super infections, Skin rashes, HA, Dizziness. Less comonly–tendonitis, tendon rupture, leg cramps, & myalgias. Contraindicated in–pregnant women & children b/c animal studies show damage to cartilage. Some may cause prolonged QT interal. May cause tendon rupture in ppl >60 yo & in pts taking Prednisone. 4) Resistance: Chromosome-encodede mut in DNA gyrase, plasmid-mediated resistance, efflux pumps

53
Q

Enoxacin

A

1) Gram-negative rods of urinary & GI tracts (including Pseudomonas), Neisseria, some gram-positive orgs 2) Fluoroquinolone; Inhib DNA gyrase (topoisomerase II) & topoisomerase IV. Bacterocidal. Must not be taken w/ antacids. 3) GI upset, Super infections, Skin rashes, HA, Dizziness. Less comonly–tendonitis, tendon rupture, leg cramps, & myalgias. Contraindicated in–pregnant women & children b/c animal studies show damage to cartilage. Some may cause prolonged QT interal. May cause tendon rupture in ppl >60 yo & in pts taking Prednisone. 4) Resistance: Chromosome-encodede mut in DNA gyrase, plasmid-mediated resistance, efflux pumps

54
Q

Nalidixic acid

A

1) Gram-negative rods of urinary & GI tracts (including Pseudomonas), Neisseria, some gram-positive orgs 2) Quinolone; Inhib DNA gyrase (topoisomerase II) & topoisomerase IV. Bacterocidal. Must not be taken w/ antacids. 3) GI upset, Super infections, Skin rashes, HA, Dizziness. Less comonly–tendonitis, tendon rupture, leg cramps, & myalgias. Contraindicated in–pregnant women & children b/c animal studies show damage to cartilage. Some may cause prolonged QT interal. May cause tendon rupture in ppl >60 yo & in pts taking Prednisone. 4) Resistance: Chromosome-encodede mut in DNA gyrase, plasmid-mediated resistance, efflux pumps

55
Q

Metronidazole

A

1) Txs Giardia**, Entamoeba, Trichomonas*, Gardnerella vaginalis, Anaerobes (Bacteroides, C. dificile). Used w/ proton pump inhib & Clarithromycin for “triple therapy” against H. Pylori* (GET GAP on the Metro w/ metronidazole!) 2) Forms free radical toxic metabolites in the bacterial cell that damage DNA. Bactericidal, antiprotozoal 3) Disulfuram-like rxn w/ alcohol; HA, Metallic taste

56
Q

Antimicrobial Drugs: Prophylaxis & Tx -M. tuberculosis -M. avium-intracelluare -M. leprae

A

Antimicrobial Drugs: Prophylaxis & Tx -M. tuberculosis–Prophylaxis=Isoniazid & Tx=Rifampin, Isoniazid, Pyrazinamide, Ethambutol (RIPE for tx) -M. avium-intracelluare–Prophylaxis=Azithromycin & Tx=Azithromycin, Rifampin, Ethanobutol, Streptomycin -M. leprae–Prophylaxis=N/A & Tx=Long-term tx w/ Dapsone & Rifampin for tuberculoid form. Add Clofazimine for lepromatous form.

57
Q

Isoniazid (INH)

A

1) Mycobacteriium tuberculosis; Only drug used as solo prophylaxis against TB 2) Antimicrobial; Decreases synth of mycolic acids. Bacterial catalase-peroxidases (KatG) needed to convert INH to active metabolite 3) Neurotoxicity, Hepatotoxicity. Pyridoxine (vit B6) can prevent neurotoxicity, lupus (INH–Injures Neurons & Hepatocytes) 4) Different INH half-lives in fast vs slow acetylator

58
Q

Rifampin

A

1) Mycobacterium tuburculosis; Delays resistance to dapsone when used for leprosy. Used for meningococcal prophylaxis and chemoprophylaxis in contacts of children w/ Haemophilus influenzae type B 2) Antimicrobial; Inhib DNA-dep RNA polymerase 3) Minor hepatotoxicity & drug rxns (increased P-450); Orange body fluids (nonhazardous side effect) 4) 4 Rs–RNA polymerase inhib, Revs up microsomal P-450, Red/orange body fluids, Rapid resistance if used alone

59
Q

Pyrazinamide

A

1) Mycobacterium tuberculosis 2) Antimicrobial; Mech unknown–thought to acidify intracellular env via conversion to pyrazinoic acid. Effective in acidid pH of phagolysosomes, where TB engulfed by macs is found 3) Hyperuricemia, Hepatotoxicity

60
Q

Ethambutol

A

1) Mycobacterium tuberculosis 2) Antimicrobial; Decreases carbohydrate polymerization of mycobacterum cell wall by blocking arabinosyltransferase 3) optic neuropathy (red-green color blindness)

61
Q

Antimicrobial Prophylaxis: -Meningococcal infection

A

-Ciprofloxacin (Rx of choice) -Rifampin for children

62
Q

Antimicrobial Prophylaxis: -Gonorrhea

A

-Ceftriaxone

63
Q

Antimicrobial Prophylaxis: -Syphilis

A

-Benzathine penicllin G

64
Q

Antimicrobial Prophylaxis: -History of recurrent UTIs

A

-TMP-SMX

65
Q

Antimicrobial Prophylaxis: -Endocarditis w/ surgical or dental procedures

A

-Penicillins

66
Q

Antimicrobial Prophylaxis: -Pregnant woman carrying group B strep

A

-Ampicillin

67
Q

Antimicrobial Prophylaxis: -Strep pharyngitis in child w/ prior rheumatic fever

A

-Oral penicllin

68
Q

Antimicrobial Prophylaxis: -Prevention of postsurgical infection due to S. aureus

A

-Cefazolin

69
Q

Antimicrobial Prophylaxis: -Prevention of gonococcal or chlamydial conjunctivitis in newborn

A

-Erythromycin ointment

70
Q

HIV: Prophylaxis Tx & Infection -CD4 < 200 cells/mm3 -CD4 < 100 cells/mm3 -CD4 < 50 cells/mm3

A

HIV Prophylaxis Tx & Infection: -CD4 < 200 cells/mm3=*TMP-SMX; Pneumocytis pneumonia -CD4 < 100 cells/mm3=*TMP-SMX=Pneumocytis pneumona & Toxoplasmosis -CD4 < 50 cells/mm3=Azithromycin; Mycobacterium avium complex *Aerosolized Pentamidine–can be used if pt is unable to tolerate TMP-SMX, butt this may not prevent toxoplasmosis

71
Q

Tx for highly resistant bacteria: -MRSA -VRE

A

-MRSA tx = Vancomycin -VRE tx =Linezolid & Streptogramins (quinupristin/dalfopristin)

72
Q

Amphotericin B

A

1) Serious systemic mycoses, Cryptococcus (w or w/o Flucytosine for cryptococcal meningitis), Blastomyces, Coccidioides, Histoplasma, Candida, Mucor. Intrathecally for fungal meningitis. 2) Antifungal; Alters membrane fnx–Binds ergosterol (unique to fungi), forms membrane pores that allow leakage of electrolytes (AmphoTERicin “TEARs” holes in fungal membrane) 3) Fever/chills (“shake & bake”), Hypotension, Nephrotoxicity, Arrhythmias, Anemia, IV phlebitis (“AMPHOTERRIble); Hydration reduces nephrotoxicity (see line #4); Liposomal Amphotericin reduced toxicity 4) Supplement K & Mg b/c of altered renal tubule permeability

73
Q

Nystatin

A

1) “Swish & swallow” for oral candidiasis (thrush); Topical for diaper rash or vaginal candidiasis 2) Antifungal; Same MOA as Amphotericin B [=Alters membrane fnx–Binds ergosterol (unique to fungi), forms membrane pores that allow leakage of electrolytes (AmphoTERicin “TEARs” holes in fungal membrane)]. Topical form b/c too toxic for systemic use

74
Q

Fluconazole

A

1) Local & Less serious systemic mycoses; Floconazole specific=Chronic suppression of cryptoccal meningitis in AIDs pts & candida infection of all types 2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol to ergosterol 3) Testosterone synth inhib (gynecomastia) Liver dysfnx (inhib cytochrome P-450)

75
Q

Ketoconazole

A

1) Local & Less serious systemic mycoses 2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol to ergosterol 3) Testosterone synth inhib (gynecomastia, esp Ketoconazole) Liver dysfnx (inhib cytochrome P-450)

76
Q

Clotrimazole

A

1) Local & Less serious systemic mycoses; Clotrimazole (& Miconazole) specific=Topical fungal infections 2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol to ergosterol 3) Testosterone synth inhib (gynecomastia) Liver dysfnx (inhib cytochrome P-450)

77
Q

Miconazole

A

1) Local & Less serious systemic mycoses; Miconazole (& Clotrimazole) specific=Topical fungal infections 2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol to ergosterol 3) Testosterone synth inhib (gynecomastia) Liver dysfnx (inhib cytochrome P-450)

78
Q

Itraconazole

A

1) Local & Less serious systemic mycoses; Itraconazole specific=Tx for Bastomyces, Coccidiodes, & Histoplasma 2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol to ergosterol 3) Testosterone synth inhib (gynecomastia) Liver dysfnx (inhib cytochrome P-450)

79
Q

Voriconazole

A

1) Local & Less serious systemic mycoses 2) Antifungal-Azole; Inhib fungal sterol (ergosterol) synth by inhib P-450 enzyme that converts lanostrerol to ergosterol 3) Testosterone synth inhib (gynecomastia) Liver dysfnx (inhib cytochrome P-450)

80
Q

Flucytosine

A

1) Tx of systemic fungal infections (esp. meningitis caused by Cryptococcus) in combo w/ Amphotericin B 2) Antifungal; Inhib DNA & RNA biosynth by conversion to 5-fluorouracil by cytosine deaminase 3) BM suppression

81
Q

Caspofungin

A

1) Invasive aspergilliosis, Candida 2) Antifungal; Inhib cell wall synth by inhibiting synth of Beta-glucan 3) GI upset, flushing (by histasmine release)

82
Q

Micafungin

A

1) Invasive aspergilliosis, Candida 2) Antifungal; Inhib cell wall synth by inhibiting synth of Beta-glucan 3) GI upset, flushing (by histasmine release)

83
Q

Terbinafine

A

1) Tx dermatophytoses (esp onchomycosis=fungal infection of finger or toe nails) 2) Antifungal; Inhib fungal enzyme squalene epoxidase 3) Abn LFTs, Visual disturbances

84
Q

Griseofulvin

A

1) PO tx of superficial infections; Inhib growth of dermatophytes (tinea, ringworm) 2) Antifungal; Interferes w/ microtubule fnx; Disrupts mitosis. Deposits in keratin-containing tissues (e.g. nails) 3) Teratogenic, Carinogenic, Confusion, HAs, Increase P-450 & warfarin metabolism

85
Q

Pyrimethamine

A

1) Tx Toxoplasmosis 2) Antiprotozoan

86
Q

Suramin

A

1) Tx Trypanosoma brucei 2) Antiprotozoan

87
Q

Melarsoprol

A

1) Tx Trypanosoma brucei 2) Antiprotozoan

88
Q

Nifurtimox

A

1) Tx Trypansoma cruzi 2) Antiprotozoan

89
Q

Sodium stibogluconate

A

1) Tx Leishmaniasis 2) Antiprotozoan

90
Q

Chloroquine

A

1) Tx of plasmodial species other than P. falciparium ( d/t high resistance; see line #4) 2) Blocks detoxification of heme into hemozoin. Heme accumulates and is toxic to plasmodia 3) Retinopathy 4) P. falciparum mechanism of resistance: Membrane pump that decreases intracellular concentration of Chloroquine; Tx P. falciparum w/ Artemether/Lumifantrine OR Atovaquone/Proguanil; Tx life-threatening malaria w/ Quinidine in US (quinine elsewere) or Artisunate

91
Q

Txs for P. falciparum

A

-Artemether/Lumifantrine OR Atovaquone/Proguanil -NOT Chloroquine (d/t resistance)

92
Q

Txs for life-threatening malaria

A

-Quinidine in US (quinine elsewere) or Artisunate

93
Q

Mebendazole

A

2) Antihelminthic therapy; Immobilize helminths

94
Q

Pyrantel pamoate

A

2) Antihelminthic therapy; Immobilize helminths

95
Q

Ivermectin

A

2) Antihelminthic therapy; Immobilize helminths

96
Q

Diethylcarbamazine

A

2) Antihelminthic therapy; Immobilize helminths

97
Q

Praziquantel

A

1) Tx for flukes (trematodes, e.g. Schistosoma) 2) Antihelminthic therapy; Immobilize helminths

98
Q

Zanamivir

A

1) Tx and prevention of: Influenza A & B 2) Antiviral therapy; Inhib influenza neuraminidase, Decreasing the release of pogeny virus

99
Q

Oseltmavir

A

1) Tx and prevention of: Influenza A & B 2) Antiviral therapy; Inhib influenza neuraminidase, Decreasing the release of pogeny virus

100
Q

Ribavirin

A

1) RSV, Chronic hepatitis C 2) Antiviral therapy; Inhib synth of guanine nucleotides by competitively inhibiting IMP dehydrogenase 3) Hemolytic anemia, Severe teratogen

101
Q

Acyclovir

A

1) HSV & ZVZ; Weak activity against EBV. No activity against CMV. Used for HSZ-induced mucocutaneous & genital lesions as well as encephalitis. Prophylaxis in immunocompromised pts. No effect on latent forms of HSZ & ZVZ. 2) Antiviral therapy; Monophosphorylated by HSV/VZV thymidine kinase. Guanosine analog. Triphosphate formed by cellular enzymes. Preferentially inihib viral DNA polymerase by chain termination 4) Mechanism of resistance: Mutated viral thymidine kinase

102
Q

Valacyclovir

A

1) HSV & ZVZ; Weak activity against EBV. No activity against CMV. Used for HSZ-induced mucocutaneous & genital lesions as well as encephalitis. Prophylaxis in immunocompromised pts. No effect on latent forms of HSZ & ZVZ. 2) Antiviral therapy; **= a prodrug of Acyclovir, so has better oral bioavailability vs Acyclovir** Monophosphorylated by HSV/VZV thymidine kinase. Guanosine analog. Triphosphate formed by cellular enzymes. Preferentially inihib viral DNA polymerase by chain termination 4) Mechanism of resistance: Mutated viral thymidine kinase

103
Q

Famciclovir

A

1) Herpes Zoster 2) Antiviral therapy; **Related to Acyclovir**

104
Q

Ganciclovir

A

1) CMV, esp in immunocompromised pts. 2) Antiviral therapy; 5’-monophosphate formed CMV viral kinase Guanosine analog. Triphosphate formed by cellular kinases. Preferentially inhib viral DNA polymerase 3) Leukopenia, Neutropenia, Thrombocytopenia, Renal toxicity; More toxic to host enzymes vs Acyclovir 4) Mechanism of resistance: Mutated CMV DNA polymerase or lack of viral kinase

105
Q

Valganciclovir

A

1) CMV, esp in immunocompromised pts. 2) Antiviral therapy; **a prodrug of Ganciclovir, so has better ora bioavailability vs Ganciclovir** 5’-monophosphate formed CMV viral kinase Guanosine analog. Triphosphate formed by cellular kinases. Preferentially inhib viral DNA polymerase 3) Leukopenia, Neutropenia, Thrombocytopenia, Renal toxicity; More toxic to host enzymes vs Acyclovir 4) Mechanism of resistance: Mutated CMV DNA polymerase or lack of viral kinase

106
Q

Foscarnet

A

1) CMV retinitis in immunocompromised pts when Ganciclovir fails; Acyclovir-resistant HSV 2) Antiviral therapy; A pyrophosphate analog (Foscarnet=pyroFOSphate analog). Viral DNA polymerase inhib that binds to pyrophosphate-binding site of the enzyme. Does not req activation by viral kinase 3) Nephrotoxicity 4) Mechanism of resistance: Mutated DNA polymerase

107
Q

Cidofovir

A

1) CMV retinitis in immunocompromised pts; Acyclovir-resistant HSV 2) Antiviral therapy; Preferentially inhib viral DNA polymerase. Does not req phosphorylation by viral kinase. Long t-1/2. 3) Nephrotoxicity (co-admin w/ Probenecid & IV saline to reduce toxicity)

108
Q

HIV Therapy: -Name -When to initiate -Drug regimen

A

-Highly active antiretroviral therapy (HAART) -Initiate when pts present w/ AIDS-defining illness, low CD4+ cts (<500 cells/mm3), or high viral load -Regimen consists of (3) drugs to prevent resistance: –2 nucleoside reverse transcriptase inhib (NRTIs) + –1 non-nucleoside reverse transcriptase inhib (NNRTI) OR 1 protease inhib OR 1 integrase inhib

109
Q

Lopinavir

A

1) HIV therapy 2) Protease inhib; Prevents maturation of new viruses by cleaving HIV-1 protease (Assembly of virions depends on HIV-1 protease, which cleaves polypeptide products of HIV mRNA into their functional parts) 3) Hyperglycemia, GI intolerance (N/D), Lipodystrophy, Nephropathy 4) All protease inhibitors end in -navir [Navir (never) tease a protease]

110
Q

Atazanavir

A

1) HIV therapy 2) Protease inhib; Prevents maturation of new viruses by cleaving HIV-1 protease (Assembly of virions depends on HIV-1 protease, which cleaves polypeptide products of HIV mRNA into their functional parts) 3) Hyperglycemia, GI intolerance (N/D), Lipodystrophy, Nephropathy 4) All protease inhibitors end in -navir [Navir (never) tease a protease]

111
Q

Darunavir

A

1) HIV therapy 2) Protease inhib; Prevents maturation of new viruses by cleaving HIV-1 protease (Assembly of virions depends on HIV-1 protease, which cleaves polypeptide products of HIV mRNA into their functional parts) 3) Hyperglycemia, GI intolerance (N/D), Lipodystrophy, Nephropathy 4) All protease inhibitors end in -navir [Navir (never) tease a protease]

112
Q

Fosaprenavir

A

1) HIV therapy 2) Protease inhib; Prevents maturation of new viruses by cleaving HIV-1 protease (Assembly of virions depends on HIV-1 protease, which cleaves polypeptide products of HIV mRNA into their functional parts) 3) Hyperglycemia, GI intolerance (N/D), Lipodystrophy, Nephropathy 4) All protease inhibitors end in -navir [Navir (never) tease a protease]

113
Q

Saquinavir

A

1) HIV therapy 2) Protease inhib; Prevents maturation of new viruses by cleaving HIV-1 protease (Assembly of virions depends on HIV-1 protease, which cleaves polypeptide products of HIV mRNA into their functional parts) 3) Hyperglycemia, GI intolerance (N/D), Lipodystrophy, Nephropathy 4) All protease inhibitors end in -navir [Navir (never) tease a protease]

114
Q

Ritonavir

A

1) HIV therapy 2) Protease inhib; Prevents maturation of new viruses by cleaving HIV-1 protease (Assembly of virions depends on HIV-1 protease, which cleaves polypeptide products of HIV mRNA into their functional parts) 3) Hyperglycemia, GI intolerance (N/D), Lipodystrophy, Nephropathy 4) All protease inhibitors end in -navir [Navir (never) tease a protease]; Ritonavir specific=CYP450 inhib

115
Q

Indinavir

A

1) HIV therapy 2) Protease inhib; Prevents maturation of new viruses by cleaving HIV-1 protease (Assembly of virions depends on HIV-1 protease, which cleaves polypeptide products of HIV mRNA into their functional parts) 3) Hyperglycemia, GI intolerance (N/D), Lipodystrophy, Nephropathy; Indinavir specific ADE=Hematuria 4) All protease inhibitors end in -navir [Navir (never) tease a protease]

116
Q

Tenofovir (TDF)

A

1) HIV therapy 2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group) 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy, Lactic Acidosis 4) Is a nucleotide analog, so does not have to be activated (vs other NRTIs, which are nucleoside analogs & therefore, req activation)

117
Q

Emtricitabine (FTC)

A

1) HIV therapy 2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group) 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis 4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

118
Q

Abacavir (ABC)

A

1) HIV therapy 2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group) 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis 4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

119
Q

Lamivudine (3TC)

A

1) HIV therapy 2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group) 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis 4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

120
Q

Zidovudine (ZDV, formerly AZT)

A

1) HIV therapy 2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group) 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis; ZDZ specific ADE=Anemia 4) Used for general prophylaxis & during pregnancy to reduce risk of fetal transmission; Must be phosphorylated to be activated (the second statement is true of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

121
Q

Didanosine (ddl)

A

1) HIV therapy 2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group) 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis 4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

122
Q

Stavudine (d4T)

A

1) HIV therapy 2) Nucleoside reverse transcriptase inhib (NRTI); Completely inhib nucleotide binding to reverse transcriptase & terminate te DNA chain (lack a 3’ OH group) 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Lactic acidosis 4) Must be phosphorylated to be activated (True of all NRTIs, except Tenofovir b/c it is a nucleotide vs nucleoside analog)

123
Q

Nevirapine

A

1) HIV therapy 2) Non-nucleoside reverse transcriptase inhib (NNRTI); Bind to reverse transcriptase at site different from NRTIs (Nucleoside RTIs). Do not req phosphorylation to be active or compete w/ nucleotides 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Rash

124
Q

Efazirenz

A

1) HIV therapy 2) Non-nucleoside reverse transcriptase inhib (NNRTI); Bind to reverse transcriptase at site different from NRTIs (Nucleoside RTIs). Do not req phosphorylation to be active or compete w/ nucleotides 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Rash

125
Q

Delavirdine

A

1) HIV therapy 2) Non-nucleoside reverse transcriptase inhib (NNRTI); Bind to reverse transcriptase at site different from NRTIs (Nucleoside RTIs). Do not req phosphorylation to be active or compete w/ nucleotides 3) BM suppression (can be reversed w/ G-CSF & EPO), Peripheral neuropathy; Rash

126
Q

Raltegravir

A

1) HIV therapy 2) Integrase inhib; Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase 3) Hypercholesterolemia

127
Q

IFN-Alpha

A

1) Chronic hepatitis B & C; Kaposi’s sarcoma 2) Interferon; Glycoproteins synth by virus-infected cells; Blocks replication of both RNA & DNA viruses 3) Neutropenia, Myopathy

128
Q

IFN-Beta

A

1) MS 2) Interferon; Glycoproteins synth by virus-infected cells; Blocks replication of both RNA & DNA viruses 3) Neutropenia, Myopathy

129
Q

IFN-Gamma

A

1) NADPH oxidase deficiency 2) Interferon; Glycoproteins synth by virus-infected cells; Blocks replication of both RNA & DNA viruses 3) Neutropenia, Myopathy

130
Q

Abx to avoid in pregnancy

A

Contraindicated in Pregnancy –> Adverse Effect: -Sulfonamides –> Kernicterus -Aminoglycosides –> Ototoxicity -Fluoroquinolones –> Cartolage damage -Clarithromycin –> Embryotoxic -Tetracyclines –> Discolored teeth, Inhib of bone growth -Ribavirin (antiviral) –> Teratogenic -Griseofulvin (antifungal) –> Teratogenic -Chloramphenicol –> “Gray baby” (SAFe Children Take Really Good Care)

131
Q

Sulfadiazine

A

1) Gram-positive, gram-negative, Nocardia, Chlamydia. Triple sulfas or SMX for simple UTI. 2) Sulfonamides; PABA antimetabolites inhib dihydropteroate synthase. Bacteriostatic. 3) Hypersensitivity rxns, Hemolysis if G6PD deficient, Nephrotoxicity (tubulointerstitial nephritis), Photosensitivity, Kernicterus in infants, Displace other drugs from albumin (e.g. Warfarin) 4) Resistance: Altered enzyme (bacterial dihydropteroate synthase), Decreased uptake, or Increased PABA synthesis