Immuno/Microbio Flashcards
1
Q
<p>Immunosuppressants</p>
A
<p class="large" style="text-align: center;">Cyclosporine Tacrolimus (FK-506) Sirolimus (rapamycin) Azathioprine Muromonab-CD3 (OKT3)</p>
2
Q
<p>Cyclosporine</p>
A
<p>1. Post-transplant immunosuppression; select autoimmune disorders
2. Binds to cyclophilins. Complex blocks differentiation and activation of Tcells--> inhibiting calcineurin--> preventing production of IL-2 and its receptor
3. Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor, gingival hyperplasia, hirsutism
4. Think old man with diabetes who wants to look good for his date so he put in dentures and got hair plugs: old (renal failure, HTN, cholesterol), diabetes (hyperglycemia), dentures (gum hyperplasia), hair plugs (hirsutism, and he is taking the drug because of his hair transplant)
</p>
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
<p class=”large” style=”text-align:center”;>Tacrolimus (FK-506)</p>
A
<p class=”large” style=”text-align:center”;>1. Post- organ transplant immunosuppression; POTENT
- Binds to FK protein->inhibiting calcineurin->preventing IL-2
- Nephrotoxicity, hypertension, hyperlipidemia, hyperglycemia, tremor
- Think old with diabetes who is nervous because he is super sick: old (renal failure, HTN, cholesterol), diabetes (hyperglycemia), nervous (tremor), super sick (strong immunosuppressant)
</p>
4
Q
<p>Sirolimus (rapamycin)</p>
A
<p>1. Immunosuppression post-KIDNEY transplant (Give with cyclosporine); used with drug-eluting stents
2. Inhibits mTOR. Decreased cell proliferation in response to IL-2
3. Hyperlipidemia, thrombocytopenia, leukopenia
4. SIROlimus= SERIOUS complications: immunosuppression
</p>
5
Q
<p class=”large” style=”text-align:center”;>Azathioprine</p>
A
<p class=”large” style=”text-align:center”;>1. Immunosuppression post-KIDNEY transplant; autoimmune disorders (including glomerulonephritis and hemolytic anemia)
- Antimetabolite. Blocks 6-mercaptopurine synth-> decreased synthesis of nucleic acids. Toxic to proliferating lymphocytes.
- Bone marrow suppression.
- Active metabolite (mercaptopurine) is metabolized by xanthine oxidase so more toxic when given with allopurinol
</p>
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
<p>Muromonab-CD3 (OKT3)</p>
A
<p>1. Immunosuppression post-KIDNEY transplant
2. Monoclonal antibody to CD3 on T-cells. Blocks interaction with CD3 responsible for T-cell signal transduction
3. Cytokine release syndrome, hypersensitivity reaction
4. Antibodies= hypersensitivity, hypersensitivity= cytokine release
- nab= monocolonal antibody therapy (usually)
</p>
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
<p class=”large” style=”text-align:center”;>Recombinant Cytokines</p>
A
<p class="large" style="text-align:center";>Aldesleukin (interleukin-2) Epoetin alfa (erythropoietin) Filgrastim (CSF-G) Sargramostim (CSF-GM) Alpha-Interferon Beta-Interferon Gamma-Interferon Oprelvekin (interleukin-11) Thrombopoietin</p>
8
Q
<p>Aldesleukin </p>
A
<p>1. Renal cell carcinoma
Metastatic Melanoma
2. Cytokine: Interleukin-2
MOA: increases helper, cytotoxic, and regulatory T cells</p>
10
Q
<p class=”large” style=”text-align:center”;>Epoetin alfa </p>
A
<p class=”large” style=”text-align:center”;>1. Anemias (esp in renal failure)
2. Cytokine: Erythropoietin
MOA: Stimulates Erythrocyte replication</p>
10
Q
<p>Filgrastim</p>
A
<p>1. Recovery of bone marrow
2. GM-CSF (Granulocyte Colony Stimulating Factor) </p>
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
12
Q
<p class=”large” style=”text-align:center”;>Sargramostim (CSF-GM)</p>
A
<p class=”large” style=”text-align:center”;>1. Recovery of bone marrow
2. GM-CSF (Granulocyte-Macrophage Colony Stimulating Factor)</p>
12
Q
<p>Alpha-Interferon</p>
A
<p>1. Hepatitis B and C
Kaposi's Sarcoma
Leukemia
Malignant Melanoma
2. Inhibit viral protein synthesis and activates NK cells to kill virally infected cells</p>
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)
14
Q
<p class=”large” style=”text-align:center”;>Beta-Interferon</p>
A
<p class=”large” style=”text-align:center”;>Multiple Sclerosis</p>
14
Q
<p>Gamma-Interferon</p>
A
<p>1. Chronic Granulomatous disease
2. Activates macrophages and Th1 cells
Suppresses Th2 cells.
4. (G)amma = (G)ranulomatous</p>
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
<p class=”large” style=”text-align:center”;>Oprelvekin</p>
A
<p class=”large” style=”text-align:center”;>1. Thrombocytopenia
2. IL-11
</p>
17
Q
<p class=”large” style=”text-align:center”;>Thrombopoietin</p>
A
<p class=”large” style=”text-align:center”;>Thrombocytopenia</p>
17
Q
<p>Theraputic Antibodies</p>
A
<p class="large" style="text-align: center;">Muromonab-CD3 (OKT3 Digoxin Immune Fab Infliximab Adalimumab Abciximab Trastuzumab (Herceptin) Rituximab Omalizumab </p>
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)
19
Digoxin Immune Fab
Target: Digoxin | Use: Antidote for Digoxin toxicity
19
Digoxin Immune Fab
Target: Digoxin | Use: Antidote for Digoxin toxicity
20
Cefotaxime
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)
22
Infliximab
Target: TNF-alpha Use: Crohn's Disease, Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis
22
Abciximab
Target: Glycoprotien IIb/IIIa Use: Prevent cardiac ischemia in unstable angina and patients treated with percutaneous coronary intervention MOA: Prevents platelet aggregation by inhibiting the platelet-GIIb/IIIa-fibrinogen bonds
22
Abciximab
Target: Glycoprotien IIb/IIIa Use: Prevent cardiac ischemia in unstable angina and patients treated with percutaneous coronary intervention MOA: Prevents platelet aggregation by inhibiting the platelet-GIIb/IIIa-fibrinogen bonds
23
Ceftaroline
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
Rituximab
Target: CD20 | Use: B-cell non-Hodgkin's lymphoma
24
Rituximab
Target: CD20 | Use: B-cell non-Hodgkin's lymphoma
26
-azole
Antifungal | Ex: Ketoconazole
26
-azole
Antifungal | Ex: Ketoconazole
27
Meropenem
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
29
-navir
Antibiotic, protease inhibitor Ex: Saqyubavir
29
-navir
Antibiotic, protease inhibitor Ex: Saqyubavir
30
Streptomycin
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
-cillin
Penicillin | Ex: Methicillin
31
-ane
Inhalational general anesthetic Ex: Halothane
32
-cycline
Antibiotic, protein synthesis inhibitor Ex: Tetracycline
33
-operidol
Butyrophenone (neuroleptic) Ex: Haloperidol
33
Neomycin
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
35
-triptan
5-HT 1B/1D agonists (for migranes) Ex: Sumatriptan
36
-zolam
Benzodiazepine | Ex: Alprazolam
36
Demeclocycline
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.
37
-caine
Local anesthetic | Ex: Lidocaine
38
-etine
SSRI | Ex: Fluoxetine
38
-etine
SSRI | Ex: Fluoxetine
40
-barbital
Barbituate | Ex: Phenobarbital
40
-triptyline
TCA | Ex: Amitriptyline
42
-azepam
Benzodiazepine | Ex: Diazepam
42
-terol
B2-agonist | Ex: Albuterol
42
Chloramphenicol
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
44
-ipramine
TCA | Ex: Imipramine
44
-oxin
Cardiac glycoside (inotropic agent) Ex: Digoxin
45
Sulfisoxazole
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
46
-afil
Erectile Dysfunction Ex: Sildenafil
46
-afil
Erectile Dysfunction Ex: Sildenafil
48
-tidine
H2 antagonist | Ex: Cimetidine
48
-tidine
H2 antagonist | Ex: Cimetidine
48
Ciprofloxacin
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
Penicillin G
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
51
Methicillin
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)
52
-pril
ACE inhibitor | Ex: Captopril
52
Nafcillin
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!
54
Ampicillin
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
55
Enoxacin
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
56
Ticarcillin
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
57
Carbenicillin
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
59
Clavulonic Acid
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)
60
Rifampin
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
61
Tazobactam
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)
62
Cefazolin
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)
64
Cefoxitin
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)
65
Antimicrobial Prophylaxis:
| -Syphilis
-Benzathine penicllin G
66
Cefuroxime
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)
67
Ceftriaxone
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)
69
Ceftazidime
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)
70
Cefepime
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)
71
Antimicrobial Prophylaxis:
| -Prevention of gonococcal or chlamydial conjunctivitis in newborn
-Erythromycin ointment
72
Ertapenem
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.
2) Beta-lactam, **Newer** 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
73
Doripenem
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.
2) Beta-lactam, **Newer** 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
74
Aztreonam
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
76
Imipenem (w/ Cilastatin)
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
76
Fluconazole
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)
77
Vancomycin
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)]
79
Tobramycin
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
80
Amikacin
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
82
Gentamicin
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
83
Minocycline
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.
85
Doxycycline
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.
85
Terbinafine
1) Tx dermatophytoses (esp onchomycosis=fungal infection of finger or toe nails)
2) Antifungal; Inhib fungal enzyme squalene epoxidase
3) Abn LFTs, Visual disturbances
86
Tetracycline
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.
87
Erythromycin
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.
88
Clarithromycin
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.
89
Azithromycin
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.
91
Clindamycin
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)
92
Sulfadiazine
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
94
Sulfamethoxazole (SMX)
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
95
Trimethoprim (TMP)
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
97
Norfloxacin
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
98
Levofloxacin
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
99
Ofloxacin
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
99
Praziquantel
1) Tx for flukes (trematodes, e.g. Schistosoma)
| 2) Antihelminthic therapy; Immobilize helminths
100
Sparfloxacin
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
101
Moxifloxacin
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
102
Gatifloxacin
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
104
Nalidixic acid
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
105
Metronidazole
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
106
Antimicrobial Drugs: Prophylaxis & Tx
- M. tuberculosis
- M. avium-intracelluare
- M. leprae
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.
107
Isoniazid (INH)
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
109
Pyrazinamide
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
110
Ethambutol
1) Mycobacterium tuberculosis
2) Antimicrobial; Decreases carbohydrate polymerization of mycobacterum cell wall by blocking arabinosyltransferase
3) optic neuropathy (red-green color blindness)
111
Antimicrobial Prophylaxis:
| -Meningococcal infection
- Ciprofloxacin (Rx of choice)
| - Rifampin for children
112
Antimicrobial Prophylaxis:
| -Gonorrhea
-Ceftriaxone
114
Antimicrobial Prophylaxis:
| -History of recurrent UTIs
-TMP-SMX
115
Antimicrobial Prophylaxis:
| -Endocarditis w/ surgical or dental procedures
-Penicillins
116
Antimicrobial Prophylaxis:
| -Pregnant woman carrying group B strep
-Ampicillin
117
Antimicrobial Prophylaxis:
| -Strep pharyngitis in child w/ prior rheumatic fever
-Oral penicllin
118
Antimicrobial Prophylaxis:
| -Prevention of postsurgical infection due to S. aureus
-Cefazolin
120
HIV: Prophylaxis Tx & Infection
- CD4 < 200 cells/mm3
- CD4 < 100 cells/mm3
- CD4 < 50 cells/mm3
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
121
Tx for highly resistant bacteria:
- MRSA
- VRE
- MRSA tx = Vancomycin
| - VRE tx =Linezolid & Streptogramins (quinupristin/dalfopristin)
122
Amphotericin B
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
123
Nystatin
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
125
Ketoconazole
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)
126
Clotrimazole
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)
127
Miconazole
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)
128
Itraconazole
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)
129
Voriconazole
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)
130
Flucytosine
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
131
Caspofungin
1) Invasive aspergilliosis, Candida
2) Antifungal; Inhib cell wall synth by inhibiting synth of Beta-glucan
3) GI upset, flushing (by histasmine release)
132
Micafungin
1) Invasive aspergilliosis, Candida
2) Antifungal; Inhib cell wall synth by inhibiting synth of Beta-glucan
3) GI upset, flushing (by histasmine release)
134
Griseofulvin
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
135
Pyrimethamine
1) Tx Toxoplasmosis
| 2) Antiprotozoan
136
Suramin
1) Tx Trypanosoma brucei
| 2) Antiprotozoan
137
Melarsoprol
1) Tx Trypanosoma brucei
| 2) Antiprotozoan
138
Nifurtimox
1) Tx Trypansoma cruzi
| 2) Antiprotozoan
139
Sodium stibogluconate
1) Tx Leishmaniasis
| 2) Antiprotozoan
140
Chloroquine
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
141
Txs for P. falciparum
- Artemether/Lumifantrine OR Atovaquone/Proguanil
| - NOT Chloroquine (d/t resistance)
142
Txs for life-threatening malaria
-Quinidine in US (quinine elsewere) or Artisunate
143
Mebendazole
2) Antihelminthic therapy; Immobilize helminths
144
Pyrantel pamoate
2) Antihelminthic therapy; Immobilize helminths
145
Ivermectin
2) Antihelminthic therapy; Immobilize helminths
146
Diethylcarbamazine
2) Antihelminthic therapy; Immobilize helminths
148
Zanamivir
1) Tx and prevention of: Influenza A & B
| 2) Antiviral therapy; Inhib influenza neuraminidase, Decreasing the release of pogeny virus
149
Oseltmavir
1) Tx and prevention of: Influenza A & B
| 2) Antiviral therapy; Inhib influenza neuraminidase, Decreasing the release of pogeny virus
150
Ribavirin
1) RSV, Chronic hepatitis C
2) Antiviral therapy; Inhib synth of guanine nucleotides by competitively inhibiting IMP dehydrogenase
3) Hemolytic anemia, Severe teratogen
151
Acyclovir
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
152
Valacyclovir
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
153
Famciclovir
1) Herpes Zoster
| 2) Antiviral therapy; **Related to Acyclovir**
154
Ganciclovir
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
155
Valganciclovir
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
156
Foscarnet
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
157
Cidofovir
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)
158
HIV Therapy:
- Name
- When to initiate
- Drug regimen
-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
159
Lopinavir
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]
160
Atazanavir
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]
161
Darunavir
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]
162
Fosaprenavir
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]
163
Saquinavir
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]
164
Ritonavir
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
165
Indinavir
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]
166
Tenofovir (TDF)
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)
167
Emtricitabine (FTC)
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)
168
Abacavir (ABC)
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)
169
Lamivudine (3TC)
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)
170
Zidovudine (ZDV, formerly AZT)
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)
171
Didanosine (ddl)
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)
172
Stavudine (d4T)
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)
173
Nevirapine
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
174
Efazirenz
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
175
Delavirdine
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
176
Raltegravir
1) HIV therapy
2) Integrase inhib; Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase
3) Hypercholesterolemia
177
IFN-Alpha
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
178
IFN-Beta
1) MS
2) Interferon; Glycoproteins synth by virus-infected cells; Blocks replication of both RNA & DNA viruses
3) Neutropenia, Myopathy
179
IFN-Gamma
1) NADPH oxidase deficiency
2) Interferon; Glycoproteins synth by virus-infected cells; Blocks replication of both RNA & DNA viruses
3) Neutropenia, Myopathy
180
Abx to avoid in pregnancy
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)
