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162 Cards in this Set
- Front
- Back
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MOA aminoglycoside resistance?
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Enzyme conjugation inactivation
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MOA macrolide resistance?
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Methyltransferase that alter drug bind site @ 50S
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MOA tetracycline resistance?
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Pump
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Most AtB are bacterio____.
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Cidal
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MOA penicillin
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Interact w/ PBP and inhibit crosslinking
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MOA penicillin resistance
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B-lactamase
PBP structural change Porin structural change |
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**What are the very narrow spectrum used for?
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B-lactamase producing Staph
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Drugs of very narrow spectrum (B-lactamase resistant) pen?
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Methicillin
Naf/Oxa-cillin |
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What are the narrow spectrum pen?
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Pen G & Pen V
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What does narrow spectrum pen cover?
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G+ cocci
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**What is Pen G DOC for?
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Treponema pallidum
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What are the broad spectrum (aminopenicillin)?
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Amp
Amox |
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What are does broad spectrum pen cover?
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G+ (not staph) + G-
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**What is DOC for Listeria monocytogenes?
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Ampicillin
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What does the very broad spectrum AtB cover?
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Lots of G-
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**What are the very broad spectrum AtB DOC for?
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Pseudomonas
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What are the very broad spectrum drugs?
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Ticar
Pipera Azlo |
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What can u give to enhance Pen actions?
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Combo w/ B-lactamase inhibitor
Synergy w/ aminoglycoside (VS pseudomonas) |
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What are penicillins biochemically?
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Weak Acids
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How is pen eliminated?
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Active tubular secretion (blocked by probenecid, which increase duration of activity)
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How are the anti-staph pen eliminated?
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Bile
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**What are the first gen (NARROW SPECTRUM) cephlasporins?
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Cefazolin & Cephalexin
U need a Ph.D (Cef dn have a Ph.D, dn let this faz u) |
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What does 1st gen cover?
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G+ cocci (not MRSA) + PEcK (Proteus, E coli, Klebsiella)
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Does 1st gen cephlasporins enter CNS?
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NO
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What are the 2nd gen cephlasporins?
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FAMily gathered to celebrate your phd, your FOXy gf is wearing FUR and drinking TEA
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Does 2nd gen cephlasporins enter CNS?
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YES
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What does 2nd gen cover?
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More G- + Anaerobes
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What are the very broad spectrum cephlasporins?
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Gen 3 & 4 (Cover even more G-)
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How do u remember 3rd gen cephlasporins?
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Contain T (for tri)
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**What is the DOC for N. gonorrhea?
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Ceftriaxone
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Does 3rd gen enter CNS?
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YES
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**Empiric tx of meningitis involves:
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Ceftriaxone
"Ax to the head" for meningitis |
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**Which AtBs do you NOT have to adjust in RF due to liver (bile) elimination?
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Ceftriaxone
Doxycycline Nafcillin |
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**Tx for neonatal meningitis?
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Amp + Ceftriaxone
**Ceftriaxone DN cover Listeria, which is a cause of neonatal meningitis |
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What is the only 4th gen cephlasporins?
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Cefepime (IV)
Enter CNS Resistant to B-lactamase |
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**What organisms are not covered by cephlasporins?
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LAME
Listeria (Amp+Gent) Atypical like chlamydia, mycoplasma (Tet/Macrolide) MRSA (Vanc) Enterococci (Amp+/- Gent) |
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What are the VERY VERY Broad Spectrum CW synthesis inhibitor?
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Imipenem/Meropenem
MOA=Pen Covers EVERYTHING |
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**Use of VERY VERY Broad Spectrum CW synthesis inhibitor
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Empiric use in severe LT infection
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What is imipenem usually co-administed?
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Cilastatin (Renal Dehydropeptidase Inhibitor) --> Inhibit metabolism to nephrotoxic metabolite
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Aztreonam MOA
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=Pen
Resistant to B-lactamase |
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What is aztreonam used for?
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G- Rod ONLY
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**What is the advantage of aztreonam?
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No cross allergy w/ pen/ceph
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What is MOA of Vanc?
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Bind D-ala terminal of muramyl pentapeptide--> Hinder cross-linking
(NO binding to PBP) |
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**What does Vanc cover?
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G+ ONLY
MRSA (hospital acquired) Enterococci (LT only) C. diff (backup to metronidazole) |
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How does VR Enterococcus Faecum (VREF) develop resistance to vanc?
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AA substitution
(Change muramyl pentapeptide terminal D-ala --> D-lactate) |
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**Unique SE of Vanc
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Red Man Syndrome (histamine release)
From pushing drug too fast, NOT ALLERGY!!! |
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Inhibitor of 50S interferes with:
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Translocation
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Inhibitor of 30S interferes with:
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Docking
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**What are the anti-ribosomal AtB?
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CLEan TAG
50S Chloramphenicol/Clindamycin Erythromycin 30S Tet Aminoglycoside |
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All anti-ribosomal are bacteriostatic, except _____, which is bacteriocidal.
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Aminoglycoside
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Now does AG enter bacteria?
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O2 dependent uptake
Say "NO": -Need O2 (Anaerobes are resistant inherently) -Nephro/Ototoxicity |
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What drug can u give w/ AG to synergistically eliminate enterococci?
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PenG (CW drug destroy CW so AG can enter)
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What drugs compounds the nephrotoxicity of AG?
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Vanc
Ampho Cisplatin Cyclosporin |
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What other SE does AG have?
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NM blockade (decrease ACh)
CI: Pt w/ MG |
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What are the drugs for AG?
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Geta/Tobramycin, Amikacin, Streptoycin
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What organisms are covered by Tet?
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Broad Spectrum + Atypicals
Chlamydia/mycoplasma Rickettsia Borrelia Treponema (backup to PenG) |
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What is Demeclocycline?
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SIADH Tx (block ADH receptor at CD)
Li can also tx SIADH by inducing DI |
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What drugs cause SIADH?
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Vincristine/blastine
TCA Haloperidol Chlorpropramide (O.Sulfonylurea=insulin secretagogue) |
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What is tigecycline?
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Super Tet (less resistance)
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What does Tet's bind?
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Divalent Cation
(eg: antacid Mg) |
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SE of Tet:
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Decrease bone growth (Go where there is metal)
Phototoxicity |
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Chloramphenicol kills _____ of the clinically important bacteria.
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Most
(Like CHLORINE, kills everything, even Anaerobes such as Bacteroides fragilis) |
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Why is chloramphenicol back up drug?
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It is extremely toxic
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SE of Chlor?
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Aplastic Anemia
Gray Baby Syndrome |
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**What is the spectrum of macrolides?
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Similar to Tet (Broad spectrum: work very well in G+ and atypicals)
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What do u use to tx Legionella?
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Macrolide
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Why does macrolide have many DI?
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P450 inhibitor (except: Azi=No DI's-->Azi=One of the SAFEST AtB)
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What are the SE of macrolide?
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Stimulate Motilin Receptor (GI distress)
Erythro> Azi>Clarithro Can be used to tx diabetic gastroparesis |
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What are the Macrolide drugs?
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Erythro
Azithro Clarithro *Telithromycin: Active against macrolide resistent S. pneumo |
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How does Clindamycin work?
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Not a macrolide, but same MOA
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What is the use of Clindamycin?
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Narrow Spectrum
Anaerobes (B. fragilis back up to metronidazole) G+ |
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**SE of Clindanycin
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Pseudomembranous Colitis (1st one discovered)
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MOA of Linezolid & Quinupristin-Dalfopristin (streptogramins)?
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Protein Synthesis Inhibitor
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What does Linezolid & Quinupristin-Dalfopristin cover?
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VRSA, VRE
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****DOC for Community Acquired Pneumonia?
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Macrolide
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What is the steps in the synthesis of THF?
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Pteridien + PABA-->
Dihydropteroic Acid + Glutamate --> DHF --> THF |
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Pteridien + PABA--> catalyzed by:
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Dihydropteroate Synthetase
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What inhibits Dihydropteroate Synthetase?
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S=Sulfonamide
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What enzyme catalyze DHF --> THF?
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Dihydrofolate Reductase
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What drugs inhibit dihydrofolate reductase?
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TMP/Pyrimethanmie
Methotrexate |
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Which enzyme in the THF synthesis pathway is present in humans & bacterias?
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Dihydrofolate Reductase
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What are SMX and TMP?
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Antimetabolite (Substance that inhibit cell growth by substituting/competing w/ natural substrate) that inhibit THF formation
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What is sulfasalazine?
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5 ASA + SP
ASA=Aminosalicylic acid: Tx Ulcerative Colitis SP=Sulfapyridine: Tx RhA |
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**What is the use of the synergistic SMX/TMP?
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Broad Spectrum (G+ &-)
Tree: Respiratory tree Mouth: GI Pee/Protozoa: GU/Toxo+PCP Syndrome: AIDS (*****PCP) |
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How are sulfonamides eliminated?
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Hepatic Conjugation
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Sulfonamides can cause _____ in neonates.
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Kernicterus
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**What SE does sulfonamide have?
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Hemolysis in G6PD deficiency
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**What SE does trimethroprim/pyrimethiamine have?
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BM supression
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**What are quinolone good for?
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G- ONLY
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MOA of quinolones
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Topoisomerase II &IV inhibitor
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Suffix of quinolones:
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-floxacin
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What do u use for drug-resistant pneumococci?
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Levofloxacin
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What limits quinolone absorption, and y?
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Fe/Ca; chelation
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**SE of quinolones
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****Tendonitis, tendon rupture
Inhibit chondrogenesis Phototoxicity |
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What is MOA of Metronidazole?
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Unknown
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****What kind of protozoa is metronidazole DOC for?
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GET
Giardia Trichomonas Entamoeba |
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****What kind of bacteria is metronidazole DOC for?
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BaC G
Bacteroides Clostridium Gardnerella |
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****Mneumonic for Metronidazole Coverage
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"GET BaC G"
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****What are the SE of metronidazole?
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Metallic Taste
Disulfiram-like effect (Block Acetaldehyde DeH) |
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****Tx for H. Pylori
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2/4 MCAT+ 1 PPI
Metronidazole Clarithromycin Amoxicillin Tet |
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**TB drugs mnemonic
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"RESPIre"
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**INH MOA
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Inhibit mycolic acid synthesis (dependent on pro-drug conversion by catalase)
Resistant derived from mutated catalase |
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**INH SE
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Peripheral Neuritis (Supplement B6 required)
SLE |
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**Rifampin SE
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Orange Pee
Induce P450 |
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**Ethambutol SE
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Retrobulbar Neuritis --> Red Green Colorblindness
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**Pyrazinamide SE
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Hyperuricemia
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Streptomycin is backup in TB tx b/c:
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Extremely toxic (Nephro/Ototoxicity b/c it is aminoglycoside)
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What are the top 2 drugs used for TB prophylaxis?
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INH
Rif |
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MOA of Amphotericin B
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Polyene --> Pores w/ ergosterol
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Use of Ampho B:
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Wide spectrum, but only in serious infection due to toxicity
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What is Ampho B combined w/ to decrease dose needed?
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Flucytosine (Synergism)
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**SE of Ampho B
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**Nephrotoxicity
Infusion related-histamine release (hypoTN), pretx w/ antihistamine |
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What kind of drug is Nystatin?
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Polyene antifungal
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Use of Nystatin
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Topical (eg: Candidiasis)=Too toxic to use systemically
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Azole MOA
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Inhibit 14 alpha-demethylase (CV Lanosterol --> Ergosterol)
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What is the only Azole that penetrate CNS?
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Fluconazole
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What is fluconazole DOC for since it is the only azole that penetrates BBB?
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Cryptoccal Meningitis
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**SE of Azoles
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Inhibit P450 (esp Keto)--> Decrease steroid synthesis --> Decrease libido, gynecomastia
"grapefruit juice and coKe w/ ur pi" |
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**MOA flucytosine
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Converted by fungal cytosine deaminase --> 5-FU --> 5-fluorodeoxyuridine monophosphate (5Fd-UMP)
-->inhibit Thymidylate Synthase |
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What is griseofulvin?
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Disrupt microtubule structure by deposit in newly formed keratin
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What is terbinafine MOA?
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Inhibit squalene epoxidase --> Decrease ergosterol
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What is use of terbinafine (allylamine) aka Lamisil?
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Onychomycoses
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****Suffix:
-avir= -ivir= -ovir (all prodrugs & nucleoside & antimetabolites)= |
AIDS (PI's)
Influenza Herpes |
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MOA Acyclovir (look like guanine)
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Monophosphorylated by VIRAL thymidine kinase (TK)
Di/Triphsophorylated by host |
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What is MOA for Acyclovir resistance?
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Lacks TK
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What is the disadvantage of acyclovir?
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Short t1/2 (other -ovir increase half-life)
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Use for acyclovir:
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Acute neuritis in shingles
NOT Post-herpetic neuralgia (TCA/gabapentin) |
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**SE of acyclovir?
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Crystalluria (tx: full hydration)
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What advantage does acyclovir have over gancyclovir?
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Not hemotoxic
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Use of gancyclovir
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CMV (prophylaxis/tx eg: neuritis)
HSV VZV |
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**SE of gancyclovir
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"Gang up on your BM"
Dose-limiting hematotoxicity |
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Foscarnet MOA
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Inhibit Viral DNA& RNA pol (not prodrug and not an antimetabolite like the -ovirs)
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Use of foscarnet
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Same as Gancyclovir
CMV VZV HSV |
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SE of foscarnet
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Nephrotoxicity
Hypocalcemia (seizure/tremor) |
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NRTI MOA || _________.
NNRTI MOA || ________. |
Acyclovir (nucleoside antimetabolites that require activation to triphosphate via non-specific phosphorylation)
Foscarnet |
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What are NRTI usu used w/?
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PI
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What is the prototype NRTI?
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Zidovudine (AZT)
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**What is the class SE of NRTI?
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Peripheral Neuropathy
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**SE of Zidovudine
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Hematotoxicity (dose limiting)
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**SE Didanosine
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Pancreatitis (Dose limiting)
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What is special about lamivudine?
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**Least toxic NRTI
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**What is the class SE of PI?
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P450 inhibitor
Steroid like effect (insulin resistance, disordered lipid& CHO metabolism, central adiposity) |
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MOA PI
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Bind and inhibit Aspartate Protease (pol gene)--> Prevent of cleavage of precursor polypeptide
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SE of Indinavir
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Crystalluria
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**SE of Ritonavir
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Major drug interactions
-induce CYP1A2 -inhibit P450 ("BOOSTER") |
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What type of pt population is fusion inhibitors used for?
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Tx experience pts
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Enfuvitide MOA
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Bind GP41 and prevent fusion to CD4 cells
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Maraviroc MOA
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Block CCR5 on T cells & prevent entry
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What is amantidine MOA?
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Block attachment/uncoating of Influenza A (target only M2 protein w/in membrane)
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Zanamivir & Oseltamivir MOA
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Inhibit neuraminidases of Influenza A & B (enzymes that prevent clumping of virion)
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Ribavirin MOA:
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Triphosphorylated to inhibit RNA Pol
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**Use of Ribavirin
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Adjunct to alpha-IFN in HCV
Management of Respiratory Syncytial Virus |
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For what protozoa is metronidazole DOC for?
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Ambiasis
Giardiasis Trichomoniasis |
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DOC for toxoplasmosis?
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Pyrimethamine+ Sulfadiazine
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What do u use as prophylaxis and tx of malaria?
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Chloroquine +/- Primaquine
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Prophylaxis for chloroquine-resistant malaria?
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Mefloquine
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Tx for chloroquine-resistant malaria
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Quinine +/- Doxycycline
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**SE of sulfa drugs & -quines
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Hemolytic Anemia in G6PD deficiency
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**SE of quinine
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Cinchonism
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What are the Co-DOC for intestinal nematodes (worms)
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Mebendazole
Pyrantel pamoate (NM agonist --> Spastic paralysis) |
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DOC for most Cestodes (tapeworm) & Trematodes (Flukes)
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Praziquantel
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**C. diff tx:
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#1: Metronidazole
#2: Vanc |
