β-lactam ('cidal); PO

Mech:

1) bind PBPs,

2) block transpeptidase x-linking,

3) activ. autolytic Es

Use: all but G(-) rods

Tox:  hypersens; hemolytic anemia

Lactamase-resistant β-lactam ('cidal)

Mech:

1) bind PBPs,2) block transpeptidase x-linking,

3) activ. autolytic Es

Use: S. aureus (not MRSA)

Tox:  hypersens; interstitial nephritis

Note "meth = iv drug use = risk staph"

Lactamase-resistant β-lactam ('cidal)

Mech: 1) bind PBPs, 2) block transpeptidase x-linking,

3) activ. autolytic Es

Use: S. aureus (not MRSA)

Tox:  hypersens

note "naf for staph"

Lactamase-resistant β-lactam ('cidal)

Mech: 1) bind PBPs, 2) block transpeptidase x-linking,

3) activ. autolytic Es

Use: S. aureus (not MRSA)

Tox:  hypersens

Wide spectrum β-lactam ('cidal)

Mech: 1) bind PBPs, 2) block transpeptidase x-linking, 3) activ. autolytic Es

Use: G(+), G(-) rods

"HELPS kill Enterococci"

Tox:  hypersens, rash, pseudomembrane colitis

Note: combine w/ clavulanic acid to enhance spectrum

"AMPed up penicillin"

Wide spectrum β-lactam ('cidal)

Mech: 1) bind PBPs, 2) block transpeptidase x-linking,

3) activ. autolytic Es

Use: G(+), G(-) rods

"HELPS kill Enterococcus"

Tox:  hypersens, pseudomembrane colitis

Note: greater PO bioavail than amp; combine w/ clavulanic acid to enhance spectrum

Antipseudomanal β-lactam ('cidal)

Mech: 1) bind PBPs, 2) block transpeptidase x-linking,

3) activ. autolytic Es

Use: Pseudomonas, G(-) rods

Tox:  hypersensNote: combine w/ clavulanic acid to enhance spectrum

Antipseudomanal β-lactam ('cidal)

Mech: 1) bind PBPs, 2) block transpeptidase x-linking,

3) activ. autolytic Es

Use: Pseudomonas, G(-) rods

Tox:  hypersens

Note: combine w/ clavulanic acid to enhance spectrum

Antipseudomanal β-lactam ('cidal)

Mech: 1) bind PBPs, 2) block transpeptidase x-linking,

3) activ. autolytic Es

Use: Pseudomonas, G(-) rods

Tox:  hypersens

Note: combine w/ clavulanic acid to enhance spectrum

1st gen cephalosporin ('cidal) - others: cefazolin

Mech: inhib cell wall synth

Use: G(+) cocci + PEcK

Tox:  hypersens (x-react w/ Pen); incr. nephrotox of aminoglycosides; disulfiram-like

2nd gen cephalosporin ('cidal) -

others: cefaclor, cefuroxime

Mech: inhib cell wall synth

Use: G(+) cocci + HEN PEcKS

Tox:  hypersens (x-react w/ Pen); incr. nephrotox of aminoglycosides; disulfiram-like

3rd gen cephalosporin ('cidal) -

others: cefotaxime, ceftazidime

Mech: inhib cell wall synth

Use: serious/resistant G(-); meningitis (penetrate BBB)

Tox:  hypersens (x-react w/ Pen); incr. nephrotox of aminoglycosides; disulfiram-like

4th gen cephalosporin ('cidal)

Mech: inhib cell wall synth

Use: G(+); Pseudomonas; serious/resistant G(-); meningitis (penetrate BBB)

Tox:  hypersens (x-react w/ Pen); incr. nephrotox of aminoglycosides; disulfiram-like

Monobactam; lactamase-resistant

Mech: binds PBP3 → inhibs cell wall synth

Use: G(-)

(pen-allergic pts whose renal insuff can't support aminoglycosides)

Tox:  nontoxic; GI upset; no x-sens w/ pen or cephs

Carbapenem; lact-R; broad-spectrum

Mech: binds PBP → inhibs cell wall synth

Use: kills everything; drug of choice for enterobacter

Tox:  GI, rash, seizures (limits use)

Note:  must admin w/ cilastatin (inhibs renal dihydropeptidase I)

Carbapenem; lact-R; broad-spectrum

Mech: binds PBP → inhibs cell wall synth

Use: kills everything; drug of choice for enterobacter

Tox:  GI, rash, (less seizures than imipenem)

Note:  stable to renal dihydropeptidase I

Antibiotic ('cidal)

Mech: binds D-ala D-ala on wall precursors → inhibs cell wall synth

Use: serious/resistant G(+) - S. aureus, C. diff, MRSA

Tox:  well-tol; nephrotox, ototox, thrombophlebitis, "red man synd" (prevent w/ anti-His pre-tx & slow infusion)

Resist: D-ala D-lac

Aminoglycoside (30S, 'cidal)

Mech: inhib formation of initiation complex & misreading of mRNA

Use: severe (G-) aerobic rods

Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen

Notes: synergy w/ β-lactams; req 02 for uptake (therefore no anaerobes)

Aminoglycoside (30S, 'cidal)

Mech: inhib formation of initiation complex & misreading of mRNA

Use: severe (G-) aerobic rods; bowel surg

Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen

Notes: synergy w/ β-lactams; req 02 for uptake

Aminoglycoside (30S, 'cidal)

Mech: inhib formation of initiation complex & misreading of mRNA

Use: severe (G-) aerobic rods

Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen

Notes: synergy w/ β-lactams; req 02 for uptake

(no anaerobes)

Aminoglycoside (30S, 'cidal)

Mech: inhib formation of initiation complex & misreading of mRNAUse: severe (G-) aerobic rods

Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen

Notes: synergy w/ β-lactams; req 02 for uptake

Aminoglycoside (30S, 'cidal)

Mech: inhib formation of initiation complex & misreading of mRNA

Use: severe (G-) aerobic rods

Tox: nephrotox (esp w/ cephs), ototox (esp w/ loops; contra: preg), teratogen

Notes: synergy w/ β-lactams; req 02 for uptake

Tetracycline (30S)

Mech: prevent attach. of aminoacyl-tRNA

Use: tick-carried bact, acne; some CNS penetration

Tox: GI, discolor teeth, inhib child bone growth (contra: preg), photosens

Notes: must not take with milk, antacids, or Fe-containing preparations (cations inhib abs)

Tetracycline (30S)

Mech: prevent attach. of aminoacyl-tRNA

Use: tick-carried bact, acne; some CNS penetration; fecally elim - used in renal failure pts

Tox: GI, discolor teeth, inhib child bone growth (contra: preg), photosens

Notes: must not take with milk, antacids, or Fe-containing preparations (cations inhib abs)

Tetracycline (30S)

Mech: prevent attach. of aminoacyl-tRNA; ADH antag

Use: tick-carried bact, acne; some CNS penetration; diuretic in SIADH

Tox: GI, discolor teeth, inhib child bone growth (contra: preg), photosens

Notes: must not take with milk, antacids, or Fe-containing preparations (cations inhib abs)

Tetracycline (30S)

Mech: prevent attach. of aminoacyl-tRNA

Use: tick-carried bact, acne; some CNS penetration

Tox: GI, discolor teeth, inhib child bone growth (contra: preg), photosens

Notes: must not take with milk, antacids, or Fe-containing preparations (2+ cations inhib abs)

Macrolide (50S)

Mech: binds 23S rRNA → blocks transloc

Use: URI, pneum, G(+) cocci STDs

Tox: GI (most com cause of noncompliance), acute cholestatic hep, eosinophilia, rashes

Interact: incr. theophylline & oral anticoag conc.

Note: "MJ #23 throw up 50 atyp. & has stds"

Macrolide (50S)

Mech: binds 23S rRNA → blocks transloc

Use: URI, pneum, G(+) cocci STDs; M. avium prophyl

Tox: GI (most com cause of noncompliance), acute cholestatic hep, eosinophilia, rashes

Interact: incr. theophylline & oral anticoag conc.

Note: "MJ #23 throw up 50 atyp. & has stds"

Macrolide (50S)

Mech: binds 23S rRNA → blocks transloc

Use: URI, pneum, G(+) cocci STDs; M. avium prophyl

Tox: GI (most com cause of noncompliance), acute cholestatic hep, eosinophilia, rashes

Interact: incr. theophylline & oral anticoag conc.

Note: "MJ #23 throw up 50 atyp. & has stds"

Antibiotic (50S)

Mech: blocks peptidyltransferase activity

Use: meningitis (esp SHiN) (kills ~everything)

Tox: limits use; anemia (dose dep), aplastic anemia (dose indep), gray baby synd (premies lack UDP-glucuronyl transferase; contra: preg)

Contra: preg

Antibiotic (50S)

Mech: blocks peptide bond formation

Use: anaerobes (above diaphr) in asperation pneumonia.

= Bacteroides and C. Perfringens

Tox: pseudomembr colitis (dt C. Diff)

Sulfonamide

Mech: PABA antimetabolite → block dihydropteroate synthetase

Use: G(+)/(-), simple UTI

Tox: hypersens, hemolysis if G6PD defic, nephrotox, photosens, kernicterus (contra: preg)

Interact: displace drugs from albumin (warfarin)

Sulfonamide

Mech: PABA antimetabolite → block dihydropteroate synthetase

Use: G(+)/(-), simple UTI (triple-sulf)

Tox: hypersens, hemolysis if G6PD defic, nephrotox, photosens, kernicterus (infant brain dmg)(contra: preg)

Interact: displace drugs from albumin (warfarin)

Sulfonamide

Mech: PABA antimetabolite → block dihydropteroate synthetase

Use: G(+)/(-), simple UTI (triple-sulf)

Tox: hypersens, hemolysis if G6PD defic, nephrotox, photosens, kernicterus (contra: preg)

Interact: displace drugs from albumin (warfarin)

Mech: inhibs (bacterial) DHF reductase

Use: combo w/ sulfonamides for recurrent UTI, Shigella, Salmonella, PCP pneum

Tox: megaloblastic anemia, leukopenia, granulocytopenia (alleviate w/ suppl folinic acid - Leucovorin rescue)

Note: "TMP Treats Marrow Poorly"

Fluoroquinolone ('cidal) - others: -flaxacin

Mech: inhib DNA gyrase (topo II)

Use: G(-) rods of GI & urinary tract (inc pseudomona)

Tox: GI, rash, cartilage dmg (contra: preg), tendonitis/rupture in adults, leg cramps/myalgias in kids

Note: must not take w/ antacids

FlouroquinoLONEs hurt attachment to BONES

AB/antiprotozoal ('cidal)

Mech; forms toxic metabolites in bact. cell → DNA dmg

Use: protozoa (giardia...), anaerobes below diaphr,

triple therapy" vs H.pylori (+bismuth & amox/tet)

Tox: disulfiram-like w/ alcohol

Mech: bind cell membr & disrupt osmotic properties

Use: resistant G(-)

Tox: neurotox, acute tubular necrosis

PolyMYXins Mix up Membranes

Anti-TB

Mech; inhib membrane E's

effective in acidic pH of phagolysosomes (where TB engulfed by Macrophages is)

Tox: hepatotox

Anti-TB

Mech: inhibs arabinosoyl transferase → block cell wall arabinogalactan synth

(dec carbohydrate polymerization of myco wall)

Tox: optic neuropathy (red-green colorblind), hepatotox

Anti-TBMech: inhibs enoyl acyl carrier prot. reductase → blocks synthesis of mycolic acids (myco cell wall)

Use: TB prophylaxis (monotherapy) or tx

Tox: inactivates B6 (& B3) → pellagra/neurotox (prevent w/ suppl pyridoxine); hepatotox

Note: diff t1/2 in fast vs. slow acetylators

Anti-TBMech: inhibs RNApol β S.U.

Use: TB, delays dapsone-resist in leprosy;

GC prophyl,H. influ b prophyl

Tox: hepatotox; red/orange body fluids (red urine)

Interact: ↑ P-450 

(50S); examples - quinopristin, dalfopristin

Use: VRE (can also use linezolid, 50S)

Antifungal

Mech: binds ergosterol → leaky membr pores

Use: systemic mycoses; intrathecally for fungal meningitis (doesn't cross BBB)

Tox: fever/chills, hypoTN, nephrotox (↓ w/ hydration), arrhythmias, anemia, IV phlebitis

Note: liposomal amphotericin reduces tox

Amphoterrible, Tears holes (pores) in cell

Mech (same as ampho):

binds ergosterol → disrupts membr

Use: Topically - swish & swallow" for thrush; topical for diaper rash/vaginal candidiasis

Tox: too tox for systemic use"

Azole antifungal

Mech: inhibs P-450 mediated conversion of lanosterol=>ergosterol

Use: systemic mycosis; crypto meningitis (fluconazole crosses BBB), candida

Tox: decr hormone synth (gynecomastia)

Interact: ↓ P-450

Azole antifungal

Mech: inhibs P-450 mediated conversion of lanosterol=>ergosterol

Use: systemic mycosis; candida

Tox: decr hormone synth (gynecomastia)

Interact: ↓ P-450

Azole antifungal

Mech: inhibs P-450 mediated conversion of lanosterol=>ergosterol

Use: Topical fungal infections.

Tox: decr hormone synth (gynecomastia)

Interact: ↓ P-450

Azole antifungal

Mech: inhibs P-450 mediated conversion of lanosterol=>ergosterol

Use: Topical fungal infections.

Tox: decr hormone synth (gynecomastia)

Interact: ↓ P-450

Antifungal

Mech: converts to 5-FU → inhibs DNA synth

Use: combo w/ ampho B for systemic fungi

Tox: n/v, diarr, marrow suppression

Note: Cytosine is deaminated to Uracil

Antifungal

Mech: inhibs β-glucan synth → blocks cell wall synth

Use: invasive aspergillosis

Tox: GI, flushing

Antifungal

Mech: inhibs squaline epoxidase (blocks squalene => lanosterol)

Use: dermatophytoses (esp onychomycosis - finger/ toenail)

Antifungal

Mech: blocks MicroTube fxn → disrupts mitosis; desposits in keratin-containing tissues (eg. nails)

Use: PO for dermatophytes

Tox: teratogenic (contra: preg), carcinogenic, confusion

Interact: ↑ P-450 & warfarin metab

Mech: blocks viral penetration/uncoating (M2 protein); causes DA release

Use: prophyl for influenza A; rubella; Parkinson's dz

Tox: cerebellar tox (ataxia, dizzy, slurred speech)

Note: 90% of flu has resistant M2

"a man ta dine take off coat"

Mech: blocks viral penetration/uncoating (M2 protein)

Use: prophyl for influenza A; rubella

Tox: fewer CNS SE than amantadine (doesn't cross BBB)

Note: 90% of flu has resistant M2

Mech: inhibs flu neuraminidase → decr. release of progeny

Use: influenza A & B

Mech: inhibs flu neuraminidase → decr. release of progeny

Use: influenza A & B

Note = Tamiflu

Mech: competitively inhibs IMP DH → inhibs G synth

Use: RSV, chronic HCV

Tox: hemolytic anemia, severe teratogen (contra: preg)

Guanosine analog

Mech: mono-P by HSV ThyKinase → tri-P by cellular Es → inhibs (preferentially viral) DNApol (chain terminator)

Use: HSV, VZV (famcyclovir for HSV), EBV; prophyl in ImuunoComp

Tox: crystalline nephrotox. (prevent w/ aggressive hydration)

Note: no effect on latent HSV/VZV

G analog

Mech: mono-P from CMV kinase or HSV/VZV TK → tri-P by cellular Es → inhibs (pref viral) DNApol

Use: CMV (esp immuno comp)

Tox: leukopenia, neutropenia, thrombocytopenia, renal tox (greater tox than acyclovir)

Pyrophosphate analog

Mech: binds DNApol (does not req activation)

Use: gancic-resist CMV retinitis; acyc-resist HSV

Tox: chelates Ca; renal Mg wasting → decr. Mg → decr. PTH release → further decr. Ca; low Mg & Ca → seizures

"FOScarnet = pyroFOSphate"

HIV protease inhib;

others(..navir)-ritonavir, indinavir, nelfinavir, amprenavir

Mech: inhibs maturation of new virus

Tox: GI, hyperglycemia, lipodystrophy, thrombocytopenia (indinavir)

"NAVIR TEASE a proTEASE"

HIV protease inhib;

others(..navir)-saquinavir, indinavir, nelfinavir, amprenavir

Mech: inhibs maturation of new virus

Tox: GI, hyperglycemia, lipodystrophy, thrombocytopenia (indinavir)

"NAVIR TEASE a proTEASE"

HIV NRTI

Use: 2 NRTIs combo w/ PI for HAART when CD4<500;

general prophyl during preg

Tox: marrow suppr, periph neuropathy, lactic acidosis, megaloblastic anemia

HIV NRTI

Use: 2 NRTIs combo w/ PI for HAART when CD4<500;

general prophyl during preg

Tox: marrow suppr, periph neuropathy, lactic acidosis

HIV NRTI

Use: 2 NRTIs combo w/ PI for HAART when CD4<500;

general prophyl during preg

Tox: marrow suppr, periph neuropathy, lactic acidosis

HIV NRTI

Use: 2 NRTIs combo w/ PI for HAART when CD4<500;

general prophyl during preg

Tox: marrow suppr, periph neuropathy, lactic acidosis

HIV NNRTI (non-nucleoside RT inhib)

Mech: bind revers transcript (site diff from NRTI)

Use: combo w/ 2NRTIs for HAART when CD4<500;

No Phosphorylation req for activity

Tox: marrow suppr, periph neuropathy, rash

"Never Ever Delavir nucleosides"

HIV NNRTI (non-nucleoside RT inhib)

Mech: bind revers transcript (site diff from NRTI)

Use: combo w/ 2NRTIs for HAART when CD4<500;

No Phosphorylation req for activity

Tox: marrow suppr, periph neuropathy, rash

"Never Ever Delavir nucleosides"

HIV NNRTI (non-nucleoside RT inhib)

Mech: bind revers transcript (site diff from NRTI)

Use: combo w/ 2NRTIs for HAART when CD4<500;

No Phosphorylation req for activity

Tox: marrow suppr, periph neuropathy, rash

"Never Ever Delavir nucleosides"

HIV fusion inhibitor

Mech: binds gp41 (inhib fusion w/ CD4s)

Use: salvage regimen when other HIV drugs not sufficient

Tox: hypersens, injection site rxns, risk of bacterial pneum

Mech: block stages of viral RNA/DNA synth; induce ribonuclease to degrade viral mRNA

Use: chronic HBV/HCV, Kaposi's sarcoma, leukemias, malignant melanoma

Tox: neutropenia

Use: Multiple Sclerosis

Tox: neutropenia

Use: NADPH oxidase deficiency; (chronic granulomatous dz)

Antihelminth

Use: Cestodes (tapeworms) & trematodes (flukes)

Antihelminth

Use: Nematodes (roundworms)

Antihelminth

Use: Loa loa, Wuchereria bancrofti, toxocara canis

Antihelminth

Use: Onchocerca volvulus, Strongyloides stercoralis

Anti-malarial

Use: kills Plasmodium in RBCs

Tox: hemolysis in G6PD defic; mefloquine contra in preg

Note: sulfadoxine + pyrimethamine, meflorquine, or quinine for resistant P. falc

Anti-malarial

Use: kills Plasmodium vivax & ovale in liver to prevent relapse

Tox: hemolysis in G6PD defic

β-lactamase inhibitor

Use: extend the spectrum of penicillin-family ABs