Term
Penicillin G (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class=Beta lactam/Penicillin MOA=Inhibition of transpeptidase crosslinking of bacterial cell wall by binding to Ser-OH on transpeptidase. Bactericidal Use=Active against non-B-lacamase producing G+ bacilli and several G- cocci Non-toxic,IV only |
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Term
Methicillin (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Beta lactam/Penicillin MOA: Inhibition of transpeptidase cross-linking of bacterial cell wall by binding to Ser-OH of transpeptidase. Use:No longer used clinically. First effective semi-synthetic pcn w/ resistance to S. auereus beta lactamase.
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Term
Ampicillin (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class: Beta lactam/PCN/Broad-spectrum/Amino-PCN MOA: Blocks transpeptidase cross-linking of bacterial cell wall. Alpha-hydrophilic group aids in passage through porins in G- bacterial outer cell membranes. Use:Broad-spectrum against G+ and G- bacteria Acid resistant, sensitive to B-lactamases
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Term
Amoxicillin (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class: Beta lactam/PCN/Broad-spectrum/Amino-PCN MOA: Blocks transpeptidase cross-linking of bacterial cell wall. Alpha-hydrophilic group aids in passage through porins in G- bacterial outer cell membranes. Use:Broad-spectrum against G+ and G- bacteria Acid resistant, sensitive to B-lactamases |
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Term
Carbenicillin (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class: Beta lactam/PCN/Broad-spectrum/Carboxy-PCN MOA: Blocks transpeptidase cross-linking of bacterial cell wall. Alpha-hydrophilic group aids in passage through porins in G- bacterial outer cell membranes. Use:Broad-spectrum against G+ and G- bacteria. Active against P. aeruginosa. Less active than ampicillin, higher doses, toxic SE, acid sensitive, IV
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Term
Cephalothin (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Beta Lactam/1st Gen. Cephalosporin MOA:Inhibition of transpeptidase enzyme action to inhibit cross-linking of bacterial cell wall. Use: Not active against methicillin-resistant strains. UTI, staph, strep Lower activity than pcn, but better range
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Term
Cefoperazone (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Beta Lactam/3rd Gen. Cephalosporin MOA: Inhibition of transpeptidase. Can cross BBB.
Use:Expanded G- coverage than other generations. Save for serious infection of hospitalized patients resistant to most other drugs
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Term
Cefotaxime (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Beta Lactam/3rd Gen. Cephalosporin MOA: Inhibition of transpeptidase. Can cross BBB.
Use:Expanded G- coverage than other generations. Save for serious infection of hospitalized patients resistant to most other drugs |
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Term
Ceftriaxone (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Beta Lactam/3rd Gen. Cephalosporin MOA: Inhibition of transpeptidase. Can cross BBB.
Use:Expanded G- coverage than other generations. Save for serious infection of hospitalized patients resistant to most other drugs |
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Term
Imipenem (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Beta Lactam/Carbapenem MOA:Inhibition of transpeptidase Use:Class has broadest spectrum of all B-lactams. Opposite steroeochemistry of pcn's Inactivated by dehydropeptidases in renal tubles. Administered w/ inh. of renal dehydropeptidase (cilastin) - PrimaxinTM
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Term
Meropenem (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Beta Lactam/Carbapenem MOA: Inh. of transpeptidase Use:Class has broadest spectrum of activity of all the B-lactams. Opposite stereochemistry of pcn's
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Term
Aztreonam (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Monobactam MOA: Different mechanism than beta-lactams Use: Inactive against G+ bacteria or anaerobes. Useful in PCN-allergic patients
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Term
Fosfomycin (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Misc. cell wall acting agent MOA: analog of phosphenolpyruvate and inhibits the synthesis of UDP-N-acetylmuramic acid, the precursor of NAM. Use: Active against both G+ and G- bacteria. Used to treat UTIs
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Term
D-Cycloserine (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class:Misc. cell wall acting agent MOA: Structural analog of D-alanine and inhibits the incorporation of D-ala into PG pentapeptide by inhibiting alanine racemase and D-Ala-D-ligase. Use: G+ and G- bacteria Can cause dose-related CNS toxicity
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Term
Bacitracin (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class: Misc. cell wall acting agent MOA: Inhibits PPiase by forming a complex with the C55 lipid phosphate. Ultimately prevents the transfer of peptides into the growing cell wall. Use: Very lipid soluble, only IV, IM, topical
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Term
Vancomycin (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class: Glycopepetide MOA: Binds to D-Ala-D-Ala terminus of new PG pentapeptide, inhibiting elongation and cross-linking Use:G+ only. Main stand-by drug for MRSA Resistance developes slowly through modification of D-Ala-D-Ala binding site of the PG building block. This results in loss of critical H-bond and loss of target activity
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Term
Isoniazid (Class, MOA, Clinical Use, Unique Characteristics) |
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Definition
Class: Nicotinamide-analog antibiotic MOA: Complex. Probably inhibition of mycolic acid biosynthesis. Inhibits FAS2 which normally catalyzes the linkage of fatty acids in mycobacterium. Bactericidal but inactive against resting cells. Use:In combo for active TB and other non-TB infections. Monotherapy for latent TB Low # of SE, some peripheral neuropathy and CNS toxicity.
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Term
Streptomycin (Class, MOA, SE, Clinical Use, Unique Characteristics) |
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Definition
Class: Antibiotic/Aminoglycoside MOA:Blocks protein biosythesis by blocking the assembly of the ribosome (blocking initiation complex), miscoding of AA in the peptide chain, and blocking the translocation of mRNA. It has a single binding site near the A & P sites of tRNA and makes contact with RNA bases leading to high sequence specificity. Bactericidal. SE: renal toxicity and ototoxicity
Use: aerobic G- bacteria (hydrophilic and small so can pass through outer membrane). Synergistic with other abx such as b-lactams. Isolated from soil organism Streptomyces griseus, first effective agent against tuberculosis.
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Term
Tobramycin (Class, MOA, SE, Clinical Use, Unique Characteristics) |
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Definition
Class: Antibiotic/Aminoglycoside MOA:Blocks protein biosythesis by blocking the assembly of the ribosome (blocking initiation complex), miscoding of AA in the peptide chain, and blocking the translocation of mRNA. It has a single binding site near the A & P sites of tRNA and makes contact with RNA bases leading to high sequence specificity. Bactericidal. SE: renal toxicity and ototoxicity
Use: aerobic G- bacteria (hydrophilic and small so can pass through outer membrane). Synergistic with other abx such as b-lactams. |
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Term
Kanamycin (Class, MOA, SE, Clinical Use, Unique Characteristics) |
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Definition
Class: Antibiotic/Aminoglycoside MOA:Blocks protein biosythesis by blocking the assembly of the ribosome (blocking initiation complex), miscoding of AA in the peptide chain, and blocking the translocation of mRNA. It has a single binding site near the A & P sites of tRNA and makes contact with RNA bases leading to high sequence specificity. Bactericidal. SE: renal toxicity and ototoxicity
Use: aerobic G- bacteria (hydrophilic and small so can pass through outer membrane). Synergistic with other abx such as b-lactams. |
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Term
Tetracycline (Class, MOA, SE, Clinical Use, Unique Characteristics) |
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Definition
Class: Antibiotic/tetracycline MOA: Binds to the 30S ribosomal subunit and prevents aminoacyl tRNA from binding. BindstoRNA only near the A site. O atoms of the phosphodiester binds from the 16S rRNA form interactions with a Mg2+ ion at the bottom edge. SE: GI irritation, photosensitivity, discoloration of teeth Use: ? Most presribed abx class after pcn's.
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Term
Doxycycline (Class, MOA, SE, Use, Unique Characteristics) |
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Definition
Class: Antibiotic/tetracycline MOA: Binds to the 30S ribosomal subunit and prevents aminoacyl tRNA from binding. BindstoRNA only near the A site. O atoms of the phosphodiester binds from the 16S rRNA form interactions with a Mg2+ ion at the bottom edge. SE: GI irritation, photosensitivity, discoloration of teeth Use: ? Most presribed abx class after pcn's. |
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Term
Tigecycline (Class, MOA, SE, Use, Unique Characteristics) |
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Definition
Class: Antibiotic/tetracycline MOA: Binds to the 30S ribosomal subunit and prevents aminoacyl tRNA from binding. BindstoRNA only near the A site. O atoms of the phosphodiester binds from the 16S rRNA form interactions with a Mg2+ ion at the bottom edge. SE: GI irritation, photosensitivity, discoloration of teeth Use: Broad spectrum
Most presribed abx class after pcn's. Recent approval. Resistant to efflux. |
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Term
Chloramphenicol (Class, MOA, SE, Use, Unique Characteristics) |
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Definition
Class: Antibiotic/Phenicol MOA: Binds reversible to the 30S subunit of ribosome and inhibits the peptidyl transferase step of protein synthesis. Bacteriostatic. SE: Hematological tox, bone marrow tox, grey baby syndrome
Use: Broad spectrum against aerobic and anaerobic G- & G+ organisms. Treats meningitis in developing countries. Used topically to treat eye infections
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Term
Erythromycin (Class, MOA, SE, Use, Unique Characteristics) |
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Definition
Class: Antibiotic/1st generation macrolide MOA:Binds to 50S rRNA blocking the aminoacyl translocation reaction and formation of initiation complexes. Bacteriostatic.
SE: Erythromycine one of safest abx in use (macrolides in general = GI irritation and hypersensitivity) Use: Diptheria, some acne creams, narrow spectrum
Isolated from streptomyces erythreus
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Term
Linezolid (Class, MOA, SE, Use, Unique Characteristics) |
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Definition
Class: Abx/Oxazolidinone MOA: Blocks protein synthesis by binding to the P site inthe peptidyl transferase center, hence blocking the first peptide bond-forming step in protein synthesis SE: hypersensitivity Use: Gram + bacteria (including VRE) high oral bioavailability, completely synthetic
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Term
Ciprofloxacin (Class, MOA, Use, Unique Characteristics) |
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Definition
Class: Abx/Fluoroquinolone MOA:Targets topoisomerase IV in G+ bacteria and topoisomerase II (a.k.a. DNA gyrase) in G- bacteria. Forms a tertiary complex with the enzyme and bound DNA (bicylclic ring system stacks with DNA bases). Use: Most active against G- bacteria, most active broad-spectrum antibacterial on the market.Used for infections in all sorts of locations. Has 6-F atom on piperazine ring to increase activity and uptake into bacterial cells.
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Term
Gemifloxacin (Class, MOA, SE, Use, MOA of resistance) |
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Definition
Class: Abx/3rd generation fluoroquinolone MOA:Targets topoisomerase IV in G+ bacteria and topoisomerase II (a.k.a. DNA gyrase) in G- bacteria. Forms a tertiary complex with the enzyme and bound DNA (bicylclic ring system stacks with DNA bases). SE: damage to growing cartilage (not recommended if 18 yo) Use: Improved activity against S. pneumonia and good activity against enterobacteria Resistance:point mutation on target enzyme or change in permeability of organism
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Term
Clinafloxacin (Class, MOA, SE, Use, MOA of resistance) |
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Definition
Class: Abx/3rd generation fluoroquinolone MOA:Targets topoisomerase IV in G+ bacteria and topoisomerase II (a.k.a. DNA gyrase) in G- bacteria. Forms a tertiary complex with the enzyme and bound DNA (bicylclic ring system stacks with DNA bases). SE: damage to growing cartilage Use: Improved activity against S. pneumonia and good activity against enterobacteria Resistance:point mutation on target enzyme or change in permeability of organism |
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Term
Novobiocin (Class, MOA, Use) |
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Definition
Class: Abx/Aminocoumarin MOA: Potent inhibitor of DNA gyrase by targeting GyrB subunit involved in energy transduction (competitive inhibitor of ATPase rxn catalized by GyrB) Use: MRSA, more potent than fluoroquinolones
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Term
Rifampin (Class, MOA, Use, DI) |
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Definition
Class: abx/? MOA: Only drug that blocks bacterial transcription. It does this by inhibiting RNA polymerase at its beta-subunit. Use: TB, inactive meningitis DI: inducer of CYP450
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Term
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Definition
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Term
Sulfonilamide (Class, MOA, Use) |
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Definition
Class: Abx/sulfonamide MOA: Inhibits bacterial growth by mimicking PABA and blocking the bacterial synthesis of folate, a co-enzyme for DNA biosynthesis. Use: UTI, eye lotions, infections of mucus membranes, gut infections. Used in combo with other antimetabolites.
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Term
Sulfamethoxazole (Class, MOA, Use) |
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Definition
Class: Abx/sulfonamide MOA: Inhibits bacterial growth by mimicking PABA and blocking the bacterial synthesis of folate, a co-enzyme for DNA biosynthesis. Use: UTI, eye lotions, infections of mucus membranes, gut infections. Used in combo with other antimetabolites. |
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Term
Sulfadoxine (Class, MOA, Use, PK) |
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Definition
Class: Abx/sulfonamide MOA: Inhibits bacterial growth by mimicking PABA and blocking the bacterial synthesis of folate, a co-enzyme for DNA biosynthesis. Use: UTI, eye lotions, infections of mucus membranes, gut infections. Used in combo with other antimetabolites. PK: once a week dosing
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Term
Daptomycin (Class, MOA (x4), SE) |
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Definition
Class: Abx/Cationic Peptide MOA: - Associates with the negative charge or binds to cationic binding sites on LPS outer membrane
- Binds to negative charge on inner membrane and inserts into membrane interface
- Aggregates into micelle-like complexes
- Flip-flops across the inner membrane
SE: significant due to interaction w/ eukaryotic cell membranes |
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Term
Polymyxin B (Class, MOA, SE, Route) |
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Definition
Class: Abx/Cationic Peptide MOA: -Associates with the negative charge or binds to cationic binding sites on LPS outer membrane
-Binds to negative charge on inner membrane and inserts into membrane interface
-Aggregates into micelle-like complexes
-Flip-flops across the inner membrane SE:Very toxic due to interaction w/ eukaryotic cell membranes Route: Generally used topically
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Term
Platensimycin (Class, MOA) |
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Definition
Class:Abx/ FabF/B Inhibitor MOA: Inhibits Fab F/B which is an enzyme involved in the condensation step in fatty acid biosynthesis. |
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Term
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Definition
Class: Abx/ FabF/B and Fab H inhibitor MOA: Inhibits Fab F/B and Fab H which blocks the condensation steps in fatty acid biosynthesis
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Term
Clavulanic Acid or Sulbactam (Class, MOA, Drugs used in combo with) |
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Definition
Class: Suicide inhibitors of beta-lactamases MOA: Inhbits beta-lactamases in order to allow beta-lactam antibiotics to survive Amoxacillin/Clavulanate = Augmentin Ticarcillin/Clavulanate = Timentin Ampicillin/Sulbactan = Unasyn |
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Term
Ketoconazole (Class, MOA, Uses) |
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Definition
Class:Antiungal/Azole MOA: Inhibits 14-alpha-demethylase to prevent ergosterol biosynthesis from lanosterol in the endoplasmic reticulum thus resulting in impaired cell membranes. Uses: Topical (dermatophytosis/candidiasis, seborrheic dermatitis)
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Term
Fluconazole (Class, MOA, Use, SE, DI, F, solubility) |
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Definition
Class:Antiungal/Azole MOA: Inhibits 14-alpha-demethylase to prevent ergosterol biosynthesis from lanosterol in the endoplasmic reticulum thus resulting in impaired cell membranes. Uses: Cryptococcal meningitis & mucocotaneous candidiases DI: Fewer than other azoles F: Good oral bioavailability Solubility: good water solubility. Gets into CNS well
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Term
Voriconazole (Class, MOA, Uses, Toxicity) |
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Definition
Class:Antiungal/Azole MOA: Inhibits 14-alpha-demethylase to prevent ergosterol biosynthesis from lanosterol in the endoplasmic reticulum thus resulting in impaired cell membranes. Uses: Candida & dimorphic fungi Toxicity: Less toxic than ampho B
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Term
Terbinafine (Lamisil) (Class, MOA, Uses, Fungicadal or Fungistatic, Resistance) |
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Definition
Class:Antifungal/Allylamine MOA: Inhibits squalene epoxidase in the endoplasmic reticulum causes high levels of squalene which increase membrane permeability. Uses: Treatment of nail infections. Topical and oral formulations.
Fungicidal No resistance so far
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Term
Amphotericin B (Class, MOA, F, Uses, Toxicity, Resistance) |
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Definition
Class: Antifungal/Polyene MOA: Interact with membrane sterols to form pores/channels. F: Poorly absorbed in GI tract Uses: Broadest spectrum antifungal, life threatening mycotic infections Toxicity: Infusion rxn and renal toxicity Resistance is rare
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Term
Caspofungin (Class, MOA, fungicidal or fungistatic, Uses, MOA of resistance) |
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Definition
Class: Antifungal/Echinocandin MOA: Non-competitive inhibitor of glucan synthetase which causes cytological and structural changes in the fungal cell wall. Yeast = fungicidal, Mold = fungistatic Uses: Candida & aspergillus Resistance: target mutation
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Term
Flucytosine (Class, MOA, Unique characteristics) |
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Definition
Class: Antifungal/pyrimidine MOA: Incorporated into RNA/DNA (F5-FUTP) or inhibits thymidylate synthase (5-FdUMP) to prevent DNA/RNA synthesis in the nucleus. Prodrug to 5-fluorouracil
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Term
Acyclovir (Class, MOA, Why specific to viral replication, Uses) |
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Definition
Class: Antviral MOA: Inhibits viral DNA polymerase by inserting into DNA template and terminating the chain. Specificity:Mammalian enzymes do not phosphorylate acyclovir as efficiently as do HSV Uses: Herpes
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Term
Valgancyclovir (Valtrex) (Class, MOA, Uses, Bioavailabiity) |
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Definition
Class: Antiviral MOA: Terminates viral DNA chain. Phosphorylated by viral thymidine kinase to form triphosphate molecule. Use: Herpes F: Increased because it is a prodrug to acyclovir
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Term
Ganciclovir (Class, MOA, Uses, F) |
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Definition
Class:Antiviral MOA:Terminates viral DNA chain and inhibits viral DNA polymerase. Use: Herpes F:Prodrug to acyclovir |
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Term
Cidofovir (Class, MOA, use) |
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Definition
Class: Antiviral MOA: Terminated viral DNA and competitively inhibits viral DNA polymerase. Does NOT require activation by thymidine kinase so less resistance Use: Herpes
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Term
Foscarnet (Class, MOA, Use) |
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Definition
Class: Antiviral MOA:Incorpirated into viral DNA to inhibit DNA chain elongation and also competitively inhibits viral DNA polymerase. Dose NOT need to be activated by viral thymidine kinase. Use: Herpes |
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Term
Lamivudine (Class, MOA, Use) |
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Definition
Class:Antiviral MOA: Inhibits hepatitis B viral polymerase by competing with deoxycytidine triphosphate for incorporation into the viral DNA Use: Hepatitis B Virus
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Term
Entecavir (Class, MOA, Use, F, tolerability) |
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Definition
Class:Antiviral MOA: Competitively inhibits all function of DNA polymerase.
Use: Hepatitis B Virus Good F and well tolerated
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Term
Telbivudine (Tyzeka) (Class, MOA, Use) |
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Definition
Class:Antiviral MOA: Nucleoside analgue that inhibits the heppatitis B virus polymerase. Use: Hepatitis B Virus |
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Term
Amantadine (Class, MOA, Use, SE) |
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Definition
Class: Antiviral MOA: Acts on RNA viruses by blocking the M2 channel which is responsible for transporting H+ into the interior of the virions and initiating the viral uncoating process. Use: Influenza A SE: GI, CNS, peripheral edema, teratogenic in rodents
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Term
Rimantadine (CLass, MOA, Use, SE) |
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Definition
Class: Antiviral MOA: Acts on RNA viruses by blocking the M2 channel which is responsible for transporting H+ into the interior of the virions and initiating the viral uncoating process. Use: Influenza A, more active than amantadine but more extensively metabolized SE: GI, CNS, peripheral edema, teratogenic in rodents |
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Term
Zanamivir (Relenza) (Class, MOA, Use) |
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Definition
Class:Antiviral MOA: Inhibits neuraminidase (analog of sialic acid) so that the sialic acid on the cell receptor cannot be cleaved and the virus cannot be released virons. Use: Influenza A & B
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Term
Oseltamivir (Tamiflu) (Class, MOA, Use) |
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Definition
Class:Antiviral MOA: Inhibits neuraminidase (analog of sialic acid) so that the sialic acid on the cell receptor cannot be cleaved and the virus cannot be released virons. Use: Influenza A & B |
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Term
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Definition
Class: Antiviral MOA: Converted in cell to ribavirin-MP which inhibits IMP dehydrogenase thus inhibits biosynthesis of RNA.
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Term
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Definition
Biologic against Hepatitis B and hepatitis C (if w/ ribavirin)
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Term
Fomivirsen (Class, MOA, Use) |
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Definition
Class:Antiviral MOA:DNA antisense molecule. Blocks the translation of viral RNA Use: Retinal inflammation caused by CMV in AIDS patients
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Term
Palivizumab (Class, MOA, Use) |
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Definition
Class: Antiviral MOA: humanized monoclonal antibody Use: treatment of respiratory syncytial infection (RSV) in babies
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Term
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Definition
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Term
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Definition
Class: Protease inhibitor Use: HIV
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Term
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Definition
Class:Protease inhibitor Use: HIV
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Term
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Definition
Class: Antiretroviral drug, entry inhibitor Use: HIV
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Term
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Definition
Class: Antiretroviral, entry inhibitor Use: HIV
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