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Bacteriacidal by inhibiting cell wall synthesis by preventing cross-linking of peptidoglycan chain General structure: thiazolidine ring and beta-lactam ring R group affects stability and resistance |
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Potent inhibitor of beta-lactamases Decreases penicillin resistance |
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Bacteriacidal by inhibiting cell wall synthesis Not stable in acid, narrow spectrum of action For Gram +ve bacteria Penicillin G benzathine delays absorption (maintains serum levels for 10 days) |
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Bacteriacidal by inhibiting cell wall synthesis Stable in acid Similar to Penicillin G |
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Bacteriacidal by inhibiting cell wall synthesis Stable in acid and beta-lactamase resistant |
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Bacteriacidal by inhibiting cell wall synthesis Stable in acid but susceptible to beta-lactamase Broad spectrum for both Gram +ve and Gram -ve bacteria |
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Bacteriacidal by inhibiting cell wall synthesis Stable in acid but susceptible to beta-lactamase Broad spectrum for both Gram +ve and Gram -ve bacteria |
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Aminoglycosides Bactericidal via irreversible inhibition of protein synthesis via binding to 30S ribosome Used against Gram -ve enteric bacteria, often with penicillins Irreversible damage to cochlear/vestibular cells, reversible damage to kidney tubules |
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Broad spectrum bacteriostatic via reversible binding to 30S ribosome at t-RNA acceptor site Readily binds to Ca2+ in newly formed bones & teeth Reduced bone growth and discolouration of teeth in children & new offspring |
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Bacteriostatic & reversible, first antibiotic used Structural analog of p-aminobenzoic acid (PABA) Competitive inhibition of dihydropteroate synthase for synthesis of folic acid Inhibit both Gram +ve and -ve Short-acting for UTIs Insoluble for ulcerative colitis and IBD |
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Inhibits bacterial dihydrofolate reductase for synthesis of nucleic acids Often used in combination with a sulfonamide |
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Quinolone Inhibits bacterial topoisomerase II required for transcription and DNA replication Broad spectrum, many are b-lactam resistant Used to treat complicated UTIs, Gram -ve infections but commonly misused & overused |
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DNA polymerase inhibitor Used to treat DNA viruses (Herpes, CMV) Phosphorylation required |
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Nucleoside/tide reverse transcriptase inhibitor (NRTI) Deoxythymidine analog Competitive inhibitor of HIV reverse transcriptase & chain termination Phosphorylated 3X Used to treat retroviruses (HIV) |
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Nucleoside/tide reverse transcriptase inhibitor (NRTI) Cytosine analog Competitive inhibitor of HIV reverse transcriptase & chain termination Phosphorylated 3X Used to treat retroviruses (HIV) |
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Neviraprine Delavirdine Efavirenz |
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Nonnucleoside reverse transcriptase inhibitors (NNRTIs) Noncompetitive inhibitors of transcriptase via enzymatic conformational change Must be combined with 2 other agents Used to treat retroviruses (HIV) |
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Protease inhibitor Prevents production of mature virion Metabolized by, and inhibits cytochrome P450 3A4 Used to treat retroviruses (HIV) |
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Fusion inhibitor Used to treat retroviruses (HIV) Binds to gp41 subunit of viral envelope protein Prevents fusion of viral and host cell memrbanes |
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CCR5 receptor antagonists Used to treat retroviruses (HIV) in patients infected with treatment-resistant strains Binds to CCR5 chemokine co-receptor Prevents fusion of viral and host cell membranes |
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Integrase inhibitor Used to treat retroviruses (HIV) in patients infected with treatment-resistant strains Binds to viral intgegrase & inhibits integration of viral DNA into host chromosome |
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Used to treat influenza (prophylaxis) in high-risk patients Inhibits viral proton channel M2 involved in fusion with endosome membrane & dissociation of ribonucleoprotein (uncoating) |
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Neuroaminidase inhibitor Binds to active sites & prevents release of virions from host Used to treat influenza (effective in all strains) |
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Nucleoside/nucleotide analog Inhibits translation of viral mRNA Used to treat hepatitis (HBV, HCV) |
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HCV-specific protease inhibitors |
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Blocks tubular secretion of penicillin |
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