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Drugs - Coggle Diagram

- - - - Penicillins
        
        Penicillinase-sensitive penicillins
        
        Amoxicillin, Ampicillin
        
        Mechanism: Same as penicillin. Wider spectrum; penicillinase sensitive
        
        Clinical use: Extended spectrum penicillin
        
        E coli
        
        Adverse effects: Hypersensitivity reactions, rash, Pseudomembranous colitis
        
        Resistance: Penicillinase (type of β-lactamase)
        
        Penicillinase-resistant penicillins (methicillin-like)
        
        Dicloxacillin
        
        Mechanism: Same as penicillin. Narrow spectrum; penicillinase resistant because of bulky R group
        
        Clinical use: S aureus (except MRSA)
        
        Adverse effects: Hypersensitivity reactions, interstitial nephritis
        
        Resistance: MRSA has altered penicillin-binding protein target site
        
        Original penicillins
        
        Penicillin G
        
        Benzathine penicillin G
        
        Penicillin V
        
        Mechanism: D-Ala-D-Ala structural analogs that binds PBPs to stop transpeptidase cross-linking of peptidoglycan
        
        Clinical use: Gram+ cocci and bacilli, and gram- cocci
        
        S pneumoniae, S pyogenes, N meningitidis
        
        Adverse effects: Hypersensitivity reactions, Coombs + hemolytic anemia, interstitial nephritis
        
        Resistance: β-lactamase and mutations in PBPs
        
        Can add Clavulanic acid to protect against destruction by β-lactamase
        
        Bactericidal
      - Cephalosporins
        
        Cephazolin (1st gen)
        
        Gram+ cocci; Neisseria spp, E coli, Klebsiella pneumoniae
        
        Cefoxitin (2nd gen)
        
        Gram+ cocci; Neisseria spp, E coli, Klebsiella pneumoniae
        
        Ceftriaxone (3rd gen)
        
        Serious gram- infections resistant to other β-lactams
        
        Cefepime (4th gen)
        
        Gram- organisms, with increased activity against gram+ organisms
        
        Mechanism: Inhibit cell wall synthesis, but are less susceptible to penicillinases; Bactericidal
        
        Adverse effects: Hypersensitivity reactions, low rate of cross-reactivity in penicillin-allergic patients, increased nephrotoxicity of aminoglycosides
        
        Resistance: Cephalosporinases (type of β-lactamase), structural changes in PBPs (transpeptidases)
      - Carbapenems
        
        Mechanism: Inhibits cell wall synthesis by binding PBPs
        
        Clinical use: Gram+ cocci, gram- rods, and anaerobes; Wide spectrum; limited use due to significant adverse effects (used only after other drugs have failed)
        
        Resistance: Carbapenemases produced by K pneumonia and E coli
        
        Adverse effects: GI distress, rash, CNS toxicity (seizures) at high plasma levels
      - Inhibit transpeptidation (D-Ala-D-Ala)
    - - Mechanism: Inhibits peptidoglycan formation by binding D-Ala-D-Ala; Bactericidal (except for C diff)
      - Clinical use: Gram+ only; for serious, multidrug-resistant organisms
        
        MRSA, S epidermis, C difficile (oral route)
      - Resistance: Change from D-Ala-D-Ala to D-Ala-D-Lac
      - Adverse effects: Vancomycin infusion reaction
  - - - Ciprofloxacin
  - - - Sulfamethoxazole
      - Mechanism: Bacteriostatic. Inhibits dihydropteroate synthase (bactericidal when combined with trimethoprim)
      - Clinical use: Gram+, gram-, TMP-SMX for simple UTI
      - Adverse effects: Hypersensitivity reactions, hemolysis of G6PD deficient, nephrotoxicity, photosensitivity, Stevens-Johnsons syndrome, kernicterus in infants, displacement of other drugs from albumin (warfarin)
      - Resistance: Altered dihydropteroate synthase, decreased drug uptake, increased PABA synthesis
    - - Mechanism:
  - - - Aminoglycosides
        
        Gentamicin
        
        Mechanism: Bactericidal. Irreversible inhibition of initiation complex; Block translocation; Require O2 for uptake, so only good for anaerobes
        
        Clinical use: Severe gram- bacilli; Synergistic with β-lactams
        
        Adverse effects: Nephrotoxicity, neuromuscular blokade (cannot use in myasthenia gravis), ototoxicity, teratogenicity
        
        Resistance: Transferase enzymes inactivate by acetylation, phosphorylation, or adenylation
      - Tetracyclines
        
        Doxycycline
        
        Specifically useful against community-aquired MRSA
        
        Mechanism: Bacteriostatic. Prevent attachment of tRNA; Don't take with milk, antacids or iron-containing preparations
        
        Clinical use: Limited CNS penetration; eliminated fecally and can be used in patients with renal failure; Acne
        
        M pneumoniae
        
        Adverse effects: GI distress, discoloration of teeth and bone grown in children; photosensitivity, Teratogenic (except doxycycline)
        
        Resistance: Decreased uptake by bacteria; Increased efflux out of bacteria through plasma-encoded protein pumps
    - - Macrolides
        
        Azithromycin
        
        Erythromycin
        
        Inhibits cytochrome P-450
        
        Mechanism: Bacteriostatic. Blocks translocation
        
        Clinical use: Atypical pneumonias, STIs, gram+ cocci (strep infections in patients allergic to penicillin)
        
        Adverse effects: GI motility issues, arrhythmias, rash, eosinophilia, increased concentration of anticoagulants
        
        Resistance: Methylation of 23S rRNA prevents binding of drug
      - Clindamycin
        
        Clinical uses: Anaerobic infections above the diaphragm
        
        Group A strep
        
        Mechanism: Bacteriostatic; Blocks peptidyltransferase
        
        Adverse effects: Pseudomembranous colitis (C diff overgrowth), fever, diarrhea
      - Oxazolidinones
        
        Lizenolid, Ketolids
        
        Mechanism: Inhibits protein synthesis by preventing formation of initiation complex
        
        Clinical use: Gram+ species including MRSA and VRE
        
        Adverse effects: Myelosuppression, peripheral neuropathy, serotonin syndrome (due to partial MAO inhibition)
        
        Resistance: Point mutations of ribosomal RNA