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Chemotherapeutic Agents, chapter 34-39

Chemotherapeutic Agents, chapter 34-39. Antibacterial compounds (procaryotes) Antifungal compounds (eucarytotes) Antiparasitic agents (eucarytotes) Antiviral compounds Anticancer compounds. Different living organisms.

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Chemotherapeutic Agents, chapter 34-39

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  1. Chemotherapeutic Agents, chapter 34-39 • Antibacterial compounds (procaryotes) • Antifungal compounds (eucarytotes) • Antiparasitic agents (eucarytotes) • Antiviral compounds • Anticancer compounds

  2. Different living organisms

  3. Antibacterial compounds, chapter 34 (- antimycobacterials) • Synthitic antibacterials (chemotherapeutica) • Antibiotics • Antibiotics • Product from metabolism (natural product) • (also applies if compd is prepared synthetically, • or is a synthetic analog of a naturally occuring antibiotic/ semisynthetic compd) Inhibit growth (bacteriostatic) or kill (bacteriocide) microorg. Effective in low conc. Antimicrobial chemotherapeutics: Antimicrobial comp ≠ Antibiotics

  4. G+ and G- bacteria

  5. Synthetic antibacterials (chemotherapeutica) Antibacterial sulfonamides

  6. Nøytral sulfonilamid dårlig vannløselig. Urine pH ca 6: Crystallization neutral form, kidney damage Modern sulfa drugs pKa 5 – 7; better solubility Sulfametoxazol Bactrim®, Trimetoprim-Sulfa ® - Urine infections Combi. with trimethoprime

  7. Inhib. of folate reductase Trimetoprim

  8. Quinolones Inhib DNA-synthesis; DNA-gyrase (prokaryoter) uwounding DNA before replic.. DNA-topoisomerase (humans), anticancer compds. ex. doxorubicin Unique mecanism, no cross resistance Broad spectrum: G+ and G- ; also mycobactria, clamydia

  9. Ciprofloksacin Ciprox®, Ciprofloxacin® Cilox® Ofloksacin Tarivid® (±)

  10. Oxazolidones Linesolid Zyvoxid® Reg. Norge 2002, 1. antibact. drug with new mechaanism of action in 35 years Inhib. protein synthesis early No cross resist.. G+ and some G-. Resistant strains New drugs?

  11. Other antibiotics

  12. Antibiotics b-Lactam-antibiotics Penicillines

  13. G+ G-

  14. Semi synthesis Stability

  15. Nat. occuring P. Semisynthetic, increased acid stability Piperacillin Tazocin® Ampicillin Pentrexyl®, Amoxicillin Amoxicillin®, Pivampicillin Pondocillin®,

  16. Kloksacillin Ekvacillin® Dikloksacillin Diclocil® Meticillin Acid labile, last resort drug resist. strains

  17. Semisynthetic, Broad spectrum, Imines Meticillinam Selexid® Pivmeticillinam Selexid® No nucleophilic cabronyl

  18. b-Lactamase Inhibitors Combination with penicillines Tazobaktam Clavulanic acid • Mechanism based irreversible enzyme inactivators Suicide substrate - kcat inhibitors - Trojan horse inhib. - latent alkylating agent ≈ Pro-drug, must be activated by the enzyme

  19. Carbapenems / Carbapenins Meropenem Meronem® Imipenem + cilastan Tienam® 2. Gen. Not cleaved by DHP-1

  20. Cephalosporins

  21. 1. generation: Relatively broad spectrum (G+, some G-) Cleaved by b-Lactamase Cephalexin Cefalex® Keflex® Cefalotin Cefalotin® Keflin® 2. generation: More broad spectrum Not cleaved by b-Lactamase Cefoxitin Mefoxitin® Cefuroxim Cefuroxim® Zinacef®

  22. 3. generation: Very broad spectrum, also Pseudomonas sp Not cleaved by b-Lactamase Acid labile Cefotaxim Cefotaxime® Claforan® Ceftazidim Fortum® Oral 3. gen (not in N): Ceftriaxon Rohephalin® R: -H, -CH=CH2, -CH2OCH3

  23. Monobactams Aztreonam Azactam®

  24. Aminoglycosides Bind to mRNA read wrong Transloc. blocked

  25. Lincomycines

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