1 / 30

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.

amalia
Télécharger la présentation

Chemotherapeutic Agents, chapter 34-39

An Image/Link below is provided (as is) to download presentation Download Policy: Content on the Website is provided to you AS IS for your information and personal use and may not be sold / licensed / shared on other websites without getting consent from its author. Content is provided to you AS IS for your information and personal use only. Download presentation by click this link. While downloading, if for some reason you are not able to download a presentation, the publisher may have deleted the file from their server. During download, if you can't get a presentation, the file might be deleted by the publisher.

E N D

Presentation Transcript

  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

More Related