Antibiotics - Anti-infectives PDF - Classification

ANTIBIOTICS- ANTI-INFECTIVES  Learning Outcomes ⚫KNOW THE DIFFERENT THERAPEUTIC CLASSIFICATION OF DRUGS ⚫GAIN KNOWLEDGE IN DIFFERENT DRUGS AVAILABLE IN THE MARKET ⚫IDENTIFY THE MECHANISM OF ACTIONS OF DIFFERENT DRUG CATEGORY ⚫PARTICIPATE ACTIVELY IN ENUMERATING AND IDENTIFYING DRUGS IN T...

ANTIBIOTICS- ANTI-INFECTIVES  Learning Outcomes ⚫KNOW THE DIFFERENT THERAPEUTIC CLASSIFICATION OF DRUGS ⚫GAIN KNOWLEDGE IN DIFFERENT DRUGS AVAILABLE IN THE MARKET ⚫IDENTIFY THE MECHANISM OF ACTIONS OF DIFFERENT DRUG CATEGORY ⚫PARTICIPATE ACTIVELY IN ENUMERATING AND IDENTIFYING DRUGS IN THE MARKET  Historical Background Sir Alexander Fleming- discovered penicillin in 1929 Florey and Chain introduced penicillin into therapy in 1938. Came from the word antibiosis which means against life “an antibiotic or antibiotic substance is a substance produced by microorganisms, which has the capacity of inhibiting the growth and even of destroying other microorganisms.”  ANTI-INFECTIVE AGENTS  Anti-infectives are designed to act selectively on foreign organisms that have invaded and infected the body  Anti-infectives- range from antibiotics, antifungals, antiprotozoals, anthelmintics, antivirals and antimycobacterial  Characteristics of a Antibiotics An antibiotic should possess selective toxicity chemical stability Slow Rate of biotransformation and elimination  NARROW SPECTRUM BROAD-SPECTRUM BACTERIOSTATIC DRUG BACTERICIDAL  General Mechanisms of Action of Anti-infective Agents Some interfere with the biosynthesis of bacterial cell WALL Some inhibit protein synthesis Some inhibit DNA/RNA synthesis Some change the cell membrane permeability  Common Adverse Reactions: Anti-infective Therapy The most common adverse effects are due to the direct action of the drugs in the following organ system- Neuro, nephro and GI system 1. Nephrotoxicity 2. Gastro-intestinal 3. CNS toxicity 4. Hypersensitivity 5.Superinfections ANTIBIOTICS  PENICILLINS CEPHALOSPHORINS B-LACTAM ANTIBIOTICS CARBAPENEMS MONOBACTAMS  ß-LACTAM ANTIBIOTICS CELL CELL MEMBRAN WALL E THFA DNA Ribosomes mRNA PABA Inhibitor of cell wall synthesis Beta Lactam ring PENICILLINS  The PENICILLINS(beta lactam antibiotics ) Narrow/Intermediate spectrum penicillins – Penicillin G – Penicillin V Broad Spectrum Penicillins (aminopenicillin) – Amoxicillin – Ampicillin – Bacampicillin Penicillinase-resistant Penicillin/ Narrow Spectrum (anti-staphyloccocal penicillins) – Cloxacillin – Nafcillin – Methicillin – Dicloxacillin – Oxacillin Extended-Spectrum penicillins (Anti-pseudomonal penicillins) – Carbenicillin – Mezlocillin – Piperacillin – Ticarcillin acid Beta-lactamase inhibitors – Clavulanic – Sulbactam – Tazobactam Example PENICILLINS available ⮚ Methicillin Sodium, USP(Staphcillin) ⮚ Oxacillin Sodium Prostaphlin (IV) ⮚ Cloxacillin Sodium Prostaphlin (oral), Secloxin ⮚ Dicloxacillin Sodium Dynapen, Veracillin ⮚ Nafcillin Sodium (Unipen) ⮚ Ampicillin (Ampicin) ⮚ Bacampicillin HCl (Spectrobid) ⮚ Amoxicillin Amoxil,Polymox,Himox,Pediamox ⮚ Carbenicillin Sodium (Geopen,Polypen) ⮚ Ticarcillin Disodium (Ticar) ⮚ Mezlocillin (Mezlin) ⮚ Piperacillin Sodium (Pipracil) Beta-Lactamase Inhibitor  ß-LACTAMASE INHIBITORS Class I: –Clavulanic acid, sulbactam, and tazobactam Class II: –The carbapenem derivative imipenem, CEPHALOSPORINS  Cephalosporins Cephalosporins are similar to penicillins in terms of mechanism of action, chemical structure, and toxicities. By targeting bacterial cell wall transpeptidases and penicillin binding proteins (PBPs), cephalosporins cause cells wall lysis, which is the basis of bacteriocidal activity for susceptible bacteria. Although many (most) bacteria contain  Oral Cephalosporins Cephalexin Cephradine Cefadroxil Cefaclor, Cefprozil Loracarbef Cefuroxime axetil Cefpodoxime proxetil Cefixime  PARENTERAL CEPHALOSPORINS Cephradine, Cefuroxime, and Cefixime cephalosporin that is used both orally and parenterally. Cephalotin Cephapirin Cefazolin Cefamandole Cefonicid Ceforanide Cefotaxime Ceftizoxine Ceftriaxone Ceftazidime Cefoperazone.  CLASSIFICATION First Generation Second Generation Third Generation Fourth Generation Fifth Generation – Based on their time of discovery  First Generation Cefalexin (Keflex, Cefalin, Ceporex) Cephradine (Velosef, Anspor, Cefralon) Cefadroxil (Duricef) Cephalothin (Keflin) Cephapirin(Cefadyl) Cefazolin (Ancef, Kefzol, Stancef)  Second Generation Cefaclor (Ceclor) Cefmetazole (Zefazone) Cefonicid Cefotetan(Cefotan) Cefoxitin (Mefoxin) Cefuroxime (Zinacef) Cefpodoxime (Cefadox,Vantin) Cefprozil (Cefzil) Loracarbef (Lorabid) Cefamandole (Mandol)  Third Generation Cefixime (Tergecef,Suprax) Cefoperazone (Cefobid) Cefotaxime(Claforan) Ceftazidime (Fortum) Ceftibuten (Cedax) Ceftizoxime(Cefizox) Ceftriaxone (Rocephin)  Fourth Generation Cefepime (Maxipime,Axepi,Cepimax) Cefpirome (Cefrom)  Fifth Generation Ceftaroline (Teflaro) Ceftobiprole (Zeftera) *under investigation  Monobactams Aztreonam Disodium, USP (Azactam) Tigemonam POLYPEPTIDES THE POLYPEPTIDES Vancomycin Hydrochloride, (Vancocin, Vancoled). Teicoplanin (Teichomycin A2, Targocid) Bacitracin Membrane-Active Agents -Polymixin -Gramicidin Agents Affecting Bacterial Protein Synthesis Agents Affecting Bacterial Protein Synthesis Aminoglycosides Macrolides Lincosamides Tetracyclines Chloramphenicols The Aminoglycosides  History 1939-discovery of streptomycin from genus Streptomyces Then followed by kanamycin, neomycin , paromomycin, gentamicin, tobramycin and netilmicin. potent broad-spectrum  The Aminoglycosides 1.Gentamicin (Garamycin) 2.Tobramycin 3.Amikacin (Amikin) 4.Netilmicin (Netromycin) 5.Kanamycin(Kantrex) 6. Streptomycin 7. Neomycin (Mycifradin, Neobiotic) 8. Paromomycin(Humantin) 9. Spectinomycin (Tobricin)  ANTIBIOTICS Macrolides  Macrolides Clarithromycin (Klaricid, Klaz)  Erythromycin  Dirithromycin (Dynabac)  Azithromycin (Zithromax)  ANTIBIOTIC THE LINCOSAMIDES  THE LINCOSAMIDES Lincomycin Hydrochloride, USP (Lincocin) Clindamycin Hydrochloride (Dalacin) – Clindamycin Palmitate Hydrochloride (Cleocin Pediatric) – Clindamycin Phosphate(Cleocin Phosphate)  ANTIBIOTICS Tetracycline  The Tetracyclines Short-acting tetracyclines: - tetracycline - oxytetracycline Intermediate acting tetracyclines : - demeclocycline - methacycline Long acting tetracyclines - doxycycline  The Tetracyclines Tetracycline (Achromycin, Cyclopar, Panmycin, Tetracyn) Rolitetracycline ( Syntetrin) Oxytetracycline Hydrochloride (Terramycin) Demeclocycline, (Declomycin) Meclocycline Sulfosalicylate, (Meclan) Doxycycline, (Vibramycin) Minocycline Hydrochloride (Minocin, Vectrin)  Chloramphenicols MOA: inhibits protein synthesis by binding reversibly to the 50S subunit of bacterial ribosome. Broad spectrum Pharmacokinetic: Orally and IV, metabolized in the liver, can cross placenta and blood-brain barrier ADR: Bone marrow toxicity OTHER ANTIBIOTICS Novobiocin Sodium Quinupristin/ Dalfopristin (Synercid) Mupirocin, ( Bactroban Linezolid (Zyvox) Agents Affecting Bacterial DNA  Quinolones Nalidixic acid (NegGram) Cinoxacin (Cinobac) Norfloxacin (Noroxin, Uritracin)400mg, 800mg dose, also useful in gonorrhea. Enoxacin (Penetrex) Ciprofloxacin –(Cipro, Ciprobay) Ofloxacin (Floxel,Floxel IV, Inoflox, Qinolon) Lomefloxacin (Maxaquin) Sparfloxacin THANK YOU AND CONGRATULATIONS IN MAKING IT UP TO THIS LAST PRESENTATION. DISCUSSION BOARD ☺