Antimicrobials

Stephen Jo T. Bonilla, RN, MD

General & Cancer Surgeon, St. Lukes Medical Center Professor, St. Lukes College of Nursing, TUA Freelance CGFNS/NCLEX/Local Nursing Board Exam Reviewer

Antimicrobials

Inhibition of cell wall synthesis - Penicillin - Cephalosporins - Vancomycin Inhibition of protein synthesis - Aminoglycosides - Tetracyclines - Erythromycin - Chloramphenicol - Clindamycin Inhibition of synthesis of bacterial RNA & DNA - Fluoroquinolones Folate antagonists - Sulfonamides - Trimethoprim - Co-trimoxazole Interference w/ cellular metabolism - Isoniazid (INH) - Rifampicin Alteration in membrane permeability - Amphotericin B - Nystatin - Polymyxin

Penicillin

Basic Penicillins - Penicillin G - Penicillin V Broad-spectrum Penicillins - Amoxicillin - Ampicillin - Amoxicillin-Clavulanic acid (Amoclav) - Ampicillin-Sulbactam (Unasyn) Penicillinase-resistant Penicillins - Cloxacillin - Oxacillin Extended-spectrum Penicillins (Pseudomonas) - Carbenicillin - Piperacillin - Ticarcillin

Penicillin

Interfere with bacterial cell wall synthesis causing cell lysis (bactericidal) Effective against actively dividing & growing bacteria Gram (+) microorganisms - Staphylococcus, Streptococcus, Bacillus, Clostridium, Corynebacterium diphtheriae, Listeria (endocarditis, urethritis, conjunctivitis) Gram (-) microorganisms (outer LPS membrane surrounding the cell wall and porins) - Neisseria gonorrhea & meningitidis, Treponema pallidum Inactive against organisms w/o structure (mycobacterium, protozoa, fungi, viruses)

Penicillin

Resistance - B-lactamase - altered penicillin binding proteins (MRSA) Absorption - incompletely absorbed in stomach (except Amoxicillin) - food decreases absorption Distribution - crosses placental barrier but is not teratogenic - penetration to bone or CSF is increased with inflammation Excretion - kidneys Adverse effects - hypersensitivity (Penicilloic acid) - diarrhea - nephritis - neurotoxicity

Cephalosporin

First generation - Penicillin G substitutes - Proteus, E. coli, Klebsiella pneumoniae, Salmonella, Shigella (PEcKSS) - Cephalexin (prototype) - Cephalotin - Cephradine - Cephapirine - Cefazolin - Cefadroxil

Cephalosporin

Second generation - Haemophilus influenzae, Enterobacter, Neisseria (HENPEcK) - Cefuroxime (prototype, crosses BBB, CAP who are immunocompromised) - Cefoxitin (Bacteroides fragilis, intrabdominal sepsis, gynecologic sepsis) - Cefaclor, Cafamandole Cefmetazole *I MET a FOX, a MAN w/ FUR & FA

Cephalosporin

Third generation - Pseudomonas, Acinetobacter, Serratia - Ceftazidime - Cefotaxime (good CSF penetration) - Cefoperazone - Ceftriaxone (longest half-life, 6-8 hrs, good bone & CSF penetration) *heres a DIME, O TAXI ME to the OPERA ZONE so I can watch TRIAXONE

Cephalosporin

Fourth generation - Cefepime - Cefpirome - broad spectrum

Vancomycin

Inhibits synthesis of bacterial cell wall phospholipids Methicillin-resistant Staphylococcus aureus (MRSA) Associated w/ proliferation of Clostridium difficile (Pseudomembranous colitis) Used as prophylaxis in dental patients, w/ prosthetic heart valves SE: Flushing (red man syndrome); Shock as a result of histamine release by rapid infusion; Hearing loss

Protein Synthesis Inhibitors

50S ribosome - Clindamycin (causes Pseudomembranous colitis) - Chloramphenicol (Aplastic anemia, Gray baby syndrome) - Erythromycin (alternative to Penicillin; cholestatic jaundice, ototoxicity) 30S ribosome - Tetracycline (binds to tissues undergoing calcification, fetal hepatotoxicity) - Aminoglycosides (effective only against aerobic organisms) > Amikacin, Gentamicin, Tobramycin, Streptomycin > ototoxicity, nephrotoxicity

Fluoroquinolones

Enters cell by passive diffusion through porins Inhibit intracellular replication of bacterial DNA by interfering w/ DNA gyrase during bacterial growth & reproduction Ciprofloxacin - most potent - URTI, UTI, GITI Norfloxacin Ofloxacin (prostatitis due to E. coli & STDs)

Folate Antagonists

Folic acid required for the synthesis of purines & pyrimidines (RNA & DNA precursors), cellular growth & replication Sulfonamides - Chlamydia trachoma (most common cause of preventable blindness worldwide) - Nocardia asteroides (pneumonia & brain abscess) - E. coli - Topical use (burns, wounds) - AE: Stevens-Johnson syndrome, hemolytic anemia, kernicterus (avoid in pregnant, newborns & infants <2 months)

Folate Antagonists

Trimethoprim - more potent than sulfonamides - AE: megaloblastic anemia, leukopenia, granulocytopenia Co-trimoxazole - Trimethoprim + Sulfamethoxazole - Pneumocystis Carinii Pneumonia (most common opportunistic fungal LRTI complicating AIDS) - Neisseria - Haemophilus influenzae - Streptococcus pneumonia - E. coli, - Proteus - Salmonella - Shigella

Antimycobacterial Drugs

Tuberculosis - Isoniazid (Peripheral neuritis, hepatitis) - Rifampin (urine & feces orange-red discoloration) - Pyrazinamide - Ethambutol (optic neuritis w/ inability to discriminate between red & green) Leprosy - Dapsone - Clofazimine

Pulmonary Tuberculosis

Current Medication Regimen 2 months: Isoniazid (INH), Rifampicin (RIF) and Pyrazinamide (PZA) 4 months: Isoniazid and Rifampicin Streptomycin & Ethambutol also recommended for initial treatment 2-4 weeks not infectious, 6 months usually sufficient for killing bacilli, treatment may continue to 1 year and at least 9 months for HIV (+)

Pulmonary Tuberculosis

Second-line drugs used for resistant patients - Capreomycin - Kanamycin - Para-aminosalicylic acid - Cycloserine Chemoprophylaxis - Isoniazid & vitamin B6