ANTIBACTERIALS

ANTIBACTERIAL
Administered in the treatment of bacterial infections Act to destroy or suppress the growth of microorganisms Drugs that are designed to act selectively on foreign organisms that have invaded and infected the body of a human host

ANTIBACTERIAL
ACTION:
Interfere with biosynthesis of bacterial cell wall (penicillin) Prevent cells from invading organisms from using substances essential to their growth and development (sulfonamides, trimethoprin) Interfere with protein synthesis (aminoglycosides, macrolides) Interfere with DNA synthesis (fluroquinolones) Alter the permeability of the cell membrane (antifungals, antiprotozoal)

ANTIBACTERIAL
SPECTRUM effectiveness of the antiinfective against invading organisms BACTERICIDAL anti-infective agents that causes the death of the cells BACTERIOSTATIC anti-infective agents that interfere with the ability of the cells to reproduce or divide PROPHYLAXIS use of anti-infective agents to prevent infection before they occur

ANTIBACTERIAL
Classifications:
Penicillins Cephalosphorins Aminoglycosides Macrolides Tetracyclines Quinolones Lactams Sulfonamides

PENICILLINS
Derived form the cultures of molds or manufactured semi-synthetically 1st generation natural extracts from several strains of Penicillium mold Natural penicillins potent gram positive killers; have little to no coverage against gram negative organisms

PENICILLINS
PHARMACODYNAMICS
Bactericidal interfere with cell wall synthesis Most effective on immature cell walls of rapidly multiplying bacteria

PHARMACOHERAPEUTICS
Gram (+) cocci S. pneumoniae Gram (-) cocci N. gonorrheae, N. meningitidis Gram (+) bacilli B. anthracis, C. tetani, C. diphtheriae, T. pallidum Prophylaxis against subacute bacterial endocarditis, RHD or CHD undergoing surgery

PENICILLINS
CONTRAINDICATIONS
Hypersensitivity and allergy
Allergy to penicillin
Sx: simple rash to anaphylaxis

Used with caution to:

Nursing mothers Neonates Clients with rena, GI, hepatic dysfunctions, bleeding disorders, MG, and epilepsy

PENICILLINS
INTERACTIONS:
Probenecid increases serum levels of penicillin by decreasing renal elimination of the antibiotic May decrease effectiveness of oral contraceptives Increased risk of bleeding when given concurrently with anticoagulants and thrombolytic agents Tetracyclines, erythromycin and other bacteriostatic antibiotics may interfere with effectiveness of penicilli Antacids may impair absorption of PO penicillins

PENICILLINS
INTERACTIONS
Cloxacillin, dicloxacillin, nafcillin, and oxacilin may be poentiated by PO anticoagulants and antiinflammatory agents Increased risk of bleeding when high IV doses of carbeicillin and ticarcillin is given concurrently with anti-inflammatory agents, NSAIDs, and platelet aggregation inhibitors Aminoglycosides may be chemically inactivated if mixed in a solution with penicilin

PENICILLINS
INTERACTIONS
Chloramphenicol may decrease effetiveness of penicillin and reduce elimination of chloramphenicol May have ampicillin-induced rash when given with allopurinol

PENICILLINS
SIDE/ADVERSE EFFECTS
GI: diarrhea, N/V, flatulence, abnormal taste, epigastric distress, sore mouth and tongue, dark discoloration of tongue, oral thrush RENAL: glomerulonephritis HEMA: bone marrow depression, decreased blood cell counts CNS: neuromascular irritability, lethargy, anxiety depression, agitation, confusion, hallucinations RESPI: wheezes, laryngospasm, laryngeal edema

PENICILLINS
NURSING RESPONSIBILITY
History taking
Prior hypersensitivity to penicillins Other conditions: bleeding disorders, GI disease, renal impairment

Given on an empty stomach ( 1 hr before or 2 hours after meals) except for amoxicillin, penicillin V, augmentin Obesrve for electrolyte imbalance

PENICILLINS
PENICILLIN G
Pregnancy category B Agent of choice for gram (+) cocci and anaerobic infections IM: peak 30 60 minutes Half life: 0.5 to 0.7 hours Protein binding: 50 60% Poor PO absorption due to destruction by gastric acid

PENICILLINS
PENICILLIN G
Nursing responsibility
IM or IV Dosage vary according to severity of infections Dosages >10 M u/day must be given via IV infusion Deep IM injections to large muscles Monitor for signs of hyperkalemia and hypernatremia Used with caution to clients with renal insufficiency

PENICILLINS
Penicillin V
Pregnancy category B Semisynthetic analog of Pen G with similar spectrum of activity but lesser potency Resistant to gastric acid May be given with meals Used for mild infections of URT, scarlet fever, otitis media, sinusitis Used as prophylaxis against bacterial endocarditis (RHD, CHD, valvular dse undergoing surgery)

PENICILLINS
Penicillin V
Peak: 30 60 minutes Half life: 1 hour Protein binding: 80 90% Excretion: tubular secretion in the kidney

PENICILLINS
Ampicillin
Pregnancy category B Effective against spectrum of both gram (+) and gram (-) organisms Stable in gastric acid Used in RTI, soft tissue infections, otitis media, septicemia, bacterial meningitis, gonococcal infections, PID, prevention of bacterial endocarditis

PENICILLINS
Ampicillin
Peak (PO): 1.5 2 hrs; (IM): 1 hour Half life: 1 1.5 hours Protein binding: 20 -25% Nursing responsibility:
Given on an empty stomach Stable in saline for 24hrs and in D5W for 2hrs, IV preparation should be given over 15-30mins

PENICILLINS
Amoxicillin
Pregnancy category B Acid-stable penicillin with a spectrum similar to ampicillin but is better absorbed from the GIT Less effective to Shigella than ampicillin Used againts infections of ENT, lower RT due to streptococci, pneumococci; GU infections caused by E. coli; skin and soft tissue infections

PENICILLINS
Amoxicillin
Peak: 2 hours Protein binding: 20 25% Half life: 1 1.3 hours Nursing reponsibility
Available only in PO form Usually given Q8hrs (TID) Available in combination with potassium clavulanate

PENICILLINS
Methicillin
Pregnancy category B Semisynthetic salt of penicillin that is active against penicillinase-producing strains of staphylococci Peak: 0.5 to 1hr Half life: 0.4 to 0.8 hour Protein binding: 40 -50% Given IV or IM Excretion: hepatic, bile, real routes

CEPHALOSPORIN
Semisynthetic broad-spectrum antibiotic, structurally related to penicillin Effective against gram (+) cocci including penicillinase-producing S. aureus BACTERICIDAL; inhibit mucopeptide synthesis in the bacterial cell wall All are Pregnancy category B Spectrum of antibacterial activity increases from 1st to 3rd generation

CEPHALOSPORIN
1st Generation
Indications:
Respiratory tract infections Otitis media Skin infections Bone infections Genitourinary tract infcetions

CEPHALOSPORIN
1st Generation
Cefazolin Cefadroxil Cephalexin

CEPHALOSPORIN
2n d Generation
Indications:
Respiratory tract infections esp. penicillin-resistant Septicemia Meningitis Gonorrhea Bone and joint infection can be used as prophylaxis treatment before surgery Can be used in conjunction with AMINOGLYCOSIDES

CEPHALOSPORIN
2nd Generation
Cefamandole Cefuroxime Cefoxitin Cefotetan Cefonicid Cefmetazol

CEPHALOSPORIN
3rd Generation
Treatment of previously mentioned infections, also enhance the spectrum of coverage for additional gram negative infections Prophylaxis for perioperative infection

4th Generation

CEPHALOSPORIN
3rd Generation
Ceftizoxine Cefoperazone Cefprozil Cefotaxime Ceftazidime Cetriaxone Cefixime

CEPHALOSPORIN
Pharmacokinetics
Absorbed rapidly in the GIT May be given w/o regard to meals but presence of food will delay the absorption Peak levels:
1hr PO 45mins IM; 15mins IV

Maximum concentrations occur in liver and kidneys; excretion kidneys

CEPHALOSPORIN
Contraindications/Cautions
Use cautiously in patients with penicillin allergy Use cautiously in patients with GI or renal disease especially those receiving diuretics

Drug-drug interactions
Alcohol: antabuse-like effect Aminoglycosides: increased risk of nephrotoxicity Aspirin: increased potential risk of bleeding Anticoagulants: increased anticoagulant effect

AMINOGLYCOSIDES
Particularly useful against gram (-) pathogens Used for treatment of sepsis, endocarditis, bacteremia Ineffective against anaerobes Work poorly under conditions of low oxygen tension and in acid environments BACTERICIDAL inhibit protein synthesis

AMINOGLYCOSIDES
Indications:
Gram (-) enteric bacilli Tuberculosis Sepsis or bacteremia Strongly indicated in combination with other antibiotics for aerobic infections Given in combination with penicillin to encourage facilitation of the aminoglycosides into the cell

AMINOGLYCOSIDES
Pharmacokinetics:
Poor GI absorption Half life is 1-4hrs Excretion: kidneys

Contraindications/Cautions:
Preexisting renal disease Neuromuscular disease Patients taking skeletal muscle relaxants

AMINOGLYCOSIDES
Drug interactions
Amphotericin B, cisplatin, cyclosporine, vancomycin, enflurane, cephalosporin, methoxyflurane increased nephrotoxicity Loop diuretics increased ototoxicity Increase effect of neuromuscular blocking agents Synergistic effect when given with penicillin against pseudomonas Decreases absorption of dogoxin

AMINOGLYCOSIDES
Streptomycin Amikacin Gentamycin (Garamycin) Tobramycin Neomycin Kanamycin

MACROLIDES
BACTERIOSTATIC inhibit the growth of microorganism Inhibit protein synthesis Indications:
Infections caused by gram (+) bacteria Indicated for acute diphthria Penicillin-sensitive/allergic clients Prophylactic treatment of ophthalmia neonatorum

MACROLIDES
Indications
Erythromycin drug of choice for legionnaires disease, whooping cough
Intestinal amoebiasis, upper and lower RTI

Treatment of H. influenza when used with sulfonamide Uncomplicated urethral, endocervical, rectal infections Syphilis caused by T. pallidum

MACROLIDES
Pharmacokinetics
PO: good absorption, should be given on empty stomach, peak: 1-4hrs, duration: 6hrs Excreted mostly in bile

Contraindications/cautions
Liver disease Pregnant or breatfeeding

MACROLIDES
Drug interactions
Carbamazepine, cyclosporine, digoxin, ergotamine, terfenadine, triazolam, warfarin may increase serum levels Chloramphenicol, clindamycin, lincomycin decreased effects of these drugs

Common Macrolides
Erythromycin Clarithromycin azithromycin

TETRACYCLINES
BACTERIOSTATIC Inhibit protein synthesis Indications
Ricketssiae, C. trachomatis V. cholerae, H. ducreyi DOXYCLINE
T. pallidum hypersensitive to penicillin Adjunct therapy fro intestinal ameobiasis

Uncomplicated gonococcal infections

TETRACYCLINES
Pharmacokinetics
Action
Short acting: tetracycline Intermediate: methacycline Long acting: doxycycline

Concentrated in bile, excreted in kidneys

Drug interactions
Do not use during tooth development Lactation Renal disease

TETRACYCLINES
Contraindications:
Do not use during tooth development Avoid use in lactation Pts with renal failure: minocycline and doxycycline

Drug interaction:
Oral contraceptives: decrease effectiveness of contraceptives Oral anticoagulants: increase effect of these agents Cimetidine: decrease GI absorption of tetracycline Digoxin: increase effect of digoxin

TETRACYCLINES
Adverse/Side Effects
Photosensitivity, manifested by an exaggerated sunburn

Common Tetracyclines
Doxycycline Minocycline

QUINOLONES
Broad spectrum synthetic antibiotic class with both gram (+) and gram (-) At by interference with DNA replication BACTERICIDAL Indications:
Uncomplicated gonorrhea Respiratory, soft tissue, and skin infections, STD caused by gonorrhea and chlamydia Prophylaxis: Transurethral surgery

QUINOLONES
Drug interactions
Theophylline: elevated levels Antacids: decreased intestinal absorption Food: intake of 1-2 hours of administration will interfere absorption

Common Quinolones
Ciprofloxacin Ofloxacin Norfloxacin Nalidixic acid Lomefloxacin