[3] PRELIMS | (P1) ANTIBACTERIAL & ANTI-INFECTIVES Flashcards
- Can eradicate an infection in the absence of host defense mechanisms
- Kills bacteria
Bactericidal
‘Cidal’ - kills; LYSE
High Concentrations
- Inhibits microbial grwoth but requires host defense mechanism to eradicate the infection
- Does not kill bacteria
Bacteriostatic
‘Static’ - inhibits
Low Concentrations
Examples of Bactericidal Medications
- (1) ____ - Tobramycin, Gentamicin, Amikacin
- (2) ____ - Penicillins (Amoxicillin), Cephalosporins (Cefazolin), Carbapenems (Meropenems),
- (3) ____ - Ciprofloxacin, Levofloxacin. Moxifloxacin
(1) Aminoglycosides
(2) Beta-Lactams
(3) Fluoroquinolones
Examples of Bactericidal Medications
- Aminoglycosides - (1) ____
- Beta-Lactams - (2) ____
- Fluoroquinolones - (3) ____
(1) Tobramycin, Gentamicin, Amikacin
(2) Penicillins (Amoxicillin), Cephalosporins (Cefazolin), Carbapenems (Meropenems)
(3) Ciprofloxacin, Levofloxacin, Moxifloxacin
Examples of Bacteriostatic Medications
- T____
- D____
- C____
- A____
- C____
- E____
- Tetracycline
- Doxycycline
- Clindamycin
- Azithromycin
- Clarithromycin
- Erythromycin
Lowest concentration of antimicrobial drug capable of inhibiting growth of an organism in a defined growth medium
Minimum Inhibitory Concentration
Cell Wall Inhibitors
- ____
- ____
- Others (____, ____, ____,)
- Beta-Lactam Antibiotics
- Beta-Lactamase Inhibitors
- Others (Bactiracin, Vancomycin, Daptomycin)
Examples of Beta-Lactam Antibiotics
- ____
- ____
- ____
- ____
- Penicillins
- Cephalosporins
- Carbapenems
- Monobactams
- Targets the cell walls of the organism
- Some antimicrobial drugs selectively interfere with the synthesis of the bacterial cell wall
Beta-Lactam Antibiotics
Beta-Lactam antibiotics contain ____ that are essential for antibacterial activity
beta-lactam rings
The mechanism of action (MOA) of Beta-Lactam Antibiotics by (1) ____ by binding to (2) ____
(1) inhibiting cell wall synthesis
(2) proteins in cell membrane
Beta-Lactam Antibiotics are most effective when ____
bacterial cells are dividing
Beta-Lactam Antibiotics
- The cell wall is composed of (1) ____ which are joined to each other by (2) ____
- Beta lactamases in (3) ____ bacteria are found in the periplasmic space
(1) polymer (peptidoglycan)
(2) peptide cross-links
(3) gram-negative
PENICILLINS - MOA
Bactericidal
- Binding to (1) ____ located in the bacterial cytoplasmic membrane
- Inhibition of (2) ____
- Production of (3) ____
(1) specific receptors (Penicillin-binding proteins or PBPs)
(2) transpeptidases
(3) autolysins
Penicillins are derived from ____
fungus
Prototype of Penicillin
Pen. G
Penicillin is widely distributed except in the ____
Cerebrospinal Fluid (CSF)
The most serious complication of penicillin is ____
hypersensitivity (allergy)
causes anaphylactic reaction
PENICILLIN - Classifications
- Narrow Spectrum: (1) ____
- Very Narrow Spectrum: (2) ____
- Extended Spectrum Penicillins: (3) ____
- Anti-pseudomonal Penicillins: (4) ____
(1) Penicillin G and Penicillin V
(2) Methicillin
(3) Ampicillin, Amoxicillin, Piperacillin, Ticarcillin
(4) Carbenicillin, Ticarcillin
Narrow Spectrum Penicillins
Highly effective against (1) ____ except (2) ____, Meningococci, spirochetes, anaerobic cocci
(1) gram-positive cocci
(2) penicillinase producing bacteria
Very Narrow Spectrum Penicillins
Active against most ____ producing ____
penicillinase producing staphylococci
Extended Spectrum Penicillins
Effective against (1) ____, (2) ____ and (3) ____
(1) gram-positive cocci
(2) enterococci
(3) Listeria monocytogenes
Anti-pseudomonal Penicillins
(1) ____, ____, and ____ – active against P. aeruginosa, P. vulgaris, Providencia, Morganella, and Enterobacter sp. but less potent than the (2) ____ against Streptococci and Enterococci
(1) Sulbenicillin, Carbenicillin and Ticarcillin
(2) extended-spectrum penicillins
Narrow Spectrum Penicillins
Syphilis:
(1) ____ 2.4 million units IM as single dose (SD)
Prophylaxis for Recurrent Rheumatic Fever:
(2) ____ 250 mg PO BID
(1) Pen G
(2) Pen V
Very Narrow Spectrum Penicillins
Cellulitis:
____ 500 mg QID
Cloxacillin
Extended Spectrum Penicillins
Cellulitis
____ 500 mg TID
Amoxicillin
Antipseudomonal Penicillins
Bone and Joint; Skin Structure Infections:
(1) ____ 3.1 g IV q4-q6
Severe Infections; Nosocomial Pneumonia:
(2) ____ 4.5 g IV q6 (CrCl > 40ml/min)
(1) Ticarcillin/Clavulanate
(2) Piperacillin/Tazobactam
PENICILLINS - Adverse Reactions
- ____ – Most important
- ____
- ____ – All Penicillins, but particularly ____ (thus methicillin is no longer available)
- ____
- ____ (primarily in antipseudomonal Penicillins – Carbenicillin and Ticarcillin)
- ____
(1) Hypersensitivity
(2) Diarrhea / methicillin
(3) Nephritis
(4) Neurotoxicity
(5) Hematologic toxicities
(6) Cation toxicity
PENICILLINS - Nursing Implications
- Carefully monitor for an allergic reaction for at least (1) ____ after its administration
- Effectiveness of oral penicillins is decreased when taken with (2) ____
- Given (3) ____ to prevent ____
(1) 30 minutes
(2) caffeine, citrus fruit, cola beverages, fruit juices, or tomato juices
(3) after meals / GI irritations
PENICILLINS
Symptoms of hypersensitivity
Fever, Rashes, Pruritus
- Are similar to penicillins, but more stable to many bacterial betalactamses and therefore have a broader spectrum of activity
Cephalosporins
CEPHALOSPORINS - Other Characteristics
- Derived from (1) ____
- (2) ____
- Does not penetrate (3) ____
(1) fungus
(2) Broad spectrum (can be used for + / - )
(3) CSF (except cefuroxime & 3rd generation agents)
CEPHALOSPORINS
- The nucleus of the cephalosporins, (1) ____ bears a close resemblance to 6-amino-penicillanic acid.
- Cephalosporins can be classified into (2) ____, depending on the spectrum of their antimicrobial activity
(1) 7-aminocephalo-sporanic acid
(2) five major groups or generations
CEPHALOSPORINS - MOA
Bactericidal
* Inhibit (1) ____ similar to penicillin, less susceptible to (2) ____
(1) cell wall synthesis
(2) penicillinases
First-Generation Cephalosporins
- Cefazolin
- Cephalexin
- Cephalothin
- Cefadroxil
- Cephapirin
Second-Generation Cephalosporins
- Cefoxitin
- Cefaclor
- Cefuroxime
- Cefamandole
- Cefonizid
- Cefotetan
- Cefprozil
Third-Generation Cephalosporins
- Ceftriaxone
- Ceftazidime
- Cefixime
- Ceftizoxime
- Cefpodoxime proxetil
- Cefotaxime
- Cefoperazone
- Moxalactam
Fourth-Generation Cephalosporins
- Cefepime
- Cefpirome
Fifth-Generation Cephalosporins
- Ceftobiprole
- Ceftaroline fosamil
First-Generation Cephalosporins
- Active against most gram-positive cocci including (1) ____ but not against (2) ____, ____, and ____
- Also active against some gram-negative bacilli: (3) ____, ____, and ____
(1) penicillin-resistant S. aureus
(2) enterococcus, Methicillin-resistant S. aureus (MRSA) and Methicillin-resistant S. epidermidis (MRSE)
(3) E. coli, K. pneumonia, and P. mirabilis
Second-Generation Cephalosporins
- (1) ____ – resistant to beta-lactamase producing gram-negative bacilli
- Improved activity against (2) ____
- Enhanced against (3) ____, ____, and some ____
(1) Cefoxitin
(2) H. influenza, M. catarrhalis, Neisseria meningitides and N. gonorrhea
(3) staphylococci, non-enterococci streptococci, and some enterobacteriaceae
Third-Generation Cephalosporins
- Effective against (1) ____, ____, and other streptococci (with exception of Ceftazidime) and have modest activity against (2) ____
- Excellent activity against N. gonorrhea, H. influenza, M. catarrhalis, and Enterobacteriaceae
(1) S. pneumoniae, S. pyogenes
(2) Methicillin sensitive S. aureus
Fourth-Generation Cephalosporins
- Active against both (1) ____ (but not MRSA) and (2) ____, including P. aeruginosa
- Inactive against (3) ____, ____, ____, ____, and ____
(1) aerobic gram-positive organisms
(2) gram-negative organisms
(3) MRSA, MRSE, Enterococcus sp., B. fragilis and ESBL
Fifth-Generation Cephalosporins
- Specifically developed to target (1) ____
- (2) ____ – active against MRSA, Penicillin-resistant S. pneumoniae, P. aeruginosa and enterococci
- (3) ____ – for acute bacterial skin and skin structure infections (ABSSSI) caused by MSSA, MRSA, S. pyogenes, E. coli and CAP caused by S. pneumoniae, S. aureus, H. influenza, K. pneumoniae, and E. coli
(1) resistant strains of bacteria
(2) Ceftobiprole
(3) Ceftaroline fosamil
First-Generation Cephalosporins
Prophylaxis for Cardiovascular and General Surgeries (Biliary Tract, Esophageal, Appendectomy or Laparoscopic Surgery): Usually (1) ____ 1-2 g IV pre-op (single-dose)
Respiratory Infections:
(2) ____ 250 mg PO q6
(1) Cefazolin
(2) Cephalexin
Second-Generation Cephalosporins
Prophylaxis for Non-perforated appendicitis:
(1) ____ 1-2 g IV pre-op
Pharyngitis/Tonsillitis:
(2) ____ 250 mg PO q12 for 10 days
(1) Cefoxitin
(2) Cefuroxime
Third-Generation Cephalosporins
CAP Mod Risk: (1) ____ 2g IV q24
CAP High Risk + Risk for P. aeruginosa infection:
(2) ____ 2 g IV q8
(1) Ceftriaxone
(2) Ceftazidime
Fourth-Generation Cephalosporins
CAP High Risk + Risk for P. aeruginosa infection:
(1) ____ 1 – 2 g IV q8-12 up to 21 days
(1) Cefepime
Fifth-Generation Cephalosporins
Skin and Soft Tissue Infections:
(1) ____ 500 mg IV infusion q12
(1) Ceftobiprole
CEPHALOSPORINS - Adverse Effects
- (1) ____ (identical to those of penicillins)
- (2) ____: Cephalotin (high doses lead to acute tubular necrosis)
- (3) ____ (Cefamandole, Cefotetan, Cefoperazone)
(1) Allergic manifestations
(2) Nephrotoxicity
(3) Disulfiram-like reactions
CEPHALOSPORINS - Nursing Implications
- Orally administered forms should be given with food to decrease (1) ____, even though this will delay absorption
- Some of these agents may cause an (2) ____ when taken with alcohol
- Monitor (3) ____
(1) GI upset
(2) Antabuse-like reaction
(3) CBC
Fused beta lactam ring and a 5-membered ring system that differs from penicillin in being saturated and containing a carbon atom instead of a sulfur atom
Carbapenems
CARBAPENEMS
- (1) ____ of activity
- Effective against (2) ____, and treatment for mix ____
- Drug of choice for (3) ____ (resistant to beta lactamase)
(1) Broad spectrum
(2) P. aeruginosa / aerobic and anaerobic infections
(3) enterobacter infections
Carbapenems
- Meropenem
- Imipenem
- Doripenem
- Ertapenem
CARBAPENEM - MOA
Inhibit (1) ____, and are highly resistant to degradation by (2) ____
(1) cell wall synthesis
(2) beta lactamases
- Interact with PBPs induces formation of long, filamentous bacterial structures
- Extremely resistant to beta lactamases
Monobactam
Monobactam
Aztreonam
MONOBACTAM - MOA
Inhibit ____ (binds to PBP3)
cell wall synthesis
Carbapenem
- (1) ____ caused by multiple-resistant and complicated polymicrobial infections caused by aerobic gram positive, gram-negative organisms, anaerobic bacteria and (2) ____
- All are recommended for (3) ____ except ____
(1) Nosocomial infections
(2) ESBL-positive organisms
(3) pseudomonal infections / Ertapenem
Monobactams
Activity limited to ____ including most Enterobacteriaceae, Aeromonas sp., N. gonorrhea, H. influenza, and P. aeruginosa
gram-negative bacilli
Carbapenem
Intraabdominal infections:
(1) ____ 1 g IV q8; (2) ____ 500 mg IV q6 or 1 g IV q8 for 4-7 days
Complicated Skin/Skin Structure Infections:
(3) ____ 500 mg IV q8
(1) Meropenem
(2) Imipenem
(3) Meropenem
Monobactams
Pseudomonal infections:
____ 2 g IV/IM q6-8
Aztreonam
CARBAPENEMS - Side Effects
- ____ and ____
- ____
- ____ allergic reactions
- Contraindicated in ____
- Nausea and vomiting (most common)
- Seizures
- Cross-sensitivity allergic reactions
- Contraindicated in epilepsy
MONOBACTAM - Side Effects
- No cross reactivity with (1) ____
- (2) ____ and ____ superinfections
- Elevation of (3) ____
- Can cause (4) test
(1) penicillin and cephalosporin
(2) Streptococcus and enterococci superinfections
(3) transaminases
(4) abnormal liver function
- Resemble beta-lactam molecules, weak antibacterials
- May inhibit bacterial beta lactamases thus protecting penicillin from inactivation
Beta Lactamase Inhibitors
Beta Lactamase Inhibitors
Fixed combinations with specific penicillins – extend spectrum of a penicillin provided that inactivity of that penicillin is due to (1) ____ and the inhibitor is active against that beta lactamase produced
(1) beta lactamase destruction
Beta-Lactamase Inhibitors
- Clavulanic acid (Usually with Amoxicillin, Ticarcillin)
- Sulbactam (Usually with Ampicillin)
- Tazobactam (Usually with Piperacillin
BETA-LACTAMASE INHIBITORS
Inhibits (1) ____ which then restores the antibacterial activity of (2) ____, ____, ____, and ____
(1) beta-lactamases
(2) amoxicillin, ampicillin, Ticarcillin and piperacillin
BETA-LACTAMASE INHIBITORS
Against beta-lactamase producing strains of ____, ____, ____, ____, ____, ____, and ____
staphylococci, gonococci, H. influenza, M. catarrhalis, Bacteroides, Klebsiella sp., and E. coli
BETA-LACTAMASE INHIBITORS
Exacerbation of chronic bronchitis:
(1) ____ 1 g BID
Severe infections; Nosocomial Pneumonia:
(2) ____ 4.5 g IV q6 (CrCl >40ml/min)
(1) Co-amoxiclav
(2) Piperacillin/Tazobactam
Inhibit cell wall mucopeptide formation by binding D-ala-D-ala portion of cell wall precursors
Vancomycin
VANCOMYCIN
Active against MSSA, MRSA, (1) ____, enterococci, streptococci, ____, ____, and ____
(1) coagulase-negative staphylococci
(2) C. diphtheria, C. difficile, and Listeria
VANCOMYCIN
____ infections:
Vancomycin 15-20 mg/kg IV q12 (adjust accordingly based on creatinine clearance)
MRSA
VANCOMYCIN - Side Effects
- (1) ____ at injection site – chills and fever
- (2) ____ (rare)
- (3) ____ – infusion related flushing (histamine induced) prolong infusion or increase dose intervals
(1) Phlebitis
(2) Ototoxicity and nephrotoxicity
(3) “Red man” or “Red neck syndrome”
Protein Synthesis Inhibitors
- ____
- ____
- ____
- ____
- ____
- ____
- ____
- Tetracyclines
- Aminoglycosides
- Macrolides/Ketolides
- Chloramphenicol
- Clindamycin
- Quinupristin/Dalfopristin
- Linezolid
TETRACYCLINE
- (1) ____ - Tetracycline, Oxytetracycline
- (2) ____ - Demeclocycline, Methacycline
- (3) ____ - Doxycycline, Minocycline, Tigecycline
(1) Short Acting
(2) Intermediate Acting
(3) Long Acting
TETRACYCLINE
- Short Acting- (1) ____, ____
- Intermediate Acting - (2) ____, ____
- Long Acting - (3) ____, ____, ____
(1) Tetracycline, Oxytetracycline
(2) Demeclocycline, Methacycline
(3) Doxycycline, Minocycline, Tigecycline
Tetracyclines
- Doxycycline
- Minocycline
- Oxtetracycline
- Tetracycline
- Tigecycline
TETRACYCLINES - MOA
Binds to (1) ____ to block binding of (2) ____ to acceptor site ribosome-mRNA complex
(1) 30S subunit
(2) aminoacyl-tRNA
TETRACYCLINES
Drug of choice for (1) ____, ____, ____, some ____ and ____, Mycoplasmas
(2) ____ patients with leptospirosis, syphilis, actinomycosis, tularemia, melioidosis and skin and soft tissue infections
(1) V. cholera, V. culnificus, B. burgdorferi, some Aeromonas and Xanthomas sp.,
(2) Penicillin allergic
TETRACYCLINES
Cervicitis/Nongonococcal urethritis/Chlmaydia infections:
Doxycycline 100 mg PO BID x (1) ____
Donovanosis:
Doxycycline 100 mg PO BID x (2) ____ until all lesions have completely healed
Lymphogranuloma venereum:
Doxycycline 100 mg PO BID x (3) ____
(1) 7 days
(2) 3-4 weeks
(3) 21 days
TETRACYCLINE - Adverse Effects
- ____
- ____
- ____
- ____
- ____
- ____
- ____
- Gastric discomfort
- Deposition in the bone and primary dentition
- Fatal hepatotoxicity
- Phototoxicity
- Vestibular problems
- Pseudotumor cerebri
- Superinfections
TETRACYCLINES
- (1) ____, ____, ____, and ____ should be avoided because of the chelation and drug-binding that occurs.
- All medications should be taken with (2) ____.
- Due to photosensitivity, avoid (3) ____
(1) Milk products, iron preparations, antacids, and other dairy products
(2) 6 to 8 ounces of fluid, preferably water
(3) sunlight and tanning beds
Mainstay for the treatment of aerobic, Gram negative bacilli
Aminoglycosides
AMINOGLYCOSIDES
A group of bactericidal inhibitors of protein synthesis originally obtained from various ____ and ____. And sharing chemical, antimicrobial, pharmacologic and toxic characteristics
Streptomyces and Micromonospora spp
AMINOGLYCOSIDES - MOA
- Diffuse through (1) ____ in the outer membrane of gram negative bacteria to enter the periplasmic space.
- Irreversible inhibition of (2) ____.
- Once inside the cell, aminoglycosides bind to (3) ____ and interfere with ____. Causes misreading and premature termination of (4) ____
(1) aqueous channels formed by porin proteins
(2) protein synthesis
(3) polysomes / protein synthesis
(4) mRNA translation
Aminoglycosides
- Amikacin
- Streptomycin
- Tobramycin
- Kanamycin
- Netilmycin
AMINOGLYCOSIDES
- Active against aerobic gram-negative bacilli; most are active against (1) ____, ____, ____, and ____
- Useful combination treatment for (2) ____
- (3) ____ against staphylococcal, streptococcal, and enterococcal endocarditis
(1) P. aeruginosa, E.coli, Klebsiella and Proteus sp.
(2) serious gram negative infections
(3) Synergistic
AMINOGLYCOSIDES
In addition to an antipseudomonal beta-lactam or carbapenem in HAP:
(1) ____ 20 mg/kg.day IV
Tuberculosis:
(2) ____ 15 (12-18) mg/kg IM per day (max 1 g/day
(1) Amikacin
(2) Streptomycin
AMINOGLYCOSIDES - Adverse Effects
- ____
- ____
- ____
- ____
- Ototoxicity
- Nephrotoxicity
- Neuromuscular paralysis
- Allergic reaction
AMINOGLYCOSIDES - Nursing Implications
- (1) ____ of these agents to prevent nephrotoxicity and ototoxicity
- Watch out for signs and symptoms of ototoxicity: (2) ____
- Watch out for signs and symptoms of nephrotoxicity: (3) ____
(1) Monitor peak and trough blood levels
(2) dizziness, tinnitus, and hearing loss
(3) urinary casts, proteinuria, increased BUN and serum creatinine levels
Macrocyclie lactone ring
14-16 atoms with attached deoxy sugars
Macrolides / Ketolides
Example of Macrolides/Ketolides
- Drug of first choice
- Alternative to penicillin in patients allergic to beta lactam antibiotics
Erythromycin
More examples of Macrolides/Ketolides
- Clarithromycin (semisynthetic)
- Azithromycin (semisynthetic)
- Telithromycin
Newer Macrolides
- Clarithromycin
- Roxithromycin
- Josamycin
- Telithromycin
- Fidaxomicin
MACROLIDES/KETOLIDES - MOA
- Bacteriostatic: Prevents the translocation at the (1) ____
- At higher doses, can be (2) ____
(1) 50s subunit
(2) bactericidal
MACROLIDES/KETOLIDES
- Active against (1) ____, Legionella, Mycoplasma, Chlamydia and some gram negative organisms
- Often used as alternatives for (2) ____
(1) aerobic gram-positive cocci and bacilli
(2) penicillin-allergic patients
MACROLIDES/KETOLIDES - AZITHROMYCIN
- (1) ____:
Azithromycin 500 mg PO BID
Day 1 then 250 mg PO OD for days 2 to 5 - (2) ____:
Azithromycin 500 mg PO single dose
(1) Acute bronchitis
(2) Cervicitis; Chancroid
MACROLIDES/KETOLIDES - ERYTHROMYCIN
- (1) ____:
Erythromycin 500 mg PO QID for 7 days - (2) ____:
Erythromycin base 500 mg PO QID for 7 days
(1) Chancroid
(2) Alternative for nononococcal urethritis
MACROLIDES/KETOLIDES - NEWER MACROLIDES
- (1) ____:
Clarithromycin 500 mg PO BID for 7 days - (2) ____: Clarithromycin 500 mg BID for 2 weeks
(1) Exacerbation of chronic bronchitis
(2) H. Pylori (together with Bismuth and Amoxicillin)
MACROLIDES/KETOLIDES - Nursing Implications
- (1) ____ and will cause severe interactions with ____
- Absorption of oral erythromycin is enhanced when taken (2) ____, but because of the high incidence of GI upset, many agents are taken (3) ____
- (4) ____ destroys erythromycin
(1) Highly protein bound / other protein-bound drugs
(2) on an empty stomach
(3) after a meal or snack
(4) Gastric acid
Inhibits the peptide bond formation at the 50s subunit
Chloramphenicol
CHLORAMPHENICOL - MOA
- Inhibition of (1) ____ at the 50s subunit.
- Blocks binding of the (2) ____ of the charged tRNA molecule to the acceptor site of ribosomal mRNA complex.
(1) peptide bond formation
(2) aminoacyl moiety
CHLORAMPHENICOL
- (1) ____ and ____ bacteria
- Standard therapy for (2) ____, ____, and ____
(1) Aerobic and Anaerobic
(2) typhoid fever, ampicillin-resistant H. influenza and intraocular infections
CHLORAMPHENICOL
(1) ____
* Severe and complicated: 100 mg/kg IV x 14-21 days
* Uncomplicated: 50-75 mg/kg x 14-21 days
(1) Fully susceptible typhoid:
CHLORAMPHENICOL - Adverse Effects
- A____
- G____
- Blocks the metabolism of ____ ____, ____, and ____, elevating their concentrations and potentiating effects
- Anemia
- Gray Baby Syndrome
- Blocks the metabolism of warfarin, phenytoin, tolbutamide, and chlorpropamide, elevating their concentrations and potentiating effects
- Chlorine-substituted derivative of Lincomycin (from Streptomyces lincolnensis)
- Better tolerated than erythromycin
Clindamycin (Lincosamides)
CLINDAMYCIN (LINCOSAMIDES) - MOA
- Interferes with formation of (1) ____ and ____ – inhibition of protein synthesis
- Distributes well in the body fluids except in the (2) ____
- Identical binding site with erythromycin on the (3) ____
(1) initiation complexes and aminoacyl translocation reaction
(2) CSF
(3) 50s bacterial ribosome subunit
CLINDAMYCIN (LINCOSAMIDES)
Useful for (1) ____, some anaerobic gram-negative bacilli and (2) ____
(1) aerobic and anaerobic gram-positive cocci
(2) protozoans
CLINDAMYCIN (LINCOSAMIDES)
- (1) ____:
Clindamycin 600 mg IV q6-8 - (2) ____:
Clindamycin cream 2%, 1 full applicator (5g) intravaginally HS for 7 days
Alternative: Clindamycin 300 mg PO BID for 7 days or Clindamycin ovules 100 mg intravaginally HS for 3 days - (3) ____:
(Except in Beta-lactams that already have anaerobic acvitity) Clndamycin 450-900 mg IV q8
(1) CA MRSA
(2) Bacterial Vaginosis
(3) Add-on Therapy to Aspiration Pneumonia
CLINDAMYCIN (LINCOSAMIDES) - Adverse Effects
- D____
- N____
- S____
- I____
- N____
- A____ (caused by colonization of C. difficile)
- Diarrhea
- Nausea
- Skin rashes
- Impaired liver function
- Neutropenia
- Antibiotic-related colitis (caused by colonization of C. difficile)
CLINDAMYCIN (LINCOSAMIDES) - Adverse Effects
-
Antibiotic-related colitis (caused by colonization of C. difficile)
– Initial treatment would be (1) ____ but in case it’s not effective, (2) ____ can be given as a substitute (to be given orally)
(1) metronidazole
(2) vancomycin
- A mixture of two streptogramins in a ratio of thirty to seventy, respectively
- Normally reserved for treatment of vancomycin resistant Enterococcus faecium (VRE)
Quinupristin / Dalfopristin
QUINUPRISTIN / DALFOPRISTIN - MOA
- Each component of this combination drug binds to a separate site on the 50S bacterial ribosome, forming a (1) ____ – interrupting protein synthesis
- Combination is (2) ____ and has a long (3) ____
(1) stable ternary complex
(2) bactericidal / post-antibiotic effect
QUINUPRISTIN / DALFOPRISTIN - Adverse Effects
- V____
- A____
- H____
- Inhibition of ____, drug interaction with ____ appears to occur.
- Venous irritation
- Arthralgia and myalgia
- Hyperbilirubinemia
- Inhibition of cytochrome P450 (CYP3A4) isozyme, drug interaction with digoxin appears to occur.
- Introduced to combat resistant gram-positive organisms, such as methicillin- and vancomycin- resistant Staphylococcus aureus, vancomycin-resistant E. faecium and E. faecalis, and penicillin-resistant streptococci
- Synthetic of oxazolidinone
Linezolid
LINEZOLID - MOA
- Inhibits bacterial protein synthesis by inhibiting the formation of the (1) ____.
- Linezolid binds to a site on the (2) ____ near the interface with the ____
(1) 70s initiation complex
(2) 50s subunit / 30s subunit
LINEZOLID - Adverse Effects
- W____
- G____
- H____
- R____
- T____
- Well tolerated
- GI upset (nausea and diarrhea)
- Headache
- Rash
- Thrombocytopenia (if taken >2 weeks)
FLUOROQUINOLONES
- (1) ____ - Nalidixic Acid
- (2) ____ - Ciprofloxacin, Norfloxacin, Ofloxacin
- (3) ____ - Levofloxacin
- (4) ____ - Moxifloxacin
(1) First generation
(2) Second generation
(3) Third generation
(4) Fourth generation
FLUOROQUINOLONES
- First generation - (1) ____
- Second generation - (2) ____, ____, ____, ____, ____
- Third generation - (3) ____, ____, ____, ____
- Fourth generation - (4) ____
(1) Nalidixic Acid
(2) Ciprofloxacin, Norfloxacin, Ofloxacin, Enoxacin, Lomefloxacin
(3) Levofloxacin, Clinafloxacin, Sparfloxacin, Gatifloxacin
(4) Moxifloxacin
Inhibitors of Folate Synthesis
- Mafenide
- Silver Sulfadiazine
- Succinylsulfathiazole
- Sulfacetamide
- Sulfamethoxazole
- Sulfasalazine
- Sulfisoxazole
Inhibitors of Folate Reduction
- Pyrimethamine
- Trimethoprim
Combination of Inhibitors of Folate Synthesis and Reduction
Cotrimoxazole
Urinary Tract Antiseptics
Methenamine
Nitrofurantoin
QUINOLONES - MOA
- Interfere with bacterial DNA synthesis by inhibiting:
— (1) ____ in gram negative organisms > Prevents relaxation of supercoiled DNA
—- (2) ____ in gram-positive organisms > Interfere with the separation of replicated chromosomal DNA during cell division - Usually (3) ____ against susceptible organisms
- Exhibit (4) ____ effect
(1) Topoisomerase II (DNA gyrase)
(2) Topoisomerase IV
(3) bactericidal
(4) post-antibiotic
1ST GEN - SPECTRUM OF ACTIVITY
NALIDIXIC ACID
* (1) ____
* Narrow (2) ____ coverage
(1) Enterobacteriaceae
(2) gram negative
2ND GEN - SPECTRUM OF ACTIVITY
CLASS I (NORFLAXACIN, ENOXACIN, LOMEFLOXACIN)
* Gram negative = (1) ____
* Gram Positive = (2) ____
(1) Excellent activity
(2) Good but limited activity
2ND GEN - SPECTRUM OF ACTIVITY
CLASS II (CIPROFLOXACIN, OFLOXACIN)
* Gram negative = (1) ____
* Gram positive = (2) ____
* Coverage of atypical pathogens: (3) ____ (Ciprofloxacin)
(1) Excellent activity
(2) Moderate to good activity
(3) Pseudomonas aeruginosa
3RD GEN - SPECTRUM OF ACTIVITY
LEVOFLOXACIN CLINAFLOXACIN, SPARFLOXACIN, GATIFLOXACIN
* Gram positive = (1) ____
* (2) ____ = Best agains gram positive cocci
* (3) ____ = some anaerobic activity
(1) Improved activity (S. pneumoniae & Staphylococci)
(2) Clinafloxacin
(3) Sparfloxacin
4TH GEN - SPECTRUM OF ACTIVITY
MOXIFLOXACIN
* Gram positive = (1) ____
* Anaerobic bacteria = (2) ____
(1) Enhanced activity
(2) Good activity
QUINOLONES - Adverse Effects
- ____ (nausea, vomiting, diarrhea)
- ____ (headache and dizziness)
- ____
- ____ (avoid in pregnancy and children <18 y/o)
- ____ (Moxifloxacin)
- Gastrointestinal (nausea, vomiting, diarrhea)
- CNS (headache and dizziness)
- Phototoxicity
- Connective tissue problems (avoid in pregnancy and children <18 y/o)
- QT interval prolongation (Moxifloxacin)
QUINOLONES - Nursing Implications
Should be taken with at least ____ per day, unless otherwise specified
3 L of fluid