antibiotics Flashcards
Five ways to categorize antimicrobial agents
• By the type of sensitive organism • By a scope of sensitive organisms • By a drug’s mechanism of action • By a drug’s ability to kill a microorganism vs. being able to only diminish reproduction of the microorganism • By the chemical structure of the drug 
Categorizing antimicrobials by type of sensitive organism
◉ Bacteria (Antibiotic) ◉ Fungi (Antimycotic) ◉ Viruses (Antiviral) ◉ Other organisms a. Mycobacterium b. Spirochetes c. Rickettsiae
Categorizing antimicrobials by their mechanism of action
- Inhibition of cell wall synthesis
- Increasing permeability of cell membrane
- Anti-metabolite action of a drug
- Inhibition of microbial DNA or RNA synthesis
- Inhibition of the action of microbial ribosomal subunits

Categorizing antimicrobial agents by ability to kill microorganisms
- -cidal is a suffix denoting ability to kill an microorganism (ex. bactericidal).
- -static is a suffix denoting ability of an agent to inhibit the proliferation of an organism (ex. bacteriostatic).
Naturally derived antibiotics
- Naturally derived antibiotics include the following drug classes:
- Penicillins
- Cephalosporins
- Macrolides
- Tetracyclines
- Aminoglycosides
Synthetic antimicrobial drugs
Sulfonamides and Quinolones
Microbial sensitivity tests
Dilution tests
• Minimum inhibitory concentration (MIC)
• Minimum bactericidal concentration (MBC)
Disk-diffusion technique
Minimum Bactericidal Concentration
lowest concentration of antibiotic required to kill the germ.
Minimum inhibitory concentration
Antimicrobials are usually regarded as bactericidal when the MBC is at least four times the MIC.
microbial resistance: Target inactivation
- Conjugation - Passage of genes from cell to cell allows for development of drug resistance to occur.
- Mutation - DNA of the microbe line is spontaneously modified.
- Transduction - Bacteriophage carries modified DNA into the microbe to confer resistance.
Pharmacokinetic factors that may dictate the drug of choice
Route of administration
Distribution of an antimicrobial into the target tissue is especially important.
Many drugs will not reach their MIC in certain tissues.
Host influences that may
dictate drug of choice
Patients with compromised immune systems may require -cidal agents.
Pus will inactivate some antimicrobials (i.e. the aminoglycosides).
• Hemoglobin in hematomas will inactivate some antimicrobials (i.e. the tetracyclines and penicillins).
• Abscesses are often acidic and some antimicrobials are inactive at a low pH (i.e. the macrolides).
antimicrobial SE
- Hypersensitivity reactions
- Toxicity
- Development of additional infection or supra-infection
Categorizing antimicrobials by chemical structure
- Sulfonamides
- Penicillins
- Cephalosporins
- Macrolides
- Tetracyclines
- Quinolones
other
Sulfonamides
- Silver Sulfadiazine/ Silvadene (topical)
- Sulfacetamide (ophthalmic drops)
- Sulfadiazine
- ***Sulfamethoxazole/ Gantanol–folic acid
- Sulfamethoxazole with Trimethoprim/ Bactrim or Cotrim
Sulfamethoxazole/ Gantanol
Class: Sulfonamide antibiotic
MOA: Competitive antagonist of para-
aminobenzoic acid (PABA) which is used
by bacteria in the synthesis of folic acid.
Char: Sensitive organisms are those that
must synthesize their own folic acid. Broad spectrum antibiotic. Bacteriostatic. Distributed throughout all tissues of the body including the CSF.
Sulfamethoxazole/ Gantanol indications and SE
● Indications: Urinary tract infections, otitis media, bronchitis. Has largely been replaced by Trimethoprim Sulfa which has a broader spectrum of activity.
● Side effects: GI – upset stomach, N/V. Headache, skin rashes, and marked photosensitization.
Sulfamethoxazole with Trimethoprim/ Bactrim
● Class: Sulfonamide antibiotic in combination with an additional folic acid inhibitor.
● MOA: Interference with folic acid formation at a successive step to sulfonamides.
● Char: Sulfamethoxazole + Trimethoprim (in a 5:1 ratio) synergistically inhibits two steps in folic acid synthesis
Indications: Urinary tract infections, otitis media, sinusitis, bronchitis, pneumonia, . Also for MRSA
● Side effects: headache, nausea, diarrhea, Hypersensitivity is approximately 3x more common than with Sulfamethoxazole alone.
scary Sulfamethoxazole with Trimethoprim/ Bactrim SE
Side effects: Megaloblastosis, leukopenia, and thrombocytopenia - characteristics of folate deficiency – TMP-Sulfa most severe SE is Stevens Johnson syndrome (toxic epidermal necrolysis).
Penicillins
The Penicillins are a group of beta-lactam antibiotics used for susceptible Gram-positive organisms.
• β-lactam antibiotics work by binding to penicillin binding proteins (PBPs)on the bacteria and inhibiting the formation of peptidoglycan cross-linkage in the bacterial cell wall,
Allergic reactions to penicillin derivatives
There is an approximate 5% cross-sensitivity between penicillin derivatives and the Cephalosporins.
extreme caution with all β-lactam antibiotics in patients with a history of severe allergic reactions (urticaria, anaphylaxis, interstitial nephritis) to any β-lactam antibiotic.
Penicillins and penicillin congeners
- Penicillin G
- Penicillin VK
- Amoxicillin/ Amoxil***
- Ampicillin/ Ampicil, Omnipen
- Amoxicillin & clavulanate/ Augmentin ***
- Cloxacillin/ Cloxapen
- Dicloxacillin/ Diclox
- Methicillin/ Methicillin
Penicillin G
• Class: Beta-lactam class antibiotic
• MOA: Beta lactam component binds to PBPs on
bacteria and thereafter inhibits cross linking of
components of bacterial cell wall.
• Indications: Pen G is not used as frequently
but still be effective against many Gram positive cocci such Streptococcus and some gram negatives such as Neisseria.
Amoxicillin/ Amoxil
● Class: Penicillin derivative antibiotic containing a thiazoladine ring, a β lactam ring and side chains.
● Char: Broad spectrum antibiotic. Bactericidal. Resistance generally due to microorganism’s ability to produce β-lactamase enzyme and/or modifications of the PBP sites.
PO and IV. Rapid oral bioavailability. Distributed widely in all tissues except in the CSF.
Indications: Useful for urinary tract, ENT infections such as Strep throat and otitis media, lower respiratory, skin infections.
Side effects: GI, however generally less diarrhea than Ampicillin. Penicillin allergy and/ or anaphylaxis.
Amoxicillin and clavulanate/Augmentin
● Class: Penicillin derivative antibiotic containing Amoxil with clavulanic acid added to prevent β lactamase inhibition.
● MOA: Similar to Amoxil, binding to penicillin binding protein and inhibiting protein synthesis in the bacterial cell wall. Broader spectrum of activity yet with far less drug resistance.
Indications: Similar to amoxicillin especially when treating infections due to lactamase producing organisms.
!!! Side effects: Notable increased GI side effects from clavulanic acid. Clavulanate alone has very little antimicrobial activity. GI distress is common. Diarrhea very common. The most severe cause of antibiotic induced diarrhea is pseudomembranous colitis.
Amoxicillin and clavulanate/Augmentin DOSAGE
• Note that the 250 mg, 500 mg and 750 mg doses of Augmentin each have the same amount of clavulanate per dose, and that the differences in dosage only applies to the amount of Amoxicillin.
!!! In other words, two 250 mg Augmentin capsules will give you twice the clavulanate dose of one 500 mg Augmentin capsule.
Cephalosporins
- Cephalosporins are bactericidal and have the same mode of action as other beta- lactam antibiotics such as the penicillins.
- The cephalosporins disrupt the synthesis of the peptidoglycan layer of bacterial cell walls
Cephalosporins
The cephalosporins are divided intofive generations of drugs, based upon their spectrum of bacterial sensitivity.
• First-generation cephalosporins are predominantly active against Gram- positive bacteria (CEPH),
and successive generations have increased activity against Gram-negative bacteria, often with reduced activity against Gram-positive organisms. (CEF)
Cephalosporins
- Cephalexin/ Keflex***
- Cefazolin/ Ancef
- Cefaclor/ Ceclor
- Cefprozil/ Cefzil
- Cefixime/ Suprax
- Ceftriaxone/ Rocephin • Cefepime/ Maxipime
Cephalexin/ Keflex
Class: Cephalosporin antibiotic, first generation.
MOA: Similar to penicillin with inhibition of protein synthesis of the bacterial cell wall via beta lactam activity.
Char: Broad spectrum coverage similar to that of Amoxil. Drug resistance generally occurs as a result of β-lactamase production or modifications of PBP.

contain Dihyrothiazolidine ring, β-lactam ring along with additional side chains.