Antibacterial Antibiotics Flashcards by Kimerie Aquino

Interfere with last step of cell wall synthesis (transpeptidation or cross
linking)

Penicillins (Penicillum notatum)

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Beta lactam attached to:

thiazolidine ring, Nucleus: 6 aminopenicillanic acid

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Beta lactamase Inhibitors

(Clavulanic acid, sulbactam, tazobactam)

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No antibacterial activity. They inactivate beta lactamases

Beta lactamase Inhibitors (Clavulanic acid, sulbactam, tazobactam)

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The beta lactam ring is not fused to another ring, no cross sensitivity with penicillin

Monobactam

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magic bullet for Pseudomonas

Aztreonam

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Thienamycin, Meropenem, Imipenem (cleaved by dihydropeptidase; cilastatin)

Carbapenems

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Drugs under Natural Penicillins

Penicillin G (Benzylpenicillin) PO, IV, IM(Procaine and Benzathine) Use: RHD and Syphilis
Penicillin V (Phenoxymethylpenicillin) PO

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Drugs under Penicillinase Resistant/Antistaphylococcal Penicillins/Narrow Spectrum

Methicillin (2,6 dimethoxyphenylpenicillin) Prototype; off the market (interstitial nephritis)
Nafcillin (2 ethocy 1 phenylpenicillin)
Isoxazolyl Penicillins (Oxacillin, Cloxacillin,Dicloxacillin best absorbed orally)

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Drugs under Aminopenicillins/Broad Spectrum

Ampicillin (Parenteral, poor GI absorption) Prodrugs: Hetacillin, Bacampicillin, Cyclacillin
Amoxicillin (PO)

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Drugs under Extended Spectrum/Anti Pseudomonal Penicillins

Carboxypenicillins (Carbenicillin, Ticarcillin)

Ureidopenicillins (Piperacillin most potent, Azlocillin, Mezlocillin)

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only for G-

Gramicidin (S. Brevis)

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only for G+ ; MOA: Alter cell membrane permeability; Polymixin B and Colostin (Polymixin E)

Polymyxin (B. Polymyxa)

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nephrotoxic (not for IV)

Bacitracin (B. Subtilis)

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DOC for Pseudomembranous colitis and MPSA

Vancomycin (S. Orientalis)

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Only IV (not orally absorbed);

Vancomycin (S. Orientalis)

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Adverse effects of Vancomycin

Flushing (Red Man Syndrome)

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Classes that binds to 30s subunit

AMINOGLYCOSIDES, TETRACYCLINES

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Classes that binds to 50s subunit

MACROLIDES, LINCOSAMIDES, CHLORAMPHENICOL

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Drugs under Aminoglycosides

(Streptomycin, Gentamicin, Netilmicin, Neomycin, Tobramycin, Amikacin from Kanamycin A)

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Drugs under Tetracyclines

(Doxycycline, Minocycline, Tetracycline, Demeclocycline)

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ingestion of expired tetracycline

Fanconi like syndrome

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Broadest spectrum antibiotic

TETRACYCLINES (Doxycycline, Minocycline, Tetracycline, Demeclocycline)

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Adverse effects of tetracyclines

Gastric discomfort, deposition in the bones and primary dentition causing discoloration and hypoplasia of the teeth and a temporary stunting of growth, hepatotoxicity, phototoxicity (demeclocycline), vestibular problems (minocycline)

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IV (not absorbed orally) except neomycin (topical and oral only)

AMINOGLYCOSIDES (Streptomycin, Gentamicin, Netilmicin, Neomycin, Tobramycin, Amikacin from Kanamycin A)

Streptomyces (mycin) | Micromonospora (micin)

AMINOGLYCOSIDES

Adverse effects of aminoglycosides

Allergic reactions, Muscle relaxation, Incompatile with B lactams, Nephrotoxic (neomycin) Ototoxic (streptomycin), G cocci only

Common chemical characteristics of MACROLIDES

A large lactone ring, A ketone group, A glycosidically linked amino sugar

Alternative/DOC for Pen G allergy and Legionnaire’s disease

Erythromycin (Ilotycin) S. erythreus

Used with Omeprazole or Lansoprazole (H.pylori eradication), more potent for strep and staph

Clarithromycin

For nongonococcal urethritis (Chlamydia, LRTI, PID, pharyngitis, Legionnaire’s)

Azithromycin, OD

For typhoid fever (Ceftriaxone new DOC), meningococcal infections and H.influenza infections in cephalosporin allergic patients, anaerobic infections

CHLORAMPHENICOL (S. venezuelae)

For abdominal and female genitourinary tract infections caused by B. fragilis

LINCOSAMIDES (Clindamycin) Streptomyces lincolnensis

Esters (eg. stearate, estolate, and ethylsuccinate) have improved acid stability

Erythromycin (Ilotycin) S. erythreus

Adverse effects of Erythromycin (Ilotycin)

epigastric distress, cholestatic jaundice (estolate form of erythromycin)

40 to 68 hours half life is prolonged because of extensive tissue sequestration and binding (↑Vd)

Azithromycin, OD

Sulfur containing; Resemble sulfonamides in antibacterial spectrum and biochemical MOA

LINCOSAMIDES (Clindamycin) Streptomyces lincolnensis

Adverse effects of Lincosamides

Pseudomembranous colitis, rash

DOC for Pseudomembranous colitis, rash

Vancomycin

Bone marrow suppression

(dose related)

Aplastic anemia

(non dose related)

Gray Baby Syndrome

(neonates)

Used topically for impetigo, eczema, staphylococcal and beta hemolytic streptococcal infections

MUPIROCIN (Pseudomonas fluorescens)

topical treatment of burns

Nitrofurazone

DOC for E. Histolytica, G. Lambia, Trichomonas vaginalis

Metronidazole

Treatment of Chagas’ disease/American Sleeping sickness (Trypanosoma cruzi)

Nifurtimox

Vector: reduviid bug/kissing bug

Nifurtimox

diarrhea (SPEcKs;) CI: Alcohol

Furazolidone (PO)

Urinary antiseptic

Nitrofurantoin

Metallic taste, Disulfiram like effect

Metronidazole

DOC for leprosy (Test: G6PD)

Dapsone

Chloroquine resistant malaria

Quinine + pyrimethamine + sulfadoxime (Fansidar®)

DOC for Pneumocystis carinii

Bactrim; alternative drug: Pentamidine (aromatic diamide)

Burn therapy

Silver sulfadiazine and Mafenide (Flammazine®)

Conjunctivitis

Sodium sulfacetamide

Patterned after nalidixic acid (introduced for the treatment of UTI and URTI)

QUINOLONES

Mechanism of Action of MUPIROCIN (Pseudomonas fluorescens)

Inhibition of RNA and DNA synthesis

Mechanism of Action of MUPIROCIN (Pseudomonas fluorescens)

Inhibition of RNA and DNA synthesis

Mechanism of Action of QUINOLONES

Inhibits DNA gyrase (topoisomerase II)

Mechanism of Action of SULFONAMIDES

Compete with PABA for dihydropteroate synthetase---prevents synthesis of folic acid

adverse effects of QUINOLONES

Diarrhea, nausea, headache, dizziness, nephrotoxicity, phototoxicity

adverse effects of SULFONAMIDES

Crystalluria, Steven Johnson Syndrome, Kernicterus, Anemia

have enhanced antibacterial activity

Fluoroquinolones

most potent

Ciprofloxacin

anti pseudomonal

Norfloxacin

Chelates with metals

QUINOLONES

(essential for antibacterial activity)

1,4 dihydro 4 oxo 3 pyridinecarboxylic acid moiety

Sulfonamides are usually used with

dihydrofolate reductase inhibitors (e.g Trimethoprim)

studied a bright dye, Prontosil (metabolized in vivo to sulfanilamide active)

Gerard Domagk

Antibacterial Antibiotics Flashcards

(69 cards)