Antimicrobial use in lung infection

Question 1

Ways to classify antimicrobial compounds…

Answer 1

CHEMICAL STRUCTURE

ORIGIN (natural/synthetic/semisynthetic)

TARGET MICROORGANISMS (viral, bacterial, fungal, protozoa)

MODE OF ACTION (DNA replication, RNA/protein/cell wall synthesis, plasma membrane, antimetabolites from metabolic pathways)

ANTIMICROBIAL ACTIVITY (bacteriostatic, bactericidal)

SPECTRUM OF ACTIVITY (broad, narrow)

Question 2

TETRACYCLINES
Classification?
Site of action?
Mechanism of action?
Spectrum?
Uses?
Side Effects?
Routes?
Pharmacokinetics?

Answer 2

Classification: BACTERIOSTATIC ANTIMICROBIAL
Site of action: BACTERIAL RIBOSOME
Mechanism of action: INHIBIT BACTERIAL PROTEIN SYNTHESIS
Spectrum: BROAD
Uses: LOW COST; FOR MIXED BACTERIAL INFECTIONS; CATTLE (RESPIRATORY INFECTIONS/PNEUMONIA/ANAPLASMOSIS/INFECTIOUS KERATOCONJUNCTIVITUS/UDDER INFECTION); SHEEP (Q FEVER/ENZOOTIC ABORTION/PNEUMONIA/FOOT ROT); PIGS (ATROPHIC RHINITIS/LOW RESPIRATORY DISEASE/ERADICATE LEPTOSPIRA); HORSES (LIMITED SPECTRUM); CATS AND DOGS (UTI/OTITIS EXTERNA/CHLAMYDIAL INFECTIONS - UPPER RESP TRACT AND CONJUNCTIVA); POULTRY (ENTERIC/RESPIRATORY INFECTION)
Side Effects: MAY BIND TO MAMMALIAN RIBOSOMES; BROAD SPECTRUM SUPPRESSION OF INTESTINAL FLORA; RENAL TUBULAR DAMAGE; IRRITANT; OCCASIONAL ANAPHYLAZIS; PHTOSENSITIVITY
Routes: IM, IV, FEED (CHICKENS)
Pharmacokinetics: SHORT ACTING; LOW ORAL ABSORPTION; ENTERS MOST TISSUES AND BODY FLUIDS; CAN CROSS PLACENTA
Example:

Question 3

MACROLIDES
Classification?
Site of action?
Mechanism of action?
Spectrum?
Uses?
Side Effects?
Routes?
Pharmacokinetics?
Examples?

Answer 3

Classification: BACTERIOSTATIC ANTIMICROBIAL; BASED ON SIZE OF MACROCYCLIC LACTONE RING
Site of action: MICROORGANISM RIBOSOME
Mechanism of action: INHIBIT PROTEIN SYNTHESIS AT TRANSLOCATION STEP
Spectrum: MODERATE - GRAM (+)(-) BACTERIA; MYCOPLASMAS, AND SOME RICKETTSIAE
Uses: ONE OF THE SAFEST ANTIMICROBIAL DRUGS; DOGS AND CATS; PIGS, HORSES; GOATS; HUMANS; CHICKENS
Side Effects: DECREASE MUCUS PRODUCTION; MAY ENHANCE HOST’S IMMUNOMODULATORY RESPONSE; ANTI-INFLAMMATORY ACTIONS; GI DISTURBANCE; THROMBOPHLEBITIS; PERIPHLEBITIS; SEVERE PAIN
Routes: ORAL, IV, IM, SC, INTRAMAMMARY
Pharmacokinetics: WEAK BASE; HIGH LIPID SOLUBILITY; BROAD DISTRIBUTION IN TISSUES; CONCENTRATED IN PHAGOCYTES; PARTLY METABOLIZED BY LIVER; EXCRETED IN BILE
Examples: ERYTHROMYCIN (CAMPYLOBACTER JEJUNI AND MYCOPLASMA) (MICOTIL, PULMOTIL, TYLAN 200); TILMICOSIN; TYLOSIN; SPIRAMYCIN (PERIDONTAL INFECTION IN DOGS AND CATS) (STROMORGYL) (DYSENTRY AND PNEUMONIA IN PIGS/CALVES/POULTRY); TULATHROMYCIN (BOVINE AND PIG RESPIRATORY DISEASE)

Question 4

AMINOGLYCOSIDES
Classification?
Site of action?
Mechanism of action?
Spectrum?
Side Effects?
Routes?
Pharmacokinetics?
Examples?

Answer 4

Classification: BACTERICIDAL ANTIMICROBIAL
Site of action: MICROORGANISM RIBOSOME
Mechanism of action: MISMATCHES CODON AND ANTICODONS FOR PROTEIN SYNTHESIS
Spectrum: NARROW
Side Effects: OTOTOXICITY - DAMAGE TO VESTIBULAR APPARATUS CELLS AND COCHLEA SENSORY CELLS; ATAXIA; VERTIGO; NYSTAGMUS; NEPHROTOXICITY - GENERALLY AFTER PROLONGED THERAPY; NEUROMUSCULAR PARALYSIS
Routes: IM, SC
Pharmacokinetics: HIGHLY POLAR; LOW LIPID SOLUBILITY; POOR GI TRACT ABSORPTION; LOW DISTRIBUTION; THERAPEUTIC CONCENTRATIONS IN JOINTS AND PLEURAL/PERICARDIAL FLUIDS; NO METABOLISM; EXCRETED UNCHANGED BY KIDNETS
Examples: STREPTOMYCIN; NEOMYCIN; KANAMYCIN; GENTAMYCIN

Question 5

FLUOROQUINOLONES
Classification?
Site of action?
Mechanism of action?
Spectrum?
Uses?
Side Effects?
Routes?
Pharmacokinetics?
Examples?

Answer 5

Classification: BACTERICIDAL ANTIMICROBIAL
Site of action: BACTERIAL CELL NUCLEUS
Mechanism of action: INHIBIT DNA REPLICATION BY BINDING TO NUCLEAR ENZYMES
Spectrum: BROAD - GRAM (-), GRAM (+), INTRACELLULAR BACTERIA (CHLAMYDIA, LEGIONELLA, BRUCELLA SPP.); MYCOPLASMA
Uses: DOGS AND CATS - UTI WITH PSEUDOMONAS AERUGINOSA; PROSTATE INFECTION IN DOGS; SKIN/SOFT TISSUE/WOUND INFECTION; SERIOUS G-NEGATIVE SYSTEMIC INFECTION; SERIOUS RESPIRATORY INFECTIONS; OSTEOMYELITIS CAUSED BY G-NEGATIVE AEROBES… SMALL MAMMALS - SKIN AND VISCERAL INFECTION… BIRDS… LARGE MAMMALS - BRD… PIGS
Side Effects: CONSIDERED RELATIVELY SAFE; EROSION OF WEIGHT-BEARING CARTILAGE; CNS PROBLEMS MAY OCCUR; OCULAR PROBLEMS IN CATS (ENROFLOXACIN)
Routes: IM, SC
Pharmacokinetics: HIGH ORAL AVAILABILITY; RAPID ABSORPTION; LOW PROTEIN BINDING; EXTENSIVE TISSUE DISTRIBUTION; LIVER/LUNGS/KIDNEY/URINARY TRACT/PROSTATE/BONE/SKIN/BILE/BRONCHIAL SECRETIONS/FLUIDS; EXCRETED IN KIDNEYS AND BILE OR MILK OF LACTATING ANIMALS
Examples: ENROFLOXACIN (BAYTRIL) - BIRDS AND REPTILES; DANOFLOXACIN (ADVOCIN); MARBOFLOXACIN (MARBOCYL, AURIZON) - KILL PASTEURELLA IN DOGS/CATS/CATTLE/PIGS; ORBIFLOXACIN (PROSATEX EAR DROPS); PRADOFLOXACIN (VERAFLOX)