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Antimicrobial Drug Therapy
Schwark's Class
68
Veterinary Medicine
Professional
01/27/2016

Additional Veterinary Medicine Flashcards

 


 

Cards

Term
Antibacterial Drug
Definition
Drug active against bacteria
Term
Antimicrobial Drug
Definition
Drug active against bacteria and other microorganisms
Term
Antibiotic
Definition
Substance produced by a microorganism that inhibits or kills other microorganisms
Term
Bacteriostatic
Definition

Inhibits growth and replication of bacteria

 

-Not good for immunosuppressed patients

Term
Bactericidal
Definition
Kills bacteria
Term
Time-Dependent Drug
Definition
Drug must be kept abve the minimal inhibitory concentration (MIC) until the infection is cleared
Term
Concentration-Dependent Drug
Definition
The higher the concentration of the drug, the more effectively it kills microorganisms
Term
Four General Mechanisms of Antibacterial Drugs
Definition

1. Target the cell wall

2. Target the cell membrane

3. Target protein synthesis

4. Target nucleic acid

Term
β-Lactam Drugs: Penicillins and Cephalosporins
Definition

-Molecule contains β-lactam ring that interferes with peptidoglycan cross-linking during cell wall formation in bacteria; Safe for mammalian cells because they lack a cell wall

-Bactericidal: Cell wall is weakened and cell bursts

-Concentration-Dependent: Keep 2-4 times above MIC during treatment

-Most effective against actively growing bacteria

-Most effective against Gram + bacteria; Gram - bacteria have outer coat surrounding cell wall so drugs have harder time acting on cell wall synthesis; Ineffective against bacteria without a cell wall (Mycoplasma)

Term

Penicillin G

aka

Benzylpeniciliin

Definition

-β lactam drug

-Produced by fungus

-Combined with procaine local anesthetic or benzathine to delay absorption from IM or SQ injection site

-Combined with potassium (K) to stabilize; Can give IV

-Tubular secretion/renal excretion

Term
Ampicillin, Amoxicillin
Definition
Broad spectrum penicillins that have been structurally altered to allow them to penetrate the outer coat of Gram - bacteria so that they are effective against both Gram - and Gram + bacteria
Term
β-Lactamase
Definition

Enzyme produced by some bacteria that degrades the β lactam ring of β lactam drugs to prevent them from working against cell wall synthesis

 

 


Term
Mechanisms of β-Lactamase Resistance in Penicillins
Definition

1. Add a molecule to the drug that makes it bigger so β-lactamase can't reach the β-lactam ring to degrade it

 

2. Add a molecule to the drug that inhibits β-lactamase

Term
Clavamox
Definition
Combination of broad spectrum amoxicillin and the β lactamase inhibitor clavulonic acid
Term
Cephalosporin Drugs
Definition

Bactericidal β-lactam drugs that act on cell wall synthesis

 

Later generation drugs become more effective against

Gram - bacteria, but may lose some efficacy against Gram + bacteria compared to older generations 

 

Secreted from renal tubules → Reach high concentration in urinary tract so good for UTI

 

Good access to bone → Good for orthopedic surgery patients 

Term
Ceftiofur (Naxcel)
Definition

3rd generation cephalosporin drug

Effective against Gram - bacteria but slightly less effective against Gram + bacteria

Can be given IV, Sub-Q or IM

Term
Cefpodoxime (Simplicef)
Definition

3rd generation cephalosporin 

 

Given orally

Term
Ceftolozane + Tazobactam
Definition

Cephalosporin drug combined with β-lactamase inhibitor 

 

Very broad spectrum

Term
Cefovicin/Convenia
Definition
3rd generation cephalosporin with high plasma protein affinity so it stays in the body for ~10 days following injection
Term
Carbapenem Drugs
Definition

β lactam drugs taht aren't susceptible to β lactamase

 

Act on cell wall synthesis - Bactericidal

 

Broad Spectrum

Term
Bacitracin
Definition

Polypeptide drug that interferes with bacterial cell wall synthesis (bactericidal) but has no β lactam ring so β lactamase is ineffective against it

 

Nephrotoxic - Mostly used topically

 

Effective against Gram + bacteria

Term
Vancomycin
Definition

Glycopeptide drug that acts against cell wall synthesis (bactericidal)

 

Toxic

Term
Polymixins
Definition

Bactericidal drugs that target bacterial cell membranes (less selective toxicity)

 

Most effective against Gram - bacteria → Able to bind and neutralize endotoxin

 

Poor oral absorption

 

Renal excretion

Term
Neosporin/Polysporin/Triple Antibiotics
Definition

Combination of:

Polymixin B (for Gram - bacteria)

Bacitracin (for Gram + bacteria)

Neomycin

Term
Neopolydexamethasone
Definition
Polymixin combined with steroid
Term
Tetracyclines
Definition

Bacteriostatic protein synthesis inhibitors

 

High affinity for calcium and is inactivated when it binds calcium (more problematic with older tetracyclines)

 

Very broad spectrum: Gram -/Gram + bacteria and protozoa

 

Renal excretion

 

Anti-inflammatory effects

Term
Doxycycline
Definition

Bacteriostatic protein synthesis inhibitor

 

High lipid solubility

 

Renal and GI excretion so better for kidney patients than other tetracyclines

 

IV form should not be used in horses

Term
Oxytetracycline
Definition

Bacteriostatic protein synthesis inhibitor

 

Commonly used in large animal medicine

Term
Minocycline
Definition
Bacteriostatic protein synthesis inhibitor being studied for anti-arthritic effects
Term
Fenicols
Definition
Bacteriostatic protein synthesis inhibiting drugs
Term
Chloramphenicol
Definition

Bacteriostatic protein synthesis inhibitor

 

Very lipid soluble

Very broad spectrum - Good for anaerobes 

Eliminated via glucuronidation (can be toxic to cats)

Inhibits p450 enzymes (be careful if coadministering with drugs that are metabolized by p450)

Can cause irreversible aplastic anemia in primates - DO NOT USE IN FOOD PRODUCING ANIMALS

Term
Florfenicol
Definition

Bacteriostatic protein synthesis inhibitor

 

Very similar to chloramphenicol, but doesn't cause aplastic anemia in primates so approved for food animals

Term
Macrolides
Definition

Bacteriostatic protein synthesis inhibitors

 

Can cause severe, possibly fatal colitis in horses

 

Inhibit P450 enzymes so can interfere with metabolism of other drugs - Possible Toxicity

Term
Erythromycin
Definition

Older macrolide that targets Gram + bacteria

 

Binds motilin receptors in stomach/upper GI tract at subantibacterial doses - Can be used to treat gastric atony

Term
Tylosin, Tiamulin, Spiramycin
Definition
Older macrolides that target Gram + bacteria
Term
Azithromycin, Clarithyromycin, Tilmicosin
Definition

Newer macrolides that are broader spectrum against Gram + and Gram - bacteria

 

Good access to respiratory tissues

Term
Lincosamides
Definition

Bacteriostatic inhibitors or protein synthesis

 

Good for Gram + infections

 

Upsets GI flora in horses and causes potentially fatal colitis

Term
Lincomysin
Definition
Lincosamide that is good for skin infections
Term

Clindamycin

 

(AKA Antirobe)

Definition

Broader spectrum lincosamide that is good for Gram + bacteria, anaerobes, and some protozoa (Toxoplasma and Neospora)

 

Good prophylactic for dental patients

 

Doesn't eliminate protozoal infections so must be given long term (possibly for life)

Term
Pirlimycin
Definition
Lincosamide commonly used to treat mastitis
Term
Aminoglycosides
Definition

-Bactericidal protein synthesis inhibitors 

-Especially good against Gram - aerobes; Work against Gram + aerobes

-Ineffective against anaerobes - Anaerobes lack pump that allows drug to enter cell

-Water soluble - Not great tissue access

-No hepatic metabolism

-Nephrotoxic if they accumulate in proximal convoluted tubules during renal excretion (dose-dependent)

-Ototoxic (vestibular and hearing problems)

-High doses can cause weakness and paralysis

 

Term
Gentamicin
Definition

Aminoglycoside often found in ear medications

 

Good against pseudomonas

Term
Neomycin
Definition
Aminoglycoside in triple antibiotics like neopolydex
Term
Tobramycin
Definition
Aminoglycoside used in ophthalmology
Term
Metronidazole (Flagyl)
Definition

Bactericidal: Products of bacterial metabolism cause DNA strands to break 

(Because DNA breakage can potentially be mutagenic/teratogenic/oncogenic, these drugs can't be used in food animals)

Good for anaerobic infections (abscesses, periodontal disease) - Combined with other antimicrobials to increase aerobic spectrum

Effective against protozoa Giardia and Trichomonas so often used for diarrhea

Hepatic metabolism - Give lower dose with liver disease to prevent neurotoxicity

Term
Rifamycin
Definition

Bactericidal antibacterial drugs that inhibit RNA polymerase to prevent mRNA synthesis

Antimycobacterial - Used for tuberculosis

Useful for intracellular infections (Rhodococcus equi, Listeria)

Effective against Gram + but not Gram - bacteria

Never use alone to prevent resistance - Give with erythromycin, clarithromycin, etc.

Term
Rifampin
Definition
Rifamycin antimicrobial drug - Inhibits RNA polymerase
Term
Sulfonamides
Definition

Bacteriostatic inhibitors of nucleic acid synthesis Competitive inhibitors of PABA which prevents folic acid synthesis needed for nucleic acid synthesis

Broad spectrum - Most effective against Gram + bacteria

Also works against protozoa - Coccidia

Lipid soluble and great tissue access

Term
Potentiated Sulfonamides
Definition

Diaminopyrimidines are combined with sulfa drugs to create a sequential blockade of bacterial enzymes involved in folic acid synthesis resulting in bactericidal effects


Diaminopyrimidines: Trimethoprim, methoprim, ormetoprim, aditoprim, pyrimethamine


Term
Fluoroquinolones
Definition

Bactericidal: Inhibits DNA gyrase needed for breaking and mending DNA strands in bacteria

 

Broad spectrum - Most effective against Gram - aerobes

Newer drugs have increased efficacy against Gram +

 

Lipid soluble - Excellent tissue penetration

Term
Lufenuron (Program)
Definition
Anti-flea medication that inhibits chitin synthesis but can be used off-label for fungal infections since they have chitin their cell walls
Term
Caspofungin
Definition

Antifungal drug that inhibits β-glycogen synthesis in the fungal cell wall

 

Rarely used because it is so expensive

Term
Amphoterin B
Definition

IV antifungal drug that affects fungal cell membrane permeability by poking holes in ergosterol

 

Nephrotoxic

Term
Natamycin
Definition
Topical antifungal medication that alters fungal cell membrane permeability by poking holes in ergosterol
Term
Azoles
Definition

Antifungal drugs that inhibit ergosterol synthesis in fungal cell membranes

 

Requires long-term therapy because fungi grow so slowly

 

Newer azoles have better tissue penetration

 

Monitor liver enzymes while treating

Term
Ketoconazole
Definition

Azole drug that inhibits fungal membrane ergosterol synthesis

 

Requires acidic stomach pH for absorption so give with food to stimulate stomach acid

 

p450 enzyme inhibitors - Potential for drug toxicity 

Term
Griseofulvin
Definition

Antifungal drug that binds to spindle microtubules and causes mitotic arrest in metaphase

 

Used for ringworm treatment

 

Teratogenic - Stops mitosis in fetus

 

Anemia - Slows RBC turnover/mitosis of progenitors 

Term
Flucytosine
Definition

Antifungal drug that is incorporated into nucleic acid and affects fungal protein synthesis

 

Enters fungal cells through the cytosine pump

Term
Fenbendazole
Definition
Benzimidazole drug that inhibits anaerobic metabolism in Giardia
Term
Ponazuril (Marquis)
Definition

Oral paste that interferes with protozoal intermediary metabolism

 

Used to treat Equine Protozoal Myeloencephalitis (Sarcocystis neurona)



Used to treat coccidiosis in dogs

Term
Amprolium
Definition

Competes with thiamine uptake in protozoa and inhibits energy metabolism

 

Used against Coccidia - More effective prophylactically 

 

Give with thiamine to avoid thiamine deficiency/neurotoxicity in patient

Term
Monensin
Definition

Antiprotozoal ionophore antibiotic used against coccidia

 

Forms complexes with Na+ or K+ ions, and the complexes block K+ transport into mitochondria which inhibits substrate oxidation and ATP metabolism in the mitochondria

 

Cardiac toxicity in horses

Term
Nitrazoxanide (Navigator)
Definition

Interferes with electron transfer in aerobic metabolism of protozoa

 

Used to treat Cryptosporidium infections in immunocompromised people in which normal symptomatic therapy (fluids) isn't enough

Term
Melarsomine (Immiticide)
Definition

Organic arsenical used to treat heartworm infections

 

Arsenic disrupts adult worm metabolism and causes slow death

 

Injected IM

 

Doxycycline is given with it to elimate Wolbachia

Term
Ivermectin (Heartgard)
Definition

Heartworm preventive given orally once a month

 

Active against heartworm larvae

 

Heartgard Plus includes pyrantel for increased spectrum

Term
Milbemycin (Interceptor)
Definition

Heartworm preventive active against larvae

 

Also affects intestinal worms

Term
Selamectin (Revolution)
Definition
Broad spectrum heart worm preventive that also has anthelmintic and insecticide activity
Term
Moxidectin (Proheart)
Definition
Heartworm preventive plus intestinal worms
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