Term
| Inhibitors of Ribosomal 30 S subunit |
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Definition
1) Aminoglycosides
2) Tetracyclines |
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Term
| Inhibitors of Ribosomal 50S subunit |
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Definition
i.Macrolides
ii.Lincosamides
iii.Phenicols |
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Term
| Aminoglycoside Drugs to know |
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Definition
i. Streptomycin
ii. Spectinomycin
iii.Neomycin
iv.Gentamicin
v.Amikacin |
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Term
| Aminoglycoside mechanism of action |
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Definition
i. Bacteria penetration = oxygen dependent
ii.Inhibition of protein synthesis |
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Term
| Aminoglycoside Spectrum of Activity |
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Definition
i.Bactericidal
ii.Concentration-dependent
iii.Post-antibiotic effect (PAE)
iv.Mainly Gram –
v.Only in aerobic conditions
vi.Less so against Gram + |
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Term
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Definition
i. Absorption
--Poorly absorbed orally
--Parenteral Use
ii. Distribution
--Mainly extracellular
--Good penetration in fluids, poor in deep tissues (except in renal and ear cells) but increased by inflammation.
iv.Elimination -Renal |
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Term
| Aminoglycosides pharmaceutical considerations |
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Definition
CANNOT be mixed in a syringe with penicillin.
Synergy and additive effect with any wall or membrane disruptor.
Antagonize all other protein synthesis inhibitor; Nitrofurans.
Also --> neutralized by acids; decreased activity in presence of divalent cations |
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Term
| Aminoglycides Adverse Effects |
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Definition
ONE OF THE MOST TOXIC ANTIBACTERIAL DRUGS.
--ototoxic; nephrotoxic
--chance of toxicity increased with use longer than 7-10 days SID; concurrent nephrotoxic drugs; not good renal function. |
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Term
| Clinical Use of Aminoglycosides |
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Definition
| High tissue residue; AVMA voluntarily adopted resolution not to use extra label in Vet Med |
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Definition
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Definition
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Definition
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Definition
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Definition
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Term
| Tetracyclines of Significance |
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Definition
i.Tetracycline
ii.Oxytetracycline
iii.Chlortetracycline
iv. Doxycycline |
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Definition
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Definition
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Term
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Definition
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Term
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Definition
Tetracyclines
Only one eliminated 100% by liver! |
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Term
| Tetracyclines Mechanism of Action |
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Definition
| Inhibition of protein synthesis |
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Term
| Tetracyclines Spectrum of Activity |
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Definition
i. Bacteriostatic
ii. Time-dependent
iii. Very Broad Spectrum! Go after all four quadrants and Protozoans!
iV. Extra and Intracellular bacteria including Mycoplasma! |
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Term
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Definition
- Absorption: Orally, Decreased by food, Decreased by anything containing Ca, Mg, Al, Fe (!!milk!!), Use orally on fasted animals. Can give as an injection to a suckling animal
-Distribution: extra- and intracellular, Enter most deep tissue (fair CNS without inflammation)
--Elimination: Mixed liver and renal elimination
Exception = Doxycycline = 100% in the liver! |
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Term
| Tetracyclines Adverse Reactions |
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Definition
i. Relatively safe drugs
ii. Major issues are Resistance and Residues
iii. Irritants
--GI upsets; inflammation at injection site
--Alteration of GI flora (!!risk of enterocolitis or superinfection in horses) Horses will collapse and die if given rapid IV |
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Term
| Macrolides: Drugs to know |
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Definition
i.Erythromycin
ii.Spiramycin
iii.Tulathromycin
iv.Tylosin
v.Tilmicosin |
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Term
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Definition
Macrolides
known for GI prokinetic agents activity |
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Definition
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Definition
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Definition
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Term
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Definition
Macrolides
--can cause caridotoxicity. |
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Term
| Macrolides Mechanisms of Action |
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Definition
| Inhibition of protein synthesis 50S |
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Term
| Macrolides Spectrum of Activity |
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Definition
i.Bacteriostatic
ii. Time-dependent
iii.Inactivated by acid environment
iv.Mainly aerobic Gram +
v. Extra- and intracellular bacteria
**Including Mycoplasm**
vi. Anaerobes are resistant |
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Term
| Macrolides Pharmacokinetics (PK) |
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Definition
i.Absorption: Unstable in acidic environment (stomach; pus)
ii. Distribution
1. Extra and Intracellular
2.Enter most deep tissues (exception: CNS, unless inflammation)
iii.Metabolism: Liver metabolism (inactivation by CYP450)--CYP450 inhibitors themselves
iv.Elimination: Mostly Liver elimination |
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Term
Macrolides Pharmaceutical Considerations:
Combinations |
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Definition
Antagonisms: All other ribosome inhibitors. CYP450 inhibition.
--KEEP IN MIND RESISTANCE.can cause resistance of 2 other classes of antibiotics as well! |
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Term
| Macrolides Adverse Reactions |
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Definition
| fairly safe; take care in herbivores |
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Term
| Lincosamides Drugs to know: |
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Definition
- Lincomycin
- Clindamycin
- Pirlimycin |
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Term
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Definition
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Definition
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Definition
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Term
| Lincosamides mechanism of action |
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Definition
| Inhibition of protein synthesis 50S |
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Term
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Definition
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Term
| Lincosamides Spectrum of Activity |
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Definition
1) bacteriostatic
2)time-dependent
3) Mainly Gram + oligate anaerobes
4) Extra and Intracellular |
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Term
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Definition
Absorption:orally (not good with food)
Distribution: extra and introcellular; enter deep tissue except CNS unless inflamed.
Metabolism: Liver affected by P450 disruptors
Elimination: liver elimination |
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Term
| Lincosamides Combinations |
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Definition
Antagonisms: with all other ribosome inhibitors
Resistance: be careful! will cause resistance to 2 other classes as well |
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Term
| Lincosamides Adverse Reactions |
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Definition
| Safe for the most part; GI upset and can cause superinfection; should be avoided in herbivores |
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Term
| Lincosamides Clinical Use |
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Definition
Considered the "penicillin alternative"
--difference is can reach deep tissue |
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Term
| Phenicols: Drugs of Significance |
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Definition
i. Chloramphenicol
ii.Florfenicol |
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Term
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Definition
Phenicols
**Bone Marrow Toxicity; cats most sensite. not an issue if treated less then 10 days
**Banned from Food Animal |
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Term
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Definition
Phenicols
**Food Animal Safe; safe if only use 2 injections; should not be used in horses. |
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Term
| Phenicols Mechanism of Action |
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Definition
Inhibition of protein synthesis
50S |
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Term
| Phenicols Spectrum of Activity |
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Definition
i.Gram + and Gram –
ii.Most obligate anaerobes (even Gram -)
iii.Extra and intracellular bacteria |
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Term
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Definition
-Absorption: Oral
-DistributionExtra and intracellular distribution
-Enter most deep tissues (even CNS!)
-Mainly liver elimination
- Liver metabolism
- Inhibitor of hepatic drug metabolism |
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Term
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Definition
| Antagonism with all other ribosome inhibitors. Inhibits liver drug metabolism. |
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Term
| Phenicol Adverse Reactions |
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Definition
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