Pharmacology Flashcards
Amoxicillin and Clavulanic Acid dose rate
125mg/kg PO q8-12h (up to 250mg/kg)
60-120mg/kg IM q12h
Amoxicillin and Clavulanic Acid PK
Bactericidal (time-dependent)
Amoxicilin: Binds to penicillin-binding proteins involved in bacterial cell wall synthesis, thereby decreasing cell wall strength and rigidity - affecting cell division/growth
Aminopenicillin with B-lactamase inhibitor that expands its spectrum
G+ bacteria especially Staphylococcus
Anaerobic bacteria
Most G- resistant
Not susceptible to inactivation by B-lactamase-producing bacteria strains because clavulanic acid inhibits B-lactamase (bacterial enzyme that inactivates many penicillins)
Amoxicillin and Clavulanic Acid Contraindications and ADR
Contraindicated with allopurinol use Most side-effects are GIT related. Hypersensitivities are other side effects are rarely reported: Anorexia Vomiting (if used orally in raptors) Diarhhoea Potential disturbance to normal flora
Azithromycin dose rate
10-40mg/kg PO q24h (use for 45 days for chlamydia)
For mycobacteria: 60mg/kg PO q24h for 3 days the off for 2 days - repeat up to 3 wks
Azithromycin PK
New generation macrolide
Azithromycin has a longer tissue half-life than erythromycin, shows better oral absorption
G+ (Staph, Strep)
Limited G – (Bordetella, Haemophilus)
Mycoplasma
Appears to be active against intracellular infections including Chlamydia, Toxoplasma, Plasmodium and Cryptosporidium
Azithromycin Contraindications and ADR
Excreted in bile thus caution in patients with impaired hepatic function
Enhanced with alkaline pH - administer on empty stomach if possible
should probably be avoided in patients with hepatopathy
Avoid in renal and hepatic failure in all species
GI irritation, V+
Injectables available but seldom used due to irritation and necrosis at site of injection
Erythromycin dose
10-20mg/kg PO Q12h
Erythromycin PK
Macrolide - inhibits peptide bond formation
Usually bacteriostatic, but may be bactericidal in high conc. (time-dependent) or against highly susceptible organisms
Active against Psittacosis in people, but not effective at dose levels in birds
G+ :Staph, Strep, Bacillus, Clostridium
Limited G- : Pasteurella, Haemophilus, most strains of Enterobacteriaceae (Pseudomonas, E.coli, Klebsiella etc.) are resistant
Good against anaerobes
Some Mycoplasma
Some Chlamydia
Some Rickettsia
Erythromycin ADR
Primarily excreted unchanged in bile, but also partly metabolized
Being a lipophilic weak base, it is concentrated in fluids that are more acidic than plasma, including milk, prostatic fluid and intracellular fluid.
should probably be avoided in patients with hepatopathy
Erythromycin should not be used in combination with other macrolide, lincosamide or chloramphenicol antimicrobials as antagonism may occur.
ADR: GI irritation, V+
Injectables available but seldom used due to irritation and necrosis at site of injection
Tylosin dose
15-30mg/kg IM q12h
50mg/kg PO q 24h – pigeons, passerines
250-1000mg/L of water
nebulization of 100 mg diluted in 5 ml DMSO and 10 ml saline
Tylosin PK
Bacteriostatic
Same mechanism of action as erythromycin
Predominantly in suspected Mycoplasma infections - good activity against mycoplasmas and has the same antibacterial spectrum of activity as erythromycin but is generally less active against bacteria.
Tylosin metbolism and ADR
Eliminated in urine and bile
IM injections can be very irritating and cause tissue necrosis
GI disturbances. The activity of tylosin is enhanced in an alkaline pH.
Gentamicin dose rate
2.5-10mg/kg IM q12h or topically
Gentamicin PK
Aminoglycoside - Bactericidal (concentration-dependent so marked post-antibiotic effect - allowing prolonged dosing intervals). Effective against many G+ (i.e. Staph) and G-
Primarily G- aerobes
- Resistance seen with Pseudomonas aeruginosa and Klebsiella
Usually reserved for serious infections
- Osteomyelitis
Mentioned use as nebulization for treatment of URT infections (sinuses, trachea, lungs)
Gentamicin ADR
More toxic than amikacin
Generally not recommended due to narrow margin of safety. Short-term treatment because of dose-related toxic effects:
- nephrotoxic (tubular necrosis) in dehydrated birds and birds with compromised renal function – dose should be reduced or a less toxic drug selected. Usually reversible if use of drug is stopped. Uric acid may be abnormal up to 7 days after cessation. Recommend concurrent fluid therapy
- ototoxic - usually irreversible
- neuromuscular synaptic dysfunction and paralysis if given IV rapidly
- May cause myositis with IM injection
Amikacin dose rate
10-20mg/kg IM q8-12h
Amikacin PK
Bactericidal (concentration-dependent so marked post-antibiotic effect - allowing prolonged dosing intervals)
Good activity against a variety of bacteria, predominantly G- aerobic bacteria
- G+ aerobes: Staphylococcus aureus (Streptococcus usually resistant)
- G-: E.coli, Klebsiella, Salmonella, Proteus, Pseudomonas, Enterobacter
- Mycoplasma spp.
- greater activity against G- bacteria, including some resistant to gentamicin and tobramycin i.e. several strains of Pseudomonas aeruginosa
- ineffective against anaerobic bacteria and in proteinaceous environments ( abscesses and exudates)
Osteomyelitis
Reaching CNS/ocular fluids limited, activity at low oxygen sites limited
PMMA bead formulation (1:14 ratio)
Elimination after parenteral admin occurs almost entirely by glomerular filtration
Less toxic side effects so is the Aminoglycoside of choice for use in birds
Not absorbed from GIT, must be administered parenterally
Aminoglycoside (amikacin, gentamicn, neomycin) contraindications
- renal disease
- age
- sepsis
- dehydration
- concurrent use of other potentially nephrotoxic drugs (i.e. NSAIDs)
- concurrent use with furosemide
Neomycin dose rate
10mg/kg PO q8-12h
Neomycin PK
Aminoglycoside
Significantly less effective against several species of G- (Klebsiella, Pseudomonas) - most of these strains are still susceptible to amikacin
Generally limited to oral tx of enteral infections due to being more nephrotoxic and less effective
than gentamicin or amikacin.
Orally administered neomycin is nearly all excreted unchanged in faeces
neomycin ADR
contraindicated in GIT obstructions. - parenteral use can be very toxic (nephrotoxic), so not recommended
- chronic use can lead to GI superinfections
- possible ototoxicity
- GI signs (D+, malabsorption)
Cefalexin dose rate
50-100mg/kg IM or PO q6-12h
Cafalexin PK
1st gen cephalosporin
Bactericidal - time-dependent
Excellent coverage against most G+ including B-lactamase bacteria (i.e. Staphs of GIT and skin)
Variable to poor against most G- (some strains of E.coli, Klebsiella, Actinobacillus, Salmonella)
Most anaerobes (except Bacteroides)
Cefalexin ADR
most are GI in nature (can alter gut flora)
potentially cause hypersensitivity reactions
Ceftazidime dose rate
50-100mg/kg IM q6-8h
Ceftazidime PK
3rd gen cephalosporin - Bactericidal - Time-dependent Variable activity against G+ Much expanded (compared to 2nd gen) G- activity For serious G- infections Pseudomonas (but resistance is an issue) Penetrates CSF and bone Not appreciable absorbed after PO
Ceftazidime ADR
Use with caution in renal disease and may need to reduce dose (primarily excreted in the kidneys). GI disturbance
Pain may be associated with injection
Tetracycline PK
Bacteriostatic: inhibiting protein synthesis at the initiation step by interacting with the 30S ribosomal unit
Chlortetracycline dose rate
15-100mg/kg PO q6-8h
2500mg/L drinking water for finch/pigeon (N/B: Assume birds consume 10% of their body weight in water per day)
Parrots - 5.0 g/L in clean water.
Nil WHP Laying hens
Chlortetracycline PK
Primarily used in water or feed treatments; or topically for ophthalmic use
Many bacteria now resistant
Poor acceptance
Immunosuppressive
Can be used for flock treatment of Chlamydiosis but doxycycline preferred
- therapeutic blood levels are reached only within 10 days – infected birds will continue to shed, and the delayed induction of proper blood levels poses additional risk for humans and other birds
Primarily hepatic metabolism and renal excretion - care in birds with hepatopathy and renal compromise
Doxycycline dose rate
Oral: 25-50mg/kg PO q24hr
In-water: 4g/400ml (parrots); 4g/800ml (pigeons)
Injectable: 50-100mg/kg IM once weekly x7
Doxycycline PK
- Many G+ (some Staphs and Streps but resistance increasing), Clostridia, Norcardia
- Poor efficacy against most avian G- isolates
- Chlamydia
- Mycoplasma
- Rickettsia
- Spirochetes (Helicobacter, Campylobacter)
Empirically set for 45 days
A/B cannot penetrate macrophage, thus cannot reach C.psittaci. During the 45 days, at least 2 complete replicate cycles of avian macrophage takes place. During division phase, the organism should be released from the cell and if the plasma conc. of A/B is sufficiently high to inhibit C.psittaci, the organism will be eliminated
Greater bioavailability than other tetracyclines = will penetrate CSF and the eye but may not be sufficient to treat infections