AMOXICILLIN
AMOXICILLIN
Chemistry - An aminopenicillin,
amoxicillin is commercially available as the trihydrate. It occurs as a
practically odorless, white, crystalline powder that is sparingly soluble in
water. Amoxicillin differs structurally from ampicillin only by having an
additional hydroxyl group on the phenyl ring.
Amoxicillin may also be
known as amoxycillin, p-hydroxyampicillin, or BRL
2333.
Storage/Stability/Compatibility - Amoxicillin capsules,
tablets, and powder for oral suspension should be stored at room temperature
(15-30¡C) in tight containers. After reconstitution, the oral suspension should
preferably be refrigerated (refrigeration not absolutely necessary) and any
unused product discarded after 14 days. After reconstitution, the injectable
veterinary suspension is stable for 3 months at room temperature and 12 months
when refrigerated.
Pharmacology/Uses/Indications - Although there may be
some slight differences in activity against certain organisms, amoxicillin
generally shares the same spectrum of activity and uses as ampicillin. Because
it is better absorbed orally (in non-ruminants), higher serum levels may be attained
than with ampicillin. Refer to the ampicillin monograph or the general
penicillin statement for more information.
Pharmacokinetics
(specific) -
Amoxicillin trihydrate is relatively stable in the presence of gastric acid.
After oral administration, it is about 74-92% absorbed in humans and animals
(monogastric). Food will decrease the rate, but not the extent of oral
absorption and many clinicians suggest giving the
drug with food, particularly if there is concomitant associated GI distress.
Amoxicillin serum levels will generally be 1.5-3 times greater than those of
ampicillin after equivalent oral doses. After absorption the volume of
distribution for amoxicillin is approximately 0.3 L/kg in humans and 0.2 L/kg
in dogs. The drug is widely distributed to many tissues, including liver,
lungs, prostate (human), muscle, bile, and ascitic, pleural and synovial
fluids. Amoxicillin will cross into the CSF when meninges are inflamed in
concentrations that may range from 10-60% of those found in serum. Very low
levels of the drug are found in the aqueous humor, and low levels found in
tears, sweat and saliva. Amoxicillin crosses the placenta, but it is thought to
be relatively safe to use during pregnancy. It is approximately 17-20% bound to
human plasma proteins, primarily albumin. Protein binding in dogs is
approximately 13%. Milk levels of amoxicillin are considered to be low. Amoxicillin
is eliminated primarily through renal mechanisms, principally by tubular
secretion, but some of the drug is metabolized by hydrolysis to penicilloic
acids (inactive) and then excreted in the urine. Elimination half-lives of
amoxicillin have been reported as 45-90 minutes in dogs and cats, and 90
minutes in cattle. Clearance is reportedly 1.9 ml/kg/min in dogs.
Doses
Dogs:
For susceptible infections:
a) 10 - 22 mg/kg PO or SubQ
q8h
b) Trihydrate injectable:
5.5 - 11 mg/kg IM or SQ q8h
Oral Forms: 11 - 22 mg/kg
PO q8-12h
c) For routine infections:
10 mg/kg PO, SQ bid
For chlolangiohepatitis: 20
mg/kg PO, SQ bid
d) 22 mg/kg PO q12h
e) 10 - 55 mg/kg q6-12h PO;
5 - 11 mg/kg IV, IM, or SQ q6-12h
f) For Lyme Disease: 22
mg/kg PO q12h for 21-28 days
Cats:
For susceptible infections:
a) 10 - 22 mg/kg PO or SubQ
q8h
b) Trihydrate injectable: 5.5
- 11 mg/kg IM or SQ q8h
Oral Forms: 11 - 22 mg/kg
PO q8-12h
c) 11 - 22 mg/kg PO q8-12h
d) For bacterial
respiratory infections: 10 mg/kg PO or parenterally q12-24h
e) 22 mg/kg PO q12h
Cattle:
For susceptible infections:
a) 6 -10 mg/kg SQ or IM
q24h (Withdrawal time = 30 days)
b) For respiratory
infections: 11 mg/kg IM or SQ q12h.
c) For respiratory
infections: 11 mg/kg IM or SQ q12h
d) Calves: Amoxicillin
trihydrate: 7 mg/kg PO q8-12h
e) 13.2 - 15.4 mg/kg IM or
SQ once daily
Horses:
For susceptible infections:
a) For respiratory
infections: 20 - 30 mg/kg PO q6h
b) Amoxicillin trihydrate:
20 mg/kg q12h IM.
Birds:
For susceptible infections:
a)
For most species: 150 - 175 mg/kg PO once to twice daily (using 50 mg/ml
suspension)
b) 100 mg/kg q8h PO
c) 100mg/kg q8h, IM, SubQ,
PO
Reptiles:
For susceptible infections:
a)
For all species: 22 mg/kg PO q12-24h; not very useful unless used in
combination with aminoglycosides.
Client Information - The oral suspension
should preferably be refrigerated, but refrigeration is not absolutely
necessary; any unused oral suspension should be discarded after 14 days. Amoxicillin
may be administered orally without regard to feeding status. If the animal
develops gastrointestinal symptoms (e.g., vomiting,
anorexia), giving with food may be of benefit.
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