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Absorption
A) Bioavailability
1) Oral, fasting state: 50%
a) No significant bioavailability differences between products has been
reported .
B) Effects of Food
Distribution sites
5) Placenta: crosses
Distribution Kinetics
1)Ampicillin volume of distribution.
19.5 to 27 L
In 9 patients with cirrhosis, the Vd was increased .
Vd in newborns is approximately 0.82 L/kg .
Vd in pregnancy is approximately 177 mL/kg .
2) Ampicillin Sodium
a) Volume of Distribution
19.5 to 27 L
Excretion
Kidney
Ampicillin
Renal Clearance (rate)
280 mL/min
Renal Excretion (%)
34% to 64%
Following oral administration; approximately 40% is excreted
unchanged in the urine .
About 34% to 64% of a single oral dose is eliminated in the urine
during the 6 or 8 hours, respectively, after administration.
Ampicillin Sodium
Renal Clearance (rate)
-280 mL/min
Renal Excretion (%)
-79% to 92%, following a parental dose , 79-92% remain unchanged.
Bile
1) Ampicillin
Concurrent probenecid administration can increase biliary excretion
to about 0.2%
2) Ampicillin Sodium
Ampicillin is excreted in bile, concentrations of the active form are
higher in bile than those in the serum
Concurrent probenecid administration can increase biliary excretion
to about 0.2%
A) Parent compound
Ampicillin and Ampicillin Sodium- 1 to 1.9 hrs (normal patients ), 4 to
5 hrs in renal failure , 15 to 20 hours in oliguria, 2 to 4 hrs in new
born , up to 6hrs in premature infant, and 1.6 hours in pregnancy
Amoxicillin- Pharmacokinetics
Absorption-
T max, oral: 1 to 2 hours ( immediate release ) , 3.1 hours extended
release
Bioavailability, amoxicillin absorption may be greater and less
variable with ampicillin.
Absorption is dose dependent at doses greater than 1000mg,
approximately 2g of amoxicillin is the maximum amount that can be
absorbed after a single dose.
As the dose of amoxicillin increases the percent of drug absorbed
decreases.
Effects of food- Immediate- release: no effect when administered at the start
of a light meal
Extended- release: rate of absorption is decreased, extent
is not affected
Amoxicillin is stable in the presence of gastric acid, however the effect
of food on absorption has only been studies when amoxicillin 400 and
875mg formulations were administered at the start of the light meal
Ingestion of amoxicillin with food produces levels within the
therapeutic range
Administration of extended release amoxicillin with food resulted in a
decreased rate of absorption as evidenced by a lower Cmax and longer
Tmax compared with immediate release of oral suspension, but the
extent of absorption was similar as evidenced by comparable AUCs.
Extracorporeal elimination
Hemodialysis- dialyzable
Amoxicillin can be removed from circulation by hemodialysis
Dialysis reduces amoxicillin half-life to 2.2 to 4.5 hours