Pipracil
PIPRACIL- piperacillin sodium injection, powder, lyophilized, for solution
Wyeth Pharmaceuticals, Inc.
Rx only
To reduce the development of drug-resistant bacteria and maintain the effectiveness of PIPRACIL and other antibacterial drugs, PIPRACIL should only be used to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
DESCRIPTION
PIPRACIL, sterile piperacillin sodium, is a semisynthetic broad-spectrum penicillin for parenteral use derived from D(-)-α-aminobenzylpenicillin. The chemical name of piperacillin sodium is sodium (2S ,5R ,6R)-6-[(R)-2-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-2-phenylacetamido]-3,-3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate. The chemical formula is C23 H26 N5 NaO7 S, and the molecular weight is 539.54. Its structural formula is:
Piperacillin sodium powder is a white to off-white solid having the characteristic appearance of products prepared by freeze-drying. It is freely soluble in water and in alcohol. The pH of an aqueous solution containing 400 milligrams per milliliter ranges from 5.5 to 7.5. One g contains 1.85 mEq (42.5 mg) of sodium (Na+).
CLINICAL PHARMACOLOGY
Intravenous Administration:
In healthy adult volunteers, mean serum piperacillin concentrations immediately after a two‑to three‑minute intravenous injection of 2, 4, or 6 g were 305, 412, and 775 μg/mL, respectively. Serum concentrations lack dose proportionality.
PIPERACILLIN SERUM CONCENTRATIONS IN ADULTS (μ g/mL) AFTER A TWO- TO THREE-MINUTE I.V. INJECTION | ||||||||||||
DOSE | 0 | 10 min | 20 min | 30 min | 1 h | 1.5 h | 2 h | 3 h | 4 h | 6 h | 8 h | |
2 | 305 (159-615) | 202(164-225) | 156 (52-165) | 67 (41-88) | 40 (25-57) | 24 (18-31) | 20 (14-24) | 8 (3-11) | 3 (2-4) | 2 (≤0.6-3) | — | |
4 | 412 (389-484) | 344 (315-379) | 295 (269-330) | 117 (98-138) | 93 (78-110) | 60 (50-67) | 36 (26-51) | 20 (17-24) | 8 (7-11) | 4 (3.7-4.1) | 0.9 (0.7-1) | |
6 | 775 (695-849) | 609 (530-670) | 563 (492-630) | 325 (292-363) | 208 (180-239) | 138 (115-175) | 90 (71-113) | 38 (29-53) | 33 (25-44) | 8 (3-19) | 3.2 (<2-6) | |
PIPERACILLIN SERUM CONCENTRATIONS IN ADULTS (μ g/mL) AFTER A 30-MINUTE I.V. INFUSION | ||||||||||||
DOSE | 0 | 5 min | 10 min | 15 min | 30 min | 45 min | 1 h | 1.5 h | 2 h | 4 h | 6 h | 7.5 h |
4 | 244 (155-298) | 215 (169-247) | 186 (140-209) | 177 (142-213) | 141 (122-156) | 146 (110-265) | 105 (85-133) | 72 (53-105) | 53 (36-69) | 15 (6-24) | 4 (1-9) | 2 (0.5-3) |
6 | 353 (324-371) | 298 (242-339) | 298 (232-331) | 272 (219-314) | 229 (185-249) | 180 (144-209) | 149 (117-171) | 104 (89-113) | 73 (66-94) | 22 (12-39) | 16 (5-49) | —— |
A 30-minute infusion of 6 g every 6 h gave, on the fourth day, a mean peak serum concentration of 420 μg/mL.
Intramuscular Administration:
PIPRACIL is rapidly absorbed after intramuscular injection. In healthy volunteers, the mean peak serum concentration occurs approximately 30 minutes after a single dose of 2 g and is about 36 μg/mL. The oral administration of 1 g probenecid before injection produces an increase in piperacillin peak serum level of about 30%. The area under the curve (AUC) is increased by approximately 60%.
Pharmacokinetics:
PIPRACIL is not absorbed when given orally. Peak serum concentrations are attained approximately 30 minutes after intramuscular injections and immediately after completion of intravenous injection or infusion. The serum half-life in healthy volunteers ranges from 36 minutes to one hour and 12 minutes. The mean elimination half-life of PIPRACIL in healthy adult volunteers is 54 minutes following administration of 2 g and 63 minutes following 6 g. As with other penicillins, PIPRACIL is eliminated primarily by glomerular filtration and tubular secretion; it is excreted rapidly as unchanged drug in high concentrations in the urine. Approximately 60% to 80% of the administered dose is excreted in the urine in the first 24 hours. Piperacillin urine concentrations, determined by microbioassay, are as high as 14,100 μg/mL following a 6-g intravenous dose and 8,500 μg/mL following a 4-g intravenous dose. These urine drug concentrations remain well above 1,000 μg/mL throughout the dosing interval.
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