No

Antibiotic, Penicillin

Treatment of susceptible bacterial infections such as osteomyelitis, septicemia, endocarditis, and CNS infections due to penicillinase-producing strains of Staphylococcus; other antistaphylococcal penicillins are usually preferred

B

Known hypersensitivity to methicillin or any penicillin

Elimination rate will be slow in neonates; modify dosage in patients with renal impairment and in the elderly; use with caution in patients with cephalosporin hypersensitivity

1% to 10%:

Dermatologic: Rash

Renal: Acute interstitial nephritis

<1%: Fever, rash, hemorrhagic cystitis, eosinophilia, anemia, leukopenia, neutropenia, thrombocytopenia, phlebitis, serum sickness-like reactions

Symptoms of penicillin overdose include neuromuscular hypersensitivity (agitation, hallucinations, asterixis, encephalopathy, confusion, and seizures) and electrolyte imbalance with potassium or sodium salts, especially in renal failure

Hemodialysis may be helpful to aid in the removal of the drug from the blood, otherwise most treatment is supportive or symptom directed

Decreased effect: Efficacy of oral contraceptives may be reduced

Increased effect: Disulfiram, probenecid may increase penicillin levels, increased effect of anticoagulants

Reconstituted solution is stable for 24 hours at room temperature and 4 days when refrigerated; discard solutions if it has a distinctive hydrogen sulfide odor and/or color turns to a deep orange; incompatible with aminoglycosides and tetracyclines

Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin binding proteins (PBPs); which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.

Distribution: Crosses the placenta; distributes into milk

Protein binding: 40%

Metabolism: Only partially

Half-life (with normal renal function):

Neonates: <2 weeks: 2-3.9 hours; >2 weeks: 0.9-3.3 hours

Children 2-16 years: 0.8 hour

Adults: 0.4-0.5 hour

Time to peak serum concentration: I.M.: 0.5-1 hour; I.V. infusion: Within 5 minutes

Elimination: ~60% to 70% of dose eliminated unchanged in urine within 4 hours by tubular secretion and glomerular filtration

I.M., I.V.:

>7 days and >2000 g: 100 mg/kg/day in divided doses every 6 hours (for meningitis: 200 mg/kg/day)

>7 days and <2000 g: 75 mg/kg/day in divided doses every 8 hours (for meningitis: 150 mg/kg/day)

<7 days and >2000 g: Same as above

<7 days and <2000 g: 50 mg/kg/day in divided doses every 12 hours (for meningitis: 100 mg/kg/day)

Children: 100-300 mg/kg/day in divided doses every 4-6 hours

Adults: 4-12 g/day in divided doses every 4-6 hours

Dosing interval in renal impairment:

Cl_cr 10-50 mL/minute: Administer every 6-8 hours

Cl_cr <10 mL/minute: Administer every 8-12 hours

Hemodialysis: Not dialyzable (0% to 5%)

Observe for signs and symptoms of anaphylaxis during first dose

Interferes with tests for urinary and serum proteins, uric acid, urinary steroids; may cause false-positive Coombs' test; may inactivate aminoglycosides in vitro

Penicillins reported to cause apprehension, illusions, hallucinations, depersonalization, agitation, insomnia, and encephalopathy

May cause leukopenia; use caution with clozapine and carbamazepine

No information available to require special precautions

Prolonged use of penicillins may lead to development of oral candidiasis

This medication can only be administered by injection. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Small frequent meals, frequent mouth care, and adequate fluids may reduce the incidence of nausea or vomiting. If diabetic, drug may cause false tests with Clinitest® urine glucose monitoring; use of glucose oxidase methods (Clinistix®) or serum glucose monitoring is preferable. This drug may interfere with oral contraceptives; an alternate form of birth control should be used. Report difficulty breathing, acute diarrhea, systemic rash, fever, white plaques in mouth or mouth sores. Breast-feeding precautions: Consult prescriber if breast-feeding.

Can be administered IVP at a rate not to exceed 200 mg/minute or intermittent infusion over 15-30 minutes; final concentration for administration should not exceed 20 mg/mL; in fluid-restricted patients, a final concentration for administration of 100 mg/mL has been used

Monitor urinalysis, BUN, serum creatinine, CBC with differential, and periodic liver function tests

Powder for injection, as sodium: 1 g, 4 g, 6 g, 10 g

Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med, 1988, 318(7):419-26 and 318(8):490-500.

Prober CG, Stevenson DK, and Benitz WE, "The Use of Antibiotics in Neonates Weighing Less Than 1200 Grams," Pediatr Infect Dis J, 1990, 9(2):111-21.

Wright AJ, "The Penicillins," Mayo Clin Proc, 1999, 74(3):290-307.

Yow MD, Taber LH, Barrett FF, et al, "A Ten-Year Assessment of Methicillin-Associated Side Effects," Pediatrics, 1976, 58(3):329-34.