No

Antibiotic, Penicillin

Active against some gram-positive organisms, generally not Staphylococcus aureus; some gram-negative organisms such as Neisseria gonorrhoeae, and some anaerobes and spirochetes

B

Known hypersensitivity to penicillin or any component

Avoid intra-arterial administration or injection into or near major peripheral nerves or blood vessels since such injections may cause severe and/or permanent neurovascular damage; use with caution in patients with renal impairment (dosage reduction required), pre-existing seizure disorders, or with a history of hypersensitivity to cephalosporins

<1%: Convulsions, confusion, drowsiness, fever, rash, electrolyte imbalance, hemolytic anemia, positive Coombs' reaction, thrombophlebitis, myoclonus, acute interstitial nephritis, Jarisch-Herxheimer reaction, hypersensitivity reactions, anaphylaxis

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: Tetracyclines may decrease penicillin effectiveness; decreased oral contraceptive effect is possible

Increased effect:

Probenecid may increase penicillin levels

Aminoglycosides may result in synergistic efficacy; heparin and parenteral penicillins may result in increased bleeding

Penicillin G potassium is stable at room temperature

Reconstituted parenteral solution is stable for 7 days when refrigerated (2°C to 15°C)

Penicillin G potassium for I.V. infusion in NS or D₅W, solution is stable for 24 hours at room temperature

Incompatible with aminoglycosides; inactivated in acidic or alkaline solutions

Interferes with bacterial cell wall synthesis during active multiplication, causing cell wall death and resultant bactericidal activity against susceptible bacteria

Distribution: Crosses the placenta; appears in breast milk; penetration across the blood-brain barrier is poor, despite inflamed meninges

Relative diffusion of antimicrobial agents from blood into cerebrospinal fluid (CSF): Good only with inflammation (exceeds usual MICs)

Ratio of CSF to blood level (%): Normal meninges: <1; Inflamed meninges: 3-5

Protein binding: 65%

Metabolism: In the liver (30%) to penicilloic acid

Half-life:

Neonates: <6 days: 3.2-3.4 hours; 7-13 days: 1.2-2.2 hours; >14 days: 0.9-1.9 hours

Children and adults with normal renal function: 20-50 minutes

End-stage renal disease: 3.3-5.1 hours

Time to peak serum concentration: I.M.: Within 30 minutes; I.V. Within 1 hour

Elimination: In urine

I.M., I.V.:

>7 days, >2000 g: 100,000 units/kg/day in divided doses every 6 hours

>7 days, <2000 g: 75,000 units/kg/day in divided doses every 8 hours

<7 days, >2000 g: 50,000 units/kg/day in divided doses every 8 hours

<7 days, <2000 g: 50,000 units/kg/day in divided doses every 12 hours

Infants and Children (sodium salt is preferred in children): 100,000-250,000 units/kg/day in divided doses every 4 hours

Severe infections: Up to 400,000 units/kg/day in divided doses every 4 hours; maximum dose: 24 million units/day

Adults: 2-24 million units/day in divided doses every 4 hours depending on sensitivity of the organism and severity of the infection

Congenital syphilis:

Newborns: 50,000 units/kg/day I.V. every 8-12 hours for 10-14 days

Infants: 50,000 units/kg every 4-6 hours for 10-14 days

Disseminated gonococcal infections or gonococcus ophthalmia (if organism proven sensitive): 100,000 units/kg/day in 2 equal doses (4 equal doses/day for infants >1 week)

Gonococcal meningitis: 150,000 units/kg in 2 equal doses (4 doses/day for infants >1 week)

Dosing interval in renal impairment:

Cl_cr 30-50 mL/minute: Administer every 6 hours

Cl_cr 10-30 mL/minute: Administer every 8 hours

Cl_cr <10 mL/minute: Administer every 12 hours

Hemodialysis: Moderately dialyzable (20% to 50%)

Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Dose as for Cl_cr 10-50 mL/minute

Observe for signs and symptoms of anaphylaxis during first dose

False-positive or negative urinary glucose determination using Clinitest®; positive Coombs' [direct]; false-positive urinary and/or serum proteins

No information available to require special precautions

No effects or complications reported

This medication will be administered I.V. or I.M. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). If being treated for sexually transmitted disease, partner will also need to be treated. Small frequent meals, frequent mouth care, sucking lozenges, or chewing gum may reduce nausea or dry mouth. Important to maintain good oral and vaginal hygiene to reduce incidence of opportunistic infection. 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 persistent diarrhea, fever, chills, unhealed sores, bloody urine or stool, muscle pain, mouth sores, or difficulty breathing.

Dosage modification required in patients with renal insufficiency

Penicillin g potassium:

Injection, as sodium: 5 million units

Injection:

Frozen premixed, as potassium: 1 million units, 2 million units, 3 million units

Powder, as potassium: 1 million units, 5 million units, 10 million units, 20 million units

American Academy of Pediatrics Committee on Infectious Diseases, "Treatment of Bacterial Meningitis," Pediatrics, 1988, 81(6):904-7.

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

Hansen JM, Kampmann J, and Laursen H, "Renal Excretion of Drugs in the Elderly," Lancet, 1970, 1(657):1170.

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.

Wickerts CJ, Asaba H, Gunnarsson B, et al, "Combined Carbon Haemoperfusion and Haemodialysis in the Treatment of Penicillin Intoxication," Br Med J, 1980, 280(6226):1254-5.

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

Yoshikawa TT, "Antimicrobial Therapy for the Elderly Patient," J Am Geriatr Soc, 1990, 38(12):1353-72.