No

Antibiotic, Penicillin

Active against some gram-positive organisms, few gram-negative organisms such as Neisseria gonorrhoeae, and some anaerobes and spirochetes; used in the treatment of syphilis; used only for the treatment of mild to moderately severe infections caused by organisms susceptible to low concentrations of penicillin G or for prophylaxis of infections caused by these organisms

B

Known hypersensitivity to penicillin or any component

Use with caution in patients with impaired renal function, seizure disorder, or history of hypersensitivity to other beta-lactams; CDC and AAP do not currently recommend the use of penicillin G benzathine to treat congenital syphilis or neurosyphilis due to reported treatment failures and lack of published clinical data on its efficacy

1% to 10%: Local: Pain

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

Store in refrigerator

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

Absorption: I.M.: Slow

Time to peak serum concentration: Within 12-24 hours; serum levels are usually detectable for 1-4 weeks depending on the dose; larger doses result in more sustained levels rather than higher levels

I.M.: Administer undiluted injection; higher doses result in more sustained rather than higher levels. Use a penicillin G benzathine-penicillin G procaine combination to achieve early peak levels in acute infections.

Group A streptococcal upper respiratory infection: 25,000-50,000 units/kg as a single dose; maximum: 1.2 million units

Prophylaxis of recurrent rheumatic fever: 25,000-50,000 units/kg every 3-4 weeks; maximum: 1.2 million units/dose

Early syphilis: 50,000 units/kg as a single injection; maximum: 2.4 million units

Syphilis of more than 1-year duration: 50,000 units/kg every week for 3 doses; maximum: 2.4 million units/dose

Adults:

Group A streptococcal upper respiratory infection: 1.2 million units as a single dose

Prophylaxis of recurrent rheumatic fever: 1.2 million units every 3-4 weeks or 600,000 units twice monthly

Early syphilis: 2.4 million units as a single dose in 2 injection sites

Syphilis of more than 1-year duration: 2.4 million units in 2 injection sites once weekly for 3 doses

Not indicated as single drug therapy for neurosyphilis, but may be given 1 time/week for 3 weeks following I.V. treatment (refer to Penicillin G monograph for dosing)

Administer by deep I.M. injection in the upper outer quadrant of the buttock; do not give I.V., intra-arterially, or S.C.; in children <2 years of age, I.M. injections should be made into the midlateral muscle of the thigh, not the gluteal region; when doses are repeated, rotate the injection site

Observe for signs and symptoms of anaphylaxis during first dose

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

May rarely cause drowsiness or confusion; penicillins reported to cause apprehension, illusions, hallucinations, depersonalization, agitation, insomnia, and encephalopathy

None reported

No information available to require special precautions

No effects or complications reported

Take as directed, for full course of therapy. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). If begin 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.

Monitor CBC, urinalysis, renal function tests

Injection: 300,000 units/mL (10 mL); 600,000 units/mL (1 mL, 2 mL, 4 mL)

Collart P, Poitevin M, Milovanovic A, et al, "Kinetic Study of Serum Penicillin Concentrations After Single Doses of Benzathine and Benethamine Penicillins in Young and Old People," Br J Vener Dis, 1980, 56(6):355-62.

Kaplan EL, Berrios X, Speth J, et al, "Pharmacokinetics of Benzathine Penicillin G: Serum Levels During the 28 Days After Intramuscular Injection of 1,200,000 Units," J Pediatr, 1989, 115(1):146-50.

Paryani SG, Vaughn AJ, Crosby M, et al, "Treatment of Asymptomatic Congenital Syphilis: Benzathine Versus Procaine Penicillin G Therapy," J Pediatr, 1994, 125(3):471-5.

U.S. Department of Health and Human Services, "1993 Sexually Transmitted Diseases Treatment Guidelines," MMWR Morb Mortal Wkly Rep, 1993, 42(RR-14).

WHO Study Group, "Rheumatic Fever and Rheumatic Heart Disease," World Health Organ Tech Rep Ser, 1988, 764:1-58.

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