Yes

Antibiotic, Penicillin

Moderately severe infections due to Treponema pallidum and other penicillin G-sensitive microorganisms that are susceptible to low but prolonged serum penicillin concentrations

B

Known hypersensitivity to penicillin or any component; also contraindicated in patients hypersensitive to procaine

May need to modify dosage in patients with severe renal impairment, seizure disorders, or history of hypersensitivity to cephalosporins; avoid I.V., intravascular, or intra-arterial administration of penicillin G procaine since severe and/or permanent neurovascular damage may occur

>10%: Local: Pain at injection site

<1%: Myocardial depression, vasodilation, conduction disturbances, CNS stimulation, seizures, confusion, drowsiness, hemolytic anemia, positive Coombs' reaction, sterile abscess at injection site, myoclonus, interstitial nephritis, pseudoanaphylactic reactions, Jarisch-Herxheimer reaction, hypersensitivity 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: 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

Store in refrigerator

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.

Absorption: I.M.: Slowly absorbed

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

Protein binding: 65%

Metabolism: ~30% of a dose is inactivated in the liver

Time to peak serum concentration: Within 1-4 hours; can persist within the therapeutic range for 15-24 hours

Elimination: Renal clearance is delayed in neonates, young infants, and patients with impaired renal function; 60% to 90% of the drug is excreted unchanged via renal tubular excretion

I.M.:

Congenital syphilis: 50,000 units/kg/day for 10-14 days

Adults: 0.6-4.8 million units/day in divided doses every 12-24 hours

Endocarditis caused by susceptible viridans Streptococcus (when used in conjunction with an aminoglycoside): 1.2 million units every 6 hours for 2-4 weeks

Neurosyphilis: I.M.: 2-4 million units/day with 500 mg probenecid by mouth 4 times/day for 10-14 days; penicillin G aqueous I.V. is the preferred agent

Hemodialysis: Moderately dialyzable (20% to 50%)

Procaine suspension for deep I.M. injection only; rotate the injection site avoid I.V., intravascular, or intra-arterial administration of penicillin G procaine since severe and/or permanent neurovascular damage may occur

Periodic renal and hematologic function tests with prolonged therapy; fever, mental status, WBC count

Positive Coombs' [direct], false-positive urinary and/or serum proteins

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 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.

Renal and hematologic systems should be evaluated periodically during prolonged therapy; do not inject in gluteal muscle in children <2 years of age

Injection, suspension: 300,000 units/mL (10 mL); 500,000 units/mL (1.2 mL); 600,000 units/mL (1 mL, 2 mL, 4 mL)

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

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.

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.