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Penicillin G Benzathine / Penicillin G Procaine

Pronunciation

Pronunciation: pen-i-SIL-in G BENZ-ah-theen/pen-i-SIL-in G PRO-cane
Class: Natural penicillin

Trade Names

Bicillin C-R
- Injection 600,000 units/dose (300,000 units each penicillin G benzathine and penicillin G procaine)
- Injection 1,200,000 units/dose (600,000 units each penicillin G benzathine and penicillin G procaine)

Bicillin C-R 900/300
- Injection 1,200,000 units/dose (900,000 units penicillin G benzathine and 300,000 units penicillin G procaine)

Pharmacology

Inhibits mucopeptide synthesis of bacterial cell wall.

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Pharmacokinetics

Absorption

Following IM administration, peak blood levels occur within 3 h.

Distribution

Protein binding is approximately 60%. Distribution varies widely throughout the body tissues with highest levels achieved in kidneys, liver, skin, and intestines.

Elimination

Excreted rapidly by tubular excretion.

Special Populations

Renal Function Impairment

Excretion of the drug is considerably delayed in neonates, children, and individuals with renal function impairment.

Indications and Usage

Treatment of moderately severe infections caused by penicillin G-susceptible microorganisms that are susceptible to serum levels common to this particular dosage form; moderately severe to severe infections of the upper respiratory tract, scarlet fever, erysipelas, and skin and soft tissue infections caused by susceptible streptococci; moderately severe pneumonia and otitis media caused by susceptible organisms. Severe pneumonia, empyema, bacteremia, pericarditis, meningitis, peritonitis, and arthritis of pneumococcal etiology are better treated with penicillin G sodium or potassium during the acute stage. When high, sustained serum levels are required, use penicillin G sodium or potassium IM or IV. This drug should not be used in the treatment of venereal diseases, including bejel, gonorrhea, pinta, syphilis, and yaws.

Contraindications

Hypersensitivity to any penicillin or to procaine.

Dosage and Administration

Streptococcal Infections Group A (upper respiratory tract, skin and soft tissue infections, scarlet fever, and erysipelas)
Adults and Children more than 60 lbs

IM 2,400,000 units.

Children 30 to 60 lbs

IM 900,000 to 1,200,000 units.

Children less than 30 lbs

IM 600,000 units.

Pneumococcal Infections (except pneumococcal meningitis)
Adults

IM 1,200,000 units repeated every 2 or 3 days until temperature is normal for 48 h.

Children

IM 600,000 units repeated every 2 or 3 days until temperature is normal for 48 h.

General Advice

  • For deep IM administration only. Do not administer intradermally, subcutaneous, or IV.
  • Do not inject into or near an artery or nerve.
  • To avoid intravascular administration, aspirate injection site.
  • Multiple concentrations are available. Ensure that the proper concentration is being used.
  • Inject prescribed dose into the upper-outer quadrant of the buttock in adults, or midlateral aspect of thigh in neonates, infants, or small children.
  • Administer injection at a slow, steady rate to prevent blocking the needle.
  • Multiple IM sites may be used to administer total dose in 1 session. An alternate regimen involves administering ½ the dose on day 1 and ½ the dose on day 3.
  • Discontinue the injection if patient complains of, or gives any indication of, severe immediate pain at the injection site.
  • Do not admix with IV solutions.

Storage/Stability

Store in refrigerator (36° to 46°F). Protect from freezing.

Drug Interactions

Probenecid

Increases and prolongs serum penicillin levels.

Tetracycline

May antagonize the bactericidal effect of penicillin.

Adverse Reactions

Cardiovascular

Cardiac arrest; cerebrovascular accident; hypotension; palpitations; pulmonary embolism; pulmonary hypertension; syncope; tachycardia; vasodilation; vasovagal reaction.

CNS

Anxiety; asthenia; coma; confusion; dizziness; euphoria; fatigue; headache; nervousness; neuropathy; seizures; somnolence; transverse myelitis; tremors; a CNS syndrome (with symptoms of severe agitation, convulsion, visual and auditory hallucinations and fear of impending death, psychosis, seizures, dizziness, tinnitus, cyanosis, palpitations, tachycardia, and abnormal taste perception).

Dermatologic

Diaphoresis.

EENT

Blindness; blurred vision.

GI

Blood in stool; intestinal necrosis; nausea; pseudomembranous colitis; vomiting.

Genitourinary

Hematuria; impotence; nephropathy; neurogenic bladder; priapism; proteinuria; renal failure.

Hematologic

Hemolytic anemia; leukopenia; lymphadenopathy; thrombocytopenia.

Metabolic

Elevated BUN, creatinine, and AST.

Respiratory

Apnea; dyspnea; hypoxia.

Miscellaneous

Allergic hypersensitivity (including skin eruptions [maculopapular to exfoliative dermatitis], urticaria, laryngeal edema, fever, eosinophilia); anaphylaxis (including shock and death); exacerbation of arthritis; injection-site reactions (including pain, inflammation, lump, abscess, necrosis, edema, hemorrhage, cellulitis, hypersensitivity, atrophy, ecchymosis, skin ulcer); joint disorder; myoglobinuria; neurovascular reactions (including warmth, vasospasm, pallor, mottling, gangrene, numbness and cyanosis of the extremities, neurovascular damage); periostitis; rhabdomyolysis; serum sickness-like reactions (including chills, fever, edema, arthralgia, prostration).

Precautions

Warnings

Not for IV use. Do not inject IV or add to other IV solutions. Inadvertent IV administration may result in cardiorespiratory arrest and death.


Monitor

Take cultures at completion of therapy to determine whether streptococci have been eradicated.


Pregnancy

Category B .

Lactation

Excreted in breast milk.

Hypersensitivity

Serious and sometimes fatal hypersensitivity reactions have occurred.

Superinfection

Prolonged use of antibiotics may result in bacterial or fungal overgrowth of nonsusceptible microorganisms.

Fibrosis/Atrophy

Quadriceps femoris fibrosis and atrophy can occur following repeated IM injections of penicillin into the anterolateral thigh.

Pseudomembranous colitis

May occur because of overgrowth of clostridia; consider the possibility in patients in whom diarrhea develops.

Overdosage

Symptoms

Neuromuscular hyperirritability, convulsive seizures.

Patient Information

  • Explain to patient or caregiver that medication will be prepared and administered by a health care provider in a health care setting.
  • Review dosing schedule and prescribed length of therapy with patient. Advise patient that dose and duration of therapy are dependent on site, cause of infection, and response to therapy.
  • Instruct patient to report the following to health care provider: diarrhea; difficulty breathing; hives; injection site reaction; itching; loose, foul-smelling stools; rash.

Copyright © 2009 Wolters Kluwer Health.

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