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Penicillin G

Pronunciation

Pronunciation: PEN-i-SIL-in
Class: Natural penicillin

Trade Names

Penicillin G Potassium
- Injection, solution 1,000,000 units
- Injection, solution 2,000,000 units
- Injection, solution 3,000,000 units

Penicillin G Potassium
- Injection, powder for solution 1,000,000 units

Pfizerpen
- Injection, powder for solution 5,000,000 units (as potassium salt)
- Injection, powder for solution 20,000,000 units (as potassium salt)

Penicillin G Procaine
- Injection, suspension 600,000 units
- Injection, suspension 1,200,000 units

Penicillin G Sodium
- Injection, powder for solution 5,000,000 units

Penicillin G Benzathine

Bicillin L-A
- Injection, suspension 600,000 units (as penicillin G benzathine)
- Injection, suspension 1,200,000 units (as penicillin G benzathine)
- Injection, suspension 2,400,000 units (as penicillin G benzathine)

Crystapen (Canada)

Pharmacology

Inhibits mucopeptide synthesis of bacterial cell wall.

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Pharmacokinetics

Absorption

Peak serum concentrations attained immediately after completion of IV infusion. Aqueous penicillin G is rapidly absorbed following both IM and subcutaneous administration. Penicillin G benzathine has an extremely low solubility and the drug is slowly released from IM injection sites (blood levels persist from 4 to 14 days depending on dose). T max is 4 h (procaine IM).

Distribution

Distributed throughout body tissues; highest levels found in kidneys with lesser amount in liver, skin, and intestines. Also, penetrates CSF; however, concentrations are low with noninflammed meninges. Protein binding is 60%, primarily albumin. Crosses the placenta; distributes into breast milk.

Metabolism

Nonrenal clearance includes hepatic metabolism, which becomes more important with renal impairment.

Elimination

Rapid renal clearance by glomerular filtration and active tubular transport. 58% to 85% of administered dose recovered in the urine. Excreted in the bile to a lesser extent. Serum half-life correlates inversely with age and CrCl.

Special Populations

Renal Function Impairment

Excretion is delayed.

Hepatic Function Impairment

When combined with impaired renal function, elimination is further delayed.

Elderly

Renal Cl is delayed and caused by decreased renal function.

Children

Neonates and premature infants have delayed excretion caused by decreased renal function.

Indications and Usage

Penicillin G Potassium/Sodium

Treatment of anthrax; actinomycosis (abdominal, cervicofacial, or thoracic disease); botulism, gas gangrene, and tetanus; diphtheria; disseminated gonococcal infections (arthritis, endocarditis); empyema, endocarditis, meningitis, pericarditis, pneumonia, and septicemia caused by Streptococcus pyogenes , group C, H, G, L, and M streptococci, Streptococcus pneumoniae , and non–penicillinase-producing strains of Staphylococcus aureus ; Erysipelothrix endocarditis; fusospirochetosis (severe infections of the genital area, lower respiratory tract, and oropharynx [Vincent]); Haverhill or rat-bite fever; Listeria infections, including endocarditis and meningitis; meningococcal meningitis and/or septicemia; Pasteurella infections, including bacteremia and meningitis; syphilis (congenital and neurosyphilis).

Penicillin G Procaine

Treatment of moderately severe infections caused by penicillin G–sensitive microorganisms that are sensitive to low and persistent serum levels achieved with this doseform, including anthrax; diphtheria; erysipeloid; fusospirochetosis; group A streptococcal endocarditis; pneumococcal infections; rat-bite fever; skin and soft tissue infections; streptococcal infections without bacteremia; syphilis; yaws, bejel, and pinta.

Penicillin G Benzathine

Mild to moderate upper respiratory tract infections, venereal diseases (eg, bejel, pinta, syphilis, yaws), and prophylaxis of rheumatic fever or chorea caused by penicillin G–sensitive microorganisms that are susceptible to the low and very prolonged serum levels common to this doseform.

Contraindications

Hypersensitivity to penicillins.

Solutions containing dextrose may be contraindicated in patients with a known allergy to corn or corn products.

Dosage and Administration

Dosage may vary with site of infection and organism being treated.

Penicillin G (Aqueous Potassium or Sodium)
Adults Actinomycosis

IV/IM 1 to 6 million units/day (cervicofacial) or 10 to 20 million units/day (abdominal or thoracic) in divided doses every 4 to 6 h.

Anthrax

IV/IM Minimum of 8 million units/day in divided doses every 6 h.

Clostridial infections

IV/IM 20 million units/day in divided doses every 4 to 6 h.

Diphtheria

IV/IM 2 to 3 million units/day in divided doses every 4 to 6 h for 10 to 12 day.

Disseminated gonococcal infections

IV/IM 10 million units/day in divided doses every 4 to 6 h.

Erysipelothrix endocarditis

IV/IM 12 to 20 million units/day in divided doses every 4 to 6 h.

Fusospirochetosis

IV/IM 5 to 10 million units/day in divided doses every 4 to 6 h.

Haverhill or rat-bite fever

IV/IM 12 to 20 million units/day in divided doses every 4 to 6 h for 3 to 4 wk.

Listeria monocytogenes endocarditis or meningitis

IV/IM 15 to 20 million units/day in divided doses every 4 to 6 h for 2 wk (meningitis) or 4 wk (endocarditis).

Meningococcal meningitis/septicemia

IV/IM 24 million units/day in divided doses every 2 h. Alternatively, a continuous IV infusion of penicillin G potassium 20 to 30 million units/day has been used.

Neurosyphilis

IV/IM 12 to 24 million units/day (2 to 4 million units every 4 h) for 10 to 14 days.

Pasteurella multocida bacteremia/meningitis

IV/IM 4 to 6 million units/day in divided doses every 4 to 6 h for 2 wk.

Serious staphylococcal infections

IV/IM 5 to 24 million units/day in divided doses every 4 to 6 h.

Serious streptococcal infections

IV/IM 12 to 24 million units/day in divided doses every 4 to 6 h.

Children Diphtheria

IV/IM 150,000 to 250,000 units/kg/day in divided doses every 6 h for 7 to 10 days.

Disseminated gonococcal infections

IV/IM For treatment of arthritis, endocarditis, or meningitis in children weighing 45 kg or more, 10 million units/day in 4 equally divided doses with the duration of therapy depending on the type of infection. In children weighing less than 45 kg, 100,000 units/kg/day in 4 equally divided doses for 7 to 10 days for the treatment of arthritis or 250,000 units/kg/day in equal doses every 4 h for 10 to 14 days (meningitis) or 4 weeks (endocarditis).

Haverhill or rat-bite fever

IV/IM 150,000 to 250,000 units/kg/day in equal doses every 4 h for 4 wk.

Listeria monocytogenes Neonates

IV/IM 500,000 to 1 million units/day.

Meningitis caused by susceptible strains of pneumococcus and meningococcus

IV/IM 250,000 units/kg/day divided in equal doses every 4 h (max, 12 to 20 million units/day) for 7 to 14 days, depending on the infecting organism.

Serious streptococcal infections and meningococcus

IV/IM 150,000 to 300,000 units/kg/day divided in equal doses every 4 to 6 h. Duration depends on infecting organism and type of infection.

Syphilis (congenital and neurosyphilis) after the newborn period

IV/IM 200,000 to 300,000 units/kg/day (administered as 50,000 units/kg every 4 to 6 h) for 10 to 14 days.

Penicillin G Procaine
Adults Anthrax

IM For postexposure treatment of inhalational anthrax, 1.2 million units every 12 h. For treatment of cutaneous anthrax, 600,000 to 1 million units/day.

Diphtheria

IM 300,000 to 600,000 units/day as adjunctive therapy with antitoxin; 300,000 units/day for 10 days for diphtheria carrier state.

Erysipeloid, fusospirochetosis, rat-bite fever

IM 600,000 to 1 million units/day.

Syphilis, yaws, bejel, or pinta

IM 600,000 units/day for 8 days (for primary, secondary, and latent infection with negative spinal fluid) or 10 to 15 days (for tertiary, neurosyphilis, and latent infection with a positive or unknown spinal fluid result).

Adults and children (at least 27 kg) Group A streptococcal infections, pneumococcal pneumonia, staphylococcal infections

IM 600,000 to 1 million units/day. Treat streptococcal group A infections for a 10-day minimum.

Children Anthrax

For postexposure treatment of inhalational anthrax, 25,000 units/kg (max, 1.2 million units) every 12 h.

Children older than 12 y Syphilis (primary, secondary, and latent infection with negative spinal fluid)

IM 600,000 units/day for 8 days.

Children (less than 27 kg) Group A streptococcal infections, pneumococcal pneumonia, staphylococcal infections

IM 300,000 units/day.

Congenital Syphilis Children (less than 32 kg)

IM 50,000 units/kg/day as a single dose for 10 days.

Penicillin G Benzathine
Adults Glomerulonephritis/rheumatic fever prophylaxis

IM 1.2 million units once a month or 600,000 units every 2 wk following an acute attack.

Group A streptococcal upper respiratory tract infections, yaws, bejel, pinta

IM 1.2 million units IM as a single dose.

Syphilis

IM 2.4 million units as a single dose for primary, secondary, or latent infection, or once every 7 days for 3 doses for tertiary infection or neurosyphilis.

Children Congenital syphilis

IM For 2 to 12 y of age, adjust dosage based on adult schedule. For younger than 2 y, 50,000 units/kg.

Group A streptococcal upper respiratory tract infection

IM 900,000 units (27 kg or more) or 300,000 to 600,000 units (less than 27 kg) as a single dose.

Renal function impairment Penicillin G Potassium/Sodium Uremia and CrCl more than 10 mL/min

IV/IM Administer a full loading dose followed by one-half the loading dose every 4 to 5 h.

CrCl less then 10 mL/min

IV/IM Administer a full loading dose followed by one-half the loading dose every 8 to 10 h.

Hepatic function impairment Penicillin G Potassium/Sodium

IV/IM Additional dosage adjustments should be made in patients with hepatic disease and renal impairment.

General Advice

  • For most acute infections, continue treatment for at least 48 to 72 h after the patient becomes asymptomatic. Treatment for group A beta-hemolytic streptococcal infections should be maintained for at least 10 days to reduce the risk of rheumatic fever.
  • Depending on route of administration, prepare solution using sterile water for injection, isotonic sodium chloride injection, or dextrose injection. Penicillin solutions are rapidly inactivated in carbohydrate solutions at alkaline pH.
  • For IM administration, inject deeply into upper outer quadrant of buttock in adults. In neonates, infants, and small children, inject in midlateral aspect of thigh. With repeated doses, rotate injection sites.
  • For IV administration, administer continuously or intermittently.
  • Do not mix with other IV solutions.
  • Penicillins are rapidly inactivated in the presence of carbohydrate solutions at alkaline pH.
  • Penicillin may inactivate aminoglycosides in vitro; do not mix in same IV solution. May be used in combination for synergy if administered separately.

Storage/Stability

  • Solutions prepared for IV infusion are stable at room temperature for at least 24 h or for 1 wk if refrigerated, between 36° and 46°F.
  • Dry powder is stable and does not require refrigeration.
  • Thaw premixed frozen solution at room temperature (77°F) or in refrigerator (between 36° and 46°F). Do not force thaw by immersion in water bath or microwave irradiation. Thawed solution is stable for 24 h at room temperature. Do not refreeze thawed solution.
  • Store penicillin G benzathine or procaine in a refrigerator, between 36° and 46°F. Keep from freezing.

Drug Interactions

Anticoagulants (warfarin and heparin)

May increase bleeding risks of anticoagulant by prolonging bleeding time. In some situations, warfarin plasma concentrations and anticoagulant effects may be decreased. Monitor coagulation status and adjust the anticoagulant dose as needed.

Aspirin, furosemide, indomethacin, sulfonamides, thiazide diuretics

These agents may compete with penicillin for renal tubular secretion, prolonging the half-life of penicillin.

Bacteriostatic antibacterial agents (eg, chloramphenicol, macrolide antibiotics [eg, erythromycin], sulfonamides, tetracyclines)

These agents may antagonize the bactericidal effect of penicillin. This has been documented in vitro; however, the clinical importance of this interaction is not well documented. Avoid concomitant use.

Contraceptives, hormonal

May reduce efficacy of oral contraceptives. Alternative methods of birth control may be advisable during the cycle in which penicillin is administered.

Live vaccines

Penicillin G potassium and penicillin G sodium may decrease the effectiveness of live vaccines. Concurrent use is not recommended.

Methotrexate

Penicillin G may increase the serum concentrations and pharmacologic effects of methotrexate. Toxicity may occur. Close clinical and methotrexate concentration monitoring is warranted.

Probenecid

Increases penicillin serum concentration.

Succinylcholine

Neuromuscular blocking effects of succinylcholine may be increased by procaine in penicillin G procaine, possibly in a dose-dependent manner. Prolonged respiratory depression with extended periods of apnea may occur. Coadminister with caution. Provide mechanical respiratory support as needed.

Tetracyclines

May impair bactericidal effects of penicillin G. Avoid concurrent use.

Laboratory Test Interactions

Proteinuria

Penicillin G has been associated with pseudoproteinuria by certain test methods.

Urine glucose test

Drug may cause false-positive results with copper sulfate tests (Benedict test, Fehling test, or Clinitest tablets); enzyme-based tests (eg, Clinistix , Tes-Tape ) are not affected.

Adverse Reactions

Cardiovascular

Cardiac arrest or arrhythmias, congestive heart failure with high doses of aqueous solutions because of sodium content.

Penicillin G benzathine

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

CNS

Headache, neurotoxicity (eg, coma, hyperreflexia, myoclonic twitches, seizures).

Penicillin G benzathine

Anxiety, confusion, dizziness, euphoria, Hoigne syndrome, nervousness, somnolence, transverse myelitis, tremors.

Dermatologic

Penicillin G benzathine

Diaphoresis.

EENT

Black or hairy tongue, stomatitis.

Penicillin G benzathine

Blindness, blurred vision.

GI

Nausea, pseudomembranous colitis, vomiting.

Penicillin G benzathine

Blood in stool, intestinal necrosis.

Genitourinary

Interstitial nephritis (eg, eosinophilia, eosinophiluria, fever, hematuria, increase in BUN, proteinuria, rash), nephropathy, renal tubular damage.

Penicillin G benzathine

Impotence, neurogenic bladder, priapism, renal failure.

Hematologic

Bleeding diathesis, Coombs positive hemolytic anemia, hemolytic anemia, leukopenia, neutropenia, thrombocytopenia.

Penicillin G benzathine

Lymphadenopathy.

Hypersensitivity

Reactions, including anaphylaxis, angioneurotic edema, bronchospasm, death, fever, hypotension, laryngeal edema, laryngospasm, pruritus, rashes ranging from maculopapular to exfoliative dermatitis, serum sickness–like symptoms, urticaria, vascular collapse.

Lab Tests

Penicillin G benzathine

Elevated AST, elevated creatinine.

Local

Pain at the injection site, phlebitis, thrombophlebitis.

Penicillin G benzathine

Injection-site reactions, including abscess, atrophy, cellulitis, ecchymosis, edema, hemorrhage, hypersensitivity, inflammation, lump, necrosis, skin ulcer; neurovascular reactions, including cyanosis of the extremities, gangrene of the extremities, mottling, neurovascular damage, numbness of the extremities, pallor, vasospasm, warmth.

Metabolic

Electrolyte abnormalities, including hyperkalemia.

Musculoskeletal

Penicillin G benzathine

Exacerbation of arthritis, joint disorder, myoglobinuria, periostitis, rhabdomyolysis.

Respiratory

Penicillin G benzathine

Apnea, dyspnea, hypoxia.

Miscellaneous

Jarisch-Herxheimer reaction.

Precautions

Monitor

Perform periodic assessment of organ system function, including frequent evaluation of electrolyte balance; hepatic, renal, and hematopoietic systems; and cardiac and vascular status during prolonged therapy with high doses of IV penicillin G.


Pregnancy

Category B .

Lactation

Excreted in breast milk. Considered compatible with breast-feeding in non-hypersensitive infants.

Hypersensitivity

Reactions range from mild to life-threatening. Administer drug with caution to cephalosporin-sensitive patients because of possible crossreactivity.

Renal Function

Use drug with caution; may require dosage adjustment.

Special Risk Patients

Use with caution in patients with histories of significant allergies and/or asthma.

Superinfection

May result in bacterial or fungal overgrowth of nonsusceptible organisms.

Clostridium difficile –associated diarrhea

Consider in patients in whom diarrhea develops. May range in severity from mild diarrhea to fatal colitis.

Electrolyte imbalance

Penicillin G sodium contains 1.68 mEq sodium per 1 million units. Penicillin G potassium contains 1.7 mEq potassium and 0.3 to 1.02 mEq sodium per 1 million units. Beware of iatrogenic electrolyte abnormalities and fluid overload.

IM injection

Avoid accidental IV or intra-arterial administration or injection into or near a major nerve or blood vessel; may produce neurovascular damage.

Procaine sensitivity

If sensitivity to procaine in penicillin G procaine is suspected, inject 0.1 mL of procaine 1% to 2% solution intradermally. If erythema, wheal, flare, or eruption develops, do not use procaine penicillin preparations.

Overdosage

Symptoms

Agitation, asterixis, coma, confusion, encephalopathy, hallucinations, hyperkalemia, multifocal myoclonus, neuromuscular hyperexcitability, seizures, stupor.

Patient Information

  • Instruct patient to finish course of therapy even if feeling better.
  • Instruct penicillin allergic patient to carry medical identification (eg, card, bracelet).
  • Inform patient of signs of hypersensitivity (eg, skin rash, itching, hives, shortness of breath, wheezing) and other side effects, such as black tongue, sore throat, nausea, vomiting, severe diarrhea, fever, and swollen joints. Instruct patient to notify health care provider should they occur.
  • Instruct patient to notify health care provider if there is no improvement in symptoms of infection.
  • Advise patient to notify health care provider of signs of superinfection (eg, vaginitis; black, hairy tongue).

Copyright © 2009 Wolters Kluwer Health.

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