Class: Natural penicillin
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
- 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
- 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)
Inhibits mucopeptide synthesis of bacterial cell wall.
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).
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.
Nonrenal clearance includes hepatic metabolism, which becomes more important with renal impairment.
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 PopulationsRenal 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 UsagePenicillin 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.
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)
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
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.
- 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.
- 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 InteractionsAnticoagulants (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 InteractionsProteinuria
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.
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.
Headache, neurotoxicity (eg, coma, hyperreflexia, myoclonic twitches, seizures).Penicillin G benzathine
Anxiety, confusion, dizziness, euphoria, Hoigne syndrome, nervousness, somnolence, transverse myelitis, tremors.
DermatologicPenicillin G benzathine
Black or hairy tongue, stomatitis.Penicillin G benzathine
Blindness, blurred vision.
Nausea, pseudomembranous colitis, vomiting.Penicillin G benzathine
Blood in stool, intestinal necrosis.
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.
Bleeding diathesis, Coombs positive hemolytic anemia, hemolytic anemia, leukopenia, neutropenia, thrombocytopenia.Penicillin G benzathine
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 TestsPenicillin G benzathine
Elevated AST, elevated creatinine.
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.
Electrolyte abnormalities, including hyperkalemia.
MusculoskeletalPenicillin G benzathine
Exacerbation of arthritis, joint disorder, myoglobinuria, periostitis, rhabdomyolysis.
RespiratoryPenicillin G benzathine
Apnea, dyspnea, hypoxia.
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.
Category B .
Excreted in breast milk. Considered compatible with breast-feeding in non-hypersensitive infants.
Reactions range from mild to life-threatening. Administer drug with caution to cephalosporin-sensitive patients because of possible crossreactivity.
Use drug with caution; may require dosage adjustment.
Special Risk Patients
Use with caution in patients with histories of significant allergies and/or asthma.
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.
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.
Avoid accidental IV or intra-arterial administration or injection into or near a major nerve or blood vessel; may produce neurovascular damage.
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.
Agitation, asterixis, coma, confusion, encephalopathy, hallucinations, hyperkalemia, multifocal myoclonus, neuromuscular hyperexcitability, seizures, stupor.
- 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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