Trade Names:Pfizerpen- Powder for injection 1,000,000 units- Powder for injection 5,000,000 units- Powder for injection 20,000,000 unitsPenicillin G Procaine
Trade Names:Wycillin- Injection, IM 600,000 units- Injection, IM 1,200,000 units- Injection, IM 2,400,000 unitsPenicillin G Sodium
Trade Names:Penicillin G Sodium- Powder for injection 5,000,000Crystapen (Canada)Penicillin G Benzathine
Trade Names:Bicillin L-A- Injection, IM 300,000 units/mL- Injection, IM 600,000 units/dose- Injection, IM 1,200,000 units/dose- Injection, IM 2,400,000 units/dose
Trade Names:Permapen- Injection 1,200,000 units/dose
Inhibits mucopeptide synthesis of bacterial cell wall.
Varies considerably, 15% to 30% (oral) and slow absorption (IM). T max is 1 to 2 h (oral), 24 h (benzathine IM), and 4 h (procaine IM). C max is 2.2 to 17 mcg/mL (IV), 0.03 to 0.05 mcg/mL (benzathine 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, as is penetration in purulent bronchial secretions. Protein binding is 60% (oral), primarily albumin. Vd is 0.5 to 0.7 L/kg (oral). Crosses the placenta; distributes into breast milk.
Hepatic metabolism accounts for less than 30% of the biotransformation.
Renal (largely unchanged); hepatic inactivation and excretion in bile; t ½ 1.4 h or less.
Sustaining levels for up to 4 wk (benzathine).
Neonates and young infants with impaired renal function have delayed excretion.
Treatment of infections caused by susceptible microorganisms.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 dose form.Penicillin G Benzathine
Mild to moderate upper respiratory tract infections, venereal diseases, 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 dosage form.
Hypersensitivity to penicillins. Do not treat severe pneumonia, empyema, bacteremia, pericarditis, meningitis, and purulent or septic arthritis with oral penicillin G during acute stage.
Dosage may vary with site of infection and organism being treated.Penicillin G (Aqueous Potassium or Sodium)Adults
IV / IM 1 to 24 million units/day in divided doses every 4 to 6 h.Children
IV / IM 100,000 to 250,000 units/kg/day in divided doses every 4 h.Infants (older than 7 days of age and more than 2,000 g)
IV / IM 100,000 units/kg/day in divided doses every 6 h (meningitis: 200,000 units/kg/day in divided doses every 6 h).Infants (younger than 7 days of age and more than 2,000 g)
IV / IM 50,000 units/kg/day in divided doses every 8 h (meningitis: 150,000 units/kg/day in divided doses every 8 h).Infants (younger than 7 days of age and less than 2,000 g)
IV / IM 50,000 units/kg/day in divided doses every 12 h (meningitis: 100,000 units/kg/day in divided doses every 12 h).Penicillin G PotassiumAdults and children older than 12 yr of age
PO 200,000 to 500,000 units every 6 to 8 h.Infants and children younger than 12 yr of age
PO 25,000 to 90,000 units/kg/day in 3 to 6 divided doses.Penicillin G Procaine (Aqueous)Adults and children (at least 27 kg)
IM 600,000 to 1.2 million units/day in 1 to 2 doses.Children (under 27 kg)
IM 300,000 units/day.Congenital Syphilis Children (under 32 kg)
IM 50,000 units/kg/day as a single dose for 10 to 14 days.Neurosyphilis Adults
IM 2.4 million units/day plus probenecid 500 mg PO 4 times daily, both for 10 to 14 days.Penicillin G BenzathineAdults
IM 1.2 to 2.4 million units in 1 dose.Children more than 27 kg
IM 900,000 to 1.2 million units in 1 dose.Children and infants less than 27 kg
IM 300,000 to 1.2 million units in 1 dose.Newborns
IM 50,000 units/kg in 1 dose.
May increase bleeding risks of anticoagulant by prolonging bleeding time.Beta-blockers
May potentiate anaphylactic reactions of penicillin.Chloramphenicol
May cause synergism or antagonism to develop.Contraceptives, oral
May reduce efficacy of oral contraceptives.Erythromycin
May cause synergism or antagonism to develop.Probenecid
Increases penicillin serum concentration.Tetracyclines
May impair bactericidal effects of penicillin G.
Penicillin may inactivate aminoglycosides in vitro; do not mix in same IV solution. May be used in combination for synergy if administered separately.Carbohydrate solutions at alkaline pH
Penicillin solutions are rapidly inactivated.
Drug may cause false-positive results.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.Urine protein determinations
Drug may cause false-positive reactions with sulfosalicylic acid and boiling test, acetic acid test, biuret reaction, and nitric acid test; bromphenol blue test ( Multi-Stix ) is not affected.
Dizziness; fatigue; insomnia; reversible hyperactivity; neurotoxicity (eg, lethargy, neuromuscular irritability, hallucinations, convulsions, seizures).
Itchy eyes; stomatitis; gastritis; sore mouth or tongue; furry tongue; black “hairy” tongue; abnormal taste perception.
Glossitis; dry mouth; nausea; anorexia; vomiting; abdominal pain or cramp; epigastric distress; diarrhea or bloody diarrhea; rectal bleeding; flatulence; enterocolitis; pseudomembranous colitis.
Interstitial nephritis (eg, oliguria, proteinuria, hematuria, hyaline casts, pyuria); nephropathy; increased BUN and creatinine.
Decreased hemoglobin, hematocrit, RBC, WBC, neutrophils, lymphocytes, platelets; increased lymphocytes, monocytes, basophils, eosinophils and platelets; abnormal coagulation tests.
Elevated serum alkaline phosphatase, hypernatremia; hypokalemia; hyperkalemia.
Hypersensitivity reactions (eg, urticaria, angioneurotic edema, laryngospasm, laryngeal edema, bronchospasm, hypotension, vascular collapse, death, maculopapular to exfoliative dermatitis, vesicular eruptions, erythema multiforme, serum sickness, skin rashes); vaginitis; hyperthermia.
Category B .
Small amount excreted in breast milk. May cause diarrhea, candidiasis, or allergic response in breast-feeding infant.
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.
May result in bacterial or fungal overgrowth of nonsusceptible organisms.
Some products contain tartrazine, which may cause allergic-type reactions in susceptible individuals.
Penicillin G aqueous sodium contains 2 mEq sodium per 1 million units. Penicillin G aqueous potassium contains 1.7 mEq potassium and 0.3 mEq sodium per 1 million units. Beware of iatrogenic electrolyte abnormalities and fluid overload.
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.
May occur because of overgrowth of clostridia.
Neuromuscular hyperexcitability, convulsions, agitation, confusion, asterixis, hallucinations, stupor, coma, multifocal myoclonus, seizures, encephalopathy, hyperkalemia.
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