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penicillin G benzathine/penicillin G procaine (Bicillin C-R, Bicillin C-R 900/300)

 

Classes: Penicillins, Natural

Dosing and uses of Bicillin C-R, Bicillin C-R 900/300 (penicillin G benzathine/penicillin G procaine)

 

Adult dosage forms and strengths

penicillin G benzathine/penicillin G procaine

injectable suspension

  • 600,000units/600,000units/2mL (ie, 1.2 million units/2mL)
  • 900,000units/300,000units/2mL (ie, 1.2 million units/2mL)

 

Streptococcal Group A Infections

Indicated for moderately severe-to-severe infections of upper-respiratory tract, scarlet fever, erysipelas, and skin and soft-tissue infections caused by streptococcal Group A

2.4 million units IM x1; divided dosage administration into multiple site

Alternatively, administer 1.2 million units IM on day 1, then repeat dose on day 3

 

Pneumococcal Infections

NOT for pneumococcal meningitis

1.2 million units IM; repeat q2-3 days until temperature is normal for 48 hr; other penicillin forms (ie, IV) necessary for severe infection

 

Renal Impairment

CrCl 10-50 mL/min: Decrease dose by 25%

CrCl <10 mL/min: Decrease dose by 50-70%

Hemodialysis: Removed by hemodialysis; administer after dialysis

 

Pediatric dosage forms and strengths

penicillin G benzathine/penicillin G procaine

injectable suspension

  • 600,000units/600,000units/2mL (ie, 1.2 million units/2mL)
  • 900,000units/300,000units/2mL (ie, 1.2 million units/2mL)

 

Streptococcal Group A Infections

Indicated for moderately severe-to-severe infections of upper-respiratory tract, scarlet fever, erysipelas, and skin and soft-tissue infections caused by streptococcal Group A

Bicillin C-r

  • <14 kg: 600,000 units IM x1
  • 14-27 kg: 900,000-1,200,000 units IM x1
  • 27 kg or more: As adults; 2.4 million units IM x1; divided dosage administration into multiple site; alternatively, administer 1.2 million units IM on day 1, then repeat dose on day 3

Bicillin C-R 900/300

  • 900 units/300 units IM x1

 

Pneumococcal Infections

NOT for pneumococcal meningitis

Bicillin C-R: 600,000 units IM; repeat q2-3 days until temperature is normal for 48 hr; other penicillin forms (ie, IV) necessary for severe infection

Bicillin C-R 900/300: 900 units/300 units IM; repeat q2-3 days until temperature is normal for 48 hr; other penicillin forms (ie, IV) necessary for severe infection

 

Renal Impairment

Not defined in children; see adult recommendations

 

Bicillin C-R, Bicillin C-R 900/300 (penicillin G benzathine/penicillin G procaine) adverse (side) effects

Frequency not defined

Skin rashes including maculopapular eruptions and exfoliative dermatitis

Urticaria

Serum-sicknesslike reactions (eg, chills, fever, edema, arthralgia, prostration)

Jarisch-Herxheimer reaction reported when treating syphilis

Pseudomembranous colitis

 

Warnings

Black box warnings

Not for IV use

Do not inject IV or admix with other IV solutions

Reports of inadvertent IV administration associated with cardiorespiratory arrest and death

Prior to administration, carefully read the warnings, adverse reactions, and dosage and administration sections of the labeling

 

Contraindications

Hypersensitivity; serious and occasionally fatal reactions have been reported

 

Cautions

For deep IM administration only; do not administer IV, SC, or It

Do not inject near nerve or artery

Pseudomembranous colitis reported with antibacterial agents, including penicillin g

Procaine reactions: Immediate toxic reactions to procaine reported, particularly when a large single dose is administered (4.8 million units); reaction manifested by mental disturbances including anxiety, confusion, agitation, depression, weakness, seizures, hallucinations, combativeness, and fear

Avoid use in neonates; increased risk for sterile abscess development and procaine toxicity

Severe pneumonia, empyema, bacteremia, pericarditis\is, 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, penicillin G sodium or potassium, either IM or IV, should be used

NOT indicated for treatment of venereal diseases, including syphilis, gonorrhea, yaws, bejel, and pinta

 

Pregnancy and lactation

Pregnancy category: B

Lactation: Excreted into breast milk, caution advised

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Bicillin C-R, Bicillin C-R 900/300 (penicillin G benzathine/penicillin G procaine)

Half-Life: 20-30 minutes after hydrolysis to penicillin g

Absorption: IM, slow

Peak Plasma Time: 3 hr

Peak Plasma Concentration: 1-1.3 units/mL

Protein Bound: 60%

Metabolism: ~30% in liver

Excretion: urine (60-90%)

 

Mechanism of action

Interferes with cell wall mucopeptide synthesis during active multiplication, resulting in bactericidal activity against susceptible microorganisms

 

Administration

IV Administration

Do not inject near artery or nerve (may result in permanent neurologic damage)

Neonates, infants, small children: Midlateral aspect of thigh preferable

Older children and adults: Deep IM injection in upper outer quadrant of buttock

Because of high concentration of suspended matter, needle may be blocked if injection is not made at slow, steady rate

 

Storage

Store refrigerated at 2-8 degrees C (36-46 degrees F)

Do not freeze