penicillin G benzathine/penicillin G procaine (Rx)

Brand and Other Names:Bicillin C-R, Bicillin C-R 900/300
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Dosing & Uses

AdultPediatric

Dosing Form & 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

Dosing Form & 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

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Interactions

Interaction Checker

and penicillin G benzathine/penicillin G procaine

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              Serious - Use Alternative (4)

              • baricitinib

                penicillin G benzathine will increase the level or effect of baricitinib by decreasing elimination. Avoid or Use Alternate Drug. Coadministration of baricitinib with strong organic anion transporter 3 (OAT3) inhibitors is not recommended.

              • cholera vaccine

                penicillin G benzathine, cholera vaccine. pharmacodynamic antagonism. Avoid or Use Alternate Drug. Avoid coadministration of cholera vaccine with systemic antibiotics since these agents may be active against the vaccine strain. Do not administer cholera vaccine to patients who have received oral or parenteral antibiotics within 14 days prior to vaccination.

                penicillin G procaine, cholera vaccine. pharmacodynamic antagonism. Avoid or Use Alternate Drug. Avoid coadministration of cholera vaccine with systemic antibiotics since these agents may be active against the vaccine strain. Do not administer cholera vaccine to patients who have received oral or parenteral antibiotics within 14 days prior to vaccination.

              • omadacycline

                omadacycline decreases effects of penicillin G procaine by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Tetracyclines may interfere with the bactericidal action of penicillins. Monitor for decreased therapeutic effects of penicillins if concomitantly used with a tetracycline.

                omadacycline decreases effects of penicillin G benzathine by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Tetracyclines may interfere with the bactericidal action of penicillins. Monitor for decreased therapeutic effects of penicillins if concomitantly used with a tetracycline.

              • sarecycline

                sarecycline decreases effects of penicillin G benzathine by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Tetracyclines may interfere with the bactericidal action of penicillins. Monitor for decreased therapeutic effects of penicillins if concomitantly used with a tetracycline.

                sarecycline decreases effects of penicillin G procaine by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Tetracyclines may interfere with the bactericidal action of penicillins. Monitor for decreased therapeutic effects of penicillins if concomitantly used with a tetracycline.

              Monitor Closely (5)

              • amifampridine

                penicillin G benzathine increases toxicity of amifampridine by Other (see comment). Modify Therapy/Monitor Closely. Comment: Amifampridine can cause seizures. Coadministration with drugs that lower seizure threshold may increase this risk.

                penicillin G procaine increases toxicity of amifampridine by Other (see comment). Modify Therapy/Monitor Closely. Comment: Amifampridine can cause seizures. Coadministration with drugs that lower seizure threshold may increase this risk.

              • apalutamide

                apalutamide will decrease the level or effect of penicillin G benzathine by increasing elimination. Use Caution/Monitor. Apalutamide weakly induces OATP1B1 and may decrease systemic exposure of drugs that are OATP1B1 substrates.

              • dienogest/estradiol valerate

                penicillin G procaine will decrease the level or effect of dienogest/estradiol valerate by altering intestinal flora. Applies only to oral forms of hormone. Low risk of contraceptive failure. Use Caution/Monitor. An alternate or additional form of birth control may be advisable during concomitant use.

              • dienogest/estradiol valerate

                penicillin G benzathine will decrease the level or effect of dienogest/estradiol valerate by altering intestinal flora. Applies only to oral forms of hormone. Low risk of contraceptive failure. Use Caution/Monitor. An alternate or additional form of birth control may be advisable during concomitant use.

              • sodium picosulfate/magnesium oxide/anhydrous citric acid

                penicillin G procaine decreases effects of sodium picosulfate/magnesium oxide/anhydrous citric acid by altering metabolism. Use Caution/Monitor. Coadministration with antibiotics decreases efficacy by altering colonic bacterial flora needed to convert sodium picosulfate to active drug.

                penicillin G benzathine decreases effects of sodium picosulfate/magnesium oxide/anhydrous citric acid by altering metabolism. Use Caution/Monitor. Coadministration with antibiotics decreases efficacy by altering colonic bacterial flora needed to convert sodium picosulfate to active drug.

              Minor (0)

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                Adverse 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

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                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

                Severe cutaneous adverse reactions (SCAR), such as Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP) reported; discontinue therapy when SCAR suspected; consider an alternative treatment

                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, 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

                Methemoglobinemia

                • Use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly; patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition
                • Patients who are administered local anesthetics are at increased risk of developing methemoglobinemia when concurrently exposed to the following drugs, nitroglycerin, nitroprusside, nitric oxide, nitrous oxide, cyclophosphamide, flutamide, hydroxyurea, ifosfamide, rasburicase, dapsone, nitrofurantoin, para­aminosalicylic acid, sulfonamides, chloroquine, primaquine, phenobarbital, sodium valproate, acetaminophen, metoclopramide, quinine, sulfasalazine
                • Advise patients or caregivers to seek immediate medical attention if patient experiences the following signs or symptoms: pale, gray, or blue colored skin (cyanosis); headache; rapid heart rate; shortness of breath; lightheadedness; or fatigue; discontinue drug and any other oxidizing agents; depending on severity of signs and symptoms, patients may respond to supportive care, including oxygen therapy and hydration; a more severe clinical presentation may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen
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                Pregnancy & 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.

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                Pharmacology

                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

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                Administration

                IM 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

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                Formulary

                FormularyPatient Discounts

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                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.