Procaine

Mechanism-of-action class: Sodium Channel Interactions.

• To reduce the development of drug-resistant bacteria and maintain the effectiveness of Bicillin C-R and other antibacterial drugs, Bicillin C-R should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy.

• A previous hypersensitivity reaction to any penicillin or to procaine is a contraindication.contraindicated

Streptococcal Infections Group A Infections of the upper-respiratory tract, skin and soft-tissue infections, scarlet fever, and erysipelas. The following doses are recommended: Adults and pediatric patients over 60 lbs. in weight: 2,400,000 units. Pediatric patients from 30 to 60 lbs.: 900,000 units to 1,200,000 units. Pediatric patients under 30 lbs.: 600,000 units. NOTE: Treatment with the recommended dosage is usually given at a single session using multiple IM sites when indicated. An alternative dosage schedule may be used, giving one-half (1/2) the total dose on day 1 and one-half (1/2) on day 3. This will also insure the penicillinemia required over a 10-day period; however, this alternate schedule should be used only when the physician can be assured of the patient's cooperation. Pneumococcal Infections (except pneumococcal meningitis) 600,000 units in pediatric patients and 1,200,000 units in adults, repeated every 2 or 3 days until the temperature is normal for 48 hours. Other forms of penicillin may be necessary for severe cases. Method of Administration Bicillin C-R is intended for Intramuscular Injection ONLY. Do not inject into or near an artery or nerve, or intravenously or admix with other intravenous solutions. (See WARNINGS section). Administer by DEEP INTRAMUSCULAR INJECTION in the upper, outer quadrant of the buttock (dorsogluteal) or the ventrogluteal site. In neonates, infants and small children, the midlateral aspect of the thigh may be preferable.

WARNING: NOT FOR INTRAVENOUS USE. DO NOT INJECT INTRAVENOUSLY OR ADMIX WITH OTHER INTRAVENOUS SOLUTIONS. THERE HAVE BEEN REPORTS OF INADVERTENT INTRAVENOUS ADMINISTRATION OF PENICILLIN G BENZATHINE WHICH HAS BEEN ASSOCIATED WITH CARDIORESPIRATORY ARREST AND DEATH. Prior to administration of this drug, carefully read the WARNINGS , ADVERSE REACTIONS , and DOSAGE AND ADMINISTRATION sections of the labeling. The combination of penicillin G benzathine and penicillin G procaine should only be prescribed for the indications listed in this insert. Anaphylaxis SERIOUS AND OCCASIONALLY FATAL HYPERSENSITIVITY (ANAPHYLACTIC) REACTIONS HAVE BEEN REPORTED IN PATIENTS ON PENICILLIN THERAPY. THESE REACTIONS ARE MORE LIKELY TO OCCUR IN INDIVIDUALS WITH A HISTORY OF PENICILLIN HYPERSENSITIVITY AND/OR A HISTORY OF SENSITIVITY TO MULTIPLE ALLERGENS. THERE HAVE BEEN REPORTS OF INDIVIDUALS WITH A HISTORY OF PENICILLIN HYPERSENSITIVITY WHO HAVE EXPERIENCED SEVERE REACTIONS WHEN TREATED WITH CEPHALOSPORINS. BEFORE INITIATING THERAPY WITH BICILLIN C-R CAREFUL INQUIRY SHOULD BE MADE CONCERNING PREVIOUS HYPERSENSITIVITY REACTIONS TO PENICILLINS, CEPHALOSPORINS OR OTHER ALLERGENS. IF AN ALLERGIC REACTION OCCURS, BICILLIN C-R SHOULD BE DISCONTINUED AND APPROPRIATE THERAPY INSTITUTED. SERIOUS ANAPHYLACTIC REACTIONS REQUIRE IMMEDIATE EMERGENCY TREATMENT WITH EPINEPHRINE. OXYGEN, INTRAVENOUS STEROIDS AND AIRWAY MANAGEMENT, INCLUDING INTUBATION, SHOULD ALSO BE ADMINISTERED AS INDICATED.

As with other penicillins, untoward reactions of the sensitivity phenomena are likely to occur, particularly in individuals who have previously demonstrated hypersensitivity to penicillins or in those with a history of allergy, asthma, hay fever, or urticaria. The following adverse reactions have been reported with Bicillin C-R during post-marketing experience: Skin and Appendages: Stevens-Johnson syndrome (SJS) and drug reaction with eosinophilia and systemic symptoms (DRESS) (See WARNINGS .) The following have been reported with parenteral penicillin G (the active moiety in Bicillin C-R): General: Hypersensitivity reactions including the following: skin eruptions (maculopapular to exfoliative dermatitis), urticaria, laryngeal edema, fever, eosinophilia; other serum sickness-like reactions (including chills, fever, edema, arthralgia, and prostration); and anaphylaxis including shock and death: severe cutaneous adverse reactions (SCAR), such as toxic epidermal necrolysis (TEN) and acute generalized exanthematous pustulosis (AGEP) (See WARNINGS .) Note: Urticaria, other skin rashes, and serum sickness-like reactions may be controlled with antihistamines and, if necessary, systemic corticosteroids. Whenever such reactions occur, penicillin G should be discontinued unless, in the opinion of the physician, the condition being treated is life-threatening and amenable only to therapy with penicillin G. Serious anaphylactic reactions require immediate emergency treatment with epinephrine.

Pregnancy Teratogenic effects Reproduction studies performed in the mouse, rat, and rabbit have revealed no evidence of impaired fertility or harm to the fetus due to penicillin G. Human experience with the penicillins during pregnancy has not shown any positive evidence of adverse effects on the fetus. There are, however, no adequate and well-controlled studies in pregnant women showing conclusively that harmful effects of these drugs on the fetus can be excluded. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Penicillin in overdosage has the potential to cause neuromuscular hyperirritability or convulsive seizures.

• May 18, 1953NDANDA050138King Pharms Llc

1. 1Drug Hypersensitivity1417%
2. 2Medication Error1316%
3. 3Hypersensitivity1012%
4. 4No Adverse Event89.9%
5. 5Wrong Drug Administered78.6%
6. 6Incorrect Route Of Product Administration67.4%
7. 7Embolia Cutis Medicamentosa56.2%
8. 8Injection Site Pain44.9%
9. 9Off Label Use44.9%
10. 10Dyspnoea33.7%
11. 11Pain33.7%
12. 12Burning Sensation22.5%
13. 13Chest Discomfort22.5%
14. 14Device Breakage22.5%
15. 15Drug Dispensing Error22.5%

Recent PubMed references pinned to Procaine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Multiplexed electrochemical aptasensor on a nanoporous electrode: towards sensitive and anti-fouling detection of procaine, ATP and adenosine in biofluids.
  Talanta · 2026 · Xie Y, Lai J, Yan X, et al.
  PMID 42048832DOI 10.1016/j.talanta.2026.129876
• Nature's touch in the laboratory: eco-friendly and green dual-mode UV-vis and smartphone RGB analysis of procaine in pharmaceuticals using a non-heated aqueous matcha green tea extract.
  Analytical methods : advancing methods and applications · 2026 · Yardımcı B
  PMID 41886068DOI 10.1039/d6ay00184j
• Outcomes with intrathecal 2-chloroprocaine 3% 60 mg and fentanyl 15 μg for cervical cerclage: a retrospective quality assurance study (2021 - 2023).
  International journal of obstetric anesthesia · 2026 · Obiora E, Smiley RM, Menon PG, et al.
  PMID 41855274DOI 10.1016/j.ijoa.2025.104808
• Central Retinal Artery Occlusion - Our Future Path to the Introduction of Intravenous Thrombolysis.
  Ceska a slovenska oftalmologie : casopis Ceske oftalmologicke spolecnosti a Slovenske oftalmologicke spolecnosti · 2026 · Sazanovych D, Schreiberová Z, Sapieta M, et al.
  PMID 41795613DOI 10.31348/2026/12
• Stability of the pH of local anesthetics after bicarbonation: an electrochemical assay of clinical mixtures.
  International journal of obstetric anesthesia · 2026 · Armstrong SL, Li Y, Hess PE, et al.
  PMID 41794005DOI 10.1016/j.ijoa.2026.104889
• Chloroprocaine vs. prilocaine for spinal anesthesia in outpatient knee arthroscopy: a prospective economic evaluation using activity-based costing.
  European review for medical and pharmacological sciences · 2026 · Franceschi C, Tasso F, Simili V, et al.
  PMID 41773612DOI 10.26355/eurrev_202602_37690
• Procaine alleviates microglial pyroptosis by inhibiting O-GlcNAcylation of NOD-like receptor family, pyrin domain-containing 3 through the Janus kinase 2/signal transducer and activator of transcription 3 signaling pathway.
  Neuroreport · 2025 · Zang R, Zhang K, Wang Q, et al.
  PMID 41269989DOI 10.1097/WNR.0000000000002226
• The Procaine-Based ProcCluster(®) Impedes the Second Envelopment Process of Herpes Simplex Virus Type 1.
  International journal of molecular sciences · 2025 · Jungwirth J, Siegert L, Gauthier L, et al.
  PMID 40806319DOI 10.3390/ijms26157185

The 10 most recently updated of 29 ClinicalTrials.gov registrations naming Procaine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Oral Amoxicillin Compared to Penicillin G Benzathine for the Treatment of Acquired Syphilis.
  Active not recruiting · Phase 3 · Interventional · 120 enrolled · Hospital de Niños R. Gutierrez de Buenos Aires
  NCT06877351updated 2025-03-14
• § Procaine Periarticular Injections for Pain Reduction in Elderly With Osteoarthritis
  Completed · Phase 3 · Interventional · 203 enrolled · Sf Luca Chronic Disease Hospital
  NCT06717724updated 2024-12-05
• Exploring Long-term Pain Relief with 5% Dextrose Added to Local Anesthetic
  Active not recruiting · Interventional · 70 enrolled · The Seekers Centre
  NCT06617065updated 2024-12-03
• Virtual Reality in Plastic Surgery: Pain Control and Augmented Satisfaction
  Completed · Observational · 40 enrolled · The Guthrie Clinic
  NCT03914937updated 2024-08-22
• Trial to Assess Chelation Therapy in Critical Limb Ischemia
  Recruiting · Phase 3 · Interventional · 50 enrolled · Mt. Sinai Medical Center, Miami
  NCT03982693updated 2024-08-21
• Efficacy of the Use of Cellular Matrix/ A-CP-HA Kit
  Recruiting · Phase 4 · Interventional · 192 enrolled · Fundación Santiago Dexeus Font
  NCT06425978updated 2024-07-16
• A Prospective Clinical Study on the Safety and Efficacy of Radiofrequency Ablation for the Treatment of Patients With Desmoid Tumors
  Not yet recruiting · Interventional · 27 enrolled · Blokhin's Russian Cancer Research Center
  NCT06355921updated 2024-04-10
• Mesotherapy in the Treatment of Chronic Migraine
  Completed · Interventional · 27 enrolled · Kanuni Sultan Suleyman Training and Research Hospital
  NCT06118190updated 2023-11-07
• Kidney Biopsy Controlled Trial of Calcineurin Inhibitor Withdrawal
  Completed · Phase 4 · Interventional · 58 enrolled · University at Buffalo
  NCT00896012updated 2023-08-14
• Continuous Infusion of Local Anesthetic for Post-operative Pain Control in Ukraine
  Terminated · Interventional · 67 enrolled · Massachusetts General Hospital
  NCT01863940updated 2022-08-25

Frequently asked questions

How does Procaine work?

Mechanism-of-action class: Sodium Channel Interactions.

What is Procaine used for?

According to FDA labeling, Procaine carries indications including: To reduce the development of drug-resistant bacteria and maintain the effectiveness of Bicillin C-R and other antibacterial drugs, Bicillin C-R should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Procaine?

Procaine is classified as Esters of aminobenzoic acid, Local anesthetics, Sodium Channel Interactions, Conduction System Depolarization, Decreased Organized Electrical Activity.

What are the contraindications for Procaine?

Procaine labeling lists contraindications including: A previous hypersensitivity reaction to any penicillin or to procaine is a contraindication.. Always consult the full prescribing information and a clinician.