procaine (Novocain, Spinocaine, Planocaine)

Introduction

Tradename: Novocain. (procaine hydrochloride)

Indications

• spinal anesthesia
• epidural & peripheral nerve block

Contraindications

• cerebrospinal disease
• heart block
• hypotension
• hypertension
• bowel pathology
• GI hemorrhage

Caution:

• cardiac disease
• hyperthyroidism

Dosage

1%, 2%, 10% (2 mL)

Pharmacokinetics

• onset of action: within 2-5 minutes
• duration of action: 30-90 minuts
• rapidly hydrolyzed by plasma enzymes to para-amino- benzoic acid & diethylaminoethanol (80% conjugated prior to elimination)
• excreted in the urine as metabolites & some unchanged

elimination via plasma

elimination via liver

elimination via kidney

1/2life = 6.7-8.7 min

protein binding = 73-92 %

elimination by hemodialysis = -

elimination by hemoperfusion = -

elimination by peritoneal dialysis = -

Adverse effects

• not common (1-10%)
  • burning sensation at site of injection, pain, tissue irritation
• uncommon (< 1%)
  • aseptic meningitis resulting in paralysis, CNS stimulation followed by CNS depression, skin discoloration, nausea/vomiting, miosis, tinnitus, chills, anaphylactoid reaction

Laboratory

• specimen:
  • plasma (heparin)
  • add 2 drops of 50% sodium arsenite (or 1 mg of echothiopate) per mL of blood
• methods: color, GLC

More general terms

• ester
• local anesthetic

Component of

• novobiocin/penicillin g/procaine
• penicillin g/procaine
• Bicillin CR
• Gerovital (GH3)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4914
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5795
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=232637