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CARDIOVASCULAR SYSTEM › VASOPROTECTIVES › AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE › Local anesthetics
procaine
C05AD05
Forms & Strengths
- Injectable solution 1%
- Injectable solution 2%
- Topical cream/ointment 1%
Adult Dosing
- Infiltration anesthesia: 1% to 2% solution, dose depends on area and procedure, maximum 1000 mg
- Peripheral nerve block: 1% or 2% solution, up to 500 mg per procedure
Pediatric Dosing
- Infiltration anesthesia: Maximum 5 mg/kg per dose
- Safety and efficacy in neonates and infants not well established
Indications
- Local anesthesia by infiltration
- Peripheral nerve block
- Anorectal conditions (topical formulations for pain and pruritus)
Mechanism of Action
- Esthetic local anesthetic that reversibly blocks sodium channels in nerve membranes
- Decreases nerve membrane permeability to sodium ions, preventing initiation and conduction of nerve impulses
Contraindications
- Hypersensitivity to procaine, PABA derivatives, or ester-type local anesthetics
- Concomitant use with sulfa drugs (PABA antagonism)
- Severe shock or heart block when used for systemic or spinal anesthesia
Adverse Reactions
- Central nervous system stimulation or depression (dizziness, tinnitus, tremors, seizures)
- Cardiovascular collapse, hypotension, bradycardia, arrhythmias
- Allergic reactions, anaphylaxis, urticaria, contact dermatitis (PABA metabolite)
Drug Interactions
- Sulfonamides: Procaine metabolites (PABA) may antagonize the antibacterial effect of sulfonamides
- Cholinesterase inhibitors: May prolong procaine toxicity by decreasing plasma metabolism
- Muscle relaxants: May enhance and prolong the neuromuscular blocking effects of succinylcholine
Curated Content: Needs Vetting Before Put to Clinical Use