[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Local anesthetics](https://durgical.com/en/pharmacology/classes/local-anesthetics/) › Procaine

[Pharmacology](https://durgical.com/en/pharmacology/) · [Local anesthetics](https://durgical.com/en/pharmacology/classes/local-anesthetics/)

# Procaine

The classic ester local anaesthetic: low potency and short-acting. Today it is used mainly as part of procaine benzylpenicillin.

Updated 2026-11-01

- Class: [Local anesthetics](https://durgical.com/en/pharmacology/classes/local-anesthetics/)
- Ion channel: Voltage-gated sodium channels (Nav)
- ATC code: N01BA02

## Mechanism of action

Procaine, the prototype ester local anaesthetic, blocks voltage-gated sodium channels and stops nerve conduction. Plasma esterases hydrolyse it rapidly, so its action is short, and one of its products is para-aminobenzoic acid (PABA), responsible for ester allergies. Combined with benzylpenicillin it forms a poorly soluble salt that releases the antibiotic slowly from muscle.

- Blocks the nerve sodium channel
- Short-lasting anaesthesia
- Plasma cholinesterase hydrolyses it to PABA
- PABA explains ester allergy

## Pharmacokinetics

**Metabolism**
Rapid hydrolysis by plasma esterases to para-aminobenzoic acid.

**Elimination**
Kidney, as metabolites.

## Indications

- Component of intramuscular procaine benzylpenicillin, whose slow release prolongs the antibiotic's effect

## Adverse effects

### Common

- Allergic skin reactions
- Dizziness and perioral numbness if much is absorbed

### Serious (rare, important)

- Severe allergic reactions, with cross-allergy to other esters
- Systemic toxicity (seizures, arrhythmias) with intravascular injection

## Contraindications

- Allergy to procaine, PABA or other ester-type anaesthetics

## Key interactions

**Other esters (tetracaine, benzocaine)**
Cross-allergy through a common metabolite.

**Neuromuscular blockers**
Procaine can enhance block at the motor end plate.

## What is monitored

- Signs of allergy after injection
- Neurological signs of toxicity if accidentally injected into a vessel

## Administration and safety

- Procaine benzylpenicillin is an intramuscular formulation: confirm the route before injecting.
- Ask first about allergy to penicillin and to ester-type anaesthetics.

## Nursing care

- Before: allergies to penicillin, procaine and other «-caines».
- After: observe the patient for a while in case allergic reactions or neurological symptoms appear.

## Memory aid

PROcaine: the «PROtotype» ester; Poor potency, Rapidly gone, Origin of PABA.

## Test yourself

Think of the answer, then tap the question to see it.

## Why is the action of procaine short?

Plasma esterases hydrolyse it rapidly.

## Which procaine metabolite explains allergies to ester anaesthetics?

Para-aminobenzoic acid (PABA).

## In which medicine is procaine most often found today?

In procaine benzylpenicillin, a slow-release salt for intramuscular injection.

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## Related drugs

- [Tetracaine](https://durgical.com/en/pharmacology/tetracaine/)
- [Benzocaine](https://durgical.com/en/pharmacology/benzocaine/)

[← Back to the class: Local anesthetics](https://durgical.com/en/pharmacology/classes/local-anesthetics/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 25 (McGraw Hill, 2023); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N01BA02) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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