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Local Anaesthetic (Amide) Pregnancy: Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity; as a precautionary measure it is preferable to avoid the use of prilocaine hydrochloride during early pregnancy. Neonatal methaemoglobinaemia has been reported after paracervical (PCB) or pudendal block in the obstetric patient, and prilocaine should not be used for these blocks. Foetal adverse effects due to local anaesthetics, such as foetal bradycardia, seem most apparent in paracervical block anaesthesia and may be due to high concentrations of anaesthetic reaching the foetus. Breast-feeding: prilocaine enters the mother's milk but no effects have been shown in breastfed newborns/infants of treated mothers.

Prilocaine

Brand names: Citanest, EMLA (with lidocaine)

Prilocaine is an amide local anaesthetic used for infiltration, regional and intravenous regional anaesthesia, and as a topical agent in combination preparations.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: Individualised — the dose is adjusted according to the response of the patient and the site of administration, and the lowest concentration and smallest dose producing the required effect should be given. No fixed adult dose per block is stated in this SPC; the maximum dose of prilocaine hydrochloride for healthy adults should not exceed 400 mg.
Route: Injection (local infiltration and regional block) — Prilocaine hydrochloride 1% Solution for Injection. Careful aspiration before and during the injection is recommended to avoid intravascular injection.
Frequency: As required for the procedure; no repeat-dose interval is stated in SPC 4.2
Max: The maximum dose of prilocaine hydrochloride for healthy adults should not exceed 400 mg. Preservative-containing solutions (multi-dose vials) should not be used for intrathecal or epidural anaesthesia, intraocular or retrobulbar injections, or in doses of more than 15 ml for other types of blockade.
Source: eMC SPC for Prilocaine hydrochloride 1% Solution for Injection. Elderly/debilitated patients require smaller doses, commensurate with age and physical status. Care should be taken to prevent toxic reactions by avoiding intravascular injection — great caution is needed since accidental intravascular injection may cause rapid onset of toxicity with marked restlessness, twitching or convulsions, followed by coma with apnoea and cardiovascular collapse. Regional anaesthetic procedures should always be performed in a properly equipped and staffed area with resuscitation equipment and drugs immediately available; when performing major blocks an i.v. cannula should be inserted before the local anaesthetic is injected. Methaemoglobinaemia is the specific hazard of prilocaine: it may occur at lower doses in patients with anaemia, congenital or acquired haemoglobinopathy (including methaemoglobinaemia) or in patients on concomitant therapy known to cause it (e.g. sulphonamides); infants are particularly susceptible due to lower activity of the enzyme that reduces methaemoglobin, and patients with cardiac insufficiency require special attention. Not approved for post-operative intra-articular continuous infusion of local anaesthetics — there have been post-marketing reports of chondrolysis with this use. Possibly porphyrinogenic: only prescribe to patients with acute porphyria when no safer alternative is available. Peribulbar injections carry a low risk of persistent ocular muscle dysfunction, and injections in the head and neck regions may be made inadvertently into an artery causing cerebral symptoms even at low doses. Paediatric restriction (SPC 4.2): prilocaine hydrochloride should not be used in children under 6 months of age, and should not be used for paracervical (PCB) block or pudendal block in the obstetric patient; there is an increased risk of methaemoglobin formation in children and in the neonate after delivery. The openFDA and WHO providers returned no content for this id.

Paediatric dose

Route: Injection (local infiltration and regional block)
Frequency: As required for the procedure; no paediatric frequency or repeat-dose interval is stated in SPC 4.2
Max: Children above the age of 6 months: dosage calculated on a weight basis up to 5 mg/kg
dosePerKg left null because the SPC states only a per-kg ceiling, not a per-kg dose to administer. Verbatim source (SPC 4.2): 'Prilocaine hydrochloride should not be used in children under 6 months of age and for use in paracervical (PCB) block and pudendal block in the obstetric patient. There is an increased risk of methaemoglobin formation in children and in the neonate after delivery. In children above the age of 6 months the dosage can be calculated on a weight basis up to 5 mg/kg.' Infants are particularly susceptible to methaemoglobinaemia due to lower activity of the enzyme that reduces methaemoglobin (SPC 4.4). Verify against a children's formulary before prescribing.

Dose adjustments

Renal

No numerical renal dose adjustment is given. SPC 4.4: in common with other local anaesthetics, prilocaine hydrochloride should be used cautiously in the elderly, patients in poor health, and patients with liver or kidney damage, if the dose or site of administration is likely to result in high blood levels.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Hypersensitivity to the active substance, to anaesthetics of the amide type, or to any of the excipients
  • Hypersensitivity to methyl and/or propyl parahydroxybenzoate (methyl-/propyl paraben) or to their metabolite para-aminobenzoic acid (PABA) — paraben-containing prilocaine formulations should be avoided in patients allergic to ester local anaesthetics or to PABA
  • Should be avoided in patients with anaemia or congenital or acquired methaemoglobinaemia

Side effects

  • Very common: hypotension and nausea (both occur more frequently after epidural blocks); common vomiting and hypertension
  • Common: paraesthesia and dizziness; uncommon signs and symptoms of CNS toxicity; rare neuropathy and peripheral nerve injury
  • Common bradycardia; rare cardiac arrest and cardiac arrhythmias; respiratory depression (frequency not known)
  • Rare: methaemoglobinaemia and cyanosis (cyanosis in the presence of methaemoglobinaemia)
  • Rare: allergic reactions including urticaria, oedema and dyspnoea, and anaphylactic reactions; diplopia (frequency not known)
  • Acute systemic toxicity from high blood concentrations: a graded CNS response beginning with circumoral paraesthesia, numbness of the tongue, light-headedness, hyperacusis, tinnitus and visual disturbances, progressing through dysarthria, muscular twitching or tremors to generalised convulsions, unconsciousness and cardiovascular collapse

Interactions

  • Class III anti-arrhythmic drugs (e.g. amiodarone) — patients should be under close surveillance and ECG monitoring should be considered, since cardiac effects may be additive (SPC 4.4, cross-referring to 4.5)
  • Drugs known to cause methaemoglobinaemia (e.g. sulphonamides) — methaemoglobinaemia may occur at lower doses of prilocaine in patients receiving such concomitant therapy (SPC 4.4)
  • Section 4.5 (interactions) was not captured in the fetched eMC bundle — check the full interaction list against the SPC before publication

Clinical monograph

How it works

It reversibly blocks voltage-gated sodium channels in nerve membranes, preventing depolarisation and the propagation of action potentials.

Prescribing in practice

  • Excessive doses can cause methaemoglobinaemia through a metabolite, so it is used with particular caution in those susceptible, and methylthioninium chloride is the treatment for significant methaemoglobinaemia.
  • As with all local anaesthetics, inadvertent intravascular injection or overdose can cause systemic central nervous system and cardiac toxicity.
  • It is often regarded as relatively favourable for intravenous regional anaesthesia, but the maximum safe dose must always be calculated for the individual patient.

Monitoring

Monitor for signs of local anaesthetic systemic toxicity and for cyanosis or low oxygen saturations suggesting methaemoglobinaemia.

Counselling the patient

  • Report dizziness, perioral tingling, ringing in the ears or a metallic taste, which can be early signs of toxicity.
  • Bluish discolouration of the lips or skin should be reported immediately.

Evidence & guidelines

Its association with methaemoglobinaemia and its use in regional anaesthesia are well documented in standard anaesthetic references and the SPC.

Reference: AAGBI IV Regional Anaesthesia Guidelines; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Related

Curated clinical cross-links plus same-class fallbacks.