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Amide LA + vasopressin analogue Pregnancy: Section 4.6: although there is no evidence of harm to the foetus, as with all drugs it should not be given in early pregnancy unless the benefits are considered to outweigh the risks. Prilocaine enters the mother's milk, but there is generally no risk of effects on the infant at recommended doses.

Prilocaine with felypressin

Brand names: Citanest with Octapressin

This is a dental local anaesthetic combining the amide anaesthetic prilocaine with the vasoconstrictor felypressin, used for infiltration and nerve-block anaesthesia in dentistry.

Adult dose

Dose: Dental local anaesthesia (dental infiltration and all dental nerve block techniques): in normal healthy adults the usual dose is 1-5 ml of the 3% prilocaine with felypressin 0.54 micrograms/ml solution.
Route: Dental infiltration and dental nerve block (injection) - the only uses covered by this SPC
Frequency: Single dose as required for the dental procedure; the SPC gives no repeat-dose interval
Max: 10 ml (SPC: 'A dose of 10 ml (5 cartridges) of Citanest with Octapressin Dental should not be exceeded.')
Strength (SPC section 2): each ml contains prilocaine hydrochloride 30 mg (3%) and felypressin 0.54 micrograms; each 2.2 ml cartridge contains 66 mg prilocaine hydrochloride and 1.19 micrograms felypressin. Indication (section 4.1): 'a local anaesthetic solution for use in dental infiltration and all dental nerve block techniques' - this is a DENTAL product; the SPC does not cover non-dental infiltration, and none is dosed here. Elderly or debilitated patients require smaller doses (no figure given). FLAG: the SPC's own ceiling reads '10 ml (5 cartridges)' while its cartridges are 2.2 ml (section 2), so five whole cartridges would exceed 10 ml; the ceiling printed in ml (10 ml) is the figure stated here. Great caution to avoid accidental intravascular injection (section 4.4); facilities for resuscitation should be available. Methaemoglobinaemia is dose-related; clinically significant levels may occur when doses of prilocaine exceed 600 mg (section 4.8). Section 7 (marketing authorisation holder) is absent from the bundle's parsed sections; DENTSPLY Limited was read from section 7 of the same MHRA PDF (docId 389148ae705784256c16a694b918aa7b709d8514), where the licence prints as PL 04690/0028.

Paediatric dose

Dose: Children under 10 years of age: approximately 1-2 ml of the 3% prilocaine with felypressin 0.54 micrograms/ml solution (dental local anaesthesia).
Route: Dental infiltration and dental nerve block (injection)
Frequency: Single dose as required for the dental procedure
As printed in SPC section 4.2: 'Children under 10 years of age require approximately 1 -2 ml.' The SPC gives no figure for children aged 10 and over and none for infants. Infants are particularly susceptible to methaemoglobinaemia due to lower activity of the enzyme that reduces methaemoglobin to haemoglobin (section 4.8).

Dose adjustments

Renal

No numerical renal adjustment. Section 4.4: use cautiously in patients with liver or kidney damage if the dose or site of administration is likely to result in high blood levels.

Hepatic

No numerical hepatic adjustment. Section 4.4: use cautiously in patients with liver or kidney damage if the dose or site of administration is likely to result in high blood levels.

Dose independently re-sourced from UK Summary of Product Characteristics (SPC) via MHRA Products — clinician-reviewed. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

  • Known hypersensitivity to anaesthetics of the amide type or to any other component of the solution (section 4.3)
  • Should be avoided in patients with anaemia or congenital or acquired methaemoglobinaemia (section 4.3)
  • Local anaesthetics should be avoided when there is inflammation in the region of the proposed injection (section 4.4)

Side effects

  • Adverse reactions are extremely rare in dental practice and are usually the result of excessively high blood concentrations from inadvertent intravascular injection, excessive dosage, rapid absorption, or hypersensitivity/idiosyncrasy (section 4.8)
  • CNS reactions: nervousness, dizziness, blurred vision and tremors, followed by drowsiness, convulsions, unconsciousness and possibly respiratory arrest (section 4.8)
  • Cardiovascular reactions (depressant): hypotension, myocardial depression, bradycardia and possible cardiac arrest (section 4.8)
  • Allergic reactions are extremely rare: cutaneous lesions, urticaria, oedema or anaphylactoid reactions (section 4.8)
  • Methaemoglobinaemia in a dose-related fashion, with cyanosis; treatable with intravenous methylene blue 1% solution at 1 mg/kg over 5 minutes (section 4.8)
  • Accidental intravascular injection may give rapid onset of toxicity with restlessness, twitching or convulsions, followed by coma with apnoea and cardiovascular collapse (section 4.4)

Interactions

  • Sulphonamides (e.g. co-trimoxazole) - increased risk of methaemoglobinaemia (section 4.5)
  • The vasopressor properties of felypressin (Octapressin) should be borne in mind (section 4.5)
  • Other local anaesthetics or agents structurally related to amide-type anaesthetics - use prilocaine with caution since toxic effects are additive (section 4.5)

Monitoring

  • Resuscitation facilities available whenever local anaesthetics are administered (section 4.4)
  • Cyanosis/methaemoglobinaemia, particularly in anaemia, haemoglobinopathy, concomitant sulphonamide therapy and infants (section 4.8)
  • Caution in the elderly, patients in poor health, epilepsy, severe or untreated hypertension, impaired cardiac conduction, severe heart disease, impaired respiratory function (section 4.4)

Clinical monograph

How it works

Prilocaine blocks neuronal sodium channels to produce local anaesthesia, while felypressin (a vasopressin analogue) causes local vasoconstriction that prolongs anaesthesia and reduces systemic absorption and bleeding.

Prescribing in practice

  • As with prilocaine generally, excessive doses risk methaemoglobinaemia, so observe maximum recommended quantities and avoid in patients prone to methaemoglobinaemia.
  • Felypressin can cause coronary and other vasoconstriction, so use with caution in severe ischaemic heart disease; it is a preferred adrenaline-free alternative when catecholamine-related effects are a concern.
  • Caution is advised in pregnancy because felypressin has theoretical oxytocic-like activity at high doses.

Monitoring

Observe for systemic local anaesthetic effects and cyanosis suggesting methaemoglobinaemia, particularly if repeated injections are needed.

Counselling the patient

  • Explain the area will be numb for a while and to avoid biting the lip, cheek or tongue or taking hot food until sensation returns.
  • Report any dizziness, palpitations or unusual blue discolouration of the lips or skin.

Evidence & guidelines

Prilocaine with felypressin is an established dental anaesthetic option, valued where an adrenaline-containing preparation is best avoided.

Reference: 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.

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