Xylocaine

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Xylocaine on Prescriptsy

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Xylocaine is the original brand name for lidocaine (also known as lignocaine), a local anaesthetic and class IB antiarrhythmic agent manufactured by Aspen (formerly AstraZeneca).

Lidocaine is one of the most widely used local anaesthetics in clinical practice worldwide.

Xylocaine is available in multiple formulations including injectable solutions (0.5%, 1%, 2%), topical gel (2%), spray (10%), ointment (5%), and combinations with adrenaline (epinephrine) for prolonged local anaesthesia.

It is used to produce numbness in specific body areas for medical, surgical, and dental procedures by blocking nerve signal transmission.

Xylocaine is a prescription-only medicine (POM) in the United Kingdom.

Local anaesthesia is fundamental to modern medical and dental practice, enabling pain-free procedures from minor skin biopsies to complex regional nerve blocks.

Lidocaine was first synthesised in 1943 by Nils Lofgren and Bengt Lundqvist at the University of Stockholm and introduced into clinical practice in 1948.

It was the first amide-type local anaesthetic, replacing the ester-type agents (such as procaine and cocaine) that were associated with higher rates of allergic reactions and shorter durations of action.

Lidocaine remains the gold-standard comparator against which newer local anaesthetics are measured.

This page provides a comprehensive clinical guide to Xylocaine, covering its mechanism of action, formulations, dosage, side effects, safety warnings, and availability in the United Kingdom.

Important safety information about Xylocaine

Before reading further, note these essential safety points about Xylocaine.

• Maximum dose limits must be strictly observed. The maximum single dose of lidocaine without adrenaline is 200 mg (3 mg/kg); with adrenaline, 500 mg (7 mg/kg).
• Adrenaline-containing formulations must not be used on end-arteries (fingers, toes, nose, ears, penis).
• Resuscitation equipment including lipid emulsion (Intralipid 20%) must be immediately available when local anaesthetics are administered by injection.
• Signs of systemic toxicity include perioral numbness, tinnitus, dizziness, visual disturbance, confusion, muscle twitching, and seizures.
• True allergy to lidocaine is extremely rare (less than 1 in 10,000 exposures).

Understanding local anaesthesia

Local anaesthesia produces reversible loss of sensation in a defined body region without loss of consciousness.

It works by blocking the transmission of nerve impulses along peripheral nerve fibres from the site of the procedure to the brain.

Pain signals are carried by small-diameter, thinly myelinated (A-delta) and unmyelinated (C) nerve fibres.

Touch and pressure are carried by larger A-beta fibres, and motor function by large, heavily myelinated A-alpha fibres.

Local anaesthetics preferentially block the smaller fibres first, producing a characteristic pattern of differential blockade where pain sensation is lost before touch, proprioception, and motor function.

Local anaesthetic techniques include topical application (to skin or mucous membranes), local infiltration (injection directly around the operative site), field block (injection around the operative field), peripheral nerve block (injection near a specific nerve or nerve plexus), neuraxial block (spinal or epidural injection), and intravenous regional anaesthesia (Bier's block).

The choice of technique depends on the type and location of the procedure, the duration of anaesthesia required, and patient factors.

How Xylocaine works

Lidocaine blocks voltage-gated sodium channels in the cell membranes of neurons.

These channels are transmembrane proteins that open in response to membrane depolarisation, allowing a rapid influx of sodium ions that propagates the action potential along the nerve fibre.

Lidocaine exists in equilibrium between an uncharged base form (which crosses the cell membrane) and a charged cationic form (which binds to the intracellular portion of the sodium channel).

The molecule binds preferentially to sodium channels in their open or inactivated states, stabilising them in the inactivated conformation and preventing further depolarisation.

This is described as use-dependent or frequency-dependent blockade: nerves that are firing rapidly (as pain fibres do during a painful stimulus) are blocked more effectively than resting nerves.

The amide linkage in lidocaine's molecular structure (diethylaminoacetyl-2,6-xylidide) distinguishes it from ester-type local anaesthetics (which have an ester linkage) and determines its metabolism.

Amide-type agents are metabolised by hepatic microsomal enzymes (primarily CYP1A2 and CYP3A4) rather than by plasma cholinesterases that metabolise ester-type agents.

This gives amide-type agents a more predictable duration of action and a much lower incidence of allergic reactions, since ester hydrolysis produces para-aminobenzoic acid (PABA), a known allergen.

Lidocaine has a pKa of 7.9, which means that at physiological pH (7.4), approximately 25% exists in the uncharged base form and 75% in the charged cationic form.

The relatively high proportion of uncharged base at physiological pH accounts for lidocaine's rapid onset of action (1 to 5 minutes for infiltration) compared with agents with higher pKa values such as bupivacaine (pKa 8.1).

In infected or inflamed tissue (where pH is lower, around 6.5 to 7.0), a greater proportion of the drug is ionised, reducing membrane penetration and explaining why local anaesthetics are less effective in infected tissue.

Xylocaine formulations available in the UK

Injectable formulations

Xylocaine is available as 0.5%, 1%, and 2% solutions for injection, with and without adrenaline (epinephrine) 1:200,000.

The 0.5% solution (5 mg/mL) is used for large-volume infiltration where a lower concentration is sufficient.

The 1% solution (10 mg/mL) is the most commonly used concentration for infiltration anaesthesia and minor nerve blocks.

The 2% solution (20 mg/mL) is used for nerve blocks requiring a smaller volume of higher concentration, including dental nerve blocks.

Adrenaline-containing formulations cause local vasoconstriction, slowing systemic absorption, prolonging duration of action by 50 to 100%, and reducing bleeding at the operative site.

Topical formulations

Xylocaine Gel 2% (20 mg/mL) contains lidocaine in a water-soluble gel base, used for urethral catheterisation, cystoscopy, and other urological procedures.

Xylocaine 10% Spray delivers approximately 10 mg lidocaine per metered actuation, used for oropharyngeal and nasopharyngeal procedures including endoscopy, intubation, and dental procedures.

Xylocaine Ointment 5% is used for anaesthesia of accessible mucous membranes including the mouth, pharynx, and anogenital region.

EMLA cream (lidocaine 2.5% with prilocaine 2.5%) is a related product for intact skin anaesthesia before venepuncture, cannulation, and minor skin procedures.

Clinical applications of Xylocaine

Dental anaesthesia is the single most common application of lidocaine worldwide.

Inferior alveolar nerve block with lidocaine 2% with adrenaline 1:80,000 (supplied as dental cartridges) provides anaesthesia of the lower teeth, lower lip, and chin for dental procedures including fillings, extractions, and root canal treatment.

Infiltration anaesthesia with lidocaine is used for upper dental procedures and soft tissue surgery in the mouth.

Minor surgical procedures in primary and secondary care frequently use lidocaine infiltration: excision of skin lesions (moles, cysts, lipomas), wound suturing, incision and drainage of abscesses, nail surgery (wedge resection for ingrowing toenails using ring block), joint aspiration, and biopsy procedures.

Emergency medicine applications include wound exploration and repair, fracture manipulation under haematoma block, and chest drain insertion.

Lidocaine is also used intravenously as a class IB antiarrhythmic agent for the acute management of ventricular tachycardia and ventricular fibrillation, although amiodarone is now preferred in most UK resuscitation protocols.

Intravenous lidocaine infusion is increasingly used as an adjunct analgesic in perioperative pain management, particularly for abdominal surgery, where it has opioid-sparing effects.

Side effects of Xylocaine

Local side effects

Injection site pain is common but transient. Bruising, swelling, and temporary sensory disturbance beyond the intended area occur occasionally.

Tissue damage from inadvertent intraneural injection is rare with proper technique.

Nerve injury from needle trauma or compression by haematoma may cause prolonged numbness, paraesthesia, or neuropathic pain; this is uncommon and usually resolves within weeks to months.

Systemic toxicity

Local anaesthetic systemic toxicity (LAST) is the most serious adverse effect and results from excessive plasma lidocaine concentrations.

The toxic plasma threshold for lidocaine is approximately 5 micrograms/mL, with a therapeutic antiarrhythmic range of 1.5 to 5 micrograms/mL. CNS toxicity precedes cardiovascular toxicity in most cases.

Early CNS symptoms include perioral and tongue numbness, metallic taste, light-headedness, tinnitus, and visual disturbance. Progressive toxicity produces drowsiness, confusion, muscle twitching, tremor, and generalised seizures.

Cardiovascular toxicity manifests as bradycardia, conduction block, hypotension, and at very high levels, ventricular arrhythmias and cardiac arrest.

The treatment of LAST includes stopping the injection, calling for help, managing the airway, treating seizures with benzodiazepines, and administering intravenous lipid emulsion (Intralipid 20%) as per the Association of Anaesthetists guidelines.

Allergic reactions

True immunoglobulin E-mediated allergy to amide-type local anaesthetics is extremely rare, estimated at less than 1 in 10,000 exposures.

Most reported reactions are vasovagal syncope (fainting from needle phobia or anxiety), psychogenic reactions, reactions to the adrenaline component (tachycardia, palpitations, tremor), or reactions to preservatives such as methylparaben or metabisulphite.

If genuine allergy is suspected, referral to an allergy clinic for skin prick testing and intradermal testing is recommended before future procedures.

Warnings and precautions

Maximum dose limits

Strict adherence to maximum dose limits is essential. For lidocaine without adrenaline: 200 mg (3 mg/kg) as a single dose.

For lidocaine with adrenaline: 500 mg (7 mg/kg) as a single dose.

Lower doses apply in elderly patients, paediatric patients, patients with hepatic impairment, patients with cardiac failure (reduced hepatic blood flow), and debilitated patients.

When multiple sites are infiltrated, the total dose across all sites must not exceed the maximum.

Resuscitation readiness

Whenever local anaesthetics are administered by injection, facilities for resuscitation must be immediately available.

This includes high-flow oxygen, suction, bag-valve-mask ventilation, oropharyngeal and nasopharyngeal airways, intravenous access, and Intralipid 20% (lipid emulsion) with dosing guidance readily accessible.

The Association of Anaesthetists of Great Britain and Ireland provides detailed guidance on the management of LAST.

Special populations

Hepatic impairment: lidocaine is extensively metabolised by the liver. Patients with severe hepatic dysfunction have significantly prolonged half-life and reduced clearance, requiring dose reduction.

Cardiac failure: reduced cardiac output decreases hepatic blood flow and lidocaine clearance. Epilepsy: lidocaine lowers the seizure threshold and should be used with caution.

Myasthenia gravis: lidocaine may exacerbate muscle weakness. Pregnancy: lidocaine crosses the placenta but is widely used during pregnancy at appropriate doses.

Breastfeeding: lidocaine is excreted in breast milk in small amounts and is considered compatible with breastfeeding.

How to get Xylocaine in the UK

Xylocaine is a prescription-only medicine in the UK.

Injectable formulations are administered by healthcare professionals (doctors, dentists, nurse practitioners) in clinical settings and are not dispensed for home use.

Topical formulations (gel, spray, ointment) can be prescribed by your GP, dentist, or specialist.

The standard NHS prescription charge in England is 9.90 pounds per item; prescriptions are free in Scotland, Wales, and Northern Ireland.

Generic lidocaine products are widely available and bioequivalent to branded Xylocaine.

Sources

• Xylocaine 1%, Summary of Product Characteristics (EMC)
• Lidocaine hydrochloride, British National Formulary (BNF)
• Management of Severe Local Anaesthetic Toxicity, Association of Anaesthetists
• Lidocaine, NHS
• MHRA Yellow Card Scheme