Patient leaflet - Prilotekal
1. What Prilotekal is and what it is used for
Prilotekal 20 mg/ml solution for injection is a type of medicine called local anaesthetic, belonging to the category of the amides, contains a medicine called prilocaine hydrochloride and is a solution for injection. Prilotekal solution for injection is used to anaesthetise (numb) specific parts of the body and prevent pain during surgery in adults.
Prilotekal is injected into lower part of your spine. This quickly stops pain from your waist down for a limited period of time (short term surgical procedures).
2. What you need to know before Prilotekal is given to you
You must not be given Prilotekal
- if you are allergic (hypersensitive) to prilocaine hydrochloride, other amide-type local anaesthetics or any of the other ingredients in this medicine (listed in section 6)
- if you have serious problems with cardiac conduction,
- if you suffer from severe anaemia,
- if you have a decompensated cardiac insufficiency,
- if you have cardiogenic and hypovolemic shock,
- if you suffer from congenital or acquired methemoglobinemia
- if you have general or specific contraindications for the technique of subarachnoid anaesthesia
You must not be given Prilotekal in a blood vessel. Prilotekal must not be used in children younger than 6 months.
Warning and Precautions
If you suffer from any of these, you should discuss it with your doctor before being given this medicine
- if you have ever had a bad reaction to an anaesthetic in the past,
- if you have a skin infection at or near the proposed site of the injection,
if you are suffering from any of the following:
- diseases of the central nervous system such as meningitis, polio and problems with your spinal cord due to anaemia, - a severe headache,
- brain, spine or any other tumours,
tuberculosis of the spine,
- recent trauma to your spine,
- very low blood pressure or low blood volume, - problems with clotting of your blood,
- acute porphyria
- fluid in your lungs,
- septicaemia (blood poisoning),
- if you have a heart condition (e.g. total or partial heart block, cardiac decompensation, arrhythmia).
- if you have any liver or kidney problems,
- if you suffer from neurological or neuromuscular disorders, such as multiple sclerosis, hemiplegia, paraplegia or neuromuscular disorders.
- if you are in reduced general condition.
Spinal anaesthesia must only be administered by a doctor with the necessary knowledge and experience. The doctor in charge is responsible for taking the measures needed to avoid injection in a blood vessel and to know how to recognize and treat undesirable effects.
Children and adolescents
Prilotekal is not recommended for the use in children and adolescents. The safety and efficacy of Prilotekal in paediatric population have not been established. No data are available. The use of Prilotekal in children younger than 6 months is contraindicated due to a higher risk of developing methemoglobinemia.
Other medicines and Prilotekal
Tell your doctor if you are taking, have recently taken or might take any other medicines, including medicines obtained without a prescription. In particular if you are taking any medicines for an irregular heartbeat (class III antiarrhythmics agents) and for pain relief.
Pregnancy and breast-feeding
If you are pregnant or breast feeding, think you may be pregnant or are planning to have a baby, ask your doctor who will decide whether or not you should be given Priolotekal. Prilocaine should not be administered for local or regional anaesthesia during childbirth.
It is not known whether prilocaine passes into breast milk. Breast-feeding can be resumed approximately 24 hours after treatment.
Driving and using machines
Do not drive and do not use any tools or machines as Prilotekal may temporarily interfere with your reactions and muscular coordination.
Prilotekal contains sodium
This medicine contains less than 1 mmol sodium (23 mg) per dose (maximum dose equal to 4 ml of Prilotekal solution for injection), that is to say essentially “sodium-free”.
3. How to use Prilotekal
This medicine will be given to you by your doctor who will decide what dose is right for you. The usual dose in adults is 40-60 mg of prilocaine hydrochloride (2-3 ml of Prilotekal); the maximal dose is 80 mg of prilocaine hydrochloride (4 ml of Prilotekal).
The doctor will give you Prilotekal into the lower part of your spine while you are in a seated position or lying down. Prilotekal is not recommended for use in children and adolescents. The safety and efficacy of Prilotekal in paediatric population have not been established. The use of Prilotekal in children younger than 6 months is contraindicated due to a higher risk of developing methemoglobinemia.
20 mg/ml solution for injection
20 mg/ml
solution for injection
20 mg/ml
solution for injection
| System Organ Class | Frequency | Undesirable Effect |
| Nervous system Disorders | Common | Paresthesia, Dizziness |
| Uncommon | Signs and symptoms of CNS toxicity (convulsions, circumoral paresthesia, loss of consciousness, shaking, feeling of numbness affecting the tongue, speech problems, hearing problems, tinnitus, visual problems) | |
| Rare | Arachnoiditis, Neuropathy, Lesions of peripheral nerves | |
| Eye disorders | Rare | Diplopia |
| Cardiac disorders | Uncommon | Bradycardia |
| Rare | Cardiac arrest, Arrhythmia | |
| Vascular disorders | Very common | Hypotension |
| Uncommon | Hypertension | |
| Respiratory, thoracic and mediastinal disorders | Rare | Respiratory depression |
| Musculoskeletal and connective tissue disorders | Uncommon | Back pain, temporary muscle weakness |
| Gastrointestinal disorders | Very common | Nausea |
| Common | Vomiting |
The signs of intoxication from local anaesthetics are similar for any injected preparation, both in the way in which they manifest, and in their treatment. In spite of the demonstrated high clinical tolerability of Prilotekal, undesirable toxic effects cannot be excluded in the presence of plasma levels above a critical threshold. These undesirable effects mainly manifest as symptoms affecting the central nervous and cardiovascular system.
The most effective prophylactic measures are scrupulous compliance with the recommended posology for Prilotekal, with it being essential for the doctor to check its action (visual and verbal contact with the patient), as well as careful aspiration prior to injecting the solution.
Mild undesirable effects (feeling dizzy or dazed) can be attributed to moderate overdose and generally resolve rapidly after reducing the dose or halting administration of Prilotekal.
Serious undesirable effects are attributable to significant overdose and/or accidental injection of local aesthetic into a blood vessel. They manifest as symptoms affecting the central nervous system (restlessness, speech problems, disorientation, dizziness, muscle contractions, cramps, vomiting, loss of consciousness, respiratory arrest and mydriasis) and the cardiocirculatory system (raised arterial pressure and pulse frequency, arrhythmia, drop in arterial pressure, asystole) following irritation and/or depression of the cerebral cortex and the cerebral marrow (see section 4.9). In addition, following inhibition or block of the cardiac conduction system, cardiac frequency may slow down and myocardial depression may occur. Any problems relating to metabolism (liver) or excretion (kidney) of Prilotekal should also be considered as other possible causes of undesirable effects. Reporting of suspected adverse reactions:
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard
4.9 Overdose
It is unlikely that Prilotekal, at the recommended posology, will induce plasma levels capable of inducing systemic toxicity.
Acute systemic toxicity
Systemic undesirable effects, which may occur in the presence of plasma levels of more than 5-10 micrograms of prilocaine/ml, are iatrogenic, pharmacodynamic or pharmacokinetic origin and concern the central nervous system and the cardiocirculatory system. Iatrogenic undesirable effects occur due to:
- injection of an excessive quantity of solution
- accidental injection into a vessel
- incorrect patient position
- high spinal anaesthesia (marked drop in arterial pressure)
In the case of accidental intravenous administration, the toxic effect occurs within 1-3 minutes. On the contrary, in the case of overdose maximum plasma concentrations are only reached after 20-30 minutes, depending on the injection site, and the onset of signs of toxicity is delayed.
Signs of overdose can be classified into two different sets of symptoms which differ in terms of quality and intensity:
- a) Symptoms affecting the central nervous system
Generally, the first symptoms are paresthesia in the mouth area, feeling of numbness of the tongue, feeling dazed, problems with hearing and tinnitus. Visual problems and muscle contractions are more severe and precede a generalized convulsion. These signs must not be erroneously mistaken for neurotic behaviour. Subsequently loss of consciousness and tonic-clonic seizure may occur, generally lasting between a few
seconds and a few minutes. The convulsions are immediately followed by hypoxia and increased levels of carbon dioxide in the blood (hypercapnia), attributable to increased muscular activity associated with respiratory problems. In serious cases respiratory arrest may occur. Acidosis potentiates the toxic effects of local anaesthetics.
The reduction or improvement of symptoms affecting the central nervous system can be attributed to the redistribution of local anaesthetics outside the CNS, with its consequent metabolism and excretion. Regression may be rapid, unless enormous quantities have been used.
- b) Cardiovascular symptoms
In serious cases cardiovascular toxicity may occur. Hypotension, bradycardia, arrhythmia and also cardiac arrest may occur in the presence of a high systemic concentration of local anaesthetics.
The first signs of toxic symptoms affecting the central nervous system generally precede toxic cardiovascular effects. This statement does not apply if the patient is under general anaesthesia or heavily sedated with medicinal products such as benzodiazepine or barbiturates.
Management of acute systemic toxicity
The following measures must be taken immediately:
- Stop administration of Prilotekal.
- Ensure an adequate supply of oxygen: keep the airways clear, administer O2, artificial ventilation (intubation) if required.
In the event of cardiovascular depression circulation must be stabilized. If convulsions occur and do not resolve spontaneously after 15-20 seconds, the administration of an intravenous anticonvulsant is recommended. Analeptics with a central action are contraindicated in the case of intoxication caused by local anaesthetics!
In the event of serious complications, when treating the patient it is advisable to obtain the assistance of a doctor specializing in emergency medicine and resuscitation (e.g. anaesthetist).
Methemoglobinemia
Methemoglobinemia may follow the administration of prilocaine. Prilotekal is contraindicated for techniques of regional anaesthesia requiring continuous administration. The doses used in subarachnoid anaesthesia do not induce blood levels capable of inducing methemoglobinemia, which occurs if the quantity of prilocaine hydrochloride administered is equal to or higher than 600 mg. There is a metabolite of prilocaine, o-toluidine, which can induce methemoglobin formation. In general, methemoglobin formation is clinically negligible, except in cases of extremely severe anaemia and high grade cardiac decompensation. Patients with severe anaemia may develop hypoxia. It is important to exclude other serious causes of cyanosis, e.g. acute hypoxia and/or cardiac insufficiency.
Management of methemoglobinemia
Proven methemoglobinemia resolves 15 minutes after the i.v. injection of 2-4 mg/kg body weight of toluidine blue.
Additional information:
Even low concentrations of methemoglobin can alter measurements of pulsoxymetria.
- 5. PHARMACOLOGICAL PROPERTIES
5.1 Pharmacodynamic properties
Pharmacotherapeutic group: anaesthetics, local; amides
ATC code: N01BB04
Mechanism of action: Prilocaine is an amide-type local anaesthetic. Prilocaine inhibits the function of the excitable structures (e.g. all types of nerve fibres [sensory, motor, autonomous nerve fibres]).
Pharmacodynamic effects: Prilocaine inhibits the excitability of sensory pain receptors and the conductivity of the sensory nerve fibres, at local level and in a reversible way, reducing the perception of pain and, subsequently, that of cold, heat, touch and pressure.
Clinical efficacy and safety.
Prilocaine reduces membrane permeability to sodium. This reduces the excitability of the nerve fibres in accordance with its concentration, through reducing the sudden peak sodium permeability, needed to form the potential for action. The effect depends on the pH of the substance and the pH of the environment. The local aesthetic effect is due to the protonated form. In inflamed tissues, the effect of the local anaesthetics is lower because of the lower pH of the environment.
5.2 Pharmacokinetic properties
Absorption and Distribution
The plasma concentration should be negligible for intrathecal use. Biotransformation and Elimination
The plasma protein binding is approximately 55%.
The bioavailability of prilocaine at the application site is 100%.
The principal metabolites of prilocaine are o-toluidine and N-n-propylalanine, both produced in the liver and kidneys by amidases. o-Toluidine undergoes extensive hydrolytic metabolism in vivo, with the bulk of the dose being excreted in the urine within 24 h. Like other aromatic amines, it is thought to undergo metabolic activation initially via N-hydroxylation, leading to covalent binding to tissue macromolecules. o-Toluidine is potent oxidant of the ferric iron of hemoglobin.
The terminal elimination half-life of prilocaine is 1.6 hours.
5.3 Preclinical safety data
The therapeutic dose used locally in humans is close to the dose which is toxic in animals after intravenous administration. In animals, signs of acute toxicity are reduced activity, convulsions, dyspnea, cyanosis and death on account of cardiac insufficiency.
The subcutaneous injection of 3 ml/kg of body weight of prilocaine hydrochloride induced reversible local necrosis in the rat. At the same posology no damaging effects were observed in the monkey.
The administration of 60 mg/kg body weight of prilocaine for 5 days a week for 7 weeks induced slight weight loss in the rat.
In mutagenesis tests, prilocaine did not demonstrate any mutagenic effects. The indices for a potential mutagen are based on knowledge relating to the metabolite o-toluidine, which caused genetic damage and cell proliferation (chromosome mutations, aneuploidy, DNA repair, cell conversion) in various tests in vitro. In carcinogenicity studies performed in the rat and the mouse with high doses of the metabolite o-toluidine, an increase in the frequency of tumours of the spleen and the bladder were observed.
Neither of the results seem significant for humans in the case of the therapeutic short-term use of prilocaine; nevertheless, for safety reasons avoiding the administration of high doses over prolonged periods is recommended. Prilocaine has no effect on the fertility of male and female rats. However, the postnatal survival of the offspring of treated females was reduced. In one study on embryotoxicity in the rat lethal effects on the foetus were observed, and dose-dependent hydronephrosis occurred in the foetuses.
- 6. PHARMACEUTICAL PARTICULARS
6.1 List of excipients
Glucose anhydrous or glucose monohydrate
Sodium hydroxide 1N (for pH adjustment)
Water for injection
6.2 Incompatibilities
Not applicable.
6.3 Shelf life
3 years
The medicinal product has to be used immediately after first opening.
6.4 Special precautions for storage
Do not store above 25°C.
Do not refrigerate or freeze.
Store in original package in order to protect from light.
6.5 Nature and contents of container
Type I clear colourless glass ampoule
Box of 10 ampoules each containing 5 ml of solution for injection
6.6 Special precautions for disposal
5 ml ampoules of solution for injection are exclusively single - use. Any remaining product must be disposed of.
The medicinal product has to be visually inspected prior to use. Only clear solutions practically free from particles should be used.
- 7. MARKETING AUTHORISATION HOLDER
Suite 3, Middlesex House
Rutherford Close
Stevenage, Hertfordshire
SG1 2EF, UK
- 8. MARKETING AUTHORISATION NUMBER(S)
PL 46926/0002
- 9. DATE OF FIRST AUTHORISATION/RENEWAL OF THE AUTHORISATION
27/01/2017
- 10. DATE OF REVISION OF THE TEXT
For patients in a compromised general condition and with established concomitant disorders (e.g. vascular occlusion, arteriosclerosis, diabetic polyneuropathy), a reduced dose is indicated.
In the case of compromised liver or kidney function a lower dosage range is recommended.
Prilotekal is injected via spinal route.
Equipment, drugs and personnel capable of dealing with an emergency, must be immediately available. Rare cases of severe reactions have been reported after using local anaesthetics, even in the absence of individual hypersensitivity in the patient’s case history.
If you have been given too much Prilotekal
The doctor giving you Prilotekal will be experienced in the use of spinal local anaesthetics, so it is unlikely that you will be given an overdose. However, if the dose is accidently injected directly into blood, you may develop problems for a short time with your sight or hearing, twitching of your muscles, tremors, trembling, fits (seizures), and loss of consciousness. Whenever you are given Prilotekal, equipment will be available to care for you if an overdose happens.
If you have any further questions on the use of this product, ask your doctor or pharmacist.
4. Possible side effects
Like all medicines, Prilotekal can cause side effects, although not everybody gets them.
As with all local anaesthetics, a drop in arterial pressure may occur and cardiac frequency may decrease.
You may feel sick, have lowered blood pressure or a slow heart beat. Other possible effects are headache after surgery, vomiting and difficulty in passing urine.
These are the possible side effects:
Very common: may affect more than 1 in 10 people
Lowered blood pressure, feeling sick (nausea)
Common: may affect up to 1 in 10 people
Paresthesia, dizziness, vomiting
Uncommon: may affect up to 1 in 100 people
Convulsions, circumoral paresthesia, loss of consciousness, shaking, feeling of numbness affecting the tongue, speech problems, hearing problems, tinnitus, visual problems, back pain, temporary muscle weakness. Slow heart beat, elevated blood pressure.
Rare: may affect up to 1 in 1,000 people
Methemoglobinemia, cyanosis. Anaphylactic shock, anaphylactic reactions, allergic reactions, itching. Arachnoiditis, neuropathy, lesions of peripheral nerves.
Diplopia. Cardiac arrest, irregular heartbeat. Respiratory depression.
Prilotekal solution for injection is unlikely to cause serious side effects unless it is accidentally injected in the wrong way or used together with other local anaesthetics. If this happens, numbness of the tongue, light-headedness, dizziness, shakiness and fits may occur. In extremely rare cases, prilocaine has been associated with heart attack, breathing difficulties, loss of feeling in your lower body and allergic reactions, which may cause rashes, swelling or very low blood pressure.
A rare, but serious undesiderable effects of spinal anaesthesia is a high or total spinal block, with consequent cardiovascular and respiratory depression.
Reporting of side effects:
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. You can also report side effects directly via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard
By reporting side effects you can help provide more information on the safety of this medicine.
5. How to store Prilotekal
Keep out of the reach and sight of children.
Do not use Prilotekal after the expiry date which is stated on the ampoules and the outer carton. The expiry date refers to the last day of that month.
Do not store Prilotekal above 25°C. Do not refrigerate or freeze. Store in original package in order to protect from light. Use immediately after first opening.
Do not use Prilotekal if you notice that the solution is not clear and free from particles.
Any remaining product must be disposed of. As it is limited to hospital use the waste drug elimination is carried out directly by the hospital. These measures will help to protect the environment.
6. Contents of the pack and other information
What Prilotekal contains:
The active substance is prilocaine hydrochloride. 1 ml of solution for injection contains 20 mg of prilocaine hydrochloride (equivalent to 2%).
1 ampoule with 5 ml solution, contains 100 mg of prilocaine hydrochloride.
The other ingredients are:
Glucose anhydrous or glucose monohydrate
Sodium hydroxide 1N (for pH adjustment)
Water for injection
What Prilotekal looks like and contents of the pack
Solution for injection. Clear, colourless solution.
Prilotekal comes in Type I clear colourless glass ampoules. Box of 10 ampoules each containing 5 ml of solution for injection
Marketing Authorisation Holder and Manufacturer:
Marketing Authorisation Holder
Sintetica Limited
Suite 3, Middlesex House
Rutherford Close
Stevenage, Hertfordshire
SG1 2EF, UK
Manufacturer:
Sintetica GmbH
Albersloher Weg 11
48155 - Münster
Germany
This leaflet was last revised in December 2022
The following information is intended for medical and healthcare professionals only:
The SPC is added at the end of the printed PL as a tear-off section.