Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2020 Publisher: Sintetica Limited, 30<sup>th</sup> Floor, 40 Bank Street, Canary Wharf, London, E14 5NR, United Kingdom
Prilotekal is indicated in adults for spinal anaesthesia in short term surgical procedures (see section 4.2).
Restricted to hospital use only.
Spinal anaesthesia must only be administered by (or under the supervision of) specialist medical personnel with the necessary knowledge and experience (see section 4.4).
The equipment, drugs and personnel capable of dealing with an emergency, e.g. maintaining the patency of the airways and administering oxygen, must be immediately available, since in rare cases severe reactions, sometimes with a fatal outcome, have been reported after using local anaesthetics, even in the absence of individual hypersensitivity in the patient’s case history.
If signs of acute systemic toxicity or total spinal block are observed, the injection of the local anaesthetic must be stopped immediately (see section 4.4).
Posology must be established on an individual basis in accordance with the characteristics of the specific case. When determining the dose, take into consideration the patient’s physical condition and the concomitant administration of other medicinal products. The lowest possible dose should be chosen.
The duration of action is dose-dependent.
The indications relating to recommended doses are valid in adults of average height and weight (approximately 70 kg) for obtaining an effective block with one single administration. There are wide individual variations with regard to extent and duration of action. The experience of the anaesthetist and knowledge of the patient’s general condition are essential for establishing the dose.
With regard to posology the following guidelines are applied:
| Extension of sensory blockade required T10 | ml | mg | Average duration of action (minutes) |
| 2-3 | 40-60 | Approx. 100-130 |
As a general guideline, the maximum recommended dose is 80 mg of prilocaine hydrochloride (= 4 ml Prilotekal).
The safety and efficacy of Prilotekal in paediatric population have not been established. No data are available.
The use of Prilotekal in children and adolescents is not recommended
The use of Prilotekal in children younger than 6 months is contraindicated (see section 4.3).
It is advisable to reduce the dose in patients in a compromised general condition. In addition, in patients 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.
Due to the glucose content Takipril is only to be used for spinal anaesthesia. It is not recommended for the use in epidural anaesthesia
Inject Prilotekal via intrathecal route into the intervertebral space L2/L3, L3/L4 and L4/L5.
Administer the injection slowly, after having aspirated a minimum quantity of CSF to confirm the correct position and check the patient’s vital functions extremely carefully maintaining continuous verbal contact.
If signs of acute systemic toxicity or total spinal block are observed, the injection of the local anaesthetic must be stopped immediately (see section 4.4).
If the patient is in a seated position, the injected solution diffuses mainly in a caudal direction (in the direction of the sacrum); if the patient is lying down, the anaesthetic diffuses by gravity according to the patient’s position (Trendelenburg and anti-Trendelenburg).
By means of the excipient glucose, the density of Prilotekal is 1.026 g/g at 20°C, equivalent to 1.021 g/g at 37°C.
It is unlikely that Prilotekal, at the recommended posology, will induce plasma levels capable of inducing 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:
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.
The following measures must be taken immediately:
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 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.
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.
3 years.
The medicinal product has to be used immediately after first opening.
Do not store above 25°C.
Do not refrigerate or freeze.
Store in original package in order to protect from light.
Type I clear colourless glass ampoule.
Box of 10 ampoules each containing 5 ml of solution for injection.
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.
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