Generality
Procaine is an active ingredient with local anesthetic action .
From the chemical point of view, procaine is an amino ester derived from para-aminobenzoic acid.
In the past, procaine was part of the composition of pharmaceutical formulations suitable for both parenteral and topical administration. However, to date (January 2019), commercially available procaine medicines are only for topical use (skin cream, ear drops, dental solution and odontological drops). These medicines are classified as over-the -counter (OTC) drugs, therefore, their free sale in pharmacies and parapharmacies is allowed.
In the drugs that contain it, procaine is normally present in the form of procaine hydrochloride and in some of them it is found in association with other active ingredients, such as phenazone (with anti-inflammatory action), benzocaine (also endowed with anesthetic action ) and 8-oxyquinoline sulphate (with antiseptic properties).
Examples of Specialties Medicines containing Procaine
- Cerulisina Dolore® (in association with fenazone)
- Dentosedina® (in association with benzocaine)
- Lenident®
- Otalgan® (in association with fenazone)
- Otomidone® (in association with phenazone)
- Ustiosan® (in combination with lidocaine and 8-oxyquinoline sulphate)
Therapeutic indications
When is Procaine Use Indicated?
Depending on the pharmaceutical form in which it is found, procaine is indicated in the following cases:
- Treatment of mouth pain and dental pain caused, for example, by caries, periodontitis and pulpopathies (dental solution in sprayer bottle or odontalgica drops);
- Treatment of pain in ear diseases (eg, ear infections) without tympanic perforation (ear drops);
- Treatment of pain and symptoms caused by superficial wounds, excoriations, insect bites, minor burns, sun rashes and skin irritations caused by chemical or physical agents (skin cream).
Did you know that ...
Procaine - always in the form of procaine hydrochloride - is also used in veterinary drugs to induce local anesthesia, epidural anesthesia and nerve conduction anesthesia. However, in these cases, the active ingredient is found in medicines suitable for parenteral administration (injectable solutions).
Warnings
Warnings and Precautions for the use of Procaine
Warnings and precautions may vary depending on the pharmaceutical form containing procaine used. However, regardless of the type of drug used, the use of procaine should be carried out only for short periods of time . If you do not notice any improvement after a few days from the start of the treatment, or on the contrary, if you notice any deterioration, you need to contact the doctor who will provide the right indications on what to do.
Procaine in dental solution and odontalgic drops
The dental solution and the odontalgic drops containing procaine should be used with caution in patients with thyrotoxicosis, renal and / or hepatic insufficiency and cardiovascular diseases.
Procaine in ear drops
Procaine in ear drops should not be used in the event of an established or suspected perforation of the eardrum.
Procaine in skin cream
The procaine skin cream should not be used on large areas of skin and / or in the presence of serious injuries (of any kind).
Please note
As a precautionary measure, before taking procaine-based medicines, it is always advisable to inform your doctor or pharmacist of your health conditions and the possible presence of any type of disorder or illness.
Pharmacological Interactions
Interactions between Procaine and Other Drugs
Procaine may negatively interfere with the therapeutic action of other drugs, such as sulfonamides.
For this reason, before using any type of procaine medicine, it is good to inform your doctor if you are taking - or have recently been taken - drugs or products of any kind, including non-prescription medicines ( SOP), other over-the-counter drugs (OTC), herbal and phytotherapeutic products and homeopathic products.
Side effects
Side effects caused by the assumption of procaine
When properly used, procaine-containing medicines are normally well tolerated.
However, the onset of allergic reactions, even serious ones, in sensitive individuals cannot be excluded.
Furthermore, if the procaine-based medicines are applied to heavily damaged skin and mucous membranes (for example, perforated eardrum, severe skin lesions, serious lesions of the gums or mucous membrane of the mouth, etc.), the active ingredient could be absorbed at the level systemic and could lead to the appearance of even serious side effects, such as:
- Hypotension;
- Cardiac rhythm disorders;
- Depression of the central nervous system;
- Respiratory depression.
Finally, it is recalled that the use of topical drugs for long periods of time could lead to the appearance of sensitization reactions.
Please note
When procaine is used in combination with other active ingredients, side effects due to the latter may also occur. To know them, we recommend reading the illustrative leaflet of the medicinal specialty that you intend to use.
Overdose and Accidental Ingestion
By correctly using procaine in the form of ear drops or skin cream, overdose is a rare occurrence. However, accidental ingestion of the aforementioned procaine formulations can cause symptoms such as diarrhea, dizziness and cyanosis.
With regard to the intake of procaine in the form of dental solution or odontological drops, instead, there is a possible risk of overdose in case of use of excessive doses and / or accidental ingestion. Symptoms such as:
- Depression of the central nervous system;
- Hypotension;
- Respiratory depression;
- Bradycardia.
Therefore, in the event of overdose and / or accidental ingestion of procaine in any pharmaceutical form, it is necessary to go immediately to the hospital - if possible, taking with you the packaging of the medicine taken - where the specific antidote, or methylene blue, will be administered .
Action mechanism
How does Procaine work?
Procaine has a local anesthetic action. Similarly to the other active ingredients with this activity, procaine is able to carry out its action through the interaction with the voltage-dependent sodium channels present on the membranes of nerve cells . Thanks to this interaction, procaine inhibits the permeability of the cell membrane to sodium, hindering its entry into the nerve cell. In this way, excitation of the nerve cell and transmission of the painful stimulus is prevented.
Method of use and Posology
How to take Procaine
Directions for use and dosage vary depending on the pharmaceutical form based on procaine you need to use.
Procaine in dental solution or odontalgic drops
The dose of procaine in the form of dental solution or odontological drops usually recommended is 1-2 sprays or 1-2 drops (depending on the medicine used) to be applied directly to the tooth or mouth area affected by pain. Applications can be made as needed or according to medical prescription. The liquid thus administered should be kept "in situ" for a few minutes and then expelled and not swallowed. For more detailed information, ask your doctor or pharmacist for advice.
Procaine in ear drops
When procaine-based ear drops are used, the dosage normally used may vary depending on the medicinal product used and the concentration of the active ingredient contained. Generally, the recommended dose varies from 3 to 8 drops to be instilled in the external auditory canal 2-4 times a day.
In any case, the treatment should never exceed 10 days in duration and if no improvement is noticed after one or two days, it is necessary to contact the doctor.
Note : before instilling the drops, it is advisable to heat the bottle with the warmth of your hands in order to avoid the annoying sensation of cold.
Procaine in skin cream
When using procaine based skin creams, it is usually recommended to apply 1-2 cm of product directly on the affected skin, once or twice a day. If necessary, this area can be covered with sterile gauze and adhesive plaster.
Pregnancy and breastfeeding
Can Procaine be taken during pregnancy and during breastfeeding?
The use of procaine in the form of a dental solution or odontalgic drops may not be recommended during pregnancy and lactation, since the degree of absorption of the active ingredient is not known when administered at the level of teeth and mouth. In these cases, therefore, it is recommended to carefully read the package insert of the medicine that you must use and to ask information to the pharmacist or your doctor.
With regard to procaine in the form of ear drops and skin cream, on the other hand, use during pregnancy and breastfeeding should be carried out only if absolutely necessary and only under the strict supervision of the doctor.
In conclusion, although the currently available procaine medicines are over-the-counter drugs, pregnant women and breastfeeding mothers must seek the advice of their doctor before using them.
Contraindications
When Procaine Should Not Be Used
The use of procaine is contraindicated in case of known hypersensitivity to procaine itself and / or to one or more of the active ingredients and / or to one or more of the excipients contained within the medicinal product that it is intended to use.
The use of procaine-based drugs should also be avoided in case of known hypersensitivity to other local anesthetics (for example, bupivacaine).
Procaine in the form of ear drops should not be used in the presence of tympanic perforation.
Furthermore, depending on the medicinal product used, use in children may also be contraindicated.
Please note
For more in-depth information on indications, warnings and precautions, interactions, side effects, use during pregnancy and during lactation and contraindications of the various procaine medicines, it is advisable to consult your doctor and read the leaflet carefully illustrative of the medicinal product to be used.
