Lidocaine/prilocaine

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Lidocaine/prilocaine
Combination of
Lidocaine Local anesthetic
Prilocaine Local anesthetic
Clinical data
Trade names Emla, Fortacin, Senstend, others
AHFS/Drugs.com Micromedex Detailed Consumer Information
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Routes of
administration
Topical
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Lidocaine/prilocaine is a eutectic mixture of equal quantities (by weight) of lidocaine and prilocaine. A 5% emulsion preparation, containing 2.5% each of lidocaine/prilocaine, is marketed by APP Pharmaceuticals under the trade name EMLA (an abbreviation for Eutectic Mixture of Local Anesthetics). [5] As a spray, it is marketed under the name Tempe (topical eutectic-like mixture for premature ejaculation) (PSD502) that can be used by men to help with premature ejaculation. The spray is manufactured by Plethora Solutions and branded as Fortacin in the UK and Recordati in the EU. [6]

Contents

Eutectic mixture

Separately, lidocaine and prilocaine are solid bases. When mixed in equal quantities by weight, however, they form a eutectic mixture – that is the melting point of the mixture is lower than the melting points of the individual components. The lidocaine/prilocaine eutectic mixture is an oil with a melting point of 18 °C, and can be formulated into preparations without the use of a non-aqueous solvent. [7] This allows higher concentrations of anaesthetic to be formulated into the preparation and maintained during application.

Clinical use

Indications

The lidocaine/prilocaine combination is indicated for dermal anaesthesia. Specifically it is applied to prevent pain associated with intravenous catheter insertion, blood sampling, superficial surgical procedures, and topical anaesthesia of leg ulcers for cleansing or debridement. [8] Also, it can be used to numb the skin before tattooing as well as electrolysis and laser hair removal. It is also sometimes used in advance of injected local anaesthetics for minor surgery and biopsies.

A topical spray consisting of an aerosol formulation of lidocaine and prilocaine was evaluated under the name PSD502 for use in treating premature ejaculation. The spray is applied on the penile skin prior to intercourse. While this formulation was not approved by the FDA, [9] a similar product, Promescent, is available over-the-counter in the U.S.

Dosage forms

Lidocaine/prilocaine eutectic mixture is marketed as a 5% oil-in-water emulsion incorporated in a cream base (EMLA cream) or a cellulose disk (EMLA patch). The cream is applied under an occlusive dressing, while the patch incorporates an occlusive dressing to facilitate absorption of lidocaine and prilocaine into the area where anaesthesia is required. Local dermal anaesthesia is achieved after approximately 60 minutes, whereupon the occlusive dressing (or patch) is removed. The duration of anaesthesia is approximately two hours following removal of the occlusive dressing.

E. Fougera & Co., makers of the generic cream widely used in the United States as Lidocaine and Prilocaine Cream, 2.5%/2.5%, recommends different timing for application of the cream as well as length of anesthesia. They state the cream must be applied at least one hour before the start of a routine procedure and for two hours before the start of a painful procedure. Additionally, they state that the duration of effective skin anesthesia will be at least one hour after removal of the occlusive dressing. [10]

Circumcision

Lidocaine/prilocaine eutectic mixture has been used during circumcision in newborn boys and has been considered efficacious and safe to lessen pain from circumcision. [11]

The European Medicines Agency concludes in its latest (2014) statement on Emla: "Safety and efficacy for the use of EMLA on genital skin and genital mucosa have not been established in children younger than 12 years. Available paediatric data do not demonstrate adequate efficacy for circumcision." [12]

The Patient Information Leaflet of EMLA in the UK states: "EMLA Cream should not be applied to the genital skin (e.g. penis) and genital mucosa (e.g. in the vagina) of children (below 12 years of age) owing to insufficient data on absorption of active substances." [13]

Tempe

The spray is a combination of local anaesthetics lidocaine and prilocaine in a metered-dose aerosol that is sprayed directly on the penis to numb sensations. It was developed by the same group that invented the erectile dysfunction drug sildenafil.[ citation needed ] The drug was approved in Europe and was released in the UK market in November 2016 and within the EU will be marketed by, early in 2017 [14] [ unreliable medical source? ] In the United States, the Food and Drug Administration (FDA) is expected to approve the drug in 2018. [15] [ unreliable medical source? ]

Compendial status

See also

Related Research Articles

<span class="mw-page-title-main">Local anesthetic</span> Medications to reversibly block pain

A local anesthetic (LA) is a medication that causes absence of all sensation in a specific body part without loss of consciousness, as opposed to a general anesthetic, which eliminates all sensation in the entire body and causes unconsciousness. Local anesthetics are most commonly used to eliminate pain during or after surgery. When it is used on specific nerve pathways, paralysis also can be induced.

<span class="mw-page-title-main">Lidocaine</span> Local anesthetic

Lidocaine, also known as lignocaine and sold under the brand name Xylocaine among others, is a local anesthetic of the amino amide type. It is also used to treat ventricular tachycardia. When used for local anaesthesia or in nerve blocks, lidocaine typically begins working within several minutes and lasts for half an hour to three hours. Lidocaine mixtures may also be applied directly to the skin or mucous membranes to numb the area. It is often used mixed with a small amount of adrenaline (epinephrine) to prolong its local effects and to decrease bleeding.

<span class="mw-page-title-main">Benzocaine</span> Local anaesthetic drug

Benzocaine, sold under the brand name Orajel amongst others, is a local anesthetic, belonging to the amino ester drug class, commonly used as a topical painkiller or in cough drops. It is the active ingredient in many over-the-counter anesthetic ointments such as products for oral ulcers. It is combined with antipyrine to form A/B ear drops. In the US, products containing benzocaine for oral application are contraindicated in children younger than two years old. In the European Union, the contraindication applies to children under 12 years of age.

<span class="mw-page-title-main">Topical medication</span> Medication applied to body surfaces

A topical medication is a medication that is applied to a particular place on or in the body. Most often topical medication means application to body surfaces such as the skin or mucous membranes to treat ailments via a large range of classes including creams, foams, gels, lotions, and ointments. Many topical medications are epicutaneous, meaning that they are applied directly to the skin. Topical medications may also be inhalational, such as asthma medications, or applied to the surface of tissues other than the skin, such as eye drops applied to the conjunctiva, or ear drops placed in the ear, or medications applied to the surface of a tooth. The word topical derives from Greek τοπικόςtopikos, "of a place".

<span class="mw-page-title-main">Betamethasone</span> Steroid medication

Betamethasone is a steroid medication. It is used for a number of diseases including rheumatic disorders such as rheumatoid arthritis and systemic lupus erythematosus, skin diseases such as dermatitis and psoriasis, allergic conditions such as asthma and angioedema, preterm labor to speed the development of the baby's lungs, Crohn's disease, cancers such as leukemia, and along with fludrocortisone for adrenocortical insufficiency, among others. It can be taken by mouth, injected into a muscle, or applied to the skin, typically in cream, lotion, or liquid forms.

<span class="mw-page-title-main">Fear of needles</span> Phobia of injections or needles

Fear of needles, known in medical literature as needle phobia, is the extreme fear of medical procedures involving injections or hypodermic needles. This can lead to avoidance of medical care and vaccine hesitancy.

<span class="mw-page-title-main">Betamethasone dipropionate</span> Glucocorticoid steroid (chemical compound)

Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities. It is applied as a topical cream, ointment, lotion or gel (Diprolene) to treat itching and other skin conditions such as eczema. Minor side effects include dry skin and mild, temporary stinging when applied. Betamethasone dipropionate is a "super high potency" corticosteroid used to treat inflammatory skin conditions such as dermatitis, eczema and psoriasis. It is a synthetic analog of the adrenal corticosteroids. Although its exact mechanism of action is not known, it is effective when applied topically to cortico-responsive inflammatory dermatoses. It is available as a generic medication.

<span class="mw-page-title-main">Cream (pharmacy)</span> Preparation for application to the skin or mucous membranes

A cream is a preparation usually for application to the skin. Creams for application to mucous membranes such as those of the rectum or vagina are also used. Creams may be considered pharmaceutical products, since even cosmetic creams are manufactured using techniques developed by pharmacy and unmedicated creams are highly used in a variety of skin conditions (dermatoses). The use of the finger tip unit concept may be helpful in guiding how much topical cream is required to cover different areas.

An occlusive dressing is an air- and water-tight trauma medical dressing used in first aid. These dressings are generally made with a waxy coating so as to provide a total seal, and as a result do not have the absorbent properties of gauze pads. They are typically used to treat open, or "sucking," chest wounds to prevent a tension pneumothorax. They are also used in conjunction with a moist sterile dressing for intestinal evisceration.

<span class="mw-page-title-main">Imiquimod</span> Chemical compound

Imiquimod, sold under the brand name Aldara among others, is a medication that acts as an immune response modifier that is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis. Scientists at 3M's pharmaceuticals division discovered the drug and 3M obtained the first FDA approval in 1997. As of 2015, imiquimod is generic and is available worldwide under many brands.

<span class="mw-page-title-main">Tetracaine</span> Local anaesthetic drug

Tetracaine, also known as amethocaine, is an ester local anesthetic used to numb the eyes, nose, or throat. It may also be applied to the skin before starting an intravenous (injection) to decrease pain from the procedure. Typically it is applied as a liquid to the area. Onset of effects when used in the eyes is within 30 seconds and last for less than 15 minutes.

A topical anesthetic is a local anesthetic that is used to numb the surface of a body part. They can be used to numb any area of the skin as well as the front of the eyeball, the inside of the nose, ear or throat, the anus and the genital area. Topical anesthetics are available in creams, ointments, aerosols, sprays, lotions, and jellies. Examples include benzocaine, butamben, dibucaine, lidocaine, oxybuprocaine, pramoxine, proxymetacaine (proparacaine), and tetracaine.

<span class="mw-page-title-main">Prilocaine</span> Local anesthetic of the amino amide type

Prilocaine is a local anesthetic of the amino amide type first prepared by Claes Tegner and Nils Löfgren. In its injectable form, it is often used in dentistry. It is also often combined with lidocaine as a topical preparation for dermal anesthesia, for treatment of conditions like paresthesia. As it has low cardiac toxicity, it is commonly used for intravenous regional anaesthesia (IVRA).

<span class="mw-page-title-main">Lotion</span> Skin treatment preparation

Lotion is a low-viscosity topical preparation intended for application to the skin. By contrast, creams and gels have higher viscosity, typically due to lower water content. Lotions are applied to external skin with bare hands, a brush, a clean cloth, or cotton wool.

<span class="mw-page-title-main">Amcinonide</span> Chemical compound

Amcinonide is a topical glucocorticoid used to treat itching, redness and swelling associated with several dermatologic conditions such as atopic dermatitis and allergic contact dermatitis. Amcinonide can also be classified as a multi-functional small molecule corticosteroid, which has been approved by the FDA and is currently marketed as an ointment, lotion, or cream. It acts as both a transcription factor for responses to glucocorticoids and modulator for other transcription factors while also regulating phospholipase A2 activity.

Dental anesthesia is the application of anesthesia to dentistry. It includes local anesthetics, sedation, and general anesthesia.

<span class="mw-page-title-main">Cold sore</span> Herpes simplex virus infection of the lip

A cold sore is a type of herpes infection caused by the herpes simplex virus that affects primarily the lip. Symptoms typically include a burning pain followed by small blisters or sores. The first attack may also be accompanied by fever, sore throat, and enlarged lymph nodes. The rash usually heals within ten days, but the virus remains dormant in the trigeminal ganglion. The virus may periodically reactivate to create another outbreak of sores in the mouth or lip.

Topical tac is a topical anesthetic solution introduced by Pryor et al. in 1980. It is recommended for use on pediatric patients.

Ocular surgery may be performed under topical, local or general anesthesia. Local anaesthesia is more preferred because it is economical, easy to perform and the risk involved is less. Local anaesthesia has a rapid onset of action and provides a dilated pupil with low intraocular pressure.

Topical antifungaldrugs are used to treat fungal infections on the skin, scalp, nails, vagina or inside the mouth. These medications come as creams, gels, lotions, ointments, powders, shampoos, tinctures and sprays. Most antifungal drugs induce fungal cell death by destroying the cell wall of the fungus. These drugs inhibit the production of ergosterol, which is a fundamental component of the fungal cell membrane and wall.

References

  1. "Emla Cream 5% (for 5 g and pre-medication packs) - Summary of Product Characteristics (SmPC)". (emc). 4 May 2017. Retrieved 27 September 2020.
  2. "Fortacin - Summary of Product Characteristics (SmPC)". (emc). 14 November 2018. Retrieved 27 September 2020.
  3. "Nulbia 5% cream - Summary of Product Characteristics (SmPC)". (emc). 18 December 2017. Retrieved 27 September 2020.
  4. "List of nationally authorised medicinal products" (PDF). ema.europa.eu. 1 December 2022. Retrieved 13 June 2023.
  5. Pesaturo KA, Matthews M (2009). "Topical Anesthesia Use in Children: Eutectic Mixture of Local Anesthetics". US Pharm. 34 (3): HS-4. Retrieved 7 January 2014.
  6. Dinsmore WW, Wyllie MG (April 2009). "PSD502 improves ejaculatory latency, control and sexual satisfaction when applied topically 5 min before intercourse in men with premature ejaculation: results of a phase III, multicentre, double-blind, placebo-controlled study". BJU International. 103 (7): 940–949. doi:10.1111/j.1464-410X.2009.08456.x. PMID   19245438. S2CID   205540753.
  7. "EMLA Official FDA information, side effects and uses". Drugs.com. Retrieved 7 January 2014.
  8. Heinen MM, van Achterberg T, op Reimer WS, van de Kerkhof PC, de Laat E (March 2004). "Venous leg ulcer patients: a review of the literature on lifestyle and pain-related interventions". Journal of Clinical Nursing. 13 (3): 355–366. doi:10.1046/j.1365-2702.2003.00887.x. PMID   15009338.
  9. "PSD502 TEMPE Spray". Promescent.com. Retrieved 4 July 2014.
  10. Lidocaine and Prilocaine Cream, 2.5%/2.5%, package insert. E. Fougera & Co. package insert. Melville, New York, 9/2007.
  11. Taddio A, Ohlsson K, Ohlsson A (2000). Ohlsson A (ed.). "Lidocaine-prilocaine cream for analgesia during circumcision in newborn boys". The Cochrane Database of Systematic Reviews (2): CD000496. doi:10.1002/14651858.CD000496. PMID   10796371. (Retracted, see doi:10.1002/14651858.cd000496.pub2 . If this is an intentional citation to a retracted paper, please replace {{ Retracted }} with {{ Retracted |intentional=yes}}.)
  12. "INN of the active substance(s): lidocaine/prilocaine" (PDF). Committee for Medicinal Products for Human Use (CHMP). European Medicines Agency.
  13. "Package leaflet: Information for the user EMLA Cream 5%" (PDF). AstraZeneca. 2017.
  14. "TEMPE Spray Delays Ejaculation". bio-medicine.org. Archived from the original on 27 September 2013. Retrieved 25 September 2013.
  15. "Viagra Inventor Develops 'Tempe Spray' To Help Men Deal With Premature Ejaculation: Is It Safe?". medicaldaily.com. 24 September 2013. Retrieved 25 September 2013.
  16. The United States Pharmacopeial Convention. "Revision Bulletin: Lidocaine and Prilocaine Cream–Revision to Related Compounds Test". Archived from the original on 5 July 2010. Retrieved 10 July 2009.