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Local Anesthetic Drugs Prilocaine For Dermal Anesthesia And Pain Relief CAS 721-50-6
|Boiling point||bp0.1 159-162°|
|Density||1.0117 (rough estimate)|
Prilocaine is a local anesthetic of the amino amide type first prepared by Claes Tegner and Nils Löfgren. In its injectable form (trade name Citanest), it is often used in dentistry. It is also often combined with lidocaine as a preparation for dermal anesthesia (lidocaine/prilocaine or EMLA), for treatment of conditions like paresthesia. As it has low cardiac toxicity, it is commonly used for intravenous regional anaesthesia (IVRA).
In some patients, a metabolite of prilocaine may cause the unusual side effect of methemoglobinemia, which may be treated with methylene blue.
Local anesthetic is a substance that causes loss of sensation only to the area to which it is applied without affecting consciousness. Most local anesthetics structures have amino-ester or an amino-amide group which are linked to hydrophilic (secondary or tertiary amine) and to hydrophobic group (aromatics) on the other side.
Local anesthetics, long duration, lower toxicity, chemicals that are also small Suitable for epidural anesthesia, block anesthesia and infiltration anesthesia, etc.
Application It is a kind of local anesthetic drug . The product has better efficacy than procaine and the local anesthesia intensity and speed being similar as lidocaine but with longer duration time and less toxicity as well as smaller accumulation effect . It is suitable for epidural anesthesia , conduction anesthesia and infiltration anesthesia.
Lidocaine and Prilocaine - Clinical Pharmacology
Mechanism of Action:
Lidocaine and Prilocaine cream, applied to intact skin under occlusive dressing, provides dermal analgesia by the release of Lidocaine and Prilocaine from the cream into the epidermal and dermal layers of the skin and by the accumulation of Lidocaine and Prilocaine in the vicinity of dermal pain receptors and nerve endings. Lidocaine and Prilocaine are amide-type local anesthetic agents. Both Lidocaine and Prilocaine stabilize neuronal membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.
The onset, depth and duration of dermal analgesia on intact skin provided by Lidocaine and Prilocaine cream, depends primarily on the duration of application. To provide sufficient analgesia for clinical procedures such as intravenous catheter placement and venipuncture, Lidocaine and Prilocaine cream, should be applied under an occlusive dressing for at least 1 hour. To provide dermal analgesia for clinical procedures such as split skin graft harvesting, Lidocaine and Prilocaine cream, should be applied under occlusive dressing for at least 2 hours. Satisfactory dermal analgesia is achieved 1 hour after application, reaches maximum at 2 to 3 hours, and persists for 1 to 2 hours after removal. Absorption from the genital mucosa is more rapid and onset time is shorter (5 to 10 minutes) than after application to intact skin. After a 5 to 10 minute application of Lidocaine and Prilocaine cream, to female genital mucosa, the average duration of effective analgesia to an argon laser stimulus (which produced a sharp, pricking pain) was 15 to 20 minutes (individual variations in the range of 5 to 45 minutes).
Dermal application of Lidocaine and Prilocaine cream, may cause a transient, local blanching followed by a transient, local redness or erythema.
Lidocaine and Prilocaine cream, is a eutectic mixture of lidocaine and prilocaine formulated as an oil in water emulsion. In this eutectic mixture, both anesthetics are liquid at room temperature (see DESCRIPTION) and the penetration and subsequent systemic absorption of both prilocaine and lidocaine are enhanced over that which would be seen if each component in crystalline form was applied separately as a topical cream.
Absorption- The amount of Lidocaine and Prilocaine systemically absorbed from Lidocaine and Prilocaine cream, is directly related to both the duration of application and to the area over which it is applied. In two pharmacokinetic studies, 60 g of Lidocaine and Prilocaine cream, (1.5 g lidocaine and 1.5 g prilocaine) was applied to 400 cm2 of intact skin on the lateral thigh and then covered by an occlusive dressing. The subjects were then randomized such that one-half of the subjects had the occlusive dressing and residual cream removed after 3 hours, while the remainder left the dressing in place for 24 hours. The results from these studies are summarized below.
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