CAS 721-50-6 Local Anesthetic Drugs Low toxicity Propitocaine Hydrochloride / Prilocaine HCl

Low toxicity Propitocaine Hydrochloride/Prilocaine HCl For local anesthetic CAS 721-50-6

Quick details

Alias:Prilocaine

Model NO.:721-50-6

Key words:Prilocaine , Local anesthesia

Character:White Powder

MF: C13H20N20

MW: 220.31

EINECS: 211-957-0

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Trademark:Pharmlab

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Standard:GMP, ISO, UP, SP,

Origin:Guangdong, China

Production Capacity:6000kg/Month

Product Categories: Active Pharmaceutical Ingredients

Packing:Foil bag or as requirments

Propitocaine HCl Description

Propitocaine hydrochloride is a local anesthetic of the amino amide type first prepared by Claes Tegner and Nils L? Fgren. In its injectable form, 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 forintravenous regional anaesthesia.

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.

Prilocaine Hydrochloride Injection - Clinical Pharmacology

Mechanism of Action

Prilocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.

Onset and Duration of Action

When used for infiltration injection in dental patients, the time of onset of anesthesia averages less than 2 minutes with an average duration of soft tissue anesthesia of approximately 2 hours.

Based on electrical stimulation studies, Prilocaine Hydrochloride Injection, USP, 4% provides a duration of pulpal anesthesia of approximately 10 minutes in maxillary infiltration injections. In clinical studies, this has been found to provide complete anesthesia for procedures lasting an average of 20 minutes.

When used for inferior alveolar nerve block, the time of onset of Prilocaine Hydrochloride Injection, USP, 4% averages less than three minutes with an average duration of soft tissue anesthesia of approximately 21/2 hours.

Hemodynamics

Excessive blood levels may cause changes in cardiac output, total peripheral resistance, and mean arterial pressure. These changes may be attributable to a direct depressant effect of the local anesthetic agent on various components of the cardiovascular system.

Pharmacokinetics and Metabolism

Information derived from diverse formulations, concentrations and usages reveals that prilocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon such factors as the site of administration and the presence or absence of a vasoconstrictor agent. Prilocaine is metabolized in both the liver and the kidney and excreted via the kidney. It is not metabolized by plasma esterases. Hydrolysis of prilocaine by amidases yields ortho-toluidine and N-proylalanine. Both of these compounds may undergo ring hydroxylation.

O-toluidine has been found to produce methemoglobin, both in vitro and in vivo (see ADVERSE REACTIONS).

Because prilocaine is metabolized in both the liver and kidneys, hepatic and renal dysfunction may alter prilocaine kinetics.

As with other local anesthetic agents, the plasma binding of prilocaine may be dependent on drug concentration. At 0.5 to 1.0 mg/mL it is 55% protein bound.

Prilocaine crosses the blood-brain and placental barriers, presumably by passive diffusion.

Factors such as acidosis and the use of CNS stimulants and depressants affect the CNS levels of prilocaine required to produce overt systemic effects. In the rhesus monkey, arterial blood levels of 20 mg/mL have been shown to be the threshold for convulsive activity.

Propitocaine hydrochloride Application :

Prilocaine is a local anesthetic of the amino amide type. Prilocaine is often used in dentistry. Prilocaine is also often combined with lidocaine as a preparation for dermal anesthesia (lidocaine/pril ocaine or EMLA), for treatment of conditions like paresthesia.

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).

The ester can be hydrolysed in plasma by the enzyme pseudocholinesterase into PARA-aminobenzoic acid. Amide is stable for longer acting and more systemic distribution. Ester types include Procaine (Novocain), Chloroprocaine (Nesacaine), Tetracaine (Pontocaine), Benzocaine, Tetracaine. Amide types include Lidocaine (Xylocaine), Mepivacaine(Carbocaine), Prilocaine (Citanest), Bupivacaine (Marcaine), Etidocaine (Duranest).

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