Portal:Local anesthetics
Portal maintenance status: (October 2018)
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Introduction
A local anesthetic (LA) is a medication that causes reversible absence of pain sensation. When it is used on specific nerve pathways (local anesthetic nerve block), paralysis (loss of muscle power) also can be achieved.
Clinical LAs belong to one of two classes: aminoamide and aminoester local anesthetics. Synthetic LAs are structurally related to cocaine. They differ from cocaine mainly in that they have a very low abuse potential and do not produce hypertension or (with few exceptions) vasoconstriction.
Selected general articles
Procaine is a local anesthetic drug of the amino ester group. It is used primarily to reduce the pain of intramuscular injection of penicillin, and it is also used in dentistry. Owing to the ubiquity of the trade name Novocain, in some regions, procaine is referred to generically as novocaine. It acts mainly as a sodium channel blocker. Today it is used therapeutically in some countries due to its sympatholytic, anti-inflammatory, perfusion-enhancing, and mood-enhancing effects.
Procaine was first synthesized in 1905, shortly after amylocaine. It was created by the German chemist Alfred Einhorn who gave the chemical the trade name Novocaine, from the Latin nov- (meaning "new") and -caine, a common ending for alkaloids used as anesthetics. It was introduced into medical use by surgeon Heinrich Braun. Prior to the discovery of amylocaine and procaine, cocaine was a commonly used local anesthetic. Einhorn wished his new discovery to be used for amputations, but surgeons preferred general anesthetic. Dentists, however, found it very useful. Read more...
Proxymetacaine (INN) or proparacaine (USAN) is a topical anesthetic drug of the aminoester group. Read more...
Tetracaine, also known as amethocaine, is a local anesthetic used to numb the eyes, nose, or throat. It may also be used before starting an intravenous 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.
Common side effects include a brief period of burning at the site of use. Allergic reactions may uncommonly occur. Long term use is generally not recommended as it may slow healing of the eye. It is unclear if use during pregnancy is safe for the baby. Tetracaine is in the ester-type local anesthetic family of medications. It works by blocking the sending of nerve impulses. Read more...
Trimecaine (systematic name (2,4,6-trimethylphenylcarbamoylmethyl)diethylammonium chloride, chemical formula C15H25ClN2O) is an organic compound used as a local anesthetic and cardial antiarrhythmic. It is white crystalline powder readily soluble in water and ethanol. It is an active ingredient in products available under trademarks Mesdicain, Mesocain, Mesokain and others. Read more...
Articaine is a dental amide-type local anesthetic. It is the most widely used local anesthetic in a number of European countries and is available in many countries around. It is the only local anaesthetic to contain a thiophene ring, meaning it can be described as 'thiophenic'; this conveys lipid solubility. Read more...
Dimethocaine, also known as DMC or larocaine, is a compound with a stimulatory effect. This effect resembles that of cocaine, although dimethocaine appears to be less potent. Just like cocaine, dimethocaine is addictive due to its stimulation of the reward pathway in the brain. However, dimethocaine is a legal cocaine replacement in some countries and is even listed by the European Monitoring Centre for Drugs and Drug Addiction (EMCDDA) under the category “synthetic cocaine derivatives”. The structure of dimethocaine, being a benzoic ester acid, resembles that of procaine. It is found as a white powder at room temperature.
When a product sold online in the UK in June 2010, advertised as dimethocaine was tested, it was found to in fact be a mixture of caffeine and lidocaine, and the lack of any dopaminergic stimulant ingredient in such mixes may explain the limited recreational effects reported by many users. Other samples tested have however been shown to contain genuine dimethocaine, and one branded "bath salt" product containing primarily dimethocaine as the active ingredient, was noted to have been particularly subject to abuse by intravenous drug users in Ireland. Read more...
Articaine is a dental amide-type local anesthetic. It is the most widely used local anesthetic in a number of European countries and is available in many countries around. It is the only local anaesthetic to contain a thiophene ring, meaning it can be described as 'thiophenic'; this conveys lipid solubility. Read more...
3β-(p-Fluorobenzoyloxy)tropane, (8-Methyl-8-azabicyclo[3.2.1]oct-3-yl 4-fluorobenzoic acid ester, 4-fluorotropacocaine, 3-Pseudotropyl-4-fluorobenzoate, 3-pseudotropyl-4-fluorobenzoate, pFBT) is a tropane derivative drug which acts as a local anaesthetic, having around 30% the stimulant potency of cocaine but around the same potency as a local anaesthetic. It has been investigated as a potential radiolabelled agent for studying receptor binding, but was not adopted for this application. The main application for fluorotropacocaine, however, has been as a designer drug analogue of cocaine, first detected by the EMCDDA in 2008, and subsequently sold as an ingredient of various "bath salt" powder products, usually mixed in combination with other stimulant drugs such as caffeine, dimethocaine, desoxypipradrol or substituted cathinone derivatives. Read more...
Cocaine, also known as coke, is a strong stimulant mostly used as a recreational drug. It is commonly snorted, inhaled as smoke, or dissolved and injected into a vein. Mental effects may include loss of contact with reality, an intense feeling of happiness, or agitation. Physical symptoms may include a fast heart rate, sweating, and large pupils. High doses can result in very high blood pressure or body temperature. Effects begin within seconds to minutes of use and last between five and ninety minutes. Cocaine has a small number of accepted medical uses such as numbing and decreasing bleeding during nasal surgery.
Cocaine is addictive due to its effect on the reward pathway in the brain. After a short period of use, there is a high risk that dependence will occur. Its use also increases the risk of stroke, myocardial infarction, lung problems in those who smoke it, blood infections, and sudden cardiac death. Cocaine sold on the street is commonly mixed with local anesthetics, cornstarch, quinine, or sugar, which can result in additional toxicity. Following repeated doses a person may have decreased ability to feel pleasure and be very physically tired. Read more...
Chloroprocaine (trade name Nesacaine, Nesacaine-MPF) (often in the hydrochloride salt form as the aforementioned trade names) is a local anesthetic given by injection during surgical procedures and labor and delivery. Chloroprocaine vasodilates; this is in contrast to cocaine which vasoconstricts. Chloroprocaine is an ester anesthetic. Read more...
Bupivacaine, marketed under the brand name Marcaine among others, is a medication used to decrease feeling in a specific area. It is used by injecting it into the area, around a nerve that supplies the area, or into the spinal canal's epidural space. It is available mixed with a small amount of epinephrine to make it last longer. It typically begins working within 15 minutes and lasts for 2 to 8 hours.
Possible side effects include sleepiness, muscle twitching, ringing in the ears, changes in vision, low blood pressure, and an irregular heart rate. Concerns exist that injecting it into a joint can cause problems with the cartilage. Concentrated bupivacaine is not recommended for epidural freezing. Epidural freezing may also increase the length of labor. It is a local anaesthetic of the amide group. Read more...
Lidocaine, also known as xylocaine and lignocaine, is a medication used to numb tissue in a specific area (local anesthetic). It is also used to treat ventricular tachycardia and to perform nerve blocks. Lidocaine mixed with a small amount of adrenaline (epinephrine) is available to allow larger doses for numbing, to decrease bleeding, and to make the numbing effect last longer. When used as an injectable, it typically begins working within four 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.
Common side effects with intravenous use include sleepiness, muscle twitching, confusion, changes in vision, numbness, tingling, and vomiting. It can cause low blood pressure and an irregular heart rate. There are concerns that injecting it into a joint can cause problems with the cartilage. It appears to be generally safe for use in pregnancy. A lower dose may be required in those with liver problems. It is generally safe to use in those allergic to tetracaine or benzocaine. Lidocaine is an antiarrhythmic medication of the class Ib type. This means it works by blocking sodium channels and thus decreasing the rate of contractions of the heart. When it is used locally as a numbing agent, local neurons cannot signal the brain. Read more...- 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). Read more...
Benzocaine, sold under the brand name Orajel among others, is an ester local anesthetic commonly used as a topical pain reliever or in cough drops. It is the active ingredient in many over-the-counter anesthetic ointments such as products for oral ulcers. It is also combined with antipyrine to form A/B otic drops to relieve ear pain and remove earwax. It is not recommended in children younger than two years old. Read more...
A local anesthetic (LA) is a medication that causes reversible absence of pain sensation. When it is used on specific nerve pathways (local anesthetic nerve block), paralysis (loss of muscle power) also can be achieved.
Clinical LAs belong to one of two classes: aminoamide and aminoester local anesthetics. Synthetic LAs are structurally related to cocaine. They differ from cocaine mainly in that they have a very low abuse potential and do not produce hypertension or (with few exceptions) vasoconstriction. Read more...
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Selected images
This LA system is designed to prevent needlestick injury. A cartridge of LA fits into the disposable needle, which can be locked when not in use and can be separated from the handle.
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