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Procaine
Procaine is a local anesthetic drug of the amino ester group. It is most commonly used in dental procedures to numb the area around a tooth and is also used to reduce the pain of intramuscular injection of penicillin. Owing to the ubiquity of the trade name Novocain or Novocaine, 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 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 ne ...
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Local Anesthetic
A local anesthetic (LA) is a medication that causes absence of pain sensation. In the context of surgery, a local anesthetic creates an absence of pain in a specific location of the body without a loss of consciousness, as opposed to a general anesthetic. When it is used on specific nerve pathways ( local anesthetic nerve block), paralysis (loss of muscle power) also can be achieved. Examples Short Duration & Low Potency Procaine Chloroprocaine Medium Duration & Potency Lidocaine Prilocaine High Duration & Potency Tetracaine Bupivacaine Cinchocaine Ropivacaine 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. They are used in various techniques of local anesthesia such as: * Topical anesthesia (surface) * Topical ad ...
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Cocaine
Cocaine (from , from , ultimately from Quechua: ''kúka'') is a central nervous system (CNS) stimulant mainly used recreationally for its euphoric effects. It is primarily obtained from the leaves of two Coca species native to South America, ''Erythroxylum coca'' and ''Erythroxylum novogranatense''. After extraction from coca leaves and further processing into cocaine hydrochloride (powdered cocaine), the drug is often snorted, applied topically to the mouth, or dissolved and injected into a vein. It can also then be turned into free base form ( crack cocaine), in which it can be heated until sublimated and then the vapours can be inhaled. Cocaine stimulates the reward pathway in the brain. Mental effects may include an intense feeling of happiness, sexual arousal, loss of contact with reality, or agitation. Physical effects may include a fast heart rate, sweating, and dilated pupils. High doses can result in high blood pressure or high body temperature. Effects ...
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Heinrich Braun
Heinrich Friedrich Wilhelm Braun (1 January 1862 – 26 April 1934) was a German surgeon remembered for his work in the field of anaesthesiology. He was a native of Rawitsch, Province of Posen (today called Rawicz, Poland). Braun attended the Kreuzschule and the ''Vitzhumsches Gymnasium'' in Dresden, completing his Abitur in 1881. He studied medicine at the Universities of Strasbourg, Greifswald and Leipzig, earning his doctorate in 1887. From 1891 to 1905 he worked at various hospitals in Leipzig, becoming an associate professor at the University of Leipzig in 1905. The following year he was appointed chief surgeon and medical director of the Royal Saxonian Hospital in Zwickau, a position he maintained until his retirement in 1923. Construction of the "Krankenstift Zwickau" in 1921 was based on his plans and recommendations. Braun made important contributions in the development of general, local and regional anaesthesia. In 1901 he devised an apparatus for mixed-gas anaesthes ...
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Penicillin
Penicillins (P, PCN or PEN) are a group of β-lactam antibiotics originally obtained from '' Penicillium'' moulds, principally '' P. chrysogenum'' and '' P. rubens''. Most penicillins in clinical use are synthesised by P. chrysogenum using deep tank fermentation and then purified. A number of natural penicillins have been discovered, but only two purified compounds are in clinical use: penicillin G (intramuscular or intravenous use) and penicillin V (given by mouth). Penicillins were among the first medications to be effective against many bacterial infections caused by staphylococci and streptococci. They are still widely used today for different bacterial infections, though many types of bacteria have developed resistance following extensive use. 10% of the population claims penicillin allergies but because the frequency of positive skin test results decreases by 10% with each year of avoidance, 90% of these patients can tolerate penicillin. Additionally, those wi ...
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Lidocaine
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. If injected intravenously, it may cause cerebral effects such as 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 i ...
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Mepivacaine
Mepivacaine is a local anesthetic of the amide type. Mepivacaine has a reasonably rapid onset (more rapid than that of procaine) and medium duration of action (shorter than that of procaine) and is marketed under various trade names including Carbocaine and Polocaine. Mepivacaine became available in the United States in the 1960s. Mepivacaine is used in any infiltration and local anesthesia. It is supplied as the hydrochloride salt of the racemate In chemistry, a racemic mixture, or racemate (), is one that has equal amounts of left- and right-handed enantiomers of a chiral molecule or salt. Racemic mixtures are rare in nature, but many compounds are produced industrially as racemates. ..., which consists of R(-)-mepivacaine and S(+)-mepivacaine in equal proportions. These two enantiomers have markedly different pharmacokinetic properties. Mepivacaine was originally synthesized in Sweden at the laboratory of Bofors Nobelkrut in 1956. References External linksMepiva ...
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Alfred Einhorn
Alfred Einhorn (27 February 1856 – 21 March 1917) was a German chemist most notable for first synthesizing procaine in 1905 which he patented under the name Novocain. Until that time the primary anesthetic in use was cocaine, however its undesirable side effects (including toxicity and addiction) led scientists to seek out newer anesthetic drugs. Novocain was found to be comparatively safe and effective, although its anesthetic effects were weaker than cocaine and some patients proved highly allergic. However, none of the other anesthetics developed during this period proved more effective and Novocain quickly became the standard local anesthesia. Although its use has largely been replaced by lidocaine, it is still in use today, most frequently in dentistry. Life Einhorn was born in Hamburg, and due to the death of his parents his education took place in Leipzig with his relatives. He studied chemistry at the University of Leipzig and later at the University of Tübingen whe ...
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Dental Anesthesia
Dental anesthesia (or dental anaesthesia) is the application of anesthesia to dentistry. It includes local anesthetics, sedation, and general anesthesia. Local anesthetic agents in dentistry In dentistry, the most commonly used local anesthetic is lidocaine (also called xylocaine or lignocaine). Lidocaine's half-life in the body is about 1.5–2 hours. As of 2018, Lidocaine is most commonly used in dental procedures to numb the area around a tooth. In root canal treatment, for example, more Lidocaine is required than for a simple filling Other local anesthetic agents in current use include articaine (also called septocaine or Ubistesin), bupivacaine (a long-acting anesthetic), prilocaine (also called Citanest), and mepivacaine (also called Carbocaine or Polocaine). Different types of local anaesthetic drugs vary in their potency and duration of action. A combination of these may be used depending on the situation. Some agents come in two forms: with and without epinephrine ...
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Amino Esters
Amino esters are a class of local anesthetics. They are named for their ester bond (and are unlike amide local anaesthetics). Structure Structurally, local anesthetics consist of three molecular components: * a lipophilic part * an intermediate aliphatic chain * a hydrophilic (amine) part The chemical linkage between the lipophilic part and the intermediate chain can be of the amide-type or the ester-type, and is the general basis for the current classification of local anesthetics. Amino esters, in reference to anesthetic agents, are rapidly metabolized in the plasma by butyrylcholinesterase to para-aminobenzoic acid derivatives, then excreted in the urine. This suggests their very short half lives. Allergy is more likely to occur with ester-type agents, as opposed to amide-type. Examples Amino ester-type include: * Cocaine * Procaine (Novocain) * Tetracaine (Pontocaine) * Benzocaine * Chloroprocaine Chloroprocaine (trade name Nesacaine, Nesacaine-MPF) (often in the hydroch ...
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Vasoconstriction
Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, in particular the large arteries and small arterioles. The process is the opposite of vasodilation, the widening of blood vessels. The process is particularly important in controlling hemorrhage and reducing acute blood loss. When blood vessels constrict, the flow of blood is restricted or decreased, thus retaining body heat or increasing vascular resistance. This makes the skin turn paler because less blood reaches the surface, reducing the radiation of heat. On a larger level, vasoconstriction is one mechanism by which the body regulates and maintains mean arterial pressure. Medications causing vasoconstriction, also known as vasoconstrictors, are one type of medicine used to raise blood pressure. Generalized vasoconstriction usually results in an increase in systemic blood pressure, but it may also occur in specific tissues, causing a localized reduction in ...
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Alkaloid
Alkaloids are a class of basic, naturally occurring organic compounds that contain at least one nitrogen atom. This group also includes some related compounds with neutral and even weakly acidic properties. Some synthetic compounds of similar structure may also be termed alkaloids. In addition to carbon, hydrogen and nitrogen, alkaloids may also contain oxygen, sulfur and, more rarely, other elements such as chlorine, bromine, and phosphorus.Chemical Encyclopedia: alkaloids
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Alkaloids are produced by a large variety of organisms including , ,

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Prilocaine
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 topical 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). Contraindications In some patients, ortho-toluidine, a metabolite of prilocaine, may cause methemoglobinemia, which may be treated with methylene blue. Prilocaine may also be contraindicated in people with sickle cell anemia, anemia, or symptomatic hypoxia. Combinations It is given as a combination with the vasoconstrictor epinephrine under the trade name ''Citanest Forte''. It is used as a eutectic mixture with lidocaine, 50% w/w, as lidocaine/prilocaine. The mixture is an oil with a melting point of . A 5% emulsion pr ...
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