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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 (without the "e" in the original German patent) or Novocaine (with the "e" in the US patent), 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 Novocain, 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 ...
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Cocaine
Cocaine is a tropane alkaloid and central nervous system stimulant, derived primarily from the leaves of two South American coca plants, ''Erythroxylum coca'' and ''Erythroxylum novogranatense, E. novogranatense'', which are cultivated almost exclusively in the Andes. Indigenous peoples of South America, Indigenous South Americans have traditionally used coca leaves for over a thousand years. Notably, there is no evidence that habitual coca leaf use causes addiction or withdrawal, unlike cocaine. Medically, cocaine is rarely employed, mainly as a topical medication under controlled settings, due to its high abuse potential, adverse effects, and expensive cost. Despite this, recreational drug use, recreational use is widespread, driven by its euphoric and aphrodisiac properties. Levamisole induced necrosis syndrome (LINES)-a complication of the common cocaine Lacing (drugs), cutting agent levamisole-and prenatal cocaine exposure is particularly harmful. Street cocaine is ...
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Local Anesthetic
A local anesthetic (LA) is a medication that causes absence of all sensation (including pain) in a specific body part without loss of consciousness, providing local anesthesia, 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 ( local anesthetic nerve block), paralysis (loss of muscle function) also can be induced. Classification LAs are of 2 types: *Clinical LAs: ** amino amide LAs ** amino ester LAs *Synthetic LAs **Cocaine derivatives Synthetic cocaine-derived LAs differ from cocaine because they have a much lower abuse potential and do not cause hypertension vasoconstriction (with few exceptions). The suffix "-caine" at the ends of these medication names is derived from the word "cocaine", because cocaine was formerly used as a local anesthetic. Examples Short Duration of Act ...
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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 anaesthesia ...
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Penicillin
Penicillins (P, PCN or PEN) are a group of beta-lactam antibiotic, β-lactam antibiotics originally obtained from ''Penicillium'' Mold (fungus), moulds, principally ''Penicillium chrysogenum, P. chrysogenum'' and ''Penicillium rubens, P. rubens''. Most penicillins in clinical use are synthesised by ''Penicillium chrysogenum, P. chrysogenum'' using industrial fermentation, deep tank fermentation and then purified. A number of natural penicillins have been discovered, but only two purified compounds are in clinical use: benzylpenicillin, penicillin G (intramuscular injection, intramuscular or Intravenous therapy, intravenous use) and phenoxymethylpenicillin, penicillin V (given by mouth). Penicillins were among the first medications to be effective against many bacterial infections caused by staphylococcus, staphylococci and streptococcus, streptococci. They are still widely used today for various bacterial infections, though many types of bacteria have developed antibiotic res ...
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Mepivacaine
Mepivacaine is a local anesthetic of the amide type. Mepivacaine has a reasonably rapid onset (less rapid than that of procaine) and medium duration of action (longer 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 a mixture that has equal amounts (50:50) 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 r ..., 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 linksMepivac ...
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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 and ventricular fibrillation. 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. I ...
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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, local anesthetic medications (LA) are often used to control any potential pain that may occur with procedures. Local anesthetic injections are given in specific areas of the mouth, rather than the whole body. Although several different medications are available, the most commonly used local anesthetic to prevent pain in the area around a tooth is lidocaine (also called xylocaine or lignocaine). Lidocaine's half-life in the body is about 1.5–2 hours. The time it takes for the anesthetic medication to prevent pain in the area (speed of onset) and length of time that the area does not have painful sensations are considerations when choosing an appropriate approach to dental treatment. Other considerations include procedural considerations, the presence of inflammation, techniques ...
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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, amino esters consist of three molecular components: * a lipophilic part (ester) * an intermediate aliphatic chain * a hydrophilic part (amine) 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 Benzocaine, sold under the brand name Orajel amongst others, is a local anesthetic, ...
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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 wher ...
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Parenteral
In pharmacology and toxicology, a route of administration is the way by which a drug, fluid, poison, or other substance is taken into the body. Routes of administration are generally classified by the location at which the substance is applied. Common examples include oral and intravenous administration. Routes can also be classified based on where the target of action is. Action may be topical (local), enteral (system-wide effect, but delivered through the gastrointestinal tract), or parenteral (systemic action, but is delivered by routes other than the GI tract). Route of administration and dosage form are aspects of drug delivery. Classification Routes of administration are usually classified by application location (or exposition). The route or course the active substance takes from application location to the location where it has its target effect is usually rather a matter of pharmacokinetics (concerning the processes of uptake, distribution, and elimination of drugs) ...
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General Anesthesia
General anaesthesia (UK) or general anesthesia (US) is medically induced loss of consciousness that renders a patient unarousable even by painful stimuli. It is achieved through medications, which can be injected or inhaled, often with an analgesic and neuromuscular blocking agent. General anaesthesia is usually performed in an operating theatre to allow surgical procedures that would otherwise be intolerably painful for a patient, or in an intensive care unit or emergency department to facilitate endotracheal intubation and mechanical ventilation in critically ill patients. Depending on the procedure, general anaesthesia may be optional or required. No matter whether the patient prefers to be unconscious or not, certain pain stimulus, pain stimuli can lead to involuntary responses from the patient, such as movement or muscle contractions, that make the operation extremely difficult. Thus, for many procedures, general anaesthesia is necessary from a practical point of view. The p ...
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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 p ...
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