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Drugs effecting the afferent innervation Substances which act in the area of afferent nerves endings: local anesthetics astringent covering adsorbtive irritative Local anesthetics Local anesthetics 1. Natural compound – aether of benzoilekgonin cocain 2. Synthetic neutrogen compounds Aether compounds (derivatives from PABA) a) easily dilluted in water : novocain (procain), dicain (tetrakain) b) badly dilluted in water: anaesthesin (benzokain), orthokain Amide compounds: lidocain (xycain), trimecain, etydocain (duranest), prilocain (citanest), articain (ultracain), piromecain (bumekain), marcain (bupivacain) STRUCTURE OF LOCAL ANESTHETICS x I (CH2)n II N III I – lipophilic aromatic group II – intermediate aliphatic chain III – hydrophilic amine-group R R Kinds of local anesthesia: terminal conductive infiltrative Terminal (superficial) anesthesia local anesthetic is spread over mucous membranes, wounds, ulcers, fresh granulations For terminal anesthesia we often use anaesthesin, dicain, xycain, trimecain, very rarely – novocain, because it badly penetrates through mucous membranes Conductive (regional) anesthesia - is an introduction of anesthetic into area of nervous truncs, ganglia, sensitive roots of spinal cord. Kinds of regional anesthesia: truncal (conductive), plexal (anesthesia of nervous plexuses), paravertebral (anesthesia of nerovus ganglia), spinal-cord, peridural For performing of this anesthesia novocain, xycain, trimecain, ultracain are used Infiltrative anesthesia – is a mixed kind of local anesthesia, in which nervous endings and fibres get turned off because of layer by layer infiltration of tissues with a solution of local anesthetic. For infiltrative anesthesia novocain, xycain, trimecain, ultracain are used Cocain (Cocainum) – alcaloid, which is extracted from leaves of South-American plant Erythroxylon coca. Its local anesthetic action overwhelms local anesthetic activity of novocain in 3 times and toxicity is 3-5 times greater It is used very rarely only for superficial anesthesia in stomatology, otholaryngology, urology in a form of 2-5 % solutions Erythroxylon coca TOXICOLOGY OF COCAIN Acute intoxication: short-time euforia, fear, tachicardia, exophtalm, dizziness, delirium, loss of consciousness, seizures, comatous condition, decreasing of arterial pressure, stop of breathing Chronic intoxication – cocainism: psychological and physical addiction, mental degradation, cretinism, atrophyc disorders, including perforation of nasal septum, gangrene, heavy cardiac arrythmias, cardiac arrest Novocain (Novocainum) – derivative of PABA (para-aminobenzoic acid) usage infiltrative anesthesia - 0,25-0,5 % solutions truncal anesthesia - 1-2 % solutions treatment blockades (paranephral, vagosympathetic) – 0,25-0,5 % solutions spinal cord anesthesia - 2-3 ml of 5 % solution (is introduced into subarachnoid space on the level higher than first lumbal vertebra) At recent time novocain was used for depression of reflexes, central nervous system, heart, in patients with gastritis, ulcer disease, hypertonic disease, stenocardia, neurodermitis, spasms of peripheral vessels. In this case this drug was introduced intravenously or intramuscularly Xycain (Lidocain) it is 2 times stronger (activity regarding) than novocain with the same toxicity usage for all kinds of local anesthesia: infiltrative - 0,25-0,5 % solutions conductive – 0,5-2 % solutions peridural – 0,5 % solution spinal cord – 5 % solution terminal – 4-10 % solutions Xycain (Lidocain) Xycain eliminates cardiac arrythmias of ventricular origin, i.e. extrasystolia, fibrillation of ventricules in acute miocardial infarction. In this cases xycain is administred intravenously, dropply, slowly, in a form of 0,2 % solution. Xycain (lidocain) can be used in individuals, which are sensybilized towards novocain and other anesthetics of complexed aehters group (dicain, anesthesin) Xycain (Lidocain) XYCAIN (LIDOCAIN) Trimecain anesthetic avtivity and action duration are 2 times greater, comparatively to novocain, toxicity is a bit higher Usage infiltrative - 0,125 %, 0,25 % and 0,5 % solutions truncal - 1 % and 2 % solutions peridural - 1 %, 2 % solutions spinal cord - 5 % solution terminal - 2-5 % solutions as an antiarythmic drug in cardial arythmias of ventricular origin - intravenously, at the begging in a form of 2 % solution very slowly after - dropply 0,2 % soluiton Bupivacain (marcain) one of the most active anesthetics of prolonged action (onset – 2-20 min, duration of action – 7 hours) Usage infiltrative, truncal, epidural anesthesia considerable cardiotoxicity ! Articain (ultracain) usage infiltrative and conductive anesthesia Analgetic action develops after 1-2 min. after introduction of the drug, lasts for 1-3,5 hours in stomatology - combined drug, which consists of ultracain and adrenalini hydrochloridum (epinephrin) - ultracain D-C Acute poisoning with local anesthetics Symptoms decreasing of arterial pressure, of heart activity, cardiac arrest, depression of CNS and breathing, seizures Treatment vasoconstriction drugs (noradrenaline, adrenaline), cardiotonic (strophantin, corglycon), antiseizure drugs (sibazone, tiopental-sodium) Prophilaxis usage of least possible volume and most possible dillution of the local anesthetics Astringent drugs Organic, of plant origin tannin, infusion of tea, herba Hyperici, flores Chamomillae, cortex Quercus Nonorganic Bismuthi subnitras, de-nol Oak tree (bark) Quercus robur L. TANNIN usage rinsing of mouth, pharynx, larynx – 1-2 % solution treatment of burned surfaces, cracks, bedsores – 3-10 % solutions gastric lavage in case of poisoning with salts of heavy metals and alcaloids – 0,5 % solution Nota bene! Tannin forms nonstable compounds with morphine, phisostigmine, atropin, nicotine, cocain Saint-John’s-wort (Hypericum perforatum L.) Matricary Chamomilla recutita L. Sage Salvia officinalis L. Drugs, which stimulate nervous endings IRRITATIVE DRUGS • • • • • Ammonium solution Menthol Oleum Terpenthini purified Mustard plaster Camphor Leaf Mustard Brassica juncea Ammonium solution 10 % (ammoniac) Usage • Unconsciousness (put a cotton ball moistured with ammonium solution to a nose) • In case of alcohol intoxication (orally 5-10 drops of solution dilluted in half of a glass of water) • For washing of surgeon’s hands (rarely) (0,5 % solution) Thanks for your attention! Good-bye !