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18 Anaesthesia and neuromuscular block SYNOPSIS The administration of general anaesthetics and neuromuscular blocking drugs is generally confined to trained specialists. Nevertheless, nonspecialists are involved in perioperative care and will benefit from an understanding of how these drugs act. Doctors from a variety of specialties use local anaesthetics and the pharmacology of these drugs is discussed in detail. General anaesthesia Pharmacology of anaesthetics Inhalation anaesthetics Intravenous anaesthetics Muscle relaxants: neuromuscular blocking drugs Local anaesthetics Obstetric analgesia and anaesthesia Anaesthesia in patients already taking drugs Anaesthesia in the diseased, the elderly and children; sedation in intensive therapy units General anaesthesia Until the mid-19th century such surgery as was possible had to be undertaken at tremendous speed. Surgeons did their best for terrified patients by using alcohol, opium, hyoscine, 1 or cannabis. With the introduction of general anaesthesia, surgeons could operate for the first time with careful delib- eration. The problem of inducing quick, safe and easily reversible unconsciousness for any desired length of time in man only began to be solved in the 1840s when the long-known substances nitrous oxide, ether, and chloroform were introduced in rapid succession. The details surrounding the first use of surgical anaesthesia were submerged in bitter disputes on priority following an attempt to take out a patent for ether. The key events around this time were: • 1842 — W. E. Clarke of Rochester, New York, administered for a dental extraction. However, this event was not made widely known at the time. • 1844 — Horace Wells, a dentist in Hartford, Connecticut, introduced nitrous oxide to produce anaesthesia during dental extraction. • 1846 — On October 16 William Morton, a Boston dentist, successfully demonstrated the anaesthetic properties of ether. • 1846 — On December 21 Robert Liston performed the first surgical operation in England under ether anaesthesia. 2 1 A Japanese pioneer of about 1800 wished to test the anaesthetic efficacy of a herbal mixture including solanaceous plants (hyoscine-type alkaloids). His elderly mother volunteered as subject since she was anyway expected to die soon. But the pioneer administered it to his wife for, 'as all three agreed, he could find another wife, but could never get another mother' (Journal of the American Medical Association 1966 197:10). 345 18 ANAESTHESIA AND N E U R O M U S C U L A R BLOCK • 1847 — James Y. Simpson, professor of midwifery at the University of Edinburgh, introduced chloroform for the relief of labour pain. The next important developments in anaesthesia were in the 20th century when the appearance of new drugs both as primary general anaesthetics and as adjuvants (muscle relaxants), new apparatus, and clinical expertise in rendering prolonged anaes- thesia safe, enabled surgeons to increase their range. No longer was the duration and type of surgery determined by patients' capacity to endure pain. STAGES OF GENERAL ANAESTHESIA Surgical anaesthesia is classically divided into four stages: analgesia, delirium, surgical anaesthesia (subdivided into four planes), and medullary paralysis (overdose). This gradual procession of stages was described when ether was given to un- premedicated patients, a slow unpleasant process. Ether is obsolete and the speed of induction with modern inhalational agents or intravenous anaes- thesia drugs makes a detailed description of these separate stages superfluous. Balanced surgical anaesthesia (hypnosis with analgesia and muscular relaxation) with a single drug requires high doses that will cause adverse effects such as slow and unpleasant recovery, and depression of cardiovascular and respiratory func- tion. In modern practice, different drugs are used to attain each objective so that adverse effects are minimised. DRUGS USED The perioperative period may be divided into three phases and in each of these a variety of factors will determine the choice of drugs given: 2 Frederick Churchill, a butler from Harley Street, had his leg amputated at University College Hospital, London. After removing the leg in 28 seconds, a skill necessary to compensate for the previous lack of anaesthetics, Robert Listen turned to the watching students, and said "this Yankee dodge, gentlemen, beats mesmerism hollow". That night he anaesthetised his house surgeon in the presence of two ladies. Merrington W R1976 University College Hospital and its Medical School: A History. Heinemann, London. Before surgery, an assessment is made of: • the patient's physical and psychological condition • any intercurrent illness • the relevance of any existing drug therapy. All of these may influence the choice of anaesthetic drugs. During surgery, drugs will be required to provide: • unconsciousness • analgesia • muscular relaxation when necessary • control of blood pressure, heart rate, and respiration. After surgery, drugs will play a part in: • reversal of neuromuscular block • relief of pain, and nausea and vomiting • other aspects of postoperative care, including intensive care. Patients are often already taking drugs affecting the central nervous and cardiovascular systems and there is considerable potential for interaction with anaesthetic drugs. The techniques for giving anaesthetic drugs and the control of ventilation and oxygenation are of great importance, but are outside the scope of this book. Before surgery (premedication) The principal aims are to provide: Anxiolysis and amnesia. A patient who is going to have a surgical operation is naturally apprehensive and this anxiety is reduced by reassurance and a clear explanation of what to expect. Very anxious patients will secrete a lot of adrenaline (epineph- rine) from the suprarenal medulla and this may make them more liable to cardiac arrhythmias with some anaesthetics. In the past, sedative pre- medication was given to virtually all patients under- going surgery. This practice has changed dramatically because of the increasing proportion of operations undertaken as 'day cases' and the recognition that sedative premedication prolongs recovery. Sedative premedication is now reserved for those who are 346 18 particularly anxious or those undergoing major surgery. Benzodiazepines, such as temazepam (10-30mg for an adult), provide anxiolysis and amnesia for the immediate presurgical period. Analgesia is indicated if the patient is in pain preoperatively or it can be given pre-emptively to prevent postoperative pain. Severe preoperative pain is treated with a parenteral opioid such as morphine. Nonsteroidal anti-inflammatory drugs and paracetamol are commonly given orally pre- operatively to prevent postoperative pain after minor surgery. For moderate or major surgery, these drugs are supplemented with an opioid towards the end of the procedure. Drying of bronchial and salivary secretions using antimuscarinic drugs to inhibit the parasympathetic autonomic system is rarely undertaken these days. The exceptions include those patients who are expected to require an awake fibreoptic intubation or those undergoing bronchoscopy. Glycopyrronium is the antimuscarinic of choice for this purpose and atropine and hyoscine are alternatives. Timing. Premedication is given about an hour before surgery. Gastric contents. Pulmonary aspiration of gastric contents can cause severe pneumonitis. Patients at risk of aspiration are those with full stomachs, e.g., bowel obstruction, recently consumed food and drink, third trimester of pregnancy, and those with incompetent gastro-oesophageal sphincters, e.g. hiatus hernia. A single dose of an antacid, e.g. sodium citrate, may be given before a general anaesthetic to neutralise gastric acid in high-risk patients. Alter- natively or additionally, a histamine H 2 -receptor blocker, e.g. ranitidine, or proton-pump inhibitor, e.g. omeprazole, will reduce gastric secretion volume as well as acidity. Metoclopramide usefully hastens gastric emptying, increases the tone of the lower oesophageal sphincter and is an antiemetic. During surgery The aim is to induce unconsciousness, analgesia and muscular relaxation. Total muscular relaxation GENERAL ANAESTHESIA (paralysis) is required for some surgical procedures, e.g., intra-abdominal surgery, but most surgery can be undertaken without neuromuscular blockade. A typical general anaesthetic consists of: • Induction: 1. Usually intravenous: pre-oxygenation followed by a small dose of an opioid, e.g., fentanyl or alfentanil to provide analgesia and sedation, followed by propofol or, less commonly, thiopental or etomidate to induce anaesthesia. Airway patency is maintained with an oral airway and face-mask, a laryngeal mask air- way (LMA), or a tracheal tube. Insertion of a tracheal tube usually requires paralysis with a neuromuscular blocker and is undertaken if there is a risk of pulmonary aspiration from regurgitated gastric contents or from blood. 2. Inhalational induction, usually with sevo- flurane, is undertaken taken less commonly. It is used in children, particularly if intravenous access is difficult, and in patients at risk from upper airway obstruction. • Maintenance: 1. Most commonly with nitrous oxide and oxy- gen, or oxygen and air, plus a volatile agent, e.g., isoflurane or sevoflurane. Additional doses of a neuromuscular blocker or opioid are given as required. 2. A continuous intravenous infusion of propofol can be used to maintain anaesthesia. This technique of total intravenous anaesthesia is becoming more popular because the quality of recovery may be better than after inhalational anaesthesia. When appropriate, peripheral nerve block with a local anaesthetic, or neural axis block, e.g., spinal or epidural, provides intraoperative analgesia and muscle relaxation. These local anaesthetic techniques provide excellent postoperative analgesia. After surgery The anaesthetist ensures that the effects of neuro- muscular blocking agents and opioid-induced res- piratory depression have either worn off or have been adequately reversed by an antagonist; the patient is not left alone until conscious, with protective reflexes restored, and a stable circulation. 347 18 AN AESTHESIA AND NEUROMUSCULAR BLOCK Relief of pain after surgery can be achieved with a variety of techniques. An epidural infusion of a mixture of local anaesthetic and opioid provides excellent pain relief after major surgery such as laparotomy. Parenteral morphine, given intermit- tently by a nurse or by a patient-controlled system, will also relieve moderate or severe pain but has the attendant risk of nausea, vomiting, sedation and respiratory depression. The addition of regular paracetamol and a NSAID, given orally or rectally, will provide additional pain relief and reduce the requirement for morphine. NSAIDs are contra- indicated if there is a history of gastrointestinal ulceration of if renal blood flow is compromised. Postoperative nausea and vomiting (PONV) is common after laparotomy and major gynaecological surgery, e.g., abdominal hysterectomy. The use of propofol, particularly when given to maintain anaesthesia, has dramatically reduced the incidence of PONV. Antiemetics, such as cyclizine, metoclo- pramide, and ondansetron, may be helpful. SOME SPECIALTECHNIQUES Dissociative anaesthesia is a state of profound analgesia and anterograde amnesia with minimal hypnosis during which the eyes may remain open (see ketamine, p. 353). It is particularly useful where modern equipment is lacking or where access to the patient is limited, e.g. at major accidents or on battlefields. Sedation and amnesia without analgesia are provided by midazolam i.v. or, less commonly nowadays, diazepam. These drugs can be used alone for procedures causing mild discomfort, e.g. endoscopy, and with a local anaesthetic where more pain is expected, e.g., removal of impacted wisdom teeth. Benzodiazepines produce anterograde, but not retrograde, amnesia. By definition, the sedated patient remains responsive and cooperative. (For a general account of benzodiazepines and the com- petitive antagonist flumazenil, see Ch. 19.) Benzodiazepines can cause respiratory depres- sion and apnoea especially in the elderly and in patients with respiratory insufficiency. The com- bination of an opioid and a benzodiazepine is particularly dangerous. Benzodiazepines depress laryngeal reflexes and place the patient at risk of inhalation of oral secretions or dental debris. Entonox, a 50:50 mixture of nitrous oxide and oxygen, is breathed by the patient using a demand valve. It is particularly useful in the prehospital environment and for brief procedures, such as splinting limbs. Pharmacology of anaesthetics All successful general anaesthetics are given intra- venously or by inhalation because these routes allow closest control over blood concentrations and so of effect on the brain. MODE OF ACTION General anaesthetics act on the brain, primarily on the midbrain reticular activating system. Many anaesthetics are lipid soluble and there is good correlation between this and anaesthetic effective- ness (the Overton-Meyer hypothesis); the more lipid soluble tend to be the more potent anaes- thetics, but such a correlation is not invariable. Some anaesthetic agents are not lipid soluble and many lipid soluble substances are not anaesthetics. Until recently it was thought that the principal site of action of general anaesthetics was the neuronal lipid bilayer membrane. The current view is that their anaesthetic activity is caused by interaction with protein receptors. It is likely that there are several modes of action, but the central mechanism of action of volatile anaesthetics is thought to be facilitation at the inhibitory y-aminobutyric acid (GABA A ) and glycine receptors. Agonists at these receptors open chloride ion channels and the influx of chloride ions into the neuron results in hyper- polarisation. This prevents propagation of nerve impulses and renders the patient unconscious. Some general anaesthetics increase the time that the chloride channels are open while others increase the frequency of chloride channel opening. 348 18 ASSESSMENT OF ANAESTHETIC AGENTS Comparison of the efficacy of inhalational agents is made by measuring the minimum alveolar concen- tration (MAC) in oxygen required to prevent move- ment in response to a standard surgical skin incision in 50% of subjects. The MAC of the volatile agent is reduced by the co-administration of nitrous oxide. Inhalation anaesthetics PREFERRED ANAESTHETICS The preferred inhalation agents are those that are minimally irritant and nonflammable, and comprise nitrous oxide and the fluorinated hydrocarbons, e.g., isoflurane. PHARMACOKINETICS (VOLATILE LIQUIDS, GASES) The level of anaesthesia is correlated with the tension (partial pressure) of anaesthetic drug in the brain tissue and this is dependent on the develop- ment of a series of tension gradients from the high partial pressure delivered to the alveoli and decreasing through the blood to the brain and other tissues. These gradients are dependent on the blood/gas and tissue/gas solubility coefficients, as well as on alveolar ventilation and organ blood flow. An anaesthetic that has high solubility in blood, i.e., a high blood/gas partition coefficient, will provide a slow induction and adjustment of the depth of anaesthesia. This is because the blood acts as a reservoir (store) for the drug so that it does not enter the brain easily until the blood reservoir has been filled. A rapid induction can be obtained by increasing the concentration of drug inhaled initially and by hyperventilating the patient. Agents that have low solubility in blood, i.e., a low blood/gas partition coefficient (nitrous oxide, sevoflurane), provide a rapid induction of anaes- thesia because the blood reservoir is small and agent is available to pass into the brain sooner. INHALATION AGENTS During induction of anaesthesia the blood is taking up anaesthetic agent selectively and rapidly and the resulting loss of volume in the alveoli leads to a flow of agent into the lungs that is independent of respiratory activity. When the anaesthetic is discontinued the reverse occurs and it moves from the blood into the alveoli. In the case of nitrous oxide, this can account for as much as 10% of the expired volume and so can significantly lower the alveolar oxygen concentration. Thus mild hypoxia occurs and lasts for as long as 10 minutes. Though harmless to most, it may be a factor in cardiac arrest in patients with reduced pulmonary and cardiac reserve, especially when administration of the gas has been at high concentration and prolonged, when the outflow is especially copious. Oxygen should therefore be given to such patients during the last few minutes of anaesthesia and the early postanaesthetic period. This phenomenon, diffusion hypoxia, occurs with all gaseous anaesthetics, but is most prominent with gases that are relatively insoluble in blood, for they will diffuse out most rapidly when the drug is no longer inhaled, i.e. just as induction is faster, so is elimination. Nitrous oxide is especially powerful in this respect because it is used at concentrations of up to 70%. Highly blood-soluble agents will diffuse out more slowly, so that recovery will be slower just as induction is slower, and with them diffusion hypoxia is insignificant. NITROUS OXIDE Nitrous oxide (1844) is a gas with a slightly sweetish smell. It is neither flammable nor explosive. It produces light anaesthesia without demonstrably depressing the respiratory or vasomotor centre provided that normal oxygen tension is maintained. Advantages. Nitrous oxide reduces the require- ment for other more potent and intrinsically more toxic anaesthetic agents. It has a strong analgesic action; inhalation of 50% nitrous oxide in oxygen (Entonox) may have similar effects to standard doses of morphine. Induction is rapid and not unpleasant although transient excitement may occur, as with all agents. Recovery time rarely exceeds 4 min even after prolonged administration. 349 18 ANAESTHESIA AND N E U R O M U S C U L A R BLOCK Disadvantages. Nitrous oxide is expensive to buy and to transport. It must be used in conjuction with more potent anaesthetics to produce full surgical anaesthesia. Uses. Nitrous oxide is used to maintain surgical anaesthesia in combination with other anaesthetic agents, e.g., isoflurane or propofol, and, if required, muscle relaxants. Entonox provides analgesia for obstetric practice, for emergency management of injuries, and during postoperative physiotherapy. Dosage and administration. For the maintenance of anaesthesia, nitrous oxide must always be mixed with at least 30% oxygen. For analgesia, a concen- tration of 50% nitrous oxide with 50% oxygen usually suffices. Contraindications. Any closed, distendable air- filled space expands during administration of nitrous oxide, which moves into it from the blood. It is therefore contraindicated in patients with: demon- strable collections of air in the pleural, pericardial or peritoneal spaces; intestinal obstruction; arterial air embolism; decompression sickness; severe chronic obstructive airway disease; emphysema. Nitrous oxide will cause pressure changes in closed, noncompliant spaces such as the middle ear, nasal sinuses, and the eye. Precautions. Continued administration of oxygen may be necessary during recovery, especially in elderly patients (see diffusion hypoxia, above). Adverse effects. The incidence of nausea and vomiting increases with the duration of anaes- thesia. Nitrous oxide interferes with the synthesis of methionine, deoxythymidine and DNA. Exposure of to nitrous oxide for more than 4 hours can cause megaloblastic changes in the bone marrow. Because prolonged and repeated exposure of staff as well as of patients may be associated with bone-marrow de- pression and teratogenic risk, scavenging systems are used to minimise ambient concentrations in operating theatres. Drug interactions. Addition of 50% nitrous oxide/ oxygen mixture to another inhalational anaesthetic reduces the required dosage (minimum alveolar concentration, MAC) of the latter by about 50%. Storage. Nitrous oxide is supplied under pressure in cylinders, which must be maintained below 25°C. Cylinders containing premixed oxygen 50% and nitrous oxide 50% (Entonox) are available for analgesia. The constituents separate out at -7°C, in which case adequate mixing must be assured before use. HALOGENATED ANAESTHETICS Halothane was the first halogenated agent to be used widely, but in the developed world it has been largely superseded by isoflurane and sevoflurane. We provide a detailed description of isoflurane, and of the others in so far as they differ. The MAC of some volatile agents is: • Isoflurane 1.2% • Enflurane 1.7% • Sevoflurane 2.0% • Halothane 0.74%. Isoflurane Isoflurane is a volatile colourless liquid, which is not flammable at normal anaesthetic concentrations. It is relatively insoluble, and has a lower blood/gas coefficient than halothane or enflurane, which allows rapid adjustment of the depth of anaesthesia. It has a pungent odour and can cause bronchial irritation, which makes inhalational induction unpleasant. Isoflurane is minimally metabolised (0.2%), and none of the breakdown products has been related to anaesthetic toxicity. Respiratory effects. Isoflurane causes respiratory depression: the respiratory rate increases, tidal vol- ume decreases, and the minute volume is reduced. The ventilatory response to carbon dioxide is diminished. Although it irritates the upper airway it is a bronchodilator. Cardiovascular effects. Anaesthetic concentrations of isoflurane, i.e. 1-1.5 MAC, cause only a slight impairment of myocardial contractility and stroke volume and cardiac output is usually maintained 350 18 by a reflex increase in heart rate. Isoflurane causes peripheral vasodilatation and reduces blood press- ure. It does not affect atrioventricular conduction and does not sensitise the heart to catecholamines. Low concentrations of isoflurane (< 1 MAC) do not increase cerebral blood flow or intracranial press- ure, and cerebral autoregulation is maintained. Isoflurane is a potent coronary vasodilator and in the presence of a coronary artery stenosis it may cause redistribution of blood away from an area of inadequate perfusion to one of normal perfusion. This phenomenon of 'coronary steal' may cause regional myocardial ischaemia. Other effects. Isoflurane relaxes voluntary muscles and potentiates the effects of nondepolarising muscle relaxants. Isoflurane depresses cortical EEG activity and does not induce abnormal electrical activity or convulsions. Sevoflurane is a chemical analogue of isoflurane. It is less chemically stable than the other volatile anaesthetics in current use. About 3% is metabolised in the body and it is degraded by contact with carbon dioxide absorbents, such as soda lime. The reaction with soda lime causes the formation of a vinyl ether (Compound A), which may be nephro- toxic. Sevoflurane is less soluble than isoflurane and is very pleasant to breathe, which makes it an excellent choice for inhalational induction of anaes- thesia, particularly in children. The respiratory and cardiovascular effects of Sevoflurane are very similar to isoflurane. Enflurane is a structural isomer of isoflurane. It is more soluble than isoflurane. It causes more respiratory depression than the other volatile anaesthetics and hypercapnia is almost inevitable in patients breathing spontaneously. It causes more cardiovascular depression than isoflurane and is occasionally associated with cardiac arrythmias. Two percent of enflurane is metabolised and prolonged administration or use in enzyme-induced patients generates sufficient free inorganic fluoride from the drug molecule to cause polyuric renal failure. There have been a few cases of jaundice and heptatoxicity associated with enflurane but the incidence of about one in 1-2 million anaesthetics is lower than with halothane. INHALATION AGENTS Desflurane has the lowest blood/gas partition co- efficient of any inhaled anaesthetic agent and thus gives particularly rapid onset and offset of effect. As it undergoes negligible metabolism (0.03%), any release of free inorganic fluoride is minimised; this characteristic favours its use for prolonged anaes- thesia. Desflurane is extremely volatile and cannot be administered with conventional vaporisers. It has a very pungent odour and causes airway irritation to an extent that limits its rate of induction of anaesthesia. Halothane has the highest blood/gas partition coefficient of the volatile anaesthetic agents and recovery from halothane anaesthesia is compara- tively slow. It is pleasant to breathe and is second choice to Sevoflurane for inhalational induction of anaesthesia. Halothane reduces cardiac output more than any of the other volatile anaesthetics. It sensitises the heart to the arrhythmic effects of catecholamines and hypercapnia; arrhythmias are common, in particular atrioventricular dissociation, nodal rhythm and ventricular extrasystoles. Halo- thane can trigger malignant hyperthermia in those who are genetically predisposed (see p. 363). About 20% of halothane is metabolised and it induces hepatic enzymes, including those of anaes- thetists and operating theatre staff. Hepatic damage occurs in a small proportion of exposed patients. Typically fever develops 2 or 3 days after anaes- thesia accompanied by anorexia, nausea and vomit- ing. In more severe cases this is followed by transient jaundice or, very rarely, fatal hepatic necrosis. Severe hepatitis is a complication of repeatedly administered halothane anaesthesia and has an incidence of 1:50000. It follows immune sensitisation to an oxidative metabolite of halothane in susceptible individuals. This serious complication, along with the other disadvantages of halothane and the popularity of sevoflurane for inhalational induction, has almost eliminated its use in the developed world. It remains in common use other parts of the world because it is comparatively inexpensive. OXYGEN IN ANAESTHESIA Supplemental oxygen is always used with inhala- tional agents to prevent hypoxia, even when air is used as the carrier gas. The concentration of oxygen 351 18 AN AESTHESIA AND N E U R O M U S C U L A R BLOCK in inspired anaesthetic gases is usually at least 30%, but oxygen should not be used for prolonged periods at a greater concentration than is necessary to prevent hypoxaemia. After prolonged adminis- tration, concentrations greater than 80% have a toxic effect on the lungs, which presents initially as a mild substernal irritation progressing to pul- monary congestion, exudation and atelectasis. Use of unnecessarily high concentrations of oxygen in incubators causes retrolental fibroplasia and per- manent blindness in premature infants. Oxygen is supplied under pressure in cylinders, when it remains in the gaseous state. In most hospitals a vacuum insulated evaporator is used to store oxygen in liquid form. This provides for huge volumes of gaseous oxygen and will supply all the piped oxygen outlets in the hospital. ATMOSPHERIC POLLUTION OF OPERATING THEATRES Pollution by inhalation anaesthetics has been suspected of being harmful to theatre personnel. Epidemiological studies have raised questions relating to excess of fetal malformations and mis- carriages, hepatitis and cancer in operating theatre personnel. Sensible use of preventive measures renders the risks negligible, e.g. use of circle systems that allow low fresh gas flows, scavenging systems, and improved ventilation of theatres. The increasing use of total intravenous anaesthesia (TIVA) and regional anaesthesia will also reduce pollution. Intravenous anaesthetics Intravenous anaesthetics should be given only by those fully trained in their use and who are experi- enced with a full range of techniques of managing the airway, including tracheal intubation. PHARMACOKINETICS Intravenous anaesthetics allow an extremely rapid induction because the blood concentration can be raised rapidly, establishing a steep concentration gradient and expediting diffusion into the brain. The rate of transfer depends on the lipid solubility and arterial concentration of the unbound, non- ionised fraction of the drug. After a single, induction dose of an intravenous anaesthetic recovery occurs quite rapidly as the drug is redistributed around the body and the plasma concentration reduces. Recovery from a single dose of intravenous anaes- thetic is not related to its rate of metabolic break- down. With the exception of propofol, repeated doses or infusions of intravenous anaesthetics will result in considerable accumulation and prolonged recovery. Attempts to use thiopental as the sole anaesthetic in war casualties led to its being described as an ideal form of euthanasia. 3 It is common practice to induce anaesthesia intravenously and then to use a volatile anaesthetic for maintenance. When administration of a volatile anaesthetic is stopped, it is eliminated quickly through the lungs and the patient regains consciousness. The recovery from propofol is rapid, even after repeat doses or an infusion. This advantage, and others, has resulted in propofol displacing thiopental as the most popular intravenous anaesthetic. Propofol Propofol (2,6-diisopropylphenol) is available as a 1% or 2% emulsion, which contains soya bean oil and purified egg phosphatide. Induction of anaes- thesia with 1.5-2.5 mg/kg occurs within 30 seconds and is smooth and pleasant with a low incidence of excitatory movements. It causes pain on injection but adding lidocaine 20 mg to an ampoule of propofol eliminates this. The recovery from propofol is rapid and the incidence of nausea and vomiting is extremely low, particularly when propofol is used as the sole anaesthetic. Recovery from a continuous infusion of propofol is relatively rapid. On stopping the infusion the plasma concentration decreases rapidly as a result of both redistribution and clear- ance of the drug. Special syringe pumps incor- porating pharmacokinetic algorithms allow the anaesthetist to select a target plasma propofol con- centration (e.g. 6 micrograms/ml for induction of anaesthesia) once details of the patient's age and weight have been entered. This technique of target- 3 Halford J J 1943 A critique of intravenous anaesthesia in war surgery. Anesthesiology 4: 67. 352 18 controlled infusion (TCI) provides a convenient method for giving a continuous infusion of propofol. Central nervous system. Propofol causes dose- dependent cortical depression and is an anticon- vulsant. It depresses laryngeal reflexes more than barbiturates, which is an advantage when inserting a laryngeal mask airway. Cardiovascular system. Propofol reduces vascular tone, which lowers systemic vascular resistance and central venous pressure. The heart rate remains unchanged and the result is a fall in blood pressure to about 70-80% of the preinduction level and a small reduction in cardiac output. Respiratory system. Unless it is undertaken very slowly, induction with propofol causes transient apnoea. On resumption of respiration there is a reduction in tidal volume and increase in rate. Metabolism. Propofol is conjugated in the liver by glucuronidation making it more water soluble; 88% then appears in the urine and 2% in the faeces. Thiopental (thiopentone) Thiopental is a very short-acting barbiturate, which induces anaesthesia smoothly, within one arm-to- brain circulation time. The typical induction dose is 3-5mg/kg. Rapid distribution (initial t 1 / 2 4min) allows swift recovery after a single dose. The terminal t l / 2 of thiopental is 11 h and repeated doses or continuous infusion lead to significant accumu- lation in fat and very prolonged recovery. Thiopental is metabolised in the liver. The incidence of nausea and vomiting after thiopental is slightly higher than after propofol. The pH of thiopental is 11 and considerable local damage results if it extravasates. Accidental intra-arterial injection will also cause serious injury distal to the injection site. Central nervous system. Thiopental has no anal- gesic activity and may be antanalgesic. It is a potent anticonvulsant. Cerebral metabolic rate of oxygen consumption (CMRO 2 ) is reduced, which leads to cerebral vasoconstriction with a concomitant reduction in cerebral blood flow and intracranial pressure. INTRAVENOUS AGENTS Cardiovascular system. Thiopental reduces vas- cular tone, causing hypotension and a slight com- pensatory increase in heart rate. Antihypertensives or diuretics may augment the hypotensive effect. Respiratory system. Thiopental reduces respiratory rate and tidal volume. Methohexitone is a barbiturate similar to thiopental but its terminal t l / 2 is considerably shorter. Since the introduction of propofol, its use is almost entirely confined to inducing anaesthesia for electrocontro- vulsive therapy (ECT). Propofol shortens seizure duration and may reduce the efficacy of ECT. Etomidate is a carboxylated imidazole, which is formulated in a mixture of water and propylene glycol. It causes pain on injection and excitatory muscle movements are common on induction of anaesthesia. It is associated with a 20% incidence of nausea and vomiting. Etomidate causes adreno- cortical suppression by inhibiting 11 (3- and 17 [3- hydroxylase and for this reason is not used for prolonged infusion; single bolus doses cause short- lived, clinically insignificant adrenocortical sup- pression. Despite all these disadvantages it remains in common use, particularly for emergency anaes- thesia, because it causes less cardiovascular depres- sion and hypotension than thiopental or propofol. Ketamine Ketamine is a phencyclidine (hallucinogen) deriva- tive and an antagonist of the NMDA-receptor. 4 In anaesthetic doses it produces a trance-like state known as dissociative anaesthesia (sedation, amnesia, dissociation, analgesia). Advantages. Anaesthesia persists for up to 15 min after a single intravenous injection and is charac- terised by profound analgesia. Ketamine may be used as the sole analgesic agent for diagnostic and minor surgical interventions. In contrast to most other anaesthetic drugs, ketamine usually produces a tachycardia and increases blood pressure and cardiac output. This effect makes it a popular choice for inducing anaesthesia in shocked patients. The 4 N-methyl-D-aspartate. 353 18 AN AESTH ESI A AN D N E U R O M U S C U L A R BLOCK cardiovascular effects of ketamine are accompanied by an increase in plasma noradrenaline (norepi- nephrine) concentration. Because pharyngeal and laryngeal reflexes are only slightly impaired, the airway may be less at risk than with other general anaesthetic techniques. It is a potent bronchodilator and is sometimes used to treat severe bronchospasm in those asthmatics requiring mechanical ventilation. (See also Dissociative anaesthesia, p. 348.) Disadvantages. Ketamine produces no muscular relaxation. It increases intracranial and intraocular pressure. Hallucinations can occur during recovery (the emergence reaction), but they are minimised if ketamine is used solely as an induction agent and followed by a conventional inhalational anaesthetic. Their incidence is reduced by administration of a benzodiazepine both as a premedication and after the procedure. Uses. Subanaesthetic doses of ketamine can be used to provide analgesia for painful procedures of short duration such as the dressing of burns, radio- therapeutic procedures, marrow sampling and minor orthopaedic procedures. Ketamine can be used for induction of anaesthesia prior to administration of inhalational anaesthetics, or for both induction and maintenance of anaesthesia for short-lasting diag- nostic and surgical interventions, including dental procedures that do not require skeletal muscle relaxation. It is of particular value for children requiring frequent repeated anaesthetics. Dosage and administration. Premedication with atropine will reduce the salivary secretions produced by ketamine and a benzodiazepine will reduce the incidence of hallucinations. Induction. Intravenous route: 1-2 mg/kg by slow intravenous injection over a period of 60 seconds. A dose of 2 mg/kg produces surgical anaesthesia within 1-2 min, which will last 5-10 min. Intra- muscular route: 5-10 mg/kg by deep intramuscular injection. This dose produces surgical anaesthesia within 3-5 min and may be expected to last up to 25 min. Maintenance. Following induction, serial doses of 50% of the original intravenous dose or 25% of the intramuscular dose is given to prevent movement in response to surgical stimuli. Tonic and clonic movements resembling seizures occur in some patients. These do not indicate a light plane of anaesthesia or a need for additional doses of the anaesthetic. A dose of 0.5 mg/kg i.m. or i.v. provides excellent analgesia and may be supplemented by further doses of 0.25 mg/kg. Recovery. Return to consciousness is gradual. Emergence reactions with delirium may occur. Their incidence is reduced by benzodiazepine pre- medication and by avoiding unnecessary disturb- ance of the patient during recovery. Contraindications include: moderate to severe hypertension, congestive cardiac failure or a history of stroke; acute or chronic alcohol intoxication, cerebral trauma, intracerebral mass or haemorrhage or other causes of raised intracranial pressure; eye injury and increased intraocular pressure; psychi- atric disorders such as a schizophrenia and acute psychoses. Precautions. Ketamine should be used under the supervision of a clinician experienced in tracheal intubation, should this become necessary. Pulse and blood pressure must be monitored closely. Supple- mentary opioid analgesia is often required in surgical procedures causing visceral pain. Use in pregnancy. Ketamine is contraindicated in pregnancy before term, since it has oxytocic activity. It is also contraindicated in patients with eclampsia or pre-eclampsia. It may be used for assisted vaginal delivery by an experienced anaesthetist. Ketamine is better suited for use during caesarean section; it causes less fetal and neonatal depression than other anaesthetics. Muscle relaxants NEUROMUSCULAR BLOCKING DRUGS A lot of surgery, especially of the abdomen, requires 354 [...]... AN D N E U R O M U S C U L A R B L O C K Neuromuscular blocking agents used in clinical practice interfere with this process Natural substances that prevent the release of acetylcholine at nerve endings exist, e.g Clostridium botulinum toxin (see p 429) and some venoms There are two principal mechanisms by which drugs used clinically interfere with neuromuscular transmission: 1 By competition with acetylcholine... comparatively short acting (10-15 minutes), depending on the initial dose Mivacurium can cause some hypotension because of histamine release Pancuronium was the first steroid-derived neuromuscular blocker in clinical use It is longer acting than vecuronium and causes a slight tachycardia Tubocurarine is obsolete and is no longer available in the UK It is a potent antagonist at autonomic ganglia and causes... hyperthermia, p 427) ANAPHYLAXIS Anaphylactic reactions result from the interaction of antigens with specific IgE antibodies, which have been formed by previous exposure to the antigen Anaphylactoid reactions are clinically indistinguishable from anaphylaxis but do not result from prior exposure to a triggering agent and do not involve IgE Intravenous anaesthetics and muscle relaxants can cause anaphylactic or... relaxants are responsible for 70% of anaphylactic reactions during anaesthesia and suxamethonium accounts for almost half of these Local anaesthetics Cocaine had been suggested as a local anaesthetic for clinical use when Sigmund Freud investigated the alkaloid in Vienna in 1884 with Carl Koller The latter had long been interested in the problem of local anaesthesia in the eye, for general anaesthesia... in ophthalmology Observing that numbness of the mouth occurred after taking cocaine orally he realised that this was a local anaesthetic effect He tried cocaine on animals' eyes and introduced it into clinical ophthalmological practice, whilst Freud was on holiday Freud had already thought of this use and discussed it but, appreciating that sex was of greater importance than surgery, he had gone to... then began to search for less toxic substitutes, with the result that procaine was introduced in 1905 Desired properties Innumerable compounds have local anaesthetic properties, but few are suitable for clinical use Useful substances must be watersoluble, sterilisable by heat, have a rapid onset of effect, a duration of action appropriate to the operation to be performed, be nontoxic, both locally 358... which, in the concentrations used, does not affect the heart rate or blood pressure and may be preferable in patients with cardiovascular disease OTHER EFFECTS Local anaesthetics also have the following clinically important effects in varying degree: • Excitation of parts of the central nervous system, which may manifest as anxiety, restlessness, tremors, euphoria, agitation and even convulsions, which . of specialties use local anaesthetics and the pharmacology of these drugs is discussed in detail. General anaesthesia Pharmacology of anaesthetics Inhalation . general anaesthetics and as adjuvants (muscle relaxants), new apparatus, and clinical expertise in rendering prolonged anaes- thesia safe, enabled surgeons

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