Anesthetics muscle relaxants

Rapacuronium bromide Raplon Organon Anesthetic, muscle relaxant 9/19/1999 3/30/2001 7 months Bronchospasm 23 million... 

According to whether receptor occupancy leads to a blockade or an excitation of the endplate, one distinguishes nondepolarizing from depolarizing muscle relaxants (p. 186). As adjuncts to general anesthetics, muscle relaxants help to ensure that surgical procedures are not disturbed by muscle contractions of the patient (p. 216). 

Clinically important, potentially hazardous interactions with beta-blockers, local anesthetics, muscle relaxants... 

Isoflurane is a respiratory depressant (71). At concentrations which are associated with surgical levels of anesthesia, there is Htde or no depression of myocardial function. In experimental animals, isoflurane is the safest of the oral clinical agents (72). Cardiac output is maintained despite a decrease in stroke volume. This is usually because of an increase in heart rate. The decrease in blood pressure can be used to produce "deHberate hypotension" necessary for some intracranial procedures (73). This agent produces less sensitization of the human heart to epinephrine relative to the other inhaled anesthetics. Isoflurane potentiates the action of neuromuscular blockers and when used alone can produce sufficient muscle relaxation (74). Of all the inhaled agents currently in use, isoflurane is metabolized to the least extent (75). Unlike halothane, isoflurane does not appear to produce Hver injury and unlike methoxyflurane, isoflurane is not associated with renal toxicity. 

Desflurane is less potent than the other fluorinated anesthetics having MAC values of 5.7 to 8.9% in animals (76,85), and 6% to 7.25% in surgical patients. The respiratory effects are similar to isoflurane. Heart rate is somewhat increased and blood pressure decreased with increasing concentrations. Cardiac output remains fairly stable. Desflurane does not sensitize the myocardium to epinephrine relative to isoflurane (86). EEG effects are similar to isoflurane and muscle relaxation is satisfactory (87). Desflurane is not metabolized to any significant extent (88,89) as levels of fluoride ion in the semm and urine are not increased even after prolonged exposure. Desflurane appears to offer advantages over sevoflurane and other inhaled anesthetics because of its limited solubiHty in blood and other tissues. It is the least metabolized of current agents. 

Neuroleptic analgesia is so called because the combination of a major tranquilizer, a neuroleptic dmg, and a potent opiate produces an anesthetic state characterized by sedation, apathy, and mental detachment (see Psychopharmacological agents) (152). Iimovar [8067-59-2] a combination of droperidol [648-72-2], C22H22FN2O2, (19) and fentanyl (9) citrate, is used for procedures that do not require muscle relaxation. However, the onset of action is slow. 

Verapamil. Verapamil hydrochloride (see Table 1) is a synthetic papaverine [58-74-2] C2qH2 N04, derivative that was originally studied as a smooth muscle relaxant. It was later found to have properties of a new class of dmgs that inhibited transmembrane calcium movements. It is a (+),(—) racemic mixture. The (+)-isomer has local anesthetic properties and may exert effects on the fast sodium channel and slow phase 0 depolarization of the action potential. The (—)-isomer affects the slow calcium channel. Verapamil is an effective antiarrhythmic agent for supraventricular AV nodal reentrant arrhythmias (V1-2) and for controlling the ventricular response to atrial fibrillation (1,2,71—73). 

The anesthesiologist selects the anesthetic drug that will produce safe anesthesia, analgesia (absence of pain), and in some surgeries, effective skeletal muscle relaxation. General anesthesia is most commonly achieved when the anesthetic vapors are inhaled or administered intravenously (IV). Volatile liquid anesthetics produce anesthesia when their vapors are inhaled. Volatile liquids are liquids that evaporate on exposure to air. Examples of volatile liquids include halothane, desflurane, and enflurane. Gas anesthetics are combined with oxygen and administered by inhalation. Examples of gas anesthetics are nitrous oxide and cyclopropane. 

An anesthetic gas, cyclopropane has a rapid onset of action and may be used for induction and maintenance of anesthesia Skeletal muscle relaxation is produced with full anesthetic doses. Cyclopropane is supplied in orange cylinders. Disadvantages of cyclopropane are difficulty in detecting the planes of anesthesia, occasional laryngospasm, cardiac arrhythmias, and postanesthesia nausea, vomiting, and headache Cyclopropane and oxygen mixtures are explosive, which limits the use of this gas anesthetic. 

Ethylene is an anesthetic gas with a rapid onset of action and a rapid recovery from its anesthetic effects. It provides adequate analgesia but has poor muscle-relaxant properties. The advantages of ethylene include minimal bronchospasm, laryngospasm, and postanesthesia vomiting. A disadvantage of ethylene is hypoxia. This gas is supplied in red cylinders. Mixtures of ethylene and oxygen are flammable and explosive. 

Enflurane (Ethrane) is a volatile liquid anesthetic that is delivered by inhalation. Induction and recovery from anesthesia are rapid. Muscle relaxation for abdominal surgery is adequate, but greater relaxation may be necessary and may require the use of a skeletal muscle relaxant. Enflurane may produce mild stimulation of respiratory and bronchial secretions when used alone Hypotension may occur when anesthesia deepens. 

Halothane (Fluothane) is a volatile liquid given by inhalation for induction and maintenance of anesthesia Induction and recovery from anesthesia are rapid, and the depth of anesthesia can be rapidly altered. Halothane does not irritate the respiratory tract, and an increase in tracheobronchial secretions usually does not occur. Halothane produces moderate muscle relaxation, but skeletal muscle relaxants may be used in certain types of surgeries. This anesthetic may be given with a mixture of nitrous oxide and oxygen. 

The triazinoisoquinoline 151 was prepared by cyclocondensation of the diaminoisoquinoline derivative 150 with biacetyl. Treatment of 151 with ethanesulfonic acid in acetonitrile gave the triazinoisoquinolinium salt 152, which is useful as a local anesthetic, antidepressant, tranquilizer, sedative, and muscle relaxant (89GEP3833615). 

The contribution of pseudocholinesterase, also known simply as cholinesterase, to drug metabolism is much greater as it possesses considerably broader substrate selectivity. In addition to acetylcholine, it will hydrolyze other choline esters like the muscle relaxant succinylcholine. It will also hydrolyze non-choline-containing drugs like the local anesthetic procaine and the anti-inflammatory agent aspirin (Fig. 6.5). Cholinesterases, particularly... 

TIVA has become feasible thanks to the introduction of agents with a suitably short duration of action, including the injectable anesthetics propofol and etomidate, the analgesics alfentanil und remifentanil, and the muscle relaxant mivacurium. These drugs are eliminated within minutes after being adminster-ed, irrespective of the duration of anesthesia. 

Methoxyflurane is an extremely powerful inhalation anesthetic that is an excellent skeletal muscle relaxant. However, its use is somewhat limited by its relatively high solubility, which causes the patient to make a slow transition back into consciousness. Another disadvantage of methoxyflurane is that fluorine ions are the product of its biotransformation, which may lead to the development of renal failure. Therefore, it is recommended to use methoxyflurane for anesthesia during interventions of no more than 2 h. A very common synonym for methoxyflurane is penthrane. 

Nitrous oxide, which is also called laughing gas, is a weak anesthetic. It is usually used together with hypnotics, analgesics, and muscle relaxants. It is sometimes called an ideal anesthetic because of the absence of any kind of suppressive influence on respiration. However, according to the latest information, use of nitrous oxide for more than 2 h is counterproductive since it causes a severe reduction of methionine synthesis, which in turn can cause a severe decrease in the level of vitamin Bj2 with all its subsequent consequences. 

In surgical practice, two barbiturates are primarily used thiopental and methohexital. However, it should be stated that barbiturates are hypnotics, and at therapeutic doses has a very weak analgesic and muscle relaxant effect, which general anesthetics must possess. 

Spinal anesthesia Spinal anesthesia is the introduction of local anesthetics directly into the spinal fluid, which causes a sympathetic blockage, or loss of feeling as well as muscle relaxation resulting from the interaction of anesthetic with every spinal nerve tract. This method is used during major surgical interventions. As a rule, lidocaine, mepivacaine, and bupivacaine are used for this purpose. 

General anesthetic - 50 to 100 meg/kg with oxygen and a muscle relaxant when attenuation of the responses to surgical stress is especially important. 

Drugs that may interact with vancomycin include aminoglycosides, anesthetics, neurotoxic/nephrotoxic agents, and nondepolarizing muscle relaxants. 

---