Anesthetic agents general

The total U.S. market value for the anesthetic agents Hsted was 299.9 million ia 1990 (162). General inhalation agents, valued at 154.5 million, comprised over half (51.5%) of the 1990 market. General iv anesthetics were valued at 111.5 million (37.2%). Local iajectable agents, at 33.9 million, represented the smallest portion of the market (11.3%). U.S. sales for selected anesthesia pharmaceuticals are given ia Table 6. 

Volatile anesthetic agents - Close perioperative monitoring is recommended in patients undergoing general anesthesia who are on amiodarone therapy as they may be more sensitive to the myocardial depressant and conduction effects of halogenated inhalational anesthetics. 

An effective anesthetic agent must be easy to use, quickly render the patient unconscious, and not produce any toxicity. Dr. William T. G. Morton first publicly demonstrated the use of ether as an effective anesthetic agent at the Massachusetts General Hospital on 16 October 1846 before a crowd of skeptical physicians. Raymundus Lullius, a Spanish chemist, discovered ether (CH3CH2)20 in 1275. Its hypnotic effects were soon appreciated (and enjoyed by some), but for many decades ether was only used to treat the occasional medical ailment. Even with ether, the success of surgical procedures did not improve until the introduction of antiseptic procedures and infection control some 20 years later. Ether was replaced by cyclopropane in 1929, which was replace by halothane in 1956. While anesthetic agents are desirable for the patient, exposure of hospital staff is highly undesirable and an important occupational consideration. 

The use of inhalational anesthetics is generally reserved for maintenance of anesthesia. The development of an anesthetic concentration in the brain occurs more slowly with inhalational anesthetics than with IV drugs. Once an anesthetic level has been achieved, however, it is easily adjusted by controlling the rate or concentration of gas delivery from the anesthesia machine. The rate of recovery from a lengthy procedure in which inhalational agents are used is reasonably rapid, since inhalational anesthetics are eliminated by the lungs and do not depend on a slow rate of metabolism for their tissue clearance. Thus, inhalational drugs meet the requirement for a relatively prompt return of the patient s psychomotor competence. 

Table 8.2 Fluorinated general anesthetic agents data ...

The physiologic state induced by general anesthetics typically includes analgesia, amnesia, loss of consciousness, inhibition of sensory and autonomic reflexes, and skeletal muscle relaxation. The extent to which any individual anesthetic agent can produce these effects depends on the specific drug, the dosage, and the clinical situation. 

Ensuring an adequate depth of anesthesia depends on achieving a therapeutic concentration of the anesthetic in the CNS. The rate at which an effective brain concentration is achieved (ie, time to induction of general anesthesia) depends on multiple pharmacokinetic factors that influence the brain uptake and tissue distribution of the anesthetic agent. The pharmacokinetic properties of the intravenous anesthetics (Table 25-1) and the physicochemical properties of the inhaled agents (Table 25-2) directly influence the pharmacodynamic effects of these drugs. These factors also influence the rate of recovery when the administration of anesthetic is discontinued. 

Most local anesthetic agents consist of a lipophilic group (eg, an aromatic ring) connected by an intermediate chain via an ester or amide to an ionizable group (eg, a tertiary amine) (Table 26-1). In addition to the general physical properties of the molecules, specific stereochemical configurations are associated with differences in the potency of stereoisomers (eg, levobupivacaine, ropivacaine). Because ester links are more prone to hydrolysis than amide links, esters usually have a shorter duration of action. 

Many ethers, including diethyl ether, are effective as general anesthetics. Because simple ethers are quite flammable, their place in medical practice has been taken by highly halogenated nonflammable ethers. Two such general anesthetic agents are isoflurane and enflurane. These compounds are isomeric isoflurane is l-chloro-2,2,2-trifluoroethyl difluoromethyl ether enflurane is 2-chloro-l,l,2-trifluoroethyl difluoromethyl ether. Write the structural formulas of isoflurane and enflurane. 

Pharmacological Profile. The profile of the ideal local anesthetic agent depends largely on the type and length of the surgical procedure for which it is applied. Procedures could include neuraxial (spinal and epidural) anesthesia, nerve and plexus blocks, or field blocks (local infiltration). In general, tine ideal agent should have a short onset of anesthesia and be useful for multiple indications such as infiltration, nerve blocks. 

Eger El, 2nd. Characteristics of anesthetic agents used for induction and maintenance of general anesthesia. Am J Health Syst Pharm. 2004 61(suppl 4) S3-S10. 

This involves considerable art, which must be learned in the clinic. It falls into two divisions (1) surface application to the mucous membranes, especially of the eye, nose, throat, and urethra and (2) injections about nerves, in different parts of their course and distribution, from their spinal roots to their ultimate fibrils. The advantages and disadvantages in comparison with general anesthesia and the selection of the local anesthetic agent also depend on clinical discrimination. Nervous, fearful, and excitable patients often suffer severely from apprehension, which also disposes toward accidents. They may be at least somewhat quieted by sedatives, morphine (0.015 g hypodermically) half an hour before the operation, or by barbiturates. The latter also tend to prevent convulsions. 

---