Local anesthetic pharmacologic properties

Oxolamine [959-14-8] (57) is sold in Europe. It is an oxadiazole, and its general pharmacological profile is described (81). The compound possesses analgesic, antiinflammatory, local anesthetic, and antispasmodic properties, in addition to its antitussive activity. Although a central mechanism may account for some of the activity, peripheral inhibition of the cough reflex may be the dominant effect. The compound has been shown to be clinically effective, although it is less active than codeine (82,83). The synthesis of oxolamine is described (84). 

Cocaine is another example of a dmg with a complex pharmacological profile responsible for different properties probably concurring due to QT prolongation. It has a local anesthetic action (and therefore shares the pharmacological properties mentioned above), but recent reports also indicate the blockade of hERG K+ currents [47-49]. Thus, it is not unexpected that cocaine has been associated with QT prolongation and occurrence of TdP [50-53]. 

Belladonna alkaloids have an extremely broad pharmacological spectrum. In addition to their ability to block M-receptors, atropine and scopolamine also act on other receptors, thus showing corresponding effects. They can only block nicotinic cholinergic receptors, however, in significantly larger doses than those used in clinics. Atropine also exhibits properties of local anesthetics and histamine (Hj) receptor blockers. Atropine and... 

These changes substantially alter the pharmacological properties of procainamide however, flecainide maintains local anesthetic properties. 

Cocaine is a local anesthetic with a peripheral sympathomimetic action that results from inhibition of transmitter reuptake at noradrenergic synapses (see Chapter 6 Introduction to Autonomic Pharmacology). It readily enters the central nervous system and produces an amphetamine-like effect that is shorter lasting and more intense. The major action of cocaine in the central nervous system is to inhibit dopamine reuptake into neurons in the "pleasure centers" of the brain. These properties and the fact that it can be smoked, "snorted" into the nose, or injected for rapid onset of... 

Little of value has come out of pharmacological studies on these alkaloids (34) local anesthetic properties (35) have been reported, and none of the alkaloids have shown antimalarial properties (36). 

Local anesthetics are drugs that produce reversible conduction blockage of nerve impulses. Autonomic system blockade followed by sensory anesthesia and skeletal muscle paralysis occur when local anesthetic concentration is increased. The effects of local anesthetics are completely reversible, with no evidence of structural damage to the nerve fibers. Another prominent clinical feature of local anesthesia is that loss of sensation occurs without loss of consciousness. This property makes local anesthetics highly useful for many office procedures and for eye surgery. This chapter considers the pharmacologic properties of anesthetics cmrently used for ophthalmic procedures. 

Ixxtal anesthetics do not rely on blood circulation to reach their site of action, as they are usually administered at. or close to. their site of action. Systemic side effects ari.se be-caiLse the local anesthetic agent is carried away in the blood hefure it can be fully metabolized. Con.sequently. the chemi-ciil iind pharmacological properties of local anesthetics arc of major importance in determining not only the effectiveness of the drug but also its systemic. side effects. 

Opening with the history of kava, this book proceeds to describe the botany, cultivation, harvesting and economic aspects of kava. A major part of the book is then devoted to the chemical and pharmacological properties of the kavalactones, the psychoactive constituents of kava that are reported to have sedative, anxiolytic, analgesic, local anesthetic, anticonvulsant, and neuroprotective properties. The medical and clinical studies that provide evidence for the therapeutic benefits are balanced with an assessment of the known adverse effects and interactions and the recently reported cases of severe liver toxicity in which kava has been implicated. 

The foregoing studies have dealt chiefly with model substrates in vitro. Several of the early papers by Augustinsson, referred to in Section 4.1.1, considered substrate specificity from the viewpoint of species variations. It is also important to recognize that plasma cholinesterase may be associated with the hydrolysis, in vivo, of a large number of drugs (K4, LI, L4) that contain ester bonds susceptible to enzymic hydrolysis. Apart from succinylcholine (Section 3.1), cholinesterase is known to be responsible in man for the hydrolysis of cocaine (S40), procaine (K2), and other esters with local anesthetic properties. Whether enzymatic hydrolysis terminates the pharmacologic effect depends on the whole mechanism of action of the particular drug. 

The Erythrophleum alkaloids represent a clearly defined class, both as regards their chemical structure and pharmacological properties. They are alkamine esters of monocarboxylic acids of the diterpene series and possess remarkable cardiac activity of the digitalis type coupled with very intense local anesthetic action. 

I. Pharmacology. Diphenhydramine Is an antihistamine with anticholinergic, anti-tussive, antiemetic, and local anesthetic properties. The antihistaminio property... 

The challenge at hand is to achieve optimal patient comfort while avoiding the risks of oversedation and respiratory depression. The type of local anesthetic and the dose delivered are important in addition to appropriate conscious sedation. As a general rule, it is desirable to select an anesthetic agent that is rapid in onset in combination with one that offers sustained action. A list of pharmacologic properties of commonly used local anesthetic agents is found in Table 4.6. 

Table 4.6 Pharmacologic properties of commonly used local anesthetic agents.

The pharmacological activity and toxicity of coca is generally attributed to cocaine. In addition to its local anesthetic, central nervous system stimulant, and addictive (similar to amphetamines) properties, cocaine has many other activities (goodman and oilman list and hOrhammer martindale morton 3). Little is known of the effects of the other alkaloids present in coca leaf. ... 

Diazepam, lorazepam, and midazolam are used in anesthetic procedures. The primary indication is for premedication because of their sedative and amnestic properties. (The basic pharmacology of benzodiazepines is discussed in Chapter 22 Sedative-Hypnotic Drugs.) Diazepam and lorazepam are not water-soluble, and their intravenous use necessitates nonaqueous vehicles, which may cause local irritation. Midazolam formulations are water-soluble and thus produce less irritation, but the drug becomes lipid-soluble at physiologic pH and readily crosses the blood-brain barrier. 

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