Thiopental characteristics

Figure 3.5 Comparison of the structures and physicochemical characteristics of pentobarbital and thiopental.

The induction of unconsciousness may be the result of exposure to excessive concentrations of toxic solvents such as carbon tetrachloride or vinyl chloride, as occasionally occurs in industrial situations (solvent narcosis). Also, volatile and nonvolatile anesthetic drugs such as halothane and thiopental, respectively, cause the same physiological effect. The mechanism(s) underlying anesthesia is not fully understood, although various theories have been proposed. Many of these have centered on the correlation between certain physicochemical properties and anesthetic potency. Thus, the oil/water partition coefficient, the ability to reduce surface tension, and the ability to induce the formation of clathrate compounds with water are all correlated with anesthetic potency. It seems that each of these characteristics are all connected to hydrophobicity, and so the site of action may be a hydrophobic region in a membrane or protein. Thus, again, physicochemical properties determine biological activity. 

Whether given orally or parenterally, drugs are distributed nonuniformly throughout the body. Factors that regulate this distribution are the lipophilic characteristics of the drugs, the blood supply to the tissues, and the chemical composition of various organs and tissues. The distribution of drugs not only influences their onset of action but also at times determines their duration of action. For example, thiopental, an intravenous anesthetic, produces unconsciousness 10 to 20 s after its administration, and consciousness returns in 20 to 30 min. The rapid onset of action is due to the rapid transport of thiopental to the brain. The short duration of action stems from its subsequent redistribution to other tissues, such as muscle and fat. 

As soon as a drug finds its way into the blood stream, it tries to approach the site of biological action. Hence, the distribution of a drug is markedly influenced by such vital factors as tissue distribution and membrane penetration, which largely depends on the physico-chemical characteristics of the drug. For instance, the effect of the ultra-short acting barbiturate thiopental may be explained on its dissociation constant and lipid solubility. It is worthwhile to observe here that the dmation of thiopental is not influenced by its rate of excretion or metabolism, but by its rate of distribution. 

The infrared spectrum of thiopental sodium and/or thiopental has undergone considerable investigation [8-11]. The infrared spectrum of thiopental sodium and thiopental, both as KBr disks, were obtained on a Hitachi 270-30 infrared spectrophotometer. The spectra, presented as Figure Two and Three, respectively, display absorption characteristics in good agreement with those previously rqiorted. Frequency assigmnents for some of the characteristic bands are giv i in Table 1. 

Thiopental Injection. Link Pharmaceuticals Ltd. UK Summary of product characteristics, January 2003. 

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