Amobarbital dependence

In this study, potential oscillation was measured in the presence of lOOmM sodium salts of barbital, allobarbital, phenobarbital, and amobarbital in phase wl [19]. Their chemical structures are shown in Fig. 15. Amplitude and the oscillatory and induction periods were noted to depend on the particular hypnotic used. Amplitude decreased in the order, barbital > allobarbital > phenobarbital > amobarbital. The oscillatory period increased in the order, barbital < allobarbital < phenobarbital < amobarbital. Induction period increased in the order, barbital < allobarbital < phenobarbital < amobarbital. These parameters changed depending on drug concentration. Hypnotics at less than 5 mM had virtually no effect on the oscillation mode. 

Pentobarbital is 65% plasma protein bound with a volume of distribution of 0.5 to 1.0 L/kg.6 After intravenous administration, estimates of the plasma half-life have averaged between 20 and 30 h. Amobarbital is similar to pentobarbital in the degree of plasma protein binding (59%) with a slightly larger volume of distribution (0.9 to 1.4 L/kg). The plasma half-life, however, is dose dependent, with a range of 15 to 40 h.6 Phenobarbital is approximately 50% plasma protein bound... 

Several classes of pharmacologic agents are available for insomnia. Barbiturates are the oldest agents that have been used for insomnia and include pentobarbital, secobarbital, and amobarbital. Barbiturates are currently not recommended because of their high abuse potential (due to rapid development of tolerance) and lethal potential in overdose situations. Barbiturates potentiate the GABAergic-induced increase in chloride ion conductance at low doses, and at high doses they depress calcium-dependent action potentials. Caution should be exercised in patients with marked renal or liver dysfunction, severe respiratory disease, suicidal tendencies, or history of alcohol/drug abuse. 

Barbiturates, hydantoins, and imides contain functional groups related to amides but tend to be more reactive. Barbituric acids such as barbital, phenobarbital, amobarbital, and metharbital undergo ring-opening hydrolysis, as shown in Scheme 15.80-81 Decomposition products formed from these drug substances are susceptible to further decomposition reactions such as decarboxylation. The hydrolysis rates of these substances depend on the substituents Ri, R2, and R3. For some allylbarbituric acids, the effects of these substituents on hydrolysis rates can be explained in terms of Hammett s o value.82... 

Schedule 11 drugs have an accepted medical use in the United States and a high rate of abuse, with either severe psychological or physical dependence potential. These drugs include morphine, codeine, cocaine, amphetamine, and most barbiturate preparations containing amobarbital, secobarbital, and pentobarbital. 

---