Barbiturate potentiation

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. 

Alcohol, CNS depressants (narcotics, barbiturates) Potentiate CNS depression... 

BDZs are the most widely prescribed class of psychoactive drugs in current therapeutic use, despite the important unwanted side-effects that they produce such as sedation, myorelaxation, ataxia, amnesia, ethanol and barbiturate potentiation, and tolerance. The existence of a new family of ligands with a flavonoid structure was recentlv demonstrated in the... 

Studies of administration of 300 mg/kg ashwagandha report a barbiturate potentiation (Rao and Karanth 1990) or a reduction in barbiturate-induced sleeping time (Singh et al. 1978). A fourth study indicated that a dose of 1 g/kg of ashwagandha produced a potentiation of barbiturates (Singh et al. 1979). 

Diffutin (see above) has pronounced adaptogenic (anti-stress and anti-anxiety) activity, as well as being a mild CNS depressant (barbiturate potentiation). It also has a marked inotropic effect in perfused frog heart, and shows no arrhythmogenic properties. In addition, it potentiates the contractile response of guinea pig vas deferens to catecholamines, without inhibition of the uptake of adrenalin. At 500 mg/kg, diffutin is nontoxic to dogs. The use of Canscora in Indian medicine as a herbal remedy for certain mental disorders is supported by these observations. 

Barbiturate potentiation - in vivo (mouse), route not given, at 1.0 mg/kg. 218... 

The various barbiturates differ m the time required for the onset of sleep and m the duration of their effects All the barbiturates must be used only m strict accordance with instructions to avoid potentially lethal overdoses Drug dependence m some mdi viduals IS also a problem... 

The potential for normal brain tissue injury is one of the limiting factors in the use of XRT for brain tumors. Pentobarbital is a cerebral radioprotectant in rodent and primate models after single doses, but is associated with significant risks. Of alternative barbiturates, thiopental given to tats receiving 70-Gy (7000-rad) whole-brain irradiation in a single fraction enhances the 30-day survival similarly to pentobarbital, whereas ethohexital and phenobarbital show no radioprotective activity (250). 

As expected, heterocyclic enols and potential enols (i.e, compounds existing mainly in the CH form) behave toward diazomethane similarly to the open chain and isocyclic enols, i.e. they form enol methyl ethers by reactions of the SnI type (cf. footnote 29). Examples of this behavior are barbituric acid, picrolonic acid, dchydroacetic acid (64), 3-methyl-l-phenylpyrazolin-5-one, 1-phenylpyrazoli-dine-3,5-dione, 1,2-diphenylpyrazolidine-3,5-dionc, 3-hydroxy-... 

The proplnts described above are in the realm of prior art and depict those NC proplnts with low smoke potential that are used primarily as gun proplnts. Recent research and development work has been concentrated on creating both gun proplnts and rocket proplnts with reduced smoke output in order to foil countermeasures. Lavitt (Ref 76) found that the concurrent use of optimum proportions of lead stearate and sodium barbiturate in double-base proplnts resulted in a marked reduction in smoke output. This was attributed to the synergistic interaction of the two salts to produce more complete oxidation of the exhaust products. The importance of using the optimum ratio of the two catalysts is demonstrated by the higher smoke values shown in Table 4 for Propellants 105, 106 and 107, when compared to other... 

Like the barbiturates, the miscellaneous drugp sedative or hypnotic effects diminish after approximately 2 weeks. Ffersons taking these dragp for periods longer than 2 weeks may have a tendency to increase the dose to produce the desired effects (eg, sleep, sedation). Physical and psychological dependence may occur, especially after prolonged use of high doses. However, their addictive potential appears to be less than that of the... 

When amphotericin B or diuretics are administered with ACTH, the potential for hypokalemia is increased. There may be an increased need for insulin or oral antidiabetic drag s in the patient with diabetes who is taking ACTH. There is a decreased effect of ACTH when the agent is administered with the barbiturates. Profound muscular depression is possible when ACTH is administered with the anticholinesterase drugp. Live virus vaccines taken while taking ACTH may potentiate virus replication, increase vaccine adverse reaction, and decrease the patient s antibody response to the vaccine... 

Benzodiazepines and similar agents occupy a position of intermediate abuse potential, compared with most other sedative-hypnotics (Griffiths and Weerts 1997). Animal models of abuse habihty indicate that the reinforcing effects of benzodiazepines are less pronounced than are those of the barbiturates, opioids, and stimulants. Differences in abuse potential within the class have not been consistently demonstrated however, most chnicians agree that benzodiazepines with a rapid onset and short duration of action pose the greatest risk in susceptible individuals. 

Intracellular steroid receptors, which alter gene expression, exist for corticosteroids, oestrogens and progesterone in the brain, as in the periphery but they cannot account for the relatively rapid depression of CNS function induced by some steroids. This was explained when Harrison and Simmonds (1984) discovered that alphaxalone (the steroid anaesthetic) potentiated the duration of GABA-induced currents at the GABAa receptor in slices of rat cuneate nucleus just like the barbiturates (Fig. 13.6). Of the... 

This area has been covered in a review by Eldefrawi and Eldefrawi [23]. The GABA -receptor channel is activated by GABA (Fig. 2), avermectin, muscimol, taurine (Fig. 2) and j -alanine (Fig. 2). The activation by agonists is potentiated by benzodiazepines and barbiturates. The channel is blocked by the competitive... 

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