Barbiturates minor

Downers Barbiturates, minor tranquilizers, and related depressants. 

There are three common protocols for barbiturate detoxification. In all approaches, the goal is to prevent the occurrence of major symptoms and to minimize the development of intolerable minor symptoms. The first procedure is based on protocols described by several authors (Ewing and BakeweU 1967 Isbell 1950 Wilder 1968) (see Table 3 ). The first step is to determine the severity of tolerance. If the patient is intoxicated, no additional barbiturate should be given until the symptoms of intoxication have resolved. If there is substantial evidence or strong suspicion of chronic barbiturate use, it is not necessary or desirable to wait until withdrawal symptoms appear. A 200-mg oral dose of pentobarbital may be given on an empty stomach to a... 

Convulsive disorders are still a serious therapeutic problem and new agents are being actively sought. Classical therapy was based upon the barbiturates that are no longer in favor because of their many side effects and their suicide potential. Interestingly, a seemingly minor structural variation of phenobarbital (152, shown as its sodium salt) leads to an anticonvulsant of increased potency and which has less hypnotic activity. In this case, sodium phenobarbital serves as its own base (so the yield is limited to 50%) and reacts readily with... 

In order to determine the applicability of retention indices, based on the alkyl arylketone scale, as the basis of a reproducible method of reporting retentions, the separation of 10 barbiturates and a set of column test compounds were examined on an octadecylsilyl bonded silica (ODS-Hypersil) column with methanol-buffer of pH 8.5 as eluent [100]. The effects on the capacity factors and retention indices, on changing the eluent composition, pH, ionic strengthened temperature, showed that the retention indices of the barbiturates were much less susceptible to minor changes in the eluent than the capacity factors. 

However, metabolic cleavage represents only a very minor pathway for barbiturates, and it has been questioned whether the ring-opened products are really metabolites or artifacts resulting from workup procedures. The most important metabolic pathway for barbiturates is oxidation of the 5-substituent. 

There appears to be little difference between benzodiazepines and kava extract in anxiolytic activity. However, kava extracts seem to have fewer side effects. Two studies with more than 3000 patients each found unwanted events in about 2% of patients during treatment with kava extract. The more frequently reported side effects were gastrointestinal complaints, allergic skin reactions, headache, and photosensitivity (Pittler and Ernst, 2000). There have been isolated reports of hepatotoxicity and acute liver failure (Escher et ah, 2001). Kava may potentiate the sedative effects of other medications including barbiturates and benzodiazepines. Kava can also cause behavioral disinhibition in a minority of individuals, including children. The most common problem, which is usually associated with persistent and excessive usage, is a scaly skin rash called kava dermopathy, which is reversible. 

Sedatives (also called hypnotics, sedative-hypnotics, minor tranquilizers, antianxiety agents) Secobarbital (barbiturate) Glutethimide (nonbarbiturate hypnotic) Diazepam (benzodiazepine antianxiety agent) Chloral hydrate (miscellaneous hypnotic) alcohol ( substance )... 

Benzodiazepines are also known as minor tranquilizers. Not as potent or dangerous as barbiturates, the benzodiazepines do find use as antianxiety drugs because of their safety and efficacy. In higher doses they will also induce sleep. All benzodiazepines cause a dose-... 

There is a very great demand for drugs for the relief of anxiety. This was formerly met by the use of alcohol, bromides or barbiturates, which carried the risk of abuse or dangerous toxicity. The first of the modern minor tranquilizers, introduced from 1946 onwards, were drugs described as skeletal muscle relaxants. These were mainly derivatives of polyhydric alcohols, but heterocyclic examples included metaxolone (161), which is related to the aryl ethers of glycerol, chlorzoxazone (162) and chlormezanone (163). Dantrolene sodium (164) is a muscle relaxant and CNS depressant. 

Tea Tree (Melaleuca alternifolia) Uses Rx of superficial wounds (bacterial, viral, fungal, insect bites, minor burns, cold sores, acne Action Broad-spectrum antibiotic activity against E. coli, S. aureus, C. albicans Available forms Topical creams, lotions, oint, oil apply topically PRN Notes/SE Ataxia, contact dermatitis, D, drowsiness, GI mucosal irritation Interactions Effects OF drugs that affect histamine release EMS effects of Benadryl Valerian (Valeriana officinalis) Uses Anxiolytic, antispasmodic, dys-menorrheal, restlessness, sedative Action Inhibits uptake stimulates release of GABA, which T GABA concentration extracellularly causes sedation Available forms Ext 400-900 mg PO 30 min < hs, tea 2-3 g (1 tsp of crude herb) qid, PRN, tine 3-5 mL (1/2-1 tsp) (1 5 ratio) PO qid, PRN Efficacy Probably effective sedative (reduces sleep latency) Notes/SE GI upset, HA, insomnia, N/V, palpitations, restlessness, vision changes Interactions T Effects OF barbiturates, benzodiazepines, opiates, EtOH, catnip, hops, kavakava, passion flower, skullcap effects OF MAOIs, phenytoin, warfarin EMS T Effects of benzodiazepines and opiates abruptly D/C may cause withdrawal symptoms... 

Schedule IV - Drugs have an accepted medical use and are generally the long-acting barbiturates,hypnotics and minor tranquilizers, e.g., meprobamate, phenobarbital. 

The same type of chain reaction is observed in the case of l,3,6Me3Ura with one minor difference while with l,3Me2Ura the only chain product is the glycol, there are two chain products in l,3,6Me3Ura, its glycol and 1,3,6-trimethyliso-barbituric acid, formed in a ratio of 2 1 (Rashid et al. 1991). The latter is believed to arise from the sulfate by an elimination of sulfuric acid. A deprotonation at methyl does not take place. This is quite in contrast to the situation in l,3Me2Thy and other Thy systems discussed above. 

STREET NAMES Minor tranquilizers (benzodiazepines BZDs, tranks, downers, benzos, goofballs, happy pills, sedative-hypnotics, anxiolytics) (barbiturates Amys, barbs, blues, downers, yellow jackets, rainbows, red devils) (nonbarbiturate sedative-hypnotics ludes, Sopors)... 

Sedative-hypnotics A class of depressants that induces restfulness m low doses and sleep in higher doses. Alcohol, barbiturates, and the minor tranquilizers make up this class of drugs... 

Minor tranquilizers and sedative-hypnotics are widely used in general medical practice and psychiatry. Although the benzodiazepines as a class are much safer than earlier medications (there is less risk of dependency and abuse, and withdrawal symptoms are generally much less dangerous than with barbiturates), problems do exist when patients begin to reduce doses, especially if they discontinue rapidly or "cold turkey." Benzodiazepine withdrawal sjmdromes are encoimtered frequently. They cause considerable patient distress, can be dangerous at times, and are almost always avoidable if the clinician follows the discontinuation guidelines carefully. 

Tolerance and abstinence may develop with any of the barbiturates. It has been reported that abrupt withdrawal of secobarbital (given 0.8-2.2 g/d for 6 weeks) causes both minor symptoms (tremors, anorexia, insomnia, and apprehension) and major symptoms (seizures, delirium, and hypothermia) that can persist for up to 2 weeks after discontinuation. Tolerance to barbiturates can develop within 2 weeks of treatment because of induction of hepatic microsomal enzymes (2). 

Phenytoin and barbiturates display tautomerism of the imine-imide type, as shown in Figure 3.16. The predominant tautomer is the imide form, although some older textbooks list the structure of the drug as the minor tautomer. 

The hypothesis that the 1-2 hydrolytic opening of the barbiturate ring is associated with the undissociated form was not fully supported by experimental evidence.319,322 The 1-6 ring opening is favored in all barbiturates and the 1-2 opening is of minor importance, except when some steric factors, such as a bulky C-5 substituent or the presence of some N-substituents, inhibit the 1-6 alternative.329 The results of other studies support this view,305 308 312 313 344 but its definite and detailed experimental proof is still lacking. 

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