Sedative-hypnotics history

Barbituric acid was first pre pared in 1864 by Adolf von Baeyer (page 112) A histori cal account of his work and the later development of barbiturates as sedative-hypnotics appeared in the October 1951 issue of the Journal of Chemical Education (pp 524-526)... 

The third protocol is to determine the level of drug use and calculate equivalent doses of phenobarbital (Table 3-5). The patient is stabilized on this dose (divided into administration every 8 hours) for a few days, and then the dose is tapered by 10% daily. Although this method has its proponents, the determination of equivalency is an approximation, drug histories are unreliable, and mixed sedative-hypnotic dependence will complicate the procedure. 

Information about prescription drag use alcohol or other substance use family medical history and history of trauma, depression, or head injury should be obtained. It is important to rule out medication use as a contributor or cause of symptoms (e.g., anticholinergics, sedatives, hypnotics, opioids, antipsychotics, and anticonvulsants) as contributors to dementia symptoms. Other medications may contribute to delirium, e.g.,... 

Psychotic symptoms may also occur with the withdrawal of alcohol, sedatives, hypnotics, and anxiolytics The following symptoms may occur persecutory delusions, perceptual distortions, and vivid hallucinations in any modality, most classically visual and tactile hallucination of insects crawling under the skin (formication) Substance abuse history may be elicited from the history and confirmed by finding urinary metabolites Confirmation of schizophrenia can only be made if the psychotic symptoms persist for at least a month following drug withdrawal... 

Allgulander, C. History and current status of sedative-hypnotic drug use and abuse. Acta Psychiatr. Scand. 73, 465-478, 1986. 

Specific factors to consider are both psychiatric and physical contraindications. For example, bupropion is contraindicated in a depressed patient with a history of seizures due to the increased risk of recurrence while on this agent. Conversely, it may be an appropriate choice for a bipolar disorder with intermittent depressive episodes that is otherwise under good control with standard mood stabilizers. This consideration is based on the limited data suggesting that bupropion is less likely to induce a manic switch in comparison with standard heterocyclic antidepressants. Another example is the avoidance of benzodiazepines for the treatment of panic disorder in a patient with a history of alcohol or sedative-hypnotic abuse due to the increased risk of misuse or dependency. In this situation, a selective serotonin reuptake inhibitor (SSRI) may be more appropriate. 

Eight healthy male subjects with a mean age of 34.1 years volunteered for this study. During their participation in the study, they resided on a clinical research unit. The subjects had extensive histories of illicit drug use that included recent ingestion (within the past 2 years) of opiates, marijuana, stimulants, alcohol, and sedative-hypnotics, although they were not dependent on any drug (except nicotine). 

Various older agents have an extensive prior history of use as sedative-hypnotics. These include barbiturates and related compounds such as ethclorvynol and ethin-... 

May cause less dependence than some other sedative hypnotics, especially in those without a history of substance abuse... 

Assess medical and drug history (interacts with alcohol, narcotics, and other sedative-hypnotics)... 

A careful haseline physical examination, ECG, and laboratory work-up are essential. Underlying ECG changes (U waves, prolonged QT interval, or flattened T waves) secondary to hypokalemia or bradycardia and atrioventricular block from starvation may be present. AU antidepressants can cause seizures thus a careful risk-benefit assessment is warranted if the patient has predisposing factors such as a personal or family history of seizures, cerebrovascular disease, or alcohol or sedative-hypnotic withdrawal. 

IV. Diagnosis Is usually based on the history of Ingestion or recent Injection. The differential diagnosis should Include other sedative-hypnotic agents, antidepressants, antipsychotics, and narcotics. Coma and small pupils do not respond to naloxone but will reverse with administration of flumazenil (see below). 

IV. Diagnosis is usually based on the history of ingestion and findings of CNS depression, often accompanied by muscle twitching or hyperreflexia. The differential diagnosis should include other sedative-hypnotic agents (see p 335). 

The second catastrophe that influenced the development of medicines regulation far more than any event in history was the thalidomide disaster. Thalidomide was a sedative and hypnotic that first went on sale in Western Germany in 1956. Between 1958 and 1960 it was introduced in 46 different countries worldwide resulting in an estimated 10,000 babies being born with phocomelia and other... 

The speciflc clinical use of the numerous available benzodiazepines depends on their individual pharmacokinetic and pharmacodynamic properties. Drugs with a high affinity for the GABAa receptor (alprazolam, clonazepam, lorazepam) have high anxiolytic efficacy drugs with a short duration of action (temazepam) are used as hypnotics to minimise daytime sedative effects. Diazepam has a long half-life and duration of action and may be favoured for long-term use or when there is a history of withdrawal problems oxazepam has a slow onset of action and may be less susceptible to abuse. 

The most frequent adverse effect which occurs in at least one-third of patients is drowsiness, often accompanied by incoordination or ataxia. Problems with driving, operating machinery, or falls can result, particularly in the elderly, and can be an important source of morbidity, loss of physical function, and mortality (47,48). Memory impairment, loss of insight, and transient euphoria are common paradoxical reactions of irritability or aggressive behavior have been well documented (11) and appear to occur more often in individuals with a history of impulsiveness or a personality disorder (40), and in the context of interpersonal stress and frustration (49). Tolerance to the sedative and hypnotic effects generally occurs more rapidly than to the anxiolytic or amnestic effects (1). 

Acute kidney injury has also been associated with a variety of sedatives and hypnotics including barbiturates, benzodiazepines, glutethimide and dilorpro-mazine [107,108,119]. The acute kidney injury is usually related to rhabdomyolysis but the classical clinical picture of acute interstitial nephritis has been reported in one patient with the use of diazepam, although no renal biopsy was performed [186]. In fhose patients with rhabdomyolysis, multiple seizures often develop prior to the rhabdomyolysis and others are febrile at the time. However, the most common presentation is that of a young person without a prior medical history who presents with coma-stupor of one to several days duration, variable signs of volume depletion, limb compression and follows the typical course of acute tubular necrosis with a high likelihood of renal recovery [107-109]. 

It is one of the oldest sedatives and hypnotic which gets absorbed very quickly after oral administration and helps to induce sleep within 10-15 minutes after a 4-to 8-mL dose. Its application has been resticted in patients with a history of asthma or other pulmonary diseases beeause it gets... 

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