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Barbiturates and Nonbarbiturate Sedative Hypnotics

At the turn of the twentieth century, bromide were being used to combat sleeplessness, anxiety, and minor pain, but with the discovery of barbituric acid in
the late 1800s, bromides were gradually replaced with the barbiturates. In 1903 the first barbiturate, Veronal, was places on the market, and it was soon
followed by Luminal. More recenctly the nonbarbiturates such as glutethimide and methaqualone have flooded the prescription market.

Although recently overshadowed by tranquilizers, the barbiturates and nonbarbiturate hypnotic sedative (see tables 8.1 and 8.2) are among the most
popular tools of the physician. They are used (1) in daytime, low dose sedative therapy to treat normal and neurotic patients by reducing tension and
anxienty without inducing lethargy that could lower mental alertness to potentially dangerous levels or reduce the quality of life by decreasing reactivity to
environment, and (2) in moderate dose or hypnotic therapy at bedtime in order to counteract insomnia. Onset of sleep occurs sooner and a dreamless night's
sleep ensues. There drugs are not analgesics, but aften aid in reducing the psychological component involved in cardiovascular, gastrointestinal,
respiratory, or other diseases and reduce anxiety that the patient may experience from the somatic symptoms of these disease.

Because of the antianxienty and antitension qualities of the sedative hypnotics, their illegal use increased dramatically, and with their misuse and abuse, tha
dangers (and cross tolerance to other depressant drugs) and psychic and physcial dependence, and that abrupt withdrawal after chronic abuse would bring
on an abstinence syndrome more severe than that caused by any other drug, because life threatening convulsions accompanied withdrawal. The dependece-
producing nature of these drugs and their potential for respiratory depression stimulated medical research for safer substances. The drugs that emerged
from this research were the sedative hypnotics-tolerance, depence, and overdose.

The barbiturate and nonbarbiturate sedative hypnotics produce their depressant effect by inhibitting the arousal systems of the central nervous systems, that
is, they depress the reticular formation by interfering with oxygen consumption and energy producing mechanisms. The depression here reduce the nerve
signals that reach the cortex, thus promoting sleep. A sedative dose makes one only slightly drowsy, but damps out enough incoming stimuli to reduce
anxiety and tension.

The body eliminates these sedative hypnotics via the kidneys at varying rates, and it is mainly this rate of elimination that determines the duration effects
of any one drug. There is an exception here in that short and ultrashort acting barbiturates rapidly redistribute themselves in adipose tissue, thus lessening
their levels and effects in the brain. The intermediate and long acting drugs are metabolized more slowly and may produce some residual sedation
(hangover) because they have not been thoroughly metabolized.

An interesting paradox with these drugs is that abusive levels in chronic users or normal dose in susceptible patients, especially the elderly, can produce
exciatation before the customary depressant action sets in. Another interesting effect of barbiturates is that when taken in the presence of psychological
stress or extreme pain, they may cause delerium and other side effect such as nausea, nervousness, rash, and diarrhea (16). Another adverse effect of
barbiturates, glutethimide, and other drugs of this classification is that they decrease the potency of certain anticoagulant drugs.

The tarnqulilizers are divided into antipsychotic and antianxiety substances, also commonly known as the major transquilizers (drugs such as Thorazine
and Reserpine) hold no hazard of physical dependence and are not street drugs of misuse or abuse. Thorazine (generic name, chlorpromazine) is the drug of
choice in most mental hospital for alleviating the symptoms of psychosis and rendering patients more susceptible to therapy (see table 8.3).

The remainder of this cahpter refers only to the minor tranquilizers which, like the barbiturate and nonbarbiturate sedative hypnotics, are common drugs of
misuse and abuse. The rise in consumption of tranquilizers began in the 1960s with Miltown and Equanil (generic name, meprebamate) as the prototypes,
and these were later replaced by Librium and Valium. In 1968 40 million prescriptions were written by physicians in the United State. (More prescriptions
here are that many Americans are trying to solve their problems through the use of psychotropic drugs, and that American physicians feel that tranquilizers
are the most efficient manner in which to deal with their anxiety-ridden patients. The all out prescribing of tranquilizers has its impact on the street drug
scene in two ways-directly, by supplying legitimate drug (via theft) to the black market system, and indirectly, through parental example of attitude toward
drugs. Use of illicit drugs by teenagers has been ahown to parallel their parents us of tranquilizers, with children being especially influenced by their
mother use of these drugs.

The action of tranquilizers on the central nervous system is quite dissimilar to that of the sedative hypnotics. Rather than suppress activity of the reticular
activating system, the tranquilizers act on the limbic system, which in involved in emotional response. Experimental research has shown a "taming" action
of tranquilizers on hostile and vicious animals and subsequent anxiety reduction in humans. These drugs are depressants and at higher than normal dosage
levels can cause sedation or death from overdose, and will potentiate other depressant drugs.

The drugs of concern in this chapter are characterized by those listed in Tables 8.1, 8.2 and 8,4. Those are, of course, countless other barbiturates,
nonbiturates, and tranquilizers on the market. If taken in excessive doses over a long enough period of time, all of the drugs that are listed will create
tolerance and physical and psycological dependence.

From currently avalaible information we find that (1) as seen fig 8.1 the drugs in question are dangerous drugs, (b) the supply exceeds the demand (30),
and (c) these drugs do not solve problem of anxiety-they marely treat the symptoms. In view of these facts, we wonder why pharmaceutical companies
continue to manufacture them and doctors continue to prescribe them. Meares (20) suggested three answers to the letter question, the firts being that a
barbiturate prescription occasionally relieves the anxiety of physicians who feel that unless they prescribe something for their patients, theya are not doing
their duty. Second, even though the physician know that insomnia or anxiety is a symptom of a deeper inner conflict, he or she may not have sufficient
time to help resolve the patient's real problem. Hence a prescription is made out to treat the symptom. Third, either the physician may be unwilling to use
new drugs or is not up to date on current medicine.

In prescribing sedative hypnotics or tranquilizers to a patient who is in an anxious state of mindn the physician is placing a dangerous drug in the hands of
a person who, in his or her mental state, may be depence or suicide prone.


Insomnia is a common condition and can arise numerous underlying causes :
1. Situational (e.g. Jet lag, being in unfamiliar surroundings)
2. Medical (e.g. Pain)
3. Psychological (e.g. Anxiety, inadequacy, neurosis)
4. Drug intake or withdrawal (e.g. Alcohol, caffeine)

The sedative hypnotics have ben used as sleeping aids for various difficulties in sleeping-inability to fall asleep, early morning awakenings, inability to
stay asleep, and combinations of these. For whatever purpose is not "normal" sleep.

An important drawback of prescribing the sedative hypnotics for relief of insomnia is that many of these drugs reduce REM (rapid eye movement) sleep
time. This includes chloral hydrate, barbiturates (especially pentobarbital, secobarbital, and amobarbital), glutethimide, and methaqualone. The
benzodiazepines, diazepan, and chlordiazepoxide produce quantitatively less depression of REM both acutely and chronically (14). It appears that REM
sleep is necessary, for if individuals are deprived of this period of sleep in which dreams occur, they grow irratable, anxious, and even neurotic. In a normal
night's sleep, five or six periods of orthodox sleep occur broken up by short periods of REM sleep, with the first period