Common sleeping medicine / drugs that can make you sleep

Often we need sound sleep but we can’t. There are some most common sleeping medicine / drugs that can make you sleep. All of them are described in detail.

As far back as recorded history goes, men and women have sought sleep and release into hallucinatory states-by means of naturally occurring drugs.

The Aztecs of Central America used sacred mushrooms; and from the east came hashish derived from the plant Cannabis sativa and opium, from the poppy.

But among all the old sleep inducing potions, those made from the root of the mandrake plant enjoyed the greatest popularity.

The mandrake a member of the potato family is often shaped as if it had arms and legs and this characteristic has made it the subject of many legends.

The mandrake contains hyoscien, a drug related to belladonna which in large doses is dangerous.

The use of these naturally occurring drugs to promote sleep has now beesuperseded in developed countries by synthetic chemical drugs.

All the chemical sleeping drugs described in this page are prescription drugs. Over the counter, off prescription preparations are nearly all ineffective.

We should point out here that a prescribed drug should be taken only by the person for w home it was prescribed, neverin quantities larger than prescribed, and always kept out of reach of children.

Prescribed drugs generally have two names; the approved name of the chemical and the trade name. We will be referring to all drugs by their approved name, and to somewhere appropriate, also by their trade name, which is always written with a capital first letter.

Many trade names differ from country to country so to avoid complication the text we have included an appendix on page 116 that lists the approved and trade name in several countries of all the drugs mentioned in the book. 

The first chemical sleeping sleeping medicine / drugs

By the nineteenth century the rise of modern chemistry began to bring arterial chemical agents which, though less romantic than those of the middle ages were safer and more effective. 

Common sleeping medicine drugs

Bromides

In England in 1857 Sir Charles Locock introduced bromides into medicine for the treatment of epilepsy and they were found to cause drowsiness. The use of bromides continued well into the twentieth century, but today they have rightly nearly disappeared.

Though effective in reducing epileptic seizures, the bromides were not really suitable for use as sleeping drugs or hypnotics as they are sometimes called since only by gradual accumulation over a period of days and weeks can they caused drowsiness, and the effect is present by day as well as by night affecting both alertness and general health. 

Paraldehyde

This is a colorless liquid that smells strongly and has a burning taste. It used to be given with various masking agents to camouflage the taste and smell and up until a few years ago it still figured in the official list of drugs available in Britain as the sleeping draught Haustus Paraldehyde. Some patients grew to love the way is burned their throat like whisky.

Paraldehyde could also be injected through a syringe a practice that has continued with diminishing frequency up to the present day. It is an effective drug for inducing sleep and for relieving the insomnia caused by the withdrawal of alcohol.

But the great disadvantage of paraldehyde is that some of it leaves the body again as vapor through the lungs so that the whole house or a whole hospital, reeks of paraldehyde if anyone present has received it in the last twelve hours. 

Chloral hydrate

This chemical compound came into use as a sleeping drug in the nineteenth century and in a modified form it is still used today in proprietary pills such as Welldorm, Noctec and Triclofos.

It was first prepared by the chemist, Baron Justus Von Leibig in Munich in 1832. Whereas other sleeping drugs, such as the bromides, had a great many other unwanted side-effects, chloral had a more selective action, and in this respect was the forerunner of modern sleeping drugs.

It was synthesized by Leibig from chloroform and an alkali, and was wrongly thought to release chloroform (then recently introduced for use in anaesthesia) into the blood- stream.

It was chloral hydrate, mixed into alcoholic drinks, that furnished the original Mickey finn knock-out draught. The nineteenth-century Pre-Raphaelite painter and poet, Dante Gabriel Rossetti, was thought to have been a chloral addict.

Chloral, however, remains an effective and safe hypnotic, of which there is little criticism; though, because it is old, little money has been invested to carry out the kind of careful research that is devoted to modern sleeping drugs, and so there is perhaps some deficiency of critical research into the merits of chloral.

The  ½ -1 g dosage for adults is very large compared with the minute quantities of modern sleeping drugs, which  seem to  have a way of latching on to the nerve cells so that incredibly small quantities can have widespread effects.

The barbiturates

The most famous sleeping pills in the twentieth century have been the barbiturates. In Berlin in 1864, Adolf von Baeyer created barbituric acid in his chemical laboratory, making it from malonic acid and urea.

He went out to celebrate his achievement at a local drinking house much favored by artillery officers and did so on the Day of St Barbara-the patron saint of artillery officers-and so from the words ‘Barbara’ and ‘urea’ was born the word ‘barbiturate’.

Then in 1903, Fischer and Von Mering, again working in Berlin, made barbitone, the old Veronal, Barbitone was the first barbiturate sleeping drug, and its use spread rapidly across the world.

Sure enough, it made people sleep; but once taken into the body, it was many days before it left again, and so people were sleepy all day as well as at night.

In 1912 came phenobarbitone (Luminal), perhaps the most famous of them all, which was very widely prescribed not only to induce sleep and soothe the nerves of insomniacs by day, but much more effective to treat epilepsy.

Like barbitone, phenobarbitone was not really a suitable drug for making people sleep at night, because there was almost as much left in the body at breakfast-time as there had been before midnight.

There then followed a number of shorter-acting barbiturates, that are still prescribed today, and  are known by trade names such as Sodium Amytal, Nembutal, and Sonery1.

These later barbiturates were very effective in relieving anxiety and inducing sleep.

Variations were introduced in which the anxiety-relieving effects of a barbiturate were supposed to be preserved of dexamphetamine, a drug causing wakefulness.

These mixtures, of which the so as drugs that would give a ‘high’, and addiction and trafficking developed.

Considerable quantities of barbiturates are still dispensed throughout the world, mainly to elderly people who have been reluctant to give up the crutch they have known for so many years.

Unfortunately the barbiturates are dangerous in overdose, and the rate of deaths per prescription from barbiturates has risen in recent years, despite an overall reduction in their prescribing.

The non-barbiturates

As it became recognized those barbiturates were liable to abuse and dependence, with unpleasant symptoms when they were stopped after regular intake, a variety of newer compounds were introduced, such as glutethimide (Doriden), meprobamate (Equanil) and the ill-fated thalidomide.

Another was methaqualone:  the mandrakes of olden times were to be succeeded by the new Mandrax, a pill containing methaqualone mixed with a drug called diphenhydramine.

Introduced in the 1960s, Mandrax was an instant success, and most especially among drug abusers who found in it another avenue to a quick ‘high’.

Both Mandrax and barbiturates became popular targets for drug pushers, who would often break into pharmacists’ shops in order to steal these drugs and then sell them; and so Mandrax, after a few dizzy years of success, has departed from the prescribing scene even more rapidly than the barbiturates.

There have been recent claims made by one or two researchers in the United States that pills containing the amino acid tryptophan, found naturally in food protein, are effective in promoting sleep. Our research in Edinburgh, however, does not confirm these claims.

The benzodiazepines

In 1957 a new drug was discovered called chlordiazepoxide that a few years later come to be sold as Librium. A great many chemically related drugs have followed, belonging to the general class known as benzodiazepines.

They all have the same actions in human beings, of relieving anxiety and promoting sleep. However, they differ in three respects: in the dosage necessary; in the further chemical compounds into which they are changed once they have entered the body; and in the persistence in the body both of the original compound and of the changed compounds.

Some, like diazepam (Valium) and flurazepam (Dalmane) are like the barbiturate phenobarbitone in that, with repeated intake, the concentrations of drug in the tissues build up cumulatively until eventually a plateau is reached.

This means that almost as much drug affect the brain by day as by night. Others, especially some of the newer ones like lormetazepam (Noctamid), when taken at bedtime, do to accumulate in the same way, about half of a bedtime dose being gone by breakfast-time.

The benzodiazepines are very much safer drugs than their predecessors. An overdose of most barbiturates can lead to death, whereas an overdose of benzodiazepine drugs virtually never does.

One of the curious features of benzodiazepines is that if somebody take twenty pills of, say, nitrazepam (Mogadon) then the  next morning they do not appear very much more doped than if they had taken only two or three (though they will stay dopey for longer).

The explanation seems to be that the molecules of the drug can only act on the brain cells by attaching themselves to the drug can only act on the brain cells by attaching themselves to certain positions, called ‘receptors’.

The number of these receptors is very limited, so that if they are occupied nearly to the full by a small intake of the drug, there is not much scope for further action even if a very large quantity has been taken.

This would also explain why amazingly small doses of some of the benzodiazepines are effective. Whereas the dose of chloral hydrate might be 1 g, and the dose of a barbiturate such as amylobarbitone sodium (Sodium Amytal) 200 mg, the dose of one of the newer and modified benzodiazepines called triazolam (Halcion) is 0.125 mg.

It is the safety factor that is the greatest merit in the benzodiazepines. They are not knock-out drops in the way that the barbiturates or Mandrax were, and they do not give a ‘high’, and so have held little attraction for drug abusers and pushers.

It would be wrong, however, to imagine that there are not some people who abuse benzodiazepines, or to think that dependence does not develop.

Dependence on these drugs is common, but he severity both of the dependence and of the symptoms on the withdrawal of benzodiazepines is much milder than after prolonged intake of a barbiturate.

This is partly because most of the benzodiazepines, like flurazepam (dalmane) or nitrazepam (Mogadon), are slowly eliminated from the body’s tissues, so that the let-down is gradual.

The newer benzodiazepines, like lormetazepam (Noctamid), leave the body faster, but give a sharper let-down on withdrawal.

Taken regularly, benzodiazepines do lead to dependence, but the social effects are few compared with dependence upon alcohol, and the dangers smaller than with barbiturates.

Benzodiazepines have been very successful in financial terms, but many of us in the medical profession believe that they have been greatly over prescribed.

Even though for commercial purposes some are advertised as sleeping pills and some as tranquillizers to soothe the nerves by day, all benzodiazepines have both these effects.

Alcohol

People don’t usually think of alcohol as a drug, but of course that’s exactly what it is. Alcohol certainly makes many of us sleepy, at least if we take it in the evening; and there are those who like to take a hot toddy or some other small but strong drink at bedtime, with a view to promoting sleep.

In spite of its effectiveness in bringing on sleep, alcohol is not only a cause of great social problems, but is also a leading cause of bad sleep.

It gets you to sleep more quickly, but you pay for it later through the rebound that will be described in the next section as well as through gastritis lack of appetite in the morning, and often a headache as well.

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