Barbiturates (Sleeping Pills)
Barbiturates Information
A History Of Barbiturates
Barbituric acid (a combination of urea and malonic acid) the base material of barbiturates, which itself does not affect the CNS, was first synthesized on December 4, 1863 by Adolph von Bayer (his pharmaceutical firm also first synthesized Aspirin and many other compounds).
The date of the discovery was the feast day of Saint Barbara, so he named his discovery Barbara's urates in her honor.
Because barbituric acid does not effect the CNS, it took close to forty years before a use could be found for Barbituric acid.
That's when Barbital (barbitone) was synthesized and introduced, in 1903 under the brand name Veronal, as a sedative. Barbiturates were an effective sedative for the terminally nervous.
They helped dyed-in-the-wool insomniacs sleep like babies. They reduced seizure activity in epileptics and quieted the terror of long-hospitalized mental patients. They helped anesthetize patients before surgery.
Since 1903 a large number of barbiturates have been manufactured under a variety of names. In short, barbiturates, all 2,500 or so, that were eventually derived from Bayer's original formula were true wonder drugs of their day.
Widely used at first, their medical use has now been drastically reduced since the introduction of the benzodiazepines (valium, xanax, etc) and they are now confined to a few specific situations.
The reason why is, they turned out to be addictive, and they cause life-and-death problems when used to excess, or when a heavily addicted user (years of use) quits cold turkey.
The withdrawal syndromes, can assume lethal forms, especially because of the occurrence of seizures. Acute intoxication results in coma, and chronic intoxication can cause damage to the liver and delirium.
Barbiturates affect the GABA receptors (like GHB) and thereby bring about a general inhibition of the activity of the CNS, especially that part of the brain stem which governs the rhythm of waking and sleeping.
By inhibiting activating stimuli, they induce sleep. The only activating stimuli which are not inhibited by barbiturates are pain stimuli.
Chronic barbiturate users often display irritability and aggressiveness, as well as lethargy, confusion and lack of emotional control (crying). They also display neurological phenomena such as nystagmus, dysarthria and cerebellar ataxia.
As in the case of other CNS inhibitors (like Rohypnol), enforced staying awake after taking barbiturates can produce a paradoxical intoxication, an effect that is also relatively common among the aged and patients with organic disturbances of the CNS.
Barbiturate use leads to an increase in the activity in the liver of the cytochrome P450, leading to a reduction in the breakdown of other exogenous and endogenous substances (including steroids), while stimulating other enzyme systems, so that some drugs have a reduced effect (incl. chlorpromazine, griseofulvin and coumarines).
As a result, disturbances of the endocrine balance regularly occur among chronic barbiturate users and there is a risk of negative interaction with other drugs.
Other Sedatives
Besides barbiturates, a number of sedatives have been developed, such as Glutethimide (brand name: Doriden), a nonbarbiturate sedative with mild side effects, according to the manufacturer.
Nevertheless, cases of persistent addiction to this drug have been described, including not only the same phenomena as in chronic barbiturate use, but above all loss of weight because of the extreme loss of appetite.
Another of these drugs is methaqualone (brand names: Mandrax, Revonal, Isonox), which also affects the metabolism of other drugs and is therefore dangerous in combinations.
Types Of Barbiturates
Ultrashort-acting: Examples are methohexital (Brevital), thiamylal (Surital), thiopental (Pentothal), Sodium Pentothal. They produce their effects quickly, usually within 20 minutes. They're used most often to prepare surgical patients for anesthesia.
Short / Intermediate-acting: Examples are Seconal and Nembutal. This group takes a little longer to start their effects, but work over a longer period of time. After oral administration, the onset of action is from 15 to 40 minutes and the effects last up to 6 hours.
These drugs are primarily used for sedation or to induce sleep. Veterinarians use pentobarbital for anesthesia and euthanasia. This group is usually used recreationally.
Lone-acting barbiturates: Examples are phenobarbital (Luminal) and mephobarbital (Mebaral) Long-acting barbs may not achieve full effectiveness for hours or days. They're often used for daytime sedation, to reduce seizures, and calm anxiety.
Dosage
Low doses (50mg or so) are similar to alcohol. Effects involve a mild impairment of thought and coordination and the same release of inhibition that enables drinkers to sing (even if they're tone deaf) or flirt (even if they're shy).
Moderate doses (100-200mg) produce effects that are more pronounced, with sleep a more-or-less predictable outcome. Doses at this level can also cause a mild intoxication, complete with slurred speech, clouded judgment, and a greater release of inhibition.
High doses (more than 200mg, in a non-addicted person), result in an even more intense, and more unpredictable, level of intoxication. Here, users display wide mood swings, and may talk in a babbling, incoherent manner.
Coordination can be reduced to the point that ordinary activities, walking down stairs or driving a car, become serious, life-on-the-line emergencies. Normal judgment is markedly reduced at best, nearly nonexistent at worst.
In the body, higher doses can cause life- threatening symptoms from lowered blood pressure and heart rate to cardiovascular collapse. When that happens you're dead.
Use
Barbiturates are usually taken orally, but people who are used to using a needle to take heroin or other drugs, may inject them. Mixing alcohol and barbs (or other depressants) not only produces a deeper level of intoxication; it also produces a much greater depressant action on the heart and lungs, bad news.
Problems
Addicts usually take a lot of barbiturates for a long time. And that causes a lot of problems like impaired thinking and memory, bad reflexes, depression, reduced sex drive, and paranoia.
On the physical side, there's deterioration of the central nervous system and damage to the liver and pancreas, both linked to the toxicity of the drug in the body.
Tolerance builds quickly. That means users have to keep raising their dosage to keep feeling the way they felt yesterday and the day before that.
And that can mean disaster because while tolerance to the intoxicating effects of barbiturates is fast, tolerance to the respiratory-depressant effects is slow, which means that things can get lethal quickly.
Overdose
The best way to handle an overdose is to
a) maintain breathing
b) keep the person awake and moving (preferably in the direction of the nearest hospital)
c) don't try coffee or anything else that will slow down going to a hospital
Don't count on first class service, emergency room staff have little sympathy for overdoses. Seeing babies dying from car accidents and other crap that they have to deal with everyday, leaves them with little respect for people who "do it to themselves"
What Are Goof Balls ?
Street names for barbiturates include barbs, red devils, goof balls, yellow jackets, block busters, pinks, reds, blues, and Christmas trees.
Legal
All sedatives and hypnotics are Prescription Only under the Medicines Act. This means that they can only be sold at a pharmacy, in accordance with a doctor's prescription.
All the misusable barbiturates, others from the same class of barbiturates, others from the same class of barbiturates and the sedative methaqualone are in class B of the Misuse of Drugs Act.
Their unauthorized production, supply or possession are offences. It is also an offences to allow premises to be used for supplying or producing these drugs.
Quitting
See your doctor before quitting, after regular use, tolerance and psychological dependence are likely to develop in any sedative but the danger with barbiturates is that the amount needed to cause respiratory failure increases relatively little.
Serious problems of physical dependency are unlikely, but withdrawal effects can include irritability, fainting, nervousness, nausea and convulsions. Sudden withdrawal from very high doses can even be fatal. Medical advice is essential.
Entertainers
Barbiturates seem to have it in for popular entertainers. Marilyn Monroe and Jimi Hendrix were only the two most prominent names on coroner's reports listing barbiturate poisoning or depressant drug OD as the cause of death.
Thousands of other names, famous and not famous, were there, too. That's the main reason the drugs have declined both as medical drugs and in street availability in recent years.
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