Opiates

Opiate drugs can be both, natural or man-made, which generates the typical effects of opiate (the natural resin present in opium poppy) - a blend of euphoria, out of the world, slackened breathing, reduced feeling of pain, constipation and fixed pupils.

Instead of using the term opiates, occasionally scientists make use of the more common word 'opioids', which comprise drugs that have a resemblance to substances present in the opium poppy, in addition to endogenous opioids that function in the form of neurotransmitters in the brain.

Precisely speaking, opium denotes a formulation of opium poppy (botanical name Papaver somniferum). All over the world, opium is usually obtained by means of an extremely low-tech, manual method.

People who cultivate opium cut the growing seed pod of the opium poppy and save the gum-like fluid that secretes from the place where the seed pot has been cut during the following few days. Subsequently, various different methods are applied to refine the sap.

For instance, some cultivators may dry the sap and turn it into a ball (gum opium) for direct use. Alternately, it may also be dried and ground into a powder, called the opium powder.

Raw or unrefined opium has the appearance of a brown colored tar-like substance. Opium may also be used to prepare tincture of opium, which is actually an alcohol-water extract of opium.

In effect, this alcohol-water extract is one of the well-known laudanum of the era dating back to your great-great-grandmother or an opium-based painkiller (paregoric) from that period!

While countries like Afghanistan, Burma and Thailand in Southeast Asia and Colombia in South Africa grow opium in substantial amounts, Mexico supplies with the basic material for preparing illegal heroin that is offloaded in the United States.

Generally, the opium poppies cultivated in the South-eastern countries provide heroin for the European countries, but some of it is also transported to the United States.

However, the bulk of the opium poppy for heroin comes to the United States from nations like Mexico and Columbia.

If you intent to prepare an effective drug using opium poppy, the simplest method is to begin with the compounds that occur naturally in it and have some specific influence on the user. This is exactly what the pharmacologists have done with opium poppy.

In effect, no less than five significant opiate analgesics exist and these are either prepared directly from the opium seed pods or trivial modifications of the seed pod of the opium poppy.

One of the important constituents of the opium seed pod is morphine, which is basically a very strong opiate that is used in the forms of pills or injections to alleviate pain following a surgery.

Another constituent is called codeine, which is comparatively less potent and is primarily used in the form of pills to provide relief from mild pains.

Several people have come across this constituent in the form of an acetaminophen-codeine formulation, which is generally employed to ease dental pain or forms an ingredient of prescription cough medications, such as terpin hydrate with codeine, Robitussin A-C, Cheracol and many others.

In order to balance the lower strength of codeine, a number of drug users just drink the whole four-ounce content of the bottle that does not have any inebriating volume.

Such cough syrups were generally available as over-the-counter drugs till recently, when their recreational use became extremely fashionable.

Several other amalgams are formulated synthetically by means of transforming the substances present in the opium. Such compounds include oxycodone, hydromorphone and also hydrocodone.

In fact, hydromorphone (Dilaudid) is an extremely potent opiate and also a useful analgesic, which is abused extensively.

Oxycodone is prepared by synthesizing the non-analgesic substance present in opium called thebaine and, from the view of its potency in relieving pain, this compound is graded just after morphine and before codeine.

Among all forms of opiate drugs, heroin is definitely the most ill-famed drug. Actually, heroin is a synthetically refined form of morphine that is developed from partially distilled morphine.

Generally, this narcotic substance is prepared in so-called refineries that are located in the neighbourhood of the place of opium production in the countries mentioned above.

In addition, heroin is split into small quantities and is generally found on the street in plastic bags in the form of a loose powder. Each such bag usually contains approximately 100 mg of this white powder.

The real color of heroin may vary from white to brown or even black conditional on the source of the substance as well as the quality of the preparation method. Heroin hydrochloride that is extremely purified generally has a white appearance and is valued for its clarity.

On the other hand, as its name suggests, the heroin available from Mexico, called the Mexican 'black tar', has a black appearance. Usually the user directly sniffs the powder or liquefies it in salty water and injects the solution.

The genuine constituents of the powder is dependent on the person supplying the substance and may vary from about 10 per cent to 70 per cent of heroin mixed with a variety of impurities, which may include baking powder, talc, and even quinine, maintaining a specific balance.

If the fact is that heroin is simple morphine which has been somewhat chemically modified, what benefits it offers? Precisely speaking, when heroin goes into the brain, it is again transformed into morphine.

Nevertheless, the enhanced fat solubility of the converted morphine provides specific benefits, for instance, it enters the brain more rapidly.

In effect, several medical practitioners are campaigning for the use of heroin in cancer patients who are in their last stages of life because using heroin means relieving the pain even faster.

It is worth mentioning here that meperidine (Demerol) is employed in the similar way as morphine for easing extreme pains suffered by a patient following a surgery and it also works excellently when given orally.

However, using meperidine also results in a number of adverse effects. For instance, when taken in high doses, meperidine may lead to convulsions - an aspect that has actually prompted the physicians to lessen the use of this substance in recent times.

On the other hand, methadone is an exceptionally enduring opiate that may even be taken in the pill form. The exceptional time course of this opiate makes this drug especially effective in the treatment of withdrawing addicts, in addition to chronic pain.

This drug starts working slowly and mildly which helps to avoid any withdrawal symptoms, but the user does not experience a 'high'. The use of meperidine for such purposes has given rise to controversies in a number of circles.

Despite the fact that it obviously helps in developing tolerance and physical dependence, meperidine actually offers a safe as well as effectual treatment with no similar problems for abuse.

Fentanyl (Sublimaze) is another drug that is extremely fat soluble and, as an analgesic, works extremely fast. This is the main reason why anesthesiologists use this drug when they want the patient to fall asleep.

In addition, fentanyl is also used in patches, which release the drug gradually through the skin to make it possible for the patient to experience pain relief for a longer period.

In effect, several addicts also use the injectable form of fentanyl and it is often a widespread reason for overindulge.

When one uses fentanyl, he or she get a 'high' very soon, but the sensation is very extreme, short-lived and only one step away from an inhibition of breathing that may turn fatal.

Before concluding, we need to make a mention of another opiate drug - propoxyphene (Darvon). As this drug is a very inferior type of opiate, several physicians do not prefer to use it.

In addition, findings of clinical studies have revealed that compared to a placebo, propoxyphene is no better. Nevertheless, there are many people who have faith in this drug, but the basic fact is that it is just somewhat more potent compared to aspirin.

How opiates are taken

Majority of the opiate drugs get into the bloodstream without any difficulty from several dissimilar means as they are fat soluble and this makes their entry into the cells easy.

However, heroin is an exception because it dissolves in fatty substances so easily that it can even be taken up by the mucosal lining inside the nose.

Many other opiate drugs do not dissolve in fatty substances so easily and, therefore, they cannot be soaked up by the mucosal lining of the nose properly even when snorted.

Nevertheless, when heated, a number of opiate drugs, counting the naturally occurring constituents of the opium poppy, release a vapour that can be absorbed by the body provided they are smoked.

In fact, this forms the basis of using the 'opium pipe' - a device that has been used traditionally to take in opiates and its use also continues to this day. On the other hand, nearly all types of opiate drugs can be soaked up by the body from the stomach.

However, injecting the opiates still remain the more effective way of taking them, especially in the instance of morphine, which, compared to other opiates, is poorly absorbed even from the stomach.

In effect, till date, intravenous injection continues to be the most effective and fastest means for delivering opiates into the bloodstream.

As intravenous injection is comparatively difficult as well as a dangerous method compared to other methods, most people using opiates do not use this means.

Rather, majority of the people would prefer to start taking opiates by injecting the drugs just below the skin (subcutaneously). Usually, heroin powder is liquefied in water and then injected.

On the other hand, injectable form of morphine, meperidine and fentanyl injections that is always available as legal drugs, which have been sidetracked from medical use, while some amount of fentanyl is also produced illegally at secretive laboratories.

Of late, snorting heroin has become more popular that taking heroin injections, particularly among the new drug users.

This is partially owing to the reason that many drug users are making an effort to avoid the disgrace as well as the perils of developing AIDS that are common when they take injections.

There are some other drug users who falsely believe that they are unlikely to turn addicts if they do not take heroin injections, but snort the substance.

On the other hand, propoxyphene and codeine are two opiates that are mostly taken by mouth. While the more potent opiate preparations like oxycodone (OxyContin, Percodan), hydromorphone (Dilaudid), methadone (Dolophine) and meperidine (Demerol) are available in the pill form.

Occasionally, some desperate drug users also pound the codeine, methadone or hydrocodone pills, prepare a suspension dissolving them in saline water and inject the suspension when they are unable to obtain injectable form of the opiates by any means.

However, it needs to be underlined that doing this is highly dangerous because the components of the pills do not dissolve properly in saline water.

When you inject particles into the bloodstream, they are likely to cause irritation and this may set off a series of reactions resulting in inflammation of the blood vessels and even causing irreversible harm to them.

Moreover, the particles of the pills may also settle down in any part of the blood vessel, thereby, completely blocking the blood circulation to any particular part of the body.

Opiate effects

As mentioned earlier, all types of opiates create a pleasurable, sleepy condition wherein users forget about everything and often fall asleep. In addition, owing to their analgesic attribute, the opiates also help to lessen all painful sensations.

In fact, the sensations are all the more strong when people use the injectable form of opiates, as it causes a rush within.

It has been found that people who are experiencing the effects of opiates often say that they are no longer troubled regarding their problems; in effect, they are in a very unique and safe condition wherein they are unconscious of all their problems and miseries.

Therefore, the attraction for using opiates is very much comprehensible. However, the users seldom realize in the beginning that using opiates also lead to miseries as well as withdrawal symptoms.

Even as the individual using opiate feels drowsy and is in an enjoyable condition, his/ her breathing slows down, the pupils become pinpointed and they usually suffers from queasiness and may also vomit.

While the impact of the drug on breathing may prove to be fatal, the additional physical symptoms are rather gentle. For instance, even if you take opiates, it will not cause any drastic change in your blood pressure, provided you are healthy and in the best of health.

Most of the influences caused by opiates are on the brain, particularly on the opiate receptors in those areas of the brain that are engaged in regulating breathing and additional reflex functions.

To understand this better, you will notice opiate users vomiting and this is owing to the fact that morphine invigorates a specific center within the brain - called the chemoreceptor trigger zone - which works to cause vomiting in reaction to digestive disorders caused by any toxin.

It may be noted that opiate produces a very significant impact on the body and for generations this has made the life of people traveling abroad much easy.

Actually, opiate augments the pressure in specific muscles present in the digestive tract with the intention that the usual propulsive movements that make the food travel down are not able to function efficiently and this results in constipation - a well-known effect of using opiates.

In effect, this can prove to be very beneficial for you in case you are having a traveler's diarrhea and are currently in Mexico. Using diphenoxylate (Lomotil) makes use of an efficient chemical way to stop diarrhea causing no effect whatsoever on the brain.

The usual opiate molecule is somewhat modified with the intention that it does not become so soluble in fat that it may go inside the brain.

This actually provides you with an extremely safe as well as useful medication that many pharmaceutical firms have endeavoured to make better, but have had very little success thus far, and is certainly an extensively used drug that is helpful in treating mild cases of diarrhea.

Opiates also tighten the urinary bladder muscles using a similar modus operandi and may result in problems while urinating.

How opiates move through the body

The time taken by opiates to enter the brain or the pace at which they travel to the brain is largely dependent on the route the user adopts to take them.

In fact, the quickest manner to enter the brain or become 'high' is to take the injectionable form of opiates, as it helps the opiates to get into the bloodstream directly.

Smoking is the second fastest way for the opiates to enter the brain. It may be noted that when people inject opiates into their bloodstream or smoke them, it takes only a few minutes to attain the peak level or a 'high'.

Among all opiates, fentanyl is known to dissolve in fatty substances most easily and, hence, it also achieves the utmost concentrations in the brain within seconds.

In fact, this is one reason why this opiate is so popular among the drug users, especially those who use it for non-medicinal purposes.

Heroin, on the other hand, is a little sluggish in entering the brain - a couple of minutes are needed for it to enter the brain. Morphine is even slower in entering the brain and takes about five minutes to do so - not much slower when compared to heroin.

It needs to be cautioned, the fastest an opiate gets into the brain and gives a 'high', more is the chance of death owing to overdo, as the levels of the drug in the brain is able to go up so rapidly.

It is very natural that snorting or sniffing opiates takes a longer time for the body to take them up. In this case, the drug will have to pass through the mucous membranes within the nose and then to the blood vessels beneath them.

We have talked about injecting and snorting opiates, so what happens when we take opiate pills?

In this case it takes a much longer time for the opiate to reach the brain and, therefore, the 'high' too also comes very slowly for the drug must first be taken up by the small intestine and then pass it on to the bloodstream, which will take the opiate to the liver for metabolizing most of the dosage before it can get back to circulation and enter the brain.

Hence, it takes about 30 minutes for the drug from the time to popping the pill to reach the brain. Therefore, in this case no rush is created within.

The primary reason why methadone is very effective for the treatment of drug addicts and also in the form of an analgesic (pain killer) is that it does not create a rush.

However, at times, regular drug users are able to find a way to get around the opiate formulations that are meant to have a gradual onset - OxyContin is an ideal as well as notorious example of this.

In effect, OxyContin is an extended-release form of oxycodone, which is intended to release its contents slowly helping the sufferers to experience relief from pain over a prolonged period.

However, when the users crush the pill and take it orally or inject a saline suspension of the drug, it gives a quick 'high' - something that was never intended by its manufacturers. Because of its abuse by drug users, OxyContin soon gained the repute of being a 'hot' drug.

However, the fact remains that OxyContin is just a garden-form of opiate analgesic medication that can effectively ease pain provided it is used in the appropriate manner.

When abused, this drug may lead to a series of undesirable effects. Hence, OxyContin is neither an exceptional drug, nor is it magical.

As far as the time for which the buzz after taking opiates lasts is concerned, there is little diversity. However, there are certainly some differences as to how fast the buzz starts.

For instance, the buzz brought about by majority of the opiate drugs discussed in this article usually continues for anything between four and six hours.

While the precise time may range from a minimum of two hours (in the case of morphine) to a maximum of about six hours (in the case of propoxyphene), but, generally speaking, all opiates are somewhat same.

However, there are just two major exceptions to this. The effect of methadone continues for anything between 20 hours and 24 hours and, hence, a single daily dose of this opiate drug may be sufficient.

On the other hand, fentanyl is another extreme - its effects generally fade away within just an hour.

Precisely speaking, the period for which the action of the opiates lasts is largely conditional on the time consumed by the enzymes which metabolize the drugs in the liver to disintegrate any particular opiate drug.

How opiates work

The endeavour of the opium poppy to produce opium alkaloids may perhaps mirror the original plant evolution to contest the biology of their pillagers/ pollinators.

In fact, the opium poppy plant has been able to work out the process to produce a compound that had an influence on their brains.

Precisely speaking, it is not only the poppy plant which has been achieve to attain this feat, as there are several plants that also produce compounds, which are psychoactive.

In other words, several plants are able to make compounds that have a significant effect on the mental process. For instance, several species of hallucinogenic mushrooms, the marijuana plant and the coca shrub are among such plants that also possess the aptitude to have an influence on the actions as well as functioning of animals that consume them.

In addition, plants are not the only living things that can produce opioids, as specific types of frogs can also produce compounds that are similar to opioids. These frogs produce the opioids on their skin and most possibly they are also used for similar purposes.

All opiates work on particular receptor molecules for the enkephalin/endorphin category of neurotransmitters within the brain.

Such endogenous opioids are basically chemical neurotransmitters, which regulate the movement, dispositions and functioning of the animals.

They also assist in regulating several other physical activities, counting breathing, digestion and controlling the body temperature of the animals.

In addition, these endogenous opioids facilitate in processing the feelings of pain, and they also turn on the reward circuits, and when they are excited, they make you experience a 'high'.

All such actions occur when the neurons present in the different areas of the brain release enkephalins or endorphins. Generally, every single neuron does its own work, and starts shooting only when it is required.

It may be noted that virtually there never occurs a situation when all the endogenous opioid neurons are activated at the same time.

When you take heroin, it causes an effect which is something like all the endogenous opioid neurons within the brain firing simultaneously.

Now the question arises as to which of the several endogenous opioid neurons in the brain are precisely responsible for experiencing a 'high' after taking an opiate.

The first among them is a small set of neurons present in the hypothalamus of the brain.

In fact, this is the place where the neurons which make use of the primary endorphin neurotransmitter beta-endorphin first get activated and, subsequently, they extend or split up all over the brain.

According to a hypothesis, all these neurons turn out to be dynamic when there is too much pressure and work to calm down the opiate user.

The theorists hypothesize that when the body is enduring intense stress, for instance, when one is just about to die, a feeling of peaceful relaxation is all that is most needed at that particular moment.

In such situations, beta-endorphin neurons shoot as if they are wild and bring on a pleasing condition something akin to those induced by opioids.

It may be mentioned here that at present, scientists are almost half-way on their mission of substantiating that beta-endorphin has the aptitude to bring about such a condition.

We are aware of the fact that taking beta-endorphin injections in the brain generates several phases of such a condition, which also includes decelerated breathing, drowsiness as well as analgesia.

Unlike the beta-endorphin, the case of enkephalins presents a different story. Various dissimilar types of neurons utilize enkephalins to be in touch with other neurons.

The enkephalins are present in the areas of the brain that are engaged in processing sensations related to pain, regulating breathing as well as additional functioning that are affected by the opiates.

In fact, the enkephalins are also present in the gastrointestinal tract and here their job is to regulate the digestive function.

Most importantly, the enkephalins are also present in numerous places in our body that are concerned with the reward system and their presence in such places may possibly be vital.

Nevertheless, they possibly do not work in cohesion or as an organized unit, something different from the endorphin neurons.

Therefore, it may be said that the enkephalins and endorphins are actually dissimilar members belonging to an intimately associated neurotransmitter 'family'.

A third member of this so-called family is called the dynorphins and they too perform similar actions, including analgesia, but, in reality, result in disagreeable instead of an enjoyable feeling.

All these three different neurotransmitters also share common receptors. Probably, this is one resourceful evolutionary ploy by the brain to obtain the maximum 'excitement for the money spent' from the neurotransmitters as well as their receptors.

It is possible to generate numerous potential combinations that would eventually turn out a vast assortment of effects by merging the dissimilar opioid peptides with their receptors.

These neurotransmitters generate a variety of influences by means of sharing three dissimilar types of receptor molecules.

The most important opiate receptor, which is called 'mu' - a Greek alphabet, offers the key effects of opiates, which include ecstasy, analgesia, slowed respiration and others - the effects produced by all opiates.

The principal supporting receptor, called the 'delta' works together with 'mu' in some areas to facilitate in generating similar effects. The third receptor is called the 'kappa' and this has a bizarre nature.

Drugs which are especially meant for this particular receptor generate sensations like analgesia, but they never give the user a 'high'. This might make you think that this is an ideal analgesic drug that does not lead to addiction.

However, it has one downside too - invigorating this receptor itself results in a state that is just opposite of euphoria, or dysphoria (a condition of restiveness, dissatisfaction and nervousness).

It is really unfortunate that every clinically helpful drug that we are currently using is only specific for the 'mu' receptor, and, hence, all these drugs are addictive too.

The fact is that so far it is not possible to differentiate the addicting properties of the opiates from their analgesic attributes.

Comments

Post your comments, tips, or suggestions.
©2002-2025 herbs2000.com