Opioids: The Whats and Hows of this Painkilling Drug

In terms of survival, there’s one thing that keeps us away from the things that damage us: Pain. It makes us avoid things that hurt us, and force us to nurse ourselves, helping us recover. One such example is sore muscles. We tend to massage them to ease the pain out, and by doing so, helps stimulate muscle cells to work faster, and smoothening the inflammatory process, allowing a quicker recovery.

The same idea can be applied to nearly everything that damages us. Thanks to pain, we know something is wrong with us and we need to nurse it or protect it.

Pain is not something your muscles actually feel. The brain is responsible for creating this sensation by the use of its chemical messengers known as Neurotransmitters. When there’s an abundance of them on a certain part of your body, you feel pain there.

Identification of these neurotransmitters is what allowed researchers to make advances in painkilling medication. This, in turn, helped created refined drugs called Opioids that effectively manipulate the nerves and brain, bringing about a sense of pleasure and the elimination of pain.

What Are Opioids?

Opioids are compounds that look like neurotransmitters and act like neurotransmitters, whose single message is to take the pain away. They are classified as narcotic medication and the realms of medicine, utilized by doctors for people suffering from chronic pain.

The History of Opioids

The very first use of Opioids goes as far back as 3400 BC. The white poppy plant or opium poppy plant was recognized for its painkilling and joy-giving qualities, so much that it was harvested and used to treat people who were suffering from various ailments. It’s joy-giving qualities also made it a popular recreational plant, used by the Assyrians. Eventually, they passed the practices to the Egyptians, who utilized the plant in a similar manner.

Even Hippocrates, known today as the Father of Modern Medicine, acknowledged it’s used as a narcotic and used it widely in epidemics. The usefulness of the plant as both for medicine and recreation continued on with the Arabs, Greeks, and Romans.

Its uses as an effective sedative were further acknowledged when it was first used by a Chinese surgeon around 220 AD to help patients undergoing major surgery, such as amputations, which were common during those times.

In the 1800’s, Friedrich Wilhelm Adam Sertürner, a German chemist, managed to isolate an alkaloid from the poppy plant mixture. This compound was known as morphine, named after Morpheus, the god of dreams. Aptly done because of Morphine’s powerful sedative abilities. The more powerful opiate was then used for various ailments that involved pain and anxiety.

It found a lot of use in the military, where the substance was used to help injured soldiers cope with the pain of their injuries. Unfortunately, this led them to become addicted to Morphine. The addiction and subsequent withdrawal effects were known back then as “Soldier’s Disease.”

The hypodermic needle was invented in 1853, giving an opportunity to use morphine more effectively during surgery, marking the proper medicalization of the substance, but with higher effectivity came more opportunities for abuse, so they sought for an alternative.

In 1898, Heroin was synthesized, advertised as a cough suppressant. It was also advertised to be a non-addictive derivative of morphine for medical use. They used Heroin to treat morphine addiction, which ironically, made the patient addicted to Heroin instead. The addiction spread like an epidemic and soon, in 1909, Congress made moves to restrict morphine use, along with its derivatives.

In the same vein, the University of Frankfurt created Oxycodone, another morphine derivative, intended to keep the same painkilling effect, with dramatically fewer dependence issues compared to morphine and heroin. Despite their efforts, oxycodone abuse became a problem. Morphine, Heroin and Oxycodone abuse still affected the country.

This went on, with pharmaceutical companies creating more derivatives in the attempt to keep as much effect as they can. This lead to the development of morphine derivatives that release the substance at a much slower rate. This allowed the painkilling effects to be active for a longer period of time and minimizing the pleasurable effects which may lead to addiction. Formulations like Fentanyl, Hydromorphone, and Methadone were synthesized to this effect.

To this day, addiction and dependence to Opioids still go on, albeit a bit quieter than before thanks to the advances made by the government and law enforcement.

How do Opioids Work?

The opioids extracted from the poppy plant or synthesized from raw chemicals. These chemicals are nearly the same as the neurotransmitters that our brain naturally has, so when it’s injected or introduced into the body, it goes through the blood, eventually reaches the brain and attaches to the nerves and brain cells. This causes the cells block any other neurotransmitters that may send signals of distress or pain, subsequently causing a feeling of utter goodness, pleasure and well being.

The chemicals in Opioids are not actual neurotransmitters but are structurally the same. They are also small enough to pass through the blood-brain barrier. This barrier is a layer of densely packed cells that only allow very select molecules to pass. Even some of the smallest bacteria can’t pass through it. Commonly, fat-soluble chemicals such as caffeine and alcohol can pass, and that includes all forms of opiates and opioids.

The effect is a bit similar to ibuprofen. The over-the-counter painkiller blocks prostaglandin, a chemical responsible for pain transmission and inflammation in cells. Except, opioids block every kind of pain transmitter in the body, which often causes a slight feeling of lethargy.

Apart from the brain, it can also affect the limbic system, which governs how the body expresses emotions, the brainstem which controls a majority of our involuntary actions, notably breathing, and the spinal chord, the first organ to receive the pain message.

What Drugs are Classified as Opioids?

There are many kinds of formulations, made for all manner of ailment relief, pain, diarrhea, to cough relief. These are the known formulations of Opioids used widely in medicine, especially in pain management.

  • Morphine
  • Methadone
  • Buprenorphine
  • Hydrocodone
  • Oxycodone
  • Codeine
  • Fentanyl

Then we have a few opioids used to control other minor ailments, all of which are over the counter:

  • Loperamide. Used to stop bowel movements by relaxing the intestines. The formulation doesn’t pass the blood-brain barrier and only majorly affects the bowels. This does not cause an opiate effect, and the only pleasure you’ll feel is the care nurses will give in the ICU.
  • Cough Medications. They contain a trace amount of codeine that helps relax the throat. Recent reformulations have removed codeine entirely with DMX, known as Dextromethorphan, a non-addictive derivative.
  • Doxylamine. Known as sleeping pills. They used to contain codeine to help you relax, but now they are a specially formulated antihistamine, whose secondary effect is to knock you out gently.

Presently, none of these will get you high, and taking them in large doses will only give you grief both from the damage you’ll cause your liver, and the medical bills that will come afterward. There’s nothing like the low of heavy debt.

Then we have Heroin. It was supposedly made as a version of Morphine without the addictive effects, but it failed. Heroin turns into morphine as soon as it enters the body, and the effect is not as strong as morphine and not as long. It had no more place in the medicinal world but somehow found a place in illegal drug trade.

What are Opioids Used For?

They are widely used for pain, but for what kind of pain? Opioids also have secondary effects that doctors and pharmaceutical companies take advantage of.

  • Pain Relief

The intended use. Since Opioids block the neurotransmitters responsible for sending pain signals, it helps nurses, doctors, and surgeons properly deal with the matter at hand, without causing the patient extreme discomfort.

Increased amounts of pain can cause blood pressure spikes, trouble breathing, muscle spasms, and psychological trauma. All of these can endanger a patient’s life or livelihood. It also has a more compassionate use, to help relieve terminally ill patients of the pain and discomfort they feel, so that what limited time they have is not spent writhing in pain.  

  • Anesthesia

Anesthesia is a combination of Analgesia, no pain; Amnesia, no memory; and Sedation; no consciousness. These three are key, because the body may still register the damage being done to you during surgery, causing latent trauma.

Oxymorphone, Fentanyl, Hydromorphone, and Morphine are the commonly used opioids for Anesthesia, and the fastest method is usually through the olfactory mucous membrane, aka breathing it in.

  • Antitussive

Also known as cough suppression. It’s actually a side effect of most opioids, perfect for persistent dry cough. A majority of the medicinal opioids such as codeine and hydrocodone are used for cough syrups before, but now they use dextromethorphan. It’s still technically an opioid, but it has none of the side effects and is not addictive.

  • Antimotility

Opioids have constipation as one of their other side effects. This means it can be used to suppress diarrhea. One thing worth remembering is that it’s incredibly hazardous to use suppress diarrhea caused by infection. Your body has a good reason to get them off your stomach, so let it do so. Opioids are better used for issues such as irritable bowel syndrome and other non-infective issues.

  • Rehabilitation Aid

Methadone is one example of an opioid that’s used to help people suffering from opiate/opioid addiction. Think of Methadone as an opioid that the brain sees as such, but doesn’t affect it. At low doses, this can help patients reduce withdrawal symptoms dramatically.

The side effect though, is that they have to go through withdrawal from Methadone afterwards, which isn’t as bad, thankfully.

Are Opioids and Opiates The Same?

In terms of effect, yes, they are practically the same. Opiates are drugs derived from Opium, this means opium is farmed and harvested, extracted and the compounds are mixed or refined into their intended forms, like Morphine.

Opioid has the suffix, “oid” that means “resembling but with imperfection” much like humanoid means, humanlike and android means, “man-like.” Opioids were once the name of synthesized opium, meaning they made it out of base compounds using an intricate process.

Presently, the term Opiate and Opioid are used interchangeably. But recent trends now gravitate to using the word Opioid as the general term for all natural, semisynthetic, and synthetic opium.

How Do Opioids Affect the Brain? How Does it Lead to Addiction?

Addiction has two arms, so to speak. The first one is the psychological effect of the drug in question. It can be opioids, alcohol, or cocaine. As long as it has an effect that helps rid the person of their stresses, it will work. Caffeine is one of the most popular “functional” addictions, as many people would not have a good day without a cup of joe. Thankfully, coffee is healthy for you when taken moderately.

If a person has enough stresses and experiences how the drug can take those stress away, they would want more of the drug, either to escape the stress or to be functional in the presence of it. Since opioids provide feelings of joy and well-being, it’s an instant hit to those who want an escape. If the stressors remain, the drug’s purpose continues.

This is why some people label opioids as the drug you’ll get addicted to, as soon as you take one. This is not true, of course, but the idea is correct in a lot of cases outside medicinal use.

The second arm is the body’s tolerance of the drug. Our body has a way of adapting to toxins and other chemicals that invade our body.  In the case of drugs, the body produces more enzymes, antibodies, or chemicals that counteract the drug, cleaning it out of the body faster. This means the high felt by the drug becomes less and less, getting to a point where the person must take more of the drug to feel the same high.

Combine the constant stressors, with the tolerance, and way to get a supply of the drug, and you have yourself an addict.

 

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