Morphine – action, use, dosage, contraindications, side effects. Addiction to morphine

Proven content

Morphine is the most common psychoactive drug found in opium and is a powerful pain reliever. As a drug, morphine is used in clinical pain relief, but it is also illegally used for recreational purposes by drug users. It is potentially highly addictive and can cause intense physical dependence which leads to overuse of morphine.

Morphine – what is it?

Morphine (Latin. Morphinum) is an organic chemical compound from the group of alkaloids. It occurs naturally in the dark brown, resinous form of the poppy (Papaver somniferum). It can be taken by mouth or injected. It acts directly on the central nervous system (CNS), inducing analgesia and changing the perception and emotional response to pain. Physical and psychological dependence may develop upon repeated administration. Morphine can be used for both acute and chronic pain, and is also often used for pain associated with myocardial infarction, kidney stones, and during childbirth.

Morphine can be administered orally, by injection into a muscle, by subcutaneous injection, by intravenous injection, in the space around the spinal cord, or rectally. Its maximum effect is achieved after about 20 minutes with intravenous administration and 60 minutes with oral administration, while its duration of action is between 3 and 7 hours. Potentially serious side effects of morphine include decreased breathing effort, vomiting, nausea, and low blood pressure.

Morphine was first isolated in 1803-1805 by the German pharmacist Friedrich Sertürner, who originally named the substance morphium after the Greek dream god Morpheus, because it tends to induce sleep.

The morphine derivatives include:

1. codeine – methyl ether,
2. thebaine – dimethyl ether,
3. heroin – a diacetyl derivative,
4. dionine – ethyl ether.

See also: Opium without poppy

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Morphine – action

Morphine is considered the classic opioid pain reliever and other painkillers have been compared with it. Like other drugs in its class, morphine has an affinity for delta, kappa and mi-opioid receptors. Morphine produces most of its analgesic effects by binding to the mu-opioid receptor in the central nervous system (CNS) and the peripheral nervous system (PNS).

The final effect of morphine action is the activation of descending inhibitory pathways of the central nervous system, as well as the inhibition of nociceptive afferents of the peripheral nervous system, which leads to an overall reduction in nociceptive transmission.

The repeated use of morphine may lead to the development of drug tolerance and physical and psychological dependence.

Morphine – application

The use of morphine – pain

Morphine is primarily used to treat acute and chronic severe pain. Its analgesic effect lasts approximately three to seven hours. The side effects of nausea and constipation are rarely severe enough to warrant discontinuation of treatment.

Morphine is also used for pain caused by a heart attack and for pain in labor. However, there are concerns that morphine may increase mortality from non-ST segment elevation myocardial infarction.

Morphine has also been used traditionally to treat acute pulmonary edema. However, the 2006 review found little evidence to support this practice. A 2016 Cochrane review concluded that morphine is effective in relieving cancer pain.

The use of morphine – shortness of breath

Morphine is beneficial in reducing symptoms of dyspnoea due to neoplastic and non-neoplastic causes. For dyspnea at rest or with minimal exertion from conditions such as advanced cancer or end-stage cardiorespiratory disease, regular low doses of sustained-release morphine significantly safely reduce dyspnea and its benefits persist over time.

Morphine use – opioid use disorder

Morphine is also available as a slow release preparation for opiate substitution therapy (OST) in Austria, Germany, Bulgaria, Slovenia and Canada for opioid addicts who are intolerant to neither methadone nor buprenorphine.

Morphine – dosage

Administration of morphine can be by various carriers. Morphine is usually administered via the oral, intravenous (IV), epidural and intrathecal routes. Oral formulations are available in both immediate and sustained release for the treatment of acute and chronic pain. Pain that is more severe and not well controlled can be controlled with single or continuous doses of intravenous, epidural and intrathecal preparations.

Intravenous dosing can vary widely between patients and depends largely on how they tolerate opiates. Morphine is also commonly administered intramuscularly. Morphine is also available as a suppository.

Morphine is widely used and abused. As a result, people found ways to snort the drug. Morphine is also available as an oral solution and can be administered sublingually. Sublingual morphine is very popular in palliative care.

Morphine – contraindications

Morphine is an extremely beneficial drug if used appropriately. However, in some situations, the remedy may be clearly contraindicated. In the event of severe respiratory depression and exacerbation of asthma, special care is required as morphine may further reduce the respiratory drive.

In addition, morphine should be avoided in the event of a previous hypersensitivity reaction and discontinued immediately in the event of an active reaction. Caution should also be exercised with the concomitant use of monoamine oxidase inhibitors (MAOIs), as these drugs are additive with morphine. This combination can then induce severe hypotension, serotonin syndrome, or worsen respiratory depression in patients.

Another important contraindication is gastrointestinal obstruction. It is also considered by many to be a contraindication to administering opioids to people who already have problems related to opioid substance abuse. While this is a very controversial topic, most clinicians will agree that pain requires treatment. However, most will agree and admit that there are alternatives to opioid painkillers.

See also: Is heavy breathing harmful to your health?

Morphine – side effects

Constipation is among the more common side effects of morphine use. This effect occurs by stimulating mu opioid receptors in the muscle plexus, which in turn inhibits gastric emptying and reduces peristalsis.

Other common side effects include depression of the central nervous system, nausea, vomiting and urinary retention. Respiratory depression is one of the more serious adverse reactions associated with opiate use, and monitoring is particularly important in post-operative patients.

Other reported side effects include dizziness and sedation. Patients often report nausea and vomiting, so many emergency departments are given morphine together with an antiemetic such as ondansetron.

Other symptoms include euphoria, dysphoria, agitation, dry mouth, anorexia, and biliary spasm, so some doctors will avoid morphine when patients experience pain in the right upper quadrant and suspect possible biliary pathology.

Morphine can also affect the cardiovascular system and reportedly can cause hot flashes, bradycardia, hypotension, and syncope. It should also be remembered that patients may experience itching, hives, swelling and other skin rashes.

See also: How do antiemetics work?

Morphine – addiction

Morphine is a highly addictive substance. In controlled studies comparing the physiological and subjective effects of heroin and morphine in former opiate addicts, subjects showed no preference for one drug over the other. Equivalent injected doses had comparable courses of action, with no difference in the self-esteem of euphoria, ambition, nervousness, relaxation, or sleepiness.

Short-term addiction studies by the same researchers found that tolerance developed at a similar rate as heroin and morphine. Compared to the opioids hydromorphone, fentanyl, oxycodone, and pethidine / meperidine, addicts preferred heroin and morphine to a greater extent, suggesting that heroin and morphine are particularly prone to abuse and addiction. Morphine and heroin were also significantly more prone to eliciting euphoria and other positive subjective effects compared to these other opioids.

The choice of heroin and morphine over other opioids by ex-drug addicts may also be because heroin is a morphine ester and a morphine prodrug, essentially meaning that they are identical drugs in vivo. Heroin is converted into morphine before it binds to opioid receptors in the brain and spinal cord, where morphine produces the subjective effects that addicts seek.

For the purposes of verification of addicts, it is allowed to perform a Shipping test for the presence of psychoactive substances – semi-quantitative determination. You can buy the survey at a favorable price on Medonet Market.

See also: This drug killed Prince and many people in the US

Morphine – tolerance

Several hypotheses have been made about the development of tolerance, including phosphorylation of the opioid receptor (which would alter the conformation of the receptor), functional separation of receptors from G proteins (leading to receptor desensitization), internalization of the μ-opioid receptor, or receptor downregulation (reduction in the number of receptors available to which are influenced by morphine) and the upregulation of the cAMP pathway (an anti-regulatory mechanism for opioid effects).

Drugs that antagonize CCK, in particular proglumid, have been shown to slow the development of tolerance to morphine.

Morphine – withdrawal syndrome

Discontinuation of morphine dosing leads to opioid withdrawal syndrome which, unlike barbiturates, benzodiazepines, alcohol, or sedatives and hypnotics, is not in itself fatal in healthy people.

Acute morphine withdrawal syndrome, along with any other opioid, goes through several stages. Other opioids differ in the intensity and length of each, and weak opioids and mixed antagonists can cause acute withdrawal syndromes that do not reach the highest levels. The following are listed:

1. Stage I, 6 to 14 hours after the last dose: craving drugs, anxiety, irritability, sweating and mild to moderate dysphoria;
2. Stage II, 14 h to 18 h after the last dose: yawning, profuse sweating, mild depression, lacrimation, crying, headache, runny nose, dysphoria, also exacerbation of the above symptoms, trance;
3. Stage III, 16 to 24 hours after the last dose: runny nose (runny nose) and increase in other symptoms mentioned above, dilated pupils, piloerection (goose bumps), muscle twitching, hot flushes, cold flushes, bone and muscle pain, loss appetite and the onset of intestinal cramps;
4. Stage IV, 24 to 36 hours after last dose: Increase in all of the above symptoms including severe cramps and involuntary movements of the legs (also called restless legs syndrome), loose stool, insomnia, increased blood pressure, moderate increase in body temperature, increased frequency of breathing and tidal volume, tachycardia (high pulse), restlessness, nausea
5. Stage V, 36 to 72 hours after the last dose: Increase in prior symptoms, embryonic position, vomiting, loose and frequent diarrhea which can sometimes speed up the time of food transfer from the mouth to the excretory system, weight loss by 2 kg to 5 kg per day , increased number of white blood cells and other changes in the blood;
6. Stage VI, restoration of appetite and proper bowel function, beginning of the transition to acute and chronic symptoms that are mostly psychological in nature, but may also include increased pain sensitivity, hypertension, colitis or other gastrointestinal motility complaints and problems with control scales in both directions.

In advanced stages of withdrawal, some patients have shown ultrasound signs of pancreatitis that are presumably attributed to spasm of Oddi’s sphincter.

The psychological dependence associated with morphine addiction is complex and chronic. Long after the physical need for morphine has passed, the addict usually still thinks and talks about using morphine (or other medications) and feels weird coping with daily activities without being influenced by morphine.

The psychological withdrawal of morphine is usually a very long and painful process. Addicted people often suffer from severe depression, anxiety, insomnia, mood swings, amnesia, low self-esteem, confusion, paranoia, and other mental disorders. Without intervention, the syndrome will progress and most of the overt physical symptoms will disappear within 7 to 10 days, including psychological dependence.

A high likelihood of relapse occurs when morphine is discontinued when neither the physical environment nor the behavioral motivators that contributed to the abuse have changed. The evidence of the addictive and restorative nature of morphine is the frequency of its relapses. Morphine (and heroin) abusers have one of the highest relapse rates among all drug users, reaching 98% according to some medical experts.

See also: When may mood swings happen?

Morphine – toxicity

Morphine can be potentially lethal if not used properly. It causes many symptoms associated with depression of the central nervous system. Severe respiratory depression is the most frightening complication of morphine in overdose. Immediate injection of naloxone is required to reverse the effects of morphine.

In the event of morphine poisoning, vomiting is usually induced with the administration of activated charcoal in an aqueous solution (even if morphine has been administered intravenously as it passes into the stomach) or with laxatives.

The minimum lethal dose of morphine is approx. 0,2 g, however, in case of hypersensitivity, death may occur even after taking 60 mg. It should be added, however, that when it comes to addicted people, they show increased tolerance to the drug and in their case even doses of 2-3 g per day do not cause symptoms of intoxication.

See also: Morphine poisoning