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Use of opioids such as morphine and heroin can lead to drug addiction. Despite this problem, opioids remain vital in medicine for treating severe pain. Non-addictive alternatives to opioids are often unavailable.

Medicinal properties of opioids, the alkaloids derived from the opium poppy plant, are well known from ancient history. Various derivatives of natural morphine are know at present time. Despite different properties, chemically they are very similar.

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One of the most powerful painkillers in medical use is diamorphine. Diamorphine is also known as morphine diacetate or heroin. This is a derivative of natural alkaloid morphine.

Heroin was synthesized for the first time by acetylation of morphine in 1874, by R.C. Alder Wright who worked at St. Mary’s Hospital Medical School in London. The discovery didn’t attract much attention. Felix Hoffmann from German company Aktiengesellschaft Farbenfabriken (now known as Bayer) has synthesized the drug again 23 years later.

From 1898 to 1910 the drug was advertised by Bayer under the name Heroin as a non-addictive substitute of morphine and cough medicine. This is still considered as one of the biggest blunders in the company’s history. During the 1920s the legislation was adopted in most countries to ban the drug.

Diamorphine has multiple medical applications

In medicinal purposes diamorphine is used to treat severe pain. The conditions such as heart attack, severe injury and post-surgical pain often require the use of strong analgesic drugs such as diamorphine. The drug is also used for patients suffering from severe pain at terminal stages of some illnesses like cancer.

Diamorphine has essentially the same uses as another opioid analgesic drug, morphine. Diamorphine shows less severe side effects than morphine. Essentially, this is a faster acting form of morphine.

Like other opioids, diamorphine can be used as both analgesic and recreational drug.

Diamorphine is the pro-drug of morphine. This means that it is metabolically converted inside the body into morphine.

Chemically two compounds are very similar. Diamorphine has two additional acetyl groups. These groups get removed in the body with the help of enzymes called esterase.

Diamorphine is more potent than morphine. As a result, smaller doses of diamorphine are needed to achieve the same effect. This is a result of higher solubility of diamorphine in lipids and, consequently, better ability to cross the blood – brain barrier. Most of the physiological targets of these drugs are located in various regions of brain.

Opioid alkaloids bind to the specific proteins in the body called opioid receptors that mediate their effects. There are several types of opioid receptors in the human body. They include µ-opioid receptors, as well as κ- and δ-receptors. Heroin works on µ-opioid receptors only.

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