Desomorphine

Desomorphine strikes with a velocity that borders on violent. Within moments of entering the bloodstream, it detonates a rush of warmth so intense and so sudden that the body recoils before surrendering to it. The onset is not a transition -- it is a collision, a full-body impact that obliterates the boundary between discomfort and relief in a single, devastating instant. The rush is often described as comparable to heroin but compressed into an even narrower window, a concentrated blast of mu-opioid activation that saturates every receptor it can reach.

At the peak, the body becomes a furnace of artificial comfort. Warmth radiates from the core with an almost unbearable intensity, flooding the extremities, dissolving muscular tension with the efficiency of a solvent. The euphoria is profound and immediate -- not the gentle contentment of weaker opioids but a roaring, all-consuming satisfaction that crowds out every other sensation. The mind goes quiet. Thought does not so much slow as become unnecessary; the body is so thoroughly saturated with pleasure that cognition seems redundant. Pain, anxiety, memory -- all of it retreats behind a wall of pharmacological warmth so thick it feels permanent, even though some part of you knows it is not.

The physical signature is unmistakable: pinpoint pupils, skin flushed and warm to the touch, breathing reduced to a shallow, almost imperceptible rhythm. Nausea may strike but is often overridden by the sheer force of the euphoria. The characteristic opioid itch manifests strongly, crawling across the face and chest, but even this sensation is woven into the tapestry of pleasure, something to scratch with absent, dreamy satisfaction. The limbs are impossibly heavy, weighted with a gravitational pull that makes standing feel like an act of defiance against the compound's will.

But desomorphine's defining characteristic is its brevity. The peak lasts perhaps ninety minutes to two hours before the warmth begins to evaporate with startling speed. The decline is precipitous -- the wall of comfort crumbles rather than erodes, and the body is left exposed to the raw air of baseline consciousness with jarring suddenness. Muscles that were liquid moments ago begin to ache. The stomach turns. A creeping dysphoria seeps in from the edges, cold and insistent, the photographic negative of the warmth that preceded it.

The aftermath is harsh and unforgiving. The brevity of the experience means the body cycles from peak to withdrawal with punishing frequency. Within hours of the last dose, restlessness and discomfort announce themselves with a clarity that makes the preceding euphoria feel like a hallucination. Sleep is elusive, the body too agitated to rest, the mind too aware of the emptiness where warmth used to be.

he drug can be made from codeine and iodine derived from over-the-counter medications and red phosphorus from match strikers, in a process similar to the manufacturing of methamphetamine from pseudoephedrine. Like methamphetamine, desomorphine made this way is often contaminated with various agents. The street name in Russia for homemade desomorphine is krokodil (Russian: крокодил, crocodile), possibly related to the chemical name of the precursor α-chlorocodide, or the resemblance of the skin damage caused by the drug to a crocodile's leather.

Like other opiates, desomorphine exerts its effects by binding to and activating the μ-opioid receptor as an agonist. This occurs due to the way in which opioids functionally mimic the body's natural endorphins. Endorphins are responsible for analgesia (pain reduction), sleepiness, and feelings of pleasure and enjoyment. They can be released in response to pain, strenuous exercise, orgasm, or excitement. This mimicking of natural endorphins results in the drug's euphoric, analgesic (pain relief), and anxiolytic (anti-anxiety) effects.

Due to a lack of anecdotal reports using high purity desomorphine, the following effects are extrapolated from early clinical reports and inferences based on its relation to codeine and morphine. Desomorphine is considered to be powerfully euphoric opiate analgesia, with a fast onset and shorter duration that can encourage compulsive usage.

• Toxicity of desomorphine

Like most opioids, unadulterated desomorphine does not cause many long-term complications other than dependence and constipation. Outside of the extremely powerful addiction and physical dependence potential, the harmful or toxic aspects of desomorphine usage are exclusively associated with not taking appropriate precautions in regards to its administration, overdosing and using impure products derived from low-quality black-market self-manufacture.

Animal studies comparing pure desomorphine to morphine showed it to have increased toxicity, more potent relief of pain, higher levels of sedation, decreased respiration, and increased digestive activity

Heavy dosages of desomorphine can result in respiratory depression, leading to fatal or dangerous levels of anoxia (oxygen deprivation). This occurs because the breathing reflex is suppressed by agonism of µ-opioid receptors proportional to the dosage consumed.

Desomorphine can also cause nausea and vomiting; a significant number of deaths attributed to opioid overdose are caused by aspiration of vomit by an unconscious victim. This is when an unconscious or semi-conscious user who is lying on their back vomits into their mouth and unknowingly suffocates. It can be prevented by ensuring that one is lying on their side with their head tilted downwards so that the airways cannot be blocked in the event of vomiting while unconscious (also known as the recovery position).

• Toxicity of "krokodil"

Illicitly produced desomorphine is typically far from pure and often contains large amounts of toxic substances as a result of being "cooked" and used without any significant effort to remove the byproducts and leftovers from synthesis. Injecting any such mixture can cause serious damage to the skin, blood vessels, bone, and muscles, sometimes requiring limb amputation in long-term users.

Causes of this damage include iodine, phosphorus, and leftover solvents like gasoline and paint-thinner that are not adequately removed after synthesis. Strong acids and bases such as hydrochloric acid and sodium hydroxide are also employed without measuring pH of the final solution. Failure to remove insoluble fillers and binding aids from the codeine tablets used as starting material, as well as co-administration with pharmaceuticals such as tropicamide, are also cited as possible contributors to the high toxicity observed in users.

The frequent occurrence of tissue damage and infection among illicit users are what gained the drug its nickname of the "flesh-eating drug." The pure form of the drug itself does not cause this damage. Despite the severe health impacts and short survival times commonly reported, there are also rarer cases of krokodil users more skilled in the manufacturing process who have used the drug for many years without experiencing the tissue damage associated with the impure "street" product.

It is strongly recommended that one use harm reduction practices when using this drug.

As with other opiate-based painkillers, the chronic use of desomorphine can be considered extremely addictive and is capable of causing both physical and psychological dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops their usage.

Tolerance to many of the effects of desomorphine develops with prolonged use, including therapeutic effects. This results in users having to administer increasingly large doses to achieve the same effects. The rate at which this occurs develops at different rates for different effects with tolerance to the euphoric effects growing most quickly. Desomorphine presents cross-tolerance with Cross-all other opioids, meaning that after the consumption of desomorphine all opioids will have a reduced effect.

• Overdose

Depending on drug interactions and numerous other factors, death from overdose can take anywhere from several minutes to several hours. Death usually occurs due to lack of oxygen resulting from the lack of breathing. Many fatalities reported as opiate overdoses are probably caused by interactions with other depressants such as alcohol or benzodiazepines. It should also be noted that since opiates can cause nausea and vomiting, a significant number of deaths attributed to opiate overdose are caused by aspiration of vomit by an unconscious person.

The risk of fatal opioid overdoses rise sharply after a period of cessation and relapse, largely because of reduced tolerance. To account for this lack of tolerance, it is safer to only dose a fraction of one's usual dosage if relapsing. It has also been found that the environment one is in can play a role in opioid tolerance. In one scientific study, rats with the same history of heroin administration were significantly more likely to die after receiving their dose in an environment not associated with the drug in contrast to a familiar environment.

Opiate overdose is usually treated with an opioid antagonist, such as naloxone (Narcan). This reverses the effects of opioids like desomorphine and causes an immediate return of consciousness but may result in withdrawal symptoms. The half-life of naloxone is shorter than most opioids, so it may have to be administered multiple times until the body has metabolized the opioid.

• Depressants** (1,4-Butanediol, 2M2B, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation and sedation caused by each other and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.

• Germany:** Desomorphine is controlled under BtMG Anlage I, making it illegal to manufacture, import, possess, sell, or transfer it without a license.

• Russia:** Desomorphine is a Schedule I controlled substance.

• Switzerland: Desomorphine is a controlled substance specifically named under Verzeichnis A. Medicinal use is permitted.

• United States:** Desomorphine is a Schedule I substance in the United States. It is illegal to manufacture, buy, possess, or distribute without a DEA license.

• Responsible use

• Volumetric liquid dosing

• Safer injection guide

• Sharing injection materials

• Cotton fever

• Naloxone

• Opioid

• Codeine

• Morphine

• Desomorphine (Wikipedia)

• Desomorphine (Erowid Vault)

• Desomorphine (Isomer Design)

• Desomorphine (DrugBank)

• Gahr, M., Freudenmann, R. W., Hiemke, C., Gunst, I. M., Connemann, B. J., & Schönfeldt-Lecuona, C. (2012). Desomorphine goes “crocodile”. Journal of Addictive Diseases, 31(4), 407-412. https://doi.org/10.108//10550887.2012.735570

Desomorphine was first synthesized and patented in the United States in 1932. It was originally synthesized with the intention to create an alternative to morphine in terms of tolerance and addiction properties and improve the side effect profile. However, desomorphine fell short of these expectations and showed an increased dependence potential compared with morphine.

Desomorphine was used in Switzerland and introduced to the Swiss market in 1940 by the company Hoffman-La Roche, under the registered trade name of Permonid. It was used predominantly for postoperative pain due to its fast onset of action and reduced the tendency to cause respiratory depression and nausea. Its name is derived from crocodile (krokodil in Russian) and refers to the scaly, green-black skin discoloration frequently noted in its users. Krokodil is produced by synthesizing desomorphine from codeine and combining it with other low-cost, easily obtained additives. in a process similar to the manufacturing of methamphetamine from pseudoephedrine. Like methamphetamine, desomorphine made this way is often contaminated with various agents. The street name in Russia for homemade desomorphine iskrokodil (Russian: крокодил, crocodile), possibly related to the chemical name of the precursor α-chlorocodide, or the resemblance of the skin damage caused by the drug to a crocodile's leather.

Like other opiates, desomorphine exerts its effects by binding to and activating the μ-opioid receptor as an agonist. This occurs due to the way in which opioids functionally mimic the body's natural endorphins. Endorphins are responsible for analgesia (pain reduction), sleepiness, and feelings of pleasure and enjoyment. They can be released in response to pain, strenuous exercise, orgasm, or excitement. This mimicking of natural endorphins results in the drug's euphoric, analgesic (pain relief), and anxiolytic (anti-anxiety) effects.

Due to a lack of anecdotal reports using high purity desomorphine, the following effects are extrapolated from early clinical reports and inferences based on its relation to codeine and morphine. Desomorphine is considered to be powerfully euphoric opiate analgesia, with a fast onset and shorter duration that can encourage compulsive usage.

• Toxicity of desomorphine

Like most opioids, unadulterated desomorphine does not cause many long-term complications other than dependence and constipation. Outside of the extremely powerful addiction and physical dependence potential, the harmful or toxic aspects of desomorphine usage are exclusively associated with not taking appropriate precautions in regards to its administration, overdosing and using impure products derived from low-quality black-market self-manufacture.

Animal studies comparing pure desomorphine to morphine showed it to have increased toxicity, more potent relief of pain, higher levels of sedation, decreased respiration, and increased digestive activity

Heavy dosages of desomorphine can result in respiratory depression, leading to fatal or dangerous levels of anoxia (oxygen deprivation). This occurs because the breathing reflex is suppressed by agonism of µ-opioid receptors proportional to the dosage consumed.

Desomorphine can also cause nausea and vomiting; a significant number of deaths attributed to opioid overdose are caused by aspiration of vomit by an unconscious victim. This is when an unconscious or semi-conscious user who is lying on their back vomits into their mouth and unknowingly suffocates. It can be prevented by ensuring that one is lying on their side with their head tilted downwards so that the airways cannot be blocked in the event of vomiting while unconscious (also known as the recovery position).

• Toxicity of "krokodil"

Illicitly produced desomorphine is typically far from pure and often contains large amounts of toxic substances as a result of being "cooked" and used without any significant effort to remove the byproducts and leftovers from synthesis. Injecting any such mixture can cause serious damage to the skin, blood vessels, bone, and muscles, sometimes requiring limb amputation in long-term users.

Causes of this damage include iodine, phosphorus, and leftover solvents like gasoline and paint-thinner that are not adequately removed after synthesis. Strong acids and bases such as hydrochloric acid and sodium hydroxide are also employed without measuring pH of the final solution. Failure to remove insoluble fillers and binding aids from the codeine tablets used as starting material, as well as co-administration with pharmaceuticals such as tropicamide, are also cited as possible contributors to the high toxicity observed in users.

The frequent occurrence of tissue damage and infection among illicit users are what gained the drug its nickname of the "flesh-eating drug." The pure form of the drug itself does not cause this damage. Despite the severe health impacts and short survival times commonly reported, there are also rarer cases of krokodil users more skilled in the manufacturing process who have used the drug for many years without experiencing the tissue damage associated with the impure "street" product.

It is strongly recommended that one use harm reduction practices when using this drug.

As with other opiate-based painkillers, the chronic use of desomorphine can be considered extremely addictive and is capable of causing both physical and psychological dependence. When physical dependence has developed, withdrawal symptoms may occur if a person suddenly stops their usage.

Tolerance to many of the effects of desomorphine develops with prolonged use, including therapeutic effects. This results in users having to administer increasingly large doses to achieve the same effects. The rate at which this occurs develops at different rates for different effects with tolerance to the euphoric effects growing most quickly. Desomorphine presents cross-tolerance with Cross-all other opioids, meaning that after the consumption of desomorphine all opioids will have a reduced effect.

• Overdose

Depending on drug interactions and numerous other factors, death from overdose can take anywhere from several minutes to several hours. Death usually occurs due to lack of oxygen resulting from the lack of breathing. Many fatalities reported as opiate overdoses are probably caused by interactions with other depressants such as alcohol or benzodiazepines. It should also be noted that since opiates can cause nausea and vomiting, a significant number of deaths attributed to opiate overdose are caused by aspiration of vomit by an unconscious person.

The risk of fatal opioid overdoses rise sharply after a period of cessation and relapse, largely because of reduced tolerance. To account for this lack of tolerance, it is safer to only dose a fraction of one's usual dosage if relapsing. It has also been found that the environment one is in can play a role in opioid tolerance. In one scientific study, rats with the same history of heroin administration were significantly more likely to die after receiving their dose in an environment not associated with the drug in contrast to a familiar environment.

Opiate overdose is usually treated with an opioid antagonist, such as naloxone (Narcan). This reverses the effects of opioids like desomorphine and causes an immediate return of consciousness but may result in withdrawal symptoms. The half-life of naloxone is shorter than most opioids, so it may have to be administered multiple times until the body has metabolized the opioid.

• Depressants** (1,4-Butanediol, 2M2B, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation and sedation caused by each other and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.

• Germany:** Desomorphine is controlled under BtMG Anlage I, making it illegal to manufacture, import, possess, sell, or transfer it without a license.

• Russia:** Desomorphine is a Schedule I controlled substance.

• Switzerland: Desomorphine is a controlled substance specifically named under Verzeichnis A. Medicinal use is permitted.

• United States:** Desomorphine is a Schedule I substance in the United States. It is illegal to manufacture, buy, possess, or distribute without a DEA license.

• Responsible use

• Volumetric liquid dosing

• Safer injection guide

• Sharing injection materials

• Cotton fever

• Naloxone

• Opioid

• Codeine

• Morphine

• Desomorphine (Wikipedia)

• Desomorphine (Erowid Vault)

• Desomorphine (Isomer Design)

• Desomorphine (DrugBank)

• Gahr, M., Freudenmann, R. W., Hiemke, C., Gunst, I. M., Connemann, B. J., & Schönfeldt-Lecuona, C. (2012). Desomorphine goes “crocodile”. Journal of Addictive Diseases, 31(4), 407-412. https://doi.org/10.108//10550887.2012.735570