Hydromorphone

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Death may occur when opiates are combined with other depressants such as benzodiazepines, barbiturates, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances.[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

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Summary sheet: Hydromorphone


Hydromorphone
Hydromorphone.svg
Chemical Nomenclature
Common names Dilaudid, Jurnista, Palladone
Substitutive name Hydromorphone
Systematic name (4R,4aR,7aR,12bS)-9-hydroxy-3-methyl-1,2,4,4a,5,6,7a,13-octahydro-4,12-methanobenzofuro[3,2-e]isoquinoline-7-one
Class Membership
Psychoactive class Opioid
Chemical class Morphinan
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold 0.5 - 1 mg
Light 1 - 2 mg
Common 2 - 4 mg
Strong 4 - 8 mg
Heavy 8 mg +
Duration
Onset 20 - 45 minutes
Peak 3 - 4 hours








Intravenous
Dosage
Threshold 0.5 - 1 mg
Light 1 - 2 mg
Common 2 - 4 mg
Strong 4 - 6 mg
Heavy 6 mg +
Duration
Onset 10 - 90 seconds
Peak 1 - 2 hours

DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Hydromorphone (also known by the brand name Dilaudid in the United States) is a semisynthetic opioid of the morphinan chemical class that produces analgesic and euphoric effects when administered. It is occasionally prescribed for use in the management of moderate to severe pain and is structurally similar to other opioids such as morphine and heroin.

Hydromorphone is commonly used in a medical setting, mostly intravenously due its very low oral, rectal, and intranasal bioavailability.

If using this substance intravenously in a non-medical, recreational setting, the safer injection guide should be followed along with all harm reduction practices. Sublingual administration is also considered to be superior to oral administration in due to its increased bioavailability; however, hydromorphone is bitter and hydrophilic so it is absorbed poorly and slowly through mouth membranes.[2]

Chemistry

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Hydromorphone is an opioid of the morphinan class. Hydromorphone and other molecules of this class contain a polycyclic core of three benzene rings fused in a zig-zag pattern called phenanthrene. A fourth nitrogen containing ring is fused to the phenanthrene at R9 and R13 with the nitrogen member looking at R17 of the combined structure. This structure is called morphinan. Hydromorphone is a hydrogenated ketone of morphine and thus is extremely similar in structure.

It is a derivative of morphine; to be specific, it is a hydrogenated ketone thereof. Comparatively, hydromorphone is to morphine as hydrocodone is to codeine—that is, also a semi-synthetic drug.

Pharmacology

Hydromorphone molecules exert their effects by binding to and activating the μ-opioid receptor as an agonist. This occurs due to the way in which opioids structurally mimic endogenous endorphins. Endorphins are responsible for analgesia, sedation, and cognitive euphoria along with physical euphoria. 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.

The recreational effects of this compound, including cognitive euphoria and physical euphoria, occur because opioids structurally mimic endogenous endorphins which are naturally produced within the body and are also active on the μ-opioid receptor set in the brain. The way in which synthetic opioids such as heroin structurally mimic these natural endorphins results in their euphoric, pain relief and anxiolytic effects. This is because natural endorphins are responsible for reducing pain, causing sedation, and feelings of pleasure. The natural endorphins can be released in response to pain, strenuous exercise, orgasm, or general excitement.

Subjective effects

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The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.

Physical effects
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Cognitive effects
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Visual effects
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Toxicity and harm potential

Like most opioids, unadulterated hydromorphone does not cause many long-term complications other than psychological and physical dependence and constipation.[3] The harmful or toxic aspects of hydromorphone's usage as a recreational substance are exclusively associated with not taking appropriate precautions in regards to its administration, overdosing, and using impure or adultered batches of the substance.

Heavy dosages of hydromorphone can result in respiratory depression, leading onto fatal or dangerous levels of oxygen deprivation. This occurs because the breathing reflex is suppressed by agonism of µ-opioid receptors - this effect is proportional to the dosage of opiates consumed.

Hydromorphone 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 on their own vomit. 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).

Opioid overdoses can be fatal if not treated immediately by calling the local emergency medical services and administering an opioid antagonist such as naloxone to the overdosed user.

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

Tolerance and addiction potential

As with other opiate-based painkillers, the chronic use of hydromorphone 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 hydromorphone 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 constipation-inducing effects developing particularly slowly.

The risk of fatal opioid overdoses rise sharply after a period of cessation and relapse, largely because of reduced physical tolerance to the depressant effects of the opioid.[4] To account for this lack of tolerance, it is safer for a user that has been sober for an extended period of time to only dose a fraction of one's usual dosage when using again. It has also been found that the environment one is in can play a role in opioid tolerance.

In one 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.[5] Because of the structral and chemical similarity of hydromorphone and heroin, it can be assumed that the same interaction between physical tolerance and the environment occurs in hydromorphone use.

Dangerous interactions

Hydromorphone is dangerous to use in combination with other depressants as many fatalities reported as overdoses are caused by interactions with other depressant drugs like alcohol or benzodiazepines, resulting in dangerously high levels of respiratory depression.[6]

  • Depressants (1,4-Butanediol, 2m2b, alcohol, barbiturates, benzodiazepines, GHB/GBL, methaqualone) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another 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.
  • Dissociatives - This combination can result in 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.
  • Stimulants - It is dangerous to combine hydromorphone, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of hydromorphone, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of hydromorphone will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only taking a certain amount of hydromorphone. Some stimulants may also lower the seizure threshold.
  • Monoamine oxidase inhibitors - There have been rare cases of serotonin syndrome when opioids are used with monoamine oxidase inhibitors.[7][8]This has also been reported with other drugs that increase extracellular serotonin like selective serotonin reuptake inhbitors.[9]

Legality

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  • Austria: Hydromorphone is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich).[citation needed]
  • United Kingdom - Hydromorphone is a Class A, Schedule 2 drug in the United Kingdom.[10]
  • United States - Hydromorphone is a Schedule II Controlled Substance in the United States.[11]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. Hydromorphone Sheet|https://www.drugs.com/pro/hydromorphone.http
  3. Merck Manual of Home Health Handbook – 2nd edition, 2003, p. 2097
  4. Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2
  5. Siegel, S., Hinson, R., Krank, M., & McCully, J. (1982). Heroin “overdose” death: contribution of drug-associated environmental cues. Science, 216(4544), 436–437. https://doi.org/10.1126/science.7200260
  6. Fatal heroin 'overdose': a review (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/8997759
  7. Serotonin syndrome probably triggered by a morphine-phenelzine interaction. | https://www.ncbi.nlm.nih.gov/pubmed/25903219
  8. Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity. | https://www.ncbi.nlm.nih.gov/pubmed/16051647
  9. Serotonin syndrome induced by fluvoxamine and oxycodone. | https://www.ncbi.nlm.nih.gov/pubmed/16368927
  10. Home Office Controlled Drugs | https://www.gov.uk/government/publications/controlled-drugs-list--2/list-of-most-commonly-encountered-drugs-currently-controlled-under-the-misuse-of-drugs-legislation
  11. Drug Enforcement Administration Controlled Substances | https://www.deadiversion.usdoj.gov/schedules/orangebook/e_cs_sched.pdf