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Difference between revisions of "Hydromorphone"

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== Also known as ==
  
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Dilaudid, palladone, D, footballs, dust, juice, smack, dillies
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== Classification ==
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Opioid, analgesic
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[[Category:Opioids]][[Category:Analgesics]]
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== Overview ==
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Hydromorphone is an opioid pain medication. An opioid is sometimes called a narcotic. Hydromorphone is used to treat moderate to severe pain <ref name="1053a">'''Hydromorphone''', 2017, https://www.drugs.com/mtm/hydromorphone.html</ref>.
 +
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An opioid analgesic derived from morphine and used mainly as an [[analgesic]]. It has a shorter duration of action and is more potent than morphine <ref name="1055a">'''Hydromorphone''', 2017, https://www.drugbank.ca/drugs/DB00327</ref>.
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== Medical usage ==
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Hydromorphone is used to treat severe pain that isn't controlled by other opioid drugs <ref name="1056a">'''Hydromorphone''', 2017, http://www.healthline.com/drugs/hydromorphone/oral-tablet</ref>.
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== Why take it? ==
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=== Sought after effects ===
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* intense pleasure,
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* physical relaxation and decreased tension,
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* decreased anxiety and worry,
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* increased sleepiness <ref name="1054a">Patterson, E., '''Signs & Symptoms of Hydromorphone Abuse''', 2017, http://drugabuse.com/library/signs-symptoms-of-hydromorphone-abuse/</ref>.
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=== Undesired effects ===
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* nausea,
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* vomiting,
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* constipation,
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* headache,
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* insomnia,
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* decreased appetite,
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* feeling lightheaded or dizzy,
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* increased sweating,
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* hyperalgesia, or worsening pain,
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* anxiety,
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* depression <ref name="1054a"/>.
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== Dosage ==
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=== Abuse ===
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==== Oral ====
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* threshold 0.5 - 1 mg,
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* light 1 - 2 mg,
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* common 2 - 4 mg, 3 - 4 mg <ref name="1051a">'''Hydromorphone''', 2017, http://drugs.tripsit.me/hydromorphone</ref>,
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* strong 4 - 8 mg,
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* heavy 8 mg + <ref name="1046a">'''Hydromorphone''', 2017, https://psychonautwiki.org/wiki/Hydromorphone</ref>.
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==== Insufflated ====
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* threshold 0.5 - 1 mg,
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* light 1 - 2 mg,
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* common 2 - 4 mg,
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* strong 4 - 6 mg,
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* heavy 6 mg + <ref name="1046a"/>.
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==== Intravenous ====
 +
 +
* light 1 - 2mg,
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* common 2 - 4mg,
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* strong 4 - 6mg+ <ref name="1051a"/>.
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== What are the different forms? ==
 +
 +
Oral liquid, immediate-release tablet, extended-release tablet, injectable solution, suppository <ref name="1054a"/>.
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== How long do its effects last? ==
 +
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=== Onset of effects ===
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* oral - 20 - 45 minutes <ref name="1046a"/>, 30 - 60 minutes <ref name="1051a"/>, 20 - 40 minutes <ref name="1052a">'''Hydromorphone''', 2017, https://wiki.tripsit.me/wiki/Hydromorphone</ref>.
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* intravenous - 10 - 90 seconds <ref name="1046a"/>, 0 - 1 minutes <ref name="1051a"/>.
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* insufflated - 5 - 10 minutes <ref name="1051a"/>.
 +
 +
=== Peak ===
 +
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* oral - 3 - 4 hours <ref name="1046a"/>.
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* intravenous - 1 - 2 hours <ref name="1046a"/>.
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=== Duration of effects ===
 +
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* oral - 3 - 4 hours <ref name="1051a"/>.
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* intravenous - 1 - 2 hours <ref name="1051a"/>.
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* insufflated - 2 - 3 hours <ref name="1051a"/>.
 +
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=== After-effects ===
 +
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* oral - 1 - 6 hours <ref name="1051a"/>.
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* intravenous - 1 - 6 hours <ref name="1051a"/>.
 +
* insufflated - 1 - 6 hours <ref name="1051a"/>.
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 +
== 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]], and [[anxiolytic]] effects.
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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 <ref name="1046a"/>.
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=== Pharmacodynamics ===
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Hydromorphone is a hydrogenated ketone derivative of morphine that acts as a narcotic analgesic. It has a shorter duration of action than morphine. Hydromorphone is approximately 8 times more potent on a milligram basis than morphine. In addition, hydromorphone is better absorbed orally than is morphine. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the [[central nervous system]] and gastrointestinal tract. Its primary actions of therapeutic value are analgesia and sedation. Hydromorphone appears to increase the patient's tolerance for pain and to decrease discomfort, although the presence of the pain itself may still be recognised. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Opioids also produce respiratory depression by direct action on brain stem respiratory centres <ref name="1055a"/>.
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=== Absorption ===
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Better absorbed orally than morphine <ref name="1055a"/>.
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=== Bioavailability ===
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Oral 51.35% +/- 29.29%, insufflated 52.4%, rectal 36.33% +/- 29.6% <ref name="1051a"/>.
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=== Metabolism ===
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Primarily hepatic. After absorption hydromorphone is metabolised by the liver to the glucuronide conjugate which is then excreted in the urine. Hydromorphone is metabolised to the major metabolites hydromorphone-3-glucuronide, hydromorphone-3-glucoside and dihydroisomorphine-6-glucuronide <ref name="1055a"/>.
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=== Half-life ===
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2.6 hours (oral); 18.6 hours for sustained release Palladone <ref name="1055a"/>.
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=== Elimination ===
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Only a small amount of the hydromorphone dose is excreted unchanged in the urine. Most of the dose is excreted as hydromorphone-3-glucuronide along with minor amounts of 6-hydroxy reduction metabolites <ref name="1055a"/>.
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=== Lethal dosage ===
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2.9191 [[LD50]] mol/kg in rats <ref name="1055a"/>.
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=== Toxicity ===
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Hydromorphone is a schedule II narcotic which can lead to physical dependence or addiction <ref name="1055a"/>.
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=== Tolerance ===
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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 <ref name="1046a"/>.
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=== Mechanism of action ===
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Hydromorphone is a narcotic analgesic; its principal therapeutic effect is relief of pain. Hydromorphone interacts predominantly with the opioid mu-receptors. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the [[central nervous system]] and gastrointestinal tract. Hydromorphone also binds with kappa-receptors which are thought to mediate spinal analgesia, [[miosis]] and [[sedation]] <ref name="1055a"/>.
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== Signs of usage ==
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* lie to and manipulate others for money or the substance,
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* struggle to perform routine activities like going to work or school,
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* have problems paying their bills/fulfilling financial obligations,
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* schedule many doctors' appointments to receive multiple prescriptions,
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* isolate themselves or spend time with new groups of people <ref name="1054a"/>.
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== Effects ==
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=== Physical effects ===
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* physical euphoria,
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* pupil constriction,
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* skin flushing,
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* appetite suppression,
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* orgasm suppression,
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* pain relief,
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* respiratory depression,
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* sedation,
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* constipation,
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* difficulty urinating,
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* itchiness,
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* nausea <ref name="1046a"/>.
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=== Cognitive effects ===
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* cognitive euphoria,
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* compulsive redosing,
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* dream potentiation,
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* anxiety suppression,
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* decreased libido <ref name="1046a"/>.
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=== Visual effects ===
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* internal hallucinations <ref name="1046a"/>.
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=== Minor effects ===
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==== More common ====
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* constipation,
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* difficulty with moving,
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* joint pain,
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* muscle pain or stiffness,
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* nausea <ref name="1053a"/>.
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==== Less common ====
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* acid or sour stomach,
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* back pain,
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* belching,
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* oedema,
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* diarrhoea,
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* discouragement,
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* feeling sad or empty,
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* heartburn,
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* indigestion,
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* irritability,
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* dysphoria,
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* muscle spasms,
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* pain in the arms or legs,
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* stomach discomfort, upset, or pain,
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* tingling of the hands or feet,
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* trouble concentrating,
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* unusual weight gain or loss <ref name="1053a"/>.
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==== Less common or rare ====
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* being forgetful,
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* bleeding after defecation,
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* clumsiness,
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* tinnitus,
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* crying,
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* delusions of persecution, mistrust, suspiciousness, or combativeness,
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* difficulty with swallowing,
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* difficulty with walking,
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* double vision,
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* excess air or wind in the stomach or intestines,
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* feeling of constant movement of self or surroundings,
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* full feeling,
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* increased appetite,
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* joint pain, stiffness, or swelling,
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* loss in sexual ability, desire, drive, or performance,
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* loss of balance,
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* low body temperature,
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* muscle aches,
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* muscle twitching or jerking,
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* overactive reflexes,
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* rhythmic movement of muscles,
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* runny nose,
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* seeing, hearing, or feeling things that are not there,
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* sensation of spinning,
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* shivering,
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* slurred speech,
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* sneezing,
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* oedema
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* trouble with speaking <ref name="1053a"/>.
 +
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==== Incidence not known ====
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* bad, unusual or unpleasant (after) taste,
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* burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings,
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* chills,
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* constricted, pinpoint, or small pupils (black part of the eye),
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* deep or fast breathing with dizziness,
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* drowsiness,
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* dry mouth,
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* false or unusual sense of well-being,
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* fear or nervousness,
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* feeling of warmth,
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* hives or welts,
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* itching,
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* muscle stiffness or tightness,
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* numbness of the feet, hands, and around the mouth,
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* redness of the face, neck, arms, and occasionally, upper chest,
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* relaxed and calm feeling,
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* shaking,
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* uncontrolled eye movements,
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* upper stomach pain <ref name="1053a"/>.
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=== Major effects ===
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==== Less common or rare ====
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* agitation,
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* bloody, black, or tarry stools,
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* blurred vision,
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* changes in behaviour,
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* chest pain or discomfort,
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* convulsions,
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* decreased urination,
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* dry mouth,
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* fast, pounding, slow or irregular heartbeat,
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* lightheadedness, dizziness, or fainting,
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* mood or mental changes,
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* rapid breathing,
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* severe stomach pain, cramping, or burning,
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* stiff neck,
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* sunken eyes,
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* thoughts of killing oneself,
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* trouble breathing,
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* unusual tiredness,
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* vomiting of material that looks like coffee grounds, severe and continuing,
 +
* wrinkled skin <ref name="1053a"/>.
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==== Incidence not known ====
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* cyanosis,
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* change in the ability to see colours, especially blue or yellow,
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* cold, clammy skin,
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* confusion,
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* cough,
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* decrease in frequency of urination or urine amount,
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* difficulty in passing urine (dribbling),
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* dizziness,
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* fast or weak pulse,
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* headache,
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* irregular, fast or slow, or shallow breathing,
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* loss of appetite,
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* noisy breathing,
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* painful urination,
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* sweating,
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* tightness in the chest,
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* insomnia <ref name="1053a"/>.
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=== Positive ===
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* euphoria,
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* pain relief <ref name="1052a"/>.
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=== Neutral ===
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* pupil constriction,
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* itching,
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* sedation <ref name="1052"/>.
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=== Negative ===
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* drowsiness,
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* [[CNS]] depression,
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* dizziness,
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* nausea,
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* vomiting,
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* constipation,
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* sweating <ref name="1052a"/>.
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=== Side-effects needing medical attention ===
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The following symptoms may be more serious and may require immediate medical attention -
 +
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* rash or hives,
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* new and unexplained swelling,
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* trouble breathing,
 +
* difficulty swallowing,
 +
* chest pain,
 +
* extreme drowsiness,
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* fainting,
 +
* seizures <ref name="1054a"/>.
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=== Overdose ===
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 +
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 <ref name="1046a"/>.
 +
 +
* difficulty breathing,
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* slowed or stopped breathing,
 +
* excessive sleepiness,
 +
* dizziness,
 +
* fainting,
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* limp or weak muscles,
 +
* narrowing or widening of the pupils,
 +
* cold, clammy skin,
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* slow or stopped heartbeat,
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* cyanosis,
 +
* loss of consciousness or coma <ref name="1045a">'''Hydromorphone''', 2017, https://psychonautwiki.org/wiki/Hydromorphone</ref>,
 +
* convulsions/seizures <ref name="1053a"/>.
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== Dangerous interactions ==
 +
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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 <ref name="1047a">Darke, S. and Zador, D., '''Fatal heroin 'overdose': a review''', ''Addiction'', 1996, 91, 12, 1765-1772, https://doi.org/10.1046/j.1360-0443.1996.911217652.x, http://www.ncbi.nlm.nih.gov/pubmed/8997759</ref>, <ref name="1046a"/>.
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* '''Depressants (1,4-Butanediol, 2m2b, [[alcohol]], barbiturates, benzodiazepines, [[GBL / GHB]], 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.
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* '''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.
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* '''Monoamine oxidase inhibitors''' - There have been rare cases of serotonin syndrome when opioids are used with monoamine oxidase inhibitors <ref name="1048a">Mateo-Carrasco, H. and Muñoz-Aguilera, E. M. and García-Torrecillas, J. M. and Abu Al-Robb, H., '''Serotonin syndrome probably triggered by a morphine-phenelzine interaction''', ''Pharmacotherapy'', 2015, 35, 6, 102-105, https://doi.org/10.1002/phar.1581, https://www.ncbi.nlm.nih.gov/pubmed/25903219</ref>, <ref name="1049a">Gillman, P. K., '''Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity''', ''British Journal of Anaesthesia'', 2005, 95, 4, 434-441, https://doi.org/10.1093/bja/aei210, https://www.ncbi.nlm.nih.gov/pubmed/16051647</ref>. This has also been reported with other drugs that increase extracellular serotonin like selective serotonin reuptake inhibitors <ref name="1050a">Karunatilake, H. and Buckley, N. A., '''Serotonin syndrome induced by fluvoxamine and oxycodone''', ''Annals of Pharmacotherapy'', 2006, 40, 1, 155-157, https://doi.org/10.1345/aph.1E671, https://www.ncbi.nlm.nih.gov/pubmed/16368927</ref>, <ref name="1046a"/>.
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=== Dangerous ===
 +
 +
* '''[[Ketamine]]''' - Both substances bring a risk of vomiting and unconsciousness. If the user falls unconscious while under the influence there is a severe risk of vomit aspiration if they are not placed in the recovery position.
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* '''[[MXE]]''' - This combination can potentiate the effects of the opioid.
 +
* '''[[DXM]]''' - [[CNS]] depression, difficult breathing, heart issues, hepatoxic, just very unsafe combination all around. Additionally if one takes [[dxm]], their tolerance of opiates goes down slightly, thus causing additional synergistic effects.
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* '''[[Cocaine]]''' - Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
 +
* '''[[Alcohol]]''' - Both substances potentiate the [[ataxia]] and [[sedation]] caused by the other and can lead to unexpected loss of consciousness at high doses. Place affected patients in the recovery position to prevent vomit aspiration from excess. Memory blackouts are likely.
 +
* '''[[GBL / GHB]]''' - The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position
 +
* '''[[Tramadol]]''' - Concomitant use of [[tramadol]] increases the seizure risk in patients taking other opioids. These agents are often individually epileptogenic and may have additive effects on seizure threshold during coadministration. Central nervous system- and/or respiratory-depressant effects may be additively or synergistically present.
 +
* '''Benzodiazepines''' - Central nervous system and/or respiratory-depressant effects may be additively or synergistically present. The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position. Blackouts/memory loss likely <ref name="1051a"/>.
 +
 +
=== Caution ===
 +
 +
* '''[[PCP]]''' - [[PCP]] can reduce opioid tolerance, increasing the risk of overdose.
 +
* '''[[Nitrous oxide]]''' - Both substances potentiate the ataxia and sedation caused by the other and can lead to unexpected loss of consciousness at high doses. While unconscious, vomit aspiration is a risk if not placed in the recovery position. Memory blackouts are likely.
 +
* '''Amphetamines''' - Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
 +
* '''MAOIs''' - Coadministration of monoamine oxidase inhibitors (MAOIs) with certain opioids has been associated with rare reports of severe and fatal adverse reactions. There appear to be two types of interaction, an excitatory and a depressive one. Symptoms of the excitatory reaction may include agitation, headache, diaphoresis, hyperpyrexia, flushing, shivering, myoclonus, rigidity, tremor, diarrhoea, hypertension, [[tachycardia]], seizures, and coma. Death has occurred in some cases <ref name="1051a"/>.
 +
 +
== Withdrawal ==
 +
 +
* restlessness,
 +
* increased sensations of pain,
 +
* inability to sleep,
 +
* nausea,
 +
* diarrhoea,
 +
* vomiting,
 +
* agitation,
 +
* muscle spasms,
 +
* cold flashes,
 +
* sweating,
 +
* increased blood pressure and heart rate <ref name="1054a"/>.
 +
 +
== Drug testing ==
 +
 +
=== How long does hydromorphone stay in the urine? ===
 +
 +
Hydromorphone can be detected in the urine for 3 - 4 days <ref name="1045a"/>.
 +
 +
=== How long can hydromorphone be detected in blood? ===
 +
 +
A blood test can detect Hydromorphone for up to 24 hours <ref name="1045a"/>.
 +
 +
=== How long can a saliva test detect hydromorphone? ===
 +
 +
A saliva test can detect Hydromorphone for up to 1 - 4 days <ref name="1045a"/>.
 +
 +
=== How long can a hair test detect hydromorphone? ===
 +
 +
Hydromorphone can be detected with a hair follicle drug test for up to 90 days <ref name="1045a"/>.
 +
 +
== Statistics ==
 +
 +
* Pain relievers are the most abused drugs after marijuana and hashish.
 +
* In 2014, 4.3 million people in the U.S. admitted using painkillers non-medically.
 +
* In a 2011 survey, 1 million people admitted to abusing hydromorphone in their lifetime <ref name="1054a"/>.
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 +
== History ==
 +
 +
Knoll introduced it to the mass market in 1926 under the brand name ''Dilaudid'', indicating its derivation and degree of similarity to morphine (by way of laudanum). The brand name Dilaudid is more widely known than the generic term hydromorphone, and because of this, Dilaudid is often used generically to mean any form of hydromorphone <ref name="1052a"/>.
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----
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== References ==
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<references />
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Revision as of 15:51, 3 May 2017

Also known as

Dilaudid, palladone, D, footballs, dust, juice, smack, dillies

Classification

Opioid, analgesic

Overview

Hydromorphone is an opioid pain medication. An opioid is sometimes called a narcotic. Hydromorphone is used to treat moderate to severe pain [1].

An opioid analgesic derived from morphine and used mainly as an analgesic. It has a shorter duration of action and is more potent than morphine [2].

Medical usage

Hydromorphone is used to treat severe pain that isn't controlled by other opioid drugs [3].

Why take it?

Sought after effects

  • intense pleasure,
  • physical relaxation and decreased tension,
  • decreased anxiety and worry,
  • increased sleepiness [4].

Undesired effects

  • nausea,
  • vomiting,
  • constipation,
  • headache,
  • insomnia,
  • decreased appetite,
  • feeling lightheaded or dizzy,
  • increased sweating,
  • hyperalgesia, or worsening pain,
  • anxiety,
  • depression [4].

Dosage

Abuse

Oral

  • threshold 0.5 - 1 mg,
  • light 1 - 2 mg,
  • common 2 - 4 mg, 3 - 4 mg [5],
  • strong 4 - 8 mg,
  • heavy 8 mg + [6].

Insufflated

  • threshold 0.5 - 1 mg,
  • light 1 - 2 mg,
  • common 2 - 4 mg,
  • strong 4 - 6 mg,
  • heavy 6 mg + [6].

Intravenous

  • light 1 - 2mg,
  • common 2 - 4mg,
  • strong 4 - 6mg+ [5].

What are the different forms?

Oral liquid, immediate-release tablet, extended-release tablet, injectable solution, suppository [4].

How long do its effects last?

Onset of effects

  • oral - 20 - 45 minutes [6], 30 - 60 minutes [5], 20 - 40 minutes [7].
  • intravenous - 10 - 90 seconds [6], 0 - 1 minutes [5].
  • insufflated - 5 - 10 minutes [5].

Peak

  • oral - 3 - 4 hours [6].
  • intravenous - 1 - 2 hours [6].

Duration of effects

  • oral - 3 - 4 hours [5].
  • intravenous - 1 - 2 hours [5].
  • insufflated - 2 - 3 hours [5].

After-effects

  • oral - 1 - 6 hours [5].
  • intravenous - 1 - 6 hours [5].
  • insufflated - 1 - 6 hours [5].

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, and anxiolytic 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 [6].

Pharmacodynamics

Hydromorphone is a hydrogenated ketone derivative of morphine that acts as a narcotic analgesic. It has a shorter duration of action than morphine. Hydromorphone is approximately 8 times more potent on a milligram basis than morphine. In addition, hydromorphone is better absorbed orally than is morphine. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Its primary actions of therapeutic value are analgesia and sedation. Hydromorphone appears to increase the patient's tolerance for pain and to decrease discomfort, although the presence of the pain itself may still be recognised. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Opioids also produce respiratory depression by direct action on brain stem respiratory centres [2].

Absorption

Better absorbed orally than morphine [2].

Bioavailability

Oral 51.35% +/- 29.29%, insufflated 52.4%, rectal 36.33% +/- 29.6% [5].

Metabolism

Primarily hepatic. After absorption hydromorphone is metabolised by the liver to the glucuronide conjugate which is then excreted in the urine. Hydromorphone is metabolised to the major metabolites hydromorphone-3-glucuronide, hydromorphone-3-glucoside and dihydroisomorphine-6-glucuronide [2].

Half-life

2.6 hours (oral); 18.6 hours for sustained release Palladone [2].

Elimination

Only a small amount of the hydromorphone dose is excreted unchanged in the urine. Most of the dose is excreted as hydromorphone-3-glucuronide along with minor amounts of 6-hydroxy reduction metabolites [2].

Lethal dosage

2.9191 LD50 mol/kg in rats [2].

Toxicity

Hydromorphone is a schedule II narcotic which can lead to physical dependence or addiction [2].

Tolerance

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 [6].

Mechanism of action

Hydromorphone is a narcotic analgesic; its principal therapeutic effect is relief of pain. Hydromorphone interacts predominantly with the opioid mu-receptors. These mu-binding sites are discretely distributed in the human brain, with high densities in the posterior amygdala, hypothalamus, thalamus, nucleus caudatus, putamen, and certain cortical areas. They are also found on the terminal axons of primary afferents within laminae I and II (substantia gelatinosa) of the spinal cord and in the spinal nucleus of the trigeminal nerve. In clinical settings, Hydromorphone exerts its principal pharmacological effect on the central nervous system and gastrointestinal tract. Hydromorphone also binds with kappa-receptors which are thought to mediate spinal analgesia, miosis and sedation [2].

Signs of usage

  • lie to and manipulate others for money or the substance,
  • struggle to perform routine activities like going to work or school,
  • have problems paying their bills/fulfilling financial obligations,
  • schedule many doctors' appointments to receive multiple prescriptions,
  • isolate themselves or spend time with new groups of people [4].

Effects

Physical effects

  • physical euphoria,
  • pupil constriction,
  • skin flushing,
  • appetite suppression,
  • orgasm suppression,
  • pain relief,
  • respiratory depression,
  • sedation,
  • constipation,
  • difficulty urinating,
  • itchiness,
  • nausea [6].

Cognitive effects

  • cognitive euphoria,
  • compulsive redosing,
  • dream potentiation,
  • anxiety suppression,
  • decreased libido [6].

Visual effects

  • internal hallucinations [6].

Minor effects

More common

  • constipation,
  • difficulty with moving,
  • joint pain,
  • muscle pain or stiffness,
  • nausea [1].

Less common

  • acid or sour stomach,
  • back pain,
  • belching,
  • oedema,
  • diarrhoea,
  • discouragement,
  • feeling sad or empty,
  • heartburn,
  • indigestion,
  • irritability,
  • dysphoria,
  • muscle spasms,
  • pain in the arms or legs,
  • stomach discomfort, upset, or pain,
  • tingling of the hands or feet,
  • trouble concentrating,
  • unusual weight gain or loss [1].

Less common or rare

  • being forgetful,
  • bleeding after defecation,
  • clumsiness,
  • tinnitus,
  • crying,
  • delusions of persecution, mistrust, suspiciousness, or combativeness,
  • difficulty with swallowing,
  • difficulty with walking,
  • double vision,
  • excess air or wind in the stomach or intestines,
  • feeling of constant movement of self or surroundings,
  • full feeling,
  • increased appetite,
  • joint pain, stiffness, or swelling,
  • loss in sexual ability, desire, drive, or performance,
  • loss of balance,
  • low body temperature,
  • muscle aches,
  • muscle twitching or jerking,
  • overactive reflexes,
  • rhythmic movement of muscles,
  • runny nose,
  • seeing, hearing, or feeling things that are not there,
  • sensation of spinning,
  • shivering,
  • slurred speech,
  • sneezing,
  • oedema
  • trouble with speaking [1].

Incidence not known

  • bad, unusual or unpleasant (after) taste,
  • burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings,
  • chills,
  • constricted, pinpoint, or small pupils (black part of the eye),
  • deep or fast breathing with dizziness,
  • drowsiness,
  • dry mouth,
  • false or unusual sense of well-being,
  • fear or nervousness,
  • feeling of warmth,
  • hives or welts,
  • itching,
  • muscle stiffness or tightness,
  • numbness of the feet, hands, and around the mouth,
  • redness of the face, neck, arms, and occasionally, upper chest,
  • relaxed and calm feeling,
  • shaking,
  • uncontrolled eye movements,
  • upper stomach pain [1].

Major effects

Less common or rare

  • agitation,
  • bloody, black, or tarry stools,
  • blurred vision,
  • changes in behaviour,
  • chest pain or discomfort,
  • convulsions,
  • decreased urination,
  • dry mouth,
  • fast, pounding, slow or irregular heartbeat,
  • lightheadedness, dizziness, or fainting,
  • mood or mental changes,
  • rapid breathing,
  • severe stomach pain, cramping, or burning,
  • stiff neck,
  • sunken eyes,
  • thoughts of killing oneself,
  • trouble breathing,
  • unusual tiredness,
  • vomiting of material that looks like coffee grounds, severe and continuing,
  • wrinkled skin [1].

Incidence not known

  • cyanosis,
  • change in the ability to see colours, especially blue or yellow,
  • cold, clammy skin,
  • confusion,
  • cough,
  • decrease in frequency of urination or urine amount,
  • difficulty in passing urine (dribbling),
  • dizziness,
  • fast or weak pulse,
  • headache,
  • irregular, fast or slow, or shallow breathing,
  • loss of appetite,
  • noisy breathing,
  • painful urination,
  • sweating,
  • tightness in the chest,
  • insomnia [1].

Positive

  • euphoria,
  • pain relief [7].

Neutral

  • pupil constriction,
  • itching,
  • sedation Cite error: Invalid <ref> tag;

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Negative

  • drowsiness,
  • CNS depression,
  • dizziness,
  • nausea,
  • vomiting,
  • constipation,
  • sweating [7].

Side-effects needing medical attention

The following symptoms may be more serious and may require immediate medical attention -

  • rash or hives,
  • new and unexplained swelling,
  • trouble breathing,
  • difficulty swallowing,
  • chest pain,
  • extreme drowsiness,
  • fainting,
  • seizures [4].

Overdose

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 [6].

  • difficulty breathing,
  • slowed or stopped breathing,
  • excessive sleepiness,
  • dizziness,
  • fainting,
  • limp or weak muscles,
  • narrowing or widening of the pupils,
  • cold, clammy skin,
  • slow or stopped heartbeat,
  • cyanosis,
  • loss of consciousness or coma [8],
  • convulsions/seizures [1].

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 [9], [6].

  • Depressants (1,4-Butanediol, 2m2b, alcohol, barbiturates, benzodiazepines, GBL / GHB, 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 [10], [11]. This has also been reported with other drugs that increase extracellular serotonin like selective serotonin reuptake inhibitors [12], [6].

Dangerous

  • Ketamine - Both substances bring a risk of vomiting and unconsciousness. If the user falls unconscious while under the influence there is a severe risk of vomit aspiration if they are not placed in the recovery position.
  • MXE - This combination can potentiate the effects of the opioid.
  • DXM - CNS depression, difficult breathing, heart issues, hepatoxic, just very unsafe combination all around. Additionally if one takes dxm, their tolerance of opiates goes down slightly, thus causing additional synergistic effects.
  • Cocaine - Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
  • Alcohol - Both substances potentiate the ataxia and sedation caused by the other and can lead to unexpected loss of consciousness at high doses. Place affected patients in the recovery position to prevent vomit aspiration from excess. Memory blackouts are likely.
  • GBL / GHB - The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position
  • Tramadol - Concomitant use of tramadol increases the seizure risk in patients taking other opioids. These agents are often individually epileptogenic and may have additive effects on seizure threshold during coadministration. Central nervous system- and/or respiratory-depressant effects may be additively or synergistically present.
  • Benzodiazepines - Central nervous system and/or respiratory-depressant effects may be additively or synergistically present. The two substances potentiate each other strongly and unpredictably, very rapidly leading to unconsciousness. While unconscious, vomit aspiration is a risk if not placed in the recovery position. Blackouts/memory loss likely [5].

Caution

  • PCP - PCP can reduce opioid tolerance, increasing the risk of overdose.
  • Nitrous oxide - Both substances potentiate the ataxia and sedation caused by the other and can lead to unexpected loss of consciousness at high doses. While unconscious, vomit aspiration is a risk if not placed in the recovery position. Memory blackouts are likely.
  • Amphetamines - Stimulants increase respiration rate allowing a higher dose of opiates. If the stimulant wears off first then the opiate may overcome the patient and cause respiratory arrest.
  • MAOIs - Coadministration of monoamine oxidase inhibitors (MAOIs) with certain opioids has been associated with rare reports of severe and fatal adverse reactions. There appear to be two types of interaction, an excitatory and a depressive one. Symptoms of the excitatory reaction may include agitation, headache, diaphoresis, hyperpyrexia, flushing, shivering, myoclonus, rigidity, tremor, diarrhoea, hypertension, tachycardia, seizures, and coma. Death has occurred in some cases [5].

Withdrawal

  • restlessness,
  • increased sensations of pain,
  • inability to sleep,
  • nausea,
  • diarrhoea,
  • vomiting,
  • agitation,
  • muscle spasms,
  • cold flashes,
  • sweating,
  • increased blood pressure and heart rate [4].

Drug testing

How long does hydromorphone stay in the urine?

Hydromorphone can be detected in the urine for 3 - 4 days [8].

How long can hydromorphone be detected in blood?

A blood test can detect Hydromorphone for up to 24 hours [8].

How long can a saliva test detect hydromorphone?

A saliva test can detect Hydromorphone for up to 1 - 4 days [8].

How long can a hair test detect hydromorphone?

Hydromorphone can be detected with a hair follicle drug test for up to 90 days [8].

Statistics

  • Pain relievers are the most abused drugs after marijuana and hashish.
  • In 2014, 4.3 million people in the U.S. admitted using painkillers non-medically.
  • In a 2011 survey, 1 million people admitted to abusing hydromorphone in their lifetime [4].

History

Knoll introduced it to the mass market in 1926 under the brand name Dilaudid, indicating its derivation and degree of similarity to morphine (by way of laudanum). The brand name Dilaudid is more widely known than the generic term hydromorphone, and because of this, Dilaudid is often used generically to mean any form of hydromorphone [7].

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 1.7 Hydromorphone, 2017, https://www.drugs.com/mtm/hydromorphone.html
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 2.7 2.8 Hydromorphone, 2017, https://www.drugbank.ca/drugs/DB00327
  3. ↑ Hydromorphone, 2017, http://www.healthline.com/drugs/hydromorphone/oral-tablet
  4. ↑ 4.0 4.1 4.2 4.3 4.4 4.5 4.6 Patterson, E., Signs & Symptoms of Hydromorphone Abuse, 2017, http://drugabuse.com/library/signs-symptoms-of-hydromorphone-abuse/
  5. ↑ 5.00 5.01 5.02 5.03 5.04 5.05 5.06 5.07 5.08 5.09 5.10 5.11 5.12 5.13 Hydromorphone, 2017, http://drugs.tripsit.me/hydromorphone
  6. ↑ 6.00 6.01 6.02 6.03 6.04 6.05 6.06 6.07 6.08 6.09 6.10 6.11 6.12 6.13 Hydromorphone, 2017, https://psychonautwiki.org/wiki/Hydromorphone
  7. ↑ 7.0 7.1 7.2 7.3 Hydromorphone, 2017, https://wiki.tripsit.me/wiki/Hydromorphone
  8. ↑ 8.0 8.1 8.2 8.3 8.4 Hydromorphone, 2017, https://psychonautwiki.org/wiki/Hydromorphone
  9. ↑ Darke, S. and Zador, D., Fatal heroin 'overdose': a review, Addiction, 1996, 91, 12, 1765-1772, https://doi.org/10.1046/j.1360-0443.1996.911217652.x, http://www.ncbi.nlm.nih.gov/pubmed/8997759
  10. ↑ Mateo-Carrasco, H. and Muñoz-Aguilera, E. M. and García-Torrecillas, J. M. and Abu Al-Robb, H., Serotonin syndrome probably triggered by a morphine-phenelzine interaction, Pharmacotherapy, 2015, 35, 6, 102-105, https://doi.org/10.1002/phar.1581, https://www.ncbi.nlm.nih.gov/pubmed/25903219
  11. ↑ Gillman, P. K., Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity, British Journal of Anaesthesia, 2005, 95, 4, 434-441, https://doi.org/10.1093/bja/aei210, https://www.ncbi.nlm.nih.gov/pubmed/16051647
  12. ↑ Karunatilake, H. and Buckley, N. A., Serotonin syndrome induced by fluvoxamine and oxycodone, Annals of Pharmacotherapy, 2006, 40, 1, 155-157, https://doi.org/10.1345/aph.1E671, https://www.ncbi.nlm.nih.gov/pubmed/16368927

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