Hydrocodone

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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.

Summary sheet: Hydrocodone
Hydrocodone
Hydrocodone.svg
Chemical Nomenclature
Common names Vicodin (with paracetamol), Zohydro ER (extended-release)
Substitutive name Hydrocodone
Systematic name 4,5α-epoxy-3-methoxy-17-methylmorphinan-6-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 3 - 5 mg
Light 5 - 10 mg
Common 10 - 25 mg
Strong 25 - 40 mg
Heavy 40 mg +
Duration
Total 4 - 8 hours
Onset 10 - 60 minutes









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.

Hydrocodone (commonly sold as Vicodin when combined with paracetamol) is a semi-synthetic opioid morphinan synthesized from codeine, one of the opioid alkaloids found in the opium poppy. It is a narcotic analgesic used orally as a cough suppressant, but also commonly taken orally for relief of moderate to severe pain.[2] Those who take hydrocodone for recreational purposes report a sense of relaxation and euphoria, especially at higher doses.

Hydrocodone is prescribed predominantly within the United States, with the International Narcotics Control Board reporting that 99% of the worldwide supply in 2007 was consumed in the United States.[3]

Like many opioids, such as dextropropoxyphene, hydrocodone is often combined with acetaminophen (paracetamol) to enhance analgesia and deter abuse. Acetaminophen overdoses and long-term use, often due to recreational use, can cause serious or fatal liver damage. Currently, the only brand of hydrocodone in the United States that does not have acetaminophen is Zohydro ER which comes in doses of up to 50mg.

Chemistry

Hydrocodone, or 3-methyl-dihydromorphinone, is an opioid of the morphinan class. Hydrocodone and other molecules of this class contain a polycyclic core of three benzene rings fused in a zig-zag pattern called a 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.

Hydrocodone, along with other morphinans, contains an ether bridge between two of its rings, connecting R4 and R5 through an oxygen group. It contains a carbonyl group bound at R6 and a methyl group located on the nitrogen atom at R17. The carbon-oxygen double bond of the carbonyl saturates the benzene ring it is bonded with, thus hydrocodone lacks the double bond on that ring found in codeine.

Hydrocodone also shares the 3-methoxy substitution found in codeine; the two differ only from their R6 substituents. Hydrocodone is analogous to the other morphinans including dihydrocodeine, heroin, ethylmorphine, codeine, and oxycodone.

Pharmacology

The euphoria, anxiety suppression and pain relief effects appear to stem from the way in which opioids mimic endogenous endorphins. Endorphins are responsible for analgesia (reducing pain), causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or excitement. This mimicking of natural endorphins results in the drug's effects. It acts primarily on μ-opioid receptors, with about six times lesser affinity to δ-opioid receptors.

In the liver, hydrocodone is transformed into several metabolites. It has a serum half-life that averages 3.8 hours.[4] The hepatic cytochrome P450 enzyme CYP2D6 converts it into hydromorphone, a more potent opioid.

Subjective effects

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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Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

Potentiation

Taking hydrocodone with grapefruit juice is believed to enhance its psychoactive effects. It is hypothesized that the CYP3A4 inhibitors in grapefruit juice may interfere with the metabolism of hydrocodone,[5] although there has been no research into this issue.

Toxicity and harm potential

Hydrocodone has not been shown to be toxic and is physically benign at reasonable dosages. As with all opioids, long-term effects can vary but can include diminished libido, apathy and memory loss. Some people may also have an allergic reaction to hydrocodone, such as the swelling of skin and rashes. It is potentially fatal at heavy dosages.

Like most opioids, unadulterated hydrocodone at appropriate dosages does not cause many long-term complications other than dependence and constipation. Outside of the extremely powerful addiction and physical dependence, the harmful or toxic aspects of opioid usage are exclusively associated with not taking the necessary precautions in regards to its administration, overdosing and using impure products.

Heavy dosages of hydrocodone can result in respiratory depression, leading onto 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.

Hydrocodone 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). In case of overdose, it is advised to administer a dose of naloxone intravenously or intramuscularly to reverse the effects of opioid agonism.

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 hydrocodone can be considered moderately 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 hydrocodone 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. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). Hydrocodone presents cross-tolerance with all opioids, meaning that after the consumption of hydrocodone all opioids will have a reduced effect.

The risk of fatal opioid overdoses rise sharply after a period of cessation and relapse, largely because of reduced tolerance.[6] 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.[7]

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

  • 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 hydrocodone, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of hydrocodone, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of hydrocodone 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 hydrocodone.

Legal status

  • Australia: Hydrocodone is a Schedule 8 (S8) or controlled drug.[citation needed]
  • Austria: Hydrocodone is regulated in Austria in the same fashion as in Germany (see below) under the Austrian Suchtmittelgesetz (SMG). Since 2002, it has been available in the form of German products and those produced elsewhere in the European Union under Article 76 of the Schengen Treaty.[citation needed]
  • Belgium: Hydrocodone is no longer available for medical use.[citation needed]
  • Canada: Hydrocodone is a Schedule I controlled substance and is available by prescription only. Hydrocodone is prescribed alone as well as in proprietary combinations, typically with an NSAID or paracetamol.[citation needed]
  • France: Hydrocodone is no longer available for medical use. Hydrocodone is a prohibited narcotic.[citation needed]
  • Germany: Hydrocodone is no longer available for medical use. Hydrocodone is listed under the Betäubungsmittelgesetz as a Suchtgift in the same category as morphine.[citation needed]
  • Luxembourg: - Hydrocodone is available by prescription under the name Biocodone. Prescriptions are more commonly given for use as a cough suppressant (antitussive) rather than for pain relief (analgesic).[citation needed]
  • The Netherlands: Hydrocodone is not available for medical use and is classified as a List 1 drug under the Opium Law.[citation needed]
  • Sweden: Hydrocodone is no longer available for medical use in Sweden. The last remaining formula was deregistered in 1967.[citation needed]
  • United Kingdom: Hydrocodone is not available for medical use and is listed as a Class A drug under the Misuse of Drugs Act 1971. Various formulations of dihydrocodeine, a weaker opioid, are frequently used as an alternative.[citation needed]
  • United States: As of October 6, 2014, all hydrocodone products are now designated as Schedule II controlled substances.[8] They are no longer Schedule III narcotics. Prescriptions can no longer have refills and a handwritten paper script must be obtained for each fill.[citation needed]

See also

External links

References

  1. Risks of Combining Depressants (Tripsit) | https://tripsit.me/combining-depressants/
  2. Karch, Steven B. (2008). Pharmacokinetics and pharmacodynamics of abused drugs. Boca Raton: CRC Press. pp. 55–56. ISBN 1-4200-5458-9.
  3. International Narcotics Control Board Report 2008. United Nations Pubns. 2009. p. 20. ISBN 9211482321. | https://books.google.co.uk/books?id=7iDhYnsYaocC&pg=PA20&hl=en#v=onepage&q&f=false
  4. Davis, Mellar P. (2005). "Hydrocodone". Opioids for cancer pain. Oxford UK: Oxford University Press. pp. 59–68. ISBN 0-19-852943-0. | https://books.google.co.uk/books?id=BK0WduGnx2kC&pg=PA59&lpg=PA59&dq=potency+of+hydrocodone&hl=en
  5. Prescription drug abuse: insight into the epidemic (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/20686478
  6. Why Heroin Relapse Often Ends In Death - Lauren F Friedman (Business Insider) | http://www.businessinsider.com.au/philip-seymour-hoffman-overdose-2014-2
  7. 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
  8. https://www.dea.gov/druginfo/ds.shtml