Hydrocodone

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Hydrocodone
Chemical Nomenclature
Common names	Vicodin (with paracetamol), Zohydro ER (extended-release), Norco
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 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.
Interactions
Stimulants
MAOIs
Nitrous
PCP
Alcohol
Benzodiazepines
DXM
GHB
GBL
Ketamine
MXE
Tramadol
Grapefruit

Hydrocodone is a semi-synthetic opioid synthesized from codeine, one of the opioid alkaloids found in the opium poppy. It is a narcotic analgesic used orally as an antitussive/cough suppressant, but also commonly taken orally for relief of moderate to severe pain.[1]

Many users of hydrocodone report a sense of satisfaction (euphoria), especially at higher doses. A number of users also report a warm or pleasant numbing sensation throughout the body, one of the best-known effects of narcotics.[29][medical citation needed] A simultaneous warming of the stomach and rest of the body with the possible sensation of pleasant cooling in the lungs is sometimes also reported, as with opium and hydromorphone [30]

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.[2]

Chemistry

This chemistry section is incomplete. You can help by adding to it.

Pharmacology

As a narcotic, hydrocodone relieves pain by binding to opioid receptors in the brain. 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.[17] The hepatic cytochrome P450 enzyme CYP2D6 converts it into hydromorphone, a more potent opioid.

The euphoria, anxiety suppression and pain relief effects appear to stem from the way in which opioids appear to 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.

Taking hydrocodone with grapefruit juice is believed to enhance its narcotic effect. It is hypothesized that the CYP3A4 inhibitors in grapefruit juice may interfere with the metabolism of hydrocodone,[32] although there has been no research into this issue. Additionally, many medications are either substrates (competing for metabolism and exhausting available enzymes) or direct inhibitors of CYP3A4. Inhibition of another enzyme, CYP2D6, would also increase the duration of hydrocodone's elevated concentration in the blood, leading to exaggerated effects. Complete inhibition of both enzymes would theoretically inhibit 60% of the factors involved in hydrocodone metabolism. Inducing CYP2D6 with, for example, glutethimide or promethazine, also increases the hydrocodone-hydromorphone conversion in the liver, and promethazine is an opioid potentiator used with everything from codeine to alphaprodine in clinical settings, which may increase effects but also muddy the picture vis à vis serum levels at any given time.

Subjective effects

This subjective effects section is a stub. As such, it is still in progress and may contain incomplete or wrong information. You can help by expanding or correcting it.

Toxicity and harm potential

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

Tolerance and addiction potential

Tolerance to many of the effects of hydrocodone develops with prolonged use, including therapeutic effects. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance.

As with other opiate-based pain killers, chronic use of hydrocodone can be considered as highly 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.

Legal issues

• Australia - In Australia, hydrocodone is a Schedule 8 (S8) or Controlled Drug.
• Austria - Hydrocodone is regulated in Austria in the same fashion as in Germany (see below) under the Austrian Suchtmittelgesetz; 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—prior to this, no Austrian companies produced hydrocodone products, with dihydrocodeine, nicomorphine, and nicocodeine being more commonly used instead.
• Belgium - In Belgium, hydrocodone is no longer available for medical use.
• Canada - In 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.
• France - In France, hydrocodone is no longer available for medical use. Hydrocodone is a prohibited narcotic.
• Germany - In Germany, hydrocodone is no longer available for medical use. Hydrocodone is listed under the Betäubungsmittelgesetz as a Suchtgift in the same category as morphine.
• Luxembourg - In 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).
• The Netherlands - In the Netherlands, hydrocodone is not available for medical use and is classified as a List 1 drug under the Opium Law.
• Sweden - Hydrocodone is no longer available for medical use in Sweden. The last remaining formula was deregistered in 1967.
• United Kingdom - In the 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 for the aforementioned indications of hydrocodone use.
• United States - As of 6 October 2014 all hydrocodone products are listed as Schedule II Controlled substance. They will no longer be a Schedule III narcotic. Prescriptions can no longer have refills and a handwritten paper script must be obtained for each fill. In some states a Schedule II substance can be electronically prescribed if the doctor has the proper technology and an electronic signature license.

References

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