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Hydrocodone or dihydrocodeinone is a semi-synthetic opioid derived from either of two naturally occurring opiates: codeine[1] and thebaine[2].
Hydrocodone and compounds containing it are marketed, in varying forms, under a number of trademarks, including Vicodin, Hydrococet, Symtan, Anexsia, Biocodone, Damason-P, Dicodid, Hycodan (or generically Hydromet), Hycomine, Hycet, Lorcet, Lortab, Norco, Novahistex, Hydrovo, Duodin, Kolikodol, Orthoxycol, Panacet, Zydone, Mercodinone, Synkonin, Norgan, Xodol and Hydrokon.
As a narcotic, hydrocodone relieves pain by binding to opioid receptors in the brain and spinal cord. Studies have shown hydrocodone is stronger than codeine but only one-tenth as potent as morphine at binding to receptors and reported to be only 59% as potent as morphine in analgesic properties.
Hydrocodone can be habit-forming, which leads to physical and psychological dependence, but the potential for addiction varies from individual to individual depending on unique biological differences. As with many other opioids, it is quite possible to reduce the amount of hydrocodone needed to stop a certain level of pain by having the patient take the hydrocodone along with one of the medications with analgesic-sparing properties, also known as potentiators.
Hydrocodone also interacts relatively well with most adjuvant and atypical analgesics used for severe and neuropathic pain such as first-generation anti-depressants, anticholinergics, anticonvulsants, centrally acting stimulants, NMDA antagonists, etc.
When sold commercially in the United States, hydrocodone is always combined with another medication.
Mixing hydrocodone with alcohol, cocaine, amphetamines, methylphenidate, benzodiazapines, barbiturates, and a number of other medications can have severe adverse reactions including but not limited to heart failure, heart attack, respiratory distress, pulmonary failure, liver or kidney failure, jaundice, amnesia, seizures, blackouts, and coma.[citation needed] Also, hydrocodone can cause false indications on blood and urinalysis testing for morphine, codeine, hydromorphone and cocaine depending on usage and dosing. There are serious health risks posed by concurrently consuming alcohol with hydrocodone compounds. The most common medication compounded with hydrocodone is paracetamol (acetaminophen), which is metabolized solely by the liver.
Common side effects include dizziness, itching, lightheadedness, nausea, sweating, drowsiness, constipation, vomiting, and euphoria.
Some of the effects of hydrocodone come from the fact that a fraction of it is changed to hydromorphone in the liver, as is the case with all codeine-based analgesics (codeine into morphine, dihydrocodeine into dihydromorphine, nicocodeine into nicomorphine etc.).
Hydrocodone, along with most other opioids, may also severely decrease testosterone levels in men and may cause menstrual irregularities in women.
Hydrocodone presents much of the same side-effects as other opioids including euphoria, sedation and somnolence.
Hydrocodone may be quantitated in blood, plasma or urine to monitor for misuse, confirm a diagnosis of poisoning or assist in a medicolegal death investigation. In Germany, hydrocodone is available as single-active-ingredient tablets as Dicodid (by analogy to the original manufacturer's other products Dilaudid and Dinarkon and others) available in 5- and 10-mg strengths.
Hydrocodone is regulated in the same fashion as in Germany 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 and nicomorphine being more commonly used for the same levels of pain and the former for coughing. In the Netherlands, hydrocodone is not available for medical use and is classified as a List 1 drug under the Opium Law. In the UK, hydrocodone is not available for medical use and is listed as a Class A drug under the Misuse of Drugs Act 1971. Under the Controlled Substances Act (CSA) hydrocodone is listed as both a Schedule II and Schedule III substance depending on the formulation.
Schedule II lists hydrocodone in pure form and any formulations of combination products containing more than 15 mg hydrocodone per dosage unit. Schedule III lists hydrocodone in formulations of combination products containing up to 15 mg hydrocodone per dosage unit. Hydrocodone was until recently the active antitussive in more than 200 formulations of cough syrups and tablets sold in the United States. At the present time, doctors, pharmacists, and codeine-sensitive or allergic patients or sensitive to the amounts of histamine released by its metabolites must choose among rapidly dwindling supplies of the Hycodan-Codiclear-Hydromet type syrups, Tussionex—an extended-release suspension similar to the European products Codipertussin (codeine hydrochloride), Paracodin suspension (dihydrocodeine hydroiodide), Tusscodin (nicocodeine hydrochloride) and others—and a handful of weak dihydrocodeine syrups.
As of July 2010, the FDA is considering banning some hydrocodone and oxycodone fixed-combination proprietary prescription drugs—based on the paracetamol content and the widespread occurrence of liver problems.
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It is an orally active narcotic analgesic (pain reliever) and antitussive (cough suppressant). Sales and production of this drug have increased significantly in recent years, as have diversion and illicit use. The most common, one of the most effective with hydrocodone, and safest is hydroxyzine (often marketed under the brand name Vistaril). Hydrocodone can usually be successfully used with duloxetine (Cymbalta) for neuropathic pain, especially that from diabetic neuropathy, provided that the patient has normal relative and absolute levels of Cytochrome P450-related liver enzymes. Those combined with paracetamol (acetaminophen) are known by various trademark names, such as Vicodin and Lortab. Another argument for combining hydrocodone with paracetemol (acetaminophen) is that it limits the potential for misuse.
These patients are regarded to be poor or intermediate metabolizers of opioid medications and would need higher concentrations of opioids to experience the same therapeutic benefits as a person without the polymorphism.
Generally this effect is only present when doses are taken for long periods of time, and the effect ceases after cessation of use. Therefore the risk of fatal overdose due to hepatotoxicity can occur with significantly lower levels of paracetamol when mixed with ethanol. Vomiting in some patients is so severe that hospitalization is required, although this can be due to alcohol consumption before taking the medication.[citation needed] Some less common side effects are allergic reaction, blood disorders, changes in mood, racing heartbeat, mental fogginess, anxiety, lethargy, difficulty urinating, spasm of the ureter, irregular or depressed respiration, and rash.
The percentage can vary based on both other medications taken and inherited metabolic quirks involving the Cytochrome P450 metabolic pathways—some cannot process it at all, whereas a smaller percentage can get even more strength from it than usual. Short-term use of opioids will usually result in a decrease in testosterone with a subsequent rebound post-cessation.
Hydrocodone is one of the most common recreational prescription drugs in America, along with oxycodone. Many commercial opiate screening tests cross-react appreciably with hydrocodone and its metabolites, but chromatographic techniques can easily distinguish hydrocodone from other opiates. Prescriptions are more commonly given for use as a cough suppressant (antitussive) rather than for pain relief (analgesic). Hydrocodone is listed under the Betaubungsmittelgesetz as a Suchtgift in the same category as morphine.
Various formulations of dihydrocodeine, a weaker opioid, are frequently used as an alternative for the aforementioned indications of hydrocodone use. In late 2006, the FDA began forcing the recall of many of these formulations due to reports of deaths in infants and children under the age of six. The low sales volume and Schedule II status of Dilaudid cough syrup predictably leads to under-utilisation of the drug. FDA action on this suggestion would ostensibly also affect codeine, dihydrocodeine, and propoxyphene products such as the Tylenol With Codeine and Panlor series of drugs and Darvocet.
Baselt, Disposition of Toxic Drugs and Chemicals in Man, 9th edition, Biomedical Publications, Seal Beach, CA, 2011, pp. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist. This material is provided for educational purposes only and is not intended for medical advice, diagnosis or treatment. It is commonly available in tablet, capsule, and syrup form, and is often compounded with other, generally less effective non-opioid compounds such as paracetamol (also known as acetaminophen) or ibuprofen, often added both to discourage recreational use[citation needed] (as paracetamol can cause potentially fatal liver toxicity at high doses), and to provide a possible synergy of analgesic effects between hydrocodone and the non-opioid compounds present. The trade name Dicodid was chosen because hydrocodone is the codeine analogue of hydromorphone (Dilaudid and the naming scheme extended to related drugs like Dihydrin (dihydrocodeine) and Dinarkon (oxycodone). Also the mixture can potentially cause serious damage to the liver, kidneys, and stomach wall.
These factors can also cause hydrocodone and related drugs to have a threshold effect, cause significant lengthening or shortening of the duration of effects in the absence of tolerance, and increase or decrease the de facto conversion ratio between hydrocodone and other drugs like morphine, hydromorphone, and synthetics like levorphanol and methadone. Recreational hydrocodone use is particularly prevalent among teenagers and young adults because of the drug's widespread availability.


The presence of paracetamol in hydrocodone-containing products allegedly deters many users, at least in theory, from taking excessive amounts.
The legal status of drug formulations originally sold between 1938 and 1962—before FDA approval was required—was ambiguous. There are several conflicting views concerning the US availability of cough preparations containing ethylmorphine (also called dionine or codethyline)—Feco Syrup and its equivalents were first marketed circa 1895 and still in common use in the 1940s and 1950s, and the main ingredient is treated like codeine under the Controlled Substances Act of 1970.
An extended-release hydrocodone-only product is apparently close to final approval for marketing in the United States, and single-ingredient tablets of oxycodone and codeine are currently marketed. The particular niche in which hydrocodone is most commonly used is as an intermediate centrally acting analgesic.
The trade name Vicodin refers to hydrocodone being six times stronger than codeine by mouth, as in the Roman numeral VIcitation needed. It may interact with monoamine oxidase inhibitors, as well as other drugs that cause drowsiness. Those containing less than or equal to 15 mg per dosage unit in combination with paracetamol or another non-controlled drug are called hydrocodone compounds and are considered Schedule III drugs. Especially in the case of carisoprodol, it is imperative that the titration and addition of the potentiator be done under strict supervision of a physician. In a study on cancer survivors using opioids for chronic pain relief, 90% of the subjects had hypogonadal levels of testosterone. However, some users will bypass this danger by using cold water extraction to extract and dispose of a portion of the paracetamol, taking advantage of the water-soluble element of the drug. The purpose of the non-controlled drugs in combination is often twofold: 1) To provide increased analgesia via drug synergy. Mixtures of these drugs with other drugs such as Vicoprofen (hydrocodone & ibuprofen), Combunox (ibuprofen and oxycodone), Synalgos DC (aspirin and dihydrocodeine), and the Empirin With Codeine series are also currently available. Abrupt discontinuation of hydrocodone (Vicodin, Vicodin ES, and Norco) may result in withdrawal symptoms.
Hydrocodone is typically found in combination with other drugs such as paracetamol, aspirin, ibuprofen and homatropine methylbromide. This may occur due to both a negative feedback at both the hypothalamus-pituitary and at the gonadal (testicular) level. 2) To limit the intake of hydrocodone by causing unpleasant and often unsafe side effects at higher-than-prescribed doses (See Below). Animal reproduction studies have shown an adverse effect on the fetus, and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks. As stated above, hydrocodone is not available in pure form in the United States due to a separate regulation, and is always sold with an NSAID, paracetamol, antihistamine, expectorant, or homatropine. In addition, a newborn of a mother taking the medication may exhibit breathing problems or withdrawal symptoms. 2) To limit the intake of hydrocodone by causing unpleasant and often unsafe side effects at higher-than-prescribed doses. Patients using opioid therapy should be screened for such endocrinological problems periodically through blood tests and inquiry of symptoms, which include loss of libido, erectile dysfunction, anxiety, fatigue, loss of muscle mass, and infertility. The cough preparation Codiclear DH is the purest US hydrocodone item, containing guaifenesin and small amounts of ethanol as active ingredients. Hydrocodone is not available in pure form in the United States due to a separate regulation, and is always sold with an NSAID, paracetamol, antihistamine, expectorant, or homatropine. In Germany and elsewhere, hydrocodone is available as single-active-ingredient tablets as Dicodid (by analogy to the original manufacturer's other products Dilaudid and Dinarkon and others) available in 5- and 10-mg strengths.



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