Hydrocodone , sold under brand names such as Vicodin and Norco among many others, are semisynthetic opioids derived from codeine, one of the opioid alkaloids found in opium poppy. It is a narcotic analgesic used orally to relieve moderate to severe pain, but is also commonly used in liquid form as an antitussive/cough suppressant.
Hydrocodone is an opioid, and acts as a selective agonist of the -opioid receptor, the primary biological target of endogen neuropeptide? -endorphin.
Hydrocodone is prescribed primarily in the United States, with the International Narcotics Control Agency reporting that 99% of world supplies in 2007 were consumed in the United States. Some common traces for hydrocodone are M365, M366, M367.
Video Hydrocodone
Medical use
Hydrocodone is used to treat moderate to severe pain and as an antitussive to treat cough. In one study comparing the potential of hydrocodone with oxycodone, it was found that it takes 50% more hydrocodones to achieve the same degree of miosis (pupil contraction). The researchers interpret this to mean that oxycodone is about 50% stronger than hydrocodone.
However, in the study of emergency patients with fractures, it was found that an equal number of drugs were given about the same level of pain relief, suggesting that there was little practical difference between them when used for that purpose. Some references suggest that the analgesic action of hydrocosision begins in 20-30 minutes and lasts about 4-8 hours. The manufacturer's information says the onset of action is about 10-30 minutes and the duration is about 4-6 hours. Recommended dosing interval is 4-6 hours.
Available form
Hydrocodone is available in various formulations for oral administration:
- Hydrocodone immediate release with paracetamol (acetaminophen) (Vicodin, Lortab, Lorcet, Maxidone, Norco, Zydone)
- Hydrocodone immediate release with ibuprofen (Vicoprofen, Ibudone, Reprexain)
- Fast release hydrocodon with aspirin (Alor 5/500, Azdone, Damason-P, Lortab ASA, Panasal 5/500)
- Hydrocodone released controlled (ER Hysingla, Zohydro ER)
Hydrocodone is not available in parenteral or other non-oral forms.
Maps Hydrocodone
Side effects
Common side effects of hydrocodone are nausea, vomiting, constipation, drowsiness, dizziness, dizziness, anxiety, abnormal or sad mood, dry throat, difficulty urinating, rash, itching, and narrowing of pupils. Serious side effects include slow or irregular breathing and chest tightness.
Some cases of progressive bilateral hearing loss unresponsive to steroid therapy have been described as rare adverse reactions to abuse of hydrocodone/paracetamol. This adverse effect has been considered by some people because of the ototoxicity of hydrocodone. Other researchers claim that paracetamol is the primary agent responsible for ototoxicity.
Hydrocodone is in the US Food and Drug Administration (FDA) pregnancy category. No human controlled and adequate studies have been conducted. Newborns from mothers who take opioid drugs regularly before birth will be physically dependent. The baby may also show respiratory depression if the dose of opioids is high. An epidemiological study shows that opioid treatment during early pregnancy results in an increased risk of multiple birth defects.
Symptoms of hydrocodone overdose include dilated or dilated pupils; slow, shallow, or stop breathing; slow or stop the heartbeat; cold, sweaty, or blue skin; excessive sleepiness; lost consciousness; seizures; or death.
Hydrocodone can form habits, causing physical and psychological dependence. Responsibility for abuse is similar to morphine and less than oxycodone.
Interactions
Patients who consume alcohol, other opioids, anticholinergic antihistamines, anti-psychotics, anti-anxiety agents, or central nervous system (CNS) depressants together with hydrocodone may exhibit CNS additive depression. Hydrocodone can interact with serotonergic drugs.
Pharmacology
Pharmacodynamics
Hydrocodone is a highly selective agonist of the -opioid receptor (MOR). This is the main biological target of endogenous opioid neuropeptide? -endorphin. Hydrocodine has a low affinity for the -opioid receptor (DOR) and the -opioid receptor (KOR), where it is the same agonist.
Research shows that hydrocodone is stronger than codeine but only one tenth of potent morphine in binding receptors and is reported to be only 59% as efficacious as morphine in analgesic properties. However, in tests performed on rhesus monkeys, the potential for hydrolysis analgesics is actually higher than morphine. The oral hydrobeon has a mean daily equivalent dose (MEDD) factor of 0.4, which means that 1 mg of hydrocarbons is equivalent to 0.4 mg of intravenous morphine. However, due to the low oral bioavailability of morphine, there is a 1: 1 correspondence between orally administered morphine and orally administered hydrocodone. The relative milligram strength of the hydrocodone for codeine is given as 6-fold, ie 5 mg having a 30 mg codeine effect; by Roman means this figure VI is said to have caused the Vicodin trade name.
Pharmacokinetics
Absorption
Hydrocodone is only available as a pharmaceutical oral drug. It is well absorbed, but the oral bioavailability of the hydrolysis is only about 25%. The onset of action of hydrocodone through this route is 10 to 20 minutes, with the peak effect (T max ) occurring at 30 to 60 minutes, and having a duration of 4 to 8 hours.
Distribution
The hydrocodone distribution volume is 3.3 to 4.7 L/kg. The plasma protein binding to hydrocodone is 20 to 50%.
Metabolism
At heart, hydrocodone is converted into several metabolites, including norhydrocodone, hydromorphone, 6? -hydrocodol (dihydrocodeine), and 6? -hydrocodol. 6? - and 6? -hydromorphol is also formed, and conjugated hydrolyzone metabolites (via glucuronidation). Hydrocodone has an average half-life terminal of 3.8 hours (range 3.3-4.4 hours). Cytochrome P450 CYP2D6 liver enzyme converts hydrocortone into hydromorphone, a more potent opioid (5 fold higher affinity binding to MOR). However, broad and poor cytochrome 450 CYP2D6 metabolites have physiologic and subjective responses similar to hydrocodones, and quinidine CYP2D6 inhibitors do not alter the response of broad metabolism, suggesting that inhibition of CYP2D6 metabolism from hydrocodones has no practical importance. The ultra-fast CYP2D6 metabolism (1-2% of the population) may have an increased response to hydrocarbons; However, the metabolism of hydrocodone in this population has not been studied.
Norhidrokodon, a major metabolite of hydrocodone, is primarily formed by CYP3A4 catalyzed oxidation. Unlike the hydromorphone, it is described as inactive. However, norhydrocodone is actually a MOR agonist with the same potential as hydrocodone, but has been found to produce only minimal analgesia when given peripherally to animals (probably due to poor blood-brain barrier and thus central nervous system penetration). Inhibition of CYP3A4 in a child who, in addition, is a poor CYP2D6 producer, results in a fatal hydrocodon overdose. About 40% of hydrolysine metabolism is associated with a non-cytochrome P450-catalyst reaction.
Elimination
Hydrocodone is excreted in the urine, especially in the form of conjugation.
Chemistry
Detection in body fluids
The concentration of hydrocarbons is measured in blood, plasma, and urine to look for evidence of abuse, to confirm the diagnosis of poisoning, and to assist in the investigation of death. Many commercial opiate screening tests react indiscriminately with hydrocodones, other opiates, and their metabolites, but chromatographic techniques can easily distinguish hydrocodons uniquely. Blood and plasma hydrocodone concentrations typically fall within the range of 5-30 Âμg/L among people taking therapeutic drugs, 100-200 Âμg/L among recreational users, and 100-1,600 Âμg/L in acute cases, a fatal overdose. Co-administration of drugs with food or alcohol can greatly increase the resulting plasma hydrocodone concentration which is then achieved.
History
Hydrocodone was first synthesized in Germany in 1920 by Carl Mannich and Helene LÃÆ'¶wenheim. It was approved by the Food and Drug Administration on March 23, 1943 for sale in the United States and approved by Health Canada for sale in Canada under the brand name Hycodan.
Hydrocodone was first marketed by Knoll as Dicodid, beginning in February 1924 in Germany. This name is analogous to other products introduced by the company or marketed: Dilaudid (hydromorphone, 1926), Dinarkon (oxycodone, 1917), Dihydrin (dihydrocodeine, 1911), and Dimorphan (dihydromorphine). Paramorfan is a trade name of dihydromorphine from other manufacturers, such as Paracodin, for dihydrocodeine.
The name Dicodid was registered in the United States and appeared without a monograph until the end of 1978 in Reference Desk Doctor; Dicodid may have been marketed to some extent in North America in the 1920s and early 1930s. The drug is pure hydrocodone in small tablets 5 and 10 mg, physically similar to Dilaudid tablets. This is no longer manufactured by Knoll in Germany, nor is it generically available. Hydrocodone is never common in Europe as in North America - dihydrocodeine is used for spectrum indications. Germany is the number two consumer of hydrocodone until the manufacture of the drug is stopped there. Today, the world outside the United States accounts for less than 1% of annual consumption. It's listed as Suchtgift under the German BetÃÆ'¤ubungsmittelgesetz and is set up like morphine. It became available in the Schengen Area of ​​the European Union on 1 January 2002 under Title 76 of the Schengen Agreement.
Society and culture
Formulation
Combination products
Most hydrocodones are formulated in combination with a second analgesic, such as paracetamol (acetaminophen) or ibuprofen. Examples of hydrolysis combinations include Norco, Vicodin, Lortab, Vicoprofen, and Riboxen.
Zohydro ER
In 2014, the FDA approves a hydrolysed formulation called Zohydro ER made by Zogenix Pharmaceuticals. The approval of Zohydro ER is controversial, due to concerns over potential substance abuse. The FDA approves Zohydro ER for the objection of its own review panel, which elects 12 to 2 on approval. The panel states that if approved, Zohydro ER is likely to be "abused, possibly to a greater extent than the currently available hydrocodone combination product". Thirty US states asked the FDA not to approve Zohydro ER in capsule form because of its potential and ease that could be misused, by being destroyed and then snorted or injected. Zohydro ER was banned in Massachusetts before a federal judge ruled that the country's ban was preceded by previous federal approval.
Legal status
United States
The US government imposes strict prescribing rules for hydrocodons by 2014, changing drugs from Schedule III to Schedule II. In 2011, hydrocodone products were involved in about 100,000 emergency department-related visits in the United States, more than doubling in 2004.
See also
- Equianalgesic
References
External links
- Hydrocodone at the US National Drug Library: Drug Information Portal
- "DEA Schedule of Controlled Substance: Hydroquomb Combination Product Scheduling From Schedule III to Schedule II". Federal List. Oct 6, 2014.
Source of the article : Wikipedia
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