Vicodin

Vicodin

Combination of
Hydrocodone	Opioid Analgesic
Paracetamol	Anilide Analgesic
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]	US FDA: Vicodin
Pregnancy category	C
Routes of administration	Oral
Legal status
Legal status	US: Schedule III
Identifiers
CAS Number	330988-71-1

File:Vicodin5mg.jpg

Brand name Vicodin-hydrocodone and acetaminophen (also known as paracetamol or abbreviated as APAP) 5-500 tablets (Abbott Laboratories).

Vicodin is a trademarked brand narcotic analgesic product containing hydrocodone and paracetamol (also known as acetaminophen). Vicodin is used to relieve moderate to severe pain. It is usually found in tablet form with either the names Vicodin, Vicodin ES, or Vicodin HP imprinted on one side. Analgesics with the same chemical composition and a similar physical appearance are found under many other trade names, including Anexsia, Anolor DH5, Bancap HC, Zydone, Dolacet, Lorcet, Lortab, and Norco. The hydrocodone/paracetamol drug formula is also available under generic brands. Hydrocodone also comes in a combination with ibuprofen, available under the trade name Vicoprofen.

Main Ingredients Vicodin is made as a mixture of hydrocodone and paracetamol. Paracetamol, which is also called acetaminophen, acts as an analgesic/antipyretic. Hydrocodone is a semi-synthetic opioid analgesic.

• Vicodin contains 500 mg paracetamol and 5 mg hydrocodone. Typical dosage is 1–2 tablets as needed, max 8 tablets/day.
• Vicodin ES contains 750 mg paracetamol and 7.5 mg hydrocodone. Typical dosage is 1 tablet as needed, max 5 tablets/day.
• Vicodin HP contains 660 mg paracetamol and 10 mg hydrocodone. Typical dosage is 1 tablet as needed, max 6 tablets/day.

Non-active ingredients included in each pill as well: colloidal silicon dioxide, starch, croscarmellose sodium, dibasic calcium phosphate, magnesium stearate, microcrystalline cellulose, povidone, and stearic acid.

Regulation and Scheduling

In the United States, Vicodin production is regulated in part by the Controlled Substances Act of 1970. This guarantees that all manufacturing, importing, possession, and distribution of drugs is to be overseen and regulated by the federal government.

In the U.S. Vicodin is a Schedule III drug. Pure codeine and hydrocodone are Schedule II drugs but when compounded with paracetamol or with an NSAID they can become a Schedule III drug. Schedule III drugs are classified by the U.S. government as potentially causing moderate or low physical dependence, or a high psychological dependence if misused.

Ban proposed in the U.S.

On June 30, 2009 a U.S. Food and Drug Administration (FDA) advisory panel voted by a narrow margin to advise the FDA to remove Vicodin and another painkiller, Percocet, from the market because of "a high likelihood of overdose from prescription narcotics and acetaminophen products". The panel cited concerns of liver damage from their acetaminophen component, which is also the main ingredient in commonly-used nonprescription drugs such as Tylenol. Each year, acetaminophen overdose is linked to about 400 deaths and 42,000 hospitalizations.

The FDA is not required to follow its advisory committee recommendations, but usually does.

Hydrocodone, the narcotic component of Vicodin, is still available in Canada as a single drug and marketed under the trade name Hycodan in syrup and tablet forms by Bristol-Myers-Squibb.

Manufacture

The principal constituent of Vicodin, hydrocodone, has the same basic structure as morphine but is metabolized by different enzymes. There are three variations of Vicodin, with different amounts of hydrocodone / paracetamol (acetaminophen) in each. Hydrocodone, like oxycodone, is an intermediate-strength analgesic which has similar effects as morphine, though it should be noted that hydrocodone is less potent than morphine. The tablets are made with less hydrocodone than paracetamol. The theory of using the mix comes from the idea that these drugs alleviate pain using different mechanisms and also that the adverse side effects of each separate drug are reduced by using reduced dosages of both drugs in order to get the same analgesic effect.

Both hydrocodone and acetaminophen are white crystalline powders, which are then manufactured into tablet form. Manufacturers of hydrocodone (generic or otherwise) include Abbott Laboratories (makers of trademark Vicodin), Amerisource Health Services Corp, Cardinal Health, Drx Pharmaceutical Consultants Inc, Eckerd Corp, Hospira Inc, Mallinckrodt Pharm. Quality Care, Pdrx Pharmaceuticals Inc, Physicians Total Care Inc, Rx Pak Div of Mckesson Corp, Sandhills Packaging Inc, and Watson Pharmaceuticals.

Pharmacodynamics

Besides the activity of hydrocodone and acetaminophen on their own, there is observed a factor of analgesia related to the two substances in tandem which is not altogether understood, but this independent synergy has been observed to be related to the inhibition of prostaglandins. The pharmacodynamics of a mixed drug such as Vicodin depends on the kinetics of the drugs that comprise it.

Hydrocodone: acts at mu opioid receptors. Hydrocodone is metabolized to hydromorphone by the activity of cytochrome P450 2D6 (cytochromes of the p450 family are enzymes involved in oxidation of various substances, including modification of foreign compounds). Cytochrome 3A4 forms the substrate norhydrocodone. Note that this conversion is only somewhat responsible for the effects of hydrocodone. Hydrocodone passes through the Blood Brain Barrier because of its modifications, the brain is typically where the analgesic effects are being carried out. Many of the side effects of this drug are caused by the fact that it so readily crosses the blood-brain barrier. The half-life of hydrocodone is approximately 3.8 hrs.

Paracetamol: the major active metabolites are sulphates and glucuronide conjugates. Its main mode of action is to inhibit the activity of the enzyme cyclooxygenase (COX). COX enzymes are necessary for the production of prostaglandins. Prostaglandins are a form of hormone (although rarely classified as such), which are indicated to be mediators of pain, fever and inflammation. The half-life of paracetamol may be measured either by salivary or plasma counts. Both measurements give a varying half-life between 1 and 4 hours. Peak levels are reached between 40–60 minutes after ingestion. It has been proposed that paracetamol aids in the reduction of pain by increasing seratonergic neurotransmissions. Paracetamol is a peripherally acting drug, and hence does not cross the BBB as readily as hydrocodone.

Indications

Vicodin, like other opioid analgesics, is used to manage pain. It is most commonly prescribed for relief of moderate to moderately severe pain of acute, chronic, or post-operative types. It can also be used to treat severe cough.

Pregnancy

This drug is classified under pregnancy category C. Although not enough research has been done to deem this drug safe for pregnant women, if the positive effects outweigh the possible negatives, then it can be taken. If taken in the time before delivery, it may give rise to respiratory depression in the baby. Mothers who use any opioids regularly during pregnancy run the risk of their babies being substance dependent and therefore going through withdrawal symptoms after birth. Withdrawal symptoms include: excessive crying, vomiting, irritability, tremors and fever. Nursing mothers should not use this drug as paracetamol is transferred through breast milk and it is unknown if hydrocodone is.

Side effects

Side effects for Vicodin are most commonly upset stomach, nausea, and altered mental status (e.g., dizziness, light headedness). Other more rare side effects include allergic reaction, seizures, clammy skin, hallucinations, severe weakness, dizziness, hyperventilation, unconsciousness, jaundice (yellowing of eyes or skin), unusual fatigue, bleeding, bruising, stomach pain, constipation, dry mouth, decreased appetite, muscle twitches, sweating, hot flashes, itching, tinnitus, hearing loss, decreased urination, and altered sex drive. Vicodin also has depressant effects on the central nervous system. However, some of the less mundane effects can be desirable effects that are sought after by some. Those effects include euphoria and drowsiness, as well as slowing of the pulse.

Unlike NSAIDs, paracetamol does not cause ulcers. However, paracetamol can cause liver damage and thus dosages should never exceed 4g a day; this is especially important and may be a smaller number of doses when using mixed drugs like Vicodin. It is imperative that users of this drug follow physician-prescribed dosages. Liver damage can manifest ranging from abdominal pain to outright liver failure, and can necessitate a liver transplant to avoid death.

Norco

Norco is a trademarked brand analgesic product marketed by Watson Pharmaceuticals. It contains a mixture of hydrocodone, a semi-synthetic opiate narcotic, and paracetamol (also known as acetaminophen, or more completely, para-acetylaminophenol), an aniline pain reliever and fever reducer. Norco is generally used for short-term relief of moderate to severe pain.

The principal constituent of Norco, hydrocodone, has the same basic structure as morphine, but it is less potent and is metabolized by different enzymes (though, due to morphine's poor oral bioavailability, PO hydrocodone and morphine have the same therapeutic potency). Like the better known analgesic Vicodin, which contains the same two active ingredients, Norco is manufactured in tablets containing either 5, 7.5, or 10 milligrams hydrocodone. Unlike Vicodin, however, all three Norco varieties contain 325 milligrams paracetamol, considerably less than Vicodin's 500 to 750 milligrams per tablet. Consequently, Norco can be safely taken in higher doses than Vicodin because its lower paracetamol content is less damaging to the liver.

Besides the individual activity of hydrocodone and acetaminophen, there is an observed factor of pain relief related to the two substances working in tandem. Though the pharmacodynamics of this interaction are not completely understood, the synergy has been observed to be related to the inhibition of prostaglandins.

Adverse side effects of Norco are most commonly upset stomach, nausea, and altered mental status (e.g., dizziness and/or light headedness). More rare adverse side effects include allergic reaction, seizures, clammy skin, hallucinations, severe weakness, hyperventilation, unconsciousness, jaundice, unusual fatigue, bleeding, bruising, constipation, dry mouth, decreased appetite, muscle twitches, sweating, hot flashes, itching, tinnitus, hearing loss, decreased urination, and altered sex drive. Norco also has a depressant effect on the central nervous system, making it dangerous to use along with other CNS depressants such as alcohol, benzodiazepines, and barbituates.

Other more desirable side effects, such as euphoria and increased sense of well-being, have led to the use of Norco as a recreational drug. Tolerance to hydrocodone may develop rapidly, especially if it is misused. This can lead users to seek increasing doses of Norco, often resulting in physical dependence and/or addiction. Withdrawal from Norco can then cause acute insomnia, night sweats, tremors, and agitation.

Legal status

United States

To qualify for treatment as a Schedule III medication in the United States, hydrocodone must be combined with a non-narcotic ingredient in a recognized therapeutic amount. There are four dosage forms recognized by the U.S. authorities:

• per 100 ml (i.e. a liquid), which must have no more than 300 mg of (dissolved) hydrocodone in addition to the therapeutic amount of a non-narcotic ingredient
• per dosage unit (i.e. a solid, pill or capsule) which must have no more than 15 mg of hydrocodone in addition to the therapeutic amount of a non-narcotic ingredient

Compounded dosages seen on the market include:

• per 15 ml of syrup:
  • 15 mg/80 mg hydrocodone/acetaminophen (paracetamol)
  • 30 mg/80 mg hydrocodone/acetaminophen
  • 45 mg/80 mg hydrocodone/acetaminophen
• per capsule:
  •   5 mg/ 80 mg hydrocodone/acetaminophen
  • 10 mg/ 80 mg hydrocodone/acetaminophen
  • 15 mg/ 80 mg hydrocodone/acetaminophen
  • 10 mg/100 mg hydrocodone/acetaminophen
  • 15 mg/100 mg hydrocodone/acetaminophen
  • 10 mg/200 mg hydrocodone/acetaminophen
  • 15 mg/200 mg hydrocodone/acetaminophen
  •   5 mg/325 mg hydrocodone/acetaminophen
  •   5 mg/500 mg hydrocodone/acetaminophen
  • 10 mg/200 mg hydrocodone/ibuprofen
  • 15 mg/200 mg hydrocodone/ibuprofen

References in popular media

A portion of the popular American television medical drama, House, M.D.'s plot centers on the central character's habitual use of Vicodin to manage pain stemming from an infarction in his quadriceps muscle incurred some years earlier.

Vicodin is referenced in multiple songs by rapper Eminem such as "Kill You", "Under the Influence", "Deja Vu", "Old Time's Sake", and "Underground". He also featured a vicodin pill on the cd of his debut album The Slim Shady LP. The rapper has admitted to an addiction to the painkiller (along with other substances), the hiatus in rapping that it caused, and the subsequent rehabilitation required to return to his career.

Rock band Queens of the Stone Age also referenced the drug in their song "Feel Good Hit of the Summer", on their second studio album Rated R. Vicodin appeared alongside other iconic drugs in the mantra-like verse 'nicotine, valium, vicodin, marijuana, ecstasy and alcohol...'.

See also

• Hydrocodone

External links

• Norco information from Drugs.com
• Norco Website
• Vicodin U.S. DEA Drug Schedule
• Vicodin U.S. Federal Regulations
• U.S. National Library of Medicine: Drug Information Portal - Vicodin

cs:Vicodin sr:Викодин