Hydrocodone
Hydrocodone is a semi-synthetic opioid derived from codeine. Hydrocodone is used orally as a narcotic analgesic and antitussive (cough medicine), often in combination with paracetamol (acetaminophen) or ibuprofen. Hydrocodone is prescribed predominantly within the United States; elsewhere it is rare. The International Narcotics Control Board reported 99% of the worldwide supply in 2007 was consumed in the United States.
The relative milligramme strength of hydrocodone to codeine is given as 6 fold, that is 5 mg has the effect of 30 mg of codeine; by way of the Roman numeral VI this is said to given rise to the trade name Vicodin.
History
Hydrocodone was first synthesized in Germany in 1920 by Carl Mannich and Helene Löwenheim. Hydrocodone is derived from codeine. As a semi-synthetic opioid, it is most often used orally as a narcotic analgesic and antitussive. Used mostly in combination with Acetaminophen (Vicodin) or Ibuprofen. If you have a drug with acetaminophen in it, we strongly recommend you cold water (CWE) extract the acetaminophen away. CWE methods can be found Here
Dosage
Hydrocodone is a prodrug, insufflated and intravenous dosing is dangerous.
The following refers to hydrocodone in the form of hydrocodone mixture with Acetaminophen/Ibuprofen.
| Light | 5-10mg |
| Common | 10-25mg |
| Strong | 25-40mg+ |
Recommended dosing interval is 4–6 hours.
Duration
| Onset | 10-30 minutes |
| Total duration | 4-6 hours |
Half-Life depends on a lot of factors such as weight, BMI, and metabolism, but average plasma half-life is 3.8 hours.
Effects
Positive
- Improvement of mood
- Reduction of pain
- Euphoria
Neutral
- Itching
- Light-headedness
- Sedation
- Changes in focus and attention
Negative
- Dizziness
- Constipation
- Nausea and vomiting
- When insufflated, burning in nose and sinuses
Chemistry and Pharmacology
As a narcotic, hydrocodone relieves pain by binding to opioid receptors in the CNS. It acts primarily on μ-opioid receptors, with about six times lesser affinity to δ-opioid receptors. In blood, 20–50% of hydrocodone is bound to protein.
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. However, in tests conducted on rhesus monkeys, the analgesic potency of hydrocodone was actually higher than morphine. Per os hydrocodone has a mean equivalent daily dosage (MEDD) factor of 0.4, meaning that 1 mg of hydrocodone is equivalent to 0.4 mg of intravenous morphine. However, because of morphine's low oral bioavailability, there is a 1:1 correspondence between orally administered morphine and orally administered hydrocodone.
Harm Reduction
Warning
Any dose of Hydrocodone may be fatal. Do not mix with other drugs or alcohol.
Excessive alcohol/grapefruit juice drinking while taking drug that contains APAP, can cause liver damage, other severe medical conditions, and even death.
Please consider CWE if your hydrocodone contains APAP, as APAP is harmful to your liver and doctors recommend no more than 4g.
Potentiators
The following products may react negatively with hydrocodone and may cause overdose if mixed together.
- Grapefruit Juice
- Diphenhydramine
Legal status
- Australia - In Australia, hydrocodone is a Schedule 8 (S8) or Controlled Drug.
- Austria - Hydrocodone is regulated 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 and nicomorphine being more commonly used for the same levels of pain and the former for coughing.
- Belgium - In Belgium, hydrocodone is no longer available for medical use.
- France - In France, hydrocodone (Vicodin) 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. The last remaining formula was banned in 1967.
- United Kingdom - 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. Various formulations of dihydrocodeine, a weaker opioid, are frequently used as an alternative for the aforementioned indications of hydrocodone use.
- United States - In the U.S., formulations containing more than 15 mg per dosage unit are considered Schedule II drugs, as would any formulation consisting of just hydrocodone alone. Those containing less than or equal to 15 mg per dosage unit in combination with acetaminophen or another non-controlled drug are called hydrocodone compounds and are considered Schedule III drugs. Hydrocodone is typically found in combination with other drugs such as acetaminophen, aspirin, ibuprofen and homatropine methylbromide. The purpose of the non-controlled drugs in combination is often twofold: 1) To provide increased analgesia via drug synergy. 2) To limit the intake of hydrocodone by causing unpleasant and often unsafe side effects at higher-than-prescribed doses. Hydrocodone is not commercially 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. Pure hydrocodone is a more strictly controlled Schedule II and sold by compounding pharmacies. The cough preparation Codiclear DH is the purest commercial US hydrocodone item, containing guaifenesin and small amounts of ethanol as active ingredients.
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.
*However as of February 23, 2013, all formulations of hydrocodone, regardless of whether they are paired with a combination product or not, have been bumped up to Schedule II.
Hydrocodone was until recently the active antitussive in more than 200 formulations of cough syrups and tablets sold in the United States. 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 legal status of drug formulations originally sold between 1938 and 1962—before FDA approval was required—was ambiguous. As a result of FDA enforcement action, by August 2010, 88% of the hydrocodone-containing medications had been removed from the market.
At the present time[when?], 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. The low sales volume and Schedule II status of Dilaudid cough syrup predictably leads to under-utilisation of the drug. 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.[citation needed] In the U.S., hydrocodone is always found in combination with other drugs such as paracetamol (also called acetaminophen), aspirin, an NSAID, ibuprofen, an antihistamine, an expectorant, or homatropine methylbromide due to compounding regulations. These combinations are considered C-III substances, prescriptions for which are generally valid for 6 months, including refills. The purpose of the non-controlled drugs in combination is often twofold:
1. To provide increased analgesia via drug synergy.
2. To limit the intake of hydrocodone by causing unpleasant and often unsafe side effects at higher-than-prescribed doses (see below).
The cough preparation Codiclear DH is the purest US hydrocodone item, containing guaifenesin and small amounts of ethanol as active ingredients.[citation needed] As of July 2010, the FDA was considering banning some hydrocodone and oxycodone fixed-combination proprietary prescription drugs—based on the paracetamol content and the widespread occurrence of liver problems. FDA action on this suggestion would ostensibly also affect codeine and dihydrocodeine products such as the Tylenol With Codeine and Panlor series of drugs.[citation needed] In 2010, it was the most prescribed drug in the USA, with 131.2 million prescriptions of hydrocodone (combined with paracetamol) being written
SOURCES
- "Controlled Substances Act". Wikipedia. Retrieved 8 February 2012.
- "Medical News: FDA Pulls Plug on 200-Plus Unapproved Cough Syrups With Hydrocodone—in Product Alert, Prescriptions from". MedPage Today. Retrieved 2010-08-22.
- DeNoon, Daniel J. (April 20, 2011). "The 10 Most Prescribed Drugs". eMedicineHealth. Retrieved 16 August 2012.