Hydromorphone drugs

A study in the April 5, 2000 issue of the Journal of the American Medical Association found that hydromorphone use for medical indications increased by 19% from 1990 to 1996. This increase coincided with an decrease in the number of hydromorphone drug abuse mentions during this period. The decrease in hydromorphone drug abuse (15%) suggests a low risk of addiction associated with the medical use of hydromorphone in the treatment of severe pain. 

Morphine, when extracted from raw opium and treated chemically, yields the semisynthetic narcotics hydromorphone, oxymorphone, oxycodone, and heroin. Heroin is an illegal narcotic in the United States and is not used in medicine. Synthetic narcotics are those man-made analgesics with properties and actions similar to the natural opioids. Examples of synthetic narcotic analgesics are methadone, levorphanol, remifen-tanil, and meperidine Additional narcotics are listed in the Summary Drug Table Narcotic Analgesics. 

Opioids maybe administered in a variety of routes including oral (tablet and liquid), sublingual, rectal, transdermal, transmucosal, intravenous, subcutaneous, and intraspinal. While the oral and transdermal routes are most common, the method of administration is based on patient needs (severity of pain) and characteristics (swallowing difficulty and preference). Oral opioids have an onset of effect of 45 minutes, so intravenous or subcutaneous administration maybe preferred if more rapid relief is desired. Intramuscular injections are not recommended because of pain at the injection site and wide fluctuations in drug absorption and peak plasma concentrations achieved. More invasive routes of administration such as PCA and intraspinal (epidural and intrathecal) are primarily used postoperatively, but may also be used in refractory chronic pain situations. PCA delivers a self-administered dose via an infusion pump with a preprogrammed dose, minimum dosing interval, and maximum hourly dose. Morphine, fentanyl, and hydromorphone are commonly administered via PCA pumps by the intravenous route, but less frequently by the subcutaneous or epidural route. 

Hydromorphone (I) and hydrocodone (II) belong to the morphine group of drugs and are used invariably in combination with other ingredients in a number of proprietory antitussive and analgesic antipyretic mixtures. However, interest in the pharmacokinetics of hydromorphone and hydrocodone in human subjects required an adequate assay for drug levels in plasma. 

RIA for hydromorphone and hydrocodone are fairly sensitive in the nanogram per millilitre range but essentially require the preparation of a specific antibody. The laid-out RIA method is quite capable of estimating the above drugs within a range of 2.5-20 ng ml 1 using standard 100 pi plasma sample only. 

Hydromorphone Hydromorphone, 4,5-epoxy-3-hydroxy-N-methyl-6-oxomorphinane (3.1.22), is a compound related to morphine that differs in the absence of a double bond between C7-C8 and the presence of a keto group instead of a hydroxyl group on Cg. The drug is synthesized by the isomerization of morphine in the presence of a palladium or platinum catalyst [11,12]. The other way is by oxidation of dihydroporphine [13,14]. 

Hydromorphone is more soluble than morphine and approximately eight times more active upon parenteral administration. High solubility permits a lower volume of injected fluid, which is important if multiple injections are needed. It begins to work faster than morphine, but lasts for a shorter amount of time. It has a high sedative effect and a lessened capability of causing euphoria. Hydromorphone is used the same way as morphine. Side effects are analogous. Synonyms for this drug are dilaudid and others. 

Oxymorphone Oxymorphone, 4,5-epoxy-3,14-dihydroxy-N-methyl-6-oxyomorphinane (3.1.26), is chemically similar to hydromorphone. It differs from hydromorphone in that it contains a hydroxyl group on C13. The drug is synthesized from thebaine (3.1.23), which during oxidation with hydrogen peroxide in formic acid changes into 14-hydroxycodeinone... 

Hydrocodone (Hycodan), oxycodone (Roxicodone), dihydrocodeine, hydromorphone (Dilaudid), and oxy-morphone (Numorphan) are derivatives of codeine and morphine. All are indicated for the relief of mild to severe pain or for their antipyretic effects they are often used in combination with nonopioid analgesics. The drugs vary in potency, but their pharmacological effects do not differ significantly from those of codeine or morphine. 

The patient who uses hydromorphone repeatedly may develop a tolerance to the drug s analgesic effect as well as physical dependence. 

Heroin is a Schedule I drug morphine, codeine, fentanyl, hydrocodone, hydromorphone, and oxycodone are Schedule II drugs codeine plus aspirin or acetaminophen is Schedule III propoxyphene is Schedule IV and codeine sold over the counter is Schedule V. 

Among the compounds that fall within this class are hydrocodone (e.g., Vicodin), oxycodone (e.g., OxyContin—an oral, controlled-release form of the drug), morphine, fentanyl, codeine, and related medications. Morphine and fentanyl are often used to alleviate severe pain, while codeine is used for milder pain. Other examples of opioids prescribed to relieve pain include propoxyphene (Darvon) hydromorphone (Dilaudid) and meperidine (Demerol), which is used less often because of its side effects. In addition to their effective pain-relieving properties, some of these medications can be used to relieve severe diarrhea (for example, Lomotil, also known as diphenoxylate) or severe coughs (codeine). 

Depending on the country where the drug is manufactured, a number of different time-release preparations are available. Palladone , a controlled-release preparation consisting of hydromorphone HC1 pellets, was withdrawn from the U.S. market in 2005. When taken with alcohol the pellets rapidly released their contents leading to dangerously elevated peak plasma concentrations.60 Interaction with ethanol and dose dumping is not the only concern. Any CNS depressant may enhance the depressant effects of hydromorphone. 

Preston, K.L. and Bigelow, G.E., Drug discrimination assessment of agonist-antagonist opioids in humans a three-choice saline-hydromorphone-butorphanol procedure, J. Pharmacol. Exp. Ther., 271, 48, 1994. 

FIGURE 14.3 The single-carrier or single-ion scenario illustrated for hydromorphone, lidocaine, and quinine. Transport numbers (mean + SD, n> 3) are essentially constant for these three drugs despite a significant increase in donor drug concentration. (Data taken from Padmanabhan, R.V. et al., J. Control. Release, 11 (3), 123, 1990 Marro, D. et ah, Pharm. Res., 18 (12), 1701, 2001.)... 

Dextromethorphan is not classified as a controlled substance under the Controlled Substances Act (CSA) of 1970. The CSA was created as a means to regulate the distribution and use of prescription drugs that are highly addictive, such as codeine, oxycodone, morphine, and hydromorphone. 

Hydromorphone is a semi-synthetic prescription drug that has similar pain-relieving properties to that of morphine and codeine. It is classified as an opioid or narcotic analgesic. It is an effective treatment for moderate-to-severe pain and is sometimes used in patients with a non-productive cough. It is used to treat several types of pain, including headache, cancer pain, and back pain. 

Most of the illegal opiates, especially heroin, enter the United States through the Mexican border. According to some law enforcement officials, heroin use may be supplanted in future years by increased use of prescription narcotics, provided that they continue to be available. As a result, the distribution and use of prescription narcotics is closely monitored by state and federal law enforcement agencies. Illicit hydromorphone abuse has not reached the same epidemic levels as Oxy-Contin but remains a problem and a concern for drug enforcement authorities. 

Hydromorphone is available through injections, tablets, oral solution, and suppositories. The usual route of administration is by way of swallowing tablets. For patients who have difficulty swallowing tablets, a flavored oral solution is available. This liquid form of the drug can be poured into a medicine dropper for measurement by the patient or a nurse. The liquid can also be added to soft foods to make it easier for the patient to ingest. Some of these liquid formulations may contain alcohol. 

Hydromorphone is also used to treat chronic pain syndromes. These pain syndromes can develop from a variety of injuries and can affect muscles, joints, and other parts of the body. In such cases, patients often take the drug on an as needed basis. Hydromorphone is frequently prescribed to treat pain associated with moder-ate-to-severe osteoarthritis. Narcotic analgesics are generally prescribed for these patients when other painkilling drugs are not effective. 

Hydromorphone is highly addictive. Its use needs to be carefully monitored by the treating physician. Longterm use of the drug can lead to physical and psychological dependency. Mood can also be affected by hydromorphone and other narcotic analgesics. Infrequently, hallucinations and disorientation can develop. Insomnia develops in a minority of cases. 

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