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Dolophine

Methadone is a synthetic opioid analgesic synthesized in 1937 by German scientists Max Bockmühl and Gustav Ehrhart at IG Farben (Hoechst-Am-Main) who were searching for an analgesic that would be easier to use during surgery and also have low addiction potential. Methadone is a Schedule II drug under the Single Convention on Narcotic Drugs. more...

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On September 11, 1941 Bockmühl and Ehrhart filed an application for a patent for a synthetic substance they called Hoechst 10820 or polamidon and whose structure had no relation to morphine or the opioid alkaloids (Bockmühl and Ehrhart, 1949). Although chemically unlike morphine or heroin, methadone also acts on the opioid receptors and thus produces many of the same effects. Chemically, methadone is the simplest of the opioids.

Methadone was introduced into the United States in 1947 by Eli Lilly and Company as an analgesic (They gave it the trade name Dolophine® which is now registered to Roxane Laboratories). Since then, it has been best known for its use in treating narcotic addiction, though it is also used in managing chronic pain due to its long duration of action and very low cost. In late 2004, the cost of a one month supply of methadone is 20 USD, as compared to an equivalent analgesic amount of Demerol at 120 USD. The old name Dolophine comes from the German Dolphium. The name derives from the Latin "dolor" (pain).

Methadone (as Dolophine) was first manufactured in the USA by Mallinckrodt pharmaceuticals, a St. Louis-based subsidiary of the Tyco International corporation. Mallinckrodt held the patent up until the early 1990s. Today a number of pharmaceutical companies produce and distribute methadone. However, the major producer remains Mallinckrodt. Mallinckrodt sells bulk methadone to most of the producers of generic preparations and also distributes its own brand name product in the form of tablets, dispersable tablets and oral concentrate under the name "Methadose" in the United States. Generally, one will only hear "dolophine" used by older addicts who used the product in the 1960's and 1970's. Medical professionals who believe that dolophine is the generic name for methadone, when actually it is the reverse, may also use the old brand name.

Methadone has a slow metabolism and very high lipid solubility making it longer lasting than morphine-based drugs. Methadone has a typical half life of 24-48 hours, permitting the administration only once a day in heroin detoxification and maintenance programs. The most common mode of delivery at a Methadone clinic is in an oral solution. Methadone is almost as effective when administered orally as by injection. Just like heroin, tolerance and dependence frequently develop. Current research in this area shows methadone has a unique affinity for the NMDA brain receptor. Some researchers propose that NMDA (N-methyl-D-aspartic acid) may regulate psychic dependence and tolerance by exhibiting opioid antagonist-like activity. Withdrawal symptoms are generally less acutely severe than those of morphine and heroin at equivalent doses, but are significantly more prolonged. Considered generally effective in management of heroin addiction and harm reduction (reduction of HIV rates, etc...). At proper dosing, it reduces the appetite for heroin. However, some heroin addicts feel that it is actually harder to quit methadone than heroin itself. Treatment at a methadone maintenance clinic is intended to be for an indefinite duration, as the treatment is not curative.

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Methadone Hydrochloride 0.33-mg/mL Oral Solution
From International Journal of Pharmaceutical Compounding, 9/1/05

METHOD OF PREPARATION

1. Calculate the required quantity of each ingredient for the total amount to be prepared.

2. Accurately weigh and/or measure each ingredient.

3. Dissolve the methadone hydrochloride in the purified water and add sufficient cherry syrup to volume and mix well.

4. Package and label.

PACKAGING

Package in tight, light-resistant containers.1

LABELING

Keep out of reach of children. Use only as directed.

STABILITY

A beyond-use date of up to 6 months would be appropriate for this preparation.1

USE

Methadone hydrochloride in oral liquid dosage forms has been used in the treatment of moderate to severe pain in patients unable to swallow oral solids (tablets, capsules, etc.) The concentration of methadone hydrochloride can be changed easily to accommodate the needs of the patient.

QUALITY CONTROL

Quality-control assessment can include weight/volume, pH, specific gravity, active-drug assay, color, clarity, rheological properties/pourability, physical observation, and physical stability (discoloration, foreign materials, gas formation, mold growth).2

DISCUSSION

Dolophine Hydrochloride Syrup (Methadone Hydrochloride Syrup) was commercially available at a concentration of 10 mg/30 mL until 2002. Using this basic formulation, the concentration can be changed easily to meet the needs of the patient, especially the hospice patient.

Methadone hydrochloride (C^sub 21^H^sub 27^NO.HCl, MW 345.91) occurs as colorless crystals or as a white, crystalline, odorless powder. It is soluble in water, freely soluble in alcohol and in chloroform, and practically insoluble in glycerin. It has a pH in the range of 4.5 to 6.5 in a 1% solution in water. The powder should be stored in a tight, light-resistant container.1 Methadone Hydrochloride Oral Solution USP contains not less than 90.0% and not more than 110.0% of the labeled amount of methadone hydrochloride. It should be stored in a tight, light-resistant container at controlled room temperature. The official product has a pH between 1.0 and 4.0.1

Cherry syrup contains cherry juice (475 mL), sucrose (800 g), and alcohol (20 mL) in sufficient purified water to make 1000 mL. It should be packaged in tight, light-resistant containers and not exposed to excessive heat. It contains between 1.0% and 2.0% alcohol. The pH of cherry syrup is generally about 3. There are several different types of cherry syrup on the market, many of which are used for flavoring foods and beverages. They should be used for this formulation only if they contain the necessary preservatives and have the necessary pH. If necessary, citric acid can be added to adjust the pH to the compendial standard of a pH between 1.0 and 4.0.1 Numerous other vehicles with a pH between 1 and 4 could be used.

Purified water is used to describe potable water from a public water supply that is suitable for drinking and is the beginning point of the official waters. It is a clear, colorless, odorless, and tasteless liquid. Purified water is water that is obtained by distillation, ion exchange, reverse osmosis, or some other suitable process. Water has a specific gravity of 0.9971 at room temperature, a melting point of 0°C and a boiling point of 100°C. It is miscible with most polar solvents and is chemically stable in all physical states (ice, liquid, and steam).1

References

1. United States Pharmacopeial Convention, Inc. United States Pharmacopeia IB-National Formulary 23. Rockville, MD: US Pharmacopeial Convention, Inc.; 2004: 1233-1235, 2345-2349, 2457-2460, 2899, 2988.

2. Allen LV Jr. Standard operating procedure for quality assessment of oral and topical liquids. IJPC 1999; 3(2): 146-147.

3. Ellison A, Nash RA, Wilkin MJ. Water. In: Rowe RC, Sheskey PJ, Weller PJ, eds. Handbook of Pharmaceutical Excipients. 4th ed. Washington, DC: American Pharmaceutical Association; 2003: 672-676.

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