| | Methadone hydrochloride Basic information |
| | Methadone hydrochloride Chemical Properties |
| Melting point | 232-2340C | | density | 1.0103 (rough estimate) | | refractive index | 1.5790 (estimate) | | Fp | 11 °C | | storage temp. | 2-8°C | | solubility | Soluble in water, freely soluble in ethanol (96 per cent) | | form | powder | | color | white to off-white | | Water Solubility | 120 mg/mL | | Stability: | Stable. Incompatible with strong oxidizing agents. | | CAS DataBase Reference | 1095-90-5(CAS DataBase Reference) |
| | Methadone hydrochloride Usage And Synthesis |
| Description | (±)-Methadone (hydrochloride) (Item No. ISO00145) is an analytical reference material categorized as an opioid. (±)-Methadone has analgesic activity. Formulations containing (±)-methadone have been used in the treatment of opioid addiction. (±)-Methadone is regulated as a Schedule II compound in the United States. This product is intended for research and forensic applications. | | Chemical Properties | White Solid | | Originator | Dolophine ,Lilly,US,1947 | | Uses | Controlled substance (opiate). Methadone hydrochloride is used in treatment of opioid dependence. | | Definition | A synthetic narcotic. | | Manufacturing Process | Diphenylacetonitrile is condensed with 2-chloro-1-dimethylaminopropane to give 4-(dimethylamino)-2,2-diphenyl valeronitrile. It is then reacted with ethyl magnesium bromide and then hydrolyzed using HCl to give methadone hydrochloride. | | Brand name | Dolophine Hydrochloride (Roxane); Dolophine Hydrochloride (Xanodyne);
Methadose (Mallinckrodt); Westadone (Sandoz). | | Therapeutic Function | Narcotic analgesic | | Hazard | Toxic. Addictive narcotic. Use restricted. | | Clinical Use |
Treatment of opioid drug addiction
Analgesic for moderate to severe pain | | Drug interactions | Metabolised in the liver to the Potentially hazardous interactions with other drugs
Analgesics: possible opioid withdrawal with
buprenorphine and pentazocine.
Antibacterials: metabolism increased by rifampicin;
increased risk of ventricular arrhythmias with
delamanid and telithromycin.
Antidepressants: concentration possibly increased
by fluoxetine, fluvoxamine, paroxetine and sertraline;
possible CNS excitation or depression with MAOIs
and moclobemide - avoid; possibly increased
sedative effects with tricyclics; concentration possibly
reduced by St John's wort.
Antiepileptics: concentration reduced by
carbamazepine, phenobarbital and phenytoin.
Antifungals: concentration increased by fluconazole,
ketoconazole, voriconazole and possibly itraconazole
- may need to reduce methadone dose with
voriconazole, avoid with ketoconazole.
Antihistamines: increased sedative effects with
sedating antihistamines.
Antimalarials: increased risk of ventricular
arrhythmias with piperaquine with artenimol -
avoid.
Antipsychotics: enhanced hypotensive and sedative
effects; increased risk of ventricular arrhythmias with
antipsychotics that prolong the QT interval - avoid
with amisulpride.
Antivirals: methadone possibly increases
concentration of zidovudine; concentration
reduced by efavirenz, fosamprenavir and ritonavir;
concentration possibly reduced by abacavir,
nevirapine and rilpivirine; concentration possibly
affected by boceprevir; concentration of didanosine
possibly reduced; increased risk of ventricular
arrhythmias with saquinavir and telaprevir - avoid
with saquinavir and use with caution with telaprevir.
Atomoxetine: increased risk of ventricular
arrhythmias.
Cytotoxics: possible increased risk of ventricular
arrhythmias with bosutinib, ceritinib, panobinostat
and vandetanib.
Dopaminergics: avoid with selegiline.
Nalmefene: avoid concomitant use.
Sodium oxybate: enhanced effect of sodium oxybate
- avoid | | Metabolism | Metabolised in the liver to the major metabolite
2-ethylidine-1,5-dimethyl-3,3-diphenylpyrrolidine
and the minor metabolite 2-ethyl-3,3-diphenyl-5-
methylpyrrolidine, both of them inactive. Two other
metabolites have also been identified.
These metabolites are excreted in the faeces and urine
with unchanged methadone | | Purification Methods | The salt crystallises from EtOH, or EtOH/Et2O. |
| | Methadone hydrochloride Preparation Products And Raw materials |
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