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LAAM
drug data and news
LAAM drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | LAAM | ||
| Brand Names/Synonyms | Dea No. 9648; LAAM; Levacetilmetadol [Inn-Spanish]; Levacetylmethadol; Levacetylmethadolum [Inn-Latin]; Levo-Alphacetylmethadol; Levo-Methadyl Acetate; Levomethadyl; Levomethadyl Acetate; Levomethadyl Acetate [Usan]; Methadyl Acetate; Nor-Laam; Orlaam | ||
| Indication | LAAM is indicated for the treatment and management of opiate dependence. It is sometimes used to treat severe pain in terminal patients. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | LAAM is a synthetic synthetic opioid analgesic with multiple actions quantitatively similar to those as morphine, the most prominent of which involve the central nervous system and organs composed of smooth muscle. However, LAAM is more active and more toxic than morphine. The principal actions of therapeutic value are analgesia and sedation and detoxification or temporary maintenance in narcotic addiction. The LAAM abstinence syndrome, although qualitatively similar to that of morphine, differs in that the onset is slower, the course is more prolonged, and the symptoms are less severe. | ||
| Mechanism Of Action | Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. LAAM effectively opens calcium-dependent inwardly rectifying potassium channels (OP1 receptor agonist), resulting in hyperpolarization and reduced neuronal excitability. | ||
| LAAM News (When available) |
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| Dosage Forms | SOLUTION | ||
| Drug_Category | Narcotics; Analgesics, Opioid | ||
| Absorption | LAAM is rapidly absorbed from an oral solution. | ||
| Interactions | Not Available | ||
| Toxicity | Signs of overdose include apnea, circulatory collapse, pulmonary edema, cardiac arrest, and death. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | (6-dimethylamino-4,4-diphenyl-heptan-3-yl) acetate | ||
| Chemical Formula | C23H31NO2 | ||
| Molecular Weight | 353.498 g/mol | ||
| Smiles String | CCC(C(CC(C)N(C)C)(C1=CC=CC=C1)C2=CC=CC=C2)OC(=O)C | ||
| Melting Point | Not Available | ||
| Water Solubility | >15 mg/mL | ||
| State | Solid | ||
| LogP/Hphobicity | 6.139 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | LAAM undergoes extensive first-pass metabolism to the active demethylated metabolite nor-LAAM, which is further demethylated to a second active metabolite, dinor-LAAM. These metabolites are more potent than the parent drug. | ||
| Half Life | 2.6 days | ||
| Protein Binding [%] | ~ 80% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/LAAM.html http://www.rxlist.com/cgi/generic2/levomethadyl.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00745 | ||
| CAS Registry Number | 1477-40-3 | ||
| KEGG Compound ID | C08012 | ||
| PubChem ID | SID:158449 | ||
| PharmGKB ID | PA450215 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
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