Orlaam
Orlaam - General Information
A narcotic analgesic with a long onset and duration of action. It is used mainly in the treatment of narcotic dependence. [PubChem]
Pharmacology of Orlaam
Levomethadyl acetate (also known as 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, levomethadyl acetate 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 levomethadyl acetate 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.
Orlaam for patients
Orlaam Interactions
Orlaam Contraindications
ORLAAM is contraindicated in patients with known or suspected QT prolongation (QTc interval greater than 430 [male] or 450 [female] ms). This would include patients with congenital long QT syndrome, or conditions which may lead to QT prolongation such as: 1) clinically significant bradycardia (less than 50 bpm), 2) any clinically significant cardiac disease, 3) treatment with Class I and Class III anti-arrhythmics, 4) treatment with monoamine oxidase inhibitors (MAOI's), 5) concomitant treatment with other drug products known to prolong the QT interval, and 6) electrolyte imbalance, in particular hypokalemia and hypomagnesemia. ORLAAM is contraindicated in patients with known hypersensitivity to LAAM.
Additional information about Orlaam
Orlaam Indication: For the treatment and management of opiate dependence. It is sometimes used to treat severe pain in terminal patients.
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. Levomethadyl acetate effectively opens calcium-dependent inwardly rectifying potassium channels (OP1 receptor agonist), resulting in hyperpolarization and reduced neuronal excitability.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Levomethadyl Acetate
Synonyms: 1-alpha-acetylmethadol; LAAM; Levacetilmetadol [Inn-Spanish]; Levacetylmethadol; Levacetylmethadolum [Inn-Latin]; Levo-Alphacetylmethadol; Levo-Methadyl Acetate; Levomethadyl; Nor-LAAM
Drug Category: Narcotics; Analgesics, Opioid
Drug Type: Small Molecule; Approved
Other Brand Names containing Levomethadyl Acetate: Orlaam;
Absorption: Levomethadyl acetate is rapidly absorbed from an oral solution.
Toxicity (Overdose): Signs of overdose include apnea, circulatory collapse, pulmonary edema, cardiac arrest, and death.
Protein Binding: Approximately 80%
Biotransformation: Levomethadyl acetate undergoes extensive first-pass metabolism to the active demethylated metabolite nor-levomethadyl acetate, which is further demethylated to a second active metabolite, dinor-levomethadyl acetate. These metabolites are more potent than the parent drug.
Half Life: 2.6 days
Dosage Forms of Orlaam: Solution, concentrate Oral
Chemical IUPAC Name: [(3S,6S)-6-dimethylamino-4,4-di(phenyl)heptan-3-yl] acetate
Chemical Formula: C23H31NO2
Levomethadyl Acetate on Wikipedia: https://en.wikipedia.org/wiki/Levomethadyl_Acetate
Organisms Affected: Humans and other mammals
