Ambenonium drug data and news

Ambenonium 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.

Generic name Ambenonium
Brand Names/Synonyms Ambenonium; Ambenonium Base; Ambenonium Kation; Ambenonium [Usan]; Ambenonum; CHEMBANK2927; Mytelase
Indication Ambenonium is used to treat muscle weakness due to muscle disease (myasthenia gravis).
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Description Not Available
Pharmacology Ambenonium, similar to pyridostigmine and neostigmine, is used for the treatment of muscle weakness and fatigue in people with myasthenia gravis. It is postulated to exert its therapeutic effect by enhancing cholinergic function by inhibiting the hydrolysis of acetylcholine by acetylcholinesterase. Increased levels of acetylcholine has peripheral effects, as acetylcholine is also used in the brain, where it tends to cause excitatory actions. The glands that receive impulses from the parasympathetic part of the autonomic nervous system are also stimulated in the same way. This is why an increase in acetylcholine causes a decreased heart rate and increased production of saliva. Ambenonium is used less commonly than neostigmine or pyridostigmine but may be preferred in patients hypersensitive to the bromide ion. Ambenonium produces fewer muscarinic side effects than neostigmine, but more than pyridostigmine.
Mechanism Of Action Ambenonium exerts its actions against myasthenia gravis by competitive, reversible inhibition of acetylcholinesterase. The disease myasthenia gravis occurs when the body inappropriately produces antibodies against acetylcholine receptors, and thus inhibits proper acetylcholine signal transmission (when acetylcholine binds to acetylcholine receptors of striated muscle fibers, it stimulates those fibers to contract). Ambenonium reversibly binds acetylcholinesterase, and as acetylcholinesterase is responsible for the hydrolysis of acetylcholine, this inhibition increases levels of acetylcholine. In turn this facilitates transmission of impulses across the myoneural junction and effectively treats the disease.
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Dosage Forms TABLET (10 mg)
Drug_Category Antiarrhythmic Agents; Antimyasthenics; ATC:N07AA30
Absorption Oral - poorly absorbed from the gastrointestinal tract.
Interactions Interactions for Ambenonium:
Interactions can occur with the following medications: demecarium (Humorsol), echothiophate (Phospholine Iodide), isoflurophate (Floropryl), malathion (using these medicines with antimyasthenics may result in serious side effects), guanadrel (Hylorel), guanethidine (Ismelin), mecamylamine (Inversine), procainamide (Pronestyl), and trimethaphan (the effects of these medicines may interfere with the actions of the antimyasthenics).
Toxicity Mouse, oral LD50: 150±44 mg/kg. Symptoms of overdose include muscle twitching, weakness and paralysis of voluntary muscles including the tongue, shoulders, neck and arms, blood pressure increase (with or without a slowing of heart rate), a sensation of internal trembling, severe anxiety, and panic. Death may occur rapidly if untreated.
Organisms Affected Humans and other mammals
Chemical IUPAC Name (2-chlorophenyl)methyl-[2-[2-[(2-chlorophenyl)methyl-diethyl-ammonio]ethylcarbamoylformyl]aminoethyl]-diethyl-ammonium
Chemical Formula C28H42Cl2N4O2
Molecular Weight 537.564 g/mol
Smiles String CC[N+](CC)(CCNC(=O)C(=O)NCC[N+](CC)(CC)CC1=CC=CC=C1Cl)CC2=CC=CC=C2Cl
Melting Point 196-199 °C
Water Solubility Soluble
State Solid
LogP/Hphobicity Not Available
Isoelectric Point Not Available
Biotransformation Plasma and hepatic
Half Life Not Available
Protein Binding [%] Not Available
RxList Link Not Available>RXlist
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Drug Reference http://www.drugs.com/cons/Ambenonium.html
Drug Type Approved Drug
Accession No APRD00771
CAS Registry Number 7648-98-8
KEGG Compound ID C07773
PubChem ID SID:9975
PharmGKB ID PA448362
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available

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