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European Journal of Drug Metabolism and... 1991Serum levels of ambenonium chloride (AC) were monitored in 4 myasthenic patients. This determination revealed important intraindividual variations (up to 10-fold) over a...
Serum levels of ambenonium chloride (AC) were monitored in 4 myasthenic patients. This determination revealed important intraindividual variations (up to 10-fold) over a period of 24 h. Levels varied considerably between different patients (maximum serum concentration of ambenonium chloride ranged from 0.129 to 0.812 micrograms/ml) and no correlation between the daily dose and the AUC was found. These characteristic properties of ambenonium chloride could explain the erratic pattern of bioavailability observed as well as the difficulty in controlling the disease in some patients.
Topics: Administration, Oral; Adult; Aged; Aged, 80 and over; Ambenonium Chloride; Biological Availability; Female; Humans; Male; Myasthenia Gravis
PubMed: 1823874
DOI: 10.1007/BF03189975 -
A.M.A. Archives of Neurology and... Jan 1956
Topics: Ambenonium Chloride; Chlorides; Ions; Myasthenia Gravis; Parasympathomimetics
PubMed: 13275166
DOI: 10.1001/archneurpsyc.1956.02330190107013 -
Journal of Chromatography Nov 1989An effective and selective procedure for the extraction of ambenonium chloride (AMBC) from serum using a weak cation-exchange extraction cartridge has been developed....
Sensitive determination of ambenonium chloride in serum from patients with myasthenia gravis using ion-exchange resin extraction and reversed-phase ion-pair chromatography.
An effective and selective procedure for the extraction of ambenonium chloride (AMBC) from serum using a weak cation-exchange extraction cartridge has been developed. The solid-phase extraction procedure permitted the extraction of AMBC from serum without adhesion to materials such as the containers. A 200-microliter volume of the eluate could be directly injected on to a reversed-phase ion-pair high-performance liquid chromatographic column. The recovery was in the range 97-100%. The limit of detection for AMBC was 0.5 ng/ml in serum (signal-to-noise ratio = 3). The method was used to determine the serum concentration of AMBC in patients with myasthenia gravis. The method would be useful for monitoring AMBC in serum in order to study its pharmacokinetic behaviour in patients under oral administration therapy.
Topics: Adult; Ambenonium Chloride; Chemical Phenomena; Chemistry; Chromatography, Ion Exchange; Female; Humans; Male; Middle Aged; Myasthenia Gravis; Piperidines; Spectrophotometry, Ultraviolet
PubMed: 2613842
DOI: 10.1016/s0378-4347(00)82587-6 -
The New England Journal of Medicine Dec 1964
Topics: Ambenonium Chloride; Atropine; Drug Therapy; Gastrointestinal Motility; Geriatrics; Humans; Mecamylamine; Paralysis; Parasympathetic Nervous System; Pharmacology; Toxicology; Urinary Bladder Diseases; Urination Disorders
PubMed: 14234274
DOI: 10.1056/NEJM196412102712410 -
Acta Neurologica Scandinavica 1966
Comparative Study
Topics: Adolescent; Adult; Aged; Ambenonium Chloride; Anabolic Agents; Child; Child, Preschool; Ephedrine; Female; Humans; Hyperthyroidism; Infant; Infant, Newborn; Male; Middle Aged; Myasthenia Gravis; Neostigmine; Oculomotor Muscles; Pregnancy; Pyridostigmine Bromide; Respiratory Tract Infections; Thymectomy; Thymus Gland
PubMed: 5957970
DOI: 10.1111/j.1600-0404.1966.tb04768.x -
Journal of the Neurological Sciences Jul 1981Ambenonium chloride was administered orally in a dosage of 6 mg/kg/day to rats for 14-360 days. Motor end-plate fine structure and junctional AChR were quantitatively...
Ambenonium chloride was administered orally in a dosage of 6 mg/kg/day to rats for 14-360 days. Motor end-plate fine structure and junctional AChR were quantitatively analyzed and red (soleus) and white (EDL) muscle fibers. In treated animals, degeneration and simplification of postsynaptic folds and widening of synaptic clefts were often observed in soleus end-plates, but infrequently in EDL end-plates. On the other hand, the postsynaptic AChR was reduced markedly in both soleus and EDL end-plates. No presynaptic changes were observed. These results show that long-term administration of Anti-ChE agents in myasthenia gravis may have an adverse effect on neuromuscular transmission.
Topics: Ambenonium Chloride; Animals; Female; Motor Endplate; Myasthenia Gravis; Neuromuscular Junction; Rats; Receptors, Cholinergic
PubMed: 7252521
DOI: 10.1016/0022-510x(81)90060-5 -
Molecular Pharmacology May 1992Steady state patterns of inhibition of purified human erythrocyte acetylcholinesterase by three inhibitors were analyzed. Edrophonium acted essentially as a competitive... (Comparative Study)
Comparative Study
Steady state patterns of inhibition of purified human erythrocyte acetylcholinesterase by three inhibitors were analyzed. Edrophonium acted essentially as a competitive inhibitor, whereas tacrine and ambenonium gave mixed competitive and uncompetitive inhibition with acetylthiocholine as substrate. Inhibition constants for the competitive components were 470 microM for edrophonium, 65 microM for tacrine, and 0.12 nM for ambenonium. The extremely high affinity of ambenonium permitted analysis of the rates of approach to steady state inhibition. These rates were characterized by a single exponential time course with rate constants, kexp, that showed a linear dependence when plotted against ambenonium concentration, at fixed substrate concentration. The intercepts of these plots were independent of the substrate concentration and indicated an ambenonium dissociation rate constant of 0.013 +/- 0.002 sec-1. The slope of the plot at the lowest substrate concentration approximated the ambenonium bimolecular or association rate constant and gave a value of 5.2 +/- 0.6 x 10(7) M-1 sec-1. Three models were examined to account for the nearly linear dependence of the slopes of these plots on the substrate concentration. These models indicated that ambenonium and acetylthiocholine competed for a peripheral anionic site in the acetyl-enzyme intermediate formed during substrate hydrolysis. The apparent equilibrium dissociation constant of acetylthiocholine for this peripheral site (1.2-1.4 mM) was significantly different from that calculated from substrate inhibition data (20.1 +/- 2.8 mM). We propose that acetylthiocholine can interact with the acetyl-enzyme both at the peripheral site and at the active site but that only the latter interaction inhibits substrate hydrolysis.
Topics: Acetylcholinesterase; Ambenonium Chloride; Cholinesterase Inhibitors; Edrophonium; Erythrocytes; Humans; Kinetics; Mathematics; Models, Theoretical; Molecular Structure; Tacrine
PubMed: 1588924
DOI: No ID Found -
Arzneimittel-Forschung Feb 1989Plasma concentrations of ambenonium chloride (Mytélase) were studied, using a high pressure liquid chromatographic technique, in 11 dogs, after intravenous or oral...
Plasma concentrations of ambenonium chloride (Mytélase) were studied, using a high pressure liquid chromatographic technique, in 11 dogs, after intravenous or oral administration of the drug. The results found suggest a complex multi-compartment storage with several periodical releases in general circulation.
Topics: Administration, Oral; Ambenonium Chloride; Animals; Chromatography, Ion Exchange; Dogs; Injections, Intravenous; Male
PubMed: 2730696
DOI: No ID Found -
Acta Neurologica Scandinavica Apr 2022Myasthenia gravis (MG) is a rare autoimmune disorder of neuromuscular junction. MG healthcare burden has not been studied in Poland before.
INTRODUCTION
Myasthenia gravis (MG) is a rare autoimmune disorder of neuromuscular junction. MG healthcare burden has not been studied in Poland before.
METHODS
Data were drawn from the National Health Fund database; MG patient was defined as a person who received at least once medical service with ICD-10 code MG (G70) and at least two reimbursed prescriptions for pyridostigmine bromide or ambenonium chloride in two consecutive years. We have analyzed treatment: immunosuppression, intravenous immunoglobulins (IVIg), plasma exchange (PE), the number and length of hospitalizations (LOS), intensive care unit (ICU) care, and deaths between 2013 and 2018.
RESULTS
In 2018, there were 9012 MG patients (F:M 1.62:1), and 30.6% had early -onset MG (<50 years). 66.3% received symptomatic treatment only, 33.7%-glucocorticoids (CS) and/or other immunosuppressants (IS), 64.6%-CS only, 17.5%-azathioprine plus CS, 11%-azathioprine only, 4.6%-CS plus other IS (methotrexate, mycophenolate mofetil, cyclosporine, or tacrolimus), and 2%-other IS only. In 2018, 42.3% of patients were hospitalized at least once (mean 2.05/year), 13.7% due to MG (1.47/year). In 2018, 1.63% patients received PE, 2.33% IVIg. In 2013-2018, 2.7%-3.2% of MG patients required hospitalization in ICU. ICU mean LOS 2013-2018 was 11.5-15.0 days/per patient/year. 2.1% of all MG patients had myasthenic crisis. Mean age at death was 75.7 years for MG and 73.9 for general population (p = .006). All-cause mortality was higher for men (4.1%-5.1%) than for women (2.5%-3.1%), p < .01.
CONCLUSIONS
Our findings confirm significant healthcare burden of MG, comprising a tool to plan resources needed for MG patients.
Topics: Cohort Studies; Female; Humans; Immunoglobulins, Intravenous; Male; Myasthenia Gravis; Plasma Exchange; Pyridostigmine Bromide
PubMed: 34981830
DOI: 10.1111/ane.13576 -
Journal of Chromatography Oct 1987
Topics: Ambenonium Chloride; Chromatography, Ion Exchange; Humans; Indicators and Reagents
PubMed: 3429595
DOI: 10.1016/0378-4347(87)80426-7