56-94-0CN(CCCCCCCCCCN(C)C(=O)Oc1cccc([N+](C)(C)C)c1)C(=O)Oc1cccc([N+](C)(C)C)c1.[Br-].[Br-]YHKBUDZECQDYBR-UHFFFAOYSA-LDemecarium bromide is the methobromide salt of the N,N'-bis[3-(dimethylamino)phenyl carbamate] derivative of 2,13-diazatetradecane. It is an inhibitor of acetylcholinesterase and pseudocholinesterase, with a long duration of action. It is used in the treatment of chronic open-angle glaucoma: in the eye, it causes constriction of the iris sphincter muscle and the ciliary muscle, facilitating the outflow of the aqueous humor and so reducing intraocular pressure. It has a role as an EC 3.1.1.8 (cholinesterase) inhibitor and an EC 3.1.1.7 (acetylcholinesterase) inhibitor. It is a bromide salt, a carbamate ester and a quaternary ammonium salt. It contains a demarcarium.
56-94-0CHEMBL1200514CHEBI:4391WHITE POWDER
SLIGHTLY YELLOW, CRYSTALLINE POWDER
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
AQ SOLN ARE STABLE
STABLE TO AUTOCLAVING, & RETAIN THEIR POTENCY FOR PROLONGED PERIODS
DECOMP @ 162-167 °C
CONSISTS OF 2 NEOSTIGMINE MOLECULES CONNECTED @ CARBAMATE NITROGEN ATOMS BY SERIES OF 10 METHYLENE GROUPS /DEMECARIUM/
SLIGHTLY HYGROSCOPIC
化学的特性White Solid
安全情報は参考情報です。供給元の安全データシート(SDS)、適用法令、専門家による評価に代わるものではありません。
Danger
H300 (100%): Fatal if swallowed [Danger Acute toxicity, oral]
P264, P270, P301+P316, P321, P330, P405, and P501 (click each P-code to see the statement)
The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.
IN SOME PT, DEMECARIUM MAY PRODUCE CONTACT DERMATITIS. IRIS CYSTS HAVE BEEN REPORTED, PARTICULARLY IN CHILDREN, FOLLOWING PROLONGED USE... /DEMECARIUM/
SIDE EFFECTS OF DEMECARIUM...MAY INCL CILIARY OR ACCOMODATIVE SPASM, BLURRED VISION, OCULAR OR BROW PAIN, HEADACHE, PHOTOPHOBIA, & TWITCHING OF EYELIDS. RARELY, RETINAL DETACHMENT MAY RESULT FROM SEVERE CILIARY SPASM. CONGESTIVE IRITIS, IRIDOCYCLITIS, & CONJUNCTIVAL & INTRAOCULAR HYPEREMIA MAY...OCCUR. /DEMECARIUM/
SYSTEMIC EFFECTS ARE MANIFESTATIONS OF PARASYMPATHETIC STIMULATION & MAY INCL NAUSEA, VOMITING, ABDOMINAL PAIN, DIARRHEA, FREQUENT URINATION, EXCESSIVE SALIVATION & SWEATING, FLUSHING, BRONCHIAL CONSTRICTION, HYPOTENSION, & BRADYCARDIA. ...INGESTION...WILL PRODUCE SIMILAR...EFFECTS &...CONVULSIONS, SHOCK & COLLAPSE.
IT HAS NOW BEEN ESTABLISHED THAT TREATMENT OF GLAUCOMA WITH POTENT, LONG-ACTING ANTI-CHOLINESTERASE AGENTS (INCL DEMECARIUM...) FOR 6 MO OR LONGER CARRIES HIGH RISK OF DEVELOPMENT OF SPECIFIC TYPE OF CATARACT, DESCRIBED AS ANTERIOR SUBCAPSULAR VACUOLES... INCIDENCE OF LENTICULAR OPACITIES...AS HIGH AS 50%... /DEMECARIUM/
For more Human Toxicity Excerpts (Complete) data for DEMECARIUM BROMIDE (6 total), please visit the HSDB record page.
Drug-Induced Liver Injury Severity and Toxicity (DILIst)
demecarium bromide
DILI Positive
DOI:10.1016/j.drudis.2019.09.022
SYSTEMIC ABSORPTION FROM NOSE CAN OCCUR, CAUSING TREMORS & COLLAPSE.
NEUROACTIVE COMPD & VERTEBRAL TERATOGENESIS IN BIRD EMBRYO. QUAIL EMBRYOS EXPOSED TO DEMECARIUM BROMIDE (1.5 MG) SHOWED VERTEBRAL FUSIONS & NECK DEFORMITIES AFTER 3 DAYS. MECHANISM OF TERATOGENESIS IS DISCUSSED.
...SYSTEMIC TOXICITY, ATROPINE SULFATE OR PRALIDOXIME CHLORIDE, ADMIN SC OR IV, IS EFFECTIVE ANTIDOTE. ADMIN OF SHORT-ACTING BARBITURATE MAY ALSO BE NECESSARY & ARTIFICIAL RESPIRATION MAY BE REQUIRED TO MAINTAIN ADEQUATE VENTILATION.
MARKED INCR IN INTRAOCULAR PRESSURE MAY BE OVERCOME BY LOCAL INSTILLATION OF EPINEPHRINE IF NECESSARY. ... SEVERE HYPEREMIA MAY BE RELIEVED BY LOCAL INSTILLATION OF 1 OR 2% EPINEPHRINE.
APPEARANCE OF.../IRIS CYSTS/ HAS BEEN ATTRIBUTED TO FREQUENCY OF ADMIN & THEY HAVE DISAPPEARED UPON WITHDRAWAL OF DRUG. PT SHOULD BE EXAMINED REGULARLY FOR APPEARANCE OF IRIS CYSTS & THERAPY SHOULD BE DISCONTINUED, AT LEAST TEMPORARILY, IF THEY OCCUR.
/INCR FACILITY OF AQ OUTFLOW/...ACCOMPANIED BY VASODILATATION OF CONJUNCTIVAL VESSELS & INCR PERMEABILITY OF BLOOD-AQ BARRIER. INDIRECT DECR IN ACTIVITY OF EXTRAOCULAR MUSCLES OF CONVERGENCE ALSO OCCURS. ...CHOLINESTERASE INHIBITION PRODUCED BY DEMECARIUM IS "REVERSIBLE".
DEMECARIUM BROMIDE...IS A QUATERNARY AMMONIUM ANTICHOLINESTERASE DRUG. ... RESULTING ACCUM OF ACETYLCHOLINE PRODUCES MIOSIS & STIMULATES CILIARY MUSCLE...REDUCING INTRAOCULAR PRESSURE BY INCR FACILITY OF AQ OUTFLOW.
Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system.
MEDICATION
MEDICATION (VET)
N,N'-DIMETHYL-1,10-DECAMETHYLENEDIAMINE IS ADDED TO MOLTEN 3-(DIMETHYLAMINO)PHENYL CARBONATE TO PRODUCE 1,10-DE CAMETHYLENEBIS[3-(DIMETHYL-AMINO)PHENYL N-METHYLCARBAMATE]. AFTER PURIFICATION THIS ESTER...A VISCOUS OIL, IS DISSOLVED IN ETHANOL & DOUBLY QUATERNIZED WITH AID OF AN ACETONE SOLN OF METHYL BROMIDE.
SCHMID, US PATENT 2,789,981 (1957 TO OESTERREICHISCHE STICKSTOFFWERKE).
使用Demecarium is a disymmetrical compound that contains two ammonium and two carbamate groups. It is a reversible cholinesterase inhibitor that is longer lasting than the others. It is used to constrict pupils, elevate intraocular pressure in treating glaucoma, and also for alleviating atropine mydriasis.
使用Demecarium Bromide is an acetylcholinesterase inhibitor and veterinary medicine used to treat elevated intraocular pressure associated with primary glaucoma.
一般的な説明Demecarium bromide,(m-hydroxyphenyl)trimethylammonium bromide, decamethylenebis[methylcarbamate] (Humorsol), is the diester of(m-hydroxyphenyl)trimethylammonium bromide with decamethylene-bis-(methylcarbamic acid) and thus is comparableto a bis-prostigmine molecule.It occurs as a slightly hygroscopic powder that is freelysoluble in water or alcohol. Ophthalmic solutions of the drughave a pH of 5 to 7.5. Aqueous solutions are stable and maybe sterilized by heat. Its efficacy and toxicity are comparableto those of other potent anticholinesterase inhibitor drugs. Itis a long-acting miotic used to treat wide-angle glaucomaand accommodative esotropia. Maximal effect occurs hoursafter administration, and the effect may persist for days.
定義ChEBI: The methobromide salt of the N,N'-bis[3-(dimethylamino)phenyl carbamate] derivative of 2,13-diazatetradecane. It is an inhibitor of acetylcholinesterase and pseudocholinesterase, with a long duration of action. It is u ed in the treatment of chronic open-angle glaucoma: in the eye, it causes constriction of the iris sphincter muscle and the ciliary muscle, facilitating the outflow of the aqueous humor and so reducing intraocular pressure.
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