Demecarium bromide

716.59

714.235535

200-301-9

61D5V4OKTP

DTXSID6045240

C65367

WHITE POWDER|SLIGHTLY YELLOW, CRYSTALLINE POWDER

2924296000

59.08000

0.77020

162-167 °C (decomp)

FREELY SOL IN WATER, ALCOHOL; SPARINGLY SOL IN ACETONE; INSOL IN ETHER

AQ SOLN ARE NEUTRAL

DECOMP @ 162-167 °C|CONSISTS OF 2 NEOSTIGMINE MOLECULES CONNECTED @ CARBAMATE NITROGEN ATOMS BY SERIES OF 10 METHYLENE GROUPS /DEMECARIUM/|SLIGHTLY HYGROSCOPIC

III

9

3077

3

S22-S26-S36/37-S36/37/39

STABLE TO AUTOCLAVING, & RETAIN THEIR POTENCY FOR PROLONGED PERIODS

...INHIBITION PRODUCED BY DEMECARIUM IS "REVERSIBLE". LOCAL EFFECTS OF DRUG CAN BE ANTAGONIZED BY ATROPINE AS WELL AS BY PRALIDOXIME (PROTOPAM). EFFECTS OF DEMECARIUM ARE NOT INHIBITED BY PRIOR INSTILLATION OF PHYSOSTIGMINE. /DEMECARIUM/

Cholinesterase Inhibitors; Miotics|/IN TREATMENT OF ESOTROPIA/ THERAPY SHOULD BE DISCONTINUED AFTER 4 MO IF INSTILLATION AS OFTEN AS EVERY 2 DAYS IS STILL REQUIRED.|/CONGESTIVE IRITIS, IRIDOCYCLITIS, & CONJUNCTIVAL & INTRAOCULAR HYPEREMIA/ ... CAN BE MINIMIZED BY INSTILLATION OF SOLN OF LOWEST EFFECTIVE CONCN @ BEDTIME, & THEY OFTEN SUBSIDE AFTER FIRST FEW DAYS OF THERAPY. INSTILLATION OF 10% PHENYLEPHRINE HYDROCHLORIDE SOLN MAY BE HELPFUL IF CIRCUMCORNEAL INJECTION IS SEVERE.|FOLLOWING INSTILLATION OF DEMECARIUM IN EYE, MIOSIS APPEARS WITHIN 1 HR & REACHES ITS MAX IN 2 TO 4 HR. REDUCTION OF INTRAOCULAR PRESSURE OCCURS IN CA 12 HR & IS FREQUENTLY PRECEDED BY SLIGHT RISE IN PRESSURE. PUPILLARY CONSTRICTION & DECR INTRAOCULAR PRESSURE MAY PERSIST FOR WK OR MORE FOLLOWING SINGLE INSTILLATION.|For more Therapeutic Uses (Complete) data for DEMECARIUM BROMIDE (10 total), please visit the HSDB record page.

GONIOSCOPIC EXAM SHOULD CONFIRM THAT ANGLE OF EYE IS OPEN PRIOR TO DEMECARIUM THERAPY... IN PT WITH NARROW ANGLE (CONGESTIVE) GLAUCOMA, INTRAOCULAR PRESSURE MAY BE INCR & ACUTE ATTACKS MAY BE PPT. ...INCR IN INTRAOCULAR PRESSURE MAY OCCUR EVEN WHEN ANGLE IS OPEN...|DEMECARIUM IS CONTRAINDICATED IN PT WITH MARKED VASOMOTOR INSTABILITY, BRONCHIAL ASTHMA, SPASTIC GI CONDITIONS, PEPTIC ULCER, SEVERE BRADYCARDIA OR HYPOTENSION, RECENT MYOCARDIAL INFARCTION, EPILEPSY, OR PARKINSONISM.|.../DEMECARIUM/ SHOULD BE USED WITH GREAT CAUTION, IF AT ALL, IN PT WITH HISTORY OF RETINAL DETACHMENT & IN THOSE WITH OCULAR HYPERTENSION ACCOMPANIED BY INTRAOCULAR INFLAMMATORY PROCESSES. ...CONTRAINDICATED IN PT WITH NARROW ANGLE GLAUCOMA.|/DEMECARIUM/...SHOULD NOT BE ADMIN PRIOR TO IRIDECTOMY IN ANGLE-CLOSURE GLAUCOMA BECAUSE...MORE APT TO AGGRAVATE ANGLE CLOSURE THAN WEAKER MIOTICS.

CHOICE OF POTENT CHOLINESTERASE INHIBITOR DEPENDS ON INDIVIDUAL RESPONSE; SOME PT REFRACTORY TO OR INTOLERANT OF ONE DRUG MAY RESPOND TO OR TOLERATE ANOTHER. ... TOLERANCE TO ANTICHOLINESTERASE DRUGS MAY DEVELOP ON PROLONGED USE.

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. (See all compounds classified as Cholinesterase Inhibitors.)

DEMECARIUM IS ABSORBED THROUGH CONJUNCTIVAL SAC AS WELL AS THROUGH INTACT SKIN... /DEMECARIUM/

/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.

...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.

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.

demecarium

DEMECARIUM BROMIDE: HUMORSOL (MERCK SHARP & DOHME). TOPICAL: AQ SOLN (OPHTHALMIC, STERILE) 0.125% & 0.25% WITH SODIUM CHLORIDE & BENZALKONIUM CHLORIDE IN 5 ML CONTAINERS.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients