Pyridostigmine bromide

261.12

260.016

202-929-9

KVI301NA53

758435|679759

DTXSID9023540

C47697

WHITE OR PRACTICALLY WHITE, CRYSTALLINE POWDER

2933399090

33.4

0.9613 g/cm3 (20ºC)

152-154 °C

1.48 (20ºC)

Very soluble in water and in ethanol (96 per cent).FREELY SOL IN CHLOROFORM, SLIGHTLY SOL IN SOLVENT HEXANE

Refrigerator

AGREEABLE ODOR

137.2 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

HYGROSCOPIC

II

6.1

UN28116.1/PG2

3

26/27/28-43

22-36/37/39-45

UU5270000

T+

P260, P261, P262, P264, P270, P271, P272, P280, P284, P301+P310, P302+P350, P302+P352, P304+P340, P310, P311, P320, P321, P322, P330, P333+P313, P361, P363, P403+P233, P405, P501

H300 + H310 + H330-H317

|Danger|H300 (72.88%): Fatal if swallowed [Danger Acute toxicity, oral]|P260, P261, P262, P264, P270, P271, P272, P280, P284, P301+P310, P302+P350, P302+P352, P304+P340, P310, P311, P320, P321, P322, P330, P333+P313, P361, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 59 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

ACTIONS OF ANTICHOLINESTERASE AGENTS ON AUTONOMIC EFFECTOR CELLS & ON CORTICAL & SUBCORTICAL SITES IN CNS, WHERE RECEPTORS ARE LARGELY OF MUSCARINIC TYPE, ARE BLOCKED BY ATROPINE. /ANTI-CHE AGENTS/|A SINGLE CASE HAS BEEN REPORTED IN WHICH METHOCARBAMOL MAY HAVE IMPAIRED THE THERAPEUTIC EFFECT OF PYRIDOSTIGMINE BROMIDE IN A PATIENT WITH MYASTHENIA GRAVIS.|In anesthetized patients, pyridostigmine bromide mestinon 10 mg iv antagonized the neuromuscular block induced by d-tubocurarine chloride 0.29 mg/kg/hr. Adequate recovery from the neuromuscular block should be judged by the return of the twitch height to the control level & also by the restoration of well-sustained tetanus 30 cycles/sec to the level seen before d-tubocurarine chloride administration.|Prolonged effect of succinylcholine after neostigmine and pyridostigmine administration in patients with renal failure.|The amino acid gamma-aminobutyric acid (GABA), when given as supplement to pyridostigmine bromide reduced the incidence of malformations in chicken embryos.

Photolytic degradation of solutions of pyridostigmine bromide gave 3-hydroxy-l-methylpyridinium bromide and a small amt of unidentifiable tar.

Breast milk concn of pyridostigmine was determined in 2 nursing mothers who were receiving oral doses of pyridostigmine bromide, 120-300 mg daily. The amt of pyridostigmine per kg body wt ingested by the nursing infant was only 0.1% or less than that taken by the mother.

Cholinesterase Inhibitors; Parasympathomimetics|A QUATERNARY AMMONIUM ANTICHOLINESTERASE DRUG ...PRINCIPAL USE IS IN THE TREATMENT OF MYASTHENIA GRAVIS. ...|DOSAGE: THE EQUIVALENT PARENTERAL DOSE OF...PYRIDOSTIGMINE IS APPROX 1/30TH OF THE ORAL DOSE.|PYRIDOSTIGMINE HAS A SLOWER ONSET (13 MIN) THAN EDROPHONIUM (3 MIN) OR NEOSTIGMINE (6-8 MIN), BUT A LONGER DURATION OF ACTION THAN EITHER. FOR THIS REASON, IT HAS BEEN RECOMMENDED FOR PATIENTS WITH RENAL IMPAIRMENT.|For more Therapeutic Uses (Complete) data for PYRIDOSTIGMINE BROMIDE (9 total), please visit the HSDB record page.

BROMIDE SENSITIVITY OCCASIONALLY OCCURS.|Maternal Medication usually Compatible with Breast-Feeding: Pyridostigmine: Reported Sign or Symptom in Infant or Effect on Lactation: None. /from Table 6/

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.)

ITS ONSET OF ACTION BY ORAL ROUTE IS ABOUT 320 MIN...ITS DURATION OF ACTION BY THE ORAL ROUTE IS USUALLY SOMEWHAT LONGER AND ABSORPTION IS LESS ERRATIC THAN NEOSTIGMINE, WHICH ARE ADVANTAGES.|Plasma concn of pyridostigmine was determined in 2 nursing mothers who were receiving oral doses of pyridostigmine bromide, 120-300 mg daily. The drug was not detectable in infant plasma and there were no signs of drug effects in the infant.

PYRIDOSTIGMINE AND ITS QUATERNARY ALCOHOL ARE...THE PREDOMINANT ENTITIES FOUND IN URINE AFTER ADMIN OF THIS DRUG TO MAN.

After admin of pyridostigmine bromide (200 nmol/kg, iv) to human subjects, the disposition half-life was 0.6-1.78 min and terminal half-life was 14.81-37.01 min. Clearance was 9.3-26.5 ml/min/kg which was greater than the presumptive value for glomerular filtration rate and the vol of distribution was 246.5-833.9 ml/kg.

...PHARMACOLOGICAL EFFECTS OF ANTICHOLINESTERASE AGENTS ARE DUE PRIMARILY TO PREVENTION OF HYDROLYSIS OF /ACH/ ACETYLCHOLINE BY ACHE /ACETYLCHOLINESTERASE/ @ SITES OF CHOLINERGIC TRANSMISSION. TRANSMITTER THUS ACCUMULATES, AND THE ACTION OF ACH /ACETYLCHOLINE/ THAT IS LIBERATED BY CHOLINERGIC IMPULSES OR THAT LEAKS FROM THE NERVE ENDING IS ENHANCED.|Following admin of pyridostigmine bromide to rats, erythrocyte acetylcholinesterase activity recovered only slowly due to the covalent nature of inhibition. The logarithm of the plasma concn of pyridostigmine bromide was linearly related to the increase in tibialis twitch tension due to facilitation of neuromuscular transmission.|Of 12 analogs of pyridostigmine prepared by reacting 2-substituted 3-pyridinols with the desired carbamoyl chloride 2-iodo-3-(dimethylcarbamoyloxy)pyridine methiodide was the most active inhibitor of acetylcholinesterase and butyrylcholinesterase. The progressive inhibition curves for AChE and BuChE are compared and related to ionic attraction and steric requirements of the inhibitors.

1) ESTABLISH CLEAR AIRWAY & TISSUE OXYGENATION BY ASPIRATION OF SECRETIONS & IF NECESSARY, BY ASSISTED PULMONARY VENTILATION WITH OXYGEN. IMPROVE TISSUE OXYGENATION AS MUCH AS POSSIBLE BEFORE ADMINISTERING ATROPINE TO MINIMIZE THE RISK OF VENTRICULAR FIBRILLATION. /CARBAMATES, CHOLINESTERASE INHIBITORS/|2) ADMIN ATROPINE SULFATE IV, OR IM IF IV INJECTION IS NOT POSSIBLE... IN MODERATELY SEVERE POISONING: ADULT DOSAGE, INCLUDING CHILDREN OVER 12 YR: 0.4-2.0 MG REPEATED EVERY 15 MIN UNTIL ATROPINIZATION IS ACHIEVED (TACHYCARDIA, FLUSHING, DRY MOUTH, MYDRIASIS). MAINTAIN ATROPINIZATION BY REPEATED DOSES FOR 2-12 HR, OR LONGER, DEPENDING ON SEVERITY OF POISONING... DOSAGE FOR CHILDREN UNDER 12 YEARS: 0.05 MG/KG BODY WT REPEATED EVERY 15 MIN UNTIL ATROPINIZATION IS ACHIEVED. MAINTAIN ATROPINIZATION WITH REPEATED DOSAGE OF 0.02-0.05 MG/KG. SEVERELY POISONED INDIVIDUALS MAY EXHIBIT REMARKABLE TOLERANCE TO ATROPINE; TWICE THE DOSES SUGGESTED ABOVE MAY BE NEEDED... /CARBAMATES, CHOLINESTERASE INHIBITORS/|3. PRALIDOXIME (PROTOPAM-AYERST, 2-PAM) IS OF DOUBTFUL VALUE IN POISONINGS BY CARBAMATE INHIBITORS OF CHOLINESTERASE. ATROPINE ALONE IS ALMOST ALWAYS AN ADEQUATE ANTIDOTE. PRALIDOXIME IS PROBABLY CONTRAINDICATED IN POISONINGS BY CARBARYL, SPECIFICALLY. IF VICTIM OF CARBAMATE POISONING EXHIBITS SEVERE MUSCLE WEAKNESS &/OR RESPIRATORY DEPRESSION, OR IF POISONING INVOLVES A COMBINATION OF CARBAMATE & ORGANOPHOSPHATE, A DILUTE SOLUTION OF PRALIDOXIME (TOTAL DOSE IN 250 ML 5% GLUCOSE SOLN) MAY BE GIVEN CAUTIOUSLY IV. THE INFUSION SHOULD BE TERMINATED IF PATIENT'S CONDITION WORSENS. PRALIDOXIME DOSAGE: ADULTS, 1.0 G; FOR CHILDREN UNDER 12 YR, 20-50 MG/KG. 4. OBSERVE TREATED PATIENTS CLOSELY AT LEAST 24 HR TO INSURE THAT SYMPTOMS (POSSIBLY PULMONARY EDEMA) DO NOT RECUR AS ATROPINIZATION WEARS OFF. IN VERY SEVERE POISONINGS, METABOLIC DISPOSITION OF TOXICANT MAY REQUIRE SEVERAL HR OR DAYS DURING WHICH ATROPINIZATION MUST BE MAINTAINED. /CARBAMATES, CHOLINESTERASE INHIBITORS/|6. IF...INGESTED IN QUANTITY SUFFICIENT TO CAUSE POISONING, EMPTY THE STOMACH & INTESTINE. A. IF VICTIM IS ALERT & RESPIRATION IS NOT DEPRESSED, GIVE SYRUP OF IPECAC, FOLLOWED BY 1-2 GLASSES OF WATER TO INDUCE VOMITING; ADULTS (INCLUDING CHILDREN OVER 12), 30 ML; CHILDREN (UNDER 12 YR), 15 ML. CAUTION: OBSERVE VICTIM CLOSELY AFTER ADMIN IPECAC, IF CONSCIOUSNESS LEVEL DECLINES, OR IF VOMITING HAS NOT OCCURRED IN 15 MIN, PROCEED IMMEDIATELY TO INTUBATE THE STOMACH. FOLLOWING EMESIS, HAVE VICTIM DRINK A SUSPENSION OF /PRC: 30 G ACTIVATED CHARCOAL IN 3-4 OZ OF WATER (CHILDREN), 100 G IN 8-10 OZ OF WATER (ADULTS)/...TO BIND TOXICANT REMAINING IN THE GI TRACT. /CARBAMATES, CHOLINESTERASE INHIBITORS/|For more Antidote and Emergency Treatment (Complete) data for PYRIDOSTIGMINE BROMIDE (6 total), please visit the HSDB record page.

EFFECTS...ON CENTRAL NERVOUS SYSTEM ARE...CHARACTERIZED BY STIMULATION OR FACILITATION AT VARIOUS SITES, SUCCEEDED BY INHIBITION OR PARALYSIS AT HIGHER CONCN. ... RESPIRATORY & OTHER SUBCORTICAL CENTERS LIKEWISE SHOW STIMULATION AFTER LOW DOSES AND DEPRESSION WITH HIGHER OR TOXIC DOSES. /ANTI-CHOLINESTERASE AGENTS/|GI SYMPTOMS OCCUR EARLIEST AFTER INGESTION, & INCL ANOREXIA, NAUSEA & VOMITING, ABDOMINAL CRAMPS, & DIARRHEA. WITH PERCUTANEOUS ABSORPTION OF LIQ, LOCALIZED SWEATING & MUSCULAR FASCICULATION IN IMMEDIATE VICINITY ARE GENERALLY EARLIEST MANIFESTATIONS. /ANTI-CHOLINESTERASE AGENTS/|...EFFECTS ON CNS INCL CONFUSION, ATAXIA, SLURRED SPEECH, LOSS OF REFLEXES, CHEYNE-STOKES RESP, GENERALIZED CONVULSIONS, COMA, & CENTRAL RESP PARALYSIS. ... TIME OF DEATH AFTER SINGLE ACUTE EXPOSURE MAY RANGE FROM LESS THAN 5 MIN TO NEARLY 24 HR, DEPENDING UPON DOSE, ROUTE, AGENT... CAUSE OF DEATH IS PRIMARILY RESPIRATORY FAILURE USUALLY ACCOMPANIED BY A SECONDARY CARDIOVASCULAR COMPONENT. /ANTI-CHOLINESTERASE AGENTS/|NICOTINIC ACTIONS @ NEUROMUSCULAR JUNCTIONS OF SKELETAL MUSCLE...FATIGABILITY & GENERALIZED WEAKNESS, INVOLUNTARY TWITCHINGS...SEVERE WEAKNESS & PARALYSIS; UNDOUBTABLY A CENTRAL COMPONENT OF ACTION CONTRIBUTES TO SOME OF THESE EFFECTS. THE MOST SERIOUS CONSEQUENCE...IS PARALYSIS OF RESPIRATORY MUSCLES. /ANTI-CHOLINESTERASE AGENTS/|For more Human Toxicity Excerpts (Complete) data for PYRIDOSTIGMINE BROMIDE (7 total), please visit the HSDB record page.

Bromide, Pyridostigmine

AVAILABLE FOR ORAL USE IN 60-MG TABLETS, IN 180-MG SUSTAINED RELEASE TABLETS AND IN A SYRUP THAT CONTAINS 12 MG/ML, AS WELL AS IN AN INJECTABLE FORM THAT CONTAINS 5 MG/ML IN 2-ML AMPULS.|MESTINON IS AVAILABLE AS THE CHLORIDE SALT, UPON SPECIAL REQUEST FROM THE MANUFACTURER, ROCHE LABORATORIES.

The proposed spectrophotometric method is highly sensitive with good accuracy (97.7 to 100% recovery) and precision (SD +/- 0.6-1.2%).

A liquid chromatography assay with a reversed phase chromatographic column isolation technique is described for the determination of plasma and urine levels of pyridostigmine bromide given im to rats. A detection limit of 40 ng/ml was obtained.

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