298-50-0CC(C)[N+](C)(CCOC(=O)C1c2ccccc2Oc2ccccc21)C(C)CVVWYOYDLCMFIEM-UHFFFAOYSA-NPropantheline is a member of xanthenes.
Pharmaceuticals -> Listed in ZINC15
Pharmaceutical
184.1 Ų [M+H]+ [CCS Type: DT; Buffer gas: N2; Ionization: ESI+; Dataset: TOXCAST; Source Identifier: DTXSID2023519]
182.55 Ų [M]+ [CCS Type: TW; Method: calibrated with polyalanine and drug standards]
Crystals from isopropanol plus ether; very soluble in water, alcohol, chloroform; practically insol in ether, benzene; mp: 159-161 °C /Bromide/
WHITE OR NEARLY WHITE CRYSTALS; ODORLESS & HAS BITTER TASTE; MELTS BETWEEN 156 & 162 °C WITH DECOMP /BROMIDE/
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。
Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).
SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.
GI ABSORPTION OF PROPANTHELINE IS INCR BY SODIUM BICARBONATE...
RATE & EXTENT OF ABSORPTION OF.../ORALLY/ DOSED PARACETAMOL IS REDUCED BY...PROPANTHELINE...
CONCURRENT USE OF PROPANTHELINE WITH SLOW-DISSOLVING TABLETS OF DIGOXIN MAY CAUSE INCR SERUM DIGOXIN LEVELS. THIS INTERACTION CAN BE AVOIDED BY USING ONLY THOSE DIGOXIN TABLETS THAT ARE FAST DISSOLVING BY USP STD.
.../TREATMENT WITH/ PROPANTHELINE, INCR /GI/ ABSORPTION /OF PHENOLSULFOPHTHALEIN IN MAN/ UP TO 24% OWING TO DECR GI TRANSIT RATE.
For more Interactions (Complete) data for PROPANTHELINE (14 total), please visit the HSDB record page.
Like other anticholinergic agents, propantheline has not been linked to episodes of liver enzyme elevations or clinically apparent liver injury. It is metabolized at least partially in the liver. A reason for its safety may relate to the low daily dose.
Only tests relating to glaucoma apparently have consisted of admin doses of 15 mg ... orally to 20 normal patients and to 20 patients with various kinds of glaucoma and evaluating intraocular pressure by tonometry performed hourly for 3 hr. ... Tension did not change in normal eyes ... . /Propantheline bromide/
A - Alimentary tract and metabolism
QA - Alimentary tract and metabolism
Propantheline is an anticholinergic drug, a medication that reduces the effect of acetylcholine, a chemical released from nerves that stimulates muscles, by blocking the receptors for acetylcholine on smooth muscle (a type of muscle). It also has a direct relaxing effect on smooth muscle. Propantheline is used to treat or prevent spasm in the muscles of the gastrointestinal tract in the irritable bowel syndrome. In addition, Propantheline inhibits gastrointestinal propulsive motility and decreases gastric acid secretion and controls excessive pharyngeal, tracheal and bronchial secretions.
Action is achieved via a dual mechanism: (1) a specific anticholinergic effect (antimuscarinic) at the acetylcholine-receptor sites and (2) a direct effect upon smooth muscle (musculotropic).
ANTICHOLINERGIC DRUGS BLOCK THE ACTION OF ACETYLCHOLINE AT POSTGANGLIONIC CHOLINERGIC SITES, THEREBY INCREASING BLADDER CAPACITY BY REDUCING THE NUMBER OF MOTOR IMPULSES REACHING THE DETRUSOR MUSCLE. /ANTICHOLINERGIC DRUGS/
1306V2B0Q8
PROPANTHELINE
Established Pharmacologic Class [EPC] - Anticholinergic
Mechanisms of Action [MoA] - Cholinergic Antagonists
Propantheline is an Anticholinergic. The mechanism of action of propantheline is as a Cholinergic Antagonist.
Various agents with different action mechanisms used to treat or ameliorate PEPTIC ULCER or irritation of the gastrointestinal tract. This has included ANTIBIOTICS to treat HELICOBACTER INFECTIONS; HISTAMINE H2 ANTAGONISTS to reduce GASTRIC ACID secretion; and ANTACIDS for symptomatic relief.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
読み込み中…
298-50-0DTXSID6047230CHEMBL1180725CHEBI:8481Symptoms and signs of drug abuse: Vital signs - temperature elevated; heart rate increased; possibly decreased blood pressure. Mental status - drowsiness or coma, sensorium clouded, amnesia, disorientation, visual hallucinations, body image alterations, confusion; with propantheline, restlessness, excitement. /Anticholinergic agents, from table/
VERY HIGH DOSES BLOCK THE SKELETAL NEUROMUSCULAR JUNCTION. THE USUAL CLINICAL DOSE ... ACTS FOR ABOUT 6 HOURS.
An elderly woman presented with preumonia and mental status changes and was found to have bromide /intoxication/ due to ingestion of propantheline bromide over a 2 mo period. The interference of bromide with serum chloride measurements on ion selective electrode resulted in spurious hyperchloremia and was crucial in making the diagnosis. /Propantheline bromide/
Drug-Induced Liver Injury Severity and Toxicity (DILIst)
propantheline
DILI Negative
Oral
DOI:10.1016/j.drudis.2019.09.022
Propantheline bromide a drug used for the treatment of peptic ulcers, was /evaluated/ in male and female Fischer 344/N rats and B6C3F1 mice for subchronic toxicity. The drug was admin in the feed for 13 wk at 0, 220,670, 2000, 6000 and 24,000 ppm in both species. /The cmpd/ caused a decr in weight gain at 24,000 ppm in male and female rats and at 6000 and 24,000 ppm in male and female mice. All rats survived treatment. The top dose of 24,000 ppm was fatal. Clinical signs of toxicity (dilated pupils and decr gastrointestinal emptying, similar to the atropine effects ... /observed/ in man, were seen in male and female rats at 24,000 ppm. Hyperplasia of the transitional epithelium of the urinary bladder was seen in high dose male rats and the end of 13 wk. /Propantheline bromide/
Propantheline bromide (PB) ... was tested for its effects on reproduction & fertility in CD-1 mice using the RACB protocol. Data on food & water consumption, body weights, & clinical signs during a 2 wk dose-range-finding study (Task 1) were used to set exposure concns for the Task 2 continuous cohabitation study at 0.0, 0.05, 0.16, & 0.5% in feed. Based on mean body weight & avg feed consumption data, the estimated daily doses were 71, 235, & 760 mg/kg bw. In the F0 animals, there were no deaths during Task 2. Body weight gain for the top dose males was reduced by a factor of 4, compared to controls. There was a statistically significant, but small (6%) reduction in the number of litters/pair at the top dose. The only other changes in reproductive indices for the F0 pairs occurred at the high dose level, & were a reduction in the mean weight of F1 pups adjusted for litter size at the top dose, by 4%, & an incr in the length of time to deliver each litter. This delay was greatest for the first 3 litters, while the difference was less for the last 2 litters. These modest reproductive effects (6% decr in litters/pair, & 4% decr in adjusted live pup weight) were considered too small to be detectable in the single litter generated by the Task 3 crossover, so Task 3 was not conducted. There were no adverse effects of PB consumption on the growth or viability of the F1 offspring in the last litter that was reared for second generation testing. After weaning the F2 mice, the F1 mice from control, middle & high dose groups were killed & necropsied. There were no weight changes or gross lesions noted in females, while male body weights were reduced by 11% at the top dose. There were no changes in sperm indices or in estrous cycle parameters. Only mice from the control & high dose groups were kept & treated with PB from weaning to the mating trial at /postnatal day/ 74 +/- 10. Compared to controls, the high dose PB mice had similar-sized litters, with the same proportion of live pups, & same sex ratio, but the adjusted live pup weight was reduced by 11%. After the delivery & evaluation of the F2 litters & estrous cycle data collection, the F1 adults were killed & necropsied. There was an 8% reduction in female body weight, & no change in organ weights. For males, body weight was reduced by 10%, & prostate weight was reduced by 25%. Epididymal sperm density was reduced at the high dose by 15%, while estrous cycle length & characteristics were unchanged. Thus, propantheline bromide caused detectable but small reductions in litter number, in both generations reduced adjusted pup weight, & reduced F1 prostate weight & sperm count. These effects were seen concomitant with male body weight changes but no other significant non-reproductive toxicities. /Propantheline bromide/
Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).
Approximately 70% of the dose is excreted in the urine, mostly as metabolites.
AFTER 95 HR HUMANS EXCRETED IN URINE 5% OF DOSE (0.03 G) OF PROPANTHELINE BROMIDE GIVEN ORALLY. /PROPANTHELINE BROMIDE, FROM TABLE/
The quarternary ammonium derivatives of the belladonna alkaloids are poorly absorbed after an oral dose; nevertheless, some of these compounds applied locally to the eye can cause mydriasis and cycloplegia. /Quarternary ammonium derivatives of belladonna alkaloids/
MEDICATION (VET)
MEDICATION
Cusic, Robinson, J Org Chem (16) 1921, 1951; US patent 2,659,732 (1953 to Searle). /Bromide/
Prepared by reacting xanthene-9-carboxylic acid chloride with 2-diisopropylaminoethanol, followed by alkylation with methyl bromide. /Bromide/
Corrigast; Ercotina; Pro-Banthine; Neo-Metantyl; Pantheline
BETA-DIISOPROPYLAMINOETHYL 9-XANTHENECARBOXYLATE METHOBROMIDE; (2-HYDROXYETHYL)DIISOPROPYLMETHYLAMMONIUM BROMIDE XANTHENE-9-CARBOXYLATE; NEOPEPULSAN; PRO-BANTHINE BROMIDE; PROPANTHELINE BROMIDE; XANTHENE-9-CARBOXYLIC ACID, ESTER WITH (2-HYDROXYETHYL)DIISOPROPYLMETHYLAMMONIUM BROMIDE. /BROMIDE/
用途鎮痙薬(平滑筋弛緩薬)平滑筋の痙攣を緩解する
使用Anticholinergic.