기본 정보
- CAS
7085-45-2- 표준 SMILES
CC(O)C(=O)O.OC(CCN1CCCCC1)(c1ccccc1)C1CC2C=CC1C2- InChIKey
GLPUBCPQWZZFNJ-UHFFFAOYSA-N- 분자식
- C24H35NO4
- 평균 분자량
- 401.5 g/mol
- 단동위원소 질량
- 401.2566086
개요
A muscarinic antagonist that has effects in both the central and peripheral nervous systems. It has been used in the treatment of arteriosclerotic, idiopathic, and postencephalitic parkinsonism. It has also been used to alleviate extrapyramidal symptoms induced by phenothiazine derivatives and reserpine. [PubChem]
이름 및 식별자
- 우선 이름
- Biperiden Lactate
- IUPAC
- 1-(2-bicyclo[2.2.1]hept-5-enyl)-1-phenyl-3-piperidin-1-ylpropan-1-ol;2-hydroxypropanoic acid
- 영어명
- BIPERIDEN LACTATE
- 분자식
- C24H35NO4
- 분자량
- 401.55
이름 및 동의어
이름 더 보기
데이터베이스 식별자
- CAS
7085-45-2- PubChem CID
- 197083
- DTXSID
DTXSID40991120- ChEMBL
CHEMBL1201067- UNII
- 09TD6C5147
- EC Number
- 230-388-9
물성
구조 계산 물성
- 극성 표면적
- 81 Ų
- 수소 결합 공여자 수
- 3
- 수소 결합 수용자 수
- 5
- 회전 가능 결합 수
- 6
- 무거운 원자 수
- 29
- 형식 전하
- 0
- 복잡도
- 481
실험 및 물리화학적 성질
Human Drugs
Breast Feeding; Lactation; Milk, Human; Antiparkinson Agents; Parasympatholytics; Muscarinic Antagonists
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
물리화학적 성질
- 녹는점
- 97 · 97-101°C
- 저장 조건
- -20 °C · -20°C Freezer
- 용해도
- 클로로포름(약간 용해됨), DMSO(약간 용해됨), 메탄올(약간 용해됨)
- 물리적 상태
- 고체
- 색상
- 하얀색
안전 및 규제
독성 정보
Treatment
Treatment of acute overdose revolves around symptomatic and supportive therapy. If Biperiden was administered orally, gastric lavage or other measures to limit absorption should be instituted. A small dose of diazepam or a short acting barbiturate may be administered if CNS excitation is observed. Phenothiazines are contraindicated because the toxicity may be intensified due to their antimuscarinic action, causing coma. Respiratory support, artificial respiration or vasopressor agents may be necessary. Hyperpyrexia must be reversed, fluid volume replaced and acid-base balance maintained. Urinary catheterization may be necessary. Routine use of physostigmine for overdose is controversial. Delirium, hallucinations, coma, and supraventricular tachycardia (not ventricular tachycardias or conduction defects) seem to respond. If indicated, 1 mg (half this amount for the children or elderly) may be given intramuscularly or by slow intravenous infusion. If there is no response within 20 minutes, and additional 1 mg dose may be given; this may be repeated until a total of 4 mg has been administered, a reversal of the toxic effects occur or excessive cholinergic signs are seen. Frequent monitoring of clinical signs should be done. Since physostigmine is rapidly destroyed, additional injections may be required every one or two hours to maintain control. The relapse intervals tend to lengthen as the toxic anticholinergic agent is metabolized, so the patient should be carefully observed for 8 to 12 hours following the last relapse. (L1712)
Toxicity Summary
Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as biperiden is considered to relate to competitive antagonism of acetylcholine at cholinergic receptors in the corpus striatum, which then restores the balance.
Signs and Symptoms
Signs of overdose include dilated and sluggish pupils, warm, dry skin, facial flushing, decreased secretions of the mouth, pharynx, nose, and bronchi, foul-smelling breath, elevated temperature, tachycardia, cardiac arrhythmias, decreased bowel sounds, urinary retention, delirium, disorientation, anxiety, hallucinations, illusions, confusion, incoherence, agitation, hyperactivity, ataxia, loss of memory, paranoia, combativeness, and seizures.
화학 및 산업
약리 정보
MeSH Pharmacological Classification
Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists.
Agents that inhibit the actions of the parasympathetic nervous system. The major group of drugs used therapeutically for this purpose is the MUSCARINIC ANTAGONISTS.
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.
용도 및 제조
응용 분야
용도Anticholinergic; antiparkinsonian.
공급사11 곳
관련 반응
현재 필터 조건에 해당하는 반응 기록이 없습니다.
화합물 노트
불러오는 중…