Anticholinergics are drugs that oppose the effects of acetylcholine at receptor sites in the substantia nigra and the corpus striatum, thus helping to restore chemical balance in the area. Anticholinergics used to treat Parkinson’s disease include benztropine (Cogentin), diphenhydramine (Benadryl), and trihexyphenidyl (generic).
The anticholinergics used to treat parkinsonism are synthetic drugs that have been developed to have a greater affinity for cholinergic receptor sites in the CNS than for those in the peripheral nervous system. However, they still block, to some extent, the cholinergic receptors that are responsible for stimulation of the parasympathetic nervous system’s postganglionic effectors. This blockage is associated with the adverse effects, including slowed gastrointestinal (GI) motility and secretions, with dry mouth and constipation, urinary retention, blurred vision, and dilated pupils.
Anticholinergic drugs are indicated for the treatment of parkinsonism, whether idiopathic, atherosclerotic, or postencephalitic, and for the relief of symptoms of extrapyramidal disorders associated with the use of some drugs, including phenothiazines. Although these drugs are not as effective as levodopa in the treatment of advancing cases of the disease, they may be useful as adjunctive therapy and for patients who no longer respond to levodopa.
The anticholinergic drugs are variably absorbed from the GI tract, reaching peak levels in 1 to 4 hours. They are metabolized in the liver and excreted by cellular pathways. All of them cross the placenta and enter breast milk. Benztropine, diphenhydramine, and biperiden are available in oral and intramuscular/intravenous forms. Trihexyphenidyl is only available in an oral form.
➧ Anticholinergic agents are used to suppress the stimulatory effects of acetylcholine in the substantia nigra, bringing balance into the control of movement.
抗胆碱能药物用于抑制黑质乙酰胆碱的兴奋效应，使运动控制恢复平衡。
➧ The adverse effects associated with the anticholinergic drugs are related to blocking of the acetylcholine in the parasympathetic nervous system—dry mouth, constipation, urinary retention, increased heart rate, decreased sweating.
blood–brain barrier – 血脑屏障
substantia nigra – 黑质
idiopathic – a. 突发性的，原因不明性的
mainstay – n. 骨干，唯一依靠 Rytary – n.【奥】瑞泰利
postencephalitic parkinsonism 脑炎后帕金森综合征 anticholinergic – a. n. 抗胆碱能药(的)
acetylcholine – n. 乙酰胆碱
corpus striatum – n. 纹状体
benztropine – n. 苯扎托品 Cogentin – n. 苯扎托品商标名
diphenhydramine – n. 苯海拉明 Benadryl – n. 苯那君
trihexyphenidyl – n. 苯海索
affinity – n. 亲和力
parasympathetic – a. 副交感神经的
postganglionic – a. （神经）节后的
effector – n. 效应器
phenothiazine – n. 酚噻嗪
cellular pathway – 细胞通路/途径
biperiden – n. 比哌立登
1. Anticholinergic drugs are used
A. To allow the sympathetic system to dominate
B. To block the parasympathetic system, which is commonly hyperactive
C. As the drugs of choice for treating ulcers
D. To stimulate GI activity 2. Atropine and scopolamine work by blocking what receptor(s) in the parasympathetic nervous system?
A. Nicotinic receptors only
B. Muscarinic and nicotinic receptors
C. Muscarinic receptors only
D. Adrenergic receptors to allow cholinergic receptors to dominate
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答案Answers
1. A. To allow the sympathetic system to dominate
It decreases GI activity and secretions in the treatment of ulcers and to decrease other parasympathetic activities to allow the sympathetic system to dominate. More specific and less systemically toxic drugs are available for treatment of ulcers. 2. C. Muscarinic receptors only
Atropine and scopolamine work by blocking only the muscarinic effectors in the parasympathetic nervous system and the few cholinergic receptors in the SNS.
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