Cholinomimetics

Acetylcholine Precursors. Early efforts to treat dementia using cholinomimetics focused on choline [62-49-7] (12) supplement therapy (Fig. 3). This therapy, analogous to L-dopa [59-92-7] therapy for Parkinson s disease, is based on the hypothesis that increasing the levels of choline in the brain bolsters acetylcholine (ACh) synthesis and thereby reverses deficits in cholinergic function. In addition, because choline is a precursor of phosphatidylcholine as well as ACh, its supplementation may be neuroprotective in conditions of choline deficit (104). 

Therapeutic Function Miotic, cholinomimetic Chemical Name 1-Azabicyclo(2.2.2] octan-3-ol acetate Common Name 3-Quinuclidlnol Acetate... 

The memory deficits characteristic of Alzheimer s disease have not yet been successfully treated. There is reason to believe that potent acetylcholinesterase-resistant cholinomimetics might be effective in treating these deficits, but systemic administration of agents of this type, such as bethanechol, does not adequately deliver such... 

REM sleep (Kodama et al, 1990 Leonard Lydic, 1995, 1997) and cholinergic REM sleep enhancement (Lydic et al., 1991), ACh release is significantly increased in the same regions of the pontine reticular formation where microinjection of cholinomimetics enhances REM sleep (1.3 and 1.4 on Fig. 5.1). These results support the conclusion that at the level of ACh release, the cholinergic enhancement of REM sleep is a faithful model of spontaneous REM sleep. 

Kshatri, A. M., Baghdoyan, H. A. Lydic, R. (1998). Cholinomimetics, but not morphine, increase antinociceptive behavior from pontine reticular regions regulating rapid eye movement sleep. Sleep 21, 677-85. 

Some quinolizine derivatives are employed as drugs. One of them is flumequine 280, a member of the quinolone family of antibacterial agents. Cytisine 9 is a ligand of the nicotinic acetylcholine receptor that acts primarily as a cholinomimetic at the ganglionar level, being used as a respiratory stimulant in some countries. Cytisine analogues with improved ability to cross the blood-brain barrier have also been developed <1999FA438>. 

The answer is a. (Katzung, pp 471, 473, 482.) The phenothiazines as a class are the most potent anticholinergics of the neuroleptics. Tolerance to their anticholinergic effects occurs in most patients Cholinomimetic agents may be used to overcome symptoms that persist. 

The cholinomimetic drug that is useful for treating postoperative abdominal distention and gastric atony is... 

The answer is a. (Hardman, pp 146—147, 167.) When applied topically to the eye, both the direct-acting cholinomimetic agents (e g., pilo-... 

Overflow (atonic bladder) Cholinomimetics Bethanechol (25-50 mg three or four times daily) on an empty stomach Avoid use if patient has asthma or heart disease. Short-term use only. Never give IV or IM because of life-threatening cardiovascular and severe Gl reactions. 

Comment on the use of cholinomimetic drugs in the treatment of Alzheimer s disease... 

Phentolamine is also a derivative of imidazoline that exhibits a direct a-adrenoblocking, muscle-relaxant effect on smooth muscle as well as cholinomimetic, histamine, and sympathomimetic effects. The chemical variation of its stmcture permits a few of its properties to be more expressed. For example, the aforementioned tolazoline, 2-benzyl-2-imidazoline, a structural analog of phentolamine, has more of an expressed muscle-relaxant effect on smooth muscle than an a-adrenoblocking effect. 

So, parasympathetic nerves use acetylcholine as a neurotransmitter and cholinomimetic drugs mimic the action of acetylcholine at its receptors. Muscarinic receptor subtypes are found on neuroeffector junctions. Nicotinic receptor subtypes are found on ganglionic synapses. Chohnomimetics can be classified as ... 

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