Atropine objects

Esters of tropine have a venerable place in medicinal chemistry. One such compound, cocaine, the object of some current interest, was the natural product lead which led eventually to most of today s local anesthetics. A distantly related analogue is prepared by reaction of tropine (132) with 3,5-dimethylbenzoyl chloride. This leads to an ester structurally related to another ]ii ominent natural product, atropine (133). The product, tropanaerin (134), is described as an iinti.serotonergic agent intended for antimigraine use [34]. 

The muscle fibres of the ciliary bodies are innervated by the mrd or oculomotor nerve. As explained above, when these fibres contract they allow the lens to take up its natural shape. Direct stimulation of the Illrd nerve therefore produces accommodation for near objects. Parasympathomimetic drugs have a similar action, whereas atropine paralyses this effect and so accommodates the lens for seeing distant objects. 

Antimuscarinic drugs block contraction of the iris sphincter and ciliary muscles of the eye produced by ACh. This results in dilation of the pupil (mydriasis) and paralysis of accommodation (cycloplegia), responses that cause photophobia and inability to focus on nearby objects. Ocular effects are produced only after higher parenteral doses. Atropine and scopolamine produce responses lasting several days when applied directly to the eyes. 

There are reports of studies in which short-term tests have been used to determine the genotoxic potential of the anticholinergic compounds 3-quinuclidlnyl benzilate (BZ). atropine, and scopolamine. The objective of this discussion is to evaluate the data available on these compounds, to determine whether they are genotoxic. Such information would aid in the overall assessment of the potential of these drugs to produce long-term adverse health effects. 

Marzulll, F.N., Cope, O.B. 1950 Subjective and Objective Study of Healthy Males Injected Intraoiuscularly With 1, 2, Or 3 mg of Atropine Sulfate. Medical Division Research Report No. 24. 

If a patient has severe dyspnea or vomiting (or retching), he or she may be unable to vocalize, but it can be assumed that the discomfort is severe. Therapy should be titrated against the complaints of dyspnea and objective manifestations such as retching administration of the contents of MARK I kits (or atropine alone) should be continued at intervals until relief is obtained. Seldom are more than two to three MARK I kits required to provide relief. Because eye or head pain is not relieved by MARK I injections, a patient with severe eye or head pain from miosis will complain when he has no other injury that causes more overwhelming discomfort. Topical application of atropine or homatropine is quite effective in relieving this severe pain. 

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