Scopolamine toxicity

Generally speaking, alkaloids are more toxic for vertebrates than for invertebrates. The coefficients of the selective toxicity show that alkaloids are very dominantly selective toxins to vertebrates (Table 26). Vertebrate very strong selectivity (<0.01) is observed in such alkaloids as ajmalicine, brucine, ephedrine, ergometrine, harmaline, lupanine, lupinine, scopolamine and... 

Piva, G., Morlacchini, M., Pietri, A., Fusari, A. and Corradi, A. and Piva, A. 1997. Toxicity of dietary scopolamine and hyoscyamine in pigs. Livestock Production Science, 51 29-39. 

Atropine and scopolamine, the main toxic alkaloids of Datura stramonium and Datura ferox, were detected and quantified using HPLC-ESl-MS both in Datura seeds and in the gastric content of a man whose death was ascribed to a fatal heart attack [100]. 

A number of drugs in addition to atropine and scopolamine have antimuscarinic properties. Tbese include tricyclic antidepressants, phenothiazines, and antihistamines. Physostigmine has been used in the treatment of acute toxicity produced by these compounds. However, physostigmine can produce cardiac arrhythmias and other serious toxic effects of its own, and therefore, it should be considered as an antidote only in life-threatening cases of anticholinergic drug overdose. 

Chuang DM, Gao X-M, Paul SM N-methyl-D-aspartate exposure blocks glutamate toxicity in cultured cerebellar granule cells. Mol Pharmacol 42 210-216, 1992 Chugh Y, Saha N, Sankaranarayanan A, et al Enhancement of memory retrieval and attenuation of scopolamine-induced amnesia following administration of S-HTj antagonist ICS 205-930. Pharmacol Toxicol 69 105-106, 1991 Ciraulo DA, Jaffe JH Tricyclic antidepressants in the treatment of depression associated with alcoholism. Clin Psychopharmacol 1 146, 1981 Ciraulo DA, Barnhill JG, Jaffe JH Clinical pharmacokinetics of imipramine and desipramine in alcoholics and normal volunteers. Pharmacol Ther 43 539-548, 1988... 

In the doses usually used, atropine has minimal stimulant effects on the CNS, especially the parasympathetic medullary centers, and a slower, longer-lasting sedative effect on the brain. Scopolamine has more marked central effects, producing drowsiness when given in recommended dosages and amnesia in sensitive individuals. In toxic doses, scopolamine, and to a lesser degree atropine, can cause excitement, agitation, hallucinations, and coma. 

Scopolamine Unknown mechanism in CNS Reduces vertigo, postoperative nausea Prevention of motion sickness and postoperative nausea and vomiting Transdermal patch used for motion sickness IM injection for postoperative use Toxicity Tachycardia, blurred vision, xerostomia, delirium Interactions With other antimuscarinics... 

Datura alba Nees. D. fastuosa L. var. alba Clark D. innoxia Mill. D. metel L. D. stramonium L. D. talula L. Man Tu Luo (Jimsonweed) (leaf, seed, flower) Scopolamine, hyoscyamine, daturodiol, daturolone, hyoscine.33-144 450 This herb is toxic. Spasmolytic, analgesic, antiasthmatic, antirheumatic agent. A general anesthetic for major operations. 

Physochlaina infundibularis Kuang. Hua Shan Seng (root) Hyoscyamine, scopolamine, scopoletin, scoplin.33 This herb is toxic. A cholinergic blocking agent, relaxing effect on bronchial muscles. 

A single oral administration of CSE ameliorated the ethanol-induced impairments of memory. The increase of errors and the decrease in number of learned mice were significantly improved. It had no effect, however, on acquisition or retrieval in normal mice, and did not improve the scopolamine-induced impairment of memory registration in mice in either ST or SD test [12] suggesting that CSE has a specific ameliorating effect on ethanol-induced memory deficiency or the toxic effects of alcohol. 

Albricht (614) found that in cats a combination of morphine with narcotine was a more effective and less toxic analgesic than morphine. In mice (615) the analgesic effect of narcotine was smaller than that of morphine but its toxicity was greater. Bloch et al. (616) administered i.v. a mixture of scopolamine, morphine, and narcotine as an additional analgesic in local anesthesia. For the sedative and analgesic effects of narcotine, see Oelkers and Fiedler (103), Jeske et al. (617), and Krissig (618). 

Many different classes of drugs can produce hallucinations when given in toxic doses (e.g. the anticholinergics, such as atropine and scopolamine), but such symptoms are generally associated with confusion and lack of sensory clarity. As such, hallucinations are a component of a toxic psychosis. 

Anisodine is a natural TTA that represents a derivative of the scopolamine structure mono-hydroxylated at the tropic acid moiety (Fig. 1). Similar to anisodamine it was extracted from Chinese herb Anisodus tanguticus (Maxim.) Pascher and also exhibits al-AR blocking properties and non-specific anticholinergic effects. Accordingly, in China anisodine is used for the therapy of the same indications as described for anisodamine, most often to treat transmissible shock. Toxicity and side effects of anisodine are smaller than those for atropine, scopolamine and anisodamine [5],... 

Besides scopolamine, //-hyoscyamine represents the most toxic TA in Datura plants causing severe to fatal intoxications. Evidence of Datura intoxication was enabled by LC-MS procedures presented in this chapter [11-15, 53, 55, 57],... 

Contraindications Extremely toxic. Even moderate doses could be fatal. Root contains apoatropine which can be lethal even in small amounts, especially when taken orally. Use not recommended. See ATROPINE and SCOPOLAMINE. 

Contraindications Excessive amounts toxic. May cause blacking out and severe headaches. Yaqui Indian brujos claims that smoking or ingestion of flowers will cause insanity. See SCOPOLAMINE and ATROPINE. 

Hyoscyamine (duboisine) and the racemate atropine are mACh-R antagonists and a number of atropine derivatives also have this property, namely anisodamine (6P-hydroxyhyoscyamine), 7 (3-hydroxyhyoscyamine, hyoscine (6,7-epoxyhyoscyamine or scopolamine), benzoyltropein (tropine benzoate), littorine (tropine a-hydroxyphenylpropionate), tigloidine (pseudotropane tiglate) and tropacocaine (pseudotropine benzoate). The further derivatives apoatropine (a-dehydrohyoscyamine) and tropine are very toxic. 

Combining opiates with anticholinergic drugs is a common practice in recreational abuse (SEDA-21, 34). Heroin mixed with hyoscine (scopolamine) is nicknamed polo and point on point. Mixed drug toxicity, with atypical signs and symptoms of opiate abuse, has been reported (70). 

The root was highly prized for its reputed aphrodisiac properties as well as its toxic and therapeutic effects, which presumably made the effort of collection worth while. In the Middle Ages it was often used for poisoning, the root being allowed to ferment to produce a poisonous brew. The infamous Dr Crippen used scopolamine to kiU his wife. Some of the effects of scopolamine are employed to good effect by criminals, as it can... 

Systemic reactions from the topical administration of scopolamine are quite similar to those of atropine. However, CNS toxicity appears to be more common with scopolamine than with atropine. In a series of several hundred patients whose pupils were dilated with 1% scopolamine, seven cases of confiisional psychosis were observed. The reactions included restlessness, confusion, hallucinations, incoherence, violence, amnesia, imcon-sciousness, spastic extremities, vomiting, and urinary incontinence. Others have reported similar acute psychotic reactions in children receiving from 0.6 to 1.8 mg of topically administered scopolamine. However, no deaths have been reported from topical ocular use of scopolamine.Treatment of toxic reactions is the same as that far atropine toxicity. 

Anticholinergic agents are typically used as treatment for anticholinesterase poisoning and vice versa. Riysostlgmlne, tetrahydroamlnoacrldlne, and other cholinesterase Inhibitors were used successfully as antidotes In several dozen subjects. The demonstration of physosclgmlne s effectiveness led to the first controlled study of Its ability to reverse delirium due to scopolamine (31). Riysosclgmlne has been used to overcome anticholinergic toxicity. 

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