Atropine Ethanol

Esters of diphenylacetic acids with derivatives of ethanol-amine show mainly the antispasmodic component of the atropine complex of biologic activities. As such they find use in treatment of the resolution of various spastic conditions such as, for example, gastrointestinal spasms. The prototype in this series, adiphenine (47), is obtained by treatment of diphenyl acetyl chloride with diethylaminoethanol. A somewhat more complex basic side chain is accessible by an interesting rearrangement. Reductive amination of furfural (42) results in reduction of the heterocyclic ring as well and formation of the aminomethyltetrahydro-furan (43). Treatment of this ether with hydrogen bromide in acetic acid leads to the hydroxypiperidine (45), possibly by the intermediacy of a carbonium ion such as 44. Acylation of the alcohol with diphenylacetyl chloride gives piperidolate (46). ... 

To a cold solution of 29 g of atropine in 250 ml of acetone a solution of 1 3 g of propane-1,3-sultone in 100 ml of acetone is generally added. The combined solution is left for 48 hours. The white precipitate of fine crystalline needles is separated, washed several times with acetone, and then recrystallized from ethanol. It melts at 220°C. 

By extraction of Solanacean drugs, especially Atropa belladonna, Hyoscyamus niger or other species. On careful extraction L-hyoscyamine is obtained first, which can be racemized to atropine by addition of alkali in ethanolic solution. 

Drug solutions and implantation of osmotic mini-pumps Physostigmine hemisulphate and procyclidine hydrochlorid were obtained from Sigma (St.Louis, U.S.A.), scopolamine hydrobromid from Merck (Darmstadt, Germany), atropine sulphate was obtained from ACF (Amsterdam, The Netherlands), and diazepam from Roche (The Netherlands). HI-6 was made available by the Defence Research Establishment, Suffield, Canada. Soman (O-pinacolyl methylphosphonofluoridate) was synthesised at TNO. Alzet Osmotic Mini-pumps with a constant delivery rate of 0.55 pl/hr (Model 2002, Alza Corp., Palo Alto, USA) were used to deliver PYR, PHY and SCO. The vehicle consisted of 20% propylene glycol, 10% ethanol and 70% water. The pumps were implanted subcutaneously under isoflurane/02 inhalation anesthesia. 

Hypotensive activity. Essential oil, administered intravenously to dogs at a dose of 3 p,L/kg, was active. The ethanol (70%) extract, administered intravenously to dogs at a dose of 75 mg/kg, was active. There was a dip followed by rise in blood pressure° . Ethanol (80%) extract of the aerial parts, at a dose of 10 mg/kg, was not blocked by atropine. The extract did not inhibit pressor response of norepinephrine either . Ethanol (95%) extract of the seed, administered intravenously to dogs at a dose of 10 mg/kg, produced a transient effect that was blocked by atropine ". Petroleum ether fraction chromatographed and fraction eluted with chloroform, administered intravenously to rabbits at a dose of 0.80 mg/kg, was inactive. Methanol extract, administered intravenously to dogs and rabbits at a... 

Drugs may be solid at room temperature (eg, aspirin, atropine), liquid (eg, nicotine, ethanol), or gaseous (eg, nitrous oxide). These factors often determine the best route of administration. The most common routes of administration are described in Chapter 3. The various classes of organic compounds—carbohydrates, proteins, lipids, and their constituents—are all represented in pharmacology. 

Diphenoxylate Hydrochloride. l-(3-Cyano-3,3-diphenylpropyl)-4-phenyl-4-piperidinecarboxylic acid monohydrochlorhydrate [3810-80-8] (Lomotil) (13) is a white, ododess, crystalline powder that melts at 220—226°C. It is soluble in methanol, sparingly soluble in ethanol and acetone, slightly soluble in water and isopropyl alcohol, freely soluble in chloroform, and practically insoluble in ether and hexane. The method of preparation for diphenoxylate hydrochloride is available (11). Diphenoxylate hydrochloride [3810-80-8] (13) is an antidiarrheal that acts through an opiate receptor. It has effects both on propulsive motility and intestinal secretion. Commercial forms are mixed with atropine to discourage abuse. 

Varma, D.R., Ferguson, J.S., Alarie, Y. (1988). Inhibition of methyl isocyanate toxicity in mice by starvation and dexa-methasone but not by sodium thiosulfate, atropine and ethanol. 

Ipratropium Bromide. Ipratropium bromide, 3-(.Thy-droxy-l-oxo-2-phenylpnopoxy)-8-methyI-8-(l-methylethyl,-8-a/oniabicyclo[3.2.l oclanc bromide (Atrovent). is a quaternary ammonium derivative of atropine. It is freely soluM in water and ethanol but insoluble in chloroform and ether. The salt is stable in neutral and acidic solutions but lapiiU hydrolyzed in alkaline solutions. 

Hyoscyamine is readily racemized to atropine when warmed in an ethanolic alkaline solution or by the action of heat (27,54). It racemizes slowly in ethanol (4). 

A quantity of alkaloidal solution or tablets containing between 1.6 to 2.4 mg of atropine is rendered alkaline and extracted with chloroform. The alkaloid is re-extracted from the chloroform with 6% acetic acid and ethanol. An exact aliquot of the resulting extract is transferred into an evaporating dish and evaporated just to dryness on a water bath, fuming nitric acid (0.2 ml) is immediately added to the residue and again evaporated to dryness. The resulting residue is dissolved in acetone (about 3 ml) and made up to volume (10 ml). A 3.0% potassium hydroxide in methanol (0.1 ml) is added and the mixture allowed to stand for 5 minutes. A purple color is developed and the intensity of this color is then measured in a photoelectric absorptiometer. The con-... 

A combined TLC and UV determination method for atropine and hyoscyamine was reported (98). The test solution (150-250 pi) containing 1% of the alkaloid (atropine or hyoscyamine) was applied as 8 cm long bands to 0.25 mm thick layers of silica gel GF2 3 4 plates. The chromatograms were developed for 12 cm with a mixture of CHCI3-acetone-ammonical ethanol (5 4 1) at pH 12.4. 

A rapid and sensetive RIA procedure has been developed for the quantitation of atropine and hyoscyamine from unpurified ethanolic extracts of Atropa belladonna (153). 

The most frequently used color reactions are those developed by Vital and Gerrard and may be briefly described as follows The Vitali Reaction (1). A minute quantity (as little as 0.0001 mg. is sufficient) of solid atropine, Z-hyoscyamine or Z-scopolamine, on a watch glass, is treated with a drop of fuming nitric acid and the liquid evaporated to dryness at 100°. The residue when treated with a drop of freshly prepared solution of ethanolic potassium hydroxide develops a bright purple coloration which slowly fades to a dark red and finally to a colorless liquid. The color sequence can be reproduced by the addition of more potassium hydroxide reagent. 

Initial laboratory data included a blood ethanol of 190 ing/dL, hut electrolytes were normal. An electrocardiogram revealed atrial fibrillation with a high degree of atrioventricular block The ventricular rate did not exceed 50/min. Atropine had no effect on the ventricular rate and a transvenous pacing catheter iros therefore inserted, with ventricular pacing instituted at 60/min. 

Psilocybin, mescaline, and LSD have similar central (via serotonergic systems) and peripheral (sympathomimetic) effects. None of these hallucinogenic drugs have been shown to have teratogenic potential. Contrast this with the established potential for teratogenicity or other fetal toxicity with abuse of ethanol, amphetamines, and cocaine. Unlike most hallucinogens, phencyclidine acts as a positive reinforcer of self-administration in animals. Scopolamine is not a positive reinforcer but does exert atropine-like effects. The answer is (D). 

Amyl nitrate, sodium nitrate, sodium thiosulfate Atropine, pralidoximine IV ethanol, hemodialysis Oxygen, methylene blue Oxygen... 

Cyanide antidotes such as sodium nitrite and sodium thiosulfate were not effective in combating methyl isocyanate poisoning (Bucher et al. 1987a,b Vijayaraghavan and Kaushik 1987). Atropine and ethanol were also ineffective. 

CiiHi NjOa, Mr 208.26, oily liquid or crystals, mp. 34 °C (as hydrochloride 193-205 °C, nitrate I74°C), bp. 260°C (0.7 kPa), [a] > +106° (HjO), soluble in water, ethanol, chloroform forms well crystallizing salts with acids. P. is the main alkaloid of the South American jaborandi tree (Pilocarpus jaborandi). It is isolated from the leaves. P. is also easily accessible by synthesis and is used as its salts in medicine as a cholinergic parasympathicomimetic, miotic (for glaucoma) agent and as an atropine antagonist it is also used in veterinary medicine for colics and constipation. Detection by means of Helch s reaction. Pilocarpus species contain further imidazole alkaloids (see table). 

Titrate an aliquot portion of the ethanolic solution with 0-02N hydrochloric acid using methyl red as indicator and from this titre calculate the total alkaloidal content. To the titration liquid add the exact equivalent of sodium bicarbonate and shake out with 15 ml quantities of chloroform, three portions being found sufficient for a titre of 10 ml. Remove the solvent, titrate the residue and continue the process until two consecutive titrations differ by not more than 0 2 ml of 0 02N acid from this figure calculate the hyoscine. 1 ml 0-02N = 0 006064 g. The difference between total alkaloidal content and the sum of the hyoscyamine and hyoscine gives the amount of atropine present. 

Dissolve about 01 g in 40 ml of water and add 20 ml of dilute sulphuric acid followed by 30 ml of 1 per cent ammonium reineckate solution. Mix and allow to stand for thirty minutes. Filter through a tared Gooch crucible and wash with water saturated with atropine metho-reineckate until free from sulphate. Wash with 3 ml of water followed by 2 ml of 95 per cent ethanol and dry over P2O5 in vacuo to constant weight. 1 g of residue = 0 5884 g C18H26O6N2. 

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