Atropine sulphate

The crude alkaloid, together with that regenerated from the mother liquors after the removal of /-hyoscyamine oxalate, is racemised by dissolving 52 parts in 520 volumes of 95% alcohol containing 4.16 parts of sodium hydroxide 71 (loc. cit.). The solution is allowed to stand, at room temperature, until it shows no optical activity, after which it is neutralised with oxalic acid, the alcohol is removed, and the oxalate recrystallised from water until a melting point of 196°-197° is obtained. From this the base is regenerated and converted into the sulphate, as described above in the case of hyoscyamine. 

Atropine sulphate is a white crystalline powder. M.p. 194°. It dissolves in 0.4 part of water, and in 4 parts of 90% alcohol. The aqueous solution is neutral in reaction, and should be optically inactive. 

No colour should be imparted by the salt to sulphuric acid. 

Three cubic centimetres of a 1 in 60 solution should 5deld no precipitate when mixed with 1 c.c. of ammonia solution (10 %) 

Atropine C17H2303N, 289, is prepared by regenerating the base from the pure oxalate and crystallising from aqueous alcohol. 

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A comparison of the activities of these three alkaloids lias been made by Graliam and Gunn using their antagonism to the effects of carbamjd-choline chloride on isolated mammalian intestine. The relative activities found were, atropine sulphate 1 I-hyoscyamine sulphate 2-4 hyoscine hydro bromide 1-5. The results of previous authors are discussed and reasons suggested for some of the differences found. 

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. 

Atropine Sulphate Foreign Alkaloids and Development Products ... 

Irreversible anticholinesterases include the organophosphorus inhibitors and ambenonium, which irreversibly phosphorylate the esteratic site. Such drugs have few clinical uses but have been developed as insecticides and nerve gases. Besides blocking the muscarinic receptors with atropine sulphate in an attempt to reduce the toxic effects that result from an accumulation of acetylcholine, the only specific treatment for organopho-sphate poisoning would appear to be the administration of 2-pyridine aldoxime methiodide, which increases the rate of dissociation of the organophosphate from the esteratic site on the enzyme surface. 

Atropine-, hyoscine- and hyoscyamine-based drugs are developed on a large scale and they also have a variety of clinical purposes. Atropinol, for example, is based on atropine. This drug contains atropine sulphate. Another example is Buscopan, based on hyoscine. Hyoscyamine is used in transdermal plasters. Bella sanol also contains hyoscyamine. The therapeutic use is similar to that of atropine. At least 50 different products from these alkaloids have been developed and introduced on the pharmaceutical market. 

Specific treatment starts with the administration of atropine sulphate, a competitive antagonist of acetylcholine at muscarinic receptors. Sufficient atropine should be given to control hypersecretion and produce tachycardia and pupillary dilation. Very large doses of atropine are required atropine sulphate 2-A mg should be given intravenously every few minutes during the first hour, and then by continuous infusion. Patients may require up to 500 mg intravenously during the first day, and treatment may be needed for days. 

Solution 1 is prepared from exactly 5 ml of 0.4092% w/v atropine sulphate solution and exactly 1 ml of 2.134% w/v homatropine hydrobromide solution. The solution is basified and extracted, the solvent is removed and the residue is treated with 2 ml of BSA and then diluted to 50 ml with ethyl acetate. Solution 3 is prepared from exactly 2 ml of eyedrops and exactly 1 ml of 2.134% w/v homatropine hydrobromide solution. The solution is basified and extracted, the solvent is removed and the residue is treated with 2 ml of BSA and then diluted to 50 ml with ethyl acetate. 

This was the amount originally present in 2 ml of eyedrops therefore percentage of w/v of atropine sulphate in eyedrops... 

Also used for parenteral administration called hypodermic tablets e.g. atropine sulphate tablets. 

Abbara et al. performed simultaneous quantification of different antidotes (diazepam, pralidoxime and atropine) typically co-administered for the therapy of anticholinesterase poisoning (Table 5) [44], PK data resulting from i.m. drug injection by means of a bi-compartemental auto-injector were calculated from human plasma concentrations measured by LC-ESIMS/MS with MRM settings. Administration of 2 mg atropine sulphate yielded plasma peak concentrations of about 4 ng/ml 15 min after injection. 

Fig. 6 Concentration-time profile of antidotal atropine and its enantiomers S- and / -hyoscyamine in plasma of an in vivo swine study. Swine were topically exposed to the nerve agent VR (302 pg/ kg, t0) followed by administration of atropine sulphate (30 pg/kg) and the reactivating oxime HI 6 (12.8 mg/kg) via three i.m. injections into the rear leg at 30 (I), 180 (II) and 330 min (III). Blood samples were collected at distinct time points to generate EDTA plasma. Maximum concentrations were found 4 min after drug administration each. No differences of S- and R-Hyo concentrations were evident underlining similar elimination kinetics for both enantiomers. Data are mean and SD from duplicate measurement using the enantioselective LC-MS/MS approach of John et al. [47,49]. Black circles, total hyo grey circles, S-hyo grey triangles, R-hyo...

Accordingly, Siluk et al. performed chiral chromatographic APCI-MS analysis of human plasma samples obtained from a PK study after administration of atropine sulphate (10 ug/kg as initial i.v. bolus followed by 30 min infusion of 20 pg/kg) [48], Peak plasma concentrations of both enantiomers were not reported in detail but were presumably about 5 ng/ml as deduced from the illustrated concentrationtime profile. The authors found that. S -hyoscyaminc was eliminated slightly faster than //-hyoscyaminc. 

A man was found dead after having ingested an unknown amount of atropine sulphate tablets. The blood contained 0.2 pg/ml and the urine 1.5pg/ml of atropine (B. W. Corbett and A. J. McBay, Bull. int. T55. forens. Toxicol., 1978,14 ), 36-37). 

Preparations of diphenoxylate hydrochloride usually contain subclinical amounts of atropine sulphate in an attempt to prevent abuse by deliberate overdosage. 

Prajmalium Bitartrate 579.0 Loprazolam Mesylate 694.8 Atropine Sulphate... 

Atropine Sulphate Betamethasone Valerate Dextromoramide Tartrate Ergotoxine Ouabain... 

Carpentier, P., Foquin, A., Rondouin, G., LemerNatoli, M., deCroot D.M.G., Lallement, G. (2000). Effects of atropine sulphate on seizure activity and hrain damage produced by soman in guinea-pigs ECoG correlates of neuropathology. 

Culluablne, H., McKee. W.H.E., Creasey, N.H. 1955 The Effects of Atropine Sulphate Upon Healthy Male Subjects. Quart. J. Exp. Physiol. 40 . 309-319. 

Holland, P., White, R.G., Colllnge, B. 1971 Atropine Sulphate Absorption In Humans Following Intra Muscular Injection of a Mixture of The Oxime, P2S, And Atropine. Technical Note No. 68, Chemical Defence Establishment, Porton Down, Salisbury, Wilts. 

Atropine Sulphate ophthalmic ointment Atropine Sulphate ophthalmic solution Atropine Sulphate tablets Glass, 1.8 M x 2mm I.D. 3% G3 /SlAB Nitrogen 225 FID Homatropine Hydrobromide USP (24, p. 179) USP (24, p. 179)... 

Grainger S L, Smith S E 1983 Dose-response relationships of intravenous hyoscine butylbromide and atropine sulphate on heart rate in healthy volunteers. British Journal of Clinical Pharmacology 16 ... 

Convulex valproic acid, co-phenotrope atropine sulphate diphenoxylate, copper sulphate cupric sulfate, corbadrine levonordefrin. 

Diarphen atropine sulphate diphenoxylate. Diarrest codeine. 

LomotiP atropine sulphate diphenoxylate, lomustine [ban, inn, usan] (CCNU CEENU ) Is a lipid-soluble nitrosourea that is an alkylating cytotoxic agent. It can be used as an anticancer agent, particularly for Hodgkin s disease and certain solid tumours. 

NEUROTOXIN constituent of the fly agaric fungus Amanita muscaria and various /nocyfte spp. It is a very potent MUSCARINIC CHOLINOCEPTOR AGONIST with pronounced PARASYMPATHOMIMETIC actions. It is a HYPOTENSIVE, causes bronchoconstriction and stimulates gut, bladder and exocrine glands. Stereoisomers show only a fraction of the activity, and it is valuable as a pharmacological tool in studies on muscarinic receptors. It is very toxic orally, with stimulatory actions on the CNS (atropine sulphate may be used as an antidote). 

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