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Hyoscine

Scopolamine, also known as hyoscine, is a tropane alkaloid drug obtained from plants of the Solanaceae family (Nightshade), such as henbane or jimson weed (Datura stramonium). It is part of the secondary metabolites of plants. more...

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It is structurally similar to the neurotransmitter acetylcholine and acts by blocking the muscarinic acetylcholine receptors; it is thus classified as an anticholinergic.

In medicine, it is usually used in the form scopolamine hydrobromide. It can be used as a depressant of the central nervous system, though it can cause delirium in the presence of pain, mydriasis (pupillary dilation), and cycloplegia (paralysis of the eye muscles). When combined with morphine, it produces a tranquilized state known as twilight sleep and amnesia. Although originally used in obstetrics it is now considered dangerous.

It is used in ophthalmology to deliberately cause cycloplegia and mydriasis so that certain diagnostic procedures may be performed. It is also used in the treatment of iridocyclitis.

In otolaryngology it has been used to ease the trauma of intubation.

It is also an antiemetic (prevents vomiting), antivertigo (prevents dizziness), and antispasmodic (reduces smooth muscle contractions; although a derivate called butylscopolamine, that does not cross the BBB, is used preferably). It can be used as a pre-anesthetic sedation, as an antiarrhythmic (preventing irregular heartbeat) during anesthesia, and for the prevention of motion sickness.

The drug is highly toxic and has to be used in minute doses. An overdose can cause delirium, delusions, paralysis, stupor and death.

The use of scopolamine as a truth drug was investigated by various intelligence agencies, including the CIA, during the 50s. see:Project MKULTRA. It was found that, due to the hallucinogenic side effects of the drug, the truth was prone to distortion, and the project was subsequently abandoned.

Scopolamine is used criminally as a date rape drug and as an aid to robbery, the most common act being the clandestine drugging of a victim's drink. It is preferred because it induces retrograde amnesia, or an inability to recall events prior to its administration. Victims of this crime are often admitted to a hospital in police custody, under the assumption that the patient is experiencing a psychotic episode. A telltale sign is a fever accompanied by a lack of sweat.

In Colombia a plant admixture containing scopolamine called Burundanga has been used shamanically for decades. In recent years its criminal use (as outlined above) has become an epidemic. Approximately fifty percent of emergency room admissions for poisoning in Bogotá have been attributed to scopolamine.

Due to its effectiveness against sea-sickness it has become commonly used by scuba divers. However, this has lead to the discovery of another side effect. In deep water, below 50-60 feet, some divers have reported pain in the eyes, but the pain subsides quickly if the diver ascends to a depth of 40 feet or less. No study has been reported regarding the drug's effect on intra-ocular pressure or its effect on the eye's ability to adjust to pressure, so the medication should be used with extra caution among divers who intend to go below 50 feet.

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Scopolamine Hydrobromide 0.2% Nasal Spray
From International Journal of Pharmaceutical Compounding, 1/1/04

METHOD OF PREPARATION

Note: This preparation should be prepared in a laminar airflow hood in a cleanroom (or via isolation barrier technology) by a validated aseptic compounding pharmacist using strict aseptic technique.

1. Calculate the required quantity of each ingredient for the total amount to be prepared.

2. Accurately weigh and/or measure each ingredient.

3. Dissolve the scopolamine hydrobromide, citric acid, dibasic sodium phosphate and sodium chloride in approximately 95 mL of sterile water for injection.

4. Add the benzalkonium chloride 50% solution and mix well.

5. Adjust the pH if necessary, using either additional citric acid or sodium hydroxide 10% aqueous solution to a pH of 6.5.

6. Add sufficient sterile water for injection to volume and mix well.

7. Filter through an appropriate sicrilc 0.2-µm filter into a sterile container.

8. Package and label.

PACKAGING

Package in nasal-spray containers that are tight and light-resistant.1

LABELING

Keep out of reach of children. Use only as directed. For the nose.

STABILITY

A beyond-use date of up to 6 months can be used for this preparation.1

USE

Scopolamine hydrobromide 0.2% nasal spray has been used in the treatment of motion sickness.2

QUALITY CONTROL

Quality-control assessment can include final volume, pH, specific gravity, active-drug assay, color, clarity, physical observation, physical stability (discoloration, foreign materials, gas formation, mold growth), osmolality and sterility.3-5

DISCUSSION

Scopolamine hydrobromide is a naturally occurring tertiary amine antimuscarinic used for the prevention of nausea and vomiting induced by motion. An advantage to this nasal formulation is a rapid onset of action.

Scopolamine hydrobromide (C^sub 17^H^sub 21^NO^sub 4^.HBr.^sub 3^H2O, MW 438.31, hyoscine hydrobromide) occurs as colorless or white crystals or as a white, granular powder. It melts at about 197°C with decomposition. It is odorless and slightly efflorescent in dry air. It is freely soluble in water (l g in 1.5 mL) and soluble in alcohol (l g in 20 mL).1,6

The pH of the solution has been shown to affect the extent and rate of absorption. In a study using solutions prepared at pH levels of 4.0, 7.0 and 9.0, the higher the pH, the faster were the T^sub max^ values and the higher were the C^sub max^ values. The pH 7.0 formulation selected here provides relatively rapid onset of action and good absorption and is in the allowable pH range of the USP injection that goes up to pH 6.5.1,7

Citric acid, available in an anhydrous form (C^sub 6^H^sub 8^O^sub 7^, MW 192.12) or in a monohydrate form (C^sub 6^H^sub 8^O^sub 7^.H2O, MW 210.14), occurs as colorless or translucent crystals, or as a white crystalline. One gram is soluble in less than 1 mL of water and 1.5 mL of ethanol.8

Dibasic sodium phosphate (NaHPO^sub 4^.xH2O) is available in an anhydrous form (MW 141.96) and as a dihydrate (MW 177.99), heptahydrate (MW 268.07) and dodecahydrate (MW 358.14). It is used as a buffering agent and as a sequestering agent. It is very soluble in water but practically insoluble in ethanol.9

Benzalkonium chloride is a bactericidal antimicrobial. Benzalkonium Chloride Solution NF is a clear liquid, colorless or slightly yellow unless a color has been added. Benzalkonium chloride is composed of a mixture of straight-chain homologs.10

REFERENCES

1. US Pharmacopeial Convention, Inc. United States Pharmacopeia 26-National Formulary 21. Rockville, MD:US Pharmacopeial Convention, Inc.; 2003:1668,1939, 2197-2201, 2580.

2. Klocker N, Hanschke W, Toussaint S et al. Scopolamine nasal spray in mot!on sickness: A randomized, controlled, and crossover study for the comparison of two scopolamine nasal sprays with oral dimenhydrinate and placebo. Eur J Pharm Sci 2001;13:227-232.

3. Alien LV Jr. Standard operating procedure for performing physical quality assessment of oral and topical liquids. IJPC 1999;3:146-147.

4. Alien LV Jr. Standard operating procedure for particulate testing for sterile products. IJPC1998;2:78.

5. Alien LV Jr. Standard operating procedure: Quality assessment for injectable solutions. IJPC 1999;3:406-407.

6. McEvoy GK, ed. XlWFS Drug Information-2003. Bethesda, PVID:American Society of Health-System Pharmacists; 2003:1214-1218.

7. Ahmed S, Sileno AP, deMeireles JC et al. Effects of pH and dose on nasal absorption of scopolamine hydrobromide in human subjects. Pharm Res 2000;17:974-977.

8. Amidon GE. Citric acid monohydrate. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Association; 2000:140-142.

9. Kearney AS. Sodium phosphate, dibasic. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Association; 2000:493-495.

10. Kibbe AH. Benzalkonium chloride. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Association; 2000:33-35.

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