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DRUGS_ACTING_ON_NERVOUS_SYSTEM.pdf (Crude drugs)
1. DRUGS ACTION ON
NERVOUS SYSTEM
P r e p a re d B y : M s . D i v y a K a n o j i y a
A s s i s t a nt P r o f e s s o r i n P h a r m a c o g n o sy
D e p a r t m e nt o f P h a r m a c y, S u m a n d e e p V i d ya p e et h
D e e m e d t o b e U n i v e r s i t y, P i p a r i a , Va d o d a ra .
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2. Content:
1 . H YO S C YA M U S
2 . B E L L A D O N N A
3 . E P H E D R A
4 . O P I U M
5 . T E A L E AV E S
6 . C O F F E E S E E D S
7 . C O C A
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3. Hyoscyamus
Synonyms:
Common Henbane, Hyoscyamus, Hog’s-
bean, Jupiter's bean, Symphonica,
Cassilata, Cassilago, Deus Caballinus.
Biological Source:
Hyoscyamus consists of the dried leaves
and flowering tops of Hyoscyamus niger
Linn., belonging to family Solanaceae. It
contains not less than 0.05% alkaloids,
calculated as hyoscyamine.
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Figure: Hyoscyamusplant
4. Geographical Source:
It is found throughout Central and
Southern Europe and in Western
Asia, extending to India and Siberia.
As a weed of cultivation it now
grows also in North America and
Brazil. Apart from these countries,
it grows in Scotland, England and
Wales and also in Ireland, and has
been found wild in 60 British
countries.
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Figure: Hyoscyamusplant
5. Chemical constituents:
The chief constituent of Henbane leaves is the alkaloid Hyoscyamine, together
with smaller quantities of Atropine and Hyoscine, also known as Scopolamine,
The proportion of alkaloid in the dried drug varies from 0.045% to 0.14%.
Other constituents of Henbane are a glucosidal bitter principle called
hyoscytricin, choline, mucilage, albumin, calcium oxalate and potassium
nitrate.
On incineration, the leaves yield about 12% of ash.
The chief constituent of the seeds is about 0.5–0.6% of alkaloid, consisting of
Hyoscyamine, with a small proportion of Hyoscine, The seeds also contain
about 20% of fixed oil.
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7. Uses:
It is used as antispasmodic, hypnotic and mild diuretic. The leaves have long
been employed as a narcotic medicine.
It is similar in action to belladonna and stramonium, though milder in its
effects.
The drug combines the therapeutic actions of its two alkaloids, hyoscyamine
and hyoscine.
Because of the presence of the former, it tends to check secretion and to relax
spasms of the involuntary muscles, while through the narcotic effects of its
hyoscine it lessens pain and exercises a slight somnifacient action.
It will also relieve pain in cystitis.
It is used to relieve the griping caused by drastic purgatives, and is a common
ingredient of aperient pills, especially those containing aloes and colocynth.
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8. Marketed products:
It is one of the ingredients of the
preparations known as Muscle and
joint rub (Himalaya Drug Company),
Brahmi vati, Sarpagandhaghan Vati
(Dabur) and Zymnet drops (Aimil
Pharmaceuticals).
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9. Synonyms:
Belladonna herb; Belladonna leaf; Deadly night
shade leaves; Banewort; Death’s herb, Dwale;
Poison black cherry; Folia belladonnae.
Biological Source:
Belladonna consists of dried leaves and flowering
tops of Atropa belladonna Linn. (European
Belladonna), belonging to family Solanaceae. It
contains about 0.35% of total alkaloids calculated
as hyoscyamine.
Belladonna
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Figure: Belladonnaplant
10. Geographical Source:
A. belladonna is cultivated in United States, Canada, UK, Germany and India.
Chemical constituents:
Belladonna contains 0.3–1.0% total alkaloids, the prominent base is l-
hyoscyamine and other components are atropine, apoatropine, as choline,
belladonnine, cuscohygrine, chrysa tropic acid, volatile bases, such as
atroscine, leucatropic acid; phytosterol, N-methylpyrroline, homatropine,
hyoscyamine N-oxide, rutin, kaempferol-3-rhamnogalactoside and 7-glu coside,
quercetin-7-glucoside, scopoletin, calcium oxalate, 14% acid soluble ash and
4% acid-insoluble ash.
Addition of ammonia to the alcoholic solution of scopoletin shows blue
florescence. This test is useful to detect Belladonna poisoning.
Atropine is formed by racemization during the extraction process.
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12. Uses:
The drug is used as adjunctive therapy in the treatment of peptic ulcer;
functional digestive disorders, including spastic, mucous and ulcerative
colitis; diarrhoea, diverticula litis and pancreatitis. Due to anticholinergic
property, it is used to control excess motor activity of the gastrointestinal
tract and spasm of the urinary tract.
Belladonna is anticholinergic, narcotic, sedative, diuretic mydriatic and
used as anodyne and to check secretion. Other uses are similar to
Hyoscyamus. It relieves spasm of gut or respiratory tract.
Consumption of Belladonna checks excessive perspiration of patients
suffering from tuberculosis. Belladonna acts as a parasympathetic
depressant.
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13. Marketed products:
It is one of the ingredients of the preparation known as Belladona
plaster (Surgi Pharma) for backache, stiffness of muscles and boil,
swollen joints.
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14. Synonyms: Ma Huang.
Biological Source:
Ephedra consists of the dried aerial parts of Ephedra gerardiana Wall, Ephedra sinica Stapf,
Ephedra equisetina Bunge, Ephedra nebrodensis Tineo and other Ephedra species, belonging to
family Ephadreaceae.
Geographical Source: It is mainly found in China, India, Nepal, Turkey, Pakistan and Bhutan.
Ephedra
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Figure: Ephedra plant
16. Parameter Ephedra
Gerardina
Ephedra Sinica Ephedra
Equisetina
Ephedra
Nebrodensis
Fracture Fibrous in the cortex, pitch
containing brownish powdery
mass.
- Fibrous in the
cortex, pitch
containing
brownish
powdery mass.
Leaves Brownish to
whitish brown,
Scaly, Connate,
Opposite,
Dicussate
A pair of leaves
at the node,
are fused at
the base
Fused leaf
enriching the
node
Brownish to
whitish brown,
Scaly, Connate,
Opposite,
Dicussate
Apex Obtuse Acute &
Recurred
Short Acute
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18. Chemical constituents:
Ephedra contains alkaloids Ephedrine (water-soluble salt of an alkaloid),
Pseudoephedrine (analog of ephedrine), Norpseudoephedrine (An analog
of ephedrine). The leaves and stems of ephedra also contain many
potentially active compounds, such as tannins, saponin, flavone and
volatile oils.
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19. Chemical test:
To the drug (10 mg) in water (1 ml) dilute HCl (0.2 ml), copper sulphate
solution (0.1 ml) and sodium hydroxide solution (2 ml) are added; the
liquid turns violet. On adding solvent ether (2 ml) and shaking vigorously,
the ethereal layer turns purple and the aqueous layer becomes blue.
Uses:
Ephedrine is antiallergenic, antiasthmatic, antispasmodic, decongestant,
cough suppressant, stimulant and vasocon strictor. Pseudoephedrine is
decongestant, cough suppressant and norpseudoephedrine is peripheral
vasodilator used to treat angina. As a whole it is decongestant; it opens
sinuses, increases sweating, dilates bronchioles (antiasthmatic use),
diuretic, CNS stimulant, raises blood pressure, alleviates aches and
rheumatism, alleviates hay fever/colds, etc.
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22. Synonyms: Crude Opium; Raw Opium; Gum Opium; Afim.
Biological Source: Opium is the air dried milky latex obtained by incision
from the unripe capsules of Papaver somniferum Linn, or its variety P. album
Decand., belonging to family Papaveraceae. Opium is required to contain
not less than 10% of morphine and not less than 2.0% of codeine. The
thebaine content is limited to 3%.
Geographical Source: It is mainly found in Turkey, Russia, India, Pakistan,
Iran, Afghanistan, China, Burma, Thailand and Laos. In India, Opium is
cultivated in M.P. (Neemuch) and U.P. for alkaloidal extraction and seed
production.
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23. Cultivation-The cultivation and other aspects of opium are under the control of
government of the respective countries.
→ In India the cultivation, production etc of opium is done under the control of
Narcotic Drugs and Psychotropic Substances Act. 1985.
→ Opium is obtained from poppy plant.
→ Poppy plant is an annual herb about 50 cm to 1.5 meters in height.
→ It bears bluish white or purple colored flowers.
→ Leaves are linear, oblong or ovate oblong with dentate or serrate margin.
→ The different types of varieties viz P. somniferum var album, P. somniferum var
glabrum and P. somniferum var nigrum are described here.
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24. → The plants are cultivated by sowing the seeds in the month of November.
Seeds are sown by mixing them with 3 or 4 parts of sand.
→ The distance maintained between two plants is about 25cm. Soil required
for opium poppy should be fertile, well drained loamy with fine sand and the
pH should be around 7.
→ The thinning of the plants is done periodically and are kept free from weeds
and insects. Farmyard manures and fertilizers are added for better growth
and high quality yield.
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25. Collection and Preparation:
→ After 3-4 months of sowing the plant bears the flowers and these are
converted into capsules. Each plant bears about 5-8 capsules.
→ When the capsules are green or just show a tint of yellow incisions are
made by knives which vary in shape in different countries.
→ In India the incisions are made vertically in afternoon by a instrument
known as "nustur". It penetrates about 2mm into the capsules.
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26. → By this latex exudes out and is partly dried which is scrapped and collected in
next morning by "charpala". This incising operation is repeated on each
capsule three or four times at interval of two or three days.
→ The latex is collected in plastic containers.
→ For next propagation capsules are dried in sun and seeds are collected by
beating. The average yield of opium varies from 20-30 kg per hectare.
→ After collection of opium by the cultivators it is brought to the weightment
centers and from there it is transferred to the factory at Ghazipur (UP) where
the opium is further processed.
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27. Macroscopic Characters:
→ Odour - Strong and Characteristic
→ Taste - Bitter
→ Indian opium - It occurs in cubical pieces, weighing about 900gms.and is dark
brown in colour.
→ It is enclosed in tissue paper and is plastic in nature.
→ It is also exported in 5 kg to 10 kg of blocks. Powder form of the drug is also
available. This opium contains 9-12% of morphine.
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28. → Natural Turkish or European opium-
→ It occurs in more or less rounded or conical, frequently some what
flattened masses weighing between 250gms. to 1kg, and is brown or dark
brown in colour. It is covered with poppy leaves.
→ It is soft when fresh but on keeping it becomes hard and brittle.
→ Manipulated Turkish Opium-
→ It occurs in oval masses with flattened upper and lower surface weighing
usually about 2000gms. and is chocolate-brown in color.
→ It is covered with broken poppy leaves and is moderately plastic when fresh
but it become brittle after some time.
→ This opium contains 10 to 15% of morphine.
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29. → Manipulated European opium - It occurs in elongated masses with rounded
ends weighing about 160 to 500gms. and internally dark brown in colour. It
is hard and brittle.
→ Persian or Iranian opium - It occurs in brick shaped masses and is dark
reddish brown in colour. It is covered with red paper. This opium contain 10
to 12.5% of morphine and is brittle in nature. It is available in 400-500 gms
of masses.
→ Chemical Constituents:
→ Opium contains more then 25 alkaloids which belongs either to
phenanthrene ring system or of benzylisoquinoline ring system.
→ Morphine (10 to 20% ), codeine (0.3 to 4%) and thebaine (0.2 to 0.5%)
belongs to phenanthrene system and are strong bases where as papaverine,
narcotine and narceine belongs to isoquinoline ring system and are weak
bases.
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30. → Morphine (C17 H19 NO3, H₂O) is in colourless crystals and is slightly soluble in
cold water but readily soluble in caustic alkalies or alkaline earths. It is insoluble in
cold ether, chloroform or benzene. Morphine is a powerful hypnotic.
→ Codeine (C18 H21 NO3) or methyl morphine is in rhombic crystals soluble in 80
parts of water and readily soluble in chloroform.
→ Narcotine (CH23 NO) is in rhombic prisms or needles. It is soluble in 160 parts of
ether.
→ The alkaloids of opium are in combination with meconic acid and sulphuric acid.
Other constituents like mucilage, wax, sugar and salts of calcium and magnesium
are present in small quantities. Starch, oxalic acid and tannins are not present in
opium.
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32. → Chemical Tests:
→ 1. Aqueous extract of Opium with FeCl3 solution gives deep reddish
purple colour which persists on addition of HCl. It indicates the
presence of meconic acid.
→ 2. Morphine gives dark violet colour with conc. H2 SO4 and
formaldehyde.
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33. Uses:
1. Opium and morphine have narcotic, analgesic and sedative action and
used to relieve pain, diarrhoea dysentery and cough.
2. Poppy capsules are astringent, somniferous (sleep inducing),
soporific(sleep inducing), sedative (CNS depressants) and narcotic and
used as anodyne and emollient.
3. Codeine is mild sedative and is employed in cough mixtures.
4. Noscapine is not narcotic and has cough suppressant action acting as a
central antitussive drug.
5. Papaverine has smooth muscle relaxant action and is used to cure
muscle spasms. Opium, morphine and the diacetyl derivative heroin,
cause drug addiction.
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34. Biological Source:
It contains the prepared leaves and leaf buds of Thea sinensis (Linne) kuntz.,
belonging to family Theaceae.
Geographical Source:
It is mainly cultivated in India (Assam), Ceylon, Japan and Java.
Tea leaves
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Figure: Twig of Tea plant
Figure: Tea plant
35. Morphology:
Shape: Lanceolate or elliptical
Colour: Dark green
Odour: Characteristics
Taste: Bitter
Apex: Blunt
Base: Tapering
Margin: Shortly serrate
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36. Chemical constituents:
The leaves are a rich source of caffeine (1–5%). It also contains theobromine
and theophylline in minor quanti ties. The colour of tea leaves is due to tannin
(10–20% gallotannic acid).
The agreeable odour is due to presence of a yellow volatile oil. Tea leaves also
contain protein, wax, resin and ash.
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37. Chemical test:
1. Caffeine and other purine alkaloids, gives murexide colour reaction. Caffeine is
taken in a Petri dish to which hydrochloric acid and potassium chlorate are
added and heated to dryness. A purple colour is obtained by exposing the
residue to vapors of dilute ammonia. In addition of fixed alkali the purple colour
disappears.
2. Caffeine also produces white precipitate with tannic acid solution.
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Uses:
It is used as stimulant, astringent and also as diuretic.
39. Synonyms: Coffee bean, coffee seed, Arabica coffee,
Arabian coffee, Abyssinian coffee, Brazilian coffee.
Biological Source:
It is the dried ripe seeds of Coffea arabica Linn,
belonging to family Rubiaceae.
Geographical Source:
It is indigenous to Ethiopia, Brazil, India, Vietnam,
Mexico, Guatemala, Indonesia and Sri Lanka.
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Coffee seeds
Figure: Coffee plant
40. Chemical constituents:
The main constituents of coffee are caffeine, tannin, fixed oil and proteins. It
contains 2–3% caffeine, 3–5% tannins, 13% proteins, 10–15% fixed oils.
In the seeds, caffeine is present as a salt of chlorogenic acid. Also it contains
oil and wax.
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41. Chemical test:
1. Caffeine and other purine alkaloids, gives murexide colour reaction. Caffeine is
taken in a Petridis to which hydrochloric acid and potassium chlorate crystals are
added and heated to dryness. A purple colour is obtained by exposing the residue to
vapors of dilute ammonia. In addition of fixed alkali the purple colour disappears.
2. Caffeine also produces white precipitate with tannic acid solution.
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Uses:
Coffee is widely used as a flavoring agent, as in ice cream, pastries, candies and
liquors. Source of caffeine, dried ripe seeds are used as a stimulant, nervine and
diuretic, acting on CNS, kidneys, heart and muscles. Very valuable in cases of
snake-bite, helping to ward off the terrible coma. It also exerts a soothing action
on the vascular system, preventing a too rapid wasting of the tissues of the body;
these effects are not only due to the volatile oil but to the caffeine it contains.
43. Synonyms: Coca, Cuca, Cocaine, Folium cocae, Peruvian coca, Truxillo coca,
Java coca, Bolivian coca.
Biological Source: Coca consists of the dried leaves of various species of
Eryth mxylon, that is, Erythroxylon coca Lam (Huanco or Bolivian coca) or
Erythroxylon coca var. Spruceanum (Peruvian, Truxillo or Java coca) also
known as Erythroxylon truxillense Rusby., belonging to family
Erythroxylaceae.
Geographical Source: It is mainly found in Bolivia, Peru, Indonesia, Ceylon,
Java and India.
Coca
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45. Morphology:
Erythroxylon coca: leaves are brownish-green in colour, oval, entire and
glabrous, with a bitter taste, 3–8 cm long and 1.5–4 cm wide.
Erythroxylon truxillense: the leaves are much smaller and pale green in
colour, elliptical, entire, glaborous, not glossy, with bitter taste.
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46. Chemical constituents:
Coca leaves contain the alkaloids Cocaine, Annamyl Cocaine, and
Truxilline or Cocamine. Truxillo or Peru vian leaves contain more
alkaloid than the Bolivian, though the latter are preferred for medicinal
purposes. Java Coca contains tropacocaine and four yellow crystalline
glucosides in addition to the other constituents.
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47. Uses:
The actions of Coca depend principally on the alkaloid Cocaine. Cocaine has
stimulant action on CNS. The leaves are extensively chewed to relieve
hunger and fatigue.
Coca alkaloids cause also hallucination. Coca leaves are used as a cerebral
and muscle stimulant, especially during convalescence, to relieve nausea,
vomiting and pains of the stomach without upsetting the digestion.
Cocaine also has local anesthetic action on skin and mucous membrane;
and is used as dental anesthesia and minor local surgery of ophthalmic, ear,
nose and throat. Chemical structure of cocaine has lead to several synthetic
anesthetics like anesthesia, novocain, stovain, etc.
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