21
I- Drugs Containing Alkaloids

I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Embed Size (px)

Citation preview

Page 1: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

I- Drugs Containing Alkaloids

Page 2: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

1- Solanaceous Leavesa- Belladonna leaf (Folium Belladonnae)

"Deadly nightshade"

Origin: the dried leaf and flowering top of Atropa belladonna F. Solanaceae

Morphology: leaves are ovate, yellowish green in colour, petiolate, the lamina is simple, with entire margin, acuminate apex and decurrent base, lateral veins are anastomosing near the margin by a series of arches.

Page 3: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Powder: green to brownish green, showing fragments of:

1. epidermis with wavy walls, striated cuticle, stomata are anisocytic.

2. Non-glandular hairs, multicellular, uniseriate.

3. Clavate hair, glandular with unicellular curved stalk and multicellular club-shaped head.

4. Idioblasts: parenchyma cells contain microsphenoidal crystals of Ca oxalate.

Page 4: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Active constituents: Mydriatic alkaloids: hyoscyamine, atropine, hyoscine

(scopolamine) and belladonnine.

N.B. hyoscyamine (levorotatory) and atropine (racemic) are isomers, atropine is absent in fresh plant but produced during drying by racemization of hyoscyamine.

Uses: "Parasympatholytic"1. Mydriatic2. Antispasmodic (for colic) and reduces hyperacidity, so

used in peptic ulcer.3. Local anaesthetic.4. Sedative to the respiratory nerves to relieve spasmodic

cough.

Page 5: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Chemical tests:

1. Mayer's test: powder + dil. HCl, boil, filter, add Mayer's reagent → white ppt.

2. Vitali's test: boil the powder with dil. HCl, filter, evaporate to dryness, cool add 10 dps. of conc. nitric acid → yellow solution, evaporate to dryness, add 2 drops of alcoholic KOH → violet colour.

Page 6: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

b- Stramonium Leaf(Folium Stramonii)"Thorn Apple Leaf"

Origin: the dried leaves and flowering tops of Datura stramonium" F. Solanaceae

Morphology: Leaves are petiolate showing long petiole hooked when dried, lamina is ovate coarsely dentate with acuminate apex and asymmetric base.

Page 7: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Powder: grayish green to brownish green in colour, showing fragments of:

1. Epidermis with wavy walls, smooth cuticle and anisocytic stomata.

2. Clavate hair.3. Non-glandular hair,

multicellular uniseriate with enlarged basal cell covered with warty cuticle.

4. Cluster crystals of calcium oxalate arranged in crystal layer.

Page 8: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Active constituents:Mydriatic alkaloids: hyoscyamine, atropine,

apoatropine, belladonnine and scopolamine (hyoscine).

Uses:1. relax bronchial muscle in the bronchial spasms

of asthma.2. Scopolamine is effective in the prevention of

nausea and vomiting associated with motion sickness.

3. Scopolamine is used for preanaesthetic sedation.

Chemical tests: as belladonna.

Page 9: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

c- Hyoscyamus Leaves(Folium Hyoscyami)"Egyptian Henbane"

Origin: the dried leaves, smaller stems and flowering tops of "Hyoscyamus muticus" F. Solanaceae

Morphology: Leaves are pale green,

fleshy, ovate lanceolate , broadly dentate margin, acuminate apex and asymmetric base.

Page 10: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Powder: yellowish brown with salty taste, showing fragments of:

1. epidermis with more or less straight walls, smooth cuticle except at the base of the hairs it's striated, anisocytic stomata.

2. Branched glandular hair.

3. Prisms and twin prisms of calcium oxalate.

Page 11: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Active constituents:0.7-1.5% of total alkaloids, most of which are

hyoscyamine, scopolamine.Uses:1. scopolamine is a sedative to the central

nervous system and used as hydrobromide as a sedative in acute maniacal excitement.

2. Combined with purgatives to obviate their griping action.

3. Mydriatic.

Chemical tests: as belladonna.

Page 12: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

2- Jaborandi Leaf(Folium Jaborandi)

Origin: the dried leaflets of various Pilocarpus species, mainly Pilocarpus jaborandi known as Pernambuco Jaborandi and Pilocarpus microphyllus known as Maranham Jaborandi F. Rutaceae

Active constituents:1- Myotic alkaloids: pilocarpine,

isopilocarpine, pilocarpidine and pilosine.

2- Volatile oil

Page 13: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Uses: "Parasympathomimetic"1- Diaphoretic and sialagogue.2- Myotic to hasten the contraction of eye pupil

after mydriatics and for treatment of glaucoma.3- in congestion of the middle and inner ear and in

alopecia.4- antidote for atropine poisoning.

Chemical test:1. Mayer's test: powder + dil. HCl, boil, filter, add

Mayer's reagent → white ppt.2. Helch's test: extract the powder with dil. H2SO4,

filter, add H2O2 + K2Cr2O7, shake with benzene → violet colour in benzene.

Page 14: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

3- Cinchona BarkOrigin: the dried stem and root

bark of Cinchona succirubra and its hybrids known as red Cinchona, C. Ledgeriana and C. calisaya and their hybrids known as yellow Cinchona, C. officinalis and its hybrids known as pale Cinchona F. Rubiaceae.

Morphology: flat, curved and quill, with rough grayish outer surface and longitudinally striated inner surface.

Page 15: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Powder: reddish brown, showing fragments of:

1. cork cells thin walled suberized with brown content.

2. Phloem fibre, long, fusiform, thick wall, lignified with narrow lumen, pointed apex and showing funnel-shaped pits.

3. parenchyma with starch granules.

4. Idioblasts contain microprisms of calcium oxalate.

Page 16: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Active constituents:Alkaloids: quinine, quinidine, cinchonine and cinchonidine in

combination with cinchotannic acid.

Uses:1. Quinine is antimalyrial.2. Quinine is used externally as hair tonic.3. Quinidine is antiarrythmic.4. Cinchonine and cinchonidine are antirhumatic.5. Total alcohol extract is bitter stomachic and tonic.

Chemical test:1. Mayer's test: +ve.2. Extract gives blue fluorescence with oxygenated acids due to

quinine.3. Dry heat test: gives purple fumes due to cinchona red colouring

matter.

Page 17: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

4- Nux vomica Seed(Semen Strychni)

Origin: dried seeds of Strychnos nux-vomica F. Loganiaceae.

Morphology: the seeds are disc-shaped, about 20-25 mm in diameter and 4 mm thick, ash-grey to greenish-grey in colour usually not quite flat being a little depressed on one side.

Page 18: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Powder: yellowish grey to brownish grey with bitter persistent taste, showing fragments of:

1. epidermal cells strongly thickened, lignified extended to form a trichome, each trichome has ten lignified rods.

2. Lignified rods of the trichomes.

3. Cells of endosperm.

Page 19: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Active constituents:Alkaloids: mainly strychnine and brucine.

Uses: 1. bitter stomachic and tonic.2. Increase peristalsis and so used in constipation.3. CNS stimulant.4. In high doses leads to convulsions involves respiratory

muscles and death may occur due to asphyxia.

Chemical test: 1. Powder + nitric acid → orange red colour in the

endosperm cells.2. Powder + sulfovanadic acid → pink to violet colour

especially in endosperm cells.

Page 20: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

5- Pomegranate Bark(Cortex Grantii)

Origin: dried stem and root bark of Punica granatum F. Punicaceae.

Page 21: I- Drugs Containing Alkaloids. 1- Solanaceous Leaves a- Belladonna leaf (Folium Belladonnae) "Deadly nightshade" Origin: the dried leaf and flowering

Active constituents: 1- five alkaloids, four liquid alkaloids:

pelletierine, isopelletierine, methylpelletierine and methylisopelletierine and one solid alkaloid pseudopelletierine.

2- about 22% gallotannic acid.

Uses: anthelmintic for tapeworm.

Chemical test: +ve Mayer's test.