Alkaloids

Alkaloids are naturally occurring basic nitrogenous compounds containing

one or more N atoms organized in a heterocyclic ring & have diverse and
important physiological effects on humans and other animals.
Examples of alkaloids are morphine, strychnine, quinine, ephedrine, and
nicotine.

Atropine
Nicotine
2
 Areca/areca nut/betel nut
Biological source: Areca is the dried, ripe seed of Areca catechu Linne of Palmae
family.
Geographical source: The plant is a tall beautiful palm. It is extensively cultivated
in India, Sri Lanka, southern Asia, the East Indies and to some extent East Africa.

Constituents: The total alkaloid content is 0.45%

Arecoline ( 0.20% )
Arecaidine
Guvacine
Guvacoline
Areca also contains
❖ Tannins (15%)
❖ Lipid Arecoline
❖ Volatile oils
❖ Gum
Uses:
Anthelmintic in veterinary practice as vermicide (expel intestinal worms) and
taenifuge (expel tapeworms).
 Belladonna

Biological source:
Belladonna leaf consists of dried leaf and flowering or fruiting tops
of Atropa belladonna Linne or its variety acuminata of Solanaceae
family.
Belladonna root consists of dried roots of Atropa belladonna Linne
of Solanaceae family.

Geographical source:
It is indigenous to central and southern Europe and to Asia Minor
and is cultivated in sunny locations in England, Germany, India and
USA.
Constituents:
Belladonna leaf yields about 0.4% (no less than 0.35%) and
belladonna root yields about 0.6% alkaloids containing
❑ Hyoscyamine
❑ Atropine
❑ Apoatropine
❑ Belladonnine
❑ Scopolamine
❑ Cuscohygrine
 Uses:
i. As mydriatics
ii. As parasympatholytic agent (depress or block parasympathetic
nerve).
Used as adjunct therapy in peptic ulcer and different GIT
disorders because it decreases the flow of most secretions like
saliva, sweat, milk, gastric secretion etc.
Used as spasmolytic agent (able to relieve spasm of smooth
muscle)
ii. Used to control excess motor activity of GIT
iii. Used to control spasm of urinary tract
 Coca/coca leaf

Biological source:
It is the dried leaves of Erythroxylum coca Lamack (Huanuco coca) or
E. truxillence Rusby (Truxillo coca) of Erythroxylaceae family.
The plant is a shrub or small tree attaining a height of about 2m.

Geographical source:
The plant is indigenous to some areas of South America and
cultivated in Bolivia, Peru, Colombia, Indonesia and Sri Lanka.
 Constituents:
Coca contains three basic types of alkaloids

❖ Derivatives of ecgonine
a. Cocaine
b. Cinnamylcocaine
❖ Derivatives of tropine
❖ Derivatives of hygrine

Uses:
❖ Cocaine and its hydrochloride salt are local anesthetic (applied as 1-4%).
❖ When taken internally it is CNS stimulant.
❖ Used as an ingredient in Brompton’s cocktail which is used to control
severe pain associated with terminal cancer
Cinchona/Peruvian bark/cinchona bark

Biological source:
It is the dried bark of the stem or the roots of Cinchona succirubra
Pavon et Klotzsch or its hybrids (red cinchona) and C. ledgeriana Moens et
Trimen, C. calisaya Weddell or hybrids of these with other Cinchona
species (yellow cinchona) of Rubiaceae family.
The plant is a tall tree attaining 15-20m.

Geographical source:
It is indigenous to Ecuador and Peru. It is cultivated in India and
Indonesia. The plant grows at elevation of 1000-3000 meters. The drug is
cultivated in Netherlands and Germany from the bark obtained from
elsewhere.
 Constituents:
Cinchona contains about 25 closely
related alkaloids. The average yield is
6-7%. The alkaloids include
❖ Quinine
❖ Quinidine
❖ Cinchocine
❖ Cinchonidine

Uses:
❑ Cinchona bark and its alkaloids have been used in the treatment of malaria
fever for many years. Quinine is still used in malarial treatment in many parts of
the world.
❑ Quinidine is cardiac depressant and used to prevent auricular (atrial) fibrillation
to coordinate contraction of the auricular (atrial) muscle.
 Opium/gum opium

Biological source:
The air dried milky exudates obtained by incising the unriped
capsules of Papaver somniferum Linne of Papaveraceae family.
The plant poppy is an annual herb with large, showy, solitary
flowers having color of pink to purple.

Geographical source:
The plant is indigenous to Asia Minor. The plant poppy is cultivated
in many countries but legal opium production is not permitted in all
countries.
 Constituents:
More than 30 alkaloids
are found in opium. The Others alkaloids include:
most important are the ❑ Narceine
alkaloids: ❑ Protopine
❑ Morphine (4 to 21%) ❑ Laudanine
❑ Codeine (0.8 to 2.5%) ❑ Codamine
❑ Thebaine (0.5 to 2%) ❑ Cryptopine
❑ Noscapine (4 to 8%) ❑ Lanthopine
❑ Papaverine (0.5 to 2.5%) ❑ Meconidine

Uses:
The drug acts on CNS and first stimulates then depresses nerve response. It serves as
❖ Analgesic
❖ Hypnotic
❖ Narcotic
 Ipecac
Biological source:
It is the dried rhizomes and roots of Cephaelis ipecacuanha A.
Richard (known as Rio ipecac) and C. acuminata (panama ipecac)
of Rubiaceae family.
Geographical source:
The plants are indigenous to central and south America.
C. ipecacuanha is indigenous to Brazil and cultivated there as
well as Malaysia and India.
C. acuminata is indigenous to northern portion Colombia and
also in panama and Nicaragua.
Constituents:
Ipecac yields 2-2.5% alkaloids (not less than 2%) containing 5 alkaloids 3 of
which are
i. Emetine
ii. Cephaeline
iii. Psychotrine

Uses:
i. It is emetic and used in poisoning treatment.
ii. It is also used in amoebic dysentery.
 Ergot/Rye ergot/Secale cornutum

Biological source:
Ergot is obtained on a commercial scale from both parasitic and saprophytic source.
Parasitic source → It is the dried sclerotium (resting body of the ergot fungus given next) of
Claviceps purpurea Tulasne from Clavisipitaceae family which is developed on rye plants
(Secale cerale Linne. Of Graminae family).
Saprophytic source → In this case the ergot alkaloids are obtained from the fermentation
broth in which the mycelium of selected strains of Claviceps paspali Stevens & Hall has been
grown saprophytically in submerged culture.

Geographical source:
Originally source of ergot were Spain, Russia and the Balkan countries. Currently it is
cultivated in Czechoslovakia (former), Germany, Hungary and Switzerland.
Constituents:
Ergot contains no less than 0.15% total alkaloids. It contains a large
number of alkaloids. The most important ones are
i. Ergonovine (principal water soluble alkaloid)
ii. Ergotamine
iii. Ergotoxine (mixture of ergocristine, ergokryptine, ergocornine)
Significant semisynthetic alkaloids include
i. Methylergonovine
ii. Dihydroergotamine
iii. Hydergine
 Rauwolfia serpentine

Biological source:
Rauwolfia serpentina is the dried root of Rauvolfia serpentina
(also Rauwolfia serpentina) Bentham ex Kurz of Apocynaceae family.
The plant is an erect shrub that reaches 1m in height and has
cylindric stems.

Geographical source:
The plant is native to Bangladesh, India, Burma, Sri Lanka,
Vietnam, Malaysia, Indonesia and Philippines. Commercial supply
comes from mostly India and Thailand.
Rauwolfia serpentina contains 3 types of alkaloids,
1. weakly basic indole alkaloids (Principal alkaloids)
❑ reserpine
❑ rescinamine
2. indoline alkaloids of intermediate basicity
❑ ajmaline
❑ isoajmaline
❑ rauwolfinine
3. strong bases
Reserpine
❑ serpentine
❑ serpentinine

Rescinnamine

Uses:
i. Hypotensive.
ii. The chief alkaloid reserpine is antihypertensive and used as tranquilizer drug.
 Pilocarpus

Biological source:
It consists of the leaflets of Pilocarpus jaborandi Holmes, P. microphyllus
Stapf or P. pinatifolius Lamaire of Rutaceae family.
The plants are shrubs.

Geographical source:
It is indigenous to Brazil. Also found in West Indies and Central America.

Constituents:
It contains-
i. Pilocarpine
ii. Isopilocarpine
iii. Pilosine
iv. Isopilosine etc. Pilocarpine
The main constituent is Pilocarpine.

Use:
The principal constituent Pilocarpine is used to treat glaucoma.
 Ephedra

Biological source:
It is the entire plant or the overground portion of Ephedra sinica Stapf of
Gnetaceae family.
The plant is a low, dioecious (male and female reproductive organs on
different plants) practically leafless shrub that attain 60-90 cm height.

Geographical source:
It grows and cultivated in China, India, and Pakistan.

Constituents:
The important constituent is ephedrine.
It may also contain pseudoephedrine and
some other related compounds.

Use:
i. Ephedrine is a potent sympathomimetic (excites the sympathetic
nervosusystem).
ii. It raises blood pressure and causes mydriasis and act as bronchodilator.
 Coffee

Biological source:
It is the dried, ripe seeds of Coffea Arabica Linne of Rubiaceae family.
The plant is small evergreen tree or shrub.

Geographical source:
It is indigenous to Ethiopia and other parts of Eastern Africa and is widely
cultivated in tropical countries like Indonesia and Sri Lanka and central and South
America.

Constituents:
It contains-
i. Caffeine (1-2%)
ii. Trigonelline (0.25%)
iii. Tannin (3-5%)
Caffeine
iv. Sugar (15%)
v. Fatty oil (10-13%)
vi. Protein (10-13%)
Use:
Caffeine is the main principle which is CNS stimulant
 Tea/Thea

Biological source:
Tea is the prepared leaves or leaf buds of Camelia sinensis O. Kuntze of Theaceae family.
It is a shrub or small tree with alternate, evergreen leaves.

Geographical source:
It is indigenous to Eastern Asia. It is extensively cultivated in Bangladesh, China, Japan,
India and Indonesia.

Constituents:
Tea contains-
i. Caffeine (1-4%)
ii. Adenine
iii. Theobromine
iv. Theophylline
v. Xanthine
vi. 15% gallotannic acid
vii. 0.75% of a yellow volatile oil. Caffeine Theophylline

Uses:
i. As beverage
ii. As smooth muscle relaxant attributed to theophylline
iii. Diuretic