PCOG211Lec FINALS 1

PHARMACOGNOSY AND PLANT CHEMISTRY LECTURE - FINALS 2nd Semester
Instructor: Ms. Maria Suzette Agluba, RPh A.Y. 2022-2023
ARAOJO| CUENCA | GERMAR | IMPERIAL
ALKALOIDS PART 1
Alkaloids ★ Labiatae (Mint Family)
➔ Definition: the term “alkaloid (” alkali- like) is commonly

used to designate basic heterocyclic nitrogenous
compounds of plant origin that are physiologically
active.
➔ DISTRIBUTION AND OCCURENCE
★ Rare in lower plants.
★ Dicots are more rich in
★ Alkaloids than Monocots.
➔ CHEMICAL PROPERTIES
★ Nitrogen
○ Primary amines R NH- 2 (e.g. Norephedrine)
○ Secondary amines R2 -NH (e.g. Ephedrine)
○ Tertiary amines R3 -N (e.g. Atropine)
○ Quaternary ammonium salts R4 N (e.g
d-Tubocurarine)
★ Basicity
○ R2 -NH > R-NH2 > R3 -N
➔ FAMILIES RICH IN ALKALOIDS
○ Saturated hexacyclic amines is more basic than
★ Apocynaceae (Dogbane Family)
aromatic amines
➔ NOMENCLATURE
★ The genus of the plant; Atropine (Atropa belladona)
★ The plant species; Cocaine (Erythroxylon coca).
★ The common name; Ergotamine (ergot).
★ The name of the discoverer; Pelletierine (Pelletier).
★ The physiological action; Emetine (emetic)
★ A prominent physical character, Hygrine that is
★ Rubiaceae (Coffee Family, Bedstraw Family)
hygroscopic
➔ SOLUBILITY
★ Both alkaloidal bases and their salts are soluble in
alcohol.
★ Generally, the bases are soluble in organic solvents
and insoluble in water
★ Salts are usually soluble in water and, insoluble or
sparingly soluble in organic solvents.
★ Solanaceae (Nightshades) ★ Exceptions:
○ Salts insoluble in water: quinine monosulphate.
○ Salts soluble in organic solvents: lobeline and
apoatropine hydrochlorides are soluble in
chloroform.
★ Papaveraceae (Poppy Family)
➔ FAMILIES FREE IN ALKALOIDS

★ Rosaceae (Rose Family) ○ Most of the alkaloids are crystalline solids,
although a few are amorphous.
○ An additional few, coniine, nicotine, and
sparteine, which lack oxygen in their molecules,
are liquids.
○ Alkaloidal salts are crystalline- useful means in
microscopic identification.
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Second Metabolites ➔ Isoquinoline (e.g. papaverine)
➔ Indole (e.g.ergometrine)
➔ Imidazole (e.g. pilocarpine)
➔ MAJOR TYPES OF ALKALOIDS, THEIR AMINO

ACID PRECURSORS, AND WELL-KNOWN
EXAMPLES OF EACH TYPE
➔ Purine (e.g. caffeine)
➔ Steroidal (e.g. Solanum and Veratrum alkaloids)

➔ CLASSIFICATION BASED ON THE RING
STRUCTURE OR NUCLEUS OF THE CHIEF
ALKALOID GROUP IN THE PLANT DRUG
➔ Pyridine and piperidine (e.g. lobeline, nicotine)
➔ Alkaloidal Amines
➔ Tropane (e.g. Atropine)
➔ Quinoline (e.g.quinine and quinidine) ➔ The amino acids that most often serve as
alkaloidal precursors include
★ Phenylalanine,
★ Tyrosine,
★ Tryptophan,
★ Histidine,
★ Anthranilic Acid,
★ Lysine,
★ Ornithine
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➔ Biosynthesis - Nicotine and Tropane Alkaloids ➔ Areca is mixed with lime, the leaves of Piper betle
Linne’
➔ The mixture is used as a stimulant masticatory in India
and the East Indies.
➔ "punsupari.”
➔ Taenicide
➔ Question: Nganga is consumed, why?
★ Stimulant Masticatory
Areca Alkaloids
➔ Arecoline (arecaidine methyl ester)- the most abundant
and physiologically most active alkaloid, is a liquid.
➔ Arecaidine (N-methyl guvacine)
➔ Guvacine (tetrahydronicotinic acid)
➔ Guvacoline (guvacine methyl ester).
➔ The total alkaloid content can reach 0.45%.
➔ USE AND DOSE
Pyridine
★ Areca is classified as an anthelmintic in veterinary
➔ A tertiary base practice and is employed as a vermicide and
➔ Upon reduction it is converted into the secondary base, taenifuge. The usual dose in dogs is 2 to 4 g; in
piperidine sheep, 4 to 8 g, based on the weight of the animal
➔ 3 subgroups
Lobelia or Indian Tobacco
★ (1) derivatives of piperidine, including lobeline from
lobelia ➔ Consists of the dried leaves and tops of Lobelia inflata
★ (2) derivatives of nicotinic acid, including from Linne’ (Fam. Lobeliaceae).
areca ➔ Its emetic properties were first observed in 1785, and
★ (3) derivatives of both pyridine and pyrrolidine, the drug was introduced into medicine in 1807.
including nicotine from tobacco. ➔ The drug contains 14 alkaloids, of which lobeline is the
➔ The important alkaloidal drugs and their alkaloids that major and most important, a pungent volatile oil, resin,
are classified in this group are areca, arecoline lipids, and gum.
hydrobromide, lobelia, lobeline, and nicotine. ➔ Lobeline, (-)-lobeline, or alpha lobeline (to distinguish it
from a mixture of the lobelia alkaloids formerly
Nicotine
designated as lobeline)
➔ The Swiss chemist Trier proposed that nicotine was ➔ Emetic Property
biosynthesized from nicotinic acid and proline. ➔ Uses and Dose
➔ Nicotine is primarily a product of root metabolism, but ★ Lobeline produces similar, but weaker,
the formation of small amounts, as well as subsequent pharmacologic effects to those of nicotine on the
reactions such as the demethylation of nicotine, can peripheral circulation, neuromuscular junctions,
occur in the leaves of plants. and the central nervous system. For this reason, a
➔ USE 2.0-mg dose of lobeline sulfate is incorporated in
★ Nicotine is bound to an ion exchange resin in a tablets or lozenges that are intended to aid in
chewing gum base as a temporary aid to the breaking the tobacco habit (smoking deterrents).
cigarette smoker seeking to give up smoking.
Lobeline and Nicotine
➔ BRAND: Nicorette
Areca
➔ Areca, areca nut, or betel nut is the dried, ripe seed of
Areca catechu Linne (Fam. Palmae).
➔ Betel nut
➔ India is a major producer of areca, but its production is Tropane Alkaloids
mostly consumed domestically. Tropane
➔ Is a dicyclic compound formed by the condensation of
a pyrrolidine precursor (ornithine) with 3
acetate-derived carbon atoms. Both pyrrolidine and
piperidine ring systems can be discerned in the
molecule. tropine
➔ Its esterification with (-)-tropic acid yields hyoscyamine
(tropine tropate), which may be racemized to form
atropine.
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➔ Talumpunay ★ Control Spasm of the Urinary Tract
★ Control Motor effect at GIT
★ Antidiarrheal
★ Parasympathetic Action has a drying effect on
mucous secretion.
➔ Belladonna leaf is commonly administered in the form
of the tincture (30 mg alkaloids/100 ml) or the extract
(1.25 g alkaloids/100 g).
★ Angel’s trumpet ➔ The usual dose is 0.6 to 1.0 ml of the tincture or 15 mg
★ Datura metel (Solanaceae) of the extract, 3 or 4 times a day.
★ Talong punai ➔ Most of the alkaloids are derived from Egyptian
Synthesis of Hyoscyamine and Atropine henbane (Hyoscyamus muticus Linne).
➔ T. Smith and H. Smith of Edinburgh, Scotland,
developed a purely synthetic process for the formation
of atropine starting with tropine. Although this process
was successful, it was not economical; at present,
atropine and the related alkaloids are still produced
from Duboisia and from Hyoscyamus muticus
Solanaceous Alkaloids
Solanaceous Alkaloids
➔ Atropine
➔ Scopolamine
➔ Hyoscyamus
➔ Stramonium
➔ Hyoscyamine
Tropine Derivatives
➔ The principal alkaloids of this group are (-) -
➔ Because of the commercial importance of hyoscyamine; atropine [(±)-hyoscyamine]; scopolamine
hyoscyamine and scopolamine, investigation of their (also known as hyoscine); and the anhydride of
biosynthesis has been extensive, especially in Datura atropine (apoatropine) and its stereoisomer,
species. belladonnine. These are tropine derivatives and esters
➔ Phenylalanine is the precursor of tropic acid. ➔ Atropine and scopolamine are competitive with
➔ Esterification of tropic acid with tropine produces acetylcholine at the postganglionic synapse
hyoscyamine. (muscarinic site) of the parasympathetic nervous
system
Belladonna
➔ Atropine Toxicity
➔ Belladonna leaf, belladonna herb, or deadly ★ Mouth Dryness
nightshade leaf consists of the dried leaf and flowering ★ Difficulty in Urination
or fruiting top of Atropa belladonna Linne’ or of its ★ Eye Pain and Light Sensitivity
variety acuminata Royle ex Lindley (Fam. Solanaceae)
Hyoscyamine
➔ The leaf yields alkaloids in concentrations ranging up
to more than 1%. About three fourths of the isolated ➔ is the tropine ester of (-)tropic acid and is asymmetric
alkaloid mixture is ( - )-hyoscyamine; the remainder is and accounts for the natural occurrence of the optical
atropine. isomer.
➔ Atropine is formed by racemization during the ➔ Hyoscyamine sulfate
extraction process. Small but varying amounts of other ★ is the sulfate of an alkaloid usually obtained from
bases are found in the root but not in the leaf. These species of Hyoscyamus Linne or other genera of
include apoatropine, belladonnine, cuscohygrine, and Solanaceae.
scopolamine. ★ It is extremely poisonous.
➔ Hyoscyamine is an Anticholinergic, like Atropine. What
are its uses in the GIT?
★ ANSWER: Control of gastric secretion, visceral
spasm, hypermotility in spastic colitis, pylorospasm
and cramps.
➔ Hyoscyamine is an anticholinergic drug. To what
➔ Belladonna is used as a Parasympathetic Depressant. symptoms of Parkinsonism can it help?
What are the different indications of Belladonna? ★ ANSWER: Tremors, rigidity, Sialorrhea and
★ ANSWER: as Spasmolytic Agent, for digestive associated hyperhidrosis
disorders, ulcerative colitis, diarrhea, diverticulitis, ➔ When used for Parkinsonism to control tremors and
pancreatitis rigidity,
➔ Parasympathetic Depressant is also known as
Anticholinergic Effect
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➔ The usual dose, oral or sublingual, is 125 to 250 ug, 3 ★ At usual therapeutic doses, "scopolamine is a
or 4 times a day. The parenteral dose is 250 to 500 ug central nervous system depressant, whereas
given subcutaneously, intramuscularly, or atropine is a stimulant. For this reason,
intravenously, 3 or 4 times a day, as needed. scopolamine hydrobromide is used for
Atropine preanesthetic sedation and for obstetric amnesia in
conjunction with analgesics; it is also employed for
➔ It is optically inactive but usually contains some calming delirium. It is administered subcutaneously
levorotatory hyoscyamine, the limit of which produces or intramuscularly in a single dose of 320 to
an angular rotation not to exceed - 0.70°. 650mg.
➔ Atropine sulfate ★ Effective in the prevention of nausea and vomiting
★ Occurs as colorless crystals or as a white, associated with motion sickness.
crystalline powder. ★ Has Anticholinergic Effect
★ It is extremely poisonous. ○ It is applied as the free base in a transdermal
★ It efflorescence in dry air, is slowly affected by light, system behind the ear at least 4 hours before
and is an anticholinergic. the antiemetic effect is required. The
➔ Atropine is an anticholinergic. In surgery Atropine is scopolamine is gradually released from an
necessary, why? adhesive matrix of mineral oil and
★ Antisialogogue, to control bronchial, nasal, polyisobutylene. A continuous controlled
pharyngeal, and salivary secretions release of scopolamine flows from the drug
★ This is given when reduction in pulse range and reservoir through a rate-controlling membrane
cessation of cardiac action are attributable to to maintain a constant plasma level for 3 days.
increased vagal activity
➔ Atropine as an Anticholinergic Hyoscyamus or Henbane
★ It can be given in cases of Pylorospasm and other ➔ Is the dried leaf, with or without the stem and flowering
spastic conditions of the gastrointestinal tract and or fruiting top, of Hyoscyamus niger Linne (Fam.
for ureteral and biliary colic when administered Solanaceae)
concomitantly with morphine. The usual dose, ➔ Contains not less than 0.04% of the alkaloids of
tablets, is 300 to 600 ug, 3 or 4 times a day; hyoscyamus.
injection, 400 to 600 ug, 4 to 6 times a day ➔ USE
★ An antidote to cholinesterase inhibitors ★ Hyoscyamus is a parasympatholytic, but the crude
○ Intravenously, 2 to 4 mg initially, followed by 2 drug is rarely employed in medicine today.
mg intramuscularly, repeated every 5 to 10 Stramonium, Jimson Weed, or Jamestown Weed
minutes until muscarinic symptoms disappear
or signs of atropine toxicity appear; topically to ➔ Consists of the dried leaf and flowering or fruiting tops
the conjunctiva, 0.1 ml of a 0.5 to 4% solution, 3 with branches of Datura stramonium Linne or of its
times a day. variety tatula (Linne) Torrey (Fam. Solanaceae).
➔ Powdered stramonium is an ingredient in preparations
Scopolamine or Hyoscine that are intended to burn.
➔ Is an alkaloid that is particularly abundant in Datura ➔ The resultant vapor is inhaled for the relief of asthma.
fastuosa var. alba and in D. metel. These so-called asthma powders were widely sold on
➔ It is an ester that, upon hydrolysis, yields tropic acid an over-the counter basis until thrillseekers began to
and scopoline, a base resembling tropine. ingest them in order to become intoxicated. In 1968,
➔ It occurs as an almost colorless, syrupy liquid from its the Food and Drug Administration placed
chloroformic solution and as colorless crystals from its stramonium-containing asthma powders in the
ether solution. It is levorotatory. prescription-drug category
➔ Scopolamine hydrobromide or hyoscine hydrobromide ➔ What is the similarity of Stramonium and Belladonna?
➔ Occurs as colorless or white crystals or as a white, ★ Anticholinergic Effect
granular powder that is odorless and slightly ➔ Stramonium Seed
efflorescent in dry air. ★ Is the ripe seed of D. stramonium.
➔ It is extremely poisonous. ★ Stramonium is generally regarded as a noxious
➔ TALUMPUNAY weed and has frequently caused poisoning in
★ Yields tropane alkaloids such as hyoscyamine, children when seeds were ingested. The chief toxic
scopolamine, anisodamine and anisodine. symptoms are those of atropine poisoning: dilated
★ Flowers - Scopolamine, 0.5%; hyoscyamine, pupils, impaired vision, dryness of the skin and
0.04%; atropine, 0.01%. secretions, extreme thirst, hallucinations, and loss
★ Leaves: Total alkaloid content is 0.426%, mainly as of consciousness.
atropine and small amount of hyoscyamine. ★ These effects are collectively called?
★ Seeds contain 0.426% alkaloid, mainly ○ Anticholinergic Effects or Atropine-like toxicity
hyoscyamine. Other Solanaceous Alkaloids
★ Roots: contain 0.35% hyoscyamine
➔ USE AND DOSE ➔ Pituri or Australian Tobacco
★ Scopolamine hydrobromide is classified as an ➔ Duboisia
anticholinergic. ➔ Coca
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➔ Cocaine
➔ Withania
➔ Huanuco Coca
➔ Truxillo Coca
➔ Mandragora
Withania
Huanuco Coca
➔ Is the dried root of Withania somnifera Dunal
➔ Contains 0.5 to 1% of ester alkaloids, derivatives of
(Fam.Solanaceae)
tropine and ecgonine, of which cocaine constitutes the
➔ Studies have shown that withania, which is closely
major part. Cuscohygrine is the principal nonester
related botanically to belladonna and hyoscyamus,
alkaloid in the leaf.
contains about a dozen biochemically heterogeneous
alkaloids.
➔ The principle responsible for the sedative action of the
drug has not yet been determined
➔ What is the action of Withania?
Duboisia
➔ Consists of the dried leaves of Duboisia myoporoides
R. Brown (Fam. Solanaceae) Truxillo Coca
➔ The drug contains (-)-hyoscyamine, scopolamine, and ➔ Has a somewhat lower content of ester alkaloids, but a
a number of related alkaloids, in addition to small much higher percentage (up to 75%) of this quantity is
amounts of nicotine and nornicotine. cocaine.
➔ Duboisia currently is a chief source of atropine, the ➔ The shrub was known as "The Divine Plant of the
racemic mixture of the isomers of hyoscyamine, which Incas." Monardes published an extensive article on the
is formed during the extraction process. drug in 1569.
Pituri or Australian Tobacco ➔ The natives chew the leaf, either as such or mixed with
lime and are thus able to travel great distances without
➔ Is the leaf of D. hopwoodii F. von Mueller and is used experiencing fatigue and without any but the most
in Australia like tobacco. It contains nicotine and meager food rations
nornicotine.
➔ Mandragora or European mandrake is the root of Cocaine
Mandragora officinarum Linne contains hyoscyamine, ➔ Is an alkaloid obtained from the leaves of Erythroxylum
scopolamine, and mandragorine. coca and its varieties. As explained subsequently,
➔ This drug and its method of collection are the subjects much of the alkaloid is actually prepared by
of many superstitions and forklore tales. It should not semi-synthesis from plant-derived ecgonine.
be confused with the resin-containing American ➔ When hydrolyzed, it splits into ecgonine, benzoic acid,
mandrake (podophyllum) and methyl alcohol.
Coca or Coca Leaves ➔ Cinnamylcocaine splits into ecgonine, methyl alcohol,
and cinnamic acid, whereas a- and (3-truxilline split
➔ The dried leaves of Erythroxylum coca Huanuco coca, into ecgonine, methyl alcohol, and a- and (3-trux-illic
➔ or of E. truxillense rusby, known commercially as acids. (The truxillic acids are isomeric dicinnamic
Truxillo coca (Fam. Erythroxylaceae). acids.)
➔ Three varieties yielding the commercial drug may be
distinguished:
1. var. coca (= E. coca Lamarck sensu stricto), yields
Huanuco (Bolivian) coca.
2. var. spruceanum Bruck (= E. truxillense Rusby)
yields Truxillo (Peruvian) coca.
3. var. novogranatense (Morris) Hieron yields a type
of Truxillo coca from Colombia. ➔ Cocaine is the methyl ester of bezoylecgonine
➔ Cocaine was first isolated in 1860, but until 1884, coca
was considered only as an inferior substitute for tea. In
that year, Koller discovered its local anesthetic
properties.
➔ Coca leaves contain 3 basic types of alkaloids
➔ Derivatives of ecgonine (cocaine, cinnamylcocaine, a-
and Rtruxilline) ➔ Cocaine has multiple central and peripheral nervous
➔ Tropine (tropacocaine, valerine) system actions. Over most of its effective dose range,
➔ Hygrine (hygroline, cuscohygrine). it is a psychomotor stimulant with a strong abuse
★ Only the ecgonine derivatives are commercially potential.
important.
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➔ The action responsible for the rewarding property, and ➔ Biosynthesis of Cinchona Alkaloids
hence the abuse liability, is through a prolongation of
dopamine in the synapse by blocking the dopamine
reuptake mechanism.
➔ Cocaine and cocaine hydrochloride, as agents of
abuse, are generally inhaled or sniffed and are rapidly
absorbed across the pharyngeal mucosa, resulting in
cerebral stimulation and euphoria.
➔ Inhalation of the vapors of alkaloidal cocaine, known
as "free-basing," has become a popular practice
because of the rapidity of onset and the intensity of the
euphoric experience.
➔ Cocaine Hydrochloride
★ Is the hydrochloride of the alkaloid cocaine. It ➔ Biosynthesis of Quinoline Alkaloids
occurs as colorless crystals or as a white, ★ Alkaloid Precursors. Tryptophan is a precursor of
crystalline powder. quinine in cinchona. Because quinine is the first
★ USES secondary compound derived from this amino acid
○ Cocaine hydrochloride is a local anesthetic. It is to be considered, it is convenient to review the
applied topically to mucous membrane as a 1 to biosynthesis of tryptophan.
4% solution.
★ Cocaine hydrochloride is an ingredient in
Brompton's cocktail, which is widely used to control
severe pain associated with terminal cancer.
Because of its CNS stimulant properties, cocaine
counteracts the narcotic-induced sedation and
respiratory depression associated with the narcotic ➔ Biosynthesis of Quinine
analgesic ingredient (morphine or methadone)
used in the cocktail. It also potentiates the
analgesic effect
★ Morphine/ Methadone + Cocaine HCl + Alcohol =
Brompton’s Cocktail
➔ Is this Cocaine free-base or Cocaine salt?
★ Free-base. The reason for converting cocaine
hydrochloride to the free amine is that the latter
substance volatilizes at about 98°C whereas the
salt volatilizes at 195°C, a temperature at which
some of the cocaine is decomposed
➔ It causes such pleasurable effects as reduced fatigue,
increased mental clarity, and a rush of energy the more
one takes cocaine, the less one feels its pleasurable ★ The biosynthetic pathway leading to, tryptophan in
effect which causes the addict to take higher and higher plants is unknown; however, it has been
higher doses of cocaine in an attempt to recapture the elucidated in microorganisms using auxotrophic
intensity of that initial high. mutants of Escherichia coli and Enterobacter
Quinoline or Cinchona Alkaloids aerogenes that required tryptophan for growth.
➔ Biosynthetic Pathway Leading to Tryptophan in
➔ Quinine Higher Plants is Still Unknown
★ Quinine Sulfate
➔ Cuprea Bark (Quinidine)
★ Quinidine Sulfate
★ Quinidine Gluconate
★ Quinidine Polygalacturonate
➔ Quinidine
Quinoline Alkaloids
➔ Alkaloids containing quinoline as their basic nucleus
include those obtained from cinchona (quinine,
quinidine, cinchonine, and cinchonidine)
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Cinchona ★ It is available in sustained release tablets.
➔ Quinidine polygalacturonate
➔ Cinchona, cinchona bark, or Peruvian bark
★ Affords controlled and more uniform absorption
➔ Calisaya bark or yellow bark
through the intestinal mucosa than does quinidine
➔ Is the dried bark of the stem or of the root of Cinchona
sulfate.
succirubra Pavon et Klotzsch, or its hybrids, known in
★ In addition, it produces a lower incidence of
commerce as red cinchona; or of C. ledgeriana
gastrointestinal irritation.
(Howard) Moens et Trimen, C. calisaya Weddell, or
➔ Quinine
hybrids of these with other species of Cinchona, known
★ It occurs as white, odorless, bulky, bitter crystals or
in commerce as calisaya bark or yellow cinchona
as a crystalline powder. It darkens when exposed
(Fam. Rubiaceae).
to light and efflorescence in dry air.
➔ Quinine, quinidine, cinchonine, and cinchonidine
★ It is freely soluble in alcohol, ether, and chloroform
➔ What is the similarity of these fruits to Cinchona Bark?
but slightly soluble in water.
★ They are acted upon by Oxidase. This enzyme is
➔ Quinine sulfate
also responsible for the discoloration of fruits when
★ Is the sulfate of an alkaloid obtained from the bark
cut.
of Cinchona species.
➔ Quinine fluoresces under UV light
★ It occurs as white, odorless, bitter, fine, needlelike
crystals that are usually lusterless.
★ It becomes brownish when exposed to light.
Quinine
➔ Quinine has a skeletal muscle relaxant effect, affecting
the distribution of calcium within the muscle fiber.
➔ FOR nocturnal recumbency leg cramps in a dose of
260 to 300 mg at bedtime.
➔ Daily doses of 0.2 to 0.4 g as a tonic or as an
➔ Cinchona Alkaloids analgesic in the treatment of colds were used
★ Quinidine extensively in the past.
○ Is a stereoisomer of quinine and is present in ➔ One of the sources of Quinine – Cinchona succirubra
cinchona barks to the extent of 0.25 to 1.25%. (Rubiaceae)
○ It depresses myocardial excitability, conduction ➔ Use
velocity, and, to a lesser extent, contractility. ★ The drug is an antimalarial and once was the only
★ Quinidine Sulfate agent available to treat it.
○ Is the sulfate of an alkaloid obtained from ○ Quinine's antimalarial action is believed to be
various species of Cinchona and their hybrids the intercalation of the quinoline moiety into the
and from Remijia pedunculata, or prepared DNA of the Plasmodium parasite, thereby
from quinine. reducing the effectiveness of DNA to act as a
○ It is readily soluble in water, alcohol, methanol, template.
and chloroform. ➔ Anopheles freeborni mosquito – intermediate host and
vector for Plasmodium sp.
Quinidine
★ Recently, it has regained considerable importance
➔ USE AND DOSE in the treatment of chloroquine-resistant falciparum
★ Quinidine is used to treat various cardiac malaria in combination with pyrimethamine and
arrhythmias such as premature atrial, AV junctional, sulfadiazine or tetracycline.
and ventricular contractions; atrial and ventricular ★ The usual dose is 650 mg every 8 hours for 10 to
tachycardia; atrial flutter; and atrial fibrillation. 14 days.
★ The usual oral dose for all available salts is 10 to
Opium Alkaloids
20 mg/kg/day in 4 to 6 divided doses in order to
obtain the average therapeutic serum levels of 3 to ➔ Morphine
6 mg/ml ➔ Codeine
➔ Gluconate or Sulfate salt ➔ Heroin
★ When administered orally, the peak serum levels ➔ Papaverine
are slightly lower with the gluconate and ➔ Hydromorphone
polygalacturonate salt than with the sulfate salt. Isoquinoline Alkaloids
➔ Cinchona Toxicity / Cinchonism
➔ Hydrastis or goldenseal sanguinarine
★ Toxic reactions occur at levels above 8 mg/ml.
➔ The majority of its alkaloids have the isoquinoline
The patient should be instructed to notify the
ring structure
physician if skin rash, fever, unusual bleeding or
➔ These phenanthrene alkaloids are derived
bruising, ringing in the ears, or visual disturbance
biosynthetically from benzylisoquinoline
occurs.
intermediates.
➔ Quinidine Gluconate
★ Occurs as a white powder that is odorless and has Biosynthesis of Alkaloids
a bitter taste. ➔ Biosynthesis of isoquinoline alkaloids
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★ These compounds result from the condensation
phenylethylamine derivative with a
phenylacetaldehyde derivative.
★ Both of these moieties are derived from
phenylalanine or tyrosine. Administration of
tyrosine-2-”C to Papaver somniferum resulted
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ALKALOIDS PART 2
Isoquinoline Alkaloids Ipecac
➔ Ipecac (emetine, cephaline, psychotrine) ➔ consists of the dried rhizome and roots of Cephaelis
➔ Curare ipecacuanha (Brotero) A. Richard, known in commerce
➔ Hydrastis or goldenseal Sanguinarine as Rio or Brazilian ipecac, or of Cephaelis acuminata
➔ Opium alkaloids Karsten, known in commerce as Cartagena,
★ Morphine Nicaragua, or Panama ipecac (Fam. Rubiaceae).
★ Codeine ➔ Principal Alkaloids: Emetine, Cephaeline and
★ Heroin Psychotrine
★ Papaverine ➔ What is the use of Ipecac, since it contains emetine?
★ Hydromorphone ★ USES AND DOSE
○ used in the treatment of drug overdose and in
certain poisonings.
○ The usual dose in adults and children older
than one year of age is 15 ml, followed by one
to 2 glasses of water and may be repeated
once in 20 minutes if emesis does not occur.
➔ Ipecac syrup should not be confused with ipecac fluid
extract, which is 14 times stronger. Ipecac mixed with
➔ The majority of its alkaloids have the isoquinoline ring opium (as Dover's powder) acts as a diaphoretic.
structure. Ipecac syrup is included in poison antidote kits
➔ These phenanthrene alkaloids are derived because of its emetic properties
biosynthetically from benzylisoquinoline intermediates. Emetine or Methylcephaeline
➔ The structure of Isoquinoline is because of the
➔ Is an alkaloid obtained from ipecac or prepared
benzylisoquinoline intermediates
synthetically by methylation of cephaeline.
Biosynthesis of Alkaloid ➔ It was discovered by Pelletier and Magendie in 1817.
Biosynthesis of Isoquinoline Alkaloids Emetine Hydrochloride
➔ These compounds result from the ➔ USES AND DOSE
condensation of a phenylethylamine ★ The usual dose is, intramuscularly or
derivative with a phenylacetaldehyde subcutaneously, 1 mg per kg of body weight, but
derivative. not exceeding 65 mg daily, for not more than 5
➔ Both of these moieties are derived days.
from phenylalanine or tyrosine. ➔ Emetine hydrochloride has been used extensively as
Administration of tyrosine2-"C to an antiprotozoan, particularly in the treatment of
Papaver somniferum resulted in the amebic dysentery, pyorrhea alveolaris, and other
formation of papaverine labeled in amebic diseases.
corresponding positions. Norlaudanosoline is an ➔ Emetine hydrochloride that is used as antiamebic is
intermediate in this reaction not given orally. Why?
Biosynthesis of Reticuline ★ ANSWER: It possesses expectorant and emetic
property. It may cause nausea and vomiting when
given orally.
Hydrastis or Goldenseal
➔ consists of the dried rhizome and roots of Hydrastis
canadensis Linne (Fam. Ranunculaceae).
➔ Hydrastis was known to the Cherokee Indians, who
used it as a dye and an internal remedy. These Indians
introduced its use to the early American settlers.
➔ Principal alkaloids: Hydrastine, Berberine and
Canadine
➔ USE
★ The hydrastis alkaloids, hydrastine and berberine,
are used as astringents in inflammation of the
mucous membranes
➔ Norlaudanosoline serves as a key intermediate. This
Hydrastine
medicinally important alkaloid is derived from a
benzylisoquinoline metabolite. ➔ is readily soluble in chloroform, alcohol, and ether but
➔ What is the reaction that will lead to the formation of almost insoluble in water
Morphine from Codeine?
★ ANSWER: Demethylation
Page 10 | PCOG211Lec

Berberine ○ to control convulsions of strychnine poisoning
and of tetanus
➔ is readily soluble in water but almost insoluble in ether.
○ As a diagnostic aid in myasthenia gravis.
The salts of berberine form bright yellow crystals.
- Usual initial dose, intramuscularly or
Sanguinaria or Bloodroot intravenously, is 200 to 400 mg per kg of
➔ is the dried rhizome of Sanguinaria canadensis Linne body weight, not exceeding 27 mg, then 40
(Fam. Papaveraceae). to 200 mg per kg, repeated as necessary.
➔ stain their faces and was also used as an acrid emetic. Opium or Gum Opium
➔ Its use in homemade cough remedies
➔ is the air-dried milky exudate obtained by incising the
➔ Sanguinaria contains alkaloids of the protopine series,
unripe capsules of Papaver somniferum Linne or its
including sanguinarine (about 1%), chelerythrine,
variety album DeCandolle (Fam. Papaveraceae).
protopine, and allocryptopine. These alkaloids are
➔ In 1806, Sertürner first isolated the alkaloid morphine
colorless but tend to form colored salts.
from opium.
➔ All alkaloids of sanguinaria are found in other members
➔ Externally, opium is pale olive-brown or olivegray. It is
of the Papaveraceae (Poppy) and, like berberine and
more or less plastic when fresh and becomes hard and
hydrastine, are isoquinoline derivatives.
brittle or tough when kept.
➔ Species of the families Ranunculaceae (Crowfoot),
➔ Brittle and tough when kept!
Berberidaceae (Barberry), Menispermaceae
➔ USES
(Flowering plant), and Papaveraceae contain alkaloids
★ A pharmaceutic necessity for the production of
of this type.
powdered opium
➔ USES AND DOSE
★ It acts chiefly on the CNS; its action first stimulates
★ Sanguinaria has stimulating expectorant and
and then depresses nerve response
emetic properties.
★ It serves as an analgesic, a hypnotic and a narcotic
○ The usual dose is 125 mg.
★ It checks excessive peristalsis and contracts the
Curare or South American Arrow Poison pupil of the eye
➔ is a crude dried extract from the bark and stems of Indian Opium
Strychnos castelnaei Weddell, S. toxifera Bentham, S.
➔ At present it is the only licit source of opium.
crevauxii G. Planchon (Fam. Loganiaceae) and from
➔ Indian opium yields about 10% of anhydrous morphine.
Chondodendron tomentosum Ruiz et Pavon (Fam.
➔ More than 30 different alkaloids have been obtained
Menispermaceae).
from opium and its extracts, some of which are
➔ The young bark is scraped off the plants, mixed with
alteration products of the alkaloids occurring naturally
other substances, and boiled in water and strained or
in drug. The most important of these are:
extracted by crude percolation with water. It is
★ morphine- which exist to the extent of 4 to 21%
evaporated to a paste over a fire or in the sun.
★ Codeine- ().8 – 25%
➔ The earliest available preparations were named
★ Noscapine (formerly narcotine)- (4-8%) •
according to the containers in which the drug was
Papaverine (0.5- 2.5%)
packaged: calabash (gourd), tube (bamboo), or pot
★ Thebaine (0.5- 2%)
(clay pot) curare.
➔ It is a brownish or black, shiny, resinoid mass with a Paregoric or Camphorated Opium Tincture
bitter taste. ➔ Is classed s an antiperistaltic
➔ (+) Tubocurarine, the most important constituent, ➔ It may be mixed before taking with small of water to
➔ The crude extract exhibits a paralyzing effect on form milky solution
voluntary muscle (curariform effect) by blocking nerve ➔ Relatively small doses of opium are effective in
impulses to skeletal muscles at the myoneural junction. controlling diarrhea and do not produce substantial
➔ It also produces a toxic action on blood vessels as well analgesia
as a histamine like effect.
Laudanum, Opium Tincture, or Deodorized Opium
➔ Curare was brought to England by Sir Walter Raleigh
in 1595, but it has only recently come into prominence Tincture
in medical circles. ➔ Used similarly to paregoric
➔ Tubocurarine chloride is standardized by the Poppy Seed or Maw Seed
"head-drop" crossover test in rabbits in which groups
of animals for testing and for control are used on ➔ Dried seed of Papaver somniferum var. nigrum
alternate days (crossover). DeCandolle
➔ What is the importance of the “headdrop” test? ➔ Poppy seeds are used in baking (poppy seed rolls)
★ ANSWER: describes the least amount of ➔ They contain about 50% of a fixed oil (poppy seed oil)
Tubocurarine to produce muscle relaxation which is used in some parenteral formulations, by
➔ Upon knowing the effects of Curare, what is the use of artists as a drying oil and also for food and salad
this constituent in medicine? dressings. Poppy seed oil cake is used as cattle food.
★ USES AND DOSE ➔ Poppy seeds are used in baking, with this idea does
○ as a skeletal muscle relaxant to secure muscle the Poppy seed contain significant amount of
relaxation in surgical procedures without deep alkaloids?
anesthesia.

★ ANSWER: there are no significant amount of ➔ It is used principally for the relief of cerebral and
alkaloids present peripheral ischemia complicated by arrhythmias
Alkaloids of Opium Morphine Hydromorphone Hydrochloride or
➔ Most important of the opium alkaloids Dihydromorphinone
➔ Morphine and related alkaloids are morphinan ➔ Differs from morphine hydrochloride because one of
isoquinoline derivatives. the hydroxyl groups of morphine is replaced by a
➔ A prototype of opiate analgesic drugs which acts at ketone group, and the adjacent double bond is
several sites in the CNS to produce analgesia removed
➔ Analgesia at the supraspinal level as well as euphoria, ➔ It is prepared by reducing morphine in HCl solution
respiratory depression, and physical dependence with hydrogen in the presence of a catalyst.
results from agonist activity at µ receptor. ➔ A powerful narcotic analgesic and tends to strongly
Opium Alkaloids depress the respiratory mechanism
➔ Its dosage is smaller than that of morphine; it causes
➔ Agonist activity at the kappa receptor is responsible for nausea and constipation less frequently than does
analgesia at supraspinal level, miosis, and sedation morphine, and perhaps it is less habit forming
➔ Their use tends to induce nausea, vomiting, ➔ It is well known by the trade name Dilaudid
constipation and habit formation. ➔ What major drawback does Hydromorphone have to its
★ Morphine and the related opium alkaloids that have users?
analgesic activity possess these structural features. ★ Respiratory Depression
In the case of morphine, the central carbon atom is
C-13; the phenyl ring attached to C-13 is Hydromorphone
composed of carbon atoms 1 to 4 and 11 to 12: and ➔ Formulations
the tertiary nitrogen atom is linked via a two-carbon ➔ Schedule II
bridge (C-15, C-16) to the central carbon atom. ➔ 2 to 8 times the analgesic potency of morphine but
➔ Always look at the pupils; the pupil size can give very shorter acting and more sedating
good clinical information.
Hydrocodone Bitartrate or Dihydrocodeinone
Bitartrate
➔ Bears the same relation to codeine as
dihydromorphinone does to morphine- a ketone group
replaces one of the hydroxyl groups and the adjacent
double bond is saturated.
➔ antitussive and FOR COUGH
Indole Alkaloids
➔ Three series of alkaloids have been reported
★ weakly basic indole alkaloids
○ The principal alkaloids are reserine,
rescinnamine, and deserpidine are tertiary
indole alkaloids that have a carboxylic structure
in ring E and are of the corynane type
★ Indoline alkaloids of intermediate basicity
Codeine or Methylmorphine ○ Ajmaline, isoajmaline, rauwolfininethese bases
➔ Codeine and its salts are narcotic analgesics and do not have tranquilizing act
antitussive; they are used as sedatives, especially in ★ Strong anhydronium bases
allaying coughs. ○ Serpentine, serpentinine and alstoine
➔ Although its action is similar to that of morphine, ➔ Exert their hypotensive effects by depletion of
codeine is considerably less toxic and involves much catecholamine and serotonin stores in many organs,
less danger of habit formation. including the brain and adrenal medulla, and by the
➔ Street retail reduction of uptake of catecholamines by adrenergic
★ Bag in NYS may be a “cap” or “1/4 spoon” in other neurons.
parts of US ➔ Their sedative and tranquilizing properties are thought
★ “Dope” in NYS may be “smack” or “junk” to be related to depletion of amines in the CNS
Heroin Autonomic Nervous System
Papaverine Inhibition of NE Synthesis

➔ Occurs naturally in opium to the extent of about 1%,
but it may also be produced synthetically.
Papaverine Hydrochloride
➔ Occurs as white crystals or as a white crystalline
powder. It is odorless but has a slightly bitter taste.
➔ Is a smooth muscle relaxant.

➔ In male sexual performance, erection is linked to
increased cholinergic activity which results in
increased penile blood flow, decreased penile blood
outflow, or both, causing erectile stimulation.
➔ Adrenergic System Antagonist
➔ a2 - selective antagonist
➔ Chief active compound in Pausinystalia yohimbine
(bark)
➔ Effects opposite of Clonidine
➔ Enters CNS => increased sympathetic output =>
increased heart rate, blood pressure, can cause
severe tremors
➔ Ingredient in many weight loss products
Rauwolfia Serpentina ➔ Extensive (past) use in treatment of male sexual
dysfunction
➔ Is the dried root of Rauwolfia serpentina (Fam.
➔ Yohimbine is a sympatholytic or a Sympathomimetic
Apocynaceae)
drug?
➔ It contains not less than 0.15% and NMT 0.20% of the
★ ANSWER: Sympatholytic, simce it is an alpha-2
reserpine- rescinnamine group of alkaloids, calculated
antagonist
as reserpine
Catharanthus or Vinca
Powdered Rauwolfia Serpentina
➔ Is he dried whole plant of Catharanthus roseus (Fam.
➔ Is a R. serpentina root reduced to fine or very fine
Apocynaceae), formerly designated Vinca rosea Linne’
powder that is adjusted, if necessary, to conform to the
➔ Botanically it is closely related to Vinca minor Linne’,
official requirements
the common periwinkle
➔ Hypotensive
➔ oral hypoglycemic agent- folkloric use
➔ Reserpine - chief alkaloid – hypotensive and sedative
➔ the ability of certain fractions to produce
➔ used in mild essential hypertension
granulocytopenia and bone marrow depression I rats
➔ relieves the symptoms in agitated psychotic states
was observed by the Canadian group of Noble, Beer
such as schizophrenia in patients unable to tolerate
and Cutts. Continued study led to the isolation of an
other antipsychotic agents.
alkaloid, vinblastine, which produced severe
Reserpine leukopenia in rats
➔ Is a white or pale buff to slightly yellow, odorless, ➔ Four bisindole compounds vinblastine, vinleurosine,
crystalline powder that darkens slowly when exposed vinrosidine, and vincristine, possess demonstrable
to light and rapidly when in solution. oncolytic activity
➔ An antihypertensive and antipsychotic agent ➔ Nearly 500 kg of catharanthus are utilized to produced
➔ Obtained in commercial quantities from four different 1 g of vincristine
species of Rauwolfia; R. serentina, R. micrantha, R. Vinblastine Sulfate
tetraphylla and R. vomitoria.
➔ AKA Vincaleukoblastine Sulfate or VLB
Rescinnamine ➔ Is the salt of an alkaloid extracted from catharanthus.
➔ AKA 3,4,5-trimethoxycinnamic acid ➔ sealed ampules,
➔ Is an alkaloid that occurs in several species of ➔ Used for the treatment of a wide variety of neoplasms
Rauwolfia. and is recommended for generalized Hodgkin’s
➔ Its appearance, properties, and solubility are disease, lymphocytic anemia, histiocytic lymphoma,
somewhat similar to those of reserpine mycosis fungoides, advanced testicular carcinoma,
➔ It is used to treat mild essential hypertension Kaposi’s sarcoma and choriocarcinoma and breast
cancer
Deserpidine
➔ Effective as a single agent but is usually administered
➔ AKA 11-desmethoxyreserpine / Canescine / with other antineoplastic agents in combination therapy
Recanescine for an enhanced therapeutic effect without additive
➔ Alkaloid obtained from the root of Rauwolfia canescens toxicity
➔ Same uses as Rauwolfia serpentina and reserpine and ➔ It is administered intravenously
is claimed to have fewer side effects
Vincristine Sulfate
Yohimbine
➔ AKA Leurocristine Sulfate / VCR or LCR
➔ An indole alkaloid of corynane type obtained from the ➔ Also obtained from catharanthus
bark of West African tree Pausinystalia yohimbe (Fam. ➔ The structure is similar to vinblastine, differing only in
Rubiaceae) the substitution of an N-formyl group for the N-methyl
➔ Treated impotence in patients with vascular or diabetic group of vinblastine
problems ➔ Despite the structural similarities, there are differences
➔ Its peripheral autonomic nervous system effect is to in the antitumor spectra of the two compounds, and no
increase cholinergic and decrease adrenergic activity cross resistance has been observed

➔ It is recommended for the treatment of acute ★ less toxic than strychnine, used commercially as an
lymphocytic leukemia and in combination therapy in alcohol denaturant because it is extremely bitter
Hodgkin’s disease, lymphosarcoma, reticulum cell Physostigma, Calabar Bean or Ordeal Bean
sarcoma, rhabdomyosarcoma, neuroblastoma and
Wilm’s tumor ➔ Is the dried, ripe seed of Physostigma venenosum
(Fam. Fabaceae) yielding not less than 0.15% of the
Vindesine alkaloids of Physostigma.
➔ Is a semisynthetic derivative of vinbastine where the ➔ In 1846, Daniell described the use of seed, known as
cetyl group at position 4 of the vindoline has been esere by the natives of old Calabar, to prove the
removed. innocence or guilt of persons accused of crime
➔ Even though it is derived from vinblastine, it has ➔ Calabar bean contains several alkaloidsphysostigmine
antineoplastic activity more closely resembling that of (eserine), eseramine, geneserine, and physovenine
vincristine. Physostigmine or Eserine
➔ Clinical trials indicate that it has good activity in
difficult-to-treat or refractory cancer types, and there ➔ An alkaloid usually obtained from the dried, ripe seed
appears to be a lack of cross resistance with vincristine of P. venenosum
and vinblastine ➔ Degradation products are irritating to the eye and lack
substantial pharmacologic activity.
Vinorelbine Tartrate ➔ Should be preserved in tight, lightresistant containers
➔ The derivative is a 3’- noranhydrovinblastine. in quantities not exceeding 1 g.
➔ It is indicated as a single agent or in combination with ➔ A reversible inhibitor of the cholinesterases and thus
cisplatin for the first line treatment of non-small cell enhances the effects of endogenous acetylcholine.
lung cancer ➔ In the eye, increase in cholinergic activity leads to
Review on Mitosis miosis, contraction of the ciliary muscle, and a
decrease in intraocular pressure caused by an
increases out-flow of the aqueous humor.
➔ USE: Employed in ophthalmology to treat glaucoma
Physostigmine Salicylate or Eserine Salicylate
➔ Because it prolongs and exaggerates the effect of
acetylcholine, it is given by injection as an antidote in
poisonings caused by anticholinergic agents.
➔ Physostigmine sulfate or eserine sulfate
➔ It is a cholinergic (ophthalmic) used in the form of a
Vinca Alkaloids 0.25% ointment that is applied topically to the
conjunctiva.
➔ Binds to microtubuli- Supression of microtubuli
dynamicsMetaphase arrest Depolymerization of Effect of Glaucoma
microtubuli high conc.
Nux Vomica
➔ Is a dried ripe seed of Strychnos nux vomica Linne’
(Fam. Loganiaceae)
➔ strychnine and brucine, -chief alkaloids
➔ Nux vomica and the seeds of the closely related
Strychnos ignatii (ignatia or St. Ignatius bean) serve as
a commercial source of strychnine and brucine. the
former alkaloid is commonly marketed as strychnine
sulfate or strychnine phosphate.
Strychnine and Brucine
➔ AKA dimethoxystrychnine
➔ Strychnine ➔ Magkaka-glaucoma ka talaga, ‘pag nakita mo siyang
★ extremely toxic masaya sa iba (sheesh)
★ functioning as a central stimulant Indole Alkaloids
★ Relevant in neuroresearch. The alkaloid produces
➔ Three series of alkaloids have been reported
excitation of all parts of the CNS and blocks
★ (1) weakly basic indole alkaloids The
inhibitory spinal impulses at the postsynaptic level.
principal alkaloids are reserine, rescinnamine,
This leads to an exaggeration in reflexes, with
and deserpidine are tertiary indole alkaloids
resulting tonic convulsions.
that have a carboxylic structure in ring E and
★ Fatal poisoning in humans ordinarily results from
are of the coryanne type
doses of 60-90 mg.
★ (2) Indoline alkaloids of intermediate
○ Vermin killer
basicity Ajmaline, iso ajmaline, rauwolfia nine
➔ Brucine
these bases do not have tranquilizing action

★ (3) Strong Anhydronium bases Serpentine, ➔ It is used to prevent or abort vascular headaches,
serpentine and alstine including migraine and cluster headaches.
➔ Exert their hypotensive effects by depletion of
catecholamine and serotonin stores in many organs,
including the brain and adrenal medulla, and by the
reduction of uptake of catecholamines by adrenergic
neurons.
➔ Their sedative and tranquilizing properties are thought
to be related to depletion of amines in the CNS
Rauwolfia Serpentina
Ergotamine
➔ Is the dried root of Rauwolfia
serpentina (Fam. Apocynaceae) ➔ MOA: Direct vasoconstriction of the dilated carotid
➔ It contains not less than 0.15% and artery bed with a concomitant decrease in the
NMT 0.20% of the reserpine- amplitude of pulsations
rescinnamine group of alkaloids, ➔ It may inhibit reuptake of norepinephrine at
calculated as reserpine sympathetic nerve endings, increasing the
vasoconstrictive action, and the drug is also an
Ergot, Rye Ergot or Secale Cornutum
antagonist of serotonin activity
➔ Formerly defined in the official compendia as the dried ➔ Better with caffeine
sclerotium of Claviceps purpurea (Fam.
Ergotoxine
Clavicipitaceae) developed on plants of rye, Secale
cereale Linne’ (Fam. Gramineae) ➔ Formerly employed as reference standard in the form
➔ It was required to yield not less than 0.15% of the total of ergotoxine ethanesulfonate
alkaloids of ergot calculated as ergotoxine and ➔ Mixture of ergocristne + ergokrytine + ergocornine.
water-soluble alkaloids equivalent to not less than ➔ A mixture of equal parts of these component alkaloids
0.01% of ergonovine. is hydrogenated to eliminate the ∆9 double bond of the
lysergic acid nucleus and to yield an equivalent mixture
Ergot
of dihydroergocristine, dihydroergokryptine, and
➔ Because these sclerotia are long and somewhat dihydroergocrnine.
pointed, the common name of spurred rye has been
Ergoloid Mesylates
applied to the drug
➔ At present ergot alkaloids are obtained on a ➔ They produce vasorelaxation, increased cerebral blood
commercial scale from both parasitic and saprophytic flow, lowering of systemic blood pressure, and
sources. The former is the dried sclerotium of C. bradycardia.
Purpurea developed on the rye plants Methysergide Maleate
➔ Claviceps paspali has been grown saprophytically in
➔ The salt of methylergonovine that has an additional
submerged culture
methyl group attached to the nitrogen at position 1 of
➔ At present, both peptide and non peptide alkaloids
the lysergic acid nucleus.
(water soluble) are obtained from parasitically develop
➔ A serotonin antagonist employed in the prophylaxis of
ergot sclerotia. Only the latter type is produced
vascular headache.
commercially in saprophytic culture.
➔ The patient should be advised to take medicine with
Ergonovine Maleate or Ergometrine Maleate meals and to notify the physician if cold, numb, or
➔ The accepted chemical name of isolysergic acid painful hands, leg cramps, abdominal or chest pain, or
isomer of ergonovine is ergometrinine change in skin color occurs
➔ The oxytocic effect of the drug, either rally, SC, or IM, Lysergic Acid Diethylamide or LSD
is sometimes noted within 5 minutes after giving the
➔ Does not occur in nature but is prepared by
dose.
semisynthesis.
Methylergonovine Maleate ➔ The compound has a two fold action, producing a
➔ Is a semi synthetic homolog of ergonovine prepared predominant central sympathetic stimulant that
from lysergic acid and 2-aminobutnol parallels a slight depression.
➔ It occurs as a white to pinkish tan microcrystalline ➔ Discovered by A. Hofmann
powder ➔ It is the most active and most specific psychotomimetic
➔ An oxytocic reputed to be slightly more active and agent known
longer acting than ergonovine ➔ The effective oral dose in humans is 30 to 50 µg
➔ Causes fusion of senses
Ergotamine Tartrate
➔ “bad trip”- fear, depression and anxiety
➔ Brand name: Avamigran ➔ Nausea. Tremors. nausea
➔ Occurs as a colorless crystals or as white , crystalline
How is LSD Consumed?
powder, sparingly soluble in water or in alcohol
➔ Possess oxytocic activity, but it is not employed for that ➔ LSD is generally taken orally, either as a pill, a piece of
effect blotter paper (as seen on right), or via liquid dripped

onto a sugar cube. LSD can also be absorbed through Types of Glaucoma
the user's skin.
Drugs Related to Ergot
Ololiuqui/Morning Glories
➔ An ancient Aztec hallucinogenic drug still used in
Mexico for magicoreligious purposes
➔ Seeds of ololiuqui, Rivea corymbosa Linne’ (Fam.
Convolvulaceae),
➔ (+)- Lysergic acid amide (ergine), the principal
psychotomimetic compound in these species, is Steroidal Alkaloids
accompanied by (+)- isolysergic acid (ergenine), ➔ Derived biosynthetically from six isoprene units and
rergonovine, (+)- lysergic acid methylcarbinolamide, could be classified as triterpenoids or steroids;
and certain clavinet alkaloids however they also contain nitrogen giving them basic
Imidazole Alkaloid properties. The nitrogen may be part of a ring system,
usually incorporated at a late stage in biosynthesis, or
Pilocarpine
it may be as an N-methyl substituted amino group.
➔ Pilcarpus or jaborandi consists of the leaflets of
Veratrum Viride
Pilocarpus jaborandi Holmes(Pernambuco jaborandi),
or of P. pinnatofolius(Paraguay jaborandi) (Fam. ➔ AKA American or Green Hellebore
Rutaceae) ➔ Consists of a fried rhizome and roots of Veratrum viride
➔ Directly stimulates the muscarinic receptors in the eye, Aiton (Fam. Liliaceae)
causing constriction of the pupil and contraction of the ➔ Possess hypotensive, cardiac depressant and sedative
ciliary muscle properties
➔ In narrow angle glaucoma, miosis opens the anterior ➔ It has been used in the treatment of hypertension
chamber angle to improve the outflow of aqueous White Hellebore or European Hellebore
humor
➔ Is the dried rhizome of Veratrum album,Linne (Fam.
➔ In chronic open-angle glaucoma, the increase in
Liliaceae).
outflow is independent of the miotic effect. Contraction
➔ White hellebore possesses hypotensive properties, but
of the ciliary muscle enhances the outflow of aqueous
the crude drug is not used therapeutically.
humor via indirect effects on the trabecular system
➔ Both white and green hellebores are also employed as
What’s the Difference Between a Closed Angle and insecticide.
an Open Angle Glaucoma
Alkaloidal Amines
➔ What is the main difference of alkaloidal amines from
other classes of alkaloid?
★ ANSWER: the nitrogenous portion (or the amine) is
not part of the cyclic ring
➔ The alkaloids in this group do not contain heterocyclic
nitrogen atoms.
➔ Many are simple derivatives of phenyllethylamine and,
such, are derived from the common amino acids,
phenylalanine or tyrosine.
➔ Other alkaloidal amines are tryptamine derivatives and,
as such, are biosynthesized from tryptophan.
Pilocarpine HCL
➔ gramine in Hordeum vulgare,
➔ Obtained from the dried leaf of Pilocarpus jaborandi or ➔ psilocybin in the Mexican hallucinogenic mushroom,
of P. microphyllus Psilocybe semperviva, and
➔ It is hygroscopic ➔ serotonin and bufotenine in number of plant and
Pilocarpine Nitrate animal species.
➔ It is stable in air but is affected by light. Ephedrine

➔ Occurs as colorless, translucent, odorless, faintly bitter ➔ Ephedra or ma huang
crystals, shiny, white crystals ➔ Is the entire plant or the over ground portion of
➔ Applied topically as 0.25 to 10% solution of pilocarpine Ephedra sinica Stapf (Fam. Gnetaceae).
HCl or as a 0.5 to 6% solution of pilocarpine nitrate to ➔ In Chinese characters, “ma” means astringent and
the conjunctiva. “huang” means yellow, probably referring to the taste
➔ Also available in an ocular therapeutic system that and color of the drug.
provides continuous release over one week following ➔ Its used in modern medicine began in 1923
placement in the conjunctival cul-de-sac. ➔ Chief alkaloid in Ephedra, no clinical use
➔ Found in many dietary supplements:
“EnergyBoosters”, Diet pills (Metabolife®)

➔ Ingredient in many herbal preperations: Ephedra, Ma Other Alkaloidal Amine Drugs
Huang
Khat or Abyssinian Tea
➔ The FDA has received more than 800 reports of
adverse effects associated with use of products ➔ Consist of the fresh leaves of Catha edulis Forskal
containing ephedrine alkaloid since 1994. These (Fam. Celatraceae)
serious adverse effects, include hypertension (elevated ➔ The leaves are chewed to alleviate the sensations of
blood pressure), palpitations (rapid heart rate), hunger and fatigue (Africa, arabia)
neurophathy (nerve damage), myopathy (muscle ➔ The Expert Committee on Addictionproducing drugs of
injury), psychosis, stroke, memory loss, heart rate the WHO does not classify khat as a drug that
irregularities, insomnia, nervousness, tremors, produces habituation or addiction, but the French
seizures, heart attacks, and death. government considers it a narcotic
➔ In Feb ‘04, the agency has banned the marketing of ➔ Contains a potent phenylalkylamine alkaloid called (-)-
dietary supplements containing ephedrine alkaloids cathinone
(ban challenged by court order in April ‘05). ➔ It has pharmacologic properties analogous to those of
(+)-amphetamine and is of similar potency with a
Ephedrine Sulfate
similar mechanism of action, namely, the induction of
➔ Ephedrine sulfate is used to combat hypotensive catecholamine release from storage sites
states and for allergic disorders, such as bronchial ➔ In older leaves, it is converted to the weakly active
asthma, as well as for local treatment and nasal compounds (+)-norpseudoephedrine (80%) and (-)-
congestion. norephedrine (20%). This conversion also occurs
Ephedrine Hydrochloride rapidly during the drying of the young leaves
➔ Also occurs as fine, white, odorless crystals or as a Peyote or Mescal Buttons
powder and is affected by light. ➔ Consists of the dried tops of Lophophora williamsii
➔ It has the same pharmacologic properties as ephedrine (Fam. Cactaceae)
and is used as a sympathomimetic. Both of these salts ➔ It disturbs normal mental function and causes
are readily soluble in water and in hot alcohol but not in concomitant hallucinations and euphoria
ether. ➔ Ingestion of mescal buttons results in mydriasis
Allied Plants accompanied by unusual and bizarre color perception
Flashing lights and vivid configurations characterize by
➔ In addition to Ephedra sinica (the source of ma huang)
visions at first; later the colors become dim and the
and E. equisetina Bunge (the chief source of the
subjects become drowsy; eventually, sleep is
extracted alkaloid), E. distachya Linne also yields
produced.
ephedrine.
➔ The drug contains several alkaloids including
Colchicine mescaline (the most active of the peyote constituents),
➔ Colchicum seed anhalanine, anhalamine, and anhalidine.
➔ is the dried, ripe see of colchicum autumnale Linne Purine Alkaloids
(Fam. Liliaceae). Colchicum corm is the dried corm of
Purine Bases
the same species.
➔ Dioscorides mentions Colchicum. The arabs ➔ Purines are derivatives of a heterocyclic nucleus
recommended the used of the corm for gout in consisting of the 6-membered pyrimidine ring fused to
medieval times, but The drug was abandoned because the 5-membered imidazole ring.
of its toxicity. It again came into used in Europe about ➔ The pharmaceutically important bases of this group are
the middle of the 17th century. all methylated derivatives of 2,6- dioxypurine
➔ is an alkaloid obtained from various species of (xanthine)
Colchicum, usually Colchicum autumnale. Natural Methylxanthines
➔ It has also been found in other generations of the lily
➔ Caffeine – 1, 3, 7- trimethylxanthine
family. Colchicine has one amido nitrogen atom.
➔ Theophylline – 1, 3- dimethylxanthine
➔ The compound lacks pronounced basicity and does
➔ Theobromine – 3, 7- dimethylxanthine
not form a well-defined series of salts as do other
alkaloids. Methylxanthines
➔ The exact mechanism of action of colchicines in the ➔ The methylxanthines competitively inhibit
treatment of gout is not unknown. It does not inhibit phosphodiesterase, which results to increase of cyclic
leukocyte migration and reduces lactic acid production adenosine monophosphate with a subsequent release
by leukocytes which results in a decreased deposition of endogenous epinephrine. This results to:
of uric acid. ★ direct relaxation of the smooth muscles of the
➔ In addition, there is a reduction in phagocytosis which bronchi and pulmonary blood vessels
decreases the inflammatory response. Colchicine is ★ a stimulation of the CNS
used as a suppressant for gout. ★ an induction of diuresis
★ increase in gastric acid secretion

★ Inhibition of uterine contractions and a weak Sources of Caffeine
positive chronotropic and inotropic effect on the
heart Drink/Food Amount of Amount of
Drink/Food Caffeine
Kola, Cola or Klanuts
➔ Dried cotyledon of Cola nitida or of other species of Jolt 12 oz 71.2 mg
Cola (Fam. Sterculiaceae)
➔ During the drying process, the complex is split, yielding Mountain dew 12 oz 55.0 mg
free caffeine and Theobromine and converting the
Coke 12 oz 34.0 mg
colorless kolacatechin to the redbrown cola red
➔ Possesses the central stimulating action of caffeine
Diet coke 12 oz 45.0 mg
➔ It is an ingredient in several carbonated beverages
Coffee Bean or Coffee Seed Pepsi 12 oz 38.0 mg
➔ Is the dried, ripe seed of Coffea Arabica or C. liberica 7-up 12 oz 0 mg
(Fam. Rubiaceae), deprived of most of the seed coat.
➔ ROASTED COFFEE – becomes dark, with distinct Brewed coffee 5 oz 115 mg
aroma (drip)
➔ COMPONENTS OF COFFEE SEEDS
★ 1 to 2% of caffeine Iced tea 12 oz 70 mg
★ about 0.25% of trigonelline (N-methylbetaine of
nicotinic acid) Dark chocolate 1 oz 20 mg
★ from 3 to 5% of tannin
Milk chocolate 1 oz 6 mg
★ about 15% of glucose and dextrin
★ 10 to 13% f fatty oil consisting chiefly of Cocoa beverage 5 oz 4 mg
trioleoylglycerol and tripalmitoylglycerol and 10 to
13% of proteins Chocolate milk 8 oz 5 mg
➔ When the coffee is roasted, the seeds swell, change in
color to dark brown, and develop the characteristic Cold relief pills 1 oz 30 mg
odor and flavor
Guarana
➔ The aroma is caused by caffeol-released when
roasting ➔ Dried paste composed chiefly of the crushed seed of
Paullinia cupana (Fam. Sapindaceae)
Caffeine
➔ Enters into the preparation of a stimulating beverage
➔ However, chlorogenic acid and caffeol are also that is used like tea and coffee by the people of Brazil.
physiologically active Also contains 25% of tannin(cathechutannic acid)
➔ The usual cup of brewed coffee contains about 100 to ➔ Its action is caused by the caffeine present, but it also
150 mg of caffeine and a cup of instant coffee contains possesses astringent properties.
about 85 to 100 mg of caffeine
Mate or Paraguay Tea
★ Cup of tea- 60- 75 mg
★ Cocoa- 5 to 40 mg ➔ Consist of the leaves of Ilex paraguariensis (Fam.
★ 12 oz of cola drink- 40 to 60 mg Aquifoliaceae)
○ The estimated daily dose of caffeine is 1.5 g ➔ Contains caffeine up to 2% and tannin
○ Although coffee is mainly dietetic, it is also a ➔ USE: in large doses as laxative or purgative
stimulant and diuretic ➔ Also has a diaphoretic and diuretic property
○ It is of value in the treatment of poisoning by ➔ Employed in South America in the preparation of a
certain CNS depressants tealike beverage
➔ Synthesized from the same precursors in Coffea Theophylline
arabica as are the purine bases in all other biologic
systems that have been investigated ➔ THEA OR TEA
➔ 1,3,7-trimethylxanthine occurs in coffee, tea, cacao, ★ Consist of the prepared leaves and leaf buds of
guarana, kola and mate Camellia sinensis (Fam. Theaceae)
➔ GREEN TEA
Decaffeinized Coffee ★ Prepared in china and Japan by rapidly drying the
➔ Prepare by extracting most of the caffeine from the freshly picked leaves in copper pans over a mild
coffee bean yet retaining the pleasant characteristic artificial heat. The leaves are often rolled in the
aroma of coffee palm of the hand as they dry.
➔ Such preparations normally contain up to 0. 08% of Black Tea
caffeine
➔ Occurs as more or less crumpled, bright green or
blackish green, mass.
➔ odor: agreeable and aromatic.
➔ Taste: astringent and bitter.

➔ Contains 1 to 45 of caffeine (theine) and small
amounts of adenine, Theobromine, Theophylline and
xanthine
➔ The stimulating action: caffeine
➔ astringent properties: tannin content
Theophylline or 1, 3- Dimethylxanthine
➔ Isomeric with thebromine and was first isolated from
tea in 1885
➔ Prepared synthetically from caffeine or by other means
➔ Serves as a smooth muscle relaxant, antiasthma and
diuretic
Theobromine or 3, 7- Dimethylxanthine
➔ Compound prepared from the dried, ripe seed of
Theobroma cacao (Fam. Sterculiaceae) or is made
synthetically
➔ A diuretic and a smooth muscle relaxant
➔ It has little stimulant action on the CNS
ENDOCRINE PRODUCTS AND ENZYMES
Glands ○ Somatomedins are synthesized in the liver, in

response to stimulation by the GH
➔ An organ which secretes particular chemical ★ Effect on Protein and Mineral Metabolism:
substances for use in the body or for discharge into the ○ On protein metabolism:
surroundings. - GH is protein anabolic hormone.
★ There are three types of glands in our body: ○ On mineral metabolism:
○ Endocrine glands - Increase calcium absorption from GIT
○ Exocrine glands - Decrease sodium, potassium, calcium
○ Heterocrine gland and phosphorous
Exocrine Glands ★ Effect on carbohydrate and fat metabolism:
➔ Example: ○ On carbohydrate
★ Sweat glands - GH is diabetogenic, because it produce
★ Salivary glands hyperglycemia
★ Mammary glands ○ On fat metabolism
★ Stomach - GH has catabolic effect
★ Liver Control of Growth Hormone
★ Pancreas ➔ The release of GH is primary under the control of two
Heterocrine Glands hypothalamic hormones:
➔ These are glands that perform both exocrine and ★ GH releasing hormone
endocrine functions. For example pancreas ★ GH inhibiting hormone
Endocrine Glands Diseases Related to Growth Hormone
➔ Example: ➔ Gigantism:
★ Pituitary gland ★ It is due to overproduction of GH during
★ Pancreas adolescence.
★ Thyroid gland ★ It is characterized:
★ Adrenal glands ○ Tall stature
○ Bilateral gynecomastia.
Endocrine System ○ Large hand and feet.
➔ Consists of glands and group of capillaries which ➔ Acromegaly:
facilitates diffusion of hormones to bloodstream ★ It is due excessive secretion of GH during
adulthood
Pituitary Gland
★ It is characterized by:
➔ The pituitary gland consists of: ○ Broad, thick nose
★ Adenohyphophysis ○ Thickening of the skin
○ It is influenced by hormones which come from ○ Prominent brow
the hypothalamus. ➔ Dwarfism:
★ Neurohypophysis ★ Deficiency of GH secretion.
○ It is influenced by neurons which convey ★ Shortness of stature
hormones directly from hypothalamic nuclei for ★ Small genitalia
storage of posterior lobe ★ Delicate extremities
Hormones Prolactin
➔ Anterior lobe: ➔ Actions of prolactin:
★ Growth hormone (GH) ★ Prolactin plays an important role in the
★ Prolactin development of the mammary gland and in milk
★ Thyroid stimulating hormone (TSH) synthesis.
★ Adrenocorticotrophic hormone (ACTH)
Control of Prolactin Secretion
★ Follicle stimulating hormone (FSH)
★ Luteinizing hormone (LH) ➔ Stimulating factors:
➔ Intermediate lobe: ★ They act via stimulating Prolactin releasing factor
★ A and B melanocyte stimulating hormone ➔ Inhibitory factors:
➔ Posterior lobe: ★ which is released by the hypothalamus inhibits
★ Vasopressin (ADH) prolactin secretion from the anterior pituitary
Hormones of Anterior Pituitary Thyroid-Stimulating Hormone (TSH)
Growth Hormone (GH) ➔ It stimulates the thyroid gland to produce:
★ Thyroxin (T4), and
➔ Action of growth hormone
★ Triiodothyronine (T3)
★ Stimulating of growth of bones, cartilage and
connective tissue:

Adrenocorticotrophic Hormone (ACTH) ➔ Thyroid is not absolutely essential for life, but its
removal in adults leads to:
➔ It is secreted by the anterior pituitary gland.
★ Poor resistance to cold
➔ It is often produced in response to biological stress.
★ Mental and physical slowing and in children’s:
Follicle Stimulating Hormone (FSH) ★ Mental retardation
➔ It is synthesized and secreted by anterior pituitary ★ Dwarfism
gland Thyroid Hormones
➔ FSH regulates the development, growth, pubertal
➔ Triiodothyronine (T3)
maturation and reproductive processes of the body
★ It affects almost every physiological process in the
Luteinizing Hormone (LH) body:
➔ It is a hormone produced by the anterior pituitary ○ Growth and development,
gland. ○ Metabolism,
➔ In females, an acute rise of LH triggers ovulation and ○ Body temperature, and
development of the corpus luteum ○ Heart rate
➔ In males, it stimulates the production of testosterone ➔ Thyroxin (T4)
★ Controls development and maturation
Hormones of Intermediate Lobe
★ Excess thyroxin results rapid development
➔ It secretes: ★ Deficiency of thyroxin results in delayed
★ α melanocyte stimulating hormone development
★ β melanocyte stimulating hormone ➔ Calcitonin
➔ Function: ★ It is a hormone secreted by the C cells of the
★ They stimulate the production of melanin by thyroid gland
melanocytes in skin and hair ★ Its main actions are:
★ MSH signals to the brain have effects on appetite ○ to increase bone calcium
and sexual arousal ○ to decrease blood calcium levels
Hormones of Posterior Pituitary ★ Calcitonin opposes the effects of parathyroid
hormone, which acts to increase the blood level of
Anti-Diuretic Hormone (ADH)
calcium.
➔ AKA Vasopressin
Regulation of Thyroid Secretion
➔ It is a hypothalamic hormone synthesized in the cells
of the supra optic nucleus ➔ Thyroid stimulating hormone (TSH) controls the
➔ ADH is stored in the posterior pituitary regulation of thyroid hormones.
➔ Functions: ★ The release of TSH by the anterior lobe of the
★ Its two primary functions pituitary, is regulated by the hypothalamus via
○ To retain water in the body negative feedback mechanism.
○ To constrict blood vessel ★ It is a reaction that causes a decrease in function. It
occurs in response to some kind of stimulus.
Diseases Related to ADH
Diseases Related to Thyroid Gland
➔ Diabetes Insipidus:
★ It is a condition characterized by: ➔ Goiter
○ Excessive thirst ★ Any enlargement of the thyroid gland is called
○ Excretion of large amounts of severely diluted goiter Caused by iodine deficiency.
urine ★ Characteristic features:
➔ Polyuria ○ Swelling in the neck
★ It is the excessive or abnormally large production of ○ Breathing difficulties
urine (at least 2.5 or 3L /in adults) ○ Cough
○ Hoarseness
Oxytocin
○ Swallowing difficulties
➔ Oxytocin is synthesized in the hypothalamus ➔ Hypothyroidism
➔ Stored in the posterior lobe of pituitary gland ★ It is the condition resulting from reduced circulating
➔ Action: levels of T3 and T4.
★ Oxytocin stimulates contraction of mammary gland ★ Characteristic features:
to produce milk. ○ Goiter
★ Stimulate contraction of the smooth muscles of the ○ Puffiness of face with
uterus ○ Periorbital swelling
Thyroid Gland ○ Loss of scalp hairs
○ Ptosis, i.e., drooping of upper eyelid.
➔ Anatomy
○ Dry, thickened, rough and yellow skin
★ The thyroid gland is situated in the neck in front of
➔ Hyperthyroidism or Graves Disease
the larynx and trachea
★ It is the condition resulting from increased
★ It weighs about 25g
circulating level of T3 and T4
★ It looks like butterfly in shape
★ Characteristic features:
★ Consisting of two lobes

○ Moderate enlargement of thyroid gland ○ Promotes gluconeogenesis
○ Exophthalmos ➔ Somatostatin
Parathyroid Gland ★ A hormone that is widely distributed throughout the
body, especially in the hypothalamus and pancreas
➔ In humans there are 4 parathyroid glands ★ Action:
➔ Parathyroid glands are essential for life, as their ○ It regulates the endocrine and Nervous system
removal can cause death from asphyxia functions
➔ Function:
★ Parathyroid glands contains chief cells which Diseases Related to Insulin
secrete parathyroid hormone. ➔ Diabetes Mellitus
★ The main function of parathyroid hormone is to ★ It is a group of metabolic diseases in which there
increase the blood calcium level are high blood sugar over a prolonged period.
Diseases Related to Parathyroid Gland ★ This high blood sugar produces the symptoms of:
○ frequent urination,
➔ Rickets ○ increased thirst, and
★ It is a disease characterized mainly by bone ○ increased hunger.
deformities in young children’s
★ The disease of children sets in about 6th month of Adrenal Glands
life ➔ There are two adrenal glands,
★ Characteristic features: ➔ About 4 cm long and 3 cm thick
○ Deformed bones ➔ It has two parts:
○ Thick wrist and ankles ★ outer part is cortex and
○ Retarded growth ★ the inner part is medulla.
➔ Osteomalacia Adrenal Cortex
★ This is due to inadequate absorption of calcium
due to deficiency of Vitamin D and Calcium in the ➔ Glucocorticoids
diet ★ Cortisol, corticosterone and cortisone are the main
★ The disease is limited to females, usually appears Glucocorticoids
after multiple pregnancies and lactation. ★ They are essential for life, regulating metabolism
➔ Hypoparathyroidism and stress
★ It is an abnormally low level of calcium in the blood ★ They are high in between 4 to 8 am
★ Characteristic features: ★ Lowest between midnight and 3 am
○ Psychiatric disturbance ★ Effects:
○ Paraesthesia ○ Gluconeogenesis (formation of new sugar)
○ Development of cataract ○ Lipolysis (breakdown of triglycerides into fatty
➔ Hyperparathyroidism acids and glycerol for energy production).
★ Excessive secretion of parathyroid hormone. ○ In pathology and pharmacology:
★ Characteristic features: - Have an anti-inflammatory action.
○ Formation of renal calculi - Suppress the immune response.
○ Polyuria - Suppress the response of tissue to injury.
○ Polydipsia - Delay wound healing
○ Anorexia ➔ Mineralocorticoids (Aldosterone)
○ Muscle weakness ★ Aldosterone is the main mineralocorticoids
○ General fatigue ★ It maintains Water and electrolyte balance
○ Calcification of soft tissue ➔ Sex hormones
★ Androgens are the main sex hormones
Pancreas ★ They contribute to the onset of puberty
Pancreatic Hormones Disorders of Adrenal Cortex
➔ Insulin ➔ Cushing’s Syndrome
★ Actions: ★ It is caused due to hypersecretion of
○ On carbohydrate metabolism: glucocorticoids
- Insulin increases the glucose entry into ★ Characteristic features:
most of body cells ○ Pain in face, neck and abdomen
- Insulin produce hypoglycemia ○ Pathological fractures
○ On protein metabolism: ○ Diminished protein synthesis
- Insulin promotes amino-acid uptake ○ Suppression of growth
- It decrease protein breakdown ○ Hypertension
- It promotes protein synthesis especially in ○ Menstrual disturbance
muscles ○ Peptic ulcers
➔ Glucagon ➔ Conn’s Syndrome
★ Glucagon act mostly on the liver and adipose ★ This is due to excessive secretion of
tissues where it antagonizes the actions of insulin mineralocorticoids.
○ Stimulate glycogenolysis

★ It is usually caused by tumor affecting only one 75 amino acids (molecular weight of 5000 daltons
adrenal gland to 7500 daltons) are considered proteins instead of
➔ Addision’s Disease peptides.
★ It is due to hyposecretion of glucocorticoids and ➔ Denaturation can be induced by any condition that
mineralocorticoids disrupts the stabilizing forces such as salts, organic
★ Caused by autoimmune disease solvents, extremes of pH, heating and freezing, and
★ Effects: detergents, although various proteins will have varied
○ Muscle weakness. sensitivities to different denaturants.
○ Vomiting and diarrhea. ➔ Protein = Enzymes split the amino acids apart
○ Tiredness. ➔ Amino Acids = Can be used to build up new proteins
○ Mental confusion. Primary Structure of Proteins
○ Low blood volume.
○ Hypotension. ➔ The particular sequence of amino acids that is the
○ Loss of body hairs in women. backbone of a peptide chain or protein
Adrenal Medulla Secondary Structure – Alpha Helix
➔ It is surrounded by the cortex ➔ Three-dimensional arrangement of amino acids with

➔ It produces two hormones the polypeptide chain in a corkscrew shape ▪ Held by
★ adrenaline and H bonds between the H of –N-H group and the –O of
★ noradrenaline C=O of the fourth amino acid along the chain ▪ Looks
like a coiled “telephone cord”
Adrenaline and Noradrenaline
Secondary Structure – Beta Pleated Sheet
➔ Noradrenaline and adrenaline are released into the
blood ➔ Polypeptide chains are arranged side by side
➔ They are structurally very similar and have similar ➔ Hydrogen bonds form between chains
effects ➔ R groups of extend above and below the sheet
➔ Together they potentiate by: ➔ Typical of fibrous proteins such as silk
★ Increasing heart rate Secondary Structure – Triple Helix
★ Increasing blood pressure ➔ Three polypeptide chains woven together
★ Increasing metabolic rate ➔ Glycine, proline, hydroxy proline and hydroxylysine
★ Dilating the pupils ➔ H bonding between –OH groups gives a strong
Disorders of Adrenal Medulla structure
➔ The effects of excess adrenaline and noradrenaline ➔ Typical of collagen, connective tissue, skin, tendons,
are: and cartilage
★ Hypertension Enzymes
★ Hyperglycemia ➔ Organic catalysts produced by living organisms
★ Raised metabolic rate ➔ Common properties:
★ Nervousness ★ They are colloids and are soluble in water and
★ Headache dilute alcohol and are precipitated by concentrated
Thymus Gland alcohol
➔ Thymus is located in the anterior part of the upper Substrate
mediastinum
➔ At birth it weighs 10-12 gms
➔ During childhood and adolescence 20-30 gms
➔ During old age it weighs 3-6 gms
➔ Functions:
★ It initiates and maintain Tlymphocytes
★ HORMONE: Thymosin
○ It is required for the development of
T-lymphocytes for cell mediated immunity
Proteins ➔ Most enzymes act best at temperatures between 35
and 40°C; temperatures above 65°C, especially in the
➔ are polymers of amino acid joined together by peptide
presence of moisture usually destroy them, whereas
bonds.
their activity is negligible at 0°c
➔ Loss of tertiary structure results in denaturation of the
➔ Certain heavy metals, formaldehyde and free iodine
protein and loss of activity.
retard the enzyme’s activity
➔ What is the difference between a Protein and a
➔ Activity is highly affected by the pH of the medium in
Peptide?
which they act or by the presence of other substances
★ ANSWER: The distinction between proteins and
in the medium
peptides is one of length of the amino acid chain
➔ If the enzyme is combined with organic substance, the
and molecular weight and is somewhat arbitrary,
non protein organic substance is termed as
but generally polypeptide chains in excess of 50 to
COENZYMES.

➔ If the enzyme is combined with inorganic ions, the non ➔ It causes the hydrolysis of fats into glycerin and fatty
protein organic substance is termed as activators acids
6 Major Classes of Enzymes Pectase
Oxidoreductases ➔ Spilts pectin into pectic acid and methyl alcohol
➔ Catalyzing oxidoreductions between two substances Steapsin
Transferases ➔ A lipolytic enzyme capable of digesting dietary fat
➔ Catalyzing a transfer of a group, other than hydrogen, Ureases
between a pair of substances ➔ Obtained from soybean
Hydrolases ➔ Used as a laboratory agent for converting urea to
ammonia
➔ Catalyzing hydrolysis of ester, ether, peptide, glycosyl,
acid anhydride, C-C, C-halide, or P-N bonds Proteolytic Enzymes
Lyases Pepsin
➔ Catalyzing the removal of groups from substrates by ➔ A proteolytic enzyme found in the gastric juice
mechanisms other than hydrolysis, leaving double ➔ Most active at pH 1.8, but in neutral or alkaline media,
bonds pepsin is entirely inactive.
Isomerases ➔ It converts proteins into proteoses and peptones
➔ Catalyzing interconversion of optic, geometric, or Trypsin

positional isomers ➔ Formed when the proenzyme, trypsinogen, is acted on
Ligases by the enterokinase of the intestinal juices.
➔ A proteolytic enzyme that is considerably more active
➔ Catalyzing linkage of two compounds coupled to the than pepsin, converting proteoses and peptones into
breaking of a pyrophosphate bond in ATP or a similar polypeptides and amino acids.
compound. ➔ It acts best in alkaline medium of about pH 8 and may
Amylolytic Enzymes or Carbohydrases thus be distinguished from pepsin, which acts only in
➔ Two well known amylolytic enzyme acid media.
➔ Diastase and amylase- Two well known amylolytic Erepsin
enzyme ➔ A proteolytic enzyme found in intestinal juices. It
➔ Salivary diastase or ptyalin and pancreatic diastase or converts proteoses and peptones into amino acids.
amylopsins are found in the digestive tract of animals.
They are sometimes called animal diastase Renin
➔ Malt diastase is formed during the germination of ➔ Is a coagulating enzyme present in the mucous
barley grains and converts starch into maltose. It is membrane of the stomach of mammals. It curdles the
most active in solutions that are approximately neutral; soluble casein of milk
acidity of pH 4 destroys the enzyme Papain
Invertase or Sucrase ➔ A mixture of active proteolytic enzyme found in the
➔ Found in the yeast and in intestinal juices unripe fruit of papaya tree.
Maltase ➔ It is used as meat tenderizer
➔ Causes the conversion of maltose into glucose, is also Oxidizing Enzymes

found in yeast and intestinal juices Peroxidases
Zymase ➔ Are widely distributed in plants.
➔ Fermenting enzyme causing the conversion of ➔ They bring about the oxidation reactions that cause the
monosaccharides into alcohol and carbon dioxide discoloration of bruised fruits.
Emulsin Thrombin
➔ Enzyme found in almonds. ➔ Converts the fibrinogen of the circulating blood into the
➔ It causes the hydrolysis of Beta-glucosides insoluble fibrin of the blood clot
➔ Amygdalin = benzaldehyde and HCN Zymase
Myrosin ➔ Although splitting monosaccharides, is essentially an
➔ Found in white and black mustard oxidizing enzyme because the monosaccharide is split
➔ It hydrolyses sinalbin, sinigrin and other glycosides by oxidation
Esterases Malt Extract
Lipase ➔ Is the product obtained by extracting malt, the partially

and artificially germinated grain of one or more
➔ A lipolytic enzyme widely distributed in the plant and varieties of Hordeum vulgare.
animal kingdom ➔ Use(s)
➔ It is found in the pancreatic juice of animals oily seeds

★ Used as an easily digested nutrient ★ Accelerate tissue repair especially following
★ As an aid in digesting starch episiotomy
Malt or Malted Barley Trypsin
➔ Is dried, artificially germinated barley grain ➔ Crystallized trypsin is a proteolytic enzyme crystallized
➔ It resembles barley but is more crisp, has an agreeable from the pancreas of the ox, Bos Taurus (Bovidae)
odor and has a sweet taste. ➔ Used for debridement of necrotic and pyogenic surface
➔ Used in brewing and alcohol industries lesions
Barley Chymotrypsin
➔ Dried grain of one or more varieties of Hordeum ➔ is a proteolytic enzyme crystallized from the pancreas
vulgare Linn. Graminae of the ox, Bos Taurus (Bovidae)
Diastase ➔ available as chymotrypsin for ophthalmic solution
➔ Is a yellowish white, amorphous powder obtained from Hyaluronidase

an infusion of malt. It can convert 50 times its weight of ➔ for injection is sterile, dry, soluble, enzyme product
potato starch into sugars. prepared from mammalian testes and capable of
Lactase hydrolyzing mucopolysaccharides of the type of
hyaluronic acid
➔ An enzyme that hydrolyzes LACTOSE into ➔ Use: spreading agent
GALACTOSE AND GLUCOSE
➔ It is obtained commercially from yeast Streptokinase
Pepsin ➔ Is a purified bacterial protein elaborated by group c

beta hemolytic streptococci. It is supplied as
➔ A substance containing a proteolytic enzyme obtained lyophilized powder. It acts to convert plasminogen to
from the glandular layer of the fresh stomach of the the proteolytic enzyme plasmin. PLASMIN degrades
hog, Sus scrofa. not only fibrin clots but also fibrinogen and other
➔ Scaly pepsin-pepsin allowed to dry in glass plates plasma proteins
➔ Spongy pepsin-pepsin evaporated in vacuum ➔ It is indicated for pulmonary embolism, deep vein
➔ USED: Administered to assist gastric digestion thrombosis and embolism, arteriovenous cannula
Pancreatin occlusion and coronary artery thrombosis
➔ Is a substance containing principally AMYLASE, Urokinase
LIPASE, and PROTEASE ➔ Isolated from the human urine or obtained from human
➔ obtained from the pancreas of the hog or of the ox kidney cells by tissue culture techniques
➔ Uses ➔ It acts on the endogenous fibrinolytic system
★ a digestive aid converting plasminogen to the enzyme plasmin.
★ used in the preparation of predigested foods for the PLASMIN degrades not only fibrin clots but also
invalids fibrinogen and other plasma proteins
★ Enteric coated granules have been used to treat ➔ Use: indicated for pulmonary embolism, arteriovenous
infants with celiac disease and related pancreatic cannula occlusion and restoring the patency of
deficiencies intravenous catheters
Pacrelipase Fibrinolysin
➔ Is essentially a more concentrated form of ➔ It is in the blood serum as a protease and in plasma
PANCREATIN fraction with streptokinase
➔ Uses: ➔ Use: used primarily in the treatment of blood clots
★ As a digestive aid within the cardiovascular system, exclusive of the
★ Pancrelipase increases the intestinal absorption of thrombi of the coronary and cerebral arteries
fat, thus aiding in the control of steatorrhea
Sutilains
Chymopapain
➔ derived from the bacterium Bacillus subtilis
➔ A non pyrogenic proteolytic enzyme obtained from the ➔ used for wound debridement
latex of Carica papaya
➔ Use Collagenase
★ Employed in the treatment of herniated lumbar ➔ obtained from the fermentative cultures of Clostridium
intervertebral disk histolyticum
Bromelains ➔ cleaves collagen and is used topically to debride
dermal; ulcers and severely burned areas
➔ Bromelain or Bromelain is the mixture of protein
digesting and milk clotting enzymes obtained from the L-Aspariginase
juice of pineapple plant, Ananas comosus. ➔ Is an enzyme obtained from the cultures of E. coli
➔ Use(s) ➔ Use: Antitumor agent
★ adjunctive therapy to reduce inflammation and
edema
VITAMINS AND ANTIBIOTICS
Vitamins ➔ Increased respiratory infections

➔ May cause hypothyroid state
➔ The word vitamin is derived from a combination of two
words “vital” and “amine” and was first devised by a Vitamin D
polish chemist Casimir Funk in 1912. ➔ The precursor of Vit D is made in the liver. This
Division precursor migrates to the skin and is converted to a
second precursor with the help of UV rays. The liver
Fat-Soluble and kidney convert this second precursor to active
➔ Vit. A vitamin
➔ Vit. D Sources
➔ Vit. E
➔ Fish liver oils
➔ Vit. K
➔ Egg yolk
Water-Soluble ➔ Butter
➔ Vit. B COMPLEX ➔ Light- sprouted Seeds
➔ Vit. C Deficiency
Fat-Soluble Vitamins ➔ Osteomalacia
Vitamin A ➔ Weakness
➔ Rickets
➔ Functions:
➔ Tetany or muscle spasm and pain
★ Eye, Bone, Teeth
★ Helps maintain epithelial integrity, with ZINC Uses
★ Involved in photoreceptors of the retina, particularly ➔ Osteoporosis
rhodopsin formation ➔ Kidney related bone problems
★ Considered to be essential in protecting against ➔ Hypoparathyroidism
infection
Vitamin E (Alpha Tocopherol)
★ An antioxidant
➔ The major form of vitamin A is an alcohol (retinol), but ➔ A potent antioxidant which neutralizes free radicals
can also exist as an aldehyde (retinal), or as an acid ➔ Works with selenium to destroy cell peroxidases
(retinoic acid). Precursors to the vitamin (a provitamin) Sources
are present in foods of plant origin as some of the
➔ Wheat germ oil
members of the carotenoid family of compounds
➔ Sunflower seeds
Sources ➔ Sunflower oil
➔ Fish liver oils ➔ Safflower oil
➔ Animal fats ➔ Almonds
➔ Liver ➔ Peanut oil
➔ Egg yolk ➔ Soybean oil
➔ Apricots ➔ Asparagus
➔ Cantaloupe ➔ Spinach
➔ Peaches ➔ Brown rice
➔ Carrots Deficiency
➔ Yellow and dark green leafy vegetables
➔ May cause blood cells to lyse
Deficiency ➔ Lead to nerve damage and symptoms of lethargy,
➔ Night blindness apathy, inability to concentrate
➔ Prefolicular hyperkeratosis – small bumps around hair Uses
follicles
➔ Decreased the number of sickle cells in persons
➔ Xeropthalmia – corneas become ulcerated and swollen
suffering from sickle cell anemia
➔ First there is dryness of the conjunctiva (xerosis) as
➔ Also used in the treatment of Alzheimer’s disease
the normal lacrimal and mucus secreting epithelium is
➔ Antioxidant
replaced by a keratinized epithelium. This is followed
➔ Acts as anti- blood clotting agent
by the build-up of keratin debris in small opaque
➔ Promotes normal RBC formation
plaques (Bitot's spots) and, eventually, erosion of the
roughened corneal surface with softening and Vitamin K
destruction of the cornea (keratomalacia) and total ➔ K1- Phytonadione
blindness ➔ K2 – Menaquinone
➔ Keratomalacia – thickening of the bone shaft ➔ K3 – Menadione
➔ Decreased immunity ➔ Essential for the synthesis of five proteins involved in
➔ Allergies blood clotting
➔ Loss of tooth enamel, gum disease

➔ It is also involved with calcium in the development of ➔ Yeast
bone ➔ Organ meats
Sources ➔ Milk
➔ Lean meats
➔ Green leafy vegetables ➔ potatoes
➔ Vegetable oils
➔ Soybean oil Deficiency
➔ Wheat bran ➔ Anorexia
➔ Liver ➔ Severe constipation
➔ Milk ➔ Lower stomach acid secretion
➔ Meats ➔ General apathy and fatigue
➔ Egg yolk ➔ Wernicke Korsakoff syndrome
➔ K1 in chlorophyll ➔ Wernicke's encephalopathy (lack of coordination) and
➔ K2 made by intestinal bacteria Korsakoff's psychosis (this effects short term memory)
➔ K3 is synthetic, water soluble Uses
Deficiency ➔ Useful in anemia, megaloblastic anemia
➔ Hemorrhagic diseases ➔ Beriberi
Uses ➔ Alcoholism
➔ Used in blood coagulation Vitamin B2 (Riboflavin)

➔ Osteoporosis ➔ Functions
Water-Soluble Vitamins ★ It is essential for growth, healthy eyes, tissue
respiration.
B Vitamins ★ important coenzyme for the breakdown of
➔ Vitamin B4: Adenine, a E. (1935) — also called carbohydrates, fats and proteins. It is also needed
'Enteral factor' — is a water and alcohol nucleobase for the maintenance of skin and mucous
➔ Vitamin B7: "Vitamin I" of Centanni soluble rice-bran membranes, and has a role in many
factor which prevents digestive disturbance in pigeons. oxidationreduction reactions in the body.
It governs the anatomical and functional integrity of the Sources
intestinal tract. Later found in yeast. Possible
➔ Enriched cereals
candidates for this substance are inositol, niacin
➔ Milk and dairy foods
(nicotinic acid), and biotin. Carnitine was also claimed
➔ Organ meats
to be a candidate but is not soluble in alcohol
➔ Breads
➔ Vitamin B8: adenosine monophosphate, or alternately
➔ Eggs
inositol has also been called vitamin B8
➔ Green leafy vegetable
➔ Vitamin B10: para-aminobenzoic acid, or PABA
➔ Vitamin B11: – Chick growth factor, which is a form of Deficiency
Folic acid. Later found to be one of five folates ➔ Cheilosis -Characteristic cracks at corners of mouth
necessary for humans; (Lcarnitine) is called Vitamin ➔ Glossitis - tongue becomes red swollen
B11 in France ➔ sebborheic dermatitis - Scaly, greasy skin folds
Vitamin B1 ➔ Aversion to bright light
➔ Depression
➔ Function
★ Thiamine plays a large role in energy metabolism Uses
as part of the enzyme thiamine pyrophosphate ➔ Cataract prevention
★ It aids in carbohydrate metabolism ➔ Rheumatoid arthritis
★ Essential for the metabolism of alcohol ➔ Carpal tunnel
★ Thiamine is also required by the nervous system as ➔ Skin disorders
it is a coenzyme in the production of acetylcholine
Vitamin B3 (Niacin)
(a neurotransmitter). A neurotransmitter is a
compound that travels across the synapse (the gap ➔ Functions
between nerve cells) by diffusion and acts as a ★ Participates in energy metabolism as an enzyme
messenger between nerve cells. system (NAD, NADP) for transfer of hydrogen,
metabolism of amino acids and carbohydrates
Sources
★ It is synthesized by intestinal bacteria
➔ Found in brewer’s yeast
Deficiency
➔ Sunflower seeds
➔ Bean ➔ Skin eruptions
➔ Nuts ➔ Dark, scaly dermatitis
➔ Whole grains ➔ Diarrhea
➔ Green vegetables ➔ Nervous depression
➔ Rice bran ➔ Severe deficiency may cause confusion and pellagra
➔ Wheat germ ★ A condition of dermatitis, diarrhea and dementia

Uses ➔ Chicken
➔ Yeast
➔ Used to decrease cholesterol in cardiovascular
➔ Legumes
disease, diabetes, depression, anxiety, insomia,
migraines, nerve conditions Uses
Sources ➔ Prevents hypochromic anemia
➔ Seborrheic dermatitis
➔ Peanuts
➔ Mucous membrane lesions and peripheral neuritis
➔ legumes
➔ Milk Vitamin B9 (Folic Acid)
➔ Fish ➔ Also called vitamin M
➔ Liver ➔ folacin
➔ Meat ➔ pteroylglutamic acid
➔ Poultry ➔ This vitamin often functions in conjunction with other
➔ Many grains vitamins in the body, for example it interacts with
➔ Eggs vitamin B12 in the synthesis of DNA. Also in
Vitamin B5 (Pantothenic Acid) combination with B12 and vitamin C it is used in the
breakdown of proteins and the formation of
➔ Its major role is to combine with other molecules to
hemoglobin.
form coenzyme A, a required compound for energy
metabolism Sources
➔ used in the breakdown of carbohydrates, lipids and ➔ Liver
some amino acids and is also used in the synthesis of ➔ Yeast
coenzyme A. ➔ green vegetables
➔ produced by bacteria that live in the intestine region of ➔ whole grains
the gastrointestinal tract
Deficiency
Sources
➔ macrocytic anemia
➔ FOOD – milligrams of panthothenic acid in 100 gram ➔ elevated levels of homocysteine
portion (approx 3 oz) ➔ in pregnant women can lead to birth defects. (neural
➔ Yeast, brewer’s 12 tube defects)
➔ Yeast, torula 11 ★ Neural tube defects result in malformations of the
➔ Liver, calf 8 spine (spina bifida), skull, and brain (anencephaly).
➔ Liver, beef 3.9 ★ Supplementation is often recommended during
➔ Peanuts 2.8 pregnancy.
Uses Vitamin B12 (Cyanocobalamin)
➔ Malabsorption syndrome ➔ It is important for metabolism, the formation of red
➔ Depression blood cells, and the maintenance of the central
➔ Burning foot syndrome nervous system, which includes the brain and spinal
➔ Pregnancy and lactation cord
Vitamin B6 (Pyridoxine) ➔ This vitamin though cannot be directly absorbed by the
body, for absorption to occur vitamin B12 must
➔ Involved in protein metabolism as a coenzyme,
combine with a mucoprotein that is produced in the
breaking down and the synthesis of amino acids and in
stomach called the intrinsic factor. Once the molecules
the synthesis of unsaturated fatty acids from essential
are bonded together absorption occurs in the small
fatty acids
intestine.
➔ Also involved in hemoglobin synthesis
➔ It is important for maintaining healthy brain function, Sources
the formation of red blood cells, the breakdown of ➔ Beef liver
protein and the synthesis of antibodies in support of ➔ Salt- water fish
the immune system ➔ Oysters
➔ Adult RDA: 2 mg ➔ Brewer’s yeast
➔ Water-soluble ➔ Sea vegetables
Sources ➔ Liver
➔ Kidney
➔ Peanuts
➔ Milk and dairy foods
➔ Fish
➔ Meat eggs
➔ Poultry
➔ Meat bananas Deficiency
➔ Whole grains ➔ Pernicious Anemia
➔ Egg yolk ➔ Noise or light intolerance
➔ Legumes ➔ Achlorhydria
➔ Bran ➔ Progressive peripheral neuropathy
➔ Watermelon

Uses Some Clinically Important Antibiotics
➔ Used in anemia; pernicious anemia, anemia of
pregnancy, macrocytic anemia
➔ Used in neuralgias
Vitamin C
➔ Essential for growth
➔ Plays a role in metabolism of amino acids, conversion
of folic acid
➔ Essential for production of collagen, antioxidant
➔ USES
★ to increase immunity
★ Wound healing
➔ It promotes a healthy immune system, helps wounds
heal, maintains connective tissue and aids in the
absorption of iron
➔ RDA: 60 mg
➔ Water-soluble
Sources
➔ Citrus fruits
➔ Tomato
➔ Melon
➔ Pepper
➔ Raw cabbage
➔ Guava
➔ Pineapple
➔ potato
Deficiency
➔ Scurvy
➔ Fatigue, weakness, muscle cramps
➔ A deficiency of vitamin c may lead to a condition called
scurvy, characterized by weakness, anemia, bruising,
bleeding gums and loose teeth
Names and Roles of Vitamins
➔ Vitamin A (Retinol) - Phototransduction
➔ Vitamin B1 (Thiamine) - Carbohydrate metabolism
➔ Vitamin B2 (Riboflavin) - Redox, respiration
➔ Vitamin B3 (Niacin) - Redox
➔ Vitamin B5 (Pantothenic Acid) - tca, fa, and cholesterol
➔ Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal) - aa
metabolism, glycogenolysis
➔ Vitamin B7 (Biotin) - Gluconeogenesis, tca, fa,
➔ Vitamin B9 (Folic Acid) - IC metabolism
➔ Vitamin B12 (Cobalamin) - IC & H metabolism
➔ Vitamin C (Ascorbic Acid) - Hydroxylation
➔ Vitamin D (Cholecalciferol) - Bone remodeling
➔ Vitamin E (Tocopherols) - Antioxidant
➔ Vitamin K (Phytylmenaquinone,
Multiprenylmenaquinone) - Coagulation, bone
remodeling
BIOLOGICS AND HERBAL SUPPLEMENTS
Biologics Naturally Acquired Active Immunity
➔ Any product derived from a living plant and animal ➔ Example: Recovery from an infection such as measles
source and scarlet fever (Acquired naturally)
➔ The law refers to “any virus”, therapeutic serum, toxin, Artificially Acquired Active Immunity
antitoxin or analogous product.
➔ The immunity may be produced as the response to a
➔ 2 General Categories of Biologics
series of injections (Typhoid or pertussis vaccine), thus
★ Antibodies
stimulating the body cells to make their own antibodies
★ Antigen
and it is developed gradually and usually long-lasting
Antigen Examples: Vaccines and toxoids
➔ A material that provokes the immune response Passive Immunity
➔ Usually a protein
➔ Developed by introduction of preformed antibodies (not
➔ Pollen is an Antigen or an Antibody?
antigens) into the body. ▪ In this type, the body cells
★ ANSWER: Antigen, it provokes the immune system
are not stimulated to produce their own antibodies.
Antibodies ➔ Passive Immunity is the consequence of one person
➔ Found predominantly in serum fraction of the blood receiving preformed immunity made by another person
➔ For Passive Immunity we have:
5 Subclasses
★ Diphtheria antitoxins
IgA ★ Gamma globulin
➔ Most common formed in the mucous membrane Naturally Acquired Passive Immunity
➔ Can be found in body secretions (saliva, tears, breast ➔ Example: the immunity passed into the newborn infant
milk) through transmission of antibodies from the blood of
➔ Considered as MOST ABUNDANT in the body the mother
IgD ➔ It is produced quickly but it is not long lasting
➔ It can be found in the blood, lymph, and in the V cells Artificially Acquired Passive Immunity
surface (hindi ko gaano maintindihan sinabi dito) ➔ Example: Injection of immunizing biologics containing
IgE preformed antibodies in forms such as diptheria
➔ It binds to muscles and basophils participants in the antitoxin or gamma globulin
allergic reactions ➔ Produced quickly, not long lasting
IgG Vaccines
➔ This is most abundant in the serum ➔ It is used as inoculations to stimulate the production of
antibodies
IgM
Herbal Supplements
➔ IgM – “M” MALAKI
➔ It appears first in response to primary infection Origin
➔ Short-lived making it valuable to disease ➔ Primitive men and women treated illnesses using
➔ For diagnosis plants, animal parts, and minerals not part of a
Immunity common diet.
➔ Physical evidence goes back 60,000 years to the burial
➔ IMMUNITY: site of a Neanderthal man who was buried with 8
★ INNATE/NATURAL – (inborn) Genetic factors species of plants.
★ ACQUIRED ➔ Seven of these plants are still used in medicine today.
➔ ACQUIRED:
★ ACTIVE – Own antibodies Herbal Supplements Today
★ PASSIVE – Ready-made antibodies ➔ A resurgence of interest in herbal medicine originated
➔ ACTIVE: in the 1970’s.
★ NATURAL – Exposure to infectious agent ➔ This movement began with people’s disillusionment
★ ARTIFICIAL – Immunization with modern medicine- its high cost and inability to
➔ PASSIVE: cure everything.
★ NATURAL – Material antibodies ➔ Despite the importance of plants and medicines, FDA
★ ARTIFICIAL – Antibodies from other sources considered some herbal medicines to use worthless or
Active Immunity potentially dangerous.
➔ But now herbal medicines or herbal products can only
➔ A specific immunity developed by an individual in be marketed as food supplements and must have the
response to the introduction of antigenic substances FDA’s approval to make specific health claims
into the body
➔ Developed slowly but it is usually long lasting

➔ The partisans of this resurgence were more ➔ In cases of major depression, it may worsen the case.
enthusiastic than knowledgeable. No laws were made ➔ Blurred vision, constipation, urinary retention, and
about labeling products and outrageous claims were excessive drowsiness.
made about the abilities of herbal supplements. ➔ St John’s wort is called the “Herb of Happiness”, why?
Use of Herbal Supplements ★ ANSWER: it is able to treat mild to moderate
depression
➔ PHYSICAL
★ For the treatment of sickness and disease Neem
★ Athletic and Weight-loss purposes. ➔ Azadirachta indica (Meliaceae) ▪ the seed oil (margosa
★ Usual used of herbal supplements is for weight loss oil) has been widely used in Indian medicines.
➔ MENTAL ➔ USES:
★ For the treatment of memory loss, depression, ★ anti-inflammatory
sleep, and stress. ★ antibacterial
Treatment of Sickness and Disease ★ Antipyretic
★ hypoglycemic property
➔ All herbal medicines can be prepared as a tea ★ antifertility agent
➔ Drink a glass 3 times a day, use the dried leaves of the ➔ effect similar to Reye’s syndrome
plant, and usually use about half an ounce of the herb ➔ Characteristic odor of seed due to sulfur containing
Common Herbs compounds.
➔ Leaf has antimalarial activity, against gastric ulcer has
Aloe Vera
been demonstrated
➔ Claims: “Cure all” tonic, for the treatment of acne, ➔ There is also a potential for the development of
burns, minor wounds insecticides: Azadirachtin - active agent
➔ Commonly used as moisturizer ➔ with anti feedant property
➔ Effective for the topical treatment of wounds, burns,
Garlic
and frostbite
➔ Effectiveness varies with product ➔ Claims: Antibiotic, antiviral, general cure all, lowering
★ Advised not to use for internal uses of blood pressure, cholesterol, and regulation of
○ Could lead to abdominal cramping, diarrhea, circulatory system.
loss of potassium, discoloration of urine. ➔ Well studied herb
➔ Commonly used in Europe as an approved remedy for
Karela
cardio vascular conditions and for the use of flu and
➔ Momordica charantia (Cucurbitaceae)- Control of colds
Diabetes ★ Shown to lower cholestreol by 9-12% in 8-16
➔ Used to lower down the level of blood sugar weeks of use.
➔ What are the different Momordica preparations present ★ May also possess antibiotic activities.
in the market? ★ Large doses may cause heartburn
★ ANSWER: Most common is the charantia then
Ginger
meron din ampalaya plus, Momordica tea, karela
➔ Claims: Treatment of arthritis, heart tissue, motion
St. John’s Wort
sickness and nausea.
➔ common name for Hypericum perforatum ➔ Proven to be effective in nausea, motion sickness, and
(Hypericaceae) arthritis.
➔ This is serotonin reuptake inhibitor ➔ It is possible that it treats heart tissue but not likely
➔ The compound in the plant suspected to have ➔ However, there are many precautions for the use of
antidepressant effect ginger.
Uses ★ The use of ginger may inhibit the chemicals
involved in platelet aggression.
➔ Prevent depression
★ This leads to increased and prolonged bleeding
➔ Decrease Stress Levels
➔ Help nervous conditions Peppermint
➔ Decrease severity of bacterial infection ➔ CLAIMS:
➔ treat mild to moderate depression (current use) ★ Muscle Spasms
➔ Anti-inflammatory agent (Greece) ★ Abdominal Pain
➔ It can reduce plasma concentrations of the protease ★ Diarrhea
inhibitor indinavir ★ Irritable Bowl Syndrome
★ Hyperecins- anti depressant principle ★ Chills and nausea
★ Hyperforins also have this property ★ Convulsions
➔ Has been proven to be mildly helpful in very mild to ★ Headaches
moderate cases of depression. The more serious the ➔ Has only been proved to decrease muscle spasms
case, the less that St. John’s Wort helps. In the worst ➔ Overuse can lead to heartburn, esophageal sphincter
cases of depression, it can actually hurt the situation. relaxations, irritation of mucous membranes, and
Side Effects allergic reactions.

Mental Supplements ★ Magazines and tabloids often carry ads for herbal
supplements, usually accompanied by a man with
➔ There are several very popular mental supplements
a body like Brad Pitt or a woman who looks like
designed to aid in memory, stress, depression, sleep,
she’s walked straight out of “Baywatch”.
and other mental related problems.
★ Kapag nagpropromote ng mga supplements na
➔ Although there are only a few of the herbal
pampapayat mga model na ginagamit is mga payat
supplements they are widely used and accepted by the
na talaga or yung may mga itsura na talaga (naol)
public.
★ So in today’s world many people are taking herbal
➔ There are many claims regarding the effectiveness of
supplements to increase their energy and to loss
these supplements, and the only difficult problem is
weight
discovering which claims are true and which are false
➔ Do They Really Work?
Ginkgo Biloba ★ ANSWER: Despite these claims, some experts
➔ CLAIMS AND EFFECTS: have serious doubts about the efficacy of these
★ Improved memory herbal remedies as answers for weight loss and
★ Reduce Alzheimer’s effects energy.
★ Helps hearing loss Exercise and Diet Supplements
★ Helps depression
➔ COMMON SUPPLEMENTS:
★ Helps calm asthma
★ EXERCISE
➔ Ginkgo balboa extract increases blood flow to the brain
○ Ginseng
by inhibiting blood platelet aggregation and by
○ Bell pollen
regulating blood vessel elasticity. It has also been
★ WEIGHT LOSS
shown to improve blood flow through major blood
○ Ephedra
vessels and capillaries.
➔ SIDE EFFECTS: Ginseng
★ Mild Gastrointestinal Upset ➔ Most common form is Asian ginseng
★ Mild Headaches ➔ A perennial herb of northern China, Korea, Japan, and
Sleep Aids Russia
➔ Must be grown for 5 years before harvested
➔ There are many different herbal sleep aids that are
➔ The root is the most widely used part
considered safer than, and sometimes as effective as
➔ Harvested in the fall just before defoliation
prescription sleep aids. These herbs can help sleep by
➔ How it works?
using aromas or teas.
★ Not known…it is suggested that ginseng increases
➔ CLAIMS AND EFFECTS:
cerebrovascular flow
★ Helps Insomnia
➔ DOSAGE:
★ Helps all chronic sleep disorders
★ Usual daily dose is 200mg
★ Helps all chronic sleep disorders
➔ DOES IT WORK?
➔ EXAMPLES OF HERBAL SLEEP AIDS:
★ In a 9-week, double blind, placebo- controlled trial
★ Chamomile (an essence)
of 30 highly trained athletes, treatment with
★ Hops
ginseng produced significant improvements in
★ California Poppy
aerobic capacity
★ Catnip
★ But There were negative results in an 8-week,
★ Lemon Balm
double blind trial that followed 31 healthy men in
★ Lavender
their twenties and another 8-week trial which
★ Passion Flower
showed that ginseng improved aerobic capacity in
★ Skullcap
people who did not exercise, but gave no additional
★ Valerian Root
benefit to those who did.
➔ Herbal sleep aids do work, and actually with little to no
side effects. They are successful at calming and Bee Pollen
relaxing the body and assisting in the reduction of ➔ Referred to as nature’s most complete food
insomnia and other various sleep disorders ➔ Praised in the Bible and ancient Chinese texts
➔ How many of you have seen this? ➔ WHAT IS BEE POLLEN?
★ It is the male seed of a flower blossom which has
been gathered by the bees and to which special
elements from the bees has been added. The
honeybee collects pollen and mixes it with its own
digestive enzymes. One pollen granule contains
from one hundred thousand to five million pollen
spores, each capable of reproducing its entire
species.
★ Bee pollen rejuvenates your body, stimulates
organs and glands, enhances vitality, and brings
about a longer life span.

★ Bee pollen's ability to consistently and noticeably Mugwort
increase energy levels makes it a favorite
➔ Artemisia vulgaris (Asteraceae)
substance among many world class athletes and
those interested in sustaining and enhancing B. Spores
quality performance. ➔ a number of common molds produce spores which
➔ BEE POLLEN CONTAINS: cause rhinitis and asthma in some sensitive individuals
★ 25% complete protein
C. Rhus
★ 18 amino acids
★ 12 vitamins ➔ Toxicodendron spp. (Anacardiaceae)
★ 28 minerals ➔ Rhus radicans (Poison ivy)
★ 11 enzymes ➔ produce severe dermatitis associated with watery
★ 14 beneficial fatty acids blisters which burst and quickly spread macros the
★ 11 carbohydrates skin.
★ Basically, everything needed for human survival ➔ Allergens are contained in the plant sap
➔ The compounds are known as URUSHIOLS and are
Bee Pollen and Exercise
belong to a class of alkenyl polyphenol
➔ Produces an accelerated rate of recovery normal heart
Teratogens
rate and breathing
➔ It provides energy, stamina, and strength, and ➔ MAJORITY CONTAINS NITROGEN
enhances performance levels. ➔ Leucaena leucocephala (Fabaceae)
➔ Improves second performances ➔ Lupins
➔ DOES IT WORK? ★ Lupinus sericeus (Fabaceae)
★ Numerous studies have shown that taking Bee Pesticides
Pollen does in fact increase your energy and
➔ Insecticides
stamina during exercise and repeated events
Pyrethrum Flowers
Ephedra
➔ Insect flowers, Dalmatian Insect flowers
➔ Also known as “Ma Huang”
➔ from Chrysanthemum cinerariifolium (Compositae)
➔ Popular diet supplement in the U.S.
➔ Has been used in Chinese medicine for thousands of Derris and Lonchocarpus
years ➔ Derris (Derris elliptica) Fabaceae and
➔ HOW DOES IT WORK? ➔ Lonchocarpus (Lonchocarpus utilis) Fabaceae
★ Ephedrine alkaloids - naturally occurring ➔ contain about 3-10 % rotenone (isoflavone derivative)
compounds which act as a mild stimulant
Nicotinoids
★ Enhances energy
★ Similar to caffeine ➔ In 1763 nicotine, in the form of tea prepared from
★ Stimulates fat metabolism tobacco recommended for the destruction of aphids
○ Burns fat and sugar more effectively ➔ the insecticidal component is Nacylnornicotine
★ Reduces appetite Sabadilla or Cevadilla Seed
○ Mobilizes stored fat and carbohydrate reserves
➔ contained veratrine
➔ DOES IT WORK?
➔ used as a dust or spray to control thrips and various
★ Numerous studies have shown that ephedra is
true bugs which attack vegetable
effective for losing weight
★ It is most effective when used with caffeine Ryania
★ Popular diet supplements containing ephedra are ➔ Ryania speciosa Salicaceae
Metabolife and MetaboMax ➔ Ryanodine: principal alkaloid
Natural Allergens ➔ used to control lepidopterous larvae which attack fruits
➔ A. Pollen – responsible for seasonal hay fever, which
may progress to chronic asthma
Cocksfoot
➔ Dactylis glomerata (Poaceae)
Timothy
➔ Phleum pratensis (Poaceae)
Perennial Rye
➔ Lolium perenne (Poaceae)
Pollen of Nettle
➔ Urtica dioca (Urticaceae)
Plantain
➔ Plantago spp. (Plantaginaceae)

PCOG211Lec FINALS 1

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PCOG211Lec FINALS 1

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PHARMACOGNOSY AND PLANT CHEMISTRY LECTURE - FINALS 2nd Semester

Instructor: Ms. Maria Suzette Agluba, RPh A.Y. 2022-2023

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Alkaloids ★ Labiatae (Mint Family)

➔ Definition: the term “alkaloid (” alkali- like) is commonly

★ Papaveraceae (Poppy Family)

➔ FAMILIES FREE IN ALKALOIDS

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➔ Imidazole (e.g. pilocarpine)

➔ MAJOR TYPES OF ALKALOIDS, THEIR AMINO

➔ Purine (e.g. caffeine)

➔ Steroidal (e.g. Solanum and Veratrum alkaloids)

➔ Tropane (e.g. Atropine)

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Isoquinoline Alkaloids Ipecac

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Papaverine Inhibition of NE Synthesis

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➔ It is stable in air but is affected by light. Ephedrine

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ENDOCRINE PRODUCTS AND ENZYMES

Glands ○ Somatomedins are synthesized in the liver, in

Endocrine Glands Diseases Related to Growth Hormone

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Adrenal Medulla Secondary Structure – Alpha Helix

➔ It is surrounded by the cortex ➔ Three-dimensional arrangement of amino acids with

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➔ Catalyzing interconversion of optic, geometric, or Trypsin

➔ Causes the conversion of maltose into glucose, is also Oxidizing Enzymes

Esterases Malt Extract

Lipase ➔ Is the product obtained by extracting malt, the partially

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➔ Is a yellowish white, amorphous powder obtained from Hyaluronidase

Pepsin ➔ Is a purified bacterial protein elaborated by group c

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VITAMINS AND ANTIBIOTICS

Vitamins ➔ Increased respiratory infections

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➔ Used in blood coagulation Vitamin B2 (Riboflavin)

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BIOLOGICS AND HERBAL SUPPLEMENTS

Biologics Naturally Acquired Active Immunity

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