Pharma Presentation No.1 (Natural Drugs) Hafsa Farooq (102,222590) 7th M

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NATURAL

DRUGS
PREPARED BY:
HAFSA FAROOQ
Roll no: 102 (222590)
7th Semester (M)
Contents
Overview of key ideas
 What Are Natural Drugs?
 Rise In Modern Era
 Sources
 Research And Biodiversity
 Usage
 Safety And Efficacy
 Storage
 Commonly Used Natural Drugs
1 What Are Natural Drugs?

The Introduction, An Overview


Natural Drugs
The Introduction

“A number of natural products have been found to be useful as


drugs.”
One way to make those drugs available to humans is to harvest the
natural products, extract the active ingredient, and make that
ingredient available as a drug. That process is long and difficult,
and it may often threaten the survival of the organism from which
the drug is obtained.
A far better approach is to determine the chemical
structure of the active ingredient and then to find a way of making
that chemical in the laboratory. Once a method for synthesizing the
chemical has been determined, preparing the drug becomes a
routine process of chemical production.
2 Rise In Modern Era
Use Of Modern Chemistry
Prior to the 19th century, practitioners of the healing arts knew essentially nothing about

VOLUTIO
either the chemical composition of natural products or the mechanisms by which they work.
That situation began to change in the early 1800s with the rise of organic chemistry.
• One of the first chemicals to be purified from a natural product for use as a drug was Morphine. In
1805, the German chemist Friedrich Wilhelm Sertürner (1783–1841) isolated the compound from
opium while trying to find out how that substance induces sleep.
• Finally, in 1925, the English chemist Sir Robert Robinson determined the structural formula for
morphine.
• The most effective of the quinine analogs mefloquine was developed during the Vietnam War as the
result of a program developed by the Walter Reed Army Institute for Research to protect American
soldiers against malaria.
• In 1972 Chinese scientists identified the active ingredient in qinghoa, a substance they called
qinghaosu.
Those accomplishments have formed the basis of a whole new phase of the pharmaceutical industry in
which natural products and their derivatives provide an extensive source of new drugs.
3 SOURCES
MICRORGANISMS
Plants remained essentially the sole source of natural product
drugs until well into the 20th century. Then in 1928 the
discovery of penicillin by the Scottish bacteriologist Sir
Alexander Fleming (1881–1955) opened an entirely new area of
research in the field of anti-infective drugs.
• Penicillin was only the first of a new category of drugs that
came to be called antibiotics.
• Scientists discovered a flood of new antibiotics in a relatively
short period of time:

 Streptomycin, by Waksman in 1943.


 Bacitracin, by American bacteriologist Frank Meleney in 1943.
 The Cephalosporins, by Giuseppe Brotzu in 1945.
 Chloramphenicol, by the research team of John Ehrlich, Paul Burkholder
and David Gotlieb, in 1947.
 Chlortetracycline, by the American plant physiologist Benjamin Minge
Duggar in 1947.
People have long used marine organisms as the source of a
limited number of synthetic products used in everyday life.
Perhaps, the most famous of these organisms has been the
mollusk Murex brandaris, from which a beautiful purple dye
can be extracted.

Researchers at the University of California have extracted an


anti-inflammatory agent, which they named pseudopterosin,
from a Caribbean sea whip called Pseudopterogorgia
elisabethae. Pseudopterosin is currently used as an additive to a
cosmetic skin cream called Resilience® produced by Estée
Lauder.

Another commercially available product containing naturally

Marine occurring marine products is Formulaid®, produced by Martek


Biosciences as a nutritional supplement for infant formulas.

Organisms
An especially intriguing pair of products obtained from marine
organisms in recent years are Vent® and Deep Vent® DNA
polymerase. These products are used in DNA research studies.
Since 1960, only seven plant-derived drugs have been approved
by the FDA for use as anticancer agents. Four of those drugs,
vinblastine, vincristine, etoposide, and teniposide, were
discovered in the 1950s. The last three Taxol®, topotecan, and
irinotecan—were discovered and approved much more
recently.
Robert Noble isolated two chemicals from the periwinkle
leaves, which he named vinblastine and vincristine, that
markedly decreased white blood cell counts in patients with
certain forms of cancer.

By 1985, the FDA had approved two compounds derived from


camptothecin, Hycamtin® and Camptostar®, for use against

PLANT
ovarian and colon cancer.
SOME OTHER EXAMPLES:
 Combretastatin A4, isolated from the South African medicinal tree,
Combretum caffrump.
 Homoharringtonine, from the tree Cephalotaxus harringtonia
found in mainland China.
 Ingenol 3-O-angelate, originally obtained from a common English
PRODUCTS
and Australian tree Euphorbia peplus, etc.
4 RESEARCH AND
BIODIVERSITY
Reasearch And
Biodiversity
The widespread popularity of some natural products has resulted in
their rapid destruction in the environment

• The popularity of Ginseng has already led to its extinction in some parts of the world (such as South Korea) and to its
classification as an endangered species in other parts (such as China) due to overharvesting.
• Goldenseal is yet another threatened herb in the United States and other parts of the world. It currently sells for about
$100 a pound, making it highly popular for individual, independent workers who tear it out of its natural habitat.
• Scientists have no idea how many species there are in the world, but reasonable estimates place the numbers at about
250,000 plant species and up to 1 million marine species. So far, no more than about 10 percent of all plants and 1
percent of all marine organisms have been studied for possible use as drugs.
Such losses are potentially serious problems for drug research. Maintaining biodiversity is an essential component of future
research efforts to identify possible drugs in the world’s plant and marine resources
5 USAGE
• Echinacea – to stimulate the immune system and aid the body in
fighting infection. Used to treat ailments such as boils, fever and
herpes.
• Dong quai (dang gui) – used for gynaecological complaints
such as premenstrual tension, menopause symptoms and period
pain. Some studies indicate that dong quai can lower blood
pressure.
• Garlic – used to reduce the risk of heart disease by lowering
levels of blood fats and cholesterol (a type of blood fat). The
antibiotic and antiviral properties of garlic mean that it is also
used to fight colds, sinusitis and other respiratory infections.
• Ginger – many studies have shown ginger to be useful in
treating nausea, including motion sickness and morning
sickness.
• Ginkgo biloba – commonly used to treat poor blood circulation
and tinnitus (ringing in the ears).
• Ginseng – generally used to treat fatigue, for example during
recovery from illness. It is also used to reduce blood pressure and
cholesterol levels, however overuse of ginseng has been
associated with raised blood pressure
6 SAFETY
AND
EFFICACY
Safety And Efficacy
In reference to medications, safety is the likelihood of not causing
harm under the proposed conditions of use, while efficacy is the
capacity to induce a clinical benefit. Randomized clinical trials
controlled with placebos reveal a number of potential adverse
effects associated with drug treatment.

A number of traditionally used medicinal plants and their


constituents are suspected of being human and/or
rodent carcinogens. Because a vast majority of herbal medicines
and their constituents have not undergone any screening for
carcinogenicity.

Severity of drug-induced liver toxicity (DILI) ranges from mild


dysfunction leading to raised serum levels of alanine
aminotransferase (ALT) unaccompanied by increases
in bilirubin levels and clinical symptoms reversible upon treatment
discontinuation, to jaundice and overt hepatic failure that could
culminate in liver transplantation or death. 
7 STORAGE
Storage
Natural drugs include herbs, herbal materials, herbal preparations and finished herbal products.
Storage of crude drugs in dry condition in airtight container placed in dry dark place is very
important for stability and quality maintenance.

Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so.
Properly discard this product when it is expired or no longer needed. Consult your pharmacist or
local waste disposal company for more details about how to safely discard your product.
8 SOME
COMMONLY USED
NATURAL DRUGS
1. MORPHINE
Morphine is used to relieve

Why is it
moderate to severe pain.
Morphine extended-release

Prescribed?
tablets and capsules are only
used to relieve severe
(around-the-clock) pain that
cannot be controlled by the
use of other pain
medications.

Morphine is in a class of
Class of medications called opiate
(narcotic) analgesics.
Medication
DOSAGE
Morphine injection may be administered subcutaneously, intramuscularly or intravenously.

Administration Adults and adolescents over 12 years


Intravenously 2.5-10mg

Subcutaneously, intramuscularly 5 - 20 mg
Morphine is a popular narcotic analgesic that is
derived from the opium poppy, Papaver
somniferum.

SOURCE

• Seizures • Rash • Blue or purple color


• Nausea • Itching to skin
• Dizziness • Hoarseness • Agitation
• Fever • Swelling • Hallucnations

SIDE EFFECTS • Chest pain • Rash • Shivering


CHEMISTRY
Structure
Molecular Formula C17H19NO3

Molecular Weight 285.34 g/mol

morphine
Morphinum
Morphium
Synonyms
Morphin
l-Morphine
57-27-2

Chemical safety Irritant


CHEMISTRY
The structure of morphine proposed in the 1920s by J.M. Gulland and
R. Robinson was confirmed in 1952 by its total synthesis,
accomplished by M. Gates and G. Tschudi. Synthetic organic chemistry
also has provided a number of compounds
(as meperidine, methadone, and pentazocine) that have in part
supplanted morphine in medical use.

Morphine is extracted from the dried milky exudate of


the unripe seed capsule of the opium poppy (Papaver
somniferum). It occurs as colourless crystals or a white
crystalline powder.
2. SUDAFED
Pseudoephedrine is used for

Why is it
the temporary relief of stuffy
nose and sinus pain/pressure

Prescribed?
caused by infection (such as
the common cold, flu) or
other breathing illnesses
(such as hay
fever, allergies, bronchitis).  

Class of Pseudoephedrine belongs to


Amphetamine class.

Medication
DOSAGE
Do not take the day and night tablets at the same time. Do not take more than a total of 6
tablets in a 24-hour period. Take only as directed.

Administration Adults and children 12 years and over

Ask a doctor Take 1 tablet every 4 hours

Use only as directed. Do not take more than 6 tablets in 24 hours


Pseudoephedrine is a natural substance that
occurs in shrubs of the Ephedra genus, which
grow worldwide.

SOURCE

• Sickness • Dry mouth • Irregular heart


• Nausea • Headache beats
• Dizziness • Hoarseness • Nervous
• Fever • Increased blood • Shaky

SIDE EFFECTS • Chest pain pressure • Shivering


CHEMISTRY
Structure
Molecular Formula C10H15NO

Molecular Weight 165.23 g/mol

PSEUDOEPHEDRINE
(+)-Pseudoephedrine
Synonyms d-Pseudoephedrine
Isoephedrine
Sudafed

Chemical safety Irritant


CHEMISTRY
Although pseudoephedrine occurs naturally as an alkaloid in certain
plant species, as a constituent of extracts from the Ephedra species, the
majority of pseudoephedrine produced for commercial use is derived
from yeast fermentation of dextrose
 in the presence of benzaldehyde. In this process, specialized strains of
yeast (typically a variety of Candida utilis or Saccharomyces cerevisiae)
are added to large vats containing water, dextrose and the
enzyme pyruvate decarboxylase . After the yeast has begun fermenting
the dextrose, the benzaldehyde is added to the vats, and in this
environment the yeast converts the ingredients to the precursor l-
phenylacetylcarbinol (L-PAC). L-PAC is then chemically converted to
pseudoephedrine via reductive amination.
.
3. ASPIRIN
Aspirin is a common drug

Why is it
for relieving minor aches,
pains, and fevers. People
also use it as an anti-
inflammatory or a blood Prescribed?
thinner. 

Aspirin is a nonsteroidal anti-


Class of inflammatory drug (NSAID). It
was the first of this class of drug
Medication to be discovered.
DOSAGE
Aspirin should be taken with food. Doses range from 50 mg to 6000 mg daily depending on the use.

For Rheumatoid Arthritis Adult Dose For Fever


Initial dose: 3 g orally per day in divided doses Oral: 300 to 650 mg orally every 4 to 6 hours as
Maintenance: Adjust dose as needed for anti- needed
inflammatory efficacy Maximum dose: 4 g in 24 hours
It comes from Spiraea, a biological genus of shrubs that
includes natural sources of the drug's key ingredient:
salicylic acid. This acid, resembling what's in modern-
day aspirin, can be found in jasmine, beans, peas, clover
and certain grasses and trees.
SOURCE

• Ulcerations • Headache
• Abdominal Burning • Nausea
• Pain • Gastritis 
• Cramping • Liver Toxicity.
SIDE EFFECTS
CHEMISTRY
Structure
Molecular Formula C9H8O4 or HC9H7O4

Molecular Weight 180.16 g/mol

aspirin
ACETYLSALICYLIC ACID
Synonyms 50-78-2
2-Acetoxybenzoic acid
2-(Acetyloxy)benzoic acid

Chemical safety Irritant


CHEMISTRY
Aspirin is prepared by chemical synthesis from salicylic acid, through
acetylation with acetic anhydride. Prostaglandins are found throughout the
body and are made to help manage injury or infection. Prostaglandins up
regulate the sensitivity of pain receptors. As a control mechanism, they act
locally at the site of synthesis which limits the extent of their activity. They
are also broken down rapidly by the body. The enzymes that produce
prostaglandins are cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2),
they have diverse roles and are widely dispersed throughout body tissue. 
Cox-1 has a protective role for the stomach lining and COX-2 is involved in
pain and inflammation. Aspirin binds to and acetylates serine (an amino acid
used by the body to make proteins) residues in the active site of
cyclooxygenase enzymes, leading to reduced production of prostaglandin.
This in turn mediates aspirin’s effect of reduced inflammation and pain in
affected tissues. Additionally, aspirin acts on prostaglandins in the
hypothalamus to reset and reduce a raised body temperature. Importantly,
aspirin does not decrease normal body temperature.
Thank
you

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