21/11/1435

Introduction (p.3 -6) Introduction (p.3 -6)

Herbal Medicine
referred to as Phytotherapy, Herbalism, Phytomedicine
Herbal Medicine
or Botanical Medicine as preferred by FDA. , It is:

**The use of herbs for their therapeutic or medicinal value.

**The type of medicine that Capasso, Francesco, et al. Phytotherapy: A Quick Reference to
Herbal Medicine. Berlin, Heidelberg: Springer-Verlag, 2003
uses plants or their crude products in treatment of diseases.
An herb:
is a plant or plant part valued for its medicinal or aromatic
qualities.
It produces and contains a variety of chemical substances that
act upon the body.
Course Specification
Herbal medicines originated from the
ancient use of wild plants.

Introduction (p.3 -6)

Historical Background
Facts about Herbal Medicine
– Herbal medicine is the oldest form of healthcare known to
*The German Commission E: mankind.
 *A special committee of the Federal Department of
Health in Germany – Herbs had been used by all cultures throughout history.
– It was an integral part of the development of modern civilization.
 A consulting body appointed by the German, equivalent
to the FDA in U.S. – Primitive man observed and appreciated the great diversity of
plants available to him.
 Was constituted (1990) – The plants provided food, clothing, shelter, and medicine.
 24 experts (naturalists, doctors, chemists, and – Most of the medicinal uses of plants have been developed:
pharmacologists) ** through observations of wild animals,
** by trial and error.
 *They were given the task of collecting and evaluating
existing documentation on phytopharmaceutical – The scientifically collected information on herbs,
products. developed the well-defined herbal pharmacopoeias.
4

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Historical Background Historical Background

The German Commission E: * The German Commission E:

elaborated more than 300 monographs,
 The monographs with well defined qualitative and
quantitative standards approved by the German each devoted to a single drug including:
Commission E, have been inserted in the German  Historical information
pharmacopoeia.
 Chemical, pharmacological, clinical and toxicological
studies
 Currently, herbal substances conforming to the  Case reports, epidemiological data
requirements in the German Commission E monographs
 Unpublished manufacturer’s data
can be authorized for sale .

6 5

Introduction (p.3 -6) Introduction (p.3 -6)

-Herbal medicines are also in great demand in the
developed world for primary health care because of their
efficacy, safety and lesser side effects.
- They also offer therapeutics for age-related disorders like
memory loss, osteoporosis, immune disorders, etc. for which no
modern medicine is available.
the basis for a large
- Substances derived from the plants remain
proportion of the commercial medications used today for
the treatment of heart disease, high blood pressure, pain, asthma, and
other problems. For example:
Ephedra herb used in TCM for more than 2000 years to treat asthma
and other respiratory problems.
Ephedrine, (Act. const. of Ephedra) is used in the commercial
pharmaceutical preparations for the relief of asthma symptoms and
other respiratory problems. It helps the patient to breathe more easily.
– Indeed, well into the 20th century most of the
pharmacopoeia of scientific medicine was derived
from the herbal tradition of native peoples.
– Many drugs commonly used today are of herbal origin.
– Indeed, about 25 % of the prescription drugs dispensed
in the United States
** contain at least one active ingredient derived from plant
material.
** Some are made from plant extracts;
** others are synthesized to mimic a natural plant compound.
– Official herbal plants and their products have great
social and economic importance as:
* they are used today in four principles sectors:
(Food, Cosmetics, Health and Medicine).

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Introduction (p.3 -6)

By the beginning of the 20th century, about 110 years ago, Historical Background
Modern Pharmaceutical Manufacturers Another example of the use of an herbal preparation in
were primarily involved in modern medicine is:

marketing and developing ,Extracting

the active constituents present in
.medicinal plants  Foxglove plant:
Correlation between
 This herb had been in use since 1775.
Chemical Structure Biological Activity
 At present, the powdered leaf of this plant is
This initiates the newly formed pharmaceutical companies to
identify, test and develop successfully Potential New Drugs known as the cardiac stimulant digitalis to
Depends on the
intellectual the millions of heart patients it keeps alive
cooperation of
worldwide.
Pharmacognosy Pharmacology
Medicinal chemistry
(Medicinal botany) 9

Introduction (p.3 -6)

Definitions: Industrialized countries

Herbs:
include crude plant material such as leaves, flowers, fruits,
seeds, stems, woods, barks, roots, rhizomes or other plant Synthetic drugs Medicinal plants
parts, which may be entire, fragmented or powdered.

Herbal materials: include, in addition to herbs, fresh juices, USA ,Canada ,England , Germany ,France ,Italy ,
gums, fixed oils, essential oils, resins and dry powders of herbs. Australia Austria

Herbal preparations: These are the basis for finished herbal products. Herbal medicines offer these advantages compared to conventional
They may include comminuted or powdered herbal materials, or medicines:
extracts, tinctures and fatty oils of herbal materials. Relative safety
Lack of significant side effects
They are produced by extraction, fractionation, purification, Generally lower cost
concentration, or other physical or biological processes.
The use of herbs also has application as adjuncts to complement
 They also include preparations made by steeping or heating herbal
traditional pharmacotherapy.
materials in alcoholic beverages and/or honey, or others.

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Finished herbal products:

Definitions: consist of herbal preparations made from one or more herbs.
(contu.) If more than one herb is used, the term mixture herbal product.

herbal remedy is not synonymous for homeopathic
remedy as frequently stated by people and practitioners.
• Herbal remedies
Contain active principles which exert a pharmacological effect
while
• Homeopathic remedies
Contain herbal and active principles in amounts so low to be
immeasurable (a sufficient molecular memory exerts a therapeutic effect).
“let like be cured by like” using substances which
produce symptoms
e.g. Zicam Cold Remedy is marketed as “homeopathic" product. It contains a
number of highly diluted ingredients as [93] histamine dihydrochloride
 - Finished and mixture herbal products may contain excipients in
addition to the active ingredients. However,
 - Finished products or mixture products to which chemically
defined active substances have been added, including synthetic
compounds and/ or isolated constituents from herbal materials,
are not considered to be herbal.
Phytopharmaceutical:
• A term used for those medicinal preparations made by extracting
botanical products with appropriate solvents to yield extracts, tinctures ,..
• Ideally, such preparations have been standardized to :
* a chemical marker or
* a pharmacologically active constituents, named
"active principles".

Forms of Herbs
 The goal of the herbalist is to release the volatile oils, Definitions:
antibiotics, aromatics, and other healing chemicals contained by (contu.)
the herb.
 Herbs can be prepared in a variety of forms,
depending on their purpose. Such techniques include: Pharmacopoeia
 Juice squeezed from herbs. • An official book, which lists all the
 Mashing herbs into a paste. medicines and the characteristics that those
 Decoction or extracting the active ingredients by boiling down the must posses in order to go on sale.
herb in water.
 Hot infusion (like hot tea) - Herb is steeped in hot water. Crude drugs, botanical medicines,
 Cold infusion (like sun tea) - Herb is steeped in cold water. phytomedicines and phytopharmaceuticals,
 Herbs ground into a powder and used as such or as like conventional medicines
compressed into a pill. should be included in every
country's Pharmacopoeia.
 Herbal wine made by adding the herb to water and sugar
and letting it ferment.

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* Requirements for the preparation of
medicinal plant products from a plant:
1-Selection of the plant
2-Identity of the plant
3- Phytochemical study of the drug
4-Pharmacological study of the drug
5-Pharmaceutical formulation
6-Clinical studies
18
(Contu.)
3- Phytochemical study of the drug:
* Preparation of the aqueous and hydro-
alcoholic extracts.
* Qualitative screening of the extracts.
* Fractionation of the extracts
(by solvents with different polarities).
* Preparation of the specified extracts and
fractions, to be tested pharmacologically.
* Preparation of standardized extract or fraction
(according to the active constituents, after the
pharmacological screening).
5
Forms of Herbs (Contu.)
 Tincture, made by combining ground herbs with alcohol,
glycerin or vinegar and used internally.
 Liniment - Made like a tincture except it is used externally.
 Ointments made by adding herbs to a medium such as
petroleum jelly.
 Syrups - Made by adding herb to a medium such as honey,
sugar or glycerin.
 Poultice - Herb is applied directly to a wound or body part
and held in place with a cloth.
 Herbal Oil - Usually made with common base oil, such as
olive, almond, grape seed, or sesame oils. The herb is
allowed to sit in the oil for a week. It is strained and bottled.
 In general,
delicate leaves and flowers are best infused.
(Boiling may cause them to lose the volatile essential oils).
Roots, barks and seeds are best made into decoctions.
Requirements for the preparation of
medicinal plant products from a plant
1- Selection of the plant: depends on:
** Folk medicinal use.
** Safety and efficacy (long term use of the drug).
** Good literature survey.
2- Identity of the plant:
* Latin name of the plant followed by the plant organ:
e.g. Digitalis purpurea leaves.
* Source of the plant (wild, cultivated or imported).
* Macro-and micro-morphological identification of the
drug.
* The form of the drug (entire, small pieces or powder).
* The process of production of herbal drug preparation.
21/11/1435

(Contu.) (Contu.)

4 - Pharmacological study of the drug:

5 - Pharmaceutical formulation of the - Preliminary pharmacological screening
active extract or fraction in a dosage (in-vitro and in-vivo tests); should be carried out on

form: specified extracts and fractions).

To be studied in clinical trials. This pharmacological-guided screening leads to:

6 - Clinical studies on the standardized ** Detection of the active extract, fraction(s) and
constituent(s).
formulated drug:
** Determination of LD50 of the drug.
The chemical complexity of herbal medicines
** Preliminary estimation of the therapeutic dose
causes multiple effects in humans which must be
of the drug.
tested only throughout clinical trials.

Neutraceuticals
include
Functional foods Medical foods Dietary supplements
Functional foods ( Medicinal foods)
Modified food or food ingredient included in potentially healthy
products, to provide health benefits beyond the traditional nutrients it
contains. Fermented foods or foods fortified with vitamins
Medical foods
Special dietary foods intended for use solely under medical
supervision to meet nutritional requirements in specific medical conditions.
foods for management of diabetes mellitus generally contain slowly
digested carbohydrates
Dietary supplements Products intended to supplement the diet;
they contain one or more of the following dietary ingredients:
Vitamin, mineral, herb, amino acids a dietary substance (flavonoids,
carotenoids, terpenoids, catechins, polyphenols, phytoestrogen, protease
inhibitors) a concentrate metabolite, constituent or extract.
Definitions:
(contu.)
Nutraceuticals
- Food-derived nutrients which at
o doses sometimes exceeding their minimal daily requirement,
o have beneficial pharmacological effects.
- Nutraceuticals support human health or return one to relative
health from a disease or medical disorder.
- Only during the last 50 years,
Foods are being scientifically investigated for their ability to
prevent or reduce the risk of life style related diseases such as
cardiovascular diseases, diabetes and cancer.
- Common nutraceuticals:
Vitamins , minerals, plant-derived antioxidants
such as flavonoids, isoflavones and proanthocyanidins.

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Nutraceuticals also used to help individuals having

general weakness (without specific disease), such as Types of Nutraceuticals products:
Children (infants) need more of certain specific nutrients,
vitamins and minerals.
Potential
Elderly (illness, multiple medicine & aging) need more (May become established only after clinical data have Established
nutrients than that recommended for their age. demonstrated a benefit)

Women (during pregnancy & breast-feeding), need to take

adequate amounts of vitamins (folic acid), minerals and amino
acids.
People (who use specific medicines) & have deficiency in some
nutrients
Antibiotics  vitamin K & H
Anticonvulsants  Folic acid, calcium phosphate, vitamin B, D3, K
Corticosteroids  Calcium, potassium, vitamin C, B6, D3, zinc
Diuretics  Calcium, magnesium, potassium, zinc
Oral contraceptives & estrogens  Folic acid, vitamin C, B6, B12
Alcohols & Smoking  Folic acid, vitamin B6.
Nutraceuticals must be standardized (Contain the same
amount of active compounds per dose), because these products
may be defined and formulated differently by the manufacturers.
Pharmacopoeial standards for identity and quality of
Nutraceuticals, including:
 Microbial limit test
 Disintegration and dissolution of nutritional substances
 Weight variation of nutritional substances
 Manufacturing practices

The Complexity of Herbal Medicines The Dietary Supplement and Health Education
Act (DSHEA)
 The quality of herbal medicine is believed to * in 1994, this committee has provided for herbs and botanical
be directly related to its active principles preparations to be available for sale as dietary supplements,
(secondary plant metabolites). so
D.S. do not have to be subjected to FDA regulation
 Usually the medicinal effects of before marketing.
the entire plant Herb supplements are currently being used by more
were found to be better than than 80% of the global population.
the sum of the isolated components. The most popular herbal supplements currently
used in the world including:
Ginseng, Garlic, Grape seeds,
Green tea, Liquorice, Onion,
Psylium, Red clover, Soy, …..

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The Complexity of Herbal Medicines: The Complexity of Herbal Medicines:

 B -There is also the possibility of interactions between plant
constituents
 These agents may be closely related both chemically and
therapeutically to the main constituents responsible for the
pharmacological activity. for example
Foxglove,, contains about 30 different closely related glycosides.
These cardiotonic agents, with small structural differences, have
different rates of onset of action and
different durations of their effects:
* digitoxin, given orally, has an onset of action of 1- 4 hours with
peak activity at 8-14 hours;
* digoxin has an onset of action of 1/2 -2 hours and
reaches a peak activity level in 2-6 hours).
For these reasons:
Foxglove preparations provide an activity of short onset
and long duration but they are very seldom used
because it is difficult to standardize.
 A - herbal medicine contain other constituents (either in
large or small amounts), which may
improve the efficacy of the active principles. Examples:
Aromatic or bitter substances,
stimulate the gastric and intestinal secretions, thus
making the dissolution and the absorption of the active principle
more complete.
Saponins
(are very common in vegetable plants, as the salt of organic acids )
- may facilitate intestinal absorption of active plant constituents,
through effects on intestinal motility or bile secretion.
Mucilage and pectin substances, vitamins can
modify the functions of the intestine mucous membrane
and consequently the absorption

The Complexity of Herbal Medicines:

The Complexity of Herbal Medicines:
Differences between Herbal and Conventional medicines:
C - Sometimes the herbal medicine may contain
Medicine a variety of pharmacologically active constituents
that
Herbal Conventional are not related chemically or therapeutically.
(St. John's Wort) (Prozac)

- several active principles - one active principle

(in low concentration)
 - other substances
(salt of organic acids, bitter and
aromatic substances , tannins,
saponins, mucilages, minerals,
pectic substances, etc)
 - Complex Medicine
Promoted for several divergent uses
(in high concentration) In most cases,herbal medicines represent a
synergic complex of active constituents,
- other substance
(excipient) whose actions and applications can be
difficult to reproduce.
Contrary of conventional drugs,
herbal medicine must be as a complex
- Simple Medicine pharmaceutical preparation
Singular indication
(preferably in the form of an extract).

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On the other hand, there is a native view that:
* what are natural can only be good
* the belief that herbal medicines are completely
innocuous in contrast to conventional medicines.
The safety reputation of herbs may be due to:
• The use of herbal medicines by millions of people since
long time.
• Herbal medicines promote healing responses rather
than obstacle pathologies
(because herbs have a complex chemical composition).
• Herbal medicines are free from adverse effects, because:
(they are used at lower effective doses than conventional medicines).
• Absence of serious information about adverse reactions
and toxicity of herbs.
If a preparation of a given herb is shown
to be effective,
• this does not necessarily mean that another
preparation of the same drug is similarly
effective.
• The use of preparations inadequately
standardized involves :
* a considerable risk of distortion &
* produces a false negative overall result.
9
•Chapter 5 (p. 13 – 20)
Are the Herbal Medicines Safe?
Adverse reactions are impossible to be completely
eliminated Because these are:
• Part of the normal pharmacological actions of
all medicines.
• Represent an indirect consequence of the
principle action of the medicine.
• Such reactions, being pharmacologically predictable
and dose –dependent,
can be - anticipated
- reduced by dose reduction
but never eliminated. So,
The statement that medicines are safe and effective
is very relative.
Many herbal medicines widely available today
have not been properly evaluated for their
undesirable effects in clinical studies.
The situation is complicated in several ways:
• The sources of the herbal material are variable.
• The active (toxic) components vary
(as a result of climate, soil quality, genetic factors
and exposure to chemicals).
• Lack of quality control, which may lead to:
** contaminations with heavy metals or microorganisms.
** adulteration with botanicals and/or chemicals during
preparation, storage or shipping.
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Drugs improperly standardized for Standardization of herbal medicines

therapeutic activity by their level of : may solve these problems,
but it makes little sense when:
e.g. Echinacea  echinacosides.
* Most herbal medicines yet to yield identity
St. John`s wort  hypericin of their pharmacologically active principles.

* Trials for standardization are obstructed by

** Currently the 0.3% hypericin of St John`s Wort the complex composition of herbs.
has been found to be inactive as
an anti-depressant compared to "hyperforin.“ * The active principles may antagonist or
agonist themselves.
Because of this:
the Germans are now revamping their products
The problem is to determine the active component
to standardize to hyperforin.
upon which standardization will be based.

To carry out reliable clinical trials

The use of cultivated rather than wild the herbal medicines
plants may reduce some causes of must be of standardized quality.
inconstancy of chemical composition.
"Standardization" means:
Cultivated plants : the body of information and controls
* grow in homogeneous climatic conditions,
that are necessary to guarantee:
* harvested quickly at the right time
* dried in a controlled time and temperature. ** the constancy of composition, & consequently

Correct drying is the most important phase

in the whole process of production. ** the constancy of activity,
of an herbal medicine.

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Standardization of crude drugs & extracts

Standardized drug extract
Because of
The Latin name Ginkgo biloba Crataegus the complex composition of herbal medicine
of the plant L. monogyna the process of production of botanical
The plant organ Leaves Leaves & flowers
preparation must be kept constant;
The drug / 35 - 67 : 1 W/W 4 -7 : 1 W/W
extract ratio a standard herb  a standardized herbal preparation.
The solvent --- 70 % ethanol
(used for extraction) Standardized crude drug
The physical Dry (semi-purified Dry extract
form standardized) The latin name Ginkgo biloba L. Atropa belladonna L.
(liquid, dried extract) extract of the plant
The content of 22-27 % flavone 2.25 % total The plant organ Leaves Leaves
the active glycosides or flavonoids, The content of the 0.8 % flavonol 0.9 % total alkaloids,
constituents active constituents glycosides calculated as hyocyamine
5-7 % ginkgolides or 4-5% oligomeric
( as DS in US)
procyanidins

The problem is that, Standardized vs. Whole

• the action of the herb may be from
a number of constituents and not
from just one or two ingredients.
• Thus, the standardized preparation
may omit some of the ingredients and we
will lose out the effect from the complex
combination of the constituents.
Herb
• As the herbs are getting more popular,
manufacturers are supplying standardized
herb extracts.
• A standardized extract means that:
The manufacturer has verified that the active
ingredient believed to be present in the herb
is present in the preparation.
• The potency and the amount of the
active ingredient are assured in the
preparation.

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"The safety of herbal medicines depends on HPLC Chromatographic fingerprint of

their correct use" different DGL extracts (DGL-Ev, DGL-Ge and
DGL-Ph)

An herbal medicine, like any medicine, is a 140

UV
DGL (EVA)
UV
DGL (Gemini)
UV
DGL (phyto)
140

double-edged word. Therefore,

051DGL (EVA).dat 049DGL (Gemini).dat 050DGL (phyto).dat

120 120

both patients and physicians must be able to make 100 100

Liquiritigenin
the risk/benefit assessment, before using any herbal
medicine. 80 80

mAU

mAU
60 60

Risk/Benefit ratio.
The beneficial effects can outweigh the adverse effects. 40 40

20 20

DGL-Ev
0
DGL-Ge 0

0.0 2.5 5.0 7.5 10.0 12.5 15.0 17.5 20.0 22.5 DGL-Ph
25.0 27.5 30.0
Minutes

Uses of Herbal Medicines in

Pregnancy Specific Situations (p. 61 – 69)

 The use of natural or synthetic medicines during the first phase The use of plant-derived drugs in
of pregnancy should in general be avoided. Pregnancy and Breast Feeding
 by the time the women is aware of the pregnancy requires particular care.
(usually 5-6 weeks after conception) she may have been
exposed to the mutagen/teratogen for quite some time.

 Unfortunately, in practice this

recommendation has not always Caution is also required for :
helped to resolve the problem of mutagenicity because: ** the very Young or Old patients
** When the mother receives a medicine it may reach the fetus in a ** those suffering from hepatic or renal
concentration great enough to produce a toxic effect.
insufficiency.
** In addition, the mother may be at risk of abortion or hemorrhage
during birth.

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Adverse
effects of
certain herbal Pregnancy
medicines
during
pregnancy  Those medicines suspected to affect the
fetus obviously need to be avoided.

 This is equally valid for botanical drugs

Cascara, Cinnamon, Ginger Peppermint, and especially for drugs which may affect
Rhubarb, Turmeric Thyme uterine motility.
Senna Abortifaciant
Uterine Stimulants Emmenagogue Emmenagogue
Abortifaciant
Abortifaciant Mutagenic
Emmenagogue
Mutagenic
Mutagenic
Genotoxic actions

Nursing Nursing
The nursing mother therefore should Milk can transmit chemical or substances of
always be advised to: alimentary origin which affect the newborn
avoid or reduce the intake of medicines Producing:
including herbal medicines containing:  Allergy: such as nettle-rash
** laxatives,  Diarrhea: from Aloe
** xanthines (caffeine),  Sleepiness: from sedatives for anxiety
** tranquillizers,
** contraceptives or narcotics {e.g. opiates} for pain.
** anticoagulants.

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Pediatric Age Group

 Children, because of their immaturity, are often more
susceptible than adults to the effects of drugs.

 Some medications can adversely affect normal

development in children.
 In newborn babies
* hepatic microsomial and non-microsomial enzyme
systems (involved in the transformation of medicines) are not
fully functional.
* The blood-brain barrier is not completely developed.
* the excretory system (in particular the kidneys) is immature.

Geriatric Age Group Pediatric Age Group

 It has been estimated that:
for people over 65 years of age Undesirable effects This clearly makes:
are double those of young people.
 The newborn particularly vulnerable to Drug-
 In the elderly, side effects are mainly due to: induced toxicity, especially to the liver and kidneys.
impaired absorption, biotransformation and
elimination.
 Therefore, the use of botanical drugs in this age
 For therapeutic intervention to be effective
it is essential to take into consideration
group must be carefully evaluated.
the patient's capacity to follow instructions.
This may be impaired in the older patient due to
cerebral insufficiency and social isolation.

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Precautions
The risks from herbal medicines, and indeed all drugs, are Geriatric Age Group
greatly reduced if some precautionary norms are followed:

 Patients over 65 years of age should begin treatment with low  For these reasons pharmacological therapy
doses of herbal medicines.
 Pregnant and breast-feeding mothers should not take herbal
should be simplified as far as possible (in oral form),
medicines. not only for the patients but for those who are
 Herbal medicines should not be used for children under two years
old.
involved in their care.
 Chronically ill patients should bear in mind that plant-derived
drugs may interact with conventional drugs taken concurrently.  Because of the perceived safety and "gentle"
 Do not ignore toxic symptoms of any kind.
action of many herbal medicines,
 Essential oils should be used with caution (they are highly in recent years there has been an increase
concentrated and small quantities may cause serious harm). in the use of these products in geriatric
 Herbal medicines should be taken only at the prescribed dose patients.
and for limited periods of time.

15