Transcript Pharmacological effects and Clinical efficacy

THE RESPIRATORY
SYSTEM
The Respiratory System
 Minor common disorders of respiratory system
and the more serious diseases such as
bronchitis ,emphysema and pneumonia can be
successfully treated with phytotherapy.
However, we can use decongestants ,
broncholytics expectorants, demulcents,
antivirals, Immune system modulators,
anti_allergics,antimuscarinic drugs ,
platelet_activating factor, Leukotriene
antagonists, natural compounds, cough
suppressants , and antitussives .
A. Bronchodilators and Decongestants :1. Ma huang , Ephedra spp. :
Ma huang is an ancient Chinese medicine
,which is now used worldwide. It was the
original source of ephedrine, a useful
decongestant and bronchodilator. It is used to
treat asthma and nasal congestion, in the
form of nasal drops. Pseudoephedrine is now
used more widely for respiratory congestion
as it has fewer CNS stimulatory properties.
The medicinal part of this plant is stems and
branches.
 Constituents
 Alkaloids, up to about 3%; the major alkaloid
is ephedrine. Other alkaloids include
pseudoephedrine, norephedrine ,
 Other components are catechin derivatives
 Diterpenes, including ephedrannin A and
mahuannin A.
 Pharmacological effects and Clinical efficacy
 Ephedra has been used to treat asthma and
hay fever , as a bronchodilator,
sympathomimetic, CNS and cardiac
stimulant ,
 Herbalists also use it to treat enuresis,
allergies, narcolepsy and other disorders,
and anti-inflammatory activity has been
observed is extracts. Also used in some
types of bradycardia.
 Pharmacological effects and Clinical efficacy
Continue…
 Pseudoephedrine , the isomer of ephedrine,
is usually the compound of choice for
isolated alkaloid preparations. Ephedra herb
is used as antiallergic agent
 Toxicology
 The herb has been abused as a slimming aid,
this can be very dangerous if high doses are
used for long periods. For example ,
hypertension and CVS events and exacerbation
of hepatitis. The herb isn’t normally considered
to cause HTN since the other components ,
such as the ephedradins, mahuannins and
maokonine , are actually hypotensive. However,
it should be avoided in cases of thyrotoxicosis ,
narrow angle glaucoma , and urinary retention.
 Therapeutic doses of the herb are up to 30mg of
alkaloids , calculated as ephedrine .
2. Theophylline
 Although theophylline is a natural xanthine
which is found is cocoa , coffee and tea , it is
almost invariably used as the isolated
compound. It is indicated in reversible airway
obstruction particularly in a cute asthma.
 Because of narrow therapeutic window of
theophylline , and the fact that t1/2 is highly
variable between patients, especially smokers,
care must be taken.
 The usual does is 125-250mg is adults, three
times daily , and half of that in children.
 Theophylline…Continue
 Toxicology :
S/Es include 1)tachycardia. 2) palpitations.
3)nausea. 4) other GI upsets .
these can be reduced by sustained release
preparations, which is the usual form of
theophylline products.
 Inhalations:
 Essential oil containing drugs are often used with
aromatic compounds (especially camphor) as
1) chest rubs, steam inhalations or nasal sprays , for
their decongestant properties. They are useful for
infants ,children ,asthmatics and pregnant
women for whom systemic decongestants aren’t
appropriate.
2)They may be used orally, in pastilles, lozenges , or
“cough sweets”.
Oils distilled from the aerial parts of members of
pine family and the Australian Myrtaceae are
used frequently.
3)These oils can be used in steam baths.
 Eucalyptus Oil:
 The blue gum tree yields a highly
characteristic oil which is widely used as a
decongestant and solvent.
 Constituents : The oil contains cineole as
the major component and eucalyptol.
 Pharmacological effects and clinical efficacy:
 The oil is antiseptic, antispasmodic,
expectorant, stimulant and insect repellent.
It may be taken internally in small doses, as
ingredient of :
1)cough mixtures. 2)sweets and pastilles
3)inhalation.
It is applied also externally in the form of
1)linemet , 3)ointment 3)vapor rub .
The leave extract and oil has antiseptic effects
against variety of bacteria and yeasts .
 Pharmacological effects and clinical efficacy:
continue….
The oil is also insect repellent
 Toxicology :
Eucalyptus oil is irritant.
 Camphor:
 Camphor, a pure natural product, is derived
from Asian camphor tree. It is combined with
the essential oil containing drugs as an
aromatic stimulant and decongestant and
expectorant.
Pharmacological effects and clinical efficacy :
Camphor has antiseptic, secretolytic and
decongestant effects. Small doses were
taken internally for colds, diarrhea, and for
other complaints , but now it is used
externally .
 Camphor….continue
 Toxicity :
Overdose causes vomiting, convulsions and
palpitations and can be fatal. If used
externally in therapeutic doses, it is well
tolerated .
 Menthol:
 Menthol is a monoterpene extracted form
mint oils , or made synthetically. Whole
peppermint oil is used in herbal
combinations to treat colds and influenza
and for colic, etc. But isolated menthol is
effective decongestant used in nasal sprays
and inhales.
 Toxicity :
Menthol can be irritant and toxic in over
dose , but is well tolerated in normal usage.
 Anti-allergics:
 Most antihistamines are synthetic in origin.
They are the most potent drugs used as
anti_allergics,e.g: Cetirizine, desloratidine,
fexofenadine or chlorpheniramine .
 1) Khella “toothpick plant” :
 Khella “toothpick plant” :
The used part is the fruits and the botanical
drug has been used as an anti_spasmodic
in renal colic, for asthma, and as a coronary
vasodilator for angina.
 Constituents :
bitter principles: khellin, visnagin.
 Khella “toothpick plant” :…..continue
 Pharmacological effects and clinical efficacy : khellin,
visnagin are vasodilators , with calcium channel
blocking and spamolytic activity.
 Khellin was the starting material for development of
several semi_synthetic derivatives such as :
1) Sodium cromoglycate , which is widely used as
prophylactic treatment for asthma ,hay fever and
other allergic conditions, in the form of an inhaler or
eye drops.
2) Nifedipine ( CCB and vasodilator ): used for heat
diseases.
3) Amiodarone : cardiac anti-arrhythmic.
 2) Butterbur:
 Butterbur :
The root and herb are used.
 Constituents :it contains :
1) eremophinolides.
2) Flavonoids.
3) Toxic alkaloids may be present, usually in higher
concentrations in the root.
Pharmacological effects and clinical efficacy:
Butterbur is:
• used for asthma (extracts inhibit leakotriene synthesis
and are spasmolytic ), colds, headaches and urinary
tract disorders.
• Used as antihistamine for seasonal allergic rhinitis.
(Butterbur extract is as potent as cetirizine ).
 Butterbur:….continue
• used as prophylactic treatment for migraine.
• has anti-inflammatory activity
Toxicology:
• Internal use isn’t recommended unless the
alkaloids are present in negligible amounts
or removed from preparations.
• Maximum intake of alkaloids should be less
than 1Mg daily for fewer than 6 weeks per
year.
 Expectorants and Mucolytics
1) Balm of Gilead (poplar buds):
 The buds and the bark of these species are
used.
 Constituents :
1)
2)
3)
4)
Phenolic glycosides.
Volatile oil.
Flavonoids.
Lignans.
 Pharmacological effects and clinical efficacy :
1) Balm of Gilead is an expectorant , stimulant ,
antipyretic and analgesic.
 Expectorants and Mucolytics…continue
2) It is a common ingredient of herbal cough
mixtures, and also ointments used for
rheumatic and other muscular pains.
3) The phenolic glycosides and the volatile oil
constituents have antiseptic and expectorant
activity.
Toxicology :
1) Balm of Gilead is generally nontoxic ,except for
patients who are allergic to salicylates.
 Expectorants and Mucolytics…continue
2)


1)
Thyme and Wild Thyme:
The leaves are used.
Constituents:
The active principle is the volatile oil thymol
and Carvocrol
2) Flavonoids.
 Expectorants and Mucolytics…continue
Pharmacologic effects and clinical efficacy:
1) Thyme, and oil of thyme, are carminative,
antiseptic, antitussive ,expectorant
2) They are used for coughs, bronchitis,
sinusitis, whooping cough and other
respiratory disorders.
Toxicology :
Thyme is irritant and toxic in large and
overdose.
 Expectorants and Mucolytics…continue
3) Sage:
 The leaves are the used part.
Constituents:
1) Volatile oil.
2) Diterpene bitters picrosalvin, carnosolic acid,
3) Flavonoids.
 Expectorants and Mucolytics…continue
 Pharmacological logical effects and clinical
efficacy:
1) An infusion of sage is used as a gargle or
mouthwash for pharyngitis, tonsillitis , sore
gums , mouth ulcers, and other disorders.
2) sage extracts and oil have antimicrobial
activity.
3) The flavonoids and phenolic acids have
anti_viral and anti_inflammatory activity.
4) Sage enhance memory, supported by
anticholinesterase activity.
 Expectorants and Mucolytics…continue
4) Senega:
 The roots are the used part.
 Constituents:
Triterpenoid saponins: senegin.
 Pharmacological effects and clinical
efficacy:
1) Senega is used primarily for chronic
bronchitis, catarrh, asthma ,and croup.
2) Senega usually taken orally as an infusion.
 Expectorants and Mucolytics…continue
3) Saponins are the active constituents , have
mucolytic, anti-inflammatmy, antiseptic activity and
immunopotentiating activity to protein and vital
antigens.
4) Senega extracts, senegins is hypoglycemic in
rodents , and potent inhibitors of alcohol absorption.
Toxicology:
1) The saponins are irritant and hemolytic.
2) Nausea and vomiting are the most common adverse
effects.
3) When taken orally, it doesn’t appear to cause
problems expect in high doses or in sensitive
individuals.
 Expectorants and Macolytics…continue
5) Ivy :
 Ivy is a saponin containing expectorant.
 Both leaves and berries are used.
Constituents:
1) Saponins.
2) Flavonoids.
Pharmacological effects and clinical efficacy:
1) Ivy extracts are used for bronchitis and
catarrh, as an expectorant.
 Expectorants and Mucolytics…continue
2) The saponins and sapogenins are the main active
ingredient they are expectorant and have antifungal ,
antimutagenic effects.
3) Ivy extracts are used in cosmetics preparations to
treat cellulite.
4) Both saponin and the flavonoid fractions are
spasmolytic .
Toxicology:
1) Like all saponin containing drugs, Ivy can be irritant
and allergenic.
 Expectorants and Macolytics…continue
6) Tolu balsam:
 The used part is the resin which is collected
from incisions in the bark.
 Constituents:
1) Cinnamic and benzoic acids.
2) Their esters such benzyl benzoate and
cinnamyl cinnamate.
3) Ester with resin.
 Expectorants and Mucolytics…continue
 Pharmacological effects and clinical efficacy:
1.Balsam of tolu is expectorant, stimulant,
antiseptic and demulcent which is used in
cough mixtures and as lozenge base.
2.It has antibacterial activity , due to the benzyl
benzoate and benzyl cinnamate content.
 Toxicology:
Tolu balsam can cause allergic reactions.
 Expectorants and Macolytics…continue
7) Ipecacuanha, Ipecac , Emetic roots:
 The used part is the roots.
 Constituents:
Alkaloids isoquinoline group are the active
principles, the most important are :
1) Cephaline.
2) Emetine.
 Expectorants and Macolytics…continue
Pharmacological effects and clinical efficacy:
1) Ipecac extracts used in many cough
preparations, both elixirs because of their
expectorant activity.
2) Emetic
3) Antiamoebic
4) GIT antiseptic.
Toxicology:
Ipecac causes vomiting in large doses and the
alkaloids are cytotoxic.
E. COUGH SUPPRESSANTS
 Cough is a reflex action and symptoms of the
disease such as asthma and cold due to nasal
drip.
Cough suppressants may be useful in some
instances but efficacy is not fully proven and in
some cases it will cause sputum retention
When we use cough suppressants?
1-Children who are highly susceptible to respiratory
depression caused by opiate.
2-with sever cases of lung cancer with sever cases
of cough we can use dextromethorphan (semi
synthetic opiate) and codeine
Codeine
It is found in opium in the form of phosphate salt
pharmacological effects:
1.Treatment of cough (antitussive) 10-20mg every
four hour
2.Treatment of diarrhea 240mg daily in divided dose
3.Mild narcotic analgesic
Toxicity of codeine :
1.Sedation
2.Constipation
3.In large dose it will cause respiratory distress
4.Addiction and its liability to abuse
codical
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codacamol
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F. GENERAL PHYTOMEDICINE
USED IN
COLD AND
INFLUENZA
• Demulcent and emollient
Demulcent is an agent that form a soothing film
over mucous membrane relieving minor pain
Emollient is a substance that soften and soothing
the dry skin
1. Elder Flower (flowers and berries are used )
The constituents : Triterpenes including :
1. ursolic acid
2. oleonolic acid derivatives
3. Flavonoids : rutin , quercetin
 PHARMACOLOGICAL EFFECT
Elder flower is used as an infusion or herbal tea and
as a mixture of peppermint for cold and influenza
because :
1- It induce perspiration
2- It increase inflammatory cytokines
3- It has a direct antiviral action
The dose is 3g of flower infused with 150ml of hot
water
 Toxicity Elder Flowers are non toxic and no side
effect have been reported
2- LINDEN FLOWER(FLOWERS
ARE USED)
Constituents
1. Volatile oil (linalool , geraniol , cineole)
2. Flavonoids (hesperidin, quercetin, astralagin
3. Mucilage of arabinose
1.
2.
3.
4.
Pharmacological effects
Colds, cough and influenza symptoms
It induce perspiration
For nervous disorders
Polysaccharides are smoothing and adhere to
epithelial tissue producing a demulcent effect
3- MALLOW FLOWER (FLOWERS
AND LEAVES ARE USED)
Constituents:
1. Mucilages are the main constituent
2. Flavonoids glycosides
3. Anthocyanins (malvin)
Pharmacological effects :
1. Mallow is demulcent and pectoral , so an
infusion is made for cold and cough
2. The mucilage from the leaves is antiinflammatory with anti-complement activity
4- MARSHMALLOW LEAF AND
ROOT
 Constituents
1. Mucilage consisting of a number of polysaccharide
(galactose , rhamnose , galacturonic acid and
glucuronic acid)
2. Favonoids (quercetin , kaempferol)
 Pharmacological effects
1. Both roots and leaves are used internally as a
demulcent for irritable coughs and throat
2. Extracts of both are used for gastric and urinary
inflammation
3. They may applied as a soothing poultice(‫ )كمادة‬and
vulnerary ‫دواء الئم للجراح‬
4. The most common use of extracts is the making of
confectionery
Colts foot leaves and flowers
 Constituents :
1. Mucilage composed of acidic polysaccharide
2. Flavonoids and triterpenes
3. Pyrrolizidine alkaloids
 Pharmacological effects
Coltsfoot is used for pulmonary complaints
,irritating or spasmodic, cough ,whooping
cough ,bronchitis ,laryngitis and asthma.
The polysaccharides are anti-inflammatory and
immuno-stimulating, as well as demulcent ,
and the flavonoids also have antiinflammatory and antispasmodic action.
 TOXICOLOGY
Pyrrolizidine alkaloids cause hepatotoxicity on
high dose not in daily dose
• IMMUNOSTIMULANTS
1- Echinacea (Roots are used)
 Constituents
1. Caffeic acid derivatives including echinacoside
(echinacin) , cichoric acid
2. Alkylamides which are unsaturated fatty acid
 Pharmacological effects:
1. Treatment of respiratory and urinary track
infection
2. Topically for slow healing wounds
3. Pain and inflammatory skin condition and
toothache
4. Echinacea are often combined with garlic for the
treatment of cold and allergic reactions
2- ASTRAGALUS(ROOTS ARE
USED)

1.
2.

1.
Constituents
Triterpenoids saponins (astragalosides)
Polysaccharide known as astregaloglucans
Pharmagological effects :
It is used for colds and upper respiratory infections
, it is used prophylactically
2. It is used as an adjunctive in the treatment of
cancer and appear to potentiate the action of
interferon
3. It is also have antioxident , hapatoprotective and
antiviral activity