LECTURE 14 – Phytopharmaceuticals for
external use – Part 2
Dr. Ivana Daňková
Dept. of Natural Drugs, Faculty of Pharmacy, VFU Brno
PHYTOPHARMACEUTICALS
academic year 2018/19
DERMATOLOGICS
2
 = preparations used topically
 in case of skin diseases
 for skin irritation, blood congestion (hyperaemia), induction
a feeling of warm
 for protection of health skin against external influences
 Disinfectants, antiseptics, antibacterials, antivirals, antifungals
 Antipruritics, antiseborrheic agents, antipsoriatics, antiscabietics
 Astringents, antiphlogistics
 Keratolytic, emollients
 Preparations used for repairing wounds (re-epithelisation,
re-granulation)
 Preparations used to treat burns, frostbites,…
 Preparations used to treat muscular injuries, contusions, external
antirheumatics,…
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 „counterirritant agent“
 externally applied substance that causes irritation or mild
inflammation of the skin for the purpose of relieving pain in
muscles, joints and viscera distal to the site of application.
 They differ from the anaesthetics, analgesics, and antipruritic
agents, however, in that the pain relief they produce results from
stimulation --- rather than depression --- of the cutaneous sensory
receptors and occurs in structures of the body other than the skin
areas to which they are applied as for example, in joints,
muscles, tendons.
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CAPSAICIN
 Capsicum anuum, C. frutescens, Solanaceae
chilli pepper
 an alkaloid that makes the chilli peppers taste „hot“
 it binds to nociceptors in the skin, or mucous membrane, causing an
initial excitation of the neurones and a period of enhanced sensitivity
(due to a selective stimulation of afferent C fibres and release of
substance P) – perceived as itching, pricking, or burning, with
cutaneous vasodilatation. This is followed by a refractory period with
reduced sensitivity and, after repeated applications, persistent
desensitisation.
 topical preparations are used to treat pain from rheumatoid arthritis,
osteoarthritis, neuralgia, diabetic neuropathy, also to treat pain due to
pruritis, psoriasis, cluster headaches, etc.
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 CAPSICOLLE
DRM EMP MED 110 mm x 190 mm (Spofaplast, ČR)
 medicated plaster, cutaneous use
 Nonivamidum (= capsaicin derivative) 25 μg
Belladonnae radicis extractum spissum 426 μg
(refers to Atropini sulfas 6 μg)
 SUKL code: 0192930
Selected medicinal product
 ATC: M02AB
(Capsaicin and related compounds)
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 CAPSAICIN WARMING PLASTER
(Tym pro Farmacii, ČR)
 70 mm x 100 mm, or 120 mm x 180 mm
 extr. Capsicum anuum 2,89 %
olibanum 12,5 %
menthol 9,6 %
camphor 9,6 %
extr. Ferula assa-foetida 7,5 %
Cinnamomi cortex 5 %
Rehmanniae radix 5 %
extr. Atropa belladonna 1,52 %
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CAMPHORA
 Camphora officinarum (Cinnamomum camphora)
Lauraceae, camphor
 natural D-camphor, or synthetic D,L (racemic)
 chemically manufactured from turpentine oil
 is readily absorbed through the skin and produce
a feeling of cooling, and acts as a slight local
anesthetic and antimicrobial agent, stimulates blood
circulation
 is available as and essential oil for aromatherapy or
topical applications – used in anti-itch gels, cooling
gels (to relief pain),...
 oral administration for minor heart symptoms and
fatigue
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OPODELDOK
 Linimentum saponato-camphoratum
(ČsL 3 = Czechoslovak Pharmacopoeia 3)
 Camphora 20 g
Sapo medicinalis 50 g
Ammonium
Aqua purificata 70 g
Ethanolum 95 % (V/V) 800 g
Lavandulae etheroleum
Rosmarini etheroleum
 the history of „opodeldoc“ – in 16th century,
Paracelsus made a mixture of soap in alcohol,
camphor and several herbal ingredients for
treatment of rheumatoid disorders
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Refit OPODELDOK (Edwin Ozimek, ČR)
 a traditional ointment with the intensive effects
of camphor, lavender and rosemary
 It is most commonly used in relieving
joint and muscular pain, to promote
blood circulation
 used in inflammation, rheumatism
and gout
 OPODELDOK Extra Strong
 contains also peppermint (refreshing effect)
 OPODELDOK Warming
 contains also capsaicin, ginger and cinnamon
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Priessnitz (Simply You, ČR)
 COOLING LINIMENT De Luxe
 camphor, menthol, lavender oil
 WARMING LINIMENT De Luxe
 capsaicin
camphor
dwarf pine oil – Pinus mugo var. pumilio
Boswellia serrata (Burseraceae) – resin
 JOINT LINIMENT Classic
JOINT LINIMENT De Luxe
 camphor, menthol
rosmarin oil
Boswellia
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Boswellia
 Boswellia sp., Burseraceae – trees or shrubs
native to tropical regions of Africa and Asia
 fragrant resin exuded from the tree after damage
 previously called „frankincense“or „olibanum“
(mentioned in the Bible as one of the three gifts that
the wise men gave to the young child Jesus)
 active principles: 1-3 % essential oil (mono- and
sesquiterpene structures), 60-70 % resin (triterpene
acids – boswellic acids), about 20 % of gum,…
 anti-inflammatory, immunomodulatory activity,
antibacterial, antifungal activities; treatment of
asthma, spasmogenic effect
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ALPA
 ALPA Francovka
 alcohol-based solution of natural essential oils
and isolated compounds (menthol, linalool,
nerol,…)
 used to relieve pain and discomfort due to
rheumatic arthritis and muscular rheumatism,
for hematoma, dislocation and contusions
 for disinfection of small scratches and wounds
 for reflex massages in case of rheumatic muscle
pain
 addition of other natural extracts, essential
oils,...
 other application forms – emulsions, gels,
creams, baths
http://alpa.cz/en
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 Symphyti radix
Symphytum officinale, Boraginaceae,
comfrey
 the main component is allantoin
(0.6-0.8 %), which supports regeneration
 4-6 % tannins, mucilage, triterpenes,…
 pyrrolizidine alkaloids, partly as N-oxides
(necines) = hepatotoxic effect !!!
 externally in the form of poultices, ointments and pastes as
an anti-inflammatory in damage to the periosteum, inflammation of
joints, tendons; arthritic swellings, for promoting callus formation in
fractures, dislocations, contusions, sprains, haematomas,…
 ointments or other preparations for external use containing 5-20 %
of the drug
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 Arnicae flos
Arnica montana, Asteraceae
 the main constituents are sesquiterpene
lactones (helenalins, and their esters
with lower fatty acids)
 flavonoids, essential oil of a buttery
consistency (containing 40-50 % fatty
acids, n-alkanes and mono- and sesquiterpenes), cinnamic acid
derivatives, coumarins, polyacetylenes, carotenoids
 used for wound healing, and as a wound antiseptic, antiphlogistic,
antirheumatic, antineuralgic
 used for injuries and accidents (sprains, dislocations, bruising,
haematomas, oedema associated with fractures), in arthralgia and
rheumatic pains in the joints
 the most frequently used form of the drug is the tincture
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TRAUMAPLANT
DRM UNG 1X50GM (Harras Pharma
Curarina GmbH, Germany)
 composition in 100 g:
 Symphyti peregrini herbae
succus 10 g
 vehicles, sorbic acid,…
 SUKL code: 0043979
OTC medicinal product
 ATC: V11 (Phytopharmaceuticals)
 contains a concentrate of
a juice pressed out of freshly
harvested haulm of comfrey
(Symphytum peregrinum) and
has anti-inflammatory effects
 suitable to apply to sport injury
wounds, bruises, sprains,
in muscle and joint pain
 Notice: in persons with a very
sensitive skin reddening of the
area treated with the ointment
can very rarely occur.
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 COMFREY OINTMENT
 many producers, e. g.
Aromatica, Dr. Müller, Grešík,
Dr. Popov, Topvet,...
 ARNICA OINTMENT
 many producers, e. g.
Aromatica, Dr. Müller,
Kneipp, Dr. Popov, Weleda,...
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 Chestnut
Aesculus hippocastanum seed/flower
 active substances: saponines (aescin), tannins, flavonoid glycosides
 They help to increase the elasticity of vascular walls, blood perfusion,
vascular flow and limit formation of oedemas. They have also a significant
anti-inflammatory and healing effect.
 Juniper
Juniperus communis (pseudo)fruit/wood
 it contains mainly essential oil (terpenes)
 activates the lymphatic system, which helps to eliminate toxic substances
from the body. It effectively accelerates regeneration.
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 HORSE BALSAM Warming
(Herbamedicus, Switzerland)
 natural nourishment for joints, muscles and spine,
relieves rheumatic conditions, provides help with lumbago
problems
 made from 25 herbs
 horse chestnut (Aesculus hippocastanum seed and flower
extract)
 comfrey (Symphytum officinale root)
 Arnica montana, Juniperus communis,
Calendula officinalis, Echinacea purpurea,
Agrimonia eupatoria,…
 chilli extract, cinammon, camphor, lavender,
rosemary, thyme, mint, chamomile,…
The exact composition see at: http://www.herbamedicus.ch/products/
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 HORSE BALSAM Cooling
(Herbamedicus, Switzerland)
 natural nourishment for joints, muscles and spine
 effective for relief and refreshment of pulled
muscles and „heavy“ legs
 made from 25 herbs, similar composition
as the „warming“
 with Eucalyptus extract – cooling effect
 without Capsici extract (!)
 fortified versions
 HORSE BALSAM Forte Warming
 HORSE BALSAM Forte Cooling
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 HORSE BALSAM Warming
Herbal Liquid with Spirit
(Herbamedicus, Switzerland)
 real relief for muscles, back and knees
 The balsam initiates intensive warming and perfusion,
thus increasing the effect of the active agents and
accelerating convalescence.
 Spirit contained in the product evaporates after
application, and therefore the active ingredient
more quickly get to the skin and hasten the onset of action
 HORSE BALSAM Cooling
Herbal Liquid with Spirit
 The balsam initiates intensive cooling