LECTURE 5 – Preparations used to treat
some disorders of cardiovascular system
Dr. Ivana Daňková
Dept. of Natural Drugs, Faculty of Pharmacy, VFU Brno
PHYTOPHARMACEUTICALS
academic year 2018/19
PHYTOPHARMACEUTICALS
vs. Cardiovascular system (CVS)
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Major CVS disorders
 Heart failure
 Angina pectoris, heart attack
 Abnormal heart rhythms
 Hypertension/Hypotension
 Peripheral vascular diseases
(arterial/venous)
Phytotherapy is suitable only as
supplementary and supporting
therapy!!
Therapy of cardiovascular diseases
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 drugs influencing heart
 cardiotonics (cardiostimulants)
 antirrhythmics
 drugs influencing vessels
 vasodilators
 vasoconstrictors
 antihypertensive drugs
 vasoprotective drugs
 antihyperlipidaemic drugs
CARDIAC GLYCOSIDES
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 = cardiotonic glycosides (CG),
„digitalis“ glycosides
 positive inotropic effect – enlargement
of the contractile force of heart muscle
(due to the inhibition of Na+/K+ ATPase
→ increase of intracellular Na+ →
increase of intracellular Ca2+ → ↑ inotropy)
 Indication: chronic congestive hear failure,
atrial fibrillation or flutter
 Overdose of CG, intoxication can cause life-threatening arrhythmias,
contracture
 !!! plant drugs containing cardiac glycosides are not allowed to be
components of phytopharmaceuticals due to their toxicity and narrow
therapeutic margin.
CARDIAC GLYCOSIDES
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 Plant drugs containing CG:
 Digitalis lanatae folium
 Digitalis purpureae folium
 Convallariae herba
 Adonidis herba
 Strophanthi semen
 Strophanthus sp.
 other plants containing CG:
 Helleborus niger, Nerium
oleander, Urginea maritima,
Acokanthera ouabaio,
Erysimum sp., Thevetia sp.
Convallaria majalis
Adonis vernalis
Digitalis purpurea
Therapy of ARRHYTHMIA
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 abnormal heart rhythms,
irregular heartbeat
 tachycardia – too fast
 bradycardia – too slowly
 premature contraction
– too early
 fibrillation – too irregularly
 partially possible using of phytomedicines
Therapy of ARRHYTHMIA
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 quinidine
 alkaloid from Cinchona bark
(stereoisomer of quinine)
 acts as a class Ia antiarrhythmic agent
 prescription-only drugs
 ajmaline
 indole alkaloid from Rauwolfia serpentina root
 acts as a class Ia antiarrhythmic agent
 prescription-only drugs
 bradycardia
 plant drugs containing caffeine
 hawthorn leaf/flower – Crataegus sp.
 tachycardia, palpitations
 plant drugs with sedative effect
HYPERTENSION
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 blood pressure („arterial“ BP) over
140/90 mmHg
 primary (essential) hypertension
= high BP with no obvious underlying
medical cause
 secondary HT– as a consequence of
other disturbances (e.g. in renal diseases,
by endocrine conditions, obesity,…)
 phytomedicines can be used only as
a part of supplement therapy !!
 first steps
 low sodium intake diet (be careful
about using of Liquiritiae radix)
 reduction of body weight
Therapy of HYPERTENSION
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 Crataegi folium cum flore
Crataegi fructus
 Crataegus oxyacantha, C. monogyna,
and other species, Rosaceae
= hawthorn
 major constituents:
 flavonoids – quercetin glycosides
(e.g. hyperoside – mainly in fruits),
and apigenin glycosides (vitexin
derivatives – mainly in leaves)
 oligomeric procyanidines, triterpene
acids, phenylpropanoid acids,
aminopurines, xanthines, K+ salts
Therapy of HYPERTENSION
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 Crataegi folium cum flore
Crataegi fructus
 improvement of blood circulation, also in
coronary arteries; effect on the control of
the intracellular Ca2+ concentrations
 Indications:
 hypertension (used to treat both high BP
and low BP)
 It might be effective against initial cardiac
insufficiency (congestive heart failure),
as well as for the ageing heart, against
a feeling of pressure and tightness in the
cardiac region (chest pain) and mild
bradyarrhythmia
Therapy of HYPERTENSION
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 Hawthorn tea
(MEGAFYT Pharma)
 POR SPC 20X1.5GM
 Crataegi folium cum flore
 SUKL code: 0076436, OTC medicinal product
 ATC: V11 (Phytopharmaceuticals and animal
products)
 herbal preparation suitable for treatment of mild
forms of hypertension, for improvement of heart
blood flow, as a cardiostimulant
 Hawthorn drops (Grešík, Herba Vitalis, Topvet, ...)
 alcoholic extracts of Crataegus oxyacantha and/or
Crataegus monogyna
Therapy of HYPERTENSION
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 Visci albi herba
 Viscum album, Santalaceae
– mistletoe
major constituents: proteins and polypeptides (viscotoxins), lectins,
polysaccharides
BUT active principles in therapy of hypertension are probably
flavonoids, phenylpropanes and lignans, biogenic amines
 !! A clear distinction must be made between
oral use of the drug in the form of aqueous extract (herbal tea – as
an adjuvant in the treatment of high BP), and the parenteral use
of isolated constituents, e.g.in the form of intradermal injections (for
treating degenerative inflammation of the joints, or as palliative
therapy for malignant tumours).
Therapy of HYPERTENSION
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 Visci albi herba
 Viscum album, Santalaceae
– mistletoe
 There are no real grounds for the use of
mistletoe tea as a supportive agent in
treating of high BP
 !! It has indeed been shown that the isolated
viscotoxins have hypotensive effect on
parenteral administration, but they can not be
considered as the active principle since they
are not absorbed orally; moreover they are
highly irritating to the skin, at high dose they
even cause necrosis.
Therapy of HYPERTENSION
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 ALVISAN Neo
(LEROS)
 POR SPC 20 x 1.5 g or 1x 100g
 SUKL code: 0004364, 0043954
 OTC product
 ATC: V11 (Phytopharmaceuticals and
animal products)
 not suitable for children until 18 years,
for pregnant and lactating women
 ! mind the presence of Hyperici herba
 photosensitivity, interactions with
certain concurrently administered
drugs, loss of concentration,…
 Matricariae flos
Crataegi folium cum flore
Crataegi fructus
Equiseti herba
Hyperici herba
Melissae herba
Menthae piperitae herba
Visci albi herba
Therapy of HYPERTENSION
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 Hypotonic herbal tea
(MEGAFYT)
 POR SPC 20 x1.5 g
 SUKL code: 0084373
 OTC product
 ATC: V11
 herbal preparation suitable
for treatment of mild forms
of hypertension
Composition (in one tea bag = 1.5 g):
 Crataegi folium cum flore 375 mg
Visci albi herba 375 mg
Polygoni avicularis herba 225 mg
Rubi fruticosi folium 225 mg
Crataegi fructus 150 mg
Melissae herba 150 mg
PHYTOPHARMACEUTICALS
in the treatment of VASCULAR DISEASES
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 Tea for high blood
pressure
(Fytopharma, Slovakia)
 Visci albi herba
Millefolii herba
Leonuri herba
Melissae herba
 Tea for blood pressure
(Pavel Váňa)
 Crataegi folium cum flore
Filipendulae herba
Melissae herba
Leonuri herba
Leonurus cardiaca
Lamiaceae
Therapy of HYPERTENSION
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Formerly used plant drugs:
 Veratri albi radix
Veratrum album, Melanthiaceae
 steroid alkaloids
 Rauwolfiae radix
Rauwolfia serpentina, Apocynaceae
 alkaloids – reserpin – formerly used
in composite medicinal preparations
(e.g. CRYSTEPIN)
 Secale cornutum
Claviceps purpurea, Clavicipitaceae
 alkaloids, especially dihydroderivatives
(e.g. dihydrocristine, in CRYSTEPIN)
Rauwolfia serpentina
Therapy of HYPERTENSION
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Supplementary and support therapy:
 Diuretics (!) – plant drugs containing:
 flavonoids
 saponins
 essential oils
 Plant drug with significant antioxidative activity, e.g.:
 Oleae folium (Olea europea)
 Allii sativi bulbus
Therapy of HYPERTENSION
 OptiTensin® (Walmark)
 Oleae folium extract 350 mg
 Olive leaves extract helps to
maintain normal blood pressure
and helps to protect organism
against negative effects of free
radicals.
 Dosage: 1-2 tablets daily.
It is recommended to use
minimally for the period
of 8 weeks
 Garlic (Walmark)
 highly concentrated oil extract
from Allium sativum 2.0 mg in
1 capsule
(eqv. 1000,0 mg of fresh garlic)
 Garlic contributes to normal
function of immune system.
 Garlic helps to maintain normal
cholesterol level and the health
of heart.
Therapy of HYPERTENSION
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 ω-3 fatty acids
 EPA and DHA cause vasodilation, low blood
pressure
 source: oil seeds and fruits, sea fish, cereals,
some vegetables…
 plant sterols
 have positive influence on blood cholesterol level
 beta-sitosterol, beta-sitostanol
 source: oil seeds (e.g. rapeseed), nuts, cereals
(e.g. corn),…
HYPOTENSION
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 chronic hypotension – systolic BP below 105 mmHg
 primary hypotension – generally has no clinical importance. If
symptoms such as lassitude and dizziness occur, a program of
physical exercise instead of drug is advisable
 secondary hypotension – is a sign of an underlying disease that
should be treated first
 acute hypotension
 failure of orthostatic regulation
 Therapy of hypotension
 increase sodium intake in a diet
 physical activity
 caffeine plant drugs