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Herbal medicine

Cardiovascular system
CVS
By
Dr. Mostafa Mahmoud Hegazy (
PH.D.)
Peripheral and cerebral insufficiency
Ginkgo leaves
Lesser periwinkle
Ginkgo leaves ( Ginkgo biloba )
‫أوراق الجنكة‬
standardized ginkgo extract
• USP31 (Ginkgo). The dried leaf of Ginkgo biloba (Ginkgoaceae)
containing not less than 0.5% of flavonoids, calculated asflavonol
glycosides, with a mean molecular mass of 756.7, and not less than
0.1% of terpene lactones, both on the dried basis. The leaf is khaki
green to greenish-brown. Protect from light and moisture.

• Ginkgo Biloba is a 50:1 leaf extract standardized to 24%


ginkgoflavonglycosides and a minimum of 6%terpenelactones.
• the ratio 50:1, that means 50 grams of ginkgo biloba leaves is
equivalent to 1 gram of standardized ginkgo biloba extract.
Constituents:
• 1- Flavonoids
- Kaempferol, quercetin, isorhamnetin
- myricetin, 3- methylmyricetin
- biflavonoids, catechins and proanthocyanidins

• 2- Diterpene lactones
• Ginkgolides A, B, C, Jand M

• 3- Sesquiterpene lactone
• Bilobalide
Mechanism of actions:
1increasesblood flow,
2increasestissue oxygenation and nutrition,
3Prevention of membrane damage caused by free radicals.
4Enhances memory and cognitive function, especially in the elderly.
5- Has platelet-activating factor (PAF) antagonism;
The PAFantagonism: Platelet -activating factor (PAF) is an ether-linked
phospholipid which is formed by platelets, basophils, neutrophils,
monocytes and macrophages. It is a potent platelet-aggregating agent
and inducer of systemic anaphylactic symptoms.
The ginkgolides are potent and specific PAFantagonists.
Indications:
1-Disorders and symptoms due to restricted cerebral blood flow (memory
impairment, dizziness, tinnitus, anxiety /depression, fatigue and stroke).
2-Early stages of primary degenerative dementia (Alzheimer-type)
3- Effects of high altitude (altitude sickness) or hypoxia.
4- Disorders due to reduced retinal blood flow, senile macular degeneration.
5- Inner ear disorders of vascular origin: tinnitus and vertigo
6-Peripheral arterial disease (particularly intermittent claudication).
7May also be used for disorders due to restricted peripheral blood flow
(including diabetic vascular disease, atherosclerosis, Raynaud's syndrome);
8-Osteoarthritis.
9-protection against ischemia and reperfusion injury.
10- Powerful antioxidant;
• Dosage:Usually the daily dose is 120 mg of a ginkgo standardized extract
equivalent to 27-30 mg ginkgo flavone glycosides and about 10 mg terpenoids
per day (this corresponds to 4-8 gof leaf, depending on the quality).
• Proprietary names: Ginko®, Tanakan®, Tebonina forte®, Brain Power®, Ginkor
fort®.
• Adverse Effects: include headaches, dizziness, palpitations, gastrointestinal
disturbances, bleeding disorders, and skin hypersensitivity reactions.
• Poisoning: convulsions induced by ingestion of large amounts of ginkgo seeds.
Convulsions were thought to be due to the presence of 4-methoxypyridoxine, a
competitive antagonist of pyridoxine; giving suitable quantities of a vitamin-B6
source may be of benefit in preventing suchconvulsions.
• Interactions: It has been suggested that ginkgo biloba should be used with
caution in patients receiving anticoagulants or drugs that affect platelet
aggregation. For reference to a possible interaction with warfarin.
Lesser periwinkle (Vinca minor )
Constituents:
Alkaloids: Vincamine (the principle alkaloid), vincine, vincaminine, vincinine and
vincanorine.

Vincamine
Mechanism of actions:
1-Vincamine is claimed to increase cerebral circulation and utilization of oxygen
2- The total alkaloids of Vinca minor show a pornounced hypotensive effect.
• Indications:

• 1- Disorders and symptoms due to restricted cerebral blood flow.


• 2- Age related troubles, such as memory troubles, concentration disorders,
attention and awareness disorders;
• 3- Degenerative trophic diseases e.g. diabetes, and atherosclerosis;
• 4- After acute cerebral accidents e.g. post-traumatic, post-apoplectic and
hypertensive encephalopathy.
• 5- Dizziness, vertigo, vascular headache and migraine;
• 6- Hearing and Visual troubles of vascular origin;
• 7- Psychiatric disorders e.g. space-time orientation and emotional disturbances
• 8- Toimprove the intellectual capacity in children and adolescents.
• Dosage:
• Crude drug: 3.0 g/day orally.
• Vincamine has been given by mouth in doses of 40 to 80 mg daily and
has also been administered intramuscularly and by intravenous infusion.

• Children: 5 mg three times daily. Adults: 10-20 mg three timesdaily


• Proprietary names: Oxybral®, Depovinc®.
Vinpocetine is a derivative of vincamine (above) that has been given orally in
cerebrovascular disorders and dementia.
Good evidence to support its use in cognitive impairment is lacking.
Essential hypertension
Treatment:
a)Diet and lifestyle
b)Herbal drugs
1- Rauwolfia
2 Mistletoe
3 Valerian
4 Olive leaves
5 Coleus forskohlii
6 Cramp bark
7 Yarrow
8 dandelion leaves
Rauwolfia ( Rauwolfia serpentina )
USP 31: The dried roots of Rauwolfia serpentina (Apocynaceae). It contains
not less than 0.15% of reserpine-rescinnamine group alkaloids calculated as
reserpine. Store at 15° to 30° in a dry place.
• Constituents: Alkaloids, the most important are
reserpine (antihypertensive) and ajmaline (anti-
Arrhythmic).
Reserpine
• Mechanism of Action
• Reserpine irreversibly blocks the vesicular monoamine
transporter (VMAT). This normally transports free
norepinephrine, serotonin, and dopamine from the
cytoplasm of the presynaptic nerve terminal into
storage vesicles for subsequent release into the
synaptic cleft (exocytosis) .Unprotected
neurotransmitters are metabolized by MAO as well as
by COMT in the cytoplasm and consequently never
reach the synapse.
• It may take the body days to weeks to replenish the
depleted VMAT,so reserpine's effects are long-lasting.
• Indication:
1- Anti-hypertensive
• Dosage:
• Whole extract: 2mg, given once a day to begin with and several times daily later.

• Pure alkaloid reserpine: initial 0.2 -0.3 mg is given three times daily to begin with,
0.1- 0.2 mg twice daily for maintenance.

2- As a tranquillizers for ttt of chronic psychosesin daily doses of up to 1 mg.


Mistletoe ( Viscumalbum )
• it is semi-parasite plant, It occurs as a mixture of
broken stems and leaves and occasional fruits ?.
(Nausea, Vomiting, diarrhea, and brady cardia)
• Constituents:
• These are alkaloids, viscotoxins (cause hypotension, acetylcholine agonists),
and lectins. All of Three classes are cytotoxic compounds.
• Lectins with cytotoxic and immunomodulatory actions?
• Action and uses:
1Mild anti-hypertensive drug. Choline derivatives are known to effect
parasympathetic stimulation and vasodilation.
2-preparations have been given by injection in a number of neoplastic
diseases.
• Blood pressure tea:
• mistletoe for its gentle hypotensive effect, hawthorn to improve coronary
circulation, and melissa as a heart sedative:
• Mistletoe herb, Hawthorn leaves and flowers and Melissa leave equal parts to
make 100.0
• One cup morning and night prepared by infusing of 2 teaspoons of themixture
for 5 -10 minutes taken in sips while still warm.

• Antihypertonicum SSchuck, Ger.


• Betula ; crataegus ; mistletoe; olive; rhododendron leaf; rutoside;proxyphylline.
• Atherosclerosis; hypertension.
• Cefalektin Cefak, Ger.
• Mistletoe.
• Malignant neoplasms.
Valerian (Valeriana): whether this drug acts as a peripheral or central vasodilator or if the activity is due to a
general calming effect on the nervous system is not known. It is usually prescribed for stressed patients.

Olive leaves (Olea europaea ): has been proven to lower high blood pressure in clinical trials provided the dose is
sufficiently high. Constituents: Choline-type substances and glycoside, oleoside.

Coleus forskohlii: can have a pronounced lowering effect on high blood pressure. Only varieties containing
forskolin should be used. Coleus also has pronounced antiplatelet activity, which may be desirable in some cases.
Cramp bark ( Viburnum opulus ): Yarrow ( Achillea millefolium ): is Taraxacum officinale (dandelion
this herb is thought to relax smooth used by some herbalists to leaves) has diuretic activity and high
muscle and has been used to specifically; lower an elevated levels of potassium and can be
augment antihypertensive diastolic blood pressure. useful especially for the treatment
prescriptions as avasorelaxant. of elevated systolic pressure in the
elderly.
Crataegus (hawthorn): as well as reducing high blood pressure this herb has a
trophic effect on the heartmuscle.
Angina
Treatment:
• a) Diet and lifestyle
• b) Herbal drugs
Hawthorn Berry
‫زعرور األودية‬
• Ph. Eur. 6.2 (Hawthorn Berries). The dried false fruits of Crataegus
oxyacantha (C. laevigata), or C. monogyna, or their hybrids or a
mixture of these false fruits. They contain not less than 1% of
procyanidins, calculated as cyaniding chloride with reference to
the dried drug. Protect fromlight.
• Ph. Eur. 6.2 (Hawthorn Leaf and Flower). The whole or cut, dried
flower bearing branches of Crataegus oxyacantha(C. laevigata), or
C. monogyna, or their hybrids or, more rarely, other European
Crataegus species including C. pentagyna, C. nigra, and C. azarolus.
It contains not less than 1.5% of flavonoids, calculated as
hyperoside calculated with reference to the dried drug. Protect
from light.
constituents:
- Flavonoids ( including hyperoside , rutin , and vitexin) and oligomeric
proanthocyanidins (largely responsible for action of drug).
- Biogenic amines (such as tyramine)(some of cardiotonic action)
- Triterpenes

hyperoside vitexin
Mechanism of action;
- Inhibition of phosphodiesterase activity in tissue with a subsequent inhibition of cAMP is
believed to be the mechanism of action.

- Hawthorn does not have a digitalis-like effect, but the drug have a completely different site
of action in the myocardium. Hawthorn does not exert its action in the contractile system of
the myocardium, but improves the myocardial energy metabolism. This probably explains
why hawthorn requires a much Longer time than digitalis to take effect and why myocardial
reactivity must exist in order for the herbal drug to take effect.

- Hawthorn's biological profile of action summarized as follows:


1- Hawthorn increases coronary and myocardial circulation.
2- Hawthorn improves myocardial contractility (slightly positive inotropic).
3- It has a eurhythmic effect on certain types of electrical heart instabilities.
4- Hawthorn increases myocardial tolerance to oxygen deficiency.
5- Hawthorn increases cardiac output, reduces peripheral resistance (a parameter of after-
load), and increases cardiac performance.
Indication:

- Cardiotonic (mild), cardioprotective, hypotensive, antiarrhythmic. i.e. increases force of


myocardial contraction, increases coronary blood flow, reduces myocardial oxygen demand,
protects against myocardial damage, improves heart rate variability. Can be used for
congestive heart disease due to ischemia or hypertension; cardiac insufficiency.
- Reduction of cholesterol.
- Stabilization of connective tissue tone (collagen stabilizing);
- Antioxidant activity; co-factor for vitamin Cintake;

Interactions:
Hawthorn may act in synergy with digitalis glycosides, beta-blockers and other hypotensive
drugs. Modification of drug dosage may be required.
Dosage:
a)1.5 - 3.5 g of dried berry, flower or leaf per day, as infusion or decoction.
b)Hawthorn tablets (1 g leaves and flowers, standardized to 15-20 mgoligomeric
procyanidins and 6-7 mg flavonoids) 2-3 times perday.
c)3 - 6 ml of 1: 2 liquid extract of hawthorn leaf per day, 3 -
7 ml of 1: 2 liquid extract of hawthorn berry per day,
7.5 - 15 ml of 1: 5 tincture of hawthorn leaf per day,
7.5 - 17.5 ml of 1: 5 tincture of hawthorn berry per day.
Higher doses than these may be necessary for effective control of hypertension.
- There is no restriction on the long-term use of hawthorn and, if used to treat heart
conditions, it should be prescribed over a period of at least 2 months.
Garlic (Alliumsativum)
Constituents:
Alliin, allicin, S-propylcysteinesulfoxide and5-methylcysteine-sulfoxide.
Action and uses:
Garlic (Allium sativum) has Protective effects against stroke, coronary thrombosis,
atherosclerosis, platelet aggregation.
- Antibacterial, antifungal, antiviral, antioxidant, antineoplastic, hypolipidemic,antiarthritic
actions and hypoglycemic functions.
- General tonic effect thought stimulation ofhypophyseal function.
Dosage:
Bulb: 10 - 25 g;
Alliin: 10 mg;
Allicin: 4 mg.
Preparations:

1Carefully dried garlic powder which preserves the compound alliin (S-
allylcysteine sulphoxide) and the enzyme alliinase. On disintegration of
tablets or capsules containing this powder in the digestive tract, alliin comes
into contact with alliinase and is converted to allicin.

2Aged garlic extracts or 'odorless' garlic products which are produced by a


fermentation process. These preparations contain modified sulfur compounds
such as S-allylcysteine.

3 Steam-distilled preparations of garlic (garlic oil) which are rich indiallylsulfides.


- Salvia miltiorrhiza (dan shen) is a Chinese herb, which has been
clinically studied for angina and other heart conditions. Itsbenefits
include cardioprotective, vasodilator and anti-platelet activities.

-Anti-platelet herbs such as Coleus forskohlii. Allium sativum (garlic),


Zingiber (ginger) and Curcuma longa (turmeric) may have value even
if the patient is taking aspirin.
Hyperlipidemia
Gymnema (Gymnema sylvestre)
‫الغورمار )باركستا( أو حارق السكر‬

• Constituents:
• Saponins (Gymnemic Acids), alkaloids, flavones and anthraquinones.

• Action and uses:


• Saponins have been reported to
- Decrease plasma-cholesterol levels.
- Decrease blood glucose levels.
- Antiobesity.
• Mechanism of actions:
• Saponins decrease intestinal absorption of cholesterol and glucose and
• increases insulin secretion in human β-cells.
• It has anti-sweetness (which decrease the appetite
• Dosage:
• - 200:400 mg of extract taken by mouth twice daily
• - 2 ml of an aqueous decoction(10 grams of shade-dried powdered leavesper
100 milliliters) three times daily have beenstudied.
Statins (HMG-CoA reductaseinhibitors):
• Inhibiting cholesterol synthesis
• Increasing LDLuptake: draw cholesterol out of the circulation.
• 1- Lovastatin
It was isolated in the 1970s in the broths of Monascus ruber (red yeast rice),
Aspergillus terreus and Pleurotus ostreatus (oyster mashroom). Lovastatin,the
first commercially marketed statin, was approved by the FDAin 1987.
2-Simvastatin 3-Mevastatin ( compactin) 4-Pravastatin
A semi-synthetic derivativeof The first member Another statin, pravastatin (US$3.6
lovastatin is simvastatin, a of the group (compactin; mevastatin) billion per year), is made through
major hypocholesterolemic drug, was isolated as an different biotransformation
selling for US$7 billion per year antibiotic product of Penicillium processes from compactin by
before becoming generic. brevicompactum and later from Streptomyces carbophilus and
Penicillium citrinum. Actinomadura sp.

5-A synthetic compound, modeled from the structure of the natural statins, is
atorvastin, which has been the leading drug of the entire pharmaceutical industry in
terms of market share (approximately US$14 billion per year) for many years.
Varicose veins
• Causes
• Weakness of the vein wall and poor venous tone can lead tovenous
valves becoming incompetent.
Horse-chestnut seed
(Aesculus hippocastanum)
‫كستناء الحصان‬
Constituents:
• Saponins (3- 6%) (the mixture of saponins collectively referred to as escin; α- and -escin as
major glycosides), Coumarins, flavonoids and tannins.

Action and uses:


- It can be used for chronic venous insufficiency, varicose veins, edema of the lower limbs.
• - It is used as prophylactic to decrease the incidence of deep venous thrombosis following
surgery.
• - Topically for hematoma, contusions, non-penetrating wounds and injuries involving
edema.
- Skin care products: for normal skin, baby skin, sensitive skin; to tone the skin; as an anti-
inflammatory; to treat fragile capillaries, pimples, sunburn or cellulite.
Mechanism of actions:
• (Increases venous tone, increases capillary resistance, decreases capillary permeability,
improves circulation by toning veins; decreases edema from lymphatic congestion or of
inflammatory origin, i.e. venotonic, anti-edematous,anti-inflammatory)
Dosage:
• Dried seed: 1 - 2 g per day.
• Horse-chestnut tablets (200 mg of 5 : 1 concentrated extract, standardized to contain 40
mg escin): 2-3 tablets per day.

Proprietary names:
• Reparil® Tablets, Reparil® gel, Escinogel® gel, Prostatin® suppositories
Melilot (Melilotus officinalis)
‫الحندقوق الطبي أو إكليل الملك‬

• Constituents:
• Melilot contains coumarin and flavones.
• Action and uses:
• Internally in the treatment ofvaricose veins and thrombophlebitis.
• Preparations:
• Melilot tea, 1-2 teaspoons to a cup of boiling water, left to infuse,
taking 3-4 cups daily.
Flavonoids as Polyphenolic compounds e.g.
anthocyanins and maintaining healthycirculation.
• Anthocyanins could also reduce the incidences of fragility of capillaries, inhibit
blood platelet aggregation, and strengthen the collagen matrix which is a
component of the connectivetissues.
• These polyphenolics such as anthocyanins and flavonoids might also act as the
beneficial in vivo inhibitors of LDLoxidation.
• In fact, the “French paradox” which represents the apparent compatibility ofa
high fat diet with a low incidence of coronary atherosclerosis has daily been
attributed to the regular drinking of the red wines.
• ex. bilberry and grape seeds extract.
Rue (Rutagraveolens)
‫سذاب شديد الرائحة‬
• Constituents and uses:
• It contains rutin, considered to be a compound with vitamin Pactivity.

• Preparations:
• Ruta Ctablets® and Rutin Ctablets® contain 50 mg of rutin (rutoside),
so that the drug is easy to prescribe.
Functional heart disease,
nervous heart

Cardiovascular disease of functional origin is extremely common nowadays.

The drugs used in these cases should have a gentle cardiotonic and sedative
action. They are therefore also known as cardiosedatives. The plant kingdom
provides a number of drugs for this purpose, all of which have stood the test of
time.

Motherwort and convallaria (Lily of the valley) are gentle and Intermediate
cardiotonics respectively .
Motherwort (Leonurus cardiaca)
‫ذنب األسد‬
Constituents:
Alkaloids: leonurine Stachydrine, betonicine, and turicin ; flavonoids; iridoids; tannins;
terpenoids ... etc.

Uses:
Mainly for functional heart complaints due to autonomic imbalance. It appears to be
predominantly sedative, similar to valerian. It is necessary, however, to take the drug for
a long period, over months.

A tea combining the drug with convallaria and melissa (as a sedative) is very useful.
Motherwort herb
Lily of the valley herb
Melissa leaves
equal parts to make 100.0
Infuse two teaspoons in a cup of boiling water, 1 cup to be taken regularly morning and
night for some weeks.
Lily of the valley (Convallaria majalis)
‫زنبق الوادي‬
Constituents:

Cardiac glycoside: Convallamarin and Convallarin convallatoxin , trace of volatile oil,


tannin

Uses:
cardiac tonic and diuretic.

Mechanism of actions:

The action of the drug closely resembles that of Digitalis, though it is less powerful

Dose

The infusion of 3 teaspoonful of herb to 2 cup of boiling water is also taken in


tablespoonful doses
Digoxin
A cardiotonic glycoside obtained from the leaves of Digitalis lanata
(Scrophulariaceae).
Digoxin in Pharmacopoeias.
• Ph. Eur. 6.2 (Digoxin). A white or almost white powder or colourless
crystals. Practically insoluble in water; slightly soluble in alcohol; freely
soluble in a mixture of equal volumes of dichloromethane and methyl
alcohol. Protect from light.

• USP31 (Digoxin). Acardiotonic glycoside obtained from theleaves of


Digitalis lanata (Scrophulariaceae). Clear to white, odourless, crystals,or
a white, odourless, crystalline powder. Practically insoluble in water and
in ether; slightly soluble in diluted alcohol and in chloroform; freely
soluble in pyridine. Store in airtight containers.
Uses:
Digoxin is a cardiac glycoside used in the management of
1supraventricular arrhythmias, particularly atrialfibrillation
and
2 in heart failure.
• Pharmacology
The principal actions of digoxin are
1an increase in the force ofmyocardial contraction
(positive inotropic activity) ,
2decrease heart rate (negative chronotropic effects ) and
3- decreased AV nodal activity(negativedromotropy).
1-By inhibiting the Na+/K+-ATPase, cause increase intracellular sodium
concentration, which leads to an accumulation of intracellular calcium via the Na+-
Ca++exchange system. Increased intracellular calcium.
A-In the heart, increases contractility (positive inotropic activity).
B-In vascular smooth muscle causes smooth muscle contraction and
vasoconstriction.

2-By mechanisms that are not fully understood, digoxin also increase vagal
efferent activity to the heart. This parasympathomimetic action of digoxin
(decreases heart rate; negative chronotropy) and reduces conduction velocity
of electrical impulses through the atrioventricular node (negative
dromotropy).
products examples
Egypt : Lanoxin ®tab & amp and Cardixine ®tab France:
Hemigoxine Nativelle tab ®Germany : Lanicor® tab ®UK:
Lanoxin ®tab & amp USA: Digitek ®tab.