Schedule 20 herbs

Hananja Brice-Ytsma

Alkaloids
Alkaloids are alkaline nitrogen-containing heterocyclic compounds derived from
plants, exhibiting marked pharmacological activity.( Nitrogen; in all living organisms,
primarily in amino acids and thus proteins and in the nucleic acids (DNA and RNA).
The human body contains about 3% by weight of nitrogen, the fourth most abundant
element after oxygen, carbon, and hydrogen. Nitrogen resides in the chemical structure of
almost all neurotransmitters, and is a defining component of alkaloids)
The word derives from the term vegetable alkali(= a mixture of potassium
hydroxide and carbonate), referring to the alkaline nature of these compounds.

Alkaloids are found in 15-30% of all flowering plants, common in Fabaceae,

Liliaceae, Ranunculaceae, Apocynaceae, Solanaceae, Papaveraceae.
Most common; caffeine, berberine
Names of alkaloids end on -ine
morphine, narcotine from opium; the first chemical drug derived from plants.

Synthesized by the plant from amino acids, if they are not then they are called
pseudoalkaloids, or terpenoids. (Pseudoalkaloids are terpenoids that contain
nitrogen or are derived from acetate)
May have defensive role in plants, or by-product of primary metabolism.
Most are susceptible to destruction by heat, some by exposure to heat and air. Most
water insoluble, soluble in alcohol.
Ability to cross the blood-brain barrier and exert depressant or stimulant effect on the
central nervous system, ability to interact with various neurotransmitter receptors. Most
have profound physiological actions, with nervous system effects being the most
prominent
morphine, codeine; CNS depressant , Analgesic/narcotic
caffeine, cocaine; CNS stimulants
ephedrine; sympathetic nervous system stimulant; hypertensives;
Hyoscamine; parasympathetic depressant
mydriatics (dilation of the pupil); atropine
miotics (constriction of the pupil); pilocarpine
bronchodilator; lobeline
antimicrobial; berberine

Cinchona alkaloids; quinine, quinidine

History
The medicinal properties originally discovered by the Quechua, indigenous to Peru
and Bolivia; the Jesuits were the first to bring the cinchona to Europe.
Quinine was the first effective treatment for malaria caused by Plasmodium
falciparum, appearing in therapeutics in the 17th century. It remained the
antimalarial drug of choice until the 1940s.

Quinine is still used to treat the disease in certain critical circumstances, such as severe
malaria, due to its low cost. In very small quantities found in tonic water. Quinine used
to treat lupus and arthritis. Quinine was treatment for nocturnal leg cramps, but this has
since been prohibited, in effect, by an FDA statement warning against the practice.

According to legend, the first European ever to be cured from malaria fever was the
countess of Chinchón, the wife of the Spanish Luis Jerónimo de Cabrera, 4th Count of
Chinchón - the Viceroy of Peru. (Chinchón is a small town in central Spain). In the
Viceroyalty of Peru, the court physician was summoned and urged to save the countess
from the waves of fever and chill threatening her life, but every effort failed to relieve
her. At last, the physician administered some medicine he had obtained from the local
Indians, who had been using it for similar syndromes. The countess survived the malarial
attack and reportedly brought the cinchona bark back with her when she returned to
Europe in the 1640s.
In the late 1640s, the method of use of the bark was noted in the Schedula
Romana, and in 1677, the use of the bark was noted in the London
Pharmacopoeia.
Charles II called upon Robert Talbor, who had become famous for his miraculous malaria
cure. Because at that time the bark was in religious controversy,
Talbor gave the king the bitter bark decoction in great secrecy. The treatment gave the
king complete relief from the malaria fever. In return, he was offered membership of the
prestigious Royal College of Physicians. In 1679, Talbor was called by the King of
France, Louis XIV, whose son was suffering from malaria fever. After a successful
treatment, Talbor was rewarded by the king with 3,000 gold crowns and a lifetime
pension for this prescription. Talbor, however, was asked to keep the entire episode
secret.
(Dissension, however, was rife at the time, mainly due to its source of discovery, the
Jesuits. As the great Alexander von Humboldt said, "It almost goes without saying that
among Protestant physicians hatred of the Jesuits and religious intolerance lie at the
bottom of the long conflict over the good or harm effected by Peruvian Bark".)
After Talbor's death, the French king found this formula: six drams of rose leaves, two
ounces of lemon juice and a strong decoction of the cinchona bark served with wine.
Wine was used because some alkaloids of the cinchona bark are not soluble in water, but
are soluble in the ethanol in wine.

Actions
Antimalarial, skeletal muscle relaxant, febrifuge for colds, influenza, cardiac
arrythmias
Constituents
Quinine; antipyretic (fever-reducing), antimalarial, analgesic (painkilling), and anti-
inflammatory properties and a bitter taste.
Quinine; It is a stereoisomer of quinidine
quinidine; cardiac arrythmias, atrial flutter, fibrillation; depresses myocardial
excitability, conduction, contractibility.

Pharmacology
mechanism of action of quinine on malaria has not been fully resolved. Hypothesis;
involves the inhibition of hemozoin biocrystallization, which facilitates the aggregation
of cytotoxic heme. Free cytotoxic heme accumulates in the parasites, leading to their
deaths.

Blood feeding organisms digest hemoglobin and release high quantities of free
toxic heme. To avoid destruction by this molecule, the parasite biocrystallizes
heme to form hemozoin. Hemozoin is per definitionem not a mineral and
therefore not formed by biomineralization. Heme biocrystallization has been
found in blood feeding organisms of great medical importance including
Plasmodium, Rhodnius and Schistosoma. Heme biocrystallization is inhibited
by quinoline antimalarials such as Chloroquine.

Toxicity
tinnitus, skin rash, vertigo, bleeding, bruising, visual disturbances.

Dosage; 1:5 25ml per week

Tropane alkaloids; Solanaceae

Atropa belladonna, Datura stramonium, Hyoscymus niger; containing hyoscamine,
hyoscine, atropine, scopalamine.

Tropane alkaloids; Anticholinergic, Parasympatholytic properties, and a powerful effect

on the CNS. so reduce the effects mediated by acetylcholine on acetylcholine receptors
in neurons through competitive inhibition.

(Anticholinergic, a substance that blocks the passage of certain nerve impulses

in the central nervous system by inhibiting the production of acetylcholine, a
neurotransmitter (a substance that carries signals between nerves and
muscles). An anticholinergic`s wide range of effects makes it effective as
medication before surgery. It may be put in the eyes before examination or
treatment to dilate the pupil and paralyze the muscles of accommodation (the
muscles that help focus the eye), or it may be inhaled to relieve constriction of
the airways in bronchitis.
An anticholinergic can reduce tremor and rigidity (stiffness) in mild Parkinson
disease. In the treatment of urinary frequency, it may improve bladder muscle
tone. Its usefulness in relieving or preventing spasms is limited by side
effects, such as dry mouth, visual disturbances, and urinary retention.)
Acetylcholine receptors are classified into two groups;
1. muscarinic, which respond to muscarine
2. nicotinic, which respond to nicotine

Hyoscamine; Anti-muscarinic and parasympathetic depressant (a muscarinic receptor

antagonist ; agent that blocks the activity of the muscarinic acetylcholine
receptor)
- Spasmolytic effect on bronchial and intestinal smooth muscle.
- Mydriatic effect (inhibits contraction of iris muscle).
- Reduces salivary and sweat gland secretions.
- Controls excess motor activity in GIT, antidiarrhaeal.
- Reduces rigidity and tremors of parkinsonism.

Atropa belladonna
- atropin, active flavonol glycosides speeds up the absorption

History; The plant in Chaucer's days was known as Dwale, which probably derived
from the Scandinavian dool, meaning delay or sleep. Other authorities have derived
the word from the French deuil (grief), a reference to its fatal properties.
Adult may eat two or three berries without injury, but dangerous symptoms appear if
more are taken, and it is wiser not to attempt the experiment! Though so powerful in its
action on the human body, the plant seems to affect some of the animals but little. Eight
pounds of the herb are said to have been eaten by a horse without causing any injury, and
an ass swallowed 1 lb. of the ripe berries without any bad results following. Rabbits,
sheep, goats and swine eat the leaves with impunity, and birds often eat the seeds without
any apparent effect, but cats and dogs are very susceptible to the poison.
Buchanan relates in his History of Scotland (1582) a tradition that when Duncan I was
King of Scotland, the soldiers of Macbeth poisoned a whole army of invading Danes by a
liquor mixed with an infusion of Dwale supplied to them during a truce. Suspecting
nothing, the invaders drank deeply and were easily overpowered and murdered in their
sleep by the Scots.
According to old legends, the plant belongs to the devil who goes about trimming and
tending it in his leisure, and can only be diverted from its care on one night in the year,
that is on Walpurgis, when he is preparing for the witches' sabbath.
Belladonna is said to record an old superstition that at certain times it takes the form of an
enchantress of exceeding loveliness, whom it is dangerous to look upon. Though a more
generally accepted view is that the name was bestowed on it because its juice was used
by the Italian ladies to give their eyes greater brilliancy, the smallest quantity having the
effect of dilating the pupils of the eye. Another derivation is founded on the old tradition
that the priests used to drink an infusion before they worshipped and invoked the aid of
Bellona, the Goddess of War.
The generic name of the plant, Atropa, is derived from the Greek Atropos, one of the
Fates who held the shears to cut the thread of human life - a reference to its deadly,
poisonous nature.
Gerard (1597) calls the plant the Sleeping Nightshade, and says the leaves
moistened in wine vinegar and laid on the head induce sleep.
Mandrake, a foreign species of Atropa (A. Mandragora), was used in Pliny's day as an
anaesthetic for operations. The sleeping potion of Juliet was a preparation from this
plant - perhaps also the Mandrake wine of the Ancients. It was called Circaeon, being
the wine of Circe.
The root was not used in medicine here until 1860, when Peter Squire
recommended it as the basis of an anodyne liniment.

Specific uses
- Biliary dyskinesia
- Weiss; unsurpassed as an antispasmodic drug for the GIT; intestinal spasms with
acute or chronic enterocolitis, painful spasm of gallstones, kidney stones, enuresis.
Usually needs to be used for several weeks or more.
- dysmenorrhoea.
- Tremor and rigidity of parkinsonism, including the idiopathic form, also senile
tremors, and other forms of abnormally increased motor function although
superseded by L-dopa.
- Excessive salivation, hyperhiderosis, pertussis, asthma
- Externally; neuralgia, gout, rheumatism, sciatica (root)
- Weiss; ulcers, chronic intestinal diseases, spastic constipation. When rapid action
is required e.g. gallbladder colic, may be inadequate, to get satisfactory results it is
necessary to go as close to the limit of tolerance.
- Acts rapidly, lasting effect, suppresses secretions e.g. hyperacidity
symptoms.
- Herbs and root are used similarly; dosages less for the root.- Root tends to be used
externally as anodyne and counter irritant.

Contraindications to all tropane alkaloids herbs;

- Tachycardia; may accelerate the pulse
- prostatic hypertrophy; may result in strangury
- paralytic ileus; may cause obstructions
- glaucoma; may increase intra-ocular pressure
- action may be accentuated by antidepressant drugs.

Dosage
Dried leaf; 50 mg, TDS, equivalent to 1:10 0.5ml
recommended initial dose per week 2 ml of 1:10, not exceed 10 ml per week. Root
30mg, equivalent to 0.3ml of tincture of 1:10
Root; maximum 6 ml per week.

Weiss; from the beginning the dose should be as such that there is just a slight dryness
in the mouth and perhaps mild disturbance of vision, question carefully
on 3rd, 4th day of treatment. Once dry mouth stated, slightly reduce dose, and this is
the dose adhered to for some time.
Average dosage 8gtt TDS in water for men, 6gtt TDS for women. 10gtt will result in
dry mouth within one or two days.

Duration; normally 3-4 weeks with ulcers and gastritis.

Lower dose; for spastic constipation, mucous colitis and spastic symptoms of
fermentive dyspepsia.
Severe chronic colitis; as with ulcers therapy, high dosage.
Combines well with chamomile

Toxicity to all herbs with tropane alkaloids

Dry mouth, dysphagia, pupil dilation, photophobia, bradycardia followed by rapid
heartbeat, stertorous respiration (characterized by a heavy snoring or gasping sound, i.e.
hoarsely breathing). confusion, delirium.
Treatment; emetic, stomach lavage. Strong tea without milk, tannins to inactivate
alkaloids. Recumbent position. Summon trained help immediately.
Weiss; patients with organic changes in the brain have a much greater tolerance for these
drugs than healthy people.

Datura stramonium (Thornapple)

Constituents;
tropane alkaloids, hyocyamine, hyosine, which relieve the spasm in the bronchi.

History
The practice of smoking D. ferox for asthma introduced into Great Britain from the
East Indies, and afterwards the English species was substituted for that employed in
Hindustan. Formerly the roots were much used: in Ceylon, the leaves, stem and fruit
are all cut up together to make burning powders for asthma, but in this country the
dried leaves are almost exclusively employed for this purpose

Constitnuents
atropine, which paralyses the endings of the pulmonary branches, thus relieving the
bronchial spasm. It has been proved that the smoke from a Stramonium cigarette,
containing 0.25 grams of Stramonium, leaves contains as much as 0.5 milligrams of
atropine.

Indication and specific uses

- relief of bronchitic spasm without drying up mucous secretions, can be used over
extended periods without harm.; Asthma, pertussis. According to Weiss; Used as burning
powder, can be reused over and over again. Action is enhanced by adding potassium
nitrate in asthma powders and cigarettes.
The leaves may be made up into cigarettes or smoked in a pipe, either alone, or with a
mixture of tobacco, or with cubebs, sage, belladonna cigarettes or smoked
in a pipe, either alone, or with a mixture of tobacco, or with cubebs, sage,
belladonna and other drugs.
Coarsely-ground leaves are mixed into cones with some aromatic and with equal parts of
potassium nitrate, in order to increase combustion and are burned in a saucer, the smoke
being inhaled into the lungs, the effect being more immediate when the powdered leaves
are burnt and the smoke inhaled than when smoked by the patient in the form of cigars or
cigarettes, but after constant use, the relief is not so great and the treatment is only
palliative, the causation of the attack not being affected.
- Relieves colic, visceral spasm, depresses visceral function.
- Improves coordination of lower motor centres, especially in paralysis and tremor;
parkinsonism, paralytic and tremor conditions; Weiss; relieve tremor, good results seen
in paralysis agitans, and other forms of tremor (symptomatic treatment). Tremor in
paralysed limbs of soldiers shot in the brain responded well to datura tincture. No
difference in action between Hyoscyamus or Datura.
For senile tremor start with 15 drops per day increasing to 40 or even 60 a day.
- schizophrenic excitability

Lower motor neurons (LMNs) are the motor neurons connecting the brainstem
and spinal cord to muscle fibers, bringing the nerve impulses from the upper
motor neurons out to the muscles. A lower motor neuron's axon terminates on
an effector (muscle). Damage to lower motor neurons, lower motor neuron
lesions (LMNL) cause decreased tone, decreased strength and decreased
reflexes in affected areas.LMNL ; fasciculations, paralysis, weakening of
muscles, and neurogenic atrophy of skeletal muscle.

Upper motor neurons are motor neurons that originate in the motor region of the
cerebral cortex or the brain stem and carry motor information down to the final
common pathway, that is, any motor neurons that are not directly responsible
for stimulating the target muscle.
Upper motor neuron;
Damage to the descending motor pathways anywhere along the trajectory from
the cerebral cortex to the lower end of the spinal cord; "upper motor neuron
syndrome". Signs may appear over days or weeks following brain or spinal cord
damage, including muscle weakness, decreased motor control including a loss
of the ability to perform fine movements, increased vigor (and decreased
threshold) of spinal reflexes including spasticity, and an extensor plantar
response known as the Babinski sign.

Toxicology
As above, can cause excitability, hallucinations and increased respiratory activity

Dosage
Dried leaf; 50 mg, TDS, inequivalent to 1:10 0.5ml
recommended initial dose per week 2 ml of 1:10, not exceed 10 ml per week. Root
30mg,equivalent to 0.3ml of tincture of 1:10
Root; maximum 6 ml per week.

Hyoscyamus nigra (henbane)

Constituents;
tropane alkaloids; hysoscyamine, and others. the least potent of the three

History
Henbane; commended by Dioscorides (first century A.D.), who used it to procure sleep
and allay pains. Celsus (same period) and others made use of it for the same purpose,
internally and externally, though Pliny declared it to be 'of the nature of wine and
therefore offensive to the understanding.' Later it fell into disuse.
It was omitted from the London Pharmacopoeia of 1746 and 1788, and only
restored in 1809, its re-introduction being chiefly due to experiments and
recommendations by Baron Storch, who gave it in the form of an extract, in cases
of epilepsy and other nervous and convulsive diseases.
It is supposed that this is the noxious herb referred to by Shakespeare in Hamlet: Gerard;
The leaves, the seeds and the juice, when taken internally cause an unquiet sleep, like
unto the sleep of drunkenness, which continueth long and is deadly to the patient. To
wash the feet in a decoction of Henbane, as also the often smelling of the flowers causeth
sleep.'
Culpepper: The leaves of Henbane do cool all hot inflammations in the eyes.................It
also assuages the pain of the gout, the sciatica, and other pains in the joints which
arise from a hot cause. And applied with vinegar to the forehead and temples, helps
the headache and want of sleep in hot fevers.........................................The oil of the
seed is helpful for deafness, noise and worms in the ears, being dropped therein; the juice
of the herb or root doth the same. The decoction of the herb or seed, or both, kills lice in
man or beast. The fume of the dried herb stalks and seeds, burned, quickly heals
swellings, chilblains or kibes in the hands or feet, by holding them in the fume thereof.

The remedy to help those that have taken Henbane is to drink goat's milk, honeyed
water, or pine kernels, with sweet wine; or, in the absence of these, Fennel seed, Nettle
seed, the seed of Cresses, Mustard or Radish; as also Onions or Garlic taken in wine,
do all help to free them from danger and restore them to their due temper again. Take
notice, that this herb must never be taken inwardly; outwardly, an oil, ointment, or
plaister of it is most admirable for the gout . . . to stop the toothache, applied to the
aching side......................................................................................'

The leaves or roots eaten produce maniacal delirium.

Old writer says: 'If it be used either in sallet or in pottage, then doth it bring frenzie,
and whoso useth more than four leaves shall be in danger to sleepe without waking.'
The herb was used in magic and diabolism, for its power of throwing its victims into
convulsions. It was employed by witches in their midnight brews, and from the leaves
was prepared a famous sorcerer's ointment.
Anodyne necklaces were made from the root and were hung about the necks of children
as charms to prevent fits and to cause easy teething.

In mythology; the dead in Hades were crowned with it as they wandered hopelessly
beside the Styx. The herb is also called Hog's-bean, and both its botanical name
Hyoscyamus and the tenth-century Jusquiasmus are derived from the Greek words
hyos and cyamos, signifying 'the bean of the hog,' which animal is supposed to eat it
with impunity.
An old AngloSaxon name for it was 'Belene,' probably from the bell-shaped flowers;
then it became known as 'Hen-bell,' and from the time that its poisonous properties were
recognized this name was changed to 'Henbane,' because the seeds were thought to be
fatal to poultry. Possible the name Henbane is derived from the Spanish hinna (a mule),
e.g. 'henna bell,' referring to the similarity of its seed-vessel to the bell hung upon the
neck of the mules.

Eclectic tradition; Delirium, excitability, restlessness, insomnia with nightmares,

flushed face with red eyes and wild look, especially in exhaustion from long illness or
old age, neuralgic and bone pain.

Indications and specific indications

Mainly used to relieve tremors; Paralysis agitans, senile tremor.
Prophylactic for motion sickness, Meniere’s disease.
Asthmatic constrictions, pertussis, dry coughs
Sedative and smooth muscle relaxant, to prevent griping of purgatives, painful spasm
of urinary tract, similar to Atropa belladonna but milder.
Weiss; fresh herb more preferable.
Externally the oils used for rheumatic and nerve pain.

Toxicity;
As with all tropane alkaloids; Dilated pupils, impaired vision, dryness of skin and
secretions, extreme thirst, hallucinations, loss of conciousness.

The leaves are the most powerful portion, even the odour of them when fresh; giddiness
and stupor. Accidental cases ;its roots, like those of salsafy, have sometimes been
gathered and eaten. A woman pulled up a quantity of Henbane roots which she found in
a field, supposing them to be parsnips. She boiled them in soup, which was eaten by the
family. The whole of the nine persons who had partaken of them suffered severely, being
soon seized with indistinctness of vision, giddiness and sleepiness, followed by delirium
and convulsions.
Inmates of a monastery were once poisoned by using the roots instead of chicory. The
monks partaking of the roots for supper were all more or less affected during the night
and following day, being attacked with a sort of delirious
frenzy, accompanied in many cases by such hallucinations that the
establishment resembled a lunatic asylum.
Cows, however, have been poisoned by having Henbane mixed with their forage, it is
said for the purpose of fattening them. A small quantity of the seeds of the Stramonium
or Thornapple, as well as those of Henbane, are also sometimes added, the idea appears
to be that the tendency to stupor and repose caused by these plants is conducive to
fattening. In some districts, horse-dealers mix the seeds of Henbane with their oats, in
order to fatten their animals.

Dosage
1:10 20 ml

Chelidonium majus
True Celandine, having nothing in common with the Lesser Celandine except the colour
of its flowers.

History
Used Middle Ages and is mentioned by Pliny, to whom we owe the tradition that it is
called Chelidonium from the Greek chelidon (a swallow), because it comes into flower
when the swallows arrive and fades at their departure. (The English name Celandine is
a corruption of the Greek word.)
Its acrid juice has been used in removing films from the cornea of the eye, a property
which Pliny tells us was discovered by swallows, this being a double reason why the
plant should be named after these birds.
Gerard says: 'the juice of the herbe is good to sharpen the sight, for it cleanseth and
consumeth away slimie things that cleave about the ball of the eye and hinder the sight
and especially being boiled with honey in a brasen vessell, as Dioscorides teacheth.'
In the fourteenth century, a drink made with Celandine was good for the blood.
Clusius, the celebrated Dutch botanist, considered that the juice, dropped into small
green wounds, effected rapid cure, and when dropped into the eye would take away
specks and stop incipient suffusions. The old alchemists held that it was good to
'superstifle the jaundice,' because of its intense yellow colour.
Traditional reputation as a liver herb.

Constituents;
The orange juice which is rich in alkaloids. Juice contains an enzyme capable of breaking
down nucleic acid (such as in viruses), and may be responsible for the activity against
warts.
The dried herb contains; 1.0% alkaloids including chelidonine, sanguinarine, coptisine
and chelerythrine. Also chelidonic acid and other plant acids, and the phenolic fraction
contains hydroxycinnamic acid derivatives and flavonoids.

Actions
Hepatoprotective; in vivo Oral administration of an alcohol extract of dried
Chelidonium reduced carbon tetrachloride-induced liver injury. Significant
reductions in elevated plasma levels of liver enzymes and bilirubin occurred
in the treated group.
* Cholagogue Effect; Silybum marianum, Chelidonium and Curcuma on 28
patients. In comparison to a control liquid, the herbal mixture demonstrated a greater
increase in bile flow and pancreatic secretion.
Choleretic; The total extract of the herb significantly induced choleresis (bile flow).
However, it did this without increasing the total output of bile acids (ie there was an
increased flow of more dilute bile). The increased bile flow is due to an additive effect
from all compounds in the total extract of Chelidonium and not one or two specific active
constituents or fractions.
Pancreatic secretion increased (combined with wormwood)
* Spasmolytic and analgesic; alkaloids similar to the ones found in other poppies, eg
papaverine and codeine from the opium poppy). directed at the bile ducts and bronchi.
Antimicrobial Activity against Gram-positive bacteria, such as Staphylococcus aureus,
two strains of Streptococcus and also against the fungus Candida albican.
antifungal Fluid extracts of Chelidonium prepared from dried plant showed greater than
average antifungal activity against organisms involved in skin infections such as
Microsporum gypseum, Trichophyton mentagrophytes, Epidermophyton floccosum and
Candida pseudotropicalis. The July extract was effective against Candida albicans, but
the September extract showed no activity. Antitumour Activity; Crude chelidonine and
protopine (insoluble in water), showed insignificant tumour inhibition. In vitro;
Cytotoxic, (a carcinoma of the nasopharynx. One of the cytotoxic principles was the
alkaloid coptisine.
antimutagenic effect In vitro
Anti-inflammatory Activity; in vivo, chelerythrine and sanguinarine; anti- inflammatory
activity in the carrageenan rat paw oedema test.

Clinical trials
Cramp, GIT; 608 patients were treated and observed in an open study over a 3- month
period, dried Chelidonium. (dried herb equivalent dosage was 3 to 5 g per day).
Symptoms were cramp-like pains in the gastrointestinal tract (43%) or gall ducts
(48.2%). Each Chelidonium tablet contained 2.85 mg of total alkaloids including 0.79
mg of chelidonine. The dose was initially 5 tablets/day and this was reduced to 3
tablets/day in patients who responded to treatment. The average duration of treatment
necessary was 22 days and the longest treatment time was 2.5 months.
A good or very good therapeutic effect on symptoms with a quick response in 87.4% of
cases. In most cases relief occurred within 30 minutes of taking the herbal medication
(62.3%). In 46.1% of patients, the average duration of efficacy of each tablet dose was
better than 3 hours.
Polyps;In a small, open trial an infusion of dried Chelidonium was administered as an
enema for colonic polyposis. Administration of ten or more enemas resulted in
complete disappearance of colonic polyps in several cases. Study of the fresh plant
made into a paste and administered two or three hours after an evacuant enema. 2 or 3
courses (consisting of 10- 20 enemas each). Over a 2- year period treating 149 patients
with various forms of polyposis, 87% showed improvement with 27% making a
complete recovery.

Warts, papillomas, condylomas and nodules; An alcohol extract of Chelidonium was

used as a topical application to treat nursing mothers for in an open trial.
The extract was applied to the affected area approximately 200 times per day for 2 to 3
weeks or until improvement was observed. Complete resolution of the warts occurred
after 15-20 days in 135 individuals.

Chronic bronchitis; Chelidonium was given as a syrup or extract (equivalent to 15g of

herb per day) to patients with chronic bronchitis in an open study. The effective rate
was around 80%.

Whooping cough, Chelidonium syrup or a decoction of the fresh herb was used to treat
whooping cough in an open study. Treatment was for a course of 8 to 10 days. Of 500
cases so treated, 355 were cured and 116 improved.
Intravenous

Lung cancer; Anticancer Activity Ukrain ; Ukrain is believed to modulate the immune
system.;Intravenous injection to nine men with proven lung cancer resulted in
restoration of cellular immunity, characterised by an increase in the proportion of total
T-cells and a significant decrease in the percentage of T- suppressor cells. Objective
tumour regression was seen in 4 of the 9 treated patients.
Ovarian cancer, rectal cancer; Thirty-six stage III rectal and ovarian cancer patients
were treated with intravenous injection of Ukrain. Ukrain demonstrated cytostatic
activity in malignant cells at a concentration less than that required for cytostatic
activity in normal cells. Ukrain also demonstrated favourable immunoregulatory
properties by regulating the T-lymphocyte subsets.

Indications;
- Gall bladder disease, gall stones.
- Liver disease.
- Irritable bowel syndrome.
- Skin diseases such as psoriasis (the antimitotic activity of chelidonine may be
relevant to the internal and topical use of Chelidonium for psoriasis).
- Warts and polyps, especially the fresh juice topically
- In China, Chelidonium is known as Baiqucai and is used for the treatment of
gastritis, gastric ulcer, enteritis, jaundice, abdominal pain, bronchitis and whooping
cough.
- Intravenous; A cancer chemotherapy known as Ukrain has been developed from
the alkaloids of Chelidonium.

Dose
1 to 2 mL of the 1:2 fluid extract per day, maximum of 1:2 84ml per week. Short term
use of higher doses may be necessary, eg in the Berlin study doses up to the equivalent
of 3 g per day were used.
The dose used in China is 3 to 9 g per day, or even higher. However, Chinese doses are
generally administered by decoction and this method may not efficiently extract the
Chelidonium alkaloids.

Fresh or dried?
Spasmolytic activity of Chelidonium preparations; studies found it to be inconsistent,
the medicinal action is greatly reduced on prolonged storage. Weiss writes: “I have been
able to observe this for myself in extensive experiments with Chelidonium juice made
from fresh plants. During the first six months it was clearly effective. After that time,
however, the juice had practically no effect, and soon none at all”.
Only Chelidonium dried at 80°C preserved the levels of alkaloids found in the fresh
plant. When Chelidonium was dried at temperatures between 20 and 50°C, up to half of
its alkaloid content was lost. Due to continued enzyme activity in the plant as it dried,
This explains the instability of the Chelidonium juice, since lower levels of alcohol
added to a fresh plant do not completely inhibit enzyme activity.

The best solution to the problem posed by Weiss is to use Chelidonium

preparations stabilised for a known content of alkaloids.

Adverse effects
No harmful or toxic effects from therapeutic doses have been established. However,
excessive doses should be avoided (especially alcohol-water extracts).
- A case of haemolytic anaemia was reported after oral ingestion of
Chelidonium extract. The patient was treated with corticosteroids, blood
transfusions and haemodialysis and recovered after about 12 days.
- Adverse effects noted in Chinese usage include dry mouth, dizziness, gastric
discomfort, diarrhoea, abdominal distention, nausea and mild leukopaenia in a
minority of patients. Symptoms usually disappeared in 3 to 5 days without
discontinuation of the treatment
- Hepatotoxicity; A case history (BMJ) of a 69-year-old woman developed
symptoms of acute hepatitis after taking 6 to 15 herbal tablets per day for 6 weeks,
containing horsechestnut leaf, yarrow, greater celandine, sweet clover, milk thistle
and dandelion root. Also took thyroxine and ibuprofen. Withdrawal of ibuprofen
and the herbs for two weeks returned her liver function to normal levels,
reintroduction of the herbal tablets resulted in a return of her symptoms.
- In a case study from Germany presented in 1997, hepatotoxicity after ingestion of a
preparation of greater celandine, The same authors went on to
 publish this and an additional case history one year later. In both cases, patients were
taking several capsules per day of 200 mg of dry extract of greater celandine
(equivalent to about 1 g of dried herb and containing about 4 mg of alkaloids).
- 10 cases accumulated over two years of observations, hepatitis was mild to severe
and was associated with five different commercial products containing greater
celandine. Marked bile obstruction was observed in 5 patients, but liver failure did
not occur. Other possible causes of liver disease (viral, autoimmune, hereditary,
alcohol, and secondary biliary) were excluded by laboratory tests and imaging
procedures, and liver biopsy specimens were consistent with drug-induced damage.
After discontinuation of greater celandine, rapid recovery was observed in all patients
and liver enzyme levels returned to normal in 2-6 months. Unintentional rechallenge
led to a second flare of hepatic inflammation in one patient. The mechanism remains
unclear. An idiosyncratic reaction seems most likely because there appeared to be no
dose dependency and the period of intake before symptoms appeared was long and
variable. Low-grade autoimmunity had developed in 8 of 9 tested patients.

High doses should be restricted to short-term use and long-term use of normal doses is
not recommended.
Typically, herbalists prescribe tincture or fluid extract doses which do not exceed the
equivalent of 1 g per day of dried herb and they do not prescribe the herb for extended
periods. However, a German clinical trial published in 1993 (see above) changed this
pattern of use for greater celandine in that country. (using an uncontrolled design) over a
3-month period with a high-dose standardized extract (dried herb equivalent dosage was
3 to 5 g per day).
The long term use of greater celandine at high doses as a spasmolytic is not
consistent with its main traditional use for gall bladder and liver disease.

Lobelia inflata
History
The plant was known to the Penobscot Indians and was widely used in New England
long before the time of Samuel Thomson, who is credited with its discovery.
Thomsonians; emetic, diaphoretic, expectorant, sedative, antispasmodic, and anti-
asthmatic. Conditions for which it has been used: asthma, whooping cough, bruises,
sprains, ringworm, insect bites, poison ivy symptoms.
Thomson ; “there is no vegetable which the earth produces more harmless in its effect
on the human system, and none more powerful in removing disease and promoting
health than lobelia”.
It was brought into general professional use by Cutler of Massachusetts, it was used as
an expectorant in bronchitis, counterirritant when combined with other ingredients in
ointment form,- sometimes given in convulsive and inflammatory disorders such as
epilepsy, tetanus, diphtheria and tonsilitis.
Difference of opinion with regard to its narcotic properties. Where relaxation of the
system was required Lobelia was seen as invaluable. Relaxation can be counteracted by
the stimulating and tonic infusion of capsicum. It was also used as an enema.
Externally, an infusion has been found useful in ophthalmia, and the tincture used as a
local application for sprains, bruises, or skin diseases, alone, or in powder combined with
an equal part of slippery elm bark and weak lye-water in a poultice. The oil of Lobelia
was used in tetanus. One drop of oil triturated with one scruple of sugar, and divided into
from 6 to 12 doses, useful as an expectorant, nauseant, sedative, and diaphoretic, when
given every one or two hours.

Constituents;
0.48% pyridine (piperidine) alkaloids composed mainly of lobeline (soluble in water
) with lesser amounts of lobelanine, lobelanidine, and other alkaloids. Have their N
atoms in typical 6 membered rings.
Piperine (Piper nigrum); hepatoprotective
Other constituents include resin, gum, lipids, and chelidonic acid.

Pharmacology;
- lobeline; relaxant and bronchodilator, used as respiratory stimulant in narcotic
poisoning, without the other alkaloids it would be toxic, emetic and bronchial relaxant
- similar to nicotine (Nicotine; the precursor nicotinic acid (B3) common), but less
potent. Direct effect on the monoamine systems, it alters presynaptic dopamine storage,
binding to the vesicular monoamine reuptake transporter and preventing uptake, inhibits
dopamine uptake.
- Decreases basal release of acetyl choline, binds to the nicotine acetylcholine
receptors in ganglions, thus promoting the release of epinephrine and norepinephrin,
hence the therapeutic effects in asthma.
- Release of serotonins.
- acts as antagonist at neuronal calcium channel.
- Emetic, lobeline stimulates the emetic chemoreceptor trigger zone in the area
postrema of the medulla oblongata (this area is outside the blood–brain barrier) and
activates the vagal and spinal afferent nerves that form the sensory input of the reflex
pathways involved in vomiting.

isolobeline has paradoxical effect

- stimulates catarrh secretions and expectoration (emetic reflex)
- relaxes bronchial musculature
- protects from overdose by provoking emesis.

Clinical applications
Expectorant; pneumonia, asthma, and bronchitis. Although effective when used alone
in the treatment of asthma, it has traditionally been used in combination with other
herbs. Typically it is combined with capsicum frutescens
Lobelia is also used to lessen nicotine withdrawal, as it has a similar action to
nicotine.
Pleurisy, croup, whooping cough, also where deteriorating with declining
response to bronchodilators. Infantile cough.
Tight chest and hard sputum specific indications for its use.
Liver, bladder and stomach inflammations and obstructions

Topically; muscle inflammation, as a plaster in acute bronchitis, pleurisy,

intercostal myalgia. Lotion for arthritic joints, rheumatic disease, sprains and
contusions.

Toxicology
Ingestion of toxic levels; vomiting, thereby lessening the likelihood of a fatal
outcome.
symptoms: nausea, salivation, diarrhea, disturbed hearing and vision, mental
confusion, marked weakness.
Faintness and prostration; blood pressure falls; the pulse becomes weak, rapid, and
irregular; breathing is difficult; and collapse occurs followed by convulsions. Death
may result from respiratory failure.
The antidote in acute poisoning is 2 mg of atropine, which is given
subcutaneously.

Dosage
Weekly 1:8 32ml

Ephedra sinica
Traditional use
in China since 2800 BC, used primarily in the treatment of the common cold, asthma,
hay fever, bronchitis, edema, arthritis, fever, hypotension, and urticaria. Western
medicine’s interest in ephedra began in 1923 with the demonstration that the isolated
alkaloid ephedrine.

Constituents; 2.5-3% alkaloids

– L-ephedrine (0.75%-1%)
– norephedrine
– pseudoephedrine
– norpseudoephedrine

Pharmacology
Ephedrine and epinephrine; The CNS effects similar to amphetamine (less potent)
Ephedrine; sympathomimetic or CNS stimulant, stimulator of adrenergic receptors
(both alpha- and beta-adrenergic) as well as stimulate the release of nor-epinephrine.
Effects; vasoconstriction, raised blood pressure (both diastolic and systolic),
increases cardiac output, and heart rate bronchodilation.
Also contains two hypotensive principles (ephedradine A and B), along with a
hypertensive compound (1-tyrosine betaine or maokine).
Increase coronary, cerebral, and muscle blood flow at the expense of renal and
splanchnic blood flow. Stimulation of alpha adrenergic receptors on smooth muscle
increase resistance to urine flow (diuresis)
Extracts of ephedra; in vitro, inhibit cyclic AMP activity.
Pseudoephedrine; bronchodilating activity similar to ephedrine, but has weaker
pressor, cardiac, and central nervous system effects.
pseudoephedrine and other ephedra alkaloids; anti-inflammatory effects, due to inhibition
of prostaglandin E 2 synthesis.

Ephedrine is used as nasal decongestants, bronchodilators, anaphylactic shock. Ephedrine

and pseudoephedrine; over-the-counter medications for asthma, hay fever, and rhinitis.
Pseudoephedrine is often recommended over ephedrine in the treatment of chronic
asthma as it has fewer side-effects. Natural ephedrine is better tolerated, causes fewer
heart symptoms such as palpitations.

Pharmacokinetics
The major route of elimination of ephedrine is as the unchanged drug in the urine.
Alkalinization will increase the half-life.
Half life 5.2 hours, max concentration 3.9 hours.
The peak bronchodilation effect occurs in 1 hour and lasts about 5 hours after
administration.
Effect will diminish if used over a long period of time due to the weakening of the
adrenal gland. Need to use ephedra in combination with other herbs, such as Glycyrrhiza
glabra and Panax ginseng; and nutrients.

Actions
Antiallergic, decongestant, central nervous system stimulant, sympathomimetic,
diaphoretic, diuretic.

Indications;
- Asthma, hayfever, urticaria, and other allergic conditions, enuresis,
bronchospasm, bronchitis, whooping cough (Rapidity of action; makes it
effective), dyspnoea of emphysema relieved by bronchodilation
- myasthenia gravis; as an adrenergic receptor agonist
- Narcolepsy; stimulant action on brain and SNS
- low blood pressure, circulatory insufficiency, minimal hypertensive effects
- United states; weight loss, boosting athletes performance

Weight loss aid

Human and animal studies, ephedrine has been shown to promote weight loss.
Anorexic effect, plus increasing the metabolic rate of adipose tissue.
Weight-reducing effects are most significant in those individuals with a low basal
metabolic rate, enhanced when used with methylxanthines caffeine and theophylline, as
well as aspirin (potentiates the action of ephedrine and other ephedra compounds).
In one animal study, when ephedrine was used alone, it resulted in a 14% decrease in
body weight and a 42% decrease in body fat, in combination with caffeine or
theophylline, the decreases were 25 and 75%, respectively. However, when either
caffeine or theophylline were used alone, there was no significant loss in body weight.
The reason for the greater decrease in body weight is the increased metabolic rate and fat
cell breakdown promoted by ephedrine and enhanced by caffeine and theophylline.

Adverse reactions
Insomnia, restlessness, irritability, headache
Nausea, vomiting
Disturbance in urination, urinary disorders urinary retention
Hypertension,cardiac arrhythmia, tachycardia
Anxiety. dizziness, tremors.
Ephedrine associated with dependency

Rare but serious;

Seizures
Psychiatric disturbances, toxic psychosis
Hepatotoxicity
Stroke
Myocardial infarction.deaths have been attributed to use of ephedrine

Case reports
The FDA received approximately 800 medical and psychiatric complications directly
linked to Ephedra (Ma-huang) and 34 notices of deaths between 1993 and 1997.
Marketed i.e. for weight loss, for increased energy, heightened sexual sensations and as
‘herbal highs’; exceeding the recommended dosage common.
- A 35-year-old woman was diagnosed with acute myocardial infarction, secondary to
cardiac spasm, after taking an ephedrine-containing supplement for weight loss, taken the
supplement for 30 days at the recommended dosage and had stopped for 1 week while on
vacation. The attack occurred 1-2 days after recommencing the supplement. Since
discontinuing the product she has had no further cardiac-related symptoms.
- Three weeks daily use of a dietary supplement containing ephedrine a 44-year- old
man, with no known cardiovascular risk factors, died from acute coronary artery
thrombosis.
- Seizures were experienced by a 38-year-old woman after she took 4 tablets of an
ephedrine-containing dietary supplement. She had no history of seizures and
was taking no other medication other than the contraceptive pill. At one stage she was
hospitalized and treated with antiseizure medication. It is unclear whether or not this
medication was continued. She experienced no seizures after discontinuing the dietary
supplement.
- A 39-year-old male who was taking pravastatin for hypercholesterolemia and
furosemide for hypertension developed hypersensitivity myocarditis after taking Ma-
huang for 3 months, along with other vitamin supplements. He received medical
treatment and 2 months later at a follow-up examination had no signs of myocarditis.
- A 34-year-old man suffering from psychosis after taking Ephedra (dose not stated)
over the previous 10 days. He had no history of mental illness and his symptoms
resolved quickly once he stopped taking Ephedra. No treatment was given and follow-
up confirmed that he remained free of symptoms. (BMJ 1996)
- A US Marine sergeant (27-year-old male) threatening suicide following. 3-month
history of depression, feeling overwhelmed, poor concentration, “thinking too many
thoughts at once”, irritability, guilt and suicidal thoughts. experienced episodes of
“euphoria” lasting for up to 3 days. Taking Ephedra regularly over the last 2 years to help
with workout performance. On giving up the herb his moods returned to normal and he
resumed full duty without further psychiatric intervention.

Pregnancy and lactation

- Avoid, although no increase in frequency of malformation or other harmful
effects noted on the foetus from limited use in women.
- Animal studies; Ephedrine administered to chick embryos and rats, rabbits has resulted
in cardiovascular teratogenicity and embryotoxicity (relevance to humans unknown).
- The teratogenic effect of ephedrine is potentiated by caffeine.
Not to be used in pregnancy and lactation without professional advice (not
reiterated in TCM or Commision E)

Safety in children
Only to be used in children older then 6 years.

Contraindications
Anxiety
Hypertension
Glaucoma
Impaired cerebral circulation
Heart disease, angina
Benign prostatic hyperplasia associated with urine retention
Hyperthyroidism
Pregnancy
Stop using one week before surgery.
Phaeochromocytoma
Thyrotoxicosis
Monoamine Oxidase Inhibitor drugs
WHO also adds coronary thrombosis, heart disease, diabetes

Interactions
cardiac glycosides
halothane
guanethidine
ergot alkaloid derivatives
oxytocin
CNS stimulants
sympathomimetic drugs
Antihypertensive drugs
alpha and beta adrenergic agonist
SSRIs
MAOIs (can lead to severe, possibly fatal hypertension).

Urine testing
Ephedrine in cold remedies; exceeded olympic committee cut off, resulting in
positive drug test to amphetamines.

Dosage
Initial weekly dose 10 ml of 1:4
Maximum dosage 48ml of 1:4, 60 ml of 1:5
maximum single dose 600mg
maximum daily dose 1800mg
Not to be taken long term; tolerance and dependency associated with ephedrine use

Gelsemium sempervirens (yellow jasmine)

History
In the 19th C a Mississippi planter, for whom the root was gathered in mistake for that of
another plant. After partaking of an infusion, serious symptoms arose, but when, contrary
to expectations, he recovered, it was clear that the attack of bilious fever from which he
had been suffering had disappeared. This accidental error led to the preparation from the
plant of a proprietary nostrum called the 'Electric Febrifuge.'
In America; used as an arterial sedative and febrifuge in various fevers, more
especially those of an intermittent character, but later, recommended in the treatment
of spasmodic disorders, such as asthma and whooping cough, spasmodic croup and
other conditions depending upon localized muscular spasm, convulsions.
Later mainly used in the treatment of neuralgic pains, especially those involving the
facial nerves, particularly when arising from decaying teeth.
It is said it will suspend and hold in check muscular irritability and nervous excitement
with more force and power than any known remedy. While it relaxes all the muscles, it
relieves, by its action on the general system, all sense of pain. The herb is also said to be
most useful in the headache and sleeplessness of the drunkard and in sick headache.
It was used in dysmenorrhoea, hysteria, chorea and epilepsy, and the tincture found to
be efficacious in cases of retention of urine.
Some recommend its use in acute rheumatism and pleurisy, in pneumonia and in
bronchitis, it has been advocated in the early stages of typhoid fever.

Constituents
Alkaloids (gelsimine, gelseminine, gelsemoidin)

Actions
Anodyne, antispasmodic, sedative, febrifuge, diaphoretic.
Relaxing smooth muscle and slowing respiration.
Reduces sympathetic and parasympathetic irritability, depressing excessive
reactivity in the vascular system.

Indications
- Nerve pains,trigeminal neuralgia, migraine, toothache, where a strong
sedative is needed
- functional heart complaints, used as cardiac sedative for extrasystoles and
functional heart disease
- powerful spinal depressant; its most marked action being on the anterior cornus
of grey matter in the spinal cord.
- found to be helpful in labour, and aiding dilation of the cervix.

Toxicity
Small doses may cause respiration depression, giddiness, double vision, convulsions.
Has been known to be fatal. Effects may be delayed for several hours. Sensation of
languor, relaxation and muscular weakness, followed by paralysis if the dose is
sufficiently large. The face becomes anxious, the temperature subnormal, the skin cold
and clammy and the pulse rapid and feeble. Dropping of the upper eyelid and lower jaw,
internal squint, double vision and dilatation of the pupil are prominent symptoms. The
respiration becomes slow and feeble, shallow and irregular, and death occurs from
centric respiratory failure, the heart stopping almost simultaneously. Consciousness is
usually preserved until late in the poisoning, but may be lost soon after the ingestion of a
fatal dose. The effects usually begin in half an hour, but sometimes almost immediately.
Death has occurred at periods varying from 1 to 7 1/2 hours.
Kills by its action on the respiratory centre of the medulla oblongata. Shortly after the
administration of even a moderate dose, the respiration is slowed and is ultimately
arrested, this being the cause of death.
Treatment; emetics, stomach lavage, strong tea without milk, rest and warmth.
Respiration may need to be assisted, aided by the early administration,
subcutaneously, of ammonia, strychnine, atropine or digitalis.

Dosage
Maximum of the dried root 25mg TDS, equivalent to 0.25ml of 1:10 Weekly
dose of 1:10 maximum 5ml per week, start with 1 ml per week.

Cardiac glycosides
Steroidal glycosides; similar but different than the steroidal saponins Cardiac
glycosides are composed of two structural features : the sugar (glycoside) and
the non-sugar (aglycone - steroid) moieties.

The R group at the 17-position defines the class of cardiac glycoside.

Sugar moiety : One to 4 sugars are found to be present in most cardiac glycosides. The
sugar moiety confers on the glycoside solubility properties in its absorption and
distribution in the body.

The presence of OH groups increases the onset of action and subsequent

dissipation from the body.

Two types;
1. steroidal aglycone with 23 carbons (the cardenolide glycosides)
2. steroidal aglycone with 24 carbons (the bufadienolide glycosides)

The cardiac glycosides occur mainly in plants from Liliaceae, Scrophulariaceae,

Apocynaceae.
Plants containing cardiac steroids have been used as poisons and heart drugs at least
since 1500 B.C. Throughout history these plants have been used as arrow poisons,
emetics, diuretics, and heart tonics.

Convallaria majalis
- Majalis, or Maialis; 'that which belongs to May,' and the old astrological books place
the plant under the dominion of Mercury, since Maia, the daughter of Atlas, was the
mother of Mercury or Hermes.
- Old Sussex legend that St. Leonard fought against a great dragon in the woods near
Horsham, only vanquishing it after a mortal combat lasting many hours, during which he
received grievous wounds. But wherever his blood fell, Lilies-of- theValley sprang up to
commemorate the desperate fight, and these woods, which bear the name of St.
Leonard's Forest to this day, are still thickly carpeted with them (Modern Herbal
Grieve).
- Legend says that the fragrance of the Lily of-the-Valley draws the nightingale from
hedge and bush, and leads him to choose his mate in the recesses of the glade.
- Its use dates back to ancient times, for Apuleius in his Herbal written in the fourth
century.
- Special virtues were once thought to be possessed by water distilled from the flowers,
which was known as Aqua aurea (Golden Water), and was deemed worthy to be
preserved in vessels of gold and silver. Coles (1657) gives directions for its preparation:
'Take the flowers and steep them in New Wine for the space of a month; which being
finished, take them out again and distil the wine three times over in a Limbeck. The wine
is more precious than gold, for if any one that is troubled with apoplexy drink thereof
with six grains of Pepper and a little Lavender water they shall not need to fear it that
moneth.'
Dodoens (1560) pointed out how this water 'doth strengthen the Memorie and
comforteth the Harte. '
Gerard; 'a Glasse being filled with the flowers of May Lilies and set in an Ant Hill with
the mouth close stopped for a month's space and then taken out, ye shall find a liquor in
the glasse which being outwardly applied helps the gout very much.'
- This spirit was also considered excellent as an embrocation for sprains, as well as for
rheumatism.
- old writers; decoction of the bruised root, boiled in wine, is good for pestilential
fevers, and that bread made of barley meal mixed with the juice is an excellent cure for
dropsy, also that an ointment of the root and lard is good for ulcers and heals burns and
scalds without leaving a scar.
- Culpepper said of the Lily-of-the-Valley: 'It without doubt strengthens the brain
and renovates a weak memory. The distilled water dropped into the eyes helps
inflammations thereof. The spirit of the flowers, distilled in wine, restoreth lost speech,
helps the palsy, and is exceedingly good in the apoplexy, comforteth the heart and vital
spirits.'
-The powdered flowers have been said to excite sneezing, proving serviceable in the
relief of headache and earache; but to some sick people the scent of the flowers has
proved harmful.
- It proved most useful in cases of poisonous gassing of the men at the Front.
- Russian peasants have long employed the Lily-of-the-Valley for certain forms of
dropsy proceeding from a faulty heart.

The action of the drug closely resembles that of Digitalis, though it is less powerful; it is
used as a substitute and strongly recommended in valvular heart disease, also in cases of
cardiac debility and dropsy. It slows the disturbed action of a weak, irritable heart, whilst
at the same time increasing its power.

Cardiac glycosides; convallatoxin, convalloside, convallotaxol, convallotoxoloside,

convallarin all progressesively converted to convallatoxin in a domino effect by
hydrolysis of terminal glycoside.
Convallatoxin; poorly absorbed, but other constituents aid absorption. Only 60 % of the
glycosides are active the rest potentiate availability, slow release effect, the delayed
effect extends its availablity, sustained effect 2-3 times longer.
Other constituents including flavonoids, play a major role in achieving solubity, they are
precursors of degradations products of the glycosides, and if present the mixture is 50%
more soluble than pure convallatoxin.
Saponin; convallarin - diuretic

Cardiacglycosides
1. Inhibit the sodium-potassium cellular pump leading to a rise in intracellular calcium
levels which increases the contractile force and speed of the heart muscle (positive
inotrophy). So increases the force and speed of systolic contraction. This lead to increase
cardiac output in the failing heart, cause more completely emptying of ventricles and
shortening the length of systole. The heart has more time to rest between contraction, the
increased cardiac output causes a lower heart rate and increase renal excretion

2. Heart rate decreased (negative chronotropy) via the autonomic nervous system,
conduction velocity at the atrioventricular node is slowed, action on atrial ventricular
node with secondary effect on the sinus ventricular node. Although according to Weiss;
by mouth it acts practically only on the heart muscle and not on conduction, not having
the vagus effects of digitalis
- slows down a rapid feeble pulse, more efficient and better coordinated
heartbeat.
- used in subventricular rhythm abnormalities such as atrial fibrilation.

3. Coronary and peripheral vasodilation; lowers BP and improves coronary

circulation.
Myocardial efficiency and stroke volume improved without putting extra demands on
coronary supply.

Indications
- Heart failure with oedema. Congestive heart failure with oedema, associated with
slow pulse rate. Left ventricular failure with mitral insufficiency.
- endocarditis, pericarditis
- Cardiac asthma (dyspnoea when due to heart problem), coronary insufficiency and
angina including the painful episodes.
- Arrythmia.
- When heart under strain from thyrotoxicosis, atherosclerosis, infectious disease and
nephritis.
- Weiss; used particularly for bradycardiac forms of heartfailure, but also tachycardia. By
mouth it acts practically only on the heart muscle and not on conduction, not having the
vagus effects of digitalis. This makes it suitable on the bradycardiac forms of heart
failure. Bradycardia is particulary common in senile hearts, when the heart is weakening,
but performing reasonable well at rest and not overstressed.
Effect Onset of action is rapid, and so is elimination, so no accumulation.
In combination with Crataegus spp. , enhances the availability of the cardiac
glycosides.
Precautions and CI
Avoid in ventricular tachycardia, watch out for hypokalaemia.

(Ventricular tachycardia originates in one of the ventricles of the heart. This is

a potentially life-threatening arrhythmia because it may lead to ventricular
fibrillation, asystole, and sudden death.
The diagnosis of ventricular tachycardia with ECG. It may be very difficult to
differentiate between ventricular tachycardia and supraventricular tachycardia
Various diagnostic criteria have been developed to determine whether a wide
complex tachycardia is ventricular tachycardia or a more benign rhythm, if the
individual has a past history of a myocardial infarction, congestive heart
failure, or recent angina, the wide complex tachycardia is much more likely to
be ventricular tachycardia.
Hypokalaemia; concentration of potassium (K+) in the blood is low.
Normal plasma potassium levels are between 3.5 to 5.0 mEq/L
Mild hypokalemia is often without symptoms, although it may cause a small
elevation of blood pressure, and can occasionally provoke cardiac arrhythmias.
Moderate; may cause muscular weakness, myalgia, and muscle cramps
(owing to disturbed function of the skeletal muscles), and constipation (from
disturbed function of smooth muscles).
Severe hypokalemia, flaccid paralysis and hyporeflexia may result. There
are reports of rhabdomyolysis occurring with profound hypokalemia with
serum potassium levels less than 2 mEq/L. Respiratory depression from
severe impairment of skeletal muscle function is found in many patients.
Inadequate potassium intake (rare), loss due to diarrhea, excessive
perspiration, or losses associated with surgical procedures, Vomiting although
not much potassium is lost from the vomitus, there are heavy urinary losses of
K+ in the setting of post-emetic bicarbonaturia that force urinary potassium
excretion Other GI causes include pancreatic fistulae and the presence of
adenoma.
Urinary loss; Diuretics,) are a common cause of hypokalemia. Other
medications such as the antifungal, amphotericin B, or the cancer drug,
cisplatin, can also cause long-term hypokalemia.
diabetic ketoacidosis.)

Toxicology
The compounds have low therapeutic index, so the therapeutic dose is not much lower
than the toxic dose.
Nausea, vomiting, diarrhoea, intestinal colic, vision disturbances, neurological
symptoms such as headache, neuralgia, drowsiness
cardiovascular symptoms such as worsening cardiac failure, arrhythmia.
Disturbance electrolytes, might need to give potassium.
If vomiting does not occur, and emetic should be given, keep patient warm and get
professional help.

Dosage
• Dried herb; 150mg TDS
• equivalent to 1.2ml of 1:8
• weekly of 1:8 24ml
• weekly of 1:5 15ml

Colchicum autumnale (meadow saffron)

Constituents; alkaloid colchicine
- inhibits phagocytosis of the crystals by leukocytes, thus breaking the viscous circle
of the inflammatory process.
- Does not reduce uric acid.
If not respond unlikely to be gout
Optimum effect according to Weiss when nausea, vomiting, diarrhoea also occur, though
rapidly disappear once drug discontinued.

Indications
Joint inflammation, pain in gout for acute episodes less
effect on chronic gout.

Contraindications
Senile, weak patients, heart or kidney disease.

Toxicity
Burning in the mouth, throat. Vertigo, head pain, nausea, vomiting, abdominal pain,
diarrhoea, neurological signs.
Treatment; emetic, lavage, saline purgative, sodium sulphate 30g to 250ml water,
barley water, rice or oatmeal water.
Keep recumbent and warm, get trained help.

Dosage
• Dried herb 100mg TDS
• 1 ml of 1:10 , maximum 3 ml per day in divided doses
• give 10-15 gtt of tincture, every hour, as early as possible in the attack until there
is a definite effect, then usually after 2-3 days when attack lessens, reduce dosage
and stop.
• symptoms and pain should subside in 48 hours.
Arnica montana (external use only)
Traditional use
- popular, internally and externally
Historically; Gargling with tea, or for sore throats, pharyngitis, esp when chronic and
due to poor circulation in the area.
Externally in the form of compresses with highly diluted tincture, one table spoon in litre
of water. Bruises, but also badly healing wounds, leg ulcers where arnica ointment
would be used.
Goethe(1749-1832) would ask for arnica tea, when in his old age he experienced anginal
pain due to coronary arteriosclerosis.

Constituents
• Sesquiterpene lactones of the pseudoguaianolide type, such as helenalin and their
esters
• flavonoids
• essential oils
• pyrrolizidine alkaloids (have saturated necine bases, which indicates that they are non
toxic). (Two 5 membered rings with a nitrogen in position 4, a structure called necine
bases)

Action
Anti-inflammatory;
- Possibly due to uncoupling of oxidative phosphorylation in polymorphophonuclear
neutrophils. The mode of action of sesquiterpene lactones as anti-
inflammatory agents appeared to be at multiple sites; for example, at 5 X 10(-
4) M, the sesquiterpene lactones effectively uncoupled the oxidative
phosphorylation of human polymorphonuclear neutrophils and elevated the
cyclic adenosine monophosphate levels of rat neutrophils and rat and mouse
liver cells.
- Free and total lysosomal enzymatic activity was inhibited by these agents at
5 X 10(-4) M in both rat and mouse liver and rat and human neutrophils.
- Furthermore, the structure-activity relationships for the stabilization of
lysosomal membrane for rat liver cathepsin activity followed the same
structural requirement necessary for anti-inflammatory activity; i.e., the
alpha- methylene-gamma-lactone moiety contributed the most activity,
whereas the beta-unsubstituted cyclopentenone and alpha-
epoxycyclopentanone contributed only minor activity.
- Human polymorphonuclear neutrophil chemotaxis was inhibited at low
concentrations (i.e., 5 X 10(-5) and 5 X10(-6) M), whereas prostaglandin
synthetase activity was inhibited at a higher concentration (i.e., 10(-3) M)
by the sesquiterpene lactones.
- Elevation of cAMP in neutrophils and liver cells
- Inhibition of lysosomal enzymatic activity in neutrophils and liver cells.
- Anti-ecchymotic (against bruising)
- analgesic
- antimicrobial

Clinical trials
RCT;
Topical application improves venous tone, oedema and the feeling of heaviness in the
legs of patients with chronic venous insufficiency (20% arnica tincture).
More effective than placebo for muscle ache.
Indications; externally
Bruises, sprains, swellings, unbroken chilblains, haematomas, inflammations,
dislocations, oedema associated with fracture, haemorrhoids, rheumatic, muscle and
joint complaints, inflamed insect bites, surface phlebitis, symptoms of varicose veins.
Externally for alopecia neurotica and in hair preparations to prevent dandruff and to
stimulated circulation to the scalp.
Poultice; 2-3 g of arnica covered with 150ml hot water, strain after 10 minutes.
Bandages, gauze, cotton soaked in infusion then placed on affected area.
Arnica oil; macerate one part flowers in five part of oil.
Arnica tincture used as topically as lotion or incorporated in creams (10-25% in
cream), apply TDS.

Contraindications
- Not to be taken internally
- do not apply to broken skin, or near eyes or mouth.
- Withdraw on first sign of dermatitis
- CI when allergy to arnica
- in lactation do not use near the nipple

Adverse reactions
Allergic, irritant contact dermatitis
Cross reactions with other Compositae, and Lauracea spp (sesquiterpene
lactones)
Review 1992 contact allergy reported in 11-75% of patients in dermatology clinics??????,
however the number of studies published since only up to 1.14%.

Not for prolonged external application

Prolonged treatment can cause oedematous dermatitis with the formation of
pustules.
Higher concentrations; formation of vesicles or even necrosis

Dosage; external only

• Not to be taken internally
• 1:5 tincture diluted 5 times with water and applied topically 2-3 times per day.
• Ointment containing 10-25% or tincture
Aconitum spp (monkshood)
Constituents; alkaloids (acotine)

Traditional uses; external only

Used topically only
Rheumatism, joint pain, sciatica, lumbago, pleurodynia, bruises and stiffness after
injury.
Neuralgia (trigeminal and intercostal
Dilate the coronary, cerebral, peripheral arteries, and improve capillary
circulation.
Causes paraesthesia and numbness of the skin.

- Do not apply to broken or abraded skin

- withdraw immediately if skin reaction
- absorption can cause toxic effect in some
- must be stored where impossible for children to reach

Toxicity
Contain potent cardioactive constituents, the aconitine alkaloids, toxic in low doses.
Onset symptoms of poisoning within 30 minutes of ingestion.
Symptoms; tingling of tongue, mouth and skin numbness follows, paraesthesia, muscle
weakness, metabolic and or respiratory acidosis, pulse weak, and slow then rapid with
clammy skin, dyspnoea, and vertigo, hypotension, palpitations, tachyarrhythmia,
reduced consciousness.
No antidote, emetic immediately, stomach lavage, lie flat head low, maintain body
heat, treatment is symptomatic and supportive.
Artificial respiration may be required, trained help immediately.

Toxicity has been reported when liniments have been ingested in error because of poor
labelling or instructions.

Dosage
External only 1:10 1.3%

Other schedule III for external use only

• Aspidosperma quebracho-blanco
• conium maculatum
• pilocarpus microphyllus
• rhus toxicodendron
• senecio jacobaea