Herb, Food, or Drug?

Botanically

Herb is a non-woody seed-producing plant

which die at the end of the growing season

Culinary-Wise

Vegetable products which add flavor or aroma

to food
Medicinally
Crude drugs of vegetable origin used to:
1- Treat disease states, often of chronic nature, or
2- To attain/maintain condition of improved heath

Phytomedicinals
Pharmaceutical preparations made by
extracting herbs with various solvents to yield
tinctures, extracts or fluidextracts
Popularity of Herbals

32% of kids (birth to 18 years-old)

79% of college students

47% of men >20 years old

57% of women >20 years old

65%-83% of older adults

55% of older adults use 3+ supplements

12% of older adults use 5+ supplements

$25.2 billion: herbals/natural products in 2008

Use of Ginko with coumadin can increase risk of bleeding
Impact on drug therapy & health

52%-83% of older people use Rx medications &

dietary supplements concomitantly

69% of users of Rx drugs & dietary supplements

together do not discuss these combinations with
their medical practitioner

Pharmacists regularly receive questions from

patients & care practitioners
Natural doesn’t necessarily mean safe

Strychnine, ricin, aconitine, digoxin: natural

poisons

Humans survived by accepting that the fact that

environment offers
harmful & healing compounds
Herbs versus Other Drugs
1- Dilution
Herbs: more dilute than purified therapeutic
agents, e.g.,

200 mg of caffeine (1 or 2 tablets) equivalent to

20 g coffee powder (1-2% natural occurrence) or

10 g tea (2-4%)
2- Herbs often contain additional active
principles

which may be chemically & pharmacologically

closely related to the primary constituent

Digitalis contains ~30 cardiac glycosides with a

wide array of activity, duration & onset of actions
Digitoxin: onset of action 1-4 hours/peak activity
8-14 hours

Digoxin: onset of action of 0.5-2 hours/2-6 hours

duration of activity

The effectiveness of Digitalis is attributed to its

constituents multiplicity which provide
uniform effectiveness with short onset & long
duration
3- Some herbs contain other principles that
detract the specific therapeutic utility, e.g.,

Cinchona bark: contains ~25 quinoline alkaloids

Of these, only quinine recognized effective against

malaria

If we used this herb to treat malaria,

patient will also take a notable amount of
quinidine, the related cardiac depressant alkaloid
&
cinchotannic acid which induces constipation
Standardized Remedies
To assure herbal quality, there should be an
efficient mean to isolate, quantify & assay active
constituent(s) or a marker compound, if known

If the active ingredient is a complex mixture or

unknown, or if no marker compound is available,

biological assays must be utilized such as that

employed to determine Digitalis potency (cardiac
arrest of Pigeon's heart)
Once the potency of the herb is established,
it can be mixed with appropriate quantities of other
material of greater or lesser potency to optimize
activity

Standardized extracts of ginkgo, ginseng, milk

thistle, St. John wort & many others now available
Natural medicine versus pharmacy practice
Increase the potential for: > adverse effects
> interactions with prescription drugs
delayed / ineffective treatment > other problems

Steeped Standard- Single

Raw Plant ized chemical
Tea Extract entity

Pure
concentrated
Mixture-many chemicals
chemicals
Strong drug action
Mild drug action
Strong adverse
Mild side effects
effects
Raw Plant Material

Pure Active
Ingredients

Standardized Generics
Clin. Active 1 2 3
Quality Assurance

Products usually misbranded & ingredients’

therapeutic quantities not indicated especially in
mixture-containing products
e.g.,

Adequate amount of tannins in an herb explains its

astringent effect on wounds

Consumer: buy a standardized product/specified

amount & marketed by a reputable firm
Accurately labeled products containing:

botanical scientific name

manufacturer name/address

batch number, manufacture/expiration dates

a phone number for inquires

indicate good quality assurance

Herbals Use & Guidelines

Know which cases could be self treated, e.g.,

occasional headache pain, strained muscle, mild
digestive upset, simple diarrhea, infrequent
insomnia, common cold

Cases need professional medical care:

rheumatoid arthritis, diabetes, cardiac arrythmia,
hypertension, or cancer

Herbals not recommended during pregnancy, can

cross placenta/expose fetus to teratogenic hazards
Drug excretion in mother’s milk/lactating women
Infant's enzyme systems: metabolism not well
developed

Children’s body/organ functions:

continuous state of development

Changes in relative body composition

(lipid content, protein binding, body water
compartments) produce a different distribution
pattern versus adult
Elderly should use herbal remedies with caution

Aging decreases:
renal function, hepatic microsomal
enzyme activity, total body water & mass

Drug can accumulate to a toxic level

Careful dosing/adverse reactions monitoring

multiple/serious diseases require prescription

medications

Drug-herb interactions could be a major concern

herbals should be included in patient drug history
 Paraherbalism
Faulty/inferior herbalism based on pseudoscience

Difficult to differentiate from true/rational

herbalism
advocates use of scientific or medical terminology

Paraherbalism characters:
1- Lack of scientific logic

2- Medical claims without scientific evidence

3- Clinical trials supporting use have been flawed

Homeopathy
Destructive form of paraherbalism
late 17th by the German Samuel Hahnemann

The law of similar: first tenet of homeopathy,

assumes that

illness symptoms: not direct manifestation of

disease but an outward reflections of a body
imbalance
treatment should reinforce these symptoms!!
medication should produce similar symptoms in
healthy people!!

Hence the name is derived from the Greek,

“homoios”= similar & “pathos”= suffering

“Like cures like Any substance which can

produce a totality of symptoms in a healthy
human being can cure that totality of
symptoms in a sick human being” Samuel Hahnemann
Homeopathy: Dilutions
Herbal Medicine Information Sources

Objective, accurate, honest, unbiased information

Many available information sources on herbs due

to revival of interest

Not all information sources are trustable

News, magazines, TV, online data bases, books

scientific/professional journals & German

Commission E monographs
Most trustful sources safety/ efficacy of herbal
remedies: controlled clinical trials, published in
scientific journals
correct honest/unbiased scientific methodology

One patients group administer investigated drug

versus other control group

Control group: placebo, other known effective drug

or a different dose of the tested drug

Patients: randomly assigned to either group to

eliminate bias selection
The German Commission E monographs:

one of best/valuable drug efficacy/safety

information resources

Experience gained during many years of empirical

use of phytotherapy

recognize its origin & should be taken in account

along with clinical trials, to evaluate effectiveness
Digestive System Problems
I- Nausea/Vomiting (motion sickness)

Preceded by discomfort & uneasiness

Controlled by brain emetic center

which stimulated by peripheral sites
from CTZ & brain’s cortex
Anti-emetic drugs act by inhibiting this stimulation
Antihistamines like dimenhydrinate prevent
peripheral stimuli from reaching emetic center but
cause adverse reactions like drowsiness

Anticholinergic drugs, e.g., scopolamine also

effective but cause dry mouth,
drowsiness, blurred vision &
tachycardia

effective anti-motion sickness without these side

effects is highly desired
Ginger
Rhizomes (underground stems) of Zingiber
officinale, Zingiberaceae

Medicinal Uses
I- Orally

1- Motion sickness

double blind study: 36 students with high tendency to

motion sickness: 940 mg ginger is superior to 100 mg
dimenhydrinate in reducing motion sickness/vertigo when
used 25 minutes before test in a tilted rotating chair
German Commission E:
2-4 g daily doses ginger is effective in preventing
motion sickness/digestive aid Also useful anti-
emetic in minor outpatient surgery procedures

Discrepancy in clinical trials results due to:

failure to use standardized preparations which

widely vary in chemical composition & may
contain adulterants

grown in various world areas: variable contents

to avoid such discrepancy,
Standardized ginger: containing standard amount
of shogaols & gingerols

Mechanism:

GI rather than CNS,

Ginger had no effect on inner ear nor oculomotor
system

reduces tachygastria (abnormal increase in pace

maker activity in gastric musculature)
enhance gastric emptying
2- Other digestive uses of ginger

Hyperemesis gravidum (a severe form of

pregnancy-related nausea & vomiting), peptic
ulcers, colic, dyspepsia, flatulence, loss of appetite,
anorexia & high blood cholesterol & sugar levels

3- Disequilibrium/ nausea associated with

discontinuation or tapering of selective
serotonin reuptake inhibitors (SSRIs)

3- Rheumatoid arthritis

4- U Respiratory tract infections, cough/bronchitis

Safety
Likely safe in food amount

GRAS (Generally recognized as a safe herb) in US

Maximum permissible level in food is 0.0023%

Topically: oil is well tolerated & unlikely to cause

phototoxicity

Likely safe in pregnancy in normal food level

but unsafe in larger amounts
Large dose: CNS depression/cardiac arrhythmias
Adverse Reactions
Allergic dermatitis in sensitive individuals

Ginger-Herb Interactions
Concomitant use with herbs that have coumarins
(anticoagulant) or affect platelet aggregation could
increase bleeding risk

Examples of these herbs:

Turmeric, capsicum, fenugreek, chamomile,

clove, garlic, onion, feverfew, ginkgo, ginseng,
celery
Drug Interactions
1- Interferes/antacids: sucralfate, H2-antagonists &
proton pump inhibitors
2- SSRIs/ sertraline (Zoloft):
(+)-interaction treating disequilibrium/nausea from
SSRIs discontinuation

3- Cyclophosphamide: (+)-interaction
Preventing its induced vomiting

5- Anticoagulants/ anti-platelet aggregation drugs,

increase bleeding risk
Contraindications
1- Gallstones
2- Bleeding Conditions: inhibit thromboxane synthetase/
enhance prostacyclin, produce prolonged bleeding time &
some immunological changes, used with caution for
postoperative nausea

Dosage Forms
Hard gelatin capsules: 500 mg powdered rhizome for
motion sickness taken 30 minutes before departure
Dried or fresh rhizomes: orally 0.25-1 g or as an infusion
tea three times daily: Tea prepared by steeping 0.5-1 g in
150 ml boiling H2O for 5-10 minutes
Maximum daily ginger dose is 4 g
2- Constipation

Decrease in frequency of fecal elimination/

difficulty in passing stools
~70 million / year more common in women

Laxatives should be of 2nd priority after fiber-rich

diet, adequate fluid intake/ regular physical activity

contraindicated in cases of cramps, nausea,

vomiting, bloating & undiagnosed abdominal pain
A- Bulk-Producing Laxatives
Used with enough liquid, bind water in colon,
softening & expanding fecal bulk,
enhancing peristalsis & bowel emptying

Safest laxatives/ act like high-residue/ fiber diet

Fruits & vegetables: more water soluble fiber,

Moist/soften stool, less effect on intestinal transit time
Grains, cereals & bran: insoluble poorly digested fiber
which shorten intestinal transit time & increase stool bulk
Psyllium
Clean, dry ripe seeds of Plantago psyllium
Medicinal Uses
1- Mucilage (Polysaccharide)
Neither absorbed nor digested in GIT

Swells with water contact: bulk/ lubrication &

inducing effective laxative, clinically proven

Used for irritable bowel syndrome, hemorrhoids,

anal fissures & pregnancy constipation
2- Hypocholesterolemia
Psyllium alone or mixed with water soluble dietary fibers
induce significant reduction of blood cholesterol & LDL-
cholesterol by binding & increase fecal excretion of
cholesterol & bile acids
Bile acids replaced in liver by using more serum
cholesterol for bile acid synthesis: less available cholesterol
for incorporation with blood lipoproteins

3- Cancer colon chemoprevention

Dietary fibers (in wheat bran/psyllium) bind carcinogens

& tumor promoters in colon, preventing carcinogenesis
4- Reducing peak blood glucose level by slowing
carbohydrate absorption

Safety
Likely safe orally with adequate fluid intake
Unsafe/ cause esophageal obstruction
if taken without adequate fluid intake

Crushing, chewing or grinding of non-commercial seed

preparations can release a toxic pigment that can cause
nephrotoxicity This pigment removed from commercial
forms
Interactions
Vitamin/Mineral Supplements:
Long term use of psyllium with vitamin/minerals can
reduce absorption of Ca, Fe, Zn & vitamin B12

Supplements must be administered 1 hr before or 4 hr

after psyllium to avoid this interaction

Psyllium-Drug Interaction
- Concomitant use with carbamazepine (tegretol), warfarin
(coumadin) & digoxin can reduce absorption & require
dose adjustment
- Insulin/diabetes therapy: induce hypoglycemia, careful
blood glucose monitoring is required

Dosage Forms
Start with small amounts/gradually increase to desired
response

Orally: 10-30 g /day, in divided amounts

Mix 10 g with 100 ml water to be followed by another

200 ml

Avoid chewing or crushing

At least 150 ml water for each 5 g seed required
B- Stimulant Laxatives
Some medicinal herbs contain anthraquinones, anthrones,
dianthrones, Which stimulate peristalsis by irritating
intestinal mucosa’s intraneural nerve plexus activity,
increasing motility
Act on colonic mucosal cells, opening Cl- channels,
stimulate active Cl- secretion, reduce liquid & electrolyte
absorption in the colon & increase their level in/pressure
on colonic lumen: laxative action
Anthranoid glycosides: prodrugs pass unchanged to colon
where they hydrolyzed by microbial flora enzymes to free
anthranoid aglycone/ sugar moiety, active anthrones:
Delayed-onset
Senna

Most common anthraquinone-containing stimulant

laxative

Dried leaflets of Cassia acutifolia, known as

Alexandria Senna, Fabaceae

Medicinal Uses
Laxative for constipation & hemorrhoids,
anorectal surgery, fissures, evacuating GIT before
diagnostic tests & in slimming & cleansing teas
Safety
Likely safe: When used orally for short-term
Possibly Unsafe: When used longer than 1-2 weeks can
lead to dependence
Children: Possibly safe, standardized form
Pregnancy: Possible unsafe
Lactation: Possibly unsafe, excreted in milk & may cause
diarrhea

Interactions with Herbs

- Licorice or Horsetail Increase risk of K+ depletion
-Digitalis, squill, other cardenolide-containing herbs:
cardiac toxicity due to K+ depletion
- Stimulant Laxative herbs:

Rhubarb, Jalap, Podophyllum, Gamboge, Colocynth, Aloe,

Castor Oil, Alder Buckthorn: Increase risk of K+ depletion

Adverse Reactions

Abdominal discomfort, colics & cramps

Long term use: k+ depletion, disturbed heart function,

decreased serum albumin level, neuropathy & rhino-
conjunctivitis
Chronic use can cause reversible pseudomelanosis coli,
laxative dependency
Interactions with Drugs
- Cardiac glycosides & Laxatives: K+ depletion
- Corticosteroids/K+-depleting diuretics hypokalemia
- Oral Drugs can reduce absorption of some oral drugs
due to reduced GI transits
Interfere with any urine diagnostic colorimetric tests due
to urine discoloration

Dosage Forms
15-30 mg/day calculated as sennoside B
0.5-2 g powdered leaf: infusion/maceration tea
 Senna Ginger Psylium
A B C

1- Which of A-C can interfere with digoxin/cardiac

glycosides/corticosteroids via increased K+-depletion?

2- Which of A-C can be best indicated for motion sickness?

3- Which of A-C can be used for nausea & disequilibrium

from discontinuation of SSRI sertraline (Zoloft)?
 Senna Ginger Psylium
A B C

4- Which of A-C can reduce blood cholesterol via increase

fecal excretion of cholesterol & bile acids?

5- Which of A-C can reduce Ca, Fe, Zn & vitamin B12

absorption upon long-term use?

6- Which of A-C act through enhancing gastric emptying

and reducing tachygastria and not through oculomotor or
inner ear effects?