11-PHD427-1

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Herb, Food, or Drug?

Botanically

Herb is a non-woody seed-producing plantwhich die at the end of the growing season

Culinary-Wise

Vegetable products which add flavor or aromato food

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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 byextracting herbs with various solvents to yield

tinctures, extracts or fluidextracts

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Popularity of Herbals

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

79% of college students47% of men >20 years old57% of women >20 years old65%-83% of older adults55% 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

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Impact on drug therapy & health

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

dietary supplements concomitantly

69% of users of Rx drugs & dietary supplementstogether do not discuss these combinations withtheir medical practitioner

Pharmacists regularly receive questions frompatients & care practitioners

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Natural doesn’t necessarily mean safe

Strychnine, ricin, aconitine, digoxin: naturalpoisons

Humans survived by accepting that the fact that

environment offers

harmful & healing compounds

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Herbs versus Other Drugs

1- Dilution

Herbs: more dilute than purified therapeuticagents, e.g.,

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

20 g coffee powder (1-2% natural occurrence) or10 g tea (2-4%)

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2- Herbs often contain additional activeprinciples

which may be chemically & pharmacologicallyclosely related to the primary constituent

Digitalis contains ~30 cardiac glycosides with awide array of activity, duration & onset of actions

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Digitoxin: onset of action 1-4 hours /peak activity

8-14 hours

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

The effectiveness of Digitalis is attributed to its

constituents multiplicity which provideuniform effectiveness with short onset & longduration

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Standardized Remedies

To assure herbal quality, there should be anefficient mean to isolate, quantify & assay activeconstituent(s) or a marker compound, if known

If the active ingredient is a complex mixture orunknown, or if no marker compound is available,

biological assays must be utilized such as thatemployed to determine Digitalis potency (cardiac

arrest of Pigeon's heart)

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Once the potency of the herb is established ,

it can be mixed with appropriate quantities of other

material of greater or lesser potency to optimizeactivity

Standardized extracts of ginkgo, ginseng, milkthistle, St. John wort & many others now available

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Natural medicine versus pharmacy practice

Increase the potential for: > adverse effects> interactions with prescription drugs

delayed / ineffective treatment > other problems

Raw Plant Steeped Tea

Standard- ized

Extract

Singlechemical entity

Mixture-many chemicals

Mild drug action

Mild sideeffects

Pureconcentrated chemicals

Strong adverseeffects

Strong drug action

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Standardized Generics

Clin. Active 1 2 3

Raw Plant Material

Pure ActiveIngredients

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Quality Assurance

Products usually misbranded & ingredients’

therapeutic quantities not indicated especially inmixture-containing products

e.g.,

Adequate amount of tannins in an herb explains itsastringent effect on wounds

Consumer: buy a standardized product/specifiedamount & marketed by a reputable firm

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Accurately labeled products containing:

botanical scientific name

manufacturer name/address

batch number, manufacture/expiration datesa phone number for inquires

indicate good quality assurance

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Herbals Use & Guidelines

Know which cases could be self treated, e.g.,occasional headache pain, strained muscle , milddigestive upset, simple diarrhea, infrequentinsomnia , common cold

Cases need professional medical care :rheumatoid arthritis, diabetes , cardiac arrythmia,hypertension , or cancer

Herbals not recommended during pregnancy, cancross placenta/expose fetus to teratogenic hazards

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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 prescriptionmedications

Drug-herb interactions could be a major concernherbals should be included in patient drug history

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ParaherbalismFaulty/ inferior herbalism based on pseudoscience

Difficult to differentiate from true/rationalherbalismadvocates 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

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HomeopathyDestructive form of paraherbalismlate 17 th 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

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treatment should reinforce these symptoms!!

medication should produce similar symptoms inhealthy 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

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Homeopathy: Dilutions

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Herbal Medicine Information Sources

Objective, accurate, honest, unbiased information

Many available information sources on herbs dueto revival of interest

Not all information sources are trustable

News, magazines, TV, online data bases, books

scientific/professional journals & GermanCommission E monographs

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Most trustful sources safety/ efficacy of herbal

remedies: controlled clinical trials, published inscientific journals

correct honest/unbiased scientific methodology

One patients group administer investigated drugversus 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

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The German Commission E monographs :

one of best/valuable drug efficacy/safetyinformation resources

Experience gained during many years of empirical

use of phytotherapy

recognize its origin & should be taken in accountalong with clinical trials, to evaluate effectiveness

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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 dru s act b inhibitin this stimulation

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GingerRhizomes (underground stems) of Zingiber officinale , Zingiberaceae

Medicinal UsesI- Orally

1- Motion sickness

double blind study: 36 students with high tendency tomotion sickness: 940 mg ginger is superior to 100 mgdimenhydrinate in reducing motion sickness / vertigo when

used 25 minutes before test in a tilted rotating chair

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German Commission E:

2-4 g daily doses ginger is effective in preventingmotion sickness/digestive aid Also useful anti-emetic in minor outpatient surgery procedures

Discrepancy in clinical trials results due to:

failure to use standardized preparations whichwidely vary in chemical composition & maycontain adulterants

grown in various world areas: variable contents

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to avoid such discrepancy,

Standardized ginger: containing standard amountof shogaols & gingerols

Mechanism:GI rather than CNS,

Ginger had no effect on inner ear nor oculomotorsystem

reduces tachygastria (abnormal increase in pacemaker activity in gastric musculature)enhance gastric emptying

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2- Other digestive uses of ginger

Hyperemesis gravidum (a severe form of pregnancy-related nausea & vomiting), pepticulcers, colic, dyspepsia, flatulence, loss of appetite,anorexia & high blood cholesterol & sugar levels

3- Disequilibrium/ nausea associated withdiscontinuation or tapering of selectiveserotonin reuptake inhibitors (SSRIs)

3- Rheumatoid arthritis

4- U Respiratory tract infections, cough/bronchitis

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Safety

Likely safe in food amount

GRAS (Generally recognized as a safe herb) in USMaximum permissible level in food is 0.0023%

Topically: oil is well tolerated & unlikely to causephototoxicity

Likely safe in pregnancy in normal food levelbut unsafe in larger amountsLarge dose: CNS depression/cardiac arrhythmias

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Adverse ReactionsAllergic dermatitis in sensitive individuals

Ginger-Herb Interactions

Concomitant use with herbs that have coumarins(anticoagulant) or affect platelet aggregation could

increase bleeding riskExamples of these herbs:

Turmeric, capsicum, fenugreek, chamomile,clove, garlic, onion, feverfew, ginkgo, ginseng,celery

D I i

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Drug Interactions

1- Interferes/antacids: sucralfate, H 2-antagonists &proton pump inhibitors

2- SSRIs/ sertraline (Zoloft):

(+)-interaction treating disequilibrium/nausea fromSSRIs discontinuation

3- Cyclophosphamide: (+)-interactionPreventing its induced vomiting

5- Anticoagulants/ anti-platelet aggregation drugs ,increase bleedin risk

d

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Contraindications

1- Gallstones2- Bleeding Conditions: inhibit thromboxane synthetase enhance prostacyclin , produce prolonged bleeding time &some immunological changes, used with caution forpostoperative nausea

Dosage FormsHard gelatin capsules: 500 mg powdered rhizome formotion sickness taken 30 minutes before departureDried or fresh rhizomes : orally 0.25-1 g or as an infusiontea three times daily: Tea prepared by steeping 0.5-1 g in150 ml boiling H 2O for 5-10 minutes

Maximum daily ginger dose is 4 g

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2- Constipation

Decrease in frequency of fecal elimination/

difficulty in passing stools

~70 million / year more common in women

Laxatives should be of 2 nd priority after fiber-richdiet, adequate fluid intake/ regular physical activity

contraindicated in cases of cramps, nausea,vomiting, bloating & undiagnosed abdominal pain

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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

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PsylliumClean, dry ripe seeds of Plantago psylliumMedicinal 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 H h l t l i

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2- Hypocholesterolemia

Psyllium alone or mixed with water soluble dietary fibersinduce significant reduction of blood cholesterol & LDL-cholesterol by binding & increase fecal excretion of

cholesterol & bile acidsBile acids replaced in liver by using more serumcholesterol for bile acid synthesis : less available cholesterolfor 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

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4- Reducing peak blood glucose level by slowingcarbohydrate absorption

Safety

Likely safe orally with adequate fluid intakeUnsafe/ 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 causenephrotoxicity This pigment removed from commercialforms

I t ti

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InteractionsVitamin/Mineral Supplements :

Long term use of psyllium with vitamin/minerals canreduce 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 & requiredose adjustment

- Insulin/diabetes therapy : induce hypoglycemia careful

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Insulin/diabetes therapy : induce hypoglycemia, carefulblood glucose monitoring is required

Dosage Forms

Start with small amounts/gradually increase to desiredresponse

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 Sti l t L ti

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B- Stimulant LaxativesSome medicinal herbs contain anthraquinones, anthrones,dianthrones , Which stimulate peristalsis by irritatingintestinal mucosa’s intraneural nerve plexus activity ,increasing motility

Act on colonic mucosal cells, opening Cl - channels,

stimulate active Cl - secretion, reduce liquid & electrolyteabsorption in the colon & increase their level in / pressureon colonic lumen: laxative action

Anthranoid glycosides: prodrugs pass unchanged to colonwhere they hydrolyzed by microbial flora enzymes to freeanthranoid aglycone/ sugar moiety, active anthrones:

Delayed-onset

Senna

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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 beforediagnostic tests & in slimming & cleansing teas

Safety

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Safety

Likely safe : When used orally for short-termPossibly Unsafe : When used longer than 1-2 weeks canlead to dependenceChildren : Possibly safe, standardized formPregnancy : Possible unsafe

Lactation: Possibly unsafe , excreted in milk & may causediarrhea

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:

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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-conjunctivitisChronic use can cause reversible pseudomelanosis coli ,laxative dependency

Interactions with Drugs

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Interactions with Drugs

- Cardiac glycosides & Laxatives : K + depletion- Corticosteroids/K +-depleting diuretics hypokalemia

- Oral Drugs can reduce absorption of some oral drugsdue to reduced GI transitsInterfere with any urine diagnostic colorimetric tests dueto urine discoloration

Dosage Forms15-30 mg/day calculated as sennoside B

0.5-2 g powdered leaf: infusion/ maceration tea

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SennaA

Ginger

B

Psylium

C

1- Which of A-C can interfere with digoxin/cardiacglycosides/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 & disequilibriumfrom discontinuation of SSRI sertraline (Zoloft)?

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