Comprehensive Guide to Herbs by Dr. James Meschino - HTML preview

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Meschino Health Comprehensive Guide to Herbs

Valerian (valeriana officinalis)

General Features

There are more than 200 plant species belonging to the genus Valeriana, but the most common one, and the one used

for medicinal purposes is Valeriana officinalis. 1,9 10 This plant grows wild all over Europe, but most of the Valerian

used in consumer health products is cultivated. 10 The rootstock contains its active constituents, which are

concentrated into health products used primarily for the treatment of insomnia and anxiety. 1,9,10 Scientific studies

evaluating the effects of Valerian on humans began in the 1970’s, which subsequently lead to its approval as a sleep

aid by the Germany’s Commission E Monograph in 1985. 9

Principle Active Constituents

1. Valepotriates (iridoid molecules) and valerenic acid. These compounds are exclusive to Valerian.1 It now appears

that valerenic acid is a possible active constituent, but not the valepotriates. 9

2. Volatile Oils 12

Clinical Application and Mechanism of Action

Insomnia

Valerian acts as a sedative in that its active constituents, which are not fully understood or known, are capable of

binding to the same brain receptors as Valium and other benzodiazepine drugs. Central nervous system sedation is

regulated by receptors in the brain known as GABA-A receptors (gamma amino butyric acid). Experimental test tube

studies indicate that active constituents in Valerian may weakly bind to GABA-A receptors in the brain, producing a

sedation effect. Human trials suggest that Valerian tends not to impair mental function or produce a morning

hangover, and dependency has not been reported with its use. Studies have demonstrated improved sleep quality

and insomnia relief. 1,2,3,9,11,12

Overall, studies suggest that Valerian improves sleep quality (more restful sleep), and the transition into sleep.

However, it may not increase total sleep time. These findings arise from several double-blind trials, that provide

evidence for Valerian as an effective treatment for individuals with mild to moderately severe insomnia. 2,3,4,13,14,15,16

A 28-day study, involving 121 subjects, showed that Valerian supplementation provided significant improvement in

insomnia cases, compared to the placebo. 13

A 14-day trial, involving 78 elderly patients, also showed that Valerian supplementation provided significant

improvement in insomnia cases, compared to placebo. As shown in other studies, it often takes a number of days

before the effects of Valerian appear. As such, patients tend to report more consistent improvement in relief of

insomnia after several days of Valerian supplementation (its effects are not immediate as would be the case for many

drugs prescribed for this condition). 14

There is also convincing evidence from animal studies that Valerian produces a calming effect, as well as enhanced

sleepiness, and reduced activity patterns. These studies provide important objective proof of Valerian’s natural

sedative capabilities. 18,19,20,21

In head-to-head trials testing Valerian against the drug oxazepam (10 mg at bedtime) and bromazepam, Valerian

supplementation demonstrated that it could provide equal relief for insomnia, as did these common sleep-aid

medications. 15,16

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Anxiety

Several preliminary studies indicate that Valerian may be an effective treatment in cases of uncomplicated anxiety (not

linked to major depression) and it has been used for this problem historically and clinically, although more research is

needed to better understand its application in this regard. 1,2,3,17

Dosage and Standardized Grade

Insomnia: As a mild sedative, Valerian may be taken 30-45 minutes before retiring at the following dosage and

standardized grade: Valerian extract, 200 –400 mg (standardized to 0.8% valerenic acids content) 8,11

Anxiety and Stress Reduction: 200 mg, twice per day (standardized to 0.8% valerenic acids content). 11

Adverse Side Effects, Toxicity and Contraindications

Animal studies show that it takes enormously large doses of Valerian to produce any serious side effects, and in one

suicide attempt, a human subject experienced no life threatening effects (stomach cramps, fatigue, chest tightness,

tremors and light-headedness), after taking 20 gms of valerin (20-40 times the recommended dose). 22,23 There have

been approximately 50 reported cases of overdose when subjects took a product called Sleep-Qik, containing Valerian

as well as conventional medications, but no liver damage was noted. 24,25

Generally speaking, Valerian is considered to be safe and usually causes only mild gastrointestinal upset on rare

occasions. It is on the GRAS list (generally recognized as safe) of the FDA.

Some mild impairment to attention ability may occur for a couple of hours after intake, and thus, driving immediately

after Valerian supplementation is not advised. However, Valerian is not reported to cause morning drowsiness when

taken the night before. 9,10,11 If morning sleepiness does occur, simply reduce the dosage.1

Drug-Nutrient Interactions

Valerian may potentiate the actions of the following medications and thus, it is considered to be prudent to not take

Valerian concurrently with these drugs:



Barbituates or Sedatives 26



Antidepressants 27,28,29



Anti-anxiety medications 30,31,32



Hypnotic drugs 33,34,35

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Pregnancy and Lactation

During pregnancy and lactation, the only supplements that are considered safe include standard prenatal

vitamin and mineral supplements. All other supplements or dose alterations may pose a threat to the

developing fetus and there is generally insufficient evidence at this time to determine an absolute level of

safety for most dietary supplements other than a prenatal supplement. Any supplementation practices

beyond a prenatal supplement should involve the cooperation of the attending physician (e.g., magnesium

and the treatment of preeclampsia.)

References: Pregnancy and Lactation

1. Encyclopedia of Nutritional Supplements. Murray M. Prima Publishing 1998.

2. Reavley NM. The New Encyclopedia of Vitamins, Minerals, Supplements, and Herbs. Evans and

Company Inc. 1998.

3. The Healing Power of Herbs (2nd edition). Murray M. Prima Publishing 1995.

4. Boon H and Smith M. Health Care Professional Training Program in Complementary Medicine.

Institute of Applied Complementary Medicine Inc. 1997.

1. Houghton PJ. The biological activity of Valerian and related plants. J Ethnopharmacol 1988;22(2):121-42.

2. Leathwood P, et.al.. Aqueous extract of Valerian root (Valeriana Officinalis L.) Improves sleep quality in man. Pharmacol Biochem

Behav 1982;17:65-71.

3. Bakderer G, Borbely AA. Effect of Valerian on human sleep. Pharmacol 1985;87:406-9.

4. Leathwood PD, Chauffard F. Aqueous extract of Valerian reduces latency to fall asleep in man. Planta Medica 1985;54:144-8.

5. Lindahl O, Lindwall L. Double blind study of a Velerian preparations. Pharmacol Biochem Behav 1989;32(4):1065-6.

6. Dressing H, et.al.. Insomnia: are Valeriana/Melissa combinations of equal value to Benzodiazepine? Therapiewoche 1992;42:726-36.

7. Leung A. Encyclopedia of common natural ingredients used in food, drugs, and cosmetics. New York, New York. John Wiley & Sons,

1980.

8. Murray MT. The healing power of herbs. 2nd ed. Prima Publishing, 1995.

9. Natural Products Encysclopedia www.consumerslab.com: Valerian

10. Healthnotes, Inc. 2001 www.healthnotes.com: Valerian

11. Dietary Supplement Information Bureau. www.content.intramedicine.com: Valerian

12. Mennini T, Bernasconi P, Bombardelli E, et al. In vitro study on the interaction of extracts and pure compounds from Valeriana officinalis

roots with GABA, benzodiazepine and barbiturate receptors. Fitoterapia 1993;64:291–300

13. Vorbach EU, Gortelmeyer R, Bruning J. Therapy for insomniacs:effectiveness and tolerance of valerian preparations [translated from

German]. Psychopharmakotherapie 1996;3:109-15

14. Kamm-Kohl AV, Jansen W, Brockmann P. Modern valerian therapy for nervous disorders in old age [translated from German]. Med Welt

1984;35:1450-4

15. Dorn M. Efficacy and tolerability of Baldrian versus oxazepam in non-organic and non-psychiatric insomniacs: a randomized, double-

blind, clinical, comparative study [translated from German]. Forsch Komplementarmed Klass Naturkeilkd 2000;7:79-84

16. Schmitz M, Jackel M. Comparative study for assessing quality of olife of patients with exogenous sleep disorders (temporary sleep onset

and sleep interruption disorders)

17. Kohnen R, Oswald WD. The effects of valerian, propranolol, and their combination on activation, performance and mood of healthy

volunteers under social stress conditions. Pharmacopsychiatry 1988;21:447-8

18. Hendriks H, Bos R, Woerdenbag HJ, et al. Central nervous depressant activity of valerenic acid in the mouse. Planta Med 1985;1:28-31

19. Leuschner J, Muller J, Rudmann M. Characterisation of the central nervous depressant activity of a commercially available valerian root

extract. Arzneimittelforschung 1993;43:638-41

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20. Krieglstein J, Grusla D. Centrally depressant components of valerian. However, valepotriates, valerenic acid, valeranone and the

essential oil are ineffective [in German]. Dtsch Apoth Ztg 1988;128:2041-6

21. European Scientific Cooperative on Phytotherapy. Valerianae radix. Exeter, UK: ESCOP 1996-1997:3-4 Monographs on the Medicinal

uses of Plant Drugs, Fascicule 4

22. Resecrans JA, Defeo JJ, youngken HW Jr. Pharmacological investigation of certain Valeriana officinalis L. extracts. J Pharm Sci

1961l50:240-4

23. Willey LB, Mady SP, Cobaugh DJ, et al. Valerian overdose: a case report. Vet Hum Toxicol 1995;37:364-5

24. Chan TY, Tang CH, Critchley JA. Poisoning due to an over-the-counter hypnotic, Sleep-Qik (hyoscine, cyproheptadine, valerian).

Postgrad Med J 1995;71(834):227-8

25. Chan TY. An assessment of the delayed effects associated with valerian overdose [letter]. Int J Clin Pharmacol Ther 1998;36:569

26. Hendriks H, et al. Central nervous depressant activity of valerenic acid in the mouse. Planta Med Feb1985;1:28-31

27. Houghton PJ. The biological activity of valerian and related plants. J Ethnopharmacol 1988;22(2):121-42

28. Santos MS, et al. Synaptosomal GABA release as influenced by valerian root extract – involvment of the GABA carrier. Arch Int

Pharmacodyn Ther 1994;327(2):220-31

29. Houghton PJ. The scientific basis for the reputed activity of valerian. J Pharm Pharmacol May 1999;51(5):505-12

30. Houghton PJ. The biological activity of valerian and related plants. J Ethnopharmacol 1988;22(2):121-42

31. Santos MS, et al. Synaptosomal GABA release as influenced by valerian root extract – involvment of the GABA carrier. Arch Int

Pharmacodyn Ther 1994;327(2):220-31

32. Houghton PJ. The scientific basis for the reputed activity of valerian. J Pharm Pharmacol May1999;51(5):505-12

33. Houghton PJ. The biological activity of valerian and related plants. J Ethnopharmacol 1988;22(2):121-42

34. Santos MS, et al. Synaoptosomal GABA release as influenced by valerian root extract – involvment of the GABA carrier. Arch Int

Pharmacodyn Ther 1994;327(2):220-31

35. Houghton PJ. The scientific basis for the reputed activity of valerian. J Pharm Pharmacol May1999;51(5):505-12

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Vinpocetine

General Features

Vinpocetine is a derivative of the Vinca minor (lesser periwinkle), which is native to many parts of Europe, where it

grows in woods and thickets. The isolated active constituent known as ethyl apovincaminate was discovered in the late

1960’s and since that time has been studied and used as a natural agent to enhance blood flow to the brain, with

particularly emphasis on its potential use in cerebral vascular insufficiency, dementia and ischaemic stroke.1,

Principle Active Constituents

Vinpocetine is a synthetic ethyl ester of apovincamine, derived originally from the Vinca minor.3

Clinical Application and Mechanism of Action

Vinpocetine has been shown to enhance blood flow to the brain, act as an antioxidant and protect brain cells from the

neurotoxic effects of Abeta Proteins that are linked to the development of Alzheimer’s disease. Therefore, it is being

explored as a preventive and therapeutic agent in regards to cerebral vascular insufficiency, ischaemic stroke (to

prevent a recurrence), age-related dementia and Alzheimer’s disease.1,2,3,4 Vinpocetine has demonstrated good brain

penetration, making it available to exert its bioactive effects on brain circulation and brain cells.1

1. Ischaemic Stroke

The increase in the regional blood flow in response to Vinpocetine administration is well established and strengthened

by new diagnostic techniques (e.g., transcranial Doppler technique etc.). Vinpocetine has been shown to increase

brain circulation, mainly in the thalamus, basal ganglia and visual cortex. Multicenter, randomized, placebo-controlled

clinical studies have proven Vinpocetine to be effective in patients with organic psychosyndrome. It has also been

shown to be beneficial in redistributing regional blood flow and enhancing glucose supply of brain tissue in ischaemic

post-stroke patients (using positron emission tomography studies).1 A small, but important study recruited 30 patients,

who had suffered a stroke within the past 72 hours and were given either dextran or dextran plus Vinpocetine. After

three months of follow-up, the group given the Vinpocetine showed a 30% reduction in risk of recurring stroke, as

defined by the modified Barthel Index, and 60% as defined by the modified Ranking score, compared to the group

given dextran alone.3

2. Chronic Cerebral Insufficiency

Vinpocetine supplementation was given to forty-two patients with chronic cerebral dysfunction at a daily dosage of 10

mg, three times per day for 30 days. Compared to the forty-two patients given the placebo tablets (who also had

chronic cerebral dysfunction), patients receiving the Vinpocetine treatment scored consistently better in all evaluations

as measured by the Clinical Global Impression scale, the Sandoz Clinical Assessment-Geriatric scale, and the Mini-

Mental Status Questionnaire. There were no serious side effects related to the ingestion of Vinpocetine.5

3. Dementia and Alzheimer’s disease

In a placebo-controlled, randomized double-blind, multi-center trial involving two hundred and three patients with mild

to moderate organic psychosyndrome, including dementia, half of the participants were given Vinpocetine

supplementation at 10 mg, three times daily or 20 mg, three times daily for 16 weeks versus the other half of the group

who took the placebo pills three times per day. Statistically significant improvements were found in favour of the

Vinpocetine group (at both dosages) compared to the placebo group. The Vinpocetine group demonstrated better

objective scores on the Clinical Global Impression scale and in cognitive performance (SKT). Vinpocetine was also

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superior to placebo in ratings of the severity of illness. There were no serious side effects reported from the use of

Vinpocetine and adverse events between Vinpocetine-treated patients and the placebo group were comparable,

indicating no increased attributable risk from the use of Vinpocetine.6

In regards to Alzheimer’s disease, experimental evidence has shown that Vinpocetine protects brain cells from the

toxic effects of Amyloid beta-Protein (Abeta-Protein), which is the agent known to damage brain cells in the

development of Alzheimer’s disease. Abeta-Protein induces free radical damage, which in turn, leads to severe

damage to the energy factories (mitochondria ) of the cell, vital enzymes (especially those needed to produce the

memory chemical, acetylcholine) and other cellular structures. Uncontrolled free radical damage of this nature can

ultimately lead to brain cell death of affected neurons. Vinpocetine has been shown to quench (neutralize) free radicals

produced by Abeta-Protein, reducing the oxidative damage (free radical) to brain cells under experimental conditions.

It also has been shown to protect key respiratory chain complexes within the mitochondria (energy factories of the cell)

that were exposed to Abeta-Protein. The researchers conclude that Vinpocetine can exert neuroprotective properties

which might be of importance and contribute to its clinical efficacy in the treatment of Alzheimer’s disease or other

neurodegenerative disorders in which oxidative stress is involved (e.g., Parkinson’s disease, Multiple sclerosis etc.)7

As reviewed by CD Nicholson, “Vinpocetine attenuates cognitive deficits, reduces ischaemia-induced hippocampal cell

loss and increases cerebral blood flow and glucose utilization.8 Many scientists indicate that Vinpocetine’s ability to

improve cognitive function is primarily due to its effects on enhancing blood flow to the brain, dilating blood vessels,

supporting the proper function of red blood cells and reducing blood viscosity via its influence on reducing platelet

stickiness.9,10,11

Dosage and Standardized Grade

Cerebral Vascular Insufficiency, leading to cognitive dysfunction: 5 mg, 10 or 20 mg, three times per day 2,5,6

Dementia and Alzheimer’s disease: 5 mg, 10 or 20 mg, three times per day 2,5,6

Adverse Side Effects, Toxicity and Contraindications

The available clinical studies do not indicate that Vinpocetine supplementation, when taken at recommended doses,

produces any adverse side effects or toxicity.1,3,5,6 However, it is a powerful anti-coagulant and therefore, the possibility

of a bleeding disorder in the brain or elsewhere in the body is a potential side effect that needs to be considered and

the focus of future studies.4

Drug-Nutrient Interactions

Anti-Coagulant Medications (e.g., Aspirin, Coumadin, Warfarin): Vinpocetine may potentiate the effects of these drugs

increasing the risk of a bleeding disorder in the brain or elsewhere in the body. Thus, it is contraindicated in these

cases, as is Ginkgo Biloba, which affects the brain in a similar fashion as Vinpocetine.4

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Pregnancy and Lactation

During pregnancy and lactation, the only supplements that are considered safe include standard prenatal

vitamin and mineral supplements. All other supplements or dose alterations may pose a threat to the

developing fetus and there is generally insufficient evidence at this time to determine an absolute level of

safety for most dietary supplements other than a prenatal supplement. Any supplementation practices

beyond a prenatal supplement should involve the cooperation of the attending physician (e.g., magnesium

and the treatment of preeclampsia.)

References: Pregnancy and Lactation

1. Encyclopedia of Nutritional Supplements. Murray M. Prima Publishing 1998.

2. Reavley NM. The New Encyclopedia of Vitamins, Minerals, Supplements, and Herbs. Evans and

Company Inc. 1998.

3. The Healing Power of Herbs (2nd edition). Murray M. Prima Publishing 1995.

4. Boon H and Smith M. Health Care Professional Training Program in Complementary Medicine.

Institute of Applied Complementary Medicine Inc. 1997.

1. Bönöczk P, Gulyás B, Adam-Vizi V, Nemes A, Kárpáti E, Kiss B, et al. Role of sodium channel inhibition in neuroprotection: effect of

vinpocetine. Brain Res Bull Oct2000;53(3):p245-54

2. Dietary Supplement Information Bureau: Vinpocetine. www.content.intramedicine.com. Dietary Supplement Education Alliance 2001

3. Feigin VL, Doronin BM, Popova TF, Gribatcheva EV, Tchervov DV. Vinpocetine treatment in acute ischaemic stroke: a pilot single-blind

randomized clinical trial. Eur J Neurol Jan2001;8(1):p81-5

4. Kidd PM. A review of nutrients and botanicals in the integrative management of cognitive dysfunction. Alternative Medicine Review

(ALTERN MED REV) Jun1999;4(3):144-61

5. Balestreri R, Fontana L, Astengo F. A double-blind placebo controlled evaluation of the safety and efficacy of Vinpocetine in the treatment

of patients with chronic vascular senile cerebral dysfunction. J Am Geriatr Soc 1987;35:425-30

6. Hindmarch I, et al. Efficacy and tolerance of vinpocetine in ambulant patients suffering from mild to moderate organic psychosyndromes.

Int Clin Psychopharmacol 1991;6(1):31-43

7. Pereira C, Agostinho P, Oliveira CR. Vinpocetine attenuates the metabolic dysfunction induced by amyloid beta-peptides in PC12 cells.

Free Radic Res Nov2000;33(5):p497-506

8. Nicholson CD. Pharmacology of nootropics and metabolically active compounds in relation to their use in dementia. Psychopharmacology

(Berl) 1990;101:147-59

9. Burtsev EM, et al. [10-year experience with using Cavinton in cerebrovascular disorders]. Zh Nevropatol Psikhiatr Im S S Korsakova

1992;92(1):56-60

10. Tamaki N, et al. The effect of Vinpocetine on cerebral blood flow in patients with cerebrovascular disorders. Ther Hung 1985;33:13-21

11. Osawa M, Maruyama S. Effects of TCV-3B (Vinpocetine) on blood viscosity in ischemic cerebrovascular disease. Ther Hung 1985;33:7-

12

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White Willow Bark (Salix spp)

General Features