Bioavailability Health Dictionary

Pepper, bell pepper, chili pepper, cayenne (Capsicum annuum, C. frutescens & C. chinense).

Plant Part Used: Leaf, fruit.

Dominican Medicinal Uses: The leaf is traditionally prepared as a warm poultice and applied topically for skin abscesses, boils or infections, or prepared as a tea and taken orally for menstrual cramps and related disorders. The fruit is typically used for culinary and nutritional purposes and is said to increase heat in the body.

Safety: No data on the safety of the leaf in humans (for internal or external use) has been identified in the available literature; however, in animal studies, topical application of the leaf did not show signs of toxicity or adverse effects. The fruit is widely consumed and considered safe in moderate amounts. Prolonged or excessive use may cause irritation of the mucosa or other adverse effects.

Contraindications: No data on the safety of this plant during pregnancy, lactation or in children has been identified in the available literature. The fruit should not be taken by patients with inflammatory gastro-intestinal or renal disorders. Avoid contact with the eyes or open wounds due to potential irritation of the mucosa.

Drug Interactions: Consumption of the fruit may inhibit liver microsomal enzymes and potentiate drugs metabolized by these enzymes. Aspirin and salicylic acid compounds: bioavailability may be reduced by concurrent use of peppers. Barbiturates: concomitant use of the dried fruit has been shown to potentiate the effects of hexobarbital. Anticoagulants, antiplatelet agents, thrombolytic agents: concomitant use of the fruit may increase the risk of bleeding.

Clinical Data: No human clinical trials of the leaf have been identified in the available literature. The fruit has been investigated in clinical trials for the following effects: analgesic, carotenoid bioavailability enhancement, gastroprotective, swallowing dysfunction treatment and urinary incontinence treatment.

Laboratory & Preclinical Data: The following biological activities of this plant have been investigated in laboratory and preclinical studies (in vitro or animal models): antimicrobial, antioxidant, antitumor, chemopreventive, cytotoxic, learning enhancement, learning impairment amelioration and renoprotective.

* See entry for Ají in “Part 3: Dominican Medicinal Plant Profiles” of this book for more information, including references.... ají

Sesame (Sesamum indicum).

Plant Part Used: Seed, seed oil.

Dominican Medicinal Uses: The seed oil is traditionally taken orally for asthma, bronchitis, common cold, flu and pneumonia, and the seed emulsion is taken orally for asthma, administered to both children and adults.

Safety: The seed and seed oil are generally regarded as safe for human consumption, and no adverse reactions have been reported in clinical studies.

Contraindications: None identified in the available literature.

Drug Interactions: None identified in the available literature.

Clinical Data: The following effects of the seed oil or seeds have been investigated in human clinical trials: antidiabetic, dry nasal mucosa treatment, enterolactone precursor, hypocholesterolemic, hypotensive, infant growth stimulus, postmenopausal support, sex hormone binding globulin increase, sleep improvement, thiobarbituric acid reacting substance decrease and Vitamin E status improvement.

Laboratory & Preclinical Data: The following biological activities have been investigated in laboratory and preclinical studies (in vitro or animal models): antitumor, antineoplasm, antihypertensive, antioxidant, hypocholesterolemic and improved Vitamin E bioavailability.

* See entry for Ajonjolí in “Part 3: Dominican Medicinal Plant Profiles” of this book for more information, including references.... ajonjolí

(Linn.) Merrill

Family: Bromeliaceae.

Habitat: Native to South America; cultivated mostly in Tamil Nadu, coastal Andhra Pradesh, Assam, Kerala, Karnataka, West Bengal, Tripura and Orissa.

English: Pineapple.

Ayurvedic: Anaanaasa, Bahunetra.

Unani: Anannaas.

Siddha/Tamil: Annanshippazham, Annasi.

Action: Anti-inflammatory (fresh juice used as a gargle for sore throat). A proteolytic enzyme, bromelain, is derived from the stem—anti-inflammatory, smooth muscle relaxant, digester, inhibitor of blood platelet aggregation. (It is used for cellulitis, post-operative oedema, sinusitis and for promoting digestion of proteins.)

Key application: Bromelain, the proteolytic enzyme, is used in acute postoperative and post-traumatic conditions of swellings, especially of the nasal and paranasal sinuses. (German Commission E.) In Europe, a patented tape that contains bromelain is used for debriding escharotic skin. (Internally, bromelain's bioavailability has been questioned.)... ananas comosus

Calcium-channel blockers inhibit the inward ?ow of calcium through the specialised slow channels of cardiac and arterial smooth-muscle cells. By thus relaxing the smooth muscle, they have important applications in the treatment of HYPERTENSION and ANGINA PECTORIS. Various types of calcium-channel blockers are available in the United Kingdom; these di?er in their sites of action, leading to notable di?erences in their therapeutic effects. All the drugs are rapidly and completely absorbed, but extensive ?rst-pass metabolism in the liver reduces bioavailability to around one-?fth. Their hypotensive e?ect is additive with that of beta blockers (see BETA-ADRENOCEPTOR-BLOCKING DRUGS); the two should, therefore, be used together with great caution – if at all. Calcium-channel blockers are particularly useful when beta blockers are contraindicated, for example in asthmatics. However, they should be prescribed for hypertension only when THIAZIDES and beta blockers have failed, are contraindicated or not tolerated.

Verapamil, the longest-available, is used to treat angina and hypertension. It is the only calcium-channel blocker e?ective against cardiac ARRHYTHMIA and it is the drug of choice in terminating supraventricular tachycardia. It may precipitate heart failure, and cause HYPOTENSION at high doses. Nifedipine and diltiazem act more on the vessels and less on the myocardium than verapamil; they have no antiarrhythmic activity. They are used in the prophylaxis and treatment of angina, and in hypertension. Nicardipine and similar drugs act mainly on the vessels, but are valuable in the treatment of hypertension and angina. Important di?erences exist between di?erent calcium-channel blockers so their use must be carefully assessed. They should not be stopped suddenty, as this may precipitate angina. (See also HEART, DISEASES OF.)... calcium-channel blockers

(Linn.) O. Kuntze.

Family: Ranunculaceae.

Habitat: Western temperate Himalayas from 2,500 to 4,000 m.

English: American cowslip, Marsh Marigold, Water Buttercup.

Folk: Mamiri (Punjab).

Family: Theaceae.

Habitat: Cultivated in Assam, Darjeeling, Travancore, the Nilgiris, Malabar, Bengal, Dehra Dun and Kumaon.

English: Tea.

Unani: Chaai, Shaahi, Shaayi.

Siddha/Tamil: Thaeyilai.

Action: Stimulant, diuretic, astringent. In China, used for diarrhoea and dysentery (causes gastrointestinal upsets and nervous irritability when consumed in excess). Green tea: anticancer effects have been observed in Chinese green tea, Camellia thea, extract; the extract of Japanese green tea showed antihepatotoxic effects.

Important constituents of leaf buds and very young leaves are: caffeine, with a much smaller amount of other xanthines (theophylline and theo- bromine); tannins (the main tannin in green tea is (-)-epigallocatechin); flavonoids, quercetin, kaempferol. The stimulant and diuretic are due to caffeine content, the astringency due to the tannins.

Drinking tea lowers thiamine and thiamine diphosphate losses in urine and blood serum respectively but increases niacin losses. Hot water extract of black tea facilitates Ca absorption in the body experimentally. Tea may decrease zinc bioavailability.

The tea, if added to the meal, significantly lower the availability of iron. Milk is as effective as ascorbic acid in countering the depressing effect of tea on iron availability (in vitro).

The green tea catechin inhibited car- cinogenesis in small intestines when given during or after carcinogen treatment to experimental rats. (-)-epi- gallocatechin gallate and theaflavin di- gallate from green tea inhibited the in- fectivity of both influenza A and B virus (in vitro).

Green tea, when added to a lard- cholesterol diet, decreased the cholesterol and triglyceride levels in fowls. Tea polyphenols exhibit hypocholes- terolaemic activity.

Tea polyphenols—(-)-epicatechin gallate, (-)-epigallocatechine galate, theaflavin monogallate A or B, and or theaflavin digallate—are used for treating hyperglycaemia.

Saponins from tea are used as an- tiulcer agents.

Concurrent use of tea and beta- adrenergic agonists may increase the risk of cardiac arrhythmias. Caffeine, a component of tea, may increase insulin resistance. (Sharon M. Herr.)... camellia sinensis

Linn.

Family: Papilionaceae; Fabaceae.

Habitat: Cultivated in most parts of India.

English: Bengal Gram, Chick pea.

Ayurvedic: Chanaka, Chanakaa, Harimantha, Vajimantha, Jivan, Sakal-priya.

Unani: Nakhud.

Siddha/Tamil: Kadalai, Mookkuk- kadalai.

Action: Antibilious, hypoc- holesteremic, antihyperlipidemic, antistress. Acid exudate from the plant—used in indigestion, diarrhoea, dysentery. Seed coat extract—diuretic, antifungal (externally). Dry leaf—refrigerant.

Supplementation of gram in wheat based diet helps in lysine absorption which is otherwise a limiting amino acid in cereal based diets. Germination improves mineral bioavailability. In germinated gram flour, there is significant increase in nutritional quality of protein and very significant increase in ascorbic acid.

The seeds contain pangamic acid, the stemina building, antistress and antihyperlipidemic principle of gram. Gram is given as preventive diet to atherosclerosis patients because of its rich phosphorus content.

Isoflavones, biochanin A and for- monetin exhibited hypolipidermic activity in rats. Total flavonoids reduced serum and liver cholesterol in rats.

Seeds reduced postprandial plasma glucose in human.... cicer arietinum

Linn.

Synonym: C. domestica Valeton.

Family: Zingiberaceae.

Habitat: Cultivated all over India, particularly in West Bengal, Tamil Nadu and Maharashtra.

English: Turmeric.

Ayurvedic: Haridraa, Priyaka, Haridruma, Kshanda, Gauri, Kaanchani, Krimighna, Varavarni- ni, Yoshitapriyaa, Hattavilaasini, Naktaahvaa, Sharvari.

Unani: Zard Chob.

Action: Anti-inflammatory, cholagogue, hepatoprotective, blood-purifier, antioxidant, detoxi- fier and regenerator of liver tissue, antiasthmatic, anti-tumour, anticu- taneous, antiprotozoal, stomachic, carminative. Reduces high plasma cholesterol. Antiplatelet activity offers protection to heart and vessels. Also protects against DNA damage in lymphocytes.

Key application: In dyspeptic conditions. (German Commission E, ESCOP, WHO.) As antiinflammatory, stomachic. (Indian Herbal Pharmacopoeia.)

The rhizomes gave curcuminoids, the mixture known as curcumin, consisting of atleast four phenolic diaryl- heptanoids, including curcumin and monodesmethoxycurcumin; volatile oil (3-5%), containing about 60% of turmerones which are sesquiterpene ketones, and bitter principles, sugars, starch, resin.

Curcumin related phenolics possess antioxidant, anti-inflammatory, gastroprotective and hepatoprotective activities. The antioxidant activity of curcumin is comparable to standard antioxidants—vitamin C and E, BHA and BHT.

The volatile oil, also curcumin, exhibited anti-inflammatory activity in a variety of experimental models (the effects were comparable to those of cortisone and phenylbutazone). Used orally, curcumin prevents the release of inflammatory mediators. It depletes nerve endings of substance P, the neu- rotransmitter of pain receptors.

Curcumin's cholesterol-lowering actions include interfering with intestinal cholesterol uptake, increasing the conversion of cholesterol into bile acids and increasing the excretion of bile acids via its choleretic effects.

Curcuminoids prevent the increases in liver enzymes, SGOT and SGPT; this validates the use of turmeric as a he- patoprotective drug in liver disorders. Curlone, obtained from the dried rhizome, is used against hepatitis.

Turmeric and curcumin increase the mucin content of the stomach and exert gastroprotective effects against stress, alcohol, drug-induced ulcer formation. (Curcumin at doses of 100 mg/kg weight exhibited ulcerogenic activity in rats.)

The ethanolic extract of the rhizome exhibited blood sugar lowering activity in alloxan-induced diabetic rats.

Piperine (a constituent of black and long pepper) enhances absorption and bioavailability of curcumin.

Dosage: Cured rhizome—1-3 g powder. (API Vol. I.)... curcuma longa

Linn.

Family: Curciferace, Brassicaceae.

Habitat: Native to West Asia; cultivated throughout India as a salad plant.

English: Garden Cress, Water Cress.

Ayurvedic: Chandrashuura, Chan- drikaa, Vaas-pushpaa, Pashume- hankaarikaa, Nandini, Suvaasaraa, Aashaalim.

Unani: Habb-ul-rashaad, Tukh-e- Taratezak, Haalim, Sipandaan.

Siddha/Tamil: Alivirai.

Action: Used in asthma, bronchial affections and bleeding piles. Seeds—lactagogue, diuretic, and emmenagogue. Used for treating skin disorders, fever, amoebic dysentery and asthma. Leaf— stimulant, antiscorbutic, diuretic. Roots—used in secondary syphilis and in tenesmus.

The Ayurvedic Pharmacopoeia of India recommends the use of dried seeds, in powder form, in gout.

The seeds are a good source of iron, but its bioavailability is poor (5.4% of total iron). They are used for rapid healing ofbone fractures. The ethano- lic extract of seeds significantly increased collagen synthesis and its deposition at bone fracture portion in the treated rats. The tensile strength of the broken tibiae also increased.

The seeds contain an alkaloid (0.19%), glucotropaeolin, sinapin (cho- line ester of sinapic acid), sinapic acid, mucilaginous matter (5%) and uric acid (0.108 g/kg). The seed oil exhibits pronounced oestrogenic activity.

The seed mucilage allays the irritation of the mucous membrane of intestines in dysentery and diarrhoea. It consists of a mixture of cellulose (18.3%) and uronic acid-containing polysaccharides; acid hydrolysis yield L-arabinose, D-galactose, L-rhamnose, D-glacturonic acid and D-glucose.

The plant contains pantothenic acid, pyridoxin and rutin. Ethanolic extract of the plant showed antiviral activity against rinderpest virus.

Dosage: Seed—3-6 g powder. (API, Vol. I.)... lepidium sativum

Medicines are drugs made stable, palatable and acceptable for administration. In Britain, the Medicines Act 1968 controls the making, advertising and selling of substances used for ‘medicinal purposes’, which means diagnosing, preventing or treating disease, or altering a function of the body. Permission to market a medicine has to be obtained from the government through the MEDICINES CONTROL AGENCY, or from the European Commission through the European Medicines Evaluation Agency. It takes the form of a Marketing Authorisation (formerly called a Product Licence), and the uses to which the medicine can be put are laid out in the Summary of Product Characteristics (which used to be called the Product Data Sheet).

There are three main categories of licensed medicinal product. Drugs in small quantities can, if they are perceived to be safe, be licensed for general sale (GSL – general sales list), and may then be sold in any retail shop. P (pharmacy-only) medicines can be sold from a registered pharmacy by or under the supervision of a pharmacist (see PHARMACISTS); no prescription is needed. P and GSL medicines are together known as OTCs – that is, ‘over-thecounter medicines’. POM (prescription-only medicines) can only be obtained from a registered pharmacy on the prescription of a doctor or dentist. As more information is gathered on the safety of drugs, and more emphasis put on individual responsibility for health, there is a trend towards allowing drugs that were once POM to be more widely available as P medicines. Examples include HYDROCORTISONE 1 per cent cream for skin rashes, CIMETIDINE for indigestion, and ACICLOVIR for cold sores. Care is needed to avoid taking a P medicine that might alter the actions of another medicine taken with it, or that might be unsuitable for other reasons. Patients should read the patient-information lea?et, and seek the pharmacist’s advice if they have any doubt about the information. They should tell their pharmacist or doctor if the medicine results in any unexpected effects.

Potentially dangerous drugs are preparations referred to under the Misuse of Drugs Act 1971 and subsequent regulations approved in 1985. Described as CONTROLLED DRUGS, these include such preparations as COCAINE, MORPHINE, DIAMORPHINE, LSD (see LYSERGIC ACID

DIETHYLAMIDE (LSD)), PETHIDINE HYDROCHLORIDE, AMPHETAMINES, BARBITURATES and most BENZODIAZEPINES.

Naming of drugs A European Community Directive (92/27/EEC) requires the use of the Recommended International Non-proprietary Name (rINN) for medicinal substances. For most of these the British Approved Name (BAN) and rINN were identical; where the two were di?erent, the BAN has been modi?ed in line with the rINN. Doctors and other authorised subscribers are advised to write titles of drugs and preparations in full because uno?cial abbreviations may be misinterpreted. Where a drug or preparation has a non-proprietary (generic) title, this should be used in prescribing unless there is a genuine problem over the bioavailability properties of a proprietary drug and its generic equivalent.

Where proprietary – commercially registered

– names exist, they may in general be used only for products supplied by the trademark owners. Countries outside the European Union have their own regulations for the naming of medicines.

Methods of administration The ways in which drugs are given are increasingly ingenious. Most are still given by mouth; some oral preparations (‘slow release’ or ‘controlled release’ preparations) are designed to release their contents slowly into the gut, to maintain the action of the drug.

Buccal preparations are allowed to dissolve in the mouth, and sublingual ones are dissolved under the tongue. The other end of the gastrointestinal tract can also absorb drugs: suppositories inserted in the rectum can be used for their local actions – for example, as laxatives – or to allow absorption when taking the drug by mouth is di?cult or impossible – for example, during a convulsion, or when vomiting.

Small amounts of drug can be absorbed through the intact skin, and for very potent drugs like OESTROGENS (female sex hormones) or the anti-anginal drug GLYCERYL TRINITRATE, a drug-releasing ‘patch’ can be used. Drugs can be inhaled into the lungs as a ?ne powder to treat or prevent ASTHMA attacks. They can also be dispersed (‘nebulised’) as a ?ne mist which can be administered with compressed air or oxygen. Spraying a drug into the nostril, so that it can be absorbed through the lining of the nose into the bloodstream, can avoid destruction of the drug in the stomach. This route is used for a small number of drugs like antidiuretic hormone (see VASOPRESSIN).

Injection remains an important route of administering drugs both locally (for example, into joints or into the eyeball), and into the bloodstream. For this latter purpose, drugs can be given under the skin – that is, subcutaneously (s.c. – also called hypodermic injection); into muscle – intramuscularly (i.m.); or into a vein – intravenously (i.v.). Oily or crystalline preparations of drugs injected subcutaneously form a ‘depot’ from which they are absorbed only slowly into the blood. The action of drugs such as TESTOSTERONE and INSULIN can be prolonged by using such preparations, which also allow contraceptive ‘implants’ that work for some months (see CONTRACEPTION).... medicines

Linn.

Family: Piperaceae.

Habitat: Warmer parts of India, from Central Himalayas to Assam, lower hills of West Bengal; Uttar Pradesh, Andhra Pradesh, Western

Ghats from Konkan southwards to Trivandrum. Often cultivated.

English: Indian Long Pepper, Joborandi.

Ayurvedic: Pippali, Maagadhi, Maagadha, Maagadhaa, Maagad- hikaa, Magadhodbhavaa, Vaidehi, Upkulyaa, Pippalikam, Chapalaa, Kanaa, Krishnaa. Uushnaa, Shaun- di, Kolaa, Tikshna-tandulaa.

Unani: Filfil Daraaz, Daarfilfil.

Siddha/Tamil: Thippili, Arisi thippili. Thippiliver (root).

Action: Fruits—used for diseases of the respiratory tract (cough, bronchitis, asthma); as sedative (in insomnia and epilepsy); as chola- gogue (in obstruction of bile duct and bladder), as emmenagogue, as digestive, appetizer and carminative (in indigestion); as general tonic and haematinic (in anaemia, chronic fevers and for improving intellect). Applied locally on muscular pains and inflammations.

Several aristolactams and dioxoa- porphines have been isolated from Indian long pepper. It also contains the long chain isobutyl amide, longamide, besides guineensine and the lignans, pluviatilol, methyl pluviatilol (farge- sin), sesamin and asarinine.

Piperine is the major alkaloid of peppers.

Piperine is antipyretic, hypotensive, analeptic, CNS stimulant. It has been reported to exert significant protection against CCl4-induced hepatotoxicity in mice. It improves drug availability in experimental animals, and is used for enhancing the efficacy of co- administered medicaments.

Piperine enhanced bioavailability of hexobarbital, phenytoin, propranolol and theophylline. (Sharon M. Herr.) (Piperine is also a component of Piper nigrum.)

N - isobutyl - deca - trans - 2 - trans - 4 - dienamide, isolated from the fruit, exhibited antitubercular property.

Milk extract of the fruit effectively reduced passive cutaneous anaphylaxis in rats. It protected guinea-pigs against antigen-induced bronchospasm.

In China, Piper longum oil constituents were reported to inhibit the increase in serum total cholesterol induced by triton in mice.

The root powder exhibited antifer- tility activity.

A related species, P. peepuloides Roxb., is known as Saamvali Peepal. It is used specifically against obstinate skin diseases and as a sialagogue.

Dosage: Fruit—1-3 mg (API, Vol. IV); root—1-3 g powder. (CCRAS.)... piper longum

Tamarind (Tamarindus indica).

Plant Part Used: Fruit pulp, leaf, root, branch.

Dominican Medicinal Uses: Fruit pulp: aqueous extract, orally, for insomnia, hormonal imbalance, hot flashes and nightsweats. Leaf, bark, branch: decoction, orally, liver, kidney and prostate disorders and hepatitis.

Safety: Fruit pulp: widely consumed and generally considered safe; fruit or seed pods may contain an irritating, hypoglycemic alkaloid. Bark/leaves: insufficient information available.

Drug Interactions: Ibuprofen (fruit extract increases bioavailability).

Laboratory & Preclinical Data: In vivo: antidiabetic (seed extract), anti-inflammatory (plant extracts), colonic cell proliferation effects (fruit pulp).

In vitro: antioxidant (plant extract).

* See entry for Tamarindo in “Part 3: Dominican Medicinal Plant Profiles” of this book for more information, including references.... tamarindo

Carrot (Daucus carota). Plant Part Used: Root.Dominican Medicinal Uses: Root: juice, orally, for diabetes, anemia, cancer, improved vision, tumors, uterine fibroids, menopausal hot flashes, nourishment, to strengthen the blood, diarrhea, stomach ailments, gastrointestinal inflammation and liver disorders.Safety: Generally considered safe; root is widely consumed.Clinical Data: Human clinical trials: antioxidant, colonic motility, dental caries, hypocholesterolemic (root).Laboratory & Preclinical Data: In vivo: hepatoprotective (root).In vitro: antibacterial, antispasmodic, antitumor (seed extract or constituents), antioxidant, carotene bioavailability, hormonal effects (root).Nutrition: vitamin A precursors.* See entry for Zanahoria in “Part 3: Dominican Medicinal Plant Profiles” of this book for more information, including references.... zanahoria