Quinidine Health Dictionary

Quinidine: From 1 Different Sources


An alkaloid (see ALKALOIDS) obtained from cinchona bark and closely related in chemical composition and in action to QUININE. It is commonly used in the form of quinidine sulphate to treat cardiac irregularities such as supraventricular tachycardia and ventricular arrhythmias (see HEART, DISEASES OF).
Health Source: Medical Dictionary
Author: Health Dictionary

Alkaloids

Substances found commonly in various plants. They are natural nitrogenous organic bases and combine with acids to form crystalline salts. Among alkaloids, morphine was discovered in 1805, strychnine in 1818, quinine and ca?eine in 1820, nicotine in 1829, and atropine in 1833. Only a few alkaloids occur in the animal kingdom, the outstanding example being ADRENALINE, which is formed in the medulla of the suprarenal, or adrenal, gland. Alkaloids are often used for medicinal purposes. The name of an alkaloid ends in ‘ine’ (in Latin, ‘ina’).

Neutral principals are crystalline substances with actions similar to those of alkaloids but having a neutral reaction. The name of a neutral principal ends in ‘in’, e.g. digitalin, aloin.

The following are the more important alkaloids, with their source plants:

Aconite, from Monkshood.

Atropine, from Belladonna (juice of Deadly

Nightshade).

Cocaine, from Coca leaves.

Hyoscine, from Henbane.

Morphine, Codeine, from Opium (juice of

Poppy). Thebaine, Nicotine, from Tobacco. Physostigmine, from Calabar beans. Pilocarpine, from Jaborandi leaves. Quinidine, from Cinchona or Peruvian bark. Strychnine, from Nux Vomica seeds.... alkaloids

Cinchona Officinalis

Linn.

Synonym: C. robusta How.

Family: Rubiaceae.

Habitat: Cultivated in West Bengal and Tamil Nadu.

English: Crown or Loxa Bark.

Ayurvedic: Quinine.

Unani: Al-keenaa, Kanakanaa.

Action: Antimalarial, febrifuge, astringent, orexigenic, sapasmolytic. Also prescribed in amoebic dysentery, jaundice, atonic dyspepsia, night cramps. Sometimes causes gastric and intestinal irritation.

Key application: In peptic discomforts such as bloating and fullness, loss of appetite. (German Commission E.)

The bark contains alkaloids quinine (2.35-4.42%); quinidine (1.44-2.56%); cinchonine (0.10-0.66%); cinchoni- dine (0.49-0.89%) and other alkaloids, quinamine, javanine (0.14-0.63%).

The leaves contain quercetin, kaem- pferol and avicularin.

Quinine is antimalarial; quinidine is antiarrhythmic and cardiac tonic, also used in psychic treatments.

The bark shows potent inhibitory activity against polymorphonuclear leucocytes; the activity is attributed to the alkaloids of the bark. Cinchona may potentiate coumarin derivatives. In large doses, it is sedative to CNS and cardiac plexus.

Quinine is toxic at over 3 g, quini- dine at 1 g.

Related Cinchona sp.: C. calisaya Wedd. (Nilgiris and Sikkim); C. calisaya Wedd. var. ledgeriana How. (West Bengal, Khasi Hills and Tamil Nadu); and C. succirubra Pav. ex Klotz. (Nilgiris and Annamalis in Tamil Nadu, Sikkim and West Bengal).

The bark of all the species contain quinine, quinidine, cinchonine and cinchonidine and exhibit antimalarial activity. The alcoholic extract of C. ledgeriana Moens ex Trimen bark exhibits antibacterial activity against Gram-positive bacteria comparable to sodium penicillin. The extract, however, exhibits lesser activity than di- hydrostreptomycin sulphate against Gram-negative bacteria.... cinchona officinalis

Nardostachys Jatamansi

DC.

Synonym: N. grandiflora DC.

Family: Valerianaceae.

Habitat: Alpine Himalayas, Kumaon, Sikkim and Bhutan.

English: Spikenard, Musk-root.

Ayurvedic: Maansi, Jataamaansi, Bhuutajataa, Tapaswini, Sulo- mashaa, Jatilaa, Naladaa.

Unani: Sumbul-e-Hindi, Sambul-ut- Teeb, Naardeen-e-Hindi, Baalchhar.

Siddha/Tamil: Sadamanchil.

Action: Used as a substitute for Valerian. Tranquilizer, sedative, hypotensive. Used for the treatment of epilepsy, hysteria, convulsive affections, palpitation of heart and in intestinal colic. A decoction of powdered roots is prescribed as a home remedy for high blood pressure. It is used in dysmenorrhoea for pain relief and smooth menstrual flow. It is used in hair oil for arresting hair loss and greying of hair.

The Ayurvedic Pharmacopoeia of India recommends dry rhizomes in obstinate skin diseases, erysipelas, disturbed mental state and insomnia.

The rhizome is rich in sesquiter- penoids. The crude drug gave an oil (yield 2.5% v/w), which contains d- nardostachone, valeranone and jata- mansone as the major ketonic sesqui- terpenes. The oil potentiated phenobarbital narcosis in rats, reduced brain serotonin content and decreased the conditioned avoidance performance in cats.

Jatamansone was shown to exert tranquilizing effect in mice and monkeys. In rabbits, jatamansone was found to impair biosynthesis of serotonin in the brain leading to a reduction in brain level of 5-hydroxytrypta- mine. The degradation of serotonin was unaffected. The mode of action of jatamansone was thus in variance with that of reserpine which has direct action on the cell to liberate serotonin.

On the other hand, the alcoholic extract of the roots of Indian Nard caused an overall increase in the levels of central monamines, 5-hydroxy indole acetic acid and the inhibitory amino acids, gamma-aminobutyric acid, norepinephrine, dopamine and serotonin in rat brain.

In a clinical trial on hyperkinetic children, jatamansone showed significant reduction in hyperactivity and improvement in restlessness and aggressiveness, almost at par with D- amphetamine.

The volatile oil was found to be less active than quinidine in several tests. It did not counteract digitalis induced ventricular arrhythmias.

Jatamansone semicarbazone, a sesquiterpene ketone, was found to possess antiestrogenic activity.

N. jatamansi is also used in place of Muraa (Selinum tenuifolium Wall. ex DC.)

Dosage: Root—2-3 g powder; 5-10 g for infusion; 50-100 ml infusion. (API, Vol. I; CCRAS.)... nardostachys jatamansi

Cinchonism

n. poisoning caused by an overdose of cinchona or the alkaloids quinine, quinidine, or cinchonine derived from it. The symptoms are commonly ringing noises in the ears, dizziness, blurring of vision (and sometimes complete blindness), rashes, fever, and low blood pressure. Treatment with *diuretics increases the rate of excretion of the toxic compounds from the body.... cinchonism

Cinchona

Cinchona spp.

Rubiaceae

San: Cinchona, Kunayanah

Hin: Kunain Mal: Cinchona, Quoina

Tam: Cinchona

Importance: Cinchona, known as Quinine, Peruvian or Crown bark tree is famous for the antimalarial drug ‘quinine’ obtained from the bark of the plant. The term cinchona is believed to be derived from the countess of cinchon who was cured of malaria by treating with the bark of the plant in 1638. Cinchona bark has been valued as a febrifuge by the Indians of south and central America for a long time. Over 35 alkaloids have been isolated from the plant; the most important among them being quinine, quinidine, cinchonine and cinchonidine. These alkaloids exist mainly as salts of quinic, quinovic and cinchotannic acids. The cultivated bark contains 7-10% total alkaloids of which about 70% is quinine. Similarly 60% of the total alkaloids of root bark is quinine. Quinine is isolated from the total alkaloids of the bark as quinine sulphate. Commercial preparations contain cinchonidine and dihydroquinine. They are useful for the treatment of malarial fever, pneumonia, influenza, cold, whooping couphs, septicaemia, typhoid, amoebic dysentery, pin worms, lumbago, sciatica, intercostal neuralgia, bronchial neuritis and internal hemorrhoids. They are also used as anesthetic and contraceptive. Besides, they are used in insecticide compositions for the preservation of fur, feathers, wool, felts and textiles. Over doses of these alkaloids may lead to deafness, blindness, weakness, paralysis and finally collapse, either comatose or deleterious. Quinidine sulphate is cardiac depressant and is used for curing arterial fibrillation.

Distribution: Cinchona is native to tropical South America. It is grown in Bolivia, Peru, Costa Rica, Ecuador, Columbia, Indonesia, Tanzania, Kenya, Zaire and Sri Lanka. It was introduced in 1808 in Guatemala,1860 in India, 1918 in Uganda, 1927 in Philippines and in 1942 in Costa Rica. Roy Markham introduced the plant to India. The first plantation was raised in Nilgiris and later on in Darjeeling of West Bengal. The value of the tree was learnt by Jessuit priests who introduced the bark to Europe. It first appeared in London pharmacopoeia in 1677 (Husain, 1993).

Botany: The quinine plant belongs to the family Rubiaceae and genus Cinchona which comprises over 40 species. Among these a dozen are medicinally important. The commonly cultivated species are C. calisaya Wedd., C. ledgeriana Moens, C. officinalis Linn., C. succirubra Pav. ex Kl., C. lancifolia and C. pubescens. Cinchona species have the chromosome number 2n=68. C. officinalis Linn. is most common in India. It is an evergreen tree reaching a height of 10-15m. Leaves are opposite, elliptical, ovate- lanceolate, entire and glabrous. Flowers are reddish-brown in short cymbiform, compound cymes, terminal and axillary; calyx tubular, 5-toothed, obconical, subtomentose, sub-campanulate, acute, triangular, dentate, hairy; corolla tube 5 lobed, densely silky with white depressed hairs, slightly pentagonal; stamens 5; style round, stigma submersed. Fruit is capsule ovoid-oblong; seeds elliptic, winged margin octraceous, crinulate-dentate (Biswas and Chopra, 1982).

Agrotechnology: The plant widely grows in tropical regions having an average minimum temperature of 14 C. Mountain slopes in the humid tropical areas with well distributed annual rainfall of 1500-1950mm are ideal for its cultivation. Well drained virgin and fertile forest soils with pH 4.5-6.5 are best suited for its growth. It does not tolerate waterlogging. Cinchona is propagated through seeds and vegetative means. Most of the commercial plantations are raised by seeds. Vegetative techniques such as grafting, budding and softwood cuttings are employed in countries like India, Sri Lanka, Java and Guatemala. Cinchona succirubra is commonly used as root stock in the case of grafting and budding. Hormonal treatment induces better rooting. Seedlings are first raised in nursery under shade. Raised seedbeds of convenient size are prepared, well decomposed compost or manure is applied , seeds are broadcasted uniformly at 2g/m2, covered with a thin layer of sand and irrigated. Seeds germinate in 10-20 days. Seedlings are transplanted into polythene bags after 3 months. These can be transplanted into the field after 1 year at 1-2m spacing. Trees are thinned after third year for extracting bark , leaving 50% of the trees at the end of the fifth year. The crop is damaged by a number of fungal diseases like damping of caused by Rhizoctoria solani, tip blight by Phytophthora parasatica, collar rot by Sclerotiun rolfsii, root rot by Phytophthora cinnamomi, Armillaria mellea and Pythium vexans. Field sanitation, seed treatment with organo mercurial fungicide, burning of infected plant parts and spraying 1% Bordeaux mixture are recommended for the control of the diseases (Crandall, 1954). Harvesting can be done in one or two phases. In one case, the complete tree is uprooted, after 8-10 years when the alkaloid yield is maximum. In another case, the tree is cut about 30cm from the ground for bark after 6-7 years so that fresh sprouts come up from the stem to yield a second crop which is harvested with the under ground roots after 6-7 years. Both the stem and root are cut into convenient pieces, bark is separated, dried in shade, graded, packed and traded. Bark yield is 9000-16000kg/ha (Husain, 1993).

Properties and activity: Over 35 alkaloids have been isolated from Cinchona bark, the most important among them are quinine, quinidine, cinchonine, cinchonidine, cinchophyllamine and idocinchophyllamine. There is considerable variation in alkaloid content ranging from 4% to 20%. However, 6-8% yield is obtained from commercial plantations. The non alkaloidal constituents present in the bark are bitter glycosides, -quinovin, cinchofulvic, cinchotannic and quinic acids, a bitter essential oil possessing the odour of the bark and a red coloring matter. The seed contains 6.13% fixed oil. Quinine and its derivatives are bitter, astringent, acrid, thermogenic, febrifuge, oxytocic, anodyne, anti-bacterial, anthelmintic, digestive, depurative, constipating, anti pyretic, cardiotonic, antiinflammatory, expectorant and calcifacient (Warrier et al, 1994; Bhakuni and Jain, 1995).... cinchona

Quinine

An alkaloid (see ALKALOIDS) obtained from the bark of various species of cinchona trees. This bark is mainly derived from Peru and neighbouring parts of South America and the East Indies. Other alkaloids and acid substances are also derived from cinchona bark, such as QUINIDINE and cinchonine.

Quinine is generally used in the form of one of its salts, such as the sulphate of quinine, or dihydrochloride of quinine. All are sparingly soluble in water, much more so when taken along with an acid.

Action Quinine is a powerful antiseptic (see ANTISEPTICS). Its best-known action is in checking the recurrence of attacks of MALARIA, as it destroys malarial parasites in the blood. In fevers it acts as an antipyretic (see ANTIPYRETICS).

Among its side-effects are ringing in the ears, temporary impairment of vision, and sometimes disturbance of kidney function leading to renal failure.

Uses The most important use of quinine is its original one in malaria, attacks of which it quickly cuts short or prevents altogether. It has been largely replaced by more e?ective and less toxic antimalarial drugs; however, development of malarial parasites resistant to newer drugs has revived the use of quinine. For intravenous injection, when this is necessary in cases of malaria, a soluble form of quinine, the dihydrochloride, is used. Quinine can also be given in combination with other antimalarial drugs on medical advice. The drug is sometimes used in the treatment of cramps.... quinine

Ectopic Beat

(extrasystole) a heartbeat due to an impulse generated somewhere in the heart outside the sinoatrial node. Ectopic beats are generally premature in timing; they are classified as supraventricular if they originate in the atria and ventricular if they arise from a focus in the ventricles. They may be produced by any heart disease, by nicotine from smoking, or by caffeine from excessive tea or coffee consumption; they are common in normal individuals. The patient may be unaware of their presence or may feel that his heart has ‘missed a beat’. Ectopic beats may be suppressed by drugs such as quinidine, propranolol, and lidocaine; avoidance of smoking and reduction in excessive tea or coffee intake may help. See arrhythmia.... ectopic beat



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