Snake Rauwolfia (Rauwolila serpentina Benth. Snake Rauwolfia (serpentina) - (Rauwolfia serpentina Benth.). Kutrov family - Apocynaceae A characteristic feature of ajmaline are
Rauvolfia (Rauvolfia serpentina Benth.) is a perennial shrub; grows in South and Southeast Asia. In medicine, rauwolfia root is used, which contains alkaloids (see) and rescinamine, which have a sedative and hypotensive effect, ajmaline and serpentine, which have antiarrhythmic properties, and other alkaloids.
Raunatin(Raunatinum;) contains the sum of alkaloids from the roots of rauwolfia; has hypotensive, sedative and antiarrhythmic effects.
Used for ; prescribed orally at 0.002-0.012 a per day for 3-4 weeks. Release form: tablets of 0.002 g. See also Antihypertensive drugs.
Rice. 58. Rauwolfia serpentine (left - root).
Rauwolfia (snake rauwolfia; Rauwolfia, or Rauvolfia, serpentina Benth) is a perennial evergreen shrub 0.2-0.6 m high with a straight stem and vertical rhizome, turning into a thinning, wrinkled, brown root up to 40 cm long; belongs to the kutrov family (Apocynaceae Lindl.). Grows in South and Southeast Asia (India, Ceylon, Java, Malay Peninsula). The botanical description of Rauwolfia belongs to the German physician Rauwolf (L. Rauwolf, 16th century). In medicine, rauwolfia root is used, which is dug up in the 3-4th year of the plant’s life and dried. About 40 alkaloids have been isolated from rauwolfia, divided according to the characteristics of their chemical structure and basicity into three groups: tertiary indole (weak) bases - reserpine (see), rescinamine, yohimbine; tertiary indoline bases (medium strength) - aymalinide; quaternary anhydronium bases (strong) - serpentine, etc. Reserpine is also found in other species of rauwolfia (R. canescens Linn., R. micrantha Hook, R. tetraphylla L.). In terms of pharmacological properties and therapeutic effectiveness, the most important among rauwolfia alkaloids are reserpine and rescinamine, which have a sedative and hypotensive effect, as well as ajmaline and serpentine, which have an antiarrhythmic effect.
Aymalin, unlike reserpine, does not have a tranquilizing effect, but has the ability to reduce myocardial excitability and suppress ectopic impulse formation, prolong the refractory phase and inhibit conduction function.
Aymalin used for ventricular and atrial extrasystole, sinus tachycardia, various forms of paroxysmal tachycardia, Wolff-Parkinson-White syndrome. The drug is prescribed intravenously, intramuscularly and orally. For parenteral administration, a single dose is 50 mg (the contents of one ampoule), a daily dose is 100-150 mg. 1-2 tablets (50-100 mg) are prescribed orally 3-4 times a day for 1-3 weeks. Aymalin is contraindicated in cases of severe damage to the conduction system of the heart, sudden organic changes in the myocardium, severe heart failure and hypotension.
A number of total alkaloid preparations of rauwolfia are also used in medicine (Gendon, Giuline, Raudixin, Raupina, Rauwiloid, Rauwoldin, Rivadescin, Wolfina, etc.).
Raunatin(domestic production) - an analogue of hendon, contains mainly the alkaloids reserpine, serpentine and ajmaline and has a hypotensive, antiarrhythmic and, to a lesser extent, sedative effect. Raunatin is mainly used for hypertension, especially in stages I and II. The drug is produced in tablets containing 2 mg of the sum of rauwolfia alkaloids; Prescribe 1-2 tablets per day after meals, gradually increasing the daily dose to 5-6 tablets (10-12 mg). After the therapeutic effect is achieved, the dose is gradually reduced to 1-2 tablets. The course of treatment usually lasts 3-4 weeks. The hypotensive effect of total rauwolfia preparations occurs more gradually than from reserpine; their side effects are much less pronounced.
See also Antihypertensives.
Rauwolfia serpentina Benth.
Family Cutraaceae -
Arocynaceae
Subshrub up to 1 m tall. The rhizome is vertical, 0.2-0.4 m long, with numerous roots. The rhizome and roots are woody, grayish-rusty in color. Leaves are short-petiolate, whorled, 3-5 in a whorl, less often opposite or alternate, oblong-elliptic, 8-18 cm long. The flowers are white or pink, collected in apical, less often axillary, umbellate inflorescences, reaching 3-5 cm in diameter. The fruit consists of two drupes, fused to the middle, ovoid, slightly flattened, dirty purple. The fruits ripen in March-September.
Spreading. It grows wild in India, Thailand, Indochina, Ceylon, Java, the Malay Peninsula, and Indonesia. Grows on the edges of tropical rainforests.
Medicinal raw materials. Rauwolfia root - Radix Rauwolfiae (Gen. radicis Rauwolfiae).
Raw materials are imported into the CIS and alkaloids are obtained from them.
Chemical composition. Rhizomes and roots contain more than 20 indole alkaloids (1-2%), of which reserpine and resciniamine have the greatest medicinal value.
Drugs. Reserpine - Reserpinum. An alkaloid found in rauwolfia plants. For hypertension in the early stages, 0.05-0.1 mg is usually prescribed 2-3 times a day. If well tolerated, the dose can be increased to 1 mg. If the hypotensive effect does not occur within 10-14 days, the drug is discontinued. Once the effect is achieved, the dose is gradually reduced to 0.5-0.2-0.1 mg per day. Treatment with maintenance doses is carried out in courses of 2-3 months, if necessary 3-4 times a year, under the supervision of a doctor.
Reserpine can be prescribed together with other antihypertensive drugs; in particular, the combination of reserpine with dichlorothiazide is effective.
In psychiatry and neurology, reserpine is used for neuropsychiatric disorders caused by high blood pressure. With psychomotor agitation in patients with schizophrenia, with manic agitation as part of circulatory psychosis, the circulatory form of schizophrenia, with a depressive-agitated state. In patients with presenile psychosis, reserpine is also effective, but it is inferior in activity to phenothiazine and butyrophenone derivatives. To enhance effectiveness in the treatment of schizophrenia, reserpine can be used in combination with other neutroleptic drugs. Reserpine is also used to treat alcoholic psychosis.
For mental illnesses, reserpine is prescribed orally in the first days from 0.25 to 2 mg, then the dose is gradually increased to 10-15 mg per day. The course of treatment for mental illness lasts up to 3-6 months. After a course of inpatient treatment, the patient is prescribed maintenance therapy - 0.5-1 mg 2-3 times a day. Higher doses for adults orally: single 0.002 g (2 mg), daily - 0.01 (10 mg).
Children are prescribed, depending on age, from 0.1 to 0.4 mg per day, in 2-4 doses.
Raunatin - Raunatinum. A preparation containing a sum of alkaloids from the roots of Rauwolfia serpentine or other species. Contains reserpine, serpentine, ajmaline and other alkaloids, the total content of which (in terms of dry matter) is at least 90%. In terms of its hypotensive effect, raunatin is not inferior to reserpine, although its effect on the central nervous system is less pronounced than that of reserpine. Raunatin also has an antiarrhythmic effect and has a calming effect on the central nervous system. Prescribed orally 1 tablet containing 0.002 g (2 mg) of the total alkaloids at night. On the 2nd day, take 1 tablet 2-3 times a day, on the 3rd day - up to 4-6 tablets per day. Take the drug after meals. After the onset of the therapeutic effect (usually after 10-14 days), the dose is gradually reduced to 1-2 tablets per day. The course of treatment usually lasts 3-4 weeks, but the drug can be used for a longer period of time in a maintenance dose (1 tablet per day). Treatment should be carried out under the supervision of a physician. Tablets of the drug containing 0.002 g (2 mg) of the drug are stored in well-closed jars and dark glass bottles. List B.
Under the name "Rauvazan" a similar drug is produced in Germany (in a package of 100 tablets).
Aymalin - Ajmalinum. An alkaloid found in snake and other types of rauwolfia. The alkaloid is an effective remedy for stopping attacks of atrial fibrillation and paroxysmal tachycardia (V. X. Vasilenko et al., 1973; V. L. Doshchitsin, 1968; I. G. Fomina, 1973). The drug is also effective for rhythm disturbances associated with intoxication with digitalis drugs. The drug is prescribed intravenously, intramuscularly and orally. Particularly effective when administered parenterally.
To relieve acute attacks of atrial fibrillation and paroxysmal tachycardia, 0.05 g (2 ml of 2.5% solution) in 10 ml of isotonic sodium chloride solution or 5% glucose solution is administered intravenously. Inject slowly over 7-10 minutes. If necessary, you can re-introduce another 0.05 g during the day. You can administer the drug dropwise: 2-4 ml of a 2.5% solution in 100-200 ml of isotonic sodium chloride solution. 0.05 g (2 ml of 2.5% solution) is administered intramuscularly every 8 hours up to 0.15 g per day (i.e., up to three times). If necessary, the drug is administered for several days in a row. When a therapeutic effect is achieved from parenteral administration, they switch to taking the drug orally, 1-2 tablets (0.05-0.1 g) 3-4 times a day for 1-3 weeks.
Pulsnorma - Pulsnorma. An antiarrhythmic drug produced in Yugoslavia, in the form of dragees containing ajmaline 0.03 g, sparteine sulfate 0.025 g, antazoline hydrochloride 0.05 g and phenobarbital 0.05 g. The addition of sparteine sulfate to ajmaline enhances the antiarrhythmic effect. Sparteine is an alkaloid with the same structure as pachycarpine.
Pharmacological properties. Rauwolfia alkaloids have valuable pharmacological properties. Reserpine, and to a lesser extent resciamine, have a sedative and hypotensive effect.
Reserpine is one of the main sympatholytic substances. Under its influence, catecholamines are released from the depot of presynaptic nerve endings. They are subject to the inactivating action of monoamine oxidase, which leads to a decrease in their release into the synaptic cleft and a weakening of adrenergic effects, primarily on adrenergic receptors of blood vessels. Under the influence of reserpine, the content of norepinephrine and dopamine in the central nervous system decreases. The hypotensive effect develops gradually, although it is expressed quite clearly. It persists even after discontinuation of reserpine. Along with a decrease in blood pressure, an improvement in kidney function is observed: an increase in renal blood flow, and increased glomerular filtration.
Aymalin reduces myocardial excitability, inhibits atrioventricular and intraventricular conduction, and somewhat inhibits the automatism of the sinus node, while exhibiting antiarrhythmic properties.
Therapeutic and prophylactic use. The Indians used this plant as a remedy against the bites of poisonous snakes and scorpions, as well as to obtain sedative and hypnotic drugs.
Rauwolfia preparations are widely used in the treatment of hypertension and mental illness.
Side effects, contraindications. In small doses, reserpine does not cause side effects. With increased sensitivity and with increasing doses, skin rash, stomach pain, diarrhea, bradycardia, weakness, dizziness, shortness of breath, nausea, vomiting, and nightmares may appear. With prolonged use, parkinsonism may occur.
In patients with bronchial obstruction, reserpine can cause an acute attack of bronchospasm. Bronchospasm is relieved with atropine.
During a course of treatment, patients with mental illness may develop feelings of anxiety, restlessness, persistent insomnia, and depression.
The stimulating effect of reserpine on the development of breast cancer, obtained in experiments on rats, was not confirmed. Reserpine enhances the secretion of prolactin. Careful clinical and experimental studies (N.A. Tikhonova et al., 1979) led to the denial of the idea that breast cancer in humans can occur under the influence of reserpine.
In case of side effects, reduce the dose of the drug or temporarily discontinue it. For stomach pain and diarrhea, anticholinergic substances are prescribed. With the development of extrapyramidal disorders, cyclodol, tropacin and other antiparkinsonian drugs are used. In some patients, the drug causes the development of drowsiness and general weakness, which cannot be ignored, especially in an outpatient setting.
Reserpine is contraindicated in severe organic cardiovascular diseases with symptoms of decompensation and severe bradycardia, nephrosclerosis, cerebral sclerosis, gastric and duodenal ulcers.
Raunatin usually does not cause side effects. Patients tolerate it better than reserpine. In some cases, swelling of the mucous membranes of the nose, sweating, and general weakness are observed. In patients with angina, heart pain sometimes increases. Side effects disappear when the dose is reduced or after a short break (1-3 days) in taking the drug.
Ajmaline is usually well tolerated. Some patients experience hypotension, general weakness, nausea, and vomiting. With intravenous administration - a feeling of heat. Contraindications, especially for intravenous administration, are severe damage to the cardiac conduction system, pronounced sclerotic and inflammatory changes in the myocardium, grade III circulatory failure, and severe hypotension. When ajmaline is administered to patients with acute myocardial infarction, a decrease in blood pressure and conduction disturbances are possible.
Recipes.
Rp.: Tab. Ajmalini 0.05 N. 20
D.S. 1 tablet 3 times a day
Rp.: Sol. Ajmalini 2.5% 2 ml
D.t.d. N. 10 in.ampull.
S. 2 ml intravenously in 10 ml of 5% glucose solution (administer slowly)
Rp.: Tab. Reserpini 0.0001 N. 50
D.S. 1 tablet 2-3 times a day after meals.
Rp.: Tab. Raunatini 0.002 N.D.S. 1 tablet 1-3 times a day after meals.
Rauwolfia serpentina- a subshrub up to 1 m high, of the kutra family (Arosupaceae). The leaves are short-petiolate, obovate or lanceolate, thin, glabrous, shiny, 7.5-17.5 cm long. The flowers are white or pinkish, collected on the tops of the branches or in the axils of the leaves in umbellate inflorescences. Grows medicinal plant in India, Sri Lanka. The roots and rhizomes contain up to 20 indole alkaloids in an amount of 1-2%. Among them are reserpine C 33 H 40 O 9 N 2, rescinamine C 35 H 42 O 9 N 2, ajmaline (rauwolfine) C 20 H 26 O 2 N 2, ajmalicin (raubazin) C 21 H 24 O 3 N 2, isoaimaline ( isorauwolfine) C 20 H 26 O 2 N 2, rauhimbine (coriantine) C 21 H 26 O 3 N 2, isorauhimbine C 21 H 26 O 3 N 2, rauwolfine C 19 H 24O 2 N 2, reserpilin C 23 H 28 O 5 N 2, reserpinine C 22 H 26 O 4 N 2, sarpagine (raupin), C 19 H 22 O 2 N 2, serpentine C 21 H 20 O 3 N 2, serpentine C 21 H 22 O 3 N 2, serpine C 21 H 26 O 3 N 2, 3-epi-a-yohimbine C 21 H 26 O 3 N 2, alloihimbine C 21 H 26 O 3 N 2, 3-yohimbine, thebaine, papaverine, chaindrin. The most studied is reserpine.
Pharmacological properties
Reserpine has a hypotensive effect that develops slowly and lasts several hours. This effect is due mainly to the peripheral impatolytic properties of the drug. Reserpine slows the heart rate without changing or increasing cardiac output. The drug also has sedative properties. Large doses of reserpine cause sleep close to physiological. It deepens breathing, constricts the pupil, lowers body temperature and metabolism. Reserpine reduces the content of norepinephrine in tissues. The sedative effect of reserpine is associated not so much with a change in the total content of norepinephrine, but with the depletion of the functionally active fractions of this catecholamine. Reserpine increases the resistance of animals to hypoxia. The drug inhibits interoceptive reflexes to blood pressure and breathing from the central segment of the vagus nerve, mechanoreceptors of the carotid sinus, pericardium, large and small intestines and bladder. The least resistant to the action of reserpine are reflexes from the carotid sinus and the central segment of the vagus nerve. The reflex from the tibial nerve is not inhibited. The inhibition of some autonomic reflexes does not depend on the blockade of efferent pathways and receptor formations, but is apparently associated with the effect of the drug on the central apparatus of blood circulation regulation. Reserpine has a biphasic effect on the tonic and reflex activity of the sympathetic nervous system, as well as on vasomotor reflexes. The first depressive phase of the action of reserpine on the centers of vasomotor regulation is due to the excitation of central inhibitory monoaminergic mechanisms by the released monoamines. This phase coincides with an increase in the content of free, functionally active forms of monoamines in the brain. The second phase of action after the administration of reserpine develops after 2 1/2-4 hours and is characterized by an increase in tonic activity and vasomotor reflexes and the complete elimination of reflex inhibition in the sympathetic nerves. This phase coincides in time with the period of depletion of the labile supply of monoamines in the brain tissue (N.V. Kaverina, Yu.B. Rozanov). In addition to crystalline reserpine, total preparations of rauwolfia, in particular rauwolfia, are used in medical practice. In terms of hypotensive effect, it is inferior to reserpine. To achieve the same hypotensive effect, approximately 4 times larger doses of this drug are required compared to reserpine. The hypotensive effect of raunatin develops more slowly than when using reserpine. In the mechanism of action of this drug, along with the sympatholytic activity characteristic of reserpine, peripheral adrenergic and antispasmodic properties play an important role. One of the rauwolfia alkaloids, ajmaline, has antiarrhythmic activity. This effect is associated with the stabilization of the membranes of myocardial cells and a decrease in their excitability, prolongation of the refractory phase of the heart and a slowdown in the conduction of impulses through the conduction system.
Application in medicine
Reserpine used for hypertension. It lowers blood pressure and slows the pulse, especially if it is rapid. The therapeutic effect of reserpine is fully manifested 2-6 days after starting the drug. At the same time, reserpine has a calming effect on the patient. The hypotensive effect of raunatin in hypertension is expressed in stages I and II of the disease. The action of raunatin differs from reserpine in having fewer side effects.
Under the influence of the drug, not only does blood pressure decrease, but also headaches, dizziness, irritability decrease, and sleep improves. The effectiveness of raunatin in some cases is superior to other drugs used as antihypertensive agents. Raunatin relieves arrhythmia, restores the processes of excitation and conduction in the heart muscle.
Possible side effects: swelling of the mucous membranes of the nose, sweating, weakness, increased pain in the heart area in patients with angina pectoris. These phenomena disappear when the dose is reduced or after a 2-3-day break from taking the medication. Rauwolfia preparations can provoke sinus bradyarrhythmia in cases of disturbances in the automatism of the sinus node and atrioventricular conduction and cause the phenomenon of specific hypertrophic gastritis; therefore, they are contraindicated for gastric and duodenal ulcers. Complications include depression, increased parkinsonism and tremor.
Drugs
Reserpine (Reserpinum) (A). Treatment begins with the appointment of small doses - OD-0.3 mg / day, gradually increasing the dose to 0.5-2 mg / day. If the hypotensive effect does not occur within 10-14 days of treatment, the drug is discontinued. If blood pressure decreases, the dose is reduced to 0.2-0.5 mg/day and continued for a month under medical supervision. Reserpine in a dose of up to 1 mg/day together with cardiac glycosides is also prescribed for functional disorders of cardiac activity accompanied by tachycardia. The drug is also prescribed for vegetative dystonia, with increased tone of the sympathetic system and as an adjuvant for thyrotoxicosis. Reserpine is rarely used in the treatment of mental illness.
Reserpine is contraindicated in severe disorders of the cardiovascular system with symptoms of decompensation, cerebral sclerosis, nephrosclerosis, hypotension and gastric ulcer. Available in tablets of 0.1 and 0.25 mg. Store in a cool place, protected from light.
Raunatinum (B). Total alkaloids of Rauwolfia serpentine. Brownish-yellow powder, odorless, bitter in taste. For hypertension stages I and II, on the 1st day of treatment, a dose of 0.002 g (1 tablet) is prescribed after meals, on the 2nd day - 1 tablet 2 times a day, on the 3rd day - 3 tablets, on the 4th day - 4 tablets, on the 5th day - 5 tablets, on the 6th day 6 tablets. After 10-14 days, when the hypotensive effect usually occurs, the dose of the drug is gradually reduced to 1-2 tablets per day. Duration of treatment is 20-30 days. The drug is often prescribed for a long time at a maintenance dose of 0.002 g at night. Raunatin is produced in tablets of 0.002 g, stored in tightly sealed dark glass jars. A similar drug, rauvazan, is produced in the GDR; approved for use in the USSR. Rausedil is available in tablets and ampoules for intramuscular administration for hypertensive crises and psychoses with symptoms of agitation. Ajmalinum (B) is used for arrhythmias of various types: paroxysmal supraventricular and ventricular tachycardias, tachysystolic atrial fibrillation. It is prescribed orally in tablets of 0.05 g, but the drug is especially effective when administered parenterally: intramuscularly or intravenously by drip or stream.
MINISTRY OF EDUCATION AND SCIENCE OF RUSSIA
"Maikop State Technological University"
Faculty of Pharmacy
Department of Pharmacy
Coursework on pharmacognosy
Rauwolfia serpentine and lesser periwinkle are sources of antihypertensive drugs
Completed by: third year student,
full-time education
F-31 groups
Maleeva V.E.
Checked:
teacher of the department
pharmacy
Artemyeva V.V.
Maykop, 2011
I. Introduction
II. Literature review
2.1 General characteristics of hypertension
2 Classification of antihypertensive drugs
III. Characteristics of plants used to obtain antihypertensive drugs
1 Characteristics of Rauwolfia serpentine
2.5 Characteristics of Vinca minor
IV. Conclusion. List of used literature
I. Introduction
The chosen topic is an interesting and relevant direction for course design.
Hypertension is one of the most common diseases of the cardiovascular system and is one of the most acute and unresolved problems.
Despite numerous medical studies in different countries and the synthesis of new therapeutic drugs, the incidence of essential hypertension does not decrease. In the last 20-30 years, in some countries, the incidence of hypertension has increased sharply and amounted to up to 40% of the working population, i.e. has become an epidemic. Moreover, men more often suffer from hypertension before the age of 40, and women after 40; by the age of 50, the ratio of sick women and men levels off.
In our age of information explosion, patients are well aware of the drugs used to treat a wide variety of diseases, including hypertension. Such knowledge will not harm if a person meaningfully follows the doctor’s orders and does not, according to his own understanding, strive to obtain and take medications that are recommended, for example, to a colleague. After all, even the most used and widely known drugs are prescribed by the doctor to his patient in varying dosages, replaced with other medications depending on his condition and many other circumstances, which only a specialist can evaluate. In addition, patients react differently to antihypertensive drugs, so patience is required not only from the doctor, but also from the patient to select the dose and the best combination of medications that provide the necessary reduction in blood pressure. This problem is also relevant for drugs obtained from the alkaloid-bearing plants Rauwolfia serpentina and Vinca minor, since their improper use leads to disruption of the normal functioning of internal organs, the appearance of parkinsonism and other undesirable effects associated with improper use of drugs.
Modern treatment should be aimed not only at eliminating the symptoms of the disease, but also at preventing the progression of target organ damage and the occurrence of complications.
In modern medicine, preparations of Rauwolfia serpentina and Vinca minor as effective remedies for hypertension have become known since 1953. In the 50s of the current century, alkaloids were isolated from them, among which substances with exceptionally high sedative and hypotensive activity were discovered; they are still active today widely used in therapy and research. It was revealed that treatment with reserpine increases tolerance to physical activity, improves well-being and mood, and reduces reactive anxiety, emotional lability and tension in patients. These pharmacological properties are of great importance for the treatment of arterial hypertension, since chronic emotional stress and neuropsychic overload play an important role in the development and stabilization of this disease. Vinca minor preparations dilate the coronary vessels of the heart and blood vessels of the brain.
An important goal of this course project is to deepen and expand knowledge on this topic. The study of the production of preparations from medicinal plant raw materials of Rauwolfia serpentina and Vinca minor, its procurement, acceptance, and processing are carried out by different specialists. They must have a good understanding of the regulatory and technical requirements for the quality of raw materials, know their external signs, conditions and shelf life of raw materials and the correct use of this group of drugs. This work summarizes the literature data and briefly covers these issues. . Literature review
2.1 General characteristics of hypertension
Hypertension is a disease whose main symptom is an increase in blood pressure caused by neurofunctional disorders of vascular tone. Hypertension affects men and women equally. The disease usually begins after 40 years of age. This is a very common pathology. It is called a disease of the autumn of life, although in recent decades hypertension has become much younger.
Hypertension is one of the causes of disability and mortality in patients with disorders of the cardiovascular system.
Causes of hypertension
One of the reasons is prolonged and frequent neuropsychic stress, prolonged stress. Very often, hypertension occurs in people whose work is associated with constant emotional stress. It often affects people who have suffered a concussion.
The second reason is hereditary predisposition. Usually, when interviewing patients, it is possible to identify the presence of relatives with the same disease.
One of the important causes of hypertension is physical inactivity. Age-related changes in the body (in particular, the central nervous system) also influence the appearance and development of symptoms of this disease. The high incidence of hypertension among older people is due to changes in blood vessels due to the addition of atherosclerosis. There is a definite connection between these diseases. Hypertension contributes to increased development and progression of atherosclerosis. This combination is dangerous because with severe vasospasm, blood flow to the organs (brain, heart, kidneys) is insufficient. With excessive spasm and the presence of plaques on the walls of blood vessels, blood may stop circulating through the artery. In this case, a stroke or myocardial infarction occurs.
Also of some importance are excessive consumption of table salt (namely sodium, which is part of this salt), smoking, alcohol abuse, and excess body weight, which increases the load on the cardiovascular system.
The main links in the occurrence of hypertension are:
· disruption of the processes of excitation and inhibition in the central nervous system;
· hyperproduction of substances that increase blood pressure. One of them is the stress hormone adrenaline. In addition, renal factor is also isolated. The kidneys produce substances that can raise and lower blood pressure. Therefore, when signs of hypertension appear, the patient needs to check his kidney function;
· contraction and spasm of the arteries.
Blood pressure (systolic and diastolic)
Pressure should be measured at rest - physical and emotional. The upper (systolic) pressure corresponds to the moment of contraction of the heart muscle, and the lower (diastolic) pressure corresponds to the moment of relaxation of the heart (Table 1.). In young healthy people, normal blood pressure is defined as 110/70 - 120/80 mmHg. Art. But, taking into account the dependence of blood pressure figures on age, individual characteristics, training, we can call the limits 125/65 - 80 mm Hg. Art. in men and 110 - 120/60 - 75 mm Hg. Art. among women. Blood pressure increases with age; for middle-aged people, normal figures are close to 140/90 mmHg. Art. The main symptom is an increase in blood pressure to 140 - 160/90 mm Hg. Art.
Table 1. Blood pressure indicators in normal conditions and with hypertension of varying severity.
Symptoms of hypertension
Headache is one of the most common manifestations of high blood pressure. This symptom is caused by cerebral vascular spasm. In this case, tinnitus, flashing “spots” before the eyes, blurred vision, weakness, decreased performance, insomnia, dizziness, heaviness in the head, and palpitations often occur. These complaints in the early stages of the disease are neurotic in nature. When examining the patient, heart murmurs, rhythm disturbances, and expansion of the borders of the heart to the left are revealed. In later stages, heart failure may occur due to overwork of the heart muscle due to high blood pressure.
Hypertensive crisis is one of the most dangerous manifestations of hypertension. With a sharp increase in pressure, all of the above symptoms may be accompanied by nausea, vomiting, sweating, and decreased vision. Crises can last from several minutes to several hours. In this case, patients are usually excited, tearful, and complain of palpitations. Red spots often appear on the chest and cheeks. There is an increase in heart rate. The attack may end with profuse urination or loose stools. Such crises are characteristic of the early stages of hypertension; they are more often observed in women during menopause, after emotional stress, and when the weather changes. They often occur at night or in the afternoon. There are other types of hypertensive crises. They have a more severe course, but develop gradually. Their duration can reach 4 - 5 hours. They occur in later stages against the background of high initial blood pressure. Crises are often accompanied by brain symptoms: speech impairment, confusion, changes in sensitivity in the limbs. In this case, patients complain of severe pain in the heart.
Diagnostics
To establish the correct diagnosis when identifying this disease, it is important to interview the patient in order to identify hereditary predisposition. Information about the state of the cardiovascular system of close relatives - parents, siblings - is very important. Another important link in the diagnosis is the patient’s complaints of repeated increases in blood pressure. To make a correct diagnosis, regular measurement of the patient's blood pressure is necessary. A number of studies are also carried out in the clinic: electrocardiography (ECG), fundus examination by an ophthalmologist, general blood and urine tests. Those patients who do not have sufficient effect from the prescribed treatment, as well as patients with suspected secondary hypertension, are sent to specialized hospitals to exclude diseases of the kidneys, thyroid gland, and tumors.
2 Classification of antihypertensive drugs
Antihypertensive drugs are drugs of various pharmacological groups that cause a decrease in blood pressure and are used mainly for pathological increases in systemic pressure.
The main task of treating patients with hypertension is to normalize systolic and diastolic pressure in order to prevent a number of complications, such as stroke, myocardial infarction, heart and kidney failure.
Classification of antihypertensive drugs. Drugs that affect the adrenergic innervation of the heart.
Drugs with a sedative effect.
· sedatives;
· sleeping pills (in small doses);
· tranquilizers.
2. Centrally acting antihypertensive drugs.
· clonidine
· methyldopa
3. Ganglioblockers.
· hygronium
· pyrylene
benzohexonium
4. Sympatholytics.
· octadine
· reserpine
· phentolamine
· tropafene
· prazosin
6. β-blockers.
· labetalol
talinolol
· metoprolol. Myotropic drugs.
1. Arterial vasodilators.
· apressin
Mixed type vasodilators.
sodium nitroprusside
3. Drugs with different mechanisms of action that have myotropic activity.
Dibazol
· magnesium sulfate
· papaverine
· aminophylline. Potassium channel activators.
minoxidil
Diazoxide Calcium channel blockers.
· phenigidine
Diltiazem Diuretics.
furosemide
dichlorothiazide
· spironolactone. Drugs affecting the renin-angiotensin-aldosterone system.
Angiotensin-converting enzyme (ACE) inhibitors.
captopril
· enalapril
ramipril
Angiotensin receptor blockers.
losartan
candesortan
· tazosartan
· irbesartan
Despite the successes of synthetic chemistry, plant preparations still serve as the main means for the treatment and prevention of cardiovascular diseases.
Characteristics of plants used to obtain antihypertensive drugs
1 Characteristics of Rauwolfia serpentine
Plant. Snake Rauwolfia (serpentina) - (Rauwolfia serpentina Benth.), Kutra family - Apocynaceae.
Subshrub 0.2-1 m tall, with milky sap. The rhizome is vertical, 20-40 cm long, with numerous roots. The rhizome and roots are woody, gray-rusty in color. The stem is ascending, usually not branched, covered with whitish bark with a few lentils. Leaves are short-petiolate, whorled, 3-5 in a whorl, less often opposite or alternate, oblong-elliptic, obovate or lanceolate, pointed at the apex, narrowed at the base into a petiole, thin, glabrous, shiny, light green above, paler below , 7.5-17.5 cm long. The flowers are white or pink, collected in apical, less often - axillary umbrella-shaped inflorescences with a diameter of 2.5-5 cm. The bracts are very small, the calyx remaining with the fruit is five-parted. Its lobes are almost free, sharp, from triangular to lanceolate, 1.3-3 mm long. The calyx and pedicels are bright red. The corolla is tubular, with a five-petalled bend, glabrous on the outside, hairy on the inside; its tube is 11-16 mm long, slightly swollen above the middle. The lobes are rounded-ovate, 1.5-3.5 mm long, slightly wavy along the edges. The stamens, 5 in number, are attached to the corolla tube at the site of swelling. The pistil consists of 2 free carpels connected by a thread-like style 8 mm long, ending in a well-developed cylindrical stigma. The fruit consists of 2 drupes fused to the middle (Fig. 1.). The drupes are obovate or ovate, slightly flattened, dirty purple. The seeds are round-ovate, asymmetrical, 6 mm long, compressed at the base, yellowish or grayish, reticulate-tubercular.
In the wild, Rauwolfia serpentine is found in the tropical regions of the Himalayas, Sikkim, Northern and Central Bengal, Peru, the Deccan Plateau, Sri Lanka and Java.
Medicinal plant raw materials of Rauwolfia serpentinae - roots of Rauwolfiae serpentinae radices.
Usually 3-4 year old plants are harvested. Rauwolfia roots are harvested during the fruiting phase, both from wild and cultivated plants. They are dug up, cleared of soil and cut into pieces up to 20 cm long (Fig. 2). Dry in a well-ventilated place. The roots are covered with brown cork with longitudinal grooves. The bark is not wide and can peel off in the raw material.
Loss of bark leads to a decrease in the content of alkaloids, so pieces of roots without bark are a defect in the raw material. The wood is brittle, yellowish, the fracture is even (no fibers). The smell is unpleasant. The taste is bitter (according to modern concepts, the taste of potent raw materials is not determined during its analysis). The raw materials are stored as potent (List B).
Microscopy. Cork has a characteristic layering pattern - alternating layers of smaller and larger cells. In the phloem there are single secretory cells with brown resinous contents. Starch grains are often found in parenchyma cells, and prismatic crystals of calcium oxalate are less common. There are no mechanical elements in the bark (difference from the roots of other types of rauwolfia) (Fig. 3.)
Fig.3. Microscopy of Rauwolfia serpentine.
A - fragment of a cross section of the outer part of the root - periderm;
B - fragment of a cross section of a root in the area of wood: 1 - vessel;
B - phloem parenchyma cells with starch grains and prismatic crystals of calcium oxalate.
Chemical composition. Roots and rhizomes contain up to 2% alkaloids, indole derivatives: reserpine, serpentinine, ajmaline, ajmalicin, rescinamine, isoaimaline, rauhimbine, isorauhimbine, rauwolfinine, reserpilin, reserpenine, sarpagin, serpentine, serpine, alloihimbine, thebaine, papaverine, chaindrine. The root bark contains 90% of the total alkaloids in the roots. The content of alkaloids depends on the geographical location of the plants and the time of year. Harvested in December from Assam, India, Rauwolfia roots have the highest percentage (2.57) of alkaloids. The age of the plant does not affect the accumulation of alkaloids. In addition, calcium oxalate, sterol, resins, and starch were found in the roots.
Leaves and stems contain alkaloids, carotenoids, flavonoids, milky juice (rubber).
Qualitative and quantitative analysis of the alkaloid reserpine.
Reserpine - sparingly soluble in water and petroleum ether, soluble in ethyl alcohol in a ratio of 1: 2000, in methyl alcohol 1: 400, in chloroform 1: 6. Dissolved in acetic acid. Melting point 261-265 (with decomposition). With mineral (HC1, HNO3, H2SO4, HClO4) and some organic (oxalic, picric) acids, reserpine gives easily hydrolyzed salts. Easily decomposes under the influence of light, air and oxidizing agents.
Isolation is carried out with acidified water, it is recommended to use 10% acetic acid, and insulation is carried out for 24 hours in a place protected from light. Extraction is carried out with chloroform at pH 4.0 and 8.5 (reserpine and metabolites), and purification is carried out using paper electrophoresis.
High-quality detection.
General alkaloid precipitation reagents give amorphous precipitates with reserpine. A particularly sensitive reagent is phosphomolybdic acid; sensitivity of the reaction is 0.6 μg at a maximum dilution of 1:3200; I2/KY solutions; CdI2/KY; HgI2/KY and BiI3/KY have a sensitivity of 2.5 μg at a limiting dilution of 1:8000 and phosphotungstic acid - 5 μg at a dilution of 1: 4000.
Coloring reactions are unusual. The most characteristic violet color is produced by a solution of vanillin with reserpine in the presence of hydrochloric and sulfuric acids. The reaction can detect 0.6 μg of a substance in the analyzed object.
A characteristic property of reserpine is its ability to produce yellow-green fluorescence, which is observed in freshly prepared solutions at a dilution of 1: 1,000,000.
With solutions of ammonium thiocyanate, mercuric chloride in the presence of sodium chloride and ammonium tetrarodanomercurate, reserpine gives characteristic crystalline precipitates. The reactions are quite specific and allow the detection of reserpine at dilutions of 1:200,000 and 1:20,000, respectively (data refer to aqueous solutions of the alkaloid).
Quantitative determination of reserpine and its breakdown products is carried out using the fluorometric method after isolation and purification of the alkaloid using paper electrophoresis.
Pharmacological properties and preparations. Rauwolfia alkaloids have valuable pharmacological properties. Reserpine and rescinamine have a sedative and hypotensive effect. Ajmalitsin, raufolvine, serpagin, yohimbine adrenolytic. Ajmaline has been found to have an antiarrhythmic effect.
Most rauwolfia preparations contain reserpine. Reserpine has complex effects on the body. Influencing the peripheral nervous system, it has an antihypertensive effect, influencing central neurochemical processes - neuroleptic. The hypotensive effect of reserpine develops slowly and lasts several hours. It slows down the heart rate without changing or increasing the cardiac output, and reduces the content of norepinephrine in tissues. Reserpine induces sleep close to physiological.
The sympatholytic effect of reserpine is due to the fact that under its influence catecholamines are rapidly released from granular depots of presynaptic nerve endings. Released catecholamines are inactivated by monoamine oxidase, which leads to a decrease in the release of catecholamines into the synaptic cleft. Reserpine weakens the adrenergic effect on the effector systems of peripheral organs, including adrenergic receptors of blood vessels. The action of reserpine also extends to the central nervous system (CNS). It disrupts the transport of neurotransmitters from the cellular plasma, where they are synthesized, into granules for storage. Therefore, the content of norepinephrine, dopamine and serotonin in brain tissue decreases, because they are inactivated by monoamine oxidase in cellular plasma.
Reserpine pharmacological action: sympatholytic agent, has hypotensive, antipsychotic and sedative effects. Penetrating into the presynaptic endings of postganglionic sympathetic fibers, it releases norepinephrine from vesicles while simultaneously disrupting its reverse neuronal uptake and enhancing the process of MAO inactivation. Causes depletion of neurotransmitter reserves and a persistent decrease in blood pressure. Helps reduce the concentration of dopamine in neurons (which explains possible extrapyramidal disorders), serotonin and other neurotransmitters, providing an antipsychotic effect. Weakens the influence of sympathetic innervation on the cardiovascular system, reduces heart rate and peripheral vascular resistance; maintains activity and even compensatory increases the activity of the parasympathetic nervous system; deepens and enhances physiological sleep, inhibits interoceptive reflexes. Increases gastrointestinal motility, increases the production of HCl in the stomach; slows down metabolic processes in the body; reduces and deepens respiratory movements, causes miosis, hypothermia; reduces metabolic rate. Has a positive effect on lipid and protein metabolism in patients with arterial hypertension and coronary atherosclerosis; increases renal blood flow, enhances glomerular filtration. The effect develops after a few days and reaches its maximum after 3-6 weeks; duration of action - 1-6 weeks.
Indications: arterial hypertension, thyrotoxicosis, neurosis, psychosis, late gestosis, psychomotor agitation in patients with schizophrenia, manic agitation as part of cycloid psychosis and the circular form of schizophrenia, depressive-agitated state in patients with presenile psychosis - as part of combination therapy.
Contraindications: hypersensitivity, epilepsy, Parkinson's disease, depression, peptic ulcer of the stomach and duodenum (in the acute phase), erosive gastritis, ulcerative colitis, bronchial asthma, pheochromocytoma, angle-closure glaucoma, bradycardia, AV block, electroconvulsive therapy; cerebral atherosclerosis, nephrosclerosis, concomitant treatment with MAO inhibitors; pregnancy, lactation period.
Side effects: extrapyramidal disorders, headache, dizziness, weakness, drowsiness, insomnia, anxiety, fatigue, depression, hyporeflexia, decreased ability to concentrate; dyspepsia, nausea, vomiting, diarrhea, abdominal pain, gastrointestinal bleeding, loss of appetite; dry mouth, bradycardia, arrhythmias, thoracalgia; peripheral edema, swelling and dryness of the nasal mucous membranes, urinary retention, increased urination; decreased potency and/or libido, herpes, itchy skin, hyperemia of the mucous membrane of the eyes, weight gain, allergic reactions. Overdose. Symptoms: “nightmare” dreams, parkinsonism, angina pectoris; with long-term use in high doses - liver dysfunction.
Method of administration and dosage: orally: for arterial hypertension in the initial dose - 0.1 mg 2 times a day (morning and evening), if the desired hypotensive effect is not achieved within 5-7 days of treatment, the dose is increased to 0.25-0.5 mg / day in 2-3 doses. After stabilization of the hypotensive effect, the dose is gradually reduced to 0.2-0.1 mg/day. The course of treatment is 2-3 months. For neuroses, the initial dose is 0.25 mg 2-3 times a day, with a gradual increase to 0.5 mg 3-4 times a day. For mental illnesses, the initial dose is 0.25 mg, with a gradual increase to 10-15 mg/day; course of treatment - 3-6 months. The maximum single dose is 1 mg, daily dose is 10 mg.
Interaction: increases the risk of developing bradycardia, arrhythmogenic effects of digitalis drugs; reduces the effectiveness of antiepileptic drugs and levodopa, anticholinergic drugs, reduces the analgesic effect of morphine. Enhances the central effect of barbiturates, ethanol, drugs for inhalation anesthesia, antihistamines, tricyclic antidepressants. Reserpine eliminates the effect of sympathomimetic drugs by depleting the catecholamine depot; Reserpine can prolong the action of direct-acting adrenomimetic drugs, preventing the uptake of the mediator into depot granules. A significant increase in blood pressure has been reported when phenylephrine eye drops were prescribed during treatment with reserpine; when used simultaneously with fenfluramine, the hypotensive effect of reserpine may be enhanced. Methyldopa increases the risk of developing depressive conditions; tricyclic antidepressants weaken the hypotensive effect; MAO inhibitors increase the risk of developing hyperresponsiveness and hypertensive crisis.
Reserpine is part of a number of combination drugs used for hypertension. Combined reserpine-containing drugs have advantages over taking reserpine alone, since the hypotensive effect occurs faster and with minimal doses of their components. Combination drugs usually include ingredients with different pharmacological effects, which neutralize each other's side effects and enhance the overall therapeutic effect.
Contraindicated in severe organic diseases of the cardiovascular system, peptic ulcer of the stomach and duodenum, kidney disease with impaired function.
Side effects: hyperemia (redness) of the mucous membranes of the eyes, skin rashes, dyspepsia, bradycardia, weakness, dizziness, shortness of breath. Sometimes anxiety, depression, insomnia, parkinsonism.
Adelphan-Esidrex contains reserpine 0.1 mg, dihydralazine 10 mg and dichlorothiazide 10 mg, and Adelphan-Esidrex K contains reserpine 0.1 mg, dihydralazine 10 mg, hydrochlorothiazide 10 mg and potassium chloride 0.6 g and one tablet.
Pharmachologic effect. Along with the properties of adelfan, it has a diuretic effect and also restores electrolyte balance in the body. The components of the drug are absorbed in the stomach, and potassium chloride, thanks to the special manufacturing technology of the drug, is slowly and gradually absorbed in the small intestine, without irritating the stomach and duodenum. Hypothiazide promotes the release of sodium chloride from the body, enhancing the hypotensive effect of adelfan.
Indications for use. All forms of hypertension, especially cases of essential and renal hypertension (persistent rise in blood pressure of unknown cause and persistent rise in blood pressure due to kidney disease). When taking the drug, you do not have to adhere to a salt-free diet.
Method of administration and dose. Initially, 1 tablet of the drug is prescribed 3 times a day, then this dose is gradually increased to 2 tablets 3 times a day. For long-term treatment, 2 tablets per day are usually sufficient.
Side effect. Pain in the epigastric region (the area of the abdomen located directly below the convergence of the costal arches and sternum), nasal congestion, bradycardia, drowsiness.
Contraindications: Severe renal failure (see appendix)
Brinerdin (Brinerdin) - tablets containing reserpine 0.0001, gdihydroergocristine 0.0005 g (0.5 mg), clopamide (brinaldix) 0.005 g. Dihydroergocristine is a peripheral and central adrenergic blocking agent; clopamide - saluretic. Used for hypertension and symptomatic hypertension (see appendices)
Kristepin (Crusterin) - tablets containing 0.1 mg of reserpine, 0.5 mg of dihydroergocristine and 5 mg of the diuretic clopamide. Used for various forms of arterial hypertension.
The pharmacological action blocks sympathetic impulses (transmitter release and its acceptance by the postsynaptic membrane), which leads to a decrease in the tone of vascular smooth muscles and a decrease in heart function; has diuretic activity.
Indications for the drug are mild to moderate arterial hypertension.
Contraindications: hypersensitivity, hypokalemia, severe dysfunction of the liver and kidneys, condition after a recent myocardial infarction, depression, exacerbation of peptic ulcer; pregnancy, lactation.
Side effects of the drug: fatigue, muscle weakness, headache, dyspeptic symptoms, orthostatic hypotension, electrolyte imbalance (especially hypokalemia).
Interaction: weakens the effect of indirect anticoagulants, oral hypoglycemic agents; enhances the effects of cardiac glycosides.
Method of administration and dosage: initially, 1 tablet per day orally, if necessary, the dose can be increased to 2 tablets per day; The maintenance dose is 1 tablet per day every day or every other day.
Precautions: Prescribe with caution for diabetes mellitus, gout. During treatment, food containing potassium is recommended; You should not engage in activities that require increased attention.
Storage conditions for the drug List B in a dry place, protected from light, at a temperature of 10-25 ° C. (look at the application)
Triresid - tablets containing: reserpine 0.1 mg, dihydralazine sulfate 10 mg and hydrochlorothiazide 10 mg. Trirezide is also available with an additional content of 0.35 g of potassium chloride in each tablet. When taking all of these tablets (except those containing potassium chloride), patients should be advised to eat foods rich in potassium. Monitor potassium levels.
Total preparations of rauwolfia in the mechanism of action, along with sympatholytic activity, exhibit peripheral adrenergic and antispasmodic properties. It has an antiarrhythmic effect, restoring the processes of excitation and conduction in the heart muscle. The alkaloid ajmaline has antiarrhythmic activity, stabilizing the membranes of myocardial cells and reducing their excitability, prolonging the refractory phase of the heart and slowing down the conduction of impulses through the conduction system.
Raunatinum (Rаunatinum) is a preparation containing a sum of alkaloids from the roots of Rauwolfia serpentine or other types of Rauwolfia. The main indication for the use of raunatin is hypertension, especially in stages I and II. Raunatin is not widely used in psychiatric practice due to its insufficiently pronounced neuroleptic effect, but it can be used for neurotic conditions.
Raunatin usually does not cause side effects. Some patients tolerate it better than reserpine. In some cases, swelling of the nasal mucosa, sweating, and general weakness are observed; In patients with angina pectoris, pain in the heart area sometimes increases. Side effects disappear when the dose is reduced or after a short-term (1-3 days) break in taking the drug (see Appendix).
Ajmalinum, unlike reserpine, does not have neuroleptic activity, moderately lowers blood pressure, somewhat increases coronary blood flow, has a negative ionotropic effect and a moderate adrenolytic effect.
A characteristic feature of ajmaline is its antiarrhythmic properties. It reduces myocardial excitability, lengthens the refractory period, inhibits atrioventricular and intraventricular conduction, somewhat inhibits the automatism of the sinus node, and suppresses impulse formation in ectopic foci of automatism. Belongs to group I antiarrhythmic drugs.
Aymalin is able to stop attacks of atrial fibrillation and paroxysmal tachycardia. It is also effective for rhythm disturbances associated with intoxication with digitalis preparations.
Ajmaline is usually well tolerated. Some patients experience hypotension, general weakness, nausea, and vomiting; with intravenous administration - a feeling of heat.
Contraindications (especially for intravenous administration): severe damage to the cardiac conduction system, pronounced sclerotic and inflammatory changes in the myocardium, grade III circulatory failure, severe hypotension. Caution is necessary when administering ajmaline to patients with fresh myocardial infarction: a decrease in blood pressure and conduction disturbances are possible (see Appendix).
Extracts from the roots and leaves of the plant are traditionally used in Indian folk medicine as a remedy that has pronounced sedative properties for anxiety, manic behavior, schizophrenia, insomnia and epilepsy. A decoction of the roots enhances uterine contractions, promoting the expulsion of the fetus. The juice of the leaves is used for cataracts. The roots are used in complex preparations for dysentery, cholera, intestinal diseases, as an insecticide, as well as for snake and scorpion bites. In Java - as an anthelmintic.
Storage of drugs. Pure alkaloids (substances) are stored as toxic substances (List A). Finished medicines - tablets of reserpine, raunatin and ajmaline are stored as potent substances (List B). Adelphan-esidrex, brinerdine, cristepine, etc. are stored according to the general list.
2 Characteristics of Vinca minor
Plants: Small periwinkle - (Vinca minor), cucumber family - Apocynaceae
A small evergreen shrub with opposite leaves, in the axils of which azure flowers develop. The stem is recumbent, rooting, branched, up to 60 cm. length. Flowering shoots are erect. The leaves are overwintering, glabrous, shiny above, elliptical, pointed at the end, with a short petiole. The calyx is bare, five-parted, several times shorter than the corolla tube. The corolla is funnel-shaped, with a long narrow tube, swollen in the middle, with a five-parted bend; its lobes are widened upward, bluntly cut. There are 5 stamens, the anthers converge above the stigma and have a hairy appendage. There are two ovaries with one common column, bearing at the top a membranous, downwardly bent ring, above which there is a stigma with a hairy crown. After flowering, the ovaries diverge to the sides, and from them two leaflets with seeds, without tufts, develop, opening at one seam (Fig. 5.). Blooms in spring. Grows in shrubs, forest edges and steppe slopes.
Medicinal plant raw materials of the small periwinkle - the grass of the small periwinkle (Herba vincae minoris). Raw materials are collected in the flowering phase - the beginning of fruiting, cutting off only vertical shoots at a height of 1-5 cm from the soil surface. Drying is possible in artificial dryers at a temperature of 40-50°C, under awnings, in attics with good ventilation, spreading a thin layer (3-5 cm). It is better to lay out the grass on a stretched mesh or gauze. In good weather, the raw material dries in 5-7 days. According to existing requirements, the raw material should be represented by above-ground stems with and without flowers, with leathery leaves, dark green on top, lighter underneath, with slightly curled edges. Stems are light green. There is no smell. Moisture should be no more than 14%, stems without leaves are allowed no more than 20% of the total mass of raw materials. The number of fallen leaves is not limited, mineral impurities are no more than 1%
Other types of periwinkle that have distinctive features are not allowed: herbaceous periwinkle - leaves are round-ovate, thin, non-leathery, the corolla is purple, fluffy periwinkle - leaves are acutely ovate, heart-shaped at the base, azure flowers.
Microscopy. The cells of the upper and lower epidermis are tortuous, partly thickened and clearly visible. Paracytic stomata are located only on the underside of the leaf. Along the main vein on the upper side of the leaf there are single-celled thick-walled pointed hairs and small papillae along the edge of the leaf. The leaves contain numerous straight, unsegmented lacticifers with greenish-yellow contents. Numerous glands are visible on the petiole.
Fig.6. Microscopy of Vinca minor.
Epidermis of the upper (A) and lower (B) sides of the forest from the surface:
Epidermal cell, 2 - stomata, 3 - hairs, 4 - laticifers,
Bead-shaped thickening of the cell wall; B - leaf edge with sapular outgrowths; G - petiole epidermis; 1 - piece of iron, 2 - hair.
Chemical composition. The herb contains over 20 alkaloids of the indole group, similar in nature to reserpine, their total amount is 2% (vincamine, isovincamine, vincaminorine, minorine, vinine, pubescin, ervamin, etc.). The herb also contains triterpene saponins, vitamin C (993> mg%), rutin, carotene (8 mg%), tannins, organic acids (malic, succinic, ursolic), phytosterol, sugars and mineral salts, flavonoid glycoside - robinin.
hypertonic medicinal rauwolfia periwinkle
Standardization. The quality of raw materials is regulated by the requirements of VFS 42-1728-87
Pharmacological properties and preparations. The healing properties of periwinkle were known to Pliny and Dioscorides. In the Middle Ages, periwinkle was considered a symbol of fidelity and constancy. Currently, the plant's area of application covers mainly therapeutic, obstetric-gynecological, and dermatological diseases. The results of experimental studies of herbal preparations and individual alkaloids from various types of periwinkle have revealed that most of them cause a decrease in blood pressure, dilation of the coronary vessels of the heart and brain vessels, relaxation of the muscles of the small intestine and stimulation of uterine contractions.
Vinkaton international name: Vincamine
Group affiliation: vasodilator
Dosage form: film-coated tablets
Pharmacological action: a herbal preparation, an alkaloid of Vinca minor L., has a hypotensive, antispasmodic and sedative effect. Improves cerebral and coronary circulation and oxygen supply to cells.
Increases mental performance, facilitates memorization processes. Indications: arterial hypertension of the first and second types, condition after ischemic stroke, intracranial hypertension, neurogenic tachycardia; dizziness, decreased ability to concentrate, memory and intellectual abilities in elderly patients (cerebral atherosclerosis, diabetic angiopathy, consequences of cerebrovascular accident, head injury); menopause in women; visual impairment, hearing impairment, vestibular and labyrinthine disorders of vascular origin; absent-mindedness, deterioration of speech, impaired coordination of movements in mental illness (as part of combination therapy); migraine; delayed development of intellectual abilities in children and adolescents.
Contraindications: hypersensitivity, arrhythmias, arterial hypotension, brain tumor, ischemic heart disease; pregnancy, lactation period. Side effects: allergic reactions, skin rash, decreased blood pressure, tachycardia.
Directions for use and dosage: tablets orally, regardless of food intake, 20-40 mg 3 times a day for 10 days. The frequency can be increased up to 4 times a day, and the duration of treatment up to 30 days. A maintenance dose of 20 mg 1-2 times a day can be taken for a long time. Syrup: adults 10-20 mg 3 times a day. Retard capsules: adults 30 mg 2 times a day. If necessary, 15 mg intravenously or intramuscularly 1-2 times a day. Children orally in the form of syrup, 5 mg 3 times a day; IV drip or IM - 7.5 mg 2 times a day.
Special instructions: caution should be exercised when prescribing to patients who have suffered a myocardial infarction, as well as to patients with arrhythmias.
Interaction: if necessary, can be used in combination with other antihypertensive drugs and antiplatelet agents (enhances the effect).
Vincapan. A foreign drug (Bulgaria), similar in composition and action to Vincanor. Contains the sum of vinca alkaloids (Vinca minor L.).
Used for cerebral vascular spasms, neurogenic tachycardia, and initial forms of hypertension.
Take orally, starting with 0.005 g and then 0.01 g 2 - 3 times a day. After achieving a therapeutic effect, maintenance doses are selected individually. Children are prescribed starting from 0.0025 per day.
Release form: tablets of 0.01 g.
A similar foreign drug (Hungary) is produced under the name Vincaton.
Cavinton. Cavinton is a semi-synthetic derivative of the alkaloid devincan, contained in the periwinkle plant (Vinica minor L. and Vinca erecta Rgl. et Sсhmalth); family Kutrovye (Aposynaceae). It was previously found that extracts from periwinkle have a vasodilating and hypotensive effect and have some sedative effect. The alkaloid vincamine (methyl ester of vincamic acid) isolated from periwinkle was proposed for use (under the names Devincan, Minorin) as a vasodilator. As a result of clinical studies, it was found that Devincan is especially effective in treating cerebrovascular accidents, and later the drug Cavinton was created, which received the international name “Vinpocetine”.
Cavinton dilates brain vessels, increases blood flow, improves oxygen supply to the brain, and also promotes glucose utilization. By inhibiting phosphodiesterase, Cavinton leads to the accumulation of cAMP in tissues; reduces platelet aggregation. There is only a slight decrease in systemic blood pressure. The vasodilating effect of Cavinton is associated with a direct relaxing effect on smooth muscles. Cavinton enhances the metabolism of norepinephrine and serotonin in brain tissue, reduces pathologically increased blood viscosity, and promotes the deformability of red blood cells.
Cavinton is used for neurological and mental disorders associated with cerebral circulatory disorders (after a stroke
Cavinton is taken orally in the form of tablets, 1 to 2 tablets 3 times a day. The maintenance dose of Cavinton is 1 tablet 3 times a day. Cavinton is used for a long time. Improvement is usually observed after 1 - 2 weeks; The course of treatment with Cavinton is about 2 months or more. Cavinton is used intravenously (drip only) in neurological practice for acute focal ischemic disorders of cerebral circulation, in the absence of hemorrhage. First, 10 - 20 mg is administered in 500 - 1000 ml of isotonic sodium chloride solution (drip infusion). If necessary, repeat (3 times a day) slow drip infusions are prescribed, then switch to taking Cavinton orally. There is evidence of the use of Cavinton for the prevention of convulsive syndrome in children who have suffered brain injury. Cavinton is administered intravenously by drip at a rate of 8 - 10 mg/kg per day in a 5% glucose solution, followed by 0.5 - 1 mg/kg per day after 2 - 3 weeks. Cavinton is usually well tolerated. Hypotension and tachycardia are possible with intravenous administration of Cavinton.
Contraindications for the use of Cavinton: severe ischemic heart disease, severe arrhythmias; not used during pregnancy. It is not recommended to prescribe Cavinton for labile blood pressure and low vascular tone. Caventon injection solution is incompatible with heparin. Cavinton solution should not be injected under the skin.
Forms of production of Cavinton: tablets of 0.005 g in a package of 50 pieces; 0.5% solution in ampoules of 2 ml.
Cavinton storage: list B. In a place protected from light (see appendices)
Some recipes. For hypertension, pour 1 teaspoon of dry herb into 1 cup of boiling water, keep in a steam bath for 15 minutes, cool, strain, half a glass a day. Pour 20 g of small periwinkle herb with flowers into 250 ml of vodka, heat in a water bath to a boil and immediately turn off, leave for 10 minutes. Apply morning and evening 8-10 drops for 6 days, 1 day break and another 6 days. You need to take at least 5 such small courses.
For washing purulent wounds, ulcers and itchy dermatitis:
1 tbsp. Brew l dry herb in 1 glass of boiling water, leave for half an hour, without bringing to a boil, cool, strain.
In homeopathy, an alcoholic tincture of the herb is used for headaches, nosebleeds, eczema, rashes on the face, as well as coughs and tangles (a skin disease on the head in which the hair sticks together in a dense lump).
Conclusion
Medicinal plants came into the 20th century from ancient times and still occupy a significant place in the arsenal of medicinal products. Although chemical remedies continue to be effective weapons of modern medicine and are now much more commonly used, they cannot completely replace plant medicines. It is difficult, and often almost impossible, to recreate the subtle processes occurring in plants, different species of which, growing side by side, under the same conditions, create the most complex combinations of individual organic substances inherent only to them.
Treating doctors and pharmacists should pay special attention to side effects caused by alkaloid-containing preparations of rauwolfia serpentine. Because the incorrect use of drugs containing the alkaloid reserpine and overdoses have repeatedly caused poisoning, in some cases with a fatal outcome.
Turning off the sympathetic tone leads to the dominance of the parasympathetic system, hence the side effects:
) Gastrointestinal dysfunction may occur, which is caused by increased intestinal motility, intestinal spasms, hyperacid conditions, exacerbation of gastritis and peptic ulcers associated with the release of histamine.
) Due to the increased effects of histamine, patients experience swelling of the nasal mucosa and difficulty in nasal breathing.
) Taking reserpine may be accompanied by depression of the central nervous system, weakness, and even the development of depressive states. Therefore, it is necessary to strictly determine the medical history before prescribing the drug.
) A decrease in the amount of catecholamines in the bronchi contributes to the development of bronchospasm in patients with bronchial asthma.
Vinca preparations are also effective, the main active principle of which is the alkaloid vincamine, which has a less pronounced hypotensive, but more significant sedative effect. They selectively improve blood circulation in the brain, which improves the trophism and functional state of the centers, have a sedative effect and help slow the pulse. Therefore, they are especially indicated in the initial stages of the disease, which occurs in the cerebral variant; in case of tachycardia, they cannot be used to relieve hypertensive crises, but they can be effectively used for prevention. And what is very important for patients, there are usually no side effects.
V. List of used literature:
1. Georgievsky V.P., Komisarenko I.F., Dmitruk S.E., Biologically active substances of medicinal plants. Novosibirsk: Science - 1990. - 333 p.
Karpovich V.N. Pharmacognosy. / Textbook for pharmacists. schools and departments /. M.: Medicine. - 1977. - 446 p.
Kachalov A.A., Encyclopedic Dictionary of Medicinal, Essential Oil and Poisonous Plants. - M. - 1951.
Kuznetsova M.A., Medicinal plant raw materials and preparations, M.: Higher School. - 1987.
Mashkovsky M.D. Medicines. - 15th ed., revised, corrected. And additional - M.:RIA New Wave: Publisher Umerenkov, 2008. - 1206 p.
Muravyova D.A., Samylina I.A., Yakovlev G.P. - Pharmacognosy. M.: Medicine. - 2007. - 656 p.
Pristupa A.A., Main raw materials plants and their use. - L.: Science. - 1973.
Turishchev S.N., Herbal medicine, M.: Academy. - 2003. - 304 p.
Fedorov A.A., Kiryalov N.I., Resin-bearing plants of the USSR, collection: Plant raw materials of the USSR, T. 1. M. - L.: USSR Academy of Sciences. - 1950.
Shupinskaya M.D., Karpovich V.N., Pharmacognosy. State publishing house of medical literature. - 1963. - 368 p.
Yakovlev G.P., Belodubrovskaya T.A., Berezina V.S. St. Petersburg: SpetsLit. - 2006. - 845 p.
Pharmacotherapeutic group. Hypotensive, sedative, antiarrhythmic agent.
Description of the plant
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Rice. 10.31. Rauwolfia serpentina Benth.
Roots of Rauwolfia serpentine- radices rauwolfiae serpentinae
- rauwolfia serpentina benth.
Sem. Kutrovye- apocynaceae.
evergreen shrub, containing milky juice, 0.2-0.6 (1) m high.
Has a small vertical rhizome with numerous adventitious roots and a long tap root with large lateral roots.
Stem ascending, covered with a whitish cork.
Leaves arranged whorled in groups of 3-4, less often opposite or alternate, oblong-elliptic, obovate or oblanceolate, pointed at the apex, narrowed at the base into a short petiole, thin, glabrous, shiny, 7.5-17.5 cm long.
Flowers white or pink, collected in apical, less often axillary, dense umbrella-shaped inflorescences. The calyx and pedicels are bright red.
Fetus consists of two juicy red drupes (Fig. 10.31).
Composition of Rauwolfia
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Chemical composition of rauwolfia
Currently, more than 50 alkaloids have been isolated
- reserpine,
- aymaline,
- serpentine,
- rescinamine,
- yohimbine
- and etc.
Properties and uses of rauwolfia
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Pharmacological properties of rauwolfia
Rauwolfia alkaloids have various pharmacological properties. They mainly affect the central nervous system,
- reserpine and, to a lesser extent, rescinamine have a sedative and hypotensive effect,
- yohimbine – alpha-adrenergic blocking
- ajmaline - antiarrhythmic effect.
The main pharmacological properties of reserpine is its sympatholytic effect, caused by the depletion of norepinephrine resources in adrenergic nerve endings.
Reserpine has complex effects on the body. Its antihypertensive effect is largely associated with its effect on the peripheral nervous system, and its neuroleptic effect is associated with its effect on central neurochemical processes.
Under the influence of reserpine Systolic and diastolic pressure gradually decreases in different forms and stages of hypertension. The best effect is observed in the early stages of hypertension, in the absence of pronounced organic changes in the cardiovascular system. The hypotensive effect persists for a relatively long time after discontinuation of reserpine.
Along with lowering blood pressure, kidney function improves:
- renal blood flow increases,
- glomerular filtration increases.
There is evidence of the positive effects of reserpine on lipid and protein metabolism in patients with hypertension and coronary atherosclerosis.
Aymalin does not have neuroleptic activity, moderately lowers blood pressure.
A characteristic feature of ajmaline is
- antiarrhythmic properties.
Applications of Rauwolfia
The raw materials are used to produce the drugs “Reserpine”, “Aymalin”, which are pure alkaloids, and the total drug “Raunatin”.
"Reserpine" is used to reduce blood pressure in hypertension, as well as in mental disorders.
"Raunatin" provides has a milder hypotensive and sedative effect, it also has antiarrhythmic and antispasmodic properties.
"Aymalin" is an effective remedy for stopping attacks of atrial fibrillation.
Reserpine is part of a number of combination drugs used for hypertension.
Spreading
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Spreading. Naturally grows in India, Thailand, Burma, Sri Lanka and Indonesia. Cultivated in India. Raw materials are currently imported into Russia.
Habitat. Grows along the edges of tropical rainforests.
Other types
Rauwolfia vomitoria Afz., which grows in tropical Africa from the west coast to Mozambique, r., is also used as a source of reserpine. four-leaved (grayish river) (R. tetraphylla L. = R. canescens L.), widespread in South America, India, Australia, as well as the river. caffra (R. caffra Soud.), growing in Africa. The first two species are promising for introduction into industrial culture in Transcaucasia. At the St. Petersburg Chemical and Pharmaceutical Academy, microcloning technology was proposed for their breeding, and a method for obtaining tissue culture biomass, which is a source of ajmaline, was developed and implemented.
Procurement and storage of raw materials
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Preparation. In places of natural growth, roots are harvested during the fruiting phase of plants with a well-developed root system. On plantations in India, the roots are dug up in the third or fourth year of the plant’s life.
Storage. Raw materials are stored according to list B.
External signs of raw materials
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Root pieces, cylindrical or split longitudinally, covered with brown cork.
Outside surface longitudinally wrinkled.
Kink smooth. Yellow wood is visible at the fracture.
Bark not wide, but alkaloids are localized in it, so the presence of pieces of roots with peeled bark is a defect in the raw material.
Smell characteristic, unpleasant. Taste do not define (!).