Macleay small-fruited – Macleaya microcarpa
Perennial herb up to 2,5 m, families makovыh (Papaveraceae). It grows in South-East Asia. Medicinal raw materials for the medical industry is the aboveground part of the plant.
Macleay small-fruited – Chemical composition
Aboveground part contains a number of Muckle isoquinoline alkaloids. Of these, the most abundant plant contains sanguinarine, xeleritrin, protopine and allokriptopin.
Macleay small-fruited – Pharmacological properties
Experimental studies have established, The biological activity due to the amount of alkaloids Maclay and depends, in particular, the content of the plant sanguinarine and chelerythrine. The sum of these structurally similar alkaloid was isolated as a medicament, and entitled "Sangviritrin"Well-studied pharmacological and microbiological.
The general effect and toxicity Sanguirythrine been studied in various laboratory animal species. When administered intravenously, alkaloids decreased motor activity, However, the reaction to painful stimuli and sound persisted. With increasing doses of the drug dramatically reduced physical activity, and noted a general depression. LD50 for Sanguirythrine is 19,4 mg / kg, as compared with the level of toxicity galanthamine approximately 4 half.
Pharmacological properties Sanguirythrine characterized mainly by its influence anticholinesterase. Action alkaloids on cholinergic receptors found in the classical experiments with isolated frog rectus abdominis muscle and spinal leech. In these experiments, established, sangviritrin that significantly increases the sensitivity of muscle tissue to the action of acetylcholine, Although direct effect on muscle alkaloids do not have. Strengthening response to acetylcholine influenced Sanguirythrine observed in experiments on the isolated segment of bowel. The experiments found, sangviritrin that inhibits the activity of true and false cholinesterase.
Sanguirythrine in animal experiments to stimulate the activity of the intestine. Under the influence of alkaloids tone intestine significantly increased, and the amplitude of contractions in the intestine largely increased experiments. Action Sanguirythrine on isolated organs was continued for 50-60 minutes or more, and the drug also has a tonic effect on the pregnant uterus.
Influence Sanguirythrine on blood pressure and respiration were studied in cats. When administered intravenously, the alkaloids in animals observed transient pressor response, then BP was lowered, followed by raising to baseline within 50-60 min. At high doses Sanguirythrine pressor phase missing and immediately went down on BP 7,20-8,26 kPa (54-62 Mm Hg. Art.). In separate experiments, the effect was accompanied by the emergence of vaguspulsa. At the time of the introduction of some alkaloids observed respiratory depression.
The effect on blood pressure sangviritrin is an antagonist atropine. In experiments on cats atropine completely eliminates the pressor action phase Sanguirythrine on BP. Like other anticholinesterases sangviritrin restores neuromuscular conductivity in violation of its preliminary introduction diplatsina. In experiments it was proved ditilinom, that antagonism Sanguirythrine applies only to drugs kurarepodobnymi action.
Antimicrobial action the drug was studied by serial dilutions in liquid media. Detected, sangviritrin that has a broad spectrum of antimicrobial activity: retards the development of Gram-positive (including antibiotic) Gram-negative bacteria and fungi and pathogenic parasitic protozoa.
In experimental models with the introduction of the alkaloids possessed inside chemotherapeutic activity in staphylococcal sepsis, which was reflected in some increase in survival of experimental animals. Sangviritrin, applied topically in the form of an emulsion, exerted a pronounced therapeutic effect in animals at a localized purulent infection, caused by Gram-positive microorganisms, as well as their association with gram-negative microflora. As a result, the treatment of inflammation decreased and shorten the healing necrotic surfaces.
Fungistasis Sanguirythrine been studied in 52 various strains of fungi and actinomycetes some, including filamentous fungi, causing superficial lesions of the skin and scalp, yeast-like fungi and pathogens deep, systemic mycosis. Studies demonstrate a high biological activity Sanguirythrine.
Macleay small-fruited – Use in medicine
A clinical study of the therapeutic efficacy of Sanguirythrine was conducted in conditions of hospital treatment in a number of neurological clinics. The drug was used in cerebral palsy, miopatiyah, spastic paresis of the facial nerve, when progressive muscular dystrophy and other neurological disorders.
Good results were obtained in patients, suffering from various forms of myopathies, clinical picture characterized by muscle atrophy, gait difficulty, decreased or absent tendon reflexes. Patients received the drug in tablets 0,01 g (10 mg) appointment 2 times a day after meals. Sanguirythrine used in combination with B vitamins, ATP, vitamin E, and physical therapy.
Significant improvement was seen in patients with myopathy in the background poliomyelitis. As a result of the treatment he was growing muscle strength, increased range of motion in the extremities, improved gait. Among the side effects of the drug phenomenon is sometimes observed mild intoxication (nausea, dizziness, slight headache). After discontinuation of the drug, these effects disappear.
Sanguirythrine successfully used in children with various forms of progressive muscular dystrophy, when rough cerebral palsy, spastic paresis due to birth trauma and other diseases. The drug was administered at the rate of 0,0005 g, and then at a rate 0,001 g per year of life in a day 2 reception after 30-40 minutes after eating. All the children recorded a positive result, particularly when administering the drug in combination with calcium gluconate, methionine and glutamic acid. When using Sanguirythrine glutamic acid remission increased to 2-3 months, and the drug stabilized with methionine good condition in some patients to an average of 6-8 months.
Sanguirythrine clinical study was conducted in surgical practice. Patients with purulent wounds of soft tissue administered 0,1 % aqueous solution Sanguirythrine. The solution was washed with wounds, and they moistened wipes, which was applied to the wound surface. The conducted study showed, that the drug is effective in the first phase of wound healing. In the treatment solution Sanguirythrine a few procedures positive dynamics of wound healing, umenpzalas exudation, the wound became cleaner, edge insula was activated and epite- tion. None of the observations was not observed local or general manifestations of adverse reactions.
For the treatment of purulent wounds and trophic ulcers in patients also used 1 % liniment sangviritrina, under the influence of which were rejected quickly necrotic tissue, increased growth of granulation and accelerates the regeneration process. Liniment imposed patients with dressings 1 once every 3 day. Pronounced effect observed when using liniment for burns. Epithelialization of burn surface proceeded satisfactorily, there was no festering. Healing of the skin is the primary tension.
Sanguirythrine as 1 % liniment and 0,2 % water-alcohol solution used in patients with aleveolyarnoy pyorrhea, chronic recurrent aphthous stomatitis, dekubitalnymi ulcers, herpetic stomatitis and medication, eczematous cheilitis, etc.. To ensure a more prolonged contact of the drug with the gingival tissue in pathological gingival pockets administered to 20 min thin cotton turundy, liberally moistened 0,2 % water-alcohol solution Sanguirythrine. Thus turundy changed 2-3 times a day. After 1-2 procedures, patients reported a reduction in pain, itching and bleeding gums. Then disappears hyperemia, swelling of the gums. Gums acquired normal color, tight to the teeth. Complications in the treatment of patients in this group were found. Application 1 % liniment in the form of applications for 5-10 minutes for 2-3 days also resulted in a reduction of pain and accelerate epithelialization of erosive surfaces of the gums. Positive results were also obtained when treating parodontosis. When using Sanguirythrine observed a decrease of periodontal pockets suppuration at 3-day treatment. Significantly reduces the amount of necrotic plaque, occurred faster healing of erosions in the necrotizing gingivostomatitis.
In the treatment of skin diseases sangviritrin used in patients with various dermatoses, including microbial eczema, surface blastomycosis, pyoderma, as well as candidiasis nail ridges, fungal skin lesions (microsporia, ringworm, chromophytosis, rubrofitii and yeast nail infections, candidiasis et al.).
Complete recovery was observed in patients with appointment 0,2 % aqueous-alcoholic solution of the drug in yeast nail lesions, as well as nail rubrofitii. In the latter case sangviritrin administered after surgery. When groin rubrofitii, and rubrofitii microsporia and smooth skin recovery usually occurs within 8-10 days. When microsporia scalp disappearance of filaments of the fungus was observed after 3 Sun.
Macleay small-fruited – Side effect
When applying the preparation to the wound surface possible burning sensation. In these cases sangviritrin used in lower concentrations. When taken into Sanguirythrine nausea, vomiting, stomach ache. With the cessation of these effects disappear. To reduce side effects sangviritrin encouraged to nominate after eating.
Contraindications:epilepsy,hyperkinesis, bronchial asthma, angina, liver and kidney disease.
Macleay small-fruited – Formulations, Dosing and Administration
Sangviritrin Is the inside of 0.005-0,01 g (5- 10 mg) appointment 2 times a day after meals. In the absence of the effect of the dose can be increased to 0,015 g (15 mg) appointment 2 once a day. The course of treatment the average 20 days. Babies sangviritrin appoint a common scheme, depending on age, but not more 0,001 g per year in daily life 2 admission.
For the treatment of long-term healing wounds and ulcers 1 % liniment sangviritrina applied to the wound surface dressings at daily or every 1-2 days. In these cases it is also possible to apply 0,1 % water solution, washing their wounds and ulcers, or soaking towels, which is applied to the wound area. The frequency of dressing 1-2 times a day, when burn wounds - 3 times a week. Aqueous solutions are ex 1etroge from tablets, dissolving them in hot water.
In dermatology sangviritrin used daily 1 -2 Times a day, lubricating lesions 1 % liniment or 0,2 % hydroalcoholic solution for 4-21 days.
In the treatment of otitis externa after cleaning the ear canal is administered turundy, wetted 0,2 % water-spirtovym or 0.05-0.1 % aqueous Sanguirythrine 10-15 min 2-3 times per day. Treatment continues for at least 2 Sun. In chronic suppurative otitis media after using the toilet middle ear dig 0,2 % aqueous-alcoholic solution of 5-8 drops Sanguirythrine 3 once a day.
Treatment of alveolar pyorrhea (parodontoz) carried out after the removal of dental plaque and curettage pathological gums. The gum pockets are introduced to 20 m. thin turundy, liberally moistened 0,2 % water-alcohol solution Sanguirythrine (the procedure is repeated daily or every other day, only 4-6 times). When stomatitis of various etiologies produce appliqué 1 % liniment or solutions of the drug 2-3 times a day for 2-5 days.
For external use the highest dose of liniment 3 g, water-alcohol solution - 15 ml, aqueous solutions - 30 ml.
