APITOXIN (Venennm Apis) — the dense secret of acid reaction allocated by threadlike gland of the stinging device of a working bee. Item I. contains up to 40% of a solid residue and on air quickly hardens. In water solution it is unstable and quickly rots; dried up or under a butter layer keeps activity for years. At one sting the bee allocates from 0,2 to 0,8 mg of native poison.
Main toxic component P. I. poverkhnostnoaktivny peptide the melitin making St. 50% of its dry weight is. Melittin consists of 26 remains of 12 amino acids; pier. weight (weight) of 2840. It damages cellular membranes, causes hemolysis, a cytolysis and has antibiotic properties; depolarizes excitable membranes of neuromuscular and ganglionic synapses, causing reduction of unstriated muscles; brakes activity of thromboplastin, slowing down coagulability of blood; influences some fermental systems and increases resistance of animals to action of ionizing radiation. Peptide apamin (18 remains of 11 amino acids) increases the general excitability and causes spasms of the central origin. MSD-peptide (22 rests of 9 amino acids) causes degranulation of mast cells of connecting fabric with release of a histamine (see), heparin (see) and destroys thrombocytes of blood with release of serotonin (see). Peptide minimin oppresses development of larvae of flies drosophilas. In P.'s structure I. enter also the histamine (apprx. 1% of dry weight), hyaluronidase (see), edges promotes P.'s distribution I. in fabrics, a phospholipase And, also damaging cellular membranes (through formation of lysolecithin) and the breaking life activity of cells. Products of a cytolysis and splitting of fosforilkholin cause numerous pharmakol. effects: reduction of unstriated muscles, falling of blood pressure, increase in permeability of capillaries, etc.
In a symptom complex of poisoning of P. I. mammals and the person distinguish local and general reaction. In an injection site of P. I. the aseptic inflammation with hypostasis of fabric develops. Distinguish symptoms of a stress from the general phenomena (see) which cornerstone excitement of pituitary and epinephral system, and also defeat of a nervous system (spasms, paralyzes) and systems of blood (hemolysis, an incoagulability) is. Lethal dose of P. I. for the person apprx. 0,2 g (500 — 1000 uzhaleniye). Death comes from an apnoea. On opening the hyperemia of internals and a hemorrhage in lungs is found and went. - kish. path.
At hypersensitivity to P. I. even one sting can cause heavy allergic reaction (urticaria, asthma, shock, etc.), sometimes from the death (see. Allergy , Acute anaphylaxis ). Antigens in P. I. proteinaceous components, in particular enzymes while peptides are almost absolutely deprived of antigenic properties are. Acute management at P.'s poisoning I. — see. Poisonings (table).
Item I. with to lay down. the purpose (apiotherapy) apply in the form of natural bee uzhaleniye according to the special instruction approved by M3 of the USSR and also in the form of drugs from which in the USSR find application apizartron for injections (GDR), Virapinum in the form of ointment (ChSSR), an apifor in tablets for introduction through skin by an ionophoresis (USSR). For production of drugs P. I. receive in special devices where in response to irritation emit with weak impulses of electric current of a bee poison. Droplets of poison get on glass, dry on it then they are cleaned off.
Indications for P.'s use I. as means of nonspecific therapy: diseases of a peripheral nervous system (neuralgia, do not lie you, radiculitises), hron, arthritises and arthroses, the deforming spondylarthrosis, inflammatory infiltrates (without suppuration), bronchial asthma, migraine, some vascular diseases, irites and iridocyclites.
Item I. it is contraindicated at tuberculosis, venereal, mental and acute inf. diseases, diseases of a liver and kidneys, acute purulent processes and insufficiency of heart and vessels. Do not appoint P. I. also at diseases of the hemopoietic system, new growths, at pregnancy.
Drugs of apitoxin in medical practice use in the form of native substances, containing all complex of biologically actively active ingredients and also purified, exempted from proteins. Take P.'s number for one dose (1 PIECE) I., received during the sting of one bee that averages apprx. 0,2 — 0,3 mg of dry poison.
Drugs P. I. apply in the form of solutions in water (most often) or diluted in oil is (much more rare), and also in the form of ointments and linimentums. Number of drugs P. I. use for injections (intradermal and hypodermic) and for an electrophoresis (see), but drugs for external use are most spread. At their hypodermic, intradermal or external use local reaction is most brightly shown; there is also general reaction, degree the cut in many respects depends on individual sensitivity of the patient and on a dose of drug.
Apisarthronum — dry P.'s powder I. Produce in ampoules in doses 0,1 mg (Apisarthronum-mite) and 1 mg (Apisarthronum-forte). Drug is dissolved in water for injections just before introduction, entered vnutrikozhno (at the same time blisters are formed), sometimes into Ged's zones — Snegireva, corresponding to the painful center. Begin injections with a dose of 0,005 mg of poison in 0,1 ml of water once a day, gradually increase a dose (every time by 0,005 mg). After 6 — 8 injections, at good tolerance, pass to administration of the drug «forte» (on 0,05 mg into 1 ml of water). Injections make within 15 — 17 days.
Store in the place protected from light; joint venture. B. Preparat is manufactured in GDR.
Apizartron-maz contains 1 PIECE of P. I. in 1 g of ointment, an ointment basis, 10% of methyl salicylate and 1% of essential mustard oil. Rub ointment in skin once a day. For definition of sensitivity previously rub a portion of ointment size about small pea.
Is issued in tubas on 20 g; store in the cool place. It is manufactured in GDR.
Apifor (Tabulettae «Apiphorum»; joint venture. B) — the tablets containing 0,001 g of the lyophilized P. I. Apply to an electrophoresis in the form of solution in a distilled water (1 tablet on 20 ml) which is prepared just before use since in water solutions drug quickly collapses. Enter from both poles at current in 10 ma, duration of the procedure of 10 min., a course of treatment of 15 — 20 procedures which are released daily or with breaks, depending on reaction of the patient.
Drug is very unstable, store it in well corked banks of orange glass, in the place protected from light.
Virapin — ointment. 1 g of ointment contains 0,15 mg of the lyophilized P. I. Rub 1 — 2 time a day in skin of a sore point at rheumatism, nonspecific polyarthritises, a miositis, radiculitis, a sciatica, neuralgia. Usually on site rubbing in the hyperemia, burning sensation quickly appears. Is issued in tubas on 20 g; store in the cool place. It is made in ChSSR.
Bibliography: Alesker E. M. Apitoxin in clinic of internal diseases, D., 1964; Arnaudov G. D. Medicinal therapy, the lane with bolg., page 33, Sofia, 1978; Artyomov H. M. Apitoxin, its physiological properties and therapeutic use, M. — L, 19 41; And m of m e r-man A. F. Kurs of a pharmacognosy, page 590, L., 1967; M and sh to about in with to and y M. D. Pharmaceuticals, p. 2, page 221, M., 1977; Poisons of bees and snakes in biology and medicine, under the editorship of H. M. Artyomova, Gorky, 1967; Cavagnol R. M of The pharmacological effects of hymenoptera venoms, Ann. Rev. Pharmacol. Toxicol., v. 17, p. 479, 1977; Habermann E. Bee and wasp venoms, The biochemistry and pharmacology of their peptides and enzymes are reviewed, Science, v. 177, p. 314, 1972.
H. M. Artyomov; V. P. Wingnuts (pharm.).