PRIMACHINUM (Primachinum; synonym: Avion, Primaquini Diphosphas, Primaquine Diphosphate, etc.; joint venture. B) — antimalarial means. 8-(4-amino-1 - metilbutilamino) - 6-metoksikhinolin; With 15 H 21 N 3O :
The item is used in the form of diphosphate.
Fine-crystalline powder of bright yellow color, bitter taste. Let's dissolve in water.
It is well soaked up from went. - kish. a path and in the maximum concentration collects in blood in 6 hours after intake. In 24 hours in blood traces of the Item are defined. Level P. in a blood plasma is subject to considerable individual fluctuations. It is removed by kidneys of hl. obr. in the form of metabolites.
The item is highly active concerning primary ekzoeritrotsitarny (preeritrotsitarny) forms of the activator of a tetrian fever and especially the causative agent of tropical malaria, has gamontotsidny effect on gamonts of all types of the plasmodiums causing malaria in the person and also affects secondary ekzoeritrotsitarny (paraerythrocyte) forms of plasmodiums.
The mechanism of action is caused, apparently, by the fact that P. breaks the DNA functions in cells of causative agents of malaria.
Item. apply for public chemoprophylaxis of malaria, and also for the prevention of the remote recurrence of a tetrian and quartan malaria. In a combination with P.'s Chingaminum it is possible to apply to personal chemoprophylaxis of malaria in local districts.
Appoint inside in tablets 0,009 g. A daily dose for adult 0,027 g (3 tablets); for children till 1 year of 0,00225 g (1/4 tablets), 1 — 2 years 0,0045 g (1/2 tablets), 2 — 4 years 0,00675 g (3/4 tablets), 4 — 7 years 0,009 g (1 tablet), 7 — 12 years 0,0135 g (1,5 tablets), 12 — 15 years 0,018 g (2 tablets), are more senior than 15 years 0,027 g (3 tablets). Course of treatment of 14 days.
Side effect of P. is shown by dispeptic frustration, pains in heart, the general weakness and cyanosis (owing to formation of a methemoglobin). At genetically caused deficit of a glyukozo-6-phosphate-dehydrogenase in erythrocytes (is more often at faces of some ethnic groups from the districts of the Mediterranean and Transcaucasia, and also Africa) P.'s use can cause an acute intravascular hemolysis with a haemoglobinuria. At suspicion it is necessary to appoint to this fermentopatiya of P. carefully. Before purpose of drug in such cases it is reasonable to determine sensitivity to P. Naiboley by the simple test for definition of hypersensitivity to P. slower is, than normal, a recovery rate of a methemoglobin in the presence of methylene blue.
At emergence of the first signs of toxic influence of P. on blood (sudden decrease in level of hemoglobin and number of erythrocytes in blood, darkening of urine) drug is cancelled.
Item. it is contraindicated at diseases of blood, and also at acute infectious and general diseases with a tendency to a granulocytopenia (e.g., at an active form of rheumatism, a system lupus erythematosus, etc.).
It is not necessary to appoint drug together with the substances which are potentially possessing hemolitic action or ability to oppress myeloid elements of marrow (the streptocides, sulphones derivative of aniline, etc.). Besides, P. should not appoint together with quinacrine which slows down P.'s allocation from an organism and by that increases its toxicity.
Form of release: the tablets containing 0,009 g of Primachinum of diphosphate that corresponds to 0.005 g of Primachinum of the basis. Storage: in the dry, protected from light place.
See also Antimalarial means .
Bibliography: Mashkovsky M. D. Pharmaceuticals, p. 2, page 291, M., 1977; The pharmacological basis of therapeutics, ed. by A. G. Gilman a. o., N. Y., 1980.
L. A. Serebryakov.