ISOPROMETHAZINE (Diprazinum; synonym: Pipolphenum, Allergan, Antiallersin, Atosil, Fargan, Fenazil, Fenergan, Promazinamide, Promethazini Hydrochloridum, Prorex, Provigan, Tanidil, Vallergin; GFH, joint venture. B) — antihistamine. 10-(2 Dimethylaminopropyl) - a fenotiazina a hydrochloride, C 17 H 20 N 2 S-HCl:
Inodorous white crystal powder, we will very easily dissolve in water, it is easily alcohol-soluble also chloroform, is almost insoluble on air; t pl 221 — 225 °. Powder and water solutions D. darken under the influence of light. On a chemical structure and a row pharmakol, properties D. it is close to to aminazine (see). Surpasses in antihistaminic action of D. Dimedrol (see), Suprastinum (see. Chloropyraminum ) and some other antihistamines.
Has cholinolytic, adrenolytic and mestnoanesteziruyushchy effect, reduces a tone of muscles of intestines and peripheral vessels, tones up muscles of a uterus. On influence on c. the N of page is similar to aminazine, but acts more weakly. It causes antiemetic and sedation, exponentiates effect of somnolent, analgesic and mestnoanesteziruyushchy substances, reduces body temperature. Solutions D. in concentration higher than 1% have bactericidal effect.
Drug apply hl. obr. at treatment of various allergic diseases (a small tortoiseshell, a serum disease, hay fever, etc.). At vasculomotor and allergic rhinitises, rheumatism with the expressed allergic component, a medicinal allergy, and also at a pruritic dermatosis, Menyer's disease, a chorea, encephalitis and other diseases of c. N of the page which are followed by increase in permeability of vessels at sea and aeroembolism, vomiting of pregnant women. In surgical practice of D. use in lytic mixes for potentiation of an anesthesia and receiving a hypothermia, reduction of postoperative complications.
Appoint inside (after food) 0,025 g 2 — 3 times a day, intramusculary (1 — 2 ml of 2,5% of solution) and intravenously as a part of lytic mixes to 5 — 10 ml of 0,5% or 2 ml of 2,5% of solution; under skin do not enter in connection with irritant action. To children up to 6 years appoint inside 0,008 — 0,01 g 2 — 3 times a day, 6 years — on 0,012 — 0,015 g 2 — 3 times a day are more senior. The highest doses for adults: inside — one-time 0,075 g, daily 0,5 g; intramusculary — one-time 0,05 g (2 ml of 2,5% of solution), daily 0,25 g (10 ml of 2,5% of solution).
At D.'s reception anesthesia of mucous membranes of an oral cavity, dryness in a mouth, nausea inside can be observed. Slackness, drowsiness, sometimes tachycardia, decrease in the ABP is often noted; allergic reactions (a Quincke's edema, systemic lesion of connecting fabric and vessels, diffusion damage of kidneys), dermatitis are possible (in connection with irritant action). At intravenous administration of D. can cause strong decrease in the ABP. It is necessary to appoint drug with care the patient with an abnormal liver function and kidneys. Strengthens narcotic effect of alcohol. It is not recommended to appoint D. in operating time to drivers of transport and other persons whose profession demands bystry physical. and mental reaction.
Forms of release: tablets (dragee) on 0,025 g and 2,5% solution in ampoules on 1 and 2 ml. Keep in the dry, protected from light place.
Renders irritant action on mucous membranes and can cause dermatitis therefore during the work with it it is necessary to be careful.
See also Antihistaminic substances .
Bibliography Pharmacological basis of therapeutics, ed. by L. S. Goodman a. A. Gilman, L., 1975.
S. S. Liberman.