EFEDRYN (Ephedrinum) — adreno-mimetichesky means; the alkaloid received from different types of an ephedra (Ephedra L.) this. efedrovy (Ephedraceae). In medical practice it is used in the form of ephedrine of a hydrochloride (Ephedrini hyd-rochloridum; synonym: Eciphin, Ephedrinum hydrochloricum, Ephedrosan, Fedrin, Kratedyn, Sanedrine
, etc.; GFH, joint venture. Б). £-1-fenil-2-me-tilaminopropanola-1 hydrochloride; C10H15NO • HG1:
/ V-SN — СН — N^H • NANOSECOND |
\=/the I Tkhsn,
Colourless acicular crystals or inodorous white crystal powder, bitter taste, we will easily dissolve in water (1:5), we will dissolve in 95% alcohol (1:14), it is practically not ether-soluble. Pier. weight (weight) 201,70, * °pl 216 — 220 °.
Nagai is purely allocated in 1887, E. Spath is synthesized in 1920.
AA., contained in plants, is laevoisomer. The racemate conceding on activity to laevoisomer is synthetic received.
AA. treats the adrenomimetika of indirect action (sympathomimetics) stimulating and - and R-ad-renoretseptory. Has a double focus of action. First, affecting presynaptic nerves, it promotes release of a mediator of noradrenaline (see); secondly, exerts the weak stimulating impact directly on adrenoceptors.
On the main effects E. it is similar to adrenaline (see). Ots stimulates action of the heart, raises the ABP, causes broncholitic effect, suppresses a peristaltics of intestines, expands a pupil (without influencing accommodation and intraocular pressure), raises a tone of skeletal muscles, causes a hyperglycemia. AA. differs from adrenaline gradually developing and longer (on influence on the ABP — by 7 — 10 times) in action. On activity considerably concedes to adrenaline. At repeated introduction E. with a small interval (10 — 30 min.) its pressor action quickly decreases — there is a pgakhi-filaksiya (see) connected with the progressing reduction of stocks of noradrenaline in presynaptic nerves since E. strengthens allocation of noradrenaline from them. The stimulating influence E is expressed. on c. N of page. In this respect it surpasses adrenaline, but concedes to Phenaminum (see).
Essential difference E. from adrenaline its efficiency at intake is. AA. it is steady against monoamine oxidase. In a liver it is partially deaminized (at the expense of other enzymes). Considerable part E. (apprx. 40%) it is allocated with kidneys in not changed look.
Apply E. most often as bronchial spasmolytic for prevention of bronchospasms (see), and also at allergic states (see
the Allergy). Sometimes it is appointed as pressor means. AA. often use at cold (see Rhinitis) since thanks to local vasoconstriction under its influence secretion of a mucous membrane of a nasal cavity decreases. It can be applied to elimination of the atrioventricular block (see the Heart block). AA. finds application and in ophthalmology for a mydriasis (see an Eye). In connection with the stimulating influence on c. the N of page is shown at a narcolepsy (see).
Appoint E. inside and parenterally (subcutaneously, intravenously, intramusculary), in the form of inhalations, and also locally (in the nasal courses, on a mucous membrane of an eye): inside the adult — on 0,025 — 0,05 g 2 — 3 times a day; subcutaneously and intramusculary the adult — on 0,02 — 0,05 g 2 — 3 times a day; intravenously adult — struyno (slowly) on 0,02 — 0,05 g (0,4 — 1 ml of 5% of solution) or-pelno in 100 — 500 ml of isotonic solution of sodium chloride or 5% of solution of glucose in the general dose of 0,08 g. In Ophthalmolum. to practice solutions in the form of eye drops apply 1 — 5%. At vasculomotor rhinitis solutions use 2 — 3%. To children E. appoint inside in the following doses: aged till 1 year — on 0,002 — 0,003 g; 2 — 5 years — on 0,003 — 0,01 g; from 6 to 12 years — on 0,01 — 0,02 g on reception. The highest doses E. for adults inside and under skin: one-time — 0,05 g, daily — 0,15 g.
At overdose E. the condition of excitement, the expressed increase in the ABP, sleeplessness, heartbeat, trembling of extremities, vomiting, an ischuria, the increased sweating, skin rashes are observed. At poisoning E. appoint barbiturates (see).
It is contraindicated at arterial hypertension of various etiology, the expressed atherosclerosis, at heavy organic heart diseases, sleeplessness.
Form of release: powder; tab
letka on 0,002; 0,003; 0,01 g (for children) and 0,025 g; ampoules on 1 5% of solution (for injections); 2 and 3% solutions in bottles on 10 ml (drops in a nose). Besides, E. along with other substances is a part of the nek-ry combined drugs, napr, the tablets «Theophedrinum», an aerosol of Efatin and the drug «Solutanum» applied at bronchial asthma.
Storage: powder — in well corked container protecting from effect of light; tablets, ampoules and solutions — in the place protected from light.
Bibliography: Mashkovsky M. D.
Pharmaceuticals, t. 1, page 277, M., 1984; The pharmacological basis of therapeutics, ed. by A. G. Gilman and. lake, N. Y., 1980. D. A. Harkevich.