Izadrin (isadrinum)
IZADRIN (Isadrinum). 1-(3, 4-Dioksifenil) -2 - izopropilaminoetanola hydrochloride, or N-izopropilnoradrenalina hydrochloride.
Abroad, published as hydrochloride or sulfate under the title : Izoproterenol, Izuprel, Novodrin, Euspiran, Aleudrin, Aludrin, Antasthmin, Bronchodilatin, Euspiran, Iludrin, Isodrenal, Isonorin, Isoprenalini hydrochloridum, Isoprenaline hydrochloride, Isopropylarterenol, Isoproterenol, Isorenin, Isuprel, Neodrenal , Neoepinephrine, Norisodrin, Novodrin and others.
The white crystalline powder. The easily soluble in water. Aqueous solutions are slightly greenish tint.
Izopropilnoradrenalin (izadrin) was received in 1938 in the synthesis via derivatives.
Chemically izopropilnoradrenalin belongs to the group of catecholamines and different in structure from the adrenaline that metilny substituent in amino [NH-SNz] replaced by izopropilny [NH-CH (SNz) 2].
In izopropilnoradrenalina pharmacological study found that, while some properties contests, but he is on the actions of the past. Thus, it promotes relaxation bronchi, but it is narrowing the vessels and improve peripheral blood pressure; However, like adrenaline, it is increasing and strengthening the heart.
Therefore, it was suggested a different body types adrenoreceptor, which are mainly to interact adrenaline, izopropilnoradrenalin and similar connections with them. Finally that there were two major groups adrenoreceptor (a-and b-adrenoreceptor) was formulated in 1948 (A hlquist). In the future, these subgroups were identified receptors : a 1-and-2, 1-b and b-2 adrenoretseptory.
Izopropilnoradrenalin was the first representative of a new group-adrenergic substances b-adrenergic, or b-adrenostimulyatorov.
Following this, there were new b-adrenostimulyatory. A structural feature of these compounds is that they have side chain (alkilizopropilnoy, tert - alkyl butilnoy or another), reconciling them with the structure izopropilnoradrenalina.
The drugs and therapeutic effect izopropilnoradrenalina (izadrina) due to its stimulant properties of b-adrenoretseptory.
Step izadrina distributed simultaneously in the 1-b and b-2 adrenoretseptory, so the impact on the bronchi, the cardiovascular system and other organs equipped b-adrenoretseptorami, is not selective.
There are currently several new b-adrenostimulyatorov providing selective effect on 1-b and b-2 adrenoretseptory.
In connection with the characteristic stimulant for b-adrenoretseptory izadrin has strong bronhorasshiryayuschy effect is increased frequency and reduce heart, increases cardiac ejection.
However, it reduces the total peripheral vascular resistance (due to arterial vazoplegii) lowers blood pressure, reduces the content Poly heart. The drug increases the heart needs oxygen. Under the influence of the drug decreased renal blood flow, slightly increasing abdominal vessels, skin, mucous membranes (nose), a reduction of braking uterus can occur, and other effects related to the initiation of b-adrenoreceptor.
Izadrin despite a polling b 2-adrenostimulyatorov (ortsiprenalina, fenoterola, salbutamol, etc.), is still in use for edema and prevent asthma attacks, as well as asthma and bronchitis emfizematoznyh, pnevmoskleroze and other diseases, leading to the deterioration of bronchial passage. It may be used as a means to bronhorasshiryayuschee bronhografii and tomography.
In the framework of bronhorasshiryayuschego izadrina and other b-adrenostimulyatorov (ortsiprenalina, fenoterola, salbutamol and others) played the ability of these substances stimulate adenilattsiklazu that leads to the accumulation in the cells tsAMF. The latter, affecting system proteinkinazy deprive Myosin ability to connect to aktinom, slowing the decline smooth muscles and helps to relax bronchial and lifting bronhiolospazma. Moreover, the latest figures show a b-adrenostimulyatory stall the release of fat cells chemical factors (histamine, a substance medlennodeystvuyuschego "SRS-A or leykotriena 4 D, etc.) to bronhiolospazmu events and inflammation.
Assign izadrin as bronhorasshiryayuschego funds in the form of 0.5% or 1% aqueous solution for inhalation in the form of tablets containing 0,005 grams of preparation for resorption in the oral cavity. Inhalation produced with the assistance of pocket (or other) pump : one dose inhalation 0,1 0,2 ml. Again inhalation if necessary 2 - 3 times or more a day. Poltabletki pill or keep in his mouth (with the language) to complete resorption not proglatyvaya. Apply 3 to 4 times a day.
As bronhorasshiryayuschego funds izadrin second-best developed in recent years drugs. According to I. P. Zamotaeva and LN Maximov 'efficiency euspirana (izadrina) is 22 alupenta (ortsiprenalina) 34 - and 39-fenoterola.
Izopropilnoradrenalin is also used in the treatment of patients with violations atrioventrikulyarnoy conductivity, atrioventrikulyarnoy to lift the blockade and to prevent attacks in the Stokes-Adams syndrome, Morgani. The effect is linked with improved conductivity due to the influence of the sympathetic innervation of the heart, increased excitability and uterine function attacks. Similar effects have simpatomimeticheskie various substances, including Levophed, adrenaline, ephedrine; But these drugs cause increased blood pressure, stenokardicheskie pain, increased excitability Cumulative pockets and other side effects that limit their widespread use in atrioventrikulyarnoy blockade.
Izadrin and other b-adrenostimulyatory more suitable for this purpose because they do not raise blood pressure and are less able to cause fibrillation Poly.
Izopropilnoradrenalin also used in some forms kardiogennogo shock (normovolemicheskom with low emissions and high peripheral resistance). Enter intravenous drip in 5% glucose solution in the dose of 0.5 to 5 µ g (0.0005 - 0.005 mg) per minute.
In kardiohirurgicheskih operations izadrinom enjoyed in the case of abrupt sokratimosti attack in the absence of significant gipovolemii and tachycardia, and the aetiology against nodal and ventricular rhythm (if ineffective atropine).
In applying izadrina (particularly in cardiology practice), keep in mind that he was tachycardia can activate Cumulative pockets cause arrythmia risk fibrillation Poly. In applying izadrina, like other b-adrenostimulyatorov, for the treatment of asthma should also take into account the possibility of a violation of the cardiovascular system, the emergence of nausea, hand tremor, dry mouth. In these cases, reduce the dose of the drug. Caution should be observed in the appointment izadrina patients with strokes and thyrotoxicosis.
With long-term use may develop drug resistance to the lower bronhorasshiryayuschego effect.
Aerosol izadrina (and other b-adrenostimulyatorov) must not fall into the eye, especially in patients with glaucoma.
Not recommended izadrina and other b-adrenostimulyatorov in the first three months of pregnancy and given the dampening effect on generic activities (see Fenoterol), shortly before giving birth to halt the use of these drugs.
Method of issuance : powder; 0.5% and 1% solutions in bottles of 25 and 100 ml (for inhalation); Tablets containing 0,005 grams of the drug.
Storage : List B. In a dry, cool, the dark spot.
R p. : Sol. Isadrini 0.5 ml 25%
D.S. For inhalation
R p. : Ta b. Isadrini 0,005 N. 20
D.S. At one pill (keep in the oral cavity until the resorption)
Drugs produced in Germany "Novodrin (Novodrin) is izopropilnoradrenalina sulfate (izoprenalin- sulfate). According to the corresponding izadrinu.
Product : 1% solution in vials for inhalation of 100 mL and 0.5% solution of 1 ml ampoules. Also produced aerosol aluminium cylinders 25 ml spray with a metering valve. Each dose spray with one click, contains 0,075 mg powder (particle size of about 10 microns) drug. One container contains about 350 single doses.
In threatening attack of asthma or at the beginning inhale one dose. If the effect is not there, then in 3 to 5 minutes inhale another dose. Repeated ingyalyatsii possible after 3 - 4 hours The total number of inhaling a day should not be more than 12.
Preparation "Euspiran also corresponds izadrinu.
Product : 0.5% and 1% aqueous solutions in vials for inhalation to 25 ml.
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