Timolol

Chemical name

(S)-1-(трет-Бутиламино)-3- [(4-морфолино-1,2,5-тиади��зол-3-ил)окси]-2-пропан��л (gemigidrat or maleate)

Gross

C13-H24-N4-O3-S

Characteristics

Timolola maleate and gemigidrat white crystalline powder odourless. As a gemigidrata very soluble in water, it is readily soluble in alcohol; In the form of salt maleic acid is soluble in water, methanol, ethanol.

Of drugs

The drugs-gipotenzivne, antianginalnoe, antiaritmicescoe, protivoglaucomnoe. Does beta_1- beta_2-adrainoretseptora and has no internal and simpatomimeticescoy мембраностабилизирую щей activity. Stops central sympathetic impulsaciu and renin secretion. Ters sensitivity of peripheral tissues to kateholaminam. Oppressing automaticity sinoatrialnogo unit reduces a ectopiceskih pockets in predserdiah, AV connection jeludockah (to a lesser extent). Reduces the speed of the case, airway, cardiac ejection and the need heart of oxygen. Suppress activity baroretseptorov arc rivers, their reaction to the fall of AD. Provides cardioproteguoe effect. Decreases death after myocardial infarction and the risk of sudden death. Warn a headache vascular genesis (effective 50%). The local application reduces watery secretion moisture and helps its flow by reducing the inner pressure (as high or normal). Allows control inner pressure during Sna.pri the instillation begins in 10 to 30 minutes and lasts up to 24 hours (maximum achieved in 1-2 h). T_1/2 with local software-30 min. It absorbed through the retina eyes and the mucous membrane of the nose (perhaps the systemic effects). Absorbed from the blood by 90%, the material is not more than 50% due to the effects of the "first walk" through the liver. C_max plasma achieved in 1-2 hours Linking blood plasma is less than 10%. T_1/2 after intake of 4 hrs Penetrates into breast milk, a GEB and placental barrier. Biotransformiroetsa in liver, excreted kidneys (20%) and gastrointestinal, unedited, and in the form метаболитов.Увеличив��ет recurrence feohromotsytoma in rats (300 mg / kg / day of the interior within two years) induces development in mice (500 mg / kg / day of the interior) and the sound malignant lung tumors, good polipoza uterus and adenocartinoma breast (female). The studies in vivo (mice) and in vitro no mutagennogo action, however, is the change in the Ames test. The dose of 125 times the MRDC does not affect the fertility of both male and female rats. Increases the incidence rezorbtion fruit in mice and rabbits receiving doses, in 1000 and 100 times, respectively, over MRDC. It stops the ossification of the fruit rats without affecting the post-development progeny (50 mg / kg / day).

Indications

Inside : arterial hypertension, gipertrofica cardiomyopathy, mitral prolapse valve stenocardia, preventing re myocardial infarction, migraine (preventing attacks), essencialny tremor, anxiety. Locally : greater inner pressure, glaucoma (otkratougolnaya, secondary and afakii etc.).

Restrictions on the use of

Emphysema lungs, neallergicaki chronic bronchitis, rhinitis vazomotornyi illness Reynaud, the liver and / or kidney disorders, diabetes mellitus, hypoglycaemia, Ray, male, old age, pregnancy, for the appointment system, a children's age (safety and efficiency to be determined).

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Contraindications

To assign inwards and Local : hypersensitivity, bronchial asthma (incl. disease), chronic obstructive lung diseases, cardiogenny shock acute and chronic heart failure, AV blockade II extent sinoatrialnaya blockade sinusova aetiology (less than 45-50 u. / min) syndrome weakness sinusnogo unit; in the local application : dystrophic diseases cornea severe allergic inflammation of nasal mucous membrane, breastfeeding, young child (and preterm infants).

Side-Effects

From the nervous system and sensory organs : dizziness, headaches, fatigue, fatigue, insomnia, insomnia, nightmares, depression, agitation hallucinations, temporary amnesia, the spatial orientation, paresthesia, increased symptoms of myasthenia; noise in the ears; eye irritation, impaired vision, diplopia, ptos, dry mucous membranes eye; in the local application : passing of fog (30 seconds and 5 minutes 6%) burning and itching in the eyes, a sense of foreign body in the eye, change of refraction and Conclusion slezotechenie, refers, reducing sensitivity, corneal edema, corneal epithelial inflammation edges century, conjunctivitis, blefarit, surface pitting keratopatia, Keratit.so the respiratory system : zalojennosti nose, pain in the chest, cough, shortness of breath, choking, bronhospazm (possible death), respiratory Nedostaternsti.so the circulatory system (blood, gemostaz) : heart, symptomatic aetiology, incredible, AV blockade cardiac arrest, cardiac failure (possible death), gipotenzia, collapsed syndrome Reynaud, cooling limbs, worsening peremejateisa hromota, passing the cerebral circulation, cerebral ischaemia, sinkope lower hemoglobin, Gematokrita.so part of the intestine : dry mouth, anorexia, diarrhoea phenomenon, nausea, vomiting, Diarea.so the skin : skin rashes, urticaria, and the exacerbation of psoriasis, skin, prurigo, Alopecia.prochie : angioneuroticeski swelling, the syndrome, the change in mass body volchanochny syndrome, the weakening drive, impotence, disease Peyroni, giperkaliemia, giperuriquemia, гипертриглицеридемия .

Specific guidance

Before zacapavaniem bad turn and dramatically shake (less than or equal to 1 times). The treatment may change the test results of laboratory studies.

Patient interaction

Increases (mutually), the likelihood of violations of automaticity, and conduction sokratimosti hearts in the face of evidence, simpatolitikov, diltiazema, verapamila, hinidinovykh products; the risk of hypotension and cardiac decompensation activities, in the face of digidropiridinovh calcium antagonists, inhalation anesthetics. NPVS weaken gipotenzivny effect. The local application compatible with mioticescimi means, and besides carboangidraza. The simultaneous use of eye drops containing epinephrine or norapinefrin may create midriaz. Epinefrin- and pilocarpinsoderjaschie eye drops potenziruut decline vnutriglaznogo pressure. If you are systemic and local application бета-адреноблокаторо�� possibly linking effects.

Overdosing

Symptoms : dizziness, headache, nausea and vomiting, aetiology, Already, the acute cardiac insufficiency, Bronhospazm.lechenie : in the use of eye drops, an eye rinse with water or saline solution. The ingestion-washing stomach reception activated carbons symptomatic therapy : atropine, beta-adrainomimetiki (izoprenalin, izadrin) glukagona hydrochloride, vazopressornye system tools (norapinefrin, dobutamin) beta_2-adrainomimetiki (with bronhospazme); heart glycosides, dioretiki, aminofillin (with heart failure); oxygen; Follow cardiostimulyatsii. Haemodialysis weak.

Precautions

Before treatment should be compensated for heart disease. During a therapy monitoring HR, AD and earlier identification of the symptoms of heart failure. Violation of the liver and kidneys require dose reduction. Should be repealed for 48 h before operational intervention. Masks symptoms (tachycardia) gipoglikemii amidst reception protivodiabeticakih pills and insulin and tireotoxicoza (sudden removal may cause tireotoksicski kriz). Perhaps greater extent reactions гиперчувствительност и and the lack of economies of the usual doses of epinephrine with aggravated allergologicaki history. In order to reduce the intake after putting in the eye, at 1-2 min pressure finger at slezny channel of a cat eye. In zakratougolna glaucome use only in conjunction with mioticescimi means. Instillirovti other drugs recommended at least 10 minutes before applying Timolola.pri local application, it was necessary to monitor the slezootdelenia, integrity cornea and review every six months and inner pressure (within 4 weeks after the start of therapy). During treatment are allowed to wear only rigid contact lens (it should be removed before zacapavaniem and again put in 15 minutes). When converting optical patient with the therapy etc. бета-адреноблокатора��и no admission prior drug and the following day shall timolol. In the case of the other products antiglaucomnah be within 1 day of the two funds (under the supervision vnutriglaznogo pressure), and then continue using timolola. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention.

Dosing and Administration

Inside : with hypertension 10 mg twice a day, if necessary dose increases with weekly intervals to a maximum daily 60 mg. Preventing re myocardial infarction through 1-4 weeks after the first attack to 10 mg twice a day. The maximum daily dose of 30 mg (10 mg morning and 20 mg evening). Prevention of migraine attacks, the initial dose of 10 mg twice a day. Maximum daily-30 mg (10 mg morning and 20 mg evening). Kongungualno in stung eyes, adults and children on January 11th 0.25% -0.5% solution 1-2 times a day for six weeks (not more). After stabilization vnutriglaznogo pressure on the one drop once a day.

Literature

DV Preobrazhensky, A. Sidorenko, Romanov NE, Shatunov IM Clinical pharmacology major classes of drugs antigipertenziveh / / Consilium Medicum .- 2000 .- T. 2 .- N 3 .- C. 99-127.

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