Propranolol

Chemical name

1-[(1-Метилэтил)амино]-3-( 1-нафталенилокси)-2-про панол (and as hydrochloride); in drug form contains razemical mixture of enantiomers

Gross

C16-H21-N-O2

Characteristics

Propranolola hydrochloride, a white crystalline powder. Rat in the water and alcohol.

Of drugs

The drugs-gipotenzivne, antianginalnoe, antiaritmicescoe, uterotonizirutee. Does beta_1 and beta_2-adrainoretseptora has мембраностабилизирую щее Effects. Oppressing automaticity sinoatrialnogo unit suppresses a ectopiceskih pockets in predserdiah, AV connection jeludockah (to a lesser extent). Decreases speed of the proceedings in the AV connections to lift Kent, mostly in anterogranom direction. Urejaet variation, reduces the heartbeat and heart need of oxygen. Lowers heart release, renin secretion, AD kidney bloodstream and speed clubockova filtering. Suppress reaction baroretseptorov arc Even at the lower Ad.posle receiving a single dose gipotenzivny effect lasts for 20 to 24 hours Single admission prolonged forms equivalent to the admission of several doses propranolola hydrochloride. Gipotenzia stabilize by the end of the second week of treatment. With long-term use decreases venous return has cardioproteguoe Effects (reliably reduces the risk of re-myocardial infarction and sudden death by 20-50%). The patients with a moderate form of hypertension, reduces risk of developing ischemic heart disease and cerebral stroke. The disease reduces the frequency of attacks increases the portability of loads, reduces the need for nitroglycerine. The most effective in patients younger age group (up to 40 years) with type giperdinamicheski circulatory and increased content renin. Increases tone bronchi and airway uterus (reduces bleeding during childbirth and in the aftercare period), increased secretornuu and motor activity decreases. Agregatia stops platelets and activates fibrinoliz. Oppressing lipolysis in adipose tissue, preventing increased free fatty acid (with the concentration of triglycerides in plasma and haemoglobin rate increase. Suppress glikogenoliz, glukagona secretion and insulin, making tiroksina in triyodtironin. lowers inner pressure reduces watery secretion Vlagi.dlitionoe introduction (18 months) rats and mice doses up to 150 mg / kg / day revealed no carcinogenic properties and the adverse impact on fertility. The dose of 150 mg / kg / day, 10 times higher than the MRDC, embriotoksicescoe provided the (increase in the incidence of rezorbtion fruit). The ingestion quickly and almost completely absorbed from the gastrointestinal (90%). bioavailability of 30-40% (effect "of a"), depends on the nature of food and intensity pechenerngo blood flow and increases in the long admission (metabolites formed, ingibirute liver enzymes). C_max plasma is a 1-1.5 hrs or 6900 (for the extended form). associated with the plasma protein at the 90-95%; T_1/2 is 2-5 hours (10 hours for the extended form). The distribution 3-5 l / kg collected in the lung tissue, brain, kidney, heart, passes through the placental barrier, enters the breast milk. Treated glukuronirovaniu in the liver (99%). Return to jelchew in intestine, deglukuroniruetsa and reabsorbiruetsa (T_1/2 against the backdrop of a currency can lengthen to 12 hours). excreted news in the form of metabolites.

Indications

Arterial hypertension, stenocardia, sinusova tachycardia (including the gipertireoze) najeludochkovaya tachycardia, a form of tahisistolica predserdy times, and najeludochkovaya ventricular arrythmia, gipertrofica cardiomyopathy, myocardial infarction, prolapse mitral valve subaortalny stenoses, simpatikoarenalovy kriz in patients diengjefalnam syndrome, neirocirkulatornaya distonia, portal hypertension, essencialny tremor, panic attacks, aggressive behaviour, migraine (prevention), support treatment feohromotsytome (only in combination with alfa-adrenoblokatorami) thyrotoxicosis (including preoperative preparation), tireotoksicski kriz, primary weakness generic activities menopauzne vazomotorne symptoms, the withdrawal syndrome; akatizia treatment, by neiroleptikami.

Restrictions on the use of

Chronic bronchitis, emphysema, diabetes mellitus, hypoglycaemia, acidosis, the liver and kidneys, psoriasis, spasticeski Colitis, male, pregnancy, breast-feeding, old age.

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

Hypersensitivity, AV blockade II extent sinoatrialnaya blockade aetiology (less than 55 u. / min), the weakness syndrome sinusnogo unit arterial gipotenzia, acute and severe chronic heart failure, stenocardia Prinzmetala, cardiogenny shock obliterirute Vascular Diseases, bronchial asthma.

Side-Effects

From the circulatory system and blood (blood, gemostaz) : aetiology, cardiac insufficiency, AV blockade gipotenzia violation of peripheral blood circulation, trombozitopenica purpura, lakopenia, Agranulozitoz.so the nervous system and sensory organs : fatigue, dizziness, headache, insomnia, drowsiness, nightmares, Reducing the speed of mental and motor reactions, emotional lability, depression, causing hallucinations, disorientation in time and space, temporary amnesia the sensitivity parestesia; dry eye, the disorder, �ератоконъюнктивит.Со �torona the stomach : nausea, vomiting, pain in the abdomen, diarrhoea or constipation, mezenterialna coronary artery ischemic Kolit.so the respiratory system : aringit, pain in the chest, cough, shortness of breath, and bronho- laringospazm, respiratory Distress-sindrom.so the Skin : alopecia, rash, itchy skin, bostrenie Psoriaza.prochie : the syndrome, the weakening drive, impotence, disease Peyroni, artralgia, allergies volchanochny syndrome, hypoglycaemia fever.

Specific guidance

The treatment may change the results of tests in the laboratory (more urea transaminaz, phosphatases, LDG).

Patient interaction

Do (mutually) negative impact verapamila and diltiazema the miocard, prolong the nedepoliarizuth miorelaksantov dampens down lidocaine. Gipotenzivny weaken effect NPVS, glukokortikoida, estrogena, cocaine; Add-nitrates and other gipotenzivee funds. Heparin, antatsida diminishes the level of plasma; Zimetidin and fenotiazina raise. Not recommended simultaneous with MAO inhibitors. Wrinkles theofillina metabolism and increases its concentration in plasma.

Overdosing

Symptoms : dizziness, aetiology, incredible, heart failure, gipotenzia, collapse, difficulty breathing, akrozianoz, Sudorogi.lechenie : washing stomach, and the appointment of absorbent, symptomatic therapy : atropine, beta-adrainomimetiki (izoprenalin, izadrin), sedation (diazepam, lorazepam), cardiac (dobutamin, dopamine, epinephrine) drugs vazopressornye means glukagon, etc.; Follow transvenozna stimulation. Haemodialysis ineffective.

Precautions

Treatment should be carried out with regular doctor control. With long-term use should consider the possibility of additional supplies of cardiac glycosides. Decreases compensatory cardiovascular reactions in response to the use of general anaesthetics. A few days before the narcosis must stop receiving or select an anaesthetic with the least negative effect inotrope. Not recommended / with the introduction of children. Older patients increased risk of the side effects of the central nervous system. If any of the liver to reduce doses and surveillance in the first 4 days of therapy. It may mask the symptoms gipoglikemii (tachycardia), in patients with diabetes receiving insulin, etc. gipoglikemicakie drugs. Perhaps greater extent reaction гиперчувствительност и and the lack of economies of the usual doses of epinephrine with aggravated allergologicaki history. At the time of treatment remenduetsa exclude alcohol. Be wary of during the drivers of vehicles and people skills relate to the high concentration of attention. Cease treatment gradually, within a period of approximately two weeks.

Dosing and Administration

In / in, struino, slowly adults for short adults, tireotoksicski kriza, acute Ischemia-1 mg for 1 min, in the need to repeat at intervals of 2 minutes (under the supervision of ECG and AD). The maximum dose of 10 mg. Inside, squeezed liquid or semi food (water, juice, fruit puree, pudding), adults : with hypertension, initial dose, 80 mg twice a day, supporting-dose 160-320 mg. Prolongirovanne forms : 80 mg once a day, if necessary, to 120-160 mg once, under the control of AD. In аритмиях on 10-30 mg 3-4 times a day, in subaortalinom stenoze on 20-40 mg 3-4 times a day. The gantries hypertension, stroke, migraines, anxiety, tremore initial dose of 40 mg three times a day supporting-160, 120, 80-160, 80-120, 80-160 mg / day, respectively. In feohromotsytome, 30-60 mg / day for 3 days (before surgery). In myocardial infarct, in the period from May to the 21st day after the attack on 40 mg four times a day for a period of two to three days, followed by 80 mg twice a day. To facilitate the delivery of 20 mg in 30 minutes 4-6 times (80-120 mg / day) for the prevention of postpartum hemorrhage, and 20 mg three times a day for three to five days. In glaucome - внутриконъюнктивальн о in the hit Glaz.detam : inwards initial dose : 0.5-1 mg / kg / day supporting-2-4 mg / kg / day in 2 admission.

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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