ADRENERGIC DRUGS

- medical substances which act in adrenergic synapses Adrenergic drugs - medical substances which act in adrenergic synapses

Typical localization of adrenal receptors and changes of functions of organs which are observed during stimulation of these receptors Smooth muscles of vessels: skin mucsous membranes mesentery , organs of abdominal cavity skeletal muscles coronary lungs kidneys veins 1 2 Д1 Contraction of vessels - ’’ - - ’’ - Dilation of vessles M dillatator pupillae Ciliary muscle Heart 1 Midriasis (dilation of pupil) Dilation (far vision) Increasing of power and frequency of contraction, conductivity, automatism Bronchial muscles Bronchial glands 1, 2 Dilation of bronchi Decreasing of secretion, increasing of secretion Smooth musculature of GI tract: walls - sphincters 2, 2 Decreasing of tone, peristaltic Increasing of tone Smooth musculature of urinary bladder: sphincters Relaxation Contraction Liver Decomposition of glycogen Uterus (pregnant>not pregnant) Salivary glands  Increasing of secretion К+ and Н2О Increasing of amylase secretion Sweat glands Fat cells 3 Lipolysis Rennin secretion 2 Increasing Depression Insulin secretion Decreasing Presynaptic formations of adrenergic neurons Decreasing of releasing of nor-adrenalin into synaptic split Stimulation of releasing of nor-adrenalin into synaptic split Presynaptic formations of cholinergic neurons Stimulation of releasing of acetyl-choline into synaptic split

б) adrenomimetics of indirect action or sympathomimetics а) adrenomimetics of direct action б) adrenomimetics of indirect action or sympathomimetics Adrenoblockers or adrenolytics Sympatholytics

І. Adrenomimetics - і -adrenomimetics (adrenalin hydrochloride, noradrenalin hydrotartrate) 2. dopamine-, -, -adrenomimetics (dopamine) 3. -adrenomimetics (mesatone, naftizin, galazoline) 4. -adrenomimetics (isadrine, salbutamol, phenoterol, terbutalin, dobutamine) ІІ. Sympathomimetics (ephedrine hydrochloride) ІІІ. Adrenoblockers 1. -adrenoblockers (phentolamine, tropaphen, prasosine, pyroxan) 2. -adrenoblockers (anaprilin, athenolol, talinolol, acebutolol) 3. - і -adrenoblockers (labetalol) ІІІ. Sympatholytics (reserpine, octadine)

Adrenomimetcs

adrenaline hydrochloride Administration Adrenalin (epinephrine) is a hormone of medullar layer of adrenal glands which is used in a form of a remedy adrenaline hydrochloride It is an adrenomimetic which stimulates 1,- 2- and 1,- 2-adrenoreceptors Administration sudden stoppage of heart, for example, during surgical narcosis electric trauma shock and collapse conditions bronchial spasm hypoglycemic coma treatment of open-angle glaucoma

Noradrenalin hydrotartrate (norepinephrine) Is an adrenomimetic of direct action which stimulates 1-, 2- and 1-adrenal receptors Administration in cases of acute decreasing of blood pressure - shock and collapse conditions, surgeries, traumas The drug is absolutely contraindicated for subcutaneous and intramuscular introductions

Dopamine shock and collapse Drug of choice for treatment of of different etiology, including cardiogenic and hemorrhagic

Mesaton (phenilefrin) Is a synthetic a1-adrenomimetic drug of direct action Administration acute hypotensive conditions, prophylaxis of decreasing of blood pressure in case of infectious diseases, poisonings, decreasing of blood pressure during narcosis with fluorothan and cyclopropan nose drops in case of rhinits

Naphtisin Xylometazolin are a2-adrenomimetics of direct action Usage for rhinitis in a form of nose drops – 1-2 drops 2-3 times a day It is not recommended to use the drug in case of chronic cold

Isadrin (isoprenalin, novodrin, euspiran) – is a synthetic catecholamine, which is a strong stimulant of b1- і b2-adrenal receptors Administration bradycardia, atrio-ventricular blockade bronchial spasm complex therapy of some kinds of shock (if the patient doesn’t have hypovolemia) Side effects nausea, hands tremor, dryness in mouth, in patients with ischemic heart disease – attack of stenocardia, heavy cardiac tachyarrhythmias, even fibrillation of ventricles

Salbutamol (ventolin) selective b2-adrenomimetic of direct action Administration inhalations during attacks of bronchial asthma and bronchial spasms of other etiology, передчасних child delivery, бурхливій child delivery

Terbutalin (brikanil) and phenoterol (berotek, partusisten) are stimulants of mostly 2-adrenal receptors. They posses broncholytic and tokolytic activity

Dobutamin Administration Is a synthetic 1-adrenomimetic Cardiotonic effects of dobutamin is 5 times stronger than action of dopamine Administration some forms of acute and chronic cardiac insufficiency intravenous dropping infusion with the speed of 2,5-10 mcg / (kg.min)

Sympathomimetics

Ephedrine hydrochloride (Ephedrini hydrochloridum) It is an alkaloid of plants of Ephedra family, which has indirect a-, b-adrenomimetic (sympathomimetic) action Administration collapse conditions, for prophylaxis of decreasing of blood pressure before spinal anesthesia, infectious diseases treatment of rhinitis (2 %, 3 % solution to drop into nose). prophylaxis and elimination of bronchial spasm (inhalations 0,5 %-1 % solutions of drug) SIDE EFFECTS неспокій, excitement, tremor, inconsiderable euphoria, insomnia, seizures drug addiction tachyphylaxy

Adrenoblockers

Alfa-adrenoblockers

Phentolamine, tropaphen are synthetic a1, 2-аdrenoblockers administration diagnostics and symptomatic treatment of feochromocytoma disturbances of peripheral blood circulation in case of endarteritis, Reino’s disease, trophic ulcers, decubitus complex treatment of hypertensive crises, acute cardiac insufficiency complex therapy of hypovolemic and cardiogenic shock

Selective a1- adrenoblocker Prasosin Selective a1- adrenoblocker Administration treatment of essential hypertension stabile cardiac insufficiency Side effects “phenomenon of first dose”: sudden decreasing of blood pressure and even development of orthostatic collapse after first administrations of the drug Prophylaxis: administration of half-dose before sleep

Beta-adrenoblockers

Anaprilin Administration essential hypertension Is a selective b1- і b2-adrenoblocker Administration ischemic heart disease essential hypertension cardiac tachyarrhythmias acute myocardium infarction

Talinolol or cordanum Administration is a cardioselective b-adrenoblocker Administration disorders of cardiac rhythm (extrasystolies, paroxysmal tachycardia, fibrillation and scintillation of atria) stenocardia arterial hypetension .

Atenolol (tenormin) essential hypertension cardiac arrhythmias cardioselelctive -adrenoblocker of long action Indications for administration ischemic heart disease essential hypertension cardiac arrhythmias acute myocardium infarction

1-adrenoblocker with internal sympathomimetic activity Acebutolol (sectral) 1-adrenoblocker with internal sympathomimetic activity Indications disorders of cardiac rhythm (tachyarrhythmias) hypertension ischemic heart disease

Labetolol Contraindications -, -adrenoblocker. The drug blocks 1, 2, 1 and 2-adrenoreceptors Administration treatment of patients with essential hypertension hypertensive crisis Contraindications Atrio-ventricular blockade, cardiac insufficiency

Sympatholytics

Reserpin Administration Side effects manifestations of parkinsonism is a sum of раувольфії (plant) alkaloids. Maximal hypotensive action develops after 5-7 days of regular administration of the drug. After the treatment coarse effect can still stay for two weeks. Administration treatment of different forms of essential hypertension (combined drugs trirezid, cristepin, adelfan, brinerdin) Side effects manifestations of parkinsonism в’ялість, somnolence, depression, bradycardia increasing of motor and secretory activity of gastro-intestinal tract, acute attacks of ulcer disease, diarrhea swelling of nose mucous membrane with complication of nose breathing

Octadin Is a sympatholytic with strong hypotensive effect. During administration of the drug decreasing of blood pressure develops gradually, after 2-3 days. After quitting of drug administration the effect still stays for 2 weeks. Administration heavy forms of arterial hypertension Side effects general weakness, nausea, vomiting, swelling of nose mucous membrane, diarrhea, storing of liquid in the organism, orthostatic collapse.

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