Adrenergic receptor-acting drugs (adrenomimetics, adrenoblockers, sympatholitics) Lector prof. Posokhova K.A.

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

Adrenergic synapse MAO KOMT

Adrenergic synapse Neuron Liver Tissue

Typical localization of adrenal receptors and changes of functions 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 К+ , f amylase and Н2О secretion Sweat glands Increasing of secretion Insulin secretion 2 Decreasing Increasing 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 Sympatholytics

ІІ. Sympathomimetics (ephedrine) ІІІ. Adrenoblockers І. Adrenomimetics 1. - 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) ІІІ. Adrenoblockers 1.-adrenoblockers (phentolamine, tropaphen, prasosine, pyroxan) 2. -adrenoblockers (anaprilin, athenolol, talinolol, acebutolol) 3. - і -adrenoblockers (labetalol) ІІІ. Sympatholytics (reserpine, octadine)

Adrenomimetics

adrenaline hydrochloride Adrenalin (epinephrine) is a hormone of medulla of suprarenal 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 Cardiac arrest, for example, during surgical general anesthesia, electric trauma shock (anaphylactic shock) and collapse of different origin bronchial spasm hypoglycemic coma treatment of open-angle glaucoma

Noradrenalin hydrotartrate (norepinephrine) Is an adrenomimetic of direct action which stimulates 1-, 2- and 1-adrenoreceptors 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

Necrosis

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

Mesaton (phenylefrin) 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 halothan and cyclopropan for increasing of AP in hyperglycemic coma nose drops in case of rhinitis

It is not recommended for Naphthysin 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 for chronic cold Tachyphylaxis

NAPHAZOLIN

Isadrin (isoprenalin, novodrin, euspiran) – is a synthetic katecholamine, which is a strong stimulant of β1- і β2-adrenoreceptors 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, dry mouth, in patients with ischemic heart disease – acute ischemic attack, 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 premature child delivery, rapid (vigorous) child delivery

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

Dobutamin 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 α-, β-adrenomimetic (sympathomimetic) action Administration collapse conditions, for prophylaxis of decreasing of blood pressure before spinal anesthesia, infectious diseases treatment of rhinitis (2 %, 3 % solution as nose drops). prophylaxis and elimination of bronchial spasm (inhalations 0,5 %-1 % solutions of drug) SIDE EFFECTS agitation, excitement, tremor, inconsiderable euphoria, insomnia, seizures drug addiction tachyphylaxy

Adrenoblockers

Alfa-adrenoblockers

Phentolamine, tropaphen are synthetic 1, 2-аdrenoblockers administration diagnostics and symptomatic treatment of feochromocytoma disturbances of peripheral blood circulation in case of endarteriitis, Reino’s disease, trophic ulcers, decubitus complex treatment of hypertensive crises, acute cardiac insufficiency complex therapy of hypovolemic and cardiogenic shock

Selective  1- adrenoblocker Prasosin Selective  1- adrenoblocker Administration treatment of arterial hypertension 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 arterial hypertension Is a β1- і β2-adrenoblocker Administration ischemic heart disease arterial hypertension cardiac tachyarrhythmias acute myocardium infarction

Talinolol or cordanum Administration is a cardioselective β-adrenoblocker Administration disorders of cardiac rhythm (extrasystolies, paroxysmal tachycardia, fibrillation and scintillation of atria) ischemic heart disease arterial hypertension .

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

1-adrenoblocker with inner sympathomimetic activity Acebutolol (sectral) 1-adrenoblocker with inner 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 arterial hypertension hypertensive crisis Contraindications Atrio-ventricular blockade, cardiac insufficiency

increase the production of NO in blood vessels CARVEDILOL, NEBIVOLOL increase the production of NO in blood vessels are used now for chronic cardiac insufficiency (congestive heat failure)

Stimulates NO synthesis in endothelium Nebivolol – Nebilet Stimulates NO synthesis in endothelium

Sympatholytics

dihydralazine, hydrochlorothiazide) Reserpine Adelfan - Еsidrex (Reserpine, dihydralazine, hydrochlorothiazide) Rauwolfia Serpentina

Reserpin Administration Side effects fatigue, somnolence, depression, is a sum of Rauvolfia (plant) alkaloids. Maximal hypotensive action develops after 5-7 days of regular administration of the drug. After the treatment coarsed effect can still stay for two weeks. Administration treatment of different forms of essential hypertension (drugs of a second row, second line) (combined drugs trirezid, cristepin, adelfan, brinerdin) Side effects manifestations of parkinsonism fatigue, 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 abolition 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, liquid retention in the organism, orthostatic collapse