ADRENERGIC DRUGS Adrenergic drugs medical substances which act
ADRENERGIC DRUGS
Adrenergic drugs medical substances which act in adrenergic synapses
Adrenergic synapse MAO KOMT
Adrenergic synapse Liver Neuron 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 M dillatator pupillae Ciliary muscle Heart Bronchial muscles Bronchial glands Smooth musculature of GI tract: walls - sphincters Smooth musculature of urinary bladder: walls sphincters 1 1 2 1 2 1 Д 1 1 1 2 1 Contraction of vessels - ’’ Dilation of vessles Contraction of vessels Midriasis (dilation of pupil) Dilation (far vision) Increasing of power and frequency of contraction, conductivity, automatism 2 1, 2 Dilation of bronchi Decreasing of secretion, increasing of secretion 2, 2 1 Decreasing of tone, peristaltic Increasing of tone 2 1 Relaxation Contraction Liver 2 Uterus 1 2 Contraction Relaxation (pregnant>not pregnant) Salivary glands 1 Increasing of К+ , f amylase and Н 2 О secretion Sweat glands 1 Decomposition of glycogen Increasing of secretion Insulin secretion 2 Decreasing Increasing Presynaptic formations of adrenergic neurons 2 1 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
Adrenomimetics а) adrenomimetics of direct action б) adrenomimetics of indirect action or sympathomimetics Adrenoblockers Sympatholytics
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, prazosine, pyrroxan) 2. -adrenoblockers (anaprilin, athenolol, talinolol, acebutolol) 3. - і -adrenoblockers (labetalol, carvedilol) ІІІ. Sympatholytics (reserpine, octadine)
Adrenomimetics
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 u u Cardiac arrest, for example, during surgical general anesthesia, electric trauma shock (anaphylactic shock) and collapse of different origin u bronchial spasm u hypoglycemic coma u treatment of open-angle glaucoma
For prevention of anaphylactic shock
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 Drug of a first choice for treatment of shock and collapse of different etiology, including cardiogenic and hemorrhagic
Mesaton (phenylefrin) Is a synthetic a 1 -adrenomimetic drug of direct action Administration acute hypotensive conditions, u prophylaxis of decreasing of blood pressure in case of infectious diseases, poisonings, u decreasing of blood pressure during general anesthesia with halothane u for increasing of AP in hyperglycemic coma u nose drops in case of rhinitis u
Naphthysin Xylometazolin are nonselective adrenomimetics of direct action Usage for rhinitis in a form of nose drops – 1 -2 drops 2 -3 times a day u It is not recommended for chronic cold u Tachyphylaxis
NAPHAZOLIN
Isadrin (isoprenalin, novodrin, euspiran) – is a synthetic catecholamine, which is a strong stimulant of β 1 - і β 2 -adrenoreceptors Administration bradycardia, atrio-ventricular blockade u bronchial spasm u complex therapy of some kinds of shock (if the patient doesn’t have hypovolemia) u Side effects nausea, hands tremor, dry mouth, u in patients with ischemic heart disease – acute ischemic attack, u heavy cardiac tachyarrhythmia, even fibrillation of ventricles u
Isadrin (isoprenalin, novodrin, euspiran) Isoprenaline sulphate
Salbutamol (ventolin) selective b 2 -adrenomimetic of direct action Administration u inhalations during attacks of bronchial asthma bronchial spasms of etiology and any premature child delivery, rapid (vigorous) child delivery u
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 u collapse conditions, for prophylaxis of decreasing of blood pressure before spinal anesthesia, infectious diseases u treatment of rhinitis (2 %, 3 % solution as nose drops). u prophylaxis and elimination of bronchial spasm (inhalations 0, 5 %-1 % solutions of drug) SIDE EFFECTS u agitation, excitement, tremor, inconsiderable euphoria, insomnia, seizures u drug addiction u tachyphylaxis
Drugs which contain pseudoephedrinum, used for common cold Ø Ø Ø Ø Ibuprom sinus Actifed Broncholityn Grippex Daleron Zestra Tailol hot Ø Ø Ø Ø Kaffetin Kodefemol Rinostop Terosim Теrofun Traifed Teraflu
Pseudoephedrinum u Dextroisomer of ephedrinum u Activates -adrenoreceptors of the vessels of nose mucous, decreases edema u May provoke cerebral and cardiac ischemic attacks, dependence, arterial hypertension … u Hasn’t be combined with antidepressants
Adrenoblockers
Alfaadrenoblockers
Phentolamine, tropaphen are synthetic 1, 2 -аdrenoblockers administration diagnostics and symptomatic treatment of feochromocytoma u disturbances of peripheral blood circulation in case of endarteriitis, Reino’s disease, trophic ulcers, decubitus u complex treatment of hypertensive crises, acute cardiac insufficiency u complex therapy of hypovolemic and cardiogenic shock u
Prazosin Selective 1 - adrenoblocker Administration treatment of arterial hypertension (2 nd line therapy) Side effects u “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
Betaadrenoblockers
Anaprilin Is a β 1 - і β 2 -adrenoblocker Administration ischemic heart disease u arterial hypertension u cardiac tachyarrhythmia acute myocardium infarction u u
Talinolol or cordanum is a cardioselective β-adrenoblocker Administration disorders of cardiac rhythm (extrasystolia, paroxysmal tachycardia, fibrillation and scintillation of atria) u ischemic heart disease u arterial hypertension. u
Atenolol (tenormin) cardioselelctive -adrenoblocker with long duration of action Indications for administration ischemic heart disease u arterial hypertension u cardiac arrhythmias acute myocardium infarction u u
Acebutolol (sectral) 1 -adrenoblocker with inner sympathomimetic activity Indications disorders of cardiac rhythm (tachyarrhythmia) u hypertension u ischemic heart disease u
Labetolol -, -adrenoblocker. The drug blocks 1, 2, 1 and 2 -adrenoreceptors Administration u treatment of patients with arterial hypertension u hypertensive crisis Contraindications Atrio-ventricular blockade, cardiac insufficiency
CARVEDILOL, NEBIVOLOL increase the production of NO in blood vessels are used for AH, chronic cardiac insufficiency (congestive heat failure)
u. Nebivolol Nebilet u Stimulates – NO synthesis in endothelium
Sympatholytics
Reserpine Adelfan - Еsidrex (Reserpine, dihydralazine, hydrochlorothiazide) Rauwolfia Serpentina
Reserpin is a sum of Rauvolfia (plant) alkaloids. Maximal hypotensive action develops after 5 -7 days of regular administration of the drug. After the treatment coursed 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 u fatigue, somnolence, depression, u bradycardia u increasing of motor and secretory activity of gastro-intestinal tract, u acute attacks of ulcer disease, diarrhea u swelling of nose mucous membrane with complication of nose breathing u
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
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