ADRENERGIC ADRENERGIC DRUGSDRUGS

Adrenergic drugsAdrenergic drugs

- medical substances - medical substances which act in adrenergic which act in adrenergic

synapsessynapses

Smooth muscles of vessels:- skin- mucsous membranes- mesentery , - organs of abdominal cavity- skeletal muscles- coronary- lungs- kidneys- veins

1

1

1 1

2

1

2

1

2

1

Д1

1

Contraction of vessels - ’’ - - ’’ - - ’’ - - ’’ -Dilation of vesslesContraction of vesselsDilation of vesslesContraction of vesselsDilation of vesslesContraction of vesselsDilation of vesslesContraction of vessels

M dillatator pupillaeCiliary muscleHeart

1

2 1

Midriasis (dilation of pupil)Dilation (far vision)Increasing of power and frequency of contraction,

conductivity, automatism

Bronchial musclesBronchial glands

2

1, 2

Dilation of bronchiDecreasing of secretion, increasing of secretion

Smooth musculature of GI tract:- walls - sphincters

2, 2

1 Decreasing of tone, peristaltic Increasing of tone

Smooth musculature of urinary bladder:- walls- sphincters

2

1

Relaxation Contraction

Liver 2Decomposition of glycogen

Uterus 1

2

Contraction Relaxation (pregnant>not pregnant)

Salivary glands 1

Increasing of secretionК+ and Н2ОIncreasing of amylase secretion

Sweat glands 1Increasing of secretion

Fat cells 3Lipolysis

Rennin secretion 1

2

Increasing Depression

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 2Stimulation of releasing of acetyl-choline into synaptic

split

Typical localization of adrenal receptors and changes of functions of organs which are observed during stimulation of these receptors

Adrenomimetics Adrenomimetics а) а) adrenomimetics of direct actionadrenomimetics of direct action

б) б) adrenomimetics of indirect actionadrenomimetics of indirect action or or sympathomimeticssympathomimetics

Adrenoblockers Adrenoblockers or adrenolyticsor adrenolytics

Sympatholytics Sympatholytics

І. І. Adrenomimetics Adrenomimetics 1.1.- і - і --adrenomimeticsadrenomimetics ( (adrenalin hydrochlorideadrenalin hydrochloride, ,

noradrenalin hydrotartratenoradrenalin hydrotartrate))2. 2. dopaminedopamine-, -, -, -, --adrenomimeticsadrenomimetics ( (dopaminedopamine))3. 3. --adrenomimeticsadrenomimetics ( (mesatonemesatone, , naftizinnaftizin, , galazolinegalazoline))4. 4. --adrenomimeticsadrenomimetics ( (isadrineisadrine, , salbutamolsalbutamol, ,

phenoterolphenoterol, , terbutalinterbutalin, , dobutaminedobutamine))ІІ. ІІ. Sympathomimetics Sympathomimetics ((ephedrine hydrochlorideephedrine hydrochloride))ІІІ. ІІІ. Adrenoblockers Adrenoblockers 1. 1. --adrenoblockersadrenoblockers ( (phentolaminephentolamine, , tropaphentropaphen, ,

prasosineprasosine, , pyroxanpyroxan))2.2. --adrenoblockersadrenoblockers ( (anaprilinanaprilin, , athenololathenolol,, talinolol talinolol, ,

acebutololacebutolol))3. 3. - і - і --adrenoblockersadrenoblockers ( (labetalollabetalol))ІІІ. ІІІ. Sympatholytics Sympatholytics ((reserpine, octadinereserpine, octadine))

Adrenomimetcs Adrenomimetcs

Adrenalin (epinephrineAdrenalin (epinephrine)) is a hormone is a hormone of medullar layer of adrenal glands which is used in a of medullar layer of adrenal glands which is used in a

form of a remedyform of a remedy

adrenaline hydrochlorideadrenaline hydrochloride

It is an adrenomimetic which stimulates It is an adrenomimetic which stimulates 11,- ,- 22-- and and 11,- ,- 22--adrenoreceptorsadrenoreceptors

Administration Administration sudden stoppage of heartsudden stoppage of heart, , for examplefor example, , during during

surgical narcosissurgical narcosis electric trauma electric trauma

shock and collapse conditionsshock and collapse conditions bronchial spasmbronchial spasm

hypoglycemic comahypoglycemic coma treatment of open-angle glaucomatreatment of open-angle glaucoma

Noradrenalin hydrotartrateNoradrenalin hydrotartrate ((norepinephrinenorepinephrine))

Is an adrenomimetic of direct action which Is an adrenomimetic of direct action which stimulates stimulates 11-, -, 22- - andand 11--adrenal receptorsadrenal receptors

Administration Administration in cases of acute decreasing of blood in cases of acute decreasing of blood

pressure - shock and collapse conditions, pressure - shock and collapse conditions, surgeries, traumassurgeries, traumas

The drug is absolutely contraindicated for The drug is absolutely contraindicated for subcutaneous and intramuscular subcutaneous and intramuscular

introductionsintroductions

Dopamine Dopamine

Drug of choice for treatment of Drug of choice for treatment of

shock and collapseshock and collapse of different etiology, including of different etiology, including cardiogenic and hemorrhagiccardiogenic and hemorrhagic

Mesaton Mesaton ((phenilefrinphenilefrin))Is a syntheticIs a synthetic a a11--adrenomimetic drug of direct actionadrenomimetic drug of direct action

Administration Administration acute hypotensive conditionsacute hypotensive conditions,,

prophylaxis of decreasing of blood pressure in prophylaxis of decreasing of blood pressure in case of infectious diseases, poisoningscase of infectious diseases, poisonings,,

decreasing of blood pressure during narcosis decreasing of blood pressure during narcosis with fluorothan and cyclopropanwith fluorothan and cyclopropan

nose drops in case of rhinitsnose drops in case of rhinits

NaphtisinNaphtisin

XylometazolinXylometazolinareare a a22--adrenomimetics of direct actionadrenomimetics of direct action

Usage Usage for rhinitis in a form of nose drops – for rhinitis in a form of nose drops – 1-1-

22 dropsdrops 2-3 2-3 times a daytimes a day

It is not recommended to use the drug in It is not recommended to use the drug in case of chronic coldcase of chronic cold

Isadrin Isadrin ((isoprenalinisoprenalin, , novodrinnovodrin, , euspiraneuspiran) )

– – is a synthetic catecholamineis a synthetic catecholamine, , which is a strong stimulant which is a strong stimulant ofof b b11- і b- і b22--adrenal receptorsadrenal receptors

Administration Administration bradycardiabradycardia, , atrio-ventricular blockadeatrio-ventricular blockade bronchial spasmbronchial spasm complex therapy of some kinds of shockcomplex therapy of some kinds of shock ( (if the patient if the patient

doesn’t have hypovolemiadoesn’t have hypovolemia))

Side effectsSide effects nausea, hands tremornausea, hands tremor, , dryness in mouthdryness in mouth,, in patients with ischemic heart diseasein patients with ischemic heart disease – – attack of attack of

stenocardiastenocardia,, heavy cardiac tachyarrhythmiasheavy cardiac tachyarrhythmias, , even fibrillation of even fibrillation of

ventriclesventricles

SalbutamolSalbutamol ((ventolinventolin))

selective selective bb22--adrenomimetic adrenomimetic of direct actionof direct action

Administration Administration inhalations during attacks inhalations during attacks

of bronchial asthma and of bronchial asthma and bronchial spasms of other bronchial spasms of other etiologyetiology,,

передчасних передчасних child child deliverydelivery, бурхливій , бурхливій child child deliverydelivery

Terbutalin Terbutalin ((brikanilbrikanil) ) and phenoteroland phenoterol ((berotekberotek, , partusistenpartusisten))

are stimulants of mostlyare stimulants of mostly 22--adrenal receptors. They adrenal receptors. They posses broncholytic and tokolytic activityposses broncholytic and tokolytic activity

Dobutamin Dobutamin Is a synthetic Is a synthetic 11--adrenomimeticadrenomimetic

Cardiotonic effects of dobutamin is 5 times Cardiotonic effects of dobutamin is 5 times stronger than action of dopamine stronger than action of dopamine

AdministrationAdministrationsome forms of acute and chronic cardiac some forms of acute and chronic cardiac

insufficiencyinsufficiency intravenous dropping infusion with the intravenous dropping infusion with the

speed ofspeed of 2,5-10 2,5-10 mcg mcg // ((kgkg..minmin) )

Sympathomimetics Sympathomimetics

Ephedrine hydrochlorideEphedrine hydrochloride (Ephedrini (Ephedrini hydrochloridum) hydrochloridum)

It is an alkaloid of plants ofIt is an alkaloid of plants of Ephedra familyEphedra family, , which has which has indirect indirect a-, b-a-, b-adrenomimeticadrenomimetic ( (sympathomimeticsympathomimetic) ) actionaction

Administration Administration collapse conditions, for prophylaxis of decreasing of blood collapse conditions, for prophylaxis of decreasing of blood

pressure before spinal anesthesiapressure before spinal anesthesia,, infectious diseases infectious diseases

treatment of rhinitistreatment of rhinitis (2 %, 3 % (2 %, 3 % solution to drop into nosesolution to drop into nose).).

prophylaxis and elimination of bronchial spasm prophylaxis and elimination of bronchial spasm ((inhalationsinhalations 0,5 %-1 0,5 %-1 % % solutions of drugsolutions of drug))

SIDE EFFECTSSIDE EFFECTS неспокій, неспокій, excitementexcitement, , tremortremor, , inconsiderable euphoriainconsiderable euphoria, , insomniainsomnia, ,

seizuresseizures

drug addictiondrug addiction

tachyphylaxytachyphylaxy

Adrenoblockers Adrenoblockers

Alfa-adrenoblockersAlfa-adrenoblockers

PhentolaminePhentolamine, , tropaphentropaphenare syntheticare synthetic a a11, , 22-а-аdrenoblockersdrenoblockers

administrationadministration diagnostics and symptomatic treatment of diagnostics and symptomatic treatment of

feochromocytomafeochromocytoma disturbances of peripheral blood circulationdisturbances of peripheral blood circulation

in case of endarteritis, Reino’s diseasein case of endarteritis, Reino’s disease,, trophic trophic ulcers, decubitusulcers, decubitus

complex treatment of hypertensive crisescomplex treatment of hypertensive crises,, acute cardiac insufficiencyacute cardiac insufficiency

complex therapy of hypovolemic and complex therapy of hypovolemic and cardiogenic shockcardiogenic shock

Prasosin Prasosin

SelectiveSelective a a11-- adrenoblocker adrenoblocker

Administration Administration treatment of essential hypertensiontreatment of essential hypertension stabile cardiac insufficiencystabile cardiac insufficiency

Side effectsSide effects““phenomenon of first dosephenomenon of first dose”: ”: sudden decreasing sudden decreasing of blood pressure and even development of of blood pressure and even development of orthostatic collapse after first administrations of orthostatic collapse after first administrations of the drugthe drugProphylaxisProphylaxis: : administration of half-dose before administration of half-dose before sleepsleep

Beta-adrenoblockersBeta-adrenoblockers

Anaprilin Anaprilin Is a selectiveIs a selective b b11- і b- і b22--adrenoblockeradrenoblocker

Administration Administration ischemic heart diseaseischemic heart disease

essential hypertensionessential hypertension

cardiac tachyarrhythmiascardiac tachyarrhythmias

acute myocardium infarctionacute myocardium infarction

Talinolol or cordanumTalinolol or cordanum

is a cardioselectiveis a cardioselective

b-b-adrenoblockeradrenoblocker

AdministrationAdministration disorders of cardiac rhythmdisorders of cardiac rhythm

((extrasystoliesextrasystolies,, paroxysmal tachycardia paroxysmal tachycardia, , fibrillation and scintillation of atriafibrillation and scintillation of atria))

stenocardiastenocardia

arterial hypetensionarterial hypetension

..

Atenolol Atenolol ((tenormin)tenormin)cardioselelctivecardioselelctive --adrenoblocker of long actionadrenoblocker of long action

Indications for administrationIndications for administration ischemic heart diseaseischemic heart disease essential hypertensionessential hypertension

cardiac arrhythmiascardiac arrhythmias acute myocardium infarctionacute myocardium infarction

Acebutolol Acebutolol ((sectralsectral))11--adrenoblocker with internal adrenoblocker with internal

sympathomimetic activitysympathomimetic activity

IndicationsIndications disorders of cardiac rhythm disorders of cardiac rhythm

(tachyarrhythmias(tachyarrhythmias))

hypertensionhypertension

ischemic heart diseaseischemic heart disease

Labetolol Labetolol

-, -, --adrenoblockeradrenoblocker. . The drug blocksThe drug blocks 11, , 22, , 1 1

andand 22--adrenoreceptorsadrenoreceptors

Administration Administration treatment of patients with essential treatment of patients with essential

hypertensionhypertension

hypertensive crisishypertensive crisis

ContraindicationsContraindications Atrio-ventricular blockadeAtrio-ventricular blockade,,

cardiac insufficiencycardiac insufficiency

Sympatholytics Sympatholytics

ReserpinReserpin is a sum of is a sum of раувольфіїраувольфії (plant) alkaloids (plant) alkaloids. . Maximal hypotensive actionMaximal hypotensive action developsdevelops afterafter 5-7 5-7 daysdays of regular administration of the drugof regular administration of the drug. . After the After the treatment coarse effect can still stay for two weekstreatment coarse effect can still stay for two weeks..

Administration Administration treatment of different forms of essential hypertensiontreatment of different forms of essential hypertension ((combined combined drugs trireziddrugs trirezid, , cristepincristepin, , adelfanadelfan, , brinerdinbrinerdin))

Side effectsSide effects manifestations of parkinsonismmanifestations of parkinsonism в’ялість, в’ялість, somnolencesomnolence, , depressiondepression,, bradycardiabradycardia increasing of motor and secretory activity of gastro-increasing of motor and secretory activity of gastro-

intestinal tractintestinal tract, , acute attacks of ulcer diseaseacute attacks of ulcer disease, , diarrheadiarrhea swelling of nose mucous membrane with complication swelling of nose mucous membrane with complication

of nose breathingof nose breathing

Octadin Octadin Is a sympatholytic with strong hypotensive effectIs a sympatholytic with strong hypotensive effect. . During During administration of the drug decreasing of blood pressure administration of the drug decreasing of blood pressure develops graduallydevelops gradually, , afterafter 2-3 2-3 daysdays. . After quitting of drug After quitting of drug administration the effect still stays foradministration the effect still stays for 2 2 weeksweeks..

Administration Administration heavy forms of arterial hypertensionheavy forms of arterial hypertension

Side effectsSide effects general weaknessgeneral weakness,, nauseanausea, , vomitingvomiting,, swelling of nose mucous membraneswelling of nose mucous membrane,, diarrheadiarrhea,, storing of liquid in the organism,storing of liquid in the organism, orthostatic collapseorthostatic collapse. .

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