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

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

3. Adrenergic synapse
MAO
KOMT

4. Adrenergic synapse
Neuron
Liver
Tissue

5. 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

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

7. 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)

8. Adrenomimetics

9. 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

10. 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

11. Necrosis

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

13. 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

14. 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

15. NAPHAZOLIN

16. 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

17. 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

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

19. 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)

20. Sympathomimetics

21. 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

22. Adrenoblockers

23. Alfa-adrenoblockers

24. 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

25. 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

26. Beta-adrenoblockers

27. Anaprilin Administration arterial hypertension
Is a β1- і β2-adrenoblocker
Administration
ischemic heart disease
arterial hypertension
cardiac tachyarrhythmias
acute myocardium infarction

29. 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 .

30. 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

31. 1-adrenoblocker with inner sympathomimetic activity
Acebutolol (sectral)
1-adrenoblocker with inner sympathomimetic activity
Indications
disorders of cardiac rhythm (tachyarrhythmias)
hypertension
ischemic heart disease

32. 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

33. 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)

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

35. Sympatholytics

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

37. 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

38. 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