1. Adrenergic preparations

3. ά2 β2 β1 ά1
CОМТ
МАО

5. Localization of alfa-adrenoceptors

6. Localization of alfa-adrenoceptors

7. Localization of beta-adrenoceptors

8. Localization of beta2-adrenoceptors

9. Localization of beta3-adrenoceptors
β3-adrenoceptors are located in the cells of fatty tissue, in the mast cells and in pancreatic β-cells. Their excitation leads correspondingly to increase of lipolysis, to inhibition of mast cell degranulation and to stimulation of insulin release.

11. Excitation:
Of α-receptors causes the increasing of functions (tone of smooth muscles) except intestine and uterus
Of β- receptors – decreasing of functions (tone of smooth muscles) except heart

12. Adrenomimetics Directly acting
– Adrenalini hydrochloridum – α1 α2 β1 β2 β3
-Noradrenalini hydrotartras – α1 α2 β1
- Mesatonum - α1
-Isadrinum - β1 β2
-Dobutamine - β1
-Salbutamolum - β2
Fenoterolum - β2
Indirect action –
- Ephedrini hydrochloridum α1 α2 β1 β2 β3

15. The main effects of adrenaline
the increase of automatism (heart rate),
excitability, conduction and contractility (cardiac output) of myocardium
the increase of the arterial pressure,
hyperglycemia,
dilation of bronchi,
dilation of pupils
inhibition of mast cell degranulation
increase of oxygen demand and production of energy.

16. The main effects of noradrenaline
acts predominantly upon the cardiovascular system –
increases the arterial pressure (both systolic and diastolic one)
The rapid increase of arterial pressure stimulates a reflex reaction from vascular mechanoceptors that leads to the development of sinus bradycardia
introduced only intravenously because in subcutaneous or intramuscular introduction it causes strong local vasospasm that may be accompanied by development of necrosis.

17. Ephedrini hydrochloridum
Acts upon the presynaptic membrane and stimulates noradrenaline release from the sympathetic nerve endings. It also slightly excites the adrenoceptors located on the postsynaptic membrane.
The same effects as Adrenaline, but it's less active (in times), action develops gradually and lasts longer stimulates the CNS, may cause psychomotor excitement, insomnia and euphoria (drug dependence).
In the repeated introduction of ephedrine within small interval (10-30 mm.) the tachyphylaxis appears

18. Ephedra

19. Indications for use- Adrenaline
anaphylactic shock and some other allergic reactions,
bronchial asthma,
acute hypotension (collaps),
hypoglycemic coma,
cardiac arrest,
depression of excitability and conduction of myocardium,
for extension of local anesthetics' action.
Locally- in open angle glaucoma, for the arrest of capillary hemorrhage
Adrenaline is used only by parenteral way or locally because its destroyed in oral introduction.

20. Mesatonum increases BP -indicated in collaps

21. Indications for use-
Isadrinum - indicated in bronchial asthma, atrioventricular blockade, bradycardia.
Salbutamol, fenoterol - bronchial asthma, premature or precipitated labor
Dobutamine - acute heart failure which accompanies the myocardial infarction.

22. Alpha-Adrenergic Blockers
Type of blockade Tropaphenum – non-competitive; slow onset and long duration. 2-stage blockade All the rest: competitive
Selectivity Nonselective: Tropaphenum and phentolamine alpha-1 selective: Prazosin, terazosin, others alpha-2 selective: Yohimbine alpha/beta blockers: Labetalol
Others: phenothiazines, tricyclic antidepressants

23. Pharmacological Effects
Eye - miosis
GI tract – Increased motility
Urinary bladder – decreased tone in sphincter
Metabolic effects – increased insulin secretion

24. Imidazoline derivatives - phentolamine
Many other effects including:
Parasympathomimetic
Increased gastric acid secretion
Cardiac stimulation
Increased secretion from exocrine glands, such as salivary, sweat, lacrimal, pancreatic
Coronary artery disease and peptic ulcer relative contraindication to it.

25. Alpha-1 selective blockers Prazosin
Less cardiac stimulation since it preserves alpha-2 mediated negative feedback + other mechanisms
Used in congestive heart failure and in hypertension but tolerance develops with time, maybe due to fluid retention.
Adverse effects: First dose phenomenon.
Favorable effect on plasma lipids: increase HDL/LDL ratio

26. Pharmacological Properties Propranolol
Cardiovascular
Blood pressure, heart rate, cardiac output, peripheral vascular resistance, coronary and organ blood flows
Pulmonary
Central Nervous System
Metabolic

27. Antihypertensive Effect of Beta-Blockers Mechanisms
1. Decreased cardiac output
2. Inhibition of renin-angiotensin system
3. Decreased central sympathetic outflow
4. Resetting of baroreceptor
5. Others: prejunctional receptors, prostaglandins, etc.

28. Beta-Blockers - Adverse Effects
Cardiac (mechanical; electrical)
Vascular (decreased perfusion)
Pulmonary (bronchocostriction)
Metabolic (diabetes mellitus)
Central Nervous System (depression, nightmares, etc.)
Withdrawal Syndrome