Adrenergic receptor-acting drugs

(adrenomimetics, adrenoblockers,
sympatholytic)
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: 1 Contraction of vessels

- skin 1 - ’’ -
- mucsous membranes 1 - ’’ -
- mesentery , - ’’ -
- organs of abdominal cavity 1 - ’’ -
- skeletal muscles 2 Dilation of vessles
- coronary 1 Contraction of vessels
- lungs 2 Dilation of vessles
- kidneys 1 Contraction of vessels
- veins 2 Dilation of vessles
1 Contraction of vessels
Д1 Dilation of vessles
1 Contraction of vessels
M dillatator pupillae 1 Midriasis (dilation of pupil)
Ciliary muscle 2 Dilation (far vision)
Heart Increasing of power and frequency of contraction, conductivity,
1 automatism
Bronchial muscles 2 Dilation of bronchi
Bronchial glands 1,  2 Decreasing of secretion, increasing of secretion
Smooth musculature of GI tract:
- walls 2,  2 Decreasing of tone, peristaltic
- sphincters 1 Increasing of tone
Smooth musculature of urinary bladder:
- walls 2 Relaxation
- sphincters 1 Contraction
Liver 2 Decomposition of glycogen
Uterus 1 Contraction
2 Relaxation
(pregnant>not pregnant)
Salivary glands 1 Increasing of К+ , f amylase and Н2О
 secretion
Sweat glands 1 Increasing of secretion
Insulin secretion 2 Decreasing
 Increasing
Presynaptic formations of adrenergic neurons 2 Decreasing of releasing of nor-adrenalin into synaptic split
1 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
 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
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 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
general anesthesia with halothane
 for increasing of AP in hyperglycemic
coma
 nose drops in case of rhinitis
 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
 It is not recommended for
chronic cold
 Tachyphylaxis
NAPHAZOLIN
 Isadrin (isoprenalin,
novodrin, euspiran)
– is a synthetic catecholamine, 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 tachyarrhythmia, even fibrillation
of ventricles
Isadrin (isoprenalin,
novodrin, euspiran)

Isoprenaline
sulphate
 Salbutamol
(ventolin)
selective
b2-adrenomimetic
of direct action
Administration
 inhalations during attacks
of bronchial asthma and
bronchial spasms of any
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

 tachyphylaxis
Drugs which contain pseudoephedrinum,
used for common cold

 Ibuprom sinus  Kaffetin

 Actifed  Kodefemol
 Broncholityn  Rinostop
 Grippex  Terosim
 Daleron  Теrofun
 Zestra  Traifed
 Tailol hot  Teraflu
 Pseudoephedrinum
 Dextroisomer of ephedrinum
 Activates -adrenoreceptors of
the vessels of nose mucous,
decreases edema

 May provoke cerebral and cardiac

ischemic attacks, dependence,
arterial hypertension …
 Hasn’t be combined with
antidepressants
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
 Prazosin
Selective  1- adrenoblocker
Administration
 treatment of arterial hypertension (2nd
line therapy)
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
Is a β1- і β2-adrenoblocker

Administration
 ischemic heart disease
 arterial hypertension

 cardiac tachyarrhythmia

 acute myocardium infarction

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

 arterial hypertension

.
Atenolol (tenormin)
cardioselelctive -adrenoblocker with long
duration of action
Indications for
administration
 ischemic heart disease
 arterial hypertension
 cardiac arrhythmias
 acute myocardium infarction
 Acebutolol (sectral)
1-adrenoblocker with inner
sympathomimetic activity

Indications
 disorders of cardiac rhythm
(tachyarrhythmia)
 hypertension

 ischemic heart disease

 Labetolol
-, -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
 CARVEDILOL, NEBIVOLOL

increase the production of NO in

blood vessels
are used for AH, chronic cardiac
insufficiency (congestive heat
failure)
Nebivolol –
Nebilet
 StimulatesNO
synthesis in
endothelium
Sympatholytics
 Reserpine

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