-
‫أول‬ ‫مستوى‬ ‫دواء‬ ‫علم‬
.
‫دماج‬ ‫أمين‬ ‫محمد‬ ‫د‬
Sympathomimetics
Definition
Drugs that stimulate adrenoceptors and produce
actions similar to sympathetic system
1
-
Catecholamines 2
-
Non catecholamines
A-Natural B-Synthetic
1
-
dopamine
2
-
nor adrenaline
3
-
adrenalin
1
-
isoprenaline
2
-
dobutamine
3
-
isoetharine
.
1-Ephedrine,
2-amphetamine,
3-phenylephrine
4-salbutamol.
Mechanism of action of sympathomimetics
A-Direct
1
-
catecholamines
2
-
phenylephrine
3
-
salbutamol
1
-
Amphetamine
2
-
Tyramine
1
-
Ephedrine
.
B-Indirect C-Mixed (dual)
Catecholamine drugs
1-Adrenaline :
Mechanism of action
Stimulates directly all types of receptors α – β
Administration of adrenaline
S.C , Inhalation , Intra-cardiac , Eye drops
.
Action of adrenaline
Uses of adrenaline(indications)
1. In allergy (anaphylactic shock).
2.With local anesthetics.
3.Epistaxis (locally).
4
.
Hypoglycemia
.
5
.
Glaucoma (dipivifrin is better , a prodrug)
.
6. Cardiac arrest (intracardiac).
7
.
Acute bronchial asthma
.
Contraindications of adrenaline :-
1. Hypertension.
2
.
Arrhythmia
.
3
.
Angina pectoris
.
4.Thyrotoxicosis .
5. With local anesthetics in fingers & toes → gangrene .
6.With digitalis and some general anesthetics as
halothane → arrhythmias.
7. With non selective β-blockers → severe hypertension.
2-Noradrenaline
Mechanism of action
Stimulates directly α-β1 , β3 no β2
Administration of Noradrenaline
I.V. infusion.
Uses of adrenaline(indications)
1-Acute hypotension Infusion( should not be stopped suddenly).
3-Isoprenaline (isoproterenol)
Mechanism of action
Stimulates directly β1 , β2, β3 but no α-effct
Administration of Iso prenaline.
- Sublingual, Inhalation
Uses of Isoprenaline(indications)
1
-
Heart block
.
2
-
Acute bronchial asthma
.
4-Dopamine
Mechanism of action
Stimulates directly D1 , β1 , α receptors.
Administration of dopamine
I.V. infusion. It can't pass to brain.
Small dose → ↑ D1 → V.d. of renal & mesenteric vessels .
Moderate dose →↑ D1 and β1 ↑ H.R., ↑ C.O., ↑ systolic pressure .
Large dose → α1 V.C.,↑T PR., BP.
Uses of Dopamine (indications)
1-Hypovolemic,
cardiogenic &endotoxin
shock with correction of
hypervolemia.
5-Dobutamine
Mechanism of action
Stimulates directly β1 receptors
Administration
I.V. infusion
Uses of Dobutamine (indications)
1
-
acute heart failure (cardiogenic shock)
.
6-Fenoldopa
- D1 receptor agonist which decreases P.R. by dilating arterioles.
- It is given by I.V. drip in emergency hypertension.
Side effects :
1-Headache, 2-Flushing 3-Tachycardia.
1-Non-Catecholamines drugs
A)β – stimulants B)α – stimulants
1
-
Selective β2 agonists
Ex. Salbutamol
3
-
Non Selective β agonists
Ex. Adrenaline
1
-
Selective α1 agonists
Ex. Phenylephrine
2
-
Selective α2 agonists
Ex. Clonidine
2
-
Selective β1 agonists
Ex. Dobutamine
3
-
Non Selective α agonists
EX. Adrenaline , Noradrenaline
1-Selective β2 agonists
A) β – stimulants
3-Non selective β-agonists
1
-
Salbutamol (ventolin)
2
-
terbutalin (Bricanyl
3
-
salmetrol (Serevent)
4
-
formoterol (foradil )
2- selective β1-agonists
Action of selective β2 agonist
1- Produce broncho dilatation,
2- ↓ bronchial secretions & ↓ release of allergic
mediators from mast cells.
3- Relax uterus & produce V.D.
4- ↓ B.P. & produce mild tachycardia (reflex and weak
β1 effect).
5- ↑ glycogenolysis& insulin release .
Clinical Uses
1
-
in bronchial asthma. (acute attack & prophylaxis)
.
Side effects:-
1
-
Tremors
2
-
tachycardia 3
-
nervousness
.
Ritodrine
-:
 β2 agonist, used in
1- premature labour
2-constriction ring of uterus
3- dysmenorrhea.
Non selective β-agonists
1
-
Isoxsuprine 2
-
Oriciprenaline
Used in
1
-
vascular disease
2
-
constriction ring of uterus
.
Used orally or
inhalation in bronchial
asthma
B) α – stimulants
1
-
Selective α1 agonists
Ex. Phenylephrine
2
-
Selective α2 agonists
Ex. Clonidine
2
-
Non Selective α
agonists
EX. Adrenaline , Noradrenaline
1-Phenylephrine oral, local, injection.
2-Midodrine oral (prodrug).
3-Methoxamine injection.
Action of Selective α1 agonist
1
-
Produce V.C. → decongestant
2
-
↑
P.R
,.
3
-
↑
B.P. (systolic & diastolic). → reflex
bradycardia
4-Active mydriasis (+ ve L.R.).
Clinical Uses
1. Treatment of hypotension.
2.Treatment of Paroxysmal Atrial Tachycardia ( PAT).
3.mydriatic& decongestant (phenylephrine).
Nasal decongestant
A)Local B)Systemic (oral)
1. Naphazoline (Privin)
2. Xylometazoline (otrivin, Rhinex , Balkis)
3. Tetrahydrozoline(Nazine)
4. Oxymetazoline (Afrin ,oxymet)
Non –irritant nasal drops and sprays (less rebound congestion).
B)Systemic (oral)
1-Phenylpropanolamine (coldact,Flustop ,Eskornade).
2-Pseudoephedrine.(Actifed ,Histarhine,Doldex-2):oral
common cold preparation
3-Phenylephrine (α1 agonist).(Noflu , Sine –up): oral
common cold preparation
THANK YOU
Dr. Mohammad dammage

Introduction to pharmacy students and medication

  • 1.
    - ‫أول‬ ‫مستوى‬ ‫دواء‬‫علم‬ . ‫دماج‬ ‫أمين‬ ‫محمد‬ ‫د‬
  • 2.
    Sympathomimetics Definition Drugs that stimulateadrenoceptors and produce actions similar to sympathetic system
  • 3.
    1 - Catecholamines 2 - Non catecholamines A-NaturalB-Synthetic 1 - dopamine 2 - nor adrenaline 3 - adrenalin 1 - isoprenaline 2 - dobutamine 3 - isoetharine . 1-Ephedrine, 2-amphetamine, 3-phenylephrine 4-salbutamol.
  • 4.
    Mechanism of actionof sympathomimetics A-Direct 1 - catecholamines 2 - phenylephrine 3 - salbutamol 1 - Amphetamine 2 - Tyramine 1 - Ephedrine . B-Indirect C-Mixed (dual)
  • 5.
    Catecholamine drugs 1-Adrenaline : Mechanismof action Stimulates directly all types of receptors α – β Administration of adrenaline S.C , Inhalation , Intra-cardiac , Eye drops . Action of adrenaline
  • 6.
    Uses of adrenaline(indications) 1.In allergy (anaphylactic shock). 2.With local anesthetics. 3.Epistaxis (locally). 4 . Hypoglycemia . 5 . Glaucoma (dipivifrin is better , a prodrug) . 6. Cardiac arrest (intracardiac). 7 . Acute bronchial asthma .
  • 7.
    Contraindications of adrenaline:- 1. Hypertension. 2 . Arrhythmia . 3 . Angina pectoris . 4.Thyrotoxicosis . 5. With local anesthetics in fingers & toes → gangrene . 6.With digitalis and some general anesthetics as halothane → arrhythmias. 7. With non selective β-blockers → severe hypertension.
  • 8.
    2-Noradrenaline Mechanism of action Stimulatesdirectly α-β1 , β3 no β2 Administration of Noradrenaline I.V. infusion. Uses of adrenaline(indications) 1-Acute hypotension Infusion( should not be stopped suddenly).
  • 9.
    3-Isoprenaline (isoproterenol) Mechanism ofaction Stimulates directly β1 , β2, β3 but no α-effct Administration of Iso prenaline. - Sublingual, Inhalation Uses of Isoprenaline(indications) 1 - Heart block . 2 - Acute bronchial asthma .
  • 10.
    4-Dopamine Mechanism of action Stimulatesdirectly D1 , β1 , α receptors. Administration of dopamine I.V. infusion. It can't pass to brain. Small dose → ↑ D1 → V.d. of renal & mesenteric vessels . Moderate dose →↑ D1 and β1 ↑ H.R., ↑ C.O., ↑ systolic pressure . Large dose → α1 V.C.,↑T PR., BP.
  • 11.
    Uses of Dopamine(indications) 1-Hypovolemic, cardiogenic &endotoxin shock with correction of hypervolemia.
  • 12.
    5-Dobutamine Mechanism of action Stimulatesdirectly β1 receptors Administration I.V. infusion Uses of Dobutamine (indications) 1 - acute heart failure (cardiogenic shock) .
  • 13.
    6-Fenoldopa - D1 receptoragonist which decreases P.R. by dilating arterioles. - It is given by I.V. drip in emergency hypertension. Side effects : 1-Headache, 2-Flushing 3-Tachycardia.
  • 14.
    1-Non-Catecholamines drugs A)β –stimulants B)α – stimulants 1 - Selective β2 agonists Ex. Salbutamol 3 - Non Selective β agonists Ex. Adrenaline 1 - Selective α1 agonists Ex. Phenylephrine 2 - Selective α2 agonists Ex. Clonidine 2 - Selective β1 agonists Ex. Dobutamine 3 - Non Selective α agonists EX. Adrenaline , Noradrenaline
  • 15.
    1-Selective β2 agonists A)β – stimulants 3-Non selective β-agonists 1 - Salbutamol (ventolin) 2 - terbutalin (Bricanyl 3 - salmetrol (Serevent) 4 - formoterol (foradil ) 2- selective β1-agonists
  • 16.
    Action of selectiveβ2 agonist 1- Produce broncho dilatation, 2- ↓ bronchial secretions & ↓ release of allergic mediators from mast cells. 3- Relax uterus & produce V.D. 4- ↓ B.P. & produce mild tachycardia (reflex and weak β1 effect). 5- ↑ glycogenolysis& insulin release .
  • 17.
    Clinical Uses 1 - in bronchialasthma. (acute attack & prophylaxis) . Side effects:- 1 - Tremors 2 - tachycardia 3 - nervousness . Ritodrine -:  β2 agonist, used in 1- premature labour 2-constriction ring of uterus 3- dysmenorrhea.
  • 18.
    Non selective β-agonists 1 - Isoxsuprine2 - Oriciprenaline Used in 1 - vascular disease 2 - constriction ring of uterus . Used orally or inhalation in bronchial asthma
  • 19.
    B) α –stimulants 1 - Selective α1 agonists Ex. Phenylephrine 2 - Selective α2 agonists Ex. Clonidine 2 - Non Selective α agonists EX. Adrenaline , Noradrenaline 1-Phenylephrine oral, local, injection. 2-Midodrine oral (prodrug). 3-Methoxamine injection.
  • 20.
    Action of Selectiveα1 agonist 1 - Produce V.C. → decongestant 2 - ↑ P.R ,. 3 - ↑ B.P. (systolic & diastolic). → reflex bradycardia 4-Active mydriasis (+ ve L.R.). Clinical Uses 1. Treatment of hypotension. 2.Treatment of Paroxysmal Atrial Tachycardia ( PAT). 3.mydriatic& decongestant (phenylephrine).
  • 21.
    Nasal decongestant A)Local B)Systemic(oral) 1. Naphazoline (Privin) 2. Xylometazoline (otrivin, Rhinex , Balkis) 3. Tetrahydrozoline(Nazine) 4. Oxymetazoline (Afrin ,oxymet) Non –irritant nasal drops and sprays (less rebound congestion).
  • 22.
    B)Systemic (oral) 1-Phenylpropanolamine (coldact,Flustop,Eskornade). 2-Pseudoephedrine.(Actifed ,Histarhine,Doldex-2):oral common cold preparation 3-Phenylephrine (α1 agonist).(Noflu , Sine –up): oral common cold preparation
  • 23.