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Adrenomimetic drugs adrenoceptor agonists. Department of pharmacology Zhu ling ( 朱玲 ) 2010.3. Adrenomimetic drugs adrenoceptor agonists.

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Adrenomimetic drugs adrenoceptor agonists
Adrenomimetic drugs adrenoceptor agonists

Department of pharmacology

Zhu ling (朱玲)


Adrenomimetic drugs adrenoceptor agonists1
Adrenomimetic drugs adrenoceptor agonists

  • A kind of drugs that mimic the actions and the chemistry structure (amine) of epinephrine or norepinephrine.

  • Because the action similar to sympathetic effects that stimulation are mediated by release of norepinephrine

    sympathomimetic drugs

Adrenomimetic drugs adrenoceptor agonists2
Adrenomimetic drugsadrenoceptor agonists

Adrenomimetic drugs adrenoceptor agonists

αreceptor: blood vessels of skin, gut


β1receptor:heart function enhancement


bronchial smooth muscles: relaxation

skeletal muscle vessels: relaxation

coronary artery: relaxation

Adrenomimetic drugs adrenoceptor agonists3
Adrenomimetic drugsadrenoceptor agonists


1 Basic structure :β--phenylethylamine

2 main effects in the cadiovascular systerm

3 elimination from uptake, MAO, COMT

4 main application: shock

Adrenomimetic drugs adrenoceptor agonists4
Adrenomimetic drugsadrenoceptor agonists

  • individuality

    1 structure: different substituted groups

    2 different of receptor selectivity

    3 different effects mostly on the systolic and diastolic blood pressure (pulse pressure)

Receptor agonist
αβreceptor agonist

Adrenaline Ad 肾上腺素

Epinephrine E

  • Rooted in adrenal gland medulla,instability

  • Pharmacokinetics:

    absorption : is poor with oral administration ,

    sc or i.m injection .

    distrbution: the area of noradrenergic nerve domination;

    elimilation: uptake,or inactivation by MAO, COMT

Receptor agonist adrenaline
αβreceptor agonist --adrenaline


a very potentαβreceptor agitated action

1 heart : β1receptor excitement

2 blood vessels: α1 and β2 receptor

skin vessels, mucous membrane vessels, viscus vessels contraction;

brain, pulmonary blood vessels

feeble vasoconstriction;

skeletal muscle vessels ,coronary artery


Receptor agonist adrenaline1
αβreceptor agonist --adrenaline

β2 receptor agitate

blood pressure coronary artery perfusion pressure flux

adenosine increase

  • 3 blood pressure

    systolic blood pressure increase,

    diastolic pressure steadiness or slightly fall

    pulse pressure

Receptor agonist adrenaline2
αβreceptor agonist --adrenaline

4 bronchia smooth muscle relaxation

5 metabolism: activates fat lipolysis, blood glucose↑



1 anaphylactic shock first choose drug

2 bronchial asthma( urgent outbreak)

3 sudden cardiac arrest

4 local application local anesthetics and


Receptor agonist adrenaline3
αβreceptor agonist --adrenaline

Adverse reaction

heart-throb, headache, arrhythmia

(extensions of their receptor effects in the cardiovascular )


hypertension , hyperthyroid etc

Receptor agonist ephedrine
αβreceptor agonist --ephedrine


substitution on benzene ring(Absence of ring-OH groups) and substitution on alpha carbon

preferably lipid-soluble, stabilization,

orally active, increase the distribution, prolong the action(resistant to COMT,MAO)


Agitate, accelerate NA release

1 peripheral effects like Ad but the function is slow, feeble, long duration

2 CNS effects elevation of mood

Adrenomimetic drugs adrenoceptor agonists


Receptor agonist ephedrine1
αβreceptor agonist --ephedrine

application :

  • bronchial asthma

  • congestive snuffle

    (as a nasal decongestant )

  • Prevent some hypotension (as a pressor agent)

    arachnoid below cavity and outside putamen anesthesia, local anesthetics poisoning

  • Some disease induced by allergic reaction

    Adverse reaction:

    like Ad, further insomnia (CNS effects)

Receptor agonist noradrenaline
αreceptor agonist --noradrenaline


chemical quality like Ad,

orally taking easily be destroyed,

maybe ischemia or putrescence with sc or im ,

only can be applied by iv

Receptor agonist noradrenaline1
αreceptor agonist --noradrenaline


mostly agitateαβ1 receptor

1 heart positive klinotropic effect,

positive chronotropic effect

positive inotropic effects

2 blood vessel vasoconstriction

except coronary artery

peripheral resistance

3 blood pressure

both diastolic and systolic blood pressure

Receptor agonist noradrenaline2
αreceptor agonist --noradrenaline

Clinical uses:

① shock and hypotension

② hemorrhage of the upper alimentary tract

oral administration (local application)

Adverse reaction:

marked vasoconstriction , arrhythmia

① local tissues necrosis

② acute kidney failure

Receptor agonist1
αreceptor agonist

  • metaraminal direct and indirect action

    weak, long-duration

    substitute of NA

  • Phenylephrine and methoxamine

    kidney blood vessels contract >NA

    treatmemt of paroxysmal atrial tachycardia and effictive mydriatic agent (Phenylephrine)

Receptor agonist isoproterenol isoprenaline
βreceptor agonist Isoproterenol (Isoprenaline 异丙肾上腺素)

  • Isoproterenol (Isoprenaline)

    1 pharmacokinetics:

    absorption: low bioavailability of oral administration,usually iv, sublingua administration, aerosol inhalation (through capillary vessel , rapid absorption )

    biotransformation: main metabolized by COMT,some by MAO,some by uptake

Receptor agonist isoproterenol isoprenaline1
βreceptor agonist Isoproterenol (Isoprenaline 异丙肾上腺素)

effects:more active βreceptor agonist

① heart exciting

② blood vessels potent vasodilator

③ blood pressure systolic pressure slightly increased, diastolic pressure decreased

  • bronchia smooth muscle: relaxation

  • metabolism glycogenolysis and lipolysis ↑

    increased oxygen consumption

Receptor agonist isoproterenol isoprenaline2
βreceptor agonist Isoproterenol (Isoprenaline 异丙肾上腺素)

Therapeutic application:

① Sudden cardiac arrest: (cause: ventricular automaticity slowness, severity atrioventricular block and SA nodes function failure)

② atrioventricular block

③ bronchial asthma acute outbreak

④ Infected shock

Adverse reaction:

heart-throb, arrhythmia etc

1 receptor agonist
β1 receptor agonist

Dobutamine 多巴酚丁胺

  • effects: relatively β1 selective synthetic catecholamine, positive inotropic effects characteristic:

    in low to moderate doses, it can increase, constriction and cardiac output , but slightly influence on the heart rate, cause relatively little peripheral vasoconstriction and little increase oxygen consumption

1 receptor agonist1
β1 receptor agonist

Therapeutic application:

1 shock well curative effect when companying with weak contract or renal failure

2 congestive heart failure

3 acute renal failure always with diuretic

Adverse reaction:

tachycardia, hypertension, angina, inducing tolerance

Da receptor agonist dopamine
αβDA receptor agonist – Dopamine多巴胺

Dopamine( DA 多巴胺)

  • the immediate metabolic precursor of norepinephrine

  • Exist in peripheral nerve, ganglion and central nerve


    absorption: low bioavailability of oral administration,usually iv

    distribution: difficult pass through blood-brain barrier

Da receptor agonist dopamine1
αβDA receptor agonist – Dopamine多巴胺

effect:agitate αβDA receptor

1 heart β1 R

2 blood vessel and blood pressure

  • low doses activate D1 receptor in several vascular beds vasodilation, reduce peripheral resistance

  • moderate doses β1R systolic pressure↑ diastolic pressure -unchanged

  • higher doses α β1R systolic pressure ↑ diastolic pressure ↑

    3 kidney renal vascular dilation blood flow↑ (raise glomerulus filtration rate) (clinical value)

Da receptor agonist dopamine2
αβDA receptor agonist – Dopamine多巴胺

Therapeutic application:

1 shock especially oliguria

2 congestive heart failure

3 acute renal failure (with diuretic)

Ibopamine (异波帕胺)

heart failure (difficult controlling)