Xanthine derivatives – Amylophyllin



Mechanism of action:

[A]Amynophyllin→Inhibits Phosphodiesterase enzyme→No conversion of cAMP to 5-AMP→↑cAMP→Relaxation of bronchial smooth mucle→Bronchodilation→Relief of asthma.

[B]Amynophyllin→Inhibits presynaptic adenosine receptor of brochus→↑Catecholamine release→Bronchodilation.


1)      Rapid onset of action.

2)      Suitable for acute asthma(IV).


1)      Tachycardia.

2)      Palpitation.

3)      Headache.

4)      Dizziness.

5)      Medullary stimulation.

6)      Nervousness.

7)      Hypokalaemia.

8)      Seziure.

Difference between Salbutamole and Aminophylline:


Traits Salbutamole Aminophylline/Theophylline
1.Group Adrenergic drug Xanthine derivative
2.M/A It stimulates  receptor→activates adenyl cyclase→Convert ATP to cAMP →Relaxation of bronchial smooth muscle→Bronchodilatation. Inhibits enzyme phosphodiesterase (PDE)→Prevents conversion of cAMP to 5’cAMP→↑conc of cAMP→relaxation of bronchial smooth muscle→Bronchodilation.
3.Onset of action Slow Rapid(IV)
4.Duration of action Longer shorter
5.TI High Narrow
6.Usualy form of drug/Route Inhalation IV,oral
7.Caution during administration Not needed Close observation
8.Cardiot oxicity Absent because Salbutamole has no effect. Present
9.CNS toxicity Less More(Insomnia,Tremor,Restlessness)
10.Action onGFR No action ↑GFR.

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