Xanthine derivatives – Amylophyllin

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.

Advantages:

1)      Rapid onset of action.

2)      Suitable for acute asthma(IV).

Disadvantages:

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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