enprofylline

Action and Spectrum

Actions and Spectrum:  

enprofylline is a phosphodiesterase that inhibits breaks down the cAMP and cGMP. cAMP is raised which leads to smooth muscle relaxation increasing bronchodilatory action through improve airflow in COPD. the reaction is more pronounced in an area with bronchoconstriction and increased airway resistance. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Vomiting  

Nausea  

Headache 

Black Box Warning

Black box warning:  

There is no specific black box warning associated with enprofylline. 

Contraindication / Caution

Contraindications/caution:  

• Hypersensitivity reactions 
• severe cardio vascular conditions like unstable angina or arrhythmias seizure disorders  
• peptic ulcer disease 

Pregnancy / Lactation

Pregnancy Warnings: 

Pregnancy category: Not available  

Lactation: excretion into human milk is unknown 

Pregnancy Categories:   

Category A: Satisfactory and well-controlled studies show no evidence of risk to the fetus in the first trimester or in the later trimester.   

Category B: No evidence of risk to fetus found in animal reproduction studies and there are not enough studies on pregnant women.   

Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women.   

Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category clearly outweigh risks over benefits. These category drugs should be prohibited for pregnant women.   

Category N: There is no data available for the drug under this category.    

Pharmacology

Pharmacology:  

As a bronchodilator, enprofylline helps to alleviate COPD symptoms like shortness of breath. 

Pharmacodynamics:   

phosphodiesterase is an inhibitor with a type 4 phosphodiesterase leading to bronchodilation. 

Pharmacokinetics:  

Pharmacokinetics:   

Absorption 

It is administered orally with a bioavailability of 90% and peak plasma concentration of 1 to 2 hours.  

Distribution 

the Vd is about 1 L/kg and plasma protein binding is 55% to 65%s. Metabolism 

It undergoes hepatic metabolism with CYP450 enzymes including CYP1A2 and CYP3A4.  

Excretion and Elimination 

The drug gets excreted through kidneys with half life of 10 – 12 hours.   

Adminstartion

Administration 

oral administration 

enprofylline is administered orally at same time everyday.  

Patient Information Leaflet

Patient information leaflet 

Generic Name: enprofylline 

Why do we use enprofylline?  

Enprofylline is used to treat chronic pulmonary disease (COPD) as it has bronchodilatory and anti inflammatory effect.