ephedrine/guaifenesin

Action and Spectrum

Actions and Spectrum 

ephedrine is a sympathomimetic drug that stimulates the central nervous system, causing bronchodilation, vasoconstriction, and increased heart rate. It is used as a nasal decongestant and to treat asthma and other respiratory conditions. 

guaifenesin is an expectorant that helps to loosen and thin mucus in the lungs, making it easier to cough up. It is commonly used to treat coughs and congestion associated with colds and respiratory infections. 

Drug Interaction

Adverse Reaction

Adverse Reaction  

Frequency Not Defined  

Tachycardia  

Headache  

Emotional disturbance  

Insomnia  

Hypertension  

Seizure  

Nervousness  

Hypersensitivity reaction  

Cough  

Tremor  

Black Box Warning

Black Box Warning  

The black box warning of ephedrine/guaifenesin is related to the risk of serious adverse effects such as heart attack, stroke, and death. 

Contraindication / Caution

Contraindication/Caution 

Hypersensitivity  

Cardiovascular disease  

Diabetes  

Pregnancy / Lactation

 Pregnancy/Lactation  

Pregnancy warnings:     

Pregnancy category: Insufficient data available 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

• Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 
• Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category  

Pharmacology

Pharmacology  

Epinephrine serves as a non-selective agonist for both alpha and beta receptors dedicated for adrenergic effect. By binding to alpha-1 receptors, it causes vasoconstriction and thus raises the blood pressure in the body. The stimulation of beta 1 receptors results in increased force of contraction and heart rate.  

Guaifenesin acts to loosen respiratory secretions through a modification in the physical characteristics of the mucus lining the respiratory tract. It enhances the mobility of the fluids in the respiratory tracts; it will minimize the viscosity of the mucus. It also ensures the efficient removal of mucus from the respiratory tract by promoting productive coughing. 

Pharmacodynamics 

This functions through the triggering of the sympathetic nerves which leads to the relaxation of smooth bronchial muscles thus causing dilation of the bronchi and bronchioles. This leads to increased airflow to the lungs which helps in breathing process hence enhancing respiration. 

Pharmacokinetics 

Absorption  

Epinephrine 

• Peak plasma concentration: 20 to 80 ng/mL (Oral) 

• Onset of action: 15 to 60 minutes (Oral) 

• Duration: 3 to 5 hours (Oral) 

Guaifenesin 

Onset of action: Approximately 30 minutes 

Duration: 4 to 6 hours 

Distribution  

It is widely distributed throughout the body and crosses the blood-brain barrier 

Volume of distribution (Vd): Approximately 220 to 240 L 

Metabolism  

ephedrine is primarily metabolized by the liver through N-demethylation and oxidation pathways.   

guaifenesin is primarily metabolized in the liver through oxidation pathways.  

Elimination and excretion  

ephedrine is eliminated through renal excretion and has a half-life of approximately 3 to 6 hours. guaifenesin is eliminated through renal excretion and has a half-life of approximately 1 hour 

Adminstartion

Administration 

It is taken orally in the form of tablets along with the food 

Patient Information Leaflet

Patient information leaflet 

Generic Name: ephedrine/guaifenesin 

Why do we use ephedrine/guaifenesin? 

It has a significant role in the management of respiratory and cardiovascular diseases separately. Epinephrine is mostly used to induce bronchodilation in the treatment of acute bronchospasm in patients with asthma and anaphylaxis, and in emergency treatment of cardiovascular failure to improve myocardial contractility and increase blood pressure. Guaifenesin acts as an expectorant that thins out the mucus and helps in productive cough in conditions that affect the respiratory system such as a common cold, bronchitis, and pneumonia.