etilefrine

Action and Spectrum

Actions and Spectrum: 

etilefrine’s mechanism of action involves its interaction with adrenergic receptors in the sympathetic nervous system. It acts as a direct-acting sympathomimetic agent by binding to and activating specific adrenergic receptors. 

• Alpha-1 Adrenergic Receptors: etilefrine stimulates alpha-1 adrenergic receptors in smooth muscle cells of blood vessels. Activation of these receptors causes vasoconstriction, leading to an increase in peripheral vascular resistance. This effect raises systemic blood pressure. 
• Beta-1 Adrenergic Receptors: etilefrine also stimulates beta-1 adrenergic receptors located in the heart. Activation of these receptors increases heart rate and contractility, leading to an increase in the cardiac output. This contributes to the rise in blood pressure. 

etilefrine’s primary use is to increase blood pressure in cases of hypotension or shock, where maintaining adequate blood pressure is crucial for the perfusion of vital organs. It achieves this by inducing vasoconstriction and increasing cardiac output: 

• Hypotension: etilefrine is often used when systemic blood pressure is dangerously low, such as during anesthesia, surgery, or acute cardiovascular collapse. It helps raise blood pressure to maintain organ perfusion. 
• Shock: Shock is a critical condition characterized by inadequate tissue perfusion and oxygen delivery. etilefrine may support blood pressure and restore tissue perfusion in shock cases. 
• Hypotension in Regional Anesthesia: etilefrine can counteract the vasodilatory effects of local anaesthetics in regional anesthesia procedures. By causing vasoconstriction, it helps reduce the risk of systemic absorption of the anesthetic agent and subsequent hypotension. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Epigastric pain 

Sweating 

Gangrene 

GI disturbances 

Hyperglycaemia 

Hypokalaemia 

Palpitations 

Arrhythmias 

Dysponea 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: Individuals with known hypersensitivity or allergy to etilefrine or related medications should not use etilefrine. 
• Hypertension: etilefrine is specifically indicated for treating hypotension (low blood pressure). It should not be used in individuals with hypertension (high blood pressure) as it could exacerbate the condition. 
• Coronary Artery Disease: etilefrine can increase heart rate and cardiac contractility. Individuals with a history of angina,coronary artery disease,  or other significant cardiac conditions should avoid etilefrine due to the potential to exacerbate cardiovascular problems. 
• Arrhythmias: etilefrine’s stimulatory effects on the heart can trigger or worsen cardiac arrhythmias (abnormal heart rhythms). Individuals with certain arrhythmias should not use etilefrine. 
• Severe Atherosclerosis: etilefrine’s vasoconstrictive effects can worsen conditions such as severe atherosclerosis, where blood vessels are already narrowed or compromised. 
• Pheochromocytoma: It is a rare tumor of the adrenal glands that can cause episodes of high blood pressure and other symptoms.  
• Hyperthyroidism: etilefrine’s stimulating effects on the cardiovascular system could worsen the symptoms of hyperthyroidism, a condition characterized by an overactive thyroid gland. 
• Closed-Angle Glaucoma: etilefrine’s vasoconstrictive effects can lead to increased intraocular pressure, which is particularly risky for individuals with closed-angle glaucoma. 

Caution: 

• Cardiovascular Conditions: etilefrine’s effects on the cardiovascular system can be significant.  
• Hypertension: Although etilefrine is used to treat hypotension, using it without proper medical supervision can lead to excessive increases in blood pressure, potentially causing hypertensive crises or complications. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

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

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

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 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: 

etilefrine’s pharmacological effects are primarily mediated through its interactions with adrenergic receptors in the sympathetic nervous system: 

• Alpha-1 Adrenergic Receptors: etilefrine stimulates alpha-1 adrenergic receptors located on the smooth muscle cells of blood vessels, particularly in the peripheral vasculature. Activation of these receptors leads to vasoconstriction, causing an increase in peripheral vascular resistance. This effect raises systemic blood pressure. 
• Beta-1 Adrenergic Receptors: etilefrine also stimulates beta-1 adrenergic receptors located in the heart. Activation of these receptors increases heart rate (positive chronotropic effect) and enhances the force of cardiac contraction (positive inotropic effect). As a result, cardiac output increases, contributing to the rise in blood pressure. 

Pharmacokinetics: 

Absorption  

etilefrine is well-absorbed from the gastrointestinal tract after oral administration. 

Distribution 

The drug is distributed widely throughout the body, including the heart, blood vessels, and other organs. 

Metabolism 

etilefrine is metabolized in the liver through processes like glucuronidation and sulfation. 

Elimination and Excretion 

The metabolites of etilefrine are primarily excreted in the urine. 

Adminstartion

Administration: 

Oral administration 

etilefrine tablets are taken by mouth. 

Swallow the tablet with water, with or without food. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: etilefrine 

Why do we use etilefrine? 

etilefrine is primarily used to increase blood pressure, particularly in hypotension (low blood pressure) or shock.  

• Hypotension: etilefrine is used to treat hypotension, where blood pressure falls to levels that can compromise organ perfusion and oxygen delivery. By causing vasoconstriction and increasing cardiac output, etilefrine helps raise blood pressure to a more acceptable range. 
• Shock: Shock is a critical condition characterized by insufficient blood flow to the body’s organs and tissues. etilefrine can be used in shock management to improve blood pressure, enhance tissue perfusion, and stabilize the patient’s condition. 
• Anesthesia Support: Some medications can cause a drop in blood pressure during anesthesia. etilefrine can be administered to counteract the hypotensive effects of anesthetics and maintain adequate perfusion. 
• Hypotension in Regional Anesthesia: etilefrine may also be used where regional anesthesia, such as spinal or epidural anesthesia, causes hypotension. It can help mitigate the vasodilatory effects of anesthetic agents and prevent a dangerous drop in blood pressure.