udenafil (FDA approval pending)

Action and Spectrum

Actions and Spectrum: 

Actions: 

udenafil exerts its pharmacological effects primarily by inhibiting the enzyme phosphodiesterase type 5 (PDE5). PDE5 is responsible for breaking down cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the penis. By inhibiting PDE5, udenafil helps to increase the levels of cGMP, leading to smooth muscle relaxation and increased blood flow to the penis during sexual stimulation.  

Spectrum: 

udenafil is primarily indicated for erectile dysfunction, a condition in which a man has difficulty achieving or maintaining an erection sufficient for satisfactory sexual performance. It is essential to note that udenafil is effective only when sexual stimulation occurs. 

Drug Interaction

Adverse Reaction

None reported 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Severe liver or kidney dysfunction 
• Nitrates 
• Alpha-Blockers 

Cautions: 

• Cardiovascular conditions 
• Eye conditions 
• Priapism 
• Anatomical deformities of the penis 
• Hearing loss 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the use in pregnant women. 

Breastfeeding warnings:  

The presence of the drug in 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. 

<b>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: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

As a phosphodiesterase type 5 (PDE5) inhibitor, udenafil exerts its pharmacological effects by selectively inhibiting the enzyme PDE5. This inhibition leads to increased levels of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the penis. 

Pharmacodynamics: 

udenafil works by inhibiting the enzyme phosphodiesterase type 5 (PDE5). This enzyme is responsible for breaking down cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the penile tissue. cGMP is a signaling molecule that relaxes the smooth muscles and dilates the blood vessels in the penis, allowing increased blood flow and an erection. 

Pharmacokinetics: 

Absorption 

udenafil is administered orally in the form of tablets and is rapidly absorbed after ingestion. It takes to reach maximum concentration in the blood (Tmax), typically around 30 minutes to 2 hours. 

Distribution 

udenafil is extensively distributed throughout the body after absorption. It is highly bound to plasma proteins, primarily albumin. 

Metabolism 

The primary route of metabolism for udenafil is through the liver, where it undergoes extensive hepatic metabolism by the cytochrome P450 (CYP) enzyme system, particularly CYP3A4 and CYP2C9. Metabolism leads to the formation of active metabolites. 

Elimination and Excretion 

udenafil and its metabolites are primarily eliminated from the body through feces (approximately 88%) and urine (approximately 6%). 

Adminstartion

Administration: 

udenafil is typically available as oral tablets and is administered by mouth. 

udenafil can be taken with or without food. However, taking it with a high-fat meal may delay its onset of action. Avoid heavy or fatty meals if you choose to take it with food, as they may reduce the drug’s absorption and effectiveness. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: udenafil 

Why do we use udenafil? 

udenafil primarily treats erectile dysfunction (ED) in adult men. Erectile dysfunction is when a man has difficulty achieving or maintaining an erection sufficient for sexual activity. Various factors, including physical conditions like diabetes, cardiovascular disease, neurological disorders, hormonal imbalances, psychological issues, or side effects of certain medications can cause it.