drotaverine

Action and Spectrum

Actions and Spectrum: 

Actions: 

Smooth muscular spasms are relaxed and relieved by the medicine drotaverine, which has spasmolytic characteristics. The smooth muscles in different areas of the body are the target and are affected by it. The gastrointestinal tract, including the stomach and intestines, has smooth muscles that are relaxed by drotaverine. As a result of diseases like colitis and irritable bowel syndrome (IBS), this action helps to decrease pain and discomfort in the abdomen. 

Spectrum: 

The spectrum of drotaverine is indicated in the treatment of irritable bowel syndrome, renal colic, colitis, dysmenorrhea, endometriosis, and other conditions where smooth muscle relaxation is required. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Dry mouth 

Vertigo 

Nausea 

vomitng 

Black Box Warning

Black Box Warning: 

This medication should not be taken by patients who have a rare genetic condition of galactose intolerance, complete lactase deficiency, or glucose-galactose malabsorption. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Severe renal dysfunction 
• Severe hepatic impairment 
• Cardiac dysfunction 
• Porphyria 

Cautions 

• Renal impairment 
• Hepatic impairment 
• Drug interactions 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the administration of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the excretion of drug in breast milk. 

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

Pharmacology

Pharmacology: 

drotaverine is categorized as a smooth muscle relaxant or spasmolytic. In a variety of circumstances, it is used to reduce smooth muscle spasms and the pain they cause. 

Pharmacodynamics: 

For drotaverine to function, it must first inhibit phosphodiesterase-4 (PDE-4), an enzyme involved in controlling intracellular cyclic adenosine monophosphate (cAMP) levels. drotaperine raises cAMP levels in smooth muscle cells by blocking PDE-4, which causes the smooth muscles to relax. Muscle spasms and related discomfort are relieved because of this relaxation. 

Pharmacokinetics: 

Absorption 

The time to achieve peak effect is 1-3 hours 

Distribution 

Protein-bound is 80-95% 

The volume of distribution of drotaverine is 193-195 L/kg 

Metabolism 

It seems that drotaverine goes through a lot of first-pass metabolism. O-deethylation converts it quickly into mono- and diphenolic compounds and the equivalent derivatives of glucuronic acid in the liver. 

Elimination and Excretion 

The half-life is 7-12 hours 

drotaverine is eliminated through the urine and feces after being thoroughly digested in the liver. 

Adminstartion

Administration: 

The usual method of administering rotaverine is orally, and the precise dosage and frequency of administration may change based on the health of each patient and the advice of the healthcare professional.

You can take drotaverine with or without meals. To lower the possibility of gastrointestinal distress, it is typically advised to take it with meals. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: drotaverine 

Pronounced: Droh-TAV-uh-reen 

Why do we use drotaverine? 

Essentially, drotaverine works by relaxing smooth muscles, which helps ease the discomfort and spasms that accompany them. Treatment decisions are usually based on the patient’s symptoms and the particular ailment being treated. Under the supervision and prescription of a healthcare professional, it should always be utilized.