tegaserod

Action and Spectrum

Actions and Spectrum: 

tegaserod works by promoting colonic mass movement and improving gastrointestinal motility. The 5-HT4 receptor, which is important in controlling gastrointestinal motility and secretion, is partially agonized by it. 

tegaserod’s for treating adult women with IBS-C constitute the entirety of its therapeutic range. Men or children are not permitted to utilise it. Also have therapeutic promise for treating other gastrointestinal issues such functional dyspepsia and persistent constipation. 

Drug Interaction

Adverse Reaction

Frequency defined 

1% to 10% 

Dizziness (4%) 

Migraine (≤2%)  

Specimen (≤2%)  

Tendinopathy (≤2%) 

Rectal haemorrhage (≤2%) 

Arthropathy (≤2%)  

Asthenia (≤2%)  

Flatulence (6%) 

Dyspepsia (4%) 

Increased appetite (≤2%) 

Anaemia (≤2%)  

Vertigo (≤2%) 

Diarrhea (8%) 

Nausea (8%) 

Increased creatine phosphokinase in blood 

<1% 

Suicidal tendencies 

Suicidal ideation 

>10% 

Abdominal pain (11%) 

Headache (14%) 

Post marketing report 

Cholecystitis 

Choledocholithiasis 

Cerebrovascular accident 

Mesenteric ischemia 

Hepatitis  

Hypersensitivity reaction 

Increased serum alanine aminotransferase 

Acute myocardial infarction 

Alopecia  

Anaphylaxis 

Spasm of sphincter of Oddi 

Increased serum aspartate transaminase 

Increased serum bilirubin 

Intestinal necrosis  

Ischemic colitis 

Black Box Warning

Black Box Warning: 

tegaserod’s black box warning advises patients with a history of cardiovascular illness to use the medication with caution since it has been linked to an increased risk of heart attack, stroke, and unstable angina. 

tegaserod should not be used in patients with severe renal impairment, hepatic impairment, a history of intestinal obstruction, or in patients taking specific medicines, such as strong CYP3A4 inhibitors or medications that extend the QT interval, according to the black box warning. 

Contraindication / Caution

Contraindication 

• Ischemic heart disease in the past 
• stroke or transient ischemic attack history (TIA) 
• Coronary artery disease 
• Intractable hypertension 
• renal impairment that is severe (creatinine clearance 15 mL/min) 
• Hepatic dysfunction 
• concurrent usage with erythromycin, clarithromycin, fluconazole, and other potent CYP3A4 inhibitors

Caution 

• renal impairment that is mild to moderate (creatinine clearance of 15 to 60 ml/min)  
• moderate liver dysfunction 
• Individuals who are at risk for cardiac problems include those who have diabetes, high cholesterol, have smoked in the past, or are older 
• Individuals who have previously had depression, suicidal thoughts, or suicidal actions 
• breastfeeding and becoming pregnant 
• combined use of medications that might cause cardiac arrhythmias or extend the QT interval 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

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:  

tegaserod is a selective 5-HT4 receptor agonist that primarily influences the enteric nervous system in order to improve gastrointestinal motility and promote colonic mass movement. It is thought to work by boosting acetylcholine release, which in turn stimulates cholinergic neurons in the myenteric plexus. 

The 5-HT4 receptor controls gastrointestinal secretion and motility, and its activation can result in an increase in peristaltic activity, a reduction in transit time, and an improvement in bowel function. Patients with irritable bowel syndrome with constipation have been proven to benefit from tegaserod, which has been demonstrated to enhance bowel movement frequency and lessen constipation severity (IBS-C). 

Pharmacodynamics: 

tegaserod activates the 5-HT4 receptors in the enteric nervous system of the gastrointestinal tract, which predominantly mediates its pharmacodynamic effects. tegaserod activates the 5-HT4 receptors, which are implicated in the control of gastrointestinal motility and secretion. This results in a rise in peristaltic activity, a reduction in transit time, and better bowel function. 

tegaserod is a partial agonist of the 5-HT4 receptor, which indicates that, in contrast to a complete agonist, it has just a limited capacity to activate the receptor. tegaserod can have a therapeutic effect without overly activating the receptor, which can have negative consequences. This is due to its partial agonist action. 

Pharmacokinetics: 

Absorption  

With oral treatment, tegaserod is quickly absorbed, reaching peak plasma concentrations in 1 to 2 hours. tegaserod absorption is not considerably impacted by food. 

Distribution  

tegaserod is widely disseminated throughout the body, as evidenced by its large volume of distribution. Around 96% of it is linked to plasma proteins. 

Metabolism 

tegaserod is extensively first-pass metabolized in the liver, with the cytochrome P450 enzyme CYP2C9 playing a key role. The inactive N-dealkylated metabolite is the main metabolite of tegaserod. Furthermore, the N-dealkylated metabolite’s glucuronide conjugate is produced. 

Elimination and Excretion  

Less than 1% of tegaserod is excreted in the urine, with most of the the drug’s elimination occurring in the feces. tegaserod has an elimination half-life of around 11 hours. 

Adminstartion

Administration:  

Tablets containing tegaserod are normally taken orally. Adults with IBS-C are advised to take a dosage of 6 mg twice day, before meals, for a maximum of 4 to 6 weeks. tegaserod should be taken at least 30 minutes before a meal with a full glass of water. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tegaserod 

Why do we use tegaserod? 

tegaserod is a drug that has been used to treat individuals with IBS-C (irritable bowel syndrome with constipation). 

It functions by turning on 5-HT4 receptors in the gastrointestinal tract’s enteric nerve system, which causes peristaltic activity to rise, transit time to shorten, and bowel function to improve. 

tegaserod has been demonstrated to help IBS-C patients with symptoms including constipation, bloating, and stomach discomfort.