Zelnorm (Tegaserod) is a serotonin (5-HT4) receptor agonist that increases peristaltic activity and intestinal secretion.

It is used to treat constipation and irritable bowel syndrome in female patients under 65.

Rifaximin and SSRIs are other medications recognised for treatment in IBS patients.

Zelnorm dose in Adults

Zelnorm dosage for irritable bowel syndrome coupled with constipation:

• Females younger than 65 years old:
  • 6 mg twice daily given
  • After 4 to 6 weeks of therapy, discontinue usage in individuals who did not respond as expected.

Zelnorm dose in Children

Not recommended for use in children.

Pregnancy Risk Factor: B

• Some animal reproduction studies showed adverse events.

Use Zelnorm (Tegaserod), while breastfeeding

• It is unknown if breast milk contains tegaserod.
• The manufacturer does not recommend breastfeeding due to the risk of serious adverse reactions in breastfeeding infants.

Zelnorm (Tegaserod) dose in kidney disease:

• eGFR less than 30 mL per minute per 1.73 m2:

  • No change in dose is necessary.

• eGFR more than 15 to less than 30 mL per minute per 1.73 m2:

  • In the manufacturer's labelling, no particular dose changes are mentioned.

  • Use responsibly.

• eGFR less than 15 mL per minute per 1.73 m2:

  • Use is not advised.

• End-stage renal disease on hemodialysis:

  • Use is not advised.

Zelnorm  (Tegaserod) dose in liver disease:

• Mild impairment (Child-Pugh class A):

  • No dosage adjustment is required.

• Moderate to severe impairment (Child-Pugh class B or C):

  • Use is also contraindicated.

Common Side Effects of Zelnorm (Tegaserod) Include:

• Central nervous system:

  • Headache

• Gastrointestinal:

  • Abdominal pain

Less Common Side Effects of Zelnorm (Tegaserod) Include:

• Central Nervous System:

  • Dizziness
  • Migraine

• Gastrointestinal:

  • Diarrhea
  • Nausea
  • Flatulence

• Neuromuscular & Skeletal:

  • Back Pain
  • Arthropathy
  • Leg Pain

Contraindication to Zelnorm (Tegaserod) Include:

• Ischemic colitis or other types of intestinal ischemia in the past
• Tegaserod or any component of its composition cause hypersensitivity
• (eGFR 15mL/min/1.73m2) End-stage renal disease or severe renal impairment
• Signs of gallstones
• Oddi may have sphincter dysfunction.
• A hepatic impairment that is moderate or severe (Child Puugh class B orC)
• Bowel blockage in the past
• Internal adhesions
• Angina, stroke, myocardial infarction, or transient ischemic attacks in the past

Warnings and precautions

• Cardiovascular effects

  • Patients with high cardiovascular risk factors such as smoking, hypertension, hyperlipidemia and diabetes have had serious cardiovascular events (eg stroke, myocardial damage [MI], heart attack], cardiovascular death).
  • Patients with a history or stroke, MI, transient ischemic attacks (TIA), and angina are not recommended to use this medication.
  • If MI, stroke, TIA or angina occurs, stoop.

• Diarrhea:

  • Diarrhea can occur
  • There have been serious side effects of diarrhea, including hypotension, hypotension, and syncope. These conditions may need hospitalization.
  • Patients who experience or are likely to experience frequent diarrhea should be avoided.
  • If severe diarrhea, hypotension, or syncope occurs, patients should discontinue use and consult a health care provider.

• Intestinal ischemic events:

  • It has been linked to ischemic colitis, and other forms of intestinal ischemia.
  • If you develop sudden or extreme stomach discomfort, bloody diarrhoea, or rectal bleeding, stop right away.
  • Patients suffering from ischemic colitis shouldn't be restarted on Zelnorm.

• Suicidal ideation/behavior:

  • There have been suicides, suicide attempts, ideation and suicide, and self-injury.
  • Monitor patients closely for signs of depression and suicidal thoughts or behaviours. This is especially important in the initial months of therapy.
  • Stop any therapy as soon as you feel the symptoms.

Tegaserod: Drug Interaction

Monitor:

• ECG and cardiovascular status.
• Symptoms exacerbation (blood in stools, abdominal pain etc)

How to administer Zelnorm (Tegaserod)?

• Administer at least 30 minutes before meals.

Mechanism of action:

• There is a partial 5-HT4 receptor agonist called tegaserod.
• By working at the receptor location, it can induce the peristaltic reflex, intestinal secretion, and mild visceral sensation.

Excretion:

• Via Feces (~66% as unchanged drug); urine (~33% as metabolites)

Protein binding:

• 98% primarily to α -acid glycoprotein

Distribution: V :

• 368 ± 223 L

Bioavailability:

• Fasting: 10%

Time to peak:

• ~1 hour

Metabolism:

• Metabolite (negligible activity)
• GI: Hydrolysis in the stomach
• Hepatic: Oxidation, conjugation, and glucuronidation
• Significant first-pass effect

Half-life elimination: Terminal:

• 4.6 to 8.1 hours

International Brands of Tegaserod:

• Colonaid
• Coloserod
• Gasprid
• Tegibs
• Zelmac
• Zelnorm
• Zerada

Zelnorm Brands in Pakistan: