Zelnorm (Tegaserod) For IBS-C

Zelnorm (Tegaserod) is a drug used to treat IBS-C. It works by increasing the movement of stools in the intestine. This medication was discontinued in 2007 due to cardiovascular side effects.

However it can still be used in certain patients with persistent constipation.

Serotonin’s activity in the intestines is boosted by the drug Zelnorm. As a result, feces pass through the bowels more quickly.

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Uses of Zelnorm

Women under the age of 65 with severe, persistent constipation-related irritable bowel syndrome (IBS) are treated with Zelnorm.

Zelnorm works by promoting gastrointestinal motility. This shortens the time feces stays in the gut and eases symptoms like constipation and discomfort in the abdomen. It has not been shown that this medication helps men with IBS.

Mechanism of Action of Zelnorm:

Zelnorm works by attaching to 5-HT4 receptors, which causes peristalsis to increase and the sensory response to decrease.

As a 5-HT4 agonist, it treats IBS constipation, bloating, and abdominal discomfort throughout the GI tract.

stimulates intestinal secretion and the peristaltic reflex
suppresses visceral sensitivity
improves basal motor function
restores the GI tract’s reduced motility to normal

Pharmacodynamics

Zelnorm is typically reported to be an agonist at serotonin type-4 (5-HT(4)) receptors and an antagonist at 5-HT(2B) receptors, while it is also likely to have very little affinity for 5-HT(1) receptors and very none for 5-HT(3) or dopamine receptors.

It was also discovered that Zelnorm and its main metabolite, the M29 metabolite, might encourage platelet aggregation in a lab setting.

Zelnorm considerably boosted platelet aggregation in one in-vitro research at concentrations up to 10 times the maximum plasma concentration (Cmax) at the indicated dose, increasing it by up to 74% (range 11% to 74%) compared to a control vehicle (with potentiation by different agonists). [ref]

Absorption

The absolute bioavailability of Zelnorm in subjects who are fasting is 10%. One hour after peaking, the Zelnorm plasma concentration (Tmax) averages its peak (range 0.7 to 2 hours). [ref]

However, when Zelnorm was given to people 30 minutes before a meal with a high-fat and high-calorie content (roughly 150 calories from protein, 250 calories from carbohydrates, and 250 calories from fat), the serum blood concentration of the drug was decreased by 40% to 65%.

Route of Elimination

After being taken orally, Zelnorm is partially removed intact in the feces, with the remaining one-third being eliminated in the urine as metabolites.

Half-Life

Zelnorm’s documented mean terminal elimination half-life after oral treatment is between 4.6 and 8.1 hours.

Zelnorm Dosage Information

Follow your doctor’s instructions for using Zelnorm strictly. Never take it in excess or for longer than is advised. Observe the following instructions:

Take this medicine with a full glass of water. On an empty stomach, or at least 30 minutes before a meal.
The usual dosage for Zelnorm is twice daily.
It can take up to 2 weeks for the symptoms to disappear.
Continue taking the medication as prescribed for the best effects. If your symptoms do not disappear after treatment for 4 to 6 weeks, consult your doctor.
The dosage for adult women under the age of 65 is 6 mg given orally twice daily at least 30 minutes before meals.
Stop using Zelnorm if you do not experience satisfactory symptom control after 4 to 6 weeks of treatment

What occurs if I don’t take a dose?

If you forget to take your prescription or miss a dosage, wait until it’s time for your next dose and skip the missed one. Do not take additional medicine to make up for a missed dosage.

If I take too much, what happens?

If you believe you may have taken too much of this medication, get emergency medical attention.

Vomiting, nausea, diarrhea, and stomach discomfort are all possible overdose symptoms.

While using Zelnorm, abide by your doctor’s recommendations regarding any dietary or exercise limitations

Side Effects of Zelnorm:

There are advantages and disadvantages to every drug. You could have some unpleasant side effects even if the drug is performing as intended.

If you encounter any of the following, speak with your physician.

Stroke symptoms include sudden numbness, weakness, confusion, vision loss, and difficulty speaking, walking, or talking.
Thoughts and actions that are suicidal
Extreme diarrhea

New or worsening stomach pain, rectal bleeding, and bloody diarrhea are symptoms of intestinal enlargement and damage (ischemic colitis).

As your body adjusts to the drug, the following adverse effects could improve over time. If these symptoms persist or if they get worse over time, call your doctor right away.

Typical adverse consequences

Vomiting
Migraine
Constipation
Gastritis
Unsteadiness

Added negative consequences

Tendon enlargement
Blood in the urine
Weakness
Low level of red blood cells
More appetite
Joint issue

Rare Side Effects

Nausea
Discomfort or pain in the neck, back, jaw, or arms
Sweating
Dual perception
Headache
Chest discomfort
Confusion
Having trouble speaking
Inability to move the facial muscles, arms, or legs
Being unable to talk
Attempts or ideas to end one’s life

Signs of Zelnorm overdose

The following signs appear if the drug overdoses:

Feeling unsteady or weak after standing up from a lying or seated posture
Bloated and full of energy
Chills
Extra gas or air in the intestines or stomach
Headache

Some potential side effects frequently don’t need medical attention. During therapy, as your body adjusts to the medicine, these adverse effects could disappear.

Your doctor may also be able to provide you with advice on how to prevent or decrease some of these adverse effects. Consult a doctor if any of the following adverse effects continue or if you have any concerns.

Patients’ Reviews of Zelnorm:

How real-life users felt when they were prescribed Zelnorm for IBS-C? Here are a few reviews of patients using Zelnorm for IBS-C:

“I have been dealing with IBS-C for a few years, and Zelnorm is the only medication that has ever helped. Although I have not tried every option, the medications I have tried (such as Trulance, Linzess, and Ibsrela) have always caused extreme bloating”

“I have been trying different medications since Zelnorm got taken off the market again, but nothing seems to work for me. Have any of you found an effective medication for IBS-C?”

“I started taking Zelnorm and finally had bowel movements, even though it was initially diarrhea. However, as my body got used to it, it stopped working. I added Motegrity to my medication regimen last night. Has anyone else experienced this?

“Earlier, I posted about the expensive cost of Zelnorm, which my insurance doesn’t cover, and the lack of assistance in my area. My GI doctor switched me to a higher dose of Linzess, possibly in the 200s, but it’s not as effective as Zelnorm. Despite experiencing morning diarrhea, I feel completely constipated for the rest of the day, like I’m using the world’s most unsexy butt plug. I know there are ways to optimize Linzess, but I couldn’t locate the previous post. Can anyone share their tips for improving the effectiveness of Linzess?”

“I had to switch from Zelnorm to Motegrity when it stopped working for me. While Motegrity worked for a while, it eventually became ineffective too. Currently, I am taking IBSrela, which has proven to be the most effective option for my IBS-C symptoms.”

“I have been taking a combination of Rifaximin, neomycin, and Zelnorm for hydrogen-dominant SIBO, and have been experiencing chest pressure for over three months. The pressure seems to be getting worse, especially after eating big meals, while on a two-week course of these medications. It is located down my sternum and specifically at ribs 2 and 3. The pressure increases when I sit or lie down.

Six months ago, I started having stomach pains which have now migrated to upper stomach heaviness and pressure in the sternum. Can anyone suggest any remedies to relieve this pressure?”

Conclusion:

Zelnorm (Tegaserod) is a medication used to treat IBS-C in women. It works effectively to treat the symptoms such as abdominal pain. However, it should be used only when directed by a healthcare professional.