Tegaserod is an oral, selective serotonin (5HT-4) partial agonist belonging to a chemical class known as the aminoguanidine indoles. Tegaserod is indicated for the treatment of adult women less than 65 years of age with irritable bowel syndrome with constipation (IBS-C). Safety and efficacy have not been established in men. Tegaserod has been shown to be effective in treating abdominal pain, altered bowel habit (decreased stool frequency, hardened stool consistency, straining), and bloating associated with IBS-C. Guidelines recommend tegaserod be used to treat IBS-C symptoms only in women younger than 65 years with 1 or less cardiovascular risk factors who have not adequately responded to secretagogues (e.g., lubiprostone, guanylate cyclase-C agonists). During clinical trials, significantly more tegaserod-treated patients than placebo-treated patients reported abdominal pain/discomfort and bloating improvements in the first 4 weeks of treatment. Frequency of bowel movements also increased from a median number of 3.8 per week at baseline to 6.3 per week at month one. A modest therapeutic gain of 12% to 15% vs. placebo has been noted for global IBS-C symptoms; efficacy continues with long-term treatment (i.e., 12-months). There have been reports of cardiovascular ischemic events, suicidal ideation, and bowel ischemia with tegaserod use. Discontinue in women who do not achieve adequate symptom control after 4 to 6 weeks of treatment.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Oral Administration
-Administer tegaserod at least 30 minutes before meals.
-Do not administer on an 'as needed' basis.
Gastrointestinal adverse events are the most common side effects of tegaserod. Diarrhea is one of the most common adverse reactions associated with tegaserod and may aggravate certain GI disease. Serious consequences of diarrhea, including hypovolemia, hypotension, electrolyte disorders, and syncope have been reported with tegaserod treatment, in some instances requiring hospitalization for rehydration. Diarrhea was reported in 8% of female patients receiving tegaserod for irritable bowel syndrome with constipation (IBS-C) compared to 3% of subjects receiving placebo. The majority (84%) of the tegaserod patients reporting diarrhea had a single episode. In most cases, diarrhea occurred within the first week of treatment. Typically, diarrhea resolved with continued therapy. Diarrhea resulted in discontinuation in 1.6% of tegaserod-treated patients compared to 0% in placebo. Tegaserod should be discontinued immediately in any patient who develops diarrhea, hypotension or syncope. In addition to diarrhea, the following adverse effects were reported in more than 2% of female patients receiving tegaserod for IBS-C: abdominal pain (11% vs. 10% placebo), dyspepsia (4% vs. 3% placebo), flatulence (6% vs. 5% placebo), and nausea (8% vs. 7% placebo). Increased appetite or appetite stimulation was reported in 2% or less of female patients receiving tegaserod for IBS-C. Some medications, such as lactulose, magnesium salts, misoprostol, stool softeners, some antibiotics, polyethylene glycol, cholinergic agents and stimulant laxatives may aggravate the diarrhea induced by tegaserod. Bulk-producing laxatives, such as psyllium and fiber have been used safely in combination with tegaserod.
In post-marketing reports, ischemic colitis, mesenteric or bowel ischemia, bowel necrosis, gangrenous bowel, GI bleeding (rectal bleeding), and syncope have been noted although the numbers are too small to assign causality. Sphincter of Oddi spasm, bile duct stones (cholelithiasis), cholecystitis with elevated hepatic enzymes (elevated ALT, AST, and bilirubin), and hepatitis have also been reported spontaneously. Hypokalemia secondary to diarrhea has been reported. Because these cases are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. An increase in cholecystectomies was observed in trials with tegaserod (5/2965; 0.17%) vs. placebo (1/1740; 0.06%), which lead to a higher number of abdominal surgeries in general for tegaserod (9/2965; 0.3%) vs. placebo (3/1740; 0.2%). A causal relationship between increased numbers of abdominal surgeries and tegaserod has not been established.
In clinical trials, 14% to 15% of patients receiving tegaserod reported headache vs. 10% to 12% of the placebo group. Mild to moderate headache has been reported to occur from 0.5 to 11 hours after administration of tegaserod. In some subjects the headaches persisted for up to 40 hours. The incidence of headache was dose-dependent, but the intensity did not increase with the dose. It has not been reported if headache is a transient or recurrent side effect of tegaserod. A similar incidence of headache was reported in a large extension trial, studying the long-term safety and tolerability of tegaserod in chronic constipation. Few patients reported severe headache and no incidence of headache led to drug discontinuation. Dizziness (4% vs. 3%) and migraine (2% vs. 1%) are other CNS-related adverse events reported with tegaserod use. Vertigo and asthenia were reported in 2% or less of female patients receiving tegaserod for irritable bowel syndrome with constipation (IBS-C).
Stroke, myocardial infarction (MI), and cardiovascular death (major adverse cardiovascular events [MACE]) have been reported in adults taking tegaserod who had an increased risk of developing an adverse cardiovascular event based on their medical history. A retrospective analysis of 29 placebo-controlled trials of irritable bowel syndrome with constipation (IBS-C) and other gastrointestinal motility disorders of at least 4 weeks duration was conducted. An external adjudication of the reported cardiovascular ischemic (CVI) events identified an imbalance in patients taking tegaserod (13 events, 0.1%) compared to placebo (1 event, 0.01%). One death was recorded among 4 patients experiencing a heart attack, 6 patients experienced serious chest pain (unspecified), and 3 patients suffered a stroke. A second external adjudication was conducted with additional patient-level information, and used a comprehensive pre-specified methodology regarding both case selection and assessment. This adjudication confirmed 7 CVI events (0.06%) on tegaserod compared to 1 event (0.01%) on placebo. An imbalance in MACE events (defined as cardiovascular death, non-fatal MI, non-fatal stroke) was observed in patients taking tegaserod compared to placebo, as reported in both external adjudications. All events occurred in male and female patients with a history of cardiovascular ischemic disease and/or more than 1 cardiovascular risk factor. The rate of MACE events confirmed in 2 external adjudications of the clinical trial database for tegaserod-treated patients ranged from 0.03% to 0.06% in the overall population and 0.01% to 0.03% in the female population less than 65 years of age without a history of cardiovascular ischemic disease compared to zero in the placebo-treated group. Increased blood creatine phosphokinase was reported in 2% or less of female patients receiving tegaserod for IBS-C.
Orthostatic hypotension has been reported to occur infrequently in patients receiving higher doses of tegaserod. One subject, receiving 24 mg of tegaserod, discontinued the study due to orthostatic hypotension. The causal relationship of orthostatic hypotension with tegaserod is uncertain. No other clinically relevant cardiovascular effects, including QT-interval prolongation, other ECG changes, alterations in blood pressure or heart rate have been noted.
Musculoskeletal disorders such as arthropathy and tendonitis occurred in 2% or less of patients receiving tegaserod.
During postmarketing experience with tegaserod, alopecia and hypersensitivity reactions including anaphylactoid reactions have occurred.
Suicide, suicidal attempt and suicidal ideation, and self-injurious behavior have been reported in clinical trials of irritable bowel syndrome with constipation (IBS-C) and other gastrointestinal motility disorders. Two tegaserod-treated patients committed suicide, 1 in a controlled study of IBS-C and 1 during open label treatment for another motility disorder. In 27 placebo-controlled trials, assessing tegaserod at a total daily dose of 4 mg to 50 mg (up to 4 times the recommended daily dose), or placebo for the treatment of IBS-C or other gastrointestinal motility disorders, the frequency of suicidal ideation/behavior with tegaserod treatment (8 events/10,003, or 0.08%) was higher than placebo (1 event/5,425, or 0.02%). Events on tegaserod included 1 completed suicide, 2 suicide attempts, 4 cases of self-injurious behavior, and 1 case of suicidal ideation. There was 1 suicide attempt on placebo. Of the 8 tegaserod-treated patients who experienced an event, all were less than 65 years of age, 7 were female and 3 had IBS-C. The patient who committed suicide was a female, less than 65 years of age with IBS-C, taking tegaserod 2 mg twice daily. Monitor all tegaserod-treated patients for clinical worsening of depression and emergence of suicidal thoughts and behaviors, especially during the initial few months of treatment. Counsel family members and caregivers of patients to monitor for changes in behavior and to alert the healthcare provider. Instruct patients to immediately discontinue tegaserod and contact their healthcare provider if their depression is persistently worse or they are experiencing emergent suicidal thoughts or behaviors.
Anemia was reported in 2% or less of female patients receiving tegaserod for irritable bowel syndrome with constipation (IBS-C).
Tegaserod is contraindicated in any patient with a known hypersensitivity to the drug or any of its excipients.
Tegaserod is contraindicated in patients with a history of myocardial infarction (MI), stroke, transient ischemic attack (TIA), or angina. Stroke, MI, and cardiovascular death (major adverse cardiovascular events [MACE]) have been reported in adults taking tegaserod who had an increased risk of developing an adverse cardiovascular event based on their medical history. A retrospective analysis of 29 placebo-controlled trials of irritable bowel syndrome with constipation (IBS-C) and other gastrointestinal motility disorders of at least 4 weeks duration was conducted. The rate of MACE events confirmed in 2 external adjudications of the clinical trial database for tegaserod-treated patients ranged from 0.03% to 0.06% in the overall population and 0.01% to 0.03% in the female population less than 65 years of age without a history of cardiovascular ischemic disease compared to zero in the placebo-treated group. Assess female patients less than 65 years of age for a history of cardiac disease and cardiovascular risk factors prior to treatment with tegaserod. Consider the potential risks of treatment with expectations in improvements in symptoms of IBS-C. Discontinue tegaserod in patients who experience an MI, stroke, TIA, or angina. Evaluate the risks and benefits of continued use of tegaserod in patients who develop clinical or other evidence of cardiovascular ischemic heart disease (e.g., coronary artery disease) and/or experience changes in health status that could increase cardiovascular risk (e.g., tobacco smoking, hypertension, hyperlipidemia, diabetes mellitus, obesity) during treatment with tegaserod.
Tegaserod should be used with caution in patients with a history of suicidal ideation and depression. Suicide, suicidal attempt and suicidal ideation, and self-injurious behavior have been reported in clinical trials of irritable bowel syndrome with constipation (IBS-C) and other gastrointestinal motility disorders. The frequency of suicidal ideation or attempts with tegaserod treatment (8 patients out of 10,003) was higher than placebo (1 patient out of 5,425). Suicidal ideation/behavior in clinical trials was proportionately more frequent among patients receiving antidepressant medication. Monitor all tegaserod-treated patients for clinical worsening of depression and emergence of suicidal thoughts and behaviors, especially during the initial few months of treatment. Counsel family members and caregivers of patients to monitor for changes in behavior and to alert the healthcare provider. Instruct patients to immediately discontinue tegaserod and contact their healthcare provider if their depression is persistently worse or they are experiencing emergent suicidal thoughts or behaviors.
Tegaserod is contraindicated in patients with moderate or severe hepatic impairment (Child-Pugh B or C) or hepatic disease, severe renal impairment (eGFR less than 15 mL/minute/1.73m2), or end-stage renal disease.
Tegaserod is contraindicated in patients with a history of GI obstruction, symptomatic gallbladder disease, suspected sphincter of Oddi dysfunction, abdominal adhesions, ischemic colitis or other forms of intestinal ischemia. Avoid use of tegaserod in any patient who is currently experiencing or frequently experiences diarrhea. Diarrhea, which is a common adverse effect of tegaserod, may aggravate certain GI disease. Serious consequences of diarrhea, including hypovolemia, hypotension and syncope have been reported with tegaserod treatment, in some instances requiring hospitalization for rehydration. In clinical trials, the majority (84%) of the tegaserod patients reporting diarrhea had a single episode. In most cases, diarrhea occurred within the first week of treatment. Typically, diarrhea resolved with continued therapy. Diarrhea resulted in discontinuation in 1.6% of tegaserod-treated patients compared to 0% in placebo. Tegaserod should be discontinued immediately in any patient who develops diarrhea, hypotension or syncope. Additionally, although diarrhea appears to be a transient adverse effect of tegaserod, extended diarrhea may put a patient at risk for dehydration and electrolyte imbalance. Ischemic colitis and other forms of intestinal ischemia have also been reported during postmarketing experience in patients receiving tegaserod. In some cases, hospitalization was required. Discontinue tegaserod in patients who develop symptoms of ischemic colitis, such as rectal or GI bleeding, bloody diarrhea, or new or worsening abdominal pain. Evaluate patients experiencing these symptoms promptly and perform appropriate diagnostic testing. Do not reinitiate tegaserod in patients who develop findings consistent with ischemic colitis or other forms of intestinal ischemia.
Tegaserod is not indicated in geriatric patients 65 years of age and older.
Available data from case reports with tegaserod use during pregnancy have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies, decreased survival of rat pups was observed with maternal dietary administration of tegaserod at 71 times the recommended dose during organogenesis and through lactation. Decreased body weight and delays in developmental landmarks in rat pups were observed with maternal dietary administration of 45 times the recommended dose.
There are no data regarding the presence of tegaserod in human milk, the effects on the breastfed infant, or the effects on milk production. Because of the potential for serious reactions in the breastfed infant, including tumorigenicity, advise a lactating woman that breast-feeding is not recommended during treatment with tegaserod. Tegaserod and its metabolites are present in rat milk; following oral administration, tegaserod and its metabolites are excreted in the milk of lactating rats with a milk to plasma concentration ratio of 33:1 at 8 hours.
The safety and effectiveness of tegaserod in neonates, infants, children, and adolescents have not been established.
For the treatment irritable bowel syndrome (IBS) with constipation in females:
NOTE: Safe and effective use in men has not been established.
Oral dosage:
Adults Females younger than 65 years: 6 mg PO twice daily. Discontinue if adequate control of symptoms is not achieved after 4 to 6 weeks of treatment.
Maximum Dosage Limits:
-Adults
12 mg/day PO.
-Elderly
12 mg/day PO.
-Adolescents
Use not established.
-Children
Use not established.
Patients with Hepatic Impairment Dosing
Tegaserod is contraindicated in patients with moderate or severe hepatic impairment (Child-Pugh B or C). No dosage adjustment is required in patients with mild hepatic impairment.
Patients with Renal Impairment Dosing
eGFR 30 mL/min/1.73 m2 and greater: No dosage adjustment is recommended.
eGFR less than 15 mL/min/1.73 m2 or end stage renal disease: Use is contraindicated.
Intermittent hemodialysis
Pharmacokinetic parameters were not altered in hemodialysis patients. However, tegaserod is contraindicated in patients with severe renal impairment.
Continuous hemodialysis
Pharmacokinetic parameters were not altered in hemodialysis patients. However, tegaserod is contraindicated in patients with severe renal impairment.
*non-FDA-approved indication
Acarbose: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Aliskiren; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Alogliptin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who tegaserod concomitantly.
Alogliptin; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who tegaserod concomitantly.
Alogliptin; Pioglitazone: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic drugs, such as pioglitazone. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who tegaserod concomitantly.
Alpha-glucosidase Inhibitors: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Amiloride; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Amlodipine; Valsartan; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Anticholinergics: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Atenolol; Chlorthalidone: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Atropine: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Atropine; Difenoxin: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Azilsartan; Chlorthalidone: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Belladonna; Opium: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Benazepril; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Benztropine: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Bisoprolol; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Budesonide; Glycopyrrolate; Formoterol: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Canagliflozin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Canagliflozin; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Candesartan; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Captopril; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Chlordiazepoxide; Clidinium: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Chlorothiazide: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Chlorthalidone: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Dapagliflozin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Dapagliflozin; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Dapagliflozin; Saxagliptin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Dicyclomine: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Digoxin: (Minor) When digoxin is combined with tegaserod, a reduction in digoxin peak plasma concentration occurs. Digoxin dose adjustments are unlikely to be required when combined with tegaserod. Until further clinical use is gained with tegaserod, use caution and consider monitoring digoxin levels more frequently if combined with tegaserod.
Diphenoxylate; Atropine: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Dulaglutide: (Moderate) Tegaserod can enhance gastric emptying in patients with diabetes. Typically, blood glucose could be affected, which, in turn, may affect the clinical response to antidiabetic agents. However, incretin mimetics have been shown to slow gastric emptying. The clinical effects of these competing mechanisms is not known. The dosing of antidiabetic agents may require adjustment and blood glucose should be closely monitored when coadministered with tegaserod.
Empagliflozin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Empagliflozin; Linagliptin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents, such as linagliptin. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Empagliflozin; Linagliptin; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents, such as linagliptin. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Empagliflozin; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Enalapril; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Eprosartan; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Ertugliflozin; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Ertugliflozin; Sitagliptin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Exenatide: (Moderate) Tegaserod can enhance gastric emptying in patients with diabetes. Typically, blood glucose could be affected, which, in turn, may affect the clinical response to antidiabetic agents. However, incretin mimetics have been shown to slow gastric emptying. The clinical effects of these competing mechanisms is not known. The dosing of antidiabetic agents may require adjustment and blood glucose should be closely monitored when coadministered with tegaserod.
Flavoxate: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Fosinopril; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Glimepiride: (Moderate) Tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Glipizide: (Moderate) Tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Glipizide; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Glyburide: (Moderate) Tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Glyburide; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Glycopyrrolate: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Glycopyrrolate; Formoterol: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Homatropine; Hydrocodone: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Hydrochlorothiazide, HCTZ; Moexipril: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Hyoscyamine: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Incretin Mimetics: (Moderate) Tegaserod can enhance gastric emptying in patients with diabetes. Typically, blood glucose could be affected, which, in turn, may affect the clinical response to antidiabetic agents. However, incretin mimetics have been shown to slow gastric emptying. The clinical effects of these competing mechanisms is not known. The dosing of antidiabetic agents may require adjustment and blood glucose should be closely monitored when coadministered with tegaserod.
Indacaterol; Glycopyrrolate: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Insulin Aspart: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Insulin Aspart; Insulin Aspart Protamine: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Insulin Degludec: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Insulin Degludec; Liraglutide: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. (Moderate) Tegaserod can enhance gastric emptying in patients with diabetes. Typically, blood glucose could be affected, which, in turn, may affect the clinical response to antidiabetic agents. However, incretin mimetics have been shown to slow gastric emptying. The clinical effects of these competing mechanisms is not known. The dosing of antidiabetic agents may require adjustment and blood glucose should be closely monitored when coadministered with tegaserod.
Insulin Detemir: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Insulin Glargine: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Insulin Glargine; Lixisenatide: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. (Moderate) Tegaserod can enhance gastric emptying in patients with diabetes. Typically, blood glucose could be affected, which, in turn, may affect the clinical response to antidiabetic agents. However, incretin mimetics have been shown to slow gastric emptying. The clinical effects of these competing mechanisms is not known. The dosing of antidiabetic agents may require adjustment and blood glucose should be closely monitored when coadministered with tegaserod.
Insulin Glulisine: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Insulin Lispro: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Insulin Lispro; Insulin Lispro Protamine: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Insulin, Inhaled: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Insulins: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Irbesartan; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Isophane Insulin (NPH): (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Linagliptin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents, such as linagliptin. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Linagliptin; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents, such as linagliptin. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Liraglutide: (Moderate) Tegaserod can enhance gastric emptying in patients with diabetes. Typically, blood glucose could be affected, which, in turn, may affect the clinical response to antidiabetic agents. However, incretin mimetics have been shown to slow gastric emptying. The clinical effects of these competing mechanisms is not known. The dosing of antidiabetic agents may require adjustment and blood glucose should be closely monitored when coadministered with tegaserod.
Lisinopril; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Lixisenatide: (Moderate) Tegaserod can enhance gastric emptying in patients with diabetes. Typically, blood glucose could be affected, which, in turn, may affect the clinical response to antidiabetic agents. However, incretin mimetics have been shown to slow gastric emptying. The clinical effects of these competing mechanisms is not known. The dosing of antidiabetic agents may require adjustment and blood glucose should be closely monitored when coadministered with tegaserod.
Losartan; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Meglitinides: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Metformin; Repaglinide: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Metformin; Saxagliptin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Metformin; Sitagliptin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Methscopolamine: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Metolazone: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Metoprolol; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Miglitol: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Nateglinide: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Neostigmine; Glycopyrrolate: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Olmesartan; Amlodipine; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Olmesartan; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Oxybutynin: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Phenobarbital; Hyoscyamine; Atropine; Scopolamine: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Pioglitazone: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic drugs, such as pioglitazone.
Pioglitazone; Glimepiride: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic drugs, such as pioglitazone. (Moderate) Tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Pioglitazone; Metformin: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly. (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic drugs, such as pioglitazone.
Propantheline: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Quinapril; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Regular Insulin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Regular Insulin; Isophane Insulin (NPH): (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents.
Repaglinide: (Moderate) Because tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Rosiglitazone: (Moderate) Tegaserod can enhance gastric emptying in diabetic patients, and blood glucose can be affected, which may affect the clinical response to antidiabetic drugs. Dosing of the antidiabetic agent may require adjustment in patients who receive GI prokinetic agents concomitantly.
Saxagliptin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Scopolamine: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Semaglutide: (Moderate) Tegaserod can enhance gastric emptying in patients with diabetes. Typically, blood glucose could be affected, which, in turn, may affect the clinical response to antidiabetic agents. However, incretin mimetics have been shown to slow gastric emptying. The clinical effects of these competing mechanisms is not known. The dosing of antidiabetic agents may require adjustment and blood glucose should be closely monitored when coadministered with tegaserod.
Sitagliptin: (Moderate) Because tegaserod can enhance gastric emptying in patients with diabetes, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive tegaserod concomitantly.
Solifenacin: (Major) Solifenacin, as an antimuscarinic, may slow GI motility and thus may potentially antagonize the actions of drugs that enhance gastrointestinal motility, like tegaserod.
Spironolactone; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Sulfonylureas: (Moderate) Tegaserod can enhance gastric emptying in diabetic patients, blood glucose can be affected, which, in turn, may affect the clinical response to antidiabetic agents. The dosing of antidiabetic agents may require adjustment in patients who receive GI prokinetic agents concomitantly.
Telmisartan; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Thiazide diuretics: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Tirzepatide: (Moderate) Tegaserod can enhance gastric emptying in patients with diabetes. Typically, blood glucose could be affected, which, in turn, may affect the clinical response to antidiabetic agents. However, incretin mimetics have been shown to slow gastric emptying. The clinical effects of these competing mechanisms is not known. The dosing of antidiabetic agents may require adjustment and blood glucose should be closely monitored when coadministered with tegaserod.
Tolterodine: (Major) Tolterodine is an antagonist at muscarinic cholinergic receptors; the anticholinergic actions of the drug are most potent on the urinary bladder, with less activity on GI and salivary muscarinic cholinergic receptors. Tolterodine, as an antimuscarinic, may slow GI motility and thus may potentially antagonize the actions of drugs that enhance gastrointestinal motility, like metoclopramide or tegaserod. However, the clinical significance of this potential interaction is uncertain.
Triamterene; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Trihexyphenidyl: (Major) Drugs that exert significant anticholinergic properties such as antimuscarinics may pharmacodynamically oppose the effects of prokinetic agents such as tegaserod. Avoid administering antimuscarinics along with tegaserod under most circumstances. Inhaled respiratory antimuscarinics, such as ipratropium, are unlikely to interact with tegaserod. Ophthalmic anticholinergics may interact if sufficient systemic absorption of the eye medication occurs.
Trospium: (Major) Trospium is an antagonist at muscarinic cholinergic receptors and decreases gastrointestinal motility. Trospium, therefore, may potentially antagonize the actions of drugs that enhance gastrointestinal motility, like tegaserod.
Valsartan; Hydrochlorothiazide, HCTZ: (Minor) Coadminisitration of thiazides and prokinetic agents may result in decreased bioavailability of the thiazide diuretic.
Tegaserod, a selective serotonin (5HT4) partial agonist, stimulates the peristaltic reflex. Intestinal 5HT4 receptors are involved in motor, sensory and secretory functions. Peristalsis occurs due to release of inhibitory and excitatory neurotransmitters via activation of the intrinsic afferent neurons in the GI mucosa. Additionally, increases in colonic sodium and water secretion produce a softer stool. In animal models, tegaserod has also been shown to reduce extrinsic afferent firing (i.e., through the spinal cord) and thus visceral pain sensation. These actions result in the relief of pain, discomfort and altered stool form associated with constipation-predominant IBS. Tegaserod has negligible affinity for the 5HT3 receptor or dopamine, but possesses 21% intrinsic activity at the 5HT4 receptor. Tegaserod has moderate affinity at the 5HT1 receptor. As a partial agonist, tegaserod has a lower likelihood of inducing receptor desensitization compared to full agonists, theoretically lowering the likelihood for tachyphylaxis or tolerance.
Tegaserod is approximately 98% protein-bound, primarily to alpha1-acid glycoprotein. Multiple-dose studies have confirmed there is no plasma accumulation of tegaserod. However, it exhibits pronounced distribution into the tissues following IV administration, as evidenced by a large volume of distribution. The estimated terminal half-life is 11+/-5 hours. After oral administration, acid hydrolysis occurs in the stomach followed by hepatic oxidation and glucuronidation. The main metabolite, a glucuronide, has negligible affinity at the 5HT4 receptor. Approximately two-thirds of tegaserod is excreted as the parent drug in the feces, and one-third as the main metabolite in the urine.
Affected cytochrome P450 isoenzymes and drug transporters: none
Tegaserod does not inhibit CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2E1, and CYP3A4, and it does not induce CYP3A4 and CYP2B6. Limited induction of CYP1A2 was observed at tegaserod concentrations in excess of 100 times the clinically relevant range. M29, the main metabolite of tegaserod, does not inhibit CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4, and it does not induce CYP1A2, CYP2B6, or CYP3A4. Tegaserod is a substrate for BCRP and P-gp, but not a substrate of OAT1, OAT3, OCT1, OCT2, OATP1B1, OATP1B3, MATE1, MATE2-K or BSEP. Drug transporter data indicated a potential inhibition of MATE1, MATE2-K, and BCRP by tegaserod at high concentrations. However, at the clinical dose of tegaserod, a significant in vivo drug interaction via inhibition of these transporters is unlikely. M29 is a substrate of BCRP, P-gp, OAT3 and BSEP transporters, but not a substrate of OAT1, OCT1, OCT2, OATP1B1, OATP1B3, MATE1, and MATE2-K. M29 does not inhibit the following transporters: OAT1, OAT3, OCT1, OCT2, OATP1B1, OATP1B3, MATE1, MATE2-K, BCRP, P-gp, and BSEP.
-Route-Specific Pharmacokinetics
Oral Route
Tegaserod is administered orally. Following rapid absorption, tegaserod reaches peak plasma concentrations in 1 hour. The absolute bioavailability is roughly 10%, but coadministration with food decreases bioavailability by 40% to 65% and Cmax by 20% to 40%. Similar reductions in plasma concentrations occur when tegaserod is administered within 30 minutes prior to a meal, or 2.5 hours after a meal. The reduced bioavailability appears to be due to a decrease in the extent, but not the rate of absorption. The Tmax of tegaserod is prolonged from approximately 1 hour to 2 hours when taken following a meal, but decreased to 0.7 hours when taken 30 minutes prior to a meal. The manufacturer recommends administration at least 30 minutes before a meal.
-Special Populations
Hepatic Impairment
In subjects with mild hepatic impairment, mean tegaserod AUC was 31% higher and Cmax 16% higher compared to normal subjects. In a single subject with moderate hepatic impairment, the Cmax and AUC were 140% and 200% of that observed in healthy controls. Tegaserod has not been studied in patients with moderate or severe hepatic impairment (Child-Pugh B or C) and use is contraindicated in these patients.
Renal Impairment
No change in the pharmacokinetics of tegaserod was observed in subjects with end stage renal disease (creatinine clearance normalized by body surface area (CrCL) less than 15 mL/minute/1.73 m2) requiring hemodialysis. Although renal impairment does not affect the pharmacokinetics of tegaserod, the pharmacokinetics of its main metabolite (M29) are altered, the Cmax of M29 doubling and the AUC increasing 10-fold in patients with severe renal impairment (CrCL less than 15 mL/minute/1.73 m2) compared to healthy subjects with normal renal function (CrCL greater than 80 mL/minute/1.73 m2). Tegaserod is contraindicated in patients with severe renal impairment (eGFR less than 15 mL/minute/1.73 m2) or end-stage renal disease.
Geriatric
Tegaserod is not indicated for patients 65 years of age and older.