Tegaserod

Severe (eGFR <15 mL/min/1.73 m²) or ESRD: Contraindicated.

Moderate to severe (Child-Pugh class B or C): Contraindicated.

Should be taken on an empty stomach.

History of MI, stroke, TIA, or angina; history of bowel obstruction, symptomatic gallbladder disease, suspected sphincter of Oddi dysfunction, abdominal adhesions, history of ischaemic colitis or other intestinal ischaemia; currently or frequently experiencing diarrhoea. Moderate to severe hepatic impairment (Child-Pugh class B or C); severe renal impairment (eGFR <15 mL/min/1.73 m²) or ESRD.

Patient with CV risk factors (e.g. hypertension, hyperlipidaemia, diabetes, obesity, active smoking). Efficacy and safety in men have not been established. Not indicated for use in women ≥65 years. Pregnancy and lactation.

Significant: Diarrhoea or severe diarrhoea resulting in hypotension, hypovolaemia, syncope, and electrolyte disorders; ischaemic colitis and other forms of intestinal ischaemia.
Blood and lymphatic system disorders: Anaemia.
Ear and labyrinth disorders: Vertigo.
Gastrointestinal disorders: Abdominal pain, nausea, flatulence, dyspepsia, rectal haemorrhage.
General disorders and administration site conditions: Asthenia.
Investigations: Elevated blood creatine phosphokinase.
Metabolism and nutrition disorders: Increased appetite.
Musculoskeletal and connective tissue disorders: Arthropathy, tendonitis.
Nervous system disorders: Headache, dizziness, migraine.
Potentially Fatal: Serious CV events (e.g. MI, stroke); suicide, suicidal attempts or ideation, self-injury.

PO: B

Obtain ECG before treatment initiation. Monitor renal function tests and LFTs; CV events, ischaemic colitis, and clinically-significant diarrhoea when starting treatment and regularly thereafter. Closely assess for signs and symptoms of the emergence of suicidal thoughts and behaviours or worsening depression (particularly during the initial months of therapy).

Symptoms: Headache, diarrhoea, abdominal pain, nausea, vomiting, flatulence, and orthostatic hypotension. Management: Symptomatic and supportive treatment.

Quinidine may increase the plasma concentration of tegaserod.

Decreased bioavailability and plasma concentration when taken with food.

Description:
Mechanism of Action: Tegaserod is a partial serotonin type-4 (5-HT₄) receptor agonist with prokinetic properties. Its effect on the receptor sites results in the stimulation of peristaltic reflex and intestinal secretion, inhibition of visceral sensitivity, enhancement of basal motor activity, and normalisation of impaired motility throughout the gastrointestinal tract.
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract. Decreased bioavailability and plasma concentration when taken with food. Bioavailability: Approx 10% (fasted state). Time to peak plasma concentration: Approx 1 hour.
Distribution: Widely distributed into tissues. Plasma protein-binding: Approx 98%, mainly to α₁-acid glycoprotein.
Metabolism: Metabolised in the stomach via hydrolysis, followed by oxidation, conjugation and glucuronidation in the liver to form M29 metabolite (inactive main metabolite). Undergoes significant first-pass effect.
Excretion: Via faeces (approx 66% as unchanged drug); urine (approx 33% as metabolites). Terminal elimination half-life: 4.6-8.1 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 135409453, Tegaserod. https://pubchem.ncbi.nlm.nih.gov/compound/Tegaserod. Accessed Mar. 25, 2021.

Store at 25°C. Protect from moisture.

Thuốc điều hòa tiêu hóa, chống đầy hơi & kháng viêm

A06AX06 - tegaserod ; Belongs to the class of other laxatives.

Anon. Tegaserod. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 10/03/2021.

Anon. Tegaserod. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/03/2021.

Buckingham R (ed). Tegaserod Maleate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/03/2021.

Zelnorm Tablet (US WorldMeds, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 10/03/2021.

Zelnorm Tablets (US WorldMeds, LLC). U.S. FDA. https://www.fda.gov. Accessed 10/03/2021.