Names and pronunciation
(tel-oh′tri-stat) Xermelo
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Drug reference
(tel-oh′tri-stat) Xermelo
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Func. class.: Antidiarrheal
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Chem. class.: Tryptophan hydroxylase inhibitor
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Do not confuse: Xermelo/Xarelto
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ACTION: Reduces serotonin produc tion; this decreases stools in carcinoid syndrome
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USES: Carcinoid syndrome diarrhea; used with somatostatin analogue (SSA) when SSA alone does not control symptoms
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CONTRAINDICATIONS: Hypersensitivity Precautions: Abdominal pain, breast- feeding, constipation, GI perforation/ obstruction, pregnancy
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SIDE EFFECTS CNS: Headache, depression, fever CV: Peripheral edema GI: Nausea, constipation, flatulence, anorexia, abdominal pain
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INTERACTIONS Decrease: effect of—CYP3A4 substrates; monitor for ineffective results; dose of CYP3A4 may need to be increased Decrease: effect of—octreotide; give short- acting octreotide 30-60 min after telotristat Increase: telotristat effect—P-glycopro- tein (P-gp) products Drug/Lab Increase: ALT, AST, alk phos
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DOSAGE AND ROUTES • Adult: PO 250 mg tid
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Available forms: Tablet 250 mg
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Administer: • With food • If dose is missed, give at regularly scheduled time, do not double • Store at room temperature
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Assess: • Stools: volume, color, characteristics, frequency; bowel pattern before product; rebound constipation, abdominal pain; discontinue if abdominal pain or consti- pation is severe • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, not studied in pregnancy; breastfeeding not recom- mended, effects unknown
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Evaluate: • Therapeutic response: decreased diar- T rhea without abdominal pain or severe constipation Patient and caregiver information: • To take with food • That if dose is missed, do not dou- ble; take regular dose at next sched- uled time • Pregnancy/breastfeeding: to contact health care provider if pregnancy is sus- pected or planned, or if breastfeeding • To discontinue and notify health care provider if abdominal pain or severe constipation occurs HIGH ALERT
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CLINICAL CONSIDERATIONS
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PHARMACOKINETICS Peak 0.5-2 hr, half-life 0.6 hr, 99% plasma protein binding, excreted in urine (93.2%), affected by CYP3A4, P-glycoprotein (P-gp)
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• Adult: PO 250 mg tid
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