ELETRIPTAN HBR (eletriptan hbr)

There are 7 contraindications. These drug combinations generally should not be dispensed or administered to the same patient. A manufacturer label warning that indicates the contraindication warrants inclusion of a drug combination in this category, regardless of clinical evidence or lack of clinical evidence to support the contraindication.

Drug Interaction	Drug Names
5-HT1D Agonists/Ergot Alkaloids SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: The 5-HT1D agonists and ergot alkaloids can produce vasospastic reactions. CLINICAL EFFECTS: Concurrent therapy may produce additive vasospastic effects. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturer states that sumatriptan should not be used within 24 hours of an ergotamine-containing or ergotamine-like medication (such as dihydroergotamine or methysergide).(1,2) The Australian(3) and UK(4,5) manufacturers state that 24 hours should elapse before sumatriptan is administered following an ergotamine-containing preparation and 6 hours should elapse before an ergotamine-containing preparation is administered following sumatriptan. The US manufacturer states that zolmitriptan should not be used within 24 hours of an ergotamine-containing or ergotamine-like medication.(6) The UK manufacturer states that zolmitriptan should not be used within 6 hours of an ergotamine-containing or ergotamine-like medication.(7) The The Australian manufacturer states that 24 hours should elapse before zolmitriptan is administered following an ergotamine-containing preparation and 6 hours should elapse before an ergotamine-containing medication is administered following zolmitriptan.(8) The US manufacturer states that the use of rizatriptan within 24 hours of an ergotamine-containing or ergot-type medication is contraindicated.(9) The US manufacturer states that the use of naratriptan within 24 hours of an ergotamine-containing or ergot-type medication is contraindicated.(10) The Australian manufacturer states that concurrent use of naratriptan and ergotamine or ergotamine derivatives is not recommended.(11) The US manufacturer states that the use of eletriptan within 24 hours of an ergotamine-containing or ergot-type medication is contraindicated.(12) The UK manufacturer states that the use of eletriptan within 24 hours of an ergotamine-containing or ergot-type medication is not recommended.(13) DISCUSSION: Because of the theoretical risk of additive vasospastic effects, the US manufacturer states that the use of sumatriptan within 24 hours of an ergotamine-containing or ergotamine-like medication is contraindicated.(1,2) The Australian(3) and UK(4,5) manufacturer states that 24 hours should elapse before sumatriptan is administered following an ergotamine-containing preparation and 6 hours should elapse before an ergotamine-containing medication is administered following sumatriptan. Although the pharmacokinetics of zolmitriptan were not affected by ergotamine, the UK manufacturer of zolmitriptan recommends that 6 hours should elapse between the administration of zolmitriptan and an ergotamine preparation.(7) The US manufacturer of zolmitriptan states under contraindications that zolmitriptan should not be used within 24 hours of an ergotamine-containing or ergot-type medication.(6) The Australian manufacturer states that 24 hours should elapse before zolmitriptan is administered following an ergotamine-containing preparation and 6 hours should elapse before an ergotamine-containing medication is administered following zolmitriptan.(8) Because of the additive risk of prolonged vasospastic reactions, the manufacturers of rizatriptan(9) and naratriptan(10) in the US state that the use of ergotamine-containing or ergot-type medications and these agents is contraindicated. The Australian manufacturer states that concurrent use of naratriptan and ergotamine or ergotamine derivatives is not recommended.(11) Administration of oral ergotamine one and two hours after eletriptan resulted in additive increases in blood pressure.(13)	DIHYDROERGOTAMINE MESYLATE, ERGOLOID MESYLATES, ERGOMAR, ERGOTAMINE TARTRATE, ERGOTAMINE-CAFFEINE, METHYLERGONOVINE MALEATE, METHYSERGIDE MALEATE, MIGERGOT, MIGRANAL, TRUDHESA
Eletriptan/Selected Macrolide; Ketolide Antibiotics SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Macrolide or ketolide antibiotics which are moderately-strong to strong inhibitors of CYP3A4 may inhibit the metabolism of eletriptan.(1-3) CLINICAL EFFECTS: Concurrent use may result in elevated levels of and adverse effects from eletriptan.(1,2) Antibiotic agents linked to this monograph are clarithromycin, erythromycin, josamycin, telithromycin and troleandomycin. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturer of eletriptan states that eletriptan should not be used within at least 72 hours of treatment with strong CYP3A4 inhibitors such as clarithromycin or troleandomycin.(2) The UK manufacturer of eletriptan states that eletriptan should not be used together with clarithromycin, erythromycin, or josamycin.(1) If migraine treatment is needed during macrolide or ketolide antibiotic therapy use triptans not metabolized by CYP3A4 such as frovatriptan, sumatriptan, or zolmitriptan.(4-7) DISCUSSION: In a clinical study with a moderate to strong CYP3A4 inhibitor, erythromycin 1000 mg increased the eletriptan maximum concentration (Cmax) and area-under-curve (AUC) by 2-fold and 3.6-fold, respectively. The half-life of eletriptan increased from 4.6 hours to 7.1 hours.(1) In a clinical study with a strong CYP3A4 inhibitor, ketoconazole (400 mg) increased the eletriptan maximum concentration (Cmax) and area-under-curve (AUC) by 2.7-fold and 5.9-fold, respectively. The half-life of eletriptan increased from 4.8 hours to 8.3 hours.(1) The time to Cmax (Tmax) increased from 2.8 hours to 5.4 hours.(2)	CLARITHROMYCIN, CLARITHROMYCIN ER, E.E.S. 200, E.E.S. 400, ERY-TAB, ERYPED 200, ERYPED 400, ERYTHROCIN LACTOBIONATE, ERYTHROCIN STEARATE, ERYTHROMYCIN, ERYTHROMYCIN ESTOLATE, ERYTHROMYCIN ETHYLSUCCINATE, ERYTHROMYCIN LACTOBIONATE, LANSOPRAZOL-AMOXICIL-CLARITHRO, OMECLAMOX-PAK, VOQUEZNA TRIPLE PAK
Eletriptan/Selected Azole Antifungals SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Itraconazole, ketoconazole, posaconazole and voriconazole are strong inhibitors of CYP3A4 and may inhibit the metabolism of eletriptan via this pathway.(1-3) CLINICAL EFFECTS: Concurrent use may result in elevated levels of and adverse effects from eletriptan.(1,2) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturer of eletriptan states that eletriptan should not be used within at least 72 hours of administration of a strong CYP3A4 inhibitor.(2) The UK manufacturer of eletriptan states that eletriptan should not be used together with itraconazole or ketoconazole.(1) If migraine treatment is needed during azole antifungal therapy use triptans not metabolized by CYP3A4 such as frovatriptan, sumatriptan, or zolmitriptan.(4-7) DISCUSSION: In clinical studies, ketoconazole (400 mg) increased the eletriptan maximum concentration (Cmax) and area-under-curve (AUC) by 2.7-fold and 5.9-fold, respectively. The half-life of eletriptan increased from 4.8 hours to 8.3 hours.(1) The time to Cmax (Tmax) increased from 2.8 hours to 5.4 hours.(2)	ITRACONAZOLE, ITRACONAZOLE MICRONIZED, KETOCONAZOLE, NOXAFIL, POSACONAZOLE, SPORANOX, TOLSURA, VFEND, VFEND IV, VORICONAZOLE
Eletriptan/Selected Protease Inhibitors; Cobicistat SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Cobicistat or protease inhibitors which are strong inhibitors of CYP3A4 may reduce the CYP3A4 mediated metabolism of eletriptan.(1-6) CLINICAL EFFECTS: Concurrent use of eletriptan with strong inhibitors of CYP3A4(1-7) may result in elevated levels of and adverse effects from eletriptan.(1-6) Agents linked to this monograph are: atazanavir, boceprevir, cobicistat, indinavir, lopinavir, nelfinavir, nirmatrelvir, paritaprevir, saquinavir, telaprevir, and tipranavir. PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturer of eletriptan states that eletriptan should not be used within at least 72 hours of potent inhibitors of CYP3A4.(2) The UK manufacturer of eletriptan states that eletriptan should not be used together with indinavir, nelfinavir, or ritonavir.(1) If migraine treatment is needed during protease inhibitor therapy, use triptans not metabolized by CYP3A4 such as frovatriptan, sumatriptan, or zolmitriptan.(8-11) DISCUSSION: In a clinical trial, another strong CYP3A4 inhibitor ketoconazole 400 mg, increased the eletriptan maximum concentration (Cmax) and exposure (area-under-curve, AUC) by 2.7-fold and 5.9-fold, respectively. The half-life of eletriptan increased from 4.8 hours to 8.3 hours.(1) In another trial, a high dose of a moderate to strong CYP3A4 inhibitor, erythromycin (1000 mg), increased the eletriptan Cmax and AUC by 2-fold and 3.6-fold, respectively. The half-life of eletriptan increased from 4.6 hours to 7.1 hours.(2)	APTIVUS, ATAZANAVIR SULFATE, EVOTAZ, GENVOYA, KALETRA, LOPINAVIR-RITONAVIR, PAXLOVID, PREZCOBIX, REYATAZ, STRIBILD, SYMTUZA, TYBOST, VIRACEPT
Eletriptan/Nefazodone SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Nefazodone may inhibit the metabolism of eletriptan by CYP3A4.(1) CLINICAL EFFECTS: Concurrent use may result in elevated levels of and adverse effects from eletriptan.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturer of eletriptan states that eletriptan should not be used within at least 72 hours of nefazodone.(1) DISCUSSION: Concurrent use with ketoconazole, another potent inhibitor of CYP3A4, resulted in about a 3-fold increase in the maximum concentration (Cmax) and about a 6-fold increase in the area-under-curve (AUC) of eletriptan. Eletriptan half-life increased from 5 hours to 8 hours and the time to Cmax (Tmax) increased from 2.8 hours to 5.4 hours.(1) Concurrent use with erythromycin, also an inhibitor of CYP3A4, increased the Cmax and AUC of eletriptan by about 2-fold and about 4-fold, respectively.(1)	NEFAZODONE HCL
Eletriptan/Ribociclib SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Ribociclib is a strong inhibitor of CYP3A4 and may inhibit the metabolism of eletriptan via this pathway.(1) CLINICAL EFFECTS: Concurrent use may result in elevated levels of and adverse effects from eletriptan.(1) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturer of eletriptan states that eletriptan should not be used within at least 72 hours of administration of a strong CYP3A4 inhibitor.(2) If migraine treatment is needed during ribociclib therapy use triptans not metabolized by CYP3A4 such as frovatriptan, sumatriptan, or zolmitriptan.(2-4) DISCUSSION: In a study in healthy subjects, concomitant administration of ribociclib (400 mg once daily for 8 days) with midazolam increased the midazolam maximum concentration (Cmax) and area under the curve (AUC) by 2.1-fold and 3.8-fold, respectively. Administration of ribociclib 600 mg once daily is predicted to increase the midazolam Cmax and AUC by 2.4-fold and 5.2-fold, respectively.(5)	KISQALI
Eletriptan/Levoketoconazole SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient. MECHANISM OF ACTION: Levoketoconazole is a strong inhibitor of CYP3A4 and may inhibit the metabolism of eletriptan via this pathway.(1-3) CLINICAL EFFECTS: Concurrent use may result in elevated levels of and adverse effects from eletriptan.(1,2) PREDISPOSING FACTORS: None determined. PATIENT MANAGEMENT: The US manufacturer of eletriptan states that eletriptan should not be used within at least 72 hours of administration of a strong CYP3A4 inhibitor.(2) DISCUSSION: In clinical studies, ketoconazole (400 mg), a strong CYP3A4 inhibitor, increased the eletriptan maximum concentration (Cmax) and area-under-curve (AUC) by 2.7-fold and 5.9-fold, respectively. The half-life of eletriptan increased from 4.8 hours to 8.3 hours.(1) The time to Cmax (Tmax) increased from 2.8 hours to 5.4 hours.(2)	RECORLEV

Drug contraindication overview.

Known or suspected ischemic heart disease (e.g., angina pectoris, myocardial infarction, silent ischemia), coronary vasospasm (e.g., Prinzmetal variant angina), uncontrolled hypertension, other serious underlying cardiovascular disease, cerebrovascular syndromes (e.g., stroke syndrome, transient ischemic attacks), peripheral vascular disease, or ischemic bowel disease. Basilar or hemiplegic migraine. Treatment within the previous 24 hours with another 5-HT1 receptor agonist or with an ergot alkaloid (e.g., ergotamine, dihydroergotamine, methysergide (no longer commercially available in the US)).

Severe hepatic impairment (Child-Pugh grade C). Known hypersensitivity to eletriptan or any ingredient in the formulation.

Adverse reaction overview.

Adverse effects occurring in 2% or more of patients receiving eletriptan include asthenia, headache, nausea, paresthesia, dizziness, somnolence, dry mouth, flushing or feeling of warmth, pain/pressure sensations (i.e., chest pain (tightness/pressure), abdominal pain/discomfort/stomach pain/cramps/pressure), dyspepsia, and dysphagia (i.e., throat tightness, difficulty swallowing ).

Safety and efficacy have not been established in children younger than 18 years of age. Eletriptan is not recommended for use in patients younger than 18 years of age.

Contraindicated

None

Severe Precaution

None

Management or Monitoring Precaution

None