Eletriptan Hydrobromide

(BANM, USAN, rINNM)
Eletriptan Hydrobromide Chemical formula
Synonyms: (BANM, USAN, rINNM) Eletriptaanihydrobromidi; Élétriptan, Bromhydrate d’; Eletriptanhydrobromid; Eletriptani Hydrobromidum; Hidrobromuro de eletriptán; UK-116044-04. 3-{[(R)-1-Methyl-2-pyrrolidinyl]methyl}-5-[2-(phenylsulfonyl)ethyl]indole hydrobromide.
Cyrillic synonym: Элетриптана Гидробромид.

💊 Chemical information

Chemical formula: C22H26N2O2S,HBr = 463.4.
CAS — 143322-58-1 (eletriptan); 177834-92-3 (eletriptan hydrobromide).
ATC — N02CC06.
ATC Vet — QN02CC06.

💊 Adverse Effects and Precautions

As for Sumatriptan. Eletriptan should not be used in patients with severe hepatic or severe renal impairment. Blood pressure effects of eletriptan are increased in renal impairment and therefore the dose should be reduced in patients with mild to moderate renal impairment. No dosage adjustment is needed in mild or moderate hepatic impairment.

Breast feeding.

Eletriptan is distributed into breast milk and the manufacturer has suggested that infant exposure can be minimised by avoiding breast feeding for 24 hours after treatment.

💊 Interactions

As for Sumatriptan. Eletriptan should not be given with potent inhibitors of the cytochrome P450 isoenzyme CYP3A4 such as erythromycin and ketoconazole; increased plasma levels of eletriptan have been noted after such combinations. It is recommended that eletriptan should not be taken within at least 72 hours of treatment with such drugs.

💊 Pharmacokinetics

After oral doses eletriptan is rapidly and well absorbed (at least 81%) and has a bioavailability of about 50%. Peak plasma concentrations are attained within 1.5 hours. Eletriptan is about 85% protein bound. It is primarily metabolised by the hepatic cytochrome P450 isoenzyme CYP3A4. Non-renal clearance accounts for about 90% of the elimination of eletriptan and the plasma elimination half-life is about 4 hours. A small amount is distributed into breast milk.
1. Shah AK, et al. Pharmacokinetics and safety of oral eletriptan during different phases of the menstrual cycle in healthy volunteers. J Clin Pharmacol 2001; 41: 1339–44
2. Shah AK, et al. The pharmacokinetics and safety of single escalating oral doses of eletriptan. J Clin Pharmacol 2002; 42: 520–7
3. Milton KA, et al. Pharmacokinetics, pharmacodynamics, and safety of the 5-HT agonist eletriptan following intravenous and oral administration. J Clin Pharmacol 2002; 42: 528–39.

💊 Uses and Administration

Eletriptan hydrobromide is a selective serotonin (5HT 1 ) agonist with actions and uses similar to those of sumatriptan. It is used for acute treatment of the headache phase of migraine attacks. It should not be used for prophylaxis. Eletriptan is given orally as the hydrobromide, but doses are expressed in terms of the base; eletriptan hydrobromide 24.2 mg is equivalent to about 20 mg of eletriptan. The usual dose is 40 mg; if this is ineffective, a second dose should not be taken for the same attack. If symptoms recur within 24 hours after an initial response, a second dose may be taken after an interval of at least 2 hours. Doses of 80 mg may be used in subsequent attacks, but should not be repeated within a 24-hour period. For doses in renal impairment, see below.

Administration in renal impairment.

In the UK, a dose of 20 mg of eletriptan is recommended in patients with mild to moderate renal impairment. The maximum daily dose should not exceed 40 mg. Eletriptan should not be used in severe impairment.

Migraine.

For comparison of the relative benefits of different triptans in migraine, see under Sumatriptan. Further references.
1. Mathew NT, et al. Tolerability and safety of eletriptan in the treatment of migraine: a comprehensive review. Headache 2003; 43: 962–74
2. Takiya L, et al. Safety and efficacy of eletriptan in the treatment of acute migraine. Pharmacotherapy 2006; 26: 115–28
3. McCormack PL, Keating GM. Eletriptan: a review of its use in the acute treatment of migraine. Drugs 2006; 66: 1129–49.

💊 Preparations

Proprietary Preparations

Austria: Relpax; Belg.: Relert; Canad.: Relpax; Chile: Relpax; Cz.: Relpax; Denm.: Relpax; Fin.: Relert; Fr.: Relpax; Ger.: Relpax; Gr.: Relpax; Hung.: Relpax; Israel: Relert; Ital.: Relpax; Mex.: Relpax; Neth.: Relpax; Norw.: Relpax; Pol.: Relpax; Port.: Relert; Rus.: Relpax (Релпакс); S.Afr.: Relpax; Singapore: Relpax; Spain: Relert; Relpax; Swed.: Relpax; Switz.: Relpax; Turk.: Relpax; UK: Relpax; USA: Relpax.
Published October 17, 2018.