Almotriptan Malate

(BANM, USAN, rINNM)
Synonyms: Almotriptan, Malate d’; Almotriptani Malas; LAS-31416 (almotriptan); Malato de almotriptán; PNU-180638E (almotriptan malate). 1-[({3-[2-(Dimethylamino)ethyl]indol-5-yl}methyl)sulfonyl]pyrrolidine malate (1:1).
Cyrillic synonym: Альмотриптана Малат.

💊 Chemical information

Chemical formula: C17H25N3O2S,C4H6O5 = 469.6.
CAS — 154323-57-6 (almotriptan); 181183-52-8 (almotriptan malate).
ATC — N02CC05.
ATC Vet — QN02CC05.

💊 Adverse Effects and Precautions

As for Sumatriptan. Almotriptan should not be used in patients with severe hepatic impairment since clearance is likely to be markedly impaired, and should be given with caution, and in reduced doses, to patients with mild to moderate hepatic impairment. The dose of almotriptan should also be reduced in patients with severe renal impairment. Patients with hypersensitivity to sulfonamides may theoretically exhibit a similar reaction to almotriptan.

Incidence of adverse effects.

Results from studies involving more than 2500 patients with migraine suggested that adverse effects of almotriptan were infrequent.1 The commonest adverse effects reported were dizziness, nausea and vomiting, headache, paraesthesia, fatigue, and drowsiness, all of which occurred in less than 3% of patients. The incidence of chest symptoms was 0.2% in 2 large phase III studies.
1. Dodick DW. Oral almotriptan in the treatment of migraine: safety and tolerability. Headache 2001; 41: 449–55.

💊 Interactions

As for Sumatriptan.

💊 Pharmacokinetics

After oral doses, peak plasma-almotriptan concentrations are obtained in about 1 to 3 hours, with a bioavailability of about 70%. Protein binding is about 35%. Almotriptan is metabolised, mainly by monoamine oxidase type A to the inactive indole acetic acid derivative and to a lesser extent by cytochrome P450 isoenzymes CYP3A4 and CYP2D6 to the inactive gammaaminobutyric acid derivative. More than 75% of an oral dose is excreted in the urine and the remainder in faeces. About 40 to 50% of the dose in the urine and 5% in the faeces is excreted as unchanged drug. The plasma elimination half-life is about 3.5 hours in healthy subjects, increasing to about 7 hours in severe renal impairment.
Distribution into milk has been found in studies in rats.
1. Jansat JM, et al. Absolute bioavailability, pharmacokinetics, and urinary excretion of the novel antimigraine agent almotriptan in healthy male volunteers. J Clin Pharmacol 2002; 42: 1303–10
2. McEnroe JD, Fleishaker JC. Clinical pharmacokinetics of almotriptan, a serotonin 5-HT receptor agonist for the treatment of migraine. Clin Pharmacokinet 2005; 44: 237–46.

💊 Uses and Administration

Almotriptan malate is a selective serotonin (5-HT 1 ) agonist with actions and uses similar to those of sumatriptan. It is used for the acute treatment of the headache phase of migraine attacks. It should not be used for prophylaxis. Almotriptan is given orally as the malate, and doses are expressed in terms of the base; almotriptan malate 8.75 mg is equivalent to about 6.25 mg of almotriptan. The usual dose of almotriptan is 12.5 mg in the UK and 6.25 or 12.5 mg in the USA. 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. No more than 2 doses should be taken in a 24-hour period. For doses in hepatic and renal impairment see below.
1. Holm KJ, Spencer CM. Almotriptan. CNS Drugs 1999; 11: 159–64
2. Keam SJ, et al. Almotriptan: a review of its use in migraine. Drugs 2002; 62: 387–414.

Administration in hepatic or renal impairment.

In patients with hepatic or severe renal impairment, no more than 12.5 mg of almotriptan should be taken in 24 hours; a starting dose of 6.25 mg may be used. Almotriptan is contra-indicated in patients with severe hepatic disease.

Migraine.

For comparison of the relative benefits of different triptans in migraine, see under Sumatriptan. Further references.
1. Balbisi EA. Efficacy and safety of almotriptan malate for migraine. Am J Health-Syst Pharm 2002; 59: 2184–93
2. Dodick DW. A review of the clinical efficacy and tolerability of almotriptan in acute migraine. Expert Opin Pharmacother 2003; 4: 1157–63
3. Dowson AJ. Oral almotriptan: practical uses in the acute treatment of migraine. Expert Rev Neurother 2004; 4: 339–48
4. Mathew NT. Efficacy and tolerability of almotriptan in controlled clinical trials. Eur Neurol 2005; 53 (suppl 1): 29–33
5. Pascual J. Efficacy and tolerability of almotriptan in postmarketing surveillance studies. Eur Neurol 2005; 53 (suppl 1): 34–40
6. Dahlof CG, et al. Efficacy, speed of action and tolerability of almotriptan in the acute treatment of migraine: pooled individual patient data from four randomized, double-blind, placebo-controlled clinical trials. Cephalalgia 2006; 26: 400–8
7. Diener H-C. A review of recent clinical experience with almotriptan. Drugs 2006; 66 (suppl 3): 17–25.

💊 Preparations

Proprietary Preparations

Belg.: Almogran; Canad.: Axert; Denm.: Almogran; Fin.: Almogran; Fr.: Almogran; Ger.: Almogran; Irl.: Almogran; Ital.: Almogran; Almotrex; Neth.: Almogran; Norw.: Almogran; Port.: Almogran; Amignul; Spain: Almogran; Amignul; Swed.: Almogran; UK: Almogran; USA: Axert.
Published October 09, 2018.