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Almotriptan Malate

(British Approved Name Modified, US Adopted Name, rINNM)

Drug Nomenclature

INNs in main languages (French, Latin, Russian, and Spanish):

Almotriptan MalateSynonyms:Almotriptán, malato de; LAS-31416 (almotriptan); PNU-180638E (almotriptan malate)
BAN:Almotriptan Malate [BANM]
USAN:Almotriptan Malate
INN:Almotriptan Malate [rINNM (en)]
INN: Malato de almotriptán [rINNM (es)]
INN:Almotriptan, Malate d’ [rINNM (fr)]
INN: Almotriptani Malas [rINNM (la)]
INN: Альмотриптана Малат [rINNM (ru)]
Chemical name: 1-[({3-[2-(Dimethylamino)ethyl]indol-5-yl}methyl)sulfonyl]pyrrolidine malate (1:1)
Molecular formula: C17H25N3O2S,C4H6O5 =469.6
CAS:154323-57-6 (almotriptan); 181183-52-8 (almotriptan malate)
ATC code: N02CC05

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 hypers en sitivity 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. 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.

Interactions

As for Sumatriptan.

Pharmacokinetics

After oral doses, peak plasma-almotriptan concentrations are obtained in about 1 to 3 hours, with abioavailability 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 gamma-aminobutyric 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.

Uses and Administration

Almotriptan MalateAlmotriptan malate is a selective serotonin (5-HT1) 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.

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.

Single-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Belgium: Almogran;
Denmark: Almogran;
Finland: Almogran;
France: Almogran;
Germany: Almogran;
Ireland: Almogran;
Italy: Almogran; Almotrex;
Netherlands: Almogran;
Norway: Almogran;
Portugal: Almogran;
Spain: Almogran; Amignul;
Sweden: Almogran;
United Kingdom: Almogran;
United States: Axert

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