Last update: Aug. 7, 2019

(5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate

Low Risk for breastfeeding


Moderately safe. Probably compatible.
Mild risk possible. Follow up recommended.
Read the Comment.

Ergot alkaloid and alpha adrenergic receptor antagonist with vasoconstrictor effect.
Indicated in the treatment of acute migraine attack, usually together with caffeine.
Oral administration every half hour if necessary, up to a maximum of 6 mg per day (Sandoz 2012, AEMPS 2009).

Since the last update we have not found published data on its excretion in breastmilk.

Its pharmacokinetic data (high molecular weight and high plasma protein binding) makes it unlikely it will transfer into breastmilk in significant amounts.

Although gastrointestinal absorption is 62%, hepatic metabolism makes bioavailability less than 5% (AEMPS 2009), which impedes its transfer from breastmilk to infant plasma, except in premature infants and the immediate neonatal period when there may be greater intestinal permeability.

Other ergot alkaloids, such as bromocriptine, inhibit prolactin secretion, but administration of 3mg daily of ergotamine during the first week postpartum did not affect the production of breastmilk or the weight gain of infants, who did not present problems (Jolivet 1978).

Occasional use and at a sufficient minimum dose would not create problems during breastfeeding.

Until there is more published data on this drug in relation to breastfeeding, safer known alternatives are preferable (Bordini 2016, Davanzo 2014, Duong 2010, Jürgens 2009, Loder 2007, MacGregor 2007, Moretti 2000), especially during the neonatal period and in cases of prematurity.

Sumatriptan, which is known to have minimal transfer to milk (Wojnar 1996), is a good alternative as a treatment for migraine during breastfeeding, and it is also more effective than the ergotamine/caffeine combination (Worthington 2013).

Alternatives

Suggestions made at e-lactancia are done by APILAM´s pediatricians and pharmacists, and are based on updated scientific publications.
It is not intended to replace the relationship you have with your doctor but to compound it.

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Other names

(5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate is Ergotamine Tartrate in Chemical name.

Is written in other languages:

Group

(5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate belongs to this group or family:

Tradenames

Main tradenames from several countries containing (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition:

List of 26 tradenames
  • Anergan™
  • Avamigran™
  • Bellataminal (Беллатаминал)™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Bellergal™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Bellergal-S™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Cafatine™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Cafatine-PB™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Cafergot™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Caftar™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Cefalex Plus™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Enxak™
  • Ercaf™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Ergocaf™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Ergodryl M™
  • Ergomar™
  • Ergotan™
  • Hemicraneal™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Lingraine™
  • Migergot™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Migral™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Migral Compositum™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Migral II™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Migrane™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Migretil™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Migril™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition
  • Optium (Mexico)™. Contains other elements than (5′S)-12′-Hydroxy-2′-methyl-5′-benzylergotaman-3′,6′,18-trione tartrate; (5′S)-12′-Hydroxy-2′-methyl-3′,6′,18-trioxo-5-benzylergotaman (+)-tartrate in its composition

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 2 (rectal: 5) %
Molecular weight 1.313 daltons
Protein Binding 93 - 98 %
pKa 9,7 - 11,6 -
Tmax 0,5 - 3 hours
T1/2 2 - 21 hours

References

  1. Bordini CA, Roesler C, Carvalho Dde S, Macedo DD, Piovesan É, Melhado EM, Dach F, Kowacs F, Silva Júnior HM, Souza JA, Maciel JA Jr, Carvalho JJ, Speciali JG, Barea LM, Queiroz LP, Ciciarelli MC, Valença MM, Lima MM, Vincent MB. Recommendations for the treatment of migraine attacks - a Brazilian consensus. Arq Neuropsiquiatr. 2016 Abstract Full text (link to original source) Full text (in our servers)
  2. Davanzo R, Bua J, Paloni G, Facchina G. Breastfeeding and migraine drugs. Eur J Clin Pharmacol. 2014 Abstract
  3. Worthington I, Pringsheim T, Gawel MJ, Gladstone J, Cooper P, Dilli E, Aube M, Leroux E, Becker WJ; Canadian Headache Society Acute Migraine Treatment Guideline Development Group. Canadian Headache Society Guideline: acute drug therapy for migraine headache. Can J Neurol Sci. 2013 Sep;40(5 Suppl 3):S1-S80. Review. Abstract Full text (in our servers)
  4. Sandoz. Ergotamine (Cafergot). Drug Summary. 2012 Full text (in our servers)
  5. Duong S, Bozzo P, Nordeng H, Einarson A. Safety of triptans for migraine headaches during pregnancy and breastfeeding. Can Fam Physician. 2010 Abstract Full text (link to original source) Full text (in our servers)
  6. AEMPS - Amdipharm. Ergotamina (Cafergot). Ficha técnica. 2009 Full text (in our servers)
  7. Jürgens TP, Schaefer C, May A. Treatment of cluster headache in pregnancy and lactation. Cephalalgia. 2009 Abstract
  8. Raña-Martínez N. Migraña en la mujer. [Migraine in females]. Rev Neurol. 2008 Abstract
  9. Loder E. Migraine in pregnancy. Semin Neurol. 2007 Abstract
  10. MacGregor EA. Migraine in pregnancy and lactation: a clinical review. J Fam Plann Reprod Health Care. 2007 Abstract Full text (in our servers)
  11. Moretti ME, Lee A, Ito S. Which drugs are contraindicated during breastfeeding? Practice guidelines. Can Fam Physician. 2000 Sep;46:1753-7. Review. Abstract Full text (link to original source) Full text (in our servers)
  12. Wojnar-Horton RE, Hackett LP, Yapp P, Dusci LJ, Paech M, Ilett KF. Distribution and excretion of sumatriptan in human milk. Br J Clin Pharmacol. 1996 Abstract Full text (link to original source) Full text (in our servers)
  13. Jolivet A, Robyn C, Huraux-Rendu C, Gautray JP. [Effect of ergot alkaloid derivatives on milk secretion in the immediate postpartum period]. J Gynecol Obstet Biol Reprod (Paris). 1978 Jan;7(1):129-34. French. Abstract

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