Last update May 10, 2021

8-Chloro-6,11-dihydro-11-{1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene}-5H-benzo[5,6]cyclohepta(1,2-b)pyridine (E)-2-butenedioate

Likely Compatibility

Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.

Second generation antihistamine and piperidine-type compound, without the sedative and anticholinergic effects of first generation antihistaminics.

Pharmacokinetic data (moderately high molecular weight, very large volume of distribution and high percentage of protein binding) make it unlikely an excretion into breast milk in significant amounts.

Expert authors consider antihistamines compatible with breastfeeding (So 2010).

Until more published data on this drug regarding breastfeeding is available, safer alternatives of better known drugs should be preferable, especially during the neonatal period and in case of prematurity.

Follow-up the baby for drowsiness and inappropriate infant feeding.

Alternatives

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

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Other names

8-Chloro-6,11-dihydro-11-{1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene}-5H-benzo[5,6]cyclohepta(1,2-b)pyridine (E)-2-butenedioate is Rupatadine Fumarate in Chemical name.

Is written in other languages:

Group

8-Chloro-6,11-dihydro-11-{1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene}-5H-benzo[5,6]cyclohepta(1,2-b)pyridine (E)-2-butenedioate belongs to this group or family:

Tradenames

Main tradenames from several countries containing 8-Chloro-6,11-dihydro-11-{1-[(5-methyl-3-pyridyl)methyl]-4-piperidylidene}-5H-benzo[5,6]cyclohepta(1,2-b)pyridine (E)-2-butenedioate in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 45 %
Molecular weight 532 daltons
Protein Binding 99 %
VD 138 l/Kg
Tmax 0.75 hours
T½ 5.9 hours

References

  1. AEMPS. Rupatadina. Ficha técnica. 2015 Full text (in our servers)
  2. So M, Bozzo P, Inoue M, Einarson A. Safety of antihistamines during pregnancy and lactation. Can Fam Physician. 2010 May;56(5):427-9. Abstract Full text (link to original source) Full text (in our servers)
  3. del Cuvillo A, Mullol J, Bartra J, Dávila I, Jáuregui I, Montoro J, Sastre J, Valero AL. Comparative pharmacology of the H1 antihistamines. J Investig Allergol Clin Immunol. 2006;16 Suppl 1:3-12. Review. No abstract available. Abstract Full text (link to original source) Full text (in our servers)

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