Last update: May 11, 2019

Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate

High Risk for breastfeeding


Poorly safe. Evaluate carefully.
Use safer alternative or interrupt breastfeeding 3 to 7 T½.
Read the Comment.

An alkaloid found in the roots of Rauwolfia serpentina or Rauwolfia vomitoria, a shrub which is native to India. It was the first antihypertensive ever used, nowadays superseded by new products with fewer side effects. It has centrally-acting antidrenergic effects. It can cause sedation and hypotonia.
It has been used to treat hypertension and in psychosis.
Oral administration once a day.

Since the last update we have not found any published data on its excretion in breast milk.
There are unconfirmed out-of-date reports that state it is excreted in breastmilk (Nice 2004, White 1984).

Its pharmacokinetic data - not very high molecular weight, low protein binding and very long half-life (Infomed 2018) - makes transfer to milk possible in amounts that could be significant.

It can produce hyperprolactinemia (Molitch 1992, Camanni 1981, Lee 1976).
This product is very little used at present, with a lack of bibliographic data on its pharmacokinetics.

Until there is more published data on this drug in relation to breastfeeding, safer known alternatives may be preferable (Malachias 2016, WHO 2002), especially during the neonatal period and in cases of prematurity.

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.

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

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate is Reserpine in Chemical name.

Is written in other languages:

Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate is also known as

Group

Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate belongs to this group or family:

Tradenames

Main tradenames from several countries containing Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate in its composition:

  • Adelfan
  • Diupres™. Contains other elements than Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate in its composition
  • Higroton-Res™. Contains other elements than Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate in its composition
  • Hydropres™. Contains other elements than Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate in its composition
  • Marpres™. Contains other elements than Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate in its composition
  • Regroton™. Contains other elements than Methyl 11,17α-dimethoxy-18β-(3,4,5-trimethoxybenzoyloxy)-3β,20α-yohimbane-16β-carboxylate; Methyl O-(3,4,5-trimethoxybenzoyl)reserpate in its composition
  • Serpasil
  • Serpasol
  • Tensiocomplet

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 50 %
Molecular weight 609 daltons
Protein Binding 62 %
pKa 6,6 -
Tmax 2 hours
T1/2 168 hours

References

  1. Infomed. Reserpina. Ficha técnica. 2018 Full text (in our servers)
  2. Malachias MV, Figueiredo CE, Sass N, Antonello IC, Torloni MR, Bortolotto MRF L. 7th Brazilian Guideline of Arterial Hypertension: Chapter 9 - Arterial Hypertension in pregnancy Arq Bras Cardiol. 2016 Abstract Full text (link to original source) Full text (in our servers)
  3. Frank J Nice, Deborah DeEugenio, Traci A DiMino, Ingrid C Freeny, Marissa B Rovnack, and Joseph S Gromelski. Medications and Breast-Feeding: A Guide for Pharmacists, Pharmacy Technicians, and other Healthcare Professionals Part II. Journal of Pharmacy Technology 20 (2), 85-95 2004 Full text (link to original source) Full text (in our servers)
  4. WHO / UNICEF. BREASTFEEDING AND MATERNAL MEDICATION Recommendations for Drugs in the Eleventh WHO Model List of Essential Drugs. Department of Child and Adolescent Health and Development (WHO/UNICEF) 2002 Full text (link to original source) Full text (in our servers)
  5. Molitch ME. Pathologic hyperprolactinemia. Endocrinol Metab Clin North Am. 1992 Abstract
  6. White WB. Management of hypertension during lactation. Hypertension. 1984 Abstract
  7. Camanni E, Strumia E, Portaleone P, Molinatti GM. Prolactin secretion during reserpine and syrosingopine treatment. Eur J Clin Pharmacol. 1981 Abstract
  8. Lee PA, Kelly MR, Wallin JD. Increased prolactin levels during reserpine treatment of hypertensive patients. JAMA. 1976 Abstract

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