Last update Nov. 16, 2019

Cyclobenzaprine Hydrochloride

Likely Compatibility

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

Relaxant drug of the muscle with action on the Central Nervous System and chemically related to tricyclic antidepressants.
Indicated in muscle spasms of musculoskeletal origin.
Oral administration one to three times a day, maximum 2 weeks.

Its pharmacokinetic data (large volume of distribution and high percentage of protein binding) explain the very small passage to milk observed (Burra 2019).
No problems have been observed in two infants whose mothers took it for months since birth (Burra 2019).

A 16-day-old newborn whose mother took cyclobenzaprine, paracetamol and oxycodone had recoverable cardiorespiratory problems (Beauchamp 2019).

It is recommended to use the lowest effective dose possible.
Long-term treatments or those mothers who are nursing a newborn or premature infant would be prudent the use of a known safer alternative or with a shorter elimination half life.

Alternatives

  • Carisoprodol (Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.)
  • Methocarbamol (Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.)

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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Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

Cyclobenzaprine Hydrochloride is also known as


Cyclobenzaprine Hydrochloride in other languages or writings:

Group

Cyclobenzaprine Hydrochloride belongs to this group or family:

Tradenames

Main tradenames from several countries containing Cyclobenzaprine Hydrochloride in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 33 - 55 %
Molecular weight 312 daltons
Protein Binding 93 %
VD 2 ( 0.5 - 5 ) l/Kg
pKa 8.47 -
Tmax 4.5 ( 2 - 7 ) hours
18 ( 8 - 37 ) hours
Theoretical Dose 0.00033 - 0.0015 mg/Kg/d
Relative Dose 0.4 - 0.9 %

References

  1. Burra B, Datta P, Rewers-Felkins K, Baker T, Hale TW. Transfer of Cyclobenzaprine into Human Milk and Subsequent Infant Exposure. J Hum Lact. 2019 Aug;35(3):559-562. Abstract
  2. Beauchamp GA, Hendrickson RG, Horowitz BZ, Spyker DA. Exposures Through Breast Milk: An Analysis of Exposure and Information Calls to U.S. Poison Centers, 2001-2017. Breastfeed Med. 2019 Sep;14(7):508-512. Abstract
  3. Brioschi TM, Schramm SG, Kano EK, Koono EE, Ching TH, Serra CH, Porta V. Pharmacokinetics and bioequivalence evaluation of cyclobenzaprine tablets. Biomed Res Int. 2013 Abstract Full text (link to original source) Full text (in our servers)
  4. MSyC-AgEspMedyPS. Ciclobenzaprina. Ficha técnica. 2013 Full text (in our servers)
  5. Darwish M, Hellriegel ET. Steady-state pharmacokinetics of once-daily cyclobenzaprine extended release: a randomized, double-blind, 2-period crossover study in healthy volunteers. Clin Ther. 2011 Abstract
  6. Winchell GA, King JD, Chavez-Eng CM, Constanzer ML, Korn SH. Cyclobenzaprine pharmacokinetics, including the effects of age, gender, and hepatic insufficiency. J Clin Pharmacol. 2002 Abstract
  7. Till AE, Constanzer ML, Demetriades J, Irvin JD, Lee RB, Ferguson RK. Evidence for route dependent biotransformation of cyclobenzaprine hydrochloride. Biopharm Drug Dispos. 1982 Abstract

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