Last update June 10, 2018

特非那定

Likely Compatibility

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

A 2nd generation antihistamine, derived from piperidine, with minimal sedative effects.
It is completely metabolized to fexofenadine.
Administered orally once a day.

Its high percentage of protein binding explains the negligible transfer to milk observed from fexofenadine (Lucas 1995).

In a telephone follow-up, 10% of infants whose mothers were taking terfenadine exhibited colic and irritability, which did not require treatment (Ito 1993).

American Academy of Pediatrics: medication usually compatible with breastfeeding (AAP 2001).

It has been withdrawn from sale in most countries due to serious cardiac arrhythmias when taken with many other medications and with grapefruit juice (Benton 1996, Smith 1994, Monahan 1990). Its metabolite, fexofenadine, does not cause arrhythmias.


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Other names

特非那定 is Terfenadine in Chinese.

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特非那定 belongs to this group or family:

Tradenames

Main tradenames from several countries containing 特非那定 in its composition:

List of 7 tradenames

Pharmacokinetics

Variable Value Unit
Molecular weight 472 daltons
Protein Binding 97 %
Tmax 2 - 4 hours
T½ 16 - 23 hours
M/P ratio 0.2 -
Theoretical Dose 0.006 mg/Kg/d
Relative Dose 0.3 - 0.7 %

References

  1. AAP - American Academy of Pediatrics Committee on Drugs. Transfer of drugs and other chemicals into human milk. Pediatrics. 2001 Sep;108(3):776-89. Abstract Full text (link to original source) Full text (in our servers)
  2. Benton RE, Honig PK, Zamani K, Cantilena LR, Woosley RL. Grapefruit juice alters terfenadine pharmacokinetics, resulting in prolongation of repolarization on the electrocardiogram. Clin Pharmacol Ther. 1996 Abstract
  3. Lucas BD Jr, Purdy CY, Scarim SK, Benjamin S, Abel SR, Hilleman DE. Terfenadine pharmacokinetics in breast milk in lactating women. Clin Pharmacol Ther. 1995 Abstract
  4. Smith SJ. Cardiovascular toxicity of antihistamines. Otolaryngol Head Neck Surg. 1994 Abstract
  5. Ito S, Blajchman A, Stephenson M, Eliopoulos C, Koren G. Prospective follow-up of adverse reactions in breast-fed infants exposed to maternal medication. Am J Obstet Gynecol. 1993 May;168(5):1393-9. Abstract
  6. Monahan BP, Ferguson CL, Killeavy ES, Lloyd BK, Troy J, Cantilena LR Jr. Torsades de pointes occurring in association with terfenadine use. JAMA. 1990 Abstract

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