It was patented in 1984 and came into medical use in 2001.[7] It was brought to the market in the US by Schering Corporation, later named
Schering-Plough.[3]
An emerging indication for desloratadine is in the treatment of
acne, as an inexpensive adjuvant to
isotretinoin and possibly as maintenance therapy or monotherapy.[10][11]
Desloratadine is well absorbed from the gut and reaches highest
blood plasma concentrations after about three hours. In the bloodstream, 83 to 87% of the substance are bound to
plasma proteins.[13]
Desloratadine is metabolized to 3-hydroxydesloratadine in a three-step sequence in normal metabolizers. First, N-glucuronidation of desloratadine by
UGT2B10; then, 3-hydroxylation of desloratadine N-glucuronide by
CYP2C8; and finally, a non-enzymatic deconjugation of 3-hydroxydesloratadine N-glucuronide.[16][17] Both desloratadine and 3-hydroxydesloratadine are eliminated via urine and feces with a
half-life of 27 hours in normal metabolizers.[13][18]
2% of
Caucasian people and 18% of people from African descent are desloratadine
poor metabolizers. In these people, the drug reaches threefold higher plasma concentrations at seven hours after intake, and it has a half-life of 89 hours (compared to a 27-hour half-life in normal metabolizers). Adverse effects were reported at similar rates in poor metabolizers, suggesting that it is not clinically relevant.[13][18]
^Schering Corporation (2000).
"CLARITIN brand of Loratadine - Full Prescribing Information (US FDA)"(PDF). US FDA. Retrieved 17 May 2024. loratadine is metabolized to descarboethoxyloratadine predominantly by cytochrome P450 3A4 (CYP3A4) and, to a lesser extent, by cytochrome P450 2D6 (CYP2D6).
^Lee HE, Chang IK, Lee Y, Kim CD, Seo YJ, Lee JH, et al. (December 2014). "Effect of antihistamine as an adjuvant treatment of isotretinoin in acne: a randomized, controlled comparative study". Journal of the European Academy of Dermatology and Venereology. 28 (12): 1654–1660.
doi:
10.1111/jdv.12403.
PMID25081735.
S2CID3406128.
^Layton AM (April 2016). "Top Ten List of Clinical Pearls in the Treatment of Acne Vulgaris". Dermatologic Clinics. 34 (2): 147–157.
doi:
10.1016/j.det.2015.11.008.
PMID27015774.
^
abcGonzález-Núñez V, Valero A, Mullol J (May 2013). "Safety evaluation of desloratadine in allergic rhinitis". Expert Opinion on Drug Safety. 12 (3). Informa Healthcare: 445–453.
doi:
10.1517/14740338.2013.788148.
PMID23574541.
S2CID40472187.
^Kazmi F, Barbara JE, Yerino P, Parkinson A (April 2015). "A long-standing mystery solved: the formation of 3-hydroxydesloratadine is catalyzed by CYP2C8 but prior glucuronidation of desloratadine by UDP-glucuronosyltransferase 2B10 is an obligatory requirement". Drug Metabolism and Disposition. 43 (4): 523–533.
doi:
10.1124/dmd.114.062620.
PMID25595597.