• Title/Summary/Keyword: Loratadine

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Effects of Hydrocortisone on the Pharmacokinetics of Loratadine after Oral and Intravenous Loratadine Administration to Rats

  • Choi, Jun-Shik;Choi, In;Burm, Jin-Pil
    • Biomolecules & Therapeutics
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    • v.17 no.2
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    • pp.205-210
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    • 2009
  • The present study investigated the effects of hydrocortisone on the pharmacokinetics of loratadine in rats after intravenous and oral administration. A single dose of loratadine was administered either orally (4 mg/kg) or intravenously (1 mg/kg) with or without oral hydrocortisone (0.3 or 1.0 mg/kg). Compared to the control group (without hydrocortisone), after oral administration of loratadine, the area under the plasma concentration-time curve (AUC) was significantly increased by 30.2-81.7% in the presence of hydrocortisone (p<0.05). The peak plasma concentration ($C_{max}$) was significantly increased by 68.4% in the presence of 1.0 mg/kg hydrocortisone after oral administration of loratadine (p<0.05). Hydrocortisone (1.0 mg/kg) significantly increased the terminal plasma half-life ($t_{1/2}$) of loratadine by 20.8% (p<0.05). Consequently, the relative bioavailability of loratadine was increased by 1.30- to 1.82-fold. In contrast, oral hydrocortisone had no effects on any pharmacokinetic parameters of loratadine given intravenously. This suggests that hydrocortisone may improve the oral bioavailability of loratadine by reducing first-pass metabolism of loratadine, most likely mediated by P-gp and/or CYP3A4 in the intestine and/or liver. In conclusion, hydrocortisone significantly enhanced the bioavailability of orally administered loratadine in rats, which may have been due to inhibition of both CYP 3A4-mediated metabolism and P-gp in the intestine and/or liver by the presence of hydrocortisone.

Effects of Curcumin on the Pharmacokinetics of Loratadine in Rats: Possible Role of CYP3A4 and P-glycoprotein Inhibition by Curcumin

  • Li, Cheng;Choi, Byung-Chul;Kim, Dong-Ki;Choi, Jun-Shik
    • Biomolecules & Therapeutics
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    • v.19 no.3
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    • pp.364-370
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    • 2011
  • The purpose of this study was to investigate the effects of curcumin on the pharmacokinetics of loratadine in rats. The effect of curcumin on P-glycoprotein (P-gp) and cytochrome P450 (CYP) 3A4 activity was evaluated. Pharmacokinetic parameters of loratadine were also determined after oral and intravenous administration in the presence or absence of curcumin. Curcumin inhibited CYP3A4 activity with an IC50 value of 2.71 ${\mu}M$ and the relative cellular uptake of rhodamine-123 was comparable. Compared to the oral control group, curcumin significantly increased the area under the plasma concentration-time curve and the peak plasma concentration by 39.4-66.7% and 34.2-61.5%. Curcumin also significantly increased the absolute bioavailability of loratadine by 40.0-66.1% compared to the oral control group. Consequently, the relative bioavailability of loratadine was increased by 1.39- to 1.67-fold. In contrast, curcumin had no effect on any pharmacokinetic parameters of loratadine given intravenously, implying that the enhanced oral bioavailability may be mainly due to increased intestinal absorption caused via P-gp and CYP3A4 inhibition by curcumin rather than to reduced renal and hepatic elimination of loratadine. Curcumin enhanced the oral bioavailability of loratadine in this study. The enhanced bioavailability of loratadine might be mainly attributed to enhanced absorption in the gastrointestinal tract via the inhibition of P-gp and reduced fi rst-pass metabolism of loratadine via the inhibition of the CYP3A subfamily in the small intestine and/or in the liver by curcumin.

Effects of Loratadine, Cetirizine, and Terfenadine on Histamine-Induced Wheal and Erythema Responses in Normal Canine Skin (개 피부에서 Histamine에 의한 팽진과 발적에 대한 loratadine, cetirizine과 terfenadine의 억제효과)

  • Jeong, A-Young;Jeong, Hyo-Hoon;Heo, Woo-Phil;Eom, Ki-Dong;Jang, Kawng-Ho;Oh, Tae-Ho
    • Journal of Veterinary Clinics
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    • v.19 no.2
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    • pp.186-190
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    • 2002
  • This crossover study was performed in order to compare the effects of cetirizine, loratadine, and terfenadine in canine skin. Five healthy dogs were used. Cetirizine 0.5 mg/kg, loratadine 5 mg/kg and terfenadine 5 mg/kg were administered orally 4 hours before the experiment. Erythema indices and wheal size were assessed by Hexameter ($MX^{\circledR}$ 18, CK, Germany) and skin reaction guide, respectively. Cetirizine-induced erythema inhibition was generally higher than other drugs and was significantly different from placebo. Cetirizine was superior to placebo at 3, 4, 5, 6, 7, and 8 minutes (p< 0.01). Cetirizine also was superior to placebo at 9 minutes (p< 0.05). Loratadine and terfenadine erythema inhibition were better than after placebo treatment from 4 to 9 minutes, but erythema index of terfenadine at 7 minutes was not observed probability of 95% and 99%. At 10 minutes, intradermal injection of the histamine caused a mean wheal dimension for placebo, cetirizine, loratadine and terfenadine, which were 13.25$\pm$0.75 mm,7.5$\pm$ 1.02 mm (53% reduction, p<0.007),6.2$\pm$0.58 mm(43% reduction, p <0.01), and 8.4 $\pm$0.67 mm(37% reduction, p< 0.05), respectively, comparing with placebo. Loratadine and cetirizine were good antihistamines for clinical therapy for atopic dermatitis in dog.

HPLC Determination of Loratadine in Human Plasma with UV Detection and Pharmacokinetics of Loratadine Following Oral Administration of Tablet Formulation in Human

  • Cho, Eun-Sook;Chun, In-Koo
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.420.2-421
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    • 2002
  • A validated UV determination of loratadine in human plasma was developed and the pharmacokinetic profiles of single dose of loratadine were determined in 8 healthy volunteers. Human serum samples (1.0 mL) spiked with known concentration of loratadine and 50 ng diazepam as an internal standard were alkalinized with 500 ${\mu}\ell$ ${\mu}\ell$ of 10% $Na_{2}CO_{3}$ and extracted with 7 mL of mixture of isopentane and hexane (2 : 1. v/v) for 5 min. Extracts were centrifuged and 6 mL of organic layer was back-extracted with 150 ${\mu}\ell$ of 12.5% $Na_{2}PO_{4}$ for 1 min. (omitted)

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A comparison study of the effects of loratadine-pharmacopuncture and loratadine-oral administration based on traditional Korean medicine theory on anaphylactic reaction in mice

  • Kim, Hyun-Min;Kim, Hyun-Min;Lee, Min-Jung;Cho, Min-Gi;Kang, Deok;Kim, Yu-Kyung;Kim, Changmin;Kang, Do-Hyun;Jeong, Si-Hwa;Ahn, Ik-Gyun;Hwang, Jun-Hyeok;Kim, Jae-Hyun;Lee, Hyun-Jin;Jang, Jun-Yeong;Park, Ho-Jung;Kang, Sin woo;Youm, Jieun;Baek, Seung-won;Kim, Eu Jin;Shin, Moon-Kou;Park, Chan;Son, Chang-Bin;Yim, Tae-Bin;Lim, Jung Hyun;Hong, Sung-eun;Choi, Jun-Hyuk;Kim, Jun-Dong;Yoon, Dong-ju;Lee, Dong-Min;Yu, Soo-Min;Hong, Ye-Im;Lee, Yeong-Seok;Koo, Bon-Cheol;Park, Hyoung-Jun;Uem, Chae-Yoon;Kim, Min-Jeong;Oh, Jayoung;Park, NamGyeong;Kim, Eun-Jong;Cho, Whi-Sung;Lee, Ho-Sung;Kim, Tae-oh;Yoon, Cheol;Kwon, Sung-Keun;Jeong, Dong-Hyeon;Lee, Changwon;Yu, Sang-Yeol;Shon, Chae-won;Jeon, Gyu-Ri;Hong, Yang-Seok;Moon, Phil-Dong
    • CELLMED
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    • v.8 no.1
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    • pp.5.1-5.4
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    • 2018
  • Pharmacopuncture, or herbal acupuncture, is a new form of therapy derived from combinations of two traditional therapeutic methods, herbal medicine and acupuncture therapy. To compare the efficacy between loratadine-pharmacopuncture (LP) and loratadine-oral administration (LO), the effect of loratadine was investigated in murine models. Anti-anaphylactic effects of loratadine treatments were investigated in compound 48/80-induced systemic anaphylactic reaction and passive cutaneous anaphylaxis (PCA). LP treatment significantly inhibited the compound 48/80-induced systemic anaphylactic reaction and PCA. The effect between LP and LO were on a similar level. These results indicate that LP can be used as an alternative method for LO in case of emergency.

Interaction of Nonsedating Antihistamines with Cerebral Muscarinic Receptors (비수기성 항 Histamine제와 대뇌 Muscarine 수용체와의 상호작용)

  • 김영열;이정수;박인숙
    • YAKHAK HOEJI
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    • v.43 no.5
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    • pp.642-651
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    • 1999
  • Nonsedating antihistamines do net cause sedation in therapeutic doses because these drugs hardly cross the blood-brain barrier. Since most of the peripheral side dffects of conventional antihistamines are related to their muscarinic receptor blocking action, the present study was performed to investigate whether nonsedating antihistamines interact with the muscarinic receptors and discriminate the muscarinic receptor subtypes in the rat cerebral microsomal fraction which containes both $M_1,{\;}M_2,{\;}M_3{\;}and{\;}M_4$ receptors. Five nonsedating antihistamines at high concentrations inhibited [$^3H$]QNB binding to the muscarinic receptor in a dose-dependent manner. The inhibition curves of these drugs except loratadine which showed positive cooperativity (nH=1.55) were steep (nH=1), indicating interaction with a single homogenous population of the binding sites. Astemizole, clemizole and mequitazine increased the $K_D$ value for [$^3H$]QNB without affecting the binding site concentrations, and this increase in the $K_D$ value resulted from the ability of these drugs to slow [$^3H$]QNB-receptor association. The Ki values of astemizole, clemizole and mequitazine for the inhibition for the inhibition of [$^3H$]QNB binding to muscarinic receptor were 0.58, 5.99 and $0.007{\;}{\mu}M$, respectively. However, loratadine and terfenadine inhibited noncompetitively [$^3H$]QNB binding with the normalized $IC_50$ value of about $2{\;}{\mu}M$. These results demonstrate that; 1) astemizole, clemizole and mequitazine interact directly with the muscarinic receptor at high concentrations; 2) muscarinic receptor blocking potency of these drugs varies widely among drugs; 3) these drugs do not discriminate between muscarinic receptor subtypes.

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High-Performance Liquid Chromatographic-Tandem Mass Spectrometric Determination of Itraconazole in Human Plasma for Bioavailability and Bioequivalence Studies

  • Choi, Young-Wook;Nam, Dae-young;Kang, Kyoung-Hoon;Ha, Kyung-Wook;Han, In-Hee;Chang, Byung-Kon;Yoon, Mi-kyeong;Lee, Jae-hwi
    • Bulletin of the Korean Chemical Society
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    • v.27 no.2
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    • pp.291-294
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    • 2006
  • A highly sensitive high-performance liquid chromatographic-tandem mass spectrometric method (HPLC-MSMS) has been developed to quantify itraconazole in human plasma for the purpose of pharmacokinetic studies. Sample preparation was carried out by liquid-liquid extraction using loratadine as an internal standard. Chromatographic separation used a YMC $C_{18}$ column, giving an extremely fast total run time of 3 min. The method was validated and used for the bioequivalence study of itraconazole tablets in healthy male volunteers (n = 31). The lower limit of detection proved to be 0.2 ng /mL for itraconazole.