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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/02/25 05:24:40」(JST)

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Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. It is used as a fixed-dose combination with another protease inhibitor, ritonavir, under the trade names Kaletra (high-income countries) and Aluvia (low-income countries).

Pharmacology

Lopinavir is highly bound to plasma proteins (98–99%).^[1]

There are contradictory reports regarding lopinavir penetration into the cerebrospinal fluid (CSF). Anecdotal reports state that lopinavir cannot be detected in the CSF; however, a study of paired CSF-plasma samples from 26 patients receiving lopinavir/ritonavir found lopinavir CSF levels above the IC₅₀ in 77% of samples.^[2]

Clinical properties

Side effects, interactions and contraindications have only be evaluated in the drug combination lopinavir/ritonavir.

References

^ KALETRA (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009
^ Capparelli E, Holland D, Okamoto C, et al. (2005). "Lopinavir concentrations in cerebrospinal fluid exceed the 50% inhibitory concentration for HIV". AIDS (London, England) 19 (9).

External links

Abbott: Kaletra (lopinavir/ritonavir) tablets

UpToDate Contents

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1. HIVプロテアーゼ阻害剤 hiv protease inhibitors
2. HIV抗レトロウイルス療法に関する臨床試験：ブーストしたプロテアーゼ阻害剤の単剤療法試験 clinical trials of hiv antiretroviral therapy boosted protease inhibitor monotherapy studies
3. HIV-2感染の治療 treatment of hiv 2 infection
4. HIV抗レトロウイルス療法に関する臨床試験：プロテアーゼ阻害剤 clinical trials of hiv antiretroviral therapy protease inhibitors
5. 未治療HIV感染患者のための抗レトロウイルス療法の選択 selecting antiretroviral regimens for the treatment naive hiv infected patient

English Journal

The Lipid-Lowering Effect of Tenofovir/Emtricitabine: A Randomized, Crossover, Double-Blind, Placebo-Controlled Trial.

Santos JR1, Saumoy M2, Curran A3, Bravo I4, Llibre JM1, Navarro J3, Estany C4, Podzamczer D2, Ribera E3, Negredo E5, Clotet B6, Paredes R6; Tenofovir/emtricitabine inflUence on LIPid metabolism (TULIP) Study Group.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America.Clin Infect Dis.2015 Aug 1;61(3):403-8. doi: 10.1093/cid/civ296. Epub 2015 Apr 13.
BACKGROUND: It is unknown if tenofovir disoproxil fumarate (TDF), which is often coformulated with the lipid-neutral emtricitabine (FTC), has a lipid-lowering effect.METHODS: We performed a randomized, crossover, double-blind, placebo-controlled clinical trial on human immunodeficiency virus type 1
PMID 25870325

Antiretroviral Drugs in Meconium: Detection for Different Gestational Periods of Exposure.

Himes SK1, Tassiopoulos K2, Yogev R3, Huestis MA4; Pediatric HIV/AIDS Cohort Study (PHACS).
The Journal of pediatrics.J Pediatr.2015 Aug;167(2):305-311.e3. doi: 10.1016/j.jpeds.2015.04.062. Epub 2015 May 19.
OBJECTIVES: To determine whether antiretroviral (ARV) medications can be detected in meconium from second or third trimester, labor and delivery (L&D), or postnatal exposures.STUDY DESIGN: Twenty ARV medications were quantified by liquid chromatography-tandem mass spectrometry in 598 meconium sa
PMID 26001315

Thermodynamics of Highly Supersaturated Aqueous Solutions of Poorly Water-Soluble Drugs-Impact of a Second Drug on the Solution Phase Behavior and Implications for Combination Products.

Trasi NS1, Taylor LS1.
Journal of pharmaceutical sciences.J Pharm Sci.2015 Aug;104(8):2583-93. doi: 10.1002/jps.24528. Epub 2015 Jun 8.
There is increasing interest in formulating combination products that contain two or more drugs. Furthermore, it is also common for different drug products to be taken simultaneously. This raises the possibility of interactions between different drugs that may impact formulation performance. For poo
PMID 26059413

Japanese Journal

症例報告妊婦のHIV関連血小板減少症に対してHAART療法が奏功した1例

澁谷剛志,松田秀雄,川嶋章弘 [他]
関東連合産科婦人科学会誌 49(1), 63-66, 2012-00-00
NAID 40019294203

Evidence for Time-Dependent Interactions between Ritonavir and Lopinavir/Ritonavir Plasma Levels Following P-Glycoprotein Inhibition in Sprague-Dawley Rats

Plooy Michael du,Viljoen Michelle,Rheeders Malie
Biological and Pharmaceutical Bulletin 34(1), 66-70, 2011
… The interaction between verapamil, a P-glycoprotein (P-gp) inhibitor, with ritonavir and lopinavir/ritonavir (LPV/r) after acute and chronic treatment was investigated in rats. … Lopinavir and ritonavir plasma levels were simultaneous determined by a validated LC/MS/MS method. … The lower limit of quantification for both ritonavir and lopinavir was 0.078 μg/ml. … During acute (but not chronic) LPV/r treatment, verapamil also increased the lopinavir levels (p<0.05). …
NAID 130000402264

High Performance Liquid Chromatography Using UV Detection for the Simultaneous Quantification of the New Non-nucleoside Reverse Transcriptase Inhibitor Etravirine (TMC-125), and 4 Protease Inhibitors in Human Plasma

Hirano Atsushi,Takahashi Masaaki,Kinoshita Eri [他],Shibata Masaaki,Nomura Toshiharu,Yokomaku Yoshiyuki,Hamaguchi Motohiro,Sugiura Wataru
Biological and Pharmaceutical Bulletin 33(8), 1426-1429, 2010
… Here we describe the application of HPLC with UV detection for the simulataneous assay of ETV and 4 PIs, darunavir (DRV), atazanavir (ATV), ritonavir (RTV) and lopinavir (LPV). …
NAID 130000300371

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Lopinavir
Systematic (IUPAC) name
	(2S)-N-[(2S,4S,5S)-5-[2-(2,6-dimethylphenoxy)acetamido]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide
Clinical data
AHFS/Drugs.com	International Drug Names
MedlinePlus	a602015
Pregnancy cat.	C (US)
Legal status	POM (UK) ℞-only (US)
Routes	Oral
Pharmacokinetic data
Bioavailability	Unknown
Protein binding	98-99%
Metabolism	Hepatic
Half-life	5 to 6 hours
Excretion	Mostly fecal
Identifiers
CAS number	192725-17-0
ATC code	J05AR10 (with ritonavir)
PubChem	CID 92727
DrugBank	DB01601
ChemSpider	83706
UNII	2494G1JF75
KEGG	D01425
ChEMBL	CHEMBL729
Chemical data
Formula	C37H48N4O5
Mol. mass	628.810 g/mol
	SMILES O=C(N[C@@H](Cc1ccccc1)[C@@H](O)C[C@@H](NC(=O)[C@@H](N2C(=O)NCCC2)C(C)C)Cc3ccccc3)COc4c(cccc4C)C;
	InChI InChI=1S/C37H48N4O5/c1-25(2)34(41-20-12-19-38-37(41)45)36(44)39-30(21-28-15-7-5-8-16-28)23-32(42)31(22-29-17-9-6-10-18-29)40-33(43)24-46-35-26(3)13-11-14-27(35)4/h5-11,13-18,25,30-32,34,42H,12,19-24H2,1-4H3,(H,38,45)(H,39,44)(H,40,43)/t30-,31-,32-,34-/m0/s1 ; Key:KJHKTHWMRKYKJE-SUGCFTRWSA-N ;
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英: lopinavir
商: カレトラ

[PInfo-1] KALETRA (lopinavir/ritonavir) capsules; (lopinavir/ritonavir) oral solution. Prescribing information. April 2009

[2] Capparelli E, Holland D, Okamoto C, et al. (2005). "Lopinavir concentrations in cerebrospinal fluid exceed the 50% inhibitory concentration for HIV". AIDS (London, England) 19 (9).

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lopinavir