Tìm theo
Mefloquine
Các tên gọi khác (7 ) :
  • [(R*,S*)-2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol
  • alpha-2-Piperidinyl-2,8-bis(trifluoromethyl)-4-quinolinemethanol
  • Mefloquin
  • Mefloquina
  • Méfloquine
  • Mefloquine
  • Mefloquinum
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 53230-10-7
ATC: P01BC02
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C17H16F6N2O
PTK: 378.3122
A phospholipid-interacting antimalarial drug (antimalarials). It is very effective against plasmodium falciparum with very few side effects. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H16F6N2O
Phân tử khối
378.3122
Monoisotopic mass
378.116682374
InChI
InChI=1S/C17H16F6N2O/c18-16(19,20)11-5-3-4-9-10(15(26)12-6-1-2-7-24-12)8-13(17(21,22)23)25-14(9)11/h3-5,8,12,15,24,26H,1-2,6-7H2
InChI Key
InChIKey=XEEQGYMUWCZPDN-UHFFFAOYSA-N
IUPAC Name
[2,8-bis(trifluoromethyl)quinolin-4-yl](piperidin-2-yl)methanol
Traditional IUPAC Name
mefloquine
SMILES
OC(C1CCCCN1)C1=CC(=NC2=C1C=CC=C2C(F)(F)F)C(F)(F)F
Độ hòa tan
5000 mg/L (HCl salt)
logP
3.9
logS
-4
pKa (strongest acidic)
13.79
pKa (Strongest Basic)
9.46
PSA
45.15 Å2
Refractivity
82.58 m3·mol-1
Polarizability
31.73 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Mefloquine is an antimalarial agent which acts as a blood schizonticide. Mefloquine is active against the erythrocytic stages of Plasmodium species. However, the drug has no effect against the exoerythrocytic (hepatic) stages of the parasite. Mefloquine is effective against malaria parasites resistant to chloroquine. Mefloquine is a chiral molecule. According to some research, the (+) enantiomer is more effective in treating malaria, and the (-) enantiomer specifically binds to adenosine receptors in the central nervous system, which may explain some of its psychotropic effects.
Cơ Chế Tác Dụng : A phospholipid-interacting antimalarial drug (antimalarials). It is very effective against plasmodium falciparum with very few side effects. [PubChem] Mefloquine has been found to produce swelling of the Plasmodium falciparum food vacuoles. It may act by forming toxic complexes with free heme that damage membranes and interact with other plasmodial components.
Dược Động Học :
▧ Absorption :
Well absorbed from the gastrointestinal tract. The presence of food significantly enhances the rate and extent of absorption.
▧ Volume of Distribution :
* 20 L/kg [healthy adults]
▧ Protein binding :
98%
▧ Metabolism :
Hepatic. Two metabolites have been identified in humans. The main metabolite, 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, is inactive against Plasmodium falciparum. The second metabolite, an alcohol, is present in minute quantities.
▧ Route of Elimination :
There is evidence that mefloquine is excreted mainly in the bile and feces. Urinary excretion of unchanged mefloquine and its main metabolite under steady-state condition accounted for about 9% and 4% of the dose, respectively.
▧ Half Life :
2 to 4 weeks
▧ Clearance :
* 30 mL/min
Độc Tính : Oral, rat: LD50 = 880 mg/kg. Symptoms of overdose include nausea, vomiting, and weight loss.
Chỉ Định : For the treatment of mild to moderate acute malaria caused by Mefloquineuine-susceptible strains of Plasmodium falciparum (both chloroquine-susceptible and resistant strains) or by Plasmodium vivax. Also for the prophylaxis of Plasmodium falciparum and Plasmodium vivax malaria infections, including prophylaxis of chloroquine-resistant strains of Plasmodium falciparum.
Tương Tác Thuốc :
  • Acenocoumarol Mefloquine may increase the anticoagulant effect of acenocoumarol.
  • Anisindione Mefloquine may increase the anticoagulant effect of anisindione.
  • Artemether Mefloquine may increase the adverse effects of artemether. Combination therapy is contraindicated unless there are no other treatment options.
  • Dicoumarol Mefloquine may increase the anticoagulant effect of dicumarol.
  • Halofantrine Increased risk of cardiac toxicity
  • Lumefantrine Mefloquine may increase the adverse effects of lumefantrine. Combination therapy is contraindicated unless there are no other treatment options.
  • Rifampicin Rifampin lowers mefloquine levels
  • Ritonavir Mefloquine decreases the effect of ritonavir
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Telithromycin Telithromycin may reduce clearance of Mefloquine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Mefloquine if Telithromycin is initiated, discontinued or dose changed.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Tiagabine Mefloquine increases the risk of seizure and is contraindicated in persons with a history of convulsions. Possible reduction in the therapeutic effect of Tiagabine when used for other indications may also occur.
  • Topotecan The p-glycoprotein inhibitor, Mefloquine, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Vigabatrin Mefloquine may decrease the serum concentration of Vigabatrin. This may increase the risk of seizure in patients receiving Vigabatrin to prevent seizures. Consider alternate therapy or monitor for changes in Vigabatrin serum concentration, therapeutic or adverse effects if Mefloquin is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of mefloquine by decreasing its metabolism. Additive QTc prolongation may also occur. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of mefloquine if voriconazole is initiated, discontinued or dose changed.
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Warfarin Mefloquine may increase the anticoagulant effect of warfarin.
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy should be avoided.
  • Zonisamide Mefloquine may decrease the serum concentration and therapeutic effect of zonisamide. Concomitant therapy is contraindicated in patients with history of convulsions.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Unifarm
    Sản phẩm biệt dược : Eloquine
  • Công ty : Zydus Cadila
    Sản phẩm biệt dược : Facital
  • Công ty : Cadila HC
    Sản phẩm biệt dược : Falcital
  • Sản phẩm biệt dược : Lariam
  • Công ty : Ipca
    Sản phẩm biệt dược : Larimef
  • Công ty : Alkem
    Sản phẩm biệt dược : Mefax
  • Công ty : Cipla Medpro
    Sản phẩm biệt dược : Mefliam
  • Công ty : ACI
    Sản phẩm biệt dược : Meflon
  • Công ty : AC Farma
    Sản phẩm biệt dược : Mefloquina
  • Công ty : Emcure
    Sản phẩm biệt dược : Mefloquine
  • Công ty : Zydus Cadila
    Sản phẩm biệt dược : Mefque
  • Sản phẩm biệt dược : Mephaquin
  • Công ty : Mepha
    Sản phẩm biệt dược : Mephaquin Lactab
  • Công ty : Atlantic
    Sản phẩm biệt dược : Mequin
  • Công ty : Sun
    Sản phẩm biệt dược : Mqf
  • Công ty : Newai Chem
    Sản phẩm biệt dược : Suton
  • Công ty : Investi
    Sản phẩm biệt dược : Tropicur
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00358
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4046
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505610
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07633
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D04895
ChemSpider
http://www.chemspider.com/Chemical-Structure.3906.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50022889
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/54868-5434-0
PharmGKB
http://www.pharmgkb.org/drug/PA450348
Wikipedia
http://en.wikipedia.org/wiki/Mefloquine
RxList
http://www.rxlist.com/cgi/generic2/mefloq.htm
Drugs.com
http://www.drugs.com/cdi/mefloquine.html
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