Tìm theo
Methyclothiazide
Các tên gọi khác (1) :
  • Enduron
sodium chloride symporter inhibitors
Thuốc Gốc
Small Molecule
CAS: 135-07-9
ATC: C03AA08
ĐG : Ivax Pharmaceuticals
CTHH: C9H11Cl2N3O4S2
PTK: 360.237
A thiazide diuretic with properties similar to those of hydrochlorothiazide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H11Cl2N3O4S2
Phân tử khối
360.237
Monoisotopic mass
358.956802649
InChI
InChI=1S/C9H11Cl2N3O4S2/c1-14-9(4-10)13-6-2-5(11)7(19(12,15)16)3-8(6)20(14,17)18/h2-3,9,13H,4H2,1H3,(H2,12,15,16)
InChI Key
InChIKey=CESYKOGBSMNBPD-UHFFFAOYSA-N
IUPAC Name
6-chloro-3-(chloromethyl)-2-methyl-1,1-dioxo-3,4-dihydro-2H-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
Traditional IUPAC Name
6-chloro-3-(chloromethyl)-2-methyl-1,1-dioxo-3,4-dihydro-1$l^{6},2,4-benzothiadiazine-7-sulfonamide
SMILES
CN1C(CCl)NC2=CC(Cl)=C(C=C2S1(=O)=O)S(N)(=O)=O
Độ tan chảy
225 °C
Độ hòa tan
11.2 mg/L
logP
1.42
logS
-2.6
pKa (strongest acidic)
9.29
pKa (Strongest Basic)
-3.4
PSA
109.57 Å2
Refractivity
77.28 m3·mol-1
Polarizability
31.65 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
9.4
Dược Lực Học : Methyclothiazide, a diuretic-antihypertensive agent, is a member of the benzothiadiazine (thiazide) class of drugs. Methyclothiazide has a per mg natriuretic activity approximately 100 times that of the prototype thiazide, chlorothiazide. At maximal therapeutic dosages, all thiazides are approximately equal in their diuretic/natriuretic effects. Like other benzothiadiazines, methyclothiazide also has antihypertensive properties, and may be used for this purpose either alone or to enhance the antihypertensive action of other drugs.
Cơ Chế Tác Dụng : A thiazide diuretic with properties similar to those of hydrochlorothiazide. (From Martindale, The Extra Pharmacopoeia, 30th ed, p825) Methyclothiazide appears to block the active reabsorption of chloride and possibly sodium in the ascending loop of Henle, altering electrolyte transfer in the proximal tubule. This results in excretion of sodium, chloride, and water and, hence, diuresis. As a diuretic, methyclothiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like methyclothiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of methyclothiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle.
Dược Động Học :
▧ Absorption :
Rapidly absorbed following oral administration.
Độc Tính : Acute oral toxicity (LD50): >4000 mg/kg [Rat]. Symptoms of overdosage include electrolyte imbalance and signs of potassium deficiency such as confusion, dizziness, muscular weakness, and gastrointestinal disturbances.
Chỉ Định : For use in the management of hypertension either as the sole therapeutic agent or to enhance the effect of other antihypertensive drugs in the more severe forms of hypertension. Also used as adjunctive therapy in edema associated with congestive heart failure, hepatic cirrhosis, and corticosteroid and estrogen therapy.
Tương Tác Thuốc :
  • Digoxin Possible electrolyte variations and arrhythmias
  • Lithium The thiazide diuretic, methyclothiazide, may increase serum levels of lithium.
  • Trandolapril The thiazide diuretic, Methyclothiazide, may increase the hypotensive effect of Trandolapril. Methyclothiazide may also increase the nephrotoxicity of Trandolapril. Monitor for postural hypotension at initiation of concomitant therapy and renal dysfunction during chronic therapy.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aquatensen
  • Công ty :
    Sản phẩm biệt dược : Duretic
  • Công ty :
    Sản phẩm biệt dược : Enduron
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00232
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4121
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509197
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07765
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00656
ChemSpider
http://www.chemspider.com/Chemical-Structure.3978.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-0160-01
PharmGKB
http://www.pharmgkb.org/drug/PA164748094
RxList
http://www.rxlist.com/cgi/generic3/methyclothiazide.htm
Drugs.com
http://www.drugs.com/cdi/methyclothiazide.html
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