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DƯỢC LÍ Goodman & Gilman's The Pharmacological Basis of Therapeutics 12th, 2010

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Table 25–5

Inhibitors of Na + -Cl – Symport (Thiazide and Thiazide-like Diuretics)

RELATIVE ORAL t 1/2

ROUTE OF

DRUG STRUCTURE POTENCY AVAILABILITY (HOURS) ELIMINATION

Bendroflumethiazide 10 ~100% 3–3.9 ~30% R,

(NATURETIN)

R 2 3 CH 2 , R 6 CF 3

~70% M

Chlorothiazide 0.1 9–56% (dose- ~1.5 R

(DIURIL) (Unsaturated between C3 and N4) dependent)

Hydrochlorothiazide 1 ~70% ~2.5 R

(HYDRODIURIL)

Hydroflumethiazide 1 ~50% ~17 40-80% R,

(SALURON)

20-60% M

Methyclothiazide 10 ID ID M

(ENDURON)

Polythiazide R 2 CH 3 , R 3 CH 2 SCH 2 CF 3 , R 6 Cl 25 ~100% ~25 ~25% R,

(RENESE)

~75% U

Trichlormethiazide 25 ID 2.3-7.3 R

(NAQUA)

Chlorthalidone OH

1 ~65% ~47 ~65% R,

SO

(HYGROTON) 2 NH 2

~10% B,

NH

CI

~25% U

O

Indapamide (LOZOL) H 3 C

20 ~93% ~14 M

CI

C

N

N

H 2 NO 2 S

O

H

Metolazone H

10 ~65% ID ~80% R,

(MYKROX, CH 3

~10% B,

CI N

ZAROXOLYN)

H

~10% M

H 2 NO 2 S

N

O

H 3 C

Quinethazone H

1 ID ID ID

(HYDROMOX)

CI N CH 2 CH 3

H 2 NO 2 S

O

NH

Abbreviations: R, renal excretion of intact drug; M, metabolism; B, excretion of intact drug into bile; U, unknown pathway of elimination; ID,

insufficient data.

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