Diuretics

Stacy Elder Dalpoas, PharmD, BCPS, Lipika Samal, M.D., Paul A. Pham, Pharm.D.

INDICATIONS

FDA

Diuretic Class Review

Thiazide Diuretics

FDA Indication


Pharmacokinetics

Pregnancy Risk Rating/ Breastfeeding Risk

Cost and Formulation

Hydrochlorothiazide

Treatment of mild to moderate HTN; treatment of edema in heart failure and nephrotic syndrome

A: ~50-80%

M: minimal metabolism

E: Urine

t½ = 5.6-14.8 hrs

Rating B

Enters breast milk, avoid use in lactation

Generic available.

12.5 mg: $0.42

25mg: $0.08

50mg: $0.16

Chlorothiazide

Management of mild to moderate HTN; adjunct treatment for edema

A: poor.

M: saturable. Single dose 250 or 500 mg has similar systemic absorption

E: urine.

t½ = 1-2 hrs.

Rating C, but most experts do not recommend as it crosses placenta

Enters breast milk / use caution

Generic tablets available. Oral suspension still brand.

250 mg tab: $0.69

500 mg tab: $0.25

500 mg IV: $238

Metolazone

Management of mild-to-moderate hypertension; treatment of edema in heart failure and nephrotic syndrome, impaired renal function

A: 40-65%

M: minimal metabolism

E: urine.

t½ = 20 hrs

Rating B

Enters breast milk/ not recommended.

Generic available

2.5 mg: $2.07

5 mg: $2.35

10 mg: $2.82

Potassium-Sparing Diuretics

Spironolactone

Management of edema associated with excessive aldosterone excretion; hypertension; primary hyperaldosteronism; hypokalemia; cirrhosis of liver accompanied by edema or ascites; nephritic syndrome; severe heart failure (NYHA class III-IV) to increase survival and reduce hospitalization when added to standard therapy

A: 73%

M: hepatic, multiple metabolites

E: urine and feces

t½: 1.3-2 hrs. Active metaboliteâ??s t½ = 10-35 hrs.

Rating C (teratogenic in animal studies)

Enters breast milk

Generic available

25 mg: $0.45

50 mg: $0.82

Eplerenone

Hypertension, heart failure (NYHA II-IV)

A: 70%

M: Hepatic (Cyp3A4)

E: urine and feces

t½: 3-6 hr

Rating B

Unknown whether it enters breastmilk

25 mg: $4.30

50 mg: $4.30

Triamterene

Alone or in combination with other diuretics in treatment of edema and hypertension; decreases potassium excretion caused by kaliuretic diuretics

A: rapid

M: rapid metabolism

E: < 50% by urine, the rest by biliary/fecal

t½: 1-2 hrs

Rating C

No data available in breast-feeding

No generic available.

Brand: Dyrenium®

50 : $11.49

100 mg: $11.49

Loop Diuretics

Furosemide

Management of edema associated with heart failure and hepatic or renal disease; acute pulmonary edema; treatment of hypertension (alone or in combination with other antihypertensives)

A: erratic

M: minimally hepatic

E: urine, feces

t½: 0.5- 2 hrs

Pregnancy rating C, crosses placenta but has been used to treat heart failure in pregnancy

Enters breast-milk/use caution

10 mg/mL (60 mL): $10.40

20 mg: $0.14

40 mg: $0.16

80 mg: $0.43

Bumetanide

Management of edema secondary to heart failure or hepatic or renal disease including nephritic disease; may be used alone or in combination with antihypertensives for treatment of HTN; can be used in furosemide allergic patients.

A: 85-95% bioavailability

M: partially hepatic

E: urine

t½: 1-1.5 hrs

Pregnancy Rating C

Excretion in breast milk unknown; use caution

0.5 mg: $0.99

1 mg: $1.37

2 mg: $2.36

Torsemide

Hypertension; edema secondary to heart failure, cirrhosis, chronic renal failure

A: 80% bioavailability

M: Hepativ primarily via 2C9

E: urine, feces

t1/2: 3.5 hours

Pregnancy Rating B

5 mg: $0.63

10 mg: $0.70

20 mg: $0.82

100 mg: $3.04

**Patient Assistant Program:

https://www.rxhope.com/PAP/pdf/rx_outreach_0209.pdf

** Information gathered by Heather Tran and Gladimir Elysee

A = absorption; M = metabolism; E = excretion

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Last updated: August 2, 2017