Drug intelligence / Profile preview

nitrofurantoin monohydrate + nitrofurantoin macrocrystalline

Development stage
Unknown
Lead developer
Procter & Gamble
Modality
Small Molecules
Administration
Oral
01

Overview

**Nitrofurantoin monohydrate + nitrofurantoin macrocrystalline** is a combination antibacterial agent formulated as a hard gelatin capsule containing both nitrofurantoin monohydrate and nitrofurantoin macrocrystals. It is marketed under the brand name Macrobid and is specifically indicated for the treatment of acute uncomplicated urinary tract infections (UTIs), such as cystitis, caused by susceptible bacteria[4][7][11][14]. Mechanistically, nitrofurantoin is converted by bacterial nitroreductases to reactive intermediates that inhibit essential bacterial processes, including the synthesis of DNA, RNA, proteins, and cell walls, and disrupt bacterial metabolism[1][6][9][11]. The formulation’s unique combination allows extended and controlled release, with 75% as nitrofurantoin monohydrate (forming a gel matrix for prolonged release) and 25% as macrocrystalline nitrofurantoin (allowing slower absorption for improved gastrointestinal tolerance)[7][11]. It is not effective for upper urinary tract infections (e.g. pyelonephritis) and achieves therapeutic concentrations mainly in the urine[8][14]. Nitrofurantoin has been available since 1953 in various formulations; the combination improves dosing convenience and side effect profile compared to older forms[11].

Brand names
Macrobid
Other names
nitrofurantoin monohydrate/macrocrystalsnitrofurantoin monohydrate + nitrofurantoin macrocrystals
02

Targets

NTR (Bacterial nitroreductase)

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