Pentamidine Inhalation

Generic name: pentamidine isethionate
Dosage form: inhalant
Drug classes:Inhaled anti-infectives, Miscellaneous antibiotics

Medically reviewed by Drugs.com. Last updated on Sep 21, 2021.

Pentamidine Inhalation Description

Pentamidine Isethionate, an antifungal agent, is a nonpyrogenic lyophilized product. After reconstitution with Sterile Water for Injection, USP, Pentamidine Isethionate is administered by inhalation via the Respirgard® II nebulizer [Marquest, Englewood, CO] (see DOSAGE AND ADMINISTRATION). Pentamidine isethionate, 4,4’-[1,5-pentane-diylbis(oxy)]bis-benzenecarboximidamid, is a white crystalline powder soluble in water and glycerin and insoluble in ether, acetone, and chloroform.

Each vial contains 300 mg pentamidine isethionate.

Pentamidine Inhalation - Clinical Pharmacology

Microbiology

Studies suggest that the pentamidine isethionate interferes with microbial nuclear metabolism by inhibition of DNA, RNA, phospholipid and protein synthesis. However, the mode of action is not fully understood.

Activity in vitro and in vivo

Pentamidine isethionate, an aromatic diamidine, is known to have activity against Pneumocystis jiroveci.

In 5 AIDS patients with suspected Pneumocystis jiroveci pneumonia (PJP), the mean concentrations of pentamidine determined 18 to 24 hours after inhalation therapy were 23.2 ng/mL (range 5.1 to 43.0 ng/mL) in bronchoalveolar lavage fluid and 705 ng/mL (range 140 to 1336 ng/mL) in sediment after administration of a 300 mg single dose via the Respirgard® II nebulizer. In 3 AIDS patients with suspected PJP, the mean concentrations of pentamidine determined 18 to 24 hours after a 4 mg/kg intravenous dose were 2.6 ng/mL (range 1.5 to 4.0 ng/mL) in bronchoalveolar lavage fluid and 9.3 ng/mL (range 6.9 to 12.8 ng/mL) in sediment. In the patients who received aerosolized pentamidine, the peak plasma levels of pentamidine were at or below the lower limit of detection of the assay (...