URSODIOL capsule

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

URSODIOL (UNII: 724L30Y2QR) (URSODIOL - UNII:724L30Y2QR)

Available from:

Actavis Pharma, Inc.

INN (International Name):

URSODIOL

Composition:

URSODIOL 300 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

- Ursodiol is indicated for patients with radiolucent, noncalcified gallbladder stones < 20 mm in greatest diameter in whom elective cholecystectomy would be undertaken except for the presence of increased surgical risk due to systemic disease, advanced age, idiosyncratic reaction to general anesthesia, or for those patients who refuse surgery. Safety of use of ursodiol beyond 24 months is not established. - Ursodiol is indicated for the prevention of gallstone formation in obese patients experiencing rapid weight loss. - Ursodiol will not dissolve calcified cholesterol stones, radiopaque stones, or radiolucent bile pigment stones. Hence, patients with such stones are not candidates for ursodiol therapy. - Patients with compelling reasons for cholecystectomy including unremitting acute cholecystitis, cholangitis, biliary obstruction, gallstone pancreatitis, or biliary-gastrointestinal fistula are not candidates for ursodiol therapy. - Allergy to bile acids.

Product summary:

Ursodiol Capsules USP, 300 mg are opaque white capsules imprinted WATSON on one half and 3159 on the other half of the capsule in black. Bottles of 100 (NDC 0591-3159-01) are supplied with child-resistant closures. Store at 20°C to 25°C (68°F to 77°F). [See USP controlled room temperature.] Dispense in a tight container (USP). Keep out of reach of children. Rx only Manufactured for: Teva Pharmaceuticals  Parsippany, NJ 07054 © 2023 Teva Pharmaceuticals, Inc. URS-001 Rev. 7/2023

Authorization status:

New Drug Application Authorized Generic

Summary of Product characteristics

URSODIOL- URSODIOL CAPSULE
ACTAVIS PHARMA, INC.
----------
URSODIOL CAPSULES USP
RX ONLY
PRESCRIBING INFORMATION
SPECIAL NOTE
GALLBLADDER STONE DISSOLUTION WITH URSODIOL TREATMENT REQUIRES MONTHS
OF
THERAPY. COMPLETE DISSOLUTION DOES NOT OCCUR IN ALL PATIENTS AND
RECURRENCE
OF STONES WITHIN 5 YEARS HAS BEEN OBSERVED IN UP TO 50% OF PATIENTS
WHO DO
DISSOLVE THEIR STONES ON BILE ACID THERAPY. PATIENTS SHOULD BE
CAREFULLY
SELECTED FOR THERAPY WITH URSODIOL, AND ALTERNATIVE THERAPIES SHOULD
BE
CONSIDERED.
DESCRIPTION
Ursodiol is a bile acid available as 300 mg capsules suitable for oral
administration.
Ursodiol USP (ursodeoxycholic acid) is a naturally occurring bile acid
found in small
quantities in normal human bile and in the biles of certain other
mammals. It is a bitter-
tasting, white powder freely soluble in ethanol, methanol, and glacial
acetic acid;
sparingly soluble in chloroform; slightly soluble in ether; and
insoluble in water. The
chemical name for ursodiol is 3α,7β-Dihydroxy-5β-cholan-24-oic acid
(C
H
O ).
Ursodiol, USP has a molecular weight of 392.57. Its structure is shown
below:
_Inactive Ingredients: _Colloidal silicon dioxide, magnesium stearate,
and starch (corn).
Gelatin capsules contain gelatin and titanium dioxide. The capsules
are printed with edible
ink containing black iron oxide.
CLINICAL PHARMACOLOGY
About 90% of a therapeutic dose of ursodiol is absorbed in the small
bowel after oral
24
40
4
administration. After absorption, ursodiol enters the portal vein and
undergoes efficient
extraction from portal blood by the liver (i.e., there is a large
“first-pass” effect) where it
is conjugated with either glycine or taurine and is then secreted into
the hepatic bile
ducts. Ursodiol in bile is concentrated in the gallbladder and
expelled into the duodenum
in gallbladder bile via the cystic and common ducts by gallbladder
contractions provoked
by physiologic responses to eating. Only small quantities of ursodiol
appear in the
systemic circulation and very small amounts are excreted into