TOLTERODINE TARTRATE tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

TOLTERODINE TARTRATE (UNII: 5T619TQR3R) (TOLTERODINE - UNII:WHE7A56U7K)

Available from:

Greenstone LLC

INN (International Name):

TOLTERODINE TARTRATE

Composition:

TOLTERODINE TARTRATE 1 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Tolterodine tartrate tablets are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Tolterodine tartrate tablets are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. Tolterodine tartrate is also contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients, or to fesoterodine fumarate extended-release tablets which, like tolterodine tartrate, are metabolized to 5-hydroxymethyl tolterodine.

Product summary:

Tolterodine tartrate tablets 1 mg (white, round, biconvex, film-coated tablets engraved with arcs above and below the letters "TO") and tolterodine tartrate tablets 2 mg (white, round, biconvex, film-coated tablets engraved with arcs above and below the letters "DT") are supplied as follows: Bottles of 60 1 mg NDC 59762-0170-6 2 mg NDC 59762-0800-2 Bottles of 500 1 mg NDC 59762-0170-1 2 mg NDC 59762-0800-6 Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F) [see USP Controlled Room Temperature].

Authorization status:

New Drug Application Authorized Generic

Summary of Product characteristics

TOLTERODINE TARTRATE- TOLTERODINE TARTRATE TABLET, FILM COATED
GREENSTONE LLC
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TOLTERODINE TARTRATE TABLETS
DESCRIPTION
Tolterodine tartrate tablets contain tolterodine tartrate. The active
moiety, tolterodine, is a muscarinic
receptor antagonist. The chemical name of tolterodine tartrate is
(R)-2-[3-[bis(1-methylethyl)-amino]1-
phenylpropyl]-4-methylphenol [R-(R*,R*)]-2,3dihydroxybutanedioate
(1:1) (salt). The empirical
formula of tolterodine tartrate is C
H NO , and its molecular weight is 475.6. The structural formula
of tolterodine tartrate is represented below:
Tolterodine tartrate is a white, crystalline powder. The pKa value is
9.87 and the solubility in water is
12 mg/mL. It is soluble in methanol, slightly soluble in ethanol, and
practically insoluble in toluene. The
partition coefficient (Log D) between n-octanol and water is 1.83 at
pH 7.3.
Tolterodine tartrate tablets for oral administration contain 1 or 2 mg
of tolterodine tartrate. The inactive
ingredients are colloidal anhydrous silica, calcium hydrogen phosphate
dihydrate, cellulose
microcrystalline, hypromellose, magnesium stearate, sodium starch
glycolate (pH 3.0 to 5.0), stearic
acid, and titanium dioxide.
CLINICAL PHARMACOLOGY
Tolterodine is a competitive muscarinic receptor antagonist. Both
urinary bladder contraction and
salivation are mediated via cholinergic muscarinic receptors.
After oral administration, tolterodine is metabolized in the liver,
resulting in the formation of the 5-
hydroxymethyl derivative, a major pharmacologically active metabolite.
The 5-hydroxymethyl
metabolite, which exhibits an antimuscarinic activity similar to that
of tolterodine, contributes
significantly to the therapeutic effect. Both tolterodine and the
5-hydroxymethyl metabolite exhibit a
high specificity for muscarinic receptors, since both show negligible
activity or affinity for other
neurotransmitter receptors and other potential cellular targets, such
as calcium channels.
Tolterodine has a pronounced effect on bladder function. Effects on
urody