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:

Macleods Pharmaceuticals Limited

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 to off white, round, biconvex, film-coated tablets debossed with  'CL60' on one side and plain on other side) and tolterodine tartrate tablets 2 mg (white to off white, round, biconvex, film-coated tablets debossed with  'CL61' on one side and plain on other side) are supplied as follows: Bottles of 60    1mg    NDC 33342-097-09    2mg    NDC 33342-098-09 Bottles of 500   1mg    NDC  33342-097-15   2mg    NDC 33342-098-15 Unit Dose Pack of  100  1mg        NDC 33342-097-12  2 mg       NDC 33342-098-12 Store at 20º to 25ºC (68º to 77ºF); excursions permitted to 15º to 30ºC (59º to 86ºF) [see USP Controlled Room Temperature]. All other trademarks are properties of their respective owners.   Manufactured for : Macleods Pharma USA, Inc. Princeton, NJ 08540 Manufactured by : Macleods Pharmaceuticals Ltd. Baddi, Himachal Pradesh, INDIA Revised: November 2022

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

TOLTERODINE TARTRATE - TOLTERODINE TARTRATE TABLET, FILM COATED
MACLEODS PHARMACEUTICALS LIMITED
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TOLTERODINE TARTRATE TABLETS
DESCRIPTION
Tolterodine tartrate tablets contain tolterodine tartrate, USP. 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 molecular 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, USP 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 silicon dioxide,
dibasic calcium phosphate
anhydrous, 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.
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37
7
Tolterodine has a pronounced effect on