Страна: Соединенные Штаты
Язык: английский
Источник: NLM (National Library of Medicine)
TOLTERODINE TARTRATE (UNII: 5T619TQR3R) (TOLTERODINE - UNII:WHE7A56U7K)
Proficient Rx LP
ORAL
PRESCRIPTION DRUG
Tolterodine tablets are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Tolterodine tablets are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. Tolterodine tablets are also contraindicated in patients who have demonstrated hypersensitivity to the drug or its ingredients, or to fesoterodine fumarate extended-release tablets which, like tolterodine tablets, are metabolized to 5-hydroxymethyl tolterodine.
Tolterodine Tartrate Tablets, 1 mg, are available as white, round, unscored, biconvex, film-coated tablets, debossed with “93” on one side and “0010” on the other side containing 1 mg tolterodine tartrate, packaged in bottles of 30 (NDC 71205-319-30), 60 (NDC 71205-319-60) and 90 (NDC 71205-319-90) tablets. PHARMACIST: Dispense in a tight container as defined in the USP, with a child-resistant closure (as required). Store at 20º to 25ºC (68º to 77ºF) [See USP Controlled Room Temperature]. KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN. Manufactured In India By: Cipla Ltd. Goa, India Manufactured For: TEVA PHARMACEUTICALS USA, INC. North Wales, PA 19454 Rev. D 4/2015
Abbreviated New Drug Application
TOLTERODINE TARTRATE- TOLTERODINE TARTRATE TABLET, FILM COATED PROFICIENT RX LP ---------- TOLTERODINE TARTRATE TABLETS DESCRIPTION This product contains 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). It has the following structural formula: C H NO M.W. 475.6 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. Each tolterodine tartrate tablet, for oral administration, contains 1 mg or 2 mg of tolterodine tartrate. In addition, each tablet contains the following inactive ingredients: corn starch, croscarmellose sodium, hypromellose, lactose monohydrate, microcrystalline cellulose, polyethylene glycol, sodium stearyl fumarate, 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 urodynamic parameters before and 1 and 5 hours after a single 6.4 mg dose of tolterodine immediate-release w Прочитать полный документ