Generic name: tolterodine
Brand names: Detrol, Detrol LA
Drug class: Urinary antispasmodics
What is Detrol?
Detrol is a prescription medicine for adults used to treat the following symptoms due to a condition called overactive bladder Urge urinary incontinence: a strong need to urinate with leaking or wetting accidents, Urgency: a strong need to urinate right away, Frequency: urinating often
DETROL LA Capsules contain tolterodine tartrate. The active moiety, tolterodine, is a muscarinic receptor antagonist. The chemical name of tolterodine tartrate is (R)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropanamine L-hydrogen tartrate. The empirical formula of tolterodine tartrate is C26H37NO7,. Its structure is:
Tolterodine tartrate is a white, crystalline powder with a molecular weight of 475.6. 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.
DETROL LA 4 mg capsule for oral administration contains 4 mg of tolterodine tartrate. Inactive ingredients are sucrose, starch, hypromellose, ethylcellulose, medium chain triglycerides, oleic acid, gelatin, and FD&C Blue #2.
DETROL LA 2 mg capsule for oral administration contains 2 mg of tolterodine tartrate, and the following inactive ingredients: sucrose, starch, hypromellose, ethylcellulose, medium chain triglycerides, oleic acid, gelatin, yellow iron oxide, and FD&C Blue #2.
Both the 2 mg and 4 mg capsule strengths are imprinted with a pharmaceutical grade printing ink that contains shellac glaze, titanium dioxide, propylene glycol, and simethicone.
Mechanism of Action
Tolterodine acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors. 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 5-hydroxymethyl tolterodine (5-HMT), the major pharmacologically active metabolite. 5-HMT, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect. Both tolterodine and 5-HMT 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.
Who should not take Detrol?
Do not take Detrol if you:
- Are not able to empty your bladder (urinary retention)
- Have delayed or slow emptying of your stomach (gastric retention)
- Have an eye problem called “uncontrolled narrow-angle glaucoma”
- Are allergic to Detrol or to any of its ingredients. See the end of this leaflet for a complete list of ingredients
- Are allergic to Toviaz which contains fesoterodine.
What should I tell my healthcare provider before taking Detrol?
Before starting Detrol, tell your doctor about all of your medical and other conditions that may affect the use of Detrol, including:
- Stomach or intestinal problems or problems with constipation
- Problems emptying your bladder or if you have a weak urine stream
- Treatment for an eye problem called narrow-angle glaucoma
- Liver problems
- Kidney problems
- A condition called myasthenia gravis
- If you or any family members have a rare heart condition called QT prolongation (long QT syndrome)
- If you are pregnant or trying to become pregnant. It is not known if Detrol could harm your unborn baby.
- If you are breastfeeding. It is not known if Detrol passes into your breast milk or if it can harm your baby. Talk to your doctor about the best way to feed your baby if you take Detrol.
Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Other medicines can affect how your body handles Detrol. Your doctor may use a lower dose of Detrol if you are taking:
- Certain medicines for fungus or yeast infections
- Certain medicines for bacterial infections
- Sandimmune (cyclosporine) or Velban (vinblastine)
Ask your doctor or pharmacist for a list of these medicines, if you are not sure.
Know the medicines you take. Keep a list of them with you to show your doctor or pharmacist each time you get a new medicine.
How should I take Detrol?
- Take Detrol exactly as your doctor tells you to take it.
- Your doctor will tell you how many Detrol Tablets to take and when to take them.
- Do not change your dose unless told to do so by your doctor.
- You can take Detrol with or without food.
- Take Detrol at the same times each day.
- If you miss a dose of Detrol, just take your next regular dose at your next regular time. Do not try to make up for your missed dose.
- If you take too much Detrol, call your doctor, or go to the hospital emergency room right away.
What should I avoid while taking Detrol?
Medicines like Detrol can cause blurred vision, dizziness, and drowsiness. Do not drive, operate machinery, or do other dangerous activities until you know how Detrol affects you.
What are the possible side effects of Detrol?
Detrol may cause allergic reactions that may be serious. Symptoms of a serious allergic reaction may include swelling of the face, lips, throat or tongue. If you experience these symptoms, you should stop taking DETROL and get emergency medical help right away.
The most common side effects with Detrol are:
- Dry mouth
- Stomach pain
Tell your doctor if you have any side effects that bother you or that do not go away.
These are not all the side effects with Detrol. For a complete list, ask your doctor or pharmacist.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
General information about the safe and effective use of Detrol
Medicines are sometimes prescribed for conditions that are not mentioned in the patient information leaflet. Only use Detrol the way your doctor tells you. Do not give Detrol to other people even if they have the same symptoms you have. It may harm them.
This guide summarizes the most important information about Detrol. If you would like more information, talk with your doctor. You can ask your doctor or pharmacist for information about Detrol that is written for health professionals.
How should I store Detrol?
- Store Detrol at room temperature (59 to 86° F).
- Keep it in a dry place.
Keep Detrol and all medicines out of the reach of children.
What are the ingredients in Detrol?
Active ingredients: tolterodine tartrate
Inactive ingredients: 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.
PRINCIPAL DISPLAY PANEL – 2 mg Capsule Dose Foil Pack
- Detrol® LA
- 2 mg
- Pharmacia & Upjohn Co
Div of Pfizer Inc, NY, NY 10017
SRC: NLM .