Tolterodine

Brand names of tolterodine

  • Detrol

Tolterodine is a drug used in the treatment of urinary bladder disorders that affect urination. It belongs to a group of drugs which are known as cholinergic, or acetyl-choline receptor blockers. In more general terms, it belongs to a group called anti-spasmodics.

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Our urinary bladder is like a bag made of muscles. Urine, after filtration by the kidneys, fills in the bladder due to which it is inflated, just like a balloon. Inflated muscles apply pressure inside the bladder which, after crossing a certain limit, causes a desire to urinate.

Now, the nerves of the bladder muscles release acetyl-choline, which gets attached to the receptors situated on the muscle cells causing them to contract. This further increases pressure inside the bladder and consequently the desire to urinate is also increased. When one is ready to urinate, the muscles at the bladder outlet relax, and due to the high bladder pressure, urine is forced out of it.

Normally, this whole process is under the conscious control of the individual; however, some individuals, due to some reasons, lose the normal control over the process as well as the normal sensations associated with it. They may feel a desire to urinate even when the bladder contains little urine, and may not be able to control it, resulting in involuntary urination at inappropriate times.

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Tolterodine blocks the attachment of acetyl-choline on receptors of the muscle cells, thus preventing their contraction and slowing down build-up of bladder pressure. The result is a reduced sensation to urinate and better control over urination.
Tolterodine received the FDA's approval in 1998. Another, extended release form, called Detrol LA, received its approval in 2001.

Prior to taking tolterodine let your health care provider know

  • About your allergies to tolterodine or any other drug.
  • About the prescription as well as non-prescription medicines you are taking. Don't forget to mention these medicines if you are taking them: erythromycin (E-mycin, Ery-Tab, etc.), clarithromycin (Biaxin), fluconazole (Diflucan), ketoconazole (Nizoral), itraconazole (Sporanox), medicines for glaucoma, as well as vitamin or mineral supplements.
  • About your complete medical history. Don't forget to mention these diseases if you suffer, or have ever suffered, from them: kidney diseases, liver diseases, glaucoma, and obstructive gastrointestinal diseases like pyloric stenosis.
  • About your pregnancy state. Don't forget to mention if you are already pregnant, or breast feeding, or would be pregnant during treatment. If pregnancy occurs while you are on tolterodine, inform your doctor.
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Usage

Tolterodine mainly finds use in treating an overactive bladder. It relaxes the bladder muscles to improve the patient's ability to control urination thereby reducing involuntary urination or urine leakage. It also reduces the frequent urge to urinate and decreases the need to go to bathroom too often.

How to use tolterodine

Before you begin tolterodine, read carefully the Patient Information Leaflet that comes with the package. Not only on the first buy, read it every time you buy a refill as there may be changes in instructions with more information on the drug. If you find anything ambiguous, talk to your doctor or the pharmacist.

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Tolterodine is taken orally, with food or without it, normally twice a day, unless directed otherwise by the doctor. To derive the maximum benefits, it should be used regularly, about the same time every day. Your doctor will prescribe the dose on the basis of severity of your condition, especially keeping in view kidney and liver diseases, your body's response to the drug, and the use of other medicines that may be interacting with it. So, don't increase either the dose or the frequency of taking it without first asking your doctor. This will not result in any faster improvement, but may seriously increase the risk of side effects. Inform the doctor if the condition persists or worsens.

For more details, talk to your doctor or the pharmacist.

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How tolterodine works

Tolterodine blocks the receptors on bladder muscles that provide sites for attachment of acetyl-choline thereby reducing muscle contraction and bladder pressure which decreases the urge to urinate and provides better control over the process of urination.

Side effects

Serious
Common
Less common

Possible interactions

Other medicaments
Tolterodine, taken with:
  • Other CYP 3A4 or 2D6 inhibitors, like macrolide antibiotics, ketoconazole, itraconazole, and others, may excessively increase blood levels and cause toxicity.
  • Fluoxetine (Prozac) may cause tolterodine toxicity.
  • Warfarin (Coumadin) may increase the risk of bleeding. More frequent INRs are advised.
Herbal medicines or minerals
Like tolterodine, St. John's wort may also increase sun sensitivity and so should be avoided with it. Beverages that have caffeine, like colas, ephedra, etc., may cause increased blood pressure leading to increased fluid removal needs and so, the need to urinate may also be increased. Therefore, caution is advised in their use.
Beverages
Grapefruit juice, and some teas that contain mild diuretic substances, should be avoided.
Alcohol
Alcohol may work contrary to the action of tolterodine by increasing loss of water from the body, and so should be avoided.
Tobacco smoking
Nicotine may also be counterproductive, tobacco should, therefore, be avoided in any form.
Exposure to sun
May cause sun sensitivity of the eyes if you are taking tolterodine.
Heavy exercise or exertion
Sweating is required to keep the body cool during heavy exertion or exercise. However, tolterodine may reduce sweating causing problems. Care is advised.

Storage instructions

Tolterodine should be stored at room temperature, that is 77°F or 25°C, away from light, heat and moisture. Can be stored for brief periods between 59-86°F, or 15-30°C. However, don't store in bathroom.
All medicines should be kept away from children as well as pets. They should be discarded properly when expired or no longer required, not by flushing down the toilet or pouring into a drain. Ask your pharmacist or a waste disposal company nearby for more details of safe disposal of drugs including tolterodine.

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