Tolterodine is a medication primarily used to treat overactive bladder symptoms, such as frequent urination, urgency, and urge incontinence (leakage). It belongs to a class of drugs known as antimuscarinics or anticholinergics, which work by blocking muscarinic receptors in the bladder. This action helps relax the bladder muscles, thereby increasing bladder capacity and reducing involuntary contractions.
BRAND NAMES:
Tolterodine Brand names: Neditol, Detrusitol, Mariosea.
MECHANISM OF ACTION
Tolterodine tartrate works by acting as a competitive muscarinic receptor antagonist, blocking the effects of acetylcholine on the detrusor muscle of the bladder. This helps decrease involuntary bladder contractions, expand bladder capacity, and relieve the symptoms associated with an overactive bladder.
PHARMACOKINETICS
Absorption:
Tolterodine is well-absorbed after oral administration, but its total bioavailability is highly variable due to extensive first-pass metabolism in the liver.
Distribution:
Tolterodine is extensively distributed throughout the body after oral administration, with a volume of distribution of approximately 113 liters, indicating significant tissue penetration beyond the vascular compartment.
Metabolism:
After being taken orally, tolterodine is processed in the liver, where it is converted into its main active metabolite, 5-hydroxymethyl derivative, which plays a significant role in its therapeutic effects.
Excretion:
Tolterodine is extensively metabolized by the liver before being primarily excreted through the urine. Only a small fraction is eliminated as the unchanged parent drug.
PHARMACODYNAMICS
The pharmacodynamics of tolterodine involve its action as a competitive antagonist of muscarinic receptors, particularly in the urinary bladder. By blocking these receptors, it inhibits the involuntary contraction of the bladder's detrusor muscle, helping to treat overactive bladder (OAB) symptoms such as urinary frequency, urgency, and incontinence.
ADMINISTRATION
Tolterodine is administered orally as either an immediate-release (IR) tablet or an extended-release (ER) capsule. Dosage depends on the formulation, the patient's individual response, and any existing medical conditions.
Before taking tolterodine, it's essential to consult with a healthcare professional. The information provided here is for general knowledge and should not be considered medical advice.
DOSAGE AND STRENGTH
Tolterodine is available in two oral forms, immediate-release (IR) tablets and extended-release (ER) capsules, each with different strengths and dosing frequencies. The correct dosage depends on the specific formulation and the individual's needs, with adjustments necessary for those with kidney or liver impairment.
DRUG INTERACTIONS
While some medications should never be used together, there are situations where two different drugs may be prescribed at the same time despite the possibility of an interaction. In such cases, your doctor may adjust the dosage or take other necessary precautions. If you are taking this medicine, it is particularly important to inform your healthcare provider about any other medications you are using. The interactions listed below have been selected based on their potential clinical importance but may not represent a complete list.
FOOD INTERACTIONS
There are no known food or drink interactions with tolterodine. However, it is not clear whether alcohol has any direct effect on the medication. Drinking alcohol while taking tolterodine may increase the risk of side effects such as dizziness or drowsiness.
CONTRAINDICATIONS
Tolterodine is contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma, as well as in those with a known hypersensitivity to the drug or any of its components. It should be used with caution in individuals with liver or kidney impairment.
SIDE EFFECTS:
Dry mouth – Chewing sugar-free gum or sucking on sugar-free lozenges may help relieve this.
Headache – Rest and stay well-hydrated to ease symptoms.
Dizziness, drowsiness, or a sensation of spinning (vertigo) – Take care when standing up or moving around.
Diarrhea – Drink fluids regularly to stay hydrated.
Nausea or vomiting – Eat small, light meals and avoid rich or spicy foods.
Bloating or excess gas (flatulence and burping) – Try to eat slowly and avoid carbonated drinks.
Stomach pain – Eating bland foods may help reduce discomfort.
Dry eyes – Using artificial tears or lubricating eye drops can provide relief.
OVER DOSE
An overdose of tolterodine can cause severe anticholinergic toxicity, which affects both the central and cardiovascular nervous systems. If you or someone you know has taken more than the prescribed dose, seek immediate medical attention by calling emergency services.
TOXICITY
Tolterodine toxicity, or overdose, causes severe anticholinergic effects that mainly impact the cardiovascular and central nervous systems. Overdose symptoms include blurred vision, confusion, urinary retention, and a rapid or irregular heartbeat. In rare but severe cases, an overdose can cause hallucinations, seizures, and respiratory issues.
