Tolterodin Upjohn
Extended-release antimuscarinic capsule for overactive bladder – once-daily control of urgency, frequency and urge incontinence
Tolterodin Upjohn 2 mg is an extended-release (depot) hard capsule containing tolterodine tartrate, an antimuscarinic medicine that relaxes the bladder muscle. It is prescribed for adults with overactive bladder syndrome (OAB) to reduce urinary urgency, frequency, and urge incontinence. Taken once daily, its prolonged-release mechanism provides steady 24-hour symptom control. This evidence-based guide summarises uses, correct dosing, side effects, and drug interactions in line with EMA, FDA, WHO, and AUA/SUFU international guidelines.
Quick Facts
Key Takeaways
- Tolterodin Upjohn is a prescription-only extended-release capsule (2 mg tolterodine tartrate) used to treat overactive bladder symptoms in adults, including urinary urgency, frequency, and urge incontinence.
- The standard adult dose is one 2 mg capsule taken once daily, swallowed whole at the same time each day; crushing, chewing, or opening the capsule destroys the extended-release mechanism and must be avoided.
- Dry mouth is the most common side effect (more than 1 in 10 patients), but extended-release formulations typically cause less severe dry mouth than immediate-release tolterodine tablets.
- Tolterodin Upjohn is contraindicated in urinary retention, uncontrolled narrow-angle glaucoma, myasthenia gravis, severe ulcerative colitis, and toxic megacolon; use is not recommended during pregnancy or breastfeeding.
- Treatment benefit should be re-evaluated after 2–3 months; dose reduction to 1 mg once daily is required for hepatic or renal impairment, CYP2D6 poor metabolisers, and patients on potent CYP3A4 inhibitors.
What Is Tolterodin Upjohn and What Is It Used For?
Quick Answer: Tolterodin Upjohn is a once-daily extended-release capsule of tolterodine tartrate used to treat overactive bladder (OAB) in adults. It blocks muscarinic receptors on the bladder wall, reducing involuntary detrusor muscle contractions and thereby easing urinary urgency, frequency, and urge incontinence over a full 24 hours.
Tolterodine, the active substance in Tolterodin Upjohn, is a competitive antagonist of muscarinic acetylcholine receptors. These receptors – particularly the M2 and M3 subtypes – are densely expressed on the smooth muscle of the urinary bladder, where acetylcholine release from parasympathetic nerves normally drives bladder contraction. By occupying these receptors without activating them, tolterodine prevents involuntary contractions of the detrusor muscle that cause the unpredictable urge to urinate so characteristic of overactive bladder syndrome.
Overactive bladder (OAB) is a common, chronic condition defined by the International Continence Society (ICS) as urinary urgency, with or without urge incontinence, usually with increased daytime frequency and nocturia, and in the absence of urinary tract infection or other obvious pathology. Epidemiological studies estimate a worldwide adult prevalence of 12–17%, with higher rates in women, older adults, and patients with neurological conditions. Although rarely life-threatening, OAB has a profound impact on quality of life – impairing sleep, work productivity, sexual health, and social functioning, and contributing to depression and anxiety.
What distinguishes Tolterodin Upjohn from conventional immediate-release tolterodine tablets is its extended-release (depot) technology. The hard capsule contains tolterodine tartrate in coated microspheres or a matrix that releases the active substance gradually along the gastrointestinal tract. This produces smoother, lower peak plasma concentrations than twice-daily tablets and allows convenient once-daily dosing. Clinical pharmacokinetic studies have shown that extended-release tolterodine delivers comparable 24-hour exposure (AUC) to the immediate-release formulation while producing fewer concentration peaks, which translates to a lower incidence and severity of dry mouth – the principal dose-limiting side effect.
Tolterodin Upjohn is therefore positioned as a first-line or second-line treatment for adults with moderate-to-severe OAB, particularly where adherence, convenience, or tolerability of dry mouth are important considerations. It is typically started after non-pharmacological measures such as behavioural therapy, bladder training, pelvic floor muscle exercises, and fluid or caffeine management have been attempted. In multiple randomised controlled trials, once-daily extended-release tolterodine has reduced urge incontinence episodes by approximately 70–75% from baseline and decreased daily micturition frequency by 1.5–2.5 episodes, with benefit typically observed within 4–8 weeks and maintained long-term.
Tolterodin Upjohn belongs to the broader class of urinary antispasmodics (ATC code G04BD07). Other agents in the same therapeutic class include oxybutynin, solifenacin, darifenacin, fesoterodine, and trospium. Tolterodine is notable for its relatively balanced M3/M2 receptor activity and its partial bladder selectivity, which in head-to-head studies has been associated with a more favourable dry-mouth profile than oxybutynin at equally effective doses.
What Should You Know Before Taking Tolterodin Upjohn?
Quick Answer: Before starting Tolterodin Upjohn, tell your doctor about all medical conditions – especially any history of urinary retention, glaucoma, heart rhythm problems, liver or kidney disease. Provide a complete medication list, including over-the-counter drugs and herbal products, because several important interactions are possible.
Contraindications
Tolterodin Upjohn must not be used in the following circumstances. These are absolute contraindications: the potential for harm clearly outweighs any potential benefit, and alternative treatments should be considered.
- Hypersensitivity – Known allergy to tolterodine tartrate or to any of the capsule excipients (listed in the composition section).
- Urinary retention – Inability to empty the bladder, or significant post-void residual volume that places you at high risk of retention.
- Uncontrolled narrow-angle (angle-closure) glaucoma – Antimuscarinic agents can precipitate an acute glaucoma attack in susceptible individuals.
- Myasthenia gravis – A neuromuscular condition where cholinergic transmission is already impaired; antimuscarinics may worsen muscle weakness.
- Severe ulcerative colitis – Reduced gastrointestinal motility may trigger toxic megacolon in active severe disease.
- Toxic megacolon – A medical emergency of colonic dilation; further reduction in motility is dangerous.
Warnings and Precautions
Speak with your doctor before starting Tolterodin Upjohn if any of the following apply to you. These conditions do not necessarily prevent treatment but may require a lower starting dose, closer monitoring, or additional investigations.
- Bladder outflow obstruction – In men, benign prostatic hyperplasia (BPH) with significant obstruction increases the risk of urinary retention. Consider urodynamic assessment and close follow-up.
- Gastrointestinal obstructive disorders – Conditions reducing gastric or intestinal motility, such as pyloric stenosis or gastroparesis, can be exacerbated by tolterodine's anticholinergic effect on smooth muscle.
- Hepatic impairment – Tolterodine is extensively metabolised by the liver; dose reduction to 1 mg once daily is required in moderate hepatic impairment. Tolterodin Upjohn is not recommended in severe hepatic impairment.
- Renal impairment – In patients with moderate-to-severe renal impairment (creatinine clearance 10–30 mL/min), the lower 1 mg daily dose is recommended.
- Autonomic neuropathy – Pre-existing dysautonomia (as in diabetes mellitus, Parkinson's disease, or amyloidosis) may be exacerbated.
- Hiatal hernia (diaphragmatic hernia) – Tolterodine can reduce lower oesophageal sphincter tone and worsen gastro-oesophageal reflux.
- Severe constipation or reduced gastrointestinal motility – The anticholinergic effect prolongs intestinal transit time and can precipitate faecal impaction.
- Cardiac risk factors including any of the following:
- Congenital or acquired long QT syndrome / documented QT prolongation on ECG
- Symptomatic bradycardia
- Known cardiomyopathy or left ventricular dysfunction
- Clinically significant myocardial ischaemia
- Pre-existing arrhythmia
- Chronic heart failure
- Electrolyte abnormalities – Hypokalaemia, hypocalcaemia, or hypomagnesaemia independently prolong the QT interval and amplify the cardiac risk.
Patients aged 65 years and above are at increased risk of antimuscarinic side effects, including cognitive impairment, confusion, falls, dry mouth, constipation, and urinary retention. The American Geriatrics Society Beers Criteria (2023 update) categorises tolterodine as potentially inappropriate in older adults, particularly those with dementia or cognitive impairment. A careful benefit-risk discussion – including trial of behavioural strategies, mirabegron as an alternative, and dose review – is advised.
Pregnancy and Breastfeeding
Pregnancy: Tolterodin Upjohn is not recommended during pregnancy. There are no adequate, well-controlled studies in pregnant women. Animal reproductive toxicity studies have shown malformations at doses associated with significant maternal toxicity. If you are pregnant, suspect you may be pregnant, or are planning pregnancy, inform your doctor so that alternative, better-studied options can be considered.
Breastfeeding: It is unknown whether tolterodine or its active metabolite (5-hydroxymethyl tolterodine) passes into human breast milk. In mice, tolterodine and its metabolites have been detected in the milk of lactating females. Because the effects on the breastfed infant are unknown, Tolterodin Upjohn should not be used while breastfeeding, and your doctor will help you decide whether to discontinue breastfeeding or discontinue treatment, taking into account the importance of the medicine for you.
Fertility: No data on the effect of tolterodine on human fertility are available. Animal studies have shown no impact on male or female fertility at therapeutic exposure levels.
Driving and Operating Machinery
Tolterodin Upjohn can cause dizziness, drowsiness, blurred vision, and occasionally confusion or memory impairment, any of which may impair your ability to drive a vehicle, cycle, or operate heavy machinery safely. You should assess your individual response during the first days of treatment, avoid driving if affected, and discuss persistent concerns with your doctor or pharmacist. Combining Tolterodin Upjohn with alcohol or other sedating substances amplifies these effects.
Tolterodin Upjohn 2 mg capsules contain sucrose in the controlled-release pellets. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption, or sucrase-isomaltase insufficiency should not take this medicine. Each capsule contains less than 1 mmol (23 mg) sodium, meaning it is essentially sodium-free.
How Does Tolterodin Upjohn Interact with Other Drugs?
Quick Answer: Tolterodine is metabolised primarily by the liver enzyme CYP2D6, with CYP3A4 as an alternative pathway. Strong inhibitors of these enzymes (certain antibiotics, antifungals, some HIV drugs, and SSRI antidepressants) substantially increase tolterodine exposure and side-effect risk. Drugs that prolong the QT interval and other anticholinergic medicines also require careful consideration.
Always tell your doctor and pharmacist about every medicine and supplement you take, including over-the-counter products, herbal remedies (such as St John's wort), vitamins, and recreational substances. Tolterodine tartrate can both affect and be affected by many other drugs, and some combinations need dose adjustment while others should be avoided outright.
Major Interactions – Not Recommended
Concomitant use of Tolterodin Upjohn with the following medicines is not recommended. If they are clinically essential, dose reduction of tolterodine (typically to 1 mg once daily) and close monitoring are required:
| Drug / Class | Mechanism | Clinical Significance |
|---|---|---|
| Erythromycin, Clarithromycin, Telithromycin | Potent macrolide CYP3A4 inhibitors | Markedly increase tolterodine and 5-HMT plasma levels; added risk of QT prolongation and anticholinergic toxicity |
| Ketoconazole, Itraconazole, Voriconazole, Posaconazole | Potent azole antifungal CYP3A4 inhibitors | Can double or triple tolterodine exposure; reduce tolterodine dose to 1 mg once daily and monitor closely |
| HIV protease inhibitors (ritonavir, cobicistat-boosted regimens) | Strong CYP3A4 and partial CYP2D6 inhibition | Substantial increase in tolterodine exposure; avoid combination where possible |
| Cisapride | QT-prolonging prokinetic; CYP3A4 substrate | Combined QT prolongation risk (torsades de pointes); avoid |
Moderate Interactions – Use with Caution
The following medicines may be used with tolterodine under medical supervision, but require monitoring and often dose adjustment of either agent:
| Drug / Class | Mechanism | Clinical Significance |
|---|---|---|
| Amiodarone, Sotalol, Quinidine, Procainamide, Dronedarone | Class I/III antiarrhythmics prolonging QT interval | Additive risk of QT prolongation and torsades de pointes; baseline and follow-up ECG advised |
| Fluoxetine, Paroxetine, Bupropion | CYP2D6 inhibitors (SSRI / NDRI) | Elevated tolterodine levels in CYP2D6 extensive metabolisers; monitor for anticholinergic side effects |
| Other antimuscarinics (oxybutynin, solifenacin, darifenacin, trospium, hyoscine, tricyclic antidepressants, first-generation antihistamines) | Additive anticholinergic burden | Increased risk of dry mouth, constipation, urinary retention, cognitive impairment, confusion, delirium, and heat stroke |
| Cholinergic agents (pilocarpine, bethanechol) and cholinesterase inhibitors (donepezil, rivastigmine, galantamine) | Directly opposing pharmacodynamic effects | Mutual reduction of therapeutic benefit; particularly relevant for patients treated for Alzheimer's dementia and co-existing OAB |
| Metoclopramide, Domperidone | Prokinetic dopamine antagonists | Tolterodine reduces gastric emptying and may blunt efficacy of prokinetics; also additive QT risk with domperidone |
| Diuretics (loop and thiazide) causing hypokalaemia | Electrolyte imbalance | Low potassium increases QT prolongation risk with tolterodine; monitor and correct electrolytes |
Minor Interactions
Minor interactions generally do not require dose adjustment but should be mentioned to your prescriber for awareness. These include concomitant alcohol (additive drowsiness), opioids (additive constipation and sedation), and moderate CYP3A4 inhibitors such as diltiazem, verapamil, and fluconazole. Regular large-volume consumption of grapefruit juice is a modest CYP3A4 inhibitor and should be discussed.
Tolterodin Upjohn extended-release capsules may be taken with or without food. Food does not meaningfully affect the overall 24-hour absorption. Alcohol should be limited or avoided during treatment because it worsens the sedative, dizziness, and cognitive side effects of tolterodine. Grapefruit and grapefruit juice inhibit intestinal CYP3A4 and may modestly raise tolterodine concentrations; occasional consumption is unlikely to cause harm, but regular daily intake should be discussed with your pharmacist.
What Is the Correct Dosage of Tolterodin Upjohn?
Quick Answer: The standard adult dose of Tolterodin Upjohn is one 2 mg extended-release capsule taken once daily, swallowed whole with water. In patients with hepatic or renal impairment, on potent CYP3A4 inhibitors, or in CYP2D6 poor metabolisers, the dose is reduced to 1 mg once daily (available as a lower-strength formulation). The capsule must not be crushed, chewed, or opened.
Always take Tolterodin Upjohn exactly as your doctor has prescribed. Do not change the dose or stop the medicine without medical advice, because abrupt discontinuation may allow OAB symptoms to return. Swallow the capsule whole with a glass of water, ideally at the same time each day to maintain steady 24-hour plasma concentrations. The capsule may be taken with or without food.
The extended-release mechanism depends on intact coated pellets. Crushing, chewing, or opening the capsule destroys controlled release and causes all the tolterodine to be absorbed rapidly at once, producing high peak plasma concentrations and a markedly higher risk of anticholinergic and cardiac side effects. If you cannot swallow the capsule whole, contact your doctor or pharmacist to discuss alternative formulations.
Adults (18 Years and Older)
Standard Dose
2 mg once daily – One Tolterodin Upjohn 2 mg extended-release capsule, taken at approximately the same time every day.
Reduced Dose (1 mg once daily)
The reduced dose is recommended for:
- Moderate hepatic impairment (Child-Pugh B)
- Moderate-to-severe renal impairment (creatinine clearance 10–30 mL/min)
- Concomitant use of potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin)
- Known CYP2D6 poor metaboliser status
- Troublesome antimuscarinic side effects at the standard dose
Children and Adolescents
Tolterodin Upjohn is not recommended for children or adolescents under 18 years of age. Paediatric clinical trials of tolterodine for OAB have not demonstrated meaningful efficacy over placebo, and safety data are insufficient. The European Medicines Agency has waived the requirement for studies in children under 2 years and determined that the available evidence does not support routine paediatric use for overactive bladder. Children with neurogenic detrusor overactivity may receive antimuscarinic therapy under specialist supervision, but alternative agents are generally preferred.
Elderly Patients
No specific dose reduction is mandated on the basis of age alone, but prescribers should consider initiating treatment at 1 mg once daily in frail patients, in those with reduced creatinine clearance, or where multiple anticholinergic medicines are already prescribed. The cumulative anticholinergic burden – quantified by validated scales such as the Anticholinergic Cognitive Burden (ACB) Scale – has been epidemiologically linked in older adults to increased risks of delirium, falls, and incident dementia. Practical recommendations include:
- Screen for cognitive impairment before and during treatment, using simple tools such as the Mini-Cog or MoCA.
- Review and simplify concurrent anticholinergic medicines where possible.
- Ensure adequate hydration and anticipate heat-related adverse effects during hot weather.
- Assess post-void residual volume in men with symptoms of BPH.
- Consider mirabegron (a beta-3 agonist) as a non-anticholinergic alternative if tolerability is a concern.
| Patient Group | Recommended Dose | Administration | Notes |
|---|---|---|---|
| Adults (standard) | 2 mg once daily | Swallow capsule whole with water | Same time each day; with or without food |
| Moderate hepatic impairment | 1 mg once daily | Swallow capsule whole | Use lower-strength capsule; monitor liver function |
| Severe hepatic impairment | Not recommended | — | Consider alternative therapy |
| Moderate–severe renal impairment (CrCl 10–30 mL/min) | 1 mg once daily | Swallow capsule whole | Avoid in dialysis unless specialist advice |
| Potent CYP3A4 inhibitor co-therapy | 1 mg once daily | Swallow capsule whole | Examples: ketoconazole, clarithromycin, ritonavir |
| Elderly / multiple anticholinergics | 1–2 mg once daily | Start low; titrate as tolerated | Monitor cognition, falls, urinary retention |
| Children <18 years | Not recommended | — | Insufficient efficacy and safety data |
Missed Dose
If you forget to take a dose, take it as soon as you remember on the same day. If it is already close to the time of the next scheduled dose (for example, within a few hours), skip the missed dose entirely and continue with your normal schedule the following day. Never take two doses within 24 hours to compensate for a missed capsule – double-dosing produces excessive plasma concentrations and raises the risk of anticholinergic toxicity, QT prolongation, and arrhythmia. If you miss multiple consecutive doses, contact your doctor or pharmacist for tailored advice.
Overdose
If you or someone else has taken a large amount of Tolterodin Upjohn – accidentally or intentionally – contact emergency services or a poison control centre immediately, and bring the packaging. Take the person to the nearest emergency department. Overdose symptoms can develop within hours and may include:
- Severe central excitation: agitation, confusion, hallucinations, delirium
- Seizures or tremor
- Respiratory depression or laboured breathing
- Tachycardia, palpitations, or cardiac arrhythmias
- Significant QT prolongation on ECG (risk of torsades de pointes)
- Complete urinary retention
- Mydriasis (very dilated pupils) with blurred vision
- Hyperthermia, dry flushed skin, reduced sweating
- Severe dry mouth and absent bowel sounds
Management is supportive: airway, breathing, circulation assessment; activated charcoal if presentation is within one hour; continuous cardiac monitoring; and, in severe cases, physostigmine may be considered by poisons specialists. Haemodialysis is not effective for tolterodine removal because of extensive protein binding and tissue distribution.
Treatment Duration
Tolterodin Upjohn is typically continued long-term for chronic OAB, but the benefit should be re-evaluated systematically. Clinical guidelines from the European Association of Urology (EAU) and AUA/SUFU recommend reassessing symptom response after 2–3 months of adequately dosed therapy. Validated patient-reported tools – such as the Patient Perception of Bladder Condition, 3-day bladder diary, and OAB-q short form – help quantify benefit and side-effect burden. If no meaningful improvement occurs by 3 months, options include switching to another antimuscarinic, changing class to the beta-3 agonist mirabegron, combination therapy, or referral for advanced treatments such as intravesical botulinum toxin A, percutaneous tibial nerve stimulation, or sacral neuromodulation.
Do not stop Tolterodin Upjohn abruptly without first discussing with your doctor. Although there is no physical withdrawal syndrome, OAB symptoms may return within days to weeks of discontinuation, and behavioural or lifestyle interventions should ideally be in place before stopping.
What Are the Side Effects of Tolterodin Upjohn?
Quick Answer: The most common side effect is dry mouth, reported by more than 1 in 10 patients. Other common effects include headache, constipation, dry eyes, blurred vision, dizziness, drowsiness, abdominal pain, and fatigue. Serious but uncommon reactions include angioedema, heart failure, severe allergic reactions, and significant cognitive disturbance. Extended-release capsules generally cause less severe dry mouth than immediate-release tablets.
Like all medicines, Tolterodin Upjohn can cause side effects, although not everybody gets them. Most anticholinergic effects are mild to moderate, dose-dependent, and often improve with continued use as the body adapts. The categories below reflect pooled data from randomised controlled trials and post-marketing pharmacovigilance, reported according to the MedDRA frequency convention.
- Angioedema – Sudden swelling of the face, lips, tongue, or throat; difficulty swallowing or breathing; hives with any of the above.
- Severe allergic (anaphylactoid) reaction – Widespread rash with breathing difficulty, light-headedness, or collapse.
- Signs of heart failure – Rapidly worsening breathlessness (particularly lying flat or at night), significant fatigue at rest, and swelling of the legs or abdomen.
- Severe confusion, hallucinations, or loss of consciousness.
- Inability to urinate with bladder pain – Possible acute urinary retention.
- Palpitations with dizziness or fainting – Possible arrhythmia, particularly in patients with QT-prolonging comorbidities.
Very Common
Affects more than 1 in 10 patients
- Dry mouth (xerostomia)
Common
Affects 1 in 10 to 1 in 100 patients
- Headache
- Dizziness and vertigo
- Drowsiness (somnolence)
- Dry eyes
- Blurred vision
- Constipation
- Dyspepsia (indigestion)
- Abdominal pain
- Nausea
- Diarrhoea
- Flatulence
- Dry skin
- Painful or difficult urination (dysuria)
- Urinary retention or incomplete bladder emptying
- Fatigue
- Peripheral oedema (swelling of ankles/feet)
- Sinusitis / upper respiratory tract infection
Uncommon
Affects 1 in 100 to 1 in 1,000 patients
- Allergic (hypersensitivity) reactions
- Anxiety and nervousness
- Memory impairment
- Palpitations
- Tachycardia (rapid heart rate)
- Cardiac arrhythmia
- Heart failure exacerbation
- Gastro-oesophageal reflux (heartburn)
- Chest discomfort
- Weight gain
- Bronchitis
- Paraesthesia
Rare / Post-Marketing Reports
Affects fewer than 1 in 1,000 patients
- Anaphylactoid reactions
- Angioedema
- Confusion and disorientation
- Hallucinations (visual, auditory, tactile)
- Delirium, particularly in older adults
- Worsening of pre-existing dementia
- Skin flushing
- QT prolongation and torsades de pointes
Dry mouth: Sip water frequently, use sugar-free chewing gum or lozenges, try saliva substitutes, and maintain excellent oral hygiene to reduce dental caries risk. Constipation: Increase dietary fibre and water intake, include regular physical activity, and consider an osmotic laxative (e.g., macrogol) under medical advice. Dry eyes/blurred vision: Use preservative-free lubricating eye drops; inform your optometrist before routine checks. Drowsiness: Take the capsule at the same time daily and avoid alcohol.
If you experience any side effects, including any not listed above, talk to your doctor, pharmacist, or nurse. You can also report side effects directly to your national pharmacovigilance authority – for example, the FDA MedWatch programme in the United States, the Yellow Card Scheme in the United Kingdom, or the European Medicines Agency (EMA) EudraVigilance system. By reporting side effects, you help improve the safety information available for this medicine.
How Should You Store Tolterodin Upjohn?
Quick Answer: Store Tolterodin Upjohn capsules at room temperature, below 25°C (77°F), in the original blister pack to protect from moisture. Keep out of the sight and reach of children. Do not use after the expiry date printed on the packaging.
Keep Tolterodin Upjohn in its original packaging until use. The blister film provides essential protection from light and humidity, which can otherwise degrade the coated extended-release pellets. Store at room temperature, typically below 25°C (77°F), away from direct sunlight and bathrooms or kitchens where heat and humidity fluctuate.
Always keep medicines out of the sight and reach of children. Even a single adult 2 mg capsule can cause severe anticholinergic toxicity in a small child. If a child accidentally takes any amount of Tolterodin Upjohn, contact emergency services or a poison control centre immediately.
Do not use Tolterodin Upjohn after the expiry date (EXP) printed on the blister pack or carton. The expiry date refers to the last day of the stated month. Check the capsules before each dose: they should appear intact, without cracks, discolouration, or leakage of the internal contents. Discard any capsule that looks damaged.
Do not dispose of medicines in household waste or down the toilet or sink. Return unused or expired medicines to your community pharmacy for safe disposal according to local take-back programmes. These measures help protect the environment, wildlife, and drinking water supplies from pharmaceutical contamination.
What Does Tolterodin Upjohn Contain?
Quick Answer: The active substance is tolterodine tartrate (2 mg per capsule, equivalent to approximately 1.37 mg of tolterodine base). Inactive ingredients include sugar spheres, hypromellose, ethylcellulose, medium-chain triglycerides, oleic acid, gelatin, and pharmaceutical-grade colourants used in the capsule shell.
Active Substance
- 2 mg capsules: Each hard extended-release capsule contains 2 mg of tolterodine tartrate, equivalent to 1.37 mg of tolterodine free base.
Inactive Ingredients (Excipients)
Capsule content (coated pellets): Sucrose-starch spheres, hypromellose (E464), ethylcellulose (N10), medium-chain triglycerides, and oleic acid form the extended-release matrix around the active substance.
Capsule shell: Gelatin, titanium dioxide (E171), and pharmaceutical colourants (which may include indigo carmine E132 or iron oxides E172 depending on strength) form the hard two-piece capsule shell. The capsule is printed with edible ink containing shellac and iron oxide.
Capsule Appearance
2 mg capsule: Hard gelatin capsule containing white to off-white extended-release pellets. External appearance varies by manufacturer but typically presents as a coloured opaque capsule with printed strength identification. Always check the appearance against your dispensed packaging and contact your pharmacist if anything looks different from previous supplies.
Pack Sizes
Tolterodin Upjohn 2 mg extended-release capsules are supplied in aluminium/PVC blister packs, typically in packs of 14, 28, 30, 56, 84, or 98 capsules. Not all pack sizes may be marketed in every country, and availability depends on national registration.
Tolterodin Upjohn is marketed under the Upjohn (now Viatris) corporate portfolio. For the current marketing authorisation holder, manufacturer, and local representative in your country, consult the patient information leaflet (PIL) supplied with your pack or check with your national medicines regulatory authority.
- ATC classification: G04BD07 (Urological — Drugs for urinary frequency and incontinence — Tolterodine)
- INN (International Nonproprietary Name): Tolterodine
- Chemical form used: Tolterodine L-tartrate (hydrogen tartrate salt)
- Molecular formula: C₂₂H₃₁NO · C₄H₆O₆ (tolterodine tartrate)
- WHO ICD-10 indication code: N32.81 (Overactive bladder)
Frequently Asked Questions About Tolterodin Upjohn
Tolterodin Upjohn is an extended-release (depot) capsule prescribed to adults with overactive bladder syndrome (OAB). It treats urinary urgency (a sudden, compelling need to urinate), increased frequency (passing urine more often than usual), and urge incontinence (involuntary urine leakage associated with urgency). It works by relaxing the detrusor muscle of the bladder, reducing involuntary contractions and increasing functional bladder capacity over 24 hours.
The standard adult dose is one 2 mg extended-release capsule taken once daily at approximately the same time each day. Swallow the capsule whole with water – it must not be crushed, chewed, or opened, because this destroys the extended-release mechanism and causes the full dose of tolterodine to be absorbed too rapidly, increasing the risk of side effects. The capsule can be taken with or without food.
The most common side effect is dry mouth, affecting more than 1 in 10 patients. Other common side effects include headache, constipation, dry eyes, blurred vision, dizziness, drowsiness, abdominal discomfort, and fatigue. Most are mild to moderate and often improve as the body adjusts. The extended-release capsule typically produces less severe dry mouth than immediate-release tolterodine tablets, thanks to smoother plasma concentrations over 24 hours.
No. Tolterodin Upjohn should not be used during pregnancy: human safety data are insufficient, and animal studies have demonstrated reproductive toxicity at high doses. Breastfeeding is also not recommended because it is unknown whether tolterodine passes into human breast milk. If you are pregnant, suspect pregnancy, or are planning to become pregnant, inform your doctor immediately so alternative options can be considered.
Some symptom improvement may be noticed within 1–2 weeks, but full therapeutic benefit typically takes 4–8 weeks because the bladder needs time to adjust. Current clinical guidelines recommend re-evaluating response after 2–3 months using a bladder diary and symptom questionnaires. Do not stop treatment prematurely. If no meaningful benefit has emerged by 12 weeks, your doctor may consider alternative medicines, combination therapy, or specialist interventions.
If you miss a dose, take it as soon as you remember on the same day. If it is almost time for your next scheduled dose, skip the missed capsule and continue with your regular schedule. Never take two capsules within 24 hours to make up for a missed one – double-dosing can cause excessive plasma concentrations and significantly increase the risk of anticholinergic side effects and QT prolongation. If you miss several consecutive doses, contact your doctor or pharmacist for advice.
Avoid concurrent use with potent CYP3A4 inhibitors such as the antifungals ketoconazole and itraconazole, the macrolide antibiotics erythromycin and clarithromycin, and HIV protease inhibitors (ritonavir, cobicistat-boosted combinations). Use caution with QT-prolonging antiarrhythmics (amiodarone, sotalol, quinidine), other anticholinergic medicines (oxybutynin, tricyclic antidepressants, first-generation antihistamines), cholinesterase inhibitors used for dementia (donepezil, rivastigmine), and the SSRIs fluoxetine and paroxetine (CYP2D6 inhibitors). Always give your doctor and pharmacist a complete, up-to-date medication list.
References
All medical information on this page is based on peer-reviewed research, international clinical guidelines, and official regulatory documents. The following sources were consulted:
- European Medicines Agency (EMA). Tolterodine – Summary of Product Characteristics (SmPC). European Public Assessment Reports. Available at: www.ema.europa.eu
- U.S. Food and Drug Administration (FDA). Detrol LA (tolterodine tartrate extended-release capsules) – Prescribing Information. FDA Label Archives.
- Van Kerrebroeck P, Kreder K, Jonas U, et al. Tolterodine once-daily: superior efficacy and tolerability in the treatment of the overactive bladder. Urology. 2001;57(3):414–421. doi:10.1016/S0090-4295(00)01113-4
- Chapple CR, Khullar V, Gabriel Z, et al. The effects of antimuscarinic treatments in overactive bladder: an update of a systematic review and meta-analysis. European Urology. 2008;54(3):543–562. doi:10.1016/j.eururo.2008.06.047
- Abrams P, Cardozo L, Fall M, et al. The standardisation of terminology in lower urinary tract function: Report from the standardisation sub-committee of the International Continence Society. Neurourology and Urodynamics. 2002;21(2):167–178.
- Gormley EA, Lightner DJ, Burgio KL, et al. Diagnosis and treatment of overactive bladder (non-neurogenic) in adults: AUA/SUFU guideline amendment. Journal of Urology. 2019;202(3):558–563.
- National Institute for Health and Care Excellence (NICE). Urinary incontinence and pelvic organ prolapse in women: management. NICE guideline [NG123]. 2019.
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