Spazmex

Spasmex (Trospium) is a medicine used to treat symptoms of overactive bladder (OAB). OAB is characterized by frequent urination, a strong and sudden urge, and possible urinary incontinence.

Trospium is an antimuscarinic (anticholinergic) agent. It blocks muscarinic receptors in the bladder, which leads to a decrease in the frequency and strength of contractions of the detrusor muscle of the bladder, thereby improving urinary control and reducing the frequency and intensity of the urge.

Indications Spazmex

1. Overactive bladder (OAB): This medication is used to treat symptoms of overactive bladder, such as frequent urination, a strong and sudden urge to urinate, and urge urinary incontinence.
2. Neurogenic Bladder: Spazmex may be used to treat bladder dysfunction associated with neurological diseases (eg, multiple sclerosis, spinal cord injury).

Release form

1. Tablets:
   • Film-coated tablets, dosage 5 mg.
   • Film-coated tablets, dosage 15 mg.
   • Film-coated tablets, dosage 30 mg.

These tablets are for oral use and are usually taken whole with plenty of water.

Main forms of release:

• 5 mg tablets: intended for multiple daily doses.
• 15 mg tablets: can be used as a maintenance dosage.
• 30 mg tablets: intended for patients requiring a higher dose to control symptoms.

Pharmacodynamics

1. Muscarinic receptor antagonism: Trospium is a muscarinic receptor antagonist. It blocks muscarinic receptors found in the smooth muscle of the bladder (especially M3 receptors), which are responsible for muscle contraction when stimulated by acetylcholine.
2. Decreases bladder contractions: By blocking these receptors, trospium reduces the activity of the cholinergic system, which leads to relaxation of the smooth muscles of the bladder. This reduces the frequency and strength of involuntary bladder contractions.
3. Increasing Bladder Capacity: By relaxing the bladder muscles, trospium helps increase bladder capacity, allowing you to hold more urine before you need to urinate. This helps reduce urinary frequency and improve bladder control.
4. Improving symptoms of overactive bladder: The use of trospium helps reduce urinary urgency and improve the quality of life of patients with overactive bladder.

Advantages of trospium:

• Minimal penetration of the blood-brain barrier: Trospium penetrates the blood-brain barrier poorly, which reduces the risk of central side effects such as dizziness and confusion.
• Wide therapeutic range: The drug has a relatively wide therapeutic range, which makes it effective at various dosages.

Pharmacokinetics

1. Absorption:

   • Trospium is rapidly absorbed after oral administration.
   • The maximum concentration in blood plasma is achieved 4-6 hours after administration.
   • Absolute bioavailability is about 9.6% due to the significant first pass effect through the liver.

2. Distribution:

   • Distribution volume is approximately 600 liters.
   • The drug binds to plasma proteins by 50-80%.
   • Trospium weakly penetrates the blood-brain barrier, which reduces the risk of central side effects.

3. Metabolism:

   • Trospium is metabolized in the liver. The main metabolic pathway is ester hydrolysis, leading to the formation of an inactive metabolite.
   • The drug is not metabolized by the cytochrome P450 system, which reduces the risk of interactions with other drugs metabolized by this system.

4. Excretion:

   • Trospium is excreted from the body primarily through the kidneys.
   • About 60% of the dose is excreted unchanged in the urine.
   • The half-life is approximately 5-18 hours.

5. Special populations:

   • In elderly patients, as well as in patients with impaired renal or hepatic function, the pharmacokinetics of trospium may change, which may require dosage adjustment.

Dosing and administration

Method of administration and dosage:

For adults:

• 5 mg tablets: Usually take 1-2 tablets (5-10 mg) 3 times a day. The maximum daily dose is 30 mg.
• 15 mg tablets: Usually take 1 tablet (15 mg) 2 times a day. The maximum daily dose is 30 mg.
• 30 mg tablets: Typically take 1 tablet (30 mg) once daily.

General recommendations:

• Method of administration: Tablets should be taken orally with a sufficient amount of water. The tablets should be swallowed whole without chewing.
• Time of administration: Tablets can be taken regardless of meals, but preferably 1 hour before meals.
• Duration of treatment: The duration of treatment is determined by the doctor depending on the patient's condition and his response to therapy.

Special instructions:

• Patients with renal impairment: Dosage may need to be reduced. You should consult your doctor.
• Patients with hepatic impairment: Dosage may need to be reduced. You should consult your doctor.
• Elderly patients: Dose adjustment may be required for elderly patients.

Missed dose:

• If you miss a dose, take it as soon as possible. If it is already time for your next dose, do not take a double dose to make up for the missed dose. Just continue taking it as usual.

Use Spazmex during pregnancy

Recommendations for using Spazmex during pregnancy:

1. Consult with your doctor: Before taking trospium during pregnancy, be sure to consult with your doctor. The doctor will evaluate your individual situation and decide whether to use the drug.
2. Benefit vs. Risk: The use of Spazmex during pregnancy can only be justified in cases where the potential benefits to the mother outweigh the possible risks to the fetus.
3. First trimester: Particular attention should be paid to the use of medications in the first trimester of pregnancy, when the formation of organs and systems of the fetus occurs. During this time, it is especially important to avoid unnecessary use of medications.

Contraindications

1. Hypersensitivity: The drug is contraindicated in people with a known hypersensitivity or allergic reaction to trospium or any other components of the drug.
2. Angle-closure glaucoma: Spasmex may increase intraocular pressure and its use is therefore contraindicated in patients with uncontrolled angle-closure glaucoma.
3. Tachyarrhythmias: Spazmex may aggravate tachyarrhythmias and should be avoided in patients with this condition.
4. Myasthenia gravis: The drug is contraindicated in patients with myasthenia gravis, as it may worsen their condition.
5. Severe renal failure: Spazmex is contraindicated in severe renal failure (creatinine clearance
6. Severe liver failure: The drug is contraindicated in patients with severe liver impairment due to the risk of accumulation and toxicity.
7. Gastrointestinal obstruction: Spazmex is contraindicated in patients with gastrointestinal obstruction, including paralytic ileus, due to the risk of worsening the condition.
8. Severe ulcerative colitis and toxic megacolon: The drug is contraindicated in severe ulcerative colitis and toxic megacolon, as anticholinergic effects may aggravate these conditions.
9. Urethral constriction and urinary retention: Spazmex is contraindicated in patients with urinary retention or significant urethral constriction as it may aggravate these conditions.

Side effects Spazmex

1. Very common side effects (more than 10%):

   • Dry mouth.

2. Common side effects (1-10%):

   • Constipation.
   • Dyspepsia (indigestion).
   • Stomach pain.
   • Dry eyes.
   • Nausea.
   • Headache.
   • Fatigue.

3. Infrequent side effects (0.1-1%):

   • Dizziness.
   • Drowsiness.
   • Visual disturbances, including blurred vision.
   • Rapid heartbeat (tachycardia).
   • Urine retention.
   • Urinary tract infections.

4. Rare side effects (0.01-0.1%):

   • Allergic reactions such as skin rash or itching.
   • Anaphylactic reactions.
   • Angioedema.
   • Confusion.
   • Hallucinations.
   • Heart rhythm disturbances (eg, QT prolongation, arrhythmias).

5. Very rare side effects (less than 0.01%):

   • Psychiatric disorders (eg, anxiety, depression).
   • Convulsions.
   • Worsening of glaucoma symptoms.

Overdose

1. Severe dry mouth.
2. Difficulty urinating (acute urinary retention).
3. Dilated pupils (mydriasis).
4. Tachycardia (rapid heartbeat).
5. Arrhythmias.
6. Severe dizziness.
7. Agitation and restlessness.
8. Convulsions.
9. Reddening of the skin.
10. Hyperthermia (increased body temperature).
11. Severe visual disturbances.
12. Confusion, hallucinations, and delirium.

Overdose Treatment

Treatment of trospium overdose is aimed at relieving symptoms and maintaining vital functions. Measures may include:

1. Respiratory and cardiovascular support: Administer oxygen, maintain blood pressure, monitor cardiac activity, and ensure adequate breathing.
2. Gastric lavage: May be helpful if large amounts of the drug have recently been taken.
3. Activated charcoal: Use of activated charcoal may help reduce absorption of the drug from the gastrointestinal tract if a short period of time has passed since ingestion.
4. Symptomatic therapy: Treat symptoms such as tachycardia and seizures as needed. This may include the use of beta blockers to control tachycardia or anticonvulsants for seizures.
5. Antidotes: Physostigmine may be used in some cases to counteract the anticholinergic effects, but its use should be carefully monitored due to potential side effects.

Interactions with other drugs

1. Anticholinergic drugs:

   • Concomitant use with other anticholinergic drugs (eg, atropine, scopolamine, some antidepressants and antipsychotics) may increase anticholinergic side effects such as dry mouth, constipation, blurred vision, and difficulty urinating.

2. Medicines that affect gastrointestinal motility:

   • Drugs that alter gastrointestinal motility (eg, metoclopramide) may affect the absorption of trospium.

3. Medicines that change gastric pH:

   • Antacids and other drugs that change gastric pH may affect the absorption of trospium.

4. Medicines that prolong the QT interval:

   • Concomitant use with drugs that prolong the QT interval (for example, class IA and III antiarrhythmic drugs, some antidepressants and antipsychotics) may increase the risk of cardiac arrhythmias.

5. CYP450 inducers and inhibitors:

   • Although trospium is not metabolized by the cytochrome P450 system, it is important to consider possible interactions with drugs that may affect other metabolic pathways in the liver.

6. Medicines excreted by the kidneys:

   • Drugs that affect renal function or compete for renal excretion may alter the concentration of trospium in the blood. It is important to take this into account when taking such drugs.

Interaction with food

• Trospium should be taken on an empty stomach, as food may reduce its absorption and therefore its effectiveness.