Spazmex

Spasmex (Trospiy) is a medication used to treat symptoms of overactive bladder (OAB). OAB is characterized by frequent, strong, and sudden urges to urinate, and possible urinary incontinence.

Trospium is an antimuscarinic (anticholinergic) agent. It blocks muscarinic receptors in the bladder, which results in 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 to urinate.

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 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. Pills:
   • Film-coated tablets, 5 mg.
   • Film-coated tablets, 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 dose.
• 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. Decreased bladder contractions: By blocking these receptors, trospium reduces the activity of the cholinergic system, which results in relaxation of the smooth muscles of the bladder. This reduces the frequency and strength of involuntary bladder contractions.
3. Increased 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 the frequency of urination and improve bladder control.
4. Improving symptoms of overactive bladder: Trospium helps reduce urinary urgency and improve quality of life in patients with overactive bladder.

Advantages of trospium:

• Minimal blood-brain barrier penetration: Trospium poorly penetrates the blood-brain barrier, reducing the risk of central side effects such as dizziness and confusion.
• Wide therapeutic range: The drug has a relatively wide therapeutic range, making it effective at different 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 approximately 9.6% due to a significant first-pass effect through the liver.

2. Distribution:

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

3. Metabolism:

   • Trospium is metabolized in the liver. The major metabolic pathway is ester hydrolysis, resulting in 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 and in patients with impaired renal or hepatic function, the pharmacokinetics of trospium may be altered, 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: Usually take 1 tablet (30 mg) 1 time per day.

General recommendations:

• Directions for use: Tablets should be taken orally with a sufficient amount of water. Tablets should be swallowed whole, without chewing.
• Time of administration: Tablets can be taken regardless of food intake, 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. Consult your physician.
• Patients with liver failure: Dosage may need to be reduced. 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 almost 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 the use of Spazmex during pregnancy:

1. Consultation with a doctor: Before starting to take 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 benefit to the mother outweighs the possible risks to the fetus.
3. First trimester: Particular attention should be paid to the use of drugs in the first trimester of pregnancy, when the formation of the organs and systems of the fetus occurs. At this time, it is especially important to avoid unnecessary use of drugs.

Contraindications

1. Hypersensitivity: The drug is contraindicated in people with known hypersensitivity or allergic reaction to trospium or any other components of the drug.
2. Closed-angle glaucoma: Spazmex may increase intraocular pressure and is therefore contraindicated in patients with uncontrolled closed-angle glaucoma.
3. Tachyarrhythmias: The use of Spazmex may aggravate tachyarrhythmias and should therefore be avoided in patients with this condition.
4. Myasthenia: 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 <30 ml/min), as the drug may accumulate in the body and cause toxic effects.
6. Severe liver failure: The drug is contraindicated in patients with severe liver dysfunction 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 stenosis and urinary retention: Spasmex is contraindicated in patients with urinary retention or significant urethral stenosis 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).
   • Abdominal pain.
   • Dry eyes.
   • Nausea.
   • Headache.
   • Fatigue.

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

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

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

   • Allergic reactions such as skin rash or itching.
   • Anaphylactic reactions.
   • Angioedema.
   • Confusion of consciousness.
   • Hallucinations.
   • Heart rhythm disturbances (eg, prolongation of the QT interval, arrhythmia).

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

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

Overdose

1. Severe dry mouth.
2. Difficulty urinating (acute urinary retention).
3. Dilation of the pupils (mydriasis).
4. Tachycardia (rapid heartbeat).
5. Arrhythmias.
6. Severe dizziness.
7. Excitement and anxiety.
8. Cramps.
9. Redness of the skin.
10. Hyperthermia (increased body temperature).
11. Severe visual impairment.
12. Confusion, hallucinations and delirium.

Treatment of overdose

Treatment for trospium overdose is aimed at relieving symptoms and supporting 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 been taken recently.
3. Activated charcoal: Using activated charcoal may help reduce the absorption of the drug from the gastrointestinal tract if a short period of time has passed since administration.
4. Symptomatic therapy: Treatment of symptoms such as tachycardia and seizures as needed. This may include beta blockers to control tachycardia or anticonvulsants for seizures.
5. Antidotes: In some cases, physostigmine may be used to counteract the anticholinergic effects, but its use should be carefully monitored because of possible 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 the pH of the stomach:

   • Antacids and other agents that alter gastric pH may interfere with the absorption of trospium.

4. Drugs that prolong the QT interval:

   • Concomitant use with drugs that prolong the QT interval (eg, 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 potential interactions with drugs that may affect other hepatic metabolic pathways.

6. Medicines excreted by the kidneys:

   • Drugs that affect renal function or compete for renal excretion may alter blood trospium concentrations. It is important to consider this 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.