Novitropan

Novitropan (Oxybutynin) is a medication used to treat symptoms of overactive bladder and is often used in the treatment of neurological disorders such as neurogenic bladder dysfunction. It belongs to a class of drugs known as antimuscarinic agents, which act by blocking muscarinic-type receptors in the bladder, resulting in decreased spontaneous bladder activity and decreased urinary frequency. Novitropan may help reduce the need to urinate frequently and reduce urinary incontinence. It is available in a variety of forms, including tablets and skin patches.

Indications Novitropane

1. Overuse Abnormal Urination (OAB) Syndrome: This is a condition in which patients experience a strong urge to urinate and/or urinate with excessive frequency, which can significantly impact their quality of life.
2. Urge incontinence: Patients with this condition experience a sudden and irresistible urge to urinate, which can lead to urinary incontinence.
3. Urinary incontinence: This is a condition in which patients experience an inability to control urination, which can lead to accidents and social problems.
4. Other urologic disorders: Novitropan may also be used to treat other urologic disorders associated with overactive bladder and dysuric symptoms.

Release form

1. Tablets: Usually presented as tablets that are taken whole with a small amount of water.
2. Capsules: This is another oral (internal) form, presented in the form of capsules, which are also taken whole, with water.

Pharmacodynamics

1. Mechanism of action: Oxybutynin is an antagonist of muscarinic receptors, primarily M3 receptors, which are located in the smooth muscles of the bladder. By blocking these receptors, oxybutynin reduces the activity of the muscarinic nervous system, which leads to a decrease in spontaneous activity of the bladder and an increase in its capacity.
2. Reducing bladder spasms: Blocking muscarinic receptors in the smooth muscle of the bladder results in reduced spasms and decreased frequency of bladder contractions, which alleviates symptoms associated with the feeling of needing to urinate.
3. Increased bladder capacity: Blocking muscarinic receptors also causes the bladder walls to relax, allowing it to hold more urine before the need to urinate.
4. Reducing urinary incontinence symptoms: Through its mechanism of action, oxybutynin helps improve urinary incontinence symptoms such as urinary frequency, inability to control urination, and frequent urge to urinate.

Pharmacokinetics

1. Absorption: Oxybutynin is generally well absorbed from the gastrointestinal tract after oral administration. Peak plasma concentrations are usually achieved 1-3 hours after administration.
2. Metabolism: Oxybutynin undergoes extensive metabolism in the liver, including N-demethylation and hydroxylation, resulting in the formation of active metabolites such as N-desethyloxybutynin and N-oxyoxybutynin.
3. Bioavailability: The bioavailability of oxybutynin after oral administration is approximately 6-15% due to its significant first pass through the liver.
4. Distribution: Oxybutynin and its metabolites bind to plasma proteins to a small extent. It also penetrates the blood-brain barrier.
5. Excretion: Oxybutynin and its metabolites are excreted primarily in the urine, both as unmetabolized compounds and as metabolites. About 50% of the dose is excreted unchanged in the urine.
6. Half-life: The half-life of oxybutynin is about 2-3 hours, while for its active metabolites it may be longer.

Dosing and administration

1. Dosage: The usual starting dose recommended for adults is 2.5 mg twice daily. Your doctor may adjust the dose later based on the drug's effectiveness and tolerability. The maximum daily dose is usually no more than 5 mg twice daily.
2. Directions for use: Novitropan tablets are taken whole, usually in the morning and evening, regardless of food intake. It is not recommended to chew or split the tablets.

Use Novitropane during pregnancy

The use of Novitropan during pregnancy should be carried out only for strict medical indications and under the supervision of a physician.

To date, a limited number of studies have been conducted to evaluate the safety of oxybutynin during pregnancy. Therefore, there is insufficient data on its effects on fetal development.

If a pregnant woman needs to use Novitropan, the doctor should carefully assess the potential risks to the mother and fetus before prescribing the drug. Doctors usually recommend avoiding the use of oxybutynin in the first trimester of pregnancy due to possible risks to fetal development. If it is necessary to use it in subsequent trimesters, the doctor may decide to use it, taking into account the benefits to the mother and the risks to the fetus.

Contraindications

1. Hypersensitivity: People with known hypersensitivity or allergic reaction to oxybutynin or other components of the drug should refrain from using it.
2. Severe gastrointestinal disorders: In case of acute constipation, ulcerative colitis, obstructive bowel disorders or other serious gastrointestinal disorders, the use of oxybutynin may be undesirable.
3. Glaucoma: The drug may increase intraocular pressure, so its use is not recommended in open-angle glaucoma or in patients at risk of developing it.
4. Tachyarrhythmias: Oxybutynin may be contraindicated in patients with tachyarrhythmias because it may increase the heart rate.
5. Severe liver and kidney impairment: If you have severe liver or kidney impairment, consult your doctor before taking oxybutynin.
6. Myasthenic syndrome: Oxybutynin may be contraindicated in patients with myasthenic syndrome due to its antagonist effects on muscarinic receptors.
7. Large prostatic hypertrophy: Oxybutynin should be used with caution in patients with large prostatic hypertrophy as it may increase the risk of acute urinary retention.

Side effects Novitropane

1. Dry mouth: This is one of the most common side effects of oxybutynin. Patients may experience a feeling of dry mouth, which can lead to discomfort, difficulty speaking and swallowing, and an increased risk of developing tooth decay.
2. Constipation: Oxybutynin may cause food to pass through the intestines more slowly, which may lead to difficulty passing stool and constipation.
3. Gastrointestinal disorders: These may include nausea, vomiting, dyspepsia and abdominal pain.
4. Headache: Some patients may experience headaches while taking oxybutynin.
5. Drowsiness and fatigue: Oxybutynin may cause drowsiness or fatigue, which may impair concentration and reactions, especially during the first days of treatment or when the dosage is changed.
6. Tachycardia: Some patients may experience rapid heartbeat or palpitations while taking oxybutynin.
7. Decreased tear production: Some patients may experience decreased tear production, which can lead to dry eyes and discomfort.
8. Other rare side effects: These may include changes in appetite, dizziness, sleep disturbances, allergic reactions, etc.

Overdose

An overdose of oxybutynin can lead to serious side effects and complications. Signs of overdose may include increased symptoms of side effects such as dry mouth, constipation, visual disturbances, tachycardia, arrhythmia, drowsiness, dizziness, and others.

Interactions with other drugs

1. Anticholinergic drugs: Use of oxybutynin in combination with other anticholinergic drugs (eg, antihistamines, some antidepressants) may result in increased anticholinergic effects and an increased risk of side effects such as dry mouth, constipation, tachycardia, and difficulty urinating.
2. Drugs affecting the central nervous system: Oxybutynin may enhance the effects of other drugs that affect the central nervous system, such as sedatives, benzodiazepines and alcohol, which may lead to increased drowsiness and other undesirable effects.
3. Drugs that cause tachycardia: The combination of oxybutynin with drugs that can cause increased cardiac activity (eg, sympathomimetics) may enhance the tachycardic effects and increase the risk of cardiac arrhythmias.
4. Drugs affecting metabolism: Changes in oxybutynin metabolism may occur under the influence of other drugs, including inhibitors or inducers of cytochrome P450 isoenzymes, which may lead to an increase or decrease in the concentration of oxybutynin in the blood.
5. Drugs affecting the gastrointestinal tract: The use of oxybutynin with drugs that affect gastrointestinal motility or digestion (eg, prokinetics or antacids) may alter the rate and extent of absorption of oxybutynin from the gastrointestinal tract.