Spasmex, tablets 5 mg 30 pcs

Pharmacodynamics

Trospium chloride is a quaternary ammonium base, belongs to the group of m-cholinoblockers. It is a competitive antagonist of acetylcholine at the receptors of postsynaptic membranes of smooth muscles. It has high affinity to m 1 – and m 3 -cholinoreceptors. Reduces increased activity of the detrusor of the bladder. It has antispasmodic and some ganglioblocking effects. It has no central effects.

Pharmacokinetics

Absorption and distribution

Maximum plasma concentration of trospium chloride (C max ) is reached 4-6 hours after oral administration of trospium chloride; elimination half-life (T 1/2 ) averages 5-18 hours, does not cumulate. Binding to plasma proteins is 50-80%. Plasma concentration of trospium chloride when administered orally in a single dose of 20-60 mg is proportional to the dose taken.

Metabolism and excretion

The prevailing amount of trospium chloride is excreted unchanged by kidneys, a smaller part (about 10%) – as spiroalcohol metabolite formed during hydrolysis of ester bonds.

Indications

• Incontinence of urine, imperative urge to urination (in idiopathic detrusor hyperresponsiveness; in detrusor neurogenic hyperactivity (hyperreflexia) against the background of multiple sclerosis, spinal injuries, congenital and acquired spinal cord diseases, strokes, Parkinsonism).
• Detrusor-sphincter-dyssynergy on the background of intermittent catheterism.
• In the complex therapy of cystitis accompanied by imperative symptoms.
• Pollakiuria, nycturia.
• Night-time and daytime enuresis.
• Mixed forms of urinary incontinence.

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Active ingredient

Trospium chloride

Composition

Active ingredient:

tropium chloride – 5 mg.

Auxiliary substances:

Lactose monohydrate,

Microcrystalline cellulose, <

sodium starch glycolate,

corn starch,

stearic acid,

povidone K25,

Colloidal silicon dioxide,

Hypromellose,

Titanium dioxide.

Composition of the shell:

hypromellose, titanium dioxide, microcrystalline cellulose, stearic acid.

How to take, the dosage

The dosing regimen and duration of treatment are set individually depending on the clinical picture and the severity of the disease.

The tablets should be taken before meals, without chewing, with plenty of water.

Adults and adolescents 14 years of age and older are prescribed orally 10 mg 3 times daily (daily dose of 30 mg) or 15 mg 2-3 times daily (daily dose of 30-45 mg).

In a daily dose of 45 mg, 30 mg in the morning and 15 mg in the evening may be used.

In detrusor neurogenic hyperactivity

In detrusor neurogenic hyperactivity, 15-20 mg twice daily in the morning and evening (daily dose 30-40 mg).

The duration of treatment is, on average, 2-3 months.

After symptoms have disappeared, it is recommended that a 2-4 week period of contraceptive treatment be carried out.

If longer treatment is necessary, continuation of therapy should be reconsidered every 3-6 months.

Perhaps with renal impairment

In patients with renal impairment (creatinine clearance 10-30 ml/min/1.73 m 2 ) the daily dose of the drug is 20 mg.

Interaction

The interaction with drugs influencing the system of cytochrome P 450 isoenzymes is not expected, because no interaction of trospium chloride with CYP1A2, CYP2A6, CYP3C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4 isoenzymes, involved in the breakdown of drugs in metabolism, was found.

In concomitant use of trospium chloride increases anticholinergic effect of amantadine, tricyclic antidepressants, quinidine, antihistamines, disopyramide, beta-adrenergic stimulants.

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Special Instructions

In case of dysfunction of the internal urethral sphincter or bladder detrusor, administration of the drug should be accompanied by its complete release by catheterization.

In autonomic bladder dysfunction, the cause of the dysfunction must be determined before starting treatment and organic causes of pollakiuria, nicturia and urinary incontinence, such as: heart failure, polydipsia, possible urinary tract infection and bladder cancer, must be excluded, as they require etiotropic therapy.

Impact on ability to drive vehicles and other mechanisms requiring high concentration

In the beginning of treatment, when increasing the dose of the drug, changing the drug, as well as when interacting with alcohol, visual impairment may occur, which should be considered when driving vehicles and operating moving mechanisms.

Contraindications

• painful urinary retention,
• glaucoma,
• delayed gastric evacuation and conditions predisposing to their development
• renal insufficiency requiring dialysis (creatinine clearance (CK) < 10 ml/min/1.73 m 2 );
• nonperipenic haemorrhage.Renal failure requiring dialysis (creatinine clearance (CK) < 10 ml/min/1.73 m 2 );
• Galactose intolerance;
• High sensitivity to Spasmix.

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Side effects

Cardiovascular system: infrequent – tachycardia; rarely – pain in the chest, fainting tachyarrhythmia, hypertensive crisis.

Gastrointestinal tract: frequently – dry mouth, dyspepsia, constipation, nausea, abdominal pain; infrequently – diarrhea, bloating; rarely – gastritis.

Respiratory system: infrequent – shortness of breath.

Nervous system disorders: rarely – confusion, hallucinations.

Motor system disorders: rarely – acute necrosis of skeletal muscles.

An organ of vision: infrequent – accommodation disorder.

The urinary system: infrequent – disorders of bladder emptying; rarely – urinary retention.

Hepatobiliary system: rarely – slight or moderate increase in transaminase activity.

The immune system: infrequent – skin rash; rarely – anaphylactic reactions, Stevens-Johnson syndrome.

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Overdose

Symptoms: signs of overdose are intensification of anticholinergic symptoms, such as: visual disturbances, tachycardia, dry mouth and skin hyperemia.

Treatment: gastric lavage and administration of adsorbents (activated charcoal, etc.), pilocarpine instillation – in patients with glaucoma, bladder catheterization – in case of urinary retention.

In severe cases cholinomimetics (neostigmine methyl sulfate) are prescribed. If the effect is insufficient, severe tachycardia and/or circulatory instability, intravenous beta-adrenoblockers are administered under control of ECG and blood pressure.

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Pregnancy use

In pregnancy and during breastfeeding the drug should be used if the estimated benefit to the mother exceeds the potential risk to the fetus or child.

It is contraindicated in children under 14 years of age.

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