Spasmex, 15 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

Intake and distribution

The 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%. The plasma concentration of trospium chloride with a single oral administration of 20-60 mg is proportional to the dose taken.

Metabolism and excretion

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

Indications

• Hyperactivity of the bladder, accompanied by urinary incontinence, imperative urge to urination and increased frequency of urination (in idiopathic detrusor hyperactivity of non-hormonal and inorganic etiology);
• mixed forms of urinary incontinence;
• spastic neurogenic disorders of bladder function: In neurogenic hyperactivity (hyperreflexia) of the detrusor (multiple sclerosis, spinal injuries, congenital and acquired diseases of the spinal cord, strokes, parkinsonism);
• pollakiuria;
• nicturia;
• night-time and daytime enuresis;
• in complex therapy of cystitis accompanied by imperative symptoms.

.

Active ingredient

Trospium chloride

Composition

Each coated tablet contains:

Active ingredients:

trospium chloride – 15 mg.

Excipients – lactose monohydrate,

microcrystalline cellulose,

sodium starch glycolate,

corn starch,

stearic acid,

povidone (K 25),
<
colloidal silicon dioxide,

hypromellose,

titanium dioxide.

How to take, the dosage

Inhaled before meals, without chewing and with plenty of water. For adults and children from 14 years old the drug is prescribed individually, depending on the clinical picture and severity of the disease. The drug is taken 1/2 tablet 3 times a day or 1 tablet in the morning and 1/2 tablet in the evening (45 mg).

In patients with renal insufficiency

In patients with renal insufficiency (creatinine clearance 10-30 ml/min/1.73 m²), the daily dose of the drug should not exceed 15 mg. On average, the duration of treatment is 2-3 months. If longer treatment is necessary, continuation of treatment is reconsidered by the physician every 3-6 months.

Interaction

In concomitant use trospium chloride increases the m-cholinoblocking effect of amantadine, tricyclic antidepressants, quinidine and disopyramide, antihistamine drugs, as well as the positive chronotropic effect of beta-adrenomimetics.

Trospium chloride weakens the effect of prokinetics (metoclopramide and cisapride); it affects the motor and secretory functions of the gastrointestinal tract, changing absorption of simultaneously used drugs.

Concomitant administration of drugs containing such substances as guar, colestyramine and colestipol may reduce absorption of trospium chloride.

The interaction between trospium chloride and cytochrome P450 isoenzymes (CYP1A2, 2A6, 2C9, 2C19, 2D6, 2E1, WA4) has not been found, because trospium chloride is only metabolized in small amounts by them, and hydrolysis of esters is the main route of its metabolism.

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 and operate vehicles and other mechanisms requiring high concentration

At the beginning of treatment, when increasing the dose of the drug, changing the drug, and when interacting with alcohol, vision loss may occur, which should be considered when driving vehicles and operating moving mechanisms.

Contraindications

With caution:

cardiovascular diseases in which increased heart rate may be undesirable: tachycardia, chronic heart failure, coronary heart disease; thyrotoxicosis, elevated body temperature; reflux esophagitis, esophageal hernia combined with reflux esophagitis; gastrointestinal tract diseases accompanied by obstructive conditions achalasia and gateway stenosis; intestinal atony in elderly or debilitated patients, paralytic bowel obstruction; diseases with elevated intraocular pressure: closed-angle and open-angle glaucoma; chronic inflammatory bowel disease (Crohn’s disease, ulcerative colitis); dry mouth; renal failure; chronic lung disease, especially in frail patients; autonomic (autonomic) neuropathy; pregnancy toxicity; infantile cerebral palsy; Down’s disease.

Side effects

Prevalence of side effects (number of cases: number of observations):

• frequent – more than 1:100;
• infrequent – 1:100-1000;
• rarely – less than 1:1000.

Cardiovascular system: infrequent – tachycardia; rare – 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.

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 – for patients with glaucoma, bladder catheterization – for urinary retention. In severe cases cholinomimetics (neostigmine methyl sulfate) are prescribed. If the effect is insufficient, marked tachycardia and/or circulatory instability, intravenous beta-adrenoblockers are administered under control of ECG and blood pressure.

Pregnancy use

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