Spazmex

Pharmacodynamics

Trospia chloride is a quaternary ammonium base, belongs to the group of m-anticholinergics. It is a competitive antagonist of acetylcholine at the receptors of postsynaptic membranes of smooth muscles. It has a high affinity for m 1 - and m 3 - cholinergic receptors. Reduces increased activity of the bladder detrusor. It has an antispasmodic and some ganglioblocking effect. It does not have central effects.

Pharmacokinetics

Suction and distribution

The maximum concentration of trospium chloride in blood plasma (C _max ) is achieved 4-6 hours after oral administration of trospium chloride; the half-life (T _1/2 ) averages 5-18 hours, does not cumulate. Binding to plasma proteins is 50-80%. The concentration of trospium chloride in blood plasma with a single oral administration of 20-60 mg is proportional to the dose taken.

Metabolism and excretion

The predominant amount of trospium chloride is excreted by the kidneys unchanged, a smaller part (about 10%) - in the form of a spiro-alcohol metabolite formed during the hydrolysis of ether bonds.

• Bladder hyperactivity, accompanied by urinary incontinence, imperative urination and an increase in urination frequency (with idiopathic hyperactivity detrusor non-hormonal and inorganic etiology);
• mixed forms of urinary incontinence;
• spastic neurogenic disorders of the bladder function: with neurogenic hyperactivity (hyperreflexia) of the detrusor (multiple sclerosis, spinal injuries, congenital and acquired diseases of the spinal cord, strokes, parkinsonism);
• detrusor-sphincter-dysinergy against the background of intermittent catheterism;
• pollakiuria;
• nocturia;
• night and day enuresis;
• in the complex treatment of cystitis, accompanied by imperative symptoms.

During pregnancy and during breastfeeding, the drug should be used if the intended benefit to the mother outweighs the potential risk to the fetus or baby.

• Hypersensitivity to the drug, the components of the drug;
• urinary retention;
• narrow angle glaucoma;
• tachyarrhythmia;
• myasthenia gravis;
• age up to 14 years (adequate strictly controlled studies of the use of trospium chloride in children have not been conducted). 

Incidence of side effects (number of cases: number of cases):

• often - more than 1: 100;
• infrequently - 1: 100-1000;
• rarely - less than 1: 1000.

From the cardiovascular system: infrequently - tachycardia; rarely - pain behind the sternum, fainting tachyarrhythmia, hypertensive crisis.

From the gastrointestinal tract: often - dry mouth, dyspepsia, constipation, nausea, abdominal pain; infrequently - diarrhea, bloating; rarely gastritis.

From the respiratory system: infrequently - shortness of breath.

From the nervous system: rarely - confusion, hallucinations.

From the musculoskeletal system: rarely - acute skeletal muscle necrosis.

From the side of the organ of vision: infrequently - violation of accommodation.

From the urinary system: infrequently - violation of the emptying of the bladder; rarely - urinary retention.

From the hepatobiliary system: rarely - a small or moderate increase in the activity of transaminases.

From the immune system: infrequently - skin rash; rarely - anaphylactic reactions, Stevens-Johnson syndrome.

With the simultaneous use of trospia chloride enhances the m-anticholinergic effect of amantadine, tricyclic antidepressants, quinidine and disopyramide, antihistamines, as well as the positive chronotropic effect of beta-adrenergic agonists.

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

With the simultaneous administration of preparations containing substances such as guar, colestyramine and colestipol, a decrease in the absorption of trospium chloride is possible.

No interaction was found between trospium chloride and isoenzymes of cytochrome P450 (CYP1A2, 2A6, 2C9, 2C19, 2D6, 2E1, ZA4), since trospium chloride is metabolized by them only in a small amount, and hydrolysis of esters is the main route of its metabolism.

Inside, before meals, without chewing and drinking plenty of water. Adults and children from 14 years of age are prescribed the drug 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 failure

In patients with renal failure (creatinine clearance of 10-30 ml / min / 1.73 m ² ), 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, the question of continuing treatment is reviewed by the doctor every 3-6 months.

Symptoms: signs of an overdose are increased anticholinergic symptoms, such as: visual disturbances, tachycardia, dry mouth and flushing of the skin.

Treatment: gastric lavage and intake of adsorbents (activated carbon, etc.), instillation of pilocarpine in patients with glaucoma, catheterization of the bladder with urinary retention. In severe cases, cholinomimetics are prescribed (neostigmine methyl sulfate). With insufficient effect, pronounced tachycardia and / or instability of blood circulation, beta-blockers are administered intravenously under the control of ECG and blood pressure.

Taking the drug in case of dysfunction of the internal sphincter of the urethra or detrusor of the bladder should be accompanied by its complete release by catheterization.

In autonomic disorders of the bladder, the cause of the dysfunction should be determined before treatment, the organic causes of pollakiuria, nocturia and urinary incontinence, such as heart failure, polydipsia, the possibility of urinary tract infection and bladder cancer, are excluded, since they require the appointment of etiotropic therapy.

Influence on the ability to drive vehicles and other mechanisms requiring increased concentration of attention

At the beginning of treatment, with an increase in the dose of the drug, replacement of the drug, as well as in interaction with alcohol, visual impairment is possible, which should be considered when driving vehicles and working with moving mechanisms.

Pills