Spasmex, pills 30mg, 30pcs

Composition

1 coated tablet contains:

Active ingredient:

trospium chloride – 30 mg.

Auxiliary substances:

lactose monohydrate,

microcrystalline cellulose,

sodium starch glycolate

, corn starch,

stearic acid,

povidone K 25,

colloidal silicon dioxide,

hypromellose,

titanium dioxide.

Shell composition:

hypromellose, titanium dioxide, microcrystalline cellulose, stearic acid.

Pharmacological action

Pharmacodynamics

Trospium chloride is a quaternary ammonium base, belongs to the group of m-holinoblockers. It is a competitive antagonist of acetylcholine at the receptors of postsynaptic smooth muscle membranes. It has a high affinity for m1-and m3-cholinergic receptors. Reduces the increased activity of the bladder detrusor. It has an antispasmodic and some ganglioblocking effect. It doesn’t have any central effects.

Pharmacokinetics

Suction and distribution

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

Metabolism and elimination

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

Indications

• Hyperactivity of the bladder, accompanied by urinary incontinence, imperative urination and increased frequency of urination (idiopathic detrusor hyperactivity non-hormonal and non-organic etiology);
• mixed urinary incontinence;
• spastic neurogenic dysfunction of the bladder: neurogenic hyperactivity disorder (hyperreflexia) detrusor (multiple sclerosis, spinal injury, congenital and acquired diseases of the spinal cord, stroke, Parkinsons);
• the detrusor-sphincter-dyssynergia on the background of intermittent catheterism;
• pollakiuria;
• nocturia;
• day and night enuresis;
• in the complex therapy of cystitis accompanied by a peremptory symptoms.

Use during pregnancy and lactation

During pregnancy and lactation, the drug should be used if the intended benefit to the mother exceeds the potential risk to the fetus or child.

Contraindications

With caution:  diseases of the cardiovascular system in which an increase in heart rate may be undesirable: tachycardia, chronic heart failure, ischemic heart disease; thyrotoxicosis, elevated body temperature; reflux esophagitis, hiatal hernia combined with reflux esophagitis; diseases of the gastrointestinal tract accompanied by obstructive conditions: achalasia and pyloric stenosis; intestinal atony in elderly or weakened patients diseases with increased intraocular pressure: angle-closure and open-angle glaucoma; chronic inflammatory bowel diseases (Crohn’s disease, ulcerative colitis); dry mouth; renal failure; chronic lung diseases, especially in weakened patients; autonomic neuropathy; pregnancy toxicosis; cerebral palsy; Down’s disease.

Side effects

Frequency of occurrence of side effects (number of cases: number of observations):

• 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, syncope 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.

Nervous system disorders: rarely-confusion, hallucinations.

Musculoskeletal disorders: rare-acute skeletal muscle necrosis.

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

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

From the side of the hepatobiliary system: rarely-a slight or moderate increase in transaminase activity.

Immune system disorders: infrequently-skin rash; rarely-anaphylactic reactions, Stevens-Johnson syndrome.

Interaction

When used concomitantly, trospium chloride enhances the m-holinoblocking effect of amantadine, tricyclic antidepressants, quinidine and disopyramide, antihistamines, 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 the absorption of drugs used simultaneously.

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

No interaction was found between trospium chloride and cytochrome P 450 isoenzymes (CYP1A2,2A6,2C9,2C19,2D6,2E1A4), since trospium chloride is metabolized by them only in small amounts, and hydrolysis of esters is the main route of its metabolism.

How to take, course of use and dosage

Inside, before eating, without chewing and drinking enough 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 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 required, the doctor reviews whether to continue treatment every 3-6 months.

Overdose

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

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

Special instructions

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

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

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

At the beginning of treatment, when increasing the dose of the drug, replacing the drug, as well as when interacting with alcohol, vision loss may occur, which should be taken into account when driving vehicles and working with moving mechanisms.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature of 15-25 °C

Shelf life

5 years

Active ingredient

Trospium chloride

Conditions of release from pharmacies

By prescription

Dosage form

Tablets