Spasmoblock, tablets, 20 pcs.

Spasmoblock is an analgesic combination medicine.

Pharmacodynamics

. Sodium metamizole, a pyrazolone derivative has analgesic, antipyretic and mild anti-inflammatory effects, whose mechanism is related to inhibition of prostaglandin synthesis.

Pitophenone is a myotropic antispasmodic that has a direct effect on the smooth muscles of internal organs and causes their relaxation. Phenpiverinia bromide – m-cholinoblocker has an additional antispasmodic effect on the smooth muscles.

Pharmacokinetics

Sodium metamizole: well and quickly absorbed from the gastrointestinal tract (GIT). In the intestinal wall it is hydrolyzed to form the active metabolite – unchanged sodium metamizole is absent in the blood (only after IV administration a small concentration is found in plasma).

The binding of the active metabolite with plasma proteins: 50-60%. Metabolized in the liver, excreted by the kidneys. In therapeutic doses penetrates into breast milk.

Pitophenone is quickly absorbed from the gastrointestinal tract; maximum concentration in plasma is reached within 30-60 minutes; it is quickly distributed in the organs and tissues and excreted rather quickly in the urine.

Half-life is 1.8 hours. Phenpivernia bromide is also quickly absorbed from the gastrointestinal tract and reaches maximum concentration in blood plasma within 1 hour. Excreted by the kidneys 32.4 – 40.4% unchanged, 2.5 – 5.3% of the substance is excreted in the bile.

Indications

Mild or moderate pain syndrome due to spasms of smooth muscles of internal organs:

renal colic,
spasm of the ureter and bladder;
biliary colic,
intestinal colic;
biliary dyskinesia of the hyperkinetic type,
postcholecystectomic syndrome,
chronic colitis,
algodismenorrhea.

For short-term treatment:

arthralgia,
myalgia,
neuralgia,
sciatica.

As an auxiliary drug: diseases of the pelvic organs, pain syndrome after surgical interventions and diagnostic procedures.

Pharmacological effect

Spasmoblock is a combined analgesic agent.

Pharmacodynamics

Metamizole sodium, a pyrazolone derivative, has an analgesic, antipyretic and weak anti-inflammatory effect, the mechanism of which is associated with inhibition of prostaglandin synthesis.

Pitophenone – a myotropic antispasmodic has a direct effect on the smooth muscles of internal organs and causes its relaxation. Fenpiverinium bromide – an m-anticholinergic blocker has an additional antispasmodic effect on smooth muscles.

Pharmacokinetics

Metamizole sodium: well and quickly absorbed from the gastrointestinal tract (GIT). It is hydrolyzed in the intestinal wall to form an active metabolite – unchanged metamizole sodium is absent in the blood (only after intravenous administration a small concentration is detected in the plasma).

Connection of the active metabolite with plasma proteins: 50-60%. Metabolized in the liver, excreted by the kidneys. In therapeutic doses it passes into breast milk.

Pitophenone is rapidly absorbed from the gastrointestinal tract; maximum plasma concentration is achieved within 30 – 60 minutes; quickly distributed in organs and tissues and quickly excreted in the urine.

The half-life is 1.8 hours. Phenpivernnia bromide is also rapidly absorbed from the gastrointestinal tract and reaches maximum plasma concentrations within 1 hour. 32.4 – 40.4% of the substance is excreted by the kidneys unchanged, 2.5 – 5.3% of the substance is excreted with bile.

Special instructions

Metamizole sodium metabolite can cause red coloration of urine, which has no clinical significance and disappears after discontinuation of the drug.

If agranulocytosis is suspected or thrombocytopenia is present, the drug should be discontinued.

With long-term (more than a week) use of the drug, monitoring of the peripheral blood picture and the functional state of the liver is necessary.

It is not permissible to use it to relieve acute abdominal pain (until the cause is determined). Patients with atonic bronchial asthma and hay fever have an increased risk of developing allergic reactions. During the period of use of the drug, you should not drink alcohol.

Impact on the ability to simplify vehicles and mechanisms

While taking the drug, it is not recommended to drive vehicles or engage in other potentially hazardous activities that require rapid psychomotor reactions.

Active ingredient

Metamizole sodium, Pitophenone, Fenpiverinium bromide

Composition

1 tablet contains:

active ingredients:

metamizole sodium monohydrate 527 mg in terms of metamizole sodium 500 mg,

pitofenone hydrofloride 5.25 mg equivalent to pitofenone 5 mg and fenpivirinium bromide 0.1 mg.

excipients:

wheat starch,

microcrystalline cellulose,

talc,

sodium bicarbonate,

lactose monohydrate,

gelatin and magnesium stearate.

Pregnancy

Contraindicated in children under 8 years of age, during pregnancy and lactation.

Contraindications

hypersensitivity to any of the medicinal and/or excipients of Spazmoblok (including pyrazolone derivatives),
inhibition of bone marrow hematopoiesis,
severe liver and/or renal failure,
glucose-6-phosphate dehydrogenase deficiency,
lactase deficiency.
lactose intolerance,
glucose-galactose malabsorption,
tachyarrhythmias,
severe angina,
angle-closure glaucoma,
prostatic hyperplasia (with clinical manifestations),
intestinal obstruction,
megacolon,
collapse.

The drug should be used with caution and under the supervision of a physician in case of impaired liver or kidney function, with a tendency to arterial hypotension, bronchospasm, hypersensitivity to non-steroidal anti-inflammatory drugs, a complete or incomplete combination of bronchial asthma, nasal polyposis and intolerance to acetylsalicylic acid and other non-steroidal anti-inflammatory drugs.

Side Effects

From the digestive system: very rarely – burning sensation in the epigastric region, dry mouth.

From the cardiovascular system: rarely – decreased blood pressure (BP), tachycardia.

From the hematopoietic system: very rarely (usually with long-term use) – thrombocytopenia, leukopenia, agranulocytosis (may be manifested by the following symptoms: unmotivated rise in temperature, chills, sore throat, difficulty swallowing, stomatitis, as well as the development of vaginitis or proctitis). From the urinary system: rarely (usually with long-term use or when prescribed in high doses) – impaired renal function, oliguria, anuria, proteinuria, interstitial nephritis, red staining of urine, difficulty urinating.

Allergic reactions: rarely – urticaria (including on the conjunctiva and mucous membranes of the nasopharynx), very rarely – angioedema, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), bronchospastic syndrome, anaphylactic shock.

Other: possible dizziness; very rarely decreased sweating, accommodation paresis; in isolated cases – headache.

Interaction

The simultaneous use of Spasmoblock with other non-opioid analgesics can lead to mutually enhanced effects.

When used simultaneously, tricyclic antidepressants, oral contraceptives, and allopurinol disrupt the metabolism of metamizole sodium in the liver and increase its toxicity.

When used simultaneously, barbiturates, phenylbutazone and other inducers of microsomal liver enzymes weaken the effect of metamizole sodium.

X-ray contrast agents, colloidal blood substitutes and penicillins should not be used during treatment with drugs containing metamizole sodium.

With simultaneous use of cyclosporine, the concentration of the latter in the blood decreases. Metamizole sodium, displacing oral hypoglycemic drugs, indirect anticoagulants, glucocorticosteroids and indomethacin from its binding to plasma proteins, can increase the severity of their action.

When used simultaneously, sedatives and tranquilizers enhance the analgesic effect of Spasmoblock.

When used simultaneously with H1-histamine receptor blockers, butyrophenone and phenothiazine derivatives, amantadine and quinidine, the m-cholinergic effect of the drugs may be enhanced.

When used simultaneously with ethanol, mutual enhancement of effects is possible.

Overdose

Symptoms: vomiting, decreased blood pressure, drowsiness, confusion, nausea, pain in the epigastric region, impaired liver and kidney function, convulsions.

Treatment: gastric lavage, taking activated carbon, symptomatic therapy.

Storage conditions

In a place protected from light, at a temperature not exceeding 25 °C

Shelf life

3 years.

Manufacturer

Adifarm EAD, Bulgaria