Pyrenzepine (Pirenzepinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

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Included in the formulation
  • Gastrotsepin®
    pills inwards 
    Boehringer Ingelheim International GmbH     Germany
    • АТХ:

    A.02.B.X.03   Pyrenzepine

    Pharmacodynamics:

    Blocker m1-cholinoreceptors, synthetic tertiary amine. Has predominantly peripheral anticholinergic action. Reduces basal and stimulated secretion of hydrochloric acid. Reduces peptic activity of gastric juice. Slightly reduces the tone of the smooth muscles of the stomach.

    Pepsin secretion, stimulated by insulin, is reduced by 49%, histamine - by 34%, gastrin - by 24%. Oppresses the release of bicarbonate from the epithelium into the stomach cavity in patients with an erosive lesion of the antrum and enhances the protection of the gastric mucosa; increases blood flow in the submucosal layer of the stomach and intestines, improves microcirculation.

    Has no effect on the central nervous system, practically does not change the heart rate.

    In therapeutic doses, other anticholinergic effects of pyrensepine are poorly expressed.

    Pharmacokinetics:

    After oral administration pirenzepine poorly absorbed from the digestive tract. Bioavailability is 20-30%, with simultaneous intake with food - 10-20%. Binding to plasma proteins - 10-12%. Poorly penetrates the blood-brain barrier. A very small amount of pirenzepine is metabolized.

    Half-life is 10-12 hours.About 10% is excreted unchanged in the urine, the rest - with feces.
    Indications:Stomach ulcer and duodenal ulcer (treatment and prevention); chronic hyperacid reflux-esophagitis; erosive and ulcerative lesions of the gastrointestinal tract, including those caused by anti-rheumatic and anti-inflammatory drugs; Stress ulcers of the digestive tract; Zollinger-Ellison syndrome; bleeding from erosion and ulceration in the upper gastrointestinal tract.
    ICD-10

    XI.K20-K31.K27   Peptic ulcer of unspecified site

    XI.K20-K31.K26   Duodenal ulcer

    XI.K20-K31.K25   Stomach ulcer

    XI.K20-K31.K22.1   Ulcer of the esophagus

    XI.K20-K31.K21.0   Gastroesophageal reflux with esophagitis

    XI.K90-K93.K92.2   Gastrointestinal bleeding, unspecified

    Contraindications:Hypersensitivity; hyperplasia of the prostate; paralytic obstruction of the intestine, stenosis of the pylorus; I trimester of pregnancy.
    Carefully:

    Glaucoma, prostatic hyperplasia, tachycardia.

    With hepatic insufficiency. Use with caution in renal failure (risk of side effects due to slowed withdrawal).

    With rapid subjective improvement, do not stop taking it because of a possible worsening of the condition.With intravenous administration, it is necessary to monitor the state of the cardiovascular system.

    At atony of the intestine in elderly patients.

    In chronic lung diseases in children, especially young children (a decrease in bronchial secretion can lead to a thickening of the secret and the formation of congestion in the bronchi), with brain damage in children, infantile cerebral palsy, Down's disease (reaction to anticholinergic drugs is increasing).

    In patients with diseases of the cardiovascular system, in which an increase in the heart rate may be undesirable: atrial fibrillation, tachycardia, chronic heart failure, IHD, mitral stenosis, hypertension, acute bleeding; at a thyrotoxicosis (tachycardia strengthening probably is possible).

    Pregnancy and lactation:Category of recommendations FDA is not defined. Adequate and well-controlled studies in humans and animals have not been conducted. Contraindicated in the first trimester of pregnancy. It is not recommended to use in the II and III trimesters of pregnancy. If it is necessary to use during the lactation period, it should be taken into account that pirenzepine in small amounts excreted in breast milk. Like all anticholinergics, it can suppress lactation.
    Dosing and Administration:

    Inside, intramuscularly, intravenously. Inside - 50 mg in the morning and in the evening 30 minutes before a meal, squeezed a small amount of water. The course of treatment - at least 4 weeks (4-8 weeks) without interruption.

    In severe forms of peptic ulcer of the stomach and duodenum intramuscularly and intravenously, 10 mg every 8-12 hours.
    Side effects:

    From the side digestive system: dry mouth, constipation, frequent stools, increased appetite.

    From the side organ of vision: violation of accommodation; rarely - increased sensitivity of the eyes to light.

    Other: decreased sweating.

    Overdose:

    Symptoms: visual impairment, confusion, difficulty breathing, dizziness, dry mouth, nose, throat, fever, heart palpitations, hallucinations, muscle weakness, convulsive seizures, agitation.

    Treatment: intravenously slowly physostigmine 0.5-1.0 mg to a total dose of 5 mg or neostigmine methyl sulfate intramuscularly at 0.5-1.0 mg, intravenously 0.5-2.0 mg every 2-3 hours; for arresting excitation - 100 mg of thiopental sodium, with respiratory depression - oxygen, then symptomatic treatment.

    Interaction:

    Pirenzepine, used in combination with anti-inflammatory drugs, does not reduce their anti-inflammatory effect and improves their tolerability.

    Antacid and antidiarrheal (adsorbents) means - a decrease in the absorption of pyren- zepine. Avoid the use of antacids within 2-3 hours after taking pirenzepine.

    Ketoconazole, doxycycline - decrease in absorption and efficiency.

    With simultaneous use, the clinical efficacy of cimetidine is increased.

    Means with anticholinergic activity - paralytic obstruction of the intestine.

    Funds alkalinizing urine (calcium and magnesium-containing antacids, carbonic anhydrase inhibitors, citrates, sodium hydrogen carbonate) - delayed excretion of pyrensepine.

    Special instructions:

    Against the background of long-term use of pirenzepine, it is recommended to carry out a regular measurement of intraocular pressure.

    It exhibits the least pronounced antisecretory effect in comparison with the antisecretory drugs of other pharmacological groups and is not used in the world practice due to the appearance of new, more effective antisecretory drugs.

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