Pharmacodynamics and pharmacokinetics
Platyphylline Hydrotartrate is characterized by a cholinolytic effect: by blocking M-choline receptors , it converts them into forms insensitive to acetylcholine . Due to the direct myotropic antispasmodic effect on the smooth muscles of the intestines, bile ducts, bronchi and eyes, it is considered a papaverine-like agent . In addition, it has a mild direct inhibitory effect on vascular smooth muscle, a calming effect on the central nervous system, especially on the vasomotor center, providing vasodilatory and hypotonic effects.
Platyphylline Hydrotartrate is well absorbed from the subcutaneous layer of the epidermis . However, the administration of large doses causes its accumulation in the tissues of the central nervous system in significant concentrations. It is excreted through the urinary as well as the digestive system.
Platifillina h/t (amp. 0.2% 1ml No. 10 (5x2))
A country
Russia
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Compound
For 1 ml of platyphylline hydrotartrate 2 mg.
pharmachologic effect
M-cholinergic receptor blocker. Compared to atropine, it has a less pronounced effect on peripheral m-cholinergic receptors (the effect on smooth muscle cells of the gastrointestinal tract and circular muscle of the iris is 5-10 times weaker than atropine). By blocking m-cholinergic receptors, it disrupts the transmission of nerve impulses from postganglionic cholinergic nerves to the effector organs and tissues innervated by them (heart, smooth muscle organs, exocrine glands); also suppresses n-cholinergic receptors (much weaker). The anticholinergic effect is more pronounced against the background of increased tone of the parasympathetic part of the autonomic nervous system or the action of m-anticholinergic stimulants. To a lesser extent than atropine, it causes tachycardia, especially when used in high doses. By reducing the influence of n.vagus, it improves cardiac conductivity, increases myocardial excitability, and increases cardiac output. It has a direct myotropic antispasmodic effect and causes dilation of small blood vessels in the skin. In high doses, it inhibits the vasomotor center and blocks the sympathetic ganglia, as a result of which the blood vessels dilate and blood pressure decreases (mainly with intravenous administration). Weaker than atropine, it inhibits the secretion of endocrine glands; causes a marked decrease in smooth muscle tone, amplitude and frequency of peristaltic contractions of the stomach, duodenum, small and large intestine, a moderate decrease in gallbladder tone (in persons with hyperkinesia of the biliary tract); with hypokinesia, the tone of the gallbladder increases to normal. Causes relaxation of the smooth muscles of the uterus, bladder and urinary tract; Providing an antispasmodic effect, it eliminates pain. Relaxes the smooth muscles of the bronchi caused by increased tone of the n.vagus or cholinergic stimulants, increases the volume of breathing, inhibits the secretion of the bronchial glands; reduces sphincter tone. When instilled into the conjunctival sac of the eye and parenterally administered, it causes pupil dilation due to relaxation of the orbicularis muscle of the iris. At the same time, intraocular pressure increases and paralysis of accommodation occurs (relaxation of the ciliary muscle of the ciliary body). Compared to atropine, the effect on accommodation is less pronounced and shorter. Stimulates the brain and respiratory center, and to a greater extent the spinal cord (in high doses, convulsions and depression of the central nervous system, vasomotor and respiratory centers are possible). Penetrates through the BBB.
Indications for use
Peptic ulcer of the stomach and duodenum, pylorospasm, cholecystitis, cholelithiasis, intestinal colic, renal colic, biliary colic; bronchial asthma (to prevent broncho- and laryngospasm), bronchorrhea; algodismenorrhea; spasm of the cerebral arteries; angiotrophoneurosis; arterial hypertension, angina pectoris (as part of combination therapy). Dilation of the pupil for diagnostic purposes (including examination of the fundus, determination of the true refraction of the eye); acute inflammatory eye diseases (including iritis, iridocyclitis, keratitis), eye injuries.
Mode of application
Used orally, parenterally (s.c., i.v.), rectally, locally in ophthalmology. The dose depends on the indications, route of administration, and age of the patient.
Interaction
When used simultaneously with haloperidol in patients with schizophrenia, the antipsychotic effect may be reduced. Platyphylline is an antagonist of proserine. With simultaneous use, the duration of the hypnotic effect of phenobarbital, sodium etaminal, and magnesium sulfate increases. When used simultaneously with other m-anticholinergic blockers, as well as with drugs that have m-anticholinergic activity (including amantadine, haloperidol, phenothiazine, MAO inhibitors, tricyclic antidepressants, some antihistamines), the risk of side effects increases. Morphine enhances the inhibitory effect of platyphylline on the cardiovascular system. When used simultaneously with MAO inhibitors, a positive chrono- and bathmotropic effect is observed; with cardiac glycosides - a positive bathmotropic effect. For pain associated with spasms of smooth muscles, the effect of platiphylline is enhanced by analgesics, sedatives and anxiolytics, and for vascular spasms - antihypertensive and sedatives.
Side effect
From the digestive system: dry mouth, thirst, intestinal atony. From the cardiovascular system: decreased blood pressure, tachycardia. From the central nervous system and peripheral nervous system: central nervous system excitation, dizziness, dilated pupils, accommodation paralysis, headache, photophobia, convulsions, acute psychosis. From the urinary system: difficulty urinating, urinary retention. Other: pulmonary atelectasis. Adverse reactions are most likely when using platyphylline in high doses.
Contraindications
Hypersensitivity to platiphylline.
special instructions
Use with caution in patients with diseases of the cardiovascular system, in which an increase in heart rate may be undesirable: atrial fibrillation, tachycardia, chronic heart failure, coronary artery disease, mitral stenosis, arterial hypertension, acute bleeding; with thyrotoxicosis (possible increased tachycardia); elevated temperature (may further increase due to suppression of the activity of the sweat glands); with reflux esophagitis, hiatal hernia, combined with reflux esophagitis (decreased motility of the esophagus and stomach and relaxation of the lower esophageal sphincter can slow down gastric emptying and increase gastroesophageal reflux through the sphincter with impaired function); for gastrointestinal diseases accompanied by obstruction - achalasia of the esophagus, pyloric stenosis (possibly decreased motility and tone, leading to obstruction and retention of gastric contents), intestinal atony in elderly or debilitated patients (possible development of obstruction), paralytic ileus; with an increase in intraocular pressure - closed-angle (mydriatic effect, leading to an increase in intraocular pressure, can cause an acute attack) and open-angle glaucoma (mydriatic effect can cause a slight increase in intraocular pressure; adjustment of therapy may be required); with nonspecific ulcerative colitis (high doses can inhibit intestinal motility, increasing the likelihood of paralytic intestinal obstruction, in addition, the manifestation or exacerbation of such a severe complication as toxic megacolon is possible); with dry mouth (long-term use may cause further increase in the severity of xerostomia); with liver failure (decreased metabolism) and renal failure (risk of side effects due to decreased excretion); for chronic lung diseases, especially in young children and weakened patients (a decrease in bronchial secretion can lead to thickening of secretions and the formation of plugs in the bronchi); with myasthenia gravis (the condition may worsen due to inhibition of the action of acetylcholine); prostatic hypertrophy without urinary tract obstruction, urinary retention or predisposition to it, or diseases accompanied by urinary tract obstruction (including bladder neck due to prostatic hypertrophy); with gestosis (possibly increased arterial hypertension); brain damage in children (CNS effects may be enhanced); Down's disease (possibly unusual pupil dilation and increased heart rate), cerebral palsy (reaction to anticholinergic drugs may be more pronounced). Influence on the ability to drive vehicles and operate machinery. It is necessary to refrain from potentially hazardous activities that require increased attention and speed of psychomotor reactions.
Dispensing conditions in pharmacies
On prescription
Indications for use
Used for functional disorders of the digestive tract, including spasm of smooth muscles, gastric and duodenal ulcers , colic (intestinal, hepatic and renal).
In addition, the remedy is effective for diseases such as cholecystitis , bronchial asthma , hypertension or angina pectoris , bradycardia with arrhythmia , cerebral vasospasm , diarrhea , pain due to pancreatitis , biliary dyskinesia , inflammation of the esophageal mucosa.
It is used for poisoning with substances such as acetone , boric acid , strong acids, arsenic , reserpine .
Used in diagnostic ophthalmology (examination of the fundus and determination of eye refraction) and in the treatment of keratitis , iritis , iridocyclitis , various eye injuries, in rare cases it is used to dilate the pupil.
Platyphylline hydrotartrate, 2 mg/ml, solution for subcutaneous administration, 1 ml, 10 pcs.
Increased individual sensitivity, pregnancy, lactation.
Carefully
Diseases of the cardiovascular system in which an increase in heart rate (HR) may be undesirable: atrial fibrillation, tachycardia, chronic heart failure, coronary heart disease, mitral stenosis, arterial hypertension, acute bleeding.
Hyperthyroidism (possibly increased tachycardia).
Increased body temperature (may further increase due to suppression of the activity of the sebaceous glands).
Reflux esophagitis, hiatal hernia, combined with reflux esophagitis (decreased motility of the esophagus and stomach and relaxation of the lower esophageal sphincter can slow down gastric emptying and increase gastroesophageal reflux through the sphincter with impaired function).
Diseases of the gastrointestinal tract accompanied by obstruction: achalasia and pyloric stenosis (possibly decreased motility and tone, leading to obstruction and retention of gastric contents).
Intestinal atony in elderly or debilitated patients (possible development of obstruction), paralytic intestinal obstruction.
Diseases with increased intraocular pressure: closed-angle glaucoma (mydriatic effect, leading to an increase in intraocular pressure, can cause an acute attack), open-angle glaucoma (mydriatic effect can cause a slight increase in intraocular pressure; adjustment of therapy may be required), age over 40 years (the risk of manifestation is not diagnosed glaucoma).
Nonspecific ulcerative colitis (high doses can inhibit intestinal motility, increasing the likelihood of paralytic ileus; in addition, the manifestation or exacerbation of a complication such as toxic megacolon is possible).
Dryness of the oral mucosa (long-term use may cause a further increase in the severity of xerostomia).
Liver failure (decreased metabolism) and renal failure (risk of side effects due to decreased excretion).
Chronic lung diseases, especially in young children and weakened patients (a decrease in bronchial secretion can lead to thickening of secretions and the formation of plugs in the bronchi).
Myasthenia gravis (condition may worsen due to acetylcholine inhibition).
Autonomic (autonomic) neuropathy (urinary retention and paralysis of accommodation may increase), prostatic hyperplasia without urinary tract obstruction, urinary retention or predisposition to it, or diseases accompanied by urinary tract obstruction (including bladder neck due to prostatic hyperplasia) .
Preeclampsia (possibly increased arterial hypertension).
Brain damage in children (central nervous system effects may be enhanced).
Down syndrome (possibly unusually dilated pupils and increased heart rate).
Central paralysis in children (the reaction to anticholinergic drugs may be most pronounced).
Instructions for use (Method and dosage)
Used orally, parenterally (subcutaneously, intravenously), rectally or topically.
Platiphylline Hydrotartrate is used intramuscularly if necessary - prescribed and adjusted by the attending physician, who is responsible for this prescription. The dose is determined depending on the symptoms and degree of the disease, route of administration and age of the patient.
Platyphylline Hydrotartrate is usually prescribed for the treatment of:
- Relief of acute ulcerative pain , intestinal, hepatic or renal colic, prolonged attacks of bronchial asthma , cerebral and peripheral vasospasms for adults - 1-2 ml 1 or 2 times a day.
- As an antispasmodic for adults - 1 ml daily for one month. The maximum single dose for an adult subcutaneously is 10 mg, no more than 30 mg per day.
Overdose
Clinical picture of an overdose of Platiphylline Hydrotartrate:
- dry mouth;
- increase in heart rate and decrease in blood pressure;
- dilated pupils and lack of reaction to light;
- paresis of accommodation;
- acute difficulty urinating;
- intestinal paresis;
- convulsions;
- dyspnea;
- hyperthermia and redness of the skin;
- stimulation of the central nervous system with its subsequent depression;
- various disturbances of consciousness, including hallucinations ;
- respiratory failure.
Measures taken in this case: forced diuresis, use of cholinesterase (for example Physostigmine , Galantamine or Proserin ) to weaken intestinal paresis and reduce tachycardia.
If the excitation of the central nervous system is moderate and the convulsions are not pronounced, then it is recommended to use magnesium sulfate , in severe conditions - sodium hydroxybutyrate , oxygen therapy , and artificial ventilation .
Platyfillin
Use during pregnancy and breastfeeding
There are no data on the safety of platiphylline during pregnancy and lactation (breastfeeding).
Use for liver dysfunction
Use with caution in case of liver failure.
Use for renal impairment
Use with caution in case of renal failure (risk of side effects due to decreased excretion).
Use in children
Use with caution for chronic lung diseases in young children (a decrease in bronchial secretion can lead to thickening of secretions and the formation of plugs in the bronchi); brain damage in children (CNS effects may be enhanced); Down's disease (possibly unusual pupil dilation and increased heart rate), cerebral palsy (reaction to anticholinergic drugs may be more pronounced).
special instructions
Use with caution in patients with diseases of the cardiovascular system, in which an increase in heart rate may be undesirable: atrial fibrillation, tachycardia, chronic heart failure, coronary artery disease, mitral stenosis, arterial hypertension, acute bleeding;
with thyrotoxicosis (possible increased tachycardia); elevated temperature (may further increase due to suppression of the activity of the sweat glands); with reflux esophagitis, hiatal hernia, combined with reflux esophagitis (decreased motility of the esophagus and stomach and relaxation of the lower esophageal sphincter can slow down gastric emptying and increase gastroesophageal reflux through the sphincter with impaired function); for gastrointestinal diseases accompanied by obstruction - achalasia of the esophagus, pyloric stenosis (possibly decreased motility and tone, leading to obstruction and retention of gastric contents), intestinal atony in elderly or debilitated patients (possible development of obstruction), paralytic ileus; with an increase in intraocular pressure - closed-angle (mydriatic effect, leading to an increase in intraocular pressure, can cause an acute attack) and open-angle glaucoma (mydriatic effect can cause a slight increase in intraocular pressure; adjustment of therapy may be required); with nonspecific ulcerative colitis (high doses can inhibit intestinal motility, increasing the likelihood of paralytic intestinal obstruction, in addition, the manifestation or exacerbation of such a severe complication as toxic megacolon is possible); with dry mouth (long-term use may cause further increase in the severity of xerostomia); with liver failure (decreased metabolism) and renal failure (risk of side effects due to decreased excretion); for chronic lung diseases, especially in young children and weakened patients (a decrease in bronchial secretion can lead to thickening of secretions and the formation of plugs in the bronchi); with myasthenia gravis (the condition may worsen due to inhibition of the action of acetylcholine); prostatic hypertrophy without urinary tract obstruction, urinary retention or predisposition to it, or diseases accompanied by urinary tract obstruction (including bladder neck due to prostatic hypertrophy); with gestosis (possibly increased arterial hypertension); brain damage in children (CNS effects may be enhanced); Down's disease (possibly unusual pupil dilation and increased heart rate), cerebral palsy (reaction to anticholinergic drugs may be more pronounced). Impact on the ability to drive vehicles and operate machinery
It is necessary to refrain from potentially hazardous activities that require increased attention and speed of psychomotor reactions.
Interaction
- Platiphylline Hydrotartrate is able to prolong the hypnotic effect of phenobarbital , sodium etaminal , magnesium sulfate ;
- capable of blocking proserin ;
- may increase the effect of H2-histamine blockers , Digoxin and Riboflavin ;
- may enhance mydriasis with adrenergic agonists and nitrates , increasing intraocular pressure;
- compatible with caffeine for cerebral vascular spasms;
- compatible with Cordiamin and Diafillin ;
- with Morphine eliminates bradycardia , nausea, vomiting;
- with Verapamil eliminates bradycardia .
Analogs
Level 4 ATC code matches:
Disflatil
Aprofen
Mint tablets
Spasmol
Kuplaton
Espumisan
Espumisan Baby
Espumisan L
Espumisan 40
No-Shpa
Drotaverine Hydrochloride
Bobotik
Dill water
Pepsan-R
Sub Simplex
Spasmomen
Meverin
Metacin
Niaspam
Sparex
- Platyfillin;
- Infacol;
- Enterospasmil.
