Propionylphenyl ethoxyethylpiperidine - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Opioid narcotic analgesics

Included in the formulation

Prosidol

pills inwards

GosMPS, FSUE Russia

АТХ:

N.02.A.X Other opioids

Pharmacodynamics:

The action is analgesic (opioid).

Refers to analgesics, agonists of opioid receptors.

The main mechanisms of the analgesic effect of opioid analgesics are realized at the level of the spinal cord, subcortical structures and the cerebral cortex.

I. Inhibition of pain impulses in the afferent ways of the CNS (impairment of the transfer of impulses from the end of the primary afferents to the intercalary neurons of the spinal cord).

As a result of blocking N-type calcium channels in the presynaptic endings of the axons of the primary afferents, the release of substance P and glutamate decreases, and the transmission of pain impulses to the intercalary neurons of the posterior horns of the spinal cord is impaired.

Due to post-synaptic stimulationopioid receptors is disrupted depolarization process is post-synapticth membrane and the activation of intercalary neurons under the influence of the mediator is inhibited. All this leads to a violation of transmission of pain impulses at the level of the spinal cord (spinal action).

II. Strengthening the inhibitory effect descending antinociceptive system to conduct painful impulses in the afferent pathways of the central nervous system.

When the opioid receptors are stimulated in the gray near-conductor substance and some other parts of the brain stem due to the inhibition of inhibitory GABAergic neurons, activation of the descending antinociceptive system, which inhibits the transmission of pain impulses along the afferent pathways of the spinal cord (supraspinal action), occurs. Descending inhibitory influences at the level of the spinal cord are carried out with the participation of serotonin and norepinephrine.

III. Changing the emotional assessment of pain: as a result of the action of narcotic analgesics in the higher departments of the central nervous system, the emotional assessment of pain changes, and its perception decreases (even if the feeling of pain persists, it worries the patient less).

Stimulation of opioid receptors in the gastrointestinal tract reduces motility of the gastrointestinal tract. The sphincters have no influence. Exciting the vegetative segment of the oculomotor nerve, causes miosis. Has an activating effect on the vomiting and depressing - on the cough centers. Possesses tocolytic action. Oppresses the respiratory center (much weaker than morphine).

Pharmacokinetics:

The duration of analgesic action with oral administration is 4-6 hours, with parenteral administration - 1.5-6 hours (depending on individual sensitivity and dose), 15-30 minutes after intravenous administration.

With prolonged use (more than 3 months), analgesic activity decreases (due to the development of tolerance).

Absorption is good. Penetrates through the placenta and GEB. Connection with plasma proteins - 40%. Biotransformation in the liver. Elimination of the kidneys in the form of metabolites and unchanged.

Indications:

As a component of complex anesthesia, relief of pain in the postoperative period.

Pain syndrome (strong and moderate severity):

malignant neoplasms of different localization; injury; myocardial infarction; acute pancreatitis; peptic ulcer of the stomach and duodenum; biliary colic; renal colic; intestinal colic; postoperative period; Lerish's syndrome; obliterating endarteritis; premedication; general anesthesia (as an analgesic component); painful diagnostic procedures.

ICD-10

IX.I20-I25.I21 Acute myocardial infarction

XI.K80-K87.K85 Acute pancreatitis

XIV.N20-N23.N23 Renal colic, unspecified

XVIII.R00-R09.R07.2 Pain in the region of the heart

XVIII.R50-R69.R52.0 Acute pain

XVIII.R50-R69.R52.1 Constant unrestrained pain

Contraindications:Hypersensitivity, depression of the respiratory center,hepatic and / or renal failure, coma, alcohol intoxication, arterial hypotension, organic CNS diseases, epilepsy and tonic-clonic convulsions in history, bronchial asthma, respiratory failure, bPregnancy, breast-feeding, children under 18 years of age.

Carefully:Elderly age, myxedema, hypothyroidism, adrenal insufficiency, central nervous system depression, craniocerebral trauma with psychosis, prostatic hyperplasia, urethral stricturealcohol abuse, drug abuse or drug addiction, emotional lability, suicidal thoughts or attempts (including history), general severe condition.

Pregnancy and lactation:

Category FDA is not defined. Adequate and well-controlled studies in humans and animals have not been conducted.

There is no information on the penetration into breast milk. Do not apply!

Dosing and Administration:Adults
Enter intramuscularly, intravenously, subcutaneously, 5-10 mg (0.5-1 ml of 1% solution), in some cases, up to 1.5-4 ml of 1% solution is possible. Buccal by 10-20 mg, inside by 25 mg.The daily dose is up to 250 mg.
Children
Efficiency and safety have not been studied.

Side effects:

From the nervous system: dizziness, weakness, headache; convulsions, narcolepsy.

From the digestive system: dry mouth, nausea, vomiting, impaired liver function, intestinal atony.

From the cardiovascular system: reduction of blood pressure, bradycardia.

From the genitourinary and urinary system: atony of the bladder, impaired renal function, amenorrhea, decreased libido.

Other: allergic reactions, habituation, withdrawal syndrome, with intravenous administration - respiratory failure.

Local Reactions: soreness and hyperemia at the injection site.

Overdose:

Symptoms acute and chronic overdose: cold sticky sweat, confusion, dizziness, drowsiness, decreased blood pressure, nervousness, fatigue, miosis, bradycardia, severe weakness, slow labored breathing, hypothermia, anxiety, dry mouth, delirious psychosis, intracranial hypertension (up to disorders of cerebral circulation), hallucinations, muscle rigidity, convulsions, in severe cases - loss of consciousness, respiratory arrest, coma.

Treatment: gastric lavage, recovery of respiration and maintenance of cardiac activity and blood pressure; intravenous injection of a specific antagonist opioid analgesics - naloxone in a single dose of 0.2-0.4 mg, repeating the introduction after 2-3 minutes until the total dose of 10 mg; the initial dose of naloxone for children is 0.01 mg / kg.

Interaction:

Alcohol, drugs that depress the central nervous system - potentiation of oppressive effects on the central nervous system, including the respiratory center.

Anticholinergics, antidiarrheals - the risk of severe constipation and acute retention of urine.

Antihypertensive drugs, especially ganglion blockers and diuretics - potentiation of the hypotensive effect.

Buprenorphine - a decrease in the therapeutic effect of other μ-receptor agonists, including a reduction in respiratory depression, the emergence of withdrawal syndrome in dependent individuals.

Other drugs that cause drug dependence are an increased risk of developing drug dependence.

Metoclopramide - decreased prokinetic activity of metoclopramide.

Miorelaxants - potentiation of respiratory depression.

Naltrexone, naloxone, nalorfin - antidotes of narcotic analgesics, eliminate all their pharmacological effects,including cause withdrawal syndrome in patients with drug dependence to them.

Narcotic analgesics - mutual potentiation of effects.

Phenotiazine neuroleptics - some increase, and some reduce the effect of morphine.

Special instructions:

By its structure and pharmacological properties it is close to trimereperin.

Do not use alcohol.

Impact on the ability to drive vehicles and manage mechanisms

During the period of taking the drug should refrain from transport management and the performance of potentially dangerous work requiring concentration of attention.

Instructions

Propionylphenylethoxyethylpiperidine (Propionilphenyletoxyaethylpiperidinum)