Medicinal reference book geotar. Omnopon - official * instructions for use

1 ml of solution contains:

active substances:

codeine monohydrate - 0.72 mg or 1.44 mg,

morphine hydrochloride trihydrate (in terms of morphine hydrochloride) - 5.75 mg or 11.5 mg,

noscapine - 2.7 mg or 5.4 mg, papaverine hydrochloride - 0.36 mg or 0.72 mg, thebaine - 0.05 mg or 0.1 mg.

Excipients:

disodium edetate (disodium salt of ethylenediaminetetraacetic acid) - 0.5 mg, glycerol (distilled glycerin) - 60 mg,

hydrochloric acid 1 M - up to pH 2.5-3.5, water for injection - up to 1 ml.

Omnopon increases the threshold of pain sensitivity, inhibits conditioned reflexes, causes euphoria and has a moderate hypnotic and central antitussive effect, increases the tone of the vagus nerve center, excites the vomiting center, depresses the respiratory center, causes pupillary constriction due to activation of the center of the oculomotor nerve, weakens intestinal motility, inhibits secretory activity of the glands of the gastrointestinal tract. Slightly reduces basal metabolism and body temperature, stimulates the release of antidiuretic hormone. With subcutaneous administration of Omnopon, the analgesic effect develops after 10-15 minutes and lasts for 3-5 hours.

The main pharmacological properties of Omnopon are due to the morphine contained in it. - an agonist of predominantly mu-opioid receptors, activates the endogenous antinociceptive system and thus disrupts the interneuronal transmission of pain impulses at various levels of the central nervous system, and also changes the emotional coloring of pain, affecting the higher parts of the brain.

Morphine increases the threshold of pain sensitivity to stimuli of various modalities, inhibits conditioned reflexes, has a euphoric and moderate hypnotic effect, and increases the tone of the center of the vagus nerve. Can stimulate the chemoreceptors of the starting zone of the vomiting center and cause nausea and vomiting, inhibits the respiratory and vomiting centers, causes pupil constriction due to activation of the center of the oculomotor nerve, increases the tone of the bronchi and smoothomascervical sphincters of internal organs (intestines, biliary tract, bladder), enhances the contractile activity of the myometrium, weakens intestinal motility, inhibits the secretory activity of the glands of the gastrointestinal tract. Slightly reduces basal metabolism and body temperature, stimulates the release of antidiuretic hormone. Causes dilation of peripheral blood vessels and release of histamine, which may lead to decreased blood pressure, redness of the skin, increased sweating, redness of the white of the eyes. Enhances the effect on the central nervous system of means for general anesthesia, hypnotics, sedatives, H1 blockers of histamine receptors with a central component of action, anxiolytic, antipsychotic and antidepressant drugs.

Papaverine is an antispasmodic that has a hypotensive effect, reduces tone and relaxes the smooth muscles of internal organs and blood vessels. Due to the content of papaverine, Omnopon, to a lesser extent than, causes spasms of the smooth muscles of the internal organs.

Codeine is a natural narcotic analgesic from the group of opioid receptor agonists. Analgesic activity is due to the excitation of opioid receptors in various parts of the central nervous system and peripheral tissues, leading to stimulation of the antinociceptive system and a change in the emotional perception of pain.

Thebaine is the smallest integral part drug. Thebaine is chemically similar to morphine and codeine. Thebaine has an analgesic effect by acting on opioid receptors in the central nervous system. By their own pharmacological properties Thebaine differs from morphine and codeine in that it produces an excitatory rather than a depressant effect on the nervous system. Thebaine in small doses has a weak hypnotic action. Potentiates the effect of codeine and morphine.

Noscapine is a poppy alkaloid, a derivative of benzylisoquinoline; is predominantly an agonist σ -opioid receptors, has practically no analgesic properties, has an antitussive effect. Noscapin eyeIt has an antispasmodic effect on smooth muscles. It has a potentiating effect on the antispasmodic activity of papaverine.

The volume of distribution of morphine is 4 l/kg. 30-35% of morphine binds to plasma proteins.

Morphine is excreted from the body in the form of glucuronide metabolites (up to 80%) or unchanged, mainly through the kidneys; a small part is excreted in the bile and excreted in the feces. The drug passes through the placental barrier and is found in breast milk.

Papaverine undergoes biotransformation in the liver. Excreted by the kidneys mainly as metabolites. In plasma, it binds to proteins.

Codeine undergoes biotransformation in the liver, with 10% being demethylated into. Excreted by the kidneys 5-15% as codeine and 10% as morphine and its metabolites. Communication with plasma proteins is negligible.

Thebaine is similar in pharmacokinetic properties to codeine. The main metabolite of thebaine is oripavine.

Noscapine after introduction into the body quickly disappears from the blood and passes into the tissues. During the first six hours after entering the body, it is excreted in the urine unchanged, and after the specified time, noscapine is excreted from the body in the form of conjugates. Decay products long time found in the urine (up to 1 month).

Strong pain various etiologies(postoperative period, trauma, pain in cancer patients, myocardial infarction, renal, hepatic, intestinal colic etc).

Anesthesia during painful diagnostic and therapeutic measures.

Hypersensitivity to the components of the drug.

Conditions accompanied by respiratory depression or severe depression of the central nervous system. Convulsive conditions. Increased intracranial pressure. Traumatic brain injury. Acute alcoholic conditions, including alcoholic psychosis.

Bronchial asthma. Pulmonary heart failure. Heart rhythm disturbances.

Acute surgical diseases of the abdominal organs before diagnosis.

Conditions after surgical interventions on the biliary tract. Paralytic ileus.

Co-administration with monoamine oxidase inhibitors and within 14 days after their withdrawal.

Children under 2 years old.

Elderly patients, with general exhaustion, with adrenal insufficiency; patients with a history of opioid dependence. Alcoholism, suicidal tendencies, emotional lability, epileptic syndrome, chronic obstructive pulmonary disease, hypothyroidism, surgicalinterventions on gastrointestinal tract, urinary system, hepatic or kidney failure, cholelithiasis, severe inflammatory bowel disease, strictures urethra, prostatic hyperplasia.

If you have one of the listed diseases, be sure to consult your doctor before taking the drug.

During pregnancy, childbirth and during breastfeeding, the use of Omnopon is permissible only for health reasons (the development of drug dependence in the fetus and newborn is possible).

Doses of the drug are selected individually depending on the severity of the pain syndrome, age and condition of the patient.

- Adult patients are injected subcutaneously with 1 ml of a solution with a dosage of 0.72 + 5.75 + 2.7 + 0.36 + 0.05 mg / ml. The frequency of the appointment is 4-5 hours. The highest single dose is 3 ml of solution. The highest daily dose is 10 ml.

- If it is necessary to increase the dose, 1 ml of a solution is prescribed with a dosage of 1.44 + 11.5 + 5.4 + 0.72 + 0.1 mg / ml. If necessary, the drug is re-administered after 4-5 hours. The highest single dose is 1.5 ml of solution. The highest daily dose is 5 ml.

Children over 2 years old: the drug at a dosage of 0.72 + 5.75 + 2.7 + 0.36 + 0.05 mg / ml permean in a dose of 0.1 ml (age 2-3 years) to 0.75 ml (age 12-14 years), taking into account the general condition and the required degree of anesthesia.

Euphoria, urinary disorders, allergic reactions, depression, hallucinations, nausea, rarely vomiting, dizziness, muscle weakness, constipation. Drowsiness or agitation, exacerbation of brain diseases due to increased intracranial pressure, spasms of the biliary tract and bladder sphincter, moderate respiratory depression are also possible.

To reduce side effects on the intestines, a laxative should be prescribed. funds.

Enhances the inhibitory effect on the central nervous system of general anesthesia, hypnotics, sedatives, blockers H 1 -histamine receptors with a central component of action, antidepressants, anxiolytic and antipsychotic drugs.

It is addictive and drug (opioid) dependence (physical and mental). Causes expansion of peripheral blood vessels and release of histamine, which can lead to bronchospasm, lowering blood pressure, reddening of the skin, increased sweating, reddening of the white of the eyes.

With repeated use of Omnopon for 1-2 weeks (sometimes within 2-3 days), addiction (weakening of the analgesic effect) and opioid drug dependence may develop. 1-2 days after discontinuation of the drug, signs of "withdrawal" syndrome may appear (mydriasis, yawning, muscle contractions, headache, sweating, vomiting, diarrhea, tachycardia, hyperthermia, increased blood pressure and other autonomic symptoms), which requires treatment in conditions of a specialized department.

If any of the instructions side effects get worse, or you notice any other side effects not listed in the instructions,tell your doctor about it.

Symptoms: stuporous or coma, hypothermia, lowering blood pressure, respiratory depression is observed. A characteristic feature is a pronounced constriction of the pupils (with significant hypoxia, the pupils can be dilated).

Treatment: maintaining adequate pulmonary ventilation. Intravenous administration of a specific opioid antagonist - naloxone in a dose of 0.4 to 2 mg quickly restores breathing. If there is no effect after 2-3 minutes, the administration of naloxone is repeated. The initial dose of naloxone for children is 0.01 mg/kg. The short duration of action of naloxone should be taken into account. It is also necessary to remember a thread about the possibility of developing a "withdrawal" syndrome when naloxone is administered to patients with dependence on opioids - in such cases, the dose of the antagonist should be increased gradually.

Under close supervision and in reduced doses, Omnopon should be used against the background of the action of general anesthetics, hypnotics, anxiolytics, antidepressants and antipsychotics in order to avoid excessive depression of the central nervous system and suppression of the activity of the respiratory center. Omnopon should not be combined with narcotic analgesics from the group of partial agonists ( , ) and agoniantagonists ( , ) of opioid receptors because of the danger of weakening analgesia and the possibility of provoking the “withdrawal” syndrome. The analgesic effect and undesirable effects of opioid agonists (trimeperidine, fentanyl) in the therapeutic dose range are summed up with the effects of Omnopon.

During the period of treatment, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.