Pyrrthramide (Piritramidum)

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

Opioid narcotic analgesics

Included in the formulation
АТХ:

N.02.A.C.03   Pyrrthramide

Pharmacodynamics:

Opioid analgesic, an opioid receptor agonist.It is a derivative of diphenylpropyl piperidine. It is believed that the mechanism of action of pyrithramide is due to the stimulation of opioid receptors in the structures of the spinal cord and brain. As a result, the spinal cord diminishes the release of mediators by the endings of the primary afferent fibers that transmit pain signals. In addition, the descending inhibitory effects from the supra-segmental structures on the transfer of nociceptive impulses in the posterior horns of the spinal cord are intensified.

Pyrrthramide can cause euphoria, sedation and hypnotics. Reduces the excitability of the cough and respiratory centers. As a result of activation of the center of the oculomotor nerves, miosis occurs. Pyrrthramide increases the tone of the smooth muscles of the bile ducts, the sphincter of the bladder; oppresses the peristalsis of the intestine.

Activates mu-opiate receptors in the spinal cord and in the nociceptive centers of the thalamus and the cortex of the brain. Increases the threshold of pain sensitivity and improves the tolerance of pain. Effective quickly: analgesia occurs 1-2 minutes after intravenous injection and after 15-20 minutes - with subcutaneous or intramuscular application, it remains 4-6 hours.With long-term use of pyrithramide, habituation (decreased sensitivity to the action of pyrithramide) occurs; it is possible to develop drug dependence.

Pharmacokinetics:

After a single intramuscular injection, the maximum concentration is reached after 15 minutes, biotransformed in the liver and excreted from the body with a half-life 4-10 hours

Indications:

Moderate and severe pain syndrome, including trauma, surgical interventions, diagnostic and treatment procedures, burns, myocardial infarction, cancer.

ICD-10

XVIII.R50-R69.R52.2   Another constant pain

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

XVIII.R50-R69.R52.0   Acute pain

Contraindications:Hypersensitivity, severe exhaustion, coma, respiratory depression, intracranial hypertension, senile age.
Carefully:

They are used with caution in pregnancy and breastfeeding, hypothyroidism, insufficiency of respiratory function, kidneys, liver and adrenal cortex, prostatic hypertrophy, old age and shock conditions, combination with CNS inhibitors.

Patients with impaired liver function and elderly patients, as well as with severe general condition, should be prescribed in smaller doses.
Pregnancy and lactation:

The use of pyrithramide in pregnancy and lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus or baby.

It should be borne in mind that opioid analgesics can increase the period of labor.
Dosing and Administration:

Intramuscularly, subcutaneously, an adult 7.5-15 mg or 1-2 ml of a 0.75% solution; if necessary - again, after 2-3 hours, in a smaller dose.

Intravenously slow (to achieve a rapid effect): adults - 15-20 mg, children - 0.05-0.1 mg / kg. These doses are supportive and in the case of very severe pain (for example, in malignant tumors), they can be raised and injected every 6-8 hours.

Side effects:

From the side CNS: drowsiness, impaired coordination, tremor, anxiety, sedation.

From the side of cardio-vascular system: rarely - arterial hypotension, hypotension, bradycardia, increased blood pressure.

From the side digestive system: nausea, vomiting, constipation; rarely - an increase in the tone of sphincters of the bile ducts, ducts of the pancreas.

From the side respiratory system: with frequent use or administration in elevated doses, possible respiratory depression.

From the side urinary system: rarely - difficulty urinating, associated with an increase in the tone of sphincter urinary tract.

Allergic reactions: rarely - skin rash, itching.

Physical and mental dependence, tolerance.

On the part of the system hematopoiesis: acute porphyria.

Overdose:

Symptoms: miosis, oppression and respiratory arrest, hypotension, tachycardia, dizziness, impaired consciousness, coma.

Treatment: introduction of antagonists - naloxone (repeatedly, in low doses - in adults 0.4 mg every 2-3 minutes if necessary); intensive therapy, including intubation, ventilation, hyperthermia, maintenance of circulating blood volume; intestinal atony is corrected by cholinesterase inhibitors or parasympathomimetic agents.

Interaction:

Incompatible with MAO inhibitors (can develop paroxysmal stimulation of the central nervous system and hypertension). MAO inhibitors should be discontinued 10 or more days before the start of treatment.

Barbiturates, benzodiazepines, phenothiazine derivatives, gaseous halogenated general anesthetics and hypnotic drugs potentiate respiratory depression.With the systematic administration of barbiturates, especially phenobarbital, there is a likelihood of reducing the analgesic effect of opioid analgesics. Long-term use of barbiturates or opioid analgesics stimulates the development of cross tolerance.

Specific antagonists of opioid analgesics (including naloxone), blocking opioid receptors, reduce all the effects of pyrithramide, including respiratory depression and analgesia.

Application together with other neurotropic drugs - tranquilizers, diprazine (pipolphenom) and others allows you to get a balanced analgesia (atalgesia), including for the anesthesia of childbirth. Combination with neuroleptics - droperidol (inside, at 1.25 mg 2 times a day) or haloperidol (inside, 0.5-1 mg per day) - also enhances the analgesic effect, eliminates nausea and vomiting, has a positive effect on the mental state patient.
Special instructions:

During ambulatory treatment, driving or working with potentially dangerous mechanisms is not recommended.

Instructions
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