A typical clinical and pharmacological article
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Opioid analgesic. It also has a sedative, antitussive and spasmolytic effect. Activates the antinociceptive system, changes the emotional perception of pain. Stimulating opiate receptors in the digestive tract, reduces intestinal motility. The sphincters have no influence. Causes a miosis. It has an activating effect on the emetic center, has tocolytic action. Oppresses the respiratory center (much weaker than morphine).
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).
PHARMACOKINETICS
Well absorbed in any way of administration. Connection with plasma proteins - 40%.
Metabolized in the liver with the formation of inactive glucuronized metabolites.
It is excreted mainly by the kidneys, both in the form of metabolites and in active form.
INDICATIONS
Pain syndrome (strong and moderate severity):
- Malignant neoplasms of different localization;
- trauma;
- myocardial infarction;
acute pancreatitis;
- Stomach ulcer and duodenal ulcer;
- biliary colic;
- renal colic;
- intestinal colic;
- Postoperative period;
- Lerish's syndrome;
obliterating endarteritis;
- premedication;
- general anesthesia (as an analgesic component);
painful diagnostic procedures.
DOSING MODE
With pain syndrome in oncological patients - inside, 25-50 mg 2-3 times / day; daily dose - 50-250 mg (depending on the intensity of pain and previous therapy).
In case of traumatic pain, stomach ulcer, hepatic, renal and intestinal colic, in the postoperative period - p / k or IM, 10-40 mg or IV, 5-10 mg; daily dose of 20-60 mg.
When premedication - in / m or / in the drip, 5-10 mg; with general anesthesia as an analgesic component - iv, 0.2-0.7 mg / kg / h.
In acute myocardial infarction - in / in, 0.1 mg / kg (in dilution in 20 ml of 0.9% sodium chloride solution) or in / m 5-10 mg.
With Lerish syndrome and obliterating endarteritis - in / m 10-15 mg. Buccally, 10-20 mg, inside - 25 mg. The daily dose is up to 250 mg.
SIDE EFFECT
From the side of the central nervous system: dizziness, weakness, headache; convulsions, narcolepsy.
From the digestive system: dryness of the oral mucosa, nausea, vomiting, impaired liver function, intestinal atony.
From the cardiovascular system: a decrease in blood pressure, bradycardia.
From the urogenital 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.
CONTRAINDICATIONS
hypersensitivity;
- depression of the respiratory center;
- Hepatic and / or renal insufficiency;
- a coma;
- alcohol intoxication;
- arterial hypotension;
- organic diseases of the central nervous system;
- epilepsy and tonic-clonic convulsions in the anamnesis;
- bronchial asthma;
- respiratory insufficiency.
With caution: pregnancy, lactation.
PREGNANCY AND LACTATION
With caution: pregnancy, lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindication is renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication is liver failure.
SPECIAL INSTRUCTIONS
Has significant narcogenic potential, drug dependence can not be completely ruled out.
OVERDOSE
Symptoms: dyspnea, apnea.
Treatment: antagonists of narcotic analgesics (naloxone).
DRUG INTERACTION
Strengthens the effect of antihypertensive drugs.
Tranquilizers, hypnotics, ethanol, antipsychotic drugs enhance the effect.
Naloxone and naltrexone are specific antagonists.
