Pharmacological Effects:
Antitussives central action; alkaloid fenantrenovogo series. Opiate receptor agonist, reduces the excitability of the cough center. Central antitussive effect is associated with the suppression of cough center. The analgesic activity due to stimulation of opiate receptors in different regions of CNS and peripheral tissues, leading to stimulation of the antinociceptive system and change the emotional perception of pain. To a lesser degree than morphine, respiratory depression, less likely to cause miosis, nausea, vomiting and constipation (activation of opioid receptors in the intestine causes relaxation of smooth muscles, decrease peristalsis and spasm of sphincters). The analgesic effect develops within 10-45 minutes after i / m and s / c administration and within 30-60 minutes after oral administration. The maximum effect is achieved within 30-60 minutes after i / m administration and within 1-2 h after oral administration. The duration of analgesia – 4 h, the blockade cough reflex – 4-6 hours
Indications:
Nonproductive cough (pneumonia, bronchitis, emphysema); pain mild and moderate degree (in conjunction with non-narcotic analgesics – headache, neuralgia); diarrhea.
Contraindications:
Hypersensitivity, toxic dyspepsia, diarrhea, against the background of pseudomembranous colitis caused by cephalosporins, lincosamides, penicillin, acute respiratory depression tsentra.C caution. Acute abdominal pain of unknown etiology, onset of asthma, COPD, arrhythmias, convulsions, drug dependence (including history), alcoholism, suicidal tendencies, emotional lability, gallstone disease, surgery on the gastrointestinal tract, urinary system, brain injury brain, intracranial hypertension, hepatic or renal impairment, hypothyroidism, severe inflammatory bowel disease, prostatic hyperplasia, urethral stricture, seriously ill, debilitated patient, cachexia, pregnancy, lactation period, simultaneous treatment with inhibitors, elderly, children’s age.
Side effects:
From the digestive system: more often – constipation less frequently – dry mouth, anorexia, nausea, vomiting rarely – stomachodynia, spasms in the gastrointestinal tract, biliary tract spasm, paralytic ileus, toxic megacolon (constipation, flatulence, nausea, abdominal stomach, vomiting), the frequency is unknown – hepatotoxicity (dark urine, pale stools, ikterichnost sclera and skin). From the nervous system and sensory organs: a more frequent – drowsiness, less often – dizziness, headache, fatigue, nervousness, confusion (hallucinations, depersonalization), blurred vision (including diplopia) in children – paradoxical excitement and anxiety; rare – restless sleep, nightmares, convulsions, depressed, at higher doses, muscle rigidity (especially respiratory), tremors, involuntary muscle twitching, the frequency is unknown – ringing in the ears, the deterioration of the coordination of movements of the eyeballs with visual impairment, increased tone smooth muscle (at doses above 60 mg). From the CCC: less often – arrhythmia (tachy-or bradycardia), decreased blood pressure, the frequency is unknown – increase blood pressure. On the part of the respiratory system: less often – atelectasis, inhibition of the respiratory center. From the urinary system: less frequently – reducing diuresis, ureteral spasm (difficulty and pain when urinating, frequent urge to urinate), frequency unknown – atony of the urinary bladder. Allergic reaction: less often – a skin rash, hives, itchy skin, face edema, bronchospasm, laryngeal edema, laryngospasm. Other: less often – sweating, imaginary sense of wellbeing, a feeling of discomfort, the frequency is unknown – body weight increase, with prolonged use – drug dependency syndrome “cancellation.” Overdose. Overdose. Overdose. Symptoms of acute and chronic overdose: cold clammy sweat, confusion, dizziness, drowsiness, decreased blood pressure, nervousness, fatigue, bradycardia, severe weakness, slow labored breathing, hypothermia, anxiety, miosis, spasms, in severe cases – loss of consciousness, respiratory arrest , coma. Treatment: gastric lavage, the restoration of respiration and maintenance of cardiac activity and blood pressure, in / in the introduction of a specific antagonist of opioid analgesics – naloxone.
Dosage and administration:
Inside adults in pain – 15-60 mg every 3-6 hours, with diarrhea – 30 mg 4 times a day, when you cough – 10-20 mg 4 times a day. The highest daily dose for adults – 120 mg. For children in pain – 0.5 mg / kg (15 mg / m) 4-6 times a day for diarrhea – 0.5 mg / kg 4 times a day when people cough in children younger than 2 years – not recommended, 2 — 5 years – 1 mg / kg / day divided in 4 hours, or children under 2 years of age (birth weight of 12 kg) – 3 mg every 4-6 h, the maximum dose – 12 mg / day for children aged 3 years (weight not less than 14 kg) – 3.5 mg every 4-6 hours, not more than 14 mg / day for children aged 4 years – 4 mg every 4-6 hours, not more than 16 mg / day, 5 years (body mass not less than 18 kg) – 4.5 mg every 4-6 hours, not more than 18 mg / day, 6-12 years – 5-10 mg every 4-6 hours, not more than 60 mg / day.
Cautions:
During the period of treatment should refrain from receiving ethanol and use caution when driving motor vehicles, as well as during the occupation of other potentially hazardous activities requiring a high concentration of attention and quickness of psychomotor reactions. Controlled studies for use during pregnancy has not been conducted; studies on animals have shown that a single dose of codeine into mice at a dose of 100 mg / kg causes a delay in ossification, a single dose of 120 mg / kg in rats – an increase in bone rezobtsii. The use of codeine during labor may cause a prolongation of them. It should be borne in mind that children under 2 years are more sensitive to the effects of opioid analgesics, and that they may have the paradoxical reaction. In pregnancy and during breast-feeding use is acceptable only for health reasons (possible respiratory depression and the development of drug dependence in the fetus and the newborn). Opioid analgesics reduce salivation, which may contribute to the development of caries, periodontal diseases, candidiasis of the oral mucosa. Codeine dose of 120 mg / m or 200 mg oral morphine equivalent dose of 10 mg / m
Interaction:
Enhances the inhibitory effect of ethanol on the speed of psychomotor reactions. With simultaneous application of ethanol, muscle relaxants, as well as LAN, depressing the central nervous system may increase sedation, suppression of the respiratory center and the central nervous system depression. In simultaneous reception with other opioid analgesics increases the risk of CNS depression, respiration, blood pressure lowering. Enhance effects of antihypertensive and antipsychotic LS (neuroleptics), anxiolytics (tranquilizers), barbiturates and drugs, for general anesthesia. Naloxone and naltrexone are specific antagonists. Naloxone reduces the effect of opioid analgesics, and they cause respiratory depression and central nervous system, may require higher doses to the leveling effects of butorphanol, Nalbuphine and pentazocine, have been assigned to eliminate unwanted effects dr.opioidov; can accelerate the emergence of symptoms <withdrawal> against a background of drug dependence. Naltrexone accelerates the appearance of symptoms <withdrawal> against a background of drug addiction (symptoms may occur in 5 minutes after injection of the drug, continued for 48 h, are persistent and difficult to address them) reduces the effect of opioid analgesics (analgesic, anti, antitussive); not affect the symptoms caused by histamine reaction. Drugs with anticholinergic activity, anti-LS (including loperamide) increase the risk of locking up intestinal obstruction, urinary retention, and CNS depression. Buprenorphine (including previous therapy) reduces the effect dr.opioidnyh analgesics; against the use of high doses of agonists of mu-opioid receptors reduces respiratory depression, and a background of low doses of agonists of mu-or kappa-opioid receptors – increases. Precautions should be used concurrently with MAO inhibitors because of possible overexcitation or inhibition with the emergence of hyper-or hypotensive crises (initially to assess the synergies of the dose should be reduced to 1 / 4 of the recommended). Reduces the effect of metoclopramide.
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