Codeine

When ATH: N02AA59

Pharmacological action

Centrally acting antitussive, phenanthrene alkaloid of opium series. Opioid agonist. According to the properties similar to morphine, However analgesic effect much weaker. By stimulating the opioid receptors of neurons, reduces the excitability of the cough center. To a lesser extent, than morphine, depresses the respiratory center. To a lesser extent inhibits peristalsis, but long-term use can cause constipation. Pupillary when used in therapeutic doses of codeine is weak.

Pharmacokinetics

After oral codeine and its salts are absorbed from the gastrointestinal tract. Cmax in plasma achieved through 1 no.

It is metabolized in the liver by O- и N-деметилирования в морфин, Norcodeine and other metabolites, including NORMORPHINE and hydrocodone. Codeine and its metabolites are excreted almost entirely by the kidneys, mainly in the form of conjugates with glucuronic acid.

T1 / 2 is 3-4 h after ingestion or after the / m.

Testimony

Is used to reduce or eliminate the cough in diseases of the bronchi and lungs (incl. when bronchopneumonia, bronchi, Emphysema).

Dosage regimen

Individual, depending on the age and the dosage form.

Inside, adults with pain - 15-60 mg every 3-6 hours, diarrhea - 30 mg 4 once a day, when you cough - 10-20mg 4 once a day; for kids, these doses are respectively 0,5 mg / kg 4-6 times per day, 0,5 mg / kg 4 twice a day and 3-10 mg / kg 4-6 times per day. V / m administered in the same doses, and that when given enterally. The highest daily dose - 120 mg.

Side effect

From the digestive system: rarely – nausea, vomiting, constipation.

From the central and peripheral nervous system: possible headaches, drowsiness, when used in high doses or in sensitive patients may worsen the coordination of movements of the eyeballs with visual impairment, develop respiratory depression; rarely – an increase in smooth muscle tone (at doses above 60 mg).

Allergic reactions: rarely – itching, rash type krapyvnytsы.

Other: weight gain.

Contraindications

Pulmonary failure, acute attack of asthma, Hypersensitivity to codeine. Do not use in children under the age of 1 year.

Pregnancy and lactation

Codeine is not recommended for use in the I trimester of pregnancy, before birth or abortion threat, lactation.

Cautions

In patients with impaired renal function excretion slowed codeine, so it is advisable to extend the intervals between doses of the drug.

With prolonged use may develop drug dependence.

Drug Interactions

In an application with drugs, have a depressing effect on the central nervous system (incl. opioid analgesics, ʙarʙituratami, ʙenzodiazepinami, clonidine), may increase the action of codeine.

While the use of derivatives of morphine may increase the inhibitory effect on the respiratory center; ibuprofen – enhanced analgesic effect; with carbamazepine – may increase the analgesic action, apparently, due to increased formation of a metabolite of codeine NORMORPHINE, has a stronger effect.

In an application with quinidine analgesic effect of codeine is reduced or virtually disappears.

With simultaneous use of codeine enhances effect of ethanol on psychomotor functions.