Levamisole

General characteristics. Structure:

Active ingredient: 50 mg or 150 mg of levamisole in 1 tablet.

Drug with the expressed anthelmintic and immunomodulatory action.

Pharmacological properties:

Pharmacodynamics. Anthelmintic action is caused by blockade of a succinatedehydrogenase, suppression of process of recovery of a fumarat and, as a result, disturbance of energy balance at helminths. Causes depolarization of membranes of muscle cells of helminths. The paralyzed nematodes are removed from an organism a normal peristaltics of intestines during 24 h after reception. Necator Americanus and Ancylostoma duodenale is especially active concerning Ascaris lumbricoides.

Exerts complex impact on immune system: increases development of antibodies by various antigens, strengthens the T-cellular answer, activating T lymphocytes and stimulating their proliferation, increases functions of monocytes, macrophages and neutrophils (their ability to a chemotaxis, adhesion and phagocytosis).

Pharmacokinetics. At intake it is quickly soaked up from a GIT. After reception of a single dose of 50 mg of Cmax (0,13 mkg/ml) it is reached through 1,5–2 p. T
1/2 — 3–4 h. Is exposed to biotransformation in a liver with formation of inactive metabolites which are excreted preferential by kidneys (70% within 3 days). T1/2  of metabolites is 16 h. About 5% are removed with excrements, and less than 0,2% in not changed look; more than 95% are removed by kidneys, them them about 5% in not changed look and 12% in the form of a glucuronide of p-hydroxy-levamisole.

There are uses of levamisole given about an opportunity after a resection concerning colon cancer (adjuvant therapy in a combination with ftoruratsily), at malignant new growths of bronchial tubes, mammary glands (after surgical, beam or chemotherapeutic treatment), a condition of remission at a lymphogranulomatosis, in intervals of cytostatic treatment of a leukosis and a lymphogranulomatosis; for an immunotherapy at immunodeficiency, immunodependent, including autoimmune diseases (a pseudorheumatism, a disease Krone, recurrent aphthous stomatitis, a disease of Reuters, not severe forms of a system lupus erythematosus — for maintenance of the remission reached by other means); at chronic nonspecific diseases of lungs, at a chronic glomerulonephritis, chronic pyelonephritis, a peptic ulcer of a stomach and duodenum — often recurrent current; at infectious diseases (a recurrent herpes simplex, shingles, warts, chronic active hepatitis B, a persistent viral hepatitis at which more than 3 months the surface antigen of a virus of hepatitis B is defined), recurrent sinusitis.

Indications to use:

Ascaridosis, dochmiasis, necatoriasis, strongyloidosis, трихостронгилоидоз, trichuriasis, enterobiosis, toxoplasmosis.

Route of administration and doses:

Inside. Helminthoses: once, adult — 150 mg, to children are 1–6 years — 25–50 mg, 7–14 years — 50–125 mg (as a rule at the rate of 2,5 mg/kg of body weight), if necessary a repeated course in 1–2 weeks. Toxoplasmosis: 150 mg of 1 times a day within 3 days (2–3 courses with breaks of 1 week).

Features of use:

Use at pregnancy and feeding by a breast. Use at pregnancy and feeding by a breast is not recommended (adequate and strictly controlled researches at the person are not conducted). Embriotoksichesky effect of levamisole at oral administration of doses of 160 mg/kg (at rats) and 180 mg/kg is revealed (at rabbits).

Category of action on a fruit on FDA — C. It is unknown whether levamisole in breast milk of the person is excreted, however it is excreted in milk of cows.

Before an initiation of treatment it is necessary to carry out clinical and biochemical analysis of peripheral blood.

Levamisole use sometimes led to development of an agranulocytosis (in certain cases with a lethal outcome) which often was followed by a grippopodobny syndrome, including fervescence, a fever, an ostealgia. In this regard it is necessary at least 1 разав 3 weeks to carry out the developed clinical blood test. However at a small number of patients the agranulocytosis passes asymptomatically. The Grippopodobny syndrome can meet also for lack of an agranulocytosis.

In time and after reception of HP during 24 h it is impossible to take alcoholic drinks.

Side effects:

From bodies of a GIT: nausea, vomiting, diarrhea, abdominal pain, pancreatitis, ulceration of a mucous membrane of an oral cavity.

From a nervous system and sense bodys: a headache, paresthesia, peripheral polyneuropathy, olfactory hallucinations (change of smells), generalized spasms, an entsefalitopodobny syndrome (it is connected with demyelination of nerve fibrils), disturbance of the speech, a lethargy, fatigue, a tremor, a sleep disorder, confusion of consciousness, an ataxy, change of flavoring feelings.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): a leukopenia, an agranulocytosis, sometimes fatal (see. "Precautionary measures").

Allergic reactions: skin rash, exfoliative dermatitis.

Others: damage of kidneys, hypercreatinemia, increase in activity ShchF, uterine bleedings, periorbital hypostasis.

Interaction with other medicines:

Levamisole is incompatible with lipophilic connections (for example phenoxin, tetrachlorethylene, chloroform, ether) since strengthening of its toxicity is possible, with alcohol (at joint reception the antabuspodobny syndrome develops) and the HP causing a leukopenia.

Strengthens effects of Phenytoinum and indirect anticoagulants (control of PV with possible dose adjustment of anticoagulants is necessary).

At simultaneous use with miyelotoksichny HP — strengthening of a gematotoksichnost.

Contraindications:

Hypersensitivity; the agranulocytosis caused by HP (including in the anamnesis).

Restrictions to use. Liver and/or renal failure, oppression of a marrowy hemopoiesis, cerebrovascular insufficiency, acute phase of a leukosis.

Overdose:

It was reported about lethal outcomes: the 3-year-old child — at a dose has 15 mg/kg and the adult — at a dose of 32 mg/kg.

Treatment: a gastric lavage (if after reception there passed a little time), a symptomatic and maintenance therapy.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 50 mg and 150 mg, on 1, 5 or 10 tablets in each blister, on one blister together with the application instruction in cardboard packaging.