Thalidomide

Талидомид Constitutional formula

The description is actual on 24.02.2016

  • Latin name: Thalidomidum
  • ATH code: L04AX02
  • Chemical formula: C13H10N2O4
  • CAS code: 50-35-1

Chemical name

(±)-2 (2,6-dioxopiperidine-3-silt) isoindole-1,3-izoindol-1,3-dion

Chemical properties

Thalidomide – a sedative hypnagogue. At the moment drug is used only as an immunosuppressant because of its high teratogenecity and ability to cause peripheral neuritis.

Medicine represents the white crystal powder which does not have specific taste or a smell. Substance is insoluble in gasoline and ether, is badly soluble in water, ethanol, acetic acid and methanol. This chemical compound – derivative glutaminic acid, its molecule consists of two parts: glutarimid and phthalimide. Temperature of melting of means 271 degrees Celsius. The molecule possesses an isomerism. There is a right-and left-handed isomer, the last possesses ability to be built in on cellular DNA on a site of communication and to interfere with normal process of DNA replication of a germ.

Drug was synthesized in 1954 German farm. the Chemie Grünenthal company during attempts of production of antibiotics from peptides. It was initially supposed that substance will be used as an anticonvulsant, however during researches it was found out that medicine has the expressed calming and somnolent effect. 3 years later drug officially went on sale, at the same time, it was recommended for reception to pregnant women. It was established that during the period from 56 to 62 year, as a result of treatment by this substance about 10000 children with inborn uglinesses were born. By 1961 means was withdrawn from sale. However, in the nineties the 20th centuries, scientists paid the attention to the Thalidomide again. After additional researches anticarcinogenic and immunodepressive properties of drug were found. Since 1998 medicine was approved by FDA for treatment of leprosy.

Pharmacological action

Immunodepressive, sedative.

Pharmacodynamics and pharmacokinetics

Under the influence of the drug Thalidomide there is an oppression of processes of an angiogenesis and formation of a factor of a necrosis of a tumor. Also this substance inhibits migration of leukocytes, changes the number of T-killers and T-helperov, causes growth of level of interleykin and interferon-G.

Pharmacokinetic parameters linearly depend on the accepted dosage. Medicine does not collect in an organism. Extent of linkng with proteins of plasma – about 55-66% (the right and left isomers).

The thalidomide is practically not metabolized in a liver. Allegedly, substance is exposed to spontaneous not fermental hydrolysis in a blood plasma. Products of a metabolism it is removed with urine.

Indications to use

Now drug is used:

  • for treatment of leprosy;
  • at a multiple myeloma;
  • at treatment of patients with serious oncological diseases.

Contraindications

It is impossible to appoint medicine:

  • at an allergy to active ingredient;
  • to patients 18 years are younger;
  • to pregnant women and the nursing women;
  • if the patient – the woman of childbearing age and a disease responds to treatment other drugs;
  • at the expressed neutropenia.

Side effects

Treatment by this substance has to be carried out under control of the doctor.

During drug intake can be shown:

  • weakness, drowsiness, headaches;
  • disturbance of a menstrual cycle, dizziness, fervescence;
  • peripheral neuritis, neutropenia, leukopenia;
  • thrombocytopenia, decrease in a sexual inclination;
  • tremor, tachycardia, change of the ABP, vein thrombosis, lock;
  • adynamy, lethargy, increased fatigue, light sensitivity;
  • skin allergic reactions.

Thalidomide, application instruction (Way and dosage)

Depending on weight of an illness and a form of release use different schemes of treatment which are appointed by the attending physician.

The instruction on the Thalidomide

Pill is taken inside, before withdrawal to a dream.

At a multiple myeloma about 0,2 g of drug a day are recommended to use. Each 7 days a dosage can be raised on 0,1 g. Maximum daily dose = 0,8 grams of the Thalidomide. Duration of treatment is defined in an individual order.

Overdose

Reception of high doses (to 14 grams for time) drug did not cause the lethal result or oppression of respiratory function. At overdose side effects can amplify. Treatment – symptomatic, correction of a dosage is shown.

Interaction

It is better not to combine a thalidomide with barbiturates, Chlorpromazinum, Reserpinum, alcohol, benzodiazepines, opiate analgetics, hypnagogues, anxiolytics, neuroleptics and antidepressants.

Medicine strengthens sedative action of anti-hypertensive means, Baclofenum, antihistamines.

The concomitant use of drug with zaltsitabiny, didanoziny, Vincristinum increases risk of development of peripheral neuropathy.

Doxorubicine increases probability of development of a thromboembolism and thromboses.

Terms of sale

According to the recipe.

Special instructions

With care this substance is appointed to women in childbearing age. It is recommended to use reliable barrier methods of contraception during treatment by drug and within 12 weeks after end. Also it is impossible to be the donor of sperm and blood.

Patients who accept the Thalidomide cannot steer the car.

With alcohol

Medicine strengthens sedation from alcohol intake.

Drugs in which contains (Analogues)

Coincidence on the ATH code of the 4th level:

Trade names of medicine: Softenon, Tenazadrin, Thalidomide, Kontergan, Mirin 100.

Responses

About use of this drug ambiguous. Many are afraid to take this medicine because of its sad reputation in the past. However those at whom the means dosage was picked competently up well speak of it at treatment of an illness of Bekhterev, a multiple myeloma, etc. After passing of a course remission lasts of several months before half a year. Side reactions are shown with a frequency which is specified in the official instruction.

Section: Active ingredients
PAY ATTENTION! Information on active ingredients on the website is help generalizing, collected from public sources and can form the basis for making decision on use of these substances it is not aware of treatment. Before substance Thalidomide use surely consult with the attending physician.