User:Mr. Ibrahem/Thalidomide
Immunomodulatory drug known for its ability to cause birth defects / From Wikipedia, the free encyclopedia
Thalidomide, sold under the brand name Thalomid among others, is a medication used to treat a number of cancers including multiple myeloma, graft-versus-host disease, and a number of skin conditions including complications of leprosy.[3] While it has been used in a number of HIV associated conditions, such use is associated with increased levels of the virus.[3] It is taken by mouth.[3]
Clinical data | |
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Pronunciation | /θəˈlɪdəmaɪd/[1] |
Trade names | Contergan, Thalomid, Talidex, others |
Other names | α-Phthalimidoglutarimide |
AHFS/Drugs.com | Monograph |
MedlinePlus | a699032 |
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Routes of administration | By mouth (capsules) |
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Pharmacokinetic data | |
Bioavailability | 90% |
Protein binding | 55% and 66% for the (R)-(+)- and (S)-(−)-enantiomers, respectively[2] |
Metabolism | Liver (minimally via CYP2C19-mediated 5-hydroxylation; mostly via non-enzymatic hydrolysis at the four amide sites)[2] |
Elimination half-life | 5–7.5 hours (dose-dependent)[2] |
Excretion | Urine, faeces[2] |
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Chemical and physical data | |
Formula | C13H10N2O4 |
Molar mass | 258.233 g·mol−1 |
3D model (JSmol) | |
Chirality | Racemic mixture |
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NY (what is this?) (verify) |
Common side effects include sleepiness, rash, and dizziness.[3] Severe side effects include tumor lysis syndrome, blood clots, and peripheral neuropathy.[4] Use in pregnancy may harm the baby, including resulting in malformation of the limbs.[3] In males who are taking the medication, condoms are recommended if their partner could become pregnant.[4] It is an immunomodulatory medication and works by a number of mechanisms including stimulating T cells and decreasing TNF-α production.[3]
Thalidomide was first marketed in 1957 in West Germany, where it was available over the counter.[5][6] When first released, thalidomide was promoted for anxiety, trouble sleeping, "tension", and morning sickness.[6][7] While initially deemed to be safe in pregnancy, concerns regarding birth defects were noted in 1961 and the medication was removed from the market in Europe that year.[6][5] The total number of people affected by use during pregnancy is estimated at 10,000, of which about 40% died around the time of birth.[6][3] Those who survived had limb, eye, urinary tract, and heart problems.[5] Its initial entry into the US market was prevented by Frances Kelsey at the FDA.[7] The birth defects of thalidomide led to the development of greater drug regulation and monitoring in many countries.[7][5]
It was approved for medical use in the United States in 1998.[3] It is on the World Health Organization's List of Essential Medicines.[8] It is available as a generic medication.[4] In the United Kingdom it costs the NHS about £1,194 per month as of 2018.[4] This amount in the United States costs about US$9,236 as of 2019.[9]