User:Mr. Ibrahem/Thalidomide
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| Clinical data | |
|---|---|
| Pronunciation | /θəˈlɪdəmaɪd/[1] |
| Trade names | Contergan, Thalomid, Talidex, others |
| Other names | α-Phthalimidoglutarimide |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a699032 |
| License data |
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| Pregnancy category |
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| Routes of administration | By mouth (capsules) |
| Legal status | |
| Legal status | |
| 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] |
| Identifiers | |
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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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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.[4] While it has been used in a number of HIV associated conditions, such use is associated with increased levels of the virus.[4] It is taken by mouth.[4]
Common side effects include sleepiness, rash, and dizziness.[4] Severe side effects include tumor lysis syndrome, blood clots, and peripheral neuropathy.[5] Use in pregnancy may harm the baby, including resulting in malformation of the limbs.[4] In males who are taking the medication, condoms are recommended if their partner could become pregnant.[5] It is an immunomodulatory medication and works by a number of mechanisms including stimulating T cells and decreasing TNF-α production.[4]
Thalidomide was first marketed in 1957 in West Germany, where it was available over the counter.[6][7] When first released, thalidomide was promoted for anxiety, trouble sleeping, "tension", and morning sickness.[7][8] 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.[7][6] 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.[7][4] Those who survived had limb, eye, urinary tract, and heart problems.[6] Its initial entry into the US market was prevented by Frances Kelsey at the FDA.[8] The birth defects of thalidomide led to the development of greater drug regulation and monitoring in many countries.[8][6]
It was approved for medical use in the United States in 1998.[4] It is on the World Health Organization's List of Essential Medicines.[9] It is available as a generic medication.[5] In the United Kingdom it costs the NHS about £1,194 per month as of 2018.[5] This amount in the United States costs about US$9,236 as of 2019.[10]
References[edit]
- ^ "Thalidomide". Oxford English Dictionary (Online ed.). Oxford University Press. (Subscription or participating institution membership required.)
- ^ a b c d Teo SK, Colburn WA, Tracewell WG, Kook KA, Stirling DI, Jaworsky MS, Scheffler MA, Thomas SD, Laskin OL (2004). "Clinical pharmacokinetics of thalidomide". Clinical Pharmacokinetics. 43 (5): 311–27. doi:10.2165/00003088-200443050-00004. PMID 15080764.
- ^ "WHOCC - ATC/DDD Index". www.whocc.no. Retrieved 10 September 2020.
- ^ a b c d e f g h "Thalidomide Monograph for Professionals". Drugs.com. Retrieved 14 November 2019.
- ^ a b c d British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 936. ISBN 9780857113382.
- ^ a b c d Cuthbert, Alan (2003). The Oxford Companion to the Body. Oxford University Press. p. 682. doi:10.1093/acref/9780198524038.001.0001. ISBN 9780198524038.
{{cite book}}: Unknown parameter|name-list-format=ignored (|name-list-style=suggested) (help) - ^ a b c d Miller, Marylin T. (1991). "Thalidomide Embryopathy: A Model for the Study of Congenital Incomitant Horizontal Strabismus". Transactions of the American Ophthalmological Society. 81: 623–674. PMC 1298636. PMID 1808819.
{{cite journal}}: Unknown parameter|name-list-format=ignored (|name-list-style=suggested) (help) - ^ a b c Loue, Sana; Sajatovic, Martha (2004). Encyclopedia of Women's Health. Springer Science & Business Media. p. 644. ISBN 9780306480737.
{{cite book}}: Unknown parameter|name-list-format=ignored (|name-list-style=suggested) (help) - ^ World Health Organization (2019). "World Health Organization model list of essential medicines: 21st list 2019" (Document). hdl:10665/325771.
{{cite document}}: Cite document requires|publisher=(help) - ^ "Thalomid Prices, Coupons & Patient Assistance Programs". Drugs.com. Retrieved 15 November 2019.