Thalomid (thalidomide)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Thalidomide, a synthetic glutamic acid derivative, is an immunomodulatory agent with anti-inflammatory, antiangiogenic, and sedative and hypnotic activity; the drug is also a potent teratogen.
Thalidomide has immunomodulatory, anti-inflammatory, and antiangiogenic activities. The drug also has sedative and hypnotic effects. Thalidomide is structurally similar to, but pharmacologically different from, glutethimide.
Thalidomide contains a phthalimide ring and a glutarimide ring; the glutarimide ring is similar to that contained in glutethimide and may be responsible for the sedative and hypnotic effects of thalidomide. Because the glutarimide ring has a single asymmetric carbon (chiral center), thalidomide may exist as either an optically active levorotatory or dextrorotatory enantiomer. The enantiomers rapidly interconvert in vivo and in vitro; it is unknown whether the enantiomers have distinct pharmacologic properties.
Thalidomide is commercially available as a 1:1 racemic mixture of the 2 enantiomers with a net optical rotation of zero.
The mechanism(s) of action of the immunomodulatory and anti-inflammatory effects of thalidomide are complex and have not been fully determined. Cellular activities of thalidomide are mediated through its target cereblon, a component of a cullin ring E3 ubiquitin ligase enzyme complex. Data from in vitro models suggest the effects of thalidomide appear to result in part from modulation of tumor necrosis factor alpha (TNF-alpha) levels, costimulatory or adjuvant effect on T-cells resulting in increased T-cell proliferation and increased production of interleukin-2 and interferon-gamma, and/or modulation of leukocyte migration and chemotaxis.
Other anti-inflammatory and immunomodulatory effects of the drug may include suppression of macrophage involvement of prostaglandin synthesis and modulation of interleukin-10 and interleukin-12 production by peripheral blood mononuclear cells.
The immunomodulatory and anti-inflammatory effects of thalidomide differ from those of other immunosuppressive agents, including corticosteroids, cyclosporin (e.g., cyclosporine) or macrolide (e.g., tacrolimus) immunosuppressants, pentoxifylline, immunosuppressive purine analogs (e.g. azathioprine) and purine metabolism inhibitors (e.g., mycophenolic acid), and also differ from those of nonsteroidal anti-inflammatory agents. Thalidomide does not appear to interfere with important host antimicrobial mechanisms; the drug has no substantial inhibitory effect on lymphocyte proliferation, does not impair delayed-type hypersensitivity reactions, and does not impair granuloma formation.
Thalidomide has no direct antibacterial activity against Mycobacterium leprae. In addition, results of an in vitro study using Enterocytozoon bieneusi, Encephalitozoon intestinalis, and E. cuniculi indicate that thalidomide has no direct activity against microsporidia.
USES: This medication is used to treat or prevent certain skin conditions related to Hansen's disease, once known as leprosy (erythema nodosum leprosum). Thalidomide is also used to treat a certain type of cancer (multiple myeloma). It works in Hansen's disease by reducing swelling and redness (inflammation).
It also reduces the formation of blood vessels that feed tumors.
Generic name: thalidomide
Pronunciation: (tha-LID-oh-mide)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Thalomid
Indications
The following indications are listed for Thalomid:
- Erythema Nodosum Leprosum
- Multiple Myeloma
- Prevention Of Cutaneous Erythema Nodosum Leprosum Lesion Recurrence
Also known as: Enl Leprosy Reaction, Erythema Nodosum Leprosum Leprosy Reaction, Immune Complex Reaction Co-Occurrent And Due To Multibacillary Leprosy, Maintenance Therapy For Suppression Of Enl Skin Lesions, Plasma Cell Myeloma, Prevention Of Enl Leprosy Skin Lesion Recurrence, Prevention Of Erythema Nodosum Leprosum Skin Lesion Recurrence, Secondary Prevention Of Enl Leprosy Skin Lesions, Type 2 Lepra Reaction - Erythema Nodosum Leprosum.
Dosing
Temporary interruption of therapy, dosage reduction, and/or permanent discontinuance of thalidomide may be necessary in patients experiencing grade 3 or 4 adverse effects. If constipation, somnolence, or peripheral neuropathy occurs, temporarily interrupt thalidomide therapy and consider dosage reduction upon resumption of therapy.
If angioedema, anaphylaxis, grade 4 rash, skin exfoliation, bullae, or any other severe dermatologic reaction (e.g., grade 4 rash, skin exfoliation, bullae) occurs, thalidomide therapy should be permanently discontinued.
Thalidomide is administered orally. Because administration with a high-fat meal substantially delays the time to peak plasma concentrations of thalidomide, the drug should be administered with water at least 1 hour after a meal.
When thalidomide is given as a single daily dose, the manufacturer recommends that the dose preferably be given at bedtime (to minimize the sedative effects of the drug) with water and at least 1 hour after the evening meal. When high daily dosage of thalidomide is necessary (e.g., 400 mg daily), the daily dose may be given as a single dose at bedtime or, alternatively, in divided doses given with water at least 1 hour after meals.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
In vitro, thalidomide does not inhibit or induce cytochrome P-450 (CYP) isoenzymes at clinically relevant concentrations. Thalidomide is not a substrate of CYP isoenzymes.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Thalidomide is contraindicated in females who are pregnant.
*Thalidomide is contraindicated in patients with known hypersensitivity (e.g., angioedema, anaphylaxis) to the drug or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in at least 20% of patients with multiple myeloma receiving thalidomide include fatigue, hypocalcemia, edema, constipation, sensory or motor neuropathy, dyspnea, muscle weakness, leukopenia, neutropenia, rash/desquamation, confusion, anorexia, nausea, anxiety/agitation, asthenia, tremor, fever, weight loss, thromboembolism, weight gain, dizziness, and dry skin.
Adverse effects reported in at least 10% of patients with erythema nodosum leprosum (ENL) receiving thalidomide include somnolence, rash, and headache.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Although safety and efficacy of thalidomide in pediatric patients younger than 12 years of age have not been established, the drug has been used in a limited number of children 6 months to 12 years of age+. When thalidomide was used for the treatment of graft-versus-host disease in a limited number of bone marrow transplant recipients 1.5-17 years of age+, adverse effects of the drug included somnolence (which required discontinuance of the drug in at least one child), constipation, and a syndrome of rash, eosinophilia, and pancreatitis (which resolved after the drug was discontinued).
When thalidomide was used for the treatment of Crohn disease in a limited number of children and adolescents 2-18 years of age+, the most frequent severe adverse effect was peripheral neuropathy.
Thalidomide is a human teratogen and is contraindicated for use during pregnancy.
It is not known whether thalidomide is distributed into human milk. Because many drugs are distributed into milk, and because of the potential for serious thalidomide-related adverse effects in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the mother.
The manufacturer makes no specific dosage recommendations for geriatric patients.
In clinical trials evaluating thalidomide in combination with dexamethasone, 52% of patients were 65 years of age or older and 15% were 75 years of age or older. Atrial fibrillation, constipation, fatigue, nausea, hypokalemia, thromboembolism, hyperglycemia, and asthenia occurred at a higher incidence compared with younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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