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Azathioprine is an immunosuppressive medication primarily used to increase the activity of the body's immune system.
Answer: False
Azathioprine is an immunosuppressive medication, meaning it functions to reduce, not increase, the activity of the body's immune system.
Azathioprine belongs to the antimetabolites family of medications and is classified as a purine analogue.
Answer: True
Azathioprine is indeed classified as a purine analogue within the broader family of antimetabolite medications, reflecting its mechanism of interfering with purine metabolism.
Which of the following is NOT a common brand name or abbreviation for Azathioprine?
Answer: Cyclosporin
Imuran and Jayempi are common brand names for Azathioprine, and AZA is a common abbreviation. Cyclosporin is a different immunosuppressive medication.
To which family of medications does Azathioprine belong?
Answer: Antimetabolites
Azathioprine is classified as an antimetabolite, specifically a purine analogue, due to its mechanism of interfering with cellular metabolic processes.
What is the chemical formula of Azathioprine?
Answer: C9H7N7O2S
The chemical formula for Azathioprine is C9H7N7O2S, reflecting its molecular composition.
Azathioprine is exclusively administered by injection directly into a vein.
Answer: False
Azathioprine can be administered orally, typically in tablet form, in addition to intravenous injection.
Azathioprine exerts its immunosuppressive effects by directly stimulating the production of RNA and DNA.
Answer: False
Azathioprine's immunosuppressive action involves disrupting, not stimulating, the normal synthesis of RNA and DNA by interfering with purine metabolism.
Azathioprine is absorbed from the gut at approximately 50%, with high variability among patients.
Answer: False
Azathioprine is absorbed from the gastrointestinal tract at an approximate rate of 88%, though its overall bioavailability can vary due to hepatic inactivation.
The active form of Azathioprine, 6-mercaptopurine, is formed through enzymatic conversion in the liver.
Answer: False
Azathioprine is converted to 6-mercaptopurine (6-MP) through reductive cleavage, a process mediated by glutathione and similar compounds in the intestinal wall, liver, and red blood cells, without the need for enzymes.
Azathioprine's immunosuppressive action primarily involves inhibiting purine synthesis, which is crucial for DNA and RNA production.
Answer: True
Azathioprine primarily achieves immunosuppression by inhibiting purine synthesis, thereby disrupting the production of DNA and RNA necessary for immune cell proliferation.
How does Azathioprine primarily achieve its immunosuppressive effect at a cellular level?
Answer: By disrupting the normal process of making RNA and DNA
Azathioprine's immunosuppressive action is primarily achieved by its metabolites interfering with purine synthesis and being incorporated into DNA, thereby disrupting the production and function of RNA and DNA.
What is the approximate absorption rate of Azathioprine from the gut?
Answer: Approximately 88%
Azathioprine is absorbed from the gastrointestinal tract at an approximate rate of 88%, though its overall bioavailability can vary due to hepatic inactivation.
What is the average plasma half-life for Azathioprine itself?
Answer: 26 to 80 minutes
The average plasma half-life of Azathioprine itself is relatively short, ranging from 26 to 80 minutes.
One of Azathioprine's primary uses is to prevent the rejection of transplanted organs, such as kidneys.
Answer: True
Azathioprine is indeed primarily used in organ transplantation, including kidney transplants, to prevent the recipient's immune system from rejecting the allograft.
The World Health Organization does not include Azathioprine on its List of Essential Medicines.
Answer: False
Azathioprine is included on the World Health Organization's List of Essential Medicines, signifying its importance in a basic health system.
In 2018, Azathioprine was among the top 100 most commonly prescribed drugs in the United States.
Answer: False
In 2018, Azathioprine ranked as the 358th most commonly prescribed drug in the United States, not among the top 100.
The FDA has approved Azathioprine for use in kidney transplantation and the treatment of rheumatoid arthritis.
Answer: True
The U.S. FDA has specifically approved Azathioprine for use in kidney transplantation from human donors and for the treatment of rheumatoid arthritis.
Azathioprine is typically used as a standalone therapy for organ transplantation, without other immunosuppressants.
Answer: False
Azathioprine is typically used in combination with other immunosuppressive therapies, such as corticosteroids, to prevent organ rejection.
Combining Azathioprine with other DMARDs is generally recommended for adult rheumatoid arthritis.
Answer: False
While Azathioprine can be combined with NSAIDs and corticosteroids for rheumatoid arthritis, combining it with other disease-modifying antirheumatic drugs (DMARDs) is not recommended.
Azathioprine's onset of action for Crohn's disease is rapid, often showing clinical response within days.
Answer: False
Azathioprine has a slow onset of action for Crohn's disease, often requiring several months for a clinical response.
Azathioprine is considered a 'steroid-sparing' agent because it allows for a reduction in the required dose of steroids.
Answer: True
Azathioprine is used as a 'steroid-sparing' agent in various autoimmune conditions, enabling a reduction in steroid dosage and thus minimizing steroid-related side effects.
Azathioprine is primarily used to treat which of the following conditions?
Answer: Autoimmune diseases and organ transplant rejection
Azathioprine's primary therapeutic applications are in the management of various autoimmune diseases and in preventing the rejection of transplanted organs.
Which organization includes Azathioprine on its List of Essential Medicines?
Answer: The World Health Organization (WHO)
The World Health Organization (WHO) includes Azathioprine on its List of Essential Medicines, recognizing its importance for global health systems.
For which specific conditions has the U.S. FDA approved Azathioprine?
Answer: Kidney transplantation and rheumatoid arthritis
The U.S. Food and Drug Administration (FDA) has specifically approved Azathioprine for use in kidney transplantation from human donors and for the treatment of rheumatoid arthritis.
How is Azathioprine typically used in organ transplantation to prevent rejection?
Answer: In combination with other immunosuppressive therapies like corticosteroids
Azathioprine is typically used in combination with other immunosuppressive agents, such as corticosteroids, to effectively prevent organ rejection in transplant recipients.
In the context of conditions like pemphigus and myasthenia gravis, what does it mean for Azathioprine to be a 'steroid-sparing' agent?
Answer: It helps reduce the required dose of steroids, minimizing side effects.
As a 'steroid-sparing' agent, Azathioprine allows for a reduction in the dosage of concomitant steroid therapy, thereby mitigating the adverse effects associated with long-term steroid use.
Bone-marrow suppression is a common side effect of Azathioprine, particularly in individuals with a genetic deficiency of the TPMT enzyme.
Answer: True
Bone-marrow suppression is a well-documented common side effect of Azathioprine, with increased incidence and severity in patients with reduced or absent TPMT enzyme activity due to genetic variations.
Hypersensitivity reactions like dizziness, diarrhea, and rashes are not known adverse effects of Azathioprine.
Answer: False
Hypersensitivity reactions, including dizziness, diarrhea, fatigue, and rashes, are indeed known adverse effects of Azathioprine.
The International Agency for Research on Cancer (IARC) classifies Azathioprine as a Group 1 carcinogen.
Answer: True
The International Agency for Research on Cancer (IARC) classifies Azathioprine as a Group 1 carcinogen, indicating it is considered carcinogenic to humans.
Transplant patients taking Azathioprine have a significantly lower risk for skin cancer compared to the general population.
Answer: False
Transplant patients taking Azathioprine are at a significantly higher risk for skin cancer, with incidence rates 50 to 250 times greater than the general population.
Long-term overdose of Azathioprine primarily causes severe headaches and muscle cramps.
Answer: False
Long-term overdose of Azathioprine primarily manifests as infections of unclear origin, mouth ulcers, and spontaneous bleeding, stemming from bone-marrow suppression.
What is a significant concern related to Azathioprine's effect on the bone marrow?
Answer: Reduced production of blood cells, leading to conditions like anemia
Azathioprine can cause bone-marrow suppression, which impairs the production of blood cells, potentially resulting in conditions such as anemia, leukopenia, and thrombocytopenia.
What is a potential risk associated with Azathioprine treatment for inflammatory bowel disease?
Answer: Increased risk of lymphoma
Azathioprine treatment for inflammatory bowel disease is associated with an increased risk of lymphoma, including the rare but aggressive hepatosplenic T-cell lymphoma.
Which of the following is NOT listed as an adverse effect of Azathioprine?
Answer: Increased blood clotting
Dizziness, hair loss (in transplant patients), and acute pancreatitis are listed as adverse effects of Azathioprine. Increased blood clotting is not mentioned as an adverse effect.
What monitoring is recommended for patients undergoing Azathioprine treatment due to its effect on bone marrow?
Answer: Regular monitoring of the patient's blood count
Due to the risk of bone-marrow suppression, regular monitoring of the patient's complete blood count is essential during Azathioprine therapy to detect potential hematologic abnormalities.
What is the classification of Azathioprine by the International Agency for Research on Cancer (IARC)?
Answer: Group 1 carcinogen (carcinogenic to humans)
The International Agency for Research on Cancer (IARC) classifies Azathioprine as a Group 1 carcinogen, indicating sufficient evidence of carcinogenicity in humans.
Why are transplant patients taking Azathioprine at a significantly higher risk for skin cancer?
Answer: Due to the accumulation of 6-thioguanine in DNA, triggering cancer with UVA light exposure.
The increased risk of skin cancer in transplant patients on Azathioprine is attributed to the accumulation of 6-thioguanine in their DNA, which makes them abnormally sensitive to UVA light and can trigger carcinogenesis upon exposure.
What are the main symptoms of a long-term overdose of Azathioprine?
Answer: Infections of unclear origin, mouth ulcers, and spontaneous bleeding
Long-term Azathioprine overdose primarily manifests as symptoms related to severe bone-marrow suppression, including unexplained infections, oral ulcerations, and spontaneous hemorrhage.
Allopurinol can increase the toxicity of Azathioprine by inhibiting an enzyme responsible for its breakdown.
Answer: True
Allopurinol inhibits xanthine oxidase, an enzyme that metabolizes Azathioprine, thereby increasing Azathioprine's concentration and potential toxicity.
Azathioprine decreases the effects of both nondepolarizing and depolarizing muscle relaxants.
Answer: False
Azathioprine decreases the effects of nondepolarizing muscle relaxants but increases the effect of depolarizing muscle relaxants.
Genetic variations in the TPMT gene can lead to increased TPMT enzyme activity, reducing the risk of bone-marrow suppression with Azathioprine.
Answer: False
Genetic variations in the TPMT gene typically lead to *decreased* or *absent* TPMT enzyme activity, which *increases* the risk of severe bone-marrow suppression with Azathioprine.
How does allopurinol interact with Azathioprine?
Answer: It inhibits an enzyme that breaks down Azathioprine, potentially increasing its toxicity.
Allopurinol inhibits xanthine oxidase, an enzyme involved in Azathioprine's metabolism, which can lead to increased levels of Azathioprine and heightened toxicity.
What severe interaction has been reported between Azathioprine and niacin (vitamin B3)?
Answer: Pellagra and fatal medullary aplasia
A severe interaction between Azathioprine and niacin has been reported, leading to pellagra and fatal medullary aplasia, a critical bone marrow failure.
What is the role of the thiopurine S-methyltransferase (TPMT) enzyme in Azathioprine's metabolism?
Answer: It is responsible for methylating 6-mercaptopurine into an inactive metabolite.
The TPMT enzyme plays a critical role in the deactivation of 6-mercaptopurine, an Azathioprine metabolite, by methylating it into an inactive form, thereby preventing its conversion to cytotoxic thioguanine nucleotides.
What is the approximate frequency of TPMT polymorphisms that lead to decreased enzyme activity in many ethnicities?
Answer: Approximately 5%
TPMT polymorphisms resulting in decreased or absent enzyme activity are observed in approximately 5% of many ethnic populations, with about 0.25% being homozygous for these variants.
A 2003 study indicated that Azathioprine use during pregnancy was associated with a seven-fold increase in fetal abnormalities.
Answer: True
A 2003 population-based study in Denmark reported a seven-fold increase in fetal abnormalities associated with Azathioprine and related mercaptopurine use during pregnancy.
Transplant patients should discontinue Azathioprine if they become pregnant due to severe contraindications.
Answer: False
Transplant patients already on Azathioprine are generally advised not to discontinue the medication upon becoming pregnant, unlike other immunosuppressants that are strictly contraindicated.
What is the recommendation for transplant patients regarding Azathioprine use during pregnancy?
Answer: They should not discontinue the medication upon becoming pregnant.
For transplant patients already on Azathioprine, it is generally recommended not to discontinue the medication during pregnancy, unlike certain other immunosuppressants.
Azathioprine was first synthesized in the early 1980s.
Answer: False
Azathioprine was first synthesized in 1957, not the early 1980s.
A 2007 Cochrane review found that Azathioprine increased the number of relapses in the first year of treatment for multiple sclerosis patients.
Answer: False
A 2007 Cochrane review actually found that Azathioprine reduced the number of relapses in the first year of treatment for multiple sclerosis patients.
Robert Schwartz's research in 1958 showed that 6-mercaptopurine enhanced antibody formation in rabbits.
Answer: False
Robert Schwartz's 1958 research demonstrated that 6-mercaptopurine profoundly suppressed, rather than enhanced, antibody formation in rabbits.
Sir Roy Calne initially introduced cyclosporin as an experimental immunosuppressant for transplantation before Azathioprine.
Answer: False
Sir Roy Calne initially introduced 6-mercaptopurine (a metabolite of Azathioprine) as an experimental immunosuppressant, and later Azathioprine itself. Cyclosporin was introduced much later, in 1978.
Mycophenolate mofetil is increasingly preferred over Azathioprine in organ transplantation due to its lower cost and similar side effect profile.
Answer: False
Mycophenolate mofetil is increasingly favored despite being more expensive, due to its association with less bone-marrow suppression, fewer opportunistic infections, and a lower incidence of acute rejection, not a similar side effect profile.
When was Azathioprine first synthesized?
Answer: 1957
Azathioprine was first synthesized by George Herbert Hitchings and Gertrude Elion in 1957.
What did a 2012 study conclude about a therapy combining Azathioprine with prednisone and N-acetylcysteine for idiopathic pulmonary fibrosis?
Answer: It produced worse outcomes compared to a placebo.
A 2012 study demonstrated that the combination therapy including Azathioprine for idiopathic pulmonary fibrosis resulted in worse outcomes than a placebo, leading to a reevaluation of this treatment approach.
Who were the scientists credited with synthesizing Azathioprine?
Answer: George Herbert Hitchings and Gertrude Elion
Azathioprine was synthesized by the Nobel laureates George Herbert Hitchings and Gertrude Elion in 1957.
What was the initial intended use of Azathioprine after its synthesis?
Answer: As a chemotherapy drug
Upon its synthesis, Azathioprine was initially developed and used as a chemotherapy agent.
What did Robert Schwartz discover about 6-mercaptopurine's effect on the immune response in rabbits?
Answer: It profoundly suppressed antibody formation.
Robert Schwartz's research in 1958 revealed that 6-mercaptopurine, a metabolite of Azathioprine, profoundly suppressed antibody formation in rabbits, indicating its immunosuppressive properties.
When did successful human kidney allotransplantation become possible using Azathioprine and prednisone?
Answer: 1962
Successful human kidney allotransplantation, utilizing regimens that included Azathioprine and prednisone, was first achieved in April 1962.
Why is mycophenolate mofetil increasingly favored over Azathioprine in organ transplantation?
Answer: It is associated with less bone-marrow suppression and fewer opportunistic infections.
Mycophenolate mofetil is increasingly preferred in organ transplantation due to its more favorable safety profile, including less bone-marrow suppression and a reduced incidence of opportunistic infections and acute rejection, despite its higher cost.