NSAIDS and DMARDS Flashcards
What are Eicosanoids produced by?
The actions of Phospholipase A2 on cell membranes
What is the clinical use of Epoprostenol?
Pulmonary hypertension and hemodialysis to harvest platelets
What is Dinoprostone used for?
Medical abortion and relaxing the cervix for inducing labor
What are the clinical uses of Misoprostol?
Treating peptic ulcers and medical abortion
What are the clinical uses of Alprostadil?
Opening ductus arteriosus in neonates and treating erectile dysfunction
What is the clinical use of Carboprost?
Labor induction
What is Latanoprost used to treat?
Glaucoma
What are the three main effects of NSAIDs?
Analgesic (pain-relieving), antipyretic (fever-reducing), and anti-inflammatory effects
What enzymes do NSAIDs inhibit?
Cyclooxygenase (COX) enzymes, COX-1 and COX-2
What are the three main categories of NSAID side effects?
Gastrointestinal, renal, and cardiovascular
What is the primary function of DMARDs in treating inflammatory arthritis?
Slowing down disease progression
What are four common side effects of DMARDs?
Bone marrow suppression, liver toxicity, gastrointestinal issues, and increased risk of infections
What is unique about Aspirin’s mechanism of action compared to other NSAIDs?
It irreversibly inhibits COX-1 and COX-2
What syndrome can Aspirin cause in children?
Reye’s syndrome
What are three examples of Propionic Acid Derivative NSAIDs?
Ibuprofen, naproxen, and ketoprofen
What type of arthritis are Oxicam Derivatives primarily used for?
Chronic arthritis
What are two examples of Indole Derivative NSAIDs?
Indomethacin and sulindac
What receptors do Fenmate NSAIDs block in addition to COX inhibition?
Prostaglandin receptors
What is an example of a Benzopyrrole NSAID?
Tolmetin
What two mechanisms are involved in the action of Phenylacetic Acid NSAIDs?
COX inhibition and blocking the release of Arachidonic acids
What is the main advantage of Selective COX-2 Inhibitors over traditional NSAIDs?
Lower risk of gastrointestinal side effects
What makes Nimesulide useful for certain patients?
It can be used in patients allergic to aspirin and other NSAIDs
How does Ketorolac compare to Indomethacin in potency?
It is 40 times more potent
What type of drug is Nabumetone?
A prodrug converted to its active form by the liver
What enzyme does Zileuton inhibit?
LOX (lipoxygenase)
What does Etancercept inhibit?
TNF-α receptor
What enzyme does Methotrexate inhibit?
Dihydrofolate reductase
What two conditions is Sulfasalazine commonly used to treat?
Rheumatoid arthritis and inflammatory bowel disease
What cellular process does Hydroxychloroquine interfere with?
Lysosomal activity and antigen presentation
What does Leflunomide inhibit to reduce lymphocyte proliferation?
Pyrimidine synthesis
What cellular process do Calcineurin inhibitors affect?
Dephosphorylation of NF-AT cells, regulating cytokine release
How do DMARDs differ from NSAIDs in their effect on rheumatoid arthritis?
DMARDs target the underlying disease processes, while NSAIDs provide symptomatic relief
What is a major long-term risk of DMARD use?
Increased risk of infections due to immunosuppression
What is the main trade-off when using selective COX-2 inhibitors instead of traditional NSAIDs?
Lower gastrointestinal risk but potentially higher cardiovascular risk
What is Epoprostenol and what is it an analogue of?
Epoprostenol is an analogue of PGI2
What are the two main indications for Epoprostenol?
- Pulmonary hypertension
- Hemodialysis to harvest platelets
What is Dinoprostone and what is it an analogue of?
Dinoprostone is an analogue of PGE2
What are the two main clinical uses of Dinoprostone?
- Medical abortion
- Relaxing the cervix for inducing labor
What is Misoprostol and what is it an analogue of?
Misoprostol is an analogue of PGE1
What are the two main clinical uses of Misoprostol?
- Treating peptic ulcers
- Medical abortion
What is Alprostadil and what is it an analogue of?
Alprostadil is an analogue of PGE1
What are the two main clinical uses of Alprostadil?
- Opening ductus arteriosus in neonates
- Treating erectile dysfunction
What is Carboprost and what is it an analogue of?
Carboprost is an analogue of PGF2α
What is the main clinical use of Carboprost?
Labor induction
What is Latanoprost and what is it an analogue of?
Latanoprost is an analogue of PGF2α
What is the main clinical use of Latanoprost?
Treating glaucoma
What is the mechanism of action of Aspirin?
Aspirin irreversibly inhibits COX-1 and COX-2 enzymes
What are four indications for Aspirin use?
- Pain relief
- Fever reduction
- Anti-inflammatory effects
- Cardiovascular protection (low dose)
What is a unique side effect of Aspirin in children?
Reye’s syndrome
Name three examples of Propionic Acid Derivative NSAIDs
Ibuprofen, naproxen, and ketoprofen
What is the mechanism of action of Propionic Acid Derivatives?
They reversibly inhibit COX-1 and COX-2 enzymes
What are the main indications for Propionic Acid Derivatives?
Pain, fever, and inflammation
Name two examples of Oxicam Derivative NSAIDs
Piroxicam and meloxicam
What type of COX selectivity does meloxicam have?
Meloxicam is more COX-2 selective
What is the main indication for Oxicam Derivatives?
Chronic arthritis
Name two examples of Indole Derivative NSAIDs
Indomethacin and sulindac
What are two indications for Indole Derivative NSAIDs?
- Rheumatoid arthritis
- Ankylosing spondylitis
What is a severe side effect associated with Indole Derivatives?
Aplastic anemia
Name two examples of Fenmate NSAIDs
Mefenamic acid and Meclofenamate
What is a unique feature of Fenmate NSAIDs besides COX inhibition?
They block Prostaglandin receptors
What is a characteristic of Fenmates related to protein binding?
They have high plasma protein binding
What is an example of a Benzopyrrole NSAID?
Tolmetin
What are three side effects of Benzopyrrole NSAIDs?
- GI irritation
- CNS effects
- Tinnitus
What is a unique feature of Benzopyrroles regarding anticoagulation?
They have high plasma protein binding but do not increase clotting time when given with warfarin
Name two examples of Phenylacetic Acid NSAIDs
Diclofenac and Aceclofenac
What are two mechanisms of action for Phenylacetic Acid NSAIDs?
- COX inhibition
- Blocking the release of Arachidonic acids
What are three indications for Phenylacetic Acid NSAIDs?
- Rheumatoid arthritis
- Osteoarthritis
- Ankylosing spondylitis
What is an example of a Selective COX-2 Inhibitor?
Celecoxib
What is the main advantage of Selective COX-2 Inhibitors?
Lower risk of gastrointestinal side effects
What is the main disadvantage of Selective COX-2 Inhibitors?
Higher cardiovascular risk
What is unique about Nimesulide’s effect on Prostaglandin synthase?
It’s a weak inhibitor of Prostaglandin synthase
What makes Nimesulide useful for certain patients?
It can be used in patients allergic to aspirin and other NSAIDs
How does Ketorolac compare to Indomethacin in terms of potency?
Ketorolac is 40 times more potent than Indomethacin
What type of drug is Nabumetone?
Nabumetone is a prodrug
What are two characteristics of Nabumetone?
- It’s a selective COX-2 inhibitor
- It’s converted to its active form by the liver
What enzyme does Zileuton inhibit?
Zileuton inhibits LOX (lipoxygenase)
What are three indications for Zileuton?
- Ulcerative colitis
- Asthma
- Allergic rhinitis
What does Etancercept inhibit?
Etancercept inhibits the TNF-α receptor
What is the mechanism of action of Methotrexate?
Methotrexate inhibits dihydrofolate reductase, affecting DNA synthesis
What are two indications for Methotrexate?
- Rheumatoid arthritis
- Psoriasis
What is the mechanism of action of Sulfasalazine?
Sulfasalazine has unknown mechanism but shows anti-inflammatory and immunomodulatory effects
What are two indications for Sulfasalazine?
- Rheumatoid arthritis
- Inflammatory bowel disease
What is the mechanism of action of Hydroxychloroquine?
Hydroxychloroquine interferes with lysosomal activity and antigen presentation
What are two indications for Hydroxychloroquine?
- Rheumatoid arthritis
- Lupus
What is the mechanism of action of Leflunomide?
Leflunomide inhibits pyrimidine synthesis, reducing lymphocyte proliferation
What is the main indication for Leflunomide?
Rheumatoid arthritis
What is the mechanism of action of Calcineurin inhibitors?
Calcineurin inhibitors dephosphorylate NF-AT cells, regulating the release of cytokines
Name two examples of Calcineurin inhibitors and their binding targets
- Cyclosporin - binds to cytosolic cyclophilin
- Tacrolimus (FK 506) - binds to FKB12