NSAIDS and DMARDS Flashcards by Eugene Ward

What are Eicosanoids produced by?

The actions of Phospholipase A2 on cell membranes

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What is the clinical use of Epoprostenol?

Pulmonary hypertension and hemodialysis to harvest platelets

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What is Dinoprostone used for?

Medical abortion and relaxing the cervix for inducing labor

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What are the clinical uses of Misoprostol?

Treating peptic ulcers and medical abortion

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What are the clinical uses of Alprostadil?

Opening ductus arteriosus in neonates and treating erectile dysfunction

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What is the clinical use of Carboprost?

Labor induction

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What is Latanoprost used to treat?

Glaucoma

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What are the three main effects of NSAIDs?

Analgesic (pain-relieving), antipyretic (fever-reducing), and anti-inflammatory effects

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What enzymes do NSAIDs inhibit?

Cyclooxygenase (COX) enzymes, COX-1 and COX-2

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What are the three main categories of NSAID side effects?

Gastrointestinal, renal, and cardiovascular

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What is the primary function of DMARDs in treating inflammatory arthritis?

Slowing down disease progression

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What are four common side effects of DMARDs?

Bone marrow suppression, liver toxicity, gastrointestinal issues, and increased risk of infections

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What is unique about Aspirin’s mechanism of action compared to other NSAIDs?

It irreversibly inhibits COX-1 and COX-2

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What syndrome can Aspirin cause in children?

Reye’s syndrome

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What are three examples of Propionic Acid Derivative NSAIDs?

Ibuprofen, naproxen, and ketoprofen

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What type of arthritis are Oxicam Derivatives primarily used for?

Chronic arthritis

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What are two examples of Indole Derivative NSAIDs?

Indomethacin and sulindac

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What receptors do Fenmate NSAIDs block in addition to COX inhibition?

Prostaglandin receptors

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What is an example of a Benzopyrrole NSAID?

Tolmetin

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What two mechanisms are involved in the action of Phenylacetic Acid NSAIDs?

COX inhibition and blocking the release of Arachidonic acids

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What is the main advantage of Selective COX-2 Inhibitors over traditional NSAIDs?

Lower risk of gastrointestinal side effects

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What makes Nimesulide useful for certain patients?

It can be used in patients allergic to aspirin and other NSAIDs

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How does Ketorolac compare to Indomethacin in potency?

It is 40 times more potent

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What type of drug is Nabumetone?

A prodrug converted to its active form by the liver

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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?

1. Pulmonary hypertension 2. 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?

1. Medical abortion 2. 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?

1. Treating peptic ulcers 2. 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?

1. Opening ductus arteriosus in neonates 2. 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?

1. Pain relief 2. Fever reduction 3. Anti-inflammatory effects 4. 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?

1. Rheumatoid arthritis 2. 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?

1. GI irritation 2. CNS effects 3. 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?

1. COX inhibition 2. Blocking the release of Arachidonic acids

What are three indications for Phenylacetic Acid NSAIDs?

1. Rheumatoid arthritis 2. Osteoarthritis 3. 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?

1. It's a selective COX-2 inhibitor 2. 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?

1. Ulcerative colitis 2. Asthma 3. 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?

1. Rheumatoid arthritis 2. 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?

1. Rheumatoid arthritis 2. 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?

1. Rheumatoid arthritis 2. 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

1. Cyclosporin - binds to cytosolic cyclophilin 2. Tacrolimus (FK 506) - binds to FKB12