Nsaids

Front 1

What are the general common properties of NSAIDs? (List 6)

Back 1

• Anti-inflammatory,analgesic, antipyretic

• Weak Organic acids (exceptNabumitone)

• GastricIrritants (except selective COX-2)

• InhibitPlatelet Aggregation (except COX-2, salicylates)

• Nephrotoxicity,GI bleeding, Hepatotoxicity, Hypers. Rn.

• Wellabsorbed, metablolized, protein bound (98%)

Front 2

List 4 Propionic acid derivatives:

Back 2

Ibuprufen, ketoprofen, naproxen, oxaprosin

Front 3

List 2 indole derivatives

Back 3

Indomethacin, sulindac

Front 4

Name 3 pyrrole acetic acid derivatives

Back 4

Ketorolac, tolmetin, nabumetone

Front 5

Phenylacetic acid derivatives include _________. (one)

Back 5

diclofenac

Front 6

Name two fenamates type NSAIDs

Back 6

Meclofenamic acid, meclofenamate

Front 7

Give an example of an oxican type NSAID.

Back 7

piroxicam

Front 8

An example of a pyrazolone derivative is

Back 8

phenylbutazone

Front 9

What are some common names, indications, mechanism of action, pharmacokinetics, side effects and contraindications of Ibuprofen?

Back 9

Names: Advil,Exedrin, Motrin

•Racemicmixture of 2 isomers; l-isomer is active

• Indications: Rheumatoid Arthritis, Osteoarthritis,Dysmenorrhea, mild to moderate pain

•Action: Competitively inhibits COX-1 and COX-2equally, Decrease platelet aggregation

•Pharmacokinetics:Orally 80% absorbed from gut;

•Half life:2 h

•SideEffects: GI irritation andbleeding, nausea, rash, nephrotoxicity

•Contraindication: Patient with coagulation deficit

Front 10

Give for Ketoprofen the:

name

indications

action

pharmacokinetics

half life

side effects

contraindications

Back 10

Name: Orudis

Same asibuprofen

Indications: Rheumatoid Arthritis, Osteoarthritis,Dysmenorrhea, mild to moderate pain

Action: Competitively inhibits COX-1 and COX-2,Inhibits lipoxygenase

Pharmacokinetics:Orally 100% absorbed from GItract

Halflife: 1.8 h

SideEffects: GI upset, headache,Nephrotoxicity (BUN)

Contraindication: Patients with renal impairment

Front 11

For Naproxen provide the:

Name

Indications

Action

Pharmacokinetics

Half Life

Side effects

Back 11

Name: Aleve

Same as ibuprofen, available as anion and sodium salt

Indications: Rheumatoid Arthritis

Action: Competitively inhibitsCOX-1 and COX-2 equally

Pharmacokinetics: Orally 100% absorbed fromGI tract; Naproxen sodium rapidly absorbed than acid, 99% bound to albumin

Half life: 14 h

Side Effects: GI upset and bleeding,headache, allergic reactions

Front 12

For Oxaprosin provide the:

Name

Indications

Action

Pharmacokinetics

Half Life

Side effects

Back 12

Name: Daypro

-Same asibuprofen but very long half life, once a day, mild uricosuric

Indications:Rheumatoid Arthritis,Osteoarthritis; Gouty arthritis

Action:Competitively inhibits COX-1and COX-2

Pharmacokinetics:Orally well absorbed from GItract. Rapid dissociation and absorption; 99% bound to albumin, Bioavailability(95%), Metabolized in liver by microsomal oxidation (65%) and glucuronic acidconjugation (35%)

Half life:50-60 hr

SideEffects: Nausea, Vomiting, GIirritation

Front 13

For Indomethacine, please provide the:

Name

Indications

Action

Pharmacokinetics

Half Life

Side effects

Back 13

Name: Indocin- Potent non-selectiveCOX inhibitor

Indications: RheumatoidArthritis, Osteoarthritis, Gouty Arthritis

Action: Competitivelyinhibits COX-1 > COX-2; Targets PLA and PLC.

Pharmacokinetics: Orally well-absorbed from GI tract

Half life: 4-5 hDecreases T and B lymphocyteproliferation

Side Effects: More toxic than other NSAIDs; 35-50% patients; GI: Nausea, Diarrhea, Ulcer, bleeding; CNS: Headache (25-50%); Blood dyscrasias: Thrombocytopenia,Aplastic anemia; Eye: Blurred vision

Contraindication: Nasal polyps, angioedema, may precipitate Asthma

Front 14

For Sulindac give the:

Name

Indications

Action

Pharmacokinetics

Half Life

Side effects

Back 14

Name: Clinoril--> Sufoxide prodrug metabolizedto active sulfide metabolite

Indications: Rheumatoid Arthritis

Action: Competitively inhibits COX-1 and COX-2;decreases T and B cell proliferation

Pharmacokinetics: Orally-Well absorbed from GI tract (90%);Renal excretion (50%)

Half-life: 8 hrs

Sideeffects: GI pain, constipation,blood dyscrasias, thrombocytopenia, agranulocytosis

Also usedfor regression of colorectal polyps

Front 15

_________ is a sufoxide prodrug metabolized to active sulfide metabolite used to treat the symptoms of Rheumatoid Arthritis.

Back 15

Sulindac

Front 16

Also used for regression of colonorectal polyps:

Back 16

Sulindac

Front 17

________ is more toxic than other NSAIDS. Its side effects include: GI: Nausea, Diarrhea, Ulcer, bleeding; CNS: Headache (25-50%); Blood dyscrasias: Thrombocytopenia, Aplastic anemia; Eye: Blurred vision.

Back 17

Indomethacine

Front 18

This medication apart from inhibiting COX-1 and COX-2 also targets phospholipase A and C.

Back 18

Indomethacine

Front 19

Contraindicated in nasal polyps, angioedema, may precipitate Asthma.

Back 19

Indomethacine

Front 20

This drug is like Ibuprofen but with a very long half life, once a day, mild uricosuric. It is indicated for: Rheumatoid Arthritis, Osteoarthritis; Gouty arthritis.

Back 20

Oxaprosin

Front 21

Contraindicated in patients with renal impairment.

Back 21

Ketoprofen

Front 22

It is a racemic mixture of 2 isomers. The l-isomer is the active one. It is used for rheumatoid arthritis, osteoarthritis, dysmenorrhea, mild to moderate pain.

Back 22

Ibuprofen

Front 23

Contraindicated in patients with a coagulation deficit.

Back 23

ibuprofen

Front 24

This drug is the same as ibuprofen, it is available as anion and sodium salt. It competitively inhibits COX-1 and COX-2 equally. This NSAID is indicated for the treatment of rheumatoid arthritis.

Back 24

Naproxen

Front 25

________ is also known as Relafen.

Back 25

Nabumetone

Front 26

The NSAID called __________ is a prodrugmetabolized to active metabolite 6-methoxy-2-naphthylacetic acid (6-MNA).

Back 26

Nabumetone

Front 27

This NSAID is the only 1-naphthaleneacetic acid derivative.

Back 27

Nabumetone

Front 28

This NSAID competitively inhibits COX-1 and COX-2 and is used for Rheumatoid Arthritis and Osteoarthritis.

Back 28

Tolmetin (Tolectin)

Front 29

______ is given orally and is well-absorbed from GI tract. Some of its side effects include GI, nausea,vomiting, headache.

Back 29

Tolmetin

Front 30

These NSAIDS are used to treat RheumatoidArthritis, Osteoarthritis, Analgesia, dysmenorrhea and act by competitively inhibiting COX-1, COX-2 and PLA2.

Back 30

Meclofenamate and Mefenamic Acid

Front 31

These are contraindicated in: Renal disease, GI diseases,Pregnant women, children

Back 31

Meclofenamate and Mefenamic Acid

Front 32

This NSAID inhibits COX-1 more than COX-2.

Back 32

Piroxicam

Front 33

_______ has a very long half-life it can be up to approximately 50 hours.

Back 33

Piroxicam

Front 34

Side effects for __________ are: : ~20% bleeding, ulceration inelderly, headach.

Back 34

Piroxicam

Front 35

This treatment is indicated for RheumatoidArthritis and/or acute gouty arthritis.

Back 35

Phenylbutazone

Front 36

It is a very potent anti-inflammatory drug, very toxic.

Back 36

Phenylbutazone

Front 37

This NSAID causes seriousagranulocytosis and aplastic anemia. It is currently out ofmarket in USA; Rarely used

Back 37

Phenylbutazone

Front 38

_______________ has a half-life of 60 hours.

Back 38

Phenylbutazone

Front 39

This was the firstselective COX-2 inhibitor

Back 39

Celecoxib

Front 40

Inhibits COX-2>20x than COX-1.

Back 40

Celecoxib

Front 41

This is the newest selective NSAID onthe market. It is highly selective COX2 and it is mainly used for RA and dysmenorrhea.

Back 41

Valdecoxib

Front 42

This NSAID is sensitive to sulfonamides.

Back 42

Valdecoxib

Front 43

This selective COX-2 inhibitor is used for RA, osteoarthritis, dysmenorrhea, and acute pain. It is contraindicated in:Edema,hypertension, CV problems…which lead to its discontinuation.

Back 43

Rofecoxib

Front 44

The half-life of this NSAID is 17hours.

Back 44

Rofecoxib

Front 45

This is the most widely prescribed Disease-modifyingantirheumatic drugs (DMARD).

Back 45

Methotrexate

Front 46

This type of DMARD is used for Rheumatoidand psoriatic arthritis (psoriasis).

Back 46

Methotrexate

Front 47

The mechanism of action of Methotrexate is:

Back 47

Promotesadenosine accumulation and release by inhibiting AICAR transformylase andthymidylate synthetase

Front 48

What are the side effects of Methotrexate?

Back 48

nausea, diarrhea, hepatoxicity,hypersensitivity

Front 49

__________ is contraindicated in pregnant women.

Back 49

methotrexate

Front 50

The active metabolite of cyclophosphamideand chlorambucil is....

Back 50

Activemetabolite: phosphoramide mustard

Front 51

______ and ______ are used for RA, lupus erythematosus, and vasculitis.

Back 51

cyclophosphamide and chlorambucil

Front 52

The mechanism of action cyclophosphamide and chlorambucil is:

Back 52

Cross-linksDNA to prevent cell replication; suppresses T and B cell function

Front 53

Bone marrowsuppression, and infertility are side effects of:

Back 53

cyclophosphamide and chlorambucil

Front 54

This is a synthetic DMARD

Back 54

Azathioprine

Front 55

The major metabolite of __________ is 6-thioguanine.

Back 55

Azathioprine

Front 56

______________ inhibitsinosinic acid synthesis, inhibits T and B cell function, inhibits IL-2secretion.

Back 56

Azathioprine

Front 57

The two main side effects of _________ is bone marrow suppression and GItoxicities.

Back 57

Azathioprine

Front 58

This is an antibiotic and nonbiologic DMARD.

Back 58

Cyclosporine

Front 59

____________ is used for RA, lupus erythematosus, and polymyositis.

Back 59

Cyclosporine

Front 60

What is the mechanism of action of cyclosporine?

Back 60

Inhibits IL-1, IL-2, macrophage-T cellinteraction, T-cell responsiveness, B cell function

Front 61

__________ is Metabolized by CYP3A.

Back 61

Cyclosporine

Front 62

This drug is 20-30% bioavailable, grapefruitincreases it to ~60%.

Back 62

Cyclosporine

Front 63

Chronic use of ____________ can lead to • cardiotoxicity,sterility, bladder cancer.

Back 63

Cyclosporine

Front 64

______ causes side effects such as leukopenia, thrombocytopenia,anemia.

Back 64

Cyclosporine

Front 65

This is a type of Non-biologicDMARD that is rapidly converted to its active metabolite: A77-1726.

Back 65

Leflunomide

Front 66

Response in RA is increased from ~20% to ~46% when _____________ is combined withmethotrexate.

Back 66

Leflunomide

Front 67

What is the mechanism of action of Leflunomide?

Back 67

inhibitsdihydroorotate dehydrogenase,decreases ribonucleotide synthesis; cell cycle arrest; T-cell proliferation; Bcell function

Front 68

Some side effects of Leflunomide are: (5)

Back 68

diarrhea, elevation of liverenzymes, mild alopecia, weight gain, increased bloodpressure

Front 69

A non-biologic DMARD that is contraindicated in pregnant women.

Back 69

Leflunomide

Front 70

______________ is metabolizedto sulfapyridine and 5-aminosalicylic acid.

Back 70

Sulfasalazine

Front 71

Sulfasalazine is indicated for (3):

Back 71

RA,chronic arthritis, ankylosing spondylitis

Front 72

The mechanism of action of this drug is reduction in IgA and IgM production and decreased T and B cell function.

Back 72

Sulfasalazine

Front 73

Due its side effects 30% of patients discontinue its use.

Back 73

Sulfasalazine

Front 74

These drugs are indicated for patientswith active synovitis after 3-4 months of NSAIDs, active inflammation anderosive changes, rheumatoid arthritis and juvenile RA.

Back 74

OrganicGold Salts

Front 75

The mechanism of action of organic gold salts is?

Back 75

suppressesmacrophages, reduces histamine release from mast cells, inhibits lysosomalenzymes

Front 76

Are contraindicated in pregnant women, renal andhepatic impairment patients.

Back 76

organic gold salts

Front 77

This NSAID is more effective for the treatment of Malaria,serositis, and lupus erythematosus. It was approved for RA but it was not as effective for it.

Back 77

Antimalarials: Chloroquine(Aralen); Hydroxychloroquine (Plaquenil)

Front 78

Some of the side effects of this drug are: ocular,dyspepsia, nausea, vomiting, abdominal pain, rashes, nightmares. What drug is this?

Back 78

OrganicGold Salts

Front 79

This NSAID is a metabolit of penicillin and is not used in the clinic

Back 79

Penicillamine

Front 80

_____________ is indicated for patients that didn’t respond to gold compound therapies.

Back 80

Penicillamine

Front 81

The mechanism of action of __________ is decreased lymphocyte function,DNA, collagen and mucopolysaccharides.

Back 81

Penicillamine

Front 82

Contraindications for the use of penicillamine includes (4):

Back 82

Rash, GI, myelosuppression,blood dyscrasias

Front 83

This NSAID is used orally for relief ofsevere arthritis involving many joints but prolongued use has serious toxicity issues.

Back 83

Corticosteroids

Front 84

This NSAID blocks IL-1 receptor and is indicatedfor the treatment of moderate to severe RA.

Back 84

Anakinra

Front 85

The mechanism of action of Anakinra is:

Back 85

• Decreasespain and inflammation caused by IL1

It is given by daily subcutaneous injection.

Front 86

One of its side effects is neutropenia.

Back 86

Anakinra

Front 87

____________ is a scavengerantibody to human TNF-alpha. It is given by IV in 4-8 week intervals.

Back 87

Infliximab

Front 88

The half-life of Infliximab is

Back 88

8-12 days

Front 89

The side effects of ___________ include: Upper respiratorytract infections; nausea, headache, rash, antibodies against it (humananti-chimeric antibodies-~50%).

Back 89

Infliximab

Front 90

This is a fully human anti TNF alpha monoclonalantibody given weekly in subcutaneous injection.

Back 90

Adalimunab

Front 91

The mechanism of action of Adalimumab is:

Back 91

Scavengerof TNF alpha; downregulates macrophage and T cell activity

Front 92

The most common side effects of _________ are infection, leukopenia.

Back 92

Adalimumab

Front 93

The NSAID ___________ is a recombinantfusion protein of two soluble TNF p75 receptors linkedto the Fc portion of human IgG.

Back 93

Etanercept

Front 94

This drug is given by subcutaneous injection twice a week. Its half-life is 4-5 days.

Back 94

Etanercept

Front 95

The most common side effects of etanercept are:

Back 95

erythema,pain, swelling, anti-etanercept ab’s