Drugs And Arthritis Flashcards by Alice Caporn | Brainscape

Q

Celecoxib is an example of a COX2 inhibitor, true or false

A

True

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Q

Influximab, etenercept and rituximab are examples of anticytokines, true or false

A

True

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Q

The enzyme COX2 produces prostaglandins that are involved in the production of mucous, true or false

A

False

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Q

Sulfasalazine is an example of a DMARD, true or false

A

True

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Q

Methotrexate is a cytotoxic folic acid agonist, true or false

A

False

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Q

Paracetamol has no antipyretic effect, but does have analgesic and anti inflammatory, true or false

A

False

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Q

Side effects of steroid include:

Osteoporosis
Decreased risk of infection
Suppression of normal steroid synthesis due to excessive negative feedback which may precipitate acute adrenal failure

A

1 and 3

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Q

NSAIDs have pyretic actions, true or false

A

False

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Q

NSAIDs have analgesic actions, true or false

A

True

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Q

Misoprostol is a synthetic PG given alongside NSAIDs, true or false

A

True

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Q

NSAIDs have anti inflammatory actions by increasing vasodilation and increasing permeability of venules, true or false

A

False

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Q

What does ‘itis’ mean?

A

Inflammation

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Q

Which disease affects synovial joints?

A

Osteoarthritis

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Q

Where does osteoarthritis commonly occur

A

Knee, shoulder, wrist, ankle, finger

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Q

What is secreted by the synovium and is responsible for the breakdown of collagen

A

Matrix metalloprotinases

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Q

Obesity, gender (female), age (>40), previous joint injury and genetics are all risk factors for which disease?

A

Osteoarthritis

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Q

Which disease causes joint inflammation, especially in the synovial membrane, tendon sheath and bursae

A

Rheumatoid arthritis

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Q

What causes the following symptoms?

Swollen joints, morning stiffness (>30mins), pain

A

Rheumatoid arthritis

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Q

Which disease affects joints bilaterally

A

Rheumatoid arthritis

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Q

Which disease is an autoimmune disorder, antibodies are produced against the cartilage causing it to breakdown

A

Rheumatoid arthritis

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Q

Which disease is 3 times more common in women

A

Rheumatoid arthritis

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Q

RA affects joints, but where else can it effect

A

Other tissues, salivary glands, heart

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Q

What is an eicosanoid and consists of 20 carbon atoms

A

Arachnid onion acid

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Q

What is arachidonic acid derived from

A

Linoleic acid (found in veg oils, nut oils and butter)

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Q

What does phospholipase A2 (PLA2) do?

A

Strips arachidonic acid away from the cell membrane

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Q

What strips arachidonic acid away from the cell membrane

A

Phospholipase A2

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Q

Arachidonic acid is a sub straight for which enzyme

A

COX

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Q

COX causes arachidonic acid to be broken down into what?

A

Prostaglandins, thromboxanes, macrophages

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Q

When arachidonic acid is broken down by COX it potentials the effects of histamine and bradykinin - what does this do?

A

Increases permeability of venules - leading to oedema

Increases sensitivity of C fibres (chronic dull pain)

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Q

Which COX enzyme is expressed in most tissues all the time?

A

COX1

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Q

Which COX enzyme protects GI mucosa

A

COX 1

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Q

Which COX enzyme controls renal blood flow?

A

COX1

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Q

Which COX enzyme is found in inflammatory cells, induced by injury, infection and cytokines

A

COX2

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Q

Which COX enzyme produces inflammatory mediators

A

COX2

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Q

What catalyses the reaction: arachidonic acid –> PGs and Txs

A

All COX enzymes

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Q

Where is COX3 found?

A

The CNS of some species

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Q

What inhibits the COX enzymes, decreasing production of PGs, decreasing production of inflammatory mediators and decreasing inflammation

A

NSAIDs

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Q

True or false, meloxicam is an NSAID

A

True

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Q

What type of drug is indomethacin

A

NSAID

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Q

What are NSAIDs derived from

A

Salaclic acid

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Q

Which NSAID is derived from propyonic acid

A

Ibuprofen

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Q

True or false, NSAIDs have antipyretic, analgesic and anti inflammatory effects

A

True

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Q

How do NSAIDs have an analgesic effect?

A

Reduce the sensitivity of neurons to bradykinin

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Q

NSAIDs are effective against pain of what origin?

A

Muscular/skeletal

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Q

How do NSAIDs have an antipyretic effect?

A

Inhibit the actions of prostaglandins on the hypothalamus

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Q

Which drugs only suppress the signs and symptoms of inflammation

A

NSAIDs

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Q

Which drug inhibits NFkB expression, decreasing transcription of genes for inflammatory mediators

A

Aspirin

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Q

Which drugs may induce asthma attack in asthmatics, cause angioedema, urticaria or rhinitis?

A

NSAIDs

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Q

Who are NSAIDs contraindicated for?

A

Elderly

Patients with cardiac disease/hypertension

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Q

Which NSAID has COX2 selectivity

A

Meloxicam

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Q

COX2 inhibitory NSAIDs; celecoxib and etoricoxib are used mainly in which patients

A

Patients at high risk of serious GI side effects, but little CV risk

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Q

What are the common side effects of COX2 inhibitory NSAIDs celecoxib and etoricoxib

A

Headache, dizziness, skin rash, peripheral oedema

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Q

Is paracetamol an NSAID

A

No

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Q

Why is misoprostol given alongside NSAIDs

A

Preserves the mucous lining of the GI tract by increasing production of mucous and blocking the acid pump

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Q

What are some side effects of misoprostol

A

Diarrhoea

Vaginal bleeding

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Q

Is misoprostol indicated for pregnant women?

A

No, it stimulates uterine contractions

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Q

What can be given as an alternative to misoprostol (synthetic prostaglandin) alongside NSAIDs?

A

Proton pump inhibitor eg. Omeprazole

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Q

Can aspirin be used in patients who are taking warfarin

A

No, aspirin displaces the warfarin bound to plasma cells, therefore potentials warfarins anticoagulant activity

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Q

Does paracetamol have an anti inflammatory effect

A

No

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Q

What is a toxic dose of paracetamol?

A

10-15g

Q

What disease might a patient be taking strontium ranelate for

A

Osteoarthritis

Q

What does the drug strontium ranelate do?

A

Promote osteoblast differentiation/inhibit osteoclast activity

Q

Why is strontium ranelate restricted to the treatment of severe osteoarthritis?

A

It increases risk of MI and thrombotic events

Q

What do osteoclasts do?

A

Strip calcium from the bone

Q

Where are glucocorticoids naturally produced in the body?

A

Adrenal cortex

Q

What pain relief is recommended for rheumatoid arthritis?

A

NSAIDs or opioid analgesics

Q

What hormone is released from the hypothalamus during steroid synthesis

A

Corticotropin releasing hormone

Q

Which hormone is released from the anterior pituitary and acts on the adrenal cortex during steroid synthesis

A

Adrenocorticotropin hormone

Q

Which two steroids are naturally produced by the adrenal cortex

A

Cortisone

Hydrocortisone

Q

Which natural steroid only shows mineralocorticoid actions

A

Aldosterone

Q

Hydrocortisone and cortisone are natural steroids, do they exhibit glucocorticoid actions, mineralocorticoid actions or both

A

Both

Q

Overstimulation of mineralocorticoid receptors by cortisone/hydrocortisone would cause

A

Severe hypertension

Q

Hydrocortisone/cortisone have mineralocorticoid properties, these can be inactivated by enzymes in MC sensitive tissues, where might these be found

A

Kidney

Q

Which synthetic steroid has mainly mineralocorticoid actions

A

Fludrocortisone

Q

Which steroid, with mainly mineralocorticoid activity, might be used to treat Addison’s disease

A

Fludrocortisone

Q

What type of steroid activity does Fludrocortisone have

A

Mineralocorticoid

Q

Dexamethasone, betamethasone, beclomethasone and budesonide are all steroids with which type of activity

A

Glucocorticoid

Q

Which two steroids exhibit mixed glucocorticoid and mineralocorticoid activity

A

Prednisolone

Prednisone

Q

Prednisone and prednisolone and steroids which have which type of activity

A

Mixed glucocorticoid and mineralocorticoid activity

Q

Which two steroids are short acting

A

Cortisone

Hydrocortisone

Q

How would you administer cortisone

A

Twice daily cream or intra-Articular injection

Q

How is hydrocortisone administered

A

Twice daily cream

Intra articular injection

Q

Which steroid is intermediate acting?

A

Prednisolone

Q

What is the duration of action of prednisolone

A

Intermediate acting

Q

How is prednisolone administered

A

Daily oral or intra articular injection

Q

Which steroid is long acting

A

Dexamethasone

Q

What is the route of administration of Dexamethasone

A

Intra articular injection every 3-21 days

Q

True or false, steroids are lipid soluble

A

True

Q

What has anti inflammatory and immunosuppressant actions in rheumatoid arthritis

A

Glucocorticoids

Q

Glucocorticoids have immunosuppressant actions in rheumatoid arthritis, how?

A

Decrease transcription do cytokines (eg. IL-2)

Q

Glucocorticoids have anti inflammatory actions in rheumatoid arthritis, how?

A

Increase synthesis of anti inflammatory proteins (eg. Protease inhibitors)

Q

Which glucocorticoids are used in the treatment of asthma and arthritis

A

Beclomethasone
Budesonide
Prednisolone

Q

True or false, hypotension a cushingoid feature is a common side effect of oral corticosteroids

A

False, hypertension is a cushingoid feature

Q

Which of the following is not a cushingoid feature seen as a result of taking oral corticosteroids
Buffalo hump Increased abdo fat
Muscle wastage Moon face
Osteoporosis Good wound healing
Poor wound healing Increased infection risk

A

Good wound healing

Q

How can you reduce the side effects associated with oral corticosteroids

A

Choose a different route of admin to decrease systemic concerntration
Eg. Topical

Q

Why must patients who have been taking steroid treatment not stop suddenly

A

Synthetic steroids inhibit natural production of steroids, could cause Addison’s crisis

Q

Sulfasalazine, penicillamine and aurothiomalate are all types of what drugs

A

DMARDs disease modifying anti rheumatoid drugs

Q

Which drug is the common 1st drug of choice DMARD in the uk

A

Sulfasalazine

Q

What is the route of administration of sulfasalazine

A

Enteric coated tablet

Q

Which DMARD causes the side effects GI upset, headache, skin reactions and leukopenia

A

Sulfasalazine

Q

Which DMARD is a complex of salicylate (NSAID) and sulphonamide (abx)

A

Sulfasalazine

Q

How does the DMARD sulfasalazine work

A

Scavengers free radicals (which cause damage to joints) produced by neutrophils

Q

How is the DMARD penicillamine administered

A

Orally

Q

When is the peak plasma concerntration of the DMARD penicillamine

A

1-2 hours

Q

Can penicillamine be used in conjunction with sodium aurothiomalate

A

No, cannot be used with gold compounds as it is a metal chelator, it combines with the metal and reduces its activity

Q

Which DMARD produces the following side effects

Rashes, stomatitis, anorexia, taste disturbances, fever, n&v

A

Penicillamine

Q

Which DMARD works by decreasing IL-1 generation, decreasing fibroblast proliferation and decreasing the immune response

A

Penicillamine

Q

How is the DMARD sodium aurothiomalate administered

A

Deep IM injection

Q

How is the DMARD auranofin administered

A

Orally

Q

What are the serious side effects associated with the use of gold compounds for treating rheumatoid arthritis

A

Encephalopathy
Peripheral neuropathy
Hepatitis

Q

How long does it take for the effects of aurothiomalate to work

A

3-4 months

Q

Which DMARD is often used when other treatments fail

A

Anti malarials (chloroquine/hydroxychloroquine)

Q

Which DMARDs have side effects which include n&v, dizziness and blurring of vision

A

Chloroquine/hydroxychloroquine

Q

How long does it take for the therapeutic effects of chloroquine to work in rheumatoid arthritis

A

About 1 month

Q

Anticytokines are proteins, how does this effect their administration

A

Cannot be given orally, as they would be digested

Q

How are anticytokine drugs administered

A

Sub cut or IV injection

Q

Which patients is he use of anticytokine drugs restricted to in rheumatoid arthritis

A

Those who don’t respond well to other DMARDs

Q

Which DMARDs are engineered recombinant antibodies

A

Anticytokine drugs

Q

What type of drugs are the following; etenercept, infliximab, abatacept, adalimumab, natalizumab

A

Anti cytokines

Q

How to the anticytokine drugs rutiximab, abatacept and natalizumab work

A

Target leukocyte receptors disrupting the immune signalling

Q

Which anticytokine drugs target TNF

A

Adalimumab, etenercept, infliximab,

Q

Which DMARDs can be given with methotrexate

A

Anti cytokines

Q

Which DMARDs may cause the development of latent disease, for example TB, hep B, herpes zoster

A

Anticytokines

Q

True or false, rheumatoid arthritis is an autoimmune disorder

A

True

Q

Which drug is a potent immunosuppressant but has no effect on acute inflammation

A

Ciclosporin

Q

Which immunosuppressant given to people with RA inhibits IL-2 gene transcription, decreasing T cell proliferation

A

Ciclosporin

Q

How does the immunosuppressant ciclosporin work

A

Inhibits IL-2 gene transcription, decreasing T cell proliferation

Q

Would ciclosporin be administered orally

A

No, it is poorly absorbed orally; capsules or oral solutions

Q

Which drug can cause; nephrotoxicity, hepatotoxicity, hypertension, n&v, gum hypertrophy, GI problems

A

Ciclosporin

Q

Why can ciclosporin cause toxic effects in the kidneys and liver

A

It accumulates in high concentration in tissues

Q

Which immunosuppressant is cytotoxic, interfering with purine metabolism which decreases DNA synthesis

A

Azathioprine

Q

Which phase of the immune response does azathioprine work at

A

The induction phase

Q

What is the main specific effect of the drug azathioprine

A

Suppression of bone marrow

Q

How does methotrexate work

A

Folic acid antagonist, which inhibits DNA synthesis

Q

Which cells does methotrexate target

A

Blocks the growth and differentiation of rapidly dividing cells

Q

Which drug is often prescribed with a DMARD

A

Methotrexate

Q

Should methotrexate be used in pregnancy

A

No, can cause folate deficiency

Q

Which immunosuppressant is a specific inhibitor of activated T cells

A

Leflunomide

Q

What is the route of administration of leflunomide

A

Oral, long half life

Q

Which immunosuppressant has side effects including, diarrhoea, alopecia, increase in liver enzymes (risk of hepatotoxicity)

A

Leflunomide

Q

Which drugs side effects include blood dyscrasias (abnormalities) and liver cirrhosis and folate deficiency

A

Methotrexate

Q

When is cyclophosphamide used to treat RA

A

When all other therapies have failed

Q

Which immunosuppressant used to treat RA is a pro drug

A

Cyclophosphamide

Q

When the immunosuppressant cyclophosphamide is administered orally it is activated in the liver to what

A

Phosphoramide mustard and acrolein

Q

The pro drug cyclophosphamide is activated in the liver to phosphoramide mustard and acrolein, what can acrolein caus

A

Haemorrhagic cystitis (bleeding from the kidney) can be prevented by administering with very large volumes of fluid

Q

True or false, glucocorticosteroids and other immunosuppressants increase the risk of infection and increase risk of cancer

A

True

Q

In the treatment of RA how effective is hydroxychloroquine, and what else might this drug be used for

A

50% effective, antimalarial

Q

What type of drug is etenercept, how is it usually administered

A

Anticytokine, subcut Twice a week