Arthritis Drugs Flashcards

1
Q

Ibuprofen

A

Non selective cox inhibitor

First choice drug low side effects

Mechanism of action: unknown. It does however inhibit cox and enzyme involved in synthesis of PG at the arachidonic acid pathway.

SE:
Bronchospasm ( asthma)
Nausea, heart burn, headache, dizziness, mild rash.

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2
Q

Aspirin

A

Non selective cox inhibitor

Suppresses production of PG and thromboxane a2 (platelet agrevation) by irreversible inactivation of cox enzyme.

SE:
Nausea, rash bronchospasm, gi ulcer due to reduced mucous production.

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3
Q

Diclofenac

A

Reduced leukocyte migration and PG production due to cox inhibition.

Absorbed in the GI tract completely

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4
Q

Meloxicam

A

Works by reducing PG production.

Don not drink
Do not take aspirin alongside

SE: nausea, diarrhoea, rash, flu symptoms

GI bleeding, swelling, wheezing, heat attack.

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5
Q

Paracetamol

A

Not an NSAID. Does not reduce inflamAtion.

Overdose can cause fatal damage to liver detectable 24, 48 hours post overdose.

SE:

Nausea, fever.

Dark urine or jaundice get help !!

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6
Q

Prednisolone

A

Gluco corticoid receptor agonist.
Metabolised in the liver to active form. Crosses cell membrane and binds with high affinity to cytoplasmic receptors.
Inhibition of leukocyte infiltration and humoral response to inflammation.

SE: acne, dizziness, nausea, sleeplessness

Severe: similar to allergic reaction

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7
Q

Dexamethasone

A

Glucocorticoid agonist
Cross cell membrane and bind with high affinity to receptors.

Inhibit humoral response to inflammation.

SE: nausea, dizziness, rash, sever allergic reaction.

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8
Q

Fludrocortisone

A

Binds to mineralocorticoid receptor ( aldosterone).
Causes and increase in ion and water transport. Raising extra cellular fluid volume and lowering potassium levels.

SE:
Insomnia, acne, headaches, nausea.

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9
Q

Corticosteroids

A

Block gene transcription and synthesis of inflammatory proteins.

Immunosuppressant.

Gluco corticoids
Naturally produced 
Metabolic effect
Anti inflammatory
Immunosuppressive 

Mineralocorticoid
Water and electrolyte balance between

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10
Q

Natural steroids

A

Hydrocortisone/ corticosteroids
Show both MC +GC activities

Aldosterone
Mineralocorticoid only

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11
Q

Steroid duration of action

A

Short acting :
Cortisone / hydrocortisone

Intermediate acting :
Prednisolone

Long acting :
Dexamethasone

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12
Q

Glucocorticoid action in RA

A

Anti inflammatory immunosuppressant
Lower transcription of pro inflammatory cytokines (il-2)
Reduces circulating lymphocytes

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13
Q

Beclamethasone

A

Glucocorticoid used in both asthma and arthritis

Stabilise mast cells

Reduce histamine release

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14
Q

Budesonide

A

GC for arthritis and asthma

Stabilises mast cells reducing histamine release

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15
Q

Unwanted effects of oral corticosteroids

A

Buffalo hump

Moon face

Hypertension

thinning of skin

Increased risk of infection

Poor wound healing

Osteoporosis

Can reduce these by reducing plasma concentration and choosing administration route

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16
Q

Sulfasalazine

A

Disease modifying anti rheumatoid drug

Common 1st choice
Complex of salicylate(nsaid) and sulphonamide (antibiotics)
Scavengers free radicals produced by neutrophils
Causes remission in active RA
Enteric coated tablets
SE: gi upset, headache, skin reaction, leukopenia.

17
Q

Penicillamine

A

Disease modifying anti rheumatoid drug

75% respond but effects take weeks 
Lower il1 generation 
Lower fibroblast proliferation 
Lower immune response 
Given orally 
SE: rashes, stomatitis, anorexia, taste disturbance, fever
NOT TO BE GIVEN WITH GOLD COMPOUNDS
18
Q

Gold compounds

A

Disease modifying anti rheumatoid drug

Oral auranofin - inhibits induction of il1 and tif a reducing pain and joint swelling

Sodium auranofin - deep I’m injection, concentrate in synovial cells, liver cells, kidney tubules, adrenal cortex and macrophages
Effects develop 3-4 months

SE: skin rash, flue, mouth ulcers, blood disorders.

Serious SE: encephalopathy, peripheral neuropathy, hepatitis

19
Q

Anti malarials

A

Chloroquine, hydroxychloroquine

Raise oh of intracellular vacuoles interfering with presenting antigen.

Induces apoptosis in t lymphocytes

Used when other treatments fail
One month for effects

SE: n+v, dizziness, blurred vision,

20
Q

Anti cytokine drugs

A

Engineered recombinant antibodies which bind to specific immune cells, inhibiting immune response

VERY EXPENSIVE

USE restricted to patients who don’t respond well to DMARDS.

Can be given with methotrexate

Given sc or iv injections

SE: may develop latent disease, opportunistic infection, heart failure, hypersensitivity.

21
Q

Adalimumab

A

Anti cytokine drug

Targets TNF

22
Q

Enteracept

A

Anti cytokine drug

Targets TNF

23
Q

Infliximab

A

Anti cytokine drug

Targets TNF

24
Q

Rituximab

A

Anti cytokine drug

Targets leukocyte receptor

25
Q

Abatacept

A

Anti cytokine Drug

Targets leukocyte receptor

26
Q

Tocilizumab

A

Anti cytokine drug

Blocks il6 receptor

Disrupting immune signalling

27
Q

Immunosuppressants

A

Rheumatoid arthritis is an autoimmune disorder

Suppressing the immune system will suppress disease

Inhibit DNA synthesis or T cell activation

Increase risk of infection
Increased risk of cancer

28
Q

NSAIDs

A

Eg, aspirin, ibuprofen, diclofenac, meloxicam.
Tablets, suspensions, gels, injections,
Antipyretic - inhibit PG on hypothalamus
analgesic- reduce sensitivity of neutrons to bradykinin
Anti inflammatory - reduce Vado dilation and vascular permeability.
May inhibit coz 1 (essential for PG production responsible for cv platelet agrevation, and gi mucous) and cox 2( stomach ulcer, cv events)
Scavenge oxygen radicals reducing tissue damage

29
Q

Ciclosporin

A

Immunosuppressant. First discovered in fungus.
Inhibits il2 gene transcription, reduces T cell proliferation.

Poorly absorbed orally

Accumulates in high conc. in tissues

SE: nephrotoxicity, hepatoxicity, hypertension, nausea, gum hyper trophy, GI problems

30
Q

Azathioprine

A

Immunosuppressant

Cytotoxic, interferes with dna synthesis

Depresses cell mediated and antibody mediated immune reactions

Targets cells in induction phase of immune response.

SE - suppression of bone marrow.

31
Q

Methotrexate

A

Immunosuppressant

Folic acid antagonist- inhibits DNA synthesis

Blocks growth and rapid dividing cells
Inhibits T cell activation

SE: blood abnormalities, liver cirrhosis, folate difficiency

Often prescribed with DMARD

32
Q

Leflunomide

A

Immunosuppressant

Specific inhibitor of activated T cells

Well absorbed orally with long t life

SE: diarrhoea, alopecia, high liver enzymes, heptotoxicicty

33
Q

Cyclophosphamide

A

Immunosuppressant

Only used when other therapies have failed

Pro drug - administered orally activated in liver to phosphoramide mustard and acrolein

Acrolein can result in haemohaggic cystitis - give win lots of fluids

34
Q

Osteoarthritis

A

Primary cause- wear and tear

Secondary cause- trauma, disease, obesity

Pain caused through inflammation

35
Q

Rheumatoid arthritis

A

Systemic autoimmune disorder

May affect other tissues

Pain through inflammation