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Year 3 Inflammation and GI > DRUGS USED IN THE TREATMENT OF INFLAMMATORY DISEASES(THERAPEUTICS) > Flashcards

DRUGS USED IN THE TREATMENT OF INFLAMMATORY DISEASES(THERAPEUTICS) Flashcards

1
Q

What are the main uses of paracetamol?

A

Paracetamol is mainly used as an analgesic rather than an anti-inflammatory drug due to its action on the central COX enzymes rather than the peripheral COX . It is more tolerated than the other NSAIDs

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2
Q

Ways to overcome overdosing of paracetamol?

A

-Limited legal requirements: this is where tables and capsules cannot be sold in a pack of more than 32 but the pharmacist can sell up to 100.
- Inadvertent overdose: check for duplicate prescribing where the patient may be self medicating with paracetamol or compound formulations which contains paracetamol.

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3
Q

What are the special groups in paracetamol treatment?

A

Children: In children the correct strength should be checked and also a dosing schedule should be used.
Patients with low body weight; Some patients do have a low body weight and may require different doses than other patients.
Patients with liver impairment or those with risk of hepatotoxicity: They are more risk of toxicity so it is advised to use clinical judgement here.

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4
Q

What are the situations where paracetamol is the preferred analgesic over the other ones?

A

-Elderly: there is a need to consider the weight of the patient.
- Patients with hypertension, CVD, renal impairment, GI issues.
-Patients on medications interacting with NSAIDs that is warfarin.

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5
Q

What are the formulations available for paracetamol?

A
  • Tablet, capsule, suspension, suppositories, infusion and compound preparations.
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6
Q

What are the uses of aspirin?

A

-Antiplatelet: it inhibits platelet formation, the dose of 75mg -300mg daily has anti-platelet effect and at this dose, aspirin has no analgesic effect.
- Analgesic: 300-900 every 4-6 hours PRN (max 4g a day)

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7
Q

What are the special groups of aspirin?

A

-It is contraindicated in children under 16 due to the risk of Reye’s syndrome unless when used in the treatment of Kawasaki disease.
- It is contraindicated in patients with previous peptic ulceration, bleeding disorders, severe cardiac failure , previous hypersensitivity to NSAIDs and aspirin. This is because it increases the risk of bleeding and GI irritation due to its antiplatelet effect and exacerbate cardiac failure.
- Caution in patients with asthma because it can cause bronchospasms.

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8
Q

What are the interactions involved with aspirin?

A
  • Drugs that increase the risk of GI irritation and bleeding; eg steroids, NSAIDs, SSRIs and anticoagulants.
  • Drugs that increase the risk of renal side effects like bisphosphonates.
  • Drugs where aspirin increases toxicity like methotrexate and this is because aspirin reduces the excretion of methotrexate which increases the toxicity of the drug.
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9
Q

What are the formulations available for aspirin?

A

Tablet, capsule, dispersible tablet, suppositories and compound formulations like Beecham’s, lemsip, codis 500

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9
Q

What is one of the importance of NSAIDs?

A

NSAIDs when in full effect have lasting analgesic and anti-inflammatory effects. The analgesic effect starts as soon as the first dose and the complete reaction may be up to 1 week. The anti-inflammatory effect may not be achieved up to three 3 weeks.

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10
Q

What are the key side effects of NSAIDs?

A
  • GI mucosa
  • Kidney
    -Cardiovascular system
    It is advised that if an NSAID is indicated the lowest dose should be used and for the shortest possible time.
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11
Q

What are some examples of the standard NSAID (nomn-selective).

A

-Ibuprofen, indomethacin, mefenamic acid, naproxen.

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12
Q

What are the examples of the non-selective but cox-2 preference?

A

diclofenac, etodalac, neloxicam

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12
Q

What are cox-2 selective inhibitors?

A

celecoxib, etoricoxib

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13
Q

What are the GI effects associated with NSAIDs?

A

The Gi effects associated with NSIADs is due to the inhibition of COX-1 which results in epithelial damage, ulceration and bleeding due to reduced mucus production, reduced bicarbonate formation and reduced mucosal blood flow.

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14
Q

What are the types of drugs involved in the different stages of risk in GI effects?

A

-Highest risk: piroxicam, ketoprofen and ketorolac
-Intermediate risk: indomethacin, diclofenac and naproxen.
-Lower risk: ibuprofen (low dose up to 1.2g) and coxibs.
The lowest agent is preferred and for the shortest possible time and not used with other NSAIDs.

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15
Q

What are the key points of NSAIDs in regards to GI?

A
  • Lowest risk agent preferred.
  • start at the lowest dose.
    -Use for the shortest duration (review need)
  • Do not use more than one NSAID at a time
  • Advise medication to be taken with or after food to reduce contact irritation.
  • Co-prescribe with gastropectin in those patients at risk of GI ulceration eg PPI
  • Monitor for adverse events
  • Review patient for risk factors
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16
Q

What are the interactions of NSAIDs in regards to GI?

A

-Aspirin
-Other NSAIDs
-Other drugs that incrsea the risk of GI ulceration and bleeding eg steroids and bisphosphonates.
-Other drugs that increase the risk of bleeding: SSRIs and anticoagulants.

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17
Q

What are the monitoring for NSAIDs in regards to GI?

A

-Reported symptoms of dyspepsia GI irritation.
- Signs of GI bleeding- haemoptysis, dark stools.

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18
Q

What are the risk of the different NSAIDs in regards to CV events?

A
  • Higher risks: COX-2 inhibitors, diclofenac (150mg daily), ibuprofen (2.4g or more daily)
  • Lowest thrombic risk: naproxen 1g daily
  • No evidence of risk -ibuprofen (low doses, 1.2g or less)
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19
Q

What are the key points of NSAIDs in regards to CV events?

A
  • NSAID selection.
  • Use lowest effective dose.
    -Use for the shortest duration.
    -Monitor for adverse events.
  • Review patient for risk factors.
    Cox-2 inhibitors, diclofenac and high dose ibuprofen are contraindicated in ischaemic heart disease and stages of heart failure.

Other non-selective NSAIDs have use cautioned in patients with heart failure, cerebrovascular disease, ischaemic heart disease, risk factors for CVD.

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20
Q

What are the interactions of NSAIDs in regards to CV?

A
  • Antihypertensives (opposite effect)
  • Antiplatelet dose aspirin (75mg) this may be reduced with long term use of NSAIDs.
21
Q

What are the monitoring of NSAIDs in regards to CV?

A
  • Increase occurrence or first occurrence of CV event.
  • Risk factors for increased CV risk- Bp, medical history of diabetes/hypocholesteraemia.
22
Q

What causes the renal side effects of NSAIDs?

A

Prostaglandins in itself play less role im renal function but in situations like advanced age, renal impairment, heart failure, volume depletion, river cirrhosis then prostaglandins have a role in renal function but for healthy patients, it plays a limited role.

23
Q

What are the renal side effects of NSAIDs?

A

Through the effects on the kidney, NSAID use can cause decreased blood flow and increase the risk of acute kidney injury and also can cause sodium and water retention leading to oedema and hypertension.

24
Q

What are the key points of NSAIDs in regards to renal?

A
  • Avoid in those patients with risk of renal impairment, heart failure, volume depletion, liver cirrhosis.
  • Avoid in severe impairment/ avoid or use with caution in other renal impairment.
  • Use the lowest dose for the shortest possible time.
    -Close monitoring of renal function.
25
Q

What are the interactions of NSAIDs in renal?

A
  • Co-prescribed nephrotoxic medicines- diuretics, ACE inhibitors
    -Antihypertensive
  • Lithium and methotrexate: NSAIDs reduce the excretion of these drugs thereby causing toxicity.
26
Q

What are the monitoring of NSAIDs for GI?

A

-Renal function- GFR, urine output, urea.
- Bp
-Electrolytes : sodium and potassium
-Oedema (weight, visual signs

27
Q

How does methotrexate work?

A

Methotrexate works by slowing down the immune system from making new cells and it does this by inhibiting DHFR from converting DHF to THR to N5,N10 methylenetetrahydrofolic acid and hence inhibys the de novo synthesis of purines and pyrimidines but mostly pyrimidines.

28
Q

What can methotrexate be used for?

A

-Higher doses of methotrexate can be used as cytotoxic drugs in cancer therapy.
- Low dose methotrexate can be used to treat immune diseases like RA, psoriasis.

29
Q

What are the routes of administration of methotrexate?

A

Oral (60-90% bioavailable)
IM
SC
oral is the main route but if patient is not able to tolerate the oral route due to GI effects then the other routes can be used to overcome the GI side effects.

30
Q

What are the normal starting doses for methotrexate in the treatment of RA?

A

Methotrexate is administered by giving 2.5 mg tablets only. The patient will receive a test dose of 2.5 mg to remove and idiosyncrasy effects of the drug then a normal starting dose of 7.5 mg once a week can be commenced. This dose can be increased in the range of 2.5 to 5mg in 1-3 weeks up until 20 mg.

31
Q

What are the key counselling points for methotrexate?

A

-It is always co-prescribed with folic acid but it is advisable to let the patient know not to take them on the same day. The day they take methotrexate, they should not take folic acid and vice versa.
- When a patient forgets to take a dose, they can take it in 2 days for which the next week dose should be taken at the normal day, however after 2 days they should not take it and hence miss that week dose.
- Patients on methotrexate should use effective contraceptives when on methotrexate and 3-6 months after the use of methotrexate.
- Patients should always go for their monitoring and blood tests.
-Patients should check for signs of infections like fever, sore throat and mouth ulcers and should alert their health care professional.

32
Q

What are the different monitoring for methotrexate?

A

Before taking the medication, the patient is supposed to undergo baseline tests tom see if they are okay to take methotrexate which include;
-Full blood count (FBCs); to check on their blood and their bone marrow before they start.
- Liver function test; methotrexate can cause hepatotoxicity which can be presented through jaundice.
- Renal function tests: about 80% of methotrexate is eliminated in the kidneys without being touched and hence it is important to see how the kidney can cope with it.
- Urea and electrolytes
- Chest X-ray

When taking the methotrexate the patient is also supposed to go for tests which include Full blood counts, Liver function tests, Renal function tests in 1-2 weeks but once stable then in 2-3 months.
Also the patient is supposed to take a DAS 28 score which involves
- Number of swollen joints/28
- Number of tendon joints/28
- ESR and CRP
- Overall patient wellbeing.
Scores;
- > 5.1= high active disease
- > 3.2 = low active disease
- < 2.6= remission

33
Q

What are the key side effects of methotrexate?

A
  • Feeling sick, diarrhoea and upset stomach: it should normally subside but if it continues, alert your healthcare professional. It may be that the dose of folic acid should be increased.
  • Bone marrow suppression; if the patient finds out they are getting infections easily, bleeding and bruising easily, they are to stop the medications and alert their health care professional. Also patient should check for signs like sore throat, mouth ulcers or sore mouth.
  • Thinning of hair: This is uncommon and the hair usually grows back to normal but if it becomes serious then alert the healthcare professionals.

Situations where the patient needs to stop taking their medication immediately.
- experience shortness of breath
- Signs of jaundice
- Infections including fever, chills or severe sore throats
- New unexplained bleeding or bruising.
- Sever and continuing diarrhoea or vomiting.
- Signs of pregnancy.

34
Q

What are the key contraindications with methotrexate?

A
  • Active infection.
  • Severe renal impairment
    -Hepatic impairment
    -Bone marrow suppression
  • Immunodeficiency
  • Pregnancy and breastfeeding.
35
Q

What are the key cautions with the use of methotrexate?

A

-Surgery
- Renal impairment
- Diarrhoea
- Ascites
- Peptic ulcer
- If never had chicken pox then stay aware with patients with chicken pox.

36
Q

What are the interactions with methotrexate?

A
  • Anti-folates: co-trimoxazole, trimethoprim.
  • NSAIDs
  • Live vaccines
  • Ciclosporin: it can increase the toxicity of methotrexate .
37
Q

What is leflunomide used for?

A

Leflunomide is used for psoriatic arthritis and rheumatoid arthritis.
In rheumatoid arthritis it is given at a dose 100mg daily for three days as a loading dose and followed by decrease to 10-20 mg OD. In some patients, the loading dose can lead to adverse effects and hence can be omitted.

38
Q

What are the monitoring in regards to the use of leflunomide?

A
  • Liver function tests, full blood counts and BP. These tests can are to be done before the treatment and during the therapy.
    During the therapy, they should be done every 2 weeks in the first 6 months then after that every 8 weeks.
39
Q

How long does it take for leflunomide to start to show effect?

A

leflunomide takes about 4-6 weeks before it starts working and may further improve up to 4-6 months.

40
Q

What are some side effects of leflunomide?

A
  • Hepatic impairment ( increases when used with other hepatotoxic drugs and it normally shows in the first 6 months).
  • Bone marrow suppression: leukopenia, anaemia, thrombocytopenia, pancytopenia.
  • Raised blood pressure.

Some common side effects are diarrhoea, alopecia and risk of hepatic failure, skin reactions and dizziness.

41
Q

What are the contraindications with leflunomide?

A
  • Hepatic impairment
  • Severe immunodeficiency
  • Severe infection
    -Severe hypoproteinaemia
  • Pregnancy and breastfeeding
42
Q

What are the cautions that comes with the use of leflunomide?

A

-Administration with hepatotoxic drugs.
- History of TB
- Bone marrow suppression

43
Q

What is the washout procedure that comes with leflunomide?

A

Leflunomide has a long half life of about 1-4 weeks which means it can stay in the body for a long time after cessation and hence if need to start another therapy or there is an interaction and hence needs to cleared from the body, there needs to be a washout procedure which involves;
- stopping the medication
- giving cholestyramine 8g TDS or activated charcoal 50g QDS
- Treating for 11 days
- Can repeat if needed.

44
Q

What are the additional advice of leflunomide to tell patients?

A

-Avoid live vaccines
- Avoid alcohol (increase risk of hepatic impairment)
- Can be taken with or without food.

45
Q

What are the indications of ciclosporin?

A

Ciclosporin is a calcineurin inhibitor and it has multiple effects on the immune system. It is indicated for inflammatory bowel disease, immunosuppressive drugs, psoriasis, severe atopic arthritis and rheumatoid arthritis.

46
Q

How does ciclosporin work?

A

Ciclosporin is a calcineurin inhibitor which blocks the transcription of IL-2 cytokine which is an important cytokine used in the clonal expansion and proliferation of B and T cells and hence slows down the activity of the immune system.

47
Q

What are the side effects of ciclosporin?

A

Headache, tremor, hypertension, hirsutism, renal impairment are the more common side effects of the drug but some side effects like GI, fatigue, convulsions, hyperkalaemia, hyperlipidaemia can be experienced as well.

Ciclosporin is a non-myelosuppression but it is important to know that it is highly nephrotoxic.

The side effects of the ciclosporin are dose dependent which means as the dose decreases, the side effects goes down but if it has been used for a long time, it will not.

48
Q

What are the contraindications of ciclosporin?

A
  • Abnormal baseline renal impairment
  • Malignancy
  • Uncontrolled hypertension
  • Uncontrolled infection
48
Q

What are the monitoring of ciclosporin?

A
  • Renal function
  • Hepatic function
  • Bp
  • Lipids
  • Electrolytes
  • Uric acid
49
Q

What are the cautions of ciclosporin?

A

-Elderly
- Gout
- Hepatic impairment

50
Q

What are the interactions of ciclosporin?

A

Ciclosporin is metabolised by CYP enzymes and hence there is a lot of interactions that can occur.
CYP inducers increases the levels of CYP and hence reduces the levels of ciclosporin. Egs of cyp inducers are rifampicin, carbamazepine, phenobarbital, phenytoin, st john wort.
CYP inhibitors reduce the levels of CYP and hence increases the levels of ciclosporin.
Egs of cyp inhibitors are macrolides, diltiazem, verapamil, lercanidipine, fluconazole, itraconazole, ketoconazole, grapefruit juice.
Statins
Nephrotoxic drugs; NSAIDs, Methotrexate.

Year 3 Inflammation and GI (5 decks)

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