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Pharma From Sure Success > Autacoids > Flashcards

Autacoids Flashcards

1
Q

H3 histamines use:

A

Presynaptic receptors
In heart: decrease histamine release
In sympathetic nerve: decrease NE

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2
Q

H4 receptors are in ……(3)

A

Hematopoetic cells
Eosinophil
Neutrophils
Cd4 T cells

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3
Q

Name an H3 related drug . MOA and use

A

Tiprolisant
MOA: inverse H3
Use: narcolepsy

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4
Q

Problem when using astemizole and terfenadine

A

When used with enzyme inhibitors can cause Torsades de pointes

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5
Q

Prodrug for fexofenadine is …..importance

A

Terfenadine
Does not cause torsades de pointes

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6
Q

5HT is formed from …….

Structures rich in 5HT (6)

A

Tryptophan
1. GIT enterochromaffin cells
2. Platelets
3. Lungs
4. Bone marrow
5. Pineal gland
6. CNS

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7
Q

MOA of 5HT1
MOA of 5HT4
MOA of 5HT2

A

Cerebral vasoconstriction

Hippocampal excitation

Smooth muscle contraction and plt aggregation.

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8
Q

LSD is a …..agonist

MOA of prucalopride. Use for…..

A

5HT2

5HT4, use for constipation

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9
Q

Drug to rx Irritable bowel syndrome with constipation

A

Tegaserod - 5HT4 Agonist

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10
Q

…….receptor of bradykinin activates phospholipase C
Eg of 2 bradykinin B2 receptor antagonists

A

B2

Icatibant: for acute hereditary angioedema

Aprotinin: CABG to minimise bleeding

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11
Q

MOA of zileuton and zafirleukast

A

Zileuton: 5 lipooxygenase inhibitor
Zafirleukast: LT1 receptor antagonist

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12
Q

PG that is a chemoattractant to neutrophils

PG that is increased in hypothalamus during fever

A

PGD2

PGE2

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13
Q

Leukotrienes that increase neutrophil chemo taxis and that which inhibit chemotaxis ?

A

Increase: LTA4,LTB4

Inhibit: lipoxin

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14
Q

Weak COX2 inhibitor is ……

NSAID that do not inhibit PG synthesis is …..(2)

A

Nimesulide

Atypical NSAIDS: Nefopam
Diacerein

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15
Q

Low dose aspirin is beneficial in …… diseases (2)

A

Colon cancer
Alzheimer’s disease

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16
Q

Features of aspirin toxicity

A
  1. Respiratory alkalosis :
    Tinnitus,headache,vertigo,hyperventilation
  2. Respiratory acidosis
  3. Metabolic acidosis
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17
Q

Special feature of aspirin as per dose

A

<2g/d:
increase Uric acid by decreasing Uric acid excretion in urine.

High doses: >2g/d: Uricosuric

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18
Q

First line of drugs for acute gout

A
  1. NSAIDS: indomethacin
  2. Steroids: oral,iv, intra articular: if one or two joints only.
  3. Colchicine
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19
Q

DOC for acute flare if resistance or C/I to first line drugs

A

IL1 receptor antagonist
Canakinumab
Anakinra
Rilunacept

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20
Q

DOC for chronic gout is ……

A

Allopurinol

Inhibit xanthine oxidase.
This leads to decrease in blood uric acid, the body tries to increase blood Uric acid by secreting from tissues.

This opposing factors can ppt urate crystals.

Thus allopurinol not given for acute gout.

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21
Q

Drug to prevent flare up during initial allopurinol rx

A

Colchicine > NSAID

22
Q

Drug for severe chronic tophaceous gout resistant to other drugs

A

Pegloticase iv

Pegylated uricase

Uric acid ————-> allantoin
Uricase

23
Q

Oil of wintergreeen is ……

A

Methylsalicylate- used in iodex

24
Q

Use of sulfasalazine

A

Converted to 5- ASA by bacteria in colon
Rx of ulcerative colitis

25
Q

NSAIDS that are not given iv (2)

A

Diclofenac
Acelofenac

They are 99% protein bound

26
Q

Long acting NSAIDS (2)

A

Piroxicam
Tenoxicam

27
Q

……..NSAID has been banned

A

Rofecoxib secondary to cardio toxicity

28
Q

Major metabolic pathway of PCM
Minor pathway

A

Glucoronide, sulfate conjugation

Cytochrome P450 to form NAPQI which is broken down by glutathione as mercapturic acid that undergoes renal excretion

29
Q

Toxic doses of PCM

A

4-5g/day
Can’t be taken up by glutathione and NAPQI accumulates leading to centrilobular necrosis in liver.

30
Q

MOA of colchicine

A

Antispindle, antimitotic drug
Disrupts microtubules
Inhibit neutrophil migration into joints
( MSU crystals attract WBC leading to I.F and pain- colchicine inhibits that).

31
Q

Uricosuric drugs used in chronic gout (4)

A

Probenecid
Sulfinpyrazone
Benzbromarone
Lesinurad

32
Q

S/E of colchicine (3)

A
  1. GI epithelium : N/V/D/Abdominal pain
    When diarrhoea develops, STOP the drug as colchicine can cause intestinal hemorrhage.
  2. BMS
  3. Myopathy -rhabdomyolysis
33
Q

Colchicine should never be given with …..(3)

A

Colchicine has low therapeutic drug, thus it should never be given with …..

  1. Erythromycin,clarithromycin,azithromycin

Both are metaboliized by CYP3A4 oxidation

  1. P-glycoprotein inhibitors: verapamil, cycloserin
  2. Statins : if given together can cause serious myopathy.
34
Q

Non gout uses of colchicine (6)

A
  1. Pseudogout
  2. Familial Mediterranean Fever
  3. Recurrent pericarditis
  4. Amyloidosis
  5. Scleroderma
  6. Cirrhosis
35
Q

Non gout uses of allopurinol (2)

A

Lymphoma
Leukaemia
To prevent Tumor lysis syndrome

36
Q

Drugs where dose reduction should be done when giving allopurinol or febuxostat

A

Allopurinol (XO inhibitor)(purine analogue)
Febuxostat(XO inhibitor)(non purine)

6MP ( purine analogue) used in cancer
Azathioprine (purine) used in immunosuppressants

Azathioprine ——> 6MP
Prodrug

Azathiprine and 6MP are metabolised by XO, thus when given with febuxostat can cause toxicity.

37
Q

Drugs causing hyperuricemia (3)

A
  1. Thiazides, furosemide
  2. Pyrazinamide, Ethambutol
  3. Aspirin <2g/d
38
Q

Drug with antiHTN and uricosuric action

A

Losartan

39
Q

1st line drugs in Rheumatoid arthritis

A

DMARDS
Methotrexate
Leflunomide
Sulfasalazine
HCQ

40
Q

When are corticosteroids used in RA?

A

As a bridge therapy until DMARDS take effect -slow action -6-10 weeks

41
Q

Drug which increases adenosine extra cellularly

A

Methotrexate

42
Q

Dose for methotrexate

A

High dose : 0.5g/m2 iv
Osteosarcoma
CNS lymphoma
Burkitts lymphoma

Low - moderate dose:
7.5-25 mg/week
RA
Psoriatic arthritis

43
Q

MOA and S/E of DMARDS

A
  1. Methotrexate:
    DHFR inhibitor
    Increase adenosine release

S/E : Hepatotoxicity, BM suppression

  1. Leflunomide:
    Dihydro orate dehydrogenase
    Pyrimidine synthesis inhibitor
    Decrease lymphocytes proliferation

S/E: weight loss, teratogenic, hepatotoxic

  1. Sulfasalazine:
    5ASA + sulfapyradine

S/E: BMS, oligospermia
Hemolysis in G6PD deficiency

  1. HCQ:
    Antimalaria
    S/e: bull’s eye retinopathy
44
Q

Leflunomide should be avoided in …(3)

A

Pregnant
Lactating mothers
Children

45
Q

AntiTNF alpha drugs should not be used with ….(3)

A
  1. Active TB
  2. HBV
  3. Severe CHF
46
Q

2 tests to screen for Tb

A
  1. PPD, Mantoux test
    Does not tell whether the patient has Tb, only that pt is exposed to Tb
    If positive : do sputum for tb
  2. IFN gamma release assay
    WBC of patient + MTBAg —> if exposed= IFN gamma will be elevated
47
Q

Uses of antiTNF drugs (4)

A
  1. Rheumatoid arthritis
  2. Psoriatic arthritis
  3. Ankylosing spondylitis
  4. Inflammatory bowel disease : UC, Crohn’s disease.
48
Q

New drug for SLE

A

Belimumab - antibody against B lymphocytes stimulation

49
Q

MOA of Etanercept

A

Recombinant DNA fusion protein - decoy receptor for TNF alpha

50
Q

Non TNF alpha drugs used for rheumatoid arthritis

A

ATT for RA
1. Anakinra : IL-1 blocker
2. Tocilizumab: IL-6 blocker
3. Tofacitanib : oral drug : JAK 1/3 blocker
4. Rituximab: CD20 blocker
5. Abatacept: T cell costimulation blocker:
Binding to CD80 & 86 , blocking interaction with CD 28.

51
Q

Ruxotinib is used for …..

A

Myelofibrosis : JAK 1/2 blocker

52
Q

Drug regimen for RA

A
  1. Methotrexate alone
  2. If not effective: add DMARD ( sulfazalazine, HCQ, leflunomide)
  3. Add TNF alpha inhibitor

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