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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
NSAIDS that are not given iv (2)
Diclofenac Acelofenac They are 99% protein bound
26
Long acting NSAIDS (2)
Piroxicam Tenoxicam
27
……..NSAID has been banned
Rofecoxib secondary to cardio toxicity
28
Major metabolic pathway of PCM Minor pathway
Glucoronide, sulfate conjugation Cytochrome P450 to form NAPQI which is broken down by glutathione as mercapturic acid that undergoes renal excretion
29
Toxic doses of PCM
4-5g/day Can’t be taken up by glutathione and NAPQI accumulates leading to centrilobular necrosis in liver.
30
MOA of colchicine
Antispindle, antimitotic drug Disrupts microtubules Inhibit neutrophil migration into joints ( MSU crystals attract WBC leading to I.F and pain- colchicine inhibits that).
31
Uricosuric drugs used in chronic gout (4)
Probenecid Sulfinpyrazone Benzbromarone Lesinurad
32
S/E of colchicine (3)
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
Colchicine should never be given with …..(3)
Colchicine has low therapeutic drug, thus it should never be given with ….. 1. Erythromycin,clarithromycin,azithromycin Both are metaboliized by CYP3A4 oxidation 2. P-glycoprotein inhibitors: verapamil, cycloserin 3. Statins : if given together can cause serious myopathy.
34
Non gout uses of colchicine (6)
1. Pseudogout 2. Familial Mediterranean Fever 3. Recurrent pericarditis 4. Amyloidosis 5. Scleroderma 6. Cirrhosis
35
Non gout uses of allopurinol (2)
Lymphoma Leukaemia To prevent Tumor lysis syndrome
36
Drugs where dose reduction should be done when giving allopurinol or febuxostat
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
Drugs causing hyperuricemia (3)
1. Thiazides, furosemide 2. Pyrazinamide, Ethambutol 3. Aspirin <2g/d
38
Drug with antiHTN and uricosuric action
Losartan
39
1st line drugs in Rheumatoid arthritis
DMARDS Methotrexate Leflunomide Sulfasalazine HCQ
40
When are corticosteroids used in RA?
As a bridge therapy until DMARDS take effect -slow action -6-10 weeks
41
Drug which increases adenosine extra cellularly
Methotrexate
42
Dose for methotrexate
High dose : 0.5g/m2 iv Osteosarcoma CNS lymphoma Burkitts lymphoma Low - moderate dose: 7.5-25 mg/week RA Psoriatic arthritis
43
MOA and S/E of DMARDS
1. Methotrexate: DHFR inhibitor Increase adenosine release S/E : Hepatotoxicity, BM suppression 2. Leflunomide: Dihydro orate dehydrogenase Pyrimidine synthesis inhibitor Decrease lymphocytes proliferation S/E: weight loss, teratogenic, hepatotoxic 3. Sulfasalazine: 5ASA + sulfapyradine S/E: BMS, oligospermia Hemolysis in G6PD deficiency 4. HCQ: Antimalaria S/e: bull’s eye retinopathy
44
Leflunomide should be avoided in …(3)
Pregnant Lactating mothers Children
45
AntiTNF alpha drugs should not be used with ….(3)
1. Active TB 2. HBV 3. Severe CHF
46
2 tests to screen for Tb
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
Uses of antiTNF drugs (4)
1. Rheumatoid arthritis 2. Psoriatic arthritis 3. Ankylosing spondylitis 4. Inflammatory bowel disease : UC, Crohn’s disease.
48
New drug for SLE
Belimumab - antibody against B lymphocytes stimulation
49
MOA of Etanercept
Recombinant DNA fusion protein - decoy receptor for TNF alpha
50
Non TNF alpha drugs used for rheumatoid arthritis
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
Ruxotinib is used for …..
Myelofibrosis : JAK 1/2 blocker
52
Drug regimen for RA
1. Methotrexate alone 2. If not effective: add DMARD ( sulfazalazine, HCQ, leflunomide) 3. Add TNF alpha inhibitor

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