corticosteroids, DMARDS, AND NSAIDS Flashcards
describe how corticosteroids are released in the body
3
HPA axis ( hypothalamic-pituitary axis )
1-stress causes the release of Corticotropin-releasing hormone from hypothalamus = increases the effect of the sympathetic system ie: increasing HR
2-causes pituitary gland to secrete a substance called adrenocorticotropic hormone (ACTH)
3-adrenal gland ( on top of the kidney ) releases cortisol
contrast Gluco, minercorticosteroids
6
Glucocorticosteroids : 1-Control blood sugar 2-pain relief and anti-inflammatory 3-Widely expressed receptor ie: cortisol and beclomethasone ( asthma )
Mineralcorticosteroids : 1-controls mineral levels 2-Epithelial cell-expressed ( kidney, colon, bladder) 3- Aldosterone (the body produces it) ( synthetic = fludrocortisone )
what are the properties of steroids in clinics
(3)
what do they treat
1- metabolic effects to protect the brain and heart from starvation
2-Anti-inflammatory
3-Immunosuppressive
details of the uses of corticosteroids in inflammation
(2)
short term and long term
short term :
1-suppress early stages of inflammation
( decreases T cells, lymphocyte activators )
Long term effects:
1- Suppression of chronic inflammation by making LIPOCORTIN which stops the formation of phospholipase A2 and other inflammatory mediators
common side effects of steroids
name 3 !
- inhibits HPA axis
-WITHDRAWL = PHASED
-Cushing’s syndrome ( high dose)
-Osteoporosis
-hypotension
-Skin pitting and easy bruising
-euphoria but sometimes depression
( more common in oral corticosteroids )
1) Addison disease
2) Cushing’s syndrome
(4)
1) Addisons = too little + no corticosteroids ( skinny, bronze )
2) Cushing’s = too many corticosteroids ( moon face, abdominal fat, skinny arms and legs though )
mode of action of glucocorticosteroids
(3)
how do they know where to bind?
(1)
- Type 4 cytosolic receptor
- hydrophobic so diffuses through the membrane and binds to a receptor in the cytoplasm
- Conformational change
- Enters nucleus and binds to DNA
How does it know where to bind?
-bar code!
called HORMONE RESPONSE ELEMENTS to tell them where to bind
outline the structure of the adrenal gland?
glowing
fAiries
read
ambitious medicine
from top to bottom
Zona Glomerulosa (cortex) -Mineralcorticosteroids
Zona fasiculata (cortex) -glucocorticosteroids
Zona Reticularis (cortex) - androgens (testosterone etc)
Adrenal medulla -stress hormones ( NE, Epinephrine )
what do NSAIDs treat?
4
1-Anti-inflammatory
2-Analgesic ( pain relief )
3-Anti-pyretic ( reduce fever)
4-Anti platelet
how do NSAIDS WORK? (1)
name common NSAIDS (NSAIK pneumonic )
1- inhibit cox 1 and 2 enzymes, reducing oedema, pain and vasodilation
Naproxen Salicyate acid( aspirin ) Acetylsalicylic acid Ibobrufen Ketorolac
contraindication for NSAIDS PNEUMONIC= NSAIDs
6
Not good for the entire body Sticky blood Asthma worsens Increased bleed risk Dysyfuncitoning kidneys Swelling of the heart and HT worsens
How does paracetamol work? (1)
1- they work by inhibiting the production of prostaglandins in the hypothalamus
PGI 2 effects PGE2 effects thromboxane A2 pGh2 (4)
PGI 2- prostacyclin which causes: vasodilation, antithrombin
PGE2- causes increases in temperature, pain and swelling
Thromboxane = platelet aggregation and vasoconstriction
PGH2= precursor prostaglandin
what does disease-modifying anti-rheumatic drugs do?
(DMARDS)
(3)
1- treat the cause of MSK conditions
2-improves rheumatoid arthritis
3-reduces number of swollen joints, the severity of disease, reduces pain and serum level of IGg (anti inflammatoy=)
what is methotrexate?
WHEN USED, the antagonist of what? who do we never give this to ?
1- 1st line for rheumatoid arthritis
2- folic acid antagonist inhibits Dihydroflurate reductase enzyme = immunosuppressant
3-NEVER GIVE TO PREGNANT WOMEN ( CAUSES NEURONAL DEFECTS AND SPINAL DEFECTS)
