Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

AD1 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What does a Gs subunit of a GPCR do?

A

stimulate adenylate cyclase and increase cAMP production and PKA activation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What does a Gq subunit do?

A

Stimulate phospholipase C, and increase IP3 and diacylglycerol leads to PKC activation and calcium release from the endoplasmic reticulum.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What does Gi/o subunit do?

A

inhibit adenylate cyclase, decrease cAMP production, Beta-Gamma subunit inhibits calcium ion channels and activates potassium ion channels.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Examples of ionotropic receptors?

A
  • serotonin= 5-HT3 receptors
  • ATP= P2X receptors
  • Acetylcholine= nicotinic receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What happens when an inflammatory response goes wrong?

A
  • Type I hypersensitivity
  • Airway disorders
  • autoimmune haemolytic anaemia- dogs
  • sweet itch- horses
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are some of the principle mediators of inflammation

A

Histamine, Bradykinin, nitric oxide, cytokines= interleukins, interferons, chemokines, colony-stimulating factors; Eicosanoids= prostaglandins, thromboxanes, leukotrienes; other plasma proteins= complement, coagulation and fibrinolytic factors; platelet-activating factors, Neuropeptides

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the main vascular responses to inflammation?

A
  • Vasodilation
  • Increased vascular permeability
  • Exudation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Where are mast cells produced?

A

bone marrow, released as immature cells and mature in the tissues.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

where are mast cells found?

A

-beneath the skin, throughout the respiratory system, digestive and urinary tracts

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What receptor do mast cells express?

A

FcεRI with a high affinity to IgE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are the roles of histamine?

A
  • tissue repair and inflammation
  • control of local blood supply- vasodilation and vascular permeability
  • contributes to allergic and anaphylactic reactions
  • neurotransmitters in the CNS
  • Gastric acid secretion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

where is histamine found?

A
  • Throughout the body but in high concentrations around the lungs, skin, GIT, and brain= the interfaces between the body and the outer environment.
  • Present in mast cells and basophils- that contain granules
  • Found in neurones and enterochromaffin-like cells in stomach
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are the steps of Mast cell degranulation?

A
  1. Priming of mast cell
  2. Secondary exposure to the allergen
  3. Binding of IgE which increases Ca²⁺ concentration in cell
  4. Migration and fusion of vesicles with cell membrane
  5. Degranulation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What can inhibit mast cell degranulation?

A

cAMP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What can cause histamine release?

A
  • neuropeptides

- some basic drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

How many histamine receptors are there?

A

4- and they are GPCR

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What are the histamine receptors?

A
  • H1
  • H2
  • H3
  • §H4
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What does H1 histamine receptor do?

A

This is the most important in an inflammatory response:

  • System vasodilation. ) Increased IP3 and DAG- Stimulate Ca²⁺
  • Increased vascular permeability ) ⤴︎
  • itching
  • bronchoconstriction
  • ileum contraction
  • effects on neural action potential firing
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What does the H2 histamine receptor do?

A
  • Stimulate gastric acid secretion – receptor coupling, increases cAMP
  • Relax smooth muscle
  • Speed up heart
  • inhibit antibody and cytokine production
  • inhibit neutrophil activation
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What does H3 histamine receptor do?

A

-Inhibits neurotransmitter release from neurones -> receptor coupling cAMP reduced

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What do H4 histamine receptors do?

A
  • Regulates neutrophil release from bone marrow
  • mast cell chemotaxis
  • receptor coupling reducing cAMP
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are H1 receptor antagonists?

A

Class of drugs that treat or prevent allergies

orally active and hepatically metabolised

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What does a 1st generation H1 receptor antagonist do?

A
  • Able to cross the blood-brain barrier

- 4-6 hours duration, give dose throughout day

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What does the 2nd generation H1 receptor antagonist do?

A
  • Can’t cross the blood-brain barrier

- 12-24 hour duration- one tablet lasts for the whole day.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

What are eicosanoids?

A

Eicosanoids are signalling molecules made by the enzymatic or non-enzymatic oxidation of arachidonic acid. They are generated from phospholipids which are not stored, they are generated on demand. Major involvement in inflammation= pro-inflammatory.
precursors= 20 carbon fatty acids

26
Q

What are the three types of eicosanoid?

A
  • prostaglandin
  • thromboxane
  • leukotriene
27
Q

give some examples of activators for phospholipase A2

A
  • bradykinin
  • antibody-antigen bindings on mast cells
  • thrombin
  • complement C5A
  • Cell damage
28
Q

What does Phospholipase A2 activate?

A
  • Platelet-activating factor
  • Arachidonic acid (precursor)
  • can produce other precursors- if the diet is particularly Omega 3 fatty acid-rich then a slightly different arachidonic acid is produced- PGE3 and PGI3
29
Q

What types of Prostaglandins are there?

A

PGD2, PGE2, PGI2, PGF2𝛼

30
Q

What is the enzyme responsible for converting A.Acid to PGG2/ PGH2?

A

Cyclooxygenase

31
Q

What are the two forms of cyclooxygenase?

A 
COX1= Constitutively expressed by most cells with lots of roles 
COX2=  Not normally present- expression induced by inflammatory factors
32
Q

Which cells produce leukotrienes?

A
  • Leukocytes
  • Lung tissue cells
  • Mast cells
  • Platelets
33
Q

What are the receptor classes for leukotrienes?

A
  • BLT for LTB4- activation and targeting of leukocytes and cytokine production
  • cystLT for others- important in asthma, bronchoconstriction and vasodilation
34
Q

What are the main anti-inflammatories?

A
  • NSAIDS
  • Glucocorticoids
  • H1 receptor antagonists
  • Chondroprotective drugs
  • immunosuppressants
35
Q

What hormones does the anterior pituitary release in response to Corticotropin-releasing factor?

A

Adrenocorticotropic hormone

36
Q

What gland does the Adrenocorticotropic hormone affect?

A

the adrenal gland

37
Q

What does the adrenal gland release?

A
  • mineralocorticoids

- Glucocorticoids- released in a pulsatile fashion and circadian rhythm

38
Q

What are corticosteroids?

A

Steroids released by the adrenal gland.

39
Q

What is the outer layer of the adrenal gland called and what does it release?

A

Zona Glomerulosa

releases: mineralocorticoids- these regulate water and electrolyte balance

40
Q

What’s the inner layer of the adrenal gland called? And what does it produce?

A

Zona fasciculata

Releases: Glucocorticoids

41
Q

What is the main animal glucocorticoid?

A
  • corticosterone
42
Q

What is the main human glucocorticoid?

A

Hydrocortisone

43
Q

What is the process of glucocorticoid action?

A
  • binds to receptor- in cells cytoplasm (lipid-soluble)
  • moves to nucleus
  • increases or decreases gene transcription
44
Q

What metabolic action do glucocorticoids have?

A
  • decrease glucose uptake and utilisation
  • Increase gluconeogenesis
  • decrease protein synthesis
  • increase protein catabolism
  • redistribution of fat
  • decrease Ca²⁺ absorption from gut
  • increase Ca²⁺ excretion form kidney
45
Q

Why is the adrenal gland so essential?

A

-loss of corticosteroids leads to muscle weakness, hypotension, hypoglycaemia, and weight loss.

46
Q

What is Addison’s disease?

A

loss of functional adrenal gland through chronic inflammation or autoimmune disease.

47
Q

What is Cushing’s disease?

A

-excessive corticosteroid
due to prolonged glucocorticoid administration, excessive adrenal gland activity
-Leads to polyuria, polydipsia, breakdown of proteins, coat problems, and redistribution of fat.

48
Q

What are the injectable forms of Glucocorticoids?

A
  1. Methylprednisolone
  2. Triamcinolone
  3. Dexamethasone
49
Q

Clinical uses of glucocorticoids?

A
  • Asthma
  • Recurrent airway obstruction
  • Eczema, rhinitis, allergic conjunctivitis
  • Hypersensitivity states
  • Suppress graft reaction
  • acute spinal injury
50
Q

What are chondroprotective drugs?

A
  • used in osteoarthritis and other joint diseases to protect cartilage
  • component building blocks of cartilage and lubricants
51
Q

Examples of chondroprotective drugs

A
  • Pentosan polysulfate sodium
  • Hyaluronan
  • Polysulfated glycosaminoglycan
  • Orgotein
52
Q

What is a Hyaluronan drug?

A

= component of synovial fluid and articular cartilage- may improve joint lubrication.

53
Q

Pentosan polysulfate sodium

A

= stimulates hyaluronic acid and glycosaminoglycan in damaged joints to decrease cytokine activity

54
Q

Polysulfated glycosaminoglycan

A

incorporated into healthy and damaged cartilage, inhibits PGE2 and catabolic enzymes

55
Q

Orgotein

A

Water-soluble metalloprotein for arthritis and soft tissue inflammation

56
Q

NSAIDS

A

Inhibit COX- reduce prostaglandin and thromboxane synthesis
anti-inflammatory, anti-pyretic and analgesic
some undesirable effects

57
Q

What are the two iso forms of COX

A 
COX-1 = normal housekeeping role, inhibition may cause GI issues 
COX-2 = induced by inflammation, inhibition may cause Renal issues
58
Q

NSAIDs side effects

A
  • renal toxicity
  • hepatotoxicity
  • haematology and haemostasis
  • injury to articular cartilage
59
Q

What is a Tyrosine kinase receptor?

A

Found at the plasma membrane with an extracellular ligand-binding domain, transmembrane domain and intracellular.

60
Q

What are the effects of Tyrosine kinase Receptors?

A

leads to an inflammatory response, signalling processes, differentiation, regulate proliferation

61
Q

What are tyrosine kinase receptors activated by?

A

growth factors, Cytokines and hormones

AD1 (6 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions