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Dealing with Threats > Pharmacology 1 - Anti-inflammatory Agents Corticosteroids > Flashcards

Pharmacology 1 - Anti-inflammatory Agents Corticosteroids Flashcards

1
Q

What are the two different corticosteroids and what is their funcioin?

A

Glucocorticoids - anti-inflammatory/immunosuppressive effects
Mineralcorticoids - regulation of Na/K balance

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2
Q

Why are glucocorticoids considered to be one of the most consistently effective drugs

A

Used to treat a wide variety of inflammatory/immune conditions
such as respiratory dx, dermatologic dx, GI dx, Ophthalmic dx, musculoskeletal dx, neurologic dx, immune-mediated and autoimmune dx

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3
Q

Explain the classic arachidonic acid pathway that occurs with inflammation and then explain how glucocorticoids would act on this pathway to prevent inflammation from being too much

A

If inflammation is present, the body will produce phospholipase A2 which will break down membrane phospholipids of the cell into arachidonic acid. Enzymes will act on arachidonic acid to break it down into prostaglandin H2 and leukotrienes which will magnify inflammation. Glucocorticoids act on the pathway very early on, blocking phospholipase A which will block the pathway and prevent inflammation from occurring

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4
Q

Explain how glucocorticoids will be able to be activated

A

Glucocorticoid receptors in the body will be normally inactive with the presence of hsp90. if there is inflammation or an exogenous glucocorticoid detected in the body, the receptor will activate and that will be able to translocate into the nucleus of the cell and bind to the DNA and turn on the glucocorticoid response element to activate anti-inflammatory genes and repress pro-inflammatory genes

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5
Q

Why is it that glucocorticoids can have such a widespread effect?

A

it acts on the DNA

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6
Q

How are glucocorticoids able to diffuse across the cell?

A

Unionized and lipophilic

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7
Q

What two things do glucocorticoids once activated and bound to DNA cause?

A

transactivation of anti-inflammatory genes and transpression of pro-inflammatory genes

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8
Q

Why is it important to know the mechanism of action of a glucocorticoid?

A

-affects almost every cell
-very powerful anti-inflammatory and immunosuppressive genes
-need to balance clinical effects against the adverse effects and side effects

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9
Q

Which two main cell types do glucocorticoids act on and what are examples of each?

A

inflammatory cells - neutrophils, eosinophils, T cells, mast cells, macrophages, dendritic cells
structural cells - epithelial, endothelial, smooth muscle, mucus glands

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10
Q

What are the factors you should consider when choosing a glucocorticoid?

A

glucocorticoid activity vs mineralcorticoid activity since many have both
potency
duration of action
route of admin and formulation
species differences

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11
Q

In what instance would you want a drug with mineralcorticoid activity

A

adrenocortical insufficiency (Addison’s)

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12
Q

Why is potency important when choosing a glucocorticoid?

A

related to affinity of the drug for the glucocorticoid activity

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13
Q

If a drug had a high affinity to the receptor what effect would it have on duration?

A

longer lasting

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14
Q

If a drug had a high relative potency what would the dose be compared to that of a drug with lesser relative potency?

A

lower

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15
Q

What three variables is duration of drug activity related to?

A

receptor affinity, drug, and formulation

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16
Q

What is half life measured in vs effects?

A

half life is measured in minutes
effects measured in hours

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17
Q

Hydrocortisone is _____ acting while dexamethasone is _______acting

A

short acting
long acting

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18
Q

Hydrocortisone’s relative potency is 1, would its dose be high or low? How long would it act?

A

high
short

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19
Q

Route of administration affects what?

A

formulation choice

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20
Q

Formulation choice affects duration of activity except in what two cases?

A

oral administration
topical that becomes oral

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21
Q

What is the solubility of phosphate and succinate esters? What route is it suitable for? What is its onset of action? What instances would you use these drugs?

A

highly soluble
suitable for IV admin
rapid onset
ER situations

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22
Q

What is the solubility of acetate and acetonide esters? What route is it suitable for? What is its onset of action? What instances would you use these drugs?

A

poorly soluble
suitable for IM, SC, or IA admin
onset days to weeks

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23
Q

How would a drug base compare to in an acetonide ester?

A

base would have lower potency and lesser duration while in an in an ester would have a higher potency and longer duration

24
Q

How quickly are aqueous suspensions absorbed and which routes of used?

A

rapid absorption after IM or SC admin

25
Q

What are some solutions of drugs and what route is used?

A

polyethylene glycol or alcohol vehicles with IV or IM administration

26
Q

Why should you use caution with polyethylene glycol in cats such as Dexamethasone?

A

Cats cannot metabolize this so giving multiple doses can lead to polyethylene glycol buildup and toxicity

27
Q

Prednisone is a ______ and therefore is converted to ________

A

Prodrug
prednisolone

28
Q

Define prodrug

A

meds or compounds that after administration are metabolized in the liver to an active drug

29
Q

Which species have a low bioavailabiltiy of prednisone and therefore cannot readily metabolize it into prednisolone?

A

cats and horses

30
Q

What the the prodrug for cortisol?

A

cortisone

31
Q

In what instance would you consider giving a dog prednisolone despite its high cost?

A

if dog has liver issues

32
Q

Cats require a _____ dose compared to a dog for the _____ effect

A

higher
same

33
Q

Why is it that cats require a higher dose of glucocorticoids than dogs do?

A

fewer GRs
lower affinity to GRs

34
Q

How are cats able to get a higher dose of glucocorticoids than dogs?

A

more resistant to adverse effects

35
Q

What are the commonly used systemic GCs used in each of the species below?
Dogs
Cats
Horses
Cattle, swine

A

Dogs - prednisone, prednisolone
Cats - prednisolone
Horses - prednisolone, dexamethasone
Cattle, swine - dexamethasone

36
Q

Why is dexamethasone often used in horses, cattle, and swine?

A

Convenient, cheaper, smaller dose than pred, works really well

37
Q

What effect do glucocorticoids have on leukocytes?

A

affect number of circulating immune cells - increases neutrophils and monocytes and decreases lymphocytes, eosinophils, and basophils
affect function - decreased release of inflammatory cytokines

38
Q

What can high doses of corticosteroids lead to?

A

immunosuppressive dose

39
Q

Define immunosuppression

A

inability to mount immune response, inability to fight infection

40
Q

True or False: Immunosuppression can be related to dose and/or duration of dosing

A

TRUE

41
Q

Is immunosuppression good or bad?

A

BOTH
can lead to an inability to mount of an immune response
OR treat an overactive immune response

42
Q

Explain the metabolic effects of glucocorticoids

A

can stimulate glucose and lipid production leading to hyperglycemia and increase in triglycerides and cholesterol

can mobilize amino acids from extrahepatic tissues leading to muscle breakdown

43
Q

Explain the effect glucocorticoids have on blood vessels

A

stabilize membranes and decrease vascular permeability leading to a decrease in inflammation in CNS

44
Q

Explain the endocrine effect of glucocorticoid use

A

can lead to diabetes mellitus in cats due to gluconeogenic and antagonism of insulin

45
Q

Explain how glucocorticoid use can lead to hyper and hypoadrenocorticism

A

The body normally produces cortisol endogenously and if given exogenously for a long period of time the body will forget how to make cortisol endogenously so if it is stopped abruptly, the body will not make any cortisol leading to hypoadrenocorticism or Addison’s. If too much cortisol is being produced then the animal will have hypercorticism or Cushing’s

46
Q

How can glucocorticoids result in heptatopathy or hepatomegaly?

A

GC stimulates production of the steroid specific isoenzyme of alkaline phosphate (ALP) in dogs

47
Q

How do GC lead to GI ulceration?

A

slow turnover of enterocytes, inhibition of protective prostaglandins

48
Q

What happens if glucocorticoids alter fluid and electrolyte balance?

A

sodium and fluid retention and hypokalemic alkalosis leading to PU/PD with glucosuria and behavioral changes

49
Q

Explain the relation between laminitis and horses with the use of glucocorticoids

A

likely related to genetic predisposition or metabolism issues related to obese and cresty neck horses

50
Q

Glucocorticoid adverse effects are often said to be “not if, but when” so what is an important aspect of managing this?

A

minimize not prevent

51
Q

Explain how alternate day glucocorticoid therapy works and why

A

Higher doses every other day of intermediate acting glucocorticoids to allow the body to produce own cortisol on day off - gives HPAA chance to recover

52
Q

What are examples of intermediate acting glucocorticoids you would want to use alternate day therapy with?

A

prednisone, prednisolone, and methylprednisolone

53
Q

Why is tapering the dose important and when is it used as a way to minimize adverse effects?

A

Used when discontinuing treatment to prevent signs of hypoadrenocorticism after long-term GC therapy >2 weeks

54
Q

What should be the rule of thumb when you cant discontinue the drug completely?

A

lowest possible dose at the longest possible dosing interval

55
Q

Explain the timing of the dose (i.e. what time of the day should it be administered?

A

morning - when body normally produces it

56
Q

If not looking to systemically exposure the body to a glucocorticoid what is an alternative route of administration?

A

intra-articular
inhalant
topical such as ocular or on skin

57
Q

When are IMHA IMTP drugs used? What are the significant adverse effects associated with it?

A

used in cases that dont respond to GCs alone
myelosuppression is adverse effect

Dealing with Threats (27 decks)

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