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SP1 Pharmacology > Lecture 23 4/23/24 > Flashcards

Lecture 23 4/23/24 Flashcards

1
Q

Which molecule serves as the basis for all hormones of the adrenal cortex?

A

cholesterol

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2
Q

What are the main products of the adrenal cortex?

A

C21 and C19 steroids

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3
Q

What are the C21 steroids with a two-carbon side chain at position 17 categorized as?

A

-mineralocorticoids
-glucocorticoids

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4
Q

What are the results of chemical modification of the cortisol molecule?

A

-increased glucocorticoid activity
-decreased mineralocorticoid activity
-altered protein binding
-hepatic metabolism

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5
Q

What is anti-inflammatory activity associated with?

A

glucocorticoid activity

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6
Q

How does prednisone/prednisolone differ from cortisol?

A

-introduction of a double bond between C1 and C2
-increased anti-inflammatory activity
-reduced mineralocorticoid activity

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7
Q

What are the characteristics of prednisone?

A

-originally an inactive compound
-must be converted into active form in the liver

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8
Q

What change converts prednisolone into methylprednisolone?

A

addition of a methyl group at the C6alpha position

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9
Q

What change converts prednisolone into triamcinolone?

A

insertion of a 16alpha hydroxyl group

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10
Q

How do methylprednisolone and triamcinolone differ from prednisolone in terms of activity?

A

-higher anti-inflammatory effect
-decreased mineralocorticoid activity

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11
Q

What are the characteristics of dexamethasone and betamethasone?

A

most potent anti-inflammatory glucocorticoids
-added C9a fluorine atom increases glucocorticoid activity
-added C16 methyl group decreases mineralocorticoid activity

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12
Q

What is D ring manipulation?

A

changes made to the D ring to produce “soft” glucocorticoids that have increased topical and/or inhalational absorption

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13
Q

What are the steps of glucocorticoid binding to its receptor?

A

-GCs passively diffuse into cells
-bind to cytoplasmic glucocorticoids receptor
-GC-GR complex translocates into nucleus for gene regulation

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14
Q

What are the direct actions of activated glucocorticoid receptors?

A

-inhibit pro-inflammatory transcription factors
-actively suppress transcription of inflammatory genes
-induce transcription of immunosuppressive genes

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15
Q

Why are glucocorticoids-induced biological responses slow?

A

time is required before RNA and protein levels of target gene are fully degraded

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16
Q

Which effects of glucocorticoids are induced rapidly?

A

-effects on transmembrane currents
-effects on signal transduction
-effects on second messenger cascades and intracellular Ca2+ mobilization

17
Q

What are the characteristics of glucocorticoid suppression of inflammatory and immune-mediated responses?

A

-rapid action mediated by nongenomic mechanisms
-affects only seen when supraphysiological doses are given

18
Q

Why is glucocorticoid therapy dangerous?

A

can mask severity and progression of disease and any serious side effects that may occur

19
Q

Which cells are primarily effected by glucocorticoids?

A

leukocytes

20
Q

What is plasma half life?

A

the amount of time required for 50% of the drug’s concentration to disappear from plasma

21
Q

What is biological half life?

A

-refers to duration of effects
-varies because biological effect is due to alterations in genetic regulation of protein production
-must be considered when establishing treatment protocol

22
Q

What influences duration of action for a drug?

A

-route of administration
-preparation used
-patient health
-concurrent use of other drugs

23
Q

What are the three classifications for biological half life?

A

-short-acting
-intermediate-acting
-long-acting
–all are based on duration of HPA axis suppression

24
Q

What are the advantages of oral administration?

A

-GCs are orally effective
-preferred route for systemic application
-safest route
-most convenient
-most economical

25
Q

What are the disadvantages of oral administration?

A

-vomiting
-variable absorption
-cooperation of the pet

26
Q

How does oral bioavailability differ for glucocorticoids?

A

-high: cortisol, prednisolone, methylprednisolone
-low: dexamethasone
-very low: triamcinolone, budesonide

27
Q

Why must the prednisone dose be 3-5 times higher than the prednisolone dose?

A

prednisone is the inactive form that needs to be activated; must account for losses of the inactive drug

28
Q

What are the characteristics of parenteral glucocorticoid administration?

A

-more predictable absorption than oral
-more expensive than oral
-glucocorticoids are synthesized as glucocorticoid esters
-IV admin. allows for rapid high concentrations
-IM admin. allows for prolonged effects

29
Q

What are the possible forms of topical/inhalable GCs?

A

-ointments
-creams
-gels
-solutions
-shampoos/rinses
-eye drops
-crystal suspensions
-aerosols

30
Q

What is the advantage of topical GCs?

A

provides high conc. of GC in a specific site; should reduce systemic effects

31
Q

What are the disadvantages of topical GCs?

A

-all forms can still have adverse systemic effects
-absorption is variable

32
Q

How is dose equivalency expressed for GCs?

A

-cortisol is assigned a value of 1 for both glucocorticoid and mineralocorticoid potency
-numbers higher than 1 indicate increased potency
-numbers lower than 1 indicate decreased potency

33
Q

How do the doses for prednisolone and dexamethasone differ?

A

-prednisolone dose is 1 mg/kg
-dexamethasone dose is 0.14 mg/kg

34
Q

What are the characteristics of steroid esters?

A

-GCs typically have low water solubility
-esterification can alter the lipid/water solubility ratio and duration of action
-ester also determines route of administration for drug

35
Q

What are the characteristics of water-soluble esters?

A

-esters include succinate and phosphate
-given IV, IM, or SC
-ideal for emergency
-duration of action equal to unmodified GC

36
Q

What are the characteristics of free alcohol solutions?

A

-unique to vet med
-dexa polyethylene glycol has increased water solubility
-injectable solution
-IM and IV admin.
-possible CNS side effects

37
Q

What are the characteristics of insoluble steroid esters?

A

-esters from acetate to pivalate
-IM, IA, and intralesional admin
-NO IV admin.
-depot preparation/slow release

38
Q

What is the advantage of insoluble steroid esters?

A

convenience of admin.

39
Q

What are the disadvantages of insoluble steroid esters?

A

-unpredictability of blood conc.
-long-term suppression of HPA axis
-possible induction of GC resistance
-cannot withdraw drug in case of adverse reactions

SP1 Pharmacology (27 decks)

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