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SYSTEMIC PHARMACOLOGY > LESSON 2: GLUCOCORTICOIDS & IMMUNOSUPPRESSANTS AGENTS > Flashcards

LESSON 2: GLUCOCORTICOIDS & IMMUNOSUPPRESSANTS AGENTS Flashcards

1
Q

are steroidal agent produced and released by the adrenal cortex

A

glucocorticoids

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2
Q

2 glucocorticoids predominantly affect carbohydrate metabolism; this 2 are also important naturally occuring glucocoticoids

A
  1. Cortisol
  2. corticosterone
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3
Q

Aldosterone, predominantly affect electrolyte and water metabolism

A

Mineralocorticoids

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4
Q

Predominates in human beings, pigs, and dogs

A

cortisol

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5
Q

Predominates in rabbit, mouse, and rat

A

corticosterones

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6
Q

to the non-esterified steroid component and determines its glucocorticoid, an anti-inflammatory potency, and extents its duration of action

A

glucocorticoid base

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7
Q

The ability of glucocorticoid formulation to suppress the hypothalamus-pituitary-adrenal axis (HPAA) is determined by:

A

● The dose
● Potency of the base, and
● Duration of the action of the formulation.

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7
Q

one of the major adverse effects of the glucocorticoids therapy

A

secondary hypoadrenocorticism

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8
Q

Therapeutic success with fewer side effects is possible with?

A

alternate-day therapy

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9
Q

hypothalamus secretes _________, which is brought to the anterior pituitary through the
hypothalamus-pituitary portal system

A

corticotropin –releasing hormone (CRH)

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10
Q

The ____ which are generally active during daytime (diurnal), have high blood
glucocorticoid concentration during the day, and low at night

A

DOG

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11
Q

_____ which are active at night (nocturnal), show the reverse pattern

A

cat

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12
Q

action, which may lead to increase glucose production from amino acid by way of gluconeogenesis, and to reduce the rate of incorporation of amino acid into proteins

A

hyperglycemic action

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13
Q

Glucocorticoids in large amounts (hyperadrenocorticism or Cushing’s disease)
inevitably lead to :

A
  1. polyuria- excretion of excessive volume of urine
  2. polydipsia- excessive thirst
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14
Q

Overdose of glucocorticoids may be leads to:

A
  1. hypernatremia- retention of high sodium concen. in blood
  2. hypokalemia- low cacium concen. in blood
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15
Q

Glucocorticoids in use of physiological replacement therapy:

A

This is used in the treatment of:
1. hypoadrenocorticism (Addison’s disease)
2. In iatrogenic HPA axis suppression, and
3. Adrenalectromized patients.

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16
Q

example of drugs with slow onset and intermediate duration are used for acute disease processes used for once-a-day therapy

A

● Triamcinolone acetonde
● Dexamethasone in propylene glycol

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17
Q

drugs with short duration are used for
acute and chronic condition and for
alternate –day therapy.

A

Prednisolone
Prednisone
Methylprednisolone

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18
Q

mimics diurnal cortisol production in most
animals; causes sodium retention
(not significant in dogs and cats)

A

Prednisolone

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19
Q

Those with slow onset and long
duration are for skin and joints.

A

● Triamcinolone acetonide
● Methylprednisolone acetate

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20
Q

Those with very rapid onset and short
duration are used in emergency
situation such as hemorrhagic-shock
and anaphylaxis. These are fast-acting
(within1 min) with short plasma
half-life (1-2 h), but are rather
expensive

A

● Hydrocortisone sodium succinate
● Hydrocortisone sodium
phosphate
● Prednisolone sodium succinate

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21
Q

glucocorticoids used in anti-inflammatory and anti – allergic therapy;

A

This is commonly employed in:
a. Symptomatic therapy of pruritic dermatoses
b. Allergic pulmonary disease, and
c. Allergic gastroenteritis

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22
Q

Immunosuppressive therapy (“immunosuppressive Agents “)
This use is designed for:

A

a. Immune mediated thrombocytopenia
b. Autoimmune hemolytic anemia
c. Systemic lupus erythematosus, and some forms of neoplasm

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23
Q

Prednisolone (for induction )

A

2.2-6.6 mg/kg divided bid until effects

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24
Q

Dexamethasone (for maintenance)

A

2-2.2 mg/kg every 2 days

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25
Q

Prednisolone (for maintenance)

A

0.33-1.1 mg/kg

26
Q

This is employed in the condition such as chronic arthritis, hip dysplasia, etc. dosing
may be intermittent or on alternate-day basis. Do not withdraw erratically, this may
lead to pseudorheumatism

A

Chronic palliative therapy

27
Q

Proper weaning from long-term glucocorticoids therapy should be tedious and drawn
out. Animals do not complain of minor aches and pains or of changes in mood.
However, the following signs might suggest that further prolongation of the weaning
process is necessary;

A

⮚ Dullness
⮚ Mental depression
⮚ Increase fatigability
⮚ Incoordination
⮚ Unthriftiness and weight loss
⮚ Diarrhea
⮚ Behavioural changes

28
Q

This compound has been found to suppress adrenal cortical activity in the dog, but
it is less successful in other species. Rats and monkeys are unaffected. in goats caused atrophy of the cortex and transitory cytopathologic effects of adrenal cortical cells of calves

A

o,p’DDD

29
Q

Is (3, 3- bis p-aminophenyl butane). It inhibits 17 - ketosteroid production in
human and dog

A

Amphenome B

30
Q

is very lipophilic and hydrophobic and must be solubilized before administration. It specifically inhibits T cells early in their immune response to antigenic and regulatory stimuli without affecting suppressor T cells

A

Cylosporin A

31
Q

Cylosporin binds with its cytoplasmic receptor protein

A

cyclophilin

32
Q

The resulting cylosporin – cylosphilin complex then binds with

A

calcineurin (a phosphatase)

33
Q

Unwanted effects of cylosporin is include:

A

⮚ Nephrotoxicity
⮚ Hepatotoxicity, and
⮚ Hypertension

34
Q

Less severe side effects are:

A

⮚ Anorexia
⮚ Hirsutism (in human) tremor
⮚ Paraesthesia, gum hypertrophy, and
⮚ Gastrointestinal disturbance.

35
Q

It is macrolide antibiotic with a very similar mechanism of action to cylosporin. The
main difference is that its cytoplasmic receptor is not cyclophilin but protein called
FK binding protein (FKBP)

A

Tacrolimus (a.k.a FK506)

36
Q

another macrolides, also binds with FKBP. However, the rampamycin-FKBP complex does not bind with calcinuerin nor does it effects IL-2
transcription. It interferes with signal transduction pathway blocking the cell cycle of
activated T cells in G1 phase by inhibiting a novel kinase called mTOR

A

Rapamycin

37
Q

It is an alkylating agent with particular action on lymphocytes. As a immunosuppressant it effects the clonal proliferative phase of the immune response and reduce both antibody-mediated and cell-mediated immune reactions.

A

Cyclophosphamide

37
Q

It is another alkylating cytotoxic agent similar to cyclophosphamide

A

Chlorambucil

38
Q

It is used particularly for tissue rejection in transplant surgery. It is metabolized to
mercaptopurine, a purine analogue that inhibits DNA synthesis. Both cell-mediated & antibody-mediated immune reactions, and are depressed by this drug since it inhibits clonal proliferation in the induction phase of the immune response by a cytotoxic reaction on dividing cells.

A

Azathioprine

39
Q

A semi-synthetic derivative of a fungal antibiotic, it is converted to mycophenolic acid, which restrains the proliferation of both B and tT lymphocytes and reduces the production of cytotoxic. T cells by inhibiting inosine monophosphate dehydrogenase. This pathway is essential for de novo purine synthesis B and T lymphocytes are particularly dependent on this enzyme

A

Mycophenolate mofetil

40
Q

in ring A, the double bond at _____ and keto group at ______ are essential for activity. Reduction of the double bond and the keto group result in loss of activity

A

c4 & c3

41
Q

enhances the glucocorticoid activity and
decreases mineralocorticoid activity

A

double bond c1

42
Q

this 2 are present in ring b

A
  1. a-fluorination at c9
  2. a- methylation at c6
43
Q

this increases glucocorticoids & mineralacortiocids activity

A

a-fluorination at c9

44
Q

this enhances glucocorticoids effects

A

a-methylation at c6

45
Q

a glucocorticoid commonly use in clinical therapy, differs from cortisol only in having a keto- rather than B-hydroxyll group at c11

A

Cortisone

46
Q

Cortisone is inactive, but can be transformed to _______ in the liver.

A

cortisol

47
Q

It is not useful when administered topically or injected in ???

A

joint

48
Q

in ring d The OH group at C21 must be free for ??

A

biologcal activity

49
Q

______ markedly decreases mineralocorticoid effect

A

α - or β – methylation at C16

50
Q

________ also markedly decrease mineralocorticoids effect

A

α – hydroxylation at C16

51
Q

LONG ACTING DRUGS “

A

Paramethasone
Betamethasone
Dexamethasone

52
Q

this 2 glucocorticoid ester is rapid onset of action; for IV and IM route

A
  1. Phosphates
  2. Hemmisuccinate
53
Q

a glucocorticoid ester is poorly water soluble; used as depot

A

Acetonide

54
Q

this glucocorticoid ester is very long duration of action (weeks to mo

A

Pivalate

55
Q

this glucocorticod ester is slow absorption; available as depot; action last days duration

A

Acetate, diacetate, tebutate

56
Q

secretion of _______ by the anterior pituitary is episodic rather than
continuous.

A

corticotropin

57
Q

In the normal animal, the blood glucocorticoid concentration varies with
the ??

A

circadian rhythm

58
Q

Pharmacological Effects of Glucocorticoids

A

The pharmacological effects of glucocorticoids are produced by rather than high doses. When a clinician administers a glucocorticoid to a patient, effect other than
those originally desired may also occur

59
Q

glucocorticoids cause ________ and _______ an effect secondary to cell redistribution and/or lysis, and lead to increase de-margination of neutrophils

A

lymphocytopenia & eosinopenia

60
Q

DNA-binding domain. The steroid-receptor
complexes move into the nucleus and bind to steroid-response elements in the DNA. The effects is either to ??

A
  1. repress- prevent transcription
    or
  2. induce- initiate expression
61
Q

Effectively blocks cortisol production but not corticosterone production in young pig

A

Metyrapone

SYSTEMIC PHARMACOLOGY (7 decks)

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