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Pharmacology & Medical Chemistry II > Exam 2: Lecture X, Corticosteroids > Flashcards

Exam 2: Lecture X, Corticosteroids Flashcards

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1
Q

Corticosteroids are….

A

steroid hormones produced by adrenal cortex (homeostatic organ responding to stress)

3 major groups:
Glucocorticoids
Mineralocorticoids
Sex Steroid

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2
Q

Adrenal Gland production by layer….

A

Cortex: steroid hormones

Medulla = Epi/NE

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3
Q

Glucocorticoids role in…

A

metabolic, immunity and inflammation

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4
Q

Mineralcorticoids role in…

A

electrolyte-regulating

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5
Q

Regulation fo Cortisol Secretion

A
  1. Regulated by hypothalamus-pituitary-adrenal cortex axis
  2. Corticotropin-releasing hormone
    (CRH)»ACTH»»cortisol
    • CRH produced in hypothalamus H1
    • ACTH produced in anterior pituitary H2
    • Cortisol is secreted from adrenal cortex H3
  3. Cortisol secretion is regulated by negative feedback system

The most potent stimulus of cortisol secretion is stress

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6
Q

Corticosteroids Pharmacokinetics

A

almost 90% bound to protein

Absorption is rapid

Metabolized in liver

excreted by kidney

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7
Q

Spironolactone (Aldactone, CarboSpir)

A

Diuretic! (Mineralocorticoid Antagonist)

Aldosterone antagonist at its receptor

Reverses many manifestations of aldosteronism

Also useful in preparing patients for surgery

May reduce the incidence of cardiac arrhythmia

Also used to treat heart failure

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8
Q

Fludrocortisone (Florinef Acetate)

A

Partial replacement for adrenocortical insufficiency and for hypotension treatment

Has significant glucocorticoid activity
Effective safe medication

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9
Q

Major Mineralcorticoids in humans?

A

Aldosterone

v important in regulation of blood volume and blood pressure

little glucocorticoid activity, MOA same as glucocorticoid tho

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10
Q

Secretion of aldosterone regulated by….

A

ACTH and RAA system

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11
Q

Glucocorticoid antagonist/Steroid Synthesis inhibitors

A

Ketoconazole (Nizoral)
Mifepristone (RU 486)(Mifeoprex)
Mitotane (Lysodren)

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12
Q

Mitotane (Lysodren)

A

Related to DDT insecticide

A non-selective cytotoxic action upon adrenal cortex

Reduces tumor mass in 1/3 of patients

Serious toxicity- available on compassionate basis

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13
Q

Mifepristone (RU 486)(Mifeoprex)

A

Abortifacient drug

Inhibits glucocorticoid and progesterone receptors

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14
Q

Ketoconazole (Nizoral)

A

Antifungal drug

Inhibits P450 system enzymes required for steroid hormone synthesis

Reduces steroid levels

Used for Cushing’s syndrome hirsutism and breast cancer.

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15
Q

List of Aerosolized Corticosteroids

A 
Dexamethasone
Triamcinolone
Beclomethasone
Flunisolide
Budenoside
Fluticasone
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16
Q

Aerosolized corticosteroids info

A

In asthma and similar respiratory conditions, corticosteroids have a significant affect upon large mucous membrane of the trachea-bronchial tree.

However, systemic effects have to be avoided.

Special glucocorticoids were developed for use in asthma.

Formulations readily penetrate the airway mucosa, however, systemic effects and toxicity are significantly reduced.

17
Q

Dexamethasone (Decadron)

A

Very potent and no salt-retaining actions

Very good in cerebral edema (no water retention)

18
Q

Triamcinolone (Kenalog)

A

Severe asthma

Local injections into the inflamed joints

19
Q

Prednisolone (Delta-cortef)

A

widely given orally for inflammation and allergies

20
Q

Cortisone (Cortone Acetate)

A

Orally – as a replacement therapy

Intravenously in shock and status asthmatics
Topically in eczema, enema in ulcerative colitis

21
Q

Natural Glucocorticoid

A

Cortisol (Hydrocortisone)

22
Q

Synthetic Glucocorticoids

A

Prednisolone
Betamethasone
Triamcinolone

23
Q

Glucocorticoids-Immunisuppressive effects…

A

decreased antibody production

24
Q

Glucocorticoids anti-inflammatory effect

A

ARACHIDONIC ACID METABOLITES INHIBITION

INFLAMMATORY RESPONSE IS DECREASED

NEUTROPHIL FUNCTION IS DEPRESSED

MACROPHAGE FUNCTION IS DEPRESSED

25
Q

Corticosterone

A
  • Lipophilic
    • Bind to intracellular cytosolic receptors
    • Transported into the nucleus
    • Affect the nucleus of the cell
    • Bind with glucocorticoid response element (GRE)
    • Induce gene expression within the cells
    • Induce gene expression for lipocortin/inhibits PLA2
    • Induce gene expression for antiinflammatory proteins
    • Suppress gene expression for proinflammatory proteins
    • Inhibit cytokines production
26
Q

Glucocorticoids Physiological Effects 1

A

Increase number/affinity of β-receptors

Facilitate conversion of protein to glycogen

Stimulate hepatic gluconeogenesis and liver storage of glucose as glycogen

Peripheral glucose uptake is inhibited

Net effect - rise of blood sugar (can cause hyperglycemia and diabetes mellitus)

27
Q

Glucocorticoids Physiological Effects 2

A

Catabolism of muscle proteins to aminoacids

Connective tissue, fat, and skin wasting

Catabolic effect upon bone can lead to osteoporosis

In children growth is inhibited

Stimulation of insulin secretion

Increased lipolysis

CNS effects – at times including euphoria

28
Q

Corticosteroids Clinical Use

A

Preserve life in patients with cortical insufficiency (Addison’s disease)

Acute adrenal deficiency associated with shock, infection, or trauma.

Asthma

Severe inflammatory conditions (eye, skin)

Organ transplant rejection

Collagen disease

Leukemia (to suppress lymphopoiesis)

Neurological disorders

Vomiting induced by chemotherapy

Hypercalcemia

29
Q

Corticosteroids Adverse effects

A

Corticosteroids are characterized by severe toxicity!

Toxicity limits the use of these agents!

Because of systemic toxicity, oral/intravenous agents are used as a last resort!!!

30
Q

Glucocorticoids Adverse effects

A

MOON FACE

FAT REDISTRIBUTION

HYPERGLYCEMIA

OSTEOPOROSIS

FLUID RETENTION - HYPERTENSION

ADRENAL SUPPRESSION – INSUFFICIENCY OF HORMONE PRODUCTION

NECROSIS OF BONES

PEPTIC ULCERATION

DEPRESSION

RECURRENCE OF ALLERGIC INFLAMMATION

OROPHYARYNGEAL FUNGAL INFECTIONS
CHANGES IN VOICE

BRONCHOCONSTRICTION

CATARACTS/GLAUCOMA

TUBERCULOSIS

31
Q

Methods to minimize glucocorticoid toxicity

A

Local applications
Aerosols (asthma)
Alternate day therapy
Tapering the dose after achieving a good response
Synthetic glucocorticoids are used to reduce toxicity
- higher affinity for receptors
- little or no salt retaining properties

32
Q

Chronic Adrenal Excess….

A 
Cushing’s disease – polycythemia, lymphocytopenia,
Decreased lymphoid mass
Neurosis, psychoses
Hypertension
Moon face with red cheeks
Cataracts
Buffalo hump + increased abdominal fat
Thin legs/arms -muscle wasting
Easy bruising/poor wound healing
33
Q

Chronic Adrenal Insufficiency….

A

Addison’s disease –anemia, lymphocytosis, increased lymphoid mass
Apathy, depression, irritability, psychoses
Hypotension
Muscle weakness, fatigue, weight loss
Hyperpigmentation
Hypoglycemia (during fasting)
Sodium loss, hypotension
Minor stress/trauma can trigger acute insufficiency – shock/death

34
Q

Strongest to Weakest Corticosteroids

A

Dexamethasone (36h)
Triamcinolone (24h)
Prednisolone (24h)
Cortisone (12h)

Pharmacology & Medical Chemistry II (43 decks)

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