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Pharmacology > Repro-Endo: Adrenal Gland > Flashcards

Repro-Endo: Adrenal Gland Flashcards

1
Q

Beclomethasone

A
  • Inhaled Rx
  • Beclomethasone is used to prevent and control symptoms (wheezing and shortness of breath) caused by asthma
  • Chronic Asthma in Children
  • Se: growth velocity reduction
  • Potent anti-inflammatory glucocorticoid
  • Inhibits inflammatory cells and release of Inflammatory mediators
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2
Q

Fluticasone

A
  • Used to treat a variety of Skin conditions (such as eczema, psoriasis, rash)
  • Reduces swelling (inflammation), itching, and redness
  • Cream, Ointment, Lotion
  • Oral inhalation is used to prevent difficulty breathing, chest tightness, wheezing, and coughing caused by Asthma.
  • Corticosteroids decrease inflammation by stabilizing leukocyte lysosomal membranes, preventing release of destructive acid hydrolases from leukocytes
  • Se: Burning, itching, stinging, or dryness may occur when you apply this medication, but usually only lasts a short time.
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3
Q

Budesonide

A
  • Anti-inflammatory corticosteroid
  • Potent glucocorticoid activity and weak Mineralocorticoid activity
  • Maintenance treatment for Asthma
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4
Q

Mometasone

A
  • Corticosteroid
  • Anti-inflammatory properties
  • Seasonal allergic rhinitis; Prophylaxis too
  • Elicits effects on various cells, including Mast cells and Eosinophils
  • Elicits effects on inflammatory mediators (eg, histamine, eicosanoids, leukotrienes, cytokines)
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5
Q

Prednisone

A
  • Corticosteroids
  • Prednisone is used to treat conditions such as Arthritis, Blood disorders, Breathing problems, severe Allergies, Skin diseases, Cancer, Eye problems, and Immune system disorders.
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6
Q

Prednisolone

A
  • Glucocorticosteroid
  • Decreases your Immune system’s response to various Diseases to reduce symptoms such as Pain, Swelling and Allergic-type reactions
  • Elicits mild Mineralocorticoid activity and Moderate anti-inflammatory effect
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7
Q

Methylprednisolone

A
  • Potent Glucocorticoid with minimal to no mineralocorticoid activity
  • MS, Allergies, Pneumonia in AIDS pts., Spinal cord injury
  • Controls or prevents Inflammation by controlling rate of protein synthesis, suppressing migration of polymorphonuclear leukocytes (PMNs) and fibroblasts, reversing capillary permeability, and stabilizing lysosomes at cellular level
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8
Q

Fludrocortisone

A
  • Treating adrenocortical insufficiency in Addison disease and for treating salt-losing adrenogenital syndrome.
  • Corticosteroid
  • Causing the Kidneys to retain Na and acting as a replacement for Cortisone when the body does not produce enough
  • Has both Mineralcorticoid and Glucocorticoid activity
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9
Q

Dexamethasone

A
  • Glucocorticoid
  • Dexamethasone is used to treat many different inflammatory conditions such as Allergic disorders, Skin conditions, Ulcerative colitis, Arthritis, Lupus, Psoriasis, or breathing disorders
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10
Q

Clobetasol

A
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11
Q

What causes Addison’s Disease?

A
  • Clobetasol
  • Adrenal insufficiency
  • Tx: 5 mg Prenisone in the morning to replace lack of production in Addison’s disease, after Adrenalectomy, or when other therapy inhibits Steroid biosynthesis
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12
Q

What is Apparent Mineralocorticoid Excess
(AME) disease?

A
  • Disorder of Adrenal Steroid Metabolism
  • Mutation in HSD11B2 gene (Kidney’s form of
  • *11β-hydroxysteroid dehyrodgenase)
  • -> Aldosterone** like Effect in Kidney
  • -> Decreased conversion of **Coritisol –> Cortisone
  • -> Severe HTN (Na+)andHypokalemia (K+)** through
  • *MR occupation by Cortisol**
  • Similar to Licorice Poisoning where Glycyrrhetinic acid inhibits the enzyme
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13
Q

What steroids are Prohormones?

A
  • Cortisone
  • Prednisone
  • Both require first pass metabolism by the Liver to become activated
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14
Q

Congenital Adrenal Hyperplasia?

A
  • Disorder of Adrenal Steroid Metabolism
  • Enzymatic defect (usually 21-hydroxylase)
  • -> Decreased Lvls of Cortisol and Aldosterone
  • -> Increased Angdrogens (precocious puberty)
  • -> Increased ACTH production and DHEA
  • Increased Sex Hormones (DHT and Estrogens)
  • Increased Renin
  • Hypotension
  • Hperkalemia
  • Tx: Hydrocortisone & Fludrocortisone (if Mineralcorticoids are also low)
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15
Q

Cushing’s Syndrome a/w?

A
  • Disorder of Adrenal Steroid Metabolism
  • Hypercortisolism
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16
Q

Conn’s Syndrome a/w?

A
  • Disorder of Adrenal Steroid Metabolism
  • Hyperaldosteronism
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17
Q

What is Glucocorticoid-remediable Aldosteronism?

A
  • Disorder of Adrenal Steroid Metabolism
  • Crossover placing Aldosterone synthase under the control of the Promoter for 11β-hydroxylase in the Zone Fasciculate
  • Effectively placing Aldosterone synthesis under the control of ACTH
18
Q

What is Hereditary Primary Cortisol Resistance?

A
  • Disorder of Adrenal Steroid Response
  • Due to a mutation in the Glucocorticoid receptor
19
Q

What is Steroid-resistant Asthma?

A
  • Disorder of Adrenal Steroid Response
  • Mechanism unknown
20
Q

Mifepristone

A
  • Glucocorticoid antagonist
  • Approved for the Tx of Hyperglycemia in Cushing’s syndrome pts. w Diabetes WHO ARE NOT canidates for Sx
  • Early term Abortions (anti-progestational activity)
21
Q

Spironolactone

A
  • Competitive inhibitor to Aldosterone
  • Binding to Mineralcorticoid receptor
  • Tx: HTN and Congestive Heart Failure after MI
  • Se:
    • Hyperkalemia (antimineralocorticoid)
    • Gynecomastia and Impotence (antiandrogen)
    • Mentrual disturbances (antiprogestin)
22
Q

Eplerenone

A
  • selective Mineralocorticoid receptor antagonist w/ fewer antiandrogenic and antiprogestin side effects
  • Tx: HTN and Heart failure
23
Q

Dexamethasone

A
  • Inhibitor of Adrenal Steroid biosynthesis
  • Inhibit ACTH and Endogenous Corticosteroid production
24
Q

Metyrapone

A
  • Inhibits Adrenal Steroid biosynthesis
  • Inhibits 11β-hydroxylation reaction in Biosynthetic pathway
  • Glucocorticoid and Cortisol suppression
  • The deficiency is compensated to some extend by Deoxycorticosterone, the precursor for the Hydroxylase
25
Q

Aminoglutethimide

A
  • Inhibits the first committed step in Adrenal Steroid biosynthesis
  • Inhibits Conversion of Cholesterol –> Pregnenalone
  • Inhibiting the enzyme Desmolase
  • No Salt, Sugar, Sex
26
Q

Ketoconazole

A
  • An antifungal antibiotic that inhibits side chain cleavage and 11β-hydroxylase
27
Q

ACTH

A
  • Adrenocorticotrophic hormone (ACTH, corticotropin)
  • B-LPH (Lipotropic hormone)
  • Basophil via Corticotroph cell
  • Activated by CRH from Hypothalamus
    • Negative feedback by Cortisol
  • Target organ: Adrenals
  • Increases Cortisol (adrenal cortex glucocorticoids)
  • Stress Metabolism
28
Q

CRF

A
  • Corticotropin Releasing Factor (CRF) or Corticotropin Releasing Hormone (CRH)
  • Paraventricular nucleus
  • Stress response
  • Negative Feedback by Cortisol
  • Stimulates Pituitary ACTH synthesis and secretion
  • CRH can suppress appetite, increase subjective feelings of anxiety, and perform other functions like boosting attention
29
Q

Aldosterone

A
  • Mineralcorticoid
  • Adrenal Cortex: Fasiculata cells
  • Activated by ACTH –> Positive activates Desmolase
  • -> Increases Cholesterol to Prenenolone
  • Targets the Kidney
  • Increased Na and H2O uptake in the Distal Convoluted Tubule
30
Q

Estradiol

A
  • Primary estrogen in nonpregnant women
  • Derived from ovaries or via Aromatase in the Adrenal Cortex (Reticularis)
  • Stimulates growth of the Stroma in the Endometrium
  • Causes cervical mucus to become copius and watery
  • Stimulates growth and development of the female reproductive system
  • Breast development, Prolactin secretion, maintaining Pregnancy
31
Q

Testosterone

A
  • Maintains male secondary sex characteristics
  • Enhances spermatogenesis in the Seminiferous tubules
  • Increases Libido (Sexual desire)
  • Decreased testosterone causes Male Hypogonadism, Infertility, and Decreased Libido (impotence)
32
Q

Cortisol vs. Cortisone

A
  • Cortisol and Cortisone are both steroids
  • Cortisol has an aldehyde group attached to the 17th carbon of the steroid core Carbon skeleton. Cortisone has a ketone group instead
  • Cortisol is the active form when it comes to glucocorticoid activity. Cortisone is a precursor that could be converted to cortisol upon Hydrogenation of the Ketone group at 17th position into an aldehyde group
  • Cortisol has a longer ejected half-life of 3 hours whereas cortisone only has ½ hour
33
Q

Androstenedione

A
  • Weak Adrenal androgen
  • Androstenedione is a steroid hormone used by the body to make testosterone and estrogen.
  • Androstenedione is used to increase the production of the hormone testosterone to enhance athletic performance, increase energy, keep red blood cells healthy, enhance recovery and growth from exercise, and increase sexual desire and performance.
34
Q

Dehydroepiandrosterone

(DHEA)

A
  • Weak Adrenal androgens
  • Increases production of estrogens and testosterone, decreases production of cortisol; possible effect on neurotransmitters
  • Addison’s disease, adrenal insufficiency, cognitive disorders, depression, erectile dysfunction, immunostimulant, slowing/reversing aging, systemic lupus erythematosus, vaginal atrophy (postmenopausal), menopausal hot flashes, osteoporosis, Alzheimer’s disease, weight loss
35
Q

Rx for Hypogonadism?

A
  • Adnrogen administration
  • Transdermal Testosterone preparations or Testoserone esters (Testosterone enanthate)
  • IM 2x/month or Transdermal preps of Testosterone
36
Q

Testoderm patch

A
  • Testoterone coated film is taped to skin of Scrotum
  • Scrotum must be shaved first
37
Q

Androderm patch

A
  • Skin permeation enhancers (Glycerol monooleate and Glycerin) are added to the Testosterone
  • Patches can be placed anywhere on the skin
  • Some skin irritation results from permeation enhancers
38
Q

AndroGel

A
  • Gel containing Testosterone and Permeation enhancers (excipients) are rubbed onto shoulders
39
Q

Testosterone Buccal System

A
  • Adheres to the gum and Provides sustained slow release of Testosterone through the Buccal mucosa
  • Venous drainage is to the SVC
40
Q

Topical Testosterone Solution

A
  • Solution applied to the axilla (armpit)
  • Slow release Testosterone
41
Q

Danazol and Stanozol

A
  • Tx: Hereditary Angioedema
  • Impaired C1-esterase inhibitor
  • Overactive complement cascade increases Blood vessel permeability
  • Chronic Tx: Orally Active Androgens
  • Stimulate Hepatic synthesis of the Esterase Inhibitor
  • Only Active androgens containing 17α-aliphatic groups are effective
42
Q

Performance enhancement w/ Testosterone?

A
  • Oral anabolics are modified at the 17α- position are weak and cannot induce spermatogenesis, but can cause liver damage
  • Injectible androgens are modified at the 17β- position to prolong their absorption
    • Testosterone propionate
    • Testosterone enanthate

Pharmacology (29 decks)

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