Corticosteroids Flashcards
Hydrocortisone indications
Replacement therapy for adrenal insufficiency
Hydrocortisone
- aka cortisol
- Exhibits both mineralcorticoid and glucocorticoid properties
Cortisone (Cortone) indications
Replacement therapy for adrenal insufficiency
Cortisone (cortone)
- Significant mineralcorticoid as well as glucocorticoid properties
- Cortisone must first be converted to hydrocortisone in the liver in order to be active**
Prednisone (Meticorten) and prednisolone (delta-cortef)
- More glucocorticoid effects than mineralcorticoid]
- Prednisone must first be converted to predinsolone in the liver in order to be active**
- Prednisone is the most commonly prescribed oral glucocorticoid
Triamcinolone (Kenalog), methylprednisolone (Medrol)
- Virtually no mineralcorticoid activity
- High glucocorticoid activity
- most newer glucocorticoid drugs are like these drugs**
- Differences in duration and potency
Preparations-oral
Long term therapy
Preparations-injections
Emergencies or depot administration
Preparation-inhalation or intranasal
asthma and rhinitis
Preparations-Topical
- Fairly insoluble to prevent absorption
- More potent topicals–>thick skin only
- Skin damage or thin skin: Increases systemic absorption
- Repeated application–>depot effect
Adrenocorticosteroids-therapeutic uses
- Replacement in chronic adrenal insufficency (Addisons, etc.)
- Treated w/glucocorticoid alone or glucocorticoid + mineralcorticoid**
- Use increased amounts w/stress or infection
- Acute insufficency can be life threatening**
Adrenocorticosteroids-rheumatoid arthritis
- Reduce inflammation
- Reduce pain
- Restore function
- Not curative!!
Adrenocorticosteroids-other conditions
- Intranasal for rhinitis**
- SLE, allergic rxns, shock, organ transplants, etc.
Adrenocorticosteroids-Asthma
- Inhaled-first step in asthma treatment (DOC)
- In conjunction with beta 2 agonist (increased sensitivity)
- Oral-used in patients who are not controlled by inhaled steroids
Adrenocorticosteroids important pts.
- Chronic treatment may leave the HPA subnormal for months
- Short term therapy (1-2 wks) is not likely to cause serious problems**
Adrenocorticosteroids therapeutic guidelines
- Only as long as necessary
- Lowest effective dose** (start with a higher dose and lower the dose once the inflammation reduces)
- Use LOCALLY whenever possible
- Give on alternate days** (decreases suppression of the HPA axis)
Corticosteroid therapy
- Few significant side effects with acute therapy
- Palliative effect not curative
- many adverse effects with long term, high doses
Adrenocorticosteroids adverse effects
- infection, hyperglycemia, CNS, osteoporosis, Misc. effects
- Iatrogenic Adrenal Insufficiency
- > 1-2 weeks of high dose therapy–>HPA depression
- Abrupt drug cessation–>acute adrenal insufficiency
- Stress can cause adrenal crisis in chronic patients
Infections
– May mask symptoms
– More susceptible to serious infections
Hyperglycemia adverse effect
May unmask diabetes in some pts.
CNS adverse effect
– Restlessness, insomnia, psychoses, ↑appetite
– Even with acute treatments**
Therapies to reduce HPA axis depression
Alternate days or monitoring dosing
Osteoporosis-adverse effect
-Most damaging and therapeutically limiting effect**
-30-50% of chronic patients –>fracture
-Vertebral and rib fractures most common
(treatment includes Vit D, calcium, bisphosphonates)
Contraindications in corticosteroids
- NONE IN ADRENAL INSUFFICIENCY
- Systemic bacterial or viral infection
- Poorly controlled diabetes
- Osteoporosis
- Heart disease or hypertension with congestive heart failure
- Immunosuppressed patients
- Childhood, pregnancy
Miscellaneous (cushingoid) side effects
– Acne, striae
– Truncal obesity
– Buffalo hump**
– Moon face**
(Dysmenorrhea, Skin atrophy and thinning)
Things to monitor in corticosteroid patients (8)
- Hyperglycemia & glycosuria
- Na+ retention w/ edema or hypertension
- Hypokalemia
- Peptic ulcer
- Osteoporosis
- Infections
- Growth and development in children
- Pregnancy – glucocorticoids are teratogenic
Ketoconazole (Nizoral®)
Antifungal that inhibits steroid synthesis (very high doses)
• Non-selective
• Preoperative suppression
Aminoglutethimide (Cytadren)
– Blocks adrenal and gonadal steroid synthesis**
– Corticosteroids must be given concomitantly to suppress ACTH
– Not on market anymore
Mifepristone (RU 486®)
- Antagonist of glucocorticoid and progesterone receptors**
* For inoperable Cushings patients
Spironolactone (Aldactone®)
- Mineralocorticoid (and some androgen) receptor antagonist
- Potassium-sparing diuretic
- For hyperaldosteronism and hirsutism**
