Term
| glucocorticoid antagonist: |
|
Definition
|
|
Term
| Mineralocoricoid antagonist: |
|
Definition
|
|
Term
| Corticosteroid synthesis inhibitor: |
|
Definition
|
|
Term
| Short acting corticosteroids: |
|
Definition
|
|
Term
| Intermediate acting corticosteroids: |
|
Definition
- Prednisone
- Prednisolone
- Methyprednisolone
- Triamcinolone |
|
|
Term
| Long acting corticosteroids: |
|
Definition
- Betamethasone
- Dexamethasone |
|
|
Term
|
Definition
- corticoststerone
- fludrocortisone |
|
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Term
| when grading corticosteroid potentcy, __ is standard to which all others are measured against. |
|
Definition
|
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Term
| Corticosteroids used to treat: |
|
Definition
- Rheumatoid arthritis
- Bronchial asthma
- Renal diseases
- SLE
- Ocular disorders
- Organ transplants
WITH ALL THESE CONDITIONS THESE WORK VIA ANTIINFLAMMATORY, BUT ORGAN TRANSPLANT ON IMMUNE SYSTEM.
CORTICOSTEROIDS CONTROL SYMPTOMS, THEY DO NOT STOP PROGRESSION OF THE DISEASE. |
|
|
Term
| In humans, Cortisol is the naturally occuring corticosteroid secreted by the adrenal cortex. Prednisolone, MPL and Dex are synthetic analogs. |
|
Definition
|
|
Term
| hypothalamus> CRH> pituitary> ACTH> adrenal cortex> cortisol> negative feedback and inhibits release of CRH |
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Definition
| stress can override the negative feedback system and release more cortisol, also influenced by hypoglycemia and pain |
|
|
Term
Glucocorticoids
Cortisol (95%)
Corticostrone
Cortisone
90% bound to plasma proteins
Circadian release
Of GCs; highest in
the early morning
and lowest in the
evening. |
|
Definition
|
|
Term
| Glucocorticosteroid organ and tissue effects: |
|
Definition
- metabolic effects: stimulates gluconeogenesis
- catabolic effects: protein catabolism, lymph, connective tissue, fat, and skin wasting
- Immunosuppressive effects: inhibit cell mediated actions, espically lymphocytes
- anti-inflammatory effects |
|
|
Term
Mechanism of action for anti-inflammatory corticosteroids (5):
KNOW THIS TEST |
|
Definition
1. suppress T cell activation and cytokine production
2. Suppress mast cell degranulation
3. Decrease capillary permeability indirectly by inhibiting mast cells and basophils
4. Reduce expression of cyclooxygenase II and prostaglandin synthesis
5. Reduce prostaglandin, leukotriene and platelet activating factor levels by altering phospholipase A2 activity |
|
|
Term
Coricosteroids are RAPIDLY AND COMPLETELY ABSORBED B/C FAT SOLUBLE. THEY DO CROSS THE BLOOD BRAIN BARRIER.
A lot of PROTEIN TRANSPORT, COUPLE DIFFERENT PROTEINS. 10-20% IS UNBOUND. MOST OF IT IS BOUND. |
|
Definition
|
|
Term
| Daily administration of corticosteroids at physiological concentrations for at least 2 weeks suppresses the __ resulting in decreased production of endogenous hormones. Recovery may take 9-12 months. |
|
Definition
|
|
Term
| Corticosteroids are mostly metabolized and inactivated in the __ by ____ enzymes. 25% of GCs are excreted in the __ and __, while 75% of corticosteriods are excreted in the __. |
|
Definition
- liver by CYP450 3A4
- bile and feces
- urine |
|
|
Term
| prototype corticosteroid for anti-inflammatory actions: |
|
Definition
|
|
Term
| hydrocortisone is a __ acting coricosteroid. |
|
Definition
short
plasma half life 30 min
biological half life 8-12 hrs. b/c gets absorbed in fat |
|
|
Term
| Hydrocortisone used for treatment of: |
|
Definition
- localized inflammatory conditions
- dermatitis
- Ulcerative colitis |
|
|
Term
| Contraindications to hydrocortisone: |
|
Definition
- systemic fungal infection
- recent ileocolostomy
- intestinal anatomoses
- intestinal abscess |
|
|
Term
| prednisone is ___ acting glucocorticoid. |
|
Definition
|
|
Term
| Prednisone clinical uses: |
|
Definition
- adjunct therapy for arthritis (short term admin)
- asthma
- COPD
- Ulcerative colitis
- Crohn's Disease
- Rheumatic disorders
- dermatological disorders |
|
|
Term
| Prednisone can only be given ___. |
|
Definition
|
|
Term
| hydrocortisone relative antiinflammatory potency is __. |
|
Definition
|
|
Term
| Prednisone relative antiinflammatory potency is __. |
|
Definition
| 4 (it is 4 times more potent than cortisol) |
|
|
Term
| Prednisone is inactive on its own, it must be metaabolized in the __ to an active metabolite. |
|
Definition
liver
plasma half life 60 min
biological half life 18-36 hours |
|
|
Term
| Inhaled Gluococorticoids: |
|
Definition
- Beclomethasone
- Budesonide
- Flunisolide
- Fluticasone propionate
- Triamcinolone acetonide |
|
|
Term
| Oral glucocorticoids (quick relief of asthmatic symptoms): |
|
Definition
- Prednisone
- Prednisolone
for those unresponsive to beta 2 agonists |
|
|
Term
| Prednisolone is ___ acting and can be in what 2 forms: |
|
Definition
- intermediate
plasma half life 60 minutes
biological half life 18-36 hours
Prednisolone acetate/sodium phosphate |
|
|
Term
| Clinical uses of prednisolone: |
|
Definition
- opthalmic disorders
- respiratory diseases |
|
|
Term
| Prednisolone can be given __ or __. |
|
Definition
| orally or injected (so can be systemic or local) |
|
|
Term
| Methyprednisone is ___ acting and can be in what two forms? |
|
Definition
- intermediate
plasma half life 60 minutes
biologial half life 18-36 hours
Methylprednisolone acetate/sodium succinate |
|
|
Term
| Methylprednisolone clinical uses: |
|
Definition
- Rheumatoid arthritis
- INTRA-ARTICULAR INJECTIONS
- Ulcerative colitis
- severe alcoholic hepatitis |
|
|
Term
| Methylprednisolone admin: |
|
Definition
| oral or injectable (so systemic or local) |
|
|
Term
| Methylprednisolone adverse effects: |
|
Definition
- vertigo
- headache
- weight gain
- sodium/water retention
- impaired wound healing |
|
|
Term
| Triamcinolone is ___ acting and can be in what 3 forms? |
|
Definition
- intermediate
plasma half life 60 minutes
biological half life 18-36 hours
Triamcinolone acetonide/diacetate/hexacetonide |
|
|
Term
| Triamcinolone uses and admin: |
|
Definition
- similar to prednisone uses: Opthalmic disorders, respiratory diseases
- oral or injectable (systemic or local) |
|
|
Term
Inhaled glucocorticoids are for long term control of chronic asthma symptoms. What is their mechanism of action?
KNOW THIS |
|
Definition
- reduce bronchial hypersenstivity
- decrease synthesis of inflammatory mediators (leukotrienes, prostaglandins, histamine)
- decrease infiltration by inflammatory cells (eusinophils and leukocytes)
- decreased edema of airway mucosa
- decreased mucous production
- increased responsiveness to beta 2 agonists |
|
|
Term
| Betamethasone is __ acting. |
|
Definition
long
plasma half life 300+minutes
biological half life 36-54 hours |
|
|
Term
| betamethasone relative antiinflammatory potency: |
|
Definition
|
|
Term
| betamethasone administration: |
|
Definition
- oral
- topical
- injectable |
|
|
Term
| Betamethasone clinical uses: |
|
Definition
- respiratory diseases
- respiratory distress syndrome
- local inflammatory conditions
- life threatening/disabling condition |
|
|
Term
| Dexamethasone is __ acting |
|
Definition
long
plasma half life110-210min
biological half life 36-54 hours |
|
|
Term
| Dexamethasone clinical uses: |
|
Definition
Lupus
RA
life threatening conditions |
|
|
Term
| Dexamethasone antiinflammatory potency: |
|
Definition
|
|
Term
|
Definition
|
|
Term
| Dexamethasone suppression test is used to distinguish between __ __ and __ __. |
|
Definition
Cushing's disease
Cushing's syndrome |
|
|
Term
| Dexamehasone suppression test: |
|
Definition
Patients take 1 mg of dexamethasone, a synthetic steroid, at 11 pm and cortisol and ACTH are measured at 8 the next day. Normal persons will show low ACTH and low cortisol due to proper functioning of the feedback system. Cushing’s patients “do not suppress” thus the cortisol levels remain elevated. When performed accurately this test provides a 95-97% efficiency in the diagnosis of Cushing’s.
He said no detailed questions about this on test. |
|
|
Term
| Cushing's disease has __ causes. |
|
Definition
|
|
Term
| Cushing's Syndrome has ___ causes. |
|
Definition
|
|
Term
| with cushings disease too much acth and too much cortisol. with cushings syndrome just too much cortisol. |
|
Definition
|
|
Term
| Cushings syndrome manifestations: |
|
Definition
- glaucoma/cataracts
- moonface
- hirsutism/masculinazation
- cervicodorsal fat (buffalo hump)
- abdominal striae (purple)
- protuberant abdomen
- truncal obesity
- extremity thinning/atrophy
- brittle bones/osteoporosis
- swelling: fluid retention/edema |
|
|
Term
| Adverse effects of glucocorticoids: |
|
Definition
- adrenocortical insufficiency due to HPA suppression
- adrenocortical excess> moonface/buffalo hump
- Diabetes mellitus
- CNS effects: psychological/behavioral changes
- impaired wound healing
- musculoskeletal effects: osteoporosis, muscle weakness, atrophy
- cardiovascular effects: fluid retention, edema, hypertension |
|
|
Term
| Glucocorticoid withdrawal should be performed slowly. Symptoms of withdrawal syndrome: |
|
Definition
- hypotension
- hypoglycemia
- myalgia
- fatigue |
|
|
Term
| the longer on corticosteroids, the slower the withdrawal should be. |
|
Definition
|
|
Term
| Longer period and higer dose withdrawal steps: |
|
Definition
Halve the dose weekly until 25 mg prednisolone or equivalent is reached
Later reduce by about 1mg every 3-7 days. |
|
|
Term
| drugs that enhance corticosteroid effects: |
|
Definition
- estrogen
- oral contraceptives
- antifungal agents
- antibiotics
All of these compete for CYP450 enzymes |
|
|
Term
| Drugs that reduce corticosteroid effects: |
|
Definition
- antacids- inhibit absorption
- Cholestyramine- inhibits absorption
- Phenytoin: inhibits CYP450 enzymes |
|
|
Term
| Contraindications for Corticosteroids: |
|
Definition
- infections
- hypertension with glucocorticoids
- psychosis
- peptic ulcer
- Diabetes mellitus
- Osteoporosis
- Glaucoma
- Pregnancy (prednisolone preferred) |
|
|
Term
| Precauions of glucocorticoid use during pregnancy: |
|
Definition
Follow up examinations of the patient to be done before, during and after steroid therapy
Body weight
X-ray of spine
Blood glucose
Examination of the eye
B.P. |
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