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Give an example of a mineralcorticoid
Fludrocortisone
What is the brand name of Fludrocortisone?
Florinef
What are indications for mineralcorticoids?
Replacement for adrenocortical insufficiency (Addison’s disease)
salt-losing syndrome (increases NA reabsorption)
Unlabeled: Severe orthostatic hypotension
What is the MOA of mineralocorticoids?
Causes Na resorption → increase in BP
mimics aldosterone
What are AE of mineralocorticoids?
fluid imbalance
hypokalemia (K wasting)
edema
Increase in BP
CHF
What is a normal daily dose for fludrocortisone?
0.1 - 0.2 mg PO daily
What is the MOA of glucocorticoids?
binds to intracellular receptors & alters protein synthesis
inhibit leukocyte traffic & access to site of inflammation
When are glucocorticoids or steroids indicated?
any disease involving inflammation
Rheum dis, Respiratory dis, renal dis, GI dis, hepatic dis, MS, ect
What are the 4 most common routes of administration for steroids?
oral
IV
topical
intra-articular
When are topical glucocorticoids indicated?
Psoriasis, eczema, atopic dermatitis, vitiligo, contact dermatitis, ect
When would a low potency glucocorticoid be appropriate?
thin skin
acute inflammatory lesions (diaper rash/eczema behind ear)
What is the main SE of topical glucocorticoids?
skin atrophy
acne
abnormal pigmentation
purpura (broken blood vessels)
delayed skin healing
photosensitivity
infection* - fungal
When would a medium or high potency topical glucocorticoid be used?
Chronic use
Hyperkeratotic (thick skin)
lichenified lesions
What are 3 very high potency options for glucocorticoids?
Clobetasol propionate
halobetasol propionate
betamethasone dipropionate
Strength: 0.05%
What are high potency options for glucocorticoids?
Bertamethasone dipropionate/valerate
Fluocinonide
triamcinolone acetonide
Strength: 0.2- 0.05%
What are low potency options for glucocorticoids?
Dexamethason, flucinolone, hydrocortisone (OTC)
strength: 2.5-0.01%
When would an ointment be appropriate?
thick lichenified lesion, enhance penetration drug
“meaty plaques”
When would a cream be appropriate?
acute and subacute dermatoses; moist skin and interiginous areas
rash in groin/ under boobas
When would solutions, gels & sprays be appropriate?
Scalp, where non-oil based vehicles are needed
How long should medium-high to very high potent topicals be used?
< 3 weeks
irreversible skin atrophy
How long should a medium potency in areas of thin skin be used?
less than 2 weeks
How long and what product should be used for diaper rash?
lowest potency for 3-7 days
With chronic use how should treatment proceed?
intermittent treatment preferred
every other day, weekends only
What are the 2 short-acting oral glucocorticoid options, their T 1/2 life, and potency?
Cortisone
Hydrocortisone
T 1/2: 8-12 hrs
GC<MC
What are the 2 intermediate acting oral glucocorticoid options, their T 1/2 life, with greater glucocorticoid activity than mineralocorticoid?
Prednisone
Prednisolone
T 1/2: 18-36 hrs
GC>>>MC
What are the 2 intermediate acting oral glucocorticoids that express glucocorticoid activity?
Methylprednisone
Triamcinolone
T 1/2: 18-36 hrs
What are the 2 long acting oral glucocorticoids, their T 1/2 life, and their potency?
Dexamethasone
Betamethasone
T 1/2: 36-54 hrs
GC
What is the conversion ratio of prednisone to methylprednisone?
5:4
When is a taper required for oral glucocorticoids?
if received therapy >2 weeks AND doses >20mg/day
When should oral glucocorticoids be taken?
the morning to mimic normal cycle
can cause insomina
What is considered low dose therapy, when is it used, and what AE are there?
<7.5 mg/day
maintenance therapy
relatively few
What is split daily dosing used, what are the AE?
rapid control of active disease
dose dependent, increase in AE
What is a medium dose of oral corticosteroids, when is it used, and what are the AE?
7.5 mg to <30 mg/day
primary chronic conditions (mild-moderate disease)
dose-dependent AE
Approximately how much prednisone do we naturally produce per day?
5 mg of prednisone
For RA patients what is the highest dose of prednisone they should recieve?
20 mg
What is a high dose of oral corticosteroids, when it is used, and the AE?
30 to <100 mg
used for sub-acute disease (active)
Treatment must be short term for severe AE - few days then taper
What is a very high dose of oral corticosteroids, when is it used, and the AE?
100mg
acute disease/exacerbations, usually inpt or hospital
Tx must be short-term, dramatic SE
in outpt >100 mg not give esp if pt never had it before
should live in a bubble bc high risk of infection
CNS effects (psychosis, insomnia, depression)
What is a IV pulse therapy of corticosteroids, when is it used, and the AE?
250 mg for one or a few days
sever/ life-threating disease
low incidence of AE
When converting to alterante-day dosing what is generally the rule of thumb?
2.5-3x the minimal daily dose
requires gradual increase in on days with concurrent decrease on off day dose
Give an example of a split day dosing pack?
Medrol dosepak (methylprednisolone)
When is it okay to stop glucocorticoid therapy without a taper?
Short term (<2 weeks)
low doses (<20 mg/day)
Give examples of tapering schedules for long-term therapy?
decrease by 2.5-5mg q 3-7 weeks
decrease by 2.5 mg q 1-2 weeks
decrease by 5 mg q 1-2 weeks if alternate day dosing
How can we minimize risk of HPA axis suppression when tapering glucocorticoids?
Use lowest effect dose
administer in the morning (prevent insomnia)
alternate-day dosing when appropriate
D/C therapy ASAP
What corticosteroids is more common in oncology?
Dexamethasone
no taper when used for nausea
What corticosteroids are more common in rheum?
prednisone and methylprednisolone
What are early manifestations of systemic adverse effects from systemic glucocorticoids?
Insomnia
Enhanced appetite
Weight gain
Emotional liability
Leukocytosis
Hyperglycemia
What are sustained AE of systemic glucocorticoid therapy?
Cushingoid habitus
HPA suppression
Infection
Osteoporosis
Impaired wound healing
What are delayed AE of systemic glucocorticoid therapy?
Osteonecrosis
Ecchymosis (bruising)
Cataracts
Growth retardation
Fatty liver
*Atherosclerosis
What are rare AE of systemic glucocorticoid therapy?
Psychosis
Glaucoma
Pancreatitis
Pseudotumor cerebri
What are counter indications for glucocorticoid therapy?
Live vaccines (>20mg of prednisone for more than 2 weeks do NOT)
systemic fungal infections → PCP prophylaxis w/ high doses of Bactrium
Hypersensitivity
What are some warnings for glucocorticoid use?
Active infections
DM
Osteoporosis
Peptic ulcer
Electrolyte imbalances
Stress, Trauma, or surgery
HPA suppression
What drug causes reduced elimination and metabolism of prednisone?
Ketoconazole (strong CYP 3A4 inhibitor)
What drugs causes increased elimination and metabolism of prednisone?
Phenytoin
Carbamazepine
Rifampin
Phenobarbital
What should be monitored if the patient is on Furosemide and glucocorticoids?
Check Potassium (K)
What should be monitored with concurrent Amphotericin B and glucocorticoids?
Check Potassium (K)
What occurs with concurrent use of glucocorticoids and aspirin?
may decrease serum aspirin levels
What should be monitored during glucocorticoid therapy?
Labs (glucose, electrolytes, WBC)
Stool test for occult blood loss
DEXA scan
Growth & development
blood pressure
Ophthalmologic exams
What should a patient do if they miss a dose?
Daily: take ASAP (skip if close to next dose)
QOD: take ASAP, ski that day and take the next morning
When does glucocorticoid-induced osteoporosis occur and when should they be treated?
w/in first 6-12 months of therapy
decrease bone formation w/ increase bone resorption
osteoporosis trxt may be needed for prednisone doses btwn (5-7.5mg daily)
What is the target supplementation of Vitamin D and Calcium in adults taking> 2.5/day for > 3 months?
Calcium: 800-1000mg/day
Vitamin D: 600-800 mg/day
What is the next step if supplementation of Calcium and Vitamin D is not enough to prevent glucocorticoid-induced osteoporosis?
Oral bisphosphonates (moderate to high risk)
Alendronate, ibandronate → stand 1 hr after & take with empty stomach and water
Note
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