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Pharmacology MBBS > Steroids, drugs acting on 🦴 > Flashcards

Steroids, drugs acting on 🦴 Flashcards

1
Q

Hydrocortisone

A

Least glucocorticoid effect, so t1/2 is just 8-12 hr
Effects:
Glucocorticoids x1
Mineralocorticoid x1

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2
Q

Prednisolone and

Methyl prednisolone

A 
1. Prednisolone:
• Adding double bone to hydrocortisone
• Oral
• GC  x4 & MC x0.8
2. Methyl prednisolone:
• IV
• GC x5 & MC x0.8
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3
Q

Fludrocortisone

A 
Add F to hydrocortisone
GC x15, but
MC *150
Most potent MC in MC receptor
But aldosterone has max M/C activity and it is a pure MC with MC x500
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4
Q

Steroids with bone double bond and F

A 
Pure GC like:
1. Triamcinolone:
• GC x5
• t1/2 12-36 hr
2. Betamethasone &
 Dexamethasone (most potent):
• GC x30
• Both have max GC effect
• t1/2 36-72 hr
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5
Q

Combining propionate, valerate & butyrate with clobetasol steroid

A 
🔼 lipids solubility ➡️ topical use 
Potency depends on:
1. Formulation
 Ointment 🧴 > cream 
2. Functional group
Most potent topical steroid: clobetesol propionate
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6
Q

Combining dipropionate functional group with steroids (like beclomethasone)

A

Inactivates steroids
Inhalation route
Activated in lung by esterase ➡️ 🔽 risk of oropharyngeal candidiasis

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7
Q

Steroids effects

A 
1. Glucose
 Lemon on stick, 🔼 DM
2. Musculoskeletal
3. GIT: gastric ulcer 🔼
4. Ocular
5. Skin & hair: thinning
6. 🤰: surfactant, …
7. Bone marrow
8. CNS: 🔼 psychosis,…
9. Anti-neoplastic effects: ALL, NHL
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8
Q

Steroids and glucose & GIT

A
  1. 🔽GLUT-4 ➡️ 🔼insulin ➡️ 🅱️HSL ➡️ 🅱️ lipolysis ➡️:
    • Thinning of limbs due to muscle breakdown
    • Buffalo 🦬 hump and trunkal obesity
    Lemon 🍋 on stick appearance
  2. Insulin resistance ➡️ 🔼DM
  3. GIT:
    🅱️ PG synthesis ➡️ 🔼 gastric ulcer
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9
Q

Steroids and musculoskeletal system

A
  1. Osteoporosis
  2. Growth retardation in children
  3. Myopathy
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10
Q

Steroids and 👁

A

Use:
Topically for inflammation like uveitis, optic neuritis, choroiditis
CI: HSV keratitis
can cause irreversible clouding of cornea
S/E:
1. Topical: glaucoma
2. Systemic: cataract

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11
Q

Steroids and 🤰

A
  1. Maturation of surfactant in premature labor:
    • Dexamethasone: DoC
    6 mg 12 hourly, 4 doses
    • Betamethasone: best drug (less risk of peri ventricular leukomalacia of newborn)
    12 mg 24 hourly, 2 doses
  2. Dexamethasone used in 🤰 with congenital adrenal hyperplasia baby to prevent virilisation
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12
Q

Dexamethasone is preferred during pregnancy for fetal lung maturation, but not
prednisolone

A

Prednisolone is converted to its inactive form prednisone by placental 11-βHSD. Immature
fetal lung cannot activate prednisone into prednisolone.
Dexamethasone is a poor substrate for placental 11-βHS resulting in its poor placental
metabolism along with low maternal protein binding. Thus, there is an increased transfer
of dexamethasone across the placenta to the foetus. Hence it is preferred

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14
Q

Steroids on skin/hair, CNS and bone marrow

A 
Skin/hair:
 Thinning of both ➡️ bruises and striae
Bone marrow:
 🔼 RBC & neutrophil ➡️ 🔽rest
CNS: 
 Neuropsychiatric effects: psychosis, depression, insomnia
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15
Q

Steroids and immunomodulatory and anti-inflammatory effects

mechanisms

A
  1. 🅱️ production of inflammatory mediators:
    IL-1, IL-6, TNF-α
  2. 🔼 production of anti-inflammatory mediators:
    Annexin-1, IL-10
  3. Lymphocytes:
    apoptosis and redistribution
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16
Q

Steroids and immunomodulatory and anti-inflammatory effects

side effects, contraindications and uses

A 
S/E: opportunistic infections
CI:
 Active infection except H. influenza meningitis
Uses: 
 autoimmune and inflammatory disorders
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17
Q

Mechanism of bone 🦴 resorption

A
  1. PTH / interleukin / vit D3 stimulates osteoblast
  2. Osteoblasts using its RANK ligand stimulates RANK receptor of osteoclast
  3. Structural change in bone leading to ruffled borders
18
Q

Mechanism of bone material deposition

A
  1. Bone resorption ➡️:
    • BMP (🦴 morphogenic protein)
    • PG
    • IGF-1
  2. They stimulates osteoblasts which rush to site of bone damage
  3. Induced bone formation
    📝: activated osteoclasts secrete sclerostin which 🅱️ this process
19
Q

Treatment of osteoporosis

A 
1. Inhibit 🦴 resorption:
• Denosumab: 🅱️ RANK
• Bisphasphonates: apoptosis 
• SERMs like raloxifene
• Salcatonin
2. Stimulate 🦴 formation:
• PTH analogues
• Anti-sclerostin Mab
3. Does both: strontium ranelate
20
Q

Denosumab

A

RANK ligand mab
sc route for 3-5 years
Uses:
1. Drug resistant post-menopausal osteoporosis
2. Giant cell tumour
3. Hypercalcemia associated with malignancy/ hyperparathyroidism
4. Prevention of 🦴 metastasis in prostate cancer

21
Q

Denosumab

side effects

A
  1. Osteoporosis of jaw (contradictory)
  2. Femur fracture
  3. Dermatitis
  4. 2° cancer
  5. Pancreatitis
22
Q

Bisphosphonates

Mechanism and examples

A 
Induces apoptosis of osteoclasts
Drugs:
1. Oral:
 Alendronate: glucocorticoid induced
 Risendronate
 Ibadronate
2. Parenteral:
 Zoledronate: longest acting and most potent
 Pamidronate
23
Q

Bisphosphanates

properties, pharmacokinetics and contraindications

A

All drugs 🔽 risk of vertebral and non-vertebral fractures except ibadronate which 🔽 risk of cerebral fractures only
Oral drugs reduce food absorption ➡️
They are taken on empty stomach
CI: renal failure

24
Q

Bisphosphonates

uses

A
  1. DoC for osteoporosis
    duration: 3-5 years
    t1/2: 10 years
  2. Glucocorticoid induced osteoporosis:
    alendronate
  3. DoC for Paget’s disease
  4. DoC for hypercalcemia of malignancy and hyperthyroidism
    Preferred drug is zoledronate
25
Q

Bisphosphonates

side effects

A 
1. Esophagitis: oral drugs 
 Take the drug with full glass of water and not lie down for at least 30 min
2. Osteonecrosis of jaw
 max with zoledronate 
3. Hypocalcemia:
 max with bisphosphonates (esp zoledronate)
 faster with salcatonin
4. Seizure (hypocalcemia)
5. Femoral chalk stick fracture
26
Q

SERM

selective estrogen receptor modulator wrt 🦴

A
  1. Raloxifene:
    • Rx and prophylaxis of post-menopausal osteoporosis
    • S/E: thrombosis, hot flushes
  2. Bazedoxifene:
    Prophylaxis of post menopausal osteoporosis (along with estrogen) in patients with intact uterus
27
Q

Salcatonin

A 
Calcitonin analogue
Uses:
1. SC for Paget’s disease
2. IN for prophylaxis of osteoporosis
3. Analgesic effect in vertebral fracture
S/E:
1. Fastest drug to cause hypocalcemia
2. 🔼 risk of liver cancer (but
 🔽 risk of breast cancer)
28
Q

PTH analogues

drugs and mechanism

A

Teriparatide: PTH analogue
Abolaparatide: PTH related peptide analogue
Mechanism:
Bone resorption (transient hypercalcemia) ➡️ 🔼 bone formation (supplement Ca2+)

29
Q

PTH analogues

uses

A

Uses: SC

  1. Osteoporosis of hypogonadism in post-menopausal 👱🏽‍♀️ and 👨‍🦰
  2. Severe osteoporosis (in 🔼 risk of fracture)
  3. Bisphosphonate induced femoral chalk stick fracture
30
Q

PTH analogues

side effects

A 
1. Osteosarcoma (🕋 ⚠️)
 CI in Paget’s disease
 Max duration of therapy: 2 yr
2. Hypotension
3. Pneumonia
31
Q

Strontium ranelate

A

Strontium resembles Ca2+
Mechanism:
1. Movies into bone matrix ➡️ 🔼 bone formation
2. Osteoclasts can’t remove strontium ➡️ 🔽 bone resorption
Use: osteoporosis

32
Q

Plicamycin

A 
Aka mithramycin
Inhibits bone resorption
Uses:
1. Paget’s disease
2. Hypercalcemia
33
Q

Romosuzumab

A

FDA approved in 2019
Anti-sclerostin mab ➡️ 🔼 🦴 formation
Uses:
Osteoporosis in post menopausal female with high risk of fracture

34
Q

Inhalational steroids has less systemic side effects, even though most of drug enters
GIT

A

After reaching the GIT, steroids will undergo high first pass metabolism in liver, so the
minimum amount of drug only will reach the systemic circulation. Inhalational steroids like
beclomethasone have very short t1/2 after they enter blood, so the systemic toxicity is
reduced

35
Q

Glucocorticoids are administered before thyroid in cases of initiation of therapy for
panhypopitutarism

A

Thyroid hormones increase the metabolism of cortisol. So glucocorticoids are administered
before thyroid hormone replacement to avoid acute adrenal insufficiency

Pharmacology MBBS (19 decks)

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