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Pharm > Pharm endocrine (Bone) drugs > Flashcards

Pharm endocrine (Bone) drugs Flashcards

1
Q

3 main hormones Ca+2/phosphate homeostatis

A
  1. PTH - GI tract, Kidney tubule, Bone - Mech of action = Ca+2 & phosphate increase w/Vit D action (GI) -> Ca+2 increase & Phosphat decrease (kidney)
  2. VIT D- Gi tract, bone, Parathyroid gland- Mech of action = Ca+2 & phosphat increase (GI), PTH decrease (PT)
  3. FGF-23- Kidney, GI, bone - Mech of action= Decrease Pi & calcitriol (kidney), Decrease Ca+2, Pi absorption Via low Calcitriol secretion (GI), Mineralization of Bone matrix
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2
Q

Vit D supplements

A
  • Cholecalciferol = Vit D3 (meat)
  • Ergocalciferol = Vit D2 (plant)
  • Ergo - used for food fortification (enrichment), available for high dose injection
  • MOA = reg gene transcription via Vit D receptor
  • Clinical Uses:
  • Oral admin to treat Vit D def
  • Secondary HYPERparathryroidism (Increased PTH due to hypocalcemia)
  • HYPOparathryroidism (HIGH doses, combo w/calcium supplements)
  • Rickets & osteomalacia
  • Osteoporosis (w/ca+2)
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3
Q

Vit D Adverse Effects

A
  • Hypercalcemia - bypassing feedback regulation maintains normal levels
  • Hyperphosphatemia
  • Hypercalciuria
  • Drug interactions:
  • Aluminum - in form of antacids (interferes w/ Absorption)
  • Atorvastatin (lipitor) - Vit D decrease plasma conc of atorvastatin
  • Decrease effectiveness of **CYP 3A4 meds **
  • Thiazide antidiuretics (block Na/Cl- transporter) can lead to hypercalcemia
  • Cardio drugs = digitoxin, dilitiazem (BP meds)
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4
Q

Vit D analogues

A
  • _Calcitriol (D3 meat) _
  • Management of secondary hyperpara in pts with kideney disease
  • management of hypocalcemia in pts w/hypoparathyroid
  • May cause more hypercalcemia than _paricalcitol _
  • Doxercalciferol (D2 vege)
  • Used to treat secondary hyperparathryroid (increase PTH due to low serum Ca+2) in pts with kidney disease
  • Paricalcitol (D3 meat)
  • Analog of calcitriol used for secondary hyperparathyroid in pts with kidney disease on DIALYSIS
  • Calcipotriene: analog of calcitriol
  • Research for dermatological use inflammatory disease - NO apply face
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5
Q

Vit D considerations

A
  • Is considered secosteroids:
  • Lipophilic compounds - orally absorbed - sequestered in fat (obesity lead to vit D def)
  • Drug interaction - Sunscreen
  • Parent compound NOT bioactive, adverse effects (toxicity) from VIT D itself are rare.
  • Overdose may happen when enough 25OH-D is made to active receptors = VITD overload
  • Symptoms:
  • Confusion, nausea, constipation, thrist, urination
  • Labs = PTH lvl undectable, Increase ca+2 serum & urine
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6
Q

Alendronate

A
  • Analogues of pyrophosphate
  • Sit upright/stand for 30-60 min to take
  • MOA:
  • supresses activity of osteoclasts = inhibits bone reabsorption
  • Clinical uses:
  • Osteoporosis
  • Paget’s disease
  • Adverse effects:
  • Adynamic bone (reduced osteroblast & clasts)
  • Eophageal irritation
  • RARE: osteonecrosis of Jaw
  • Similar:
  • Risedronate, ibandronate, pamidronate
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7
Q

Bisphophonates

A
  • Impair ability of osteoclasts to form ruffled border
  • Impair osteoclasts to adhere to bony surface
  • Inhibit osteoclasts ability to produce protons necessary for bone reabsoption
  • Promote osteoclast apoptosis
  • Daily oral = Alendronate, Risdronate, Ibandronate
  • Weekly oral = Alendronate, Risedronate
  • Monthly oral = Ibandronate
  • Quarterly inject = Ibandronate
  • Annual infusion = Zoledronate
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8
Q

Pamidronate & Zoledronate

A
  • Clinical use:
  • Osteolytic lesions of multiple myeloma & breast cancer - due to overexpression of RANKL (osteoclast activation)
  • Hypercalcemia assoc w/malingnancy
  • IV only
  • Osteonecrosis of JAW most common
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9
Q

RANKL atagonists - Denosumab (-)

A
  • MOA
  • Monoclonal antibody targets receptor activator of nuclear factor kappa-B ligand (RANKL)
  • Clinical uses:
  • Osteoporosis prevention/treatment - SC injection every 6 months
  • Adverse effects:
  • Jaw osteonecrosis in cancer pts (breast cancer)
  • Hypocalcemia
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10
Q

Raloxifene

A
  • Selective estrogen-receptor modulator (SERM) - oral admin
  • MOA:
  • Esterogen agonist effect in bone
  • Estrogen antagonist effects in breast & endometrium
  • Clinical uses:
  • Osteoporosis in post menopausal women
  • Decreases breast cancer
  • Adverse effects:
  • Hot Flashes
  • Thromboembolism - CONTRAindicated in women w/history DVT
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11
Q

Teriparatide (PTH)

A
  • MOA:
  • Acts through PTH receptors to increase bone formation by osteroblasts
  • Clinical uses:
  • Severe osteroporosis
  • Adverse effects
  • Hypercalcemia
  • Hypercalciuria
  • Osteoscelorosis & osteosarcoma (tumor in mesenchymal space bone)
  • Leg cramps
  • SC injection daily BEST for osteoporosis
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12
Q

Teriparatide (hPTH 1-34)

A
  • PTH analogue
  • Contraindications:
  • Open epiphyses
  • prior radiation therapy
  • Paget’s disease
  • Hypercalcemia
  • Similar = hPTH 1-84 & Fluoride for osteoporosis
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13
Q

Calcitonin

A
  • SC injection or intranasal admin (SC injection lowers serum Ca+2 hours)
  • MOA:
  • Acts through calcotonin receptors = inhibit bone resorption by osteoclasts
  • ALSO inhibits Ca+2 absorption in GI & reabsorption in kidneys
  • Clinical uses:
  • Postmeno osteoporosis (NOT 1st line)
  • Hypercalcemia
  • Adverse effects:
  • Rhinitis w/nasal spray
  • Flushing, nausea, diarrhea
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14
Q

Cinacalet

A
  • Oral admin ONLY
  • MOA: increases sensitivity to Ca+2 sensing receptor to Ca+2 in PT cells = decrease of PTH
  • Clinical use:
  • Chronic kidney disease - secondary hyperparathyroid
  • Hypercalcemia associated w/ parathryroid carcinoma
  • Adverse effects:
  • Nausea, dizziness
  • hypocalcemia
  • Adynamic bone (issues w/kidneys Low osteoblast & clast)
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15
Q

Sevelamer (phosphate binder)

A
  • MOA
  • Decreases GI absoption of inorganic phosphate
  • Lowers serum cholesterol binding to bile acids
  • Clinical uses:
  • Chronic kidney disease
  • Hypoparathyroidism
  • VIt D intoxication
  • Tumoral calcinosis (calcium deposits in soft tissue)
  • Hyperphosphatemia (hyperotosis syndrome)
  • Adverse effects:
  • Constipation
  • Thrombosis
  • Hypertension
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16
Q

Al hydroxide & Ca+2 carb/acetate (phosphate binders)

A
  • Al hydroxide: Rarely USED due to effects
  • Ca+2 carbonate & acetate: Similiar to sevelamar
  • Acidic gastric PH required for Ca+2 carbonate (CaCO3) absorption
17
Q

Calcium Supplements

A
  • MOA: essential for bone mineralization
  • Preps:
  • Ca+2 gluconate (IV)
  • Ca+2 carbonate (oral)
  • Ca+2 citrate-malate (oral)
  • Clinical uses:
  • Secondary hyperpara (High PTH due to low serum Ca+2)
  • Hypoparathyroidism
  • Rickets / oseomalacia
  • Adverse effects:
  • Constipation
  • Hypercalciuria
  • Hypercalcemia
  • Renal Calculi
  • Considerations: Needs to be taken with food (better absorption GI)
18
Q

Inorganic Phosphate

A
  • MOA:
  • Essesntial for bone mineralization
  • Clinical uses:
  • Severe Hypophosphatemia (LOW phosphate in blood)
  • Adverse effects:
  • Diarrhea
  • K+ phosphate preferred over sodium phosphate - minimize renal excretion of phosphate OR correct coexisting hypokalemia

Pharm (14 decks)

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