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Pharmacology Test 3 > Bisphosphonates > Flashcards

Bisphosphonates Flashcards

1
Q

Bisphosphonates for Osteoporosis

A
  • alendronate
  • risedronate
  • ibandronate
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2
Q

Bisphosphonates for multiple myeloma and skeletal metastases of solid tumors

A
  • zolendronic acid

- pamidronate

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3
Q

Bisphosphonates for hypercalcemia of malignancy

A
  • etidronate
  • pamidronate
  • zolendronic acid
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4
Q

Bisphosphonates for Paget’s disease of bone

A
  • alendronate
  • risedronate
  • tiludronate
  • pamidronate
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5
Q

CANT use for Paget’s disease of bone

A

teriperatide

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6
Q

RANKL drug

A

Denosumab

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7
Q

30S inhibitors

A
  • aminoglycosides
  • – blocks initiation, elongation -> termination, miscoding
  • tetracyclines
  • – blocks elongation
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8
Q

50S inhibitors

A
  • macrolides
  • – inhibit elongation
  • clindomycin
  • – blocks translocation
  • streptogramin
  • – blocks translocation, inhibits elongation
  • Linzolid
  • – blocks initiation
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9
Q

Linzolid

A

VRE

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10
Q

Classical chemotherapy targets

A

limitless replicative potential

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11
Q

taxanes a vinca are

A

natural substances

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12
Q

Antifolates

A
  • inhibit cell division by limiting availability of DNA precursors
  • DHFR = folate -> tetrafolate -> tymine nucleotides/purines
  • ** folate analog competitive inhibitors bind 100x tighter to DHFR ***
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13
Q

Antifolates Toxicity

A
  • myelosuppression
  • mucositis
  • nephrotoxicity
  • hepatotoxicity
  • neurotoxicity
  • pulmonary and alleopecia (rare)
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14
Q

Antifolate Resistance

A
  • decreased metabolism
  • change in DHFR
  • decreased cell entry
  • increased efflux
  • increased folate salvage
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15
Q

Leucovorin

A
  • rescue

- reverses antifolate toxicity

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16
Q

Bisphosphonates

anti-resorptive agent

A
  • non-hydrolyzable PCP bond
  • BIND CALCIUM and accumulate at remodeling sites
  • PREVENT DIFFERENTIATION OF MACROPHAGES into osteoclasts; inhibit osteoclast activity and cause APOPTOSIS
  • suppress remodeling and decrease number of remodeling units

-DRONATE

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17
Q

Nitrogen containing BPs inhibit

A
  • FPP, inhibiting osteoclast activity
18
Q

BP contraindications

A
  • hypocalcemia
  • GI disease
  • esophageal abnormalities
  • kidney disease
  • pregnancy
19
Q

Compared to morphine, buprenorphine would be expected to

A

precipitate withdrawal in a herone addict

20
Q

Give something other than morphine to transition?

A

methadone (40?)

21
Q

D2

D3

A

D2: Ergocalciferol: from mushrooms/fish
D3: cholecalciferol: from skin after exposure to sun

22
Q

Calcitriol

A
  • active form of Vit D

- kidney converts other D forms to calitriol

23
Q

Calcitonin

A
  • salmon
  • less critical for homeostasis
  • reduces serum calcium and phosphorous by PROMOTING BONE DEPOSITION AND STIMULATING RENAL EXCRETION
  • produced by thryoid gland
  • inhibits bone resorption by DIRECTLY BLOCKING OSTEOCLAST ACTIVITY
24
Q

Summary of Calcitonin

A
  • increases bone density, decreases fractures
  • REDUCES ACUTE PAIN due to fractures/metastases
  • DESTROYED QUICKLY IN GI TRACT: intrnasal spray or injection
  • for those who can’t tolerate estrogen or BPs
  • can worsen postmenopausal symptoms
  • injected calcitonin also for symptomatic PAGET’s DISEASE OF BONE
  • TOLERANCE is common
25
Q

Sulfonamides

A
  • PABA analogs that competitively inhibit dihydroptarate preventing creation of folate
  • bacteriostatic
26
Q

Trimethoprim

A
  • selectively inhibits bacterial DHFR preventing creation of folate
  • bacteriostatic
27
Q

TMP-SMX

A
  • bactericidal
  • # 1 UTIs
  • short course
  • allergic response common
28
Q

Abaloparatide

A
  • ONLY BUILDS bone; take with BPs
    Contraindication: osteosarcoma
  • after discontinue can have rebound bone loss -> intermittent treatment followed by BP to prevent this
29
Q

Slerostin

A
  • WNT signaling pathway
  • – stimulate osteoblast, inhibit osteoclast
  • leads to decreased bone resorption and increased bone formation
  • sclerostin deficiency inhibits WNT pathway
  • – sclerostin deficiency have high bone mass
  • calcitonin increases sclerostin production
30
Q

Romozumab

A
  • antibody against sclerostin
  • stimulate/restore WNT pathway
  • stimulate increased bone formation and decreased resorption
    CARDIOVASCULAR ADVERSE EFFECTS
31
Q

Fluoroquinolones

A
  • block bacteria DNA replication

- block DNA gyrase

32
Q

B-lactam mechanism

A
  • all look like D-Ala–D-Ala
  • – transpeptidase reacts to D-ala-D-ala to make crosslinks = peptidoglycan
  • ** transpeptidase attacks B-lactam instead of D-Ala–D-Ala ***
  • – transpeptidase and B-lactam not covalently linked and can’t be separated
  • enzyme dies
  • ** can only kill growing cells! ***
33
Q

Bacterial B-lactamases

A
  • bacterial response to B-lactam antibiotic
34
Q

B-lactamase inhibitors

A
  • ** NO ANTIBACTERIAL ACTIVITY ***
  • don’t kill bacteria
  • target and remove B-lactamases, freeing up initial drug to kill bacteria
  • inactivate B-lactamases irreversibly
35
Q

Amoxicillin

Penicillin

A
  • acid stable
  • > activity against gram -
  • inactivated by B-lactamases
  • oral, IV, IM
  • quickly broken down
  • allergic responses; all penicillin cross reactive
36
Q

Probenecid

A
  • inhibits secretion of penicillin
37
Q

Augmentin

A

penicillin + clavulanate

clavulanate = B-lactamase inhibitor

38
Q

Benzomorphans

A
  • 3 rings

SIEZURE = answer?

39
Q

6 rings

A
  • don’t breakdown = toxicities
40
Q

Morphine

A

low bioavailability; short t1/2; bad withdrawal

  • excreted via kidney - can cause renal failure
  • chronic: pain for terminal illness, particularly cancer
41
Q

Acute Morphine Toxicity

A
  • coma
  • pinpoint pupils
  • life threatening respiratory depression
  • ventilate
  • reversible with antagonists

Pharmacology Test 3 (9 decks)

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