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Musculoskeletal > Drugs 2 > Flashcards

Drugs 2 Flashcards

1
Q

Colchicine Mechanism

A

depolimerization of microtubules

-required for phagocytosing and movement of WBC (polymorphic neuclotides)

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2
Q

Colchicine Application

A
  • effective only against gouty arthritis (ACUTE)

- prophylactic agent against such attacks

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3
Q

Colchicine Use

A
  • terminate acute attacks of gout
  • prevents recurrence of gouty arthritis
  • in familiar Mediterranean fever
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4
Q

Colchicine Toxicity

A
  • GI disturbances - given to much

- Blood dyscrasias - chronic

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5
Q

Indomethancine Application

A

-treatment of acute attack of gout

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6
Q

Indomethacine Mechanism

A
  • cyclooxygenase inhibitor
  • analgesic and antipyretic
  • inhibits leukocyte motility
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7
Q

Indomethacine Dosing

A

50mg, 3 times a day (3-5 days)

-give with antacid regimen to prevent ulcer

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8
Q

Indomethacine Toxicity

A

50% of patients

  • GI-nausea, vomiting, ulcers
  • CNS- sever frontal headache
  • Hematopoietic disorders
  • antagonize furosemide and HCTZ
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9
Q

Allopurinol Mechanism

A
  • competitive inhibitor of xanthine oxidase (prevents uric acid synthesis) - reversible
  • metabatolized to oxypurinol which is a non-competitive inhibitor of X.O. - irreversible

SUCIDE INHIBITOR

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10
Q

Allopurinol Effects

A
  • reduces plasma levels and urinary excretion of U.A.
  • increases plasma levels and urinary excretion of oxypurine precursors such as Xanthine and hypoxanthine - very H2O soluble
  • facilitates dissolution of uric acid crystals in the joints and kidneys
  • prevents formation of uric acid kidney stones
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11
Q

Allopurinol Uses

A

Primary Hyperuricemia of gout due to enzyme abnormalities and in children (enzyme abnormalities)
Secondary Hyperuricemia due to hematologic disorders (like multiple myeloma) or chemo

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12
Q

Allopurinol Toxicity

A
  • increased incidence of acute gout
  • hypersensitivity rxns, dermatitis (2%), exfoliative dermatitis
  • effects on liver function
  • interactions w/6-mercaptopurine (decrease 25%)
  • ampicillin and related antibiotics are contraindicated
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13
Q

Febuxostat Mechanism

A

Xanthine Oxidase Inhibitor (direct)

  • potent inhibitor of both oxidized and reduced forms of xanthine oxidase, and the enzyme-inhibitor complex is highly stale
  • structurally unrelated to allopurinol
  • lowers urate concentrations by decreasing urate levels
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14
Q

Febuxostat Uses

A
  • more potent than allopurinol in lowering UA levels, less side effects (80mg)
  • lower ureate levels in patients who display adverse symptoms to allopurinol like hypersensitivity
  • can be used in patients with mild to moderate renal impairment
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15
Q

Febuxostat Toxicity

A

-mild, 2-3% of patients had transaminase elevations >3 times the upper limit

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16
Q

Probenecid Mechanism

A

Increase Urinary Excretion or Uric Acid - URICOSURIC AGENT

  • inhibits transport of organic (anions) across epithelial barriers
  • interferes with U.A. reabsorption (by competing) by the organic acid transporter in the brush border of proximal tubule
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17
Q

Probenecid Clinical Effects

A
  • Indicated to increase U.A. excretion in patients who excrete less than 1g or UA a day
  • dissolution of uric acid crystals in joints
  • given with adequate hydration to patients with good renal function
18
Q

Probenecid Toxicity

A

-salicylates inhibit uricosuric action of probenecid

19
Q

Pegloticase Mechanism

A

new class - Bio-uricolytic agents (uricase enzyme)
humans don’t have, but all other animals do
-enzyme urate oxidase with polyethlyene glycole
give IV in patients that all other drugs have failed
-breaks uric acid into allontoin, which is then excreted and it’s more water soluble
-recombinant Pig enzyme

20
Q

Pegloticase Effects

A
  • rapidly lowers serum levels of uric acid and reduces the urinary excretion of uric acid
  • increases serum levels of allantoin and the urinary excretion of allantoin, which is 5 times more soluble than UA
21
Q

Pegloticase Use

A
  • control hyperuricemia in patients with severe gout in whom congenital therapy has failed/contraindicated (~50,000)
  • large crystals (tophi) around hands or elbow
22
Q

Pegloticase Toxicity

A
  • gout flares (b/c crystals dissolve) give Colchicine, NSAIDS, steroids prophylactly
  • pegylated formulation of urate oxidase in order to increase elimination half-life of enzyme (would be 8 hours)
  • IV every 2 weeks, expensive $30,000 per year
  • 89% developed abs against PEG moiety of pegloticase, so need decreased dose
23
Q

Duloxetine Mechanism

A

-for fibromyalgia
inhibit reuptake of serotonin-norepinephrine
(ser more)

24
Q

Duloxetine Pharm

A

-urinary elimination

_CYP metabolism

25
Q

Duloxetine Toxicity

A
  • increase HR & BP, warning with CV issues
  • Contraindicated with closed-angle glaucoma
  • don’t give with MAOI’s
  • SIADH
  • BLACK BOX: suicidal ideation
26
Q

Pregabalin Mechanism

A

fibromyalgia

  • inhibit presynaptic alpha-2-delta subunits of L-type calcium channels
  • inhibit excitatory transmission by glutamate
  • alleviate neuropathic pain, anxiety, pain syndromes
27
Q

Pregabalin Pharm

A

renal unchanged elimination

28
Q

Pregabalin Toxicity

A

rebound symptoms upon withdrawal, dependence

-sedation , depression, suicidal thoughts, dizziness, blurred vision, xerostomia

29
Q

Cyclobenzaprine Mechanism

A

-skeletal muscle relaxer

central action, at level of brainstem

30
Q

Cyclobenzaprine Pharm

A

enterohepatic recirculation, hepatic CYP, decreased clearance in elderly

31
Q

Cyclobenzaprine Toxicity

A

additive depressant with drugs/alcohol
drowsiness, xerostomia, dizziness, fatigue, nausea/vomiting (GI) , constipation, blurred vision
-increase QT interval

32
Q

Tizanidine Mechansim

A

-skeletal muscle relaxer
agonist of pre-synaptic alpha-2 receptor agonist, decreased activation of polysynaptic spinal cord motor neurons with concomitant reduction in muscle tone, but not strength
FDA: MS, spasticity, spinal cord trauma

33
Q

Tizanidine Pharm

A

-renal excretion - decrease with age/renal function

34
Q

Tizanidine Toxicity

A

-hepatocelluar toxicity, require liver tests
-tapered cessation-rebount hypertonicity, tachycardia, HTN
additive CNS
asthenia, xerostomia, dizziness, sedation, hypotension

35
Q

Baclofen Mechanism

A

-GABAb agonist at multiple levels of the spinal cord, inhibitory signal or hyperpolarizing and reducing excitatory polysynaptic pathways
-pain relief by inhibit substance P
FDA: MS, muscle spasm, spasticity, spinal cord trauma

36
Q

Baclofen Pharm

A

renal

37
Q

Baclofen Toxicity

A
  • renal failure drug accumulation: encephalopathy, abdominal pain, seizures, respiratory depression
  • BLACK BOX: rebound-seizures, confusion, hallucinations, psychiatric
  • additive CNS depresison
  • hypotension with MAOIs
  • antidibetic: baclofen
  • drwosiness asthenia, confusion, dizziness, fatigue, headach
38
Q

Dantrolene Mechanism

A

-decreases muscle contraction by directly interfering (ryanodine) with calcium ion release from SR within skeletal muscle
FDA: malignant hyperthermia, MS, neuroleptic malignant syndrome, spasticity

39
Q

Dantrolene Pharm

A

-reconstitution delays administration

40
Q

Dantrolene Toxicity

A

CNS additive

  • with CCB Vfib, cv collapse
  • muscle weakness, drooling, dysarthria, enuresis, myalgias, backache

Musculoskeletal (19 decks)

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