Analgesics

Question 1

Anti-inflammatory

3 main classes

Analgesic Drugs

3

Answer 1

• Anti-inflammatory
  
  • Cyclo-oxygenase inhibitors
  • Antirheumatoid drugs
  • Anticytokine and other biological agents
• Analgesics
  
  • Above list and opoids and local anesthetics

Question 2

Unwanted effects of COX inhibition

4

Answer 2

• GI disturbances
  
  • COX-1 imp in producing prostaglandins for mucous and acid secretion
  • Inhibition leads to dyspepsia, nausea ulcers
• Skin rxns
• Adverse renal effects
• Cardiovascular
  
  • inc risk of stroke and MI

Question 3

Cyclo-oxygenase Inhibitor Drugs

9

Answer 3

• Aspirin
• Diflunisal
• Indomethacin
• Sulindac
• Tolmetin
• Ibuprofen
• Naproxen
• Acetaminophen
• Celecoxib

Question 4

Aspirin

Answer 4

• Used as platelet inhibitor
• Given post-MI and post-TIA to reduce thrombotic risk
• Used with other anti-coagulants (inc risk of bleeding)
• Permanent inhibition
• DOnt give to kids with viral bc of Ryes syndrome

Question 5

Diflunisal

Answer 5

• More potent COX inhibitor than aspirin
• Doesnt cross BBB, no antipyretic effect

Question 6

Ibuprofen

Answer 6

• More potent than aspirin and acetaminophen
• Fewer GI effects
• High or prolonged doses show kidney toxicity
• Not recommended during pregnancy
  
  • Acetaminophen instead

Question 7

Acetaminophen

Answer 7

• Good for kids in dental pain and prego women
• weak anti-inflammatory effects
• High doses–> Liver toxicity

Question 8

Celecoxib

Answer 8

• COX-2 inhibitor
• Fewer Gi side effects
• Was used for chronic pain (rehumatoid arthritis)
• COX-2 inhibitors associated with increased risk of myocardial infarction

Question 9

Antirheumatoid Drugs: Disease Modifying Antirheumatic Drugs

3 ex (1 with MoA)

Answer 9

• Inhibit erosion of cartilage and bone
• Slow onset, months
• Methotrexate
  
  • Folate antagonist (inhibits cell division–> immunosupressant)
• Penicillamine
• Gold compounds
• other compounds UK MoA

Question 10

Immunosuppressant Drugs

Tx 3

3 main grps

Answer 10

• Tx
  
  • autoimmune diseases, organ transplant, inflammation is problematic
• 3 groups
  
  • IL-2 inhibitors
  • Cytokine inhibitors
  • Purine/Pyridamine synthesis inhibitors

Question 11

Cyclosporin

class

action

used in

Answer 11

• Immunosupressive: IL-2 inhibitor
• Decreases proliferation of T cells
• Inhibits transplant rejection

Question 12

Cortisol (glucocorticoids)

Class

Acts

other effect

Answer 12

• Immunosuppressive: Cytokine inhibitor (including IL-2)
• Decreases immune activation by inhibiting cytokine
• Anti-inflammatory and immunosuppressive

Question 13

Biopharmaceutical anti-cytokine drugs

Action

good for

4 ex and what they block

Answer 13

• Block specific steps in cytokine paths
• Include recombinant antibodies and proteins
• Effective for chronic inflammation and leukemias
• Infliximab
• Adalinumab (TNF-alpha Ab)
• Anakinra (blocks IL-1 receptor)
• Abatacept (cytotoxic T cell AB)

Question 14

Azathioprine

class

tx

side effects

Answer 14

• Immunosupp: Purine synthesis inhibitor
• tx auto-immune diseases
• Side effects: bone marrow suppression, nausea, vomiting

Question 15

Drugs for gout

5 and acute or prophylaxis

Answer 15

• NSAIDs
  
  • Acute pain
• Glucocorticoids
  
  • acute anti-inflammatory
• Colchicine:
  
  • acute tx
• Allopurinol:
  
  • Prophylaxis
• Probenecid
  
  • Prophylaxis

Question 16

Opiod Receptors

endogenous ligands and 4 classes of receptors

Answer 16

• Enkephalins and endorphins are endogenous receptors
• Receptors form homo/heteromers–> GPCR
• 4 main classes
  
  • m
  • d
  • k
  • ORL1

Question 17

Opiod Receptos

4 classes and effect

Answer 17

• m
  
  • main site for analgesic effects
  • Respiratory depression
  • Pupil constriction
  • Dec GI motility
  • Euphoria
  • Sedation
• d
  
  • Analgesic and proconvulsant
  • Resp dep
  • Dec GI motility
• k
  
  • spinal cord, analgesia, sedation, dysphoria, hallucinations

Question 18

Morphine

Effects on CNS

Answer 18

• Activates m receptors
  
  • Analgesia good for acute and chronic pain, not effective for neuropathic syndromes
  • Euphoria, sedation
  • Resp depression cough suppresion
  • Nausea vomiting
  • Pinpoint pupils(m and k)
  • Constipation
  • Histamine release

Question 19

Opiod withdrawal symptoms

tx

Answer 19

• Severe case of flu, 7-10 days
• Restlessness, runny nose, sweating, aches, hot/cold flashes, diarrhea, vomiting
• Methadone for addicts
• Clonidine (alpha2 adrenergic agonist) help tx symptoms of withdrawal

Question 20

Opiod Drugs

10

Answer 20

• Morphine
• Heroin
• Codeine
• Oxycodone and Hydroxycodone
• Fentanyl
• Lortab
• Methadone
• Loperamide
• Naloxene
• Naltrexone

Question 21

Morphine, codeine, oxycodone, hydroxycodone, fentanyl

to tx what kind of pain

Answer 21

• Morphine
  
  • acute and chronic
• Codeine
  
  • Mild pain, metabolized to morphine
• Oxycodone and hydroxycodone
  
  • acute and chronic
• Fentanyl
  
  • Acute and anesthesia

Question 22

Lortab

is what 2 drugs combined

Answer 22

Acetaminophen + hydrocodone

Question 23

Loperamide

tx

Answer 23

• Tx for diarrhea, oral tablets OTC
• Does not cross BBB–> no euphoria or analgesia

Question 24

Naloxene

Answer 24

• Short acting opiod antagonist
• Counteracts resp dep w/ opiod OD
• Helps with withdrawal

Question 25

Nuropathic Pain tx 2

Answer 25

* Amitriptyline * TCA Antidepressant * blocks NE uptake * Gabapentin * Antiepileptic * blocks Ca