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HD 2 > Pharm - pain meds > Flashcards

Pharm - pain meds Flashcards

0
Q

Common side effects of NSAIDs (6)

A
  1. Gastrointestinal ulceration
  2. inhibited platelet aggregation
  3. HTN & adverse cardiovascular events (remove block of ADH)
  4. decreased renal function IF low CO (inhibit prostaglandin-mediated mech)
  5. inhibit uterine motility (contraindicated in pregnancy)
  6. hypersensitivity reactions (shifts to excess leukotrienes and Phosphilipase A)
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1
Q

Uses for NSAIDs

A

3 F(x)s: anti-inflammatory, anti-pyretic, analgesic.
Treatment for: Gout, neurodegenerative diseases
Prophylaxis for: heart disease (ASA), colorectal cancer.

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2
Q

Effects specific to prostaglandin E2 (aka: PGE2)

A
  • gastric cytoprotection
  • vasodilation & maintain renal blood flow
  • fever (increase set point)
  • pain (sensitize nerve endings to bradykinin)
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3
Q

NSAIDs mechanism of action

A

Competitively inhibit COX-1 & 2 synthesis (esp. 1) –> block prostaglandin synthesis = inhibit prostaglandin signaling pathways.
* do NOT block synthesis of leukotrienes or other inflammatory molecs.

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4
Q

NSAIDs vs. COX-2 inhibitors

A

NSAIDs block COX1 & 2, but preferentially 1 (constitutive pathway).

COX-2 inhibitors = specific to COX2 (inducible) –> should reduce side effects, but COX2 also in endothelium, so still heart & renal SEs.

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5
Q

Aspirin

A

NSAID, salicylate
Use: prevents platelet aggregation, anti-inflammatory.
Mech: acetylates active site for arach. acid binding –> IRREversibly inhibits COX-1 & 2 (prostaglandin synthesis). Inhibits IkB kinase –> block NFkB activation (inflammation).
Elim: liver, short half-life
SE: Reyes in children w/ viral inf; competes w/ Ibuprofen for binding –> give ASA before Ibu; HTN (reduces ADH antagonism)
* esp. effective w/ platelets bc can’t make new COX for platelet lifetime!

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6
Q

acetaminophen

A

(tylenol), = oral analgesic & anti-pyretic (NOT anti-inflamm => not true NSAID)
*Good for chronic mild/mod. pain (less gastric damage)
Mech: COX inhibitor/exact = unknown.
SE: acute liver failure w/ overdose (or EtOH)

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7
Q

allopurinol

A

oral, Gout prophylactic;
1st choice for over-producers, OR under-excreters w/ renal failure
Mech: xanthine oxidase inhibitor (non-competitive), long half-life.
SE: hepatotoxicity, skin rash, GI upset, fever.
*Add low-dose colchicine for 1st months bc frees urate from tissues.

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8
Q

celecoxib

A

NSAID - anti-inflammatory;
Mech: COX-2 selective inhibitor –> block induced protaglandin synthesis.
SE: (more gastroprotective, but) ~high risk adverse cardiac events!
*may block constitutively active vascular endothelium.

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9
Q

colchicine

A

oral, for treatment of acute gouty attacks; (use w/in 24 hrs)
may take small dose daily for gout prophylaxis
Mech: bind & depolymerize leuk microtubules –> decreased migration to inflamed area.
SE: diarrhea, nausea, vomiting, abdom. pain
* fatal toxicity if overdose (renal/hepatic/heart cell death & bone marrow suppression)

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10
Q

Febuxostat

A

oral, for treatment of gout;
Mech: xanthine oxidase inhibitor,
SE: unknown (bc new)
*as effective as allopurinol, but #2 until more known about SEs.

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11
Q

Ibuprofen

A

oral NSAID, anti-inflammatory and fever reducer;
Mech: COX 1 & 2 inhibitor
SE:

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12
Q

indomethacin

A

oral NSAID, anti-inflammatory & fever reducer;
Mech:
SE:

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13
Q

infliximab

A

IV biological DMARD (for rheumatoid arthritis).
Mech: anti-TNF-a monoclonal antibody –> blocks inflamm. signals
SE: anaphylaxis/immune rxn

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14
Q

methotrexate

A

oral or IV DMARD (for rheumatoid arthritis);
Mech: stimulates release of adenosine from cells –> reduce inflammation.
SE: inhibit dihydrofolate reductase (high doses) –> add folate to Tx.
* effectiveness: 30-40% patients don’t respond at all.

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15
Q

probenecid

A

oral uricosuric agent, Gout prophylaxis (#1 for UNDER-excreters).
Mech: increases URAT1 transporter activity –> increase uric acid secretion (bc = structural mimic).
SE: Drug-drug interactions (decrease renal secretion of acids, alter hepatic metab.), contraind: renal insufficiency
** Advise increased fluid intake & alkalinize urine while taking this**

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16
Q

Sumatriptan

A

oral/nasal spray/subcutaneous, terminates acute migraine;
Mech: 5-HT 1B/1D agonist –> direct vasodilation;
- peripheral effect: reduce excitation & peptide release
- Central effect: decrease transmission to second order neuron
SE: “triptan sensations” (flushing, chest tightness, paresthesia) - esp. w/ subQ, overuse headaches.
contraindicated if coronary artery disease

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17
Q

Dihydroergotamine

A

subcut/intramusc/nasal spray, terminates acute migraine.
Mech: non-selective vasoconstrictor (alpha-adrenergic, 5-HT, and dopamine agonist)
SE: nausea, ischemic pain.
* contraindicated in pregnancy & angina*

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18
Q

Drug classes used as migraine prophylaxis (6)

A
  1. B-adrenergic antagonists
  2. anti-epileptics
  3. anti-depressants
  4. serotonergic antagonists
  5. Ca2+ channel blockers
  6. Botulinum toxin (botox)
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19
Q

stepwise order of treatment for migraines

A
  1. (mild) Mild analgesics alone (ie: NSAIDs - ASA, naproxen, etc.)
  2. (moderate) Combination of mild analgesic + vasoconstrictor or sedative
  3. (severe) Combination Tx (like #2) + anti-emetic and prophylaxis
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20
Q

misoprostal

A

oral gastric cytoprotectant,
Mech: synthetic PGE1 analog (inhibit acid secretion, promote mucus secretion, increase gastric mucosa blood flow)
Use: give w/ NSAID to protect stomach

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21
Q

Aspirin dosing

A

Analgesic/Anti-pyretic: 325-650 mg every 4 hrs (adult)
Anti-platelet: 4-6 g/day (= 400+ mg)
(Lethal dose: 10-30 g)
*half-life increases w/ dose size

22
Q

Aspirin Toxicity

A

(reverses 2-3 days after discontinue)

  • tinnitus/high freq. hearing loss
  • headache, nausea, dim vision
  • hyperventilation (= ox. phosphorylation uncoupling, need more O2 & glucose to maintain ATP gradient, stimulate medulla/resp. center)
      • decreased ventilation (depressed medulla) w/ prolonged exposure!
23
Q

Drugs/substances contraindicated in Gout

A
  1. Aspirin (all salicylates)
  2. Diuretics
  3. Alcohol & purines
    * obesity also increases Gout problems*
24
Q

Clinical indications for pharmacological Gout prophylaxis

A
  • Treat w/ prophylaxis if > 2 gouty attacks per year.

* do NOT treat w/ prophylactics DURING acute attacks (for use only in “intercrititcal”/asymptomatic period.

25
Q

Drug treatment for acute gouty attacks

A

Effective for inflammation, not uric acid:
#1: NSAIDs (Not aspirin)
- Glucocorticoids - use instead of NSAIDs if heart disease.
- Colchicine - last choice, notable SEs.
For Uric acid: ACTH (= corticotropin)

26
Q

Types of Gout (& how to distinguish w/ testing)

A
  • Overproducer: >600 mg urateexcreted/day after 1 wk of purine-restricted diet.
  • Under-secreter: patients often non-compliant w/ diet **
27
Q

“DMARDs” (Disease-Modifying Ant-Rheumatic Drugs)

A

1 Tx of Rheumatoid Arthritis… Not curative, but:

  • suppress lymphocyte proliferation
  • -> counteract joint inflammation & destruction
  • slow joint erosion
28
Q

Rituximab

A

biological DMARD, for rheumatoid arthritis;
Mech: partially humanized anti-CD20 antibody…exact mech unknown, but likely; Ab-stimulated cytotoxicity
Use: may be better than methotrexate, VERY effective as combo.

29
Q

Types of drug treatment for Rheumatoid Arthritis

A
  1. acute relief (NSAIDS, glucocorticoids)
  2. chronic:
    a) DMARDs - start EARLY w/ methotrexate
    b) add biological after 3-4 months of DMARD
30
Q

Anti-RA “Biologicals”

A

Class of drugs for rheumatoid arthritis;
Use: #1 @ preventing degeneration of joints, (start after DMARD).
Mech: sequester cytokines/block Rs to prevent inflamm.
- Ab analogues only: may cause Complement-dependent cell toxicity (good or SE)

31
Q

Morphine

A

IV or IM opioid analgesic
Mech: m-opioid R agonist
SE: addiction, resp. depression, constipation

32
Q

Codeine

A

Oral opioid analgesic & antitussive
Mech: m-opioid R agonist (prodrug: converted to morphine in liver, then moprhine-6-glucoronide)
m6g w/ longer 1/2 life, but rapidly excreted in urine (need functional kidneys)
SE: addictive, resp. depression, constipation, antidiuresis

33
Q

Oxycodone

A

oral opioid analgesic,
Mech: m-opioid R agonist (prodrug)
SE: addictive, resp. depression, constipation

34
Q

Hydromorphone

A

oral opioid analgesic,
Mech: m-opioid R agonist (prodrug)
SE: addictive, resp. depression, constipation

35
Q

Meperidine

A

IV or IM opioid analgesic,
Mech: m-opioid R agonist, safer for pregnant women (bc baby DOES have the fetus to convert THIS to active, but not morphine)
SE: highly addictive, resp. depression, constipation
*drug interaction w/ MAOIs

36
Q

Fentanyl

A

IV or transdermal patch analgesic
Mech: m-opioid R agonist (synthetic agonist w/ high affinity)
*100x more effective than morphine!
SE: addictive, resp. depression, constipation

37
Q

Sufentanyl

A

IV or transdermal patch opioid analgesic,
Mech: m-opioid R agonist
(*high potency bc complete synthetic agonist)
SE: addictive, resp. depression, constipation

38
Q

Methadone

A

oral treatment for heroin withdrawal,
Mech: m-opioid R agonist (*long 1/2 life)
SE: IS addictive, resp. depression, constipation

39
Q

Butorphanol

A

IV or IM opioid, precipitates heroin withdrawal.

Mech: mixed agonist/antagonist for m & k-opioid Rs

40
Q

Pentazocine

A

Oral, IM, IV, or SC opioid analgesic, *can precipitate withdrawal;
Mech: m-opioid R partial agonist & k-opioid R agonist
useful in patients w/ high abuse potential
SE: delusional psychosis/delirium

41
Q

Buprenorphine

A

IM/IV opioid analgesic, for opioid addiction Tx
Mech: m-opioid R partial agonist w/ minimal activity & slow dissociation from R; reduces effect of other opioids on R!
SE: resp. depression, constipation

42
Q

Tramadol

A

IV, IM, oral opioid analgesic,
Mech: m-opioid R partial agonist, releases 5-HT, blocks 5-HT reuptake
SE: addictive, resp. depression, constipation

43
Q

Tapenadol

A

oral opioid analgesic,
Mech: m-opioid R agonist, inhibits NE reuptake
SE: addictive, resp. depression, constipation

44
Q

Naloxone

A

IV, for opioid overdose.
Mech: m-opioid R competitive antagonist (central activity)
ONLY binds to opioid Rs, not effect if not using opioids

45
Q

Naltrexone

A

IV, for opioid overdose or addiction Tx;
Mech: m-opioid R competitive antagonist
longer duration than Naloxone
ONLY binds to opioid Rs, not effect if not using opioids

46
Q

N-Methytrexone

A

oral opioid, for relief of constipation in advanced illness.
Mech: peripherally acting m-opioid R competitive antagonist (minimal CNS activity)
SE: constipation

47
Q

Alvimopan

A

oral opioid for accelerating time to upper/lower GI recovery, or opioid overdose/addictive Bxs.
Mech: peripheral acting m-opioid R competitive antagonist (minimal CNS activity)
SE: constipation

48
Q

list of partial opioid agonists

A
  1. butorphenol
  2. pentazocine
  3. buprenorphine
49
Q

Effects of mu opioid R activity

A
  1. supraspinal AND spinal analgesia,
  2. antidiuresis,
  3. euphoria & sedation
    (also: Respiratory depression, miosis, decreased GI motility, smooth muscle spasm, & very significant physical dependance)
50
Q

effects of delta opioid R activity

A
  1. supraspinal AND spinal analgesia,
  2. antidiuresis
    (also: Respiratory depression, miosis, decreased GI motility, smooth muscle spasm, & very significant physical dependance)
51
Q

effects of kappa opioid R activity

A
  1. spinal analgesia
  2. diuresis
  3. dysphoria & sedation
    (also: some respiratory depression, miosis, decreased GI motility, and physical dependance)
52
Q

Major side effects of opioid analgesics

A

1. addiction

  1. respiratory depression (threshold is constant, even though tolerance may make needed dose increase – can reach fatal “needed” dose if used for long enough) esp. w/ asthma
  2. constipation (w/ chronic use)
  3. hyperalgesia/allodynia IF used for a very long time

HD 2 (14 decks)

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