Opoids/ On Flashcards
1
Q
What are Opioids?
A
-Drugs that bind to receptors in CNS
2
Q
3 main opiate receptors
A
Mu, kappa, Delta
3
Q
Mu receptor
A
- most important
- analgesia, resp. depression, euphoria, sedation, physical dependence
4
Q
Kappa receptor
A
-Analgesic, sedation, psychotomimetic effects (psychotic)
5
Q
Delta receptor
A
opioids don’t interact with delta
6
Q
Agonists
A
- Drugs that occupy receptors and activate them
7
Q
Agonist + antagonist
A
- Offer less activation of receptor
8
Q
Antagonist
A
- Drugs that occupy receptors but do not activate them. Antagonists block receptor activation by agonists.
- No analgesia, precipitate withdrawal
- used for overdose
9
Q
Morphine is the __________
A
Gold standard
10
Q
Opioids Effect
A
- No analgesic ceiling
- You can keep going up and up
11
Q
Opioids SE
A
- Resp depression
- Sedation
- Constipation
- Nausea
- Itching
- Postural Hypotension
- urinary retention
- All of these SE are limited except Constipation
- Also has anti-tussive and anti-diarrheal properties
12
Q
Other Side Effects Opioids (less common)
A
- Neurotoxicity
- Miosis (always despite tolerance)
- Euphoria/Dysphoria: Anxiety/ sense of unease
- increased ICP- not used head injury patients
- Biliary colic- not used in cholecystitis patients
- Prolonged use -> immune depression
13
Q
Management of Resp depression/ sedation
A
- If RR below 12 bpm.. do something
- Arousal, oxygen, HOB elevated, naloxone
- IM: 30 mins
- IV: 7 mins
- SQ: 90 mins
14
Q
Management of constipation
A
Prevention: fluid/ fiber/ prune juice
Stool Softener: (docusate = Colace)/ stimulant laxative (senna= Senokot)
-Drugs for long term constipation form opiods
15
Q
Nausea/ Emesis Management
A
- Recumbent position helps
- Premediate with antiemetics
16
Q
Itching
A
Premedicate with antipruritic agent (diphenhydramine)
- Change to a different opioid
17
Q
Hypotension/ Post Hypotension
A
- don’t give if BP is too low
- Move positions slowly
- Only up with assistance
18
Q
Urinary retention
A
- Monitor, prevent with voiding q 4
- May need I&O catheter
19
Q
Morphine Sulfate
A
-DOC fro MI pain, and air hunger
20
Q
Dilaudid (hydromorphone)
A
- 2nd DOC more potent than morphine
- Normal dose 0.3 mg
21
Q
Fetanyl (Duragesic)
A
- dosed in mcg
- 80x stronger than Morphine
- used with chronic pain and anesthesia
- comes in patch and intranasal
- IV not common
22
Q
Methadone (Dolophine)
A
- Used for opiod addiction (low dose)
-For pain: long half life but harder to titrate - ## don’t use in elderly lots of deaths related to its use
23
Q
Demerol ( Meperidine)
A
- Synthetic opiod
- great pain relieving
- half- life : 2-4 hours
- toxic metabolite normeperidine half life of 24-48 hours can cause seizures
- Should only be used for short period (2 days)
- Assess for toxicity: nervousness, tremors, seizures
24
Q
Opioids that treat moderate pain
A
Codeine and tylenol (tylenol #3)
Hydrocodone and tylenol ( Vicodin, Loratab)
Oxycodone and Tylenol ( Percocet, Tylox)
Oxycontin: Extended Release
combos due to synergistic effect
25
Hydrocodone and tylenol
- most prescribed can be used with aspirin and ibuprofen
26
Non- opioid Centrally acting analgesics
MOA: analog of codeine: weak action of mu receptors and blocks norepinephrine and serotonin
Prototype: tramadol (ultram)
Mod to severe pain: onset within 1 hour, works for 6 hours
SE: sedation, dizziness, headache, dry mouth, constipation
-Serious risk of suicide
27
Opioid agonist/antagonist
- bind as agonist on kappa receptors and weak antagonist on mu receptors
- Less analgesia, less resp depression
- Lower potential for abuse
- Psychotomimetic effects: anxiety, strange thoughts, nightmares, hallucinations, delirium
- IF given to patient physically dependent on opiods-> withdrawal
- Ex: Butaphanol (stadol) and pentazocaine (Talwin)
28
Opioid Antagonist
- Bind to mu and kappa receptors but do not cause analgesia
- Naloxone (Narcan)
- Used for overdose, over sedation due to opiods
- Last 1 hour. Redosing is usually necessary
- Given IV, IM, SQ
- only effective on pure opioid agonists or opiod agonist- antagonist
29
Alvimopan (Entereg)
- Selective peripheral mu antagonist
- Blocks adverse effects on bowel action does not affect analgesia
- Short term use to prevent ileus in bowel resection surgery and accelerate bowel recovery
- Risk of heart attack only in hospitalized patients
30
Non- opioids - NSAIDS & acetaminophen
- NSAIDs work by inhibiting cyclooxygenase (COX)
| - 1st and 2nd generations
31
COX -1
Good Cox- considered the good one since it proves GI protection and hemostasis
32
Cox- 2
Bad cox - because it mediates inflammation and sensitizes tissues to pain
33
1st generation NSAIDS
- Blocks both COX-1 and 2
- Decrease pain, inflammation, fever
- Gastric ulceration, bleeding risk, renal impairment
34
1st gen NSAIDS Aspirin
- Irreversible inhibition of COX longer acting effect
- chem family: Salicylate
- Analgesic
- antipyretic
- Anti- inflammatory
- Antiplatelet agent 81 mg dose: one dose lasts a week for platelet aggregation
- Colon cancer prevention, stroke, heart attack
- stop a week before surgery
35
Aspirin SE:
- Most common: Gastric distress, heartburn, nausea
Long term ASA SE: Gastric ulceration, perforation and bleeding
-Prevent GI bleeding: adminster with food or milk. Prophalyxis with proton pump inhibitor for high risk population
- Salicylate Toxicity: high dose ASA -> tinnitus, sweating, headache, dizziness
- Contraindicated: bleeding disorders, anticoagulant drugs, renal impairment, children with viral infection, alcoholic use disorder, allergic reaction (hx of asthma, rhinitis, nasal polyps)
36
1st gen NSAID NON- ASA
- Analgesic
- Anti-inflammatory
-Anti-pyretic
Se: gastric ulceration, bleeding, renal impariment, risk of MI/ Stroke (lower than COX-2)
EX: Ibuprofen, naproxen, diclofenac
- Comes in an IV formulation: ketorolac (Toradol)
37
Prostaglandins keep what dilated
Afferent arteriole
38
IF NSAIDS block dilation?
reduces renal perfusion preventing filtration
39
2nd gen NSAIDs
```
- Only inhibit COX- 2
Analgesic
- Anti-inflammatory
-SE: GI erosion and ulcers, MI/ Stroke risk, renal impairment
-Ex: celecoxib (Celebrex)
```
40
Acetaminophen (tylenol)
- selective inhibition of prostaglandins
- Analgesic
- Anti- pyretic
- No anti- inflammatory action
- Leading cause of liver injury
- Max dose- 4 grams
- Chronic alcohol use - 2 grams
41
Acetaminophen Toxicity antidote
Antidote is Acetylcysteine (Mucomyst) is used to minimize liver damage.
- Best given 8-10 hours (100% recovery) of ingestion.
24 hours still significant effect
42
Multi Modal Therapy
Using flexiril and gabapentin
| - Tens machine
