OPIATES Flashcards
(44 cards)
1
Q
What is the biological response to stimulation of Mu (µ) receptors?
A
- Respiratory depression
- Physical depression
- Tolerance
- Constipation
- Euphoria
- Miosis (primary analgesia response)
2
Q
What is the biological response to stimulation of Kappa receptor?
A
- Spinal cord analgesia and sedation without respiratory depression
- Miosis
3
Q
What is the biological response to stimulation of Sigma receptor?
A
- Vasomotor stimulation
- Psychotomimetic effects
- Miosis
- Binds non-opioid agents
4
Q
What is the biological response to stimulation of Delta receptors?
A
- Enkephalins more selective with Delta receptors in periphery
5
Q
What opioids are the Pure/Strong Agonists? (5) How do they function?
A
Bind to Mu receptors (analgesia without “ceiling effect”)
- Phenanthrenes
- Morphine
- Hydromorphone
- Phenylheptlamines
- Methadone
- Phenylpiperidines
- Meperidine
- Fentanyl (most widely used)
6
Q
How does Morphine function?
A
- Inhibits pain reflexes (via inhibition of neurotransmitter release)
- Inhibit pain transmission
- Modulates pain in spinal cord
7
Q
What are the receptor binding affinities of Morphine?
A
- Mu: Highest
- Kappa: Varies
- Delta: Varies
- Sigma: Lowest
8
Q
What are the ACTIONS of Morphine? (10)
A
- Analgesia (INC pain threshold, alter brain’s perception of pain)
- Euphoria (contentment, well-being)
- Respiratory
- DEC cough reflex (antitussive effects via non-analgesic receptors)
- Miosis (Mu and Kappa; little tolerance observed in addicts)
- Emesis (stimulation of chemoreceptor trigger zone)
- GI
- CV
- Histamine release (Hives, sweating, vasodilation, bronchoconstriction)
- Hormonal actions
9
Q
What are Respiratory-related ACTIONS of Morphine?
A
- Respiratory Depression
- DEC CO2 sensitivity at respiratory center neurons
10
Q
What are GI-related ACTIONS of Morphine?
A
- Relieves diarrhea
- Causes constipation via DEC GI motility, and INC GI tone and anal sphincter
11
Q
What are CV-related ACTIONS of Morphine?
A
- HIGH DOSE: Bradycardia and/or HPOTN
- INC CSF
- Morphine contraindicated w/ Severe brain injury
12
Q
What are HORMONAL ACTIONS of Morphine?
A
- Inhibits release of GRH and CRH
- DEC [LH], [FSH],[ACTH], [ß-endorphin]
- DEC testosterone and cortisol levels
- INC PRL, GH release (via dopaminergic inhibition)
- INC ADH (leads to fluid retention)
13
Q
What are the therapeutic uses for Morphine?
A
- Analgesia
- Diarrhea (RARE)
- Cough (RARE)
14
Q
What are ADRs for Morphine?
A
- Respiratory and circulatory depression
- Constipation
- Sedation
- Dizziness
- HPOTN
- N/V
- Sweating
- Euphoria
- Dysphoria
- Dry mouth (Xerostomia)
- Syncope
- Urinary retention
(Patients w/ renal failure more prone to ADR)
15
Q
What precautions should be considered before administering Morphine? (pre-existing conditions)
A
- Head injuries (INC ICP)
- Acute asthmatic attack
- COPD
- BPH/urethral stricture
- Elderly/neonates
- Compromised BP
16
Q
What are drug interactions with Morphine? (CC)
A
- Co-current use of CNS depressants (e.g. EtOH, Antipsychotic, BZDP)
- Cimetidine: INC serum concentrations
17
Q
What is being monitored with Morphine?
A
- Pain control
- Signs of respiratory/CV depression
18
Q
How does Meperidine function?
A
Antimuscarinic activity (Binds to kappa receptor)
19
Q
What are therapeutic uses for Meperidine?
A
- Post-surgical (spinal analgesia)
20
Q
What are ADRs of Meperidine?
A
- Seizures
- LARGE DOSE
- Renal Failure
- HX seizures
- Long-term use (cancer patients)
- Drug interactions
21
Q
What are the contraindications for Meperidine?
A
- TX MAOI within past 14-21 days
- Patients with CHRONIC PAIN
22
Q
What are the precautions for Meperidine?
A
- Elderly
- HX
- Renal failure
- Hepatic failure
23
Q
What are drug interactions with Meperidine? (MC BP)
A
- MAOI (BP changes, excitatory, rigidity)
- Chlorpromazine
- Barbituates
- Phenytoin (DEC concentration, INC normeperidine)
24
Q
What should be monitored for with Meperidine?
A
- S/Sx jerking or twitching (may indicate normeperidine accumulation)
- Pain score evaluation
25
How does **Methadone** function?
Binds to **Mu** receptor for analgesia effect (substituted for morphine and heroin in controlled withdrawal – **LONG half-life**)
26
What are **ADRs** of **Methadone**?
* **HIGH-****RISK** toxicity (long half-life)
* Withdrawal symptoms
27
What are **drug interactions** of **Methadone**? *(I I)*
* **Inducers**: **DEC** levels and effects
* **Inhibitors**: **INC** levels and effects
28
What should be **monitored** for with **Methadone**?
* **Signs of Withdrawal**:
* Lacrimation
* Rhinorrhea
* Diaphoresis
* Yawning
* Restlessness
* Insomnia
* Dilated Pupils
* **Respriatory Depression**
29
How does **Fentanyl** compare to **Morphine**?
**MORE POTENT** than morphine
30
What are **therapeutic uses** for **Fentanyl**?
* Acute/postoperative pain
* Anesthesia (combination w/ Doperidol)
31
What are **ADRs** of **Fentanyl**?
* NO histamine release (possibly preferred when CV stability is not an issue)
32
What are **drug interactions** with **Fentanyl**? *(CII)*
* **CNS depressants**
* **Inducers** (DEC effects)
* **Inhibitors** (INC effects)
33
What are **contraindications** for **Fentanyl**?
* **Patch** for acute/postoperative pain
* ABUSE
* LACK OF TITRATION
* VARIABLE ABSORPTION
34
What **opioids** are considered **mild/moderate agonists? (5)**
* Phenanthrenes
* **Codeine**
* **Oxycodone**
* **Hydrocodone**
* Phenylpiperidine
* **Diphenoxylate**
* **Loperamide**
35
What are **indications** are considered for **codeine, oxycodone, hydrocodone?**
* **LESS efficacious** than morphine
* TX **w/ ASA, APAP**
36
What are **therapeutic uses** for **diphenoxylate**?
* **Management of diarrhea** (Combo with atropine)
(Limited abuse potential)
37
What are **therapeutic uses** for **Loperamide**?
* **Management of diarrhea**
(Limited abuse potential)
38
What **opioids** are considered **partial agonist/antagonists**? (4)
* Phenanthrenes
* **Nalbuphine**
* **Buprenorphine**
* Morphinans
* **Butorphanol**
* Benzomorphans
* **Pentazocine**
39
How does **Buprenorphine** function?
* Partial Mu agonist
* Analgesia
40
How does **Buprenorphine** compare to **Morphine**?
* **20X MORE POTENT** than Morphine
* Similiar ADRs, but may antagonize respiratory depression caused by Morphine
* Long-acting (effects slower developing)
41
How does **Butorphanol** compare to **Nalbuphine/Buprenorphine**?
* Equivalent analgesic effect
* More sedative (kappa receptor agonist)
42
How does **Pentazocine** function?
* Mild **Mu** and **Kappa** agonist
* Originally developed for analgesic effect with minimal abuse potential
43
What medication considered **opioid antagonists**? (NAME *NN)*
* **Naloxone** (short-acting, precipitates withdrawal in 30 secs, duration 60-100 min)
* **Naltrexone** (long-acting, up to 48 hours)
44
How does **Tramadol** function?
* weak **Mu** agonist
* **Inhibit NE/serotonin reuptake** in CNS
