Reading...
Play button
Play button
Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
34 Cards in this Set
- Front
- Back
|
Pro-Opiomelanocortin (POMC)
|
Protein precursor to endogenous opioid:
β-Endorphin and also - ACTH (Glucocorticoids) - MSH (Melanin) |
|
|
Pro-Enkephalin
|
Protein precursor to endogenous opioids:
1) Met-Enkephalin* 2) Leu-Enkephalin** * the 1st 5 aa of β-End ** the 1st 5 aa of Dynorphins |
|
|
Pro-Dynorphin
|
Protein precursor to endogenous opioids:
1) Dynorphins 2) Leu-Enkephalin |
|
|
μ1 Receptor
|
Opioid Receptor
Effects: - Analgesia - Euphoria - Physical dependence Endogenous ligands: Endomorphins & β-Endorphins |
|
|
μ2 Receptor
|
Opioid Receptor
Effects - Respiratory depression - Bradycardia Endogenous ligands: Endomorphins & β-Endorphins |
|
|
Naloxone
|
Opioid Receptor Antagonist
Reverses effects of Overdose/toxicity (used in the emergency scenario) - Rapid Reversal, Short acting * May require repeated administrations |
|
|
κ Receptor (1,2,3)
|
Opioid Receptor
Effects: - Miosis - Sedation - Spinal Analgesia Endogenous ligands: Dynorphins |
|
|
Σ Receptor
|
Not an opiod receptor
Effects: - Dysphoria - Mydriasis - Hallucinations |
|
|
Δ Receptor (1&2)
|
Opioid Receptor
Effects: - Spinal Analgesia - ↓ Respiratory Rate * Does not produce Euphoria or Bradycardia Endogenous ligands: Met & Leu-Enkephalins |
|
|
Somatosensory Cortex
|
Morphine blocks sensory-discriminative effect of pain
|
|
|
Limbic Cortex
|
Morphine blocks the emotional components of pain
|
|
|
Periaquaductal grey region
|
Morphine blocks ascending pain resources
|
|
|
Dorsal horn
|
Morphine blocks release of nocieptive transmitters in spinal dorsal horn
|
|
|
Clinical Signs of Opiate Over-dose
|
- Coma
- Miosis - Respiratory depression - Decreased blood pressure - Decreased body Temp - Convulsions with some opiates |
|
|
Treatment of Opiate Overdose
|
1) Naloxone
2) Ventilate 3) Drugs to control Hypotension |
|
|
Methadone
|
Maintenance of Opiate Abstinence
Abstinence - An opiod - Long Acting* μ agonist - Orally Active *The faster the onset & faster the offset, the more abusable the drug |
|
|
Clonidine
|
Maintenance of Opiate Abstinence
- α2 agonist: ↓ SNS effects of opiate withdrawl |
|
|
Naltrexone
|
Maintenance of Opiate Abstinence
- Not for the emergency room setting - Very Long acting - Slow onset |
|
|
Buprenorphine
|
Mixed agonist/antagonist
Maintenance of Opiate Abstinence - First-line Drug to treat abstinence - Blocks self-administration - Low abuse potential - Mild physical dependence |
|
|
Withdrawal from Opiods
|
1) "Flu-like" symptoms
2) Emesis (vomiting) 3) Diarrhea 4) Chills |
|
|
Morphine & Hydromorphone
|
Use: Severe pain
Duration: 4-5hrs - Drug of choice for pain associated w/ MI - Steroids use must be halted for 2wks prior to catheter insertion to prevent infection, b/c ↑ immunosuppressive effects of the steroids - It's analgesic active metabolite ____-6-glucuronide can build up with inadequate renal fx ---> respiratory depression |
|
|
Kadian
|
Time-released Morphine
|
|
|
Exalgo
|
Extended-release formulation of hydromorphone (morphine derivative)
Use: Opiod tolerant patients only - Fatal respiratory depression could occur in patients not opiod tolerant |
|
|
Herion
|
- Very fast onset: drug of abuse
- Cosses the BBB and metabolized to morphine - Not accepted medically in the USA 3x potent as morphine (faster onset) |
|
|
Codeine
|
- pro-drug: ~ 10% metabolized to morphine (so it is a weak analgesic)
- combined with acetominophen to ↑ pain relief and ↓ amt of opiate used (Tylenol #3) - Anti-tussive Use: mild to moderate pain |
|
|
Meperidine
|
Morphine derivative
- 8-10x less potent than morphine - Rapid onset/offset - Toxicity: Tremors/convulsions due to its active metabolite nor_____, proconvulsant and hallucinogenic agent |
|
|
Fentanyl, Sufentanil, Alfentanil, Remifentanyl
|
Used as adjuncts to anesthesia
- More potent than morphine - Fast acting & Fast clearing from blood - Lipid soluble (trapped in fat) - Dosage determined by lean body mass - Available for analgesia in chronic pain and post-surgical patients |
|
|
Propoxyphene
|
Highly toxic when combined with alcohol or other sedatives. Death can occur w/in 20min-1hr
Use: mild to moderate pain |
|
|
Oxycodone
|
- Combined with Acetaminophen = Percocet
- Combined with Aspirin = percodan Binds mainily to κ & μ receptors = analgesia Use: mild to moderate pain |
|
|
OxyContin
|
Time released oxycodone
Use: indicated for around-the-clock management of moderate to severe pain *Designed for opioid tolerant patients (cancer patients) |
|
|
Hydrocodone
|
Semi-synthetic opiod derived from codeine and thebaine
Use: analgesic and antitussive *Most frequently used acetaminophen containing prescription |
|
|
Tramadol
|
Dual action analgesic
1) Partial μ agonist 2) blocks presynaptic uptake of NE and Serotonin - It's 1st metabolite is as active and a potent analgesic: mono-demethyl____ ↑ toxicity when combined with serotonin type anti-depressants |
|
|
Pentazocine
|
Mixed agonist/antagonist
Analgesia Uses: κ & Σ receptors *Combination with antihistamine is know to drug abusers as "T's and Blues", more man's heroin |
|
|
Talwin NX
|
Mixed agonist/antagonist
Pentazocine with naloxone - ↓ liability of drug when injected in drug abuse situations, but when given orally nalone is not active and does not block analgesic effects of Talwin |
