Term
| What is a common combination to treat "neuroleptic analgesia"? |
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Definition
Droperidol: fentanyl
(anti-dopamine: synthetic opioid) |
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Term
The following describes this specific analgesic:
-shorter acting rel to morphine
-less spasm of smooth muscles
increased vulnerability to seizures, inhibition of cytochrome P450 metabolism of many drugs
-NEVER use by patient-controlled analgesia
-POOR CHOICE |
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Definition
Meperidine
(Totally synthetic opiate drug) |
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Term
The following describes this specific analgesic:
-use for postoperative pain, severe pain
-injection routes main use
-oral bioavailability can be erratic
-good choice for patient-controlled analgesia |
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Definition
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Term
| Name 3 Mixed opioid receptor agonists (kappa agonist, partial mu agonist) |
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Definition
Pentazocine
Nalbuphine
Butorphanol |
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Term
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Definition
Buprenorphine
(ceiling effect due to partial agonist properties) |
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Term
The following describes this specific analgesic:
-ultra long acting: constant levels over 24h
-very low abuse liability if taken orally
-increased use for chronic pain
-treatment of choice for opiate addicts
-Cheap
-Overdose hazard: patient must be educated about long half life! |
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Definition
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Term
The following describes this specific analgesic:
-low efficacy
-good for cough suppression
-used in combination w acetaminophen to permit lower dose of both
-POOR CHOICE |
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Definition
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Term
The following describes these 2 specific analgesics:
-higher efficacy than codeine
-combination w acetaminophen permits lower dose of both
-used as sustained release: have become a popular drug of abuse |
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Definition
Oxycodone, hydrocodone
(semisynthetic narcotics)
- oxycodone somewhat more efficacious of the two |
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Term
The following describes this specific analgesic:
-very lipophilic, ultrashort acting
-ideal for preanesthetic medication
-must be given IV
-problems: high muscle rigidity, high abuse potential |
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Definition
Fentanyl, sufentanil etc
-fentanyl is available as a transdermal patch, or tansmucosal for prolonged treatment: less abuse liability
-do not use in acute pain, in opiate-naive, burns, fever |
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Term
-poor choice as analgesic because kappa effects are dysphoric
-useful for addicts |
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Definition
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Term
| Poor choice of analgesic because no better than aspirin |
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Definition
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Term
| High efficacy opiates for Analgesia |
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Definition
Methadone (V long- 24h)
Hydromorphone (Medium to Long)
Morphine (Medium)
Levophanol (Medium)
Meperidine (Short; poor choice due to side effects) |
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Term
| High efficacy, Lipophilic opiates for Analgesia, Pre-anesthetic medication (ultrashort duration of action) |
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Definition
Fentanyl (IV)
Sufentanil
Alfentanil
Remifentanil |
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Term
| Moderate and Low Efficacy opiates for analgesia |
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Definition
Oxycodone
Hydrocodone
Codeine, Dihydrocodeine
Propoxyphene |
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Term
| Name three very lipophilic (and hence rapid onset of action) Opiate ANTAGONISTS. |
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Definition
Naloxone, Naltrexone, Methylnaltrexone
Naloxone: useful for overdose
Naltrexone: alcohol treatment, maintain detoxification
Methylnaltrexone Alvimopan: peripherally active mu antagonists, useful to counteract constipating effect of analgesic opioids |
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Term
| Use this narcotic for cough (name 2) |
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Definition
Codeine
-do not use chronically or in the presence of cough of unknown etiology
Dextromethorphan
-available OTC
-weak agonist but may not act through opiate receptors but via unique mechanism |
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Term
| Via what mechanisms do opiates treat Diarrhea? |
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Definition
-antisecretory (increase water reabsorption)
-decrease motility via constriction of circular muscle |
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Term
| Name 3 opiates used for treating diarrhea |
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Definition
Loperamide
Dephenoxylate
Acetorphan (Racecadotril)
(use drugs that do not cross bbb)
-Loperamide is better than morphine, doesn't get into brain
Dephenoxylate and its metabolite difenoxin: have some CNS activity, marketed in combi w atropine
Acetorphan (Racecadotril): prodrug for enkephalinase inhibitor Thiorphan- useful mainly in infants |
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Term
| Treat opiate overdose with: |
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Definition
Naloxone
-opiate antagonist that is very lipophilic (fast onset) and short acting
-breathing restored in minutes |
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Term
| Treatment for opiate withdrawal |
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Definition
Clonidine (alpha 2 agonist - to decrease NE hyperactivity)
-mu receptor activity normally inhibits NE neurons (NE hyperactivity causes withdrawal symptoms)
-alpha 2 agonist targets autoreceptors on NE neurons to decrease NE release |
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Term
Replacement strategies for opiate addictions:
1) ____________: long half life mu agonist provided orally only at approved clinics
2) ________: partial mu agonist/kappa antagonist - can be prescribed after approved training as an outpatient drug |
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Definition
1) methadone
2) Buprenorphine
-Suboxone: 4:1 buprenorphine: naloxone to prevent abuse
-subutex |
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