45 - Opioid analgesics and antagonists Flashcards
Opioid with the shortest half life
Remifentanil (3-4 mins)
Opioid with the longest half life
Buprenorphine (4-8 hours)
Receptor that inhibits respiration
Mu (Mabagal Huminga)
Receptor involved in development of tolerance
Delta (Tolerance)
Receptor involved in slowed GI transit
Kappa (Konstipation)
Most potent opioid (80000x more potent that morphine)
Ohmefentanyl
Opioid of choice for pain relief in pancreatitis and biliary colic
Meperidine
- Full Opioid Agonist Acts on Mu receptors
- Drug for moderate to severe pain, Opioid dependence, opioid withdrawal
- Used in methadone Maintenance Therapy (MMT) for dependence
- Currently being investigated as a novel treatment for leukemia
Methadone
- Partial Opioid Agonist Acts on Mu and Kappa receptors
- Drug for Mod to Severe pain, Cancer pain, Neuropathic pain, Chronic pain
- SE: Hypogonadism, hearing loss
Hydrocodone
- Partial Opioid Agonist
- Decreases sensitivity of cough receptors through sigma receptor stimulation
- Drug for cough
- SE: Addiction liability
- What is the adverse effect when combined with SSRIs of MAOIs?
- Dextrometorphan
- Serotonin syndrome
- Weak Opioid Agonist Acts on Mu receptors
- Drug for mild to moderate pain, restless legs syndrome, opioid withdrawal
- SE: Seizures, pulmo edema, fatal arrhythmia
- WITHDRAWN due to fatal cardiotoxicity
- Used in suicides
Propoxyphene
- Mixed Opioid Agonist - Antagonist
- Strong Kappa agonist
- Weak Mu antagonist
- Drug for Moderate to severe pain, opioid dependence, alcohol dependence, balanced anesthesia
- SE: Sedation, dizziness
- Resistant to naloxone reversal
Nalbuphine (Buprenorphine, Butorphanol, Pentazocine)
Opioids that can reduce craving in alcohol dependence
Buprenorphine
- Systemic opioid antagonist
- Blocks, mu, kappa and delta
- Drug for opioid overdose
- Precipitates abstinence syndrome in patients with opioid dependence
Naloxone
- Dual acting opioid analgesic
- Weak agonist at mu receptor, inhibits neuronal reuptake of serotonin and NE
- Drug for mod pain, chronic pain syndromes, neuropathic pain, fibromyalgia
- SE: Seizures (lowers seizure threshold)
- Contraindicated in patients with epilepsy
- What is the adverse effect when this is used with SSRIs?
Tramadol (Tapentadol)
Serotonin syndrome
Triad of Opioid Overdose
- Pupilary Constriction
- Comatose State
- Respiratory Depression
PCR
How do you confirm opioid overdose pharmacologically?
IV injection of Naloxone results in recovery
Analgesic of choice for MI due to reduction in preload
Morphine
Full Opioid Agonist, nonselective
Acts on Mu receptors
SE: Pruritus
Exerts hemodynamic effects on pulmonary circulation
Morphine
- Full Opioid Agonist Acts on Mu receptors; Drug for chronic pain, breakthrough cancer pain:
- Methods of administration: (2)
- Fentanyl
- May be given transdermally or via lollipop
Full Opioid Agonist Acts on Mu and Kappa receptors; Muscarinic blocking actions; Drug for moderate to severe pain, spasmodic pain (biliary, renal), preop sedation, antiemetic
Meperidine
The only opiod that DOES NOT CAUSE MIOSIS or biliary spasm
Meperidine
Metabolite of Meperidine that decreases seizure threshold
Normeperidine
adverse effect of meperidine when given with MAOi:
hyperpyrexic coma
