Pharmacology
This type of ligand binds to receptors, activates G proteins, decreases adenylate cyclase activity, reduces voltage-gated calcium channel conductance, increases potassium channel conductance, and results in the hyperpolarization of neurons, ultimately decreasing neuronal activity.
What is Opioids
What are the bolus and infusion doses of fentanyl?
Bolus: 1-2 mcg/kg/dose for analgesia
Infusion: 1-3 mcg/kg/hr
These opioids can cause dermatologic side effects such as urticaria and erythema at the injection site due to their ability to release histamine and dilate cutaneous vessels.
What are morphine and meperidine?
This opioid stands out for its unique elimination characteristics, with a rapid metabolism by nonspecific esterases in blood and tissues, leading to a context-sensitive half-time that is independent of the duration of infusion, making it ideal for short procedures where rapid recovery is desired.
What is Remifentanil??
What medications do you have to worry about serotonin syndrome with?
What is Meperidine, and fentanyl
The principle sight of action in the brain that triggers onset of opioid withdrawal syndrome is?
What is the Locus Ceruleus at the base of the brain.
What is the normal dose for Naloxone administration, and what is the continuous infusion rate?
Dose: 1-4 mcg/kg IV
Continuous infusion: 5 mcg/kg/hr
What are two common gastrointestinal side effects of opioids?
What are constipation and delayed gastric emptying.
This opioid's metabolism varies among individuals, primarily hepatic via CYP450 with no active metabolites, and it is eliminated through redistribution to fat, with a notable 10% excreted in urine and a half-life ranging from 15 to 60 hours.
What is methadone?
This opioid, known for causing less histamine release compared to morphine, requires consideration for potential CNS and respiratory depression interactions with MAOIs, alcohol, beta-blockers, and antihistamines, with large doses possibly leading to agitation and myoclonus.
What is hydromorphone?
This synthetic opioid agonist acts on µ (analgesia) and Κ (shivering) receptors, has a phenylpiperidine derivative structure, and shares similarities with local anesthetics and atropine, including the ability to penetrate the blood-brain barrier.
What is Meperidine
What is the bolus and infusion doses of Sufentanil?
Bolus: 0.1 mcg/kg
Infusion- 0.2- 0.8 mcg/kg/hr
What cardiovascular effects can opioids have (4), and how do they contribute to myocardial protection?
What are hypotension, orthostatic hypotension, bradycardia, and histamine release. Opioids enhance resistance of the myocardium to oxidative and ischemic stress, providing protection.
This opioid undergoes hepatic metabolism, including conjugation with glucuronic acid and demethylation via CYP450, producing inactive and active metabolites, with the active metabolite having a higher analgesic potency and longer duration than the parent compound.
What is Morphine?
This type of opioid administration leads to profound analgesia by directly interacting with µ opioid receptors in the spinal cord, while another type involves systemic absorption via an extensive venous plexus, with cephalad movement in the CSF depending on lipid solubility, potentially causing early or late respiratory depression.
What are intrathecal and epidural opioid administrations?
Which opioid, prized for its swift onset and peak effect in anesthesia, poses challenges due to its brief duration, requiring careful management of pain during prolonged procedures and titration adjustments for extended infusions?
What is Fentanyl?
What are the IV and IM doses of meperidine?
IV: 12.5-25mg
IM: 50-100mg
These opioids can decrease cerebral blood flow, induce EEG changes consistent with sleep, cause miosis, and lead to rigidity of the chest wall, especially with rapid administration of large doses, which can result in laryngeal musculature contraction. Sedation, occurring in up to 60% of patients receiving this opioid, precedes the onset of analgesia.
What are the CNS effects associated with opioids like morphine and meperidine?
How is codeine different from morphine in how it's absorbed and metabolized, and what should be considered when giving it to breastfeeding mothers?
broken down in the liver, and about 10% of it turns into morphine, which helps with pain. Risk of it getting into breast milk, so it should be used with caution in breastfeeding moms.
This opioid, known for its longer analgesic effect and reduced respiratory depression compared to fentanyl, is recommended to be stopped 30-40 minutes before extubation to maintain analgesia while minimizing respiratory depression.
What is Sufentanil?
What opioid medication is a partial agonist at the mu receptor and a full antagonist at the kappa receptor, responsible for reducing euphoria and tolerance, but poses risks of discomfort, relapse, and overdose if abruptly stopped in patients with substance abuse disorders?
What is Buprenorphine
A patient requires opioid analgesia, and you need to choose between codeine, hydrocodone, and oxycodone. If codeine is dosed at 60 mg, hydrocodone at 7.5 mg, and oxycodone at 5 mg, which medication provides the highest opioid dose?
Hydrocodone provides the highest opioid dose at 7.5 mg, followed by oxycodone at 5 mg, and then codeine at 60 mg.
How do opioids affect respiratory response to CO2, and what regions of the brain are involved in respiratory depression?
Opioids decrease the response to CO2, leading to an increased PaCO2 and a right shift of the CO2 response curve. primarily affecting the pontine and medullary respiratory centers.
Which opioid undergoes hepatic demethylation to produce an active metabolite that can cause CNS stimulation and myoclonus, and is associated with a decreased seizure threshold?
What is Meperidine?
What opioid has pharmacokinetics that are similar in obese and lean patients, remains unchanged in renal or liver failure patients, allows for quick recovery in neurologic assessment, direct laryngoscopy, and labor pain, and is associated with context-sensitive half-time, which is independent of the duration of infusion?
What is Remifentanil?