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Opiate agonist medication
Morphine Sulfate
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What receptors of the CNS do opiate drugs act on?
Mu and Kappa, mostly Mu
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What range on the pain scale dictates giving morphine?
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What are three indications for using morphine?
- Pain of 4-10
- Dyspnea associated with left ventricular failure and pulmonary edema
- Pre-op to decrease anxiety and induce sedation
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What routes can morphine be administered?
oral, IV, Epidural
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Is morphine easily lipid soluble? How does this affect crossing the blood/brain barrier?
Morphine is not very lipid soluble so not much actually reaches the Mu receptors.
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Why is the oral does of morphine so much larger than the IV dose? What is the ratio?
Morphine has a huge first past effect, only about 30% reaches systemic circulation. The ration is 30mg (oral) to 10mg (IV).
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What are two adverse side effects of morphine that where tolerance DOES NOT occur?
Constipation and miosis
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What are some side of effects of morphine that where tolerance DOES occur?
- Respiratory depression
- Euphoria
- Sedation
- (along with orthostatic hypotension, cough suppression, and urinary retention)
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What is a good indication that someone has not been taking the morphine they were prescribed? Why?
If they are taking their morphine they should have miosis because tolerance does not occur.
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What is the best dosing schedule for morphine? What is the worst?
Continuous is best, then fixed, then PRN
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What is the ceiling on morphine?
There is no ceiling, more drug = more effect
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Describe symptoms of physical dependence on morphine. Why would we see these symptoms?
Abrupt discontinuance of morphine can result in symptoms such as yawning, rhinorrhea, diaphoresis. Later symptoms include anorexia, irritibility and gooseflesh. Peak symptoms include sneezing, cramping, and muscle spasms.
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Is physical dependence on morphine an addiction?
No, there is addiction because there usually is not an psychological dependence on it.
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What opioid antagonist is used to reverse a morphine overdose? What is the dose?
- Naloxone (Narcan)
- Draw up 0.4 mg in 10cc syringe with 9 cc saline. Administer 1 cc over 1-2 minutes. Stop when pain is reported
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How do cyclooxygenase inhibitors work?
Cyclooxygenase inhibitors work by blocking the conversion of arachidonic acid to prostaglandins.
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What is the general role of COX?
COX is an enzyme responsible for producing prostaglandins.
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What does COX-1 do?
- Protects gastric mucosa
- Stimulates platelet aggregation
- Maintain renal blood flow
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What does COX-2 cause?
Inflammation, pain, fever
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What are effects of COX-1 inhibition?
Gastric erosion, bleeding, renal impairment
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What are effects of COX-2 inhibition?
Reduced fever, pain and inflammation
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Is aspirin selective of non-selective? What are some adverse effects? How is bleeding affected?
- Aspirin is non-selective. Adverse effects include gastric upset, ulcers and bleeding. Bleeding time, which is normally 7 minutes, can double when you are on aspirin.
- Renal impairment can also occur.
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If a person is having surgery, when should they stop taking aspirin?
7 days before surgery because it stays in the system a long time as it can attach to different tissues.
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Who should never take aspirin?
Pregnant women, it will fuck up the baby.
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What drugs should NOT be taken with aspirin?
Warfarin (coumadin), glucocorticoids, ibuprofen and alcohol
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Is Ibuprofen selective or non selective?
non-selective
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What is the primary indication for ibuprofen? Is it better or worse for dysmenorrhea than aspirin?
- Arthritis
- more effective for dysmenorrhea than aspirin
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Are ibuprofen, celebrex and acetaminophen good for preventing thrombotic events?
No
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What is a benefit of celebrex over ibuprofen and aspirin?
It is selective for COX-2, so the risk for bleeding is reduced as it does not inhibit platelet aggregation.
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Is acetaminophen an NSAID?
NO
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What is the preferred analgesic for children?
Acetaminophen
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How does excessively large doses of acetaminophen cause liver damage?
toxic accumulation of metabolites resulting in hepatotoxicity
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What are two types of analgesics?
opioids and cyclooxygenase
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What are adjuvant analgesics used for? What type of pain is it for?
Used to complement analgesics. Efficacy in neuropathic pain characterized as sharp, shooting or burning pain.
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List four adjuvant analgesics.
Tricyclic antidepressants, anticonvulsants, corticosteroids and local anesthetics
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How does lidocaine work?
Blocks sodium channels in axon membrane which blocks nerve conduction.
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What types of neurons are affected by lidocaine?
Sensory and motor neurons
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What is onset and termination of anesthesia determined by?
Molecular size and lipid solubility and degree of ionization.
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What characteristics are necessary for a quick onset and short duration of anesthesia?
Small molecule size, high lipid solubility and low ionization
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How does blood flow affect the effects of anesthesia?
Greater blood flow = short duration on effect
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What are effects of anesthesia on the heart?
bradycardia, heart block, reduced contractility, hypotension
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What are two major nursing implication of anesthesia?
Monitor vitals and LOC
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What drug alters the effect of lidocaine? How?
Epi, it is a vasoconstrictor and prolongs the effect
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What neurons does lidocaine affect?
Sensory and motor
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What are TCAs? How are they used with pain reduction?
Tricyclic antidepressants; used as adjuvant analgesics.
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When does the onset of TCAs occur? When does the maximum affect occur?
Onset of TCAs is 1-2 weeks; maximum effect is 4-6 weeks
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What are some side effects of TCAs? Why can people not take them for long?
hypotension, sedation and anticholinergic effects. The anti-cholinergic effects include constipation, so they cannot be taken over a long period of time.
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Anticonvulsant drug
Gabapentin (Neurontin)
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What is the name of a lidocaine patch?
Lidoderm
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