Opioids Flashcards
Theraputic uses of morphine? how does it relieve pain? what kind of pain is it most effective against?
relieves pain without effecting other seneses and without loss of consciousness
-Relive pain by mimicking the actions of endogenous opioid peptides, primarily at mu receptors
-Most effective against dull, constant pain rather than sharp interminant pain (sharp pain can be relived in large doses)
What is codeine widely used for?
Used widely as a cough suppressant and for pain
How do Nonopioid Centrally Acting Analgesics work?
○ Relieve pain by mechanisms largely or completely unrelated to opioid receptors
○ Do not cause respiratory depression, physical dependence, or abuse
○ Not regulated under the Controlled Substances Act
○ E.g. Tramadol [Ultram] - Suicide risk
○ Clonidine [Duraclon]
○ Ziconotide [Prialt]
○ Dexmedetomidine [Precedex]
Effects of activation of K Kappa receptors? What kind of effects do opioids have on on these receptors
Just like with Mu recpetors analgesia and sedation, kappa activation may underline psychomimecic effects seen with certain opioids
weak effects from opioids
What is codeine converted into? Roughly how much?
Converted into low dose of morphine in the body (roughly 10%)
Pharmacological effects of morphine? (what effects does it cause)
analegisa, sedation, euphoria, respiratory depression, cough supression and supression of bowel motiltiy
What is Neuropathic pain? What does it result from?
_Defined as “pain induced by injury to or disease of the somatosensory system”
Resulting from nerve injury or infections of the nervous system
How do local and general ANESTHETICs block pain?
Local anaesthetic: blocks nerve conductionand all local sensations (including pain)
General anaesthetics: cause loss of sensations and unconsciousness
What does Chronic Pain treatment require?
equires fixed schedule around-the-clock (ATC) treatment
opioids
NSAIDs
adjuvants
What is Hydrocodone? What is it combined with?
■ Most widely prescribed drug in the United States
■ Combined with aspirin, acetaminophen, or ibuprofen
What clinical uses of Opioids must we bear in mind?
○ Physical dependence
■ State in which an abstinence syndrome will occur if the dependence-producing drug is abruptly withdrawn; it is NOT equated with addiction
○ Abuse
■ Drug use that is inconsistent with medical or social norms
○ Addiction
■ Behavior pattern characterized by continued use of a psychoactive substance despite physical, psychologic, or social harm
○ Balance the need to provide pain relief with the desire to minimize abuse
○ Minimize fears about the following:
■ Physical dependence
■ Addiction
What is Oxycodone?
■ Analgesic actions equivalent to those of codeine
■ Long-acting analgesics
● Immediate-release
● Controlled-release [OxyContin]
○ Abuse: Crushes and snorts or injects medication
○ 2010 OP formulation much harder to crush and does not dissolve into an injectable solution to decrease risk of abuse
What receptor does morphine primarily act on?
primarily on mu (m) opioid receptors
brain and spinal cord
When does physical dependance to morphine start? what kind of symptoms does it present as?
■ Abstinence syndrome with abrupt discontinuation
■ About 10 hours after last dose, the initial reaction occurs and includes yawning, rhinorrhea, and sweating
■ Progresses to violent sneezing, weakness, nausea, vomiting, diarrhea, abdominal cramps, bone and muscle pain, muscle spasms, and kicking movements
■ Lasts 7 to 10 days if untreated
Adverse effects of morphine?
*Respiratory depression (most serious)
-Constipation (through actions in the CNS and gastrational tract (specifically by activating MU receptors in the gut)
-Orthostatic hypotension:lower blood pressure by blunting the baroreceptor reflex and by dilating peripheral arterioles and veins
Urinary retention and hesitancy: ■ Increases tone in the bladder sphincter
Cough suppression
Biliary colic: Induces spasm of the common bile duct
Emesis: Promotes nausea and vomiting through the direct stimulation of the chemoreceptor trigger zone of the medulla
Elevation of intracranial pressure: As a result of suppressed respirations, morphine increases the carbon dioxide content of blood, which dilates the cerebral vasculature and causes intracranial pressure to rise
Sedation: Drowsiness and some mental clouding
Euporia and dysphoria: Euphoria: An exaggerated sense of well-being caused by the activation of mu receptors
-Dysphoria: A sense of anxiety and unease
What is tramadol? What is it used for? Adverse effects? drug interactions we need to bear in mind?
It is a moderately strong analgesic with a low potential for dependance, abuse or respiratory depression
-Tramadol is an analog od codeine that relives pain in part through weak agonist activity of Mu opioid receptors by blocking uptake or serotonin and noerpeinephrine
-Approved for moderate to moderately severe pain and the drug is less effective than morphine and no more effective than codeine combined with aspirin
Most common adverse effects is sedation, dizziness, headache, dry mouth and consipation, seizures have been reported (not to be given with epoxy or neurologic disorder patients)
-Not to be coined with other CNS depresants (can intensify drug responses)
-Can cause suicide
What ways can Fentanyl be administered>
● Parenteral
○ Surgical anesthesia
● Transdermal [Duragesic®]
○ Patch: Heat acceleration
● Transmucosal
○ Lozenge on a stick [Actiq®]
○ Buccal film [Onsolis®]
○ Buccal tablets [Fentora®]
○ Sublingual tablets [Abstral®]
○ Sublingual spray [Subsys®]
