Term
| What is the MOA of Opioids? |
|
Definition
| *Binding to G-coupled receptors in brain and spinal cord regions involved in the transmission and modulation of pain |
|
|
Term
| What Mu receptors are effected by IV Opioids? |
|
Definition
|
|
Term
| What Mu receptors are effected by epidural and spinal anesthesia? |
|
Definition
|
|
Term
| How is pain transmission effected Pre-synaptically by opioid administration? |
|
Definition
| *Closure of voltage gated Calcium channels in presynaptic nerve terminal |
|
|
Term
How is pain transmission effected Post-synaptically by opioid administration?
|
|
Definition
| *Hyperpolarize by opening potassium channel thus inhibiting postsynaptic neurons |
|
|
Term
| Which has a greater affinity for receptors, agonists or antagonists? |
|
Definition
|
|
Term
| List Phenanthrene Opioids |
|
Definition
*Morpine
*Hydromorphone
*Heroin
*Codeine
*Hydrocodone |
|
|
Term
| Which analgesic has the greatest experience of euphoria? |
|
Definition
|
|
Term
| What is a synthetic phenylheptylamine opioid? |
|
Definition
|
|
Term
|
Definition
*Fentanyl
*Sufentanil
*Remifentanil |
|
|
Term
| What is the pKa of Morphine? |
|
Definition
|
|
Term
| What is the volume of distribution for Morphine? |
|
Definition
|
|
Term
| True or false: Lungs have a large role in metabolism. |
|
Definition
|
|
Term
| What is the mean total plasma clearance of Morphine? |
|
Definition
|
|
Term
| How is morphine metabolized? |
|
Definition
| *Hepatic glucuronidation by cytochrome P450 to Morphine-3-glucuronide (its inactive form). |
|
|
Term
| What is the most common opioid prodrug? |
|
Definition
|
|
Term
| What percent of Morphine is excreted unchanged in the urine? |
|
Definition
|
|
Term
| What is the 1/2 life of Morphine? |
|
Definition
|
|
Term
| How does morphine effect the GI tract? |
|
Definition
| *Increases tone and decreases propulsive contractions of the smooth muscle of the gastrointestinal tract leading to constipation. |
|
|
Term
| What is a large disadvantage of the use of Morphine? |
|
Definition
| *Histamine release resulting in dilation of cutaneous blood vessels, flushing or the face and neck, pruritus and sweating. |
|
|
Term
| How does Neostigmine effect the GI tract? |
|
Definition
| *Increases gastric motility and decreases nausea and vomiting. |
|
|
Term
| What is the onset of Morphine? |
|
Definition
|
|
Term
| What is the duration of Morphine? |
|
Definition
|
|
Term
| What is the % of protein binding in Morphine? |
|
Definition
|
|
Term
| Can protein bound drugs undergo metabolism? |
|
Definition
| *No, only unbound drugs (free) can be metabolized. |
|
|
Term
| What is the bolus dose for epidural morphine? |
|
Definition
|
|
Term
| What is the infusion rate of epidural Morphine? |
|
Definition
|
|
Term
| What is the max dose of epidural Morphine? |
|
Definition
|
|
Term
| What will cause epidural Morphine to "float" up into the epidural space? |
|
Definition
|
|
Term
| What is a disadvantage of epidural Morphine? |
|
Definition
| *Late respiratory depression |
|
|
Term
| What is a technique that can be used to continue epidural analgesia and prevent BP decreasing? |
|
Definition
| *Draw up PF Morphine with sterile water in syringe and inject into epidural space, will spread cephalad and block with out increasing the volume of epidural. |
|
|
Term
|
Definition
| A hydrogenated ketone of morphine |
|
|
Term
| What is the peak of hydromorphone? |
|
Definition
|
|
Term
| What is the duration of hydromorphone? |
|
Definition
|
|
Term
| What % of hydromorphone is protein bound? |
|
Definition
|
|
Term
| What is the half life of hydromorphone? |
|
Definition
|
|
Term
| What is the pH of hydromorphone? |
|
Definition
|
|
Term
| Can hydromorphone be used in the pregnant or nursing mother? |
|
Definition
| *No. It is excreted unchanged in breast milk and is teratogenic. |
|
|
Term
| How is hydromorphone excreted? |
|
Definition
| *Renal system in urine some of which is unchanged |
|
|
Term
| What is the equianalgesic dose of dilaudid to Morphine? |
|
Definition
| *Hydromorhone 1mg=10mg Morphine |
|
|
Term
| What is the bolus dose for an epidural using hydromorphone? |
|
Definition
|
|
Term
| What is the infusion rate for hydromorphone in an epidural? |
|
Definition
|
|
Term
| Does hydromorphone exhibit early or late respiratory depression when used epidurally. Why? |
|
Definition
*Early respiratory depression
*Lipid soluble |
|
|
Term
| What is the perception of pain at a higher intensity than normal? |
|
Definition
|
|
Term
| What is the most rapidly acting of the opiates? |
|
Definition
|
|
Term
| What is the chemical name for Heroin? |
|
Definition
|
|
Term
| If _________ groups are removed, Heroin becomes morphine. |
|
Definition
|
|
Term
| What is the duration of Euphoria with Heroin both IV and IM? |
|
Definition
*IV 7-8 seconds
*IM 5-8 minutes |
|
|
Term
| What is a major problem associated with Heroin both anesthetically and physiologically? |
|
Definition
*Infection of the heart lining and valves
*Tolerance to the drug develops along with other anesthesia drugs. |
|
|
Term
| What receptors does Heroin work on most which are responsible for physical dependency and euphoria? |
|
Definition
|
|
Term
| What is the peak for Heroin withdrawal? |
|
Definition
|
|
Term
| What is the most effective orally administered analgesic? |
|
Definition
|
|
Term
| What % of strength of Morphine is Codeine? |
|
Definition
|
|
Term
| Codeine is a ________ in which 5-10 is converted into Morphine |
|
Definition
|
|
Term
| After Codeine is metabolized into an active form, what is the ceiling effect? |
|
Definition
|
|
Term
| How is codeine converted into Morphine? |
|
Definition
|
|
Term
| What enzyme can be lacking and prevent conversion of Codeine to Morphine? |
|
Definition
|
|
Term
| What is the dose of Codeine in males and females? |
|
Definition
*7mg per 1 kg males
*6mg per 1kg in females |
|
|
Term
| What other than an analgesic can be codeine be used for? |
|
Definition
|
|
Term
| What drugs inhibit the breakdown of CYP2D6 and thus potentiate the effects of Codeine? |
|
Definition
*SSRI (Paxil, Prozac)
*Wellbutrin
*Dexamethasone
*Rifampicin |
|
|
Term
|
Definition
*A semi-synthetic opioid derived from two of the naturally occurring opiates codeine and thebaine.
*An orally active narcotic analgesic and antitussive mixed with acetaminophen. |
|
|
Term
| Can hydrocodone be given to the parturiant? |
|
Definition
|
|
Term
| What is a disadvantage to Hydrocodone? |
|
Definition
| *Habit-forming, which leads to physical and psychological addiction. |
|
|
Term
| What does the combination of Hydrocodone offer? |
|
Definition
*Twofold: To provide increased analgesia via drug synergy
*To limit the intake of hydrocodone. |
|
|
Term
| What is the most frequent opioid prescribed? |
|
Definition
| *Hydrocodone 5/500 or 7.5/500 |
|
|
Term
|
Definition
*Synthetic opioid, analgesic and antitussive
*Maintenance anti-addictive for use in patients on opioids |
|
|
Term
| What is Methadone approved for? |
|
Definition
| *Approved only for the treatment of opioid dependence. Soft analog form racemic hydrochloride is only type available in US. |
|
|
Term
| Where does Methadone exert its action? |
|
Definition
| *At the Mu-opioid receptor some affinity for the NMDA ionotropic glutamate receptor (acts as a receptor antagonist against glutamate) |
|
|
Term
| What is the half life of Methadone? |
|
Definition
*15-60 hours
*Analgesic activity is shorter than the pharmacological half life. |
|
|
Term
| What other special uses can Methadone be utilized for? |
|
Definition
*Can be given to pregnant women addicted to heroin
*Analgesic in chronic pain patient with tolerance
*Can be utilized for a drug holiday for chronic pain patients to increase effectiveness of mainstay drug. |
|
|
Term
| What is a major disadvantage to Methadone administration? |
|
Definition
| *Patient is hyperanalgesic for life |
|
|
Term
|
Definition
*Synthetic primary Mu-Opioid agonist commonly used to treat intra-operative and chronic breakthrough pain.
*100 times more potent than morphine (100 mcg of Fentanyl equivalent to 10mg of morphine) |
|
|
Term
| How much of Fentanyl is protein bound? |
|
Definition
|
|
Term
| How is Fentanyl metabolized? |
|
Definition
| *Hepatic primarily by CYP3A4 |
|
|
Term
| What is the half life of Fentanyl? |
|
Definition
|
|
Term
| How is Fentanyl excreted? |
|
Definition
| *60% Urinary (metabolites, <10% unchanged drug) |
|
|
Term
| Fentanyl is the chemical basis/root for which two drugs? |
|
Definition
| *Sufentanil and Remifentanil |
|
|
Term
|
Definition
| *Powerful synthetic opioid approximately 5-10 times more potent than its analog, fentanyl |
|
|
Term
| What is the dose at which Sufentanil produces hypnosis and anesthesia without the use of additional anesthetic agents? |
|
Definition
|
|
Term
| What dose of Sufentanil attenuates the sympathetic response to surgical stress? |
|
Definition
|
|
Term
| At which dose is the catecholamine response, particularly NE, further attenuated with hemodynamic stability and preservation of myocardial oxygen balance. |
|
Definition
|
|
Term
| ____________ maintains CO with a slight reduction in SVR during the initial post-op period. |
|
Definition
|
|
Term
| What is the alpha or the initial onset of sufentanil? |
|
Definition
|
|
Term
| What is the redistribution for Sufentanil? |
|
Definition
|
|
Term
| What is the half life for sufentanil? |
|
Definition
|
|
Term
| How much of sufentanil is protein bound by AAG? |
|
Definition
|
|
Term
| Respiratory depression, bradycardia, and hypotension may be more profound with _____________ compared to fentanyl |
|
Definition
|
|
Term
|
Definition
| *Potent ultra short-acting synthetic opioid analgesic drug |
|
|
Term
| What is the dose range for Remifentanil? |
|
Definition
|
|
Term
| What is the half life of remifentanil? |
|
Definition
|
|
Term
| How much of remifentanil is protein bound? |
|
Definition
|
|
Term
| How is Remifentanil metabolized? |
|
Definition
| *Unlike other synthetic opioids which are hepatically metabolized, remifentanil has an ester linkage which undergoes rapid hydrolysis by non-specific tissue and plasma esterases. |
|
|
Term
| What should be done prior to d/c of remifentanil? |
|
Definition
| *Administration of an analgesic 20 minutes prior to turning off infusion. |
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