Term
example of full agonist of opioids
partial
and
full antagonist |
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Definition
full agonist: morphine
partial agonist: codeine M-opioid receptor
full antagonist: naloxone works on m-opioids receptor |
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Term
| wht are 3 major receptors families? where are they located? |
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Definition
μ (mu), κ (kappa), and δ (delta), each has different specificity
Located on membranes of certain cells in the CNS, on nerve terminals in PNS, and on cells of the GI tract and other regions. |
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Term
| MAO of opioids its bunch so read it from the ppt |
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Definition
Action potentials reaching the dorsal horn can be attenuated at the presynaptic ending by opioids
Opioids also inhibit the postsynaptic neuron, as do certain neuropeptide antagonists acting at tachykinin (NK1) and other neuropeptide receptors
decrease adenylate cyclase, cAMP
2) increase K+ EFFLUX
3) hyperpolarization
4) decrease Ca INFLUX
5) decrease substance p release |
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Term
| opioid well absorption is via __, ____ and __ |
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Definition
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Term
| which two opioid meds have less first pass metabolism than other |
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Definition
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Term
| what do you have to watch out when giving high doses |
|
Definition
accumulation.
once given
Highest concentrations localized in tissue
Brain
Liver
Kidneys
Spleen
Lungs |
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Term
| opioids are secreted via ? |
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Definition
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Term
1. fentanyl is metabolized by why enzyme?
2. Codeine, oxycodone, and hydrocodone is metabolized by what enzyme? |
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Definition
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Term
| what is the medication that is given intrathecally which blocks voltage-gated N-type Ca++ channels for chronic pain |
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Definition
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Term
| can effectivenesss of morphine be lost after freq dosing |
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Definition
| yes..To reproduce the original response, a larger dose must be administered |
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Term
| what is withdrawl or abstinence syndrome? |
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Definition
| Physical dependence is defined as a characteristic withdrawal or abstinence syndrome when a drug is stopped or an antagonist is administered |
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Term
| Persistent administration of opioid analgesics would do what to the body |
|
Definition
hyperalgesia.
increase the sensation of pain |
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Term
| Resp depression is due to |
|
Definition
| inhibition of brainstem and Most reliable indicator of this depression is a depressed response to a carbon dioxide challenge |
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Term
| SE of opioid is truncal rigidity...how would u tx the this SE |
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Definition
| give opioid antagonist but then the pain will come back |
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Term
| opioids may produce miosis/mydriasis? |
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Definition
|
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Term
| what is the effect of opioids on CV, and GI? |
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Definition
most opioids Bradycardia.
GI: constipation. it is also used in tx of severe diarrhea. |
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Term
| opioids produce hypo/hyper tension and how? |
|
Definition
HYPOTENSION
directly: depresses CNS
indirect: histamine release=peripheral vasodilation....this will also cause pruritis |
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Term
| pain is measured by what? |
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Definition
|
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Term
| what are some of the use of opioids? |
|
Definition
Analgesia: severe constant pain, cancer pain
Acute pulmo edema due to LHF
given in MI
cough/ diarrhea/ shivering (All opioids reduce shivering, but meperidine has the most pronounced effect
) |
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|
Term
| why opioids are good in anesthesia? |
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Definition
| Used prior to surgery and anesthesia due to sedative, anxiolytic and analgesic properties |
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Term
| in epidural opioids are given with what else? |
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Definition
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Term
| Fentanyl patch should be reserved for what type of pt? |
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Definition
| Due to risk of respiratory depression FDA recommends the patch be reserved for patients with an oral morphine requirement of at least 60 mg/day for 1 week or more |
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Term
| what opioid is given intranasally? |
|
Definition
|
|
Term
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Definition
| NV, inc ICP, urticaria, resp depression, constipation, urinary retention |
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Term
|
Definition
| A patient who is experiencing decreasing effectiveness of one opioid analgesic regimen is "rotated" to a different opioid analgesic (eg, morphine to hydromorphone; hydromorphone to methadone) and typically experiences significantly improved analgesia at a reduced overall equivalent dosage |
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|
Term
| S & S of stopping the opioids |
|
Definition
| abstinence syndrome:::S/sx: rhinorrhea, lacrimation, yawning, chills, gooseflesh (piloerection), hyperventilation, hyperthermia, mydriasis, muscular aches, vomiting, diarrhea, anxiety, and hostility |
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Term
| morphine and heroin withdrawal signs could last up to how much time? |
|
Definition
5 days but some sx may last for months
Methadone withdraw effect could last for 2 weeks |
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Term
| to prevent dependency and withdrawal sx what should clinician do |
|
Definition
frq evaluate if pt really needs the meds.
limit the refills -- no early refills.
start them on diff analgesic when first present |
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|
Term
| what is the tx for opioid OD? |
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Definition
| Intravenous injection of naloxone dramatically reverses coma due to opioid overdose but not that due to other CNS depressants |
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Term
| what group of meds could have interaction with opioids? |
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Definition
sedative-hypnotics
antipsychotic tranquilizers
monoamine oxidase inhibitors |
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|
Term
| 3 strong agonist of M receptors |
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Definition
| morphine, hydromorphone and oxymorphone |
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Term
which drug blocks MNDA receptors and monoaminergic reuptake transporters. + it is an agonist for Mu receptors.
main use of it |
|
Definition
Methadone
useful in cancer pain |
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|
Term
| methadone should not be give at interval of no more than how many hrs |
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Definition
|
|
Term
| methadone is metabolized by what two enzymes in liver. what are some of the side effect if liver is dysfunctional. |
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Definition
| CYP3A4 and CYP2B6 --- associated with overdose effects, including respiratory depression or, more rarely, prolonged QT-based cardiac arrhythmias |
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Term
| which one is better in sense of withdrawal signs, tolerance, physical dependence ...between morphine and methadone |
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Definition
| methadone --Withdrawal signs and symptoms occurring after abrupt discontinuance of methadone are milder, although more prolonged, than those of morphine |
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Term
| what drug is used in tx of opioid abuse |
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Definition
| methadone. its withdrawal, tolerance and physical dependece properties make methadone a useful drug for detoxification and for maintenance of the chronic relapsing heroin addict |
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Term
| what are Mu mild to moderate agonists? |
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Definition
| codeine, oxycodone, dihydrocodeine, and hydrocodone. Less efficacious than morphine (they are partial agonists) or have adverse effects that limit the maximum tolerated dose when one attempts to achieve analgesia comparable to that of morphine |
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Term
| two drugs that are used in tx for diarrhea |
|
Definition
Diphenoxylate + atropine (Lomotil)
Atropine is added in a concentration too low to have a significant antidiarrheal effect but is presumed to further reduce the likelihood of abuse
Loperamide (Imodium)
Does not cross blood brain barrier
Usual dose is two tablets to start and then one tablet after each diarrheal stool |
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Term
| if nalbuphine which is a strong kappa receptor agonist and mu receptor antagonist, is given pt suffer resp depression. PA gives pt naloxone but failed to make pt breath--what happened |
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Definition
| when respiratory depression does occur, it may be relatively resistant to naloxone reversal |
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Term
| what is Buprenorphine used for |
|
Definition
| Approved for management of opioid dependence |
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Term
| this drug : blocks both serotonin reuptake and inhibits norepinephrine transporter function, it is believed to be only a weak mu receptor agonist. |
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Definition
| Tramadol -- do not give to pt with seizures |
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Term
| antitussive --opioid derivative |
|
Definition
|
|
Term
|
Definition
longer acting narcan
(antagonist...)
treats narcotic AND ETOH addictions |
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