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Pharmacology opioids

phamacology opioid info Block 2 data

A substance that binds to a receptor and causes a response: one that binds to an opioid pain receptor in the brain, causes an analgesic response—the reduction of pain sensation, based off of affinity for receptor +++ is strong, ++ moderate, & + mild. Opioid Agonist.
The opiate agonists-antagonists associated with an analgesic ceiling effect. drug reaches a maximum analgesic effect doesnt improve w/ higher doses. Good for patients not exposed to opioids & for nonescalating moderate to severe pain. pentazocine and nalbuphine
Opioid mild agonists are codeine and hydrocodone.
Opioid strong agonists are? morphine, hydromorphone, levorphanol, oxycodone, oxymorphone, meperidine, fentanyl, and methadone.
This opioid is not for long-term use because of the accumulation of a neurotoxic metabolite, which can cause seizures? Meperidine and the metabolite normeperidine. adverse CNS effects e.g. seizures.
The preferred method of opioid administration because of associated bruising and bleeding risks, as well as injection discomfort is? intravenous, oral, and transdermal routes of drug administration
Substances that bind to a receptor and cause a partial response that is not as strong as that caused by an agonist (also known as a partial agonist) or a mixed agonist, binds to a pain receptor but causes a weaker pain response than a full agonist? Agonists-antagonists
What occurs when a given pain drug no longer effectively controls a patient's pain despite the administration of the highest safe dosages? Analgesic ceiling effect
Medications that relieve pain without causing loss of consciousness (sometimes referred to as painkillers); drugs that selectively relieves pain by acting in CNS or peripheral pain mechanisms with out altering consciousness? Analgesics, (opioids and NSAIDS
A drug that binds to a receptor & prevents (blocks) response; it does not reduce pain signals & functions as competitor because it competes with & reverses effects of agonist & agonist-antagonist drugs at receptor sites is called? Antagonist
agonist-atagonists (partial/mixed) drugs in this class exert their agonist and/or antagonist effects by binding in different degrees to? kappa and mu opioid receptors (Mu receptors are the strongest).
the most responsive receptors to drug activity with the which one being the most important are? Kappa, Mu, delta; Mu is the most important, the drugs potency is based off its affinity to the receptors, & mu has the strongest.
Three different types of mu receptors based on location: Mu 1 receptor inhibits the release of pain promoting neurotransmitters (substance P & bradykinins) controls? peripheral afferent nerves
The mu receptors that are excitatory post synaptic potential (EPSP) in descending inhibitory pain pathways are located in? the mid brain
Three different types of mu receptors based on location: Mu 2 receptor inhibit post synaptic potential on neurons carrying pain input to brain are located in? spinothalmic tract.
The prototypical agonist that binds to the mu receptor: effects are supraspinal analgesia, respratory depression, euphoria & ++sedation? morphine
The prototypical agonist that binds to the K (Kappa) receptor: effects are spinal analgesia with ++++ (strong) sedation and causes miosis (pupil constriction)? ketocyclazocine.
The prototypical agonist that binds to the delta receptor: effects are analgesia? enkephalins.
Strong opioid analgesics commonly used in combination with anesthetics during surgery. These drugs are used not only to relieve pain but also to maintain a balanced state of anesthesia? fentanyl, sufentanil, and alfentanil.
The practice of using combinations of drugs to produce anesthesia is referred to as? balanced anesthesia.
Use of this opioid as an injection for management of postoperative and procedural pain has become popular due to its rapid onset and short duration? fentanyl.
This opioid comes in a patch formulation for use in long-term pain management and should not be used for postoperative or any other short-term pain control? Transdermal fentanyl.
Strong opioids are often used to control postoperative and other types of pain these opioids are? morphine, meperidine, hydromorphone, and oxycodone.
Because these opioids are available in injectable forms, they are often first-line analgesics in the immediate postoperative settings? morphine and hydromorphone.
There is a trend away from using this opioid due to its greater risk for toxicity? meperidine.
opioid receptors:specific receptor sites for opioids, named for the drugs which have a high binding affinity for them. The main ones are? mu (morphine), kappa (opioid agonist-antagonists such as pentazocine) and delta (enkephalin endogenous opioids).
All available oxycodone dosage forms are? orally administered.
The product OxyContin is a sustained-release form of oxycodone that is designed to last up to? 12 hours: Contin in the name is trademark meaning continuous, extended, long acting or sustained release for 8 to 12 hours, same as MS Contin (morphine sulfate contin).
Opiod that is most commonly used as a cough suppressant that supresses the medullary cough center in the brain? Codiene and sometimes hydrocodone but it has a depressant effect on CNS causing sedation.
Effective, safe nonopioid analgesic for mild to moderate pain. Contraindicated in hypersensitivity or intolerance to tartrazine (yellow dye 5), alcohol, sugar, or saccharin. Avoid in those anemic or have renal or hepatic disease? Acetaminophen (Tylenol).
Available in oral & rectal, Repetitive dosing can inhibit warfarin metabolism? Acetaminophen.
Acetaminophen is also a component of several prescription combination drug products, including hydrocodone +acetaminophen which is? Vicodin
oxycodone + acetaminophen is? Percocet.
Acetaminophen liquid is available in two different concentrations: infant drops contain 80 mg/0.8 mL, whereas acetaminophen liquid contains? 160 mg/5 mL.
Acetaminophen: route, onset action, peak concentration, half life & duration? PO, 10-30min, peaks: .5-2hr, half life 1-4hr. Duration 3-4hr.
It is very important for the nurse to specify which Acetaminophen liquid or drops are to be used. The amount needed should be expressed as? milligrams, not milliliters.
If a child is to receive 160 mg liquid and the parent is told to give 5 mL, & the parent uses the infant drops, that 5 mL would contain? 500 mg versus 160 mg for the liquid. This difference could provide a fatal dose.
Natural opiate alkaloid (Schedule II, high abuse), pharmaco- kinetic/dynamic properties similar to morphine. 10% of dose is metabolized to morphine in body. Less effective as an analgesic & only agonist to possess a ceiling effect? Codeine sulfate.
Opiate commonly used as an antitussive in cough preparations. Combined with acetaminophen (tablets or elixir) is classified as Schedule III controlled substance & commonly used for control of mild to moderate pain as well as cough? Codeine Sulfate.
Codeine causes? GI tract upset.
Codeine route, onset action, peak plasma, half life, & duration of action? PO, 15-30 min, peak: 34-45 minutes, half life: 2.5-4 hr. duration: 4-6hr.
Synthetic opioid (Schedule II, high abuse), treats moderate to severe pain. Available parenteral injections (Sublimaze), transdermal (Duragesic), buccal lozenges (Fentora), and buccal lozenges on a stick or “lollipop” (Actiq) is called? Fentanyl.
Fentanyl buccal Fentora & Actiq are absorbed through the oral mucosa (not “oral”) are helpful in managing? breakthrough and procedural pain.
Fentanyl injectable is used in perioperative settings & intensive care settings for sedation during? mechanical ventilation.
Fentanyl oral & transdermal are used primarily for long-term control of? both malignant and nonmalignant chronic pain.
Fentanyl is a very potent analgesic. Fentanyl at a dose of 0.1 mg given intravenously is roughly equivalent to how much morphine? 10 mg of morphine given intravenously.
The Fentanyl transdermal patch has been shown to be highly effective in the treatment of various chronic pain syndromes such as? cancer-induced pain, especially in patients who cannot take oral medications.
Fentanyl transdermal patches should not be used in? opioid-naive patients or acute pain situations such as postoperative pain because of respiratory arrest.
fentanyl patches are best used for nonescalating pain because of the difficulty of? titrating doses.
Nurses should also be aware that after the first Fentanyl patch is applied it will take 6 to 12 hours to reach steady-state pain control again, so that supplemental short-acting therapy is required.
Most patients will experience adequate pain control from Fentanyl patches for? 72 hours.
once the Fentanyl patch is removed how much time does it take for it to reduce by 50%? 17 hours.
patients who are considered opioid tolerant are those who have been taking at least ? 60 mg of oral morphine daily or at least 30 mg of oral oxycodone daily or at least 8 mg of oral hydromorphone daily or an equianalgesic dose of another opioid.
Cutting a fentanyl patch or exposing the patch to heat (e.g., via a heating pad or sauna), is hazardous because? both accelerate the diffusion of the drug into the patient's body.
This receptor is also found in the intestinal tract and is why some opioids cause constipation, a major side effect of this receptors agonists, due to inhibition of peristaltic action, which receptor is it? Mu.
Created by: larue10510