Opioids Flashcards Preview

Pharmacology > Opioids > Flashcards

Flashcards in Opioids Deck (50):
1

Opiate receptors

Mu, kappa, delta

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Opiate

derived from opium, natural, morphine

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Opioid

having properties similar to drugs derived from opium, semisynthetic- heroin, hydromorphone, oxycodone, hydrocodone, synthetic-methadone, meperidine

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Strong mu agonists

Morphine, fentanyl, hydrocodone, hydromorphone, oxycodone, methadone, meperidine, codeine, sufentanil, heroin, oxymorphone

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Partial mu agonists and mixed agonist antagonists

nalbuphine (Nubain), buprenorphine (Subutrex), pentazocine (Talwin), Tramadol (Ultram)

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opioid antagonists

naloxone (Narcan), Naltrexone (Revia)

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Mu receptor

located in brainstem, spinal cord, and limbic region, analgesia, respiratory depression, euphoria, reduced gastric motility, physical dependence

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Delta receptor

located in brainstem and limbic region, dysphoria, hallucination, some analgesia

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Kappa receptor

located in brainstem and spinal cord, analgesia, sedation, dysphoria, miosis

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dopamine is released when

mu receptors are stimulated which stimulates feelings of pressure

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endorphines, enkephalins

provide natural amount of pain relief

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norepinephrine, serotionin

plays an inhibitory role in the descending tract, explains why antidepressants can be used for pain control

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Pain receptors

opioid receptors, endogenous opioids and monoaminergic substances are released when pain is felt and play important roles in transmission of pain, many receptors provides many targets

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Classification of opioids

weak agonists, strong agonists, mixed agonist-antagonists, other analgesic, antagonists, most are strong mu agonists, modest kappa agonists, and weak delta agonists

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Analgesia/ euphoria

tolerance will develop, requiring increased dosing, no ceiling effect to analgesia with tolerability being only true limiting factor, provide pt is tolerating, no such thing as a max dose

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Depression cough reflex

Opioids can be used as cough suppressants, efficacious but use limited by DEA red tape

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Treatment of nausea

related to stimulation of chemoreceptor trigger zone in medulla

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ADRs of opioids

nausea/vomiting, hypotension, constriction of pupils, increased tone of circular smooth muscle, constipation, urinary retention, sedation, delirium, respiratory depression, urticaria/ pruritis

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Codeine

for mild-moderate pain, usually T3, weak by itself, considered very good antitussive, usually combined with APAP, prodrug lacks 2D6

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Codeine ADRs

N/V/C less sedation than opioids, higher incidence of histamine release, keep APAP content in mind

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Hydrocodone (Norco)

#1 prescribed drug in the country, only PO, usually with APAP, branded under Lorcet, Lortab, Norco, Vicodin, and more, can see used q3h

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Hydrocodone new product

Zohydro ER, BID, $$$, controversial, DEA CII, used for moderate to severe, no sig ADRs

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Oxycodone

PO only, long and short acting, often reserved for severe pain, good alternative to APAP

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Oxycodone combos

Oxycontin-extended release, Oxy IR, Roxicodone- immediate release caps, Oxyfast/Roxicodone- oral solutions, Percocet- with APAP, percodan- w/ aspirin, also combo with ibu

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Morphine

first line for moderate to severe pain, T1/2- 1.5-2 hours, lasts 3-5 hrs, metabolized to renally excreted active metabolite, dose adjust required, multiple dosage forms available

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Morphine MOA

strong opioid agonist, selective to mu receptor w/ primary actions in brain

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Morphine brands

avinza-once daily, kadian- daily or q12h, MScontin, Oramorph SR- q8-12h, MS IR- immediate release tab, suppository, and parenteral injection

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Morphine dosing

largely dependent on pt level of tolerance, renal funct, pain and more, dosing of parenteral narcotics should never be one size fits all, can be used in peds

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Hydromorphone (Dilaudid)

more potent than morphine, IV and PO, 1mgIV=7 mg morphine, use q3h, usually reserved for pt whose pain is not controlled w/morphine, safer in renal failure

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Meperidine (Demerol)

PO and IV, short duration (2-4 hrs), active metabolite- normeperidine very long duration, avoid in renal insufficiency, can trigger seizures, don't use more than 48 hrs, better options available

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Methadone

long acting, synthetic opioid mu agonists, half life 24-36 hrs, rarely used for pain control, but for heroin addicts

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Fentanyl

highly lipophilic, synthetic and structurally related to meperidine, more potent mu agonists, shorter acting, preferred in hemodynamically instability and bronchospasm

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Fentanyl dosage forms and devices

IV, buccal tablet (Fentora), Lozenge (Actiq), transdermal patch (Duragesic)

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Fentanyl advantages/ disadvantages

DOC in icu, sustained release opioid, good for poor compliance, good if drug abuse, available as generic, dis: delay onset 12-18 hrs, must remove old patch

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Most commonly used PCAs

morphine, hydromorphone, fentanyl

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PCA advantages/disadvantage

prevents chasing pain, pt involved w/ care, dec total amt of drug used, free up nursing time; dis avoid in certain pts, transition to PO difficult, family pushing button

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Pt may benefit from CI if

undergoing major surgery, severe pain expected for long time, continually maxing out pump settings, pain not controlled and not experiencing ADRs, baseline opioid tolerance exists, awakening at night

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Symptoms of opioid toxicity

CNS depression, respiratory depression, pin point pupils

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Treatment of opioid toxicity

respiratory support, give Naloxone (Narcan), IV

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Naloxone (Narcan)

used to reverse opioid toxicity, competes for receptors, works very fast, may titrate up to desired degree of reversal, always keep in mind half life of drug, syms may subside then return

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Opioid withdrawals

occurs when pt that is physically dependent on opioids undergoes repid cessation of exposure to opioids, not just concern for addicts

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Common symptoms of opioid withdrawal

yawning, irritability, rapid breathing, rhinorrhea, salivation, sweating, N/V/D, dilation of pupil, HTN, tachy

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Mixed agonists/Antagonist drugs

pentazocine (Talwin), Nalbuphine (Nubain), Butorphanol (Stadol)

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Mixed agonists/Antagonists

not first line option, lower abuse potential, can cause withdrawal with opioid pts, lacks euphoric effects, OB pts

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Buprenorphine/Naloxone (Suboxone)

used for treatment of opioid dependence, mixed opioid agonist/antagonist, attaches to empty opioid receptors, blocks other opioids from attaching, begin at first signs of withdrawal, license required

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Buprenorphine

partial agonist at mu receptor and antagonist at kappa receptor

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Naloxone

antagonist at mu receptor

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Tramadol (Ultram, Ultracet)

centrally acting opioid analgesic for moderate pain, dual mech of action, binds to mu and inhibits norepi and serotonin reuptake, used for mild-mod pain

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Tramadol (Ultram, Ultracet) ADRs

less sig, N/V/C, dizziness, resp depress, abuse tolerance less concern, seizures, caution with SSRI, SNRI, TCA, avoid in MAO-Is, dec with renal impaired and elderly

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Opioids are pri ary agents used

short term unless terminal, used with non-opioids, IV options work faster, great for post-op, better to not chase pain, be mindful of acute on chronic