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Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

Opiate receptors

A

Mu, kappa, delta

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2
Q

Opiate

A

derived from opium, natural, morphine

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3
Q

Opioid

A

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

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4
Q

Strong mu agonists

A

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

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5
Q

Partial mu agonists and mixed agonist antagonists

A

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

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6
Q

opioid antagonists

A

naloxone (Narcan), Naltrexone (Revia)

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7
Q

Mu receptor

A

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

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8
Q

Delta receptor

A

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

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9
Q

Kappa receptor

A

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

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10
Q

dopamine is released when

A

mu receptors are stimulated which stimulates feelings of pressure

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11
Q

endorphines, enkephalins

A

provide natural amount of pain relief

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12
Q

norepinephrine, serotionin

A

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

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13
Q

Pain receptors

A

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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14
Q

Classification of opioids

A

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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15
Q

Analgesia/ euphoria

A

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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16
Q

Depression cough reflex

A

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

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17
Q

Treatment of nausea

A

related to stimulation of chemoreceptor trigger zone in medulla

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18
Q

ADRs of opioids

A

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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19
Q

Codeine

A

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

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20
Q

Codeine ADRs

A

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

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21
Q

Hydrocodone (Norco)

A

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

22
Q

Hydrocodone new product

A

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

23
Q

Oxycodone

A

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

24
Q

Oxycodone combos

A

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

25
Q

Morphine

A

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

26
Q

Morphine MOA

A

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

27
Q

Morphine brands

A

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

28
Q

Morphine dosing

A

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

29
Q

Hydromorphone (Dilaudid)

A

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

30
Q

Meperidine (Demerol)

A

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

31
Q

Methadone

A

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

32
Q

Fentanyl

A

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

33
Q

Fentanyl dosage forms and devices

A

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

34
Q

Fentanyl advantages/ disadvantages

A

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

35
Q

Most commonly used PCAs

A

morphine, hydromorphone, fentanyl

36
Q

PCA advantages/disadvantage

A

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

37
Q

Pt may benefit from CI if

A

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

38
Q

Symptoms of opioid toxicity

A

CNS depression, respiratory depression, pin point pupils

39
Q

Treatment of opioid toxicity

A

respiratory support, give Naloxone (Narcan), IV

40
Q

Naloxone (Narcan)

A

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

41
Q

Opioid withdrawals

A

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

42
Q

Common symptoms of opioid withdrawal

A

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

43
Q

Mixed agonists/Antagonist drugs

A

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

44
Q

Mixed agonists/Antagonists

A

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

45
Q

Buprenorphine/Naloxone (Suboxone)

A

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

46
Q

Buprenorphine

A

partial agonist at mu receptor and antagonist at kappa receptor

47
Q

Naloxone

A

antagonist at mu receptor

48
Q

Tramadol (Ultram, Ultracet)

A

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

49
Q

Tramadol (Ultram, Ultracet) ADRs

A

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

50
Q

Opioids are pri ary agents used

A

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

Pharmacology (61 decks)

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