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Pharmacology 3 > Opiods/Narcotics > Flashcards

Opiods/Narcotics Flashcards

1
Q

What is opium?

A

dried juice from the seed-head of the opium poppy

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2
Q

what are the 3 properties of opium?

A

Analgesia
Anti-tussive
Constipating

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3
Q

What was the first opium derivative?

A

Morphine- named from Morpheus greek god of dreams

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4
Q

What is another opium derivative?

A

codeine

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5
Q

define Opioid

A

generic term for natural and synthetic substances which bind opiod receptors

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6
Q

what are the 3 types of opiod receptors?

A

Delta
Mu
Kappa

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7
Q

How do opioids work?

A

receptor agonism leads to reduction in the secretion of pain inducing NTs

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8
Q

Name the a/e of opioids (7)

A 
Sedation
Reduced peristalsis
Pruritus (histamine release)
Respiratory depression
Nausea/vomiting
Miosis
Peripheral vasodilation
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9
Q

What should you remember to monitor for a patient on opioids?

A

hypotension

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10
Q

What else does an opioid do?

A

contract sphincter of Oddi, increases biliary tree pressure and worsens pancreatic pain

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11
Q

what opioid does not contract the sphincter of oddi?

A

Meperidine

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12
Q

What is the antidote for opioids?

A

Naloxone (acute, overdose)

Naltrexone (longer acting, for detox)

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13
Q

What does Naloxone do to addicts?

A

precipitates severe withdrawal

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14
Q

How do the opioid antidotes work?

A

Reverse respiratory depression

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15
Q

What can the pharmacy in KY dispense?

A

naloxone injections/nasal sprays

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16
Q

Why is methadone good for opioid detox? Why bad?

A

you can control it, and it has a large Vd and long T 1/2

most resistant opioid against naloxone

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17
Q

What forms do opioids come in?

A

IV, SQ, TD, IT (intrathecal, epidural), PCA (patient controlled analgesia)

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18
Q

What is the gold standard opioid? Why is it unique? Used for what? Significant what?

A

Morphine
Highly hydrophilic (unlike most opioids)
Chest pain alerts- reduces sympathetic tone & little reflex tachycardia

Significant first-pass effect

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19
Q

What is first pass effect?

A

With oral ingestion, first go through the liver the drug is metabolized a lot, so PO to IV ration 6:1 for morphine

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20
Q

Meperidine-
structure
potency
metabolism

A

Structure dissimilar to MS (morphine)
75-100mg meperidine, unline MS 10 mg (less potent than MS)
hepatically metabolized to normeperidine, excreted by kidney

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21
Q

What is the ADME precaution with meperidine?

A

Normeperidine accumulation in renal failure, lowers seizure threshold

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22
Q

How long do you use meperidine?

A

72 hours or less

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23
Q

Black clouds with meperidine?

A

seizures

increased serotonin levels, so if combined with SSRI may get serotonin syndrome

24
Q

what is serotonin syndrome?

A

life threatening seizures, tremors, hallucinations, death. stop the drug and treat symptoms

25
Q

Heroin is what? what schedule? what philicity?

A

semi-synthetic agent derived from MS
C1
Lipophilic (highly)
Rapidly crosses BBB

26
Q

Meperidine has a role in what? (3 things total)

A

Obstetrics, it will not prolong labor like MS does

anticholenergic properties

weak antitussive

27
Q

Avoid meperidine in what?

A

chest pain alert, may cause reflex tachycardia

28
Q

How is codeine made? Analgesic effects derived from what?

A

Natural or via methylation of MS

Analgesic effects derived from metabolism to morphine (10% of dose)

29
Q

Indications for codeine? Where specifically??

A

mild to moderate pain
Persistent cough
ABOVE THE SHOULDERS (dental)

30
Q

What is a popular form of codeine?

A

Codeine #3– 300mg APAP with 30mg codeine

this is equal to 3mg of morphine!

31
Q

Oxycodone- made how? potency what forms?

A

semi-synthetic
2x the potency of morphine
Immediate release and continuous release

32
Q

Oxycodone comes in combination with what?

A

ASA and APAP

33
Q

Oxycodone bioavailability?

A

High systemic bioavailability even following oral administration, so LOW first pass

34
Q

Benefit of oxycodone vs morphine?

A

Less pruritus and mental status change (less histamine release)

35
Q

Issues with oxycodone?

A

high abuse potential

36
Q

Hydrocodone- class, made in combination with what, and for pain where?

A

C2, was C4
made with APAP (Vicodin, Lortab)
pain below the shoulders

37
Q

Hydromorphone comes how? potency?

A

IV and PO, 5x the potency of MS (PO), 8x the potency of MS (IV)

38
Q

Methadone acts how?

A

reduces cravings and the euphoric effects of other opiods

39
Q

Why is methadone good for drug addicts?

A

Long duration of action, large Vd

40
Q

Is methadone hydro or lipophilic?

A

HIGHLY lipophilic

41
Q

Recent concerns with methadone?

A

QT complex prolongation (torsades)

also difficult to reverse in overdose

42
Q

What is backloading?

A

use own blood to mix drug, makes it isotonic so your veins don’t collapse

43
Q

Percocet vs percodan?

A

oxycodone with APAP (percocet) and with ASA (percodan)

44
Q

Fentanyl- T1/2, potency, __philic

A

Short half life, so short-acting
100x more potent than morphine (highest)
High lipophilicity

45
Q

Fentanyl is an ideal ____ agent

A

transdermal, lasts 72 hours

46
Q

How do you get the most of a transdermal agent?

A

run it under hot water

47
Q

What are the fentanyl analogous? Potency compared to fentanyl?

A

Alfentanil (less potent)
Remifentanil (as potent, good peri-anesthetic agent)

shorter half lives than fentanyl

48
Q

Tramadol-
what is it?
How does it work?
Class

A

Centrally acting analgesic with weak opioid activity
Inhibits reuptake of NE and enhances 5-HT release

From C VI to C IV

49
Q

Tramadol benefits and risks?

A

less respiratory depression. BUT reduces seizure threshold

50
Q

What were we wrong about with tramadol?

A

higher addictive potential than we originally thought

51
Q

Tramadol is between what two drugs?

A

Toradol and true narcotic

52
Q

Bupenorphine should be used for what?

A

instead of methodone for opioid dependence and moderate-severe pain.

53
Q

How does bupenorphine work?

A

opioid agonist/antagonist (pain/dependence)

54
Q

What class is bupenorphine?

A

CIII

55
Q

What is a 6th cousin to narcotics?

A

dextromethorphan (DM) antitussive

Pharmacology 3 (10 decks)

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