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Pharmo for medic school > Learning outcome 2 > Flashcards

Learning outcome 2 Flashcards

1
Q

Peripheral nervous system neurotransmitters

A

Acetylcholine, norepi, epi only. 21 known in CNS

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2
Q

Monoamines (CNS Neurotransmitters)

A

Dopamine, Epinephrine, Noreip, Serotonin

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3
Q

Amino acids (CNS Neurotransmitters)

A

Aspartate, GABA, Glutamate, Glycine

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4
Q

Purines (CNS Neurotransmitters)

A

Adenosine

Adenosine monophosphate and triphosphates

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5
Q

Opioid Peptides (CNS Neurotransmitters)

A

Dynorphins, Endorphins, Enkephalins

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6
Q

Nonopioid Peptides (CNS Neurotransmitters)

A 
Neurotensin
Oxytocin
Somatostatin
Substance P
Vasopressin
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7
Q

Others (CNS Neurotransmitters)

A

Acetylcholine

Histamine

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8
Q

Increased therapeutic effects in CNS

A

Antipsychotics, antidepressants need to be taken for several weeks to develop full effects. Beneficial responses may be delayed as they result from adaptive changes, not direct effects.

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9
Q

Decreased side effects in CNS

A

Possible for therapeutic effects to remain the same as side effects decrease.
Phenobarb produces sedation but that declines while it still prevents seizures. Thought to be a cause of adaptive changes

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10
Q

Tolerance

A

Decreased response occurring in the course of prolonged drug use

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11
Q

Physical dependence

A

State in which abrupt discontinuation will precipitate withdrawal syndrome

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12
Q

Serendipitous

A

Occurred or happened by chance in a beneficial way

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13
Q

Difficulties finding new psych drugs

A

Can’t test on animals for obvious reasons, can’t test on healthy people because they have different effects

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14
Q

Opioid vs opiate

A

Opioid any drug (natural or synthetic) that has actions similar to morphine, where opiate applies only to compounds present in opium (morphine, codeine)

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15
Q

Three endogenous opioid peptides

A

Enkephalins, endorphins, dynorphins which serve as neurotransmitters, neurohormones, and neuromodulators

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16
Q

Three classes of opioid receptors

A

Mu, kappa, delta.
Opioid analgesics act primarily by activating mu and lesser extent kappa. Opioids generally don’t interact with delta but endogenous opioids act on all three.

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17
Q

Mu receptors

A

Responses include analgesia, respiratory depression, euphoria and sedation. Also related to physical dependence.

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18
Q

Analgesic defintion

A

Drugs that relieve pain without causing loss of consciousness

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19
Q

Psychotomimetic effects

A

relating to or denoting drugs that are capable of producing an effect on the mind similar to a psychotic state.

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20
Q

Kappa receptors

A

Produce analgesia, sedation and may underlie psychotomimetic effects

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21
Q

Partial agonist

A

Low to moderate receptor activation alone but blocks actions of full agonist if two are given together

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22
Q

Pure opioid agonists

A

Agonize Mu and Kappa, cause sedation, analgesia, euphoria, sedation, resp depression, dependence, cough suppression, and constipation
Morphine (prototype of strong opioid agonist)
Codeine (prototype of moderate to strong opioid agonist)
and other morphine like drugs

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23
Q

Agonist-antagonist opioids

A

Pentazocine (talwin, which is the prototype) , nalbuphine, butorphanol all antagonize mu and agonize kappa
Buprenorphine partial mu agonist, antagonist to kappa

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24
Q

Pure opioid antagonists

A

Antagonize mu and kappa, naloxone, naltrexone and others.

Methylnaltrexone to treat opioid induce constipation

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25
Q

Other effects of morphine

A

Resp depression, constipation, urinary retention, orthostatic hypotension, emesis, miosis, cough suppression, biliary colic.
Produce analgesia by mimicking actions of endogenous opioid peptides

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26
Q

Resp depression

A

At equinanalgesic doses, all cause resp depression to same extent by activation of mostly mu and lesser kappa
Resp depression kicks in 7 minutes after IV, 30 after IM, 90 after sub q and may persist 4-5 hours.
Morphine by spinal ejection might delay resp depression by hours

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27
Q

Constipation in opioids

A

Activating gut mu receptors suppresses propulsive intestinal contractions, intensifies nonpropulsive contractions, increase tone of anal sphincter, inhibit secretion of fluids into intestinal lumen.
Goal is to produce soft formed stool every 1-2 days.

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28
Q

Opioid constipation tx

A

Physical activity, increased fibre and fluids, enemas, senna to counter reduced bowel motility, docusate as stool softener, polyethylene glycol as osmotic laxative.
Rescue therapy is strong osmotic laxative like lactulose or sodium phosphate.
Methylnaltrexone blocks mu in intestines and is last resort (can’t cross BBB)

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29
Q

Orthostatic hypotension from opioids

A

Morphine like drugs block baroreceptor reflex and dilate peripheral arterioles and veins.
Peripheral vasodilation mostly from histamine

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30
Q

Morphine like drugs urinary retention

A

Increased tone of bladder sphincter, increase tone of detrusor muscle (elevating pressure within bladder, causing sense of urgency) and may suppress by diminishing awareness of fullness.
TCAs and antihistamines (antichols) worsen it, as well as underlying BPH
Also decreases renal blood flow which lowers urine production, and promotes releases of antidiuretic hormone

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31
Q

Morphine like drugs cough suppresion

A

May lead to accumulation. Act on medulla to suppress. Pts may need to be instructed to forcefully cough

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32
Q

Biliary colic morphine like drugs

A

Can induce spasm of bile duct, causing increased pressure in biliary tract causing epigastric distress to biliary colic.
In pts with biliary colic, opiods may intensify rather than relieve.
Morphine is worse than others for this

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33
Q

Emesis in morphine like drugs

A

Direct stimulation of chemoreceptor trigger zone of medulla. Greatest with initial dose. Occur in 15-40% of walking pts (uncommon in recumbent pts)
Stillness and antiemetics help this

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34
Q

Elevation of ICP in morphine like drugs

A

Indirect, as it suppresses resps which increase CO2 which dilates cerebral vasculature. ICP will remain normal if resps are kept normal

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35
Q

Dysphoria in morphine like drugs

A

Anxiety and unease. Uncommon if in pain, can happen if there is no pain

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36
Q

Sedation in morphine like drugs

A

Minimized with smaller more frequent dosing, short half lives, and small doses of CNS stimulants given with

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37
Q

Miosis in morphine like drugs

A

Can cause poor night vision

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38
Q

Birth defects in morphine like drugs

A

2-3x higher incidence. Worse during conception/early on.
Can cause congenital heart defects (av septal defects, hypoplastic left heart, conoventricular septal defects) and spina bifida and gastroschisis

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39
Q

Gastroschisis

A

Protrusion of intestine through abdo wall near umbilicus

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40
Q

Neurotoxicity in morphine like drugs

A

Delirium, agitation, myoclonus, hyperalgsia.
Risk factors are renal impairment, preexisting cognitive impairment, prolonged high dose use.
Manage with reduced dose and hydration and if long term use is indicated, occasionally switching

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41
Q

Long term use in morphine like drugs

A

Hormonal changes, altered immune function, decline in cortisol, increase in prolactin, decrease in LH and FSH

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42
Q

Pharmacokinetics of morphine

A

IM, IV, SUB q lasts 4-5 hours
Epidural, intracathecal up to 24 hours
Oral IR is 4-5 hours, ER up to 24.

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43
Q

Tolerance in morphine like drugs

A

Tolerance doesn’t develop to miosis and constipation

Cross-tolerance exists with other opiods but not other CNS depressants

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44
Q

Physical dependence in morphine like drugs

A

Short half lives give intense short withdrawal. Longer is longer

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45
Q

Withdrawal symptoms

A

Yawning, rhinorrhea, sweating (approx 10 hours after final dose) then anorexia, irritability, tremor, gooseflesh (term cold turkey) and peak with violent sneezing, weakness, nausea, vomiting, diarrhea, abdo cramps, bone and muscle pain, muscle spasm, kicking movements (kicking the habit)
Lasts 7-10 days in morphine
Rarely dangerous

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46
Q

Labor and delivery in morphine like drugs

A

Suppresses uterine contractions, resp depression in neonates

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47
Q

Head injury in morphine like drugs

A

Can increase ICP, and make tough to diagnose

48
Q

Other precautions in morphine like drugs

A

Inflammatory bowel disease pts can get toxic megacolon or paralytic ileus.
Liver impaired pts may hae intensified effects
BPH, hypotension, reduced blood flow pts

49
Q

CNS depressants in morphine like drugs

A

All CNS depressants can intensify sedation and resp depression

50
Q

Anticholingerics in morphine like drugs

A

Can exacerbate morphine induced constipation and urinary retention

51
Q

Hypotensive drugs in morphine like drugs

A

Can exacerbate the hypotension obvi

52
Q

Monoamine oxidase inhibitors in morphine like drugs

A

Can produce a syndrome of excitation, delirium, hyperpyrexia, convulsions and severe resp depression. Hasn’t been reported with morphine (just meperidine)

53
Q

Ampehtamines, clnidine, dextromethorphan in morphine like drugs

A

Can enhance opioid induce analgesia and can offset sedation

54
Q

Embeda

A

Moprhine/naltrexone combo. Morphine in ER capsules and inner core of naltrexone. If swallowed only morphine is absorbed, if crushed to be injected naltrexone gets released
ETOH accelerates released of morphine from embeda

55
Q

Morphine general dosing guidelines

A

Sharp stabbing pain needs higher doses than dull.

Older and younger need less, neonates need very low as BBB not developed

56
Q

Routes and dosage morphine

A

Oral is 10-30, don’t chew capsules, don’t drink ETOH,
Children IM SUBQ is 0.1-0.2mg/kg
IV over 4-5 minutes

57
Q

Fentanyl

A

100X POTENCY of morphine
Metabolized by CYP3a4
Patches come in 12.5,25,50,85,100mcg/hr don’t expose patches to heat, no strenuous exercise

58
Q

Sufentanil

A

Potency 1000X morphine, alfentanil 10x morphine

59
Q

Remifentanil

A

Rapidly metabolized by plasma and tissue esterases, not hepatic metabolism or renal excretion. About 100X potency of morphine. Effects in minutes, terminate in 5-1minutes. Given as infusion during surgery at 0.05 to 2mcg/kg/min and post operative at 0.025 to 0.2 mcg/kg/min
Muscle rigidity like fentanyl

60
Q

Meperidine

A

Used to be bigger, not so much because of short half life, adverse interactions, and toxic metabolites. Excessive activation of serotonin reuptake inhibition.

61
Q

Methadone

A

Prolonged QT, torsades in 65-400mg a day. Metabolized by CYP3A4

62
Q

Equianalgesic dosing mg codeine

A

PO 200

IM subq 130

63
Q

Equianalgesic dosing mg fentanyl

A

0.1 IM/IV

64
Q

Equianalgesic dosing mg hydrocdone

A

30 PO

65
Q

Equianalgesic dosing mg hydromorphone

A

PO 7.5

Injection 1.5

66
Q

Equianalgesic dosing mg levorphanol

A

PO 4

Injection 2

67
Q

Equianalgesic dosing mg Meperidine

A

PO 300

Injection 75

68
Q

Methadone Equianalgesic dosing mg

A

PO 20

IM IV 10

69
Q

Equianalgesic dosing mg Morphine

A

PO 30

Injection 10

70
Q

Equianalgesic dosing mg oxycodone

A

20 PO

71
Q

Equianalgesic dosing mg oxymorphone

A

PO 10
Injection 1
Rectal 10

72
Q

Tapentadol Equianalgesic dosing mg

A

PO 100

73
Q

Moderate to strong opioid agonists vs moprhine

A

Less analgesia, resp depression and have a somewhat lower potential for abuse
Can be reversed with naloxone

74
Q

Codeine

A

30mg = 325mg of acetaminophen for pain relief
10% undergoes metabolism to morphine in the liver by CYP2D6
As the dose is higher for therapeutic doses, analgesia is more difficult to attain SAFELY

75
Q

Codeine metabolism

A

Some people lack effective CYP2D6 gene and can’t convert codeine to morphine so no relief is felt
Hyper metabolism in 7% of whites, 3% of blacks, and 1% of hispanic and asians is possible, and will also prevent analgesia

76
Q

Codeine in da boob

A

Rare, but possibly for severe toxicity, usually from ultrarapid metabolism
Nursing mothers should look for excessive sleepiness, breathing difficulty, lethargy, poor feeding

77
Q

Antitussive codeine

A

10mg

78
Q

Oxycodone

A

Equivalent to codeine. Metabolized by CYP 3a4
Controlled release is oxycontin
Used to be stamped OC, now OP and are tough to crush and form a gel with liquids
Oxycontin OP burns if snorted. It is immediate release. Also gel in water or alcohol

79
Q

Hydrocodone

A

5mg
Only available in combination with ibuprofen or acetaminophen.
If used as cough suppressant combined with antihistamines and nasal decongestants.
Vicodin, vidoprofen, lortab

80
Q

Tapentadol

A

Similar pain relief to oxycodone

Differs in it activates mu receptors, also blocks reuptake of norepi (like tramadol) and causes less constipation

81
Q

Other names meperidine

A

Demerol

82
Q

Other names methadone

A

Diskets, dolophine, methadose

83
Q

Other names Hydromorphone

A

Dilaudid, exalgo, jurnista

84
Q

Other names oxymorphone

A

Opana

85
Q

Other names oxycodone

A

Oxycontin, roxicodone, oxecta, oxyIR

86
Q

Other names hydrocodone

A

Vicodin, vicoprofen, lortab

87
Q

Drug interactions tapentadol

A

ETOH, opoids, barbs, benzos will cause extra depression and sedation like anything
MAOI because it blocks reuptake of norepi can cause hypertensive crisis
Don’t mix with SSRIs or TCAs or seratonin agonsists (SSRI has no problems in clinical trials)

88
Q

4 agonist-antagonist opoids

A

Nalbuphine, butorphanol, pentazocine, buprenorphine

First three antagonize mu and agonize kappa

89
Q

Pentazocine actions and uses

A

AKA talwin.
Prototype for ag/antag
Kappa only, antags mu, therefore limited resp depression, and high doses cause anxiety, strange thoughts, nightmares, hallucinations (thought to be from kappa activation)
Also less effective for pain control
*Increases MVO2
Will trigger withdrawal in addicts as it blocks Mu AKA don’t give it to addicts
Can cause dependence but mild (cramps, fever, anxiety, restlesness)

90
Q

Nalbuphine

A

Like pentazocine
Analgesic similar to morphine at low doses, but has a ceiling and a ceiling to resp depression like penta
Less withdrawal than morph, more than penta
In labor, causes fetal bradycardia and apnea, cyanosis, hypotonia

91
Q

Butorphanol

A 
Similar to pentazocine
Less analgesia than morph
Resp depress ceiling
Psychotomimetic reactions possible but rare
Increases MVO2
92
Q

Buprenorphine (the other antag/ag opioid)

A

Partial ag at mu, antagonist at kappa.
Similar pain analgesia to morph, but don’t get significant tolerance
Depressed resp but not severe
Up to 2 weeks for withdrawal to start
Naloxone can’t reverse, but pretx can prevent toxicity (binds to tight for naloxone to displace)
Treats opioid addiction

93
Q

Buprenoprhine physically

A

Prolongs QT.
Adverse effects increased with underlying psychosis, ETOH abuse, adrenocortical insufficiency, severe liver or renal impairment
Can cause spasms of sphincter of Oddi

94
Q

Sphincter of Oddi

A

Where bile duct and pancreatic duct enter duodenum. Buprenorphine induces these, and creates risk of pancreatitis or biliary disease in the predisposed

95
Q

Withdrawal

A

Clinically significant dependence occurs within 20 days from high doses
Tape over 3 days, up to 7-10 if dependence is high

96
Q

Physical dependence definition

A

Abstinence syndrome will occur if drug is abruptly withdrawn. NOT the same as addicition

97
Q

Abuse definition

A

A drug used inconsistent with medical or social norms

98
Q

Addiction definition

A

Disease process characterized by continued use of a psychoactive substance despite physical, psychologic, or social harm. Completely separate from physical dependence, physical dependence doesn’t need to exist, does up chances of addiction tho yo

99
Q

Addiction concerns

A

Boston Collaborative Drug Study says of 12,000 hospitalized pts taking opioids, 4 became drug abusers.
Addiction is not a reason to withhold

100
Q

Drug abuse screening tool

A

NIDA-modified ASSIST

101
Q

PCA

A

Patient controlled analgesia

102
Q

Obstetric Analgesia

A

Morphine and meperidine may cause depressed fetal resps and uterine contractions given parenterally, still given though.
Fentanyl, sufentanil, alfentanil,, remifentanil shorter duration of action and don’t produce significant neonatal depression.
Also mixed like nalbuphine, butorphanol, pentazocine, buprenorphine offer increase pain relief without causing further resp depression

103
Q

MI Pain control

A

Pentazocine and butorphanol both increase MVO2 so avoid.

Morphine good for decreasing MVO2

104
Q

Opioids head injury

A

Can cause ICP, and miosis, mental clouding and vomiting can make diagnostics more difficult

105
Q

4 pure antagonists

A

Narcan, methylnaltrexone (relistor), alvimopan (entereg) and naltrexone (revia, vivitrol)

106
Q

Pharmacokinetics naloxone

A

IV immediate
IM 2-5 minutes
Half life approx 2 hours

107
Q

Methylnaltrexone actions and use

A

Selective mu antagonist for opioid induced constipation for those who have not responded to standard laxative therapy.
Methyl group prevents it from crossing BBB, so it also does not decrease ANALgesia

108
Q

Alvimopan

A

Selective peripherally acting mu opioid antagonist like methylnaltrexone
Only for short term use (methylnaltrexone can be used long term) because it increases MI risk

109
Q

Naltrexone (ReVia, Vivitrol)

A

Pure opioid antagonist used for opioid and ETOH abuse.
It prevents euphoria
It can cause withdrawal if pts still addicted. It doesn’t stop cravings like methadone
Can cause hepatocellular injury in high doses

110
Q

Nonopioid centrally acting analgesics

A

Tramadol, clonidine, zionotide, dexmedetomidine
Relieve pain by mechanisms largerly or completely unrelated to opioid receptors so little or no resp depression, dependence, or abuse

111
Q

Tramadol

A

Moderately strong analgesic with low potential for abuse, resp depression
Works through combo of opioid and nonopioid mechanisms

112
Q

MOA tramadol

A

Analog of codeine that works with weak agonist activity at mu receptors, ut mostly by blocking norepi and serotonin reuptake and thereby activating monoaminergic spinal inhibition of pain.
Naloxone only partially blocks effect

113
Q

Therapeutic use tramadol

A

Not as good as morphine, same as codeine plus asa or tylenol

Analgesia at 1 hour after oral dosing, max at 2 hours and continues for 6

114
Q

Sides of tramadol

A 
Serious adverse effects are rare, resp depression is minimal at recommended doses
Sedation, dizziness, headache, dry mouth, constipation
Rarely seizures (probably only an issue in epileptics)
115
Q

Drug interactions tramadol

A

Sedation with other CNS depressants
HTN crisis if given with MAOI
Serotonin syndrome with SSRI TCA MAOI triptans etc

116
Q

Clonidine (catapres, duraclon)

A

TX HTN and relief of severe pain

Pharmo for medic school (26 decks)

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