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(J2) GI II Test 1 > Anti-Nausea Pharm > Flashcards

Anti-Nausea Pharm Flashcards

1
Q

What is the most effective way of treating N/V?

A

TREAT THE CAUSE, not the symptom

if not treat if prophylactically

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2
Q

What are common causes of nausea/vomiting?

A
  • Chemo/radiation (CINV/RINV)
  • post-operative (PONV)
  • pregnancy (NVP)
  • vestibular
  • GI obstruction
  • pharmacologic/metabolic/infectious irritants
  • brain lesions
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3
Q

What are the main classes of antiemetics?

A

Main:

  • serotonin receptor antagonists
  • neurokinin (NK1) receptor antagonists
  • histamine (H1) receptor antagonists
  • dopamine (D2) receptor antagonists
  • muscarinic (M1) receptor antagonists
  • cannabinoid receptor agonists

also of note:

  • glucocorticoids
  • benzodiazepines
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4
Q

How does the mechanism of action of antiemetic cannabinoids differ from the other classes of antiemetics?

A

they are the only agonsts

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5
Q

What are important sites of action for antiemetics?

What antiemetics act there?

A

Chemoreceptor trigger zone (CZT):

  • dopamine (D2)
  • neurokinin (NK1/substance P)
  • serotonin (5-HT3)

Vomiting center (VC):

  • histamine (H1)
  • dopamine (D2)
  • neurokinin (NK1/substance P)
  • serotonin (5-HT3)

GI/enteric nervous system:

-serotonin (5-HT3)

Vestibular system:

  • muscarinic (M1) **only place of note for this mechanism**
  • histamine (H1)
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6
Q

What is the common suffix of serotonin receptor antagonists?

What are the main drugs in the class?

A

“-setron”

Drugs:

  • dolasetron
  • granisetron
  • ondansetron (Zofran)
  • palonosetron
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7
Q

What is the antiemetic strength of serotonin receptor antagonists?

A

strong anitemetic

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8
Q

Where do serotonin receptor antagonists act?

A
  • vagus nerve
  • area postrema (chemoreceptor trigger zone, CTZ) where the brain detects nauseating substance in the blood
  • GI tract (enterochromafin cells release 5-HT)
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9
Q

What are the general indications for serotonin receptor antagonist use?

A

most causes of N/V

  • CINV/RINV
  • PONV
  • NVP
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10
Q

What serotonin receptor antagonist is not indicated for N/V?

What is the condition it is indicated for?

A

alosetron (indicated for IBS related diarrhea)

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11
Q

What is important about the route of administration for serotonin receptor antagonists?

A
  • oral forms
  • most of them have an IV forms which is important if the nausea is bad enough that people can’t keep oral meds down
  • some have transdermal or SubQ avaliability
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12
Q

What are possible adverse effects of serotonin receptor antagonists?

A

Common:

  • mild CNS symptoms (HA and dizziness)
  • mild GI symptoms (constipation)

Worrisome:

  • dose-dependent QT prolongation (Torsade’s)
  • serotonin syndrome (rigidity, tremor, hyperthermia, confusion)
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13
Q

What are the general pharmacokinetic features of serotonin receptor antagonists?

A

-short half-lives

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14
Q

What serotonin receptor antagonists deviate from the general pharmacokinetics of the class?

A
  • palonosetron - long half-life
  • granisetron - sustained-release formulation (transdermal patch)
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15
Q

What drugs and conditions cause interactions with serotonin receptor antagonists?

A
  • antiarrhythmics/QT prolonging agents -> Torsade’s
  • hypokalmeia/magnesemia -> Torsade’s
  • serotonergic drugs -> serotonin syndrome
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16
Q

What is the common suffix of neurokinin receptor antagonists?

What are the main drugs in the class?

A

“-pitant”

Drugs:

  • aprepitant
  • fosaprepitant
  • netupitant
  • fosnetupitant
  • rolapitant
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17
Q

What is the antiemetic strength of neurokinin receptor antagonists?

A

moderate antiemetic

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18
Q

Where do neurokinin receptor antagonists act?

A
  • CTZ
  • VC
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19
Q

What are the general indications for neurokinin receptor antagonist use?

A

-CINV

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20
Q

What neurokinin receptor antagonist has an antiemetic indication beyond CINV?

What is the condition?

A

aprepitant (indicated for prophylaxis of PONV in addition to CINV)

prep them for surgery

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21
Q

What are possible adverse effects of neurokinin receptor antagonists?

A
  • CNS symptoms
  • GI symptoms
  • CYP450 inhibition -> drug interactions
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22
Q

What are pharmacokinetic/dynamic features of neurokinin receptor antagonists?

A
  • many have drug/pro-drug forms (“fos-” indicates prodrug form)
  • some have active metabolites -> longer half-lives (netupitant/rolapitant)
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23
Q

What are the main drugs in the histamine (H1)​ receptor antagonist class?

A
  • diphenydramine (benadryl)
  • dimenhydramine (active as is but also metabolized to diphenydramine)
  • hydroxyzine
  • promethazine
  • meclizine
  • cyclizine
  • doxylamine
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24
Q

What is the antiemetic strength of histamine (H1) receptor antagonists?

A

weak antiemetic (not original intended use)

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25
Where do **histamine (H1) receptor antagonists** act?
- **VC** - vestibular system
26
What are the **general indications** for **histamine (H1) receptor antagonist** use?
- **motion sickness/vertigo** - **PONV** - mild, idiopathic N/V - add-on for CINV/RINV (**not first line**)
27
What **histamine (H1) receptor antagonists** are indicated for **motion sickness/vertigo ONLY**?
- meclizine - cyclizine
28
What **histamine (H1) receptor antagonist** is the **first line** therapy for **NVP**?
**_Doxylamine_ w/ Pyridoxine (B6)** give them a Dr. Pepper (DP)
29
What are possible **adverse effects** of **histamine (H1) receptor antagonists**?
**Anticholinergic effects**: - CNS depression - dry mouth - constipation - urinary retention - blurred vision - hypotension
30
What **drug interactions** occur with **histamine (H1) receptor antagonists**?
- **anticholinergics** (worsens anticholinergic adverse effects) - other drugs with anticholinergic effects
31
What are the **main drugs** in the **dopamine (D2) receptor antagonist** class?
_Phenothiazines_: - chlorpromazine - prochlorperazine (Compazine) - perphenazine **Other**: - metoclopramide (Reglan) - some other medications that are primarily used as psychotics w/ off-label antiemetic use
32
What is the antiemetic **strength** of **dopamine (D2) receptor antagonists**?
**weak/moderate** antiemetics (most were oringinally used as antipsychotics)
33
**Where** do antiemetic **dopamine (D2) receptor antagonists** act?
-**CTZ**
34
What are the **general indications** for **dopamine (D2) receptor antagonist** use?
- mild, idiopathic N/V - PONV - NVP - CINV/RINV (only in combination)
35
What **dopamine (D2) receptor antagonist** is also indicated for **gastroparesis**/**GI dysmotility**?
-**metoclopramide** (Reglan); ACh actions in GI system -\> stimulates motility
36
What are possible **adverse effects** of **dopamine (D2) receptor antagonists**?
**Anticholinergic effects**: - CNS depression - dry mouth - constipation - urinary retention - blurred vision - hypotension - arrhythmia
37
What **drugs interactions** occur with **dopamine (D2) receptor antagonists**?
- **anticholinergics** (worsens anticholinergic adverse effects) - other drugs with anticholinergic effects - **antiarrhythmics** (QT-prologing agents) - **antihypertensives**
38
What contraindication does metoclopramide have in addition to those of other dopamine receptor antagonists?
-**GI obstruction** (due to its prokinetic effects)
39
What are the **main antiemetic drugs** in the **muscarinic (M1) receptor antagonist** class?
- **scopolamine** - glycopyrrolate
40
What is the antiemetic **strength** of **muscarinic (M1) receptor antagonists**?
-weak antiemetic (treat motion sickness which can cause N/V)
41
**Where** do antiemetic **muscarinic (M1) receptor antagonists** act?
- **vestibular system** - muscarinic receptors throughout the brain
42
What are the **general indications** for antiemetic **muscarinic (M1) receptor antagonist** use?
- **motion sickness** - excessive secretions in end-of-life care
43
What is important about the **route of admission** for **muscarinic (M1) receptor antagonists**?
**scopolamine** comes in as a transdermal **patch -\> works for 72 hours**
44
What are possible **adverse effects** of **muscarinic (M1) receptor antagonists**?
_Significant_ **anticholinergic effects** (it is an anticholinergic itself): - CNS depression - dry mouth - constipation - urinary retention - blurred vision
45
What **drugs interactions** occur with **muscarinic (M1) receptor antagonists**?
-**anticholinergics**
46
What are the main **antiemetic drugs** in the **cannabinoid receptor agonist** class?
- dronabinol - nabilone
47
What is the antiemetic **strength** of **cannabinoid receptor agonists**?
**strong** antiemetic
48
**Where** do **antiemetic cannabinoid receptor agonists** act?
**CB1 and CB2 receptors** in **VC and CTZ**
49
What are the general **indications** for antiemetic **cannabinoid receptor agonist** use? What is special about their indications?
-**treatment-resistant CINV only** (they are schdule II/III drugs and useage is restricted)
50
What are the general **pharmacokinetic** features of **cannabinoid receptor agonists**? (what is unique to each drug)
Both **act rapidly** and are **long lasting** (**active metabolites**) Dronabinol: - **large first pass effect** - only **one active metabolite** Nabilone: -**many active metabolites**
51
What are possible **adverse effects** of **cannabinoid receptor agonists**?
- emotional lability - vertigo - sedation - impaired cognition - hallucinations - dry mouth - appetite stimulation - increased HR/BP (sympathomimetic)
52
What **drugs interactions** occur with **cannabinoid receptor agonists**?
- CNS depressants - cardiovascular agents - sympathomimetics
53
What are the categories of emetic potential of chemotherapeutics?
- high (\>90%) - moderate (30-90%) - low (10-30%) - minimal (\<10%)
54
What are the **classifications** of **CINV treatment**?
- **acute** (**\<24 hours** following chemo administration) - **chronic** (**\>24 hours** following chemo administration) - **anticipatory** (given **prior** to chemo administration
55
What is the **treatment** regimen for **_high_ emetogenic CINV**?
_**3**-drug regimen_: - **neurokinin** receptor antagonist - **serotonin** receptor antagonist - corticosteroid (**dexamethasone**) - above for a _minimum_ of **_3_** days of **chronic treatment** - **anticipatory** treatment (_all cases_) - **breakthrough** treatment (_as need_)
56
How can **_high_ emetogenic** CINV treatment be **altered if unsuccessful**?
Increase to 4-drug regimen: - add **olanzapine** (D2 antagonist) - or- - can add a **cannabinoid** if resistant to treatment
57
What is the **treatment** regimen for **_moderate_ emetogenic CINV**?
_**2**-drug regimen_: - **serotonin** receptor antagonist - corticosteroid (**dexamethasone**) - above for a _minimum_ of **_2_** days of **chronic treatment** - **anticipatory** treatment (_all cases_) - **breakthrough** treatment (_as need_)
58
How can **_moderate_ emetogenic** CINV treatment be **altered if unsuccessful**?
Increase to 3-drug regimen: -add **NK1 antagonist** -or- **olanzapine** (D2 antagonist)
59
What is the **treatment** regimen for **_low_ emetogenic CINV**?
_**1**-drug regimen_ (one of the below): - \*\*corticosteroid (**dexamethasone**) -or- - \*\***serotonin** receptor antagonist -or- - **metoclopramide** (Reglan) -or- - **p****rochlorperazine​** - above for a _minimum_ of **_1_** day of **acute treatment** - **anticipatory** treatment (_all cases_) - **breakthrough treatment** (_as need_)
60
What is the **treatment** regimen for **_low_ emetogenic CINV**?
_**1**-drug regimen_ (one of the below): - corticosteroid (**dexamethasone**) -or- - **serotonin** receptor antagonist -or- - **metoclopramie** (Reglan) -or- - **prochloperazine** - above for a _minimum_ of **_1_** day of **acute treatment** - **anticipatory** treatment (_all cases_) - **breakthrough treatment** (_as need_)
61
What is the **treatment** regimen for **_minimal_ emetogenic CINV**?
_No routine drug regimen_ - **anticipatory** treatment (_all cases_) - **breakthrough treatment** (_as need_)
62
What are the **main antiemetic drugs** used to treat **motion sickness**?
- **scopolamine** - dimenhydrinate - meclizine
63
What are the **main antiemetic drugs** used to treat **vertigo**?
- **meclizine** - cyclizine \*both H1 receptor antagonists
64
What are the **main antiemetic drugs** used to treat **gastroparesis**?
-metoclopramide
65
What are the **main antiemetic drugs** used to treat **NVP**?
- **doxylamine w/ pyrioxidine (B6)** - 5HT3 antagonist - D2 antagonist

(J2) GI II Test 1 (14 decks)

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