CINV Flashcards
What is the MOA of serotonin antagonists?
These block serotonin receptors in the:
CNS: CTZ and vagal afferents (5-HT3-receptors)
Periphery: inhibits serotonin release from gastrointestinal tract
What are the generic/brand names of 5-HT3 RAs?
Dolasetron (Anzemet)
Granisetron (Kytril)
Ondansetron (Zolfran)
Palonosetron (Aloxil)
Zolfran doses for CINV treatment are:
High emotogienticity:
16-24 mg prior to chemo
Moderate: 8 mg PO Q8-12 hrs.
IV: 0.15 mg/kg/dose (MAX 16 mg/dose). Subsequent doses may be repeated 4 and 8 hrs after the 1st dose
When should 5-HT3 RAs be used in CINV?
These are standard therapy for highly and moderately emetogenic chemo.
They are used synergistically with corticosteroids.
Oral and IV dosage forms are equally efficacious.
Antiemetic effect > anti-nausea effect
What ADRs are associated with 5-HT3 RA use?
Generally well tolerated.
Common: HA, constipation
Severe: QTc prolongation
When should dexamethasone (Decadron) be used for CINV?
Not effective as monotherapy for highly or moderately emetogenic regimens.
Very effective in preventing delayed CINV due to synergistic effects.
ADRs associated with Decadron are:
Insomnia Anxiety Increased appetite Rise in blood glucose levels Many many more
What is the MOA is NK1 antagonists?
Substance P is a neuropeptide which binds to NK1 receptor in abdominal afferent vagal nerves and CTZ resulting in emesis.
NK1 antagonists have high-affinity for human substance P/NK1 receptors.
NK1 antagonists cause which ADRs?
Hiccups Dyspepsia Constipation Diarrhea HA Fatigue
What agents are NK1 antagonists?
Aprepitant (Emend)
Fosaprepitant (Emend for injection)
Netupitant/palonosetron (Akynzeo)
Rolapitant (Varubi)
When are BZDs used in CINV?
Anticipatory and breakthrough CINV
Which BZD is commonly used in CINV?
Lorazepam (Ativan)
0.5-2 mg PO/IV/SL Q4-6H PRN
Max 2 mg/dose
ADRs caused by BZD use are:
Sedation
Amnesia
Dizziness
Unsteadiness
What is the MOA of phenothiazines?
Blockade of dopamine receptors in the CTZ
When are phenothiazines used?
Breakthrough treatment of delayed CINV.
Has rapid onset
Which agents are classified as phenothiazines?
Prochlorperazine (Compazine)
Promethazine (Phenergan)
ADRs of phenothiazines are:
Sedation
EPS
What is the MOA of metoclopamide (Reglan)?
It’s antiemetic MOA is via inhibition of central and peripheral dopamine receptors.
When is Reglan used?
Delayed CINV
For higher doses, co-administered with diphenhydramine and lorazepam to prevent EPS
ADRs of Reglan are:
EPS Drowsiness Restlessness Fatigue Diarrhea
What is the MOA of olanzapine (Zyprexa)?
Blocks dopamine, serotonin, histamine, and acetylcholine.
What is the MOA of haloperidol (Haldol)?
It is a dopamine receptor antagonist
When are antipsychotics used in CINV?
Prophylaxis for highly and moderately emetogenic regimens (olanzapine)
As a rescue med for breakthrough CINV
What are the ADRs for olanzapine?
Disturbed sleep
Fatigue
Drowsiness
Dry mouth
ADRs of Haldol include:
EPS
Dystonic reactions
HA
QT prolongation (rare)
BBW associated with antipsychotics are:
Use in caution with elderly patients and dementia: antipsychotics increase risk of mortality
Which 2 agents are used to treat EPS?
Diphenhydramine and Benztropine
What is the MOA of cannabinoids?
Direct inhibition of neurotransmitters via agonist of CB1 CNS receptor
When are cannabinoids used in CINV?
In refractory cases
Which agents are cannabinoids?
Nabilone (Cesamet)
Dronabinol (Marinol)
ADRs associated with cannabinoids are:
Sedation
Dysphoria or euphoria
Concentration difficulties
Paranoia
What is the MOA of scopolamine transdermal patch (Transdermal Scop)?
It is an anticholinergic/antimuscarinic agent. It works in the CNS by blocking cholinergic transmission to the vomiting center.
When is scopolamine used in CINV?
Refractory CINV associated with motion or dizziness
ADRs caused by Transderm Scop used are?
Dry mouth
Somnolence
Blurred vision
High emetic risk IV agents (>90%) are:
AC (doxorubicin/epirubicin with cyclophosphamide Cisplatin Cyclophosphamide > 1500 mg/m2 Doxorubicin > 60 mg/m2 Ifosfamide >= 2 g/m2
Mod emetic risk IV agents (30-90%) are:
Busulfan Carboplatin Cyclophosphamide = 1500 mg/m2 Doxorubicin < 60 mg/m2 Irinotecan Methotrexate >= 250 mg/m2
Low emetic risk agents (10-30%) are:
Docetaxel
Doxorubicin liposomal
5-FU
Paclitaxel (including albumin bound)
Mod to high emetic risk oral agents are:
Busulfan >= 4 mg/d
Ceritinib
Crizotinib
Min to low emetic risk oral agents are:
‘’Nib’’
Capecitabine
Patient specific risk factors for CINV are:
Female < 50 yo History of motion sickness Pregnancy-related nausea Lack of alcohol use History of anxiety or depression Prior chemo use
