Heme - Supportive Care in Oncology Patients

Serotonin (5HT3) Antagonist

MOA: Inhibition of 5HT3 receptors on vagal afferent neurons in GI and in CTZ

Efficacy improved when used with a steroid (20%)
Well tolerated, minimal side effects
Transient, non-significant ECG changes

Serotonin (5HT3) Antagonist

MOA: Inhibition of 5HT3 receptors on vagal afferent neurons in GI and in CTZ

Efficacy improved when used with a steroid (20%)
Well tolerated, minimal side effects
Transient, non-significant ECG changes

Serotonin (5HT3) Antagonist

MOA: Inhibition of 5HT3 receptors on vagal afferent neurons in GI and in CTZ

Efficacy improved when used with a steroid (20%)
Well tolerated, minimal side effects
Transient, non-significant ECG changes

Serotonin (5HT3) Antagonist

MOA: Inhibition of 5HT3 receptors on vagal afferent neurons in GI and in CTZ

Efficacy improved when used with a steroid (20%)
Well tolerated, minimal side effects
Transient, non-significant ECG changes

Neurokinin-1 (NK-1) Receptor Antagonist

MOA: selective, high affinity antagonist of human substance P at neurokinin 1 (NK1) receptors  interferes with the substance P pathway

Drug Interactions with CYP450 system-reduce dose of dexamethasone

Corticosteroid

MOA:?decrease 5HT3 release in gut/brain stem, ?antagonism of 5HT3 receptors, ?activate glucocorticoid receptors in brain

Generally well tolerated--elevated BS, insomnia, GI sxs, edema, weight gain, agitation
Used as single agent(low)/combined with aprepitant/5HT3 antagonists(moderate-high)

Corticosteroid

MOA:?decrease 5HT3 release in gut/brain stem, ?antagonism of 5HT3 receptors, ?activate glucocorticoid receptors in brain

Generally well tolerated--elevated BS, insomnia, GI sxs, edema, weight gain, agitation
Used as single agent(low)/combined with aprepitant/5HT3 antagonists(moderate-high)

MOA: antagonize D2 receptors in CTZ

Potent Antipsychotic agents
ADR: sedation, akathisia, dystonia

MOA: antagonize D2 receptors in CTZ

Potent Antipsychotic agents
ADR: sedation, akathisia, dystonia

Dopamine (D2) receptor antagonist; benzamide analog

MOA: stimulates gut motility; blocks intestinal 5HT2 receptors

Crosses Blood Brain Barrier = EPR’s (high doses); prevention with diphenhydramine/lorazepam; age-dependent reaction (younger 30%>elderly 2%); trismus, akathisia, dystonia

Dopamine (DS) receptor antagonist; butyrophenone

MOA: antagonize D2 receptors in CTZ

As effective as Phenothiazines with less incidence of EPRs/hypotension in delayed emesis
Sedation and anticholinergic effects

Dopamine (D2) receptor antagonist; butyrophenone

As effective as Phenothiazines with less incidence of EPRs/hypotension in delayed emesis
Sedation and anticholinergic effects
Has caused cases of QT prolongation/torsades

Benzodiazepine

MOA: no antiemetic properties; antegrade amnesia used for prevention

Place in therapy for anticipatory N/V

Cannabinoid

MOA: agonism of cannabinoid(CB1) receptors in the CNS and gut; indirectly inhibit other neurotransmitters released in emesis process

Tolerance develops to adverse effects
Effective for moderate-high emetogenic regimens
Utilized in Refractory patients

Cannabinoid

MOA: agonism of cannabinoid(CB1) receptors in the CNS and gut; indirectly inhibit other neurotransmitters released in emesis process

Tolerance develops to adverse effects
Effective for moderate-high emetogenic regimens
Utilized in Refractory patients

Erythropoiesis stimulating agent

MOA: bind to the the erythropoeitin receptor on bone marrow cells, stimulating proliferation of immature RBC clones

Shorter half-life; more frequent dosing (2-3 times a week/weekly)

Special precautions: CV events, HTN, increased risk of tumor progression or recurrence

Erythropoiesis stimulating agent

MOA: bind to the the erythropoeitin receptor on bone marrow cells, stimulating proliferation of immature RBC clones

Longer half-life; less frequent dosing (every 2-3 weeks)

Special precautions: CV events, HTN, increased risk of tumor progression or recurrence

Granulocyte colony stimulating factor

Decreases transit time from stem cell to mature stem neutrophil and reduces apoptosis; stimulates entry of stem cell and progenitor cell in the cell cycle

Pegfilgrastim: chemo can not be administered within 14 days of administration

Granulocyte-monocyte colony stimulating factor

Promotes differentiation of cells in neutrophil and monocyte lineage; Increases levels of circulating neutrophils, eosinophils, and macrophages; Reduces neutrophil apoptosis and enhances macrophage phagocytosis

Also used for priming for stem cell collection, to increase stem cell recruitment.

MOA: bind competively to opioid receptors in CNS;
decreased perception of pain, decreased reaction to pain, and increased pain tolerance

Three types of opioid receptors= mu, kappa, delta; located throughout brain, spinal cord and GI tract; binding to receptors responsible for effectiveness as well as toxicities

Displaces opiods from all receptors, reverses all of the effects of opioids; effects are immediate (3-5 min)
duration is 30-45 minutes

Do not use to reverse meperidine-lead to seizures.