Treatment of Emesis and Constipation

Question 1

N/V path

Answer 1

Vomiting from chemo through 5-HT3 receptors

Pregnancy or motion through the H1 and musc receptor

Question 2

N/V chemo

Answer 2

Cisplatin, cyclo, dacarbazine

Doxo is pretty moderate

Question 3

Palonosetron

Answer 3

Can be given many diff ways

Prolonged effects after disappearing from circulation

P450 substrate

Loinger 1/2 life than ondansetron

EKG side effects more for ondansetron

Question 4

Metoclopramide

Answer 4

D2 antago
5-HT3 antag
5-HT4 ag

Side effects include etrapyramidal, restlesness, drowsiness

Question 5

Aprepitant

Answer 5

NK1 recpeotr that binds to substance P which regulates chemo-induced nausea

Anti-emetic usually used with GC and ondansetron

Question 6

Prochlorperazine

Answer 6

Widely used for suppressing emesis

Antag D2 receptor

Masks the gag reflex so choking is a problem…also a tranquilizer

Might work for chemo?

Question 7

Cannabinoids

Answer 7

Stmiulates cnnabinoid receptors around the vomiting center

Question 8

Anticholinergics and benzos

Answer 8

Anti - motion sickness

Benzo - anti-anxiety and sedative work on anticipatory effects of vomiting

Question 9

Syrup of ipecac

Answer 9

Induces vomting…mix of alkaloids that acts on chemo trigger zone and locally irriates stmach and duodenum

Emetine

Question 10

Bul-forming laxatives

Answer 10

Directly abosbr water into the intestines and inc peristalsis

Question 11

Osmotic agents and Mg hydroxide

Answer 11

Polyethylene glycol…poorly absorbed and pull water into the GI tract

MgOH is same mech

Question 12

Dipehnylmethane
Phenolphthalein
Antraquinone laxes

Answer 12

POorly understood and leads to low-grade inflammation which leads to motility

Withdrawn

Derived from natural

Question 13

Bisacodyl

Answer 13

Relief of constipation or colonic cleanse

Stimulates mucosal nerve pleuxs of the colon aliong with Cl and water

Can damage mucosa nd cause inflammatory response

Given orally and acts slowly

Question 14

Lubiprostone

Answer 14

Activates CIC-2 chloride channels followed by water that softens stool

Generally used for constipation resistant to other strategies

Question 15

Linaclotide

Answer 15

Resistant to stomach acid and has quick half life

Activiates guanylate cyclase C2

IBS

Question 16

Naloxegol

Answer 16

Form of opioid antagonist that prevents it from crossing the BBB

Question 17

Intraluminal agents for diarrhea

Answer 17

Promote bulk formation

Hydrophobic colloids and bismuth

Question 18

Loperamide

Answer 18

Antisecretory activity against cholera toxin and E.coli

Improves anal sphincter tone

Binds to perpiehral mu-opioid receptors

Overdose cna lead to CNS effects

Does NOT cross BBB due to substrate fo P-glucoprotein…worry about with protease inhibitors and HIV

Question 19

Diphenoxylate

Answer 19

Binds to peripheral mu receptors

Have CNS effects at high doses

Question 20

Eluxadoline

Answer 20

Agonist of mu opioid receptor and kappa

Antagonist delta

Diarrhea rpedominant IBS

INhibit OAT-will elevate elluxadoline…includes cyclosporine, antiretrovirals and rifampin