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Pharm 3 Module 2: GI > anti-emetics, laxatives > Flashcards

anti-emetics, laxatives Flashcards

1
Q

Where is the vomiting/emesis center

A

group of cells in the medulla oblongata

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2
Q

How is the vomiting/emesis centers activated

A

several mechanisms:
-afferent fibers in the gut
-chemoreceptor trigger zone
-cerebral cortex
vestibular aparatus

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3
Q

What is the CTZ

A

area postrema response to blood-born substances
serotonin 5-HT3
dopamine D2
Muscarinic M1 receptors

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4
Q

what is vestibular apparatus activation

A

fibers into cerebellum
triggers release of Ach/histamine

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5
Q

what is gut activation of vomiting center

A

vagal afferent pathways to solitary tract nucleus to vomiting center
nerve stimulation of CTZ
D2, 5-HT3, and neurokinin 1 (NK1) receptors

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6
Q

what are the drug categories for nausea and vomiting

A

cholinergic/muscarinic antagonists
dopamine receptor antagonists
serotonin receptor antagonists
cannabinoids
histamine antagonists

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7
Q

what is the cholinergic antagonists for N/v

A

scopolamine (hyoscine)
patch/injectables

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8
Q

what is the MOA for scopolamine

A

blocks ach at parasympathetic sites (smooth muscle, secretory glands, CNS)
reduces histamine and serotonin activity

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9
Q

what is the PK for scopolamine

A

Onset: 6-8hours
Duration: 72 hours
Metabolism: hepatic
T1/2: 9.5 hours
peak: 24 hours
Excretion: less than 10% in urine

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10
Q

what are the SE of scopolamine

A

similar to atropine (Bradycardia (initially) - tachy, flushing, orthostatic hypotension)
cognitive impairement (drowiness/blurred vision)
psychosis and hallucinations

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11
Q

what are contraindications with scopolamine

A

contraindicated in narrow-angle glaucoma or with other agents containing belladonna
anticholinergic agents, other CNS depressants (hydrocodone), magnesium sulfate, nitroglycerin, potassium citrate, SSRIs, thiazide

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12
Q

What are the dopamine receptor antagonists medications for N/V

A

phenothiazines - prochlorperazine
Butyrophenones - haloperidol, droperidol
Benzamides - metoclopramide, trimethobenzamide

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13
Q

What is the MOA of dopamine receptor antagonist medications

A

acts primarily on CTZ and afferent pathway in the gut
antagonize D2 dopamine receptors in area postrema (midbrain) and peripheral sites
M1-muscarinic and H1-histamine blocking effects
metocloperamide has weake 5-HT3 blockage at higher doses

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14
Q

what are the SE of dopamine receptor antagonists medications

A

extrapyramidal reactions (dystonia), tardive dyskinesia, hypotension, EKG abnormaliteis, CNS effects, psychological effects, hyperprolactinemia

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15
Q

what are the major interactions with Dopamine receptor antagonists

A

TCAs, SSRIs, Antipsychotics, opioids, anticholinergics, anti-parkinson drugs, alcohol, potassium

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16
Q

what are the PK of Dopamine receptor antagonists

A

onset:
PO: 30-40 min
rectal: approx 60 minutes
duration: 3-4 hours for oral, 3-12 hours for rectal

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17
Q

what is the PK for metoclopramide

A

duration: 1-2 hours
T1/2: 5-6 hours in adults
excretion in urine
CYP2D6

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18
Q

what are the serotonin receptor antagonists

A

ondansetron (zofran)
granisetron

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19
Q

what is the MOA for ondansetron

A

blocks serotonin centrally (chemoreceptor trigger zone) and peripherally (vagal nerve terminals0

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20
Q

what is the PK for ondansetron

A

onset: aprox 30 min
metabolism: CYP pathways
T1/2: aprox 3-6 hours in adults
peaks: 1-2 hours
excretion in urine and feces

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21
Q

what are the SE of ondansetron

A

QT prolongation, dizzinness, confusion, SOB, constipation

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22
Q

what are the considerations for ondansetron

A

EKG monitoring, potassium and magensium elvels
watch for serotinin syndrome with serotoninergic drugs

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23
Q

what are the contraindications with ondansetron

A

amiodarone
cyp3a4 inducers
QT prolonging agents

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24
Q

what is the Canabinoid

A

Dronabinol

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25
what is the MOA of Dronabinol
activates cannabinoid receptors
26
what is the PK of Dronabinol
Onset: 30-60 min Peak 2-4 hours duration: 4-6 hours metabolism: hepatic T1/2: 4-5/25-36 hours
27
what are the SE of Cannabinoids
euphoria, CNS changes, abdominal pain, vomiting, flushing, palpitations, hypotension, xerostonia, vertgo
28
what are the special considerations of cannabinoids
monitor HR and BP psychiatric changes/CNS effects worsening N/V/abd pain may contain propylene glycol subastance use hx
29
what are contraindicatiosn of cannabinoids
alcohol anticholinergics CNS depresssants CYP3A4 inhibitors/inducers metronidazole disulfiram warfarin
30
what are the histmaine antagonist meds for N/v
promethazine mecizine dimenhydrinate
31
what is the MOA for promethazine
blocks mesolimbic dopaminergic receptors in postsynaptic sites. blocks release of hromones from the hypothalamus. blocks histmaine 1 receptors in brainstem
32
what are the PK of promethazine
ONset: IV: 5 min,PO/IM: 20 min duration: 4-6 hours metabolism: CYP T1/2: IM approx 10 hours, IV 9-15, supp 16-19 hours
33
what are the SE of promethazine
EKG changes anticholinergic effets CNS depressionm extrapyramidal efffects orthostatic hypotension photosensitivity
34
what is the MOA of meclizine
blocks H1 histamine receptor and prevents vasodilation, increased capillary permeability, bronchoconstriction, and spasmodic contraction of gastriintestinal smooth muscle. also depress labyrinth excitability and vesticular stimulation, and may affect the medullary chemoreceptors trigger zone
35
what is the PK of meclizine
onset; aprox 1 hour duration: approx 24 hours metabolism: hepatic T1.2": aprox 5-6 hours excretion: urine and feces
36
what are the SE of meclizine
sedation, headaches, vommiting, blurred vision
37
what is the MOA of dimenhydrinate
binds to H1 receptor sites in peripheral sites including GI tract, respiratory tracts and blood vessels. blocks chemoreceptor trigger zones dpresses layrthinine function and vestibular stimulation. central anticholinergic activity
38
what are the PK of dimnhydrinate
onset: up to 30 min for IM and oral duration: 4-6 hours metabolism: hepatic T1/2: 5-8 hours excretion: renal
39
what are the SE of dimenhydrinate
tachy, sedation, dizziness, xerostimia, anorexia, epigastric distress, blurred vision, thickened brochial secretion
40
what are the types of drugs for diarrhea and IBS-D
opioid agonists serotinin receptor modulators bile acid sequestriants anti-spasmodics antimicrobial agents
41
what is the MOA of opioid agnoists
activation of opioid receptors in the smooth msucle of the GI tract, alters periostalis by preventing smooth msucle contraciton and relaxation. reduced stool volume and can prevent electroylte depletion.
42
what are the opioid agonist medicatiosn
loperamide (imodium) diphenoxylate/atropine octreotide eluxadoline
43
what is the MOA of loperamide
also incresase IAS and EAS tone
44
what is the PK of loperamide
metabolism: hepatic t1/2: 9-14 hours excretion feces
45
what are the SE of loperamide
CONSTIPATION, dizziness, abdominal pain and cramping
46
what is the MOA of diphenoxylate/atropine
contains small amount of atropine to prevent abuse
47
what ist eh PK of diphenoxylate/atropine
onset: aprox 45 min metab: hepatic T1/2: 2.5 hours Excretion: feces and urine
48
what are the SE of diphenoxylate/atropine
flushing, tachy, CNS effects, xeroderma, vomiting, toxic megacolon, urinary retetnion
49
what is the MOA of Octreotide
inhibits serotonin release. inhibits secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide
50
what is the PK of octreotide
duration: 6-12 hours metab: hepatic t1/2: aprox 2 hours excretion: urine
51
what are the SE of octreotide
bradycardia, fatigue, HA, dizziness, pruruits, hyperglycemia, hypothyroidism, cholelithiasis, abdominal pain, diarrhea, constipation, biliary obstruction, URI, cardiac arrhythmias, depression
52
what is the MOA of eluxadoline
binds to mu, kappa, and delta opioid receptors in the intestinal lumen. decreases intestinal motility without causing constipation
53
what is the PK of eluxadoline
metab? t1/2: 4-6 hours peak 1.5 hours excretion: feces and urine
54
what are the SE of eluxadoline
dizziness, drowsiness, constipation, nausea, abodminal pian, vomiting, elevated LFTs, URI
55
what are the serotonin receptor modulators
alosetron and tegaserod
56
what is the MOA of alosetron
selective 5-HT3 agonist. acts on receptors in the enteric neurons in addition to receptors in other location centrally and peripherally. affects visceral pain, colonic transit and alters secretions in the GI tract
57
what is the PK of alosetron
metab: CYP t1/2: 1.5 hours peak 1 hour excretion: urine and feces
58
what are the SE of alosetron
constipation, fatigue, HA, abodminal pain, nausea
59
what is the MOA for bile acid sequestrants
bind to bile salts in the intestine. inhbiits reuptake of bile salts, increases fecal loss of bile salt bound on LDL cholesterol as well
60
what is the PK of bile acid sequestrants
onset: peak effect 21 days no absorption excreted in feces
61
what are the SE of bile acid sequestrants
abodminal pain, bloaitng, biliary colic, gallbladder calcifcation, melena, vomiting, dental erosion/discoloration, abnromal LFTs, tinnitus, bleeding issues
62
what are the antimicrobials
rifaximin metronidazole ciprofloxacin amoxicillin neomycin
63
what is the MOA of Rifaximin
binds to bacterial DNA dependent RNA polymerase, thus inhbiting RNA synthesis
64
what are the PK of Rifaximin
metabolism: CYP T1/2: 5-6 hours excretion in feces
65
what are the SE of rifaximin
peripheral edema, dizziness, fatigue, ascites, nausea, HA prurutis
66
what are the anti-spasmodics
hyoscyamine dicyclomine
67
what is the MOA of anti-spasmodics
blocks ach at parasympathetic receptors. antagonist of histamine and serotonin
68
what is the PK of anti-spasmodics
onset: 2-3 minutes duration: 4-6 hours metab: hepatic T1/2: 3.5 hours or 7 hours for longer acting excretion in urine
69
what are the SE of anti-spasmodics
tachy, mental status changes, abdominal pain, impotence, blurred vision, urinary retnetion, increased IOP
70
what are different medication types of constipation
stool softeners bulking laxative osmotic laxatives stimulant laxatives selective opioid antagoonists guanylate cyclase-c agonists
71
what is docusate sodium
stool softener
72
what is the MOA of docusate sodium
lowers the surface tension at the oil-water interface of the aeces, allowing water and lipids to penetrate the stool this helsp to hydrate and soften the fecal materaial, facilitating natural defecation
73
what is the PK of docusate sodium
onset: 12-72 hours excretion in feces
74
what are the SE of docustate sodium
throat irritation
75
what are bulking laxatives
methycellulose psyllium husk powder wheat dextrin calcium polycarbophil
76
what is the MOA of bulking laxatives
absorb and retain water in the intestine, thus increasing the mass of stool. this promotes peristaliss through distension of intestinal lumen
77
what are the SE of bulking laxatives
bloating, flatulence, GI distress
78
what are the osmotic laxatimes
saline laxatives - magnesium oxide, sodium phosphate lactulose polyethylene glycol glycerin
79
what is the MOA of saline laxatives
retain water in intestine, thus increaseing intraluminal pressure and promotion of peristalsis
80
what are the SE of saline laxatives
blaoting abdominal pain apthous stomatitis hypokalemia and hypophosphatemia
81
what is the MOA of lactulose
disaccharide that promotes fluid retention in intestine, thus increaseing intraluminal pressure and promoting peristalsis
82
what is the PK of lactulose
colonic microbiota convert the sugars into lactic and aecitic acid. excreted in feces
83
what are the SE of lactulose
dehydration, hypernatremia, hypokalemia, bloaitng, nausea, abdominal cramping, diarrhea
84
what is the SE of polyethrylene glycol
diarrhea, faltulene, abdominal pain, nausea
85
what is the PK of glycerin suppository
onset 15-30 min. poorly absorbed
86
what are the SE of glycerin suppository
abodminal cramping, bloating, diarrhea, irritation, tenesmus
87
what are the stimulant laxatives
bisacodyl and sennosides
88
what is the MOA of stimulant laxatives
alter fluid excretion by acting directly on the cells of the intestinal mucosa. increase motility by acting on cells
89
what are the opiod antagonists
naloxegol methylnaltrexone
90
what is the MOA of naloxegol
Mu opioid receptor antagonists. bound to polyethylene glycol to prevent crossing BBB. blocks the effects of opioids on GI tract, thus decreaseing constipation
91
what is the PK of naloxegol
absorbed reapidly metabolized via YCP t1/2: 6-11 hours peaks less than 2 hours excreted in feces and urine
92
what is the MOA of methylnaloxegol
same as naloxegol. derivative of naltrexone
93
what is the pK of methylnaloxegol
T1/2: 15 hours peaks 30 min to 1.5 hours excreted in urine andfeces
94
what are the IBS-C medications
Lubiprostone Linaclotide
95
what is the MOA of Lubiprostone
activates chloride channels and increases fluid secretion by the cells int he intestinal membrane. also counteracts the antisecretory effect of opioids
96
what is the MOA of Linaclotide
acts on guanylate cyclase on the epithelium of the intestine, icnreasing cyclinc guanosine monophosphate. the stimuates the chloride and bicarbonate secretion and intraluminal pressure, promoting peristalsis. cGMP is thought to decrease visceral pain

Pharm 3 Module 2: GI (4 decks)

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