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GI > Upper GI Pharm part 2 > Flashcards

Upper GI Pharm part 2 Flashcards

1
Q

how are antiemetics catagorized?

A

according to the receptor on which they are proposed to act. However, there can be considerable overlap in multiple receptor type activation

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2
Q

treatment and prevention of the nausea and emesis associated with cancer chemotherapy

A

Use of several anti-emetic agents from different pharmacological classes may be used in combination.

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3
Q

Scopolamine is what type of antiemetic

A

Anticholinergic agent (muscarinic receptor antagonist)

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4
Q

Historic and effective for the prevention and treatment of motion sickness (prevention of postoperative nausea and vomiting)

A

Scopolamine (given as a transdermal patch)

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5
Q

Dimenhydrinate is what type of anti-emetic?

A

Histamine-1 blocker (antihistamine)

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6
Q

MOA for Dimenhydrinate

A

Histamine H1 antagonist. Some anti-muscarinic activity. Acts at vestibular afferents and within the brainstem.

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7
Q

Use of Dimenhydrinate

A

prevention and treatment of motion sickness

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8
Q

Granisentron and Ondansetron act on what receptor?

A

anti-serotoin; 5-HT3 antagonist

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9
Q

most widely used drugs for chemotherapy-induced emesis. These agents areavailable as tablets, oral solution, and intravenous preparations.

A

Ondansetron and Granisentron

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10
Q

MOA of granisentron and Ondansetron

A

5-HT3 receptors are present in several sites involved in emesis; vagal afferents, the STN and the area postrema. Serotonin is released by ECL cells of the small intestine in response to hemotherapeutic agents and may stimulate vagal afferents (via 5-HT3 receptors) to initiate the vomiting reflex.

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11
Q

Metabolism of Granisentron and Ondansetron

A

metabolized in the liver followed by glucuronide or sulfate conjugation

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12
Q

Uses of Granisentron and Ondansetron

A

Chemotherapy-induced nausea, nausea secondary to upper abdominal irradiation, hyperemesis of pregnancy, and to a lesser degree, postoperative nausea, but not
against motion sickness

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13
Q

Dopamine2 receptor antagonists

A

Prochlorperazine

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14
Q

MOA of Prochlorperazine

A

Principal mechanism is D2 receptor antagonism at the CTZ; Also some anticholinergic, antihistamine activity

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15
Q

“general-purpose” anti- emetics. Not uniformly effective in cancer chemotherapy induced emesis.

A

Prochlorperazine

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16
Q

Where is prochlorperazine metabolized? Side effects?

A

liver

sides = restlessness

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17
Q

highly lipid-soluble and is absorbed readily after oral administration. It is highly protein bound.

A

Dronabinol

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18
Q

MOA of Dronabinol

A

probably relates to neuronal CB1 receptor activation.

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19
Q

Recommended uses for Dronabinol

A

prophylactic agent in chemotherapy-induced emesis refractory to other treatments, treatment of anorexia associated with weight loss in AIDS patients.

20
Q

Side effects of Dronabinol (more so in elderly)

A

palpitations, tachycardia, vasodilation/facial flushing, dysphoria, vertigo, dizziness, lack of concentration, depersonalization, etc

21
Q

Metabolism of Dronabinol

A

Liver, active and inactive metabolites are formed

22
Q

Glucocorticoids such as______ can be useful adjuncts in the treatment of nausea in patients with cancer, possibly by suppressing tumor inflammation and prostaglandin production.

A

dexamethasone

23
Q

Substance P receptor (NK1) antagonist

A

Aprepitant

24
Q

MOA of Aprepitant

A

Inhibits substance P/NK1 receptors

25
Q

Uses of Aprepitant

A

Used in combination with other antiemetics (5-HT3 antagonist and a corticosteroid) for acute and delayed nausea and vomiting associated with chemotherapy,post-operative nausea

26
Q

broken down by CYP3A4 and bound exclusively to plasma protein

A

Aprepitant

27
Q

Agents that promote gastric emptying and GI motility by enhancing coordination.

A

Prokinetic agents

28
Q

What makes a prokinetic agent a useful one?

A

Useful prokinetic agents act “upstream” of

ACh, at receptor sites on the motor neuron, or indirectly, on neurons or non-neuronal cells one or two orders removed

29
Q

dopamine2 antagonist, however

may interact with serotonin receptors.

A

Metoclopramide

30
Q

suppression of ACh release from myenteric

motor neurons, are mediated by _________receptors.

A

D2 dopaminergic

31
Q

How are DA antagonists better then prokinetic agents?

A

antagonizing the inhibitory effect of dopamine on myenteric motor neurons, DA receptor antagonists are effective as prokinetic agents; they have the additional advantage of relieving nausea and vomiting by antagonism of DA receptors in the chemoreceptor trigger zone.

32
Q

MOA of DA antagonists like Metoclopramide

A

In addition to D2 receptor antagonist, its actions may involve 5-HT4 receptor agonism, vagal and central 5-HT3 antagonism and possible sensitization of muscarinic
receptors on smooth muscle.

33
Q

Where does metoclopramide work best?

A

upper digestive tract

34
Q

What can we use to tx diabetic gastroparesis; gastroesophageal reflux

A

oral metoclopramide

35
Q

When given parenterally, what does Metoclopramide help with?

A

gastroparesis and nausea and vomiting

36
Q

Metabolism of Metoclopramide

A

sulfation and glucuronide conjugation by the liver

37
Q

Side effects of metoclopramide

A

Tardive dyskinesia, dystonias

38
Q

is a prokinetic agent (complex actions) used for severe GERD and diabetic gastroparesis.

A

Metoclopramide

39
Q

are 5-HT3 blockers which attenuate vomiting by both action at CTZ and visceral afferents.

A

Ondansetron and Granisetron

40
Q

a dopamine2-antagonist used to treat nausea and vomiting.

A

Prochlorperazine

41
Q

is tetrahydrocannabinol (marijuana) used to treat chemotherapy-induced vomiting centrally perhaps acting at the vomiting center in the medulla. Used in cases where other therapiesare ineffective

A

Dronabinol

42
Q

is a histamine-1 blocker. Used to treat motion-induced vomiting.

A

Dimenhydrinate

43
Q

is an antimuscarinic agent and is the historical treatment for motion sickness. It acts on the cortex & inner ear.

A

Scopolamine

44
Q

is a substance P receptor antagonist. Used in combination therapy for the treatment of chemotherapy associated nausea

A

Aprepitant

45
Q

useful in the combination of other anti-nausea medications in the treatment of nausea in patients with cancer.

A

Dexamethasone

GI (14 decks)

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