SEROTONIN RECEPTORS Flashcards

1
Q

There are currently _____serontonin

A

14 serotonin receptor subtypes

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2
Q

All except ______are GS protein

A

5-HT 3 receptors,

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3
Q

5 HT3 receptors subtype is located in both the

A

central and peripheral nervous systems

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4
Q

In CNS highest concentration found in

A

Chemoreceptor ciliary Tract

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5
Q

Selective 5-HT3 receptor antagonists

A

Selectively antagonize the 5-HT3 receptor subtype

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6
Q

Selective 5-HT3 receptor antagonists

A

Dolansetron
Granisetron
ondansetron equally efficacious at equivalent doses

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7
Q

Dolansetron
Granisetron
ondansetron

A

both available in oral and IV

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8
Q

Only available in IV

A

PALONOSETRON

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9
Q

MOA of 5-HT3 receptor antagnosis

A

Selectively bind and inhibit 5-HT 3 receipts blocking the binding of serotonin at this receptor subtype and subsequent N/V
Peripherally and centrally

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10
Q

These agents are not effective in

A

motion induced N/V from vestibular stimulation

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11
Q

UNIQUE long half life

A

PALONOSETRON (ALOXI) 40 hours

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12
Q

PALONOSETRON(ALOXI)

A

Takes long ot work

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13
Q

Most common side effects

A

Headache (MOST COMMON)

Dose dependent QT prolongation

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14
Q

New warning for 5-HT3 receptor antagonists.

A

The development of serotonin syndrome reported with 5-HT3 receptors antagonist

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15
Q

New warning for 5-HT3 receptor antagonists.

A

The development of serotonin syndrome reported with 5-HT3 receptors antagonist.
reported with repeated administration, cases were fatal

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16
Q

The prototypical selective 5-HT3 receptor antagonists

A

ONdansetron 4-8mg IVP 2-4 minuts

17
Q

Ondansetron dose < or equal to 40kg

A

0.1mg/kg over 2-5 minuts for prophylaxis

18
Q

Ondansetron dose > or equal to 40kg

A

4mg IVP over 2-5 minutes for phorphylaxis

19
Q

Patients with severe hepatic impairment

A

Total dose of 8 mg

20
Q

Drug-drug interactions

A

APOMORPHINE : profound hypotension and LOC can occur and for this reason ONDANSETRON is CONTRAINDICATED with concomittant use.

21
Q

DOLASETRON metabolism

***KNOW ACTIVE METABOLITE

A

Active, not a prodrug completely metabolized by plasma carbonyl reductase enzyme to an active metabolite.
HYDRODOLASETRON

22
Q

PONV prophylaxis DOLASETRON

A

100mg PO 2 hours before surgery
12.5 mg IV 15 mins before surgery
15 min before cessation

23
Q

PONV treatment ***(compare tx vs prophylaxis)

A

12.5 mg IV as soon as NV presents

24
Q

PALONOSETRON (ALOXI)

A

good drug, last longer

DO NOT USE BECAUSE OF “cost” 200-300 a dose

25
Q

PALONOSETRON (ALOXI) not used because

A

takes forever to work

not for acute