SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI)

• Inhibition of the serotonin transporter (SERT) 

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI) MOA

Antidepressant

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI) use

• Fluoxetine (Prozac) - prototype & racemic form

• Sertraline (Zoloft) - racemic form

• Citalopram (Celexa) - racemic form

• Paroxetine (Paxil) - not optically active 

• Fluvoxamine (Luvox, Faverin) - not optically active

• Escitalopram (Lexapro) - S - enantiomer of Citalopram

high lipophilic SSRIs

• Dexfenfluramine (Redux) - an appetite suppressant

SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRI) examples

Fluoxetine (Prozac)

Sertraline (Zoloft)

Citalopram (Celexa)

Racemic form

Prozac

Fluoxetine BN

Zoloft

Sertraline BN

Fluoxetine (Prozac)

• prototype & racemic form

Celexa

Citalopram BN

Paroxetine (Paxil)

Fluvoxamine (Luvox, Faverin)

not optically active

Paxil

Paroxetine BN

Luvox, Faverin

Fluvoxamine BN

Escitalopram (Lexapro)

• S - enantiomer of Citalopram

Lexapro

Escitalopram Lexapro BN

Redux

Dexfenfluramine BN

Dexfenfluramine (Redux)

• an appetite suppressant

Bulimia

Fluoxetine (Prozac) tx

Fluoxetine (Prozac) and paroxetine

• potent inhibitors of CYP2D6 

Fluvoxamine

• inhibitor of CYP3A4 

ANTI EMESIS

They are useful in the treatment of vomiting associated with motion sickness (OTC) and chemotherapy(Rx).

ANTICHOLINERGIC

ANTIHISTAMINES

DOPAMINE ANTAGONIST

SETRONS

CANNABINOIDS (SYNTHETIC THC ANALOG)

ANTI EMESIS

Scopolamine (Hyoscine)

ANTICHOLINERGIC

• Antagonize receptor of acetylcholine receptor they reduce the excitability of labyrinth in muscarinic receptors and depress the conduction from the vestibular apparatus to the vomiting center

ANTICHOLINERGIC MOA

• treat motion sickness and in preoperative operation

Scopolamine (Hyoscine) use

• Drowsiness, dry mouth, and blurred vision

Scopolamine (Hyoscine) A/E

• Diphenhydramine

• Meclizine

• Cyclizine

• Dimenhydrinate

• Promethazine

ANTIHISTAMINES

• act by inhibiting cholinergic pathways of the vestibular apparatus 

by receptor crossover

ANTIHISTAMINES MOA

• for motion sickness, true vertigo and nausea in pregnancy

ANTIHISTAMINES Use

sedation and dry mouth

ANTIHISTAMINES A/E

• Metoclopramide (Plasil)

• Domperidone (Motilium)

DOPAMINE ANTAGONIST

• Treat nausea due to chemotherapy (use of cisplatin and doxorubicin) and narcotic induced vomiting (Metoclopramide)

• Motion sickness (Domperidone)

DOPAMINE ANTAGONIST use

• Metoclopramide (Plasil)

• Domperidone (Motilium)

• Sedation, Diarrhea, extrapyramidal effects (movement disorder), elevated prolactin secretion (responsible for milk production) (⬆ prolectin = hyperprolactinemia)

DOPAMINE ANTAGONIST A/E

• Metoclopramide (Plasil)

• Domperidone (Motilium)

• (Motilium)

• Domperidone BN

• (Plasil)

• Metoclopramide BN

Treat nausea due to chemotherapy

use of cisplatin and doxorubicin)

narcotic induced vomiting

(Metoclopramide) use

Motion sickness

(Domperidone) use

• Ondansetron (Zofran)

• Granisetron (Kytril)

• Palonosetron

• Alosetron

SETRONS

5HT3

SETRONS antagonist

(Zofran)

Ondansetron BN

(Kytril)

Granisetron BN

Ondansetron (Zofran)

• more effective than metoclopramide, against nausea induced by high dose cisplatin. (Adv: No extrapyramidal effect)

No extrapyramidal effect

Ondansetron. (Zofran) adv.

• Granisetron (Kytril)

• has a greater affinity for 5-HT3 receptors than ondansetron (zofran)

headache

SETRON COMMON A/E

THC Delta-9-tetrahydrocannabinol

CANNABINOIDS (SYNTHETIC THC ANALOG)

THC Delta-9-tetrahydrocannabinol

-psychoactive component of Marijuana

• Dronabinol (Marinol) (approved by the FDA)

• Nabilone (synthetic derivative)

• Dronabinol (Marinol) & Nabilone does not contain the components of full Marijuana just a synthetic analog

CANNABINOIDS (SYNTHETIC THC ANALOG) ex.

• chemotherapy induced nausea administered either as an oral preparation or smoked as a cigarette (if other drug is ineffective only)

CANNABINOIDS (SYNTHETIC THC ANALOG)

• THC Delta-9-tetrahydrocannabinol Use

• may act by inhibiting the vomiting center

CANNABINOIDS (SYNTHETIC THC ANALOG)

• THC Delta-9-tetrahydrocannabinol MOA

• sedation, psychoactive effects, dry mouth, and orthostatic hypotension

CANNABINOIDS (SYNTHETIC THC ANALOG)

• THC Delta-9-tetrahydrocannabinol A/E

Dexamethasone and Betamethasone Methylprednisolone

(Solu-medrol)

Glucocorticoids ex

(Solu-medrol)

Methylprednisolone BN

Glucocorticoids

● Example: Dexamethasone and Betamethasone Methylprednisolone (Solu-medrol)

can be effective as a treatment for vomiting caused by highly emetic agents. high doses are given as an intravenous bolus or orally for delayed nausea often combined with other antiemetics

may cause adrenal suppression and metabolic disturbances

Glucocorticoids

● Example: Dexamethasone and Betamethasone Methylprednisolone (Solu-medrol) A/E

Lorazepam (Ativan)

● Diazepam (Valium)

Benzodiazepine

Ativan

Lorazepam BN

Valium

Diazepam BN

GABA(gamma-amino butyric acid) Agonist (type I receptor)

◆ Increase frequency of chloride ion channel opening

Benzodiazepine MOA

Acts as anxiolytic agents to reduce anticipatory emesis diazepam is useful as a treatment for vertigo and it controls symptoms of Meniere’s disease (disorder in inner ear that can lead to dizzy spells (vertigo) and hearing loss)

Benzodiazepine

● Lorazepam (Ativan)

● Diazepam (Valium) USE

anterograde amnesia which lasts for 4-6 hours

Benzodiazepine

● Lorazepam (Ativan)

● Diazepam (Valium) A/E