Dr. A.

ALISHER MD PhD AL SABAH & ZAIH HOSPITALS, MOH, KUWAIT

Ondansetron

Ondansetron

Chemical data
Formula C18H19N3O

Mol. mass

293.4 g/mol

Ondansetron

Ondansetron
Pharmacokinetic data
Bioavailability ~60%

Protein binding
Metabolism Half-life Excretion

70%-76%
Hepatic (CYP3A4, CYP1A2,CYP2D6) 5.7 hours Renal

Ondansetron

Ondansetron
To treat nausea and vomiting following

chemotherapy; PONV Its effects are thought to be on both peripheral and central nerves.

Ondansetron
Reduce the activity of the Vagus

Nerve; Which is a nerve that activates the vomiting center in the medulla oblongata; A blockage of serotonin receptors in the chemoreceptor trigger zone.

Ondansetron

Ondansetron
It does not have much effect on

vomiting due to motion sickness.

Ondansetron
Ondansetron as developed in 1984 by scientists of the Glaxo's Laboratories

in London, UK. It is marketed by GlaxoSmithKline (GSK) under the trade name Zofran;

ONDANSETRON
9-methyl-3-((2-methyl-1H-imidazol-1-

yl)methyl)-2,3-dihydro-1H-carbazol-4(9H)one

Use in adult and pediatric

Zofran (Ondansetron Hydrochloride)

pts. Dose:0.1 mg/kg for children 2-12 yrs. If BW < 40 kg

NAUSEA / VOMITING
For patients experiencing Nausea and/or Vomiting As a result of disease Medications or Acute Motion Sickness

NAUSEA / VOMITING
Ondansetron: 4 mg IV/ IM

(Slow IV - 2-5 min.) (Repeat x 1 if no relief after 5 min.)

Post anesthetic Shivering

The efficacy of Ondansetron for Postanesthetic Shivering, a common

occurrence after surgery.

Post anesthetic Shivering

Ondansetron was found to be as effective as Pethidine

(Meperidine, Demerol) when given as a single IV dose before anesthesia.

Ondansetron blocks the 5HT3 receptor in the enteric

Irritable Bowel Syndrome

nervous system, and thereby reduces colonic contractions, sensory perception, and motility.

Irritable Bowel Syndrome

5-HT3 antagonist, have

been shown to have this effect, which positively impacts IBS with diarrhea (IBS-D)

Irritable Bowel Syndrome

Ondansetron has been

effective in treating diarrhea-predominant IBS

Adult Emetogenic
Chemotherapy & Radiotherapy

8 mg PO, 1-2 hrs prior to

treatment Followed by 8 mg PO 12 hrs later.

Adult Emetogenic
Chemotherapy & Radiotherapy

8 mg IV before treatment

To protect against delayed or prolonged emesis after

the 1st 24 hr, continued PO PO: 8 mg BD for up to 5 days.

Highly Emetogenic Chemotherapy

8-mg IV/IM before chemotherapy.
Doses > 8 mg & up to 32 mg by IV

infusion. Alternatively, 8 mg by slow IV/IM before chemotherapy,

Highly Emetogenic Chemotherapy

Followed by 2 further IV/IM doses of 8 mg 2-4 hr apart or By infusion of 1 mg/hr for up to 24 hrs.
8 mg BD PO for up to 5 days after

a course of treatment.

PONV Adult Patients

Prevention: 16 mg orally 1 hr.

prior to GA or
Single dose of 4 mg IM or slow IV

at induction of GA.

PONV Adult Patients

Treatment: Single dose of 4 mg IM

or slow IV.
Patient with Hepatic Impairment Max: 8 mg daily.

Children:
Prevention: 0.1 mg/kg
4 mg IV before, at or after induction of

GA Treatment:0.1 mg/kg Up to a max: 4 mg IV

Observed During Clinical Practice

Cardiovascular: Rarely and

predominantly with IV Ondansetron; Transient ECG changes including QT interval prolongation.

Observed During Clinical Practice

Flushing Rare cases of hypersensitivity

reactions

Observed During Clinical Practice

Severe Anaphylaxis Anaphylactoid reactions Angioedema

Observed During Clinical Practice

Bronchospasm,

Shortness of breath,
Hypotension,

Laryngeal edema,
Stridor

Observed During Clinical Practice

Laryngospasm

Shock
Cardiopulmonary Arrest have

occurred during allergic reactions in pts receiving IV Ondansetron.

Observed During Clinical Practice

Hepatobiliary: Liver enzyme

abnormalities
Lower Respiratory: Hiccups

Observed During Clinical Practice

Neurology: Oculogyric crisis, appearing alone, as well as with

other dystonic reactions

Skin: Urticaria

Special Senses: Eye Disorders:

Cases of transient blindness,

predominantly during IV administration; These cases of transient blindness were to resolve within a few minutes up to 48 hrs.

Mode of Action
Serotonin (5-HT) receptor antagonist Blocking action take place in CNS at area

postema (chemoreceptor trigger zone) and

In peripheral nervous system on terminals of

Vagus Nerve

Indications
Nausea and

Vomiting

Contraindications:

Hypersensitive to drug MH PE

ACS

Dosage
4 mg slow IV (over 2-5 min.) or 4 mg IM

Precautions
In Pregnant Women

Breast-feeding Women
Cross into breast milk Cause syncope if pushed IV to fast

Pharmacokinetics
Absorption: Variable;

Bioavailability: 50- 60%;

Distribution: 70 - 76% is

protein bound

Pharmacokinetics
Metabolism: Extensively metabolized.

Excretion:
Primarily excreted in urine
Some small amounts

excreted in feces Breast milk

Pharmacokinetics
Half-life : 4 hrs.

On 27.07.2011: 120 Patients have Side Effects when taking Zofran

Top 10 overall Zofran side effects:

Nausea

15

Nausea and Vomiting

11

Pyrexia (Fever)

11

Hypotension

10

Confusion

Neutropenia (Agranulocytosis)

Dyspnoea (Breathing difficulty)

Dysphagia (Swallowing difficulty)

Cough

10

Dermatitis Nos

Top 10 long term Zofran Side Effects:

Name 1 2 Nausea Hypersomnia (Drowsiness) Anxiety Aggravated (Stress and anxiety) Headache Somnolence (Drowsiness) Acne Promethazine Hydrochloride Plain Confusion

Number of reports 3 2

3
4 5

2
2 2

6
7 8

1
1 1

9
10

Swelling Of Feet And Legs

Cancer Pain

1
1

Side Effects
Drowsiness

Dizziness
Fatigue

Side Effects
Headache

Impaired Wound Healing

Itch

Side Effects
Bradicardia Fever Anxiety

Agitation