ANTI – EMETICS
PHARMACOLOGY & CLASSIFICATION
Name – Yogeeta
EMESIS
🌷 It is protective mechanism which serves to eliminate harmful substances from the
stomach.
🌷 Occurs due to stimulation of the emetic center situated in the medulla oblongata.
🌷 Multiple pathways can rlicit vomiting.
🌷 CTZ and NTS are the most important relay areas for afferent impulsesarisibg from
GIT, throat and other viscera.
🌷 CTZ also accessible to blood borne drugs, mediators, hormones, toxins, etc.
🤮 EMETICS 🤮
🌼 These are the drugs which are used to evoke vomiting.
1️⃣ Centrally acting – Apomorphine ( directly stimulate the CTZ or VC )
2️⃣ Peripherally acting – mustard , potassium tartrate, and hypertonic NaCl (
concentrated solutions )
3️⃣ Both – Ipecacuanha ( stimulate the VC by irritating gastric & duodenal mucosa
which stimulate afferent fibres of vagus nerve)
👉🏻 Apomorphine 💉
✏️ Semi synthetic derivative of morphine.
✏️ Given IM or SC, acts centrally.
✏️ Dose is 6 mg ( 2-8 mg )
✏️ Induces vomiting in 5-10 minutes.
✏️ Not given if respiration is depressed.
👉🏻 Ipecacuanha 🧂
✏️ Contains two alkaloids – emetine &
cephaeline .
✏️ Used as syrup ipecac.
✏️ Produces effect in 15 minutes.
✏️ Acts by irritating gastric mucosa & through
CTZ centre.
✏️ Dose – 5 ml in infants, 10-15 ml in children,
15-20 in adults.
🌼 CONTRAINDICATIONS 🚫
• 🌸 Corrosive ( acid, alkali ) poisoning.
• 🌸 CNS stimulant drug poisoning.
• 🌸 Kerosine ( petroleum ) poisoning.
• 🌸 Unconscious Patient
• 🌸 Morphine or phenothiazine poisoning.
🤮 INTRODUCTION – ANTI EMETICS
🌿 Two Centres
- Vomiting Centre (VC)
- Chemoreceptor trigger zone (CTZ)
🌿 Both near to the floor of the fourth ventricle, close to the vital centres.
🌿 VC is within the BBB
🌿 CTZ outside in the area postrema & they both are connected together.
🌿 Def. - A group of drugs which are used to control the nausea and vomiting.
🏥 CLASSIFICATION
🌺 Anti-Cholinergics
• Hyoscine
• Dicyclomine
🌺 H-1
Antigistaminics
• Promethazine
• Diphenhydramine
• Doxylamine
• Meclozine
Neuroleptices
(D-2 blockers)
• Chlorpromazine
• Triflupromazine
• Prochlorperazine
CONTD…. 💊💉
🌺 Prokinetic Drugs
• Metoclopramide
• Domeperidone
• Cisapride
• Mosapride
• itopride
🌺 5-HT3 antagonists
• Ondansetron
• Granisetron
• Palonosetron
• Ramosetron
🌺 Adjuvant-
antiemetics
• Dexamethasone
• Benzodiazepines
• Dronabinol
1. ANTICHOLINERGICS
👉🏻 HYOSCINE –
• 0.2 – 0.4 mg oral, i.m.
• Most effective for motion sickness
• Brief duration of action – produce sedation, dry mouth and anticholinergic side
effects.
👉🏻 DICYCLOMINE –
• 10-20 mg oral
• Prophylaxis of morning & motion sickness
🍁H-1 ANTIHISTAMINICS🤮
• Some antihistaminics are antiemetic like promethazine, diphenhydramine,
dimenhydinate.
• They protect from motion sickness for 4-6 hours.
• Produce sedation & dryness of mouth so driving should not be proceede after having
these drugs.
• Combination of these with other antiemetics has been used in chemotherapy-
induced nausea and vomiting (CINV)
🍁NEUROLEPTICS🤮
• The older neuroleptics ( phenothiazines, haloperidol) are potent antiemetics and
sedative.
• They act by blocking D2 receptors in the CTZ; antagonize apomorphine induced
vomiting.
👉🏻 Useful in –
- Drug induced vomiting
- Post operative nausea and vomiting
- Radiation sickness vomiting
🍁PROKINETIC DRUGS 💉
• These drugs promote GIT transit and speed gastric emptying by rnhancing
coordinated propulsive motility.
• They acts through both dopaminergic and serotonergic receptors.
• D-2 antagonism
• 5-HT3 agonism
• Sedation, dizziness, loose stools, muscle dystonias are the main side effects.
• Long term use can cause parkinsonism, galactorrhoea and gynaecomastia.
🍁5 – HT3 ANTAGONISTS 💊
• Ondansetron is prototype developed to control cancer chemotherapy induced
vomiting.
• Cytotoxic drugs produces nausea & vomiting by causing cellular damage, which
releases mediators including 5- HT from intestinal mucosa resulting in transmission
of impulses to the NTS and CTZ.
• Oral bioavailability of ondansetron is 60-70 % due to first pass metabolism.
• Elimenated by urine and faeces t1/2 is 3-5 hrs.
🌷THANK-YOU🌷

ANTI- EMETICS

  • 1.
    ANTI – EMETICS PHARMACOLOGY& CLASSIFICATION Name – Yogeeta
  • 2.
    EMESIS 🌷 It isprotective mechanism which serves to eliminate harmful substances from the stomach. 🌷 Occurs due to stimulation of the emetic center situated in the medulla oblongata. 🌷 Multiple pathways can rlicit vomiting. 🌷 CTZ and NTS are the most important relay areas for afferent impulsesarisibg from GIT, throat and other viscera. 🌷 CTZ also accessible to blood borne drugs, mediators, hormones, toxins, etc.
  • 3.
    🤮 EMETICS 🤮 🌼These are the drugs which are used to evoke vomiting. 1️⃣ Centrally acting – Apomorphine ( directly stimulate the CTZ or VC ) 2️⃣ Peripherally acting – mustard , potassium tartrate, and hypertonic NaCl ( concentrated solutions ) 3️⃣ Both – Ipecacuanha ( stimulate the VC by irritating gastric & duodenal mucosa which stimulate afferent fibres of vagus nerve)
  • 4.
    👉🏻 Apomorphine 💉 ✏️Semi synthetic derivative of morphine. ✏️ Given IM or SC, acts centrally. ✏️ Dose is 6 mg ( 2-8 mg ) ✏️ Induces vomiting in 5-10 minutes. ✏️ Not given if respiration is depressed. 👉🏻 Ipecacuanha 🧂 ✏️ Contains two alkaloids – emetine & cephaeline . ✏️ Used as syrup ipecac. ✏️ Produces effect in 15 minutes. ✏️ Acts by irritating gastric mucosa & through CTZ centre. ✏️ Dose – 5 ml in infants, 10-15 ml in children, 15-20 in adults.
  • 5.
    🌼 CONTRAINDICATIONS 🚫 •🌸 Corrosive ( acid, alkali ) poisoning. • 🌸 CNS stimulant drug poisoning. • 🌸 Kerosine ( petroleum ) poisoning. • 🌸 Unconscious Patient • 🌸 Morphine or phenothiazine poisoning.
  • 6.
    🤮 INTRODUCTION –ANTI EMETICS 🌿 Two Centres - Vomiting Centre (VC) - Chemoreceptor trigger zone (CTZ) 🌿 Both near to the floor of the fourth ventricle, close to the vital centres. 🌿 VC is within the BBB 🌿 CTZ outside in the area postrema & they both are connected together. 🌿 Def. - A group of drugs which are used to control the nausea and vomiting.
  • 8.
    🏥 CLASSIFICATION 🌺 Anti-Cholinergics •Hyoscine • Dicyclomine 🌺 H-1 Antigistaminics • Promethazine • Diphenhydramine • Doxylamine • Meclozine Neuroleptices (D-2 blockers) • Chlorpromazine • Triflupromazine • Prochlorperazine
  • 9.
    CONTD…. 💊💉 🌺 ProkineticDrugs • Metoclopramide • Domeperidone • Cisapride • Mosapride • itopride 🌺 5-HT3 antagonists • Ondansetron • Granisetron • Palonosetron • Ramosetron 🌺 Adjuvant- antiemetics • Dexamethasone • Benzodiazepines • Dronabinol
  • 10.
    1. ANTICHOLINERGICS 👉🏻 HYOSCINE– • 0.2 – 0.4 mg oral, i.m. • Most effective for motion sickness • Brief duration of action – produce sedation, dry mouth and anticholinergic side effects. 👉🏻 DICYCLOMINE – • 10-20 mg oral • Prophylaxis of morning & motion sickness
  • 11.
    🍁H-1 ANTIHISTAMINICS🤮 • Someantihistaminics are antiemetic like promethazine, diphenhydramine, dimenhydinate. • They protect from motion sickness for 4-6 hours. • Produce sedation & dryness of mouth so driving should not be proceede after having these drugs. • Combination of these with other antiemetics has been used in chemotherapy- induced nausea and vomiting (CINV)
  • 12.
    🍁NEUROLEPTICS🤮 • The olderneuroleptics ( phenothiazines, haloperidol) are potent antiemetics and sedative. • They act by blocking D2 receptors in the CTZ; antagonize apomorphine induced vomiting. 👉🏻 Useful in – - Drug induced vomiting - Post operative nausea and vomiting - Radiation sickness vomiting
  • 13.
    🍁PROKINETIC DRUGS 💉 •These drugs promote GIT transit and speed gastric emptying by rnhancing coordinated propulsive motility. • They acts through both dopaminergic and serotonergic receptors. • D-2 antagonism • 5-HT3 agonism • Sedation, dizziness, loose stools, muscle dystonias are the main side effects. • Long term use can cause parkinsonism, galactorrhoea and gynaecomastia.
  • 14.
    🍁5 – HT3ANTAGONISTS 💊 • Ondansetron is prototype developed to control cancer chemotherapy induced vomiting. • Cytotoxic drugs produces nausea & vomiting by causing cellular damage, which releases mediators including 5- HT from intestinal mucosa resulting in transmission of impulses to the NTS and CTZ. • Oral bioavailability of ondansetron is 60-70 % due to first pass metabolism. • Elimenated by urine and faeces t1/2 is 3-5 hrs.
  • 15.