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Anti-Emetics and Prokinetics
Moderator: Dr. D.A.Rizvi
Presentor: Dr. Roohana Hasan
Emesis and its causes
Pathophysiology of Emesis
Emetics
Anti emetics
Therapeutic uses of Anti-emetics
Special topics
 Motion sickness
Emesis in pregnancy
Chemotherapy induced vomiting
Post operative nausea and vomiting
Vomiting (Emesis) is the forceful expulsion of
contents of the stomach and often, the proximal
small intestine
Vomiting is a complex reflex involving both
autonomic and somatic neural pathways.
 Vomiting is a complex process that consists of
 (gastric relaxation and
retroperistalsis),
 (rhythmic action of respiratory muscles
preceding vomiting and consisting of contraction of
abdominal and intercostal muscles and diaphragm against
a closed glottis),
 (intense contraction of the abdominal
muscles and relaxation of the upper esophageal
sphincter).
Pre-ejection Phase
Retching
Ejection
Antiemetics and prokinetics by dr.roohna
 The “chemoreceptor trigger zone” or area
postrema is located at the caudal end of the
fourth ventricle.
 This is outside the blood-brain barrier but is
accessible to emetogenic stimuli in the blood or
cerebrospinal fluid.
 The chemoreceptor trigger zone is rich in
dopamine D 2 receptors and opioid receptors,
and possibly serotonin 5-HT 3 receptors and NK 1
receptors.
Antiemetics and prokinetics by dr.roohna
 These are drugs used to evoke
vomiting.
 Act on CTZ : Apomorphine
 Act reflexly and on CTZ : Ipecacuanha
EMETICS
 Poisoning
 Acute cases of poisoning (except in corrosive
substances poisoning or if patient is not fully
conscious)
 Alcoholic intoxication
 Removal of foreign bodies from the
oesophagus
Indications
Apomorphine
Semi synthetic derivative of morphine
• Given IM or SC, act centrally;
• Dose is 6 mg (2-8mg)
• Induces vomiting in 5 -10 min
• Respiratory and CNS depressant
 Contraindicated
Respiratory depression
Ipecacuanha
 Dried root of Cephaelis ipecacuanha
 Contains alkaloid - emetine
 Used as syrup ipecac.
 Produces effect in 15 min.
 Acts by irritating gastric mucosa & through CTZ
centre.
 Dose = 5ml in infants
= 10-15ml in children
= 15-20ml in adults
Contraindications
 Corrosive poisoning
 CNS stimulant drug poisoning
 Kerosene poisoning
 Unconscious patients
 Morphine poisoning
A group of drugs which are used to
control nausea and vomiting
Provide symptomatic relief
Removal of causative factor to have ultimate relief
Classification
Antiemetics and prokinetics by dr.roohna
Hyoscine (0.2–0.4 mg oral, i.m.) is the most effective drug
for motion sickness.
It has a brief duration of action;
Mechanism of Action Acts by blocking conduction of nerve
impulses across a cholinergic link in the pathway leading from
the vestibular apparatus to the vomiting centre.
Side effects sedation, dry mouth and other anticholinergic side
effects; suitable only for short brisk journies.
 Dicyclomine (10–20 mg oral) has been used
for prophylaxis of motion sickness and for
morning sickness.
H1 ANTIHISTAMINICS
 Useful mainly in motion sickness and to a
lesser extent in morning sickness,
postoperative and some other forms of
vomiting.
 Their antiemetic effect appears to be based
on anticholinergic, antihistaminic, weak
antidopaminergic and sedative properties
 Promethazine, diphenhydramine,
dimenhydrinate
 These drugs afford protection of motion
sickness for 4–6 hours, but produce sedation
and dryness of mouth.
 By their central anticholinergic action they
block the extrapyramidal side effects of
metoclopramide while supplementing its
antiemetic action.
 Doxylamine- It is a sedative H1 antihistaminic
with prominent anticholinergic activity.
 Pharmacokinetics- Oral absorption of
doxylamine is slow, and its t½ is 10 hr.
 Side effects -drowsiness, dry mouth, vertigo and
abdominal upset.
 Dose: 10–20 mg at bed time.
 Cinnarizine It is an antivertigo drug having
antimotion sickness property.
 Mechanism of Action- acts by inhibiting influx of
Ca2+ from endolymph into the vestibular
sensory cells which mediates labyrinthine
reflexes.
Theraputic Uses
 Vestibular system is important in motion sickness via
cranial nerve VIII - rich in Cholinergic M1 &
Histamine H1receptors
 Most effective drugs for motion sickness
 Vestibular disorders ( Meniere’s disease)
 Meclizine is long acting so useful in sea sickness
 Cinnarizine also has antivertigo effect. Act by
inhibiting influx of calcium to vestibular sensory
cells from endolymph
Neuroleptics
Phenothiazines:
Prochlorperazine
Promethazine
Triflupromazine
Phenothiazines are antipsychotics with potent antiemetic property due
to D2 antagonism and anti-muscarinic properties H1 and
antihistaminic property.
Side Effects- produce significant degree of sedation. Acute
muscle dystonia may occur
Therapeutic Uses:
Broad spectrum antiemetic action effective in:
 Drug induced and postoperative nausea
andvomiting (PONV).
 Disease induced vomiting: gastroenteritis,
 Uraemia, liver disease, migraine, etc.
 Malignancy associated and cancer
chemotherapy (mildly emetogenic) induced
vomiting.
 Radiation sickness vomiting (less effective).
Prokinetic Drugs
 Drugs that promote gastrointestinal transit
and speed gastric emptying by enhancing
coordinated propulsive motility.
 Effective antiemetic agents
 Two clinically important drugs:
 Metoclopramide
 Domperidone
Metoclopramide
Mechanism ofAction: acts through dopaminergic and
serotonergic receptors
 D2 antagonism: Central antidopaminergic (D2) action of
metoclopramide on CTZ is responsible for its anti emetic
activity
 5-HT4 agonism: It acts in the GIT to enhance Ach release
from the myenteric motor neurons and thereby enhance the
contractile activity.
 5HT3 antagonism: At higher concentrations it blocks 5HT3
receptors in the inhibitory myentric interneurons and in the
CTZ
D2 antagonism:
Central
antidopaminergic
(D2) action of
metoclopramide on
CTZ
5-HT4 agonism: It
acts in the GIT to
enhance Ach
release from the
myenteric motor
neurons
5HT3 antagonism:
At higher
concentrations it
blocks 5HT3
receptors in the
inhibitory myentric
interneurons and in
the CTZ
Pharmacokinetics
 Rapidly absorbed from GIT after oral administration.
 Undergoes a high degree first pass metabolism.
 It is excreted in the urine as free and as metabolites.
 It is also excreted in the breast milk.
 DOSE: 10-20mg orally or IV every 6 hrs.
As Antiemetic
 effective in postoperative, drug induced, disease
associated (especially migraine), radiation sickness,
etc,
 It has potent Antiemetic & antinausea effect.
 Blocks D2 receptors in CTZ of the medulla (area
postrema)
As Prokinetic agent
 It can selectively stimulate gut motor function.
 Blocks D2 receptor in GIT & blocks the normal
inhibitory effect of Dopamine on cholinergic smooth
muscle stimulation--- ↑ motility.
Therapeutic Uses:
 Used in emesis due to
 Uremia
 Radiation
 Viral gastro enteritis, hepatic-biliary disease
 Anticancer drugs
 Migraine
 Post operatively & pre-operatively
 Used as a gastro kinetic agent
 GERD
 Dyspepsia
Adverse Effects -
 Extrapyramidal reactions with facial and skeletal
muscle spasms- Restlessness, Dystonias ,
Parkinsonian symptoms.
More common in young and very old. Usually occur
shortly after staring treatment and subside with in 24
hours of stopping the drug.
 Diarrhea
 Drowsiness and fatigue, dizziness, restlessness and
anxiety.
 Galactorrhoea, Gynecomastia, impotence and
menstrual disorders – due to increased prolactin
levels (blocks the action of PIH)
 Domperidone- It is a D2 receptor antagonist.
 It crosses blood-brain barrier poorly.
 Extrapyramidal side effects are rare, but
hyperprolactinaemia can occur.
 Pharmacokinetics- absorbed orally, but
bioavailability is only ~15% due to first pass
metabolism.
 It is completely biotransformed and metabolites
are excreted in urine.
 Plasma t½ is 7.5 hr.
 Dose- 10-40mg
 Adverse effects
 Dry mouth
 Loose stools
 Headache
 Rashes
 Galactorrhoea
Cisapride
Mechanism of Action
 The prokinetic action is exerted mainly through
 5-HT4 agonism which promotes ACh release
from myenteric neurones, aided by
weak 5-HT3 antagonism which suppresses
inhibitory transmission in myenteric plexus.
 Enteric neuronal activation via 5-HT4 receptor
also promotes cAMP-dependent Cl– secretion in
the colon, increasing water content of stools.
 Safety of cisapride was challenged by reports of
serious ventricular arrhythmias and death.
 At high concentrations, cisapride blocks delayed
rectifying K+ channels in heart—prolongs Q-Tc interval
and predisposes to ventricular fibrillation.
 Following such reports, cisapride was suspended from
marketing in most countries several years back, but
was available in India till it was banned in March 2011.
5-HT4 agonist
 The drug functions as a motility stimulant,
achieving its desired therapeutic effects through
activation of the 5-HT4 receptors of the enteric
nervous system in the gastrointestinal tract.
 It also stimulates gastrointestinal motility and
the peristaltic reflex, and allegedly reduces
abdominal pain.
 Approved by the FDA in 2002, it was
subsequently removed from the market in 2007
due to FDA concerns about possible adverse
cardiovascular effects.
TEGASEROD
SELECTIVE 5-HT3
ANTAGONISTS
Mechanism of Action:
Blocks-the depolarization action of 5-HT exerted
through blockage of 5-HT3 receptors in the vagal
afferents of the GIT as well as in the NTS and
CTZ
It has weak 5-HT4 antagonist activity
Pharmacokinetics:
 Oral bioavailability is 60-70%
 t1/2 is 3-5hrs
 No significant drug interactions have been noted.
Adverse effects:
 Excellent safety profile
 Headache, Dizziness & constipation
 All three drugs cause prolongation of QT interval, but
more pronounced with dolasetron.
Therapeutic Uses:
 Chemotherapy and Radiation therapy induced nausea and
vomiting
 Post operative nausea and vomiting
 Advisable to administer Ondansetron(4-8 mg IV) 4 hours
before surgery is advisable.
 Drug induced vomiting
 Vomiting due to GI disorders
 Uraemia and neurological injuries induced vomiting
 Hyperemesis Gravidarum
 Granisetron: 10 times more potent than
ondansetron and effective in repeated cycles of
chemotherapy.
 Polonosetron: Longest acting (t1/2 is 40 hrs)
 Approved by the FDA in delayed cancer induced
nausea and vomiting-occurring between 2nd to
5th day
 Romosetron: Similar to ondansetron and is
marketed only in few countries
NEUROKININ-1 (NK1)ANTAGONISTS
Aprepitant
Fosaprepitant
Given orally BA = 65% , Crosses BBB.
t ½ : 11 hrs, Metabolized by hepatic CYP3A4.
MOA
• Act as Antiemetic: Selectively block NK1 receptor in
area postrema.
• Blocks the emetic action of Substance P
Uses
Used in combination with 5HT3 antagonists &
Corticosteroids for prevention of acute & chronic
nausea and vomiting from Cancer chemotherapy
Tetrahydrocannabinol (THC) main psychoactive chemical
in marijuana
It probably acts through the CB1 subtype of
cannabinoid receptors located on neurones in the
CTZ and/ or the vomiting centre itself.
Pharmacokinetics: complete absorption on oral
administration, significant 1st pass effect, metabolites
excreted slowly over days to weeks in faeces & urine
Cannabinoids
Dronabinol
Nabilone
GLUCOCORTICOIDS
Dexamethasone
Methylprednisolone
Antiemetic MOA not clear
Enhance action of 5HT3 antagonists in Cancer
chemotherapy induced Nausea & vomiting
Benzodiazepines
Diazepam
Lorazepam
 The weak antiemetic property of BZDs is primarily
based on the sedative action, relieving psychogenic
component.
 Used as adjuvant to metoclopramide/ondansetron,
 Used prior to Cancer chemotherapy to reduce
anticipatory vomiting
 Vomiting caused by anxiety
TYPES OF EMESIS
 MOTION SICKNESS
 MORNING SICKNESS (VOMITING
DURING PREGNANCY)
 CHEMOTHERAPY/ RADIATION
INDUCED NAUSEA AND EMESIS
(CIE)
 POST OPERATIVE EMESIS
Emesis and Pregnancy
Nausea and vomiting of pregnancy (NVP) is the most common
medical condition of pregnancy, affecting up to 80% of all
pregnant women to some degree
Etiology:
Exact pathogenesis is unclear
 Elevated levels of human chorionic gonadotropin (hCG)
 Chronic infection with Helicobacter pylori may play a role in
hyperemesis gravidarum.
 Delayed gastric motility caused by progesterone may be
responsible for the condition
 Psychologic factors
Doxylamine/pyridoxine:
• The only FDA-approved drug for treating nausea and vomiting in
pregnancy
• A greater form of reduction in Hyperemesis gravidarum
• No teratogenic potential
Ondansetron :
• Class B safety in pregnancy
• Most common parenteral and oral antiemetic used due to its
efficacy
Anticholinergics may be used as supportive drugs.
Ginger capsules: 250 mg taken 4 times a day have been
demonstrated to be effective against nausea and vomiting of
pregnancy
Contraindicated Drugs
 Domperidone (X)
 The combination of pyridoxine 10 mg and
doxylamine 10 mg was withdrawn from the
market due to increased risk of birth defects
with the combination.
MOTION SICKNESS
Result during space flights, taking off and
landing of an aeroplane etc.
It is a labyrinthine vomiting via stimulation of
vestibular nuclei.
Drugs used:
H1 ANTAGONIST/CENTRAL
ACTING
ANTICHOLINERGIC.
Hyoscine.
Side effects of hyoscine: anticholinergic
Blurred vision, dryness of mouth,
cyclopelgia, sedation and sleepiness.
DIPHENHYDRAMINE, CYCLIZINE,
MECLIZINE – prevents motion sickness and
treatment of vertigo due to labyrinth
dysfunction.
CINNARAZINE-Anti vertigo
drug.
Used in prevention of motion
sickness.
Acts as antihistaminic,
anticholinergic, antiserotonin &
Ca2+ channel blocker.
Inhibits influx of Ca2+ from
endolymph into vestibular
apparatus.
Chemothrapy Induced Emesis
• Anti-cancer drugs induce emesis by direct
activation of 5HT3 receptors in CTZ / may activate
vagal and splanchnic 5HT3 receptors to send
emetogenic signals to vomiting center through
neurotransmitters.
 ONDANSETRON
 GRANISETRON
 DOLASETRON
 TROPISETRON
 PALONOSETRON
 RAMOSETRON
Some Anti-emetic Regimens Used
in Cancer Chemotherapy
Antiemetics and prokinetics by dr.roohna
POST OPERATIVEVOMITING
• Complications in patients receiving general
anaesthesia.
• 5HT3 ANTAGONIST- preferred
• PROCHLORAZINE- blocks Dopamine 2 and
muscarinic receptors.
• PROMETHAZINE- potent anticholinergic and
antihistaminic.
Antiemetics and prokinetics by dr.roohna
 Elevated cholecystokinin levels slow gastric emptying and
motility and are associated with feed intolerance in critically
ill patients
☆Dexloxiglumide
 Selective and highly potent CCK-1 receptor antagonist
 Inhibits gall bladder contraction
 Improves lower oesophageal sphincter function
 Hastens colonic transit
☆Alvimopan
 High affinity for μ receptors
 Does not cross the blood–brain barrier
 No effect on gastric emptying
 hastened gut recovery and shortened time to
hospital discharge in patients after bowel
resection or hysterectomy
μ-opioid antagonist
Summary
References
 Hasketh PJ: Chemotherapy-induced nausea and
vomiting. N Engl J Med 2008;358:2482.
 LeTP et al: Update on the management of
postoperative nausea and vomiting and
postdischarge nausea vomiting in ambulatory
surgery.Anesthesiol Clin 2010;28:225.
 Roila F et al; Guideline update for MASCC and
ESMO in the prevention of chemotherapy- and
radiotherapy-induced nausea and vomiting:
Results of the Perugia consensus conference.Ann
Oncol 2010;21(Suppl 5):v232.
 DeMaeyer JH et al: 5-HT 4 receptor agonists: Similar
but not the same. Neurogastroenterol Motil
2008;20:99.
 Patrick A et al: Review article: Gastroparesis.
Aliment PharmacolTher 2008;27:724.
 Reddymasu SC et al: Severe gastroparesis: medical
therapy or gastric electrical stimulation. Clin
Gastroenterol Hepatol 2010;8:117.
 Borison H L et al. 1981 J Clin Pharmacol 21: 235-295.)
 Goodman and Gillman
 Davidson
 Guyton physiology
 KDTripathi pharmacology
 Katzung
Antiemetics and prokinetics by dr.roohna

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Antiemetics and prokinetics by dr.roohna

  • 1. Anti-Emetics and Prokinetics Moderator: Dr. D.A.Rizvi Presentor: Dr. Roohana Hasan
  • 2. Emesis and its causes Pathophysiology of Emesis Emetics Anti emetics Therapeutic uses of Anti-emetics Special topics  Motion sickness Emesis in pregnancy Chemotherapy induced vomiting Post operative nausea and vomiting
  • 3. Vomiting (Emesis) is the forceful expulsion of contents of the stomach and often, the proximal small intestine Vomiting is a complex reflex involving both autonomic and somatic neural pathways.
  • 4.  Vomiting is a complex process that consists of  (gastric relaxation and retroperistalsis),  (rhythmic action of respiratory muscles preceding vomiting and consisting of contraction of abdominal and intercostal muscles and diaphragm against a closed glottis),  (intense contraction of the abdominal muscles and relaxation of the upper esophageal sphincter). Pre-ejection Phase Retching Ejection
  • 6.  The “chemoreceptor trigger zone” or area postrema is located at the caudal end of the fourth ventricle.  This is outside the blood-brain barrier but is accessible to emetogenic stimuli in the blood or cerebrospinal fluid.  The chemoreceptor trigger zone is rich in dopamine D 2 receptors and opioid receptors, and possibly serotonin 5-HT 3 receptors and NK 1 receptors.
  • 8.  These are drugs used to evoke vomiting.  Act on CTZ : Apomorphine  Act reflexly and on CTZ : Ipecacuanha EMETICS
  • 9.  Poisoning  Acute cases of poisoning (except in corrosive substances poisoning or if patient is not fully conscious)  Alcoholic intoxication  Removal of foreign bodies from the oesophagus Indications
  • 10. Apomorphine Semi synthetic derivative of morphine • Given IM or SC, act centrally; • Dose is 6 mg (2-8mg) • Induces vomiting in 5 -10 min • Respiratory and CNS depressant  Contraindicated Respiratory depression
  • 11. Ipecacuanha  Dried root of Cephaelis ipecacuanha  Contains alkaloid - emetine  Used as syrup ipecac.  Produces effect in 15 min.  Acts by irritating gastric mucosa & through CTZ centre.  Dose = 5ml in infants = 10-15ml in children = 15-20ml in adults
  • 12. Contraindications  Corrosive poisoning  CNS stimulant drug poisoning  Kerosene poisoning  Unconscious patients  Morphine poisoning
  • 13. A group of drugs which are used to control nausea and vomiting Provide symptomatic relief Removal of causative factor to have ultimate relief
  • 16. Hyoscine (0.2–0.4 mg oral, i.m.) is the most effective drug for motion sickness. It has a brief duration of action; Mechanism of Action Acts by blocking conduction of nerve impulses across a cholinergic link in the pathway leading from the vestibular apparatus to the vomiting centre. Side effects sedation, dry mouth and other anticholinergic side effects; suitable only for short brisk journies.
  • 17.  Dicyclomine (10–20 mg oral) has been used for prophylaxis of motion sickness and for morning sickness.
  • 18. H1 ANTIHISTAMINICS  Useful mainly in motion sickness and to a lesser extent in morning sickness, postoperative and some other forms of vomiting.  Their antiemetic effect appears to be based on anticholinergic, antihistaminic, weak antidopaminergic and sedative properties
  • 19.  Promethazine, diphenhydramine, dimenhydrinate  These drugs afford protection of motion sickness for 4–6 hours, but produce sedation and dryness of mouth.  By their central anticholinergic action they block the extrapyramidal side effects of metoclopramide while supplementing its antiemetic action.
  • 20.  Doxylamine- It is a sedative H1 antihistaminic with prominent anticholinergic activity.  Pharmacokinetics- Oral absorption of doxylamine is slow, and its t½ is 10 hr.  Side effects -drowsiness, dry mouth, vertigo and abdominal upset.  Dose: 10–20 mg at bed time.
  • 21.  Cinnarizine It is an antivertigo drug having antimotion sickness property.  Mechanism of Action- acts by inhibiting influx of Ca2+ from endolymph into the vestibular sensory cells which mediates labyrinthine reflexes.
  • 22. Theraputic Uses  Vestibular system is important in motion sickness via cranial nerve VIII - rich in Cholinergic M1 & Histamine H1receptors  Most effective drugs for motion sickness  Vestibular disorders ( Meniere’s disease)  Meclizine is long acting so useful in sea sickness  Cinnarizine also has antivertigo effect. Act by inhibiting influx of calcium to vestibular sensory cells from endolymph
  • 23. Neuroleptics Phenothiazines: Prochlorperazine Promethazine Triflupromazine Phenothiazines are antipsychotics with potent antiemetic property due to D2 antagonism and anti-muscarinic properties H1 and antihistaminic property. Side Effects- produce significant degree of sedation. Acute muscle dystonia may occur
  • 24. Therapeutic Uses: Broad spectrum antiemetic action effective in:  Drug induced and postoperative nausea andvomiting (PONV).  Disease induced vomiting: gastroenteritis,  Uraemia, liver disease, migraine, etc.  Malignancy associated and cancer chemotherapy (mildly emetogenic) induced vomiting.  Radiation sickness vomiting (less effective).
  • 25. Prokinetic Drugs  Drugs that promote gastrointestinal transit and speed gastric emptying by enhancing coordinated propulsive motility.  Effective antiemetic agents  Two clinically important drugs:  Metoclopramide  Domperidone
  • 26. Metoclopramide Mechanism ofAction: acts through dopaminergic and serotonergic receptors  D2 antagonism: Central antidopaminergic (D2) action of metoclopramide on CTZ is responsible for its anti emetic activity  5-HT4 agonism: It acts in the GIT to enhance Ach release from the myenteric motor neurons and thereby enhance the contractile activity.  5HT3 antagonism: At higher concentrations it blocks 5HT3 receptors in the inhibitory myentric interneurons and in the CTZ
  • 27. D2 antagonism: Central antidopaminergic (D2) action of metoclopramide on CTZ 5-HT4 agonism: It acts in the GIT to enhance Ach release from the myenteric motor neurons 5HT3 antagonism: At higher concentrations it blocks 5HT3 receptors in the inhibitory myentric interneurons and in the CTZ
  • 28. Pharmacokinetics  Rapidly absorbed from GIT after oral administration.  Undergoes a high degree first pass metabolism.  It is excreted in the urine as free and as metabolites.  It is also excreted in the breast milk.  DOSE: 10-20mg orally or IV every 6 hrs.
  • 29. As Antiemetic  effective in postoperative, drug induced, disease associated (especially migraine), radiation sickness, etc,  It has potent Antiemetic & antinausea effect.  Blocks D2 receptors in CTZ of the medulla (area postrema) As Prokinetic agent  It can selectively stimulate gut motor function.  Blocks D2 receptor in GIT & blocks the normal inhibitory effect of Dopamine on cholinergic smooth muscle stimulation--- ↑ motility.
  • 30. Therapeutic Uses:  Used in emesis due to  Uremia  Radiation  Viral gastro enteritis, hepatic-biliary disease  Anticancer drugs  Migraine  Post operatively & pre-operatively  Used as a gastro kinetic agent  GERD  Dyspepsia
  • 31. Adverse Effects -  Extrapyramidal reactions with facial and skeletal muscle spasms- Restlessness, Dystonias , Parkinsonian symptoms. More common in young and very old. Usually occur shortly after staring treatment and subside with in 24 hours of stopping the drug.  Diarrhea  Drowsiness and fatigue, dizziness, restlessness and anxiety.  Galactorrhoea, Gynecomastia, impotence and menstrual disorders – due to increased prolactin levels (blocks the action of PIH)
  • 32.  Domperidone- It is a D2 receptor antagonist.  It crosses blood-brain barrier poorly.  Extrapyramidal side effects are rare, but hyperprolactinaemia can occur.  Pharmacokinetics- absorbed orally, but bioavailability is only ~15% due to first pass metabolism.  It is completely biotransformed and metabolites are excreted in urine.  Plasma t½ is 7.5 hr.  Dose- 10-40mg
  • 33.  Adverse effects  Dry mouth  Loose stools  Headache  Rashes  Galactorrhoea
  • 34. Cisapride Mechanism of Action  The prokinetic action is exerted mainly through  5-HT4 agonism which promotes ACh release from myenteric neurones, aided by weak 5-HT3 antagonism which suppresses inhibitory transmission in myenteric plexus.  Enteric neuronal activation via 5-HT4 receptor also promotes cAMP-dependent Cl– secretion in the colon, increasing water content of stools.
  • 35.  Safety of cisapride was challenged by reports of serious ventricular arrhythmias and death.  At high concentrations, cisapride blocks delayed rectifying K+ channels in heart—prolongs Q-Tc interval and predisposes to ventricular fibrillation.  Following such reports, cisapride was suspended from marketing in most countries several years back, but was available in India till it was banned in March 2011.
  • 36. 5-HT4 agonist  The drug functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract.  It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain.  Approved by the FDA in 2002, it was subsequently removed from the market in 2007 due to FDA concerns about possible adverse cardiovascular effects. TEGASEROD
  • 38. Mechanism of Action: Blocks-the depolarization action of 5-HT exerted through blockage of 5-HT3 receptors in the vagal afferents of the GIT as well as in the NTS and CTZ It has weak 5-HT4 antagonist activity
  • 39. Pharmacokinetics:  Oral bioavailability is 60-70%  t1/2 is 3-5hrs  No significant drug interactions have been noted. Adverse effects:  Excellent safety profile  Headache, Dizziness & constipation  All three drugs cause prolongation of QT interval, but more pronounced with dolasetron.
  • 40. Therapeutic Uses:  Chemotherapy and Radiation therapy induced nausea and vomiting  Post operative nausea and vomiting  Advisable to administer Ondansetron(4-8 mg IV) 4 hours before surgery is advisable.  Drug induced vomiting  Vomiting due to GI disorders  Uraemia and neurological injuries induced vomiting  Hyperemesis Gravidarum
  • 41.  Granisetron: 10 times more potent than ondansetron and effective in repeated cycles of chemotherapy.  Polonosetron: Longest acting (t1/2 is 40 hrs)  Approved by the FDA in delayed cancer induced nausea and vomiting-occurring between 2nd to 5th day  Romosetron: Similar to ondansetron and is marketed only in few countries
  • 42. NEUROKININ-1 (NK1)ANTAGONISTS Aprepitant Fosaprepitant Given orally BA = 65% , Crosses BBB. t ½ : 11 hrs, Metabolized by hepatic CYP3A4. MOA • Act as Antiemetic: Selectively block NK1 receptor in area postrema. • Blocks the emetic action of Substance P
  • 43. Uses Used in combination with 5HT3 antagonists & Corticosteroids for prevention of acute & chronic nausea and vomiting from Cancer chemotherapy
  • 44. Tetrahydrocannabinol (THC) main psychoactive chemical in marijuana It probably acts through the CB1 subtype of cannabinoid receptors located on neurones in the CTZ and/ or the vomiting centre itself. Pharmacokinetics: complete absorption on oral administration, significant 1st pass effect, metabolites excreted slowly over days to weeks in faeces & urine Cannabinoids Dronabinol Nabilone
  • 45. GLUCOCORTICOIDS Dexamethasone Methylprednisolone Antiemetic MOA not clear Enhance action of 5HT3 antagonists in Cancer chemotherapy induced Nausea & vomiting
  • 46. Benzodiazepines Diazepam Lorazepam  The weak antiemetic property of BZDs is primarily based on the sedative action, relieving psychogenic component.  Used as adjuvant to metoclopramide/ondansetron,  Used prior to Cancer chemotherapy to reduce anticipatory vomiting  Vomiting caused by anxiety
  • 47. TYPES OF EMESIS  MOTION SICKNESS  MORNING SICKNESS (VOMITING DURING PREGNANCY)  CHEMOTHERAPY/ RADIATION INDUCED NAUSEA AND EMESIS (CIE)  POST OPERATIVE EMESIS
  • 48. Emesis and Pregnancy Nausea and vomiting of pregnancy (NVP) is the most common medical condition of pregnancy, affecting up to 80% of all pregnant women to some degree Etiology: Exact pathogenesis is unclear  Elevated levels of human chorionic gonadotropin (hCG)  Chronic infection with Helicobacter pylori may play a role in hyperemesis gravidarum.  Delayed gastric motility caused by progesterone may be responsible for the condition  Psychologic factors
  • 49. Doxylamine/pyridoxine: • The only FDA-approved drug for treating nausea and vomiting in pregnancy • A greater form of reduction in Hyperemesis gravidarum • No teratogenic potential Ondansetron : • Class B safety in pregnancy • Most common parenteral and oral antiemetic used due to its efficacy Anticholinergics may be used as supportive drugs. Ginger capsules: 250 mg taken 4 times a day have been demonstrated to be effective against nausea and vomiting of pregnancy
  • 50. Contraindicated Drugs  Domperidone (X)  The combination of pyridoxine 10 mg and doxylamine 10 mg was withdrawn from the market due to increased risk of birth defects with the combination.
  • 51. MOTION SICKNESS Result during space flights, taking off and landing of an aeroplane etc. It is a labyrinthine vomiting via stimulation of vestibular nuclei. Drugs used: H1 ANTAGONIST/CENTRAL ACTING ANTICHOLINERGIC. Hyoscine. Side effects of hyoscine: anticholinergic Blurred vision, dryness of mouth, cyclopelgia, sedation and sleepiness. DIPHENHYDRAMINE, CYCLIZINE, MECLIZINE – prevents motion sickness and treatment of vertigo due to labyrinth dysfunction. CINNARAZINE-Anti vertigo drug. Used in prevention of motion sickness. Acts as antihistaminic, anticholinergic, antiserotonin & Ca2+ channel blocker. Inhibits influx of Ca2+ from endolymph into vestibular apparatus.
  • 52. Chemothrapy Induced Emesis • Anti-cancer drugs induce emesis by direct activation of 5HT3 receptors in CTZ / may activate vagal and splanchnic 5HT3 receptors to send emetogenic signals to vomiting center through neurotransmitters.  ONDANSETRON  GRANISETRON  DOLASETRON  TROPISETRON  PALONOSETRON  RAMOSETRON
  • 53. Some Anti-emetic Regimens Used in Cancer Chemotherapy
  • 55. POST OPERATIVEVOMITING • Complications in patients receiving general anaesthesia. • 5HT3 ANTAGONIST- preferred • PROCHLORAZINE- blocks Dopamine 2 and muscarinic receptors. • PROMETHAZINE- potent anticholinergic and antihistaminic.
  • 57.  Elevated cholecystokinin levels slow gastric emptying and motility and are associated with feed intolerance in critically ill patients ☆Dexloxiglumide  Selective and highly potent CCK-1 receptor antagonist  Inhibits gall bladder contraction  Improves lower oesophageal sphincter function  Hastens colonic transit
  • 58. ☆Alvimopan  High affinity for μ receptors  Does not cross the blood–brain barrier  No effect on gastric emptying  hastened gut recovery and shortened time to hospital discharge in patients after bowel resection or hysterectomy μ-opioid antagonist
  • 60. References  Hasketh PJ: Chemotherapy-induced nausea and vomiting. N Engl J Med 2008;358:2482.  LeTP et al: Update on the management of postoperative nausea and vomiting and postdischarge nausea vomiting in ambulatory surgery.Anesthesiol Clin 2010;28:225.  Roila F et al; Guideline update for MASCC and ESMO in the prevention of chemotherapy- and radiotherapy-induced nausea and vomiting: Results of the Perugia consensus conference.Ann Oncol 2010;21(Suppl 5):v232.
  • 61.  DeMaeyer JH et al: 5-HT 4 receptor agonists: Similar but not the same. Neurogastroenterol Motil 2008;20:99.  Patrick A et al: Review article: Gastroparesis. Aliment PharmacolTher 2008;27:724.  Reddymasu SC et al: Severe gastroparesis: medical therapy or gastric electrical stimulation. Clin Gastroenterol Hepatol 2010;8:117.  Borison H L et al. 1981 J Clin Pharmacol 21: 235-295.)  Goodman and Gillman  Davidson  Guyton physiology  KDTripathi pharmacology  Katzung

Editor's Notes

  1. In astudy, 61.8 percent of pregnant women with hyper-emesis were found to be positive for the H. pylori genome,