EMETICS AND ANTIEMETICS 2012.pdf
-
Upload
jamaluddin-ahmad-am -
Category
Documents
-
view
150 -
download
6
Transcript of EMETICS AND ANTIEMETICS 2012.pdf
![Page 1: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/1.jpg)
EMETICS AND ANTIEMETICS
Ngatidjan, Prof. MD. M.Sc. Sp.FK(K).
Department of Pharmacology and Therapy
Faculty of Medicine UGM
Lecturer in the Faculty of Medicine UMY
![Page 2: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/2.jpg)
EMETICS AND ANTIEMETICS
• Emetics
drugs or substance induced emesis or vomiting
or induce nausea lead to vomiting
- apomorphine
• Antiemetics
drugs used for therapy of vomiting
- dimenhydrinate, etc.
![Page 3: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/3.jpg)
NAUSEA AND VOMITING
• Gastrointestinal stimulation
• Motion sickness
• Hormone disturbance pregnancy sickness
• Intracranial pathology
• Metabolic disorders
• Psychogenic
• Severe pain cardiac, bile duct or ureteric
• Drug and radiation induced emesis
• Endogenous toxin
![Page 4: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/4.jpg)
(Lullmann et al., 2005)
![Page 5: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/5.jpg)
![Page 6: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/6.jpg)
Gastrointestinal stimulation
• Stimulation of mechanoreceptors by
distension or obstruction in the gut
gstric fullness
• Stimulation of chemoreceptor caused by
endotoxins cholera
• Ingestion of drugs or toxic material ipecac,
carbamates, and inject of morphine, apomorphine
![Page 7: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/7.jpg)
Gastrointestinal stimulation
• Peptic ulcer disease,
• Pancreatic disease,
• Intra-abdominal emergencies :
intestinal obstruction,
acute pancreatitis,
acute pyelonephritis,
acute cholecystitis,
acute viral hepatitis,
• Acute gastroenteritis : viral gastroenteritis,
salmonellosis, shigellosis, staphylococcal (enterotoxins),
![Page 8: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/8.jpg)
(Page et al., 2005)
![Page 9: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/9.jpg)
Motion sickness
• Nausea – and even – vomiting
caused by unwillingness motion
• Centered around the sensory input conflict of
- visual
- vestibular
- proprioceptive
inappropriate reflex sickness
![Page 10: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/10.jpg)
Hormone disturbances
• Pregnancyduring the first trimester
- approximately 85% of pregnancy nausea
- approximately 52% of pregnancy vomiting
- approximately 0,1% hyperemesis gravidarum
caused by delayed gastric emptying, changed in intra-
abdominal pressure, hormonal changes and psychogenic
• Premenstrual nausea cyclic
• Side effect of hormonal contraseptive
![Page 11: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/11.jpg)
(Page et al., 2005)
![Page 12: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/12.jpg)
(Page et al., 2005)
![Page 13: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/13.jpg)
Intracranial pathology
• Associated with severe headache may be
as the consequence of a rise in intracranial
pressure resulting from :
- intracranial hemorrhage head injury
- severe intracranial inflammatory response
• Migraine
![Page 14: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/14.jpg)
Metabolic disorders
• Hypoglycemia
• Uremia
• Diabetes mellitus
diabetic ketoacidosis
• Etc.
![Page 15: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/15.jpg)
Psychogenic
• Chronic psychogenic vomiting
• Nervous dyspepsia- nausea, vomiting, anxiety, irritability and weight loss
• Anoxia nervosa bulimia
• Certain sight, smell, or feeling may trigger revolution of fear nausea vomiting
• Anxiety
![Page 16: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/16.jpg)
Severe pain
• Cardiac pain
• Acute distension of the stomach
• Acute distension of bile duct stone
• Acute distension of ureter stone
![Page 17: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/17.jpg)
EMETICS(drug induced emesis)
![Page 18: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/18.jpg)
Drugs induced nausea and vomiting
• Cancer chemotherapy Cisplatin, cyclophosphamide > 90%,
Mercaptopurine (< 10%),
melphalan oral (< 10%) – iv (60-90%)
• Apomorphine,
• Levodopa,
• Morphine and related opioid analgesics
• Cardiac glycoside
![Page 19: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/19.jpg)
Severely emetogenic in almost all patients
Moderately emetogenic Least emetogenic
Cisplatin
Mustine
Cyclophosphamide
Dacarbazine
Doxorubicin
Mitomycin C
Procarbazine
Nitrosoureas
5-Fluorouracil
Cytarabine
6-Mercaptopurine
Bleomycin
Vinblastine
Vincristine
The number of women who were reported to get sickness with oral contraceptive,
travel or migraine and the relationship to vomiting in pregnancy
Pregnancy
sickness
Oral contraceptive
sickness
Travel sickness Migraine sickness
Vomiting
No vomiting
30 (70%)
13 (30%)
77 (63%)
46 (37%)
45 (65%)
24 (35%)
![Page 20: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/20.jpg)
Emetics
therapeutic induction of vomiting
• Apomorphine
to induce vomitus in alcoholic abuse, or using disulfiram
• Apomorphine or ipecac syrup
to induce emesis in the therapy of acute oral intoxication
![Page 21: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/21.jpg)
ANTIEMETICS
![Page 22: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/22.jpg)
(Page et al., 2005)
![Page 23: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/23.jpg)
Antiemetics
• Dopamine receptor antagonists
• Muscarinic receptor antagonists
• Histamine H1-receptor antagonsits
• 5-HT3-receptor antagonsits
• Sedatives and hypnotics
• Phenothiazines
![Page 24: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/24.jpg)
D-receptors antagonists
Block D-receptors in the brain
in the : area postrema,
dorsal motor nucleus of vagus nerve
nucleus tractus solitarius
decrease stimulation of CTZ
• Haloperidol
• Fluphenazine
• Metoclopramide
![Page 25: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/25.jpg)
![Page 26: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/26.jpg)
![Page 27: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/27.jpg)
M-receptors antagonists
Block M-receptors in the brain
in the area postrema, dorsal vagal complex
in gastrointestinal tract decrease its motility
• Scopolamine
side effects : sedation, blurred vision, urinary retention,
dry mouth (decrease saliva secretion)
contraindicated for airline pilots, bus and car drivers, etc.
![Page 28: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/28.jpg)
![Page 29: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/29.jpg)
H1-receptor antagonists
Antihistamines
Block H1-receptors in area postrema
and M-receptors in related structure
• buclizine
• cyclizine
• dimenhydrinate
• meclizine
• promethazine
![Page 30: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/30.jpg)
![Page 31: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/31.jpg)
5-HT3-receptor blockers
Seritonine antagonists
Block 5HT3-receptors in area postrema, nucleus
tractus solitarius and on vagal afferent nerve endings.
• ondansetron
• granisetron
• tropisetron
adverse effects : headache, constipation, flushing
![Page 32: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/32.jpg)
![Page 33: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/33.jpg)
Phenothiazines
• chlorpromazine
• promethazine
• prochlorperazine
• trimeprazine
mixed pharmacological blocking properties
(muscarinic blockers, antihistaminic, dopaminergic blockers,
adrenergic and serotonergic blockers)
![Page 34: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/34.jpg)
![Page 35: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/35.jpg)
ANTIEMETICS IN CHILDREN
5-HT receptor antagonists
• ondansetron,
• ganisetron,
• dolasetron,
• palonosetron.
blocks presynaptic r-5HT on sensory vagal fibers
(in the gutwall especially in the acute phase of chemotherapy induce)
![Page 36: EMETICS AND ANTIEMETICS 2012.pdf](https://reader035.fdocuments.us/reader035/viewer/2022081421/56d6cb291a28ab30169ca6ff/html5/thumbnails/36.jpg)