Drugs used in disorders of the bowel Flashcards
- Nausea
- Nausea is an unpleasant sensation,
which may be a precursor to the forceful
expulsion of gastric contents
(vomiting/emesis
Vomiting centre
The physical act of vomiting is co-ordinated centrally by the vomiting (or emetic) centre in the medulla
- A network of neural pathways that integrate signals arriving directly from other locations such as:
the inner ear through the vestibular nuclei (which explains the mechanism of motion and Meniere’s disease) * It receives input from higher cortical centres, explaining why unpleasant or repulsive sights or smells, or strong emotional stimuli, can sometimes induce nausea and vomiting. (emotional, visual, olfactory impulses)
Chemoreceptor trigger zone (CTZ)
found In the postrema of the medulla
protected by Blood brain barrier-Lipophilic drugs
It is rich in D2, 5HT and neurokinin receptors. The neurotransmitters
at these receptors are dopamine, serotonin and subst P respectively.
Opioid receptors are also found in the CTZ. why?
because opioids cause Nausea and vomit
Presence of abdominal pain
N&V as a symptom of appendicitis, cholecystitis (inflammation of gallbladder) & cholelithiasis
(presence of formation of gallstones) – abdominal pain would be the presenting symptom.
Timing of nausea and
vomiting
Early morning vomiting = ?Pregnancy / excess alcohol intake
Immediately after food = ?gastritis
1 or more hours after food = ?peptic ulcer
Conditions to eliminate
- N&V associated with headaches (migraines / raised intracranial
pressure) * N&V in neonates (birth to 1 month) = ALWAYS referred - N&V (differentiate from regurgitation) in infants (1 – 12 months) -
refer in 24 hours - N&V in children – rehydration! * Medicine-induced
- Middle ear diseases
D2 receptor antagonists
- Not for vomiting because of motion sickness/labyrinth disturbances
- Hydrophilic drugs preferred- will not cross BBB
- Will not block extrapyramidal D2 receptors: dyskinesia & restlessness
Dopamine inhibits prolactin, its blockage may cause breast tenderness,
galactorrhoea, amenorrhea.
D2 receptor antagonists: crossses BBB
Metoclopramide
postoperative vomiting
drug related N/V
empties stomach and relaxes pylorus
Prochlorperazine:
radiation therapy, oncotherapy, available as
suppositories.
* AE: jaundice
Histamine & Muscarinic receptor antagonist
Used for all types of vomiting esp motion sickness, nausea from
labyrinth disturbances
Cross BBB = vomiting centre & chemoreceptor trigger zone (CTZ)
Anticholinergic side-effects
drugs
Promethazine – sedative anithistamine – treat motion sickness &
vertigo AE: Strong anticholinergic effect ,Strong sedative effect
Cyclizine – also paediatric suppositories for over 6 years – treat motion
sickness
Cinnarizine - treat motion sickness, vertigo, vestibular disorder
5-HT3 antagonist
Examples: * Dolasetron
* Granisetron
* Ondansetron
* Palonosetron
Selective antagonists of 5HT receptors in chemoreceptor trigger zone
(CTZ) & GIT
* N/V caused by chemotherapeutic drugs, radiation therapy
* Caution in cardiac disease- ECG abnormalities
Pregnancy
Management * Reassurance
* Attention to emotional factors
* Cup of tea with a biscuit before rising
* Light frequent meals with adequate fibre intake
* Mixture of sucrose & phosphoric acid (Emetrol® or Emex®) * Drug treatment not recommended – moderate N&V
* Doxylamine (Somnil®, Restwell®) most evidence in pregnancy
* Combination preparation: S2 Asic® doxylamine + dicyclomine + pyridoxine:
2t nocte, 1t mane before rising prn
severe type of vomiting during pregnanc
Hyperemesis gravidarum (severe type of vomiting during pregnancy) * Admission to hospital * IV hydration with electrolytes and thiamine
* Parenteral antiemetics: * IM prochlorperazine
* IV metoclopramide
* Ondansetron for pregnancies over 12 weeks if vomiting does not resolve
* Exclude organic causes: thyrotoxicosis, UTI, gestational trophoblastic
diseas
Neurokinin 1 receptor antagonists
Aprepitant
Adjunct to other antiemetics for prevention of acute or delayed N&V
due to highly emetogenic chemotherapy
Irritable bowel syndrome (IBS)
A functional bowel disorder of the GIT associated with: * Abdominal pain and * Altered bowel activity * Lacking any pathological changes.
Synonyms: spastic colon, irritable colon