Drugs used in disorders of the bowel Flashcards

1
Q
  • Nausea
A
  • Nausea is an unpleasant sensation,
    which may be a precursor to the forceful
    expulsion of gastric contents
    (vomiting/emesis
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2
Q

Vomiting centre

A

The physical act of vomiting is co-ordinated centrally by the vomiting (or emetic) centre in the medulla

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3
Q
  • A network of neural pathways that integrate signals arriving directly from other locations such as:
A

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)

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4
Q

Chemoreceptor trigger zone (CTZ)

A

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.

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5
Q

Opioid receptors are also found in the CTZ. why?

A

because opioids cause Nausea and vomit

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6
Q

Presence of abdominal pain

A

N&V as a symptom of appendicitis, cholecystitis (inflammation of gallbladder) & cholelithiasis
(presence of formation of gallstones) – abdominal pain would be the presenting symptom.

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7
Q

Timing of nausea and
vomiting

A

Early morning vomiting = ?Pregnancy / excess alcohol intake
Immediately after food = ?gastritis
1 or more hours after food = ?peptic ulcer

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8
Q

Conditions to eliminate

A
  • 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
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9
Q

D2 receptor antagonists

A
  • 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.
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10
Q

D2 receptor antagonists: crossses BBB

A

Metoclopramide

postoperative vomiting
drug related N/V
empties stomach and relaxes pylorus

Prochlorperazine:

radiation therapy, oncotherapy, available as
suppositories.
* AE: jaundice

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11
Q

Histamine & Muscarinic receptor antagonist

A

Used for all types of vomiting esp motion sickness, nausea from
labyrinth disturbances
Cross BBB = vomiting centre & chemoreceptor trigger zone (CTZ)
Anticholinergic side-effects

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12
Q

drugs

A

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

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13
Q

5-HT3 antagonist

A

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

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14
Q

Pregnancy

A

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

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15
Q

severe type of vomiting during pregnanc

A

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

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15
Q

Neurokinin 1 receptor antagonists

A

Aprepitant
Adjunct to other antiemetics for prevention of acute or delayed N&V
due to highly emetogenic chemotherapy

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16
Q

Irritable bowel syndrome (IBS)

A

A functional bowel disorder of the GIT associated with: * Abdominal pain and * Altered bowel activity * Lacking any pathological changes.
Synonyms: spastic colon, irritable colon

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17
Q

Irritable bowel syndrome: sub-classification

A
  • IBS-D: IBS with predominant diarrhoea
  • IBS-C: IBS with predominant constipation
  • IBS-M: IBS with alternating constipation & diarrhoea
18
Q

Irritable bowel syndrome: aetiology

A

Multifactorial cause (not sure) * Motility dysfunction
* Diet * Genetics * Psychological factors (stress /
depression

19
Q

Antispasmodics

A

(Antimuscarinic / anticholinergic) * Dicycloverine
* Mebeverine
* Propantheline
* Hyosine*
! Reduce GI motility

20
Q

Motility stimulants (propulsives):

A

mainly IBS-C
enhance gastric emptying,
decrease small bowel transit time
& increase gastro-oesophageal
sphincter tone
Role in IBS not defined
* Metoclopramide
* Domperidone

21
Q

Propulsives

A

Domperidone
* Peripheral dopamine blocking
agent * DI: metabolised via cytochrome
P450 in liver, QT prolongation
* DI: grapefruit juice

Metoclopramide
* IBS: Off label use
* SE: CNS; drowsiness, fatigue,
dizziness, weakness, abdominal
cramps & diarrhoea !!
Extrapyrimidal effects in elderly
and children
* DI: antipsychotics, CNS
depressants, alcoho

22
Q

Inflammatory bowel disease

A

A chronic inflammatory disorder of the
gastrointestinal tract that includes both
Crohn’s disease (CD) and ulcerative
colitis.

23
Q

symptoms for both

A

: Abdominal pain, rectal bleeding,
diarrhoea and weight loss characterise
both CD and ulcerative colitis.

24
Sulfasalazine
Split by colonic bacteria into sulfapyridine and 5-aminosalicylic acid (5- ASA, mesalazine). 5-ASA believed to be responsible for beneficial effect. * Sulfapyridine absorbed, metabolised in the liver and excreted via the urine. * Most of 5-ASA eliminated unchanged in the faeces
25
Contraindications:
Prescriber’s points: * Monitor blood counts, hepatic function, urea and electrolytes with chronic therapy * GI adverse effects can be alleviated by a drug holiday and starting at a lower dose * Gastric irritation may be minimised by taking after meals, full glass of water, enteric coated tablets * Report sore throat, fever or easy bruising – indicated heamotologic abnormalities (thrombocytopenia, granulocytopenia, red cell haemolysis
26
Relapses of Crohn’s disease
Immunosuppressants e.g. azathioprine, mercaptopurine, methotrexate PLUS (if necessary) Tumour necrosis factor – α inhibitors (TNF-α inhibitors) e.g. infliximab, adalimumab
27
Constipation
A reduction in normal bowel habit accompanied with more difficult defecation and/or hard stools
28
what causes constipation
Very common, especially in the elderly Causes: sedentary lifestyle, ↓ fluid intake, poor nutriƟon, avoidance of fibrous foods, chronic illness, pregnancy, drugs, chronic use of enemas & laxatives, old age, ignoring the urge Women more likely than men Late pregnancy (40%)
29
Normal function of large intestine
Normal function of large intestine = remove water and various salts from colon, drying and expulsion of faeces
30
increase in absorption will lead to ??
Constipation.
31
Pain on defecation
Anorectal problem; constipation usually secondary to the suppression of Anorectal problem; constipation is usually secondary to the suppression of defecation, because it induces pain
32
Presence of blood
Bright red = haemorrhoids / tear in anal canal Blood mixed with stool = refer Stool appear black and tarry = upper GI bleed
33
chronic constipation duration
duration >/= 6 weeks
34
Constipation: conditions to eliminate
Medicine-induced constipation IBS Pregnancy Functional causes in children Depression Colorectal cancer Hypothyroidism Bowel obstruction
35
Non-pharmacological measures
Dietary:↑ fibre & water intake – 3-5 days Avoid caffeinated drinks and diuretics Lifestyle: ↑ exercise Encourage regular bowel habits Discourage continuous use of laxatives
36
Class of laxative
Bulk-forming-Softening and increasing feacal mass, increased bulk encourage peristalsis (mimic ↑ fibre consumpƟon) drugs Ispagula* (psyllium) (Agiobulk®, Fybogel®) * Methylcellulose * Sterulia (Normacol®) Contact/irritant--↑ GI moƟlity by directly stimulating colonic nerves Senna* (Senokot®, Soflax®) * Sodium picosulphate (metabolised by colonic bacteria to active metabolite bisacodyl) * Bisacodyl (Dulcolax® supps & enteric coated). Osmotically acting---Withdraw fluid into the bowel by osmosis drugs Lactulose* * Magnesium sulphate / hydroxide * Polyethylene glycol combinations* (Movicol®, Go-lytely®, Klean-Prep®) * Sodium phosphate* (Colo-pre
37
Bulk-forming laxatives
Non-habit-forming, supplements to dietary fibre * Indications: constipation, IBS, diverticular disease * Onset of action: 12-72 hours * Contraindications: intestinal obstruction, stenosis, ulceration or adhesions in the GIT * Caution: sodium-containing product, increase fluid intake to avoid intestinal compaction * Pregnancy √ (safe) * Drug interactions: may interfere with absorption of certain drugs (take 3 hours before or after other drugs) * Adverse effects: flatulence & abdominal distension.
38
Contact / irritant laxatives
ndications – can precipitate chronic colonic changes * Onset of action: 8-12 hours * Pregnancy – avoid * ! Abuse as slimming aid * Adverse effect: abdominal cramps, long term use Bisacodyl and Sodium picosulphate * Indicated for single dose administration to evacuate bowel in preparation for examinations of the colon (including radiological examinations) or to evacuate barium from the GIT after radiological examination
39
Osmotically acting laxative
Onset of action: 12-72 hours * Generally used for acute and rapid evacuation of the bowel (except lactulose), prolonged use not recommended * Indications: bowel preparation for colonoscopy / colon surgery / radiological examination should receive split dose preparations, significantly improve bowel cleansing. Administer half the evening before the procedure and the other half on the morning (4-6 hours) before the procedure * Polyethylene glycol combinations include Go-Lytely® and Klean-Prep® * Sodium phosphate include Colo-Prep®
40
Rectal laxative preparations
* Suppositories * Bisacodyl, * Glycerol (osmotic effect softens and lubricates faeces, mildly irritant effect causing rectal contraction, evacuation usually within 30 minutes) * Enemas * Sodium phosphate
41
Haemorrhoids
Most common problem affecting the anorectal region Varicose veins of the ano-rectal area. Is usually accompanied by a history of constipation. In older patients consider a diagnosis of underlying carcinoma. GENERAL MEASURES High-fibre diet. Counsel against chronic use of laxatives. Avoid straining at stool
42
Symptomatic treatment for painful haemorrhoids:
Bismuth subgallate compound, ointment, topical, applied 2–4 times daily OR Bismuth subgallate compound suppositories, insert one into the rectum 3 times daily. OR Lidocaine 2%, cream, topical, applied before and after each bowel action.
43
Anal fissures
Painful small cracks just inside the anal margin, sometimes a linear ulcer. It is often seen together with a sentinel pile or external haemorrhoids. May cause spasm of the anal sphincter. May cause bleeding on defecation. Dietary advice – promote soft stools