GI pharmacology Flashcards

1
Q

Function of purgatives

A

Accelerate transit through the intestine Used for alleviation of constipation

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2
Q

Define constipation

A

Infrequent or difficult evacuation of faeces

Includes: infrequent bowel movement, difficuly during defaecation, sensation on incomplete bowel evacuation

In sever cases - faecal impaction causes bowel obstruction. Presents as vomiting and tender abdomen with paradoxical diarrhoea where soft tool from the small intestine bypasses the matter in the colon

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3
Q

Name 4 causes of constipation

A

Diet

Hormones

SIde effects of medication (opiods)

Illness

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4
Q

Classes of purgatives

A

Bulk laxatives (increase volume of non-absorbable residue)

Osmotic laxatives (increase stool water content)

Faecal sottneers (alter faecal consistency)

Stimulant purgatives (increase GI motility)

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5
Q

Bulk laxatives

A

Polysaccharide polymers e.g. methylcellulose, bran, agar that are not digested in the upper Gi tract. They form a bulky mass in the gut lumen and retain water.

This softens the faecal material (improves consisteny) and promotes increased motility

Take 1-3 days to work, no side effects. First line treatment in constipation and IBS

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6
Q

Osmotic laxatives

A

Consist of poorly absorbed solutes: MgSO4, MgOH and lactulose.

Produce an osmotic load, the agents trap increased volumes of fluid in the lumen

The transfer of gut contents through the small intestine increases.

An abnormally large volume of fluid enters the colon, which causes distension and purgation.

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7
Q

Use of saline purgatives

A

MgSO4 and MgOH result in potent, rapid purgation within 1hr

Used in bowel prep for surgery

Can cause dehydration and electrolyte depletion. Not used in children or renal patients.

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8
Q

How does Lactulose cause purgation?

A

Lactulose is a semi-synthetic dissacharide.

Colonic bacteria convert it into fructose and galactose which are poorly absorbed. Fermentation produces lactic acid and acetic acid, which draws water into the lumen.

Takes 1-3 days to work. Used in negating constipating effects of opiods

Side effects: abdominal cramps, flatulence, nausea, electrolyte disturbance

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9
Q

Faecal softners

A

Surface active compounds that act in the GI tract as a detergent to produce softer faeces.

Act slowly (3-5 days)

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10
Q

Stimulant purgatives

A

Act by increaseing the electrolyte (and water secretion) by the mucosa, and icnrasing peristalsis

Bisacodyl: Stimulates rectal mucosa, resulting in mass movements and defaecation in 15-30mins. Given as a suppository, used for bowel prep

Senna: Anthracene derivative combine with sugars. Passes unchanged into the colon where bacteria release anthracine. These are absorbed and directly act on the myenteric plexus. Inhibits motlility in the proximal colon and increases contraction at the distal colon. Force of mass movements and peristalsis is increased. Act oevr 8hrs, taken at night. Overuse can lead to an atonic colon.

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11
Q

Cathartic colon

A

Anatomical and physiological changes in the colon that occur with chronic use of stimulant laxatives

Results in laxative dependency and tachyphylaxis (high dose of laxatives required)

Can lead to fluid and electrolye imbalance, steatorrhoea, vitamin and mineral deficencies.

Symptoms: bloating, feeling of fullness, abdominal pain, incomlete defaecation

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12
Q

Types of diarrhoea

A

Secretory: Increased active secretion or inhibition of absorption. No structural damage to the GIT

Osmotic: Loss of water due to a heavy osmotic load e.g. maldigestion (Coeliacs) where nutrients remain in the lumen, pulling water into the lumen

Motility: Abnormally high Gi motility decreases time available for absorption of nutrients and water. Can occur in diabetic neuropathy

Inflammatory diarrhoea: Damage to the mucosal lining or brush border leads to a passive loss of protein-rich fluids, decreased ability to absorb lost fluids. Caused by infections and AI disease

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13
Q

Treatment of diarrhoea

A

Maintenance of fluid/electrolyte balance

Anti-diarrhoeal agents

Anti-infective agents (Severe Campylobacter infections - erythromycin/ciprofloxacin)

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14
Q

Antimotility agents used in diarrhoea

A

Opiods: codeine and loperamide

Loperamide has selective action on the GIT. Acts on µ-opiod receptors in the myenteric plexus. Increases tone and rhythmic contrations of the colon, but reduces propulsive activity. Contracts sphincters.

This reduces abdominal cramps and shortens duration of illness.

Used to treat symptoms of uncomplicated diarrhoea in adults.

Chronic use can lead to paralytic ileus, constipation, cramps and dizziness

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15
Q

Antispasmodic drugs used in diarrhoea

A

Muscarinic receptor antagonists e.g. atropine, hyoscine

Inhibit parasympatheic activity.

Used in bowel colic, abdominal cramps assocaited with diarrhoea.

Side effects: dry mouth, blurred vision, urinary retention.

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16
Q

Antacids

A

Bases which counteract stomach acidity. Buffer gastric acid to raise to gastric pH

e.g. MgOH, AlOH, NaHCO3

17
Q

Alignates

A

Amino polysaccharides that bind to water form a viscous gel.

Combined with antacids for use in oesophagitis. Gel floats on the surface of the stomach contents and increases the viscosity of stomach contents. This protects the oesophageal mucosa from acid reflux and reduces the symptoms of reflux.

e.g. sodium alignate, NaHCO3, gaviscon

18
Q

Drugs that protect the gastric mucosa

A

Bismuth chelate

Misoprostol

19
Q

Action of misoprostol

A

Analogue of PGE

Inhibits acid secretion by direct action on parietal cells.
Increases mucosal blood flow
Promotes secretion of mucus and HCO3

Given orally. Used to prevent gastric damage that can occur with use of NSAIDs

Side effects: diarrhoea, stomach cramps, uterine contractions

20
Q

Action of bismuth chelate

A

Coats the mucosa and adsorbs pepsin
Enhances local prostaglandin synthesis
Stimulates HCO3- secretion

Used in combination to treat H. pylori in PUD

Side effects: nausea, vomiting, blackening of tongue and faeces.

21
Q

H2R antagonists

A

Competitively inhibit H2 receptors, which decreases basal and stimulated acid secretion by 90%

Activated in acidic environment.

Side effects: diarrhoea, dizziness, muscle pain. Do not use in hepatic or renal impairment

Cimetidine inhibits CYP450 enzymes

22
Q

Proton pump inhibitors

A

Irreversibly inhibit the H+/K+ ATPase. Drugs accumulate and are activated in parietal cells.

Both basal and stimulated acid secretion decreased

e.g. omeprazole, lasoprazole..

Side effects: headache, diarrhoea, rash

Omeprazole is given orally as enteric capsules and is degraded rapidly in low pH. Half life ~ 1hr but affects secretion for 2-3 days.

23
Q

Consequence of under-secretion of acid secretion

A

Hyperchloria: deficiency of hydrocholric acid in gastric juice.

Causes impaired ability to digest and absorb nutrients e.g. Fe, B vitamins. Increased vulnerability of GIT to bacterial infection.

24
Q

Treatment for reflux oesophagitis

A

Antacids

H2R antagonists

PPIs (prescribed)

25
Q

Treatment of H. pylori infection

A

2 antibiotics and 1 PPI

e.g. amoxicillin, metronidazole, pantoprazole

Elimination of H. pylori produces long term remission of ulcers.

26
Q

Name 3 organisms that cause infective diarrhoea

A

Norovirus

Campylobacter

Shigella

C.diff

Giardia

27
Q

Non-infective causes of diarrhora

A

Laxatives

Antibiotics

Pseudo-diarrhoea: colon cancer and constipation

IBD

28
Q

Drugs used in treatment of IBD

A

Steroids

Aminosalicylates

Immuno-modulators

29
Q

Use of steroids in IBD

A

Used for short periods to induce remission then stopped to minimize side effects.

IV: hydrocortizone

Oral: prednisolone

30
Q

Mesalazine is an aminosalicylate. Why is this given in IBD?

A

Used long-term to maintain remission.

Drugs include balsalazide, mesalazine, olsalazine and sulfasalazine.

Inhibit synthesis of leukotrienes, stimulate prostaglandins, bindto and inactivate free radicals, reduces damage by ROS and inhibit IL-1.

31
Q

Name 4 side effects of aminosalicylates

A

Dyspepsia

Headaches

Fever

Anaemia

32
Q

Name 3 immunomodulators used in IBD

A

Azathioprine

6 Mercaptopurine

Methotrexate

Cyclosporin

33
Q

Action of azathioprine

A

Antimetabolite for purines in nucleic acid synthesis. Modifies lymphocyte and plasma cell function.

Used to maintain remission of UC and Chrons. Takes up to 3 months to act. Allows steroid withdrawal.

Also used as treatment for leukemias, Rheumatoid arthritis and immunosuppresison of transplants.

Side effects: BM supression, nausea/vomiting, pancreatitis

34
Q

Side effects of methotrexate

A

BM supression

Megaloblastic anaemia

Pneumonitis

Teratogenesis

35
Q

Action of cyclosporin

A

Inhibits IL2, IL2R and IFNg production by Th cells.

Inhibits the production of B-cell activating factors.

SIde effects: nephrotoxic, hypertension, neurotoxic