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Gastrointestinal Physiology and Pathophysiology ☆ > Formulations targeting the GIT > Flashcards

Formulations targeting the GIT Flashcards

1
Q

What is used to treat dyspepsia and GORD (3)

A
  1. Antacids
  2. H2-receptor antagonists
  3. Proton pump inhibitors
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2
Q

What is used to treat IBS

A

Antispasmodics

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3
Q

What is used to treat diarrhoea and constipation (3)

A
  1. Oral rehydration therapy
  2. anti-motility
  3. laxatives
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4
Q

What is used to treat IBD

A

Aminosalicylates

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5
Q

What are antacid formulations (6)

A
  1. For relief of the symptoms of gastric hyperacidity – Calcium, aluminium and magnesium salts
  2. Chewable tablets – Sucrose, starch, saccharin & flavouring
  3. Oral suspensions – Faster relief but less convenient
  4. Simeticoneoften included as an antifoaming agent to relieve flatulence – Surface-active agent that ↓ interfacial tension of mucus-embedded gas bubbles
  5. Formulations usually contain calcium, aluminium or magnesium compounds
  6. are best given when symptoms occur or are expected, usually between meals and at bedtime, although additional doses may be required.
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6
Q

What are the properties of aluminium and magnesium-containing antacids (4)

A
  1. Aluminiumandmagnesium-containingantacids are relatively insoluble in water and are long-acting if retained in the stomach. They are suitable for most antacid purposes.
  2. Magnesium-containing antacids tend to be laxative
  3. aluminium-containing antacids may be constipating
  4. antacids containing both magnesium and aluminium may reduce these colonic side-effects.
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7
Q

what are the simeticone infant formulations (2)

A
  1. Oral drops for relief of colic and griping pain
  2. Infacol
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8
Q

What does infacol contain (8)

A
  1. Simeticone
  2. Saccharin Sodium
  3. Hypromellose
  4. Orange flavour
  5. Methyl Hydroxybenzoate 0.18 %w/v
  6. Propyl Hydroxybenzoate 0.02 %w/v
  7. Purified Water
  8. The preservatives (parahydrobenzoates) may cause delayed hypersensitivity reactions
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9
Q

what are the alginate-based formulations (3)

A
  1. Alginic acid – High MW polysaccharide isolated from seaweed
  2. Sodium alginate (soluble Na salt) hydrates quickly in aqueous environments to form a gel
  3. Many formulations comprise antacids/sodium alginate for acid reflux through formation of a floating raft
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10
Q

What is Ranitidine (3)

A
  1. Ranitidine is a specific, rapidly acting histamine H2 antagonist
  2. inhibits secretion of gastric acid
  3. Long duration of action and a single dose effectively suppresses gastric acid secretion for at least 12 hrs
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11
Q

What are the ranitidine formulations (4)

A
  1. No requirement for modified-release formulations
  2. Film-coated immediate release tablets
  3. 75 mg (GSL)
  4. 150 / 300 mg (POM)
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12
Q

What are the ranitidine oral liquids doses (3)

A
  1. 15mg/mL
  2. 30 mg/mL (POM)
  3. Each 10 mL of 30mg/mL oral liquid contains Ranitidine Hydrochloride 336 mg ( = 300 mg Ranitidine )
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13
Q

What excipients does ranitidine contain (5)

A
  1. 1.5 mg propyl hydroxybenzoate
  2. 0.75 mg butyl hydroxybenzoate
  3. 700 mg sorbitol
  4. 800 mg ethanol - this is approximately 7.5 %w/v ethanol
  5. The alcohol should be taken into account in pregnant or lactating women, high-risk groups (alcoholism, liver disease) and children, an alternative formulation of ranitidine may be considered necessary
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14
Q

What do proton pump inhibitors do (3)

A
  1. PPI’s inhibit gastric acid secretion
  2. Block the hydrogen-potassium adenosine triphosphatase enzyme system
  3. The ‘proton pump’ of the gastric parietal cell
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15
Q

What are the PPI gastro-resistant formulations (4)

A
  1. Omeprazole
  2. Esomeprazole
  3. Lansoprazole etc…
  4. Enteric-coated with pH-sensitive polymers, Methacrylic acid (polymethacrylates) & Cellulose acetate
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16
Q

What are gastro-resistant PPI capsules (4)

A
  1. Hard-gelatin capsules filled with enteric-coated pellets
  2. Acid-resistant methacrylic acid – ethyl acrylate copolymer
  3. Pass through stomach (pH 1-2) and dissolve in small intestine (pH 6-7)
  4. The capsules must not be chewed or crushed
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17
Q

What should patients with swallowing difficulties do with gastro-resistant PPI capsules (3)

A
  1. can open the capsule and swallow the contents with water or after mixing the contents in fruit juice
  2. Dispersion should be taken within 30 mins and always be stirred just before drinking and rinsed down with water
  3. Alternatively, patients can suck the capsule and swallow the pellets with water
18
Q

What are Omeprazole MUPS (6)

A
  1. Multiple-Unit Pellet System
  2. Film-coated tablets containing enteric-coated pellets
  3. Patients can break the tablet and disperse it in a spoonful of non-carbonated water and if so wished, mix with some fruit juices or apple sauce.
  4. Patients should be advised that the dispersion should be taken immediately (or within 30 minutes) and always be stirred just before drinking and rinsed down with half a glass of water.
  5. DO NOT USEmilk or carbonated water.
  6. The enteric-coated pellets must not be chewed.
19
Q

What are orodispersible PPI tablets (3)

A
  1. Zoton FasTab – Lansoprazole 15 / 30 mg ODT’s
  2. Rapidly dissolve on the tongue
  3. Can be swallowed whole
20
Q

What highly soluble/hydrophilic excipients do orodispersible PPI tablets contain (4)

A
  1. Mannitol
  2. xylitol
  3. crospovidone (disintegrant)
  4. Release the enteric-coated pellets which must be swallowed without chewing
21
Q

What are the ORT formulations (Oral rehydration therapy (ORT) for treatment of acute diarrhoea and dehydration) (6)

A
  1. Potassium chloride
  2. Sodium chloride
  3. Glucose
  4. Disodium hydrogen citrate
  5. Sachets filled with powders for reconstitution – Increased shelf-life compared with liquids
  6. Pre-cooked rice in some formulations – Enables watery stools to return to normal more rapidly
22
Q

What are the Loperamide HCL formulations (5)

A
  1. Hard gelatin capsules
  2. Basic powder formulation
  3. Freeze-dried formulation
  4. Hygroscopic and must be stored in original sealed blister packs
  5. Orodispersible tablets
23
Q

What are the basic powder loperamide HCL formulations (4)

A
  1. Lactose
  2. Maize starch
  3. Talc
  4. Magnesium stearate
24
Q

What are the freeze-dried loperamide HCL formulations (5)

A
  1. Gelatin
  2. Mannitol
  3. Aspartame
  4. Sodium hydrogen carbonate
  5. Mint flavour
25
Q

What is loperamide hydrochloride used for (4)

A
  1. antimotility drug
  2. the standard treatment when rapid control of symptoms is required.
  3. It can also be used for mild-to-moderate travellers’ diarrhoea (e.g. where toilet amenities are limited or unavailable)
  4. but should be avoided in bloody or suspected inflammatory diarrhoea and in cases of significant abdominal pain.
26
Q

Laxative formulations (3)

A
  1. Bisacodyl 5 mg gastro-resistant tablets (Dulcolax®) –methacrylic acid – methylmethacrylate copolymer enteric coat
  2. Docusate sodium 100 mg liquid filled soft gelatin capsules (Dulcoease®) – Polyethylene glycol (PEG) vehicle
  3. Lactulose oral solution 3.3g/5mL – An example of a product with no additional formulation excipients
27
Q

What is bisacodyl

A

a stimulant laxative also available as suppositories.

28
Q

What is docusate sodium

A

believed to act as both a stimulant laxative and as a faecal softener.

29
Q

What is lactulose (2)

A
  1. a semi-synthetic disaccharide which is not absorbed from the gastro-intestinal tract
  2. an osmotic laxative, which increase the amount of water in the large bowel.
30
Q

What are the antispasmodic drug formulations (7)

A
  1. Hyoscine butylbromide – Buscopan 10 mg tablets
  2. Peppermint oil – Colpermin IBS Relief Capsules
  3. Arachis oil (peanut) based formulation
  4. Liquid-filled enteric-coated capsules - additional band of gelatin around centre of capsule to prevent leakage
  5. Alverine citrate – Spasmonal® 60mg / 120mg immediate-release capsules (P)
  6. Mebeverine hydrochloride – 200mg modified-release capsules (POM) – Hard-gelatin capsules filled with ethylcellulose-coated pellets
  7. The choice of drug treatment depends on the nature and severity of the symptoms. Many drug treatment options for IBS are available over-the-counter.
31
Q

What is the mode of action of peppermint oil antispasmodics (5)

A
  1. The mode of action is local rather than systemic.
  2. The enteric coating delays opening of the capsule until it reaches the distal small bowel.
  3. Peppermint oil is then slowly released as the matrix passes along the gut.
  4. The oil exerts a local effect of colonic relaxation and a fall of intra-colonic pressure.
  5. Pharmacological studies have demonstrated that peppermint oil exerts its inhibitory effect on gastrointestinal smooth muscle by interference with the mobilisation of calcium ions.
32
Q

What drug formulations are there for IBS Diarrhoea and constipation (4)

A
  1. Loperamide HCl liquid-filled soft gelatin capsules – Propylene glycol vehicle
  2. Drug in solution = more rapid absorption – Symptomatic treatment of acute diarrhoea associated with Irritable Bowel Syndrome
  3. Linaclotide 290 mcg capsules (Constella®) – Symptomatic treatment of irritable bowel syndrome with constipation (IBS-C)
  4. Patients with IBS should be advised how on to adjust their dose of laxative or anti-motility drug according to stool consistency, with the aim of achieving a soft, well-formed stool.
33
Q

What is Linaclotide (2)

A
  1. a guanylate cyclase-C receptor agonist that is licensed for the treatment of moderate to severe irritable bowel syndrome associated with constipation.
  2. It increases intestinal fluid secretion and transit and decreases visceral pain.
34
Q

What are Aminosalicylates (5)

A
  1. Prodrug approach to targeting the lower GIT
  2. Active component is chemically bonded to an additional “carrier” compound and only released at site of action
  3. Based on knowledge of colonic microflora
  4. Anaerobic bacteria which are only present in the lower GIT break thefunctional link in the molecule
  5. Sulfazalazine was the first drug to be used in this way – Releasing the active 5-aminosalicylic acid component
35
Q

What are the sulfonamide-related side effects avoided with (4)

A
  1. newer aminosalicylates
  2. Balsalazide
  3. Olsalazine
  4. Mesalazine
36
Q

What are the most common side effects of sulfasalazine (4)

A
  1. headache
  2. nausea
  3. fever
  4. rash
37
Q

What is sulfasalazine (3)

A
  1. Sulfasalazineis a combination of 5-aminosalicylic acid (‘5-ASA’) and sulfapyridine
  2. Sulfapyridine is a carrier to the colonic site of action but still causes side-effects
  3. ~ 90% of a dose reaches the colon where bacteria split the molecule
38
Q

What are the sulfasalazine formulations (3)

A
  1. Salazopyrin Tablets 500 mg – Povidone, Starch, Magnesium stearate, Silicon dioxide
  2. Salazopyrin En-Tabs 500 mg – Cellulose acetate phthalate enteric coating
  3. EN-Tablets should be used where there is gastro-intestinal intolerance of plain tablets. They should not be crushed or broken.
39
Q

Mesalazine (5-ASA) formulations (4)

A
  1. Pentasa® sachets and tablets
  2. Both comprise prolonged release ethylcellulose-coated microgranules of mesalazine
  3. Small granules have a consistent gastric transit time and enter the duodenum within 1 h of administration, independent of food co-administration
  4. Mesalazine is continuously released from the coated microgranules throughout the GIT irrespective of pH
40
Q

Balsalazide disodium formulations (4)

A
  1. Consists of mesalazine linked to a carrier molecule (4-aminobenzoyl-ß-alanine) via an azo bond (-N=N-)
  2. Cleavage of the azo bond by bacteria releases mesalazine as an active metabolite in the colon
  3. Balsalazide and the carrier do not contribute to the pharmacodynamic action
  4. Colazide 750 mg capsules
41
Q

What is olsalazaine disodium (8)

A
  1. An inert dimer of 5-aminosalicylic acid
  2. Cleaved by colonic bacteria to produce two active molecules of 5-ASA
  3. Olsalazine is itself a relatively inert compound.
  4. Absorption in the small intestine is slight.
  5. On entering the colon it is split by bacteria into two molecules of 5-amino salicylate (5-ASA, mesalazine).
  6. 5-ASA is believed to be principal active fragment of sulfasalazine, which has been in use for 40 years in the treatment of ulcerative colitis.
  7. 5-ASA is believed to be the active form of olsalazine sodium as olsalazine has little effect in in-vitro tests or on experimental animals.
  8. The clinical benefits of sulfasalazine, 5-ASA and olsalazine are evident in ulcerative colitis, but the pharmacological mechanism is not established.
42
Q

What formulation is there for olsalazine disodium

A

Dipentum 250 / 500 mg capsules

Gastrointestinal Physiology and Pathophysiology ☆ (24 decks)

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