Chapter Three: Gastro-intestinal System

3.1-Drugs for inflammatory bowel disease.

Notes:
1-Chronic inflammatory bowel diseases (IBD) include crohn’s disease (CD) and
ulcerative colitis (UC) (1). UC is confined to the rectum and colon, while CD can
involve any part of the gastrointestinal (GI) tract (2).
2-The major drug therapies used in IBD are aminosalicylates; corticosteroids;
immunomodulators (azathioprine, mercaptopurine, and methotrexate);
immunosuppressive agents (ciclosporine and tacrolimus); antimicrobials
(metronidazole and ciprofloxacin) monoclonal antibodies (infliximab,
adalimumab, golimumab, certolizumab, natalizumab, ustekinumab, and
vedolizumab) or Janus kinase function (tofacitinib) (2).
3.1.1-Aminosalicylates
1-Aminosalicylates include Sulfasalazine [a combination of 5-aminosalicylic
acid, (‗5-ASA‘) and sulfapyridine (acts as a carrier and believed to be responsible
for many of the adverse reactions to sulfasalazine)], and the safer sulfa-free
compounds [mesalazine (mesalamine)(5-ASA), balsalazide (a pro-drug of 5-ASA)
and olsalazine (a dimer of 5-ASA)] (1-3).
2-The aminosalicylates are among the most commonly used drugs for inducing
and maintaining remission in patients with mild to moderate IBD (4).
3-Enemas are appropriate for patients with
left-sided disease because the medication will
reach the splenic flexure. Suppositories
deliver mesalamine up to approximately 20 cm
and are most appropriate for treating
proctitis (4).
4-Oral and topical mesalamine preparations
may be used together for maximal effect.
Oral mesalamine may also be used for patients
who are unwilling or unable to use topical
preparations (4).
5-The extent of disease should be considered when choosing the route of
administration. If the inflammation is distal, a rectal preparation is adequate but if
the inflammation is extended, systemic medication is required (1).
6-Enemas or suppositories (when given once daily) are preferably administered at
bedtime, preferably after a bowel movement (1).
7-Oral aminosalicylates for the treatment of ulcerative colitis are available in
different preparations and release forms. The preparation and dosing schedule
should be chosen taking into account the delivery characteristics and suitability
for the patient (1).

37
8-Unlike sulfasalazine, sulfa-free compounds are safe to use for patients with
sulfonamide allergies (3).
9-Blood count should be performed and the drug stopped immediately if there is
suspicion of a blood dyscrasia (1).
10-Patients receiving aminosalicylates, and their carers, should be advised to report
any unexplained bleeding, bruising, purpura, sore throat, fever or malaise that
occurs during treatment (Blood disorders) (1).
11-Regarding mesalazine:
A-If it is necessary to switch a patient to a different brand of mesalazine, the
patient should be advised to report any changes in symptoms (1).
B-The manufacturers of some mesalazine gastro-resistant and modified-release
medicines (Asacol MR tablets, Ipocol, Salofalk granules) suggest that
preparations that lower stool pH (e.g. lactulose) might prevent the release
of mesalazine (1).
C-Granules should be placed on tongue and washed down with water without
chewing (1).
12-Olsalazine is associated with a higher incidence of secretory diarrhea than
other aminosalicylates (4).
13-Aminosalicylates are contra-indicated in salicylate hypersensitivity (1).
14-Balsalazide and olsalazine are taken after food (1).
15-Note: sulfasalazine is also used for rheumatoid arthritis [it is one of the
Disease-Modifying Antirheumatic Drugs (DMARDs)] (1).

Aminosalicylates
Scientific name Trade names Dosage form(s)
1

Any extra notes:

38
3.2-Proton pump inhibitors (PPIs)
1-Drug action: Proton pump inhibitors inhibit gastric acid secretion by blocking
the H+/K+-ATPase (the ‗proton pump‘) of the gastric parietal cell (1).
2-PPIs are the most potent inhibitors of gastric acid secretion. PPIs include
omeprazole, lansoprazole, rabeprazole, pantoprazole, and esomeprazole (2).
3-PPIs are used for the treatments of gastric and duodenal ulcers; they are also
used in combination with antibacterials for the eradication of Helicobacter
pylori (a bacteria that is common cause of ulcer). PPIs can be used for the
treatment of dyspepsia and gastro-oesophageal reflux disease. They are also
used for the prevention and treatment of NSAID-associated ulcers (1).
4-A PPI can be used to reduce the degradation of pancreatic enzyme
supplements in patients with cystic fibrosis. They can also be used to control
excessive secretion of gastric acid in Zollinger–Ellison syndrome; high doses are
often required (1).
5-PPIs are most effective when taken 30 to 60 minutes before meals (3).The once
daily dose usually given in the morning before meals. Large doses should be
given in 2 divided doses (1) (for divided dosing, give evening dose before evening
meal instead of at bedtime) (5).
6-PPIs may take up to 72 hours to achieve optimal effectiveness and symptom
improvement (6).
7-Newer PPIs (omeprazole-sodium bicarbonate and dexlansoprazole) offer
dosing flexibility in relation to meals (5).
8-Controversial PPI drug interaction involves the antiplatelet drug clopidogrel.
Clopidogrel is converted to its active form through CYP2C19. PPIs may attenuate
the antiplatelet effect of clopidogrel by inhibiting or competing for this metabolic
pathway. FDA safety guidelines recommend that the coadministration of
omeprazole, omeprazole/sodium bicarbonate, or esomeprazole with clopidogrel be
avoided because they reduce the effectiveness of clopidogrel (2). The 2013 ACG
guidelines consider the PPI/clopidogrel interaction not clinically significant (5).
Given the limitations of existing studies, administration of clopidogrel with
PPIs should be balanced based upon cardiovascular and gastrointestinal risk
(2)
.
9-PPIs are formulated as delayed-release enteric-coated dosage forms that have
pH-sensitive granules contained in gelatin capsules (omeprazole, esomeprazole,
and lansoprazole), rapidly disintegrating tablets (lansoprazole), and delayed-release
enteric-coated tablets (rabeprazole, pantoprazole, and nonprescription omeprazole).
Omeprazole is also available in a delayed-release tablet and in a combination
product with sodium bicarbonate in an immediate-release capsule and oral
suspension (Zegerid®) (2). The sodium bicarbonate raises intragastric pH,
permitting rapid absorption of omeprazole from the duodenum (7).

39
10-Special administration:
A-Orodispersible lansoprazole tablets should be placed on the tongue, allowed
to disperse and swallowed, or may be swallowed whole with a glass of water.
Alternatively, tablets can be dispersed in a small amount of water and
administered by an oral syringe or nasogastric tube (1).
B-Losec MUPS®: Tablets (Losec MUPS®) or capules (Losec ®) containing
enteric-coated pellets can be dispersed in non-carbonated water or a slightly
acidic liquid e.g. fruit juice or apple sauce; do not use milk or carbonated water.
The dispersion should be stirred just before drinking and taken immediately,
rinsed down with half a glass of water. The enteric-coated pellets must not be
chewed (1).
C-For patients who are unable to swallow the capsule or for pediatric
patients, there are several alternative administration methods available. The
contents of the delayed-release capsules can be mixed in applesauce or placed
in orange juice. If a patient has a nasogastric tube, the contents of an
omeprazole capsule can be mixed in 8.4% sodium bicarbonate solution.
Esomeprazole granules can be dispersed in water. Esomeprazole, omeprazole,
and pantoprazole are also available in a delayed-release oral suspension powder
packet, and lansoprazole is available as a delayed-release, orally disintegrating
tablet (2).
11-PPIs can increase the risk of fractures (particularly when used at high doses
for over a year in the elderly). Patients at risk of osteoporosis should maintain an
adequate intake of calcium and vitamin D and if necessary, receive other
preventative therapy (1).
12-PPIs are generally considered interchangeable; selection of agent is usually
based on cost and formulary considerations (6).
PPIs
Scientific names Trade name Dosage form

Any extra notes:

41
3.3-Histamine-2 receptor antagonists (H2RAs)
1-Drug action: H2RAs reduce gastric acid output as a result of histamine H2-
receptor blockade (1).
2-H2RAs include cimetidine, ranitidine, famotidine, and nizatidine (2).
3-H2RAs are used for the treatments of gastric and duodenal ulcers. They can be
used for the treatment of dyspepsia and gastro-oesophageal reflux disease (1).
4-Aspiration of gastric contents (Mendelson‘s syndrome) is a potential cause of
morbidity and mortality associated with anesthesia, especially in obstetrics and in
emergency surgery (8). H2RAs also reduce the risk of acid aspiration (1).
5-Cimetidine has been used alone or with an antihistamine (H1-antagonist) in
various skin disorders. H2RAs such as cimetidine and ranitidine have produced
improvement in certain types of urticaria (8).
6-Cimetidine inhibits several CYP450 isoenzymes, resulting in numerous drug
interactions (e.g., theophylline, warfarin, and clopidogrel) (2). Avoidance of the
combination, or a reduction in the dosage of these drugs may be required (8).
7-Ranitidine has less potential for hepatic CYP450 drug interactions, while
famotidine and nizatidine do not interact with drugs metabolized by the hepatic
CYP450 pathway (3).
8-Cimetidine has demonstrated weak antiandrogenic effects, and its use in high
doses has been associated with gynecomastia and impotence in men. This effect
is reversible with discontinuation of the medication or by switching to another
H2RA (3).
9-Regaeding H2RAs use for gastro-oesophageal reflux disease (GERD):
Tolerance to the antisecretory effect may develop after several days of
regularly scheduled (continuous) use but can be avoided by taking the H2RA
only when needed (3).
H2RAs
Scientific names Trade name Dosage form

Any extra notes:

41
3.4-Treatment of H. pylori–associated ulcers
1-H. pylori is a common cause of both gastric and duodenal ulcer. General
recommendations, are to include an antisecretory agent (preferably a PPI) plus at
least two antibiotics in the eradication regimen (5).
(5)
2-Therapy duration is usually 10–14 days .
3-Several first-line therapies are recommended, but bismuth quadruple therapy
(bismuth subsalicylate, metronidazole, tetracycline, and a PPI ) for 10-14 days
should be used preferentially (2). (Table 3-1)
4-Another recommended first line therapy is concomitant therapy (PPI,
clarithromycin, with amoxicillin and metronidazole) for 10 to 14 days (2).
5-Clarithromycin triple therapy is no longer recommended in areas where H.
pylori resistance exceeds 15% (2).
6-Sequential therapy: Sequential therapy involves administration of a PPI and
amoxicillin given for the first 5 days, followed by a PPI, clarithromycin, and
tinidazole for an additional 5 days (5).
7-Quadruple-based therapy:
A-Bismuth subsalicylate, metronidazole, tetracycline, and a PPI (5).
B-Nonbismuth quadruple therapy (also called ―concomitant‖ therapy)
contains a PPI, amoxicillin, clarithromycin, and metronidazole taken together
at standard doses for 10 -14 days (2).
8-Hybrid therapy (combines the strategies of concomitant and sequential therapy)
involves 7 days of dual therapy (PPI and amoxicillin) followed by 7 days of
quadruple therapy (PPI, amoxicillin, clarithromycin, and metronidazole) (2).
9-Levofloxacin-Based Therapy
Levofloxacin has been studied as first-line therapy and (after initial treatment
failure) for H. pylori eradication. Three regimens using levofloxacin have been
suggested (levofloxacin triple therapy, levofloxacin sequential therapy and
Quadruple therapy) (Table 3-1). Concerns about using fluoroquinolones to
treat H. pylori include development of resistance and adverse effects (e.g.,
tendonitis and hepatotoxicity) (2).

42
Table 3-1. Recommended Treatment Regimens for Helicobacter pylori
Infection (5).

BID: twice daily; PPI : proton pump inhibitor; QID : four times daily; TID : three times daily.

43
3.5-Antacids:
1-Antacids are basic compounds that neutralize hydrochloric acid in the gastric
secretions. They are used in the symptomatic management of gastrointestinal
disorders associated with gastric hyperacidity such as dyspepsia, GERD, and
peptic ulcer disease (8).
2-Antacid agents include a variety of aluminum, magnesium, and calcium
products available as single and combination therapy preparations in multiple
dosage forms (6).
3-Antacids are best given when symptoms occur (i.e. when required) or are
expected, usually between meals and at bedtime (1). When taken 1 h after a meal,
antacids may act for up to 3 h compared with only 30 min–1 h if taken before
meals (9).
4-Liquids and powders generally provide faster relief and have greater
neutralizing capacity than tablets. Advantages of tablets over liquids include ease
of portability and administration (10). It might be appropriate for the patient to have
both; the liquid could be taken before and after working hours, while the tablets
could be taken during the day for convenience (9).
5-Tablets should not be swallowed whole; they should be chewed to initiate
disintegration or sucked to provide a relatively slow but sustained delivery of
antacid to the stomach (10).
6-Interactions:
A-Antacids can affect the absorption of a number of drugs (via chelation and
adsorption) (11). This interactions can usually be avoided when potentially
interacting drugs are separated by at least 2 hours (7).
B-Antacids also interact with enteric-coated tablets, capsules and granules
(Enteric coatings may be disrupted prematurely in the presence of antacids,
causing unwanted release of the drug in the stomach) (10).
7-Side effects of antacids:
A-AL-containing antacids tend to be constipating. Mg-containing antacids tend
to cause osmotic diarrhea and are useful in patients who are slightly
constipated. Thus combination products of AL and Mg salts cause minimum
bowel disturbances (9).
B-Antacids containing sod. Bicarbonate: The high sodium content may cause
fluid overload in patients with congestive heart failure, renal failure, cirrhosis,
or pregnancy, and in those on sodium restricted diets (7).
C-Calcium carbonate: It acts quickly, has a prolonged action and is a potent
neutralizer of acid. It can cause acid rebound and, if taken over long periods at
high doses, can cause hypercalcaemia and so should not be recommended for
long-term use (9).

44
8-Other drugs that may be combined with antacid formulations include
simeticone, which acts as a defoaming agent to reduce excess gas in the stomach,
and alginates, which form a gel or foam on the surface of the stomach contents
thereby impeding reflux and protecting the oesophageal mucosa from acid
attack (8).

Antacids (including those combined with simethicone, and alginate)

Scientific names Trade names Dosage form
1

Any extra notes:

3.6-Laxatives:
1-Laxatives (purgatives or cathartics) promote defecation and are used in the
treatment of constipation and for bowel evacuation before investigational
procedures such as endoscopy or radiological examination, or before surgery (8)
to ensure the bowel is free of solid contents (1).
(10)
2-Laxatives can be classified into groups depending on their mode of action
(Table 3-2).
Table 3-2: types of laxatives
Type of laxative Example(s) Approximate onset
of action
Senna, Bisacodyl, Sodium Oral:6-12hours (9)
1-Stimulant laxative picosulfate, and Glycerin (supp.) Rectal: within 1
hour (9)
Methylcellulose, Bran , Sterculia 12 -24 hours, but
2-Bulk-forming and Ispaghula (Metamucil®) onset may be
laxative delayed as long as
72 hours (7)
4-Osmotic laxative Lactulose 1-2 days (9)
45
 Linaclotide (guanylate cyclase-C receptor agonist),
5-Othrs Prucalopride (selective serotonin 5HT4-receptor agonist
with prokinetic properties) (1).
3.6.1-Stimulant laxatives:
1-Stimulant laxatives are thought to act mainly by stimulating the intestinal
mucosa to secrete water and electrolytes (12).
2-The main adverse effects of stimulant laxatives are griping and intestinal
cramps. Prolonged use may result in loss of colonic smooth muscle tone (10) .
However, many experts now believe that the risk of long-term use of stimulant
laxatives use have been overestimated and they are safe for daily use) (13).
3-Bisacodyl tablet is enteric-coated; therefore, it should be swallowed whole and
should not be taken within one hour of antacid or milk as this will lead to
dissolution of the coating and release of the drug into the stomach and cause
gastric irritation (10).
4-Senna is excreted via the kidney and may color the urine a yellowish-brown to
red color depending on its PH (12).
5-Senna is secreted in breast milk, and large dosages may cause increased gastric
motility and diarrhea in breastfed infants. Breastfeeding mothers should, therefore,
avoid this laxative (12). (However BNF-81 states that specialist sources indicate
suitable for use in breast-feeding in infants over 1 month (1)).
6-Usual doses:
Bisacodyl 5 mg tab. Adult dose: usually 1-2 tablets (dose to be taken at night).
While the dose of supp. Is one supp. (usually in the morning) (1).
Senna tab. Adult dose: usually 2 tablets (preferably at bedtime) (11).
Glycerin suppositories: Glycerol suppositories are normally used when a bowel
movement is needed quickly. The patient should experience a bowel movement in
15 to 30 minutes. Varying sizes are made to accommodate use for different ages.
The 1-g suppositories are designed for infants, the 2-g for children and the 4-g for
adults. (11).
3.6.2-Bulk-forming laxative:
1-Bulk laxatives are those that most closely resemble the normal physiological
mechanisms involved in bowel evacuation. Bulk laxatives work by swelling in the
gut and increasing faecal mass so that peristalsis is stimulated . The laxative effect
can take several days to develop (9).
2-Bulk laxatives should not be taken immediately before going to bed, because
there may be a risk of oesophageal blockage if the patient lies down directly after
taking them (10).
3-When recommending the use of a bulk laxative, the pharmacist should advise
that an increase in fluid intake would be necessary (9).
4-Adverse effects and disadvantages are relatively minor. They include:
46
  Risk of oesophageal and intestinal obstruction if preparations are not taken
with sufficient water.
 Abdominal distension and flatulence.
 They may not be suitable for patients who must restrict their fluid intake
severely (12).
5-Bulk-forming drugs are useful in controlling diarrhea associated with
diverticular disease (1).
3.6.3-Liquid paraffin:
Liquid paraffin is considered to have a limited usefulness as an occasional laxative
in situations where straining at stool must be avoided (for example, following an
operation or a myocardial infarction), but it has several drawbacks that make it
unsuitable for regular use (12) (it should never be recommended because other, safer
and more effective medications are available) (11):
-It can seep from the anus and cause irritation.
-It may interfere with the absorption of fat soluble vitamins.
-It is slightly absorbed into the intestinal wall, where it may set up foreign-body
granulomatous reactions.
-It may enter the lung through aspiration and cause lipoid pneumonia (12).
3.6.4-Lactulose:
1-It can be taken by all age group, have no drug interactions and can be safely used
in pregnancy (11). However, there are some factors that may deter patients from
using lactulose: It may take 72 hours of regular dosing to produce an effect. It is
intensely sweet in taste which makes it more palatable for children, to whom it
can be given safely (10). Adult laxative dose (1): 15 ml twice daily.
2-Serious adverse effects with lactulose are rare. Relatively minor side-effects
occur in about 20% of patients taking full doses and include flatulence, cramp and
abdominal discomfort, particularly at the start of treatment (12).

3-Lactulose syrup should be used with caution in diabetic patients because it

contains lactose and galactose (14).
4-Lactulose produces an osmotic diarrhea of low faecal pH, and discourages the
proliferation of ammonia-producing organisms. It is therefore useful in the
treatment of hepatic encephalopathy (1).
3.6.5-Product selection guidelines (Table 3-3).
Table 3-3:Product selection guidelines
Patient Preferred laxative
Pregnant women Bulk-forming laxative. Lactulose may be used (13)
Breast-feeding mother Bulk-forming laxative, lactulose (13)
Children Glycerin(supp.), lactulose (13)
Advanced age(elderly) Bulk-forming laxative, also lactulose and glycerin
(supp.) are safe (7, 11).
47
 Laxatives (try to include the different types of laxatives )
Scientific name Trade names Type Dosage form(s)
1

Any extra notes:

3.7-Antidiarrheals
The priority in acute diarrhea is the prevention or reversal of fluid and electrolyte
depletion. This is particularly important in infants and elderly patients. Oral
rehydration preparations are used in the prevention or reversal of fluid and
electrolyte depletion. Severe depletion of fluid and electrolytes requires immediate
admission to hospital and urgent replacement treatment with an intravenous
rehydration fluid is recommended (1).
3.7.1-Antimotility drugs
[Loperamide , Co-phenotrope (Diphenoxylate+Atropine)]
Note: Atropine is included at a subtherapeutic dose to discourage abuse
(unpleasant antimuscarinic effects will be experienced if higher than recommended
doses are taken)] (12).
1-Antimotility drugs are not recommended for acute diarrhea in young children (1).
In the UK, diphenoxylate hydrochloride is not licensed for children under 4 years
of age. In the UK, loperamide is not licensed for children under 4 years of age.
In the USA, loperamide is not recommended for children under the age of 2 years
(8)
.
2-Adult doses :
Loperamide: Initially 4 mg (2 tablets or capsules) , followed by 2 mg (1 tablet or
capsule) to be taken after each loose stool; usual dose 6–8 mg daily; maximum 16
mg per day (1).

48
Co-phenotrope: Initially 4 tablets, followed by 2 tablets every 6 hours until
diarrhea controlled (1).
3.7.2-Adsorbents (pectin +kaolin)
1-There is insufficient evidence to recommend adsorbent preparations (such as
kaolin) in acute diarrhea (1).
2-Kaolin can form insoluble complexes with some drugs in the gastrointestinal
tract and reduce their absorption; oral doses should not be taken at the same
time (8).
3.7.3-Oral rehydration solution (ORS)
1-A premixed solutions (7) or sachets of powder for reconstitution are available;
these contain sodium as chloride and bicarbonate, glucose and potassium (9).
2-Only water should be used to make the solution and that boiled and cooled
water should be used for children < 1 year (9).
3-To avoid risk of possible exposure to further infection, the solution should be
discarded not later than 1 hour after reconstitution, or it may be kept for up to 24
hours if stored in a refrigerator (10).
Table 3-4:Amount of rehydration
4-Table 3-4 provides the volumes
(9) solution to be offered to patients (9).
required per watery stool .
Age Quantity of solution (per
3.7.4-Probiotics (dietary watery stool)
supplement): Under 1 year 50 mL (quarter of a glass)
Probiotics are dietary supplements 1–5 years 100 mL (half a glass)
containing bacteria (including 6–12 years 200 mL (one glass)
several Lactobacillus species) that Adult 400 mL (two glasses
may promote health by enhancing
the normal microflora of the GI tract while resisting colonization by potential
pathogens (4). Probiotics have been shown to decrease the duration of infectious
and antibiotic-induced diarrhea (AAD) in adults and children (2).
3.7.5-Use of zinc in children with diarrhea:
Several large studies performed in developing countries have shown that daily
zinc supplementation in young children with acute diarrhea reduces both the
duration and severity of diarrhea. The WHO/UNICEF recommends that children
with acute diarrhea also receive zinc (10 mg of elemental zinc/day for infants
younger than 6 months; 20 mg of elemental zinc/day for older infants and children)
for 10 to 14 days (7).
Antidiarrheals
Scientific name Trade names Dosage form
1

49
3

Any extra notes:

3.8-Antispasmodics
1- Antispasmodics are drugs used for their relaxant action on smooth muscle. They
play a role in the management of gastrointestinal spasm and irritable bowel
syndrome (IBS) as well as other disorders associated with smooth muscle spasm
(8)
.
2-Antispasmodics include antimuscarinics (e.g. hyoscine butylbromide). Other
antispasmodics (mebeverine, alverine citrate, and peppermint oil) are used to
relieve pain in irritable bowel syndrome (1).
3-Conerning IBS (1):
A-Laxative (excluding lactulose as it may cause bloating) can be used to treat
constipation in IBS.
B-Loperamide is the first-line choice of anti-motility drug for relief of
diarrhea in IBS.
C-A low-dose tricyclic antidepressant, such as amitriptyline, can be used for
abdominal pain or discomfort as a second line option in patients who have not
responded to antispasmodics. A selective serotonin reuptake inhibitor may
be considered in those who do not respond to a tricyclic antidepressant.
Antispasmodics
Scientific name Trade names Dosage form
1

Note: antichloinergics may be combined with benzodiazepine (librax®) or

phenothiazine (stelabid®). Also they may be combined with an analgesics. They
areused for GIT disorders associated with smooth muscle spasm (8).
Compound anticholinergics
Trade names Scientific name Dosage form
Librax®

Stelabid®

51
Antispasmine-
co®

Riabal-co®

Any extra notes:

3.9-Nausea and vomiting

1-Prochlorperazine, metoclopramide and domperidone are used to treat or
prevent nausea and vomiting (1).
2-Cinnarizine is used to prevent motion sickness where the dose is taken 2 hours
before travel then every 8 hours if required (1).
3-Domperidone has the advantage over metoclopramide and the
prochlorperazine of being less likely to cause central effects such as dystonic
reactions (a tetanus-like reaction) because it does not readily cross the blood-
brain barrier (1).
4-Granisetron, ondansetron and palonosetron (5HT3-receptor antagonists) are of
value in the management of nausea and vomiting in patients receiving cytotoxics
and in postoperative nausea and vomiting (1).
5-Dexamethasone has antiemetic effects and it is used in vomiting associated
with cancer chemotherapy. It can be used alone or with metoclopramide,
prochlorperazine, lorazepam, or a 5HT3-receptor antagonist (1).
6-Aprepitant, fosaprepitant, and rolapitant are neurokinin 1-receptor antagonists.
They are licensed for the prevention of nausea and vomiting associated with
chemotherapy (1).
7-Doxylamine (antihistamine ) with pyridoxine (B6) combination is used for
nausea and vomiting in pregnancy (1).
8-Hyperemesis gravidarum (a severe nausea and vomiting during pregnancy) (4)
is a more serious condition, which requires regular antiemetic therapy,
intravenous fluid and electrolyte (1).
9-Domperidone, metoclopramide, 5HT3-receptor antagonists, and the
phenothiazines (except the antihistamine phenothiazine promethazine) are
ineffective in motion sickness (1).
10-I.V Metoclopramide doses should be administered as a slow bolus over at
least 3 minutes. Oral liquid formulations should be given via an appropriately
designed, graduated oral syringe to ensure dose accuracy (1).
51
11-Metoclopramide dose: Adult (body-weight up to 60 kg): Up to 500 mcg/kg
daily in 3 divided doses. Adult (body-weight 60 kg and above): 10 mg up to 3
times (1).
12-Side effects:
A-Cinnarizine may cause drowsiness which may affect performance of skilled
tasks (e.g. cycling, driving) (1).
B-Domperidone is associated with a small increased risk of serious cardiac
side-effects (arrhythmia). Patients and their carers should be told how to
recognize signs of arrhythmia and advised to seek medical attention if
symptoms such as palpitation or syncope develop (1).
C-Metoclopramide can induce acute dystonic reactions involving facial and
skeletal muscle spasms and oculogyric crises. These dystonic effects are more
common in the young (especially girls and young women) and the very old;
they usually occur shortly after starting treatment with metoclopramide and
subside within 24 hours of stopping it (1).
Antiemetics
Scientific name Trade names Dosage form(s)
1

Any extra notes:

3.10-Anti-obesity drugs
1-An anti-obesity drug should be considered only for those with a BMI of ≥ 30
kg/m2, in whom diet, exercise and behavior changes fail to achieve a realistic
reduction in weight. In the presence of associated risk factors, it may be
appropriate to prescribe an anti-obesity drug to individuals with a BMI of ≥28
kg/m2 (1).
2-Orlistat is a gastric and pancreatic lipase inhibitor that reduces the absorption of
dietary fat. Other drugs used for obesity is liraglutide (1).

52
3-Orlistat is given in a usual dose of 120 mg orally three times daily, immediately
before, during, or up to 1 hour after meals. If a meal is missed or contains no
fat, the dose should be omitted (1).
4-Treatment with orlistat may also be used to maintain weight loss rather than to
continue to lose weight (1).
5-Discontinuation of treatment with orlistat should be considered after 12 weeks if
weight loss has not exceeded 5% since the start of treatment (1).
6-Orlistat may reduce the absorption of fat-soluble vitamins (A, D, E, and K)
and patients should take a multivitamin supplement that contains these vitamins.
The supplement should be taken once a day at least 2 hours before or after the
administration of orlistat, such as at bedtime (3).
7-Because orlistat‘s main effect is to prevent dietary fat from being absorbed, the
fat is excreted unchanged in the feces and so the stool may become oily or loose
(steatorrhoea) (9).
8-Increased flatulence is also common. Bowel movements may become
frequent or urgent, and cases of fecal incontinence have been seen (9).
9-To minimize these effects, foods with high fat content should be avoided.
Taking drugs for diarrhea (such as loperamide) will not control these symptoms (9).
10-It is important to have adopted the low fat diet a few days before introducing
orlistat. Oily stools and flatulence can be controlled by reducing the dietary fat
content to somewhere in the region of 15 g per meal, and it has been suggested
that the decrease in side effects over time may be associated with long-term
acceptance and adoption of a low fat diet (9).
11-Liraglutide (Saxenda®) [a glucagon-like peptide-1 (GLP-1) receptor agonist].
A-Liraglutide, is an injectable medication, FDA-approved for long-term
obesity management as an adjunct to lifestyle modification. When used for
obesity, the dose is titrated to 3 mg daily (3).
B-If the patient has not experienced ≥4% weight loss by 16 weeks after
initiating therapy, the drug should be discontinued (3).
C-It is also marketed under the brand name Victoza® at a dose of 1.8 mg daily
for the treatment of type 2 diabetes (3).
Scientific name Trade names Dosage form
Orlistat

Liraglutide

Any extra notes:

53
3.11-Local preparations for anal and rectal disorders
1-These products are used mainly for hemorrhoids, pruritus ani and anal fissure
(1)
.
2-They are usually formulated as ointments and creams or suppositories.
Ointments and creams can be used for internal and external hemorrhoids while
suppositories are used for internal hemorrhoids. However both are used twice
daily (morning and evening) and after each bowel movement (9).
3-Many people prefer suppositories, but these products are often not effective
because they tend to slip into the rectum and melt, thus bypass the anal canal
where the medication is needed. In general ointments and creams are preferred
over suppositories (13).
4-When used intrarectally, the ointment may be inserted using an applicator or
finger but the applicator is preferred because it can reach an area where the
finger cannot reach. The applicator should be lubricated by the ointment before
insertion (7).
5-Topical preparations that contain a combination of local anaesthetics,
corticosteroids, astringents, lubricants, and antiseptics are available. They can
offer symptomatic relief of local pain and itching (1).
6-Long-term use of corticosteroid creams can cause ulceration or permanent
damage due to thinning of the perianal skin and should be avoided (1).
Local preparations for anal and rectal disorders
Scientific name Trade names Dosage form
1

Any extra notes:

3.12-Liver disorders (and related conditions), exocrine pancreatic

insufficiency.
1-Ursodeoxycholic acid is a naturally occurring bile acid. It is used for the
dissolution of cholesterol-rich gallstones in patients with functioning gallbladders.
Ursodeoxycholic acid is also used in primary biliary cirrhosis (8) (It slows disease
progression) (1).
2-Terpenes (Borneol with camphene, cineole, menthol, menthone and pinene)
(Rowachol® Capsule) are used for Biliary disorders (to be taken before food) (1).

54
3-Exocrine pancreatic insufficiency can result from chronic pancreatitis, cystic
fibrosis, obstructive pancreatic tumours, coeliac disease, Zollinger-Ellison
syndrome, and gastrointestinal or pancreatic surgical resection.
Exocrine pancreatic insufficiency is characterized by reduced secretion of
pancreatic enzymes into the duodenum. The main clinical manifestations are
maldigestion and malnutrition, associated with low circulating levels fat-soluble
vitamins. Patients also present with gastro-intestinal symptoms such as diarrhea,
abdominal cramps and steatorrhoea (1).
4-Pancreatic enzyme replacement therapy with pancreatin is the mainstay of
treatment for exocrine pancreatic insufficiency (1).
5-Pancreatin contains the three main groups of digestive enzymes: lipase, amylase
and protease. These enzymes respectively digest fats, carbohydrates and proteins
so that they can be absorbed and utilized by the body. Pancreatin should be
administered with meals (or immediately before or after food) (1).
6-Directions for administration of pancreatin
●Pancreatin is inactivated by gastric acid therefore manufacturer advises
pancreatin preparations are best taken with food (or immediately before or
after food) (1).
●Since pancreatin is inactivated by heat, excessive heat should be avoided if
preparations are mixed with liquids or food; manufacturer advises the resulting
mixtures should not be kept for more than one hour and any left-over food or
liquid containing pancreatin should be discarded (1).
●Manufacturer advises gastroresistant granules should be mixed with
slightly acidic soft food or liquid such as apple juice, and then swallowed
immediately without chewing (1).
●Capsules containing enteric-coated granules can be opened and the granules
administered in the same way (1).
●For infants, Creon ® Microgranules can be mixed with a small amount of
milk on a spoon and administered immediately (granules should not be added to
the baby‘s bottle) (1).
Scientific name Trade names Dosage form
Ursodeoxycholic acid

Pancreatin

55