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> Antacids: weak bases that react with hydrochloric acid to form salt & water.
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Used in the treatment of Hyperacidity, GERD, PUD, hyperphosphatemia, and calcium deficiency
Contain combinations of
= metallic cation (aluminum, calcium, magnesium, and sodium)
= and basic anion (hydroxide, bicarbonate, carbonate, citrate, and trisilicate)
> Pharmacodynamics, Pharmacokinetics, Pharmacotherapeutics
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Neutralize Gastric Acidity (causes “pH of the stomach and duodenal bulb)
Inhibit proteolytic activity of pepsin
Increase lower esophageal sphincter tone
Acid-neutralizing capacity ANC varies between products expressed in mEqs
If ingested in a fasting state, antacids reduce acidity for approximately 20 to 40 minutes
If taken 1 hr after a meal, acidity is reduced for 2 to 3 hrs
Asecond dose taken after a meal maintains reduced acidity for more than 4 hrs after the meal
The action of antacids occurs locally in the GI tract with minimal absorption, minimal metabolism
ALL antacids are Contraindicated in the presence of severe abdominal pain of unknown/cause, especially i
accompanied by fever
-HIGH SODIUM content: pts w/ HTN, CHF, marked renal failure, or on low-sodium diets need to use low sodium
preparation
-Concurrent administration with enteric-coated drugs, destroys the coating= alters absorption, * the risk for
adverse effects
-Administrations should be separated by at least 2 hours to decrease drug/drug interactions
Calcium based antacids: TUMS, Caltrate, Calcarb
¢ Prescribed to treat calcium deficient states, i.e. chronic renal failure, post-menopause, and osteoporosis
e Used to bind phosphates in CRF
e Require Vitamin D for absorption from the Gl tract
¢ — Excreted mainly in feces, 20% in urine
¢ ADR: Contraindicated in the presence of hypercalcemia and renal calculi
* Can cause constipation- increase bulk, fluids and mobility, stool softener
e¢ Administered 30min- 1hr on empty stomach or 3hr after meals
e Should not be administered with food containing large amounts of oxalic acid (spinach, rhubarb), or
phytic acid (bran, cereals), they decrease the absorption of calcium
¢ Taking w/ foods containing phosphorus (milk, dairy) can lead to milk-alkali syndrome (N/V, confusion,
headache).
¢ Taking with acidic fruit juice improve absorption
2. Aluminum based: AlternaGEL, Amphojel, Mylanta
‘Aluminum is not}
removed by dial
it is bound to alb}
& transferrin = df
cross dialysis
Fasily
is b/c
min
membrane
a.
e — Inhibit smooth muscle contraction and slow gastric emptying
e Used to bind phosphates in CRF
Not absorbable with routine use
¢ Aluminum concentrated in the CNS
¢ Bind with phosphate and excreted in feces
Prolonged use in patients with renal failure may result in dialysis osteomalacia
.
{ 0 Aluminum deposits in bone and osteomalacia occurs
.
Elevated aluminum tissue levels contribute to the development of dialysis encephalopathy
e Used to treat hyperphosphatemia in pts w/ renal failure & phosphate renal stone prevention
* Can cause constipation- increase bulk, fluids and mobility, stool softener
3. Magnesium based: Milk of mag, Maalox, Mylanta
‘The malfune
kidney canno}
excrete magr
hypermagne:
ning;
fesiumé
femia
e Can be used to treat magnesium deficiencies from malnutrition, alcoholism, or mag-depleting drugs
© ~ Contraindicated in patients with renal failure & used with caution in pts with renal insufficiency
° Not absorbable with routine use
e — Excreted in the urine
* — Contraindicated in patients with renal failure, use with caution for patients with any degree of renal
insufficiency
O Malfunctioning kidney is unable to excrete magnesium and hypermagnesemia may result
© Can cause diarrhea- increase fiber intake (Alkalosis may occur in renal impairment)
Clinical Use and Dosing
yr Pe eticay
Aluminum hydroxide Hyperphosphatemia
Pree cy
Adolescents or adults:
300-600 mg 3 or 4 times a day,
max 3,000 mg/day
Children: 30 mg/kg/day
AllernaGEL. Hyperacidity
Liquid: 600 mg/5 mt.
Adulis: Tablets or capsules:
Amphojel Tablets: 300 mg, 600 mg 500-1,500 mg 3-6 times daily
Alu-Tab Tablets: 500 mg between meals and at bedtime
Alu-Cap Capsules: 500 mg (sodium content Suspension: 5-30 m1. prn between
Generic <1.2 mg) meals and at bedtime
Suspension: 320 mg/5 mL Children: 300-900 mg per dose
Concentrated suspension: 450 mg/5 mL between meals and at bedtime
Concentrated suspension:
675 mg/5 mL.
Concentrated liquid: 600 mg/S mI.
Calcium carbonate Calcium deficiency in chronic Adulis: 1-2 g/day in divided doses
renal failure
Children: 45-65 mg/kg/day in
4 divided doses
Adjust dose based on serum calcium
concentration
Alka-Mints Postmenopause or osteoporosis
‘Tablets, chewable: 850 mg (sodium
Adults: 1,000-1,500 mg elemental
Tums Hyperacidity content <5 mg) calcium/d
‘Tablets, chewable: 500 mg (sodium Children >11 yr and adults: T'UMS
content <2 mg) (500 mg calcium carbonate) chew
Maalox Chewables Extra-strength, chewable: 750 mg 2-4 tablets for symptoms, not to
Generic (sodium content <4 mg) exceed 15 tablets/d; TUMS E-X
Ultra, chewable: 1,000 mg (sodium (750 mg calcium carbonate)
content <4 mg) chew 2-4 tablets for symptoms,
Lablets: 600 mg not to exceed 10 tablets/d
Tablets: 500, 600, 650, 1,250 mg Children 5 yr to 11 yr: 800 mg calcium
carbonate for symptoms; do not
exceed 4,800 mg/d
Children 2-5 yr: 400 mg as needed; do
not exceed 1,200 mg/d
Magnesium hydroxide Hyperacidity Tablets: 311 mg Children >12 yr and adults:
Phillips’ Chewables Liquid: 400 mg/5 mL ‘Tablets: 622-1,244 mg up to qid
Phillips’ Milk of Magnesia Concentrated liquid: 800 mg/5 ml. Liquid: 5-15 ml. up to qid with water
Generic Liquid: 400 mg/5 mL Liquid concentrate: 2.5-7.5 mL up to
qid with water
Phillips’ Caplets Laxative Caplets: 500 mg Adults: 30-60 mL at bedtime with
Phillips’ Milk of Magnesia
Liquid: 400 mg/5 mL.
water
Adulis and children > 12 yrs:2.to
4 caplets daily
= The atropine crosses the BBB (produces mild to moderate anticholinergic effects)
= Rapidly and extensively metabolized to diphenoxylic acid (it’s metabolite)
= Excreted in urine and feces
= The atropine component of diphenoxylate and difenoxin contraindicates their use in narrow-angle
glaucoma and requires cautious use in prostatic hyperplasia.
= Children, especially those with Down syndrome have increased sensitivity to atropine
= Use with extreme caution in children, not recommended for use in children younger than 12 y/o
= Do not use with E. Coli, Salmonella, Shigella, or in pseudomembranous colitis
= ADRs: r/t atropine: anticholinergic effects (dry mouth, flushing, tachycardia, urinary retention)
O Crosses BBB=dizziness, drowsiness, sedation, HA, euphoria, or depression
= Additive or potentiating CNS effects with other CNS depressants and additive anticholinergic effects with
other drugs that share these effects
-Difenoxin watropine Motofen): Acute diarrhea9*****
Anticholinergics are useful only with inflammatory bowel disease
= Rapidly metabolized to an inactive hydroxylated metabolite
= Excreted mainly as conjugates in urine and feces
= The atropine component of diphenoxylate and difenoxin contraindicates their use in narrow-angle
glaucoma and requires cautious use in prostatic hyperplasia.
= Children, especially those with Down syndrome have increased sensitivity to atropine
= Use with extreme caution in children, not recommended for use in children younger than 12 y/o
= Do not use with E. Coli, Salmonella, Shigella, or in pseudomembranous colitis
= ADRs: r/t atropine: anticholinergic effects (dry mouth, flushing, tachycardia, urinary retention)
O Crosses BBB=dizziness, drowsiness, sedation, HA, euphoria, or depression
= Additive or potentiating CNS effects with other CNS depressants and additive anticholinergic effects with
other drugs that share these effects
-Loperamide (Imodium): Acute diarrhea, travelers’ diarrhea, chronic diarrhea associated w/inflammatory bowel disease
© Binds to opiate receptors of the intestinal wall, slows gastric motility
e Reduces fecal volume, increases viscosity and bulk, diminishes loss of fluid and electrolytes
¢ Does not cross BBB, limited CNS ADRs
¢ Partially metabolized by the liver and undergoes enterohepatic recirculation to be completely metabolized
© — Eliminated in feces
¢ ADRs: r/t atropine: anticholinergic effects (dry mouth, flushing, tachycardia, urinary retention)
O Toalesser degree than diphenoxylate and difenoxin
0 Dizziness and drowsiness (less CNS effects than difenoxin or diphenoxylate
¢ Additive or potentiating CNS effects with other CNS depressants and additive anticholinergic effects with other
drugs that share these effects
Pharmacotherapeutics
© Precaution and contraindications
¢ Drugs that reduce intestinal motility or delay intestinal transit time may cause toxic megacolon, especially in IBD
¢ Diphenoxylate with atropine difenoxin with atropine, and loperamide should be used cautiously in IBD
0 D/Cif ABD distension occurs
e Use Diphenoxylate with atropine difenoxin with atropine, and loperamide use with caution in advanced
hepatorenal disease and in all patients with abnormal LFTs (hepatic coma may occur)
e Atropine: contraindicated in narrow-angle glaucoma and requires cautious use in prostatic hyperplasia
* Children (especially those with Downs syndrome) have increased sensitivity to atropine
© Clinical Use and Dosing
Simple, Acute Diarrhea
¢ Absorbent preparations for adults: Kaolin-pectin or bismuth subsalicylate taken after each loose stool may be
effective
¢ Majority of acute diarrhea are self-limiting, hydration important
e = Maintain hydration
oO Commercial hydrating fluids (Pedialyte) or powdered salts
0 Apinch of table salt and a half-teaspoon of honey in 8 oz of fruit juice (older children and adults)
0 Non-diet colas without carbonations (older children and adults)
0. Alternate these solutions with 8 oz of water with one-quarter teaspoon baking soda to replenish
electrolytes (NA, K, bicarbonate, and Cl)
e If the absorbents do not resolve the problem, diphenoxylate or difenoxin or loperamide may be added
Chronic Diarrhea Associated with IBD
© — Steroids and sulfasalazine are needed
¢ Loperamide may be used as adjunct therapy
0 May significantly improve symptoms especially with added fiber and anticholinergics
0 If clinical improvement does not occur with doses of 16 mg/day for 10 days, symptoms are unlikely
to be controlled by further use
Chronic Diarrhea Associated with Pancreatic Insufficiency
¢ Malabsorption r/t pancreatic insufficiency requires enzyme supplements, antidiarrheals not indicated
Chronic Infantile Diarrhea
¢ Bismuth subsalicylate: 2.5 mL every 4 hrs for children 2 to 24 months, 5 mL for 24-48 month children, and 10 mL
for children 48 to 70 months
Diarrhea in HIV/AIDS Patients Taking Antiretroviral Drugs
¢ — Crofelemer (Fulyzaq) symptomatic relief of noninfectious diarrhea in adults with HIV/AIDS on ARV therapy
¢ 125 mg tablet twice a day without regard for food
Traveler's Diarrhea
¢ Bismuth subsalicylate: two tablets or 2 Fl oz before each meal and at bedtime (QID) for up to 3 weeks
e Prevention and treatment
e High-risk areas: Central and South American, Africa, Middle East, Mexico, and Asia
¢ E.Coli is the most common causative agent followed by Campylobacter, Shigella, and Salmonella
Rational Drug Selection
e — Indication: Acute diarrhea, any of the antidiarrheals are appropriate
e — Subsalicylate and loperamide are the only drugs indicated for traveler’s diarrhea
e —Loperamide is the only drug with an indication for IBD
© Generic and brand name formulations available
Monitoring: No specific monitoring
Patient Education
¢ Take as directed, do not double doses, do not exceed max number of doses in 24 hrs
° Notify provider if diarrhea continues beyond 48 hrs or if ABD pain, fever, or distention occurs
e Use calibrated measuring devices for liquids, shake suspensions before measured
Drug interactions may occur, especially with diphenoxylate and loperamide
Do not take any OTC antidiarrheal before contacting your provider if taking digoxin, cephalosporin antimicrobials,
warfarin or heparin, or CNS depressants (including ETOH)
R/f salicylate poisoning if taking ASA and bismuth subsalicylate
R/f rebound constipation
Stop drug when s/s of diarrhea are reduced
Bismuth subsalicylate can turn the tongue and stools gray/black
Drugs with atropine: dry mouth, flushing, tachycardia, and urinary retention
Loperamide also exhibits these reactions but to a lesser degree, add fiber and use oral rehydrating solutions
GHWT
Bland food diet, remove milk, could it be lactose intolerance?
Patt) it Teh tela) eT tu) erst OU TCE
Bismuth subsalicylate’t Acute diarrhea Tablets/chewable: 262 mg Adults: 524 mg every 30 min Not to exceed 4.2 g/24h
Pepto-Bismol Liquid: 262 mg/15 mL or 1,048-1,200 mg every Not to exceed 2.4 g/24h
Kaopectate Liquid: 524 mg/15 ml. 60 min as needed Not to exceed 14 g/24h
Children 9-12 yr: 262- Not to exceed 704 mg/24h
300 mg every 30-60 min May repeat q4h; not to
as needed exceed 6 doses/24h
Children 6-9 yr: 176 mg
every 30-60 min as
needed
Children 3-6 yr: 88 mg every
30-60 min as needed
Children <3 yr weighing
>13 kg: 88 mg
Children <3 yr weighing
64-8 kg: 44 mg
May repeat q4h; not to
exceed 6 doses/24 h
Traveler's diarrhea 524 ing (2 tabletsor30mL Not to be used for more
of 262 mg/15 mL. liquid) than 48h
every 30 min for up to
8 doses
Crofelemer Symptomatic relief of 125 mg delayed-release J tablet bid, with or without
(Fulyzaq) noninfectious diarrhea tablet food
in adult patients with
HIV/AIDS on anti-
retroviral therapy
Difenoxin with atropine Acute diarrhea Tablets: 1 mg difenoxin and — Adults: 2 mg 1 mg after each loose stool
Motofen 0,025 mg atropine sulfate or I mg every 3-4 has
needed. Total 24h dose
not to exceed 8 mg
Diphenoxylate with atropine Acute diarrhea Tablets: 2.5 mg diphenoxy- Adults: 5 mg tid to qid 5 mg daily as needed; not
Lomotil late, 0.025 mg atropine initially to exceed 20 mg/d
sulfate
¢ Misoprostol: less effective for Tx of duodenal ulcers from other causes
0 Off-label: in doses >400mcg/day, Tx for duodenal ulcers not responsive to H2Ras
Rational Drug Selection
¢ Sucralfate: drug of choice for women of childbearing age
e Sucralfate preferred over misoprostol for treatment of active duodenal ulcers not caused by NSAIDs
Monitoring
¢ No specific monitoring parameters
¢ Negative pregnancy test for misoprostol
Patient Education
e Take exactly as prescribed
e Sucralfate on an empty stomach, Sucralfate is given for 4 to 8 weeks, increase fluid intake, dietary bulk, and
exercise to reduce incidence of constipation
¢ Misoprostol with food, Misoprostol given for the duration of NSAID therapy, can cause diarrhea, if persists x1 WK
notify provider
¢ Continue therapy even if you feel better
Table 20-9 Dosage Schedule: Cytoprotective Agents
Indication
Drug
Dosage Forms
Dosage Schedule
Misoprostol Cytotec
Sucralfate Carafate
Prophylaxis and
treatment of duodenal
Tablets: 100, 200 mcg
ulcers due to NSAID use
Active duodenal ulcer
Maintenance after 1g/10 mL
healing of duodenal
ulcer
Tablets: 1 g Suspension:
200 mcg gid with food.
Last dose usually at
bedtime. Taken for
duration of NSAID
therapy. If this dose is
not tolerated, 100 mcg
gid may be used.
1g qid taken 1 h before
meals and at bedtime
1g bid taken on empty
stomach
> Antiemetics:
Drug classes with antiemetic properties: antihistamines, phenothiazines, sedative hypnotics, cannabinoids, 5-HT3
receptor antagonist, anticholinergics, and a substance P/neurokinin 1 receptor antagonist
Antihistamines: dimenhydrinate (Dramamine), diphenhydramine (Benadryl), hydroxyzine (Vistaril), meclizine (Antivert)
¢ Pharmacodynamics: Antihistamines with significant antiemetic activity have strong anticholinergic effects as well as
histamine 1 blocking effects
e MOA: Bind to central cholinergic receptors to produce antiemetic effects
© especially with motion sickness due to the depression of conduction in the vestibulocerebellar pathway
e Pharmacokinetics: All the antiemetic drugs (except for TD scopolamine) are well absorbed after PO administration
e Pharmacotherapeutics: Cautious use in narrow-angle glaucoma, seizure disorders, pyloric obstruction, hyperthyroidism,
CVD, and prostatic hypertrophy
Contraindicated in severe liver disease r/t extensive liver metabolism
Cautious use in the elderly, dose reductions may be needed
Dimenhydrinate and diphenhydramine are Pregnancy Category B and safe for use in children
Meclizine is pregnancy Category B (safety and efficacy in children less than 12 not established)
Hydroxyzine Pregnancy Category C, has been used safely during labor (safety in children or lactation not
established)
eooeee
ADRs: Common adverse reactions: drowsiness, dry mouth, blurred vision & urinary retention
¢ Paradoxical excitation may occur in children
e Drug/Drug: additive CNS depression with other drugs that produce CNS depression and additive anticholinergic
effects with other drugs that have anticholinergic effects or adverse reactions
Phenothiazines: prochlorperazine (Compazine), perphenazine, promethazine (Phenergan)
¢ Pharmacodynamics: block dopamine receptors in the chemoreceptor trigger zone (CTZ)
e Also bind to and block cholinergic, alpha 1 adrenergic, and histamine 1 receptors
e Use as antiemetics is limited due to sedating and EPM effects
¢ Pharmacotherapeutics: Produce extrapyramidal reaction Contraindicated in Parkinson's Disease
© Contraindicated in narrow-angle glaucoma, bone marrow depression, and sever CVD or hepatic
disease
© Cautious use in respiratory impairment cause by acute pulmonary infection or chronic respiratory
disorders (asthma or emphysema)
May lead to the development of “silent pneumonia”
Suppress cough reflex, aspiration of vomitus is possible
Use with caution in those with r/f aspiration
Pregnancy Category C
Children of all ages are more prone to developing extrapyramidal reactions
Prochlorperazine: avoided in children younger than 5 r/t extrapyramidal reactions
¢ — R/f respiratory depression and sudden death in children 2 years of age or older
e Adverse reactions: drowsiness, (extrapyramidal reactions) dystonia, akathisia, tardive dyskinesia
oO Dry mouth, dry eyes, blurred vision, constipation, and urinary retention
0 ability to mask post-surgical and neurological conditions
O potential for agranulocytosis and blood dyscrasias 4-10 weeks after initiation
O cancause urine to turn pink to reddish brown (does not indicate hematuria)
© Promethazine Black Box Warning: Fatal respiratory depression in children younger than 2 years old
e Drug/Drug: additive CNS depression with other drugs that produce CNS depression and additive
anticholinergic effects with other drugs that have anticholinergic effects or adverse reactions
¢ Additive hypotensive effects with antihypertensive agents or acute ingestion of ETOH
¢ Concurrent administration of lithium increases r/f extrapyramidal reactions
e@ May mask s/s of lithium toxicity
e — Antithyroid agents increase r/f agranulocytosis
eoeoeee
Cabbabinoid: dronabinol (Marinol)
¢ Pharmacodynamics: Work in the CNS like cannabis to prevent NV associated w. chemotherapy & as an appetite
stimulant, especially in HIV pts
¢ Pharmacotherapeutics: Use with caution in patient with Hx of seizure disorder r/t lowering of seizure threshold
0 Cardiac disorders: monitor for hypotension, possible hypertension, syncope, or tachycardia
0 High potential for abuse
O Pregnancy Category C
e Adverse reactions: euphoria (should not drive), depression, dizziness, paranoid thoughts, somnolence, and
abnormal thoughts
0 Cardiac effects include palpitations, tachycardia, and hypotension
0 Seizures and seizure-like activity
O Drug/Drug interactions: Interacts with other CNS depressants, additive CNS depression with benzos,
barbiturates, ETOH, opioids, antihistamines, muscle relaxants, and other CNS depressants
5-HT3 receptor agonists: palonosetron (Aloxi), dolasetron mesylate (Anzemet), granisetron (Kytril, Sancuso) and
ondansetron (Zofran)
e@ Pharmacodynamics: Block serotonin both peripherally and on vagus nerve terminals & the chemoreceptor
trigger zone (CTZ) to decrease emesis
e Pharmacotherapeutics: Potential to mask progressive ileus
0 Zofran contains aspartame, use with caution in phenylketonuria
0 Dolasetron, granisetron, and palonosetron are Pregnancy Category B
e Adverse reactions: constipation, headache, fatigue, dizziness, diarrhea.
0 Less common but concerning rare cases of tachycardia, bradycardia, hypotension, and QT prolongation
Anticholinergic: Scopolamine (Transderm Scop)
e Pharmacodynamics: Belladonna alkaloid anticholinergic acts as a competitive inhibitor of muscarinic in the
parasympathetic nervous system
0 Blocks cholinergic transmission from the reticular center to the vomiting center in the brain
0 Anticholinergic effect: decreases secretion of saliva and decreases GI motility
e Pharmacotherapeutics: Contraindicated: pts w/ narrow angle glaucoma
© Caution: pts with open-angle glaucoma or gastrointestinal or bladder neck obstruction
0 Use cautiously in the elderly due to CNS effects
* Pregnancy Category C, no approved for use in children
¢ Adverse reactions: dry mouth, drowsiness, blurred vision, dilated pupils
Oo Withdraw syndrome: dizziness, NV, HA
¢ Applied in the hairless area behind the ear 4 hours prior to needed effect and can be left in place up to 3 days.
Wash hands after handling patch to avoid getting medication in the eyes (can cause blurry vision & pupil dilation)
e Decrease secretion of saliva and decrease gastric motility
NKI receptor antagonist: Aprepitant (Emend)
@ Pharmacodynamics: crosses the blood brain barrier and occupies the NK1 receptors to prevent n/v in pts
receiving chemotherapy
@ Pharmacotherapeutics: Contraindicated in patients who are hypersensitive to any component of the product
e Inhibits CYP3A4=increase serum concentrations of other drugs that are metabolized by CYP3A4
Pregnancy Category C and not approved for use in children
= Adverse reactions: fatigue, dizziness, hiccups, possible elevated ALT/AST, BUN
¢ — Drug/drug interactions: Inducer of CYP3A4 and can increase plasma concentrations of drugs metabolized
via CYP3A4 system
0 Including: hormonal contraceptives and some chemotherapy agents
Prochlorperazine
‘Compazine
Generic
Promethazine
Phenergan
Generic
Vertigo
Nausea and vomiting in
pregnancy
Antiemetic
Antiemetic
Tablets: 5, 10, 25 mg
Spansules (SR): 10, 15, 30 mg
Syrup: 5 mg/5 mL.
Injection: 5 mg/mL
Suppositories: 2.5, 5, 25 mg
Tablets: 12.5, 25, 50 mg
Syrup: 6.25 mg/S mL.
Suppositories: 12.5, 25, 50 mg
Injection: 25 mg/mL,
50 mg/ml.
Adults: 25-100 mg daily in
divided doses
Lowest dose that relieves
nausea
Children >12 yr and adults:
5-10 mg PO/IM tid or qid;
not to exceed 40 mg/d
Children 19-39 kg: 2.5 mg
PO/PR tid or 5 mg bids not
to exceed 15 mg/d
Children 15-18 kg: 2.5 mg
PO/PR bid or tid; not to
exceed 10 mg/d
Children >2 yr or 10-14 kg:
2.5 mg PO/PR qd or bid;
not to exceed 7.5 mg/d
Adults: 25 mg PO/IM/PR 4h
Children >2 pr: 0.25-0.5
mg/kg q4~Gh PO/IM/PR.
Do not exceed 25 mg/dose.
Pregnancy Category B
Do not crush or chew ER
capsules.
Administer with food or
milk or a full glass of
water to minimize GI
distress. Dilute syrup
in citrus or chocolate-
flavored drinks.
Give IM into deep, well-
developed muscle. Keep
patient recumbent for
at least 30 min follow-
ing injection to avoid
hypotensive effects.
Do not use in pediatric pa-
tients under 2 yr of age
or under 20 Ib.
For motion sickness, give
dose 1-2 h prior to
departure.
Administer with food,
water, or milk to
minimize GI distress.
Tablets may be crushed
and mixed with food or
fluids for patients with
difficulty in swallowing.
Use calibrated measuring
device when giving
liquid doses.
Give IM into deep, well-
developed muscle; SC
administration may
cause tissue necrasis,
Do not administer to chil-
dren <2 yr. Use with
extreme caution in chil-
dren using the lowest,
most-effective dose.
Trimethobenzamide
Antiemetic
Capsules: 100, 250, 300 mg
Adults: 300 mg PO tid/qids
Capsules can be opened
Tigan Injection: 100 mg/mL. TM = 200 mg tid/qid and contents mixed
Generic Children: 15-20 mg/kg/day with food or fluid for
PO divided tid/gid OR patients with difficulty
Children > 40 kg: in swallowing.
300 mg tid/gid Inject deep into well-
Children 15-40 kg: developed muscle to
100-200 mg PO tid/qid minimize tissue
or 15 mg/kg/d in irritation.
3-4 divided doses
Children <15 kg: 100 mg,
PR tid/qid
Dronabinol Refractory nausea and Capsules: 2.5 mg, 5 mg, Adults and children: 5 mg/m? Individualize the dosing
Marinol vomiting associated 10 mg 1-3 h before chemother
with cancer
chemotherapy
apy. Then every 2-4 h after
chemo. May increase as
needed by increments of
2.5 mg/m? toa max of
15 mg/m?
Dolasetron
Anzemet
Anorexia associated with
weight loss in patients
with AIDS
Prevention of nausea
and vomiting after
chemotherapy or
surgery
Tablets: 50, 100 mg
Injection solution: 20 mg/mL
Adults: 2.5 mg bid before
lunch and supper; dosage
can be reduced to 2.5 qhs
Children 216 yr and adults:
100 mg within 1 h before
chemotherapy or 2h
before surgery
Children 2 yr-16 yr: 1.8 mg
within 1 h of chemother-
apy or 1.2 mg within 2h
before surgery
Dolasetron injection solu-
tion may be diluted in
apple juice and taken
orally, This solution is
stable for 2 h.
Ondansetron
Zofran
Generic
Scopolamine
Transderm Scop
Prevention of nausea and
vomiting associated
with chemotherapy
Post-operative nausea
and vomiting
Gastroenteritis
Prevention of nausea and
vomiting associated
with motion sickness
Tablets: 4, 8 mg
ODT (disintegrating tab):
4,8mg
Solution: 4 mg/5 mL
‘Transdermal patch: 1.
Aduits: 24 mg administered
30 min before the start of
chemotherapy or 8 mg tid
Children 4-11 yr: A mg tid
Infants and children < 40 kg:
0.1 mg/kg/dose before in-
duction of anesthesia
Children > 12 yr: 44mg
Adults: 16 mg PO 1h before
induction of anesthesia,
OR4 mgIV
Infants and children 6 mo
to 10 yr.
8-15 kg: 2 mg/dose X 1
15-30 kg: 4 mg/dose X 1
> 30 kg: 8 mg/dose X 1
Adults: Apply patch to hairless
area behind one ear and
leave in place for 3 days
Routine use of ondasetron
is not recommended in
most cases of acute
gastroenteritis.
Transdermal patch is pro-
grammed to deliver
1 mg over 3 days.
> Histamine-2 receptor antagonists: H2Ras
Do nof inhibit
acetyltholine, so
they reduce
gastrid acid
secretjon by only
35%-5)%
0 Histamine 2 blockers aka histamine 2 antagonists (H2Ras)
Cimetidine (Tagamet), Famotidine (Pepcid), Nizatidine (Axid), Ranitidine (Zantac)
Used to reduce gastric acid in NPO pts for prophylaxis and management of duodenal and gastric ulcers
and GERD (not first-line treatment of GERD), if no esophageal erosive disease is present H2RA’s can be
used for maintenance therapy for relief of GERD symptoms
Also used for heart burn, acid indigestion and “sour stomach”
© Pharmacodynamics: MOA: Inhibit acid secretion by gastric parietal cells through a reversible blockade of
“lL histamine at H2 receptors
.
potent inhibitors of all phases of gastric acid secretion, including muscarinic agonists and gastrin
Effect volume and H ion concentration of gastric juice, gastric emptying, and lower esophageal sphincter
pressure (each drug to varying degrees)
Cimetidine, ranitidine, and famotidine have no effect on gastric emptying
Cimetidine and famotidine have no effect on lower esophageal sphincter pressure
Ranitidine, nizatidine, and famotidine have little or no effect on fasting or postprandial serum
gastrin
Ranitidine does not affect pepsin secretion or pentagastrin-stimulated IF secretion
Pharmacokinetics
All drugs are well absorbed with PO administration
0. All are metabolized to differing degrees by the CYP450 system and excreted in differing
percentages unchanged in urine
Pharmacotherapeutics
Caution: Renal impairment (dosage adjustments, r/f CNS ADRs), Elderly (due to decrease in renal
function)
Contraindicated: Nizatidine and Ranitidine DO NOT rx for patients w. hx of liver disease (causes
hepatocellular injury, hepatitis) elevated ALT AST
Pregnancy Category B, excreted in breast milk, use caution in breastfeeding mothers
Famotidine is labeled safe for infants & neonates (has caused agitation, stopped when drug d/ced)
Cimetidine can cause gynecomastia & impotence
oO CNS reversible reactions (mental confusion, agitation, psychosis, depression, and disorientation)
Hematological adverse reactions include agranulocytosis, granulocytopenia, thrombocytopenia, and
aplastic anemia (rare)
Less Common side effects: drowsiness, dizziness, constipation (increase fiber and fluid intake), or
diarrhea & nausea
Drug/Drug Interactions: Related to CYP450 system
0 Cimetidine is most problematic (metabolized by CYP1A2, CYP2C9, and CYP2D6)
© Other drugs metabolism inhibited by cimetidine (r/f increased serum levels and toxicity
Clinical Use and Dosing
GERD-most effective if used as on demand therapy for symptoms relief
0 Tachyphylaxis: Not first line therapy to treat GERD
0 If not erosive disease, may be used as maintenance therapy after PPI treatment
0 Infants and children have been successfully treated however no longer recommends H2Ras as
empiric treatment in infants
Rational Drug Selection
O Nospecific drug is preferred over another for effectiveness
0 Consider costs
Monitoring
0 LFTs r/t potential for hepatocellular damage
Oo Renal impairment: renal function assessment prior to initiation of therapy
Patient Education
Should be taken w/ meals or immediately after & at bedtime, daily doses are best @ bedtime,
take 1 hour away from other drugs,
& two hours away from sucralfate
OTC preparations should not be taken for more than 2 wks without consulting healthcare provider
Report black tarry stools- may indicate GI bleeding.
Sore throat, diarrhea, rash, confusion, or hallucinations should be reported promptly (might need
dosage adjustment or discontinuation),
advise pt to stop smoking (interferes with absorption of H2RA & increases gastric secretion)
¢ Prokinetics: metoclopramide (Reglan)
0 AKA gastrointestinal stimulants
© Donot stimulate gastric, biliary, or pancreatic secretions
0 Used to treat gastroparesis associated with DM, GERD, and emesis with chemotherapy
Pharmacodynamics: MOA: Stimulates motility in the upper Gl tract,
increases tone and amplitude of gastric contractions,
relaxes the pyloric sphincter and duodenal bulb,
and increases peristalsis of the duodenum and jejunum,
resulting in accelerated gastric emptying and increased speed of gastric transit
Improves gastroesophageal reflux disease symptoms by increasing lower esophageal tone
Also is a dopamine receptor agonist in the CNS, including the chemotherapy trigger zone leading to
prevention of emesis
Actions similar to phenothiazines: Produces sedation and may cause tardive dyskinesia or EPS
Induces release of prolactin and transient increases of aldosterone
Pharmacokinetics
Well absorbed after PO administration
Injectable formulation is available
High bioavailability, low protein binding
Widely distributed, crosses BBB and placenta, enters breast milk (greater than plasma)
Minimally Metabolized by the liver, liver function is not an issue
Excreted in urine (clearance is affected by renal function)
Renal impairment requires dose adjustment: dose cut in half CCr <40
Pharmacotherapeutics
ADRs
BLACK BOX WARNING: risk for developing tardive dyskinesia and parkinsonian-like symptoms, the
risk increases the longer it’s in use, treatment should not exceed 12 weeks and be discontinued
immediately if signs of movement disorder, Report involuntary movement of the eyes, face, or
limbs immediately
Contrindicated: in the presence of disorders in which stimulation of GI motility is dangerous (al
hemorrhage, mechanical obstruction, new surgery on the Gl tract, or perforation),
dopamine- associated activity affects the CNS & can cause depression (mild- severe w. suicidal
ideation), use with caution
Contraindicated in pt.s w. pheochromocytoma b/c the drug can cause hypertensive crisis
Safe to administer to pt.s with hx of impaired hepatic function if renal function is normal
Safety and effectiveness not established in infants and children
Oo EPS is more common in children, use with caution
Most serious reaction is EPS (dystonic reaction and tardive dyskinesia and parkinsonian-like
symptoms d/c in pt. exhibiting movement d/o
Neuroleptic malignant syndrome
More common: Depression, dizziness, diarrhea, and hypoglycemia in DM
Less common: galactorrhea, amenorrhea, gynecomastia, impotence secondary to
hyperprolactinemia, and fluid retention r/t elevations in aldosterone
Incidence of ADRs correlated with the dose and duration of therapy
Drug interactions: Largely related to its cholinergic and dopaminergic activity
¢ Additive CNS depression
¢ Increased r/f EPS when taking other drugs with a r/f EPS
¢ Drugs with anticholinergic effects reverse the action of metoclopramide
e¢ Hypertensive crisis if administered with MAOIs
Clinical Use and Dosing:
GERD: principal effect is on symptoms of postprandial and daytime heartburn
e For adults, for symptoms throughout the day 10 mg taken 30 minutes prior to each meal and at bedtime
is recommended
© If symptoms are confined to specific situation (after evening meal): 10 to 20 mg dose prior to that meal
or at bedtime
Patient who are more sensitive to the therapeutic dose (older adults) 5mg/dose
Neonatal 0.1 to 0.15 mg/kg/dose Q 6 hrs
© GERD in infants and children 0.4 to 0.8 mg/kg/day divided in 4 doses (30 minutes prior to teach meal)
Nausea and Vomiting
e Action on the chemoreceptor trigger zone to prevent NV
© Post-op NV in children 14 years old or younger, older children, and adults
© For high doses (as with chemo), pretreat with diphenhydramine to prevent EPS
Diabetic Gastroparesis
¢ Dose 10 mg 30 minutes AC and HS for 2 to 8 weeks
¢ Route of administration dependent of severity of symptoms
e = If early: PO is adequate
e If more severe: Parenteral therapy 10 mg IV over 1 to 2 minutes for up to 10 days may be needed before
PO therapy can be initiated
¢ Rectal formulations available
© Be cognizant that renal impairment is common in DM, dose adjustments for CCr <40
Rational Drug Selection
¢ — Efficacy: higher cost and increased ADRs, difficult to justify its use in place of H2Ras or PPIs
¢ Length of therapy: Not used for management of GERD is Tx must be long-term (8 weeks)
* Concomitant Diseases: Cautious use for those at r/f EPS, renal disease
Monitoring
¢ Renal function assessed before therapy
¢ Educate about EPS
Patient Education
Drowsiness, avoid driving until response is known
CNS depression with ETOH and additive CNS depression
Notify immediately if involuntary movement of the eyes, face, or limbs occurs
Change in mood should be reported (depression/suicidal ideation)
Avoid ETOH, NSAIDs, large meals, fatty foods, chocolate, caffeine, citrus, ad good or fluid intake within 3
hours of HS
oder: Available Dosage eT Ts Laue Loc
Metoclopramide GERD Tablets: 5 mg Adults: Some patients respond to
Reglan Tablets: 10 mg, Treatment: 10-15 mg qid doses as low as 5 mg.
Generic Syrup: 5 mg/5 mL (30 min before meals and Dose not to exceed
Injection: 5 mg/mL at bedtime) 0.5 mg/kg/d. Therapy
Prophylaxis: 20 mg at not to exceed 8 wk.
bedtime Patients with CCr
Children: 0.4-0.8 mg/kg/d in <40 mL/min, initiate
4 divided doses (30 min therapy with half the
before meals and at recommended dose.
bedtime)
Diabetic gastroparesis Adults: 10 mg gid (30 min
before meals and at
bedtime)
> Proton pump inhibitors (PPI’s):
Esomeprazole (Nexium), Lansoprazole (Prevacid), Omeprazole (Prilosec), Pantoprazole (Protonix), Rabeprazole
(Aciphex), Dexlansoprazole (Dexilant, Kapidex)
e Antisecretory drugs used to treat conditions characterized by hyperacidity
¢ Used to treat: erosive gastritis, GERD, and Zollinger-Ellison syndrome, part of the multidrug regiment for short-
term treatment of active PUD (especially duodenal ulcers caused by H. pylori)
Pharmacodynamics: MOA:
*® Do not exhibit anticholinergic or H2 blockade but suppress gastric acid secretion
© Inhibition of basal and stimulated acid secretion (regardless of stimulus) by suppressing gastric acid secretion
via reduction of H+ secretion and inhibition of the H +/K+/ATPase enzyme system at the secretory surface of
the parietal cell itself to block the final step of H+ secretion.
Pharmacokinetics
© PPI's are ironically acid labile & so most are formulated as EC tablets or granules
¢ All should be taken on an empty stomach before a meal, in the AM if possible
0 Food decreases absorption
e All drugs are distributed to the parietal cells of the stomach
© Extensively metabolized by CYP450 system (CYP2C19 and CYP3A4)
e — Little unchanged drug is excreted in urine, 90% of metabolites excreted in urine
¢ — Significant biliary excretion
* Older adults have decreased elimination rates of all drugs (decreased renal function, associated with age)
Pharmacotherapeutics
. Caution: only true contraindication is hypersensitivity to ingredients
* Extensively metabolized in the liver (CYP450), use caution hx of hepatic dysfunction & the elderly
O No dose adjustments required
© Omeprazole is Pregnancy Category C
e Lansoprazole, esomeprazole, pantoprazole, and rabeprazole are Pregnancy Category B
e — Safety and efficacy of pantoprazole and rabeprazole have not been established in children younger than 12
ADRs
¢ Typically, well tolerated when used for short-term treatment
0 Dizziness, drowsiness, ABD pain, constipation, diarrhea, and flatulence
Drug er itett ta) Saal r Dyers Maintenance Dose
Esomeprazole GERD with erosive Capsules: delayed-release: Adolescents and adulis:200r 40mg 20 mg/d
Nexium esophagitis 20, 40 mg daily for 4-8 wk. Maintenance:
Granules for suspension: 20 mg daily for 4 wk.
10, 20, 40 mg/packet Children: <20 kg: 10 mg daily for 8 wk;
>20 kg: 10-20 mg daily for 8 wk
Symptomatic GERD Adults: 20 mg daily for 8 wk
H. pylori eradication/ Children 1-11 yr: 10 mg daily for 8 wk
prevent duodenal ulcer ‘Triple therapy: Esomperazole 40 mg
daily + amoxicillin 1 g bid + cla-
rithromycin 500 mg bid for 7-10 d
Lansoprazole Duodenal ulcer Capsules, delayed-release: Children 12 yr and adults: 13mg qd 15 mg qd
Prevacid pylori eradication/ 15, 30 mg for 4 wk
prevent duodenal ulcer Tablet: 15, 30 mg H. pylori:
Suspension; 3 mg/mL. ‘Triple therapy: Lansoprazole 30 mg
bid + amoxicillin 1 g bid + clarith-
romycin 500 mg tid for 10d
Double therapy: Lansoprazole 30 mg
tid + amoxicillin 1 g tid for 14d
Benign gastric ulcer 30 mg daily for <8 wk
Erosive esophagitis 30 mg daily for <8 wk 15mg qd
Hypersecretory disorders 60 mg daily Up to 90 mg bid; doses
>120 mg/d must be divided
Erosive esophagitis Adults; 30 mg once daily for up to 8wk If not healed, repeat dose for
Children 12-17 yr and adults: 30 mg additional 8 wk
once daily for up to 8 wk Increase to 30 mg bid in
Children 1-11 yr: patients who remain
<30 kg: 15 mg daily for up to 12 wk symptomatic after 2 wk
>30 kg: 30 mg daily for up to 12 wk of therapy
Gastric ulcer associated
with NSAID therapy
Adults: 30 mg daily for up to 8 wk
15 mg/d for up to 12 wk
GERD Prevacid OTC: Capsules, Children 12-17 yr and adults: 15 mg.
delayed-release: 15 mg daily for up to 8 wk
Children 1-11 yr:
<30 kg: 15 mg daily for up to 12 wk
>30 kg: 30 mg daily for up to 12 wk
Omeprazole Duodenal ulcer Capsules, delayed-release: Adults: 20 mg daily for 4-8 wk
Prilosec 10, 20, 40 mg Infants and children: 15-30 kg: 10 mg
Generic Granules for suspension: bid, >30 kg: 20 mg bid
2.5, 10 mg/packet H. pylori:
‘Triple therapy: Omeprazole 20 mg
bid + clarithromycin 500 mg bid +
amoxicillin 1 g bid for 10 d
Double therapy: Omeprazole 40 daily +
clarithromycin 500 mg tid for
14 d; then omeprazole 20 mg daily
for 14 additional d
Benign gastric ulcer 40 mg daily for 4-8 wk
Erosive esophagitis 20 mg daily for 4-8 wk 20 mg qid
GERD Children 2-18 yr: Note: Ona per kg basis
$20 kg: 10 mg daily for 4-8 wk doses are higher for
>20 kg: 20 mg daily for 4-8 wk children than adults.
Hypersecretory disorders Adolescents > 16 yr and adults: Up to 120 mg tid; doses
60 mg daily >80 mg/d must be divided
Pantoprazole Symptomatic GERD ‘Tablets: delayed-release: 20-40 mg daily for 7-10 d 20 mg/d
Protonix 20 40 mg
Granules for suspension:
40 mg/packet
GERD with erosive 40 mg daily for up to 8 wk 40 mg/d
esophagitis If not healed, repeat same
dose for additional 8 wk
Hypersecretory disorders Individualized. 40 mg bid; may treat Doses up to 240 mg/d have
for up to 2 yr been used.
Rabeprazole Duodenal ulcers Tablets, delayed-release: Adults and adolescents >12 yr:20mg If not healed, repeat dose
Aciphex 20 mg daily after the morning meal forup for 4 wk
to4wk
GERD Adults and adolescents >12 yr:20 mg _ If symptoms, repeat dose
daily for 4 wk for 4 wk
Erosive esophagitis
20 mg daily for 4-8 wk
If not healed, repeat dose
for 4 wk
H. pylori eradication/
prevent duodenal
ulcer
Triple therapy: Rabeprazole 20 mg
bid + amoxicillin 1 g bid + clar-
ithromycin 500 mg bid for 7d
Hypersecretory disorders
Individualized: 60 mg daily; may treat
for up to 1 yr
Dose up to 100 mg/d or
60 mg bid have been used
Dexlansoprazole
Dexilant
Kapidex
Erosive esophagitis
Delayed-release capsules:
30, 60 mg
60 mg capsule
‘Treatment: 60 mg daily for 8 wk
Maintenance for healed EE:
30 mg daily for up to 6 mo
30 mg daily for 4 wk
Moderate hepatic dysfunc-
tion: 30 mg/d
Not recommended for
children <18 yr
> Laxatives
O Six classes of drugs: stimulants, osmotics, bulk-producing laxatives, lubricants, surfactant, and
hyperosmolar laxatives (methylnaltrexone (Relistor) mu-opioid receptor antagonist, used for opioid
“Laxative abuse
syndrome” most common
in women w/ depression,
personality disorders, or
anorexia nervosa. o
oO
Stepped-approach algorithm for peptic ulcer disease.
and antacids
pyloritesting and
smokers, +60 yr, COPD, CAD,
hx of bleeding or perforated
ulcer, patients on NSAIDs)
induced constipation)
All share contraindication of use in the presence of nausea, vomiting, or undiagnosed
abdominal pain, or if bowel obstruction is suspected or diagnosed
All share precautions for dependency, chronic use of laxatives may result in electrolyte
imbalances, steatorrhea, osteocalcin, and vitamin and mineral deficiencies
may cause allergic reactions including asthma, seen in pts who also have aspirin sensitivity.
© Common adverse reactions: excessive bowel activity, cramping, flatulence, and bloating
o Few drug interactions
Stimulants: cascara, senna, Bisacodyl, and castor oil
© Pharmacodynamics: MOA: Direct action on intestinal mucosa by stimulating the myenteric plexus,
releasing prostaglandins and increase cyclic adenosine monophosphate (cAMP), increasing secretion of
electrolytes and peristalsis
e Pharmacotherapeutics:
0 Bisacodyl Caution: patients with cardiovascular disease
¢ Pharmacodynamics: MOA: Antagonist to the mu-receptor in the GI track and treats the
constipation patients experience when taking opioids without affecting the analgesic effect of
opioids
© Does not cross the BBB therefore does not affect kappa receptor analgesic effect of
opioids
Pharmacokinetics: Metabolized in the liver into 5 metabolites
Pharmacotherapeutics: Caution: can cause opioid withdrawal, monitor closely
Adverse reactions: abdominal pain, nausea, diarrhea, hyperhidrosis
Do not take with other opioid antagonists, additive effects
Rapid Response and Short Term
0 Stimulants are the drug of choice when rapid response is needed
oO. All are equally effective, short term
O Osmotic laxative work quickly as well
© Magnesium hydroxide produces evacuation in 6 to 8 hours and is generally administered before HS
O PEG 3350produces a BM in 1 to 3 days
O Docusate sodium is the preferred surfactant
Slower Response and Long Term
0 Bulk-forming laxatives are the drug of choice when rapid response is not needed and long term management
with the least ADRs
© Well suited for older adults
0 Product choices depends upon patient’s acceptance of texture and taste
© Lactulose can be used if the bulk forming laxatives do not work or not well tolerated
0 Works well in older adults and children
Special Indications
O Polyethylene glycol electrolyte solutions is the best drug for cleansing the bowel for radiological or surgical
procedures
O_ Highly effective and no electrolyte disturbances
© Lactulose: effective in reducing ammonia levels in the blood and brain with patient who have hepatic
encephalopathy
0 _Lubiprostone is indicated for the treatment of constipation associated with IBS in women aged 18 and older or
chronic idiopathic constipation, opioid induced constipation with chronic noncancer pain
O Methylnaltrexone is indicated for constipation associated with chronic opioid use
Pregnancy
oO Bulk forming laxatives and surfactant are safe and effective for regular use throughout pregnancy and for
lactating women
© Magnesium hydroxide is Preg Cat B and can be used intermittently
Monitoring
0 For patients taking laxatives for more than 6 months, laboratory assessment of fluid and electrolytes, K, and Mg |
0 Careful monitoring r/t hepatic encephalopathy
oO For older adults taking lactulose for more than 6 months: lab assessment of K, Cl, and CO2
Patient Education
© Donot take laxatives with NV or ABD pain, may indicate serious d/o
© Rapid acting laxatives are best taken in the morning
0 Slower acting ones are best taken at bedtime
0 Taking on an empty stomach with a full glass of water produces more rapid results
0 Donot crush or chew EC tablets
0 Liquids can be given with fruit juice
O Be careful when pouring bulk forming powder: hypersensitivity reactions have occurred when powder inhaled
0 Lifestyle management
pyr) Indication Dosage Form prre Notes
Bisacodyl Constipation Tablets: 5 mg Children >12 yr and adults: Up to 30 mg have been
Dulcolax Suppositories: 10 mg Tablets; 10-15 mg once daily used as preparation
PR: 10 mg once daily for bowel procedure
Children 2-11 yr: ‘Vablets: 5 mg
(0.3 mg/kg) once daily
PR: 5 mg once daily
Children <2 yr: PR: 5 mg single dose
Cascara sagrada Constipation Tablets: 325 mg Children >12 yr and adults: Tablets and liquids come
Tablets: 300 mg-I g once daily in combinations with
Extract tablet: 200-400 mg daily docusate and milk of
magnesia
Castor oil Constipation Oil Children >12 yr and adults: 15-60 mL.
Generic ina single dose
Children 2-11 yr: 5-15 mL ina single
dose
Docusate calcium Constipation Capsules: 50, 240 mg Calcium
Surfake Adults: 240 mg once daily
Children >6 yr: 50-150 mg once daily
Docusate potassium Capsules: 100, 240 mg Potassium
(Diocto-K, Dialose, Adults: 100-300 mg once daily
Kasof) Children >6 yr: 100 mg once daily at
bedtime
Docusate sodium Capsules: 50, 100 mg Sodium
(Colace) Syrup: 60 mg/15 mL Children >12 yr and adults: 50-500
Liquid: 150 mg/15 mL. mg once daily
Children 6-11 yr: 40-120 mg once
daily
Children 3-6 yr: 20-60 mg once daily
Children <3 yr: 10-40 mg
Suppository:
Adults: 50-100 mg or 1 suppository
Glycerin PR Constipation Suppositories: Adult, Children >6 yr and adults: 2-3 gas
Pediatric suppository or 5-15 mg as enema
Children <6 yr: 1-1.7 g as a supposi-
tory or 2-5 ml. as enema
Lactulose Constipation Syrup: 10 g lactulose/ Adults; 15-30 mL once daily May use up to 60 mg/d;
(Cephulac, Chronulac, 15 mL Children: 7.5 mL once daily unlabeled use
Enulose)
Generic
Hepatic Adults: 30-45 mL tid—qid May be given qi-2h
encephalopathy Children and adolescents: 40-90 mL initially; goal is 2-3 soft
daily in divided doses stools/d; discontinue if
Infants: 2.5-10 mL daily in divided diarrhea develops
doses
Magnesium salts Constipation Granules: 40 mEq Mg** Hydroxide (milk of magnesia)
Epsom salts per 5g Children >12 yr and adults: 30-60 mL
Magnesium hydroxide Chewable tablets: ‘once daily (in concentrate:
Milk of magnesia 300 and 600 mg 10-20 mL. once daily)
Magnesium citrate Liquid: 80 mEq Mg* Children 6-11 yr: 15-30 mL in single
per 30 mL or divided doses
Liquid: 77 mEq Mg?+ Children 2-5 yr: 5-15 mg in divided
per 100 mL doses
Bowel prep or Citrate
bowel cleanout Children >12 yr and adults: 240 ml.
if impacted Children 6-11 yr: 100 mL.
Polyethylene glycol/ Bowel prep Inoral solution or pow- Adults: 240 mL every 10 min (up to Tastes salty, making it diffi-
electrolyte solution der for oral solution 4L) until fecal discharge is clear cult to take. Ice it. May
(Colyte, GoLYTEly) with no solid material suck on hard candy or
Children: 25-40 mg/kg/h until fecal breath mints to make
discharge is clear with no solid more palatable.
material
PEG 3350 Constipation Powder for solution: Adults: oral 17 g daily Mix with 4 to 8 oz of
(Miralax) 17 gldose Children >4 yr: 0.7-L5 g/kg daily, do beverage
not exceed 17 g
Psyllium: Constipation Powder: 3.4 g psyl- Adults: 1-2 tspipacket/wafer (3-6 g Up to 30 g/d in divided
(Fiberall, Konsyl, lium/5 mL, 6 g psyllium) in or with a full glass of doses
Metamucil) psyllium/S mL liquid bid-tid Up to 15 gid in divided
Waters: 1.7 g psyllium, Children >6 yr: 1 tsp/packet/wafer doses
3.4 psyllium (15-3 g psyllium) in or with
Effervescent powder: 4-1 glass of liquid bid-tid
3.4 g/5 mL.
Senna Constipation Tablets: 187 mg Children >12 yr and adults: Fletcher's Castoria lists a
(Senokot, Fletcher's Granules: 326 mg 360 mg-2 gat bedtime children’s dose of
Castoria) Syrup: 218 mg/5 mL Children 6-11 yr: 50% of adult dose 10-15 mL (6-15 yr) and
Liquid: 33.3 mg/mL Children 1-5 yr: 33% of adult dose 5-10 mL. (2-5 yr)
Rectal:
Children >12 yr and adults:
30 mg qid-bid
> GERD (Treatment, dosing, and patient education)
O Treatment
= Goals of treatment: reduce or eliminate symptoms, heal any esophageal lesions, manage, or
prevent complications such as stricture, Barret’s esophagus, or esophageal carcinoma, and
prevent relapse
= Meeting these goals requires both lifestyle modification and drug therapy
= Each of the contributing factors (decreased LES tone, acid, peristalsis, and mucosal exposure) are
targets for pharmacological management
= Drugs to Improve LES tone:
¢ metoclopramide and bethanechol: Not considered for monotherapy
0 Most useful in combination with aid suppression with gastroparesis
O Antimicrobials: clarithromycin, tetracycline, amoxicillin, levofloxacin, and metronidazole
O Given ina tiple drug regimen (Two antimicrobials and a PPI x 14 days) or a quadruple drug regimen that
includes bismuth subsalicylate
O Acid suppression by the PPI in conjunction with the antimicrobial help alleviate ulcer relate symptoms,
heals gastric mucosal inflammation, and may enhance the efficacy of antimicrobial agent against H.
pylori
O Goals of treatment: eradicate H. pylori, heal ulcers, manage, or prevent complications such as Gl
bleeding or gastric carcinoma, prevent relapse, and reduce or eliminate symptoms
O Meeting these goals requires both lifestyle modification and drug therapy
O Algorithm: outlines the steps in treating peptic ulcers, consists of healing the ulcer and preventing ulcer
recurrence through eradication of H. pylori
= Step 1: lifestyle modification, OTC antacids or H2RA
= Step 2: h. pylori testing and PPI if uncomplicated Step 3
= Step 3: Treatment for H. pylori with ABX and PPI
¢ PPI continue for 8-12 weeks until healing complete
0 If lowrisk: No ongoing therapy
0. If high risk: Consider chronic suppressive therapy with PPI or H2RA (smokers,
>60 y/o, COPD, CAD, Hx of bleeding or perforated ulcer, patients on NSAIDs)
= If complicated (bleeding)-Refer to GASTRO for endo-Tx for H. Pylori-Repeat endo in 12 weeks to
determine healing
O Antacids: Aluminum hydroxide/magnesium hydroxide combination
= Maalox 15-30 mL PRN 1 hr and 3 hr after meals and before bed
O PPls-multidrug regimen for ulcers, short-term therapy
= Take on an empty stomach before meals
O Education:
= Stop taking PPIs two weeks before H pylori testing ARF false negative
= Take all medications are prescribed
= ADRs
= Reasons why the drugs are being taken
IBS (Treatment, Dosing and Patient Education)
= Laxatives: stimulants and chloride channel activators
= Stimulants: cascara, sena, bisacodyl, and castor oil
oO Caster oil: contraindicated in pregnancy
= Chloride channel activator: Lubiprostone (Amitiza)
O IBS with constipation in women 18 and older
0 Nausea, take with food
O Nausea diarrhea, and dyspnea in doses 24 mcg BID
= Do not take laxatives with NV or ABD pain, may indicate serious d/o
= Rapid acting laxatives are best taken in the morning
= Taking on an empty stomach with a full glass of water produces more rapid results
= Do not crush or chew EC tablets
= Liquids can be given with fruit juice
= Lifestyle management
Traveler’s Diarrhea (Treatment, Dosing, and Patient Education)
© Bismuth subsalicylate and loperamide (Imodium)
¢ Bismuth subsalicylate: two tablets or 2 Fl oz before each meal and at bedtime (QID) for up to 3 weeks
O 524mg every 30 minutes for up to 8 doses
¢ Prevention and treatment
¢ High-risk areas: Central and South American, Africa, Middle East, Mexico, and Asia
e E.Coli is the most common causative agent followed by Campylobacter, Shigella, and Salmonella
° Decrease ASA intake while taking bismuth subsalicylate: salicylate toxicity
¢ Can turn the tongue and stool black/gray: not cause for concern, normal finding
¢ —Loperamide (Imodium): Adults 4 mg initially, 2 mg after each loose stool, not to exceed 8 mg/day OTC or
16mg/day Rx
Black box warning for metoclopramide:
. BLACK BOX WARNING: risk for developing tardive dyskinesia and parkinsonian-like symptoms, the
risk increases the longer it’s in use, treatment should not exceed 12 weeks and be discontinued
immediately if signs of movement disorder, Report involuntary movement of the eyes, face, or
limbs immediately
Step wise progression of PPls: antacids and lifestyle modifications followed by PPI trial
Effectiveness of different PPls: No significant differences between effectiveness of PPIs
Triple therapy for H.Pylori Eradication:
> Allinclude a BID dose of PPI
> Most popular ABX are clarithromycin (Biaxin) and amoxicillin
> Clarithromycin plus amoxicillin plus a PPI all BID for 10-14 days is most favorable
> Pregnant women should not take tetracycline ARF fetal harm
> Children younger than 8 should not take tetracycline ARF discoloration of teeth
Pica itr ps Pitre) DItrns es
Triple therapy Proton pump Clarithromycin Amoxicillin = ‘Treat for 10-144
inhibitor bid 500 mg bid or ighid Usual first-line therapy
metronidazole
500 mg bid
‘Triple therapy Proton pump Clarithromycin Metronidazole = ‘Treat for 7-14d
inhibitor bid 500 mg bid 500 mg bid Use as first-line therapy
in penicillin-allergic
patients
Quadruple therapy Proton pump Metronidazole ‘Tetracycline™ Bismuth sub- ‘Treat for 10-14 d
inhibitor bid or 250 mg qid 500 mg gid salicylate Usually used as second-
Ranitidine 525 mg qid line therapy in pa-
150 mg bid tients who fail first-
line therapy
Levofloxacin-based. Proton pump Levofloxacin Amoxicillin ‘Treat for 10-14 d
triple therapy inhibitor bid 250-500 mg bid 1. gm bid Second-line or rescue
therapy
Chapter 34 GERD and PUD
Misoprostol use for duodenal ulcer prophylaxis and treatment
Misoprostol (Cytotec):
Prophylaxis and Treatment of Duodenal Ulcers Associated with NSAID Use: not as reliable for Tx of ulcers from other
causes