GI Drugs 2 Flashcards by Teofilo Vallester

Salt of sucrose in SUCRALFATE is complexed to

sulfated aluminum hydroxide

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Duration of sucralfate’s tenacious paste on ulcers

6 hours

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MOA of sucralfate

It is NEGATIVELY CHARGED and it binds to the POSITIVELY CHARGED proteins in the base of ulcers

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Superficial break found only in the mucosa

Erosions

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Deeper lesions extending up to the muscularis

Ulcers

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Sucralfate vs H2RA

Sucralfate is less effective and it will only work in an ACIDIC environment

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Sucralfate is taken when?

1 hour before meals

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ADR of Sucralfate is minimal because?

It is not systemically absorbed

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Constipation in Sucralfate

Accumulation of ALUMINUM

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Methyl analog of PGE1

Misoprostol

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Dose reduction is not needed in Prostaglandin analogs. Why?

It is excreted in the urine

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Only indication of Misoprostol

MISSED ABORTION

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MOA of Prostaglandin analogs

Binding to PG receptor of parietal cell –> reduced histamine stimulated cAMP production –> acid inhibition

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Other actions of Misoprostol

Intestinal fluid and electrolyte secretion

Uterine contractions

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Increase intestinal motility is facilitated by?

It’s VASODILATING effect

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Most significant CI of Misoprostol

Mucosal protection in NSAID-induced ulcers

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2 Bismuth Compounds

Bismuth Salicylate
Bismuth subcitrate (tetracycline and metronidazole)

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Main excretion of Bismuth compounds

Stool (reduced frequency and liquidity)

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Direct anti-microbial effects of Bismuth targets what bacteria and dse?

H. pylori, Traveler’s Diarrhea (E. coli)

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Erradication of H. pylori

PPI + Bismuth subsalicylate + Bismuth subcitrate

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Most common ADR of Bismuth

Blackening of stool

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Inhibitory neurotransmitter in the GI

Dopamine

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Cholinomimetic agents

Bethanecol

Neostigmine

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Bethanecol stimulates what receptors in the muscles and myenteric plexuses?

M3 receptors

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Other uses of cholinomimetic Bethanecol

Neurogenic bladder

Ach-ase inhibitor

Neostigmine

Neostigmine is indicate for acute colonic pseudoobstruction or?

Ogilvie's Syndrome

ADR of cholinomimetic Neostigmine

Salivation | Bardycardia

Metoclopramide and Domperidone are?

D2 receptor antagonists

MOA of Metoclopramide and Domperidone?

Inhibits smooth muscle stimulation --> PROKINESIS

3 actions of Metoclopramide and Domperidone

Increase eophageal peristalsis Increase LES pressure Enhance gastric emptying time

Specificity of Metoclopramide and Domperidone

Do not affect intestinal and colonic motility

Anti-nausea and anti-emetic action

D2 receptor blockade in the CTZ

Metoclopramide use

anti-emetic

Domperidone use

GERD | Postpartum lactation

Macrolide mainly used for MOTILIN receptor stimulation

IV Erythromycin

Plant derivatives of bulk-forming laxatives

Psyllium | Methylcellulose

Intermittent constipation is best prevented by

High fiber diet Fluids Exercise Heeding of nature's call

Synthetic derivative of bulk-forming laxatives

Polycarbophil

MOA of Bulk-forming laxatives

Increase absorption of water, fromation of bulky emolient gel, increase colon distention = increase colon peristalsis

Softeners are administered

Oral or Rectal

Used in hospitalized patients to prevent constipation and minimize straining

Docusate

Vasovagal reflex in cardiac patients

strain

Lubricates fecal material, retarding water absorption from the stool

Mineral Oil

ADR of Mineral Oil

Impaired absorption of ADEK | LIPID PNEUMONITIS

Osmotic Laxatives are

soluble but nonabsorbable

PEG difference with bulk-forming laxatives

does not produce flatus

Osmotic laxative for ACUTE CONSTIPATION or for the prevention of chronic constipation

Non-absorbable Sugars and salts

Sorbitol and Lactulose are

Non absorbable SUGARS

Prevents hepatic encephalopathy

Lactulose

Non absorbable antibiotic used in HE

Neomycin

Hepatic encephalopathy pathogenesis

Stool stays in the colon serves as food to attract bacteria, digestion and end product is AMMONIA

Magnesium citrate and sodium phosphate ADR

Dehydration MOA- High volume of liquid stool followed by rapid constipation relief

Sodium Phosphate ADR

Hyperphosphatemia Hypocalcemia Hypernatremia Hypokalemia

Laxatives that are safest in long term use

Stimulant Laxatives

Stimulant laxatives that are derived from plants

Anthraquinone derivatives

Anthraquionones Oral and Rectal effect

Oral- 6-12 hours | Rectal- 2hrs

Antharquinone derivatives chronic use ADR

MELANOSIS COLI - brown spots in the colon

Bisacodyl is in what form of stimulant laxative?

Diphenylmethane derivative

Diphenylmethanes Oral and Rectal effect

Oral- 6-10 hrs | Rectal- 30-60 minutes

Used for colonic cleansing

Bisacodyl + PEG

Chloride Channel Activator

Lubiprostone

Lubiprostone Indications

Chronic constipation and IBS

Lubiprostone is derived from

Prostanoic acid

Lubiprostone MOA

Stimulates CIC 2 in the SI -> stimulates intestinal motility -> shortens transit time (soft stools)

Lubiprostone is in what category in pregnancy?

C - PregnanC

Opioid MOA on GI

Dec intestinal motility -> prolonged transit time

Selective antagonists of the u-opiod receptor and it cannot cross the BBB

Methylnaltrexone bromide and Alvimopan

Opioid induced constipation in patients receiving palliative care

Methylnaltrexone

Treatment for shortening the period of post operative ileus

Alvimopan

ADR of Alvimopan after more than 7 days of usage

Cardiotoxicity

Serotonin 5-HT4 PARTIAL agonists

Tegaserod | Cisapride

Serotonin 5-HT4 agonist that causes QT prolongation

Cisapride

High affinity for 5 HT4 receptor, found in Europe and for WOMEN

Prucalopride "PUTAlopride"

Contraindications for usage of Anti-diarrheal

Blood diarrhea High fever Systemic toxicity

Opioid agonist that does not cross the BBB thus no potential for addiction

Loperamide

Opioid agonist that do not cross the BBB having high potential for addiction

Diphenoxylate

Bile salt binding resins that decreases diarrhea by causing excess fecal bile acids

Cholestyramine Colestipol Colesevelam

Cholestyramine and colestipol

should not be given within 2 hours with other drugs

A somatostatin analog

Octreotide

Octreotide clinical indications

VIPomas Dumping syndrome Diarrhea due to vagotomy

ADR of octreotide

Steatorrhea - ADEK deficiency Gallstones (inhibits gallbladder contractions) Hypothyroidism

Serotonin 5HT3 antagonists are restricted to

Emesis due to post vagal stimulation | Emesis post-chemotheraphy

Ondansetron, Ganisetron and Dolasetron

administered daily, half-life of 4-9 hours

Greater affinity for 5HT3 and have longest (40 hrs) half life

Palonosetron "PaLONGnosetron"

Best effective for anti emesis post chemotherapeutic

30 minutes prior to chemo

Enhanced combination therapy for anti emesis post chemotherapeutic

5HT3 antagonists + Dexamethasone + NK- 1 antagonist (e.g. Aprepitant)

QT prolongation of 5HT3 antagonists is best pronounced by

Dolasetron

Corticoids used in anti-emesis

Dexamethasone | Methylprednisolone

Highly selective NK-1 antagonist that CROSSES the BBB

Aprepitant

converted to Aprepitant after infusion within 30 minutes

Fosaprepitant

Drugs that increase Aprepitant levels

Ketoconazole, Ciprofloxacin, Verapamil, Quinidine

Phenothiazines and Butyrophemones are

anti-psychotics with anti-emetic and sedative properties

Phenothiazines MOA

Inhibition of dopamine and muscarinic receptors

Extremely sedating butyrophemones

Droperidol

Droperidol ADR

Extrapyramidal effects QT prolongation Torsades de pointes

Metoclopramide and Trimethobenzamide inhibits dopamine receptor. What are their ADR?

Extrapyramidal | Parkinsonian

Meclizine and Hyoscine

Anti-histamines

Vertigo with labyrinth dysfunction

Meclizine

Best for motion sickness; given as transdermal patch

Hyoscine

Cannabinoid used as anti-emetic agent

Dronabinol

Dronabinol effects

Anti emesis | Appetite stimulant

Dronabinol ADR

Euphoria, Dysphoria, Sedation | Tachycardia + Orthostatic Hypotension