GI Motility

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DRUGS ON

G.I.
MOTILITY
Drugs affecting GI
motility /activity

01 02 03
Speed up Increase Decrease
/improve
movement of tone of GI the
intestinal tract movement
contents
Laxatives
3 major
categories
GI stimulants

Anti-Diarrheal
Laxatives
• Cathartic drugs
• Short term relief of constipation (after
surgery, MI, OB delivery, remove
poisons, antihelmintic therapy
• Diagnostic procedures
• OTC prep*
Chemical stimulants
Kinds of
Laxatives Bulk stimulants

Lubricants
Peristaltic/Myenteric Reflex

Food bolus (gut)


Stretch smooth muscle
Stretch receptors (oral to aboral)
Sensory muscles- Serotonin
Myenteric plexus-
contraction/motility
ANS (T,L,S)
- Para- rest and digest
- Sympathetic- inhibit (secretion,
digestion) contraction of GI
sphincter and BV)
ENS (Enteral Nervous System)- vagus
- Myenteric Plexus –
(neurotransmitters and receptors )
 Acting (Cholinergic)
Inhibiting (Nitrogenergic)
Chemical stimulants
• bisacodyl (lower GI tract)
• cascara (overnight effects)
• castor oil (blocks fat absorption) onset: 2-6 hours directly stimulate the nerve
• senna (tablet, syrup, rectal suppository) plexus (intestinal wall)-
• Onset: 6-8 hours (overnight) increase movement
• Hypersensitivity reactions and acute abd.
disorders (rupture, exacerbation)
• CNS effects
• Laxatives- caution- CAD, debilitation, pregnancy
(electrolyte imbalance)
Castor oil- premature labor
Magnesium laxatives- diarrhea
in neonate

WOF- Cathartic Dependence (long


term use)- Impaction
Bulk
stimulants
• Rapid acting, aggressive
which causes fecal matter to
increase in bulk
• Mechanical stimulants
• Increase fluid, Fecal matter
(increase in bulk)
Bulk laxatives
- Lactulose (osmotic laxative)
- magnesium citrate
- magnesium hydroxide (Milk of Magnesia)
- magnesium sulfate (Epsom)- hypertonic pull
- polycarbophil psyllium - gelatin like bulk

- Effective in GI tract, not absorbed systemically


- Taken orally

Pharmacokinetics - Not generally absorbed systemically


- Rapid acting
Allergy

Acute abdominal disorders- AP, Diverticulitis ,


Ulcerative Colitis

Contraindications CAD, Heart block

Change in electrolyte levels

Precipitate Labor, Pregnancy and lactation


(caution)
GI effects (diarrhea, cramping, nausea)

CNS effects
Adverse Sweating, palpitations, flushing and fainting
effects Take plenty of water

Drug interaction – 30 minutes interval


Lubricants
• docusate (Colace) - action (fat
and water)– softer stool
• glycerin (Sani-Supp) *
hyperosmolar laxative
(suppository form)
• mineral oil (Agoral Liquid) *
form slippery coat

* No stimulation in the GI tract


Pharmacokinetics
- Not absorbed systemically
- Excreted in feces
Contraindications
• allergy
• Abdominal disorders
• CAD
• Changes in electrolyte levels
Adverse effects
• Diarrhea
• Cramping
• Nausea
• Leakage and staining (mineral oil)
• CNS effects
Drug to Drug Interaction
• Mineral Oil – interfere with absorption of fat soluble vitamins ( ADEK)
Gastrointestinal Stimulants
• Stimulate parasympathetic activity (GI) – GI secretions and motility
• Rapid movement is desired
• dexpanthenol (Ilopan)- increase Acetylcholine
• metoclopramide (Reglan) – block dopamine receptors *
 increase GI motility
Pharmacokinetics
• dexpanthenol – IM injections , peak within 4 hours
• metoclopramide- orally, IM, IV, peak 60-90 minutes
• Cross placenta and BM
Contraindications
• Allergy
• GI obstruction or perforation
• Pregnancy and Lactation- category C
Adverse effects
• n/v, diarrhea
• Spasm and cramping
• Declining BP, HR, weakness,
fatigue – parasympathetic
stimulation, extrapyramidal
effects, Parkinson like syndrome
Drug to Drug Interaction
• Metoclopramide and Digoxin ( decreased absorption)
- Cyclosporine ( toxicity)
- Alcohol and sedative drugs (increased sedation)
Antidiarrheals
• Block stimulation of GI tract (relief diarrhea)
bismuth subsalicylate (Pepto- Bismol) – travelers diarrhea, cramping,
distention 2 to dietary excess/viral infection
crofelemer (Fulyzag)- non infectious diarrhea HIV/AIDS antiretroviral
meds
loperamide (Imodium)- short term diarrhea
opium derivatives (paregoric) – cramping and diarrhea
* Direct actions on the muscles of GI tract
- acute/ chronic diarrhea
- Reduce volume of ileostomies
Contraindications
• Allergy
• Pregnancy and lactation
• GI obstruction
• Diarrhea due to poisoning(increased absorption)
• Hepatic impairment
Adverse effects
• Constipation, distention, abd. Discomfort
• n/v, dry mouth,
• Toxic megacolon
Opiods- sedation, hallucination, respiratory depression, Cat C
Irritable Bowel Syndrome (IBM)
• Abdominal distress (diarrhea, constipation, bloating, nausea,
flatulence, headache, fatigue, depression, anxiety
• Stress related
alosetron ( Lotromex)- FDA rereleased * WOF ischemic colitis
lubiprostone (Amitiza) – increase motility * tx for chronic idiopathic
constipation
hyoscyamine (Anazpas) – decrease GI spasm

Stress Mgt
Miscellaneous Agents
• Cannabis/Marijuana- suppress cortical areas of CNS
• dronabinol and nabilone – only for nausea and vomiting associated
with Cancer therapy
Practice Questions
1. The laxative of choice when mild stimulation is needed to prevent
straining is:
a. Senna
b. Castor oil
c. Bisacodyl
d. Magnesium citrate
2. Cathartic Dependence can occur when:
a. Patients do not use laxatives routinely and experience severe bouts
of constipation
b. Chronic laxative use leads to reliance on the intense stimulation of
laxatives
c. Patients maintain a nutritious high fiber diet
d. Patient start an exercise program to promote bowel elimination
3. Drugs that stimulate parasympathetic activity are used to increase GI
activity and secretions. For which of the following would this group be
most likely used?
a. Doudenal Ulcers
b. Gastric Ulcers
c. Gastroesophageal reflux
d. Poisoning, to induce nausea and vomiting
4. The drug of choice for treating/preventing traveler’s diarrhea is:
a. Loperamide
b. Opium
c. Rifaximin
d. Bisacodyl

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