Gastrointestinal Drugs Flashcards
The enteric nervous system is an extensive network of interconnected ____ and ____
interneurons within the gastrointestinal ___ that can control gut function _______ of the CNS
sensory, motor, wall, independently
The enteric nervous system is characterized by the presence of a complex intrinsic neural network that includes the _____
plexus and the ______ plexus
myenteric, submucosal
The submucosal plexus is located under the ______ layer of the gut. The myenteric plexus
resides between the ______ ____ muscle layer and the ____ _______ muscle layer
submucosal, inner circular, outer longitudinal
The ENS is extensively innervated by ________ _______ nerve fibers.Its sensory and motor interneurons can also be influenced by the CNS through input from _____ and ______ subdivisions
nonadrenergic-noncholinergic (NANC), sympathetic, parasympathetic
Myenteric plexus
Yellow represents nerve endings
Plexus submucosas
Emesis is a complex reflex activity (______ reflex) and its coordination is centered in the _______. Although several afferent pathways may be responsible for initiating emesis, all signals are
coordinated by the ____ center (______ center) located in the ____ _______. An important structure outside the GI-tract that supplies afferent input is the ________ ________ _____. This is sensitive to the presence of ____ and _____ in the blood
protective, brainstem, emetic, vomiting, mid brainstem, chemoreceptor
trigger zone (CTZ or CRTZ), drugs, toxins
Emesis is _________ induced to empty the ____ portion of the digest tract. List the examples in which emesis is induced:
A number of substances induce emesis by:
* Distending the ______, ______, _____, or _______ ( _______ organs)
* ________ the epithelium of the GI-tract (gastric _____ or _____)
pharmacologically, anterior
→ Preparation for induction of general anesthesia (food in the stomach)
→ Treatment of ingested, noncorrosive poisons
pharynx, esophagus, stomach, duodenum, hollow, Irritating, mucosa, pharynx
Peripherally acting (reflex) emetics
* Distention with ____ water or ____ can induce the emetic response
* In case of toxin ingestion, administration of ____ water by _____ tube may help ____ poisons
* Emesis can be induced in dogs by oral administration of a solution of: (1) Pharyngeal placement of a small amount of plain ____ _____ or neutral ____ _____, such as sodium carbonate OR (2) Orally administered _______ ______ (__%) often induces emesis rapidly in cats and dogs → fatal ______ of hydrogen peroxide foam is possible!
Copper sulfate (1%), zinc sulfate (1%)
warm, saline, warm, stomach, dilute
warm saturated (strong) sodium chloride
table salt, salt crystals, hydrogen peroxide, 3, aspiration
Prokinetic drugs increase GI ______, enhance the transit of ______ contents, and are used in ___ and ____ animals → occasionally in ruminants to stimulate gastric _______, ____ or _____ motility
* Intestinal motility is ↓ after intestinal disease, surgery → can lead to ____
motility, intraluminal, small, large, emptying, rumen, intestinal, ileus
Metoclopramide is a ____-soluble derivate of ____-________ __. It has a central (_________) and peripheral (________ and stimulator of ______
receptors) effects.
lipid, para-aminobenzoic acid, antidopaminergic, antidopaminergic, cholinergic
Metoclopramide has multiple actions:
→ D2 ______
→ Serotonin (5-HT3) _______
→ Serotonin (5-HT4) ______
→ Increase in the release of ____ in the ____-tract
→ Increase gastric _____
→ Increase ____ of the esophageal sphincter
→ Stimulates motility of the _______ (less effect on ____ segments)
→ Endocrine effects: transient increase in ______ and ______.
antagonist, antagonist, agonist, Ach, GI, emptying, tone, duodenum, distal, prolactin, aldosterone
Prokinetic drugs increase ?
GI motility
Metoclopramide is used in small animals to:
1. Stimulate ____ upper motility following _______ surgery (for gastric _____)
2. _______
3. Postoperative ____
4. Gastric _______
5. Idiopathic _____
–> Contraindicated in GI ______ or ______.
normal, corrective, dilation, Volvulus, ileus, ulceration, gastroparesis, obstruction, perforation
Metoclopramide: use in horses
* Some equine surgeons used infusion of metoclopramide to reduce __________ ____
* It may stimulate _____ ______ but not large bowel
* Undesirable side effects are common → ________ changes and ______
pain
postoperative ileus, small intestine, behavioral, abdominal
Metoclopramide: use in ruminants
* The clinical use of metoclopramide in large animals is ____ common
* It has a little usefulness in ____. It may ↑ the motility of the _____ in cattle and in sheep
* Metoclopramide is used successfully in cattle with functional ______ ______
* At doses higher than 0.1 mg/Kg in calves cause ?
less, cattle, rumen, pyloric stenosis
severe neurological side effects
Cisapride
* Cisapride was removed from the market → serious _______ and _____ in people. These
reactions have not been reported in _____
* It is still available via ______ pharmacists
* Cisapride has a great ______ effect. Agonist for the __-___ receptor on myenteric neurons and
antagonist for __-____ receptor → It may enhance release of ___ at the myenteric plexus
* It causes dose-dependent increased activity at ___ ____ sites: (?)
arrhythmias, deaths, animals, compounding, prokinetic, 5-HT4, 5-HT3, ACh, all GI
Esophagus, stomach, jejunum, ileum, small intestine, and colon
Cisapride
Clinical use in small animals
➢ treatment for ________ reflux, _____
gastric emptying, and _____ bowel motility
disorders
➢ Compared to ________, cisapride is
more effective for increasing ____ esophageal
sphincter ____ in dogs
➢ Cisapride has been used for treating chronic _______ in cats (effect on colonic _____ muscle)
gastroesophageal, delayed, small, metoclopramide, lower, tone, constipation, smooth
Domperidone is a dopamine (D2) _______. It may also have α1-receptor _____ and serotonin (5-HT2) _______ effects
* Its mechanism of action and prokinetic effects are similar to _____
* Domperidone does not cross the ____
* Its peripheral effects accelerate _____ intestinal transit. ______ activity is unaffected
_______ drugs increase GI motility
antagonist, antagonist, antagonist, metclopramide, BBB, small, Colonic, Prokinetic
Domperidone
* Domperidone has been investigated for use in horses to treat _____ toxicity and _____
* The oral absorption in horses is only __- ____%. ____ administration of ____ mg/Kg (the approved dose) had no effect on GI function but at __ mg/Kg ↑ stomach emptying
* ↑ digital laminal microvascular blood flow (horses) → ___________ ____ receptors.
Treatment of laminitis?
Fescue grass toxicosis: forage related disease involving the endocrine disruptive effect of ______ _____ (produce by fungus Neotyphodium coenophialum) on prolactin secretion
fescue, agalactia, 1, 1.5, PO, 1.1, 5, antagonist α2, ergot alkaloids
Erythromycin → a ________ antibiotic used to treat ______ infections
* Erythromycin stimulates GI motility at ____ doses → much lower than the antibacterial dose
* It stimulates GI motility via: activation of _____ receptors, release of endogenous ______ or _____ mechanisms in the upper GI tract
* Motilin is a _______ released from endocrine cells of the ________ mucosa. It ____ the motor contraction
* Most of the motilin receptors are on the ______ and _____ intestine
* Erythromycin is used clinically to increase gastric ______ and for the therapy of ______
esophagitis
* Concerns: may cause _______ (effect on the normal bacteria flora of the _______) and its routine use may promote antibacterial _______.
macrolide, bacterial, low, motilitin, motilitin, cholinergic, peptide, duodenal, ↑, stomach, proximal, emptying, reflux, diarrhea, intestine, resistance
Lidocaine
* It is a well-known ____ anesthetic. Lidocaine is used for ____
infiltration for ____ surgical procedures and to treat cardiac ______
* IV infusions of lidocaine improve intestinal _____ in ____
→ It reduces?
local, local, minor, arrhythmias, motility, horses, postoperative ileus
Postoperative ileus (widespread clinical problem) may be caused by?
How does lidocaine restore motility?
- How lidocaine restores motility is not understood. It is said lidocaine does not have a direct prokinetic effect
- It may act by inhibiting intestinal inflammation and reperfusion injury or via
suppression of painful stimuli
What are the adverse effects of lidocaine?
Adverse effects
* Muscle fasciculation
* Ataxia and seizures ↓ rate of infusion
Name the Peripheral opiate antagonists:
alvimopan, methylnaltrexone, and naloxegol
- Activation of opiate μ receptors in the intestinal smooth muscle ____ propulsive motility
- μ-opiate receptors have been found in the _________ plexus, _______ plexus, and __________ muscle of ____
- Activating these receptors has been used to treat some forms of _____ (e.g., _______)
- Selective peripheral opiate antagonists act as peripheral opioid antagonists → they are unable to cross the ____ (______ polarity)
- Alvimopan > methylnaltrexone → ______ and _____ of activity
- Alvimopan is administered ____ → ___ bioavailability (6%) and produces a ____ effect on the intestine to promote ______.
- Naloxegol is used for ____ treatment of ____-induced constipation
↓ , submucosal, myenteric, longitudinal, ileum, diarrhea, loperamide, BBB, high, potency, duration, orally, low, local, motility, oral, opioid
List the principal drugs used to manage GI ulceration in small and large animals.
Histamine (H2) receptors antagonists
sucralfate
proton pump inhibitors (omeprazole)
antacids
List the other clinical uses of the drugs typically used to treat GI ulcers in small and large animals.
Clinical uses
* ________
* _______ ulcers
* ____________ ulcers
* _________________ ulcer ________
* ______________
* ________ cells tumor
* _______________ syndromes
* Prevention and treatment of _____-induced ulcers
Gastric HCL secretion is _________ in carnivores rather than __________ as in humans
Clinical uses
* Gastritis
* Gastritis ulcers
* Duodenal ulcers
* Gastrointestinal ulcer prevention
* Esophagitis
* Mast cells tumor
* Hypergastrinemic syndromes
* Prevention and treatment of NSAID-induced ulcers
Gastric HCL secretion is intermittent in carnivores rather than continuous as in humans
Gastrointestinal ulceration
Gastrointestinal ulceration is an important medical problem in ____.
* Prevalance in animals involved in showing and racing → ___-___%
Contributing factors:
* ____ confinement
* Intense _____
* Diet (↑ ___ concentrated in diet)
* Racing ___
* _______ feeding schedule
* ↑ stomach ____
* Use of ____
horses, 81-93, Stall, exercise, energy, stress, Intermitent, acidity, NSAIDs
Drugs for Treatment of Gastrointestinal Ulcers in Animals
Antacids
* These drugs _______ stomach acid through a simple reaction to form ____ and
neutral ___
* Antacids are bases of either ?
Adverse effects
* _____ → they are seldom administered _____-term. They are not _______
* In animals with kidney disease, ________ accumulation may be a problem
* They interfere with the _____ absorption of other drugs → chelate with ___________ or ____________. Administer the AB __ h prior to the administration of the antacid drug
neutralize, water, salt, aluminium, magnesium, or calcium, Rare, long, absorbed, magnesium, oral, fluoroquinolones, tetracyclines, 2
List the effects of the following
The Histamine (H2) receptor antagonists are?
cimetidine, ranitidine, famotidine, and nizatidine
Christine Ran For Nuj
- H2-receptor antagonists are _______, ______ inhibitors that reduce both the _______ and the ______ ion content of gastric secretion and the amount of pepsin
- These drugs became popular after their release in the 1980s. Their use has declined → more _____ and _____-acting proton pump inhibitors
- Blockade of histamine H2 receptors on gastric parietal cells inhibits gastric ____
- In studies that have measured stomach acidity, or compared results with proton pump inhibitors ___-________ _______ were less effective
reversible, competitive, amount, hydrogen, potent, longer, acidity, H2-receptors antagonist
Acid secretion is stimulated by three receptors:
- Gastrin receptors: endocrine gastrin→ CCK
- Histamine type-2 (H2): paracrine
- Muscarinic receptor type-3 (M3): neuronal ACh