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GI Drugs 1 Flashcards

1
Q

Two major physiological states of gastric acid production:

A
  • Basal

* Meal stimulated

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2
Q

Which drug causes Therapeutic neutralization of low gastric pH protecting esophageal mucosa from reflux corrosion?

A

Antacids

Time of onset: 5 minutes
Duration of action: 30 minutes to 1 hour

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3
Q

Examples of antacids

A

Aluminum hydroxide
Magnesium hydroxide
Calcium carbonate

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4
Q

Antacids shouldn’t be co administered with which drugs ? And why ?

A

tetracyclines, fluoroquinolones, itraconazole and iron

- Increased gastric pH alters dissolution of weakly charged drugs —> decreases the absorption of these drugs

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5
Q

Which antacid causes constipation?

A

Aluminum hydroxide

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6
Q

Which antacid causes osmotic diarrhea ?

A

Magnesium hydroxide

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7
Q

____ and ____ often combine to produce no net change in bowel movements

A

Al and Mg

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8
Q

Which antacid causes Co2 belching and metabolic alkalosis (milk alkali syndrome)?

A

Calcium carbonate

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9
Q

Functions of H2 Receptor antagonists

A
  • Suppress histamine induced gastric acid secretion

* Reduce signal transduction for ACh and Gastrin-induced acid production

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10
Q

Examples of H2 receptor antagonists

A

• Cimetidine: prototype with many adverse effects
• Famotidine, Nizatidine: Second generation with no
anti-adrogenic or CNS adverse effects

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11
Q

_________ strongly suppress basal gastric acid secretion and has a modest effect on meal stimulation secretion

A

H2 Receptor Antagonist

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12
Q

When do you use H2 receptor antagonists

A
  • GERD (Gastro-esophageal reflux disease)
  • PUD (Peptic ulcer disease)
  • Non-ulcer dyspepsia
  • Prophylaxis against stress-related gastritis
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13
Q

Adverse effects of H2 Receptor

A

Increased gastric pH: B12 deficiency and myelosuppression in long-term use

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14
Q

Adverse effects of Cimetidine only

A

• Gynecomastia, galactorrhea, male impotence
- Acts as a nonsteroidal anti-androgen and prolactin stimulant
• Crosses the blood-brain barrier
- Confusion, dizziness and headaches

• Potent inhibition of CYP450 system

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15
Q

Cimetidine increases the serum concentration of which drugs

A
  • Warfarin
  • Diazepam
  • Phenytoin
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16
Q

These drugs Irreversibly bind and inhibit the hydrogen-potassium (H+ - K+) ATPase pump of gastric parietal cells suppressing the final common pathway of gastric acid secretion

A

Proton pump inhibitors

  • Most potent inhibitors of gastric acid secretion
  • Inhibit of 90-98% of 24 hour acid secretion
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17
Q

Effect of PPIs on Gastric Acid Secretion

A

PPIs effectively suppress both basal- and meal- stimulated gastric acid production

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18
Q

Examples of PPI

A 
• Omeprazole
• Esomeprazole
• Rabeprazole 
• Pantoprazole
Lansoprazole
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19
Q

Which type of drugs should be used under these circumstances

• Gastrinoma(ZES)
• Non-ulcer dyspepsia
• Prophylaxis against stress-related gastritis
• Patients who fail twice-daily H2RA therapy
• Severe symptoms of GERD that impair quality of life
• (PUD) Peptic ulcer disease
- NSAID associated ulcers
- Prevention of peptic ulcer bleeding

A

PPI

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20
Q

Adverse effects of PPIs

A
  • Vitamin B12 deficiency due to reduced pepsin function
  • Increased risk of community-acquired pneumonias and C. difficile colitis
  • Hypomagnesemia
  • Osteopenia: possibly via reduced CA2+ absorption or osteoclast inhibition.

• All PPIs carry an FDA-marked mandated warning of a possible increase risk of hip, spine, and wrist fractures

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21
Q

Omeprazole: may inhibit the CYP450 metabolism of:

A
  • Warfarin
  • Diazepam
  • Phenytoin
22
Q

Omeprazole , esomeprazole and lansoprazole reduce the activation of which drug ?

A

Clopidogrel

- because it requires P450 CYP2C19 isoenzyme to be activated and these drugs inhibit CYP2C19

23
Q

How to treat H pylori

A

• Triple therapy: two antibiotics with a PPI
- clarithromycin + amoxicillin + PPI OR
- clarithromycin + metronidazole + PPI
• Quadruple therapy: 2 antibiotics with a PPI and bismuth subsalicylate
- Bisthmus subsalicylate +metronidazole +tetracycline +PPI
• Both regimens: antibiotics given for 10-13 days and the PPI for 1 month

24
Q

This drug is an analog of PGE1; binds the EP3 receptor stimulating the GI pathway to decrease gastric acid secretion; Stimulates mucus and bicarbonate secretion and Enhances mucosal blood flow

A

Mucosal Protective Agents: Misoprostol

25
Properties of misoprostol
* Approved for prevention of NSAID-induced ulcers in high-risk patients * Diarrhea, abdominal pain and/or cramps occur in 30% of patients * Contraindicated in pregnancy due to abortifacient effects
26
Forms a viscous paste that binds selectively to ulcers
Mucosal Protective Agents: Sucralfate
27
Properties of sucralfate
Sucralfate: salt of sucrose + sulfated aluminum hydroxide Forms a viscous paste that binds selectively to ulcers Negatively charged sucrose sulfate binds positively charged proteins forming a physical barrier Restricts further caustic damage Stimulates mucosal prostaglandin and bicarbonate secretion Limited to the initial management of gastroesophageal reflux disease in pregnancy
28
This drug * Suppresses H. pylori * Used in quadruple antibiotic therapy of H. pylori-positive ulcers
Bismuth subsalicylate | • Pepto-Bismol is widely used for dyspepsia and acute diarrhea
29
Adverse effects of bismuth
Harmless blackening of stool Salicylate toxicity Contraindicated in patients with renal failure
30
Prokinetic drug groups
* Motilin Agonist | * Serotonin(5HT4) Receptor Agonist
31
Properties of prokinetic agents
Should enhance coordinated GI motility • Act ‘upstream’ of ACh at receptor sites on the enteric neuron, or higher • Activation of muscarinic (M1) receptors enhance contraction in a relatively uncoordinated fashion - This produces little or no net propulsive activity - Thus, the cholinomimetic agent, bethanechol and the Ach-esterase inhibitor neostigmine are not currently preferred for treating GI motility disorders
32
Which prokinetic agent is an * Antibiotic * Agonist effects at the motilin receptor * Rapid down-regulation of motilin receptors leads to early tolerance of this drug. (Use is limited to short courses) * Best established indication: diabetic gastroparesis
Erythromycin
33
Which prokinetic drug is a * 5-HT4 receptor agonist; 5-HT3 antagonist * Direct smooth muscle stimulant * Was commonly used for gastroesophageal reflux disease, gastroparesis * No longer available in the US because of potential to induce serious and occasionally fatal cardiac ventricular arrhythmias
Cisapride
34
Which prokinetic drug is a • 5-HT4 receptor agonist • Vagal and central 5-HT3 antagonist • Dopamine (D2) receptor antagonist • Effects confined to the upper digestive tract - Increases lower esophageal sphincter tone - Stimulates antral and small intestinal contractions
Metoclopramide
35
When to use metoclopramide
* Gastroparesis * Antiemetic * GERD for symptomatic relief
36
Adverse effects of metoclopramide
Extrapyramidal effects due to Dopamine antagonism Galactorrhea by blocking the inhibitory effect of dopamine on prolactin release
37
Anti emetic drug list
* Anti-Histamines * CholinergicAntagonists * D2Antagonists * 5-HT3ReceptorAntagonists * Corticosteroids * Neurokinin-1 receptor Blockers * Benzodiazepines * Cannabinoids
38
Antimuscarinics- Scopolamine
* Treatment and prevention of motion sickness | * May have some activity in postoperative nausea and vomiting
39
H1 Antagonists examples
Diphenhydramine Meclizine Cyclizine
40
Function of h1 antagonists
* Histamine H1 antagonists act on vestibular afferents and the brainstem * Useful for motion sickness and postoperative emesis
41
This drug is * Weak D2 receptor antagonism at the CTZ * Sedative Properties are due to antihistaminic and anticholinergic properties effectively treat motion sickness * Low to moderately effective in CINV
Promethazine | D2 Antagonists- Phenothiazines
42
This drug is a - Central Dopaminergic Blockade - Potential for adverse extrapyramidal effects - Prolongation of QT Interval
Droperidol | D2 Antagonists-Butyrophenones
43
Who are the 5HT3 antagonists
* Ondansetron | * Granisetron
44
5HT3 receptors are present in several critical sites involved in emesis including;
* vagal afferents * the solitary tract nucleus (STN) * chemorecptor trigger zone (CTZ) * area postrema (AP)
45
_______________ are the drug of choice for prophylaxis against Acute CINV
5HT3 receptor antagonists are the drug of choice for prophylaxis against Acute CINV
46
5-HT3 antagonists are Effective against_________ | And Not effective against: ________________
Effective against hyperemesis gravidarum | Not effective against: Delayed CINV, motion sickness
47
These drugs work via suppression of peritumoral inflammation and prostaglandin production. They are also highly effective adjuvants in the treatment of nausea in patients with metastatic cancer
Dexamethasone | Methylprednisolone
48
These drugs are Antagonists of the NK1 receptors for substance P • Indicated for prophylaxis against delayed CINV cause by moderate to highly emetogenic drugs • Given orally in combination with dexamethasone and 5HT3 receptor antagonist
* Aprepitant | * Parenteral formulation: Fosaprepitant
49
___________ undergoes extensive CYP3A4 metabolism and may affect the metabolism of warfarin and oral contraceptives
Aprepitant
50
These drugs * Do not have intrinsic antiemetic effects * Useful adjuncts due to sedative, amnesic, and anti-anxiety effects which reduce the anticipatory component of nausea and vomiting * Facilitate GABAA action in the CNS by increasing the frequency of chloride channel opening
* Lorazepam * Alprazolam * Diazepam
51
Adverse effects of benzodiazepines
CNS depression and dependence
52
Adverse effects of cannabinoids
- Palpitations - Hypotension - Tachycardia - Conjunctival injection (bloodshot eyes) - Vasodilation * Paranoid reactions and thinking abnormalities * Abrupt withdrawal of dronabinol, abstinence syndrome

DERS Pharm (9 decks)

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