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DEMS Unit 1 > Pharmacology > Flashcards

Pharmacology Flashcards

(42 cards)

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1
Q

PPIs - Mechanism

A

Covalently bind to and irreversibly inactivate H/K/ATPase

Results in a 80-95% reduction in daily acid production; may take 2-5 days to reach steady state inhibition

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2
Q

PPIs - Pharmacokinetics

A

Systemic absorption is improved by administration as enteric-coated capsules or with sodium bicarbonate

Administered on empty stomach 1 hour before meals so that peak plasma concentration occurs with maximal proton pump secretion

Metabolized by CYP450 in the liver; dosage reduction necessary in liver disease

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3
Q

PPIs - Clinical Uses

A

GERD - First line therapy

Peptic Ulcer Disease - H.pylori and NSAID-induced; for symptomatic relief and ulcer healing

Prevention of stress gastritis

Zollinger-Ellison syndrome

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4
Q

PPIs - Adverse Effects

A

Headache, abdominal pain, nausea, constipation/diarrhea

Hypergastrinemia resulting from chronic PPI use may cause rebound gastric acidity upon discontinuation

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5
Q

Omeprazole - DDIs

A

Inhibits conversion of Clopidogrel to active form leading to a hypercoagulable state

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6
Q

H2 receptor antagonists - Agents

A

Ranitidine
Cimetidine
Famotidine
Nizatidine

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7
Q

H2 receptor antagaonists - Mechanism

A

Reversible, competitive block at parietal H2 receptors on the basolateral membrane; normally, histamine binding to H2 receptors activates Gs, increasing intracellular cAMP and leading to phosphorylation of the H/K/ATPase, which activates it

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8
Q

H2 receptor antagonists vs. PPIs

A

Somewhat less effective than PPIs but still suppress 24 hour acid secretion by 70%

Better at blocking nocturnal acid secretion (90%) than meal-stimulated acid secretion (60-80%)

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9
Q

H2 receptor antagonists - Pharmacokinetics

A

Rapidly absorbed from GI tract; some enhancement with food, decreased with antacids

No dosage adjustment necessary for liver disease; dosage reduction IS required in renal dysfunction, especially in the elderly

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10
Q

H2 antagonists - Clinical Uses

A

GERD - OTC treatment for infrequent heartburn; PPIs preferred in severe disease

PUD - Useful for suppressing nocturnal acid secretion; PPIs preferred for more severe disease

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11
Q

H2 antagonists - Adverse Effects

A

Dizziness, diarrhea, constipation, headache

Rarely CNS dysfunction / mental status changes more commonly seen with Cimetidine in the elderly

Gynecomastia, galactorrhea, decreased sperm count - with high doses of Cimetidine

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12
Q

Sucralfate - Mechanism

A

Disaccharide aluminum salt; selectively binds to necrotic ulcer tissue to form a protective barrier which prevents pepsin from hydrolyzing mucosal proteins causing further erosion/ulceration

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13
Q

Sucralfate - Pharmacokinetics

A

Activated by pH < 4 - efficacy decreased by administration with antacids; best on empty stomach 1 hour before meals

No systemic absorption; administered 2-4x/day

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14
Q

Misoprostol - Mechanism

A

Prostaglandin (PGE1) analog - inhibits cAMP formation in gastric parietal cells, decreasing H+ secretion and stimulating bicarbonate and mucous secretion

Administered orally 3-4x/day

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15
Q

Misoprostol - Uses and Adverse Effects

A

Alleviation of NSAID-induced GI ulceration

Side effects: Diarrhea, uterine cramping (contraindicated during pregnancy)

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16
Q

Ca2+ Antacids - Adverse Effects

A

Constipation

With long-term use: hypercalcemia, renal calculi, rebound acid secretion

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17
Q

Antacids - DDIs

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A

Decreased absorption of: tetracycline, fluoroquinolones, digoxin, chlorpromazine

Increased excretion of aspirin due to alkalinization of urine

Reduced bioavailability of H2 antagonists and Ketoconazole due to increased gastric pH

18
Q

Al3+ Antacids - Adverse Effects

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A

Constipation

With long-term use: CNS toxicity / Encephalopathy

19
Q

Mg2+ Antacids - Adverse Effects

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A

Diarrhea

Avoid use in renal failure as Mg2+ can occur

20
Q

Sodium Bicarbonate Antacids - Adverse Effects

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A

Contraindicated for prolonged use due to systemic effects

Na overload and alkalosis can occur; contraindicated in conditions exacerbated by fluid overload (pregnancy, CHF, HTN, edema, renal failure)

21
Q

General mechanism of prokinetic agents

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A

All promotility drugs directly or indirectly increase ACh agonist activity at smooth muscle M3 receptors

22
Q

Erythromycin

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A

Pro-motility agent

Agonist at excitatory smooth muscle motilin receptors

23
Q

Cisapride - Uses, mechanism, and adverse effects

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A

Pro-motility agent

Agonist at excitatory neural 5-HT4 receptors on enteric nervous system cholinergic motor neurons; directly increases ACh release in the gut, stimulating motility

Adverse effects: QT prolongation / arrhythmia

24
Q

Metoclopramide - Uses, mechanism, adverse effects

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A

Antagonist at pre-synaptic dopamine (D2) receptors which normally inhibit release of ACh; indirectly increases ACh release in the gut

Anti-dopaminergic effect also relieves nausea and vomiting by blocking DA receptors in chemoreceptor trigger zone

Adverse effects: Somnolence, dystonia, tardive dyskinesia

25
Bethanechol - Uses and Mechanism
Pro-motility agent Direct agonist at excitatory M3 smooth muscle receptors in the gut
26
Ondansetron - Mechanism & Adverse Effects
Blocks 5HT3 receptors at the chemoreceptor trigger zone, solitary tract nucleus, and on visceral afferents Headache, constipation, drowsiness QT prolonation
27
Metoclopramide - Mechanism and Adverse Effects
Blockade of DA receptors in chemotrigger zone causes anti-emetic effect Movement disorders / EPS, fatigue/drowsiness, diarrhea
28
Antihistamines - Agents & Mechanism
Promethazine Dimenhydrinate Doxylamine First generation anti-histamines with good CNS penetration; used for motion sickness, post-operative emesis
29
Scopolamine - Mechanism and Uses
Anticholinergic; may be administered transdermally to prevent motion sickness and post-op nausea
30
Dronabinol - Mechanism, Uses, and Adverse Effects
Stimulation of CB1 cannabinoid receptors; used to prevent nausea in cancer chemotherapy Can cause central sympathomimetic actions (tachycardia, palpitations, vasodilation with hypotension) as well as euphoria (Schedule III)
31
Substance P receptor antagonists
Blocks action of SP at the neurokinin 1 (NK1) receptor to interrupt vagal afferents carrying sensory information to the solitary tract nucleus Specifically used for delayed emesis associated with Cisplatin therapy
32
Psillyum
1st line therapy in the treatment of constipation Fiber/bulk forming laxative; approximates physiological mechanisms - absorption of water with subsequent bulk expansion stimulates peristalsis
33
Milk of Magnesia
Most commonly used for mild-moderate constipation (second-line); avoid in renal dysfunction as long-term use can lead to electrolyte imbalance Lactulose - Dissacharide metabolized by colonic bacteria to LMW acids; causes osmotic diarrhea and increased colonic peristalsis
34
Lactulose
Osmotic agent for treatment of constipation; second line Disaccharide metabolized by colonic bacteria to LMW acids; causes osmotic diarrhea and increased colonic peristalsis
35
Polyethylene Glycol Electrolyte Solutions (PEGs)
High volume solutions used for bowel prep prior to radiologic, surgical, or endoscopic procedures Low volume solutions may be given as a daily dose for the treatment of refractory constipation on a short-term basis, < 2 weeks
36
Bisacodyl
Stimulant agent for the treatment of constipation; 3rd line Induces low grade inflammation in the bowel to promote accumulation of water with stimulation of intestinal motility Side effects: Electrolyte/fluid imbalances, severe cramping
37
Docusate
Stool wetting agent / stool softener; facilitates admixture of aqueous and fatty substances Used for prevention of constipation when initiating chronic analgesic therapy; may be combined with stimulant agent
38
Loperamide - Mechanism, Uses, Side effects
Mu opioid agonist; decreases gut motility Most often used for traveler's diarrhea Side effects: CNS depression, paralytic ileus
39
Polycarbophil - Mechanism and Uses
Binds free fecal water (60x its weight!) Useful in both diarrhea (absorption of excess water) and in constipation (prevention of fecal desiccation)
40
Adsorbent Agents (Pepto Bismol, Kaopectate)
Promotes formed stools and perception of decreased fluidity of stools; small overall effect on actual volume excreted Avoid use of bismuth subsalicylate in Children < 12 due to risk of Reye's syndrome
41
Alosetron
5HT3 Antagonist - reduces pain and inhibits colonic motility Clinical use restricted to treatment of severe IBS in women with diarrhea as the prominent symptom Adverse effects: Constipation, ischemic colitis
42
Tegaserod
5-HT4 agonist - promotes gastric emptying and intestinal motility Use restricted to women < 55 with IBS with predominant constipation, or chronic idiopathic constipation refractory to other treatments

DEMS Unit 1 (1 decks)

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