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DEMS Unit 1 > Pharmacology > Flashcards

Pharmacology Flashcards

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

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

A

Constipation

With long-term use: CNS toxicity / Encephalopathy

19
Q

Mg2+ Antacids - Adverse Effects

A

Diarrhea

Avoid use in renal failure as Mg2+ can occur

20
Q

Sodium Bicarbonate Antacids - Adverse Effects

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

A

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

22
Q

Erythromycin

A

Pro-motility agent

Agonist at excitatory smooth muscle motilin receptors

23
Q

Cisapride - Uses, mechanism, and adverse effects

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

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
Q

Bethanechol - Uses and Mechanism

A

Pro-motility agent

Direct agonist at excitatory M3 smooth muscle receptors in the gut

26
Q

Ondansetron - Mechanism & Adverse Effects

A

Blocks 5HT3 receptors at the chemoreceptor trigger zone, solitary tract nucleus, and on visceral afferents

Headache, constipation, drowsiness
QT prolonation

27
Q

Metoclopramide - Mechanism and Adverse Effects

A

Blockade of DA receptors in chemotrigger zone causes anti-emetic effect

Movement disorders / EPS, fatigue/drowsiness, diarrhea

28
Q

Antihistamines - Agents & Mechanism

A

Promethazine
Dimenhydrinate
Doxylamine

First generation anti-histamines with good CNS penetration; used for motion sickness, post-operative emesis

29
Q

Scopolamine - Mechanism and Uses

A

Anticholinergic; may be administered transdermally to prevent motion sickness and post-op nausea

30
Q

Dronabinol - Mechanism, Uses, and Adverse Effects

A

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
Q

Substance P receptor antagonists

A

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
Q

Psillyum

A

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
Q

Milk of Magnesia

A

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
Q

Lactulose

A

Osmotic agent for treatment of constipation; second line

Disaccharide metabolized by colonic bacteria to LMW acids; causes osmotic diarrhea and increased colonic peristalsis

35
Q

Polyethylene Glycol Electrolyte Solutions (PEGs)

A

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
Q

Bisacodyl

A

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
Q

Docusate

A

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
Q

Loperamide - Mechanism, Uses, Side effects

A

Mu opioid agonist; decreases gut motility

Most often used for traveler’s diarrhea

Side effects: CNS depression, paralytic ileus

39
Q

Polycarbophil - Mechanism and Uses

A

Binds free fecal water (60x its weight!)

Useful in both diarrhea (absorption of excess water) and in constipation (prevention of fecal desiccation)

40
Q

Adsorbent Agents (Pepto Bismol, Kaopectate)

A

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
Q

Alosetron

A

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
Q

Tegaserod

A

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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