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x M2T4 Pharm (GI, CT/MSK) > GI Drugs > Flashcards

GI Drugs Flashcards

1
Q

Oral Rehydration Therapy:

Class?

Mech of Action?

Indications (1)?

ADRs?

Interactions?

A

ORT

Anti-diarrheal

Glucose promotes Na/Cl uptake by enterocytes, water follows in the same direction.

Indication: Significant diarrhea

No ADRs, no interactions

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2
Q

Metamucil:

Class?

Mech of Action?

Indications (1)?

ADRs?

Interactions?

A

Metamucil

Class: anti-diarrheal

Mech unknown!

Indication - diarrhea

No ADRs

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3
Q

Loperamide (Immodium)

Class?

Mech of Action?

Indications (1)?

ADRs?

Interactions?

A

Loperamide

Opioid

Mech: 50% more potent than morphine, limited ability to enter CNS

Indication: diarrhea

No ADRs

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4
Q

Laxatives: Luminally active agents

Mech of Action?

Indications (1)?

ADRs?

Interactions?

A

Laxatives: Luminally active

MoA: Hydrophilic colliods, osmotic agents, stool wetting agents

Indication: constipation

No ADRs

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5
Q

Laxatives: Stimulants or Irritants

Mech of Action?

Indications (1)?

ADRs?

Interactions?

A

Laxatives: Stimulants/irritants

MoA: Induce a low-grade inflammation in intestines –> promotes accumulation of water in intestines and stimulates intestinal motility

Indication: constipation

No ADRs!

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6
Q

Laxatives: Prokinetics

Mech of Action?

Indications (1)?

ADRs?

Interactions?

A

Prokinetics

Mech: 5HT4-R agonist, Dopamine-R antagonist, Motilides

Indication: constipation

No ADR!

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7
Q

Antacids

Class?

Mech of Action?

Indications (2)?

ADRs (for MgOH, AlOH, and CaCO3 separately)?

Interactions?

A

Class: MgOH, AlOH, CaCO3

MoA: neutralized secreted acids (does not change secretion) –> incr pH –> inactivate pepsin

Indication: relief from pyrosis, gastric acid regulation

ADRs: ∆ bowel habits

  • MgOH –> laxative properties; bowel purging
  • AlOH –> constipation; sequesters drugs and phosphate
  • CaCO3 –> incr Ca, –> cholinergic activity to release gastrin
  • Overall: systemic absorption of cations
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8
Q

Cimetidine

Class?

Mech of Action?

Indications (3)?

ADRs (3)?

Interactions?

A

Cimetidine

H2-receptor antagonist

Gastric Acid regulation

MoA: blocks stimulus to parietal cells

Indications: Duodenal ulcers; Uncomplicated GERD; Prevent nocturnal acid release to allow healing.

ADRs: Causes the most side effects via inhibition of CP450 enzymes; gyncomastia; mental confusion

Interaction: CP450 enzymes. Results in reduced clearance, increased concentration of P450 substrates

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9
Q

Cimetidine: when is best time of day to give med?

A

Effective when given between evening meal and bedtime: can prevent nocturnal acid release to promote healing

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10
Q

Rantidine

Class?

Mech of Action?

Indications (3)?

ADRs?

Interactions?

A

H2-receptor antagonist

MoA: Blocks stimulus to parietal cells

Indications (same as Cimetidine): Duodenal ulcers, Uncomplicated GERD, Prevent nocturnal acid release to promote healing

ADRs: Does not interefere with P450 activity

Interactions: Less potent androgenic effects compared to Cimetidine

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11
Q

Famotidine

Class?

Mech of Action?

Indications (3)?

ADRs?

Interactions?

A

H2-receptor antagonist

MoA: Blocks stimulus to parietal cells

Indications (same as Cimetidine): Duodenal ulcers, Uncomplicated GERD, Prevent nocturnal acid release to promote healing

ADRs: Does not interefere with P450 activity;

Interactions: Less potent androgenic effects compared to Cimetidine

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12
Q

Nizafidine

Class?

Mech of Action?

Indications (3)?

ADRs?

Interactions?

A

H2-receptor antagonist

MoA: Blocks stimulus to parietal cells

Indications (same as Cimetidine): Duodenal ulcers, Uncomplicated GERD, Prevent nocturnal acid release to promote healing

ADRs: Does not interefere with P450 activity;

Interactions: Less potent androgenic effects compared to Cimetidine

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13
Q

Omeprazole

Class?

Mech of Action?

Indications?

ADRs (4)?

Interactions (2)?

A

Omeprazole

PPI

MoA: PROdrug, metabolite binds irreversibly to H/K ATPase

Indication: GERD

ADRs: Do not give to pts with cirrhosis or hepatic insuff due to decreased elimination; can increase luminal pH and cause decr absorption of other drugs + incr risk of gut infections; Headache; Diarrhea

Interactions: Co-admin with H2 blockers can decr effectiveness of PPI; PPIs inhibit some P450 enzymes resulting in decr clearance.

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14
Q

Sucralfate

Class?

Mech of Action?

Indications (1)?

ADRs?

Interactions?

A

Gastric Acid Regulation: Sulfated Disaccharides

MoA: binds to damaged mucosal cells, protects them from pepsin and acid (LOCAL effect)

Indication: gastric acid regulation

No ADRs

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15
Q

Misoprostol

Class?

Mech of Action?

Indications (1)?

ADRs?

Interactions?

A

Gastric Acid Regulation: PGE2 analog

MoA: enhances mucosal protction by decr gastric acid secretion

Indication: prevent NSAID-induced ulcers

No ARDs

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16
Q

Name 5 different prokinetics and what class of Rx they are

A

Neostigmine - cholinergic

Bethanechol - cholinergic

Domperidone - dopamine antagonist

Metoclopramide - serotonin agonist AND dopamine antagonist

erythromycin - macrolide

17
Q

How do cholinergics work to modulate GI bowel motility?

What are 2 examples?

How do they work?

What are they largely used for?

What drug has replaced this class of drugs?

A

prokinetics - increases luminal transport via increasing SM contractions

Examples: Neostigmine and** **Bethanechol

  • causes increased ACh availability in the synaptic cleft –> SM contraction
  • indications: ileus

note: this has been largely replaced by metoclopramide

18
Q

What is Domperidone used as?

What is its mechanism of action?

What is it indicate for?

How does this different than Metoclopramide?

A

Prokinetic

**dopamine antagonist - “it inhibits the inhibition” - **blocks D2 receptors -> decreased inhibition of cholinergic fibers -> increased ACh release -> contractions

Indications: GI dysmotility and anti-emesis

Compared to Metoclopramide: Domperidone does NOT cross the BBB and won’t cause extrapyramidal effects

19
Q

What is Metoclopramide used as?

What is its mechanism of action?

What is it indicate for?

What are the side effects?

How does this different than Domperidone?

A

Prokinetic

serotonin AGONIST & dopamine ANTAGONIST

  • activation of serotinin receptors results in increased ACh release -> gastrointestinal contractions
  • inhibits D2 receptors “inhibiting the inhibition”: decreased inhibition of cholinergic fibers -> increased ACh release -> gastrointestinal contractions

Indications: Anti-emesis + GI dysmotility (ie post-surgical ileus)

Side effects *IMPT* Extrapyramidal effects (Parkinsonism)

20
Q

What is erythromycin used as?

What is its mechanism of action?

What is it indicate for?

What are the side effects?

How does this different than Domperidone?

A

Prokinetic

motilin analog - activates motilin receptor (MTLR) in the MMC -> enhanced upper GI motility with little or no effect in the colon!

Indications: Gastroparesis

Side effects: tolerance and antibiotic effects (affects GI flora)

21
Q

What 4 drugs are dopamine antagonists that act to block D2R in the Chemo-Trigger zone?

Which one is the best one to use for chemoRx or irridation-induced nausea? What is the downside of using this particular drug?

A
  • Metoclopramide* (also serotonin agonist) - best to use for ChemoRx/irradiation-induced nausea
    • increased extrapyramidal side effects
  • Phenthiazine
  • Domperidone
22
Q

What is Ondansetron used as?

What is its mechanism of action?

What is it indicate for?

What are the side effects?

How does this different than Metoclopramide?

A

Anti-emetic

Serotonin antagonist - Inhibits 5HT3-R on vagal neurons that innervate the GI -> blocks vagal afferent signal to the vomiting center the in brain -> decrease nausea and vomiting

indications: Chemo- or irradiation-induced nausea, but does NOT cause extrapyramidal symptoms like metoclopramide

ADR: NOT effective for motion sickness (use Diphenhydramine instead)

23
Q

What is Dronabinol used as?

What is its mechanism of action?

What is it indicate for?

What are the side effects?

A

Anti-emetics

  • Cannabinoid agonist - Binds cannabinoid receptors in the CNS
  • Indications: Prophylaxis for chemotherapy-induced nausea, AIDs anorexia/HIV wasting syndrome
  • ADR: High potential for abuse
24
Q

What is Diphenhydramine used as?

What is its mechanism of action?

What is it indicate for?

What are the side effects?

A

Anti-emetic

Histamine antagonist

Indications: Motion sickness (mild, moderate)

ADR: Not useful for treating chemotherapy-related nausea (use metoclopramide or ondasetron instead)

25
Q

What drugs should you use for motion sickness? (2.5)

Can these be used for chemotherapy-related nausea?

A
  • Diphenhydramine - Histamine antagonist
  • Scopolamine - Muscarinic antagonist
  • ginger..

CANNOT be used for chemotherapy-related nausea

26
Q

What is IBS and how is it treated?

What two drugs are given by certified providers that is taken off the market due to life-threatening ADRs?

A

Chronic or recurrent GI symptoms (lower abdominal pain) not explained by an organic abnormality

  • SSRI (Citalopram, Fluoxetine, Parosetine)
  • TCA (Amytriptylines)

​Drugs taken off the market due to severe ADR:

  • Alosteron **-causes ischemic**colitis, constipation, and death
  • Tegaserod - causes MI’s, unstable angina, strokes, and ischemic colitis
27
Q

What is IBD and what are some intestinal symptoms they cause?

extra-intestinal symptoms?

A
  • Chronic inflammatory intestinal conditions of unknown etiology; examples:
    • Ulcerative Colitis (Th2-mediated)
    • Crohn’s disease (Th1-mediated)
  • Sx: diarrhea, abd. pain, bleeding, anemia, wt loss, skin findings
  • Extra-intestinal Sx: ARTHRITIS, other d/o’s
28
Q

There are 5 drugs therapies for IBD.

What are they?

A
  • Sulfasalazine
  • Glucocorticoids: Prednisone, Budesonide
  • Azathioprine (6-mercaptopurine)
  • MTX
  • Infliximab (Remicade)
    • Adalimumab (Humira)
    • Certolizumab (Cimzia)
    • Natalizumab
29
Q

What is Sulfasalazine used for?

What is its mechanism of action?

A

IBD - Ulcerative colitis

MoA: PRO-drug that is cleaved at the diazo-linkage to mesalamine which acts in the colon (diazo linkage prevents absorption in the stomach or small intestines and allows release of drug in specific areas of the gut!!!)

30
Q

What are glucocorticoids used for in IBD?

Give an examples…

What some side effects as a result of chronic use?

A

Acute IBD Flare-ups

ex: Prednisone

Chronic use can result in systemic effects (Cushing, hypokalemia, etc)

31
Q

Budesonide is also a glucocorticoid indicated for IBD. Which one specifically?

How does it work?

What are the side effects?

A

Crohns

it is packaged into a capsule that dissolves only when it reaches the ileum, where the pH >5.5

Side effect: High first-pass effect in the liver, causing increased serum levels of with P450/3A4 inhibitors (erythromycin, ketoconazole, grapefruit juice)

Fewer ADRs than corticosteroids, BUT is slightly less effective and is more $$$$

32
Q

What is Azathioprine (6-mercaptopurine) used as?

What is its mechanism of action?

What is it indicate for?

What are the side effects?

A

Immune-modulator for IBD

MoA: PRO-drug + its metabolite mercaptopurine are **biologically active! **

indications: Long-term treatment of moderate-severe IBD (to maintain remission)

ADRs

  • Takes several weeks to produce effects, BUT ultimately reduces steroids required to maintain patients in remission
  • allergic reactions
  • nausea
  • hepatitis
  • Pancreatitis** (2% risk)
  • lymphoma (NHL = 0.04% risk)
  • Bone marrow depression (leukopenia)
  • Teratogen
33
Q

What is Methotrexate used as?

What is its mechanism of action?

What is it indicate for?

What are the side effects?

A

Immune-modulators for IBD - Crohns

MoA: Inhibit DHFR -> decreased DNA synthesis -> increased cell death, but role in anti-inflammatory mechanism is not well understood!

Indications: Short-term treatment for patients who are steroid-resistant or steroid-dependent

ADR:

  • Myelosuppression (reversible with leucovorin (folinic acid) rescue
  • nephrotoxicity
  • teratogenic
  • mucositis
  • microvesicular fatty change in liver
34
Q

What is Infliximab used as?

What is its mechanism of action?

What is it indicate for?

What are the side effects?

A

Anti-TNFa mAb

MoA: Induces formation of regulatory macrophages that inhibit proliferation of activated T cells and produces anti-inflammatory cytokines

Indications: IBD patients who are refractory to conventional therapies

ADR:

  • Potentially dangerous in patients with chronic infections, cancers, or immune deficiencies
  • Possible induction of neutralizing antibodies-> drug tolerance
  • Serious infections (3% risk)
  • Lymphoma (NHL = 0.06% risk)
  • Tuberculous
35
Q

Natalizumab was also an Anti-TNFa mAb. Why was it taken off the market?

A

not used anymore because it modulates the immune system systemically (receptors are present in the brain -> proliferation of JC virus -> PML)

x M2T4 Pharm (GI, CT/MSK) (6 decks)

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