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GI block > Pharm > Flashcards

Pharm Flashcards

1
Q

What are the sympathetic receptors in the GI responsible for relaxation of walls and contraction of Sphincters?

A

alpha 2 and Beta 2–> relax
Alpha 1–> contract

PSNS–> ALL m3 receptors

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2
Q

What are AE of muscarinic Agonists or AchE inhibitors?

A 
Diarrhea
Urination 
Miosis
Bronchorrhea
Bradycardia
Emesis
Lacrimation 
Salivation/ Sweating
**DUMBBELS
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3
Q

Which GI Neurotransmitter is the primarily excitatory transmitter of smooth muscle and glands. Major neuron-neuron (Ganglionic) transmitter in the ENS?

A

ACh

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4
Q

GI neurotransmitter that is Modulatory in the ENS?

A

Dopamine (inhibits ACh release)

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5
Q

GI substance that inhibits ACh release and peristalsis. May stimulate secretions?

A

Enkephalins (OPIOID peptides)

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6
Q

GI substance that inhibits secretion of water and electrolytes by the gut. Causes long lasting vasoconstriction?

A

NPY

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7
Q

GI substance that in inhibitory at ENS, especially @ Sphincters?

A

NO -> think Achalasia

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8
Q

What are some of the implicated causes of IBS?

A 
Abnormal GI motor function (hypersen, autonomic dysfunction)
Serotonin disequilibrium (Diarrhea form-excess, C-Lack)
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9
Q

What is the difference between SNS and PSNS stimulated salivary secretions?

A 
PSNS= Copious but protein POOR
SNS= Sparse But Protein RICH
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10
Q

Describe the pathway leading to salivary secretion by ACh stimulation?

A

ACh-> M3 (g-protein)-> IP3-> Ca+-> Increased Cl- discharge + H2O follows

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11
Q

What is the MOA of Cevimeline?

A

M3»M1 Agonist used to increase Salivary Flow

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12
Q

What is the MOA of Pilocarpine?

A

Muscarinic receptor Agonist== Increases Salivary flow

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13
Q

What are the AE of Cevimeline?

A

CI: Asthma, Glaucoma, iritis
Caution: COPD, driving (vision loss), MI, pregnancy, and nephrolythiasis

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14
Q

What are the AE of Pilocarpine?

A

CI: asthma, Glaucoma, iritis
Caution: Psychosis, CNS, MI, COPD, vision loss

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15
Q

Free radical scavenger that is protects the salivary glands during Head and neck radiation?

A

Amifostine–> Also protects from CISPLATIN nephrotoxicity

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16
Q

Caused by altered mucosal resistance and associated with reduced gastric acid output?

A

Gastric ulcer

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17
Q

Associated with High gastric output, and inadequate bicarbonate secretion and insufficient acid neutralization?

A

Duodenal ulcer

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18
Q

What is the goal of antacid?

A

Neutralize the gastric acid:

  1. 3-1.6= 50% neutralized
  2. 3-2.4= 90%
    * **pH > 4 == prevent Activation of Pepsin
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19
Q

What ingredient in antacid causes diarrhea? Constipation?

A 
Diarrhea= Aluminum Hydroxide 
Constipation= Magnesium
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20
Q

What is simethicon?

A

Surfactant

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21
Q

What is Mg+/ Al used for?

A

Antacids

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22
Q

MOA of calcium carbonate?

A

TUMS –> Antacid that is FAST ACTING

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23
Q

What are AE of antacids?

A

Affects absorption of other Drugs (avoid within 1-2hrs of taking other drugs)
Take 1-3 hrs after meals or @ bedtime

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24
Q

WHat is the MOA of Cimetidine, Famotidine, or any Tidines?

A

H2 receptor blockers

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25
Q

What is the affect of Cimetidine or any other H2 blocker?

A

Inhibit basal, food stimulated, and nocturnal Gastric acid secretion
**reduce BOTH volume and concentration

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26
Q

Which H2 blocker inhibits the activity of CYPs and thus slows down the metabolism of other drugs?

A

Cimetidine

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27
Q

MOA of Omeprazole, Pantoprazole, Lansoprazole?

A

PPI–> Inhibit the H+/K+ ATPase= Inhibit HCL secretion

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28
Q

What drugs are enterically coated so the Pro-drug is released in the intestines, absorbed in the blood stream. and carried to parietal cells where it has its affects?

A

PPI

**Low pH near the parietal cells Protonate the drugs and TRAP them near the Proton pumps

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29
Q

What is the MOA of protonated omeprazole, or other azoles?

A

Permits IRREVERSIBLE binding to H/K ATPase

**Results in Achlorhydria

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30
Q

What is the only way to reverse the affects of Omeprazole and other PPIs?

A

In order to return to normal acid secretion, Parietal cells must synthesize NEW H/K ATPase

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31
Q

Which PPI not a major substrate for CYP metabolism?

A

Rabeprazole-> Lower extent metabolism by CYPs

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32
Q

MOA for Bismuth subsalicylate?

A 
Pepo Bismol -->
1 Enhances secretion of mucus and HCO3
2 Inhibits pepsin activity 
3. Chelates with proteins at ulcer and forms protective barrier against acid and pepsin 
4. Inhibits H pylori 
5. effective against Travelers diarrhea
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33
Q

What drug is affective against both Travelers diarrhea and H pylori?

A

Bismuth (Pepo bismol)

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34
Q

MOA for Sucralfate?

A

Forms sticky, viscous gel –> protects gastric epithelial cells from acid and pepsin

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35
Q

What is the only cytoprotective agent that requires an ACID pH for maximal activity?

A

Sucralfate

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36
Q

What gastric protective agent is used in bedridden patients and why?

A

H2 or PPI induced pneumonia= Alkalinizing the stomach for protection would cause Pathogenic bacterial growth == Give SUCRALFATE which works in acid conditions and protects stomach

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37
Q

MOA for Misoprostol?

A

PGE1 analog

***Stimulates Mucus and HCO3 production

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38
Q

What are the AE of Misoprostol?

A

Intolerable DIARRHEA

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39
Q

When would Misoprostol be used?

A

Chronic NSAID users–> protect gastric mucosa from NSAID induced ulcers

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40
Q

What is the treatment for H pylori induced PUD?

A

H2 blocker
Bismuth
1-2 antibiotics

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41
Q

Which of the antibiotics used to treat H pylori have the highest resistance rate?

A

Metronidazole (40%)

Tetracycline (<1%)

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42
Q

What are the postural and dietary therapies for GERD?

A 
Smaller meals
Weight loss
Elevate Bed
Low Fat diet
Avoid coffee or peppermint (relax LES)
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43
Q

MOA for metoclopramide?

A

Prokinetic drug–> Dopamine receptor blockers (D2) increasing local release of ACh via 5HT4-R agonism== Enhances Gastric emptying

**D2R blocker + 5-HT4R Agonist

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44
Q

Drugs that stimulate GI smooth muscle, increase amplitude of esophageal contractions, Accelerates gastric emptying, and Increases LES pressure?

A

Meochlopramide + Domperidone

**D2 receptor blockers

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45
Q

What is the MAIN anti-reflux mechanism of Metochlopramide?

A

Enhanced Gastric motility

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46
Q

What are the AE of Metochlopramide?

A

Tardive dyskinesia

Parkinson’s like movements

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47
Q

What drug Enhances ACh release by acting on 5-HT4R?

A

Metochlopramide (also blocks D2R)

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48
Q

What is the MOA for Domperidone?

A

D2R blocker

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49
Q

What is the MOA for Sulfasalazine?

A

5-ASA = local anti-inflammatory agent

**Used in IBD

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50
Q

What are the AE for Sulfasalazine?

A

Anemia
Rash
Impotence

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51
Q

MOA for Inflizimab?

A

mab that inhibits/binds TNF alpha

**Given IV to Crohns disease patients

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52
Q

MOA for lactulose?

A

semisynthetic disaccharides + metabolized by enteric bacteria + Acidifies Feces –> traps and eliminates NH3

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53
Q

MOA of Increased fiber intake treatment for constipation?

A

Increases H2O delivery to colon
Increases Bulk
Decreases pressure in sigmoid colon
**More formed stool (also for diarrhea)

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54
Q

What is MOA for Effer-syllium/ Metamucil?

A

Metamucil–> Hydrophilic muciloid that forms gelatinous mass when mixed with water

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55
Q

AE of Effer syllium?

A 
Allergic rxn
Flatulance
Intestinal obstruction 
Borborygmi (stomach rumbles)
INHIBIT coumarin absorption
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56
Q

Hydrophilic muciliod producing substance used to relieve constipation?

A

Syllium / Metamucil

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57
Q

MOA of Mitrolan?

A

Hydrophilic resin that absorbs 60-100x water in weight

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58
Q

AE of Mitrolan?

A

Release Calcium–> CI with tetracylcine use

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59
Q

What is the MOA for all Docusates (dioctyl sodium)?

A

Anionic surfactant, STOOL softener. No affect on peristalsis

60
Q

What are the AE of Docusates laxatives?

A

Irritate intestinal mucosa
increase intestinal absorption of other drugs
Short term use

61
Q

MOA of Caster Oil?

A

RAPID acting anionic surfactant that produces Catharsis.

**COMPLETE evacuation of bowels by stimulating peristalsis

62
Q

What drug can Rapidly and completely empty bowel by stimulating intestinal peristalsis?

A

Caster Oil

63
Q

What are the AE of Caster oil?

A

Colic
Dehydration
Electrolyte imbalance
INDUCE UTERINE CONTRACTIONS in pregnants

64
Q

What laxative can induce labor in pregnant women (CI in pregnancy)?

A

Caster Oil

65
Q

What is the MOA of the stimulant laxatives?

A
  1. Increase permeability of intestinal mucosa
  2. Increase back diffusion of H2O and electrolytes
  3. Increase propulsive contractility of Colon by stimulating MYenteric plexus
  4. Stimulate Prostaglandin synthesis and Increase intestinal secretions
    * * MOSTLY ACTS IN COLON
66
Q

What are the most potent laxatives that act in the colon?

A

stimulant laxatives

67
Q

What is the MOA for Bisacodyl (Diphenmethanes)?

A

Stimulant laxative–> Pro-drug converted by Enteric bacterial into Desacetyl active form
** stimulates diffusion, contractility, prostaglandin production all in COLON

68
Q

What is pro-drug stimulant laxative that is converted by enteric bacteria?

69
Q

What is the MOA for Senokot (anthraquinones)?

A

NATURAL derivatives of Lilliaceae plants (Senna)

  • *More gentle than synthetic drugs
  • *Promote Colonic motility
70
Q

What naturally occuring substance is used to promote Colonic motility?

71
Q

WHat is the AE of Senna?

A

Abdominal pain
nephritis
Melanotic pigmentation of colonic mucosa
Abnormal urine coloration

72
Q

What laxative causes Dark stool, urine, and discolors colon?

73
Q

What are saline laxatives?

A

Contain Magnesium cations or other nonabsorbable molecules which cause Osmotic affects

74
Q

Why is Magnesium used as a laxative?

A

It is both NON absorbable and Osmotically active

75
Q

What is the MOA of Mg containing laxatives?

A

Osmotic effect

Release CCK–> increases Intestinal secretions and motility

76
Q

What laxatives are given via Enema?

A

Buffered Phosphates

77
Q

Laxative that can be used to acidify stool and trap ammonium ions?

78
Q

What is the MOA for glycerine suppositories?

A

Osmotic diarrhea

Lubricant

79
Q

MOA for mineral oil use in GI distress?

A

Hydrocarbons soften stool

80
Q

MOA for caster oil?

A

Irritates mucosa and produces a cathartic effect

81
Q

What two drugs have been approved for the treatment of IBS?

A

Lubiprostone–> Targets Cl- channel

Linaclotide–> tagets GC system

82
Q

What is MOA for Lubiprostone?

A

DIrectly Activates Cl- channels = increases secretion + motility and alleviates constipation

83
Q

What is MOA for Linaclotide?

A

Indirectly activates Cl- channels by acting on G protein receptors to Upregulate cGMP–> cAMP

84
Q

What antidiarrheal agent is also effective against Travelers diarrhea and H pylori?

A

Bismuth (pepto biismol)

85
Q

Agents that Adsorb harmful bacterial, viruses, toxin?

A

Bismuth

Charcoal

86
Q

What are the Actions of Opiates?

A

Decrease salivary, gastric, intestinal secretion
Decrease Gastric and intestinal motility
Increase Muscle tone (SPHINCTERS)
Anti-spasmodics + decrease Cramps
SUM effect= increase COntact time between ingested material and reabsorptive epithelium

87
Q

What drugs can cause contraction of illeocecal sphincter?

A

Opiates (enkaphalins)

88
Q

What is the MOA of Paregoric?

A

Opiate antidiarrheal agent–> contracts sphincters and slows motility and inhibits all secretions

89
Q

What is the MOA of Diphenoxylate + Atropine?

A

Diphenoxylate== Opiate antidiarrheal agent

**Atropine prevents ABUSE

90
Q

What is the purpose of adding Atropine to an Opiate anti diarrheal agent?

A

Prevent ABUSE due to Atropine AE

91
Q

What is the MOA for Loperamide?

A

Interacts with intestinal Opioid receptors and binds and inhibits Ca+ binding protein Calmodulin

92
Q

What antidiarrheal agent inhibits Calmodulin but is a opioid agonist?

A

Loperamide

93
Q

Where is the Emitic center located?

94
Q

What anticholinergic drug can be used to manage motion sickness?

A

Scopolamine

95
Q

What is the MOA for Scopolamine?

A

Anticholinergic that blocks activation of Muscarinic receptors by ACh from Cochlear sensations

96
Q

What are the AE of Scopolamine?

A

Sedation
Drowsiness
Dry mouth

97
Q

What are the MOA for anticholinergics as antidiarrheal agents?

A

Reduce vagal stimulation== Anti Spasmodics

98
Q

What drug is a Quaternary ammonium derivative of Atropine?

A

Prpanetheline–> alleviate CRAMPS

Dicyclomine–> Tx urinary retention

99
Q

Dimenhydrinate MOA?

A 
Anti histamine (H1) + anticholinergic 
**Prophylactic for Motion sickness
100
Q

What is the MOA for Cyclizine & Meclizine?

A

BOTH Anti histamines (H1)
cyc–> OTC for MS
mec–> depresses the Labyrinthine function= Tx vestibular disturbances

101
Q

What antihistamine can also be used to treat Vertigo and menier disease?

102
Q

What is the MOA for Promethazine?

A

Antihistamine and anticholinergic

**Tx: nausea and vomiting

103
Q

What is the AE of Promethazine?

104
Q

What types of receptors are on the Chemoreceptor Trigger zone in BBB that acts on the VC in medulla?

105
Q

What is the MOA for Chlorpromazine?

A

Centrally acting anticholinergic + antidopa

106
Q

What drug can be used to treat N&V and intractable hiccoughs?

A

Chlorpromazine

107
Q

What is the MOA for Theithylperazine?

A

Antidopaminergic that inhibits CTZ and VC

108
Q

What drug blocks Dopa 2 receptors in the CTZ and is clinically used for N&V postoperatively?

A

Droperidol

109
Q

What drug inhibits Dopamine receptors in CTZ and stimulates gastric emptying?

A

Metochlopramide

110
Q

What is the MOA for Trimethobenzamide?

A 
Dopa inhibitor (CTZ and stomach)
**AE are extrapyramidal= Short term use only
111
Q

What is the MOA for Serotonin antagonists in antiemesis?

A

Block 5HT3 in stomach + SI

  • Prevent transmission of stimuli through Vagus to CTZ and VC
  • BLOCK 5HT3 receptors @ CTZ
  • *MOST effective antiemetics
112
Q

What is the MOA of Ondasetron or Granisetron or Dolasetron?

A

ALL 5HT3 (serotonin receptor) Blockers

113
Q

What is difference between the Setrones?

A 
Ondasetron= selective, used for Antiemesis during chemo (IV) 
Dranisetron= More potent and ORAL 
Dolasetron= Long half life
114
Q

What is the MOA for Delta 9 tetrahedro cannabinol?

A

Activates CB1 cannabinoid receptors (Marijuana)

**Antiemetic

115
Q

What is the MOA of Dexamethazone as an antiemetic?

A

Prevents the production of Prostaglandin associated with CHEMO or radiation therapy

116
Q

Substance P/ neurokinin 1 (NK1) receptor antagonist?

A

Aprepitant–> Crosses BBB and inhibits emesis via CENTRAL actions

117
Q

Drug used to prevent emesis induced by cytotoxic chemo by crossing BBB and inhibiting central action?

A

Aprepitant

**Substrate for CYP3A4

118
Q

What drug is used in adjunct with other anti-emetics in patients with Anticipatory vomiting?

119
Q

What drug causes Amnesia and semnolence lasting for hours?

120
Q

What drug is preferred in HIV/ HBV coinfection?

A

Emtricitabine

Tenofovir

121
Q

What drugs are used in the treatment of HBV?

A 
Tenofovir 
Entecavir 
Telbivudine
Adifovir
Lamivudine 
Emtricitabine
122
Q

What drugs are used in the treatment of HCV?

A

Ribavirin
Tealprevir
Boceprevir
Peginteferon alpha-2b

123
Q

What drug is used in the treatment of BOTH HBV & HCV?

A

Peginterferon alpha-2a

interferon alpha 2b

124
Q

What is the mechanism of drug resistance against the Nucleoside/tide structural analogs in the treatment of HBV?

A

Structural changes in SUGAR RESIDUES
Arising from HBV DNA polymerase

L-nucleosides= Lamiv + Telbiv
Acyclic phosphonates= Adef + Tenof + Disoproxil
d-cyclopentane= Entecavir

125
Q

What is MOA for Adefovir?

A

Diphosphate incorporated in viral DNA producing chain termination –> Adenosine analog

126
Q

What is the MOA for Tenofovir?

A

Prodrug nucleotide analog of adenosine

127
Q

What is the MOA for Entecavir?

A

Guanosine analog triphosphate that inhibits DNA polymerase

128
Q

What is the MOA for Telbivudine?

A

L-isomer of Thymidine triphosphate inhibiting DNA polymerase and produces chain termination

129
Q

What do all the anti HBV drugs have in common?

A

NO CYP interactions

Competitive RENAL excretion

130
Q

What HBV drug should be taken with HIGH fat meals? Which one should not be taken with food?

A

Tenofovir + Ribavirin

Entecavir= Food delays absorption

131
Q

What are the AE of Tenofovir?

A

Nephrotoxic
BONE pain
BONE fractures

132
Q

Which anti HBV drug should be given with supplements of Vit D/ Calcium?

A

Tenofovir–> causes bone pain/fractures

133
Q

What is the mechanism of Tenofovirs Nephrotoxicity?

A

accumulation causing Mitochondrial toxicity

134
Q

causes osteoporotic fractures?

135
Q

Which HBV drugs cause Hepatotoxicity by way of Inhibiting mtDNA synthesis?

A

Adefovir
Telbivudine
Entecavir

136
Q

AE is lactic acidosis and steatosis?

A

Nucleotide analogs
Adefovir
Telbinvudine
Entecavir

137
Q

Biological effects including Antiviral, antiproliferative, and immunomodulatory?

A

Interferons

138
Q

What is the MOA of interferons?

A 
Bind cell surface receptors
Activate TK--> produce IFN enzymes 
Endoribonucleases to cleave ss viral RNA
Inhibit dsRNA
inhibit penetration and uncoating 
Inhibit assembly and release
Enhance lytic effects of CD8 T cells
139
Q

Associated with Acute influenza like syndrome following injections?

A

Interferons

140
Q

What are the AE of interferons?

A 
Depression 
Seomnolence/ confusion 
Myelosuppression (Neutropenia + thrombocyto)
Hepatotoxic 
Thyrotoxic 
Decreased serum antibodies
141
Q

May produce immune mediated destruction of thyroid and cause thyrotoxicosis?

A

Interferons

142
Q

What are the 4 actions of Ribavirin?

A
  1. Immune clearance= enhance T cells
  2. inhibit iMPHD= deplete guanosine needed for viral RNA synthesis
  3. Inhibit HCV RdRp= inhibit HCV replication
  4. RNA mutations= Create errors in HCV causing death of virus
143
Q

AE is Hemolytic anemia, non fatal MI, male teratogenecity?

144
Q

WHat are the NS3/4A protease inhibitors?

A

Telaprevir

Boceprevir

145
Q

WHat are the AE of the NS3/4A protease inhibitors?

A

Fatigue + Anemia + Nausea

Telaprevir=== serious RASH

146
Q

HCV patients presents with pruritis and a rash?

A

Telaprevir Tx

147
Q

What is unique about the metabolism of the protease inhibitors?

A

BOTH undergo Hepatic metabolism
Tela-> CYP3A4/ P-gp substrate & inhibitor
Inhibits OATP1B1
Boce-> Substrate for CYP3A4/5 P-gp

GI block (6 decks)

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