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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
What is the affect of Cimetidine or any other H2 blocker?
Inhibit basal, food stimulated, and nocturnal Gastric acid secretion **reduce BOTH volume and concentration
26
Which H2 blocker inhibits the activity of CYPs and thus slows down the metabolism of other drugs?
Cimetidine
27
MOA of Omeprazole, Pantoprazole, Lansoprazole?
PPI--> Inhibit the H+/K+ ATPase= Inhibit HCL secretion
28
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?
PPI | **Low pH near the parietal cells Protonate the drugs and TRAP them near the Proton pumps
29
What is the MOA of protonated omeprazole, or other azoles?
Permits IRREVERSIBLE binding to H/K ATPase | **Results in Achlorhydria
30
What is the only way to reverse the affects of Omeprazole and other PPIs?
In order to return to normal acid secretion, Parietal cells must synthesize NEW H/K ATPase
31
Which PPI not a major substrate for CYP metabolism?
Rabeprazole-> Lower extent metabolism by CYPs
32
MOA for Bismuth subsalicylate?
``` 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 ```
33
What drug is affective against both Travelers diarrhea and H pylori?
Bismuth (Pepo bismol)
34
MOA for Sucralfate?
Forms sticky, viscous gel --> protects gastric epithelial cells from acid and pepsin
35
What is the only cytoprotective agent that requires an ACID pH for maximal activity?
Sucralfate
36
What gastric protective agent is used in bedridden patients and why?
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
37
MOA for Misoprostol?
PGE1 analog | ***Stimulates Mucus and HCO3 production
38
What are the AE of Misoprostol?
Intolerable DIARRHEA
39
When would Misoprostol be used?
Chronic NSAID users--> protect gastric mucosa from NSAID induced ulcers
40
What is the treatment for H pylori induced PUD?
H2 blocker Bismuth 1-2 antibiotics
41
Which of the antibiotics used to treat H pylori have the highest resistance rate?
Metronidazole (40%) | Tetracycline (<1%)
42
What are the postural and dietary therapies for GERD?
``` Smaller meals Weight loss Elevate Bed Low Fat diet Avoid coffee or peppermint (relax LES) ```
43
MOA for metoclopramide?
Prokinetic drug--> Dopamine receptor blockers (D2) increasing local release of ACh via 5HT4-R agonism== Enhances Gastric emptying **D2R blocker + 5-HT4R Agonist
44
Drugs that stimulate GI smooth muscle, increase amplitude of esophageal contractions, Accelerates gastric emptying, and Increases LES pressure?
Meochlopramide + Domperidone **D2 receptor blockers
45
What is the MAIN anti-reflux mechanism of Metochlopramide?
Enhanced Gastric motility
46
What are the AE of Metochlopramide?
Tardive dyskinesia | Parkinson's like movements
47
What drug Enhances ACh release by acting on 5-HT4R?
Metochlopramide (also blocks D2R)
48
What is the MOA for Domperidone?
D2R blocker
49
What is the MOA for Sulfasalazine?
5-ASA = local anti-inflammatory agent | **Used in IBD
50
What are the AE for Sulfasalazine?
Anemia Rash Impotence
51
MOA for Inflizimab?
mab that inhibits/binds TNF alpha | **Given IV to Crohns disease patients
52
MOA for lactulose?
semisynthetic disaccharides + metabolized by enteric bacteria + Acidifies Feces --> traps and eliminates NH3
53
MOA of Increased fiber intake treatment for constipation?
Increases H2O delivery to colon Increases Bulk Decreases pressure in sigmoid colon **More formed stool (also for diarrhea)
54
What is MOA for Effer-syllium/ Metamucil?
Metamucil--> Hydrophilic muciloid that forms gelatinous mass when mixed with water
55
AE of Effer syllium?
``` Allergic rxn Flatulance Intestinal obstruction Borborygmi (stomach rumbles) INHIBIT coumarin absorption ```
56
Hydrophilic muciliod producing substance used to relieve constipation?
Syllium / Metamucil
57
MOA of Mitrolan?
Hydrophilic resin that absorbs 60-100x water in weight
58
AE of Mitrolan?
Release Calcium--> CI with tetracylcine use
59
What is the MOA for all Docusates (dioctyl sodium)?
Anionic surfactant, STOOL softener. No affect on peristalsis
60
What are the AE of Docusates laxatives?
Irritate intestinal mucosa increase intestinal absorption of other drugs Short term use
61
MOA of Caster Oil?
RAPID acting anionic surfactant that produces Catharsis. | **COMPLETE evacuation of bowels by stimulating peristalsis
62
What drug can Rapidly and completely empty bowel by stimulating intestinal peristalsis?
Caster Oil
63
What are the AE of Caster oil?
Colic Dehydration Electrolyte imbalance INDUCE UTERINE CONTRACTIONS in pregnants
64
What laxative can induce labor in pregnant women (CI in pregnancy)?
Caster Oil
65
What is the MOA of the stimulant laxatives?
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
What are the most potent laxatives that act in the colon?
stimulant laxatives
67
What is the MOA for Bisacodyl (Diphenmethanes)?
Stimulant laxative--> Pro-drug converted by Enteric bacterial into Desacetyl active form ** stimulates diffusion, contractility, prostaglandin production all in COLON
68
What is pro-drug stimulant laxative that is converted by enteric bacteria?
Bisacodyl
69
What is the MOA for Senokot (anthraquinones)?
NATURAL derivatives of Lilliaceae plants (Senna) * *More gentle than synthetic drugs * *Promote Colonic motility
70
What naturally occuring substance is used to promote Colonic motility?
Senna
71
WHat is the AE of Senna?
Abdominal pain nephritis Melanotic pigmentation of colonic mucosa Abnormal urine coloration
72
What laxative causes Dark stool, urine, and discolors colon?
Senna
73
What are saline laxatives?
Contain Magnesium cations or other nonabsorbable molecules which cause Osmotic affects
74
Why is Magnesium used as a laxative?
It is both NON absorbable and Osmotically active
75
What is the MOA of Mg containing laxatives?
Osmotic effect | Release CCK--> increases Intestinal secretions and motility
76
What laxatives are given via Enema?
Buffered Phosphates
77
Laxative that can be used to acidify stool and trap ammonium ions?
Lactulose
78
What is the MOA for glycerine suppositories?
Osmotic diarrhea | Lubricant
79
MOA for mineral oil use in GI distress?
Hydrocarbons soften stool
80
MOA for caster oil?
Irritates mucosa and produces a cathartic effect
81
What two drugs have been approved for the treatment of IBS?
Lubiprostone--> Targets Cl- channel | Linaclotide--> tagets GC system
82
What is MOA for Lubiprostone?
DIrectly Activates Cl- channels = increases secretion + motility and alleviates constipation
83
What is MOA for Linaclotide?
Indirectly activates Cl- channels by acting on G protein receptors to Upregulate cGMP--> cAMP
84
What antidiarrheal agent is also effective against Travelers diarrhea and H pylori?
Bismuth (pepto biismol)
85
Agents that Adsorb harmful bacterial, viruses, toxin?
Bismuth | Charcoal
86
What are the Actions of Opiates?
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
What drugs can cause contraction of illeocecal sphincter?
Opiates (enkaphalins)
88
What is the MOA of Paregoric?
Opiate antidiarrheal agent--> contracts sphincters and slows motility and inhibits all secretions
89
What is the MOA of Diphenoxylate + Atropine?
Diphenoxylate== Opiate antidiarrheal agent | **Atropine prevents ABUSE
90
What is the purpose of adding Atropine to an Opiate anti diarrheal agent?
Prevent ABUSE due to Atropine AE
91
What is the MOA for Loperamide?
Interacts with intestinal Opioid receptors and binds and inhibits Ca+ binding protein Calmodulin
92
What antidiarrheal agent inhibits Calmodulin but is a opioid agonist?
Loperamide
93
Where is the Emitic center located?
Medulla
94
What anticholinergic drug can be used to manage motion sickness?
Scopolamine
95
What is the MOA for Scopolamine?
Anticholinergic that blocks activation of Muscarinic receptors by ACh from Cochlear sensations
96
What are the AE of Scopolamine?
Sedation Drowsiness Dry mouth
97
What are the MOA for anticholinergics as antidiarrheal agents?
Reduce vagal stimulation== Anti Spasmodics
98
What drug is a Quaternary ammonium derivative of Atropine?
Prpanetheline--> alleviate CRAMPS | Dicyclomine--> Tx urinary retention
99
Dimenhydrinate MOA?
``` Anti histamine (H1) + anticholinergic **Prophylactic for Motion sickness ```
100
What is the MOA for Cyclizine & Meclizine?
BOTH Anti histamines (H1) cyc--> OTC for MS mec--> depresses the Labyrinthine function= Tx vestibular disturbances
101
What antihistamine can also be used to treat Vertigo and menier disease?
Meclizine
102
What is the MOA for Promethazine?
Antihistamine and anticholinergic | **Tx: nausea and vomiting
103
What is the AE of Promethazine?
SEDATION
104
What types of receptors are on the Chemoreceptor Trigger zone in BBB that acts on the VC in medulla?
5-HT3 D2 M1
105
What is the MOA for Chlorpromazine?
Centrally acting anticholinergic + antidopa
106
What drug can be used to treat N&V and intractable hiccoughs?
Chlorpromazine
107
What is the MOA for Theithylperazine?
Antidopaminergic that inhibits CTZ and VC
108
What drug blocks Dopa 2 receptors in the CTZ and is clinically used for N&V postoperatively?
Droperidol
109
What drug inhibits Dopamine receptors in CTZ and stimulates gastric emptying?
Metochlopramide
110
What is the MOA for Trimethobenzamide?
``` Dopa inhibitor (CTZ and stomach) **AE are extrapyramidal= Short term use only ```
111
What is the MOA for Serotonin antagonists in antiemesis?
Block 5HT3 in stomach + SI * Prevent transmission of stimuli through Vagus to CTZ and VC * BLOCK 5HT3 receptors @ CTZ * *MOST effective antiemetics
112
What is the MOA of Ondasetron or Granisetron or Dolasetron?
ALL 5HT3 (serotonin receptor) Blockers
113
What is difference between the Setrones?
``` Ondasetron= selective, used for Antiemesis during chemo (IV) Dranisetron= More potent and ORAL Dolasetron= Long half life ```
114
What is the MOA for Delta 9 tetrahedro cannabinol?
Activates CB1 cannabinoid receptors (Marijuana) | **Antiemetic
115
What is the MOA of Dexamethazone as an antiemetic?
Prevents the production of Prostaglandin associated with CHEMO or radiation therapy
116
Substance P/ neurokinin 1 (NK1) receptor antagonist?
Aprepitant--> Crosses BBB and inhibits emesis via CENTRAL actions
117
Drug used to prevent emesis induced by cytotoxic chemo by crossing BBB and inhibiting central action?
Aprepitant **Substrate for CYP3A4
118
What drug is used in adjunct with other anti-emetics in patients with Anticipatory vomiting?
Lorazepam
119
What drug causes Amnesia and semnolence lasting for hours?
Lorazepam
120
What drug is preferred in HIV/ HBV coinfection?
Emtricitabine | Tenofovir
121
What drugs are used in the treatment of HBV?
``` Tenofovir Entecavir Telbivudine Adifovir Lamivudine Emtricitabine ```
122
What drugs are used in the treatment of HCV?
Ribavirin Tealprevir Boceprevir Peginteferon alpha-2b
123
What drug is used in the treatment of BOTH HBV & HCV?
Peginterferon alpha-2a | interferon alpha 2b
124
What is the mechanism of drug resistance against the Nucleoside/tide structural analogs in the treatment of HBV?
Structural changes in SUGAR RESIDUES Arising from HBV DNA polymerase L-nucleosides= Lamiv + Telbiv Acyclic phosphonates= Adef + Tenof + Disoproxil d-cyclopentane= Entecavir
125
What is MOA for Adefovir?
Diphosphate incorporated in viral DNA producing chain termination --> Adenosine analog
126
What is the MOA for Tenofovir?
Prodrug nucleotide analog of adenosine
127
What is the MOA for Entecavir?
Guanosine analog triphosphate that inhibits DNA polymerase
128
What is the MOA for Telbivudine?
L-isomer of Thymidine triphosphate inhibiting DNA polymerase and produces chain termination
129
What do all the anti HBV drugs have in common?
NO CYP interactions | Competitive RENAL excretion
130
What HBV drug should be taken with HIGH fat meals? Which one should not be taken with food?
Tenofovir + Ribavirin | Entecavir= Food delays absorption
131
What are the AE of Tenofovir?
Nephrotoxic BONE pain BONE fractures
132
Which anti HBV drug should be given with supplements of Vit D/ Calcium?
Tenofovir--> causes bone pain/fractures
133
What is the mechanism of Tenofovirs Nephrotoxicity?
accumulation causing Mitochondrial toxicity
134
causes osteoporotic fractures?
TENOFOVIR
135
Which HBV drugs cause Hepatotoxicity by way of Inhibiting mtDNA synthesis?
Adefovir Telbivudine Entecavir
136
AE is lactic acidosis and steatosis?
Nucleotide analogs Adefovir Telbinvudine Entecavir
137
Biological effects including Antiviral, antiproliferative, and immunomodulatory?
Interferons
138
What is the MOA of interferons?
``` 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
Associated with Acute influenza like syndrome following injections?
Interferons
140
What are the AE of interferons?
``` Depression Seomnolence/ confusion Myelosuppression (Neutropenia + thrombocyto) Hepatotoxic Thyrotoxic Decreased serum antibodies ```
141
May produce immune mediated destruction of thyroid and cause thyrotoxicosis?
Interferons
142
What are the 4 actions of Ribavirin?
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
AE is Hemolytic anemia, non fatal MI, male teratogenecity?
Ribavirin
144
WHat are the NS3/4A protease inhibitors?
Telaprevir | Boceprevir
145
WHat are the AE of the NS3/4A protease inhibitors?
Fatigue + Anemia + Nausea | Telaprevir=== serious RASH
146
HCV patients presents with pruritis and a rash?
Telaprevir Tx
147
What is unique about the metabolism of the protease inhibitors?
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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