Pharmacology Flashcards
List the Histamine 2 Blockers
1) Cimetidine
2) Ranitidine
3) Famotidine
4) Nizatidine
Mechanism of H2 Blockers
Reversible block of histamine H2-reeptors –> Decreased H+ secretion via parietal cells
Indications of H2 Blockers
1) Peptic Ulcer
2) Gastritis
3) Mild Esophageal Reflex
H2 Blocker Relative Contraindication
Pregnancy
Cimetidine is a ___ inhibitor and has ___ effects
P-450
Antiandrogenic Effects
List the Antiandrogenic Effects of Cimetidine
1) Gynecomastia in Men
2) Galactorrhea in Women
Ranitidine and Cimetidine have effects on kidneys by decreasing the secretion of _____,
Creatinine
List the PPIs
Lansoprazole Dexlansoprazole Omeprazole Esomeprazole Pantoprazole Rabeprazole
Mechanism of PPIs
Covalently binds sulfhydryl groups of H+/K+ ATPase of parietal cells
Indications of PPIs
1) Peptic Ulcer
2) Gastritis
3) Zollinger-Ellison Syndrome
4) Component of H. Pylori Therapy
5) Stress Ulcer Prophylaxis
Relative contraindication of PPI
Pregnancy
Adverse Effects of PPI’s
1) Increased C. Difficle infection risk
2) Pneumonia
3) AKI
4) Vitamin B12 Malabsorption
5) Decreased Ca2+ and Mg2+ Absorption (Osteoporosis)
Omeprazole is a ____ inhibitor and has many drug interactions
CYP450
Sucralfate Indications
1) Increase Ulcer Healing
2) Duodenal Ulcer
Contraindications of Sucralfate
1) Severe Renal Failure (due to aluminum) - pts should also avoid antacids
Mechanism of Sucralfate
1) Provides physical protection
2) Allows HCO3- secretion to reestablish pH gradient in mucous layer
Sucralfate should not be given with ___ and ___ because it requires an acidic enviroment.
1) PPI
2) H2 Blockers
Adverse Effects of Sucralfate
1) Constipation (Aluminum Hydroxide)
Since sucralfate has many drug interactions you’ll want to take this medication as well as Bismuth ___ after other medication.
2 hours
Bismuth (Subsalicylate) Indications
1) Travelers Diarrhea
2) Combination Therapy for H. Pylori Gastritis
Relative Contraindications of Bismuth
1) Antiplatelet and Anticoagulants
2) Severe Renal Failure
Absolute Contraindications of Bismuth
1) GI bleeding
2) Salicylate Hypersensitivity
Bismuth Mechanism
1) Prevent Microbial attachment to mucosa
2) Inactivation of Enterotoxins
3) Disruption of bacterial cell wall
Adverse Effects of Bismuth
1) Constipation
2) Black/Dark (regularly-formed) stools
Misoprostol (PGE analog) Mechanism
1) Increase Production and Secretion of Gastric Mucous Barrier
2) Decrease Acid Production (Parietal Cell)
Indications of Misoprostol
Prevention of NSAID-induced peptic ulcers
Off-label usage of Misoprostol
1) Cervical Ripening
2) Post-partum Hemorrhaging
3) Pregnancy Termination
Contraindications of Misoprostol
1) Pregnancy
2) IBD (AVOID)
List the Serotonin (5-HT3) Receptor Antagonists
1) Dolasetron
2) Granisetron
3) Ondansetron
4) Palonosetron
Mechanism of action of 5-HT3 receptor antagonists
Blocks 5-HT3 Receptors at vagal nerve terminals and to CTZ
Ondansetron is most commonly used for ____
Mild N/V
Indications for 5-HT3 Blockers
1) CINV
2) RINV
3) PONV
4) NVP
5) Mild N/V
____ and ____ are 5-HT3 Blockers that are used for delayed CINV as a single dose
1) Palonosetron
2) Sustained-Release Formulation of Granisetron
Adverse Effects of 5-HT3 Blockers
1) Serotonin Syndrome
2) Dose-dependent QT Prolongation (Torsade’s)
5-HT3 Blockers Drug interaction
Antiarrhythmics/QT-prolonging agents
Which 5-HT3 blocker has the highest risk of death
Dolasetron
List the Neurokinin (NKI) Receptor Antagonists
1) Aprepitant
2) Fosaprepitant
3) Netupitant
4) Fosnetupitant
5) Rolapitant
MOA of Neurokinin (NK1) Receptor Antagonists
Blockade of NK1 (Substances P) receptors in CTZ/VC
Indications of NK1 receptors Blockers
CINV (most effective when used in combination)
Which of the NK1 Blockers have the longest half lives
1) Netupitant
2) Rolapitant
List the Histamine (H1) Receptor Antagonists
1) Diphenhydramine
2) Dimenhydrinate
3) Hydroxyzine
4) Meclizine
5) Cyclizine
6) Doxylamine
MOA of Histamine receptor antagonists
Block H1 receptors in VC and Vestibular System
Indications of H1 Blockers
1) PONV
2) NVP ( Doxylamine/B6)
3) Motion Sickness/Vertigo (Meclizine and Cyclizine)
4) CINV (Add on therapy)
5) RINV (Add on therapy)
6) Mild N/V
Adverse Effects of H1 Blockers
Anticholinergics Effects
- Drowsiness (CNS Depression)
- Dry Mouth
- Constipation
- Urinary Retention
- Blurred Vision
- Decreased BP
What is the initial therapy for NVP?
Doxylamine w/ Pyridoxine
List the Dopamine D2 Receptor Antagonists
1) Prochlorperazine
2) Olanzapine
3) Metoclopramide
4) Amisulpride
Primary MOA of D2 Receptor Blockers
1) D2 receptor blockade in CTZ
Metoclopramide is a ___ receptor blocker. What additional MOA does it have?
1) Stimulates ACh actions in GI
- Enhances GI motility (Dysmotility use)
- Increases Lower Esophageal Sphincter Tone
Indication for Amisulpride
PONV (IV FORM)
List the indications for D2 Receptor Blockers
1) PONV (Amisulpride)
2) NVP
3) Gastroparesis/Dysmotility (Metoclopramide)
4) CINV and RINV
General adverse effects of D2 Blockers
1) Drowsiness (All agents)
2) Hypotension (primarily from IV route)
Adverse Effects of Prochlorperazine
1) Drowsiness
2) Constipation
3) Urinary Retention
4) Blurred Vision
Amisulpride Adverse Effects
1) Hypokalemia
2) Hyperprolactinemia
3) Chills
List the Muscarinic Receptor Antagonists
Scopolamine
MOA of Scopolamine
Blocks ACh-stimulated muscarinic receptors from vestibular nuclei and reticular formation to VC
Indication of Scopolamine
1) Motion Sickness
2) End-of-life care for excessive secretions
Adverse Effects of Scopolamine
1) Drowsiness
2) Dry Mouth
3) Constipation
4) Urinary Retention
5) Blurred Vision
Scopolamine can be worn as a transdermal scope patch that lasts ____
72 hours
List the Cannabinoid Receptor Agonists
1) Dronabinol
2) Nabilone
MOA of cannabinoid Receptor Agonists
Stimulates CB1 (central) and CB2 (peripheral) cannabinoid receptors in VC/CTZ
- Decreases excitability of neurons
- Minimizes serotonin release from vagal afferent terminals
Indications of Cannabinoid Receptor Agonists
1) CINV (reserved for treatment-resistant scenarios) can be used as an add on
2) Appetite Stimulation
Describe H. Pylori Treatment
1) Triple therapy (14 days) - all agents 2x day
* ** Only for low Clarithromycin resistance areas and No prior exposure to Clarithromycin
- PPI
- Clarithromycin
- Amoxicillin or Metronidazole
Describe Quadruple Therapy of H. Pylori
1) PPI twice/day all other agents four times/day
- PPI
- Metronidazole
- Amoxicillin (Tetracycline; esp for PCN allergy)
- Bismuth Subsalicylate
Describe the substitutions for Quadruple Therapy of H. Pylori
1) Clarithromycin for Bismuth
2) Levofloxacin for failed eradication
Treatment for Clostridium Difficle
1) ORAL Vancomycin (Fidaxomicin = alternative)
2) I.V. Metronidazole (for severe disease + Oral Vancomycin)
Campylobacter Jejuni Treatment
Azithromycin (Ciprofloxacin = alternative)
Salmonella Spp. Treatment
Ciprofloxacin/Levofloxacin (Azithromycin (alternative)
Shigella Spp. Treatment
Ciprofloxacin/Levofloxacin (Azithromycin = Alternative)
MOA of Benzimidazoles
1) Inhibition of Microtubule polymerization via b-tubulin binding
2) Inhibition of mitochondrial fumarate reductase
List the GI Anthelmintic
1) Benzimidazoles
- Albendazole
- Mebendazole
List the GI Anti-Protozoal Agents
1) Paromomycin
2) Metronidazole
3) Tinidazole
MOA of Paromomycin
30S subunit inhibitor
Metronidazole and Tinidazole MOA
1) Disrupts Electron Transport Chain proteins –> Nitrogen free radicals
Treatment of Amebiasis: Entamoeba Histolytica
1) Metronidazole followed by paromomycin
Treatment for Hookworm: Ancylostoma Spp. and Necator Americanus
Albendazole (Mebendazole)
Roundworm Treatment: Ascaris Lumbricoides
Albendazole (Mebendazole)
Giardiasis Treatment: Giardia Spp.
Metronidazole (Tinidazole)
Tapeworm - Adult Forms: Taenia Spp. (Including T. solium, except cysticercosis)
Praziquantel
Tapeworm - Larval forms: Echinococcus Spp.
Albendazole + Praziquantel
Tapeworm - Larval Forms Taenia Solium (Cysticercosis)
Albendazole
Pinworm Treatment: Enterobius Vermicularis
Mebendazole (Albendazole)
Schistomiasis Treatment: Schictosoma Spp.
Praziquantel (+ steroids for neurological disease)
Whipworm Treatment: Trichuris Trichiura
Mebendazole (Albendazole)
Trichinellosis Treatment: Trichinella Spp.
Albendazole (Mebendazole) (+steroids for severe disease)
Cryptosporidium Spp. Treatment
Nitazoxanide
Ulcerative Colitis (U.C.) Treatment Classes
1) 5-ASA
2) Janus Kinase Inhibitors
3) IL-12/23 Inhibitors
4) TNF-a Inhibitors
5) a-4 Integrin Inhibitors
List the 5-ASA’s
1) Sulfasalazine
2) Mesalamine
3) Olsalazine
4) Balsalazide
List the Janus Kinase (JAK) Inhibitors
Tofacitinib
List the IL-12/23 inhibitors
Ustekinumab
List the U.C. TNF-a inhibitors
1) Adalimumab
2) Golimumab
3) Infliximab
List the U.C. a-4 integrin inhibitors
Vedolizumab
List the General Classes for Chrons Disease
1) IL-12/23 Inhibitors
2) TNF-a Inhibitors
3) a-4 integrin inhibitors
List the Chron Disease TNF-a Inhibitors
Adalimumab
Certolizumab
Infliximab
List the C.D. a-4 Integrin Inhibitors
Natalizumab
Vedolizumab
MOA of 5-ASA agents
1) Inhibition of PG and LT production via arachidonic acid pathway
- COX and LIPOX
2) Reduction in PMN and Macrophage chemotaxis
Contraindications of 5-ASA compounds
1) ASA-allergic pts
2) Sulfasalazine contraindicated in sulfonamide allergic pts
MOA of TNF-a
blocks leukocyte migration to site of inflammation
Which of the TNF-a inhibitors is supplied via IV
Infliximab
Side Effects of TNF-a inhibitors
1) Infections (TB testing pre-therapy)
Indications of Adalimumab
Moderate-to-severe U.C. and C.D.
Indications for Infliximab
1) Moderate-to-Severe C.D.
2) Severe U.C.
Indications for Golimumab
Moderate-to-Severe U.C. only
Indications for Certolizumab
Moderate-to-Severe C.D. only
Indications for 5-ASA Agents
1) Mild-to-Moderate U.C.
- Except Olsalazine (only for maintenance of remission)
- Except Balsalazide (only for active disease)
What are the exceptions for 5-ASA Agents
All treat Mild-to-Moderate U.C. Except:
1) Olsalazine = maintenance of remission
2) Balsalazide = Active Disease only
When should you consider TNF-a inhibitors as a treatment option?
After inadequate response to conventional or immunosuppressant therapy
MOA of a-4 integrin inhibitors
1) Prevents trans-endothelial migration of leukocytes (decrease leukocyte traffic)
Indications of a-4 Integrin Inhibitors: Natalizumab
Moderate-to-severe C.D.
Indications for a-4 Integrin inhibitors: Vedolizumab
Moderate-severe C.D. and U.C.
Side Effects of a-4 Integrin Inhibitors: Natalizumab ***cases for only Natalizumab at this time
Infections:
- PML (Progressive Multifocal Leukoencephalopathy) associated w/ John Cunningham Virus (JCV))
3 Risk Factors for PML associated Natalizumab
1) Treatment > 2 yrs
2) Prior Immunosuppressant Treatment
3) Anti-JC virus (JCV) antibodies
When should you consider a-4 integrin inhibitors
** After inadequate response to conventional or TNF-a therapy
MOA of Ustekinumab (Interleukin IL-12 and IL-23 Inhibitors)
Bind P40-subunit of IL-12 and IL-23
1) Decrease activation and differentiation of naïve T Cells
2) Decrease activation of NK cells
Side Effects of IL-12 and IL-23 Inhibitors
Infections:
- TB testing pre-therapy recommended
Indications for Ustekinumab
Moderate-to-Severe UC and CD
When should you consider Interleukin inhibitors as a treatment?
After:
1) Conventional
2) Immune Modulators
3) Steroids or TNF-a therapy
MOA of JAK Kinase Inhibitors
Bind JAK1 and JAK3 –> inhibition of gene transcription and cytokine release
Tofacitinib (oral) is used for U.C., __, ___
Psoriatic
RA
Indications for JAK’s Inhibitors
Moderate to Severe U.C.
______: concomitant use of Biologic Therapies or immunosuppressant’s not recommended
JAK’s Inhibitors
Indications for Glucocorticosteroids
Acute and/or Severe U.C. and C.D. uncontrolled by other conventional medications
*** Not for maintenance of remission unless absolutely required
List the general classes for Diarrhea
1) Prostaglandin Inhibitors
2) Opioid Agonists
3) Serotonin Antagonists
4) Chloride Channel Inhibitors
Loperamide is an ___ used for diarrhea
Opioid agonist
Loperamide causes ___ toxicities leading to death
Cardiac
Side efecft of loperamide
Anticholinergic
Diphenoxylate is an ___ and is used for diarrhea
Opioid agonist
List the Nucleoside Analogue Reverse Transcriptase Inhibitors that Treat HBV
1) Entecavir
2) Lamivudine
3) Telbivudine
Entecavir Indication
Chronic Hep B Infection
Lamivudine Indication
Chronic Hep B w/ HIV-1 Infection
Contraindication of Lamivudine
Hypersensitivity Reaction to Lamivudine
Telbivudine Indication
Chronic Hepatitis B in Adult Population
Contraindication of Telbivudine
Can’t use w/ PEGylated Interferon alfa-2a
If Telbivudine is used with PEGylated interferon alfa-2a it increases risk of….
Peripheral neuropathy
BB warning for Entecavir
1) Severe Acute Exacerbations of Hep B
2) Pts co-infected w/ HIV and HBV
3) Lactic Acidosis
4) Hepatomegaly
BB Warning of Lamivudine
1) Lactic Acidosis
2) Severe Hepatomegaly
3) Exacerbations of Hep B
BB Warning of Telbivudine
1) Lactic Acidosis
2) Severe Hepatomegaly w/ Steatosis
3) Severe Acute Exacerbations of Hepatitis B
List the Nucleotide Analogues that Treat Chronic HBV
1) Tenofovir disoproxil
2) Adefovir Pipivoxil
Indications of Tenofovir
1) HIV-1 Treatment in Adults and Peds Pts
2) Chronic HBV (12yrs or older)
Adverse Effects of Tenofovir
1) Nephrotoxicity:
- Acute Renal Failure
- Fanconi Syndrome
2) Nausea (most Common)
BB Warning of Tenofovir
1) Lactic Acidosis
2) Severe Hepatomegaly w. Steatosis
3) Post Treatment exacerbation of Hepatitis
Indications of Adefovir
1) Chronic Hep B (12yrs and older)
Contraindications of Adefovir
Hypersensitivity to any components
Adverse Effects of Adefovir
Nephrotoxicity
Asthenia
Increased Creatinine
Adefovir should not be used with other drugs that ____ or ___ because it increases risk of increased serum Adefovir
1) Reduce renal function
2) Compete for active tubular secretion
List the Drugs that Treat HCV
1) PEG-Interferon Alfa-2a
2) Elbasvir/Grazoprevir
3) Ledipasvir/Sofosbuvir
4) Velpatasvir/Sofosbuvir
5) Ribavirin
6) Boceprevir
MOA of PEG-Interferon Alfa-2a
Anti-viral and Immunomodulatory Effects
Indications of PEG-Interferon Alfa-2a
1) Chronic Hep C (18yr or older)
Contraindications of PEG-Interferon Alfa-2a
1) Hypersenstivity to INF-a
2) Autoimmune Hepatitis
3) Decompensated Liver Disease
Adverse Effects of PEG-Interferon Alfa-2a
Flu-Like Sx
BB Warning for PEG-Interferon Alfa-2a
1) Aggravate Fatal or Life-Threatening Neuropsychatric, Autoimmune, Ischemic and Infectious Disorders
-Asvir MOA
NS5A Polymerase Inhibitor
- Previr MOA
NS3/4A Protease Inhibitor
- Buvir MOA
NS5B Polymerase Inhibitor
indication for Elbasvir/Grazoprevir
Chronic Hep C
Elbasvir/Grazoprevir shouldn’t be Co-administered with a ___.
CYP3A Inducer (will Decrease its concentration)
Ledipasvir/Sofosbuvir Indication
Chronic Hep. C
Drugs interactions of Ledipasvir/Sofosbuvir
1) Poly glycoprotein Inducers
- Rifampin
- St. John’s Wort
Velpatasvir/Sofosbuvir Indication
1) Chronic Hep C.
- W/o Cirrhosis or w/ Compensated Cirrhosis
If a Pt has Decompensated Cirrhosis what should be used in combination with Velpatasvir/Sofosbuvir.
Ribavirin
Indication for Ribavirin
1) Chronic Hep C in combination w/ Interferon alfa-2a
2) CHC pts co-infected with HIV
Contraindications of Velpatasvir/Sofosbuvir
1) Pregnant Women and Men whose female partners are pregnant
2) Hemoglobinopathies
BB Warning for Velpatasvir
1) Potentiates Bradycardia w/ amiodarone co-administration
2) Caution w/ Beta Blockers, Cardiac Comorbidities and/or advanced liver disease
Indications of Ribavirin
1) Chronic Hep C infection in combination w/ interferon alfa-2a
2) CHC pts co-infected with HIV
BB Warning of Ribavirin
1) Birth Defects and Fetal Death
2) Don’t use in pregnancy and for 6mo after treatment
Contraindications of Ribavirin
1) Pregnant Women and Men whose female partners are pregnant
2) Hemoglobinopathies
Boceprevir MOA
NS3/4A Protease Inhibitor
Indication of Boceprevir
Chronic Hep. C Infection in combination with peginterferon alfa and ribavirin
Contraindication of Boceprevir
1) Contraindications of Peginterferon
- Hypersensitivity to INF-a
- Autoimmune Hepatitis
- Decompensated Liver Disease
2) Contraindications of Ribavirin
- Pregnant women and men whose female partners are pregnant
- Hemoglobinopathies
Pt who has decompensated cirrhosis needs treatment. How would you treat this pt.
1) Velpastasvir/Sofosbuvir + Ribavirin
Pt has Autoimmune Hepatitis what Drug that treats Hep C would you not want to use?
PEG-Interferon Alfa-2a