Exam #1 Pharmacology Flashcards
which salicylates are absorbed at the colon
Olsalazine
Sulfasalazine
Balsalazide
IBD treatment
obtain remission w corticosteroids and maintain remission w salicylates
Sulfasalazine adverse effects
nausea, GI upset, headache
sulfa allergy via sulfapyridine
oligosperimia
inhibits folate absorption
antibiotics used to treat Crohn’s Disease
Ciprofloxacin
Metronidazole
**adjunctive
Ciprofloxacin MOA
topoisomerase II and IV inhibitor
Ciprofloxacin contraindications
Antacid use
Patient w/ arrythmias or who are taking drugs that produce prolongation of QT
Concurrent administration of tizanidine
Metronidazole contraindication
alcohol use
Metronidazole MOA
Forms toxic free radical metabolites that interacts with DNA disrupting its structure and inhibiting replication
Metronidazole adverse effects
peripheral neuropathy
METALLIC TASTE
6-mercaptopurine and Azathioprine active metabolite
6-thioionosinic acid
6-mercaptopurine and Azathioprine moa
mimic IMP inhibiting RNA and DNA synthesis
6-mercaptopurine and Azathioprine adverse effects
bone marrow depression leading to leukopenia
hepatic toxicity
INC RISK FOR MALIGNANCY
Infliximab adverse effects
inc risk for infection
headache
abdominal pain
Cimetidine adverse effects
Diarrhea, headache, drowsiness
gynecomastia
galactorrhea
big time CYP inhibitor (will inc effects of other drugs)
Cimetidine moa
binds H2 receptor on basolateral membrane of parietal cell preventing histamine from binding
Famotidine adveres effects
renal insufficiency
prolonged QT interval
Nizatidine adverse effects
dec B12 absorption by increasing pH
Proton Pump Inhibitors MOA
suppresses both gastric basal and stimulated acid secretion by irreversible binding to and inhibiting the parietal cell H+/K+ ATP pump
**IRREVERSIBLY INHIBIT via disulfide bond
Proton Pump Inhibitors adverse effects
OSTEOPOROSIS
abdominal pain, diarrhea, flatulence vomiting, constipation (altered absorption)
headache
Omeprazole drug interaction
dec antiviral effects dec clopedigrel effects inc methotrexate effects inc warfarin effects St. John Wart and Rifampin dec omeprazole effects via induction of CYP
Esomeprazole adverse effect
headache most common
osteoporosis
Lansoprazole is special bc
has no interaction w clopedigrel
Clarithromycin adverse effects
Jaundice Ototoxicity Prolonged QT Hepatoxicity CYP 3A4 inhibitor
Amoxicillin adverse effects
Nephritis Neurotoxicity GI distress Penicillin allergy (hypersensitivity) Hematological toxicities Diarrhea inc when given w Clavulanic acid
H. pylori quadruple therapy
PPI or H2R antagonist
Bismuth subsalicylate
Metronidazole
tetracycline
Aluminum hydroxide adverse effect
constipation
**slower effect but longer duration
Magnesium hydroxide adverse effect
diarrhea via Mg+2 stimulates gastric smooth muscle contraction
**faster effect but shorter duration
Aluminum hydroxide and Magnesium hydroxide are mixed to…
dec adverse effects (counteract)
Sodium Bicarbonate adverse effects
flatulence with CO2 release
Sucralfate MOA
cytoprotective via viscous polymer that bind to and covers ulcer for up to 6hr
Antacids adverse effects
belching, nausea, abdominal distention, and flatulence with CO2 release
Hypercalcemia…patients with uremia
Rebound acid secretion…more frequent administration
milk-alkali syndrome
the chemotherapeutic agent with higher emetogenic potential
Cisplatin
Chemotherapy-induced nausea and vomiting treatment
5-HT3 receptors antagonist
enhanced by combination therapy with a corticosteroid (dexamethasone), NK1-receptor antagonist, and a dopamine D2 antagonist
Odansetron adverse effects
prolonged QT interval
serotonin syndrome
headache, dizziness
Aprepitant adverse effets
CYP 3A4 inhibitor
Ketoconazole inc serum levels
Contraindicated in patients on cisapride or pimozide, in whom life-threatening QT prolongation
H1 Receptor Antagonist name
Diphenhydramine -> drowsy
Dimenhydrinate -> drowsy
Meclizine (Minimal anticholinergic properties)
parietal cell receptors
H2: histamine -> Gs -> cAMP
CCKB: gastrin -> Gq -> IP3/DAG
M3: Ach -> Gq -> IP3/DAG
Hyoscine (scopolamine) indication
motion sickness
Metoclopramide MOA
Central D2 receptor antagonist with 5-HT3 receptor antagonist properties
Prochlorperazine, Promethazine antiemetic effects
inhibition of dopamine and muscarinic receptors
Olanzapine antiemetic effects
inhibition of dopamine D2 and serotonin 5-HT1c and 5-HT3 receptors
Droperidol antiemetic effects
indication
dopamine blockade
indication: postoperative nausea and vomiting, in conjunction with opiates and benzodiazepines
* *not first line
pregnancy nausea treatment
Pyridoxine (B6) + doxylamine (H1 antagonist)
DIAZEPAM and LORAZEPAM are used
before the initiation of chemotherapy to reduce the anticipatory vomiting caused by anxiety
Bethanechol, Carbachol MOA
Stimulate muscarinic M3 receptors on muscle cells and at myenteric plexus synapses
**uncoordinated motility
Neostigmine MOA
Acetylcholinesterase inhibitor Increase the action of acetylcholine through inhibition of its metabolism at the myenteric plexus synapses
**uncoordinated motility
Significant broad cholinergic effects
Bradycardia Flushing Diarrhea Cramps Miosis Salivation
METOCLOPRAMIDE and DOMPERIDONE MOA
inhibitor D2 receptor resulting in dec dopamine inhibition of gastric smooth muscle -> inc motility
- In addition to, antagonism on D2R Metoclopramide also presents HT4R agonism
Cisapride
MOA
Adverse Effects
MOA: 5-HT4 agonist and weak 5-HT3 antagonist
Adverse Effects: prolonged QT interval, cardiac arrhythmia
Tegaserod
MOA
Indication
MOA: partial 5-HT4 agonist
Indication: short term constipation in IBS
Bulk-forming
Agents
MOA
Adverse Effets
MOA: absorb water, forming a bulky, emollient gel that distends the colon and promotes peristalsis -Psyllium -Methylcellulose -Polycarbophil Adverse Effects: bloating
Docusate MOA
soften stool material, permitting water and lipids to penetrate
-soften stool material, permitting water and lipids to penetrate
OsmoticLaxatives agents
Magnesium hydroxide
Magnesium citrate
Magnesium citrate MOA
treatment of acute constipation or to cleanse the bowel prior to medical procedures
Magnesium hydroxide
Magnesium citrate
adveres effects
diarrhea
dehydration
hypermagnesium
Senna MOA
MOA: direct stimulation of the enteric nervous system and colonic electrolyte and fluid secretion
Adverse Effects: brown pigmentation of the colon known as “melanosis coli”
Lubiprostone MOA
increases chloride-rich fluid secretion via stimulation of type 2 chloride channel (ClC-2) into the intestine, which stimulates intestinal motility and shortens intestinal transit time
Linaclotide and Plecanatide MOA
stimulate intestinal chloride secretion by binding to and activating guanylate cyclase-C on the luminal surface
**contraindicated in pediatric children
Methylnaltrexone
MOA
Indication
Adverse effect
MOA: inhibits peripheral u-opioid receptor without effecting CNS
Indication: opioid induced constipation
Adverse effect: cardiotoxicity
Bismuth subsalicylate (Pepto-Bismol) MOA
antisecretory, anti-inflammatory, and antimicrobial effects. Bismuth also relieves nausea and abdominal cramps.
Bismuth subsalicylate (Pepto-Bismol) indication
- traveler’s diarrhea
- direct antimicrobial activity against H pylori
Bismuth subsalicylate (Pepto-Bismol) adverse effects
Reye’s syndrome
Dark stool
Black staining of the tongue
Loperamide MOA
agonist of u-opioid receptor without crossing BBB
Diphenoxylate MOA
agonist of u-opioid receptor that has no analgesic effects at low dose but does at high dose
-prolonged use can lead to opioid dependence
Diphenoxylate adverse effects
toxic megacolon
opioid dependence
Loperamide indication
Traveler’s diarrhea in conjunction w antibiotics
Octreotide indication
VIPoma
varices
carcinoid tumor
acromegaly
Crofelemer indication
diarrhea associated with antiretroviral therapy for HIV/AIDS
Crofelemer MOA
by inhibiting the cyclic AMP stimulated CFTR Cl− channel and Ca+2 activated chloride ion channels on the luminal aspect of the enterocyte -> reducing water loss associated w chloride secretion
-dont give if infection is present
