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Antiemetics/Acid controlling drugs
N/A
26
Pharmacology
Undergraduate 4
11/28/2016

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Term
Calcium carbonate (Tums®, Rolaids®) Aluminum hydroxide (Amphojel®) Magnesium hydroxide (Milk of Magnesia®)Aluminum and magnesium salts (Maalox®, Mylanta®)
Definition
Antacids
Decreases acidity in stomach by neutralizing acid; pH of stomach increases; Decreases injury to mucosal lining (renally eliminated)
AE - constipation- Calcium/Aluminum; diarrhea- magnesium
Term
Cimetidine (Tagamet®, Tagamet HB®) - Ranitidine (Zantac®, Zantac 75®)
Definition
H2 blockers
Antagonizes H2 receptors in gut; Decreases acid production; Increases pH in stomach, decreases damage (renally eliminated; cimetidine - well known CYP enzyme inhibitor - lots of drug interactions
AE - cimetidine- antiandrogen
All- ^ risk for pneumonia; All can accumulate in renal/geriatric- H1
Term
Omeprazole (Prilosec®, Prilosec OTC®)
Definition
PPIs
Inhibits H+ / K+ ATPase in parietal cells Decreases acid production
Term
PPIs
Definition
Irreversible inhibition of the proton pump
blocks basal and stimulated acid release
a single dose can reduce acid up to 97% in 2 hours vs 65% with H2RA's
effects persist until new pump is created
partial recovery 3-5 days
full recovery- weeks
Term
PPI AEs
Definition
rebound acid hypersecretion when stopped
Increased risk for pneumonia
Increased risk for Clostridium difficile
long term -hypomagnesemia
long term- Fractures (Osteoporosis)
Link to dementia?
Term
Sucralfate (Carafate®)
Definition
Anti-ulcer agent
Composed of aluminum hydroxide and sulfated sucrose. When ingested, creates a protective barrier/gel at active ulcer sites for up to 6 hours
AE - may decrease absorption of other drugs
constipation
Term
Misoprostol (mye so PRAH stole) (Cytotec®)
Definition
Anti-ulcer agent
Prostaglandin analog- suppress stomach acid
promote secretion of bicarbonate and mucus
Indications - U.S. for NSAID induced ulcers
Offlabel- for nonNSAID related ulcers
AE - Pregnancy Category X
Contraindicated during pregnancy
Educate women about use, must have negative pregnancy test within 2 weeks, be on contraceptive
Term
ondansetron – PO, IV ( 4-8 mg doses)
Definition
Serotonin Receptor Antagonists
antagonist at 5-HT3 receptors located in the CTZ as well as in the G.I. tract
Indications - CINV (chemotherapy induced N/V); N/V in pregnancy; radiation/anesthesia N/V; Post-Op N/V; toxins
AE - max dose of 16 mg (anything higher, QT prolongation)
Term
promethazine (Phenergan®) – PO, PR, IM, IV ( 6.25-25 mg doses)
Definition
Dopamine Antagonist part 1/phenothiazines
1) antagonist at D2 receptors in the brain (CTZ); 2) Antagonism at H1 receptors (also some anticholinergic properties)
Indications - traditionally for antipsychotic purposes; CINV; toxins; surgery; chlorpromazine (hiccups)
AE - Extrapyramidal Symptoms
https://www.youtube.com/watch?v=n1CesjByFFw
BOXED WARNING: tissue injury- extravasation
BOXED WARNING: respiratory depression resulting in death
CNS depression, caution w/certain medications
Term
metoclopramide (Reglan®)
Definition
Dopamine Antagonists Part 2
1) blocks dopamine AND serotonin receptors in the CTZ
2) enhances actions of acetycholine in the GI tract (resulting in increased motility)
Indications - "prokinetic;" supression of gastroesophageal reflux; diabetic gastroparesis; Post OP N/V; CINV; off label- hiccups
AE - BOXED WARNING
Extrapyramidal Symptoms
Specifically Tardive Dyskinesia
Not to be used in Bowel Obstruction, GI; perforation/hemorrhage; Cholinergic adverse effects- diarrhea
Term
dronabinol (Marinol®) controlled substance
Definition
Cannabinoids
1) agonist at cannabinoid receptors in the brain
Indications - CINV; appetite stimulant (patients w/ AIDS and muscle wasting)
AE - sedation; euphoria
Term
scopolamine patch (Transderm-Scop)
Definition
Anticholinergics
1) Block ACh receptors in the vestibular nuclei and reticular formation
Indications - motion sickness; Post op N/V
AE - dry mouth, dizziness, hallucinations, sedation, dilated pupils
Contraindications - Narrow Angle Glaucoma (must remove prior to MRI)
Term
meclizine (Antivert®)
Definition
antihistamines
1) Weakly blocks ACh receptors from the inner ear to the vomiting center
2) Block H1 receptors from the inner ear to the vomiting center
Indications - motion sickness (scopolamine is superior); vertigo
AE - sedation; anticholinergic
Term
N/V in pregnancy
Definition
doxylamine and pyridoxine (Diclegis)

ondansetron for hyperemesis gravidarum
Pregnancy Category B
Still being studied

ginger
Term
Other antiemetics
Definition
Substance P/Neurokinin Antagonists
Aprepitant
for post Op N/V and CINV
Benzodiazepines- Lorazepam
For CINV
anticipatory nausea, amnesia
Glucocorticoids- full MOA is unknown
Dexamethasone and Methylprednisolone
For CINV
Term
Anemia causes
Definition
1.) Bone Marrow
Synthesis of erythryocytes
2) Erythropoietin
Stimulates bone marrow
3) iron, folic acid, B12 (cyanocobalamin)
building blocks for erythyrocytes
Term
Different types of anemia
Definition
MIcrocytic anemia (small MCV)
many causes
Iron deficiency anemia most common
Normocytic Anemia
low H/H
Macrocytic anemias (large MCV)
many causes
megaloblastic anemias (DNA issue) most common
Vitamin B12 deficiency, folate deficiency
Term
Microcytic anemia
Definition
Iron Deficiency Anemia
Essential mineral in the body
Oxygen carrier in hemoglobin and myoglobin
Stored in the liver, spleen, and bone marrow
Iron deficiency results in anemia
Use iron to treat
Term
ferrous sulfate (Feosol)-325 mg tablet, contains 65 mg elemental iron
GOAL is 200 mg of elemental iron/day for IDA
Definition
oral iron
Iron Salt replenishment for the body when dietary is insufficient
Indications - prevention of iron deficiency anemia; treatment of iron deficiency anemia
AE - GI TRACT
nausea, heartburn, bloating, constipation (diarrhea)
liquid iron can STAIN teeth; both forms can "stain" a bowel movement- black stool normal
Term
Oral iron AE and Drug/Drug
Definition
Drug/drug - iron likes to bind with other drugs
-avoid administering with oral antibiotics (fluoroquinolones and tetracyclines)
-Ascorbic Acid is acidic (increases absorption)
-Therefore co-administration with an Antacid such as Tums (calcium carbonate) will do what?
AE - Boxed Warning: Most common cause of pediatric poisoning deaths
As little as 15 tablets can lead to overdose
Children can appear asymptomatic
Severe N/V/D, GI bleeding
Term
iron dextran (INFed)
Definition
Parenteral iron
Iron Salt replenishment for the body when dietary is insufficient
Indications - treatment of iron deficiency anemia in CKD; exception (iron dextran) can be used w/o CKD; dependent on whether or not using HD, or ESAs
AE - BOXED WARNING: anaphylactic reactions during any dose!
Iron Dextran only product requiring a small TEST dose first
Term
Epoetin Alfa (e POE e tin AL fa) (Epogen)
Definition
Erythropoesis Stimulating Agents (ESA's)
stimulates production of RBC's in the bone marrow. Natural hormone is produced by the kidneys
Ind - Anemia in CKD; Chemotherapy induced Anemia (requires REMS); few other uses
AE - Target Hgb used to be 12 g/dL, NOW its 11g/dL, HOLD if over; HYPERTENSION (most common); Heart Attack, Stroke, Heart Failure, thrombosis
Contra - Contraindications: drug allergy, uncontrolled hypertension, head and neck cancers, risk of thrombosis
Term
ESAs boxed warnings
Definition
CANCER:
ESAs shortened overall survival and/or increased the risk of tumor progression or recurrence in some clinical studies with certain cancers
CHRONIC KIDNEY DISEASE:
patients experienced greater risks of death, serious adverse cardiovascular reactions, and stroke when administered ESAs to target a hemoglobin level of greater than 11 g/dL
CARDIOVASCULAR:
Erythropoiesis-stimulating agents (ESAs) increase the risk of death, myocardial infarction (MI), stroke, venous thromboembolism, thrombosis of vascular access
Term
Macrocytic anemia
Definition
Large MCV
Folate Deficiency
Pernicious Anemia
Treatment- The B Vitamins!
B9 (folic acid)
B12 (cyanocobalamin)
Term
Folic acid
Definition
Water-soluble, B-complex vitamin (B9)
Essential for erythropoiesis
Primary uses
Folic acid deficiency
During pregnancy to prevent neural tube defects
Malabsorption syndromes are the most common cause of deficiency
Should not be used until actual cause of anemia is determined
May mask symptoms of pernicious anemia, which requires treatment other than folic acid
The folic acid supplementation will allow the RBCs to mature and have a normal MCV, but the B12 is still deficient ( can lead to neurologic damage)
Term
Cyanocobalamin (Vitamin B12)
Definition
Used to treat pernicious anemia and other megaloblastic anemias
Deficiency can result in neurologic changes, and CNS lesions
Requires Intrinsic Factor for absorption
Can be given IM, SC, orally, intranasally
Low risk for toxicity
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