Studied by 10 people
N/V receptors
CNS= stimulating the vomiting center in the medulla oblongata
Vomiting center: histamine, serotonin, muscarinic, dopamine (NK1)
Vestibular system= Labyrinth stimulated >> Histamine and muscurinic
Chemo receptor trigger zone=dopamine receptors (NK1) and serotonin receptors
GI and heart= serotonin receptors
causes of vomiting
ingestion
metabolic (pregnancy)
neurologic
presence of. noxious stimuli
gruesome sight
pungent odor
infection
anxiety
medications (chemo)
motion sickness
post op
Phenothiazines MOA
block dopamine and provide anticholinergic activity
Phenothiazines types
Promethazine (Phenergan)
Prochlorperazine (Compazine)
inexpensive
Phenothiazines contraindications
-Pregnancy cautious use
-pushed slowly IV due to phlebitis
AE: *sedation. May produce EPS therefore caution with Parkinson’s (Parkinson’s is lack of dopamine)
-Interaction with other CNS depressants: potentiates depression
-potential for abuse
Antihistamines MOA in N/V
mainly for motion sickness
interrupt visceral afferent pathways that stimulate N/V.
types of antihistamines used for N/V
hydroxyzine (Vistaril)
meclizine (Antivert)
dimenhydrinate (Dramamine)
scopolamine (Transderm Scop) (prescribed)
antihistamines contraindications
contraindicated with asthma, glaucoma, GI or urinary obstruction, Lactation, CNS depressants
AE:
-sedation, drowsiness, confusion
-Anticholinergic effects
Cant pee/cant see/cant spit/cant shit
Benzodiazepines MOA
ex. ativan
Useful in anticipatory N/V, i.e, chemotherapy
by inhibiting vomiting center
Benzodiazepines contraindications
not to be used in pregnancy
Contraindicated in renal or hepatic failure
AE: CNS depression, amnesic effect, constipation, HA, appetite changes, CNS depression
Serotonin Antagonists MOA
Block 5HT3 receptors in Chemo receptor trigger zone and UpperGI tract for chemo induced N/V, radiation, post op
ex. Ondansetron (Zofran), (oral/IV/SL)
granisetron (Kytril)
Serotonin Antagonists contraindications
SIGNIFICANT: Prolonged PR interval, QT interval and widened QRS. Cautious use with severe cardiac dysfunctions and arrhythmias.
-Pregnancy safe
-Cautious use with lactation
AE: headache, diarrhea, abd pain, increased LFT's (baseline LFT"S), HTN, fatigue, pruritus, fever
Metoclopramide (Reglan) MOA
enhances GI motility and gastric emptying. Inhibits dopamine receptors in Chemo receptor trigger zone
Used for dm gastroparesis, post op gastric stasis, GERD, CINV
Metoclopramide (Reglan) contraindication
AE: EPS, diarrhea, drowsiness
MAOIs cause HTN crisis
Corticosteroids side effects
AE: steroid psychosis, aggression, insomnia, hyperglycemia
Corticosteroids MOA
unknown. inhibition of prostaglandins for Chemo induced N/V
ex Dexamethasone (Decadron)
methylprednisolone (Solu-Medrol)
Cannabinoids MOA
unknown. Theorized effect on opiate receptors in CNS for CINV and appetite stimulation
ex dronabinol (Marinol)
Cannabinoids contraindications
Best given 6-12 hrs before chemo.
AE: sedation, ataxia, dysphoria. Tolerance with repeated dosing, appetite stimulation
Pregnancy avoid
Avoid in Lactation
Antacids MOA
coat stomach and neutralize acid
Antacids contraindications
-magnesium preparations: diarrhea
-aluminum and calcium preparations: constipation
-decrease absorption of other meds
first line for N/V
phenothiazine
second line for N/V
antihistamine or anticholinergic
third line for N/V
evaluate for another cause
causes of constipation
diet, lifestyle, medication, and diseases
more frequent in females
fiber requirements
American diet 5-14 Gms fiber; recommended 20-35 Gms fiber
bulk forming laxative uses
ex. metamusil
Bulk stimulates movement of the intestine and pulls water into the stool to swell and increase stool bulk.
Preferred agent for relief of constipation
-Can be used as antidiarrheal
bulk forming laxative contraindications
**contraindicated in Esophageal Strictures, Gi ulcerations, Gi stenosis
and Gi obstruction
**Cautious use in DM because of carbohydrate content from fiber. Many now use in sugar-free form
contains aspartame; Avoid in patients with gluten intolerance
May cause absorption blocking with quinolones or TCN.
Not useful in opioid induced constipation
Hyperosmotic Laxatives MOA
ex. miralax
-Metabolized to solutes in the intestine to draw fluid into stool by increasing osmotic pressure.
-Increased osmotic pressure stimulates intestinal motility.
suppository form increases rectal stimulation
Hyperosmotic Laxatives contraindications
-contraindicated in appendicitis, acute abd, fecal impaction, intestinal obstruction
-Lactulose containing products>> caution in diabetics
-Not useful in changed colonic transit time, IBS, severe bloating or fullness.
saline laxatives MOA
ex.mag citrate/ milk of mag
-used for pre procedure bowel prep
Draw water into intestine via osmosis into a salt >>which increases intraluminal pressure >>which increases motility.
saline laxatives contraindications
-Low salt diet
-Renal disease: can cause hypokalemia, hypermag, hypocalcemia, hypernatremia
-Caution in elderly
-Separate administration from Azole antifungals, quinolones, and TCN.
stimulant laxatives MOA
ex. doculax/senna; castor oil
-Increase peristalsis of intestine and promotes fluid accumulation.
stimulant laxatives contraindications
-can become dependent with long term treatment
**high potential for abuse
-contraindicated with fecal impaction, GI obstruction, or cause an exacerbation of hemorrhoids
surfactant laxatives MOA/use
(stool softners ) ex. docusate sodium or colace
laxative of choice to prevent straining due to constipation
-Reduces surface tension of liquid contents of bowel.
-Incorporates more liquid into stool forming a softer mass.
surfactant laxatives contraindications
-no contraindications
-interacts with mineral oil
Clinical Pearl: can be used in the ear to soften cerumen before irrigation.
Lubricant laxative MOA
ex. mineral oil
used to prevent straining in high-risk patients (post surgery, CVA, hernia, hemorrhoids)
Lubricant laxative contraindications
-contraindicated in Elderly, children, and bedbound (increased risk aspiration)
-rectal seepage in large amounts
-will impair absorption of fat soluble vitamins and warfarin
Chloride Channel Activator MOA
One drug currently: lubiprostone (Amitiza).
-used for chronic constipation prone IBS
-MOA unknown: enhances chloride-rich intestinal fluid to pull water into intestine.
Chloride Channel Activator contraindications
contraindicated in pregnant women and children, mechanical obstruction
no interactions
Guanylate Cyclase-C Agonist MOA
used for chronic idiopathic constipation (CIC) or IBS
-Increases intracellular cGMP which stimulates secretion of chloride and bicarb into the intestinal lumen to increase stool transit time
Guanylate Cyclase-C Agonist contraindications
-contraindicated in Children < 6 years
-Bowel obstruction
-no other interactions
Peripherally Acting Mu-opioid Receptor Antagonist MOA
**used for opioid induced constipation
(contains same ingredients as naloxone)
-Blocks opioid binding to the mu receptor
Peripherally Acting Mu-opioid Receptor Antagonist contraindicaions
contraindicated in suspected GI obstruction or potential for GI perforation
-Some patients may experience opioid withdrawal
interacts with other meds metabolized by CYP3A4
or other opioid antagonists
Serotonin-4 Receptor Agonist MOA
only one left due complications
GI pro kinetic agent
Serotonin-4 Receptor Agonist contraindications
-Contraindicated in mechanical obstruction or hypersensitivity
-works similar to ssri; Monitor for suicidal ideation, self-injurious ideation, and new onset or worsening depression
first line for constipation?
TLCs >>>then bulk forming lax as first choice
ex. psyllium (Metamucil® or fibercon
dry stool or straining? stool softener or glycerin syrup
second line for constipation?
hyper osmotic ex. miralax
(if contraindicated? saline/ osmotic laxative)
third line for constipation?
A stimulant ex. senna
*remember high potential for abuse
-mineral oil for those who need to avoid straining
travelers diarrhea treatment
prophylactic agents used: Pepto-Bismol--2 tabs with meals and bedtime.
Empiric agents: floroquinolone at sx onset.
Diarrhea lasting 2-4 weeks without sx
they might have giardia
-metronidazole for empiric anti-Giardia therapy
Anti-motility Agents MOA
ex. loperamide (Imodium), diphenoxylate with atropine (Lomotil)
-derivative of an opioid;
Slows GI motility by effecting intestinal musculature and increases transit time for an increased absorption of water.
-atropine prevents euphoric/analgesic
Anti-motility Agents contraindication
-exacerbates infectious diarrhea
-not recommended for kids under 4
-atropine side effects
-Diphenoxylate may potentiate CNS depression.
(drowsiness/dizziness)
-loperamide has high first pass effect--caution in liver failure
Atypical Antidiarrheals MOA
ex. pepto, kaopectate
-Antisecretory, antimicrobial, and adsorbent properties
-best for travelers diarrhea
Atypical Antidiarrheals contraindication
Contains salicylate: caution ASA sensitivity or therapy
-Do not use in children with viral infection due to Reyes Syndrome
AE: black stools, black tongue, tinnitus
Adsorbents
ex . Kaolin, pectin (Kaopectate) attapulgite (Donnagel),
Adsorbs or holds water and solidify stools.
Absorbents
ex. Polycarbophil (FiberCon, Fiberall)
Absorbs water in GI tract
may absorb nutrients and other meds
Semisynthetic Antibiotic MOA
ex. rifaximin
-Suppresses diarrhea by altering the growth of the bacteria and is effective against non invasive strains of ECOLI
Semisynthetic Antibiotic contraindications
-Peripheral edema, nausea, dizziness, fatigue, muscle spasms
-Post marketing effects: exfoliative dermatitis, rash, angioneurotic edema, urticaria
first line diarrhea
TLCs (brat diet, decrease fiber, lactose, and gluten) and diet >> if not then loperamide
second line diarrhea
Adsorbent or bismuth subsalicylate:
**do not use bismuth with flu in those under 18. bismuth is main ingredient in pepto
third line for diarrhea
diphenoxylate with atropine (lomotil)
common side effects of anti consitpation meds
-Gi upset
-Diarrhea
-Nausea
-Cramps
-Bloating
flatulance
dehydration
causes of GERD
-Transient Lower esophageal spincter relaxation
-Abdominal strain from increased gastric volume or pressure
-Hiatel hernia
-Impaired esophageal defense mechanisms
-Motility Abnormalities
Treatments for GERD
diet
sleeping with HOB raise
antacids
H2 receptors blockers
PPIs
two main causes of PUD
-infection from H pylori
-long tern NSAIDS use
PUD pharmaceutical treatment
Treatment of H. pylori = 2 antibiotics + mucus protection
ex . Clarithromycin + Amoxicillin OR Metronidazole + Tetracycline
Mucosa Protectants
-H2 Receptor Antagonists
-Proton Pump Inhibitors
-Bismuth Subsalicylate
-Antacids
-Sucralfate
-Misoprostol
H2 receptor antagonists MOA
ex. (-tidine) famotidine (Pepcid)
Suppress gastric acid and pepsin secretion by competitively and reversibly binding H2 receptors
H2 receptor antagonists contraindications
AE: blood dyscrasias, bradycardia, confusion
Interactions: warfarin, phenytoin, theophylline
Proton pump inhibitors MOA
ex. (-prazole) omeprazole (Prilosec)--OTC
-lansoprazole (Prevacid)--OTC
-pantoprazole (Protonix)--IV
-Bind to the proton pump of parietal cell to block secretion of hydrogen into gastric lumen
-Inhibits acid production; relieves pain; heals ulcers
**more rapid then H2 blockers
Proton pump inhibitors contraindications
Take 30-60 mins before meal
AE: Diarrhea/constipation, headache, Abd pain
AE w/ Long-term use: hypergastrinemia, fractures, c. diff colitis, bacterial enteritis, Vitamin B12 deficiency, hypomagnesemia
high risk groups for DM
hispanic, black, and alaskan native
4 major classifications of diabetes
type 1 - insulin dependent
type 2 - non insulin dependent (most common)
gestational - occurs during pregnancy
diabetes secondary- secondary to other conditions like pancreatic disease, long term steroids, hormonal abnormalities
type 1 cause
genetic predisposition or autoimmune response
type 2 cause
pancreas produces less insulin than body needs OR
adipose and muscle cells become less sensitive to insulin
type 3 cause
pregnancy cause the woman to become intolerant to glucose
type 2 risk factors
pathogenesis or (manor of development )of DM 2
•Insulin resistance
•Impaired insulin secretion
•Elevated glucose production by the liver
Main symptoms of DM?
•Polyuria (excessive urination)
•Polydipsia (increased thirst)
•Weight loss
•Polyphagia (increased hunger and caloric intake)
•Blurred vision
DM criteria
if A1C is greater than or equal to 6.5= DM diagnosis
Fasting glucose greater than 126= DM diagnosis
random glucose greater than 200= DM dianosis
Effective treatment programs for DM
•Self-monitoring blood glucose (SMBG)
•Medical nutrition therapy; regular exercise
•Drug therapy individualized for each patient
•Oral glucose-lowering agents for some type 2 patients
•Instruction in the prevention and treatment of acute and chronic complications, including hypoglycemia
Goals for drug therapy in DM
ADA = A1C less than 7
ACCE= endocrinologist less than 6.5
Both ADA and ACCE
•Preprandial plasma glucose level 80–130 mg/dL
•Postprandial plasma glucose level <180 mg/dL
Goals for drug therapy in DM (other labs)
DM chart
metformin no longer first line
if CVD risk >> GLP1 recepter agonist or SGLT2
if HF risk>>> SGL2 ; avoid Thiazolidinediones
if CKD>>> SGLT2; make sure on ace or arb
Therapy chosen due to treatment goals: glucose lowering efficiency, weight loss efficiency, cost and access
What is the drug of choice for DM1 or DM2 with failed oral therapy?
insulin
what are the two ways to use inulin (or the two types of insulin) ?
basal- steady amount (intermediate and long acting)
bolus - short acting
rapid acting insulin
RADID ACTING>>>LISPRO/ aspart (novolog)/ glulisine (apidra)
ONSET less then 30 min
PEAK 30 min -3 hr
DURATION 3-5 hr
short acting insulin
EX HUMULIN R ;NOVALIN R
ONSET 30 min
PEAK 2-4 hr
DURATION 6-8
intermediate acting insulin
NPH (ex. novolin n, humalin n)
ONSET 1-4 hr
PEAK 4-12 hr
DURATION 14-26 hr
long acting insulin
ex. detemir (levemir) glargine (lantus)
ONSET 1-2 hr
PEAK no peak
DURATION 24 hrs
ultra long acting insulin
EX GLARGINE (toujo); degludec (tresiba)
ONSET 30 min-4 hrs
PEAK no peak
DURATION 36-42 hr
combo insulin
•70/30-NPH/regular ratio
•50/50- NPH/regular ratio
•75/25-NPL/lispro ratio
•70/30-NPA/aspart ratio (NOT GOING TO ASK TYPES )
ONSET 5-15 min
PEAK ??
DURATION 10-16 hr
inhalation insulin contraindications
•Acute bronchospasm has been observed in patients with asthma and COPD.
•Contraindicated in patients with chronic lung disease
not recommended for DKA
not recommended for smokers or recent smokers
•Contraindication: Hypoglycemia, COPD, hypersensitivity.
•AE: hypoglycemia, cough, throat pain or irritation, headache.
inhalation insulin types
ex Afrezza-brand name (inhalation powder)
•a form of Rapid acting insulin
•used for Type 1 and Type 2
•Preprandial dosing; use before meals
recommendations for type 1
basal+ rapid acting
or combo intermediate + short acting
.4-.5 per units day (weight based)
recommendations for type 2
start on basal insulin
sensitizers- biguanides MOA
ex. metformin (Fortamet and Glumetza)
•Inhibits the production of hepatic glucose, reducing intestinal glucose absorption and improving glucose uptake and utilization
•Benefits: do not cause hypoglycemia and does not promote weight gain.
•Can combine with other hypoglycemics.
sensitizers- biguanides contraindications
•Contraindications: Renal dysfunction, *Heart failure, pregnancy
•Stop for 48-72 hrs pre and post radiographic dye studies. Can cause metabolic acidosis.
•AE: GI upset, acidosis. I have seen edema, water retention.
sensitizers- TZDs MOA
ex- piogiltazone or rosiglitazone
MOA: increase insulin sensitivity in skeletal muscle and fat
sensitizers- TZDs contraindications
-liver function tests are a MUST
-stop if liver function tests are 3x then normal
•Hypoglycemia when used with insulin or sulfonylureas
•AE: reduce oral contraceptives, increased plasma volume, weight gain
•Can cause or worsen HF
•Increased risk of bladder cancer
secretagogues two types
sulfonylureas and meglintinides
Note 
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