Octreotide, Loperamide, Creon, URSO, Ribavirin, Rifaximin, Hemorrhoid agents Flashcards
Octreotide class?
Sandostatin
Octreotide sub-class?
diarhea, other endocrine / metabolism
What is Octreotide?
Man-made protein that is similar to a natural hormone in the body called somatostatin
Octreotide MOA?
Somatostatin antagonist
inhibits multiple hormones including growth hormone, glucagon, insulin, LH, and vasoactive intestinal polypeptide (VIP)
Octreotide MOA cont..?
Reduce blood flow
Inhibit gastric acid secretion
May have gastric cytoprotective effects
Indications for Octreotide?
Management of variceal bleeding
Used as adjunctive therapy before endoscopy, or when endoscopy is unsuccessful, contraindicated, or unavailable
Also used for acromegaly, carcinod tumor symptoms, diarrhea
Octreotide pharmacokinetics?
Metabolized liver CYP450
Half-life 1-2 hrs (increased by age, liver disease) cirrhosis
Octreotide cautions and interactions that must be considered?
Hepatic, Renal, Biliary disease
Arrhythmias, HTN, CHF exacerbation
Diabetics – hyperglycemia (endocrine and VIP actions)
Many drug-drug interactions
Octreotide pregnancy cat?
B
Octreotide facts?
Means to help stabilize patients before definitive therapy can be performed
Given IV 50mcg/hr
Unknown lactation
Peds with close monitoring
loperamide (Imodium) Class?
Anti-diarrheal’s
Opiate
Indictions for loperamide (Imodium) ?
diarrhea
loperamide (Imodium) MOA?
Inhibits peristalsis by direct effect on circular and longitudinal muscles of the intestinal wall
Increases viscosity and bulk
Diminishes loss of fluid and electrolytes
Increases sphincter tone
No analgesic opioid effect
Anticholinergic effects
**low K you need to check magnesium level , K based medications watch drug interactions *
loperamide (Imodium) dosing?
2 mg PO per dose
Start: 4 mg PO x1, then 2 mg PO after each loose stool; Max: 16 mg/day
Peds dosing by age
loperamide (Imodium) Pharmacokinetics?
Metabolized by Liver CYP450
Half-life 10 hr
loperamide (Imodium) interactions and cautions?
Toxic megacolon / paralytic ileus
Avoid with potassium based
drugs
Many drug-drug interactions
loperamide (Imodium) pregnancy cat?
C
loperamide (Imodium) special populations?
Lactation probably safe
Monitor in lever disease – toxicity
Peds dosing based on age parameters over 2 years old
Drugs Treating Pancreatic Insufficiency?
Pancrelipase (Creon, Pancreaze)
Pancrelipase (Creon, Pancreaze)
class?
Digestive Enzymes
pancreatic enzyme replacement products (PERPs)
Pancrelipase (Creon, Pancreaze) MOA?
commercial mixture of pig-derived pancreatic amylase, lipase and chymotrypsin
Pills disintegrate into trypsin, amylase, and lipase, which break down proteins, carbohydrates, and fats
Pancrelipase (Creon, Pancreaze) indications?
Exocrine pancreatic insufficiency
Chronic pancreatitis
Cystic fibrosis have increased incidence of pancreatic insufficiency
Pancrelipase (Creon, Pancreaze) story?
Along with food, the CREON capsule enters the stomach.
Capsule releases enteric-coated spheres sized between 0.7 and 1.6 mm in diameter.
Enteric coating allows the spheres to travel beyond the low pH of the stomach through the pylorus, releasing enzymes into the small intestine at a pH ≥5.5.
CREON enteric-coated spheres dissolve in the small intestine, releasing pancreatic enzymes to mix with food.
CREON replaces enzymes missing in patients with EPI. In the small intestine, these enzymes work to break down fats, proteins, and carbohydrates in food.
Pancrelipase (Creon, Pancreaze) dosing?
Dosing
500-2500 lipase units/kg PO w/ meals/snacks
Peds dosing by age / weight
Pancrelipase (Creon, Pancreaze) pharmacokinetics?
Metabolized in GI tract, minimal systemic
Half-life unknown
Pancrelipase (Creon, Pancreaze) interactions and cautions?
Pork allergy (Porkinetics aka Prokenetics)
Gastric pH sensitive ( voided by concomitant use acid reducers)
Caution with Gout, Renal Dz, Crohns Dz
pancrelipase (Creon, Pancreaze) pregnancy cat?
C
pancrelipase (Creon, Pancreaze) special populations?
Lactation safety unknown
Peds dosing by age including infants
Ursodiol (Urso 250) class?
Hepatobiliary
Ursodiol (Urso 250) MOA?
decreases cholesterol synthesis, secretion, and absorption
alters bile cholesterol composition (dissolve gallstones)
Indications for using Ursodiol (Urso 250)?
primary biliary cirrhosis
steatohepatitis, non-alcoholic
primary sclerosing cholangitis
Ursodiol (Urso 250) dosing?
Primary biliary / sclerosing cirrhosis
Steatohepatitis (non-alcoholic)
Pharmacokinetics for Ursodiol (Urso 250)?
Metabolized by liver CYP450
Half-life unknown
Ursodiol (Urso 250) interactions and cautions?
jaundice
LFTs elevated
leukopenia
thrombocytopenia
Ursodiol (Urso 250) pregnancy category?
B
Ursodiol (Urso 250) special populations?
Pregnancy Cat. B
Lactation unknown
Ped’s not available
Treatment of HCV Infection?
Ribavirin (RBV, Rebetol)
Ribavirin (RBV, Rebetol)
MOA?
Inhibits viral RNA polymerase inhibiting protein synthesis
Combined with interferon therapy
Not for monotherapy
Ribavirin is often combined with ?
interferon therapy
Not for monotherapy
BBW for Ribavirin (RBV, Rebetol)?
Hemolytic anemia
May worsen cardiac disease
teratogenic
Ribavirin (RBV, Rebetol)
pharmacokinetics?
Metabolized CYP450
_________ must be used together with an_______________(such as Pegasys, PegIntron, Sylatron, or Intron A) to treat chronic hepatitis C.
Ribavirin
interferon alfa product
Ribavirin (RBV, Rebetol)
for HCV information?
Dose: 400-700 mg PO bid
dose may depend on wt;
AASLD/IDSA hepatitis C guidelines
Give w/ food
peginterferon alfa 2a combo
Caution with pts w/ CrCl <30
Refer to AASLD/IDSA hepatitis C guidelines
Rifaximin (Xifaxan) class?
anti-diarrheal, other antibacterial
Rifaximin (Xifaxan) MOA?
bacteriostatic; inhibits DNA-dependent RNA polymerase
Indications to use Rifaximin (Xifaxan) ?
Travelers diarrhea, E. coli-induced
IBS, diarrhea-predominant
Pharmacokinetics of Rifaximin (Xifaxan) ?
Liver CYP450
Half-life 6 hr
Interactions and cautions that use be considered if using Rifaximin ( Xifaxam)?
C. difficile-assoc. diarrhea (optional)
Superinfection
peripheral edema
Nausea, dizziness, fatigue, ascites, headache, muscle spasms, pruritus, abdominal pain
*can create another suer infection in the gut *
Rifaximin (Xifaxan) pregnancy category?
Avoid 1st trimester otherwise probably safe
Lactation unknown
Hemorrhoid Care medication example?
Anusol
What form does Anusol come in?
creams, ointments, and the suppository form
Active ingredient in Anusol ointment and suppositories is __________________.
zinc sulfate monohydrate
Anusol plus is zinc sulfate monohydrate and pramoxine HCL which is _________
antipruritic
Anusol HC suppositories?
added steroid
hydrocortisone/ lidocaine topical dose for hemorrhoid care?
Dosage forms: 0.5%/3%,1%/3% crm; 2.5%/3% gel