502 meds review

Levothyroxine

severe symptoms: 50-125mcg/day

older, smaller, more risk for hyperthyroid: 12.5-25 mcg/day

weight based dosing: 1mcg/kg/day

recheck every 4-8 weeks: adjust by 12.525mcg based on TSH rechecks

maintenance dose (Young adults): 130mcg/day

elderly: 110mcg/day

Levothyroxine

100mcg

Liothyronine Sodium

25 mcg

Liotrix

50 mcg/12.5 mcg

Thyroglobulin

65 mg

Desiccated thyroid

60-65 mg

Hypercortisolism (Ketoconazole)

600-800mg/day

-strong CYP3A4, 2C9, P-gp inhibitor

Hypercortisolism (Metyrapone)

750-1000mg/day BID or QID

-not mono therapy, used in combination with other inhibitors

-quick onset

Hypercortisolism (Mitotane)

1-2g/day BID or QID

-monitor urinary free cortisol, adjust as needed

Hypercortisolism (Pasireotide)

600-900mcg SUBQ BID

-50% see reduction of urinary free cortisol at 6 months

Hypercortisolism (Mifepristone)

300-1200mg daily

-symptomatic treatment only

Hyperaldosteronism (Spironolactone)

Initial: 25mg/day

Max: 400mg

--sex steroid effects; gynecomastia, impotence, menstrual irregularities

Hyperaldosteronism (Eplerenone)

initial: 50mg/day

max: 300 mg

Hyperaldosteronism (Amiloride)

Initial: 5mg BID

Max: 15 mg

-less effective than spironolactone/epleronone for BP control

Adrenal Insufficiency (Fludrocortisone acetate)

0.05mg-2mg daily

-for 1st degree adrenal insufficiency

-adjust dose q6-8 weeks based on BP, peripheral edema, electrolyte levels

Adrenal Insufficiency (hydrocortisone)

15-25 mg daily

-give 2/3 dose in AM, 1/3 6-8hrs later

-also tid dosing (wake,bkfst, evening meal)

Adrenal Insufficiency (Cortisone acetate)

20-35 mg daily

-give 2/3 dose in AM, 1/3 6-8hrs later

Adrenal Insufficiency (Prednisolone)

-alt for hydrocortisone or cortisone acetate only when once daily dosing is needed

Fast acting Insulin

-Insulin Aspart (Fiasap)

-Insulin Lispro (Lyumjev)

Onset: 15 min

Peak: 60 min

duration: 3-5 hrs

Dosed at the beginning of meal or within 20 mins after starting meal

Rapid Acting Insulin

Aspart (Novolog)

Glulisine (Apidra)

Lispro (Humalog/Admelog)

Onset: 15 min

Peak: 30-90 min

Duration: 3-5hrs

-admin immediately prior to meals

-minimize PP hyperglycemia and allow for rapid correction

-mealtime coverage insulins

Short Acting Insulins

Regular (Humulin R or Novolin R)

Onset: 30-60 min

Peak: 2-4 hrs

Duration: 5-8hrs

Humulin R U-500

Onset: 15 mins

Peak: 4-8hrs

Duration: 21 hrs

-used BID/TID, 30 mins before meals

-more concentrated insulin for patients requiring 200+u/day

Intermediate Acting insulin

NPH (Humulin N or Novolin N)

onset: 1-3hrs

peak: 8 hrs (4-10hrs)

Duration: 12-16 hrs

-background option, dose BID

-Can be mixed with regular/rapid in same syringe

Long/Basal Insulin

Insulin Detemir (Levemir)

Onset: 3-8hrs

Peak: flat

Duration: 20-26 hrs

-dosed qd or bid if elevated pre-dinner BG

-mimics normal pancreatic basal insulin secretion

-reduce risk of nocturnal hypoglycemia

Long/Basal Insulin

Insulin Glargine (Lantus)

(Basaglar, Semglee, Rezvoglar)

onset: 2-4hrs

peak: none

duration: 24 hrs

-QD injection at same time

-basaglar same protien sequence+similar glucose lowering effects

-do not mix with other insulin in same syringe

MOA: injection of acidic solution and precipitation of glargine in SC tissue—>slow dissolution of precipitates prolong action

Ultra Long insulin

Insulin Glargine (Toujeo)

onset: 6hrs

peak: none

duration: 36 hrs

-small injection volume compared to lantus

-duration is >24 h when taken at same time

-do not mix with other insulin in same syringe

Ultra Long acting insulin

Insulin Degludec (Tresbia)

onset: 90 mins

peak: none

duration: up to 42 hrs

-lower risk of hypoglycemia, allows for flexibility in dosing (true 24hr insulin)

-MOA: slows release from SC depot

-do not mix with other insulin in same syringe

Mixed Insulin

50% lispro protamine/ 50% insulin lispro (HumaLOG Mix 50/50)

75% lispro protamine/25% insulin lispro (HumaLOG Mix 75/25)

70% aspart protamine /30% insulin aspart (NovoLog Mix 70/30)

onset: 5-15 mins

peak: 1-2 hrs

duration: 10-16 hrs

Premixed cont

70% NPH/ 30% Regular (HumuLIN 70/30)

70% NPH/ 30% Regular (Novolin 70/30)

onset: 30-60 mins

peak: 2-10 hrs

duration: 10-16hrs

Premixed Insulin effects

AM: short-acting bolus, regular—>reflected in pre-lunch BG (11A)

AM: intermediate-acting basal, NPH—>reflected in pre-din BG (5P)

PM: short-acting bolus, regular—>reflected in bedtime BG (10P)

PM: intermediate-acting basal, NPH—>reflected in FBG (6A)

GLP-1 Receptor Agonists

-used for weight loss

-pts with established or increased risk of CV or renal complications

-can be used for pts who need lower glucose effects—>GLP 1s preferred prior to insulin

-MOA: delay gastric emptying, enhance glucose-dependent insulin secretion by pancreatic B cells

-SC injection except oral semaglutide (Oral: 3mg/day, 30 min before first meal/beverage with no more than 4 oz of water)

AE: n/v, diarrhea, constipation, injection site reactions, dizziness, hypoglycemia

-precautions: pancreatitis

GLP-1 Receptor Agonists Meds

Short Acting

-Exenatide (Byetta): 5-10 mcg BID

-Lixisenatide (Adlyxin): 10-20 mcg/day

(avoid in very low GFR, no CV benefit)

Long Acting

Exenatide XR (Bydureon): 2mg/week

Liraglutide (Victoza): 0.6-1.8 mg/day (CV indication)

Dulaglutide (trulicity): 0.75-4.5mg/week (CV indication)

Semaglutide (Ozempic): 0.25-1mg/week (CV indication)

Amylin Analogs

-reduce PP glucagon secretion—>suppression hepatic glucose output

-regulation gastric emptying—>control rate of nutrient delivery to SI

-reduction in food intake which controls reduction of exogenous glucose entering circulation

-may delay absorption of oral meds due to slow gastric emptying (admin 1hr prior or 2hrs after)

-do not mix with insulin

Amylin meds

Pramlintide

T2DM: reduce mealtime insulin by 50%, start 60 mcg SC ASAP before meals

increase dose from 60mcg to 120 mcg if no nausea for 3 days

T1DM: reduce mealtime insulin dose 50% start 15 mcg before meals

titrate up in 15mcg increments to max 60mcg if tolerated

Metformin (Buguanide)

-insulin sensitizer: improves target cell response to liver and peripheral tissues (pushes out more insulin)

-AMPK activators

-best candiate for newly diagnosed hyperglycemia without contraindications

-reduces A1C 1-2% and reduces FBG 50-70mg/dL

AE: diarrhea, N/V, flatulence, malabsorption, heartburn, taste distrubance, lack of energy, LACTIC ACIDOSIS (RARE)

Metformin Dosing

start 500mg once daily w/food

-adjustment: may be titrated weekly as tolerable—>titrate to BID or TID

MAX doses:

10-16yo: 2000mg/day

IR: 2550/day, XR: 2000mg/day

if eGFR 45-60: 1500mg/day

-not rec for moderate to severe renal impairment (eGFR<45), unstable/acute CHF, liver disease

SGLT-2 Inhibitors (gliflozin)

-blocks reabsorption of glucose in kidney

-best used for people who have CV risks

-not for people who have renal impairment, severe hepatic impairment, pt with recurrent genital fungal infections or UTIs, pregnant in 2nd/3rd trimester

-can be used for weight loss

AEs: UTIs, bladder cancer, dehydration, increased urination, Fourniers Gangrene, ketoacidosis, lower limb amputation

SGLT2-Inhibitor meds

Canagliflozin (Invokana): 100mg/day—>not for ESRD (1)

Dapagliflozin (Farxiga): 5mg/day—>used in HF, not for ESRD (2)

Empagliflozin(Jardiance): 10mg/day—>used in HF(1)

Etrugliflozin (Steglatro): 5mg/day

DPP4i (glipton)

MOA: enhances incretin system by inhibiting DPP4 (inactivates the incretin hormone)

-Best used for ESRD and renal insufficiency

-not for pts with HF, pts at risk for pancreatitis, pts on antivirals

-reduces A1C by .5-1%, FBG 20-40mg/dL, PPg 40-50 mg/dL

-AE: HA, upper respiratory infection, nasopharyngitis, immune defects with long term use

DPP4i meds

sitagliptin (Januvia): 100mg/day

saxagliptin (Onglyza): 2.5-5mg/day—>increase in HF risk

linaglipton (Tradjenta): 5mg/day—>no dose adjustment needed

alogliptin (Nesina): 25mg/day—>increase in HF risk

(for all dosing, reduce dose by ½ based on eGFR)

TZDs (glitazone)

MOA: enhance glucose uptake, insulin sensitizer (acts on fat and liver cells)→full effect seen in 12 weeks, PPARy agonist: active of PPARy to activate insulin-responsive genes that regulate carb and lipid metabolism

-Medchem: liver toxicity may be associated with reactive quinone metabolite oxdizied by CYP2C8 and CYP3A4

-best used for pts who have A1C less than 8% (need for combination)

-not for pts who have HF, liver disease/hepatic impairment, pregnancy

-reduce A1C by .5-1%, FBG 30-60mg/dL

AE: edema, weight gain, increase in bone fracture risk, bladder cancer, delayed clinical onset (2-4 weeks, full effect at 12 wks)

TZD meds

pioglitazone (Actos): 15-45mg/day

rosiglitazone(Avandia): 4mg/day

Sulfonylureas

-MOA: stimulate insulin secretion, need existing B cells→reduce glucose output from liver and improve insulin sensitivity

-K ATP channel modulators:block ATP sensitive channel on B cells by binding to SURI→membrane depolarization and opening of Ca channel to promote insulin secretion

-best used for recent diagnosis, added to metformin, awareness of hypoglycemia symptoms

-not for pts who have renal/aderenal/pituitary insufficiency (same meglitinides)

-can use glipizide 1mg for renal insufficiency

AE:hypoglycemia, dizziness, GI upset\

-can cause weight gain for both insulin secretagogues

Sulfonylurea meds

QD-BID with breakfest

glipizide (Glucotrol): 5mg→IR: 30m b4 food

glyburide: 1.5-5mg→NR renal impairment

glimepiride (Amaryl): 1-2mg

Meglitinides

TID 30 min before meals

-Repaglinide (Prandin): 0.5-2mg

-Nateglinide (Starlix): 60-120 mg

-not for severe renal/hepatic impairment, can be used in mild/moderate renal insufficiency

Alpha glucosidase Inhibitors

MOA: delayed absorption of glucose

-best used for pts with high PPG

-not for pts with GI disease, liver/hepatic disease

-reduce A1C 0.5-1%, FBG 20-40mg/dL, PPG 40-70mg/dL

-AE: GI upset

cons: TID dosing, slow titration

increase hypoglycemia: glyburide, glipizide

Alpha glucosidase Inhibitors meds

Acarbose (Precose): 25-50mg

Miglitol (Glyset): 25-50 mg

slow titration due to GI SE

Semaglutide (Rybelsus) GLP1 receptor agonist

Dose: 3mg QD for 30 days→increase to 7mg QD (Max: 14 mg/day)

counseling: admin 30 min before first meal/beverage with no more than 4oz of water, swallow tablets whole

AE: GI upset

Methimazole

-more potent than PTU, longer ½ life preferred

-PTU preferred in 1st trimester of pregnancy

Dose: 15-60 mg/day divided TID (initial), 5-15mg/day divided 1-3xday

HYPERTHYROIDISM

PTU

MOA: inhibits peripheral T4→T3 conversion

-half life is only an 1hr, preferred in 1st trimester of pregnancy

Dosage: 100-200mg TID (initial), 50-100mg TID (maintence)

HYPERTHYROIDISM

-inhibit type I5’ deiodinase (catalyzes T4→T3)

Complex Anions

Perchlorate (CLO4-) and Pertechentate (TcO4-)

-compete with I- for symporter→inhibit I- uptake

-used as prep for surgery

Lamivudine

-reverse transcriptase inhibitor

-HBV DNA polymerase has reverse transcriptase activity

Entecavir

-originally developed for treatment of herpes simplex

-inhibits three distinct phases of HBV DNA polymerase: HBV DNA polymerase priming, reverse transcription, synthesis of the positive stranded HBV DNA

Tenofovir alafenamide

-has a bulky group attached to protect the phosphate, it is eventually cleaved off to protect the phosphate group

-the phosphate group then becomes active and is very potent (ProDrug like)

-the dose is 25mg in comparison to tenofovir disproxil fumarate dose of 300mg

-lowers serum con which results in fewer SE

NS3/4A Protease Inhibitor

-previr

NS5A Complex Inhibitor

-asvir

NS5B Polymerase Inhibitor

-buvir

Sofosbuvir

-HCV NS5B polymerase inhibitor

-uridine nucleotide analogue, alternative substrate inhibitor

-uses protide technology→prodrug to deliver a nucleotide phosphate into the liver

-active metabolite→triphosphate made by nucleoside kinases in liver

Bulk Laxatives

-increase in bowel content volume triggers stretch receptors in the intestinal wall

-causes reflex contraction (peristalsis) that propels the bowel content forward

-soaks up water in gut, makes poop softer, helps push it out easier

Psyllium (Metamucil)

Saline and Osmotic Laxatives

-effective in 1-3 hours

-used to purge intestine

-fluid is drawn into the bowel by osmotic force, increasing volume and triggering peristalsis

Salts: Milk of Magnesia

Polyethylene glycol

Non-digestible sugars and alcohols: Lactulose

Osmotic Laxatives

-nonabsorabable sugars:sorbital and and mannitol

-PEG

MOA:accumulate water in fluid

AR: flatulence and cramps, N/V

Emollient Laxatives

-Docusate sodium (Colace)

-MOA: stool softener by incorporating water into fatty fecal matter, softens feces in 1-3days

AR: Nausea and abdominal cramping

Irritant/Stimulant laxatives

-increase GI motility

-irritate the GI mucosa and pull water into lumen

-indicated for severe constipation

Castor oil

Senna

Bisacodyl (Dulcolax)

Lubiprostone-PGE1 derivative that stimulates chloride channels, producing chloride rich secretions

What are first line laxative treatments?

-Osmotic or stimulant

Lubiprostone (Amitiza)

-chloride channel activator

MOA:activates Cl- channels in gut, increases liquid secretion into intestines, shortens intestinal transit time

-used for chronic constipation

Linaclotide (Linzess)

MOA: binds to guanylate cyclase C receptor on intestinal enterocytes in gut, activates cystic fibrosis transmembrane conductance channel, stimulates intestinal fluid secretion

-used for chronic constipation

Anti-motility agents

-reduce peristalsis by stimulating opioid receptors in the bowel

-allows for more water to be absorbed by the gut

Loperamide

-peripherally acting opioid, first line therapy

-non sedating, non addictive

-safe to use when pregnant and lactation

-taken prn, 1-2mg after bowel movement up to 16mg/day

Bismuth subsalicylate

Pepto-Bismol

Bismuth subcarbonate

MOA: antibacterial, bismuth subsalicylate inhibits formation of prostaglandins producing diarrhea (anti-diarrheal drug)

AR: Nausea, bitter taste, black hairy tongue/ dark stool

Contraindications for antidiarrheals

-dont take when sick

-dont give Imodium to pts who have hypersensitivity to loperamide hydrochloride or other excipients

-dont give imodium to pts with abdominal pain in absence of diarrhea

-dont give imodium to infants below 24 months

-dont overuse as it can cause fast/irregular heartbeat or death

Clostridium difficile

-The major cause of diarrhea and colitis in patients exposed to antibiotics

Clostridium difficile treatment

-discontinue offending antibiotic

-fecal transfer

-metronidazole (dont give in pts with liver or renal impairment)

-vancomycin (contraindicated in pts with renal impairment)

Antiemetic Therapeutics

Musarinic M1 receptor antagonist: Scopolamine

MOA: blocks acetylcholine receptor (transdermal patch)

SE: dry mouth, dizziness, restlessness, allergic rxn, delirium at high doses

Contraindications: kidney or liver disease, enlarged prostate, difficulty in urination, heart disease, glaucoma

Phenothiazines

promethazine (Phenergan-antihistamine)

prochlorperazine (Compazine-D2 blocker)

dimenhydrinate (Dramamine-antihistamine)

SE: typical antipsychotics, blurred vision, dry mouth, dizziness, seizures

Contraindications: allergy to phenthiazines, glaucoma, liver disease, prostate/bladder problems

-histamine H1/Dopamine D2 receptor agonist

-these meds can help inhibit vomiting

Serotonin 5-HT3 receptor agonist

Ondansetron

Granisetron

-great for chemotherapy induced n/v (can be given before chemo)

SE: usually well tolerated, headache, constipation