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Oral Diabetes Basic

Basics of oral medication classes, names, precautions, and actions

QuestionAnswer
TZD drug on market Actos (pioglitazone)
TZD not on market Avandia (rosiglitazone)
TZD mechanism of action increase sensitivity/use of insulin in peripheral muscle cells, possible adipose and liver tissues (has them open up and use glucose). Decrease hepatic glucose output.
Drugs that cause weight gain TZD's (Actos, Avandia), sulfonylurias, meglitiides slightly (Prandin, Starlix)
Drugs that are weight neutral (or may benefit slight w/l) biguanides (metformin), DPP4 inhibitors (Januvia, Ongylza,Tradjenta), dopamine receptor agonists? (bromocriptine mesylate/Cyclocet), alpha-glucosidase inhibitors
Avandia, Avandamet, Avandaryl reason off market increased risk of CVD and MI/risk of death from MI
New concern for Actos bladder cancer risk, banned in some of Europe
meglitinides (drugs) Prandin (repaglinide), Starlix (nateglinide)
Drugs that primarily help postprandials meglitinies (Prandin, Starlix), alpha-glucosidase inhibitors (Precose/acarbos, Glycet/miglitol), dopamine receptor agonsts
Drugs that you should take RIGHT before you eat meglitinides (Prandin, Starlix), biguanides (metformin), alpha-glucosidase inhibitors
Drugs that you should take w/in 30 min of meal ?
Drugs that can cause hypoglycemia sulfonylurias, meglitinides (Prandin, Starlix)
Pregnancy Category C (don't use in pregnancy, lactation, or kids) meglitinides, TZDs, sulfonylurias EXCEPT glyburide
meglitinides contraindications DM1, DKA, severe infection, surgery, trauma, severe stressors...
meglitinides mechanism of action cause insulin secretion like sulfonylurias, but have a shorter action and are glucose dependent
List drugs in order of hypo risk 1. sulfonylurias (can you distinguish which highest risk?), 2. Prandin?, 3. Starlix
Prandin side effects GI, UR infection, congestion, back pain, hypo
Starlix side effects mild hypo (not severe or nocturnal), dizzyness, slight 2lb weight gain (but not if taking with metformin)
What drugs do you see primary or secondary treatment failure with sulfonylurias, Prandin, (Starlix???)
parameters to watch for in TZD's Transaminases (ALT, ??) Q2 mos 1st year then periodically. Liver disease s/s. Watch for decreased H&H and WBC. Careful for fracture risk. fluid retention & CHF s/s esp if on insulin (edema, SOB, rapid w. gain, s/s HF). Tell doc if muscle aches.
Contraindications for TZD's if ALT >3x UNL, active liver disease, DKA, HD (class III or IV). If liver disease, use with caution can increase hepatic enzymes. CHF. If get jaundice. Active liver disease.
S/S of liver disease abdominal pain, fatigue, n/v, dark urine
It takes several weeks to start working TZD (Actos): might discuss ____ with patient if they are frustrated and want to stop taking it
biguanides drug and action metformin and metformin XL
biguanide action Primary: decrease hepatic glucose production through decreasing gluconeogenesis. Secondary: may also decrease intestinal absorbtion of glucose and increase insulin sensitivity in skeletal muscle
ideal candidtate for metformin as monotherapy lipid problem, insulin resistance, DM2 or pre-DM, elevated fasting BG, overweight
good side effects of metformin (biguanide) slight weight loss (2-5kg), decrease tryglyceride 16%, decrease LDL 8%, decrease total cholesterol 5%, increase HDL 2%
Pregnancy Category B metformin, alpha-glucosidase inhibitors (but not officially approved), glyburide (not other sulfonys, may be suitable if unable other option), dopamine agonistst (avoid if nursing d/t inhibit lactation and increase risk for stroke)
Drugs approved for pregnancy, child, and/or lactation metformin (kids OK, preg OK r/b, not lactation)...
predispositions to lactic acidosis with metformin taking overdose, using with contraindications, hypoxic conditions (COPD, cardiac decline), alcoholism or binges, hepatic dysfunction, DKA, taking drugs for CHF, local or systemic tissue hypoxia
metformin contraindications creatinine >1.5 (1.4 female), abnormal renal function, liver disease, taking CHF meds,
metformin positive side effects weight loss, decreased LDL and tryglycerides, poss decrease MI risk
metformin side effects metallic taste, lactic acidosis, decreased vitamin B12 (without anemia reported), GI (bloating, nausea, cramping, fullness, diarrhea 30%)
what helps decrease GI metformin effects usually self limiting 1-2 weeks.slow titration. take with meals.
when to temp hold metformin before IV contrast dye and until creatinine back to normal (hospital 48h), situations predisposing acute renal dysfunction or tissue hypoperfusion (acute MI, acute CHF exacerbation, major surgery)
older people and metformin if >80 first do 24 hour creatinine clearance; GFR baseline and periodically
alpha glucosidase inhibitor drugs acarbose (Precose), miglitol (Glyset)
alpha glucosidase inhibitors action inhibits enzymes in brush border of small intestine & pancreatic alpha-amylase --> slows carb absorption in gut so decreased carb-mediated postprandial BG. Get all nutrients just takes longer. In colon, broken down by bacteria. helps postP more than FBG
side effects of alpha glucosidase inhibitors decreased CV risk, minimal systemic absorption so good safety profile; GI (mostly at start, self-limiting, diarrhea, abd pain, flatulance 80%, increased liver enzymes (AST, ALT at doses 200-300mg/day)
alpha glucosidase inhibitors contraindications DKA, IBS, ulcers, obstructive bowel disorders, chronic intestine disorders, partial or predispose to intestine obstruction, cirrhosis, increased liver enzymes, not recc if creatinine >2 or Crt. Clearance <25ml/min
alpha glucosidase inhibitors patient teaching do activity esp. after meal to decrease gas buildup. Treat lows with lactose or glucose only (if taking antihyper too)
alpha glucosidase inhibitor monitoring monitor liver function for elevation of liver enzymes serum transamines AST and ALT (every 3 months 1st year then periodically), watch for renal function
sulfonylurea action secretagogues, release insulin from beta cells (must still have sufficient beta cell function to work), hypoglycemic agent
2nd generation sulfonylurea drugs glyburide, glipizide, glipizide XR, glimepiride
glimepiride advantages often only need once daily vs. twice daily in most others in class
glipizide XR advantages often only need once daily vs. twice daily of most others in class
sulfonyluria monitoring baseline renal and hepatic function...
what drugs have biliary excretion glyburide, slightly with glipizide...
sulfonyluria chlorpropamide precautions (1st gen) excreted unchanged in urine, SIADH/met disorder with hypNA and hypervolemia =. very long duration in elderly/renal disease (72h), watch for hypo. Alcohol antebuse flushing reaction with alcohol use
sulfonyluria tolbutamide and chlorrpropamide precautions (1st gen) abnormal hepatic function tests, thrombocytopenia, agranulocytosis, hemolytic anemia (very rare in 2nd gen)
what drugs shouldnt you use with alcohol metformin (a lot), 1st generation sulfonyluria chlorpropamide
2nd gen sulfonyluria s/e & precautions more hypo risk w/ hepatic & renal impairment, older, malnourished, irreg eating. rash (usually resolves), sun sensitivity, n/v, weight gain (2* to insulin secretion), mild GI disturbances; blood problems and met disorder s/e very rare compare to 1st gen
which drugs cause GI side effects? sulfonylurias (mild), dopamine agonists....
sulfonyluria (2nd gen) monitoring most hypo risk: elderly, debilitated, malnourished, adrenal/pituitary/hepatic insuff, renal probs. if hypersensitivity reaction, not NECC mean allergic to sulfa drugs (sulfonamides) but precaution. Daily + BG mtr, preprandial and bed usually
sulfonyluria failure Monitor for 1* 2* failure. 20% no response, 2* follow soon after (5010% ppl). over time most have failure as disease prog. less effective if first phase insulin release impairment --> use different drug class not meglitinide
sulfonyluria contras toxiciity rare by: DKA, altered BG control with infection/sx/trauma/severe met stressors dont use if DKA, DM1, allergy/hypersensitivity
sulfonyluria organ caution metabolized in liver and excreted in kidneys so be careful
first generation sulfonylurias overall rapid acting, intermediate acting, and long acting based on onset and duration (daily-3x/day). lots of s/e. Long duration esp increase hypo risk. Dymelor, Diabinese, Tolinase, Orinase
Pregnancy category C explanation animal studies show adverse effects but no controlled studies in humans OR human studies and mice studies not avail; give only if pot ben justifies pot risk
Pregnancy category B explanation animal studies couldnt prove fetal risk but no human studies OR animal lack of effects not duplicated/confirmed in controlled studies in humans first trimester
Pregnancy Category A explanation human studies fail to demonstrate first trimester fetal risk, poss of harm remote (and no evidence of risk later)
dopamine agonist action and drug bromocryptine mesylate (Cyclocet). unknown action. decreases postprandial BG without increasing plasma insulin concentrations.
drugs that decrease CVD risk ...
dopamine agonist side effects somnolence, n/v, fatigue, dizzy, headache watch for hypotension and syncope esp. when starting and increasing dose, hx of orthos, or taking HTN meds. females have 18-30% greater plasma concentrations than males of drug
dopamine agonists contras hypersensitivity to ergot related drugs, syncope migraines (decreases risk of hypotension), DKA/DM1, severe psychotic disorders
ideal candidates for meglitinides can be used in combo, esp if issues with hypos with sulf. no benefit to add meglitinide to sulfony. Shouldnt use on pt with sulfonyluria failure.
Ideal candidate for meglitinide initial monotherapy sufficient insulin production, no lipid prob, renal ok, not overweight, FBG >20 above target, not been treated long term with other oral meds
drugs that decrease A1c by 1-2% sulfonylurias and biguanides
orals that decrease A1c 0.5-1.5% meglitinides (Prandin, Starlix), TZDs (Actos, Avandia)
best candidate for initial monotherapy of alpha glucosidase inhibitors Only mild BG increase. dyslipidemia or obesity, sig. postprandial hyper, not usually monotherapy d/t decreased A1c effect 0.1-0.4 and s/e. Not great with someone with sig premeal hyper w/out much postmeal rise. must have good insulin production
combination drugs with sulfonylurea Avandaryl (no longer on market), Duetact (Actos), Glucovance (met), metaglip
what drug combos have Avandia and thus cant be Rx Avandaryl (glimepiride), Avandamet (metformin)
combo drugs with metformin Actoplus met, Avandamet, Glucovance (with sulf), Metaglip, Janumet
ADA Tier 1 Steps (well validated core therapies): all include lifestyle plus... 1. metformin (may start w/out meds but most need w/in year of dx 2. metformin plus basal OR sulfonyluria (except glyburide or chlorpropamide) 3. metformin plus intense insulin
when to add drugs go to step 2 (adding more than just life and met) if after 2-3 months not at goal. Continue adding every 3 months until at goal. If not at goal after that, change therapy every 6 months
metformin and diabetes progression if started within 3 months of diagnosis, it may preserve beta cell function and delay diabetes progression
Created by: hanalin2