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Oral Diabetes Basic
Basics of oral medication classes, names, precautions, and actions
| Question | Answer |
|---|---|
| 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
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