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Glucocorticoids

MOA: Suppress immune system and inflammation by inhibiting chemical mediators such as prostaglandins, histamine, leukotrienes, lymphocytes, phagocytic cells, neutrophils & macrophage 1) stimulate gluconeogensis & glucose secretion by liver 2) increase hepatic sensitivity 3) decrease glucose uptake and utilization by periphal tissue (adipose and muscle) 4) promote glucose storage 5) increase proteolysis and decrease protein synthesis in muscle to support gluconeogenesis activities Administration: PO, IV, IM, SQ, topically, local injection or inhalation (basically any route), but DONT put on open wound -- give in the AM (before 9am) at your bodys natural corticol release time FYIs: Taper dose if extended use or high dose, watch out for growth retardation, remember its an immunosuppressant so watch for infection Pharmacokinetics: crosses placenta. can be in breast milk (and lead to growth retardation) Uses -Rheumatoid Arthritis -Systemic Lupus Erythematosus (SLE) -Inflammatory Bowel Disease -Allergic Reactions -Asthma -Dermatoligic Disorder -Neoplasms -Suppress immune response in transplants -Prevent Respiratory Distress Syndrome Adverse Reactions (usually at high doses and brief when tapered off) -Adrenal insufficiency -Osteoporosis -Infection -Glucose intolerance hyperglycemia -Myopathy (muscle weakness in arms and legs) -Fluid & electrolytce disturbance (minimal) - Retention of water and Na. Decrease in K+ -Growth Retardation -Psychologic Disturbances (hallucinations, mood changes) -Cataracts & Glaucoma -Peptic Ulcer Disease inhibition of prostaglandins, inhbits mucous -Cushings Drugs Short-Acting -Cortisone -Hydrocortisone (high mineralcorticoid activity) Intermediate Acting -Prednisone -Prednisolone -Methylprednisolone -Triameinolone Long Acting -Betamethasone -Dexamethasone

Drug Interactions -Digoxin, thiazide, & loop diuretics glucocorts w/ high mineralcort activity can lead to: HyperNatremia and HypoKalemia -NSAIDS -Insulin & Oral hypoglycemics -Vaccines (can get the viral infect since immune system is suppressed) Contractindications -Systemic fungal infection or living vaccines Cautions -kids, pregos, osteoporosis -HTN, HF, Renal impairment -Esophagitis, PUD -Myasthenia gravis -diuretics, insulin, hypoglycemics

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Mineralocorticoids
MOA: acts on distal tubule Aldosterone = K, Na, H2O -when serum Na is low or K is high, aldosterone levels rise (RAAS system) -Renin is released from kidneys in response to low blood flow, triggers the RAAS system Low Doses mineralocorticoid effect High Doses glucocorticoid activity Pharmacokinetics -quick GI absorbtion (peak at 1.7hrs) -metabolized by liver and excreted by the kidney -crosses placenta and gets into breast milk Uses -Adrenocortical insufficiency (Addisons) -Tx of salt-losing adrenogenital syndrome Adverse Reactions Low Dose -increase in BP High Dose -inhibits endogenous adrenal cortical secretion & pituitary corticotropin excretion -promotes deposition of liver glycogen Drugs Fludrocortisone (Florinef Acetate) -has both high mineralocorticoid and glucocorticoid activity Contraindications -systemic fungal infection Cautions -pregnancy and kids

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Insulin
-Insulin is anabolic (it stores/builds up energy) -Insulin deficiency promotes hyperglycemia in 3 ways: 1) incr. glycogenolysis (glycogen glucose) 2) incr. glyconeogensis (protein/amino acids & lipids glucose) 3) reduced glucose utilization (decr. cell uptake & decr. glucose glycogen) -All insulins clear and colorless except NPH. Discard insulin if it has precipitate -If have to give a short acting & long acting insulin mix the preparations rather than inject them separately. Drug Short Duration: Rapid Insulin lispro (Humalog) AC or PC Insulin axpart (NovoLog) AC (before meal) Insulin glulisine (Apidra) PC (after meal) Short Duration: Slower Regular Insulin (Humulin R., Novolin R.) no Rx (Exubera) Intermediate Duration (give AC) NPH insulin (Humulin N., Novolin N.) No Rx, cloudy Insulin detemir (Levemir) Long Duration Insulin glargine (Lantus) Notes: -can only mix R&N insulins -Regular Insulin is the ONLY insulin you can give IV Drug Interactions -Beta Blockers can mask the S/S of hypoglycemia (tachycardia, palpations) -can also cause further hypoglycemia by blocking glycogenolysis w/ insulin cause lower BP -Sulfonylureas, Meglitinides, Beta Blockers, Alcohol Counteract actions of insulin (cause hyperglycemia) -thiazide diuretics, glucocorticoids, sympathomimetics Misc -insulin needs are affected by stress, obesity, adolescent growth -insulin needs may decrease during pregnancy Fasting plasma glucose at least 8 hrs after meal. Normal < 100 mg/dl diabetes > 126 mg/dl Casual plasma glucose any time > 200 mg/dl but must also display signs & sx (polyuria, polydypsia, ketonuria & rapid wt. loss Oral glucose tolerance test used when first 2 test were not definitive. Give glucose load of 75 g of glucose & measure plasma level 2 h later. Normal is < 140 mg/dl diabetes if > 200 mg/dl Onset 15-30 min 10-20 min 10-15 min 30-60 min 15-30 min 1-2 hr ----70 min -ONLY mix R&N insulins together -Draw short acting insulin into syringe first to avoid contamination of NPH vial. -Mixtures are stable for 28 days at room temp and 1 mo under refridg. -Insulin left out of the refrigerator is good for 1 month -All insulins can be given SQ because digestive enzymes would inactivate insulin -SQ injection sites are in the upper arm, thigh (slowest) & abdomen(fastest) (Rotate sites of injection q mo to reduce incidence of lipohypertrophy) Peak 0.52.5 hr 1-3 hr 1-1.5 hr 1-5 hr 0.5-1.5 hr 6-14 hr 6-8 hr None Duration 3-6.5 hr 3-5 hr 3-5 hr 6-10 hr 6.5 hr 16-24 hr 12-24 hr 24 hr Pt teaching -give w/ meals (before or after) 30-60 min -rotate inj sites -SQ, IM, oral, IV*

-use b/t meals, not for postprandial control -less risk of hypo/hyperglycemia

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Oral Hypoglycemics

Sulfonylureas (DM type 2 only)


MOA -Stimulate release of inuslin (pancreas) depending on how much glucose there is -avoid in pregnant women Drug Interations -no alcohol (can have antabuse reaction) -dont take drugs that intensify hypoglycemia (NSAIDs, sulfonamide antibiotics, ranitidine & cimetidine) -Beta Blockers beta rec promote insulin release & mask s/s of hyporglycemia First Generation (all PO) less potent Tolbutamide (6-12hr) Acetohexamide (12-24hr) Tolazamide (12-24hr) Chlorpropamide (24-72hr) Second Generation (all PO) potent w/ longer DOA Glipizide Standard (12-24hr) Glipizide Sustained (24hr) Glyburide Nonmicronized (12-24hr) Micronized (24hr) Glimepiride (24hr) Side Effects -hypoglycemica (fatigue, excessive hunger, profuse sweating, palpitations) -weight gain

Meglitinides (DM type 2 only)


MOA -Stimulate release of insulin (pancreas) depending on how much glucose there is -MUST eat within 30 min of taking Drug Interactions -Gemibrizol (causes hypoglycemia) Notes -if Sulfonylureas doesnt work, neither will Meglitinides -approved for mono Tx or combo w/ Metformin or a glitazone Drugs - glinide Repaglinide (Pranide) Nateglinide (Starlix) Side Effects -hypoglycemia (less than w/ sulfonylureas) -weight gain

Biguanides (DM type 1 & 2)


Drugs -Metformin (Glucophage, Fortamet, Glumetza, Riomet) MOA -Decr glucose production (liver) & enhance glucose uptake & utilization by muscles -does NOT promote insulin release -absorbed slowly in small intestine and excreted unchanged by kidney Contraindications -Creatine levels ( 1.5 for males and 1.4 for females) -Liver disease, severe infection, alcohol, pt. in shock (causes hypoxemia) Side Effects -Weight loss, dec in appetite, nausea, diarrhea -Decr. absorb of B12 & folic acid -lactic acidosis (s/s: hyperventilation, myalgia, malaise & unusual somnolence) Notes -can use alone or with Sulfonylureas or Exenatide

Thiazolidinediones

(DM type 2 only) Drugs glitazone -Rosiglitazone (Avandia) -Pioglitazone (Actos) MOA -Decr insulin resistance by incr insulin sensitivity of muscles, liver, & adipose -insulin must be present for drug to work Contraindications -Gemfibrizol -Class 3 or 4 HF or hepatoxicity Side Effects -fluid retention (edema & weight gain) -incr HDL, LDL, & TGs (triglycerides)

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Alpha-Glucosidase Inhibitors
MOA -Decr absorption of carbs by prevent breakdown of monosaccharides in small intestine Side Effects -Flatulence, cramps, abdominal distention, borborygmus (rumbling bowel sounds) -diarrhea -decr. absorpt of iron (anemia), liver dysfunction Drugs -Acarbose (Precose) -Miglitol (Glyset) Notes -can be used in mono Tx or with insulin, sulfonylurea or metformin (try to avoid metformin & alpha-gluc together b/c of GI effects)

Injectables for Hypoglycemia

Amylin Mimetics (DM type 1 & 2)


Drugs -Pramlintide (Symlin) MOA -delays gastric emptying (incr satiety lower caloric intake) -suppresses alpha cells (decr glucagon secretion) -peaks at 20 min with SQ injection Side Effects -Hypoglycemia (esp. when in combo w/ Insulin) -nausea, injections site rxns Drug Interactions -take PO drug 1hr before injection -drugs that slow motility (anti-cholinergics) -drugs that slow absorption of nutrients (acarbose, miglitol) Notes Type 1 & 2 -used as adjunct to insulin for pts that have little glucose control with insulin Type 2 -used in combo w/ Metformin and/or a Sulfonlyurea

Incretin Mimetics / Glucagon-like Peptide-1 Agonist


Drugs -Exenatie (Byetta)

(DM type 2)

MOA -delays gastric emptying -inhibits postprandial release of glucagon (decr glucagon secretion) -stimulates glucose-dependent release of insulin Side Effects -Hypoglycemia (esp. when in combo w/ Sulfonylurea) Drug Inteactions -take PO drugs 1hr before injection -oral contraceptives -antibiotics Notes -dont use in pts with end-stage renal disease Type 2 -used in combo w/ Metformin and/or a Sulfonlurea

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Thyriod Hormones -effects metabolism, cardiac function, growth & development -T3 is more potent. (T4 T3) -more T4 is released than T3 Contraindications -recent MI (titrate over 3wks if a must) Side Effects -incr effects of adrenergic agonist drugs -inhibits adrenergic antagonist drugs Throid Hormone Principle Actions 1) stimulation of energy use 2) stimulation of the heart 3) promotion of growth/dev of fetus 4) incr. production & release of other hormone (estrogen, testosterone, insulin, catecholamines, glucocorts) 5) stimulate appetite Clinical Manifestations Hyperthroidism prominent eys fine, thin hair; hot, moist skin heat intolerance appetite, weight nervous, irritable, insomia, diarrhea (diagnosis w/ Serum T3 Test) Hypothyroidism ptosis, edematous eyes dry, brittle hair; cold, dry skin cold intolerant appetite, weight lethargic, depressed, sleep constipation (diagnosis w/ Serum TSH Test)

Hypothyroidism
Drugs -Natural Thyroid Extract, Desiccated Thyroid (T3, T4) -Levothyroxine (T4) See Below -Liothyronine (T3) -Liotrix (T3, T4) ratio 1:4 Levothyroxine Na MOA -T4, rapidly converts to T3. -NARROW THERAPEUTIC INDEX. Test TSH 6-8wk after Tx starts -take 30min AC (before meal) on empty stomach Pharmacokinetics -variable absorption, metabolized by liver, eliminated by GI -slow onset with Long DOA (half-life 6-7 days. full effects in 2-3wks) Pharmacodynamics -binds to receptors throughout body incr metabolic rate -stimulates protein synthesis & promotes cell growth Side Effects (excessive dose thyrotoxicosis) -GI: weight loss, incr bowel motility -CV: tachycardia, palpitations, angina, CHF -NM: headaches, nervousness, insomnia, hyperthermia, heat intolerance, sweating -Misc: menstrual irregularities, impotence Liothyronine Compared to Levothyroxine -Absorbtion: better -Potentacy: better -Effects see: faster -DOA: shorter -Cardiotoxicity: higher Drugs that Decrease Levothyroxine Absorption -Cholestyramine, Colestipol -Ca+ supplements (Tums), Sucralfate, Aluminum-containing antacids -Fe+ supplements Drugs that Increase Levothyroxine Absorption -Phenytoin (Dilantin), Carbamazepine -Rifampin, Srtreline (Zoloft), Phenobarbital Notes -If on Warfin, reduce the dose -increases bodys response to catecholemines (epi, NE, dopamine, etc.) -low cost, synthetic (minimal allergic rxn) -long DOA -Routes: PO, injection, IV

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Hyperthyroidism
-2 treatment options: 1) Antithyroid Drugs (Propylthiouracil, Methimazole) 2) Radiation or Surgery Graves Disease -autoimmune disorder -protruding eyes (exophthalmos), enlarged thyroid gland -Thyrotoxicosis - thyroid hormone, tachycardia, dysrhythmias, angina, wt loss TX -PTU, beta blocker, glucocorticoids for exophthalmos Plummers Disease (Toxic Nodular Goiter) -Clinical Manifestations same as Graves except no exophthalmos Propylthiouracil (PTU) MOA -blocks thyroid synthesis by: 1) block peroxidase prevent iodide oxidation inhibit iodine into tyrosine 2) blocks conversion of T4 T3 in peripheral tissue Pharmacokinetics -Quick onset (30min), half-life 75min (so need continuous dosing) -Crosses placent (BUT less often than Methimazole. Choice while pregnant) Side Effects -agranulocytosis, thrombocytopenia, hepatotoxicity -sore throat, fever, N/V -ulcers in mouth, rectum, and vagina -hypothyroidism Notes -take with food -is missed dose, take ASAP -store in light resistance container -takes 6-12wks to see results Methimazole (Tapazole) -not protein bound -more potent & more toxic than PTU -long DOA (several weeks) -more effective than PTU, but many people have bad rxn so PTU is more common -dont use if pregnant or breastfeeding Beta Blockers (not a treatment) -usually Propranolol -for emergency, PO, IV -rapid onset (1hr) Important Note DOES NOT correct hyperthyroidism, ONLY controls the adrenergic effects of excessive thyroid hormone until slower-acting anti-thyroid medications can tak effect Thyroid Storm (Thyrotoxic Crisis) Causes -metabolic stressors (infection, trauma) -NOT triggered by thyroid hormones Notes -no lab tests to confirm -S/S hyperthermia, hypotension, CHF TX -PTU, beta blocker, Potassium iodide or iodine solution

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