Exam 3 Endocrine From Michelle[1]
Transcript of Exam 3 Endocrine From Michelle[1]
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Endocrine Drugs 1 of 7
GlucocorticoidsMOA: Suppress immune system and inflammation by inhibiting chemical mediators such asprostaglandins, 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 storage5) 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) atyour 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
Drugs
Short-Acting-Cortisone
-Hydrocortisone
(high mineralcorticoid
activity)
Intermediate Acting-Prednisone
-Prednisolone
-Methylprednisolone
-Triameinolone
Long Acting-Betamethasone
-Dexamethasone
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
Drug Interactions
-Digoxin, thiazide, & loop diureticsglucocorts w/ high mineralcort activity canlead 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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Endocrine Drugs 2 of 7
MineralocorticoidsMOA: 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
DrugsFludrocortisone (Florinef Acetate)
-has both high mineralocorticoid and glucocorticoid activity
Adverse Reactions
Low Dose
-increase in BP
High Dose-inhibits endogenous adrenal cortical secretion & pituitary corticotropin excretion
-promotes deposition of liver glycogen
Contraindications
-systemic fungal infection
Cautions
-pregnancy and kids
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Endocrine Drugs 3 of 7
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 ratherthan inject them separately.
-ONLYmix R&N insulins together-Draw short acting insulin into syringe firstto 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)
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, cloudyInsulin detemir (Levemir)
Long Duration
Insulin glargine (Lantus)
Notes:-can only mix R&N insulins
-Regular Insulin is the ONLY insulin you can give IV
Onset
15-30 min
10-20 min
10-15 min
30-60 min
15-30 min
1-2 hr-----
70 min
Peak
0.52.5 hr
1-3 hr
1-1.5 hr
1-5 hr
0.5-1.5 hr
6-14 hr6-8 hr
None
Duration
3-6.5 hr
3-5 hr
3-5 hr
6-10 hr
6.5 hr
16-24 hr12-24 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 forpostprandial control
-less risk of hypo/hyper-
glycemia
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/dlCasual 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. Giveglucose load of 75 g of glucose & measure plasma level 2 h later. Normal is < 140
mg/dl diabetes if > 200 mg/dl
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Endocrine Drugs 4 of 7
Oral Hypoglycemics
Sulfonylureas (DM type 2 only) Meglitinides (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
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
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, profusesweating, palpitations)
-weight gain
Drugs - glinide
Repaglinide (Pranide)
Nateglinide (Starlix)
Side Effects
-hypoglycemia (less than
w/ sulfonylureas)
-weight gain
Biguanides (DM type 1 & 2) Thiazolidinediones (DM type 2 only)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 kidneyContraindications
-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
Drugsglitazone
-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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Endocrine Drugs 5 of 7
Alpha-Glucosidase InhibitorsMOA-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 avoidmetformin & alpha-gluc together b/c of GI effects)
Injectables for Hypoglycemia
Amylin Mimetics (DM type 1 & 2) Incretin Mimetics / Glucagon-like Peptide-1 Agonist (DM type 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)
NotesType 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
Drugs
-Exenatie (Byetta)
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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Endocrine Drugs 6 of 7
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 Hypothyroidism
prominent eys
fine, thin hair; hot, moist skin
heat intolerance
appetite, weight
nervous, irritable, insomia, diarrhea
(diagnosis w/ Serum T3 Test)
ptosis, edematous eyes
dry, brittle hair; cold, dry skin
cold intolerant
appetite, weight
lethargic, depressed, sleep
constipation
(diagnosis w/ Serum TSH Test)
HypothyroidismDrugs
-Natural Thyroid Extract, Desiccated Thyroid (T3, T4)
-Levothyroxine (T4) See Below-Liothyronine (T3)
-Liotrix (T3, T4) ratio 1:4
LiothyronineCompared to Levothyroxine
-Absorbtion: better
-Potentacy: better-Effects see: faster
-DOA: shorter
-Cardiotoxicity: higher
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
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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Endocrine Drugs 7 of 7
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 lossTX
-PTU, beta blocker, glucocorticoids for exophthalmos
Plummers Disease (Toxic Nodular Goiter)
-Clinical Manifestations same as Graves except no exophthalmos
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
Propylthiouracil (PTU) Methimazole (Tapazole)
MOA
-blocks thyroid synthesis by:
1) block peroxidase prevent iodide oxidation inhibit iodine into tyrosine2) 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
-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 takeffect