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Endo Pituitary and Thyroid Drugs
Endo Pituitary and Thyroid Drugs
50
Medical
Professional
03/08/2011

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Term
The single most sensitive test of thyroid hormone stat is ___
Definition
TSH
Term
Tx hypothyroidism: drug, dosing, course (2)
Definition
Levothyroxine/T4 qd

Increase dose every 2 weeks until TSH is normal, monitor with Free T4

Takes 2-3 weeks to see it take effect because the T4 has to fill all the TBG sites before it can stay in the blood as Free T4
Full resolution by 4-6 weeks (skin/nails may take longer)

(Don't use T3 because t1/2 too short and it's too toxic.)
Term
Levothyroxine: S/E (4, 3), contraindications
Definition
S/E have to do with overtreatment (determine this by measuring TSH: suppressed indicates that you're overtreating, which is causing the symptoms)

Adults: heat intolerance, tachycardia, weight loss, nervousness
Kids: insomnia, restlessness, accelerated bone growth

Watch out for patients with known/suspected CAD or myocardial issues because levothyroxine can cause MI or afib = start them off slowly
Term
Tx myxedema coma (5)
Definition
Intubate and ventilate: reverse hypoxia and hypercapnia
Glucose: reverse hypoglycemia
Loading dose thyroxine: has to be big because the TBG sites are empty and need to be filled before there can be Free T4 in the blood

You know the patient's doing better when body temperature and mental status improve

IV fluids: use with care since the patient's already hyponatremic!
Term
Drugs that can cause hypothyroidism (2)
Definition
Corticosteroids: inhibit release of TRH and TSH, prevent T4=>T3
Lithium: inhibits T3/3 secretion in patients with previous hypothyroidism
Term
Tx hyperthyroidism (5)
Definition
KI
Methimazole
PTU
Propranolol
I-131 ablation
Term
Drug that modifies tissue response to excess T4/3
Definition
Propranolol
Term
Drugs that prevent organification of iodide and synthesis of T4/3 (2)
Definition
Methimazole
PTU
Term
Drugs that prevent T4=>T3 (2)
Definition
PTU
Propranolol
Term
Drug that prevents release of T4/3
Definition
KI
Term
1st-line hyperthyroidism drug
Definition
Propranolol
Term
Propranolol: MOA (2), physiologic effects, dosing issue
Definition
Blocks B1 and B2-R: controls autonomic symptoms like tachycardia, palpitations, tremor, anxiety

Prevents T4=>T3: controls heat intolerance, diaphoresis, weight loss, fatigue

Gotta give a lot at first since its metab will be increased in hyperthyroidism
Term
Main drugs for tx hyperthyroidism (2)
Definition
Methimazole
PTU
Term
Thioamides: MOA (4)
Definition
Inhibit thyroid peroxidase: inhibits conversion of iodide to iodine

Inhibit MIT/DIT coupling

PTU: also blocks T4=>T3

Overall: decreased synthesis of T4/3
Term
Thioamides: physiologic effects (3)
Definition
Slow onset depletion of T4 stores

After euthyroid state, minority will go into remission within 1mo-2yrs

Most will relapse, though, and then treated with I-131
Term
Thioamides: S/E (4)
Definition
Skin rash (tx w/ antihistamine)
Reversible agranulocytosis (rare)
Prego
-Only use PTU because it's highly protein-bound = doesn't cross the placenta
-Some babies will have goiter, though, so wanna use the smallest dose for the shortest amount of time

PTU: anti-vitK activitiy = potentiates warfarin
Term
I-131: MOA (3), S/E (3)
Definition
Stop PTU/KI 1 week prior to tx to allow for good I-131 uptake
Rapidly absorbed and concentrated in thyroid (want 40-60% uptake)
Beta-radiation kills the follicular cells

Follicular cell lysis can cause thyroid storm, so give KI prn
Avoid kids and pregos
May become euthyroid and then hypothyroid, requiring levothyroxine
Term
KI: MOA (2), physiologic effect
Definition
Prevents thyroglobulin proteolysis = inhibits release of T4/3
Transiently inhibits iodide trapping = inhibition of organification of iodide

Decreases size and vascularity of the gland over 2-7 days
Term
KI: indications (2)
Definition
Prep thyrotoxic patients for emergency surgery
Thyroid storm

Not used routinely or as single-agent
Term
KI: S/E (6)
Definition
Hyperthyroidism: gland actually uses the iodide to make T4/3 ("escape")
Allergies: skin rash, fever, facial swelling, joint pain, possible dyspnea
Fetal goiter
Iodism (rare): burning sensation in mouth/throat, metallic taste, sore gums

Delays action of PTU
Prevents use of I-131 for a few weeks
Term
Causes of increased TBG concentration (3)
Definition
OCPs
Prego on levothyroxine
Opiates
Term
Drugs that decrease TBG concentration (3)
Definition
Glucocorticoids
Androgens
Salicylates
Term
Drugs that increase T4 clearance (5)
Definition
Induce CYP450
-Phenobarbital
-Phenytoin
-Carbamazepine

Increase fecal loss
-Cholestyramine
-Colestipol
Term
Precipitating factor of thyroid storm
Definition
Stress
Term
Tx thyroid storm (3)
Definition
Propranolol: single-most important drug
KI or PTU
Supportive care
Term
Dissection of the pituitary stalk causes ___ DI
Definition
Transient

Disappears because eventually the normal osmotic stimuli elicit the release of AVP directly from the HT
Term
Aldo controls ____ Na not Na ___
Definition
Total body Na NOT Na concentration
Term
ADH controls Na ___ not ___ Na
Definition
Na concentration NOT total body Na
Term
If there's an issue with concentrating urine, think ___ unless ___
Definition
Think ADH unless on some other drugs
Term
V1R has a ___ effect while V2R has a ___ effect
Definition
V1R has a vasopressor effect at high [ADH]
V2R has a water reabsorption effect at low [ADH]
Term
ADH: MOA
Definition
Stimulates adenyl cyclase-coupled ADH-R on the basolateral membrane of the late distal tubule and collecting duct
cAMP, kinases, insert pores in the apical membrane (this is where most anti-ADH drugs work)
Hyperosmolar gradient in the interstitial fluid causes tubular water to move into the interstitium thereby concentrating the urine
Term
Lithium and PGE inhibit ___
Definition
ADH-dependent adenyl cyclase
Term
Additional V2R effects (2)
Definition
Increases release of Factor 8 from hepatocytes and vWF from endothelial cells
Relaxes smooth muscle = decreased TPR
Term
Tx central DI (1)
Definition
DDAVP
(HCTZ)
Term
DDAVP: MOA, pharmacokinetics (3)
Definition
ADH analog
t1/2 6-20 hrs
V2:V1 activity is 4000, so little VC

URI rhinitis or congestion slow absorption
Term
DDAVP: physiologic effect, water intake
Definition
Marked reduction in daily urine volume

Limit water intake to just enough to satisfy thirst to avoid hyponatremia
Term
Other uses of DDAVP (2)
Definition
Nocturnal enuresis
Hemophila A and vWD
Term
DDAVP: S/E (3)
Definition
HTN (rare)
Hypotension with tachycardia (IV or subcu)
Hyponatremia with excess water intake
Term
HCTZ: MOA (3), physiologic effect
Definition
Decreases GFR: urine is less dilute
Natriuresis contracts ECF volume = increased salt/water reabsorption in the proximal tubule = less volume sent to the distal tubule to be diluted
Inhibits NaCl reabsorption in the distal tubule

Decreases urinary volume
Term
Tx nephrogenic DI (4)
Definition
Adequate water intake
Partial: HCTZ or larger doses of DDAVP if partially nephrogenic
Complete: HCTZ or indomethacin
Term
Indomethacin: MOA
Definition
Block synthesis of renal PGE, which normally inhibits ADH-stimulation of adenyl cyclase
ADH can now stimulate adenyl cyclase
Term
Li-induced DI: MOA
Definition
Most Li reabsorbed in PT
Rest can be reabsorbed in the principal cells of the late DT and CD
-Li goes where Na goes and inhibits ADH
-Only place where Na and Cl don't travel together (Cl travels paracellularly)
Term
Tx Li-induced nephrogenic DI (1)
Definition
Amiloride
(HCTZ)
Term
Amiloride: MOA, physiologic effects (2)
Definition
Blocks Na-channels in the principle cells = Li can't enter

Decreases urine volume 30-40% and increases osmolality to >300

Doesn't decrease the renal clearance of Li!
Term
HCTZ: Li S/E
Definition
The increased salt/water reabsorption in the proximal tubule means that most of the Li may be reabsorbed instead of cleared

Gotta reduce the dose to prevent toxicity
Term
Causes of SIADH (4)
Definition
Non-endocrine cancers especially small cell lung cancer
CNS issues
Pulmonary infections
Adrenal insufficiency/hypothyroidism
Term
Tx SIADH (1)
Definition
Demeclocycline
(Chlorpropaminde)
Term
Chlorpropamide: MOA (2), other indication
Definition
Increases release of ADH
Potentiates renal effects of ADH

Induces insulin release in NIDDM
Term
Tx SIADH-induced hyponatremia (3)
Definition
Restrict water intake: urine output will exceed what's consumed = plasma concentration will rise
Demeclocycline
Infuse with NaCl (severe cases)
Term
Demeclocycline: MOA, indication
Definition
Tetracycline
Inhibits adenyl cyclase = inhibits ADH action in the collecting duct

Used when Na <120 and the patient has severe neuro symptoms
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