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82 Cards in this Set
- Front
- Back
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Insulin receptor
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Tyrosine Kinase
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Insulin preps are ______ in solution but need to be ____ to bind receptors.
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Hexamer
Monomer |
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What property of ultra short acting makes them short acting?
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Decreased hexamer stability --> falls apart easily
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Lispro
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Ultra short acting
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Aspart
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Ultra short acting
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Glulisine
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Ultra short acting
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Why is there no antigenic response to ultra short acting insulin preps?
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They are very similar to insulin --> decreased antigenicity
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How do you administer ultra short acting insulin preps?
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SubQ
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Regular crystalline
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Short acting
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NPH
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Intermediate
Protamine in phosphate buffer |
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Lente
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Intermediate insulin prep
Insulin with zinc in acetate buffer |
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What's preferred, Lente or NPH? Why?
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NPH preferred
LEnte + regular insulin converts all to intermediate insulin. We want 70% intermediate and 30% short acting. |
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Ultralente
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Slow acting
Increased Zn in PO4- buffer Unpredictable rate of absorption |
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Glargine
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Slow acting
Stable hexamer, predictable from SubQ |
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Why do pts have to take insulin in the middle of the night?
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Cortisol, epi, and GH increase glucose at night and can make you hyperglycemic when you wake up.
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Watch out for this class if you're allergic to sulfa drugs
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Sulfonylureas
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Main SFx of sulfonylureas as a whole
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Hypoglycemia
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Chlorpropamide Side Effects
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Alcohol induced flush
Hyponatremia(Inc. ADH in Kidney) |
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1st gen. sulfonylureas
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Tolbutaminde
Chlorpropamide(antabuse rxn, hypoNa+) Tolazamide Acetohexamide |
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2nd gen. sulfonylureas
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Glyburide
Glipizide Gliclazide Glimeripride |
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What's the difference between 1st and 2nd gen sulfonylureas?
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2nd gen. are more potent than the 1st gen.
Shorter half life. |
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Repaglinide
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Meglitinide
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Nateglinide
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Meglitinide
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Meglinitide MOA
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Simular to sulfonylureas in K+ ch. effect
No sulfur in structure* No direct effect on insulin exocytosis |
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Metformin
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NOT Hypoglycemic
Decrease liver glucose output Decrease insulin resistance Contraindics: Renal impairment Hepatic Dz ***Lactic acidosis*** in the past |
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Thiazolidinediones
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Pioglitazone, Rosiglitazone, Troglitazone
Increase glucose transporters --> insulin action Bind PPAR-y Sfx: Monitor liver function!(liver Cx risk) Increase HDL, lower LDL |
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a-glucosidase inhibitors
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Acarbose, Miglitol
Decrease carb absorption SFx: Flatulence(d/t bacteria), diarrhea, abd pain |
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GLP-1 analogs
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Exenatide
Increase glucose dependent insulin secr Given by injection (Rest are orally active) |
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Ethanol: Hyper or hypoglycemic?
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Hypo
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Diuretics: Hyper or hypoglycemic?
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Hyper
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Salicylates: Hyper or hypoglycemic?
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Hypo
Increase insulin release |
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beta-blockers: Hyper or hypoglycemic?
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Hypo
Blocks epi effects. Epi counters insulin. So beta blockers have a pro-insulin effect |
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Ca channel blockers: Hyper or hypoglycemic?
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Hyper
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Asthmatic patient taking beta 2 agonist. Will he be hyper or hypoglycemic? Tx for that?
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Hyperglycemic (Beta 2 agonist -> hyper)
Tx: Increase insulin dose |
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ADH receptor on vascular smooth muscle
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V1
Acts via PLC->Ca2+ and PKC |
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ADH receptor on principal cells and collecting duct
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V2
cAMP & PKA |
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Desmopressin
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V2 selective agonist - no vascular effects
Centra DI |
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Chlorpropamide
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Enhance ADH action
Augment V2 transduction Centra DI and 1st gen Hypoglycemic BUT - Antabuse rxn! |
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Carbamazepine/clofibrate
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Central DI
Enhance ADH action on kidney |
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Pitocin
Peptide or GlycoProtein? Uses? Sustain or induce? |
Oxytocin
Peptide **Stim uterine contractions, milk ejection, Ups PG production in uterus |
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Misoprostol
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PGE1 analog
Induces abortion, stimulate sustained contractions(PGE stimulates contractions) |
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Ergonovine/methylergonovine
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Tx: Post partum hemorrhage
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Tocolytic agents do what?
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Delay labor
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B2 selective tocolytics
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Terbutaline, ritodrine
Delay labor & relax uterus **Increase renin - Na/H20 retention - HTN! HYPERGLYCEMIA hypokalemia pulmonary edema |
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Nifedipine
Uses? |
Ca2+ ch. blocker
Relax uterine smooth muscle Vascular active Prefer vascular active to cardiac active!! |
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Indomethacin
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PG inhibitor
adverse: closure of ductus arteriosus --> i.e, treat persistent ductus(PG keeps ductus open)! |
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atosiban
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Oxytocin receptor antagonist
Stop labor! |
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Prolactin uses?
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No pharmacologic uses!!
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GH analogs
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Somatotropin - identital to humans
Somtrem - immunogenic response chance |
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LH analog
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hCG from pregnant women!
acts at LH receptor |
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Menotropins
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both FSH and LH
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Urofollitropin
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mainly FSH
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follitropin
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recombinant FSH
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Thyrotropin
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TSH agonist?
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Cosyntropin
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ACTH, diagnostic use,
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Gonadorelin
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short acting GnRH analog
pulsatile IV - stimulate LH/FSH release |
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GnRH analogs
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long acting GnRH analogs - initial increase in LH/FSH but continuous admin suppresses release
Chemical Castration; tx for precocious puberty ***Leuprolide(Prostate cancer!!!) Histrelin Deslorelin (Very potent) Nafarelin (Nasal spray) Buserelin(Nasal spray) Goserelin - 28 day continuous release Triptorelin - depot IM |
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Leuprolide
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GnRH long acting analog
continuous - suppress FSH/LH secretion Tx for: Prostate cancer |
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GnRH anatgonists
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Ganirelix
Cetrorelix Abarelix |
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Bromocriptine
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D2 agonist - inhibit PRL release, *paradoxical decrease in GH release
Also: Cabergoline, Pergolide, Quinagolide |
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Octreotide
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SST Analog
More resistant to degradation LONGER HALF LIFE |
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Pegvisomant
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GH Receptor antagonist
Acromegaly and gigantism |
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Levothyroxine
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T4
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Liothyronine
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T3
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Liotrix
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T4+T3
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Effect of high dosese of thyroid hormones?
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Cardiac arrhythmias - can look like hyperthyroid pt.
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Increase or decrease synthroid dose in pregnant woman?
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Increase...
Estrogen in pregnance increases TBG -> free T4 drops transiently |
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Glucocorticoid effect on Thyroid hormones?
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Decreases binding of T4 to TBG
But Decreases T4->T3 by Type I 5' DI |
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What other drugs inhibit type I 5' DI?
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B blockers(propanaolol in high doses)
Amiodarone |
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PTU
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Short half life - more dosing!
Inhibit Type I 5' DI - less T4->T3 conversion Block T4 and T3 synthesis |
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Methimazole
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toxicity possible to fetus
Decrease T4->T3 |
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Anti thyroid drugs - name em!
Side effects of anti-thyroid drugs? |
Agranulocytosis!! (WBC drops)
Most common side effect: rash |
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Perchlorate - BIG side effect
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Fatal aplastic anemia
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Ionic inhibits - anti thyroid
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Thiocyanate, perchlorate, fluoroborate
NIS competition -> block I2 uptake |
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Explain wolf-chaikoff effects in Anti-thyroid tx.
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Give iodide --> Decreases # NIS receptors
Pre-op tx for throidectomy & for thrytoxic crisis RAPID EFFECTS THEN ESCAPE! |
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Desmopressin
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V2 agonist - kidney effects only, no vasculature effects(which are via V1)
Tx: CENTRAL DI |
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Chlorpropamide
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POTENTIATE ADH
Augment V2 rec. transduction Disulfiram like rxn and HTN/Hypokalemia |
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Tx for lithium induced DI
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Amiloride
Blocks Li uptake into cells |
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Nephrogenic DI tx
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Hydration, Thiazide diuretics, Indomethacin( --> block PG's --> pro ADH)
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Demeclocycline
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Tetracycline antibiotic
Interferes with V2-R transduction |
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Loop diuretics in SIADH - why?
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Lose interstitial gradient so less H20 absorbed
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Lithium in SIADH
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V2-R transduction
psyhic side effects |
