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ENDOCRINE EXAM 3
| DRUG | CLASS | MOA | ADR | NOTES |
|---|---|---|---|---|
| Propylthiouracil (PTU) Methimazole (MMI) | Thioamides (for hyperthyroidism) | Inhibit TPO, blocks iodination/organificaton PTU ONLY - inhibits D1 (t4 to t3) | PTU - boxed warning hepatoxic Fetal abnormalities - MMI not used in first trimester, but used in 2nd and 3rd | MMI - increase risk of pancreatitis |
| Potassium iodide (KI) | Thioamides (for hyperthyroidism) | Inhibits t3/4 activity, blocks RAI (radioactive iodine) uptake, decrease vascularity of thyroid gland before thyroidectomy (surgery) | Wolff-chaikoff effect (thyroid homrmone shuts off) caution in pregnancy - crosses placenta | Blocks uptake of radioactive iodine to reduce risk of thyroidcancer |
| Iodine -131 | Thioamides (for hyperthyroidism) | radioactive destruction of thyroid | do not use in pregnancy | 131-I |
| Propanolol, nadolol, atenolol, metoprolol, esmolol (MEAN) | Beta blockers (for hyperthyroidism) | propanolol and nadolol inhibits D1 and D2 (t4 to t3) at high doses, use for adrenergic symptoms, thyrotoxicosis treatment, B1/2 antagonist | symptom treatment for thyroxicosis (treatment for hyperthyroidism), blocks peripheral t4 to t3 conversion | |
| Teprotummumab | Monoclonal antibody (for hyperthyroidism related eye disease) | insulin growth like factor 1 receptor antagonist, thyroid eye disease treatment, decrease TSHR and orbital fibroblast inflammation | tinnitus, hearing loss, hyperglycemia, infusion related | |
| Desiccated thyroid | Synthetic thyroid hormones (for hypo) | Synthetic T4, T3, iodine | increased HR, palpitations (dose related), thyrotoxicosis BBW - weight reduction | |
| Levothyroxine | Synthetic thyroid hormones (for hypo) | Synthetic T4 | increased HR, palpitations (dose related), thyrotoxicosis BBW - weight reduction | prohormone (prodrug), cleaved to form T3 |
| Liothyronine | Synthetic thyroid hormones (for hypo) | Synthetic T3 | increased HR, palpitations (dose related), thyrotoxicosis BBW - weight reduction | shorter t1/2 |
| Thyrolar | Synthetic thyroid hormones (for hypo) | Synthetic T4 and T3 | increased HR, palpitations (dose related), thyrotoxicosis BBW - weight reduction | |
| Sildenafil (viagra) | PDE5 inhibitors | inhibit phosphodiesterase 5 (PDE5) to increase cGMP (Nitric Oxide mediated vasodilation), CI with nitrates and 3A4 inhibitors | priapism (erection over 4 hours), sildenafil visual problems, headache, flushing, dizziness | used for ED and PAH (pulmonary arterial hypertension) |
| Tadalafil (cialis) | PDE5 inhibitors | inhibit phosphodiesterase 5 (PDE5) to increase cGMP (Nitric Oxide mediated vasodilation) CI with nitrates and 3A4 inhibitors | priapism (erection over 4 hours), headache, flushing, dizziness, tadalafil causes back/limb pain, myalgia, tadalafil has the least sides effects (most used) | used for ED, PAH, and BPH (benign prostatic hyperplasia) |
| Vardenafil (levitra), avanafil (stendra) | PDE5 inhibitors | inhibit phosphodiesterase 5 (PDE5) to increase cGMP (Nitric Oxide mediated vasodilation), CI with nitrates and 3A4 inhibitors | priapism (erection over 4 hours), headache, flushing, dizziness, vardenafil can prolong the QT interval | only used for ED |
| Alprostadil | PGE 1 analog, PGE receptor agonist | dizziness, headaceh, pain | ||
| Papaverine | selective PDE inhibitor (some GMP effects) | cirrhosis, headaceh | ||
| Phentolamine | Non-selective AR antag | dizziness, hypotension | ||
| Trazadone | a1-AR antagonist | a1/2-AR antagonist, 5-HT reuptake inhibitor | headache, drowsiness, dizziness | |
| Yohimbine | a2-AR antagonist | CV, HTN, anxiety, motor function, insomnia | ||
| Flibanserin (Addyi) | Female libido enhancers | decrease 5HT (1A agonist 2A antag) and serotonin | CNS depression, decreased alertness, hypotension, DO NOT USE WITH hepatic impairment, 3A4 inhibitors, alcohol | hypotension with alcohol |
| Bremlanotide (Vylessi) | Female libido enhancers | Increase release of dopamine, melacortin receptor agonist | nausea, flushing, skin hyperpigmentation, injection site reaction | CI with naltrexone to avoid treatment failure, slows gastric emptying |
| Teriparatide Abaloparatide | Recombinant PTH (increase osteoblast activity) | PTH receptor agonist, | Hyepercalcemia, leg cramps, orthostatic hypotension, osteosarcoma (limit use to 24 months) | for high risk of fracture pts, Osteosarcoma risk limit to 2 years |
| Romosozumab | Sclerostin antibody (increase osteoblast activity) | Sclerostin inhibitor, sclerostin inhibits Wnt in bone metabolism, this drug letss Wnt signaling increase osteoblasts | Boxed warning for risk of MI, stroke and CV death | reduces fracture risk) CV risk 1 year limit |
| Alendronate, risedronate, ibandronate, zeldronate | Bisphosphonates (inhibits osteoclasts activity) | Inhibits osteoclasts activity in hypercalcemia and osteoporosis | GI upset, esophagitis, osteonecrosis of jaw (rare), flu-like fever | preferred for pagets disease |
| Calcitonin-salmon, nasal or IV | Calcitonin (inhibits osteoclasts activity) | inhibits osteoclasts, removes Ca from blood into bone | dryness, runny nose, nose bleed, rhinitis, headache | longer t 1/2 when mixed with salmon |
| Bazedoxifene, raloxifene | SERMS (inhibits osteoclasts activity) | increase osteoblast life, kills clasts, receptor agonsit at the bone but antagonists at breast and endo (cancer drugs) | hot flashes, DVT, PE, stroke | estrogens increase osteoblasts function |
| Denosumab | RANKL antibody (inhibits osteoclasts activity) | RANKL inhibitor, similair action to OPG (what is produced by osteoblast to inhibit RANK as a decoy receptor) | boxed warning for hypocalcemia in pts with eGFR < 30 | mimics OPG to decrease RANKL activity (osteoclasts activity) |