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39 Cards in this Set
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Somatropin (Omnitrope)**
Somatrem (Protropin) |
Pathophys: Synthetic GH, Sub Q injection. Stimultes cell surface receptor MAPK/ERK to promote cartiledge form. @ liver, stims JAK-STAT to promote insulin like GF-1. Promotes cell growth & diff.
Tx: Growth stature def in kids from: Prader-Willi; Chronic Renal Dz; lack of GH secretion; Turner syndrome. In adults: short bowel syndrome; GH def d/t pituitary tumor; muscel-wasting d/t HIV/AIDS SE: Inc ICP, pancreatitis, rapid nevi growth, Inc Gluc, peripheral edema, injection site rxn, arthralgia, HA Interaxn: P450, glucocorticoids, estrogens, insulin, & oral hypoglycemic agents CI: Close epiphyses, Intracranial lesion (active), Malignancy, Prolif. DM retinopathy |
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Pegvisomant (Somavert®)
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Inhibitory analog of human growth hormone: Reduces serum levels of insulin-like growth factor-1 (IGF-1) and other GH-responsive serum proteins.Given SC, long half life (t½ about 6days).
Tx: acromegaly (LT tx, controls growth) Adverse RXN: Amplified expansion of GH-secreting tumors; Hypoglycemia; GH def; Compromised liver fxn; Hypothyroidism (acromegalics) Common SE: Non-neutralizing anti-GH antibodies (17%, implications unknown, normalized upon cessation); Jaundice, dark urine, lightening of stools, abdominal distress. CI: Allergies to any of its components; Preg or lactating mothers? DI: Insulin and/or oral hypoglycemic agents may require dose reductions & pt on opioids often needed higher serum pegvisomant concentrations. |
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Bromocriptine (Parlodel®)
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Dopamine receptor agonist: dec prolactin levels.
Ergot alkaloid dopamine agonist, activates post-synaptic receptors. Acts directly on the tuberoinfundibular process to inhibit prolactin secretion from the pituitary. Oral tablet (t½ about 15 hours). Uses: Treating hyperprolactinemia-associated dysfunctions including amenorrhea, infertility or hypogonadism. Reduce growth hormone in acromegaly. Treatment of Parkinson’s disease. |
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Cabergoline (Dostinex®)***
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Dopamine receptor agonist: dec prolactin levels.
Ergot alkaloid dopamine agonist, activates post-synaptic receptors. Greater selectivity for D-2 receptors. **Acts directly on the tuberoinfundibular process to inhibit prolactin secretion from the pituitary.** Oral tablet (t ½ about 65 hours). Less gastric distress, higher patient complience. Tx: hyperprolactinemia Adverse RXN: HTN, seizure, stroke, MI, plural & cardiac effusions, transient cortical blindness CI: uncontrolled HTN, preg, CAD SE: Hypotension, Blurred vision, Fainting, Drowsiness, Sudden sleep onset, Constipation, Anorexia, Delusional psychosis, Hallucinations, paranoia, muscle cramps (acromegalics), Transient abnormalities in liver tests (Parkinson’s) DI: Phenothiazines, haloperidol, metoclopramide, pimozide. Bromocriptine is both a substrate and an inhibitor of CYP3A4. Caution with azole antimycotics, HIV protease inhibitors. Macrolide antibiotics such as erythromycin increase the plasma levels of bromocriptine. Unpredictable outcomes when used with other ergot alkaloid. |
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Tesamorelin (Egrifta)
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Tx: Lipodystrophy from HIV infxn
SE: arthralgia, injection site rxn, edema, myalgia, glucose intol, N, night sweats ADE: allergic, mood swings, pain/numbness, hypotensive crisis CI: other pit drugs, malignancy, preg DI: CP450 |
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Mecasermin (increlex)***
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Tx: Severe primary IGF-1 def (Laron dwarfs)
SE: dizzy, joint pain, thick skin (face), bruising, injection site fxn, hypoglycemia (transient) Serious Rxn: IC HTN, pain @ walking limb joints, tonsilar hypertrophy, breathing probs w/ sleep, pain/fullness @ ear, hearing probs CI: closed epiphyses, IV admin, hypersensitivity to drug, neoplasm |
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Octreotide (Sandostatin)***
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Mimicks Somatostatin (dec GH release)
SubQ or IV injection t1/2 = 2hrs Tx: acromegaly, control H2O-y diarrhea assoc w/ metastic tumor/vasoactive GI secreting tumor SE: hypothyroidism (acromegalics), inc/dec Ca++, transient diarrhea, bradycardia, pancreatitis, GB Common SE: painful injection, HA, dizzy, flushing/edema/blurred vision/hair loss Interaxn: adj w/ cyclosporine, insulin, oral hypoglycemic agent, BB, bromocriptine |
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Cosyntropin (Cortrosyn®)
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Active ACTH agonist
Maximaly drives synthesis of 17-OH corticosteroids, 17- ketosteroids and / or 17 - ketogenic steroids. IV bolus, (t½ about 15 minutes). Uses: Testing integrity of the hypothalamus, pituitary adrenal axis (non-responsive in Addison’s Disease). ADE (rare): Anaphylactic response; inc ICP w/ papilledema; Pseudotumor cerebri; HF; Necrotizing vasculitis; shock; Pancreatitis; hypoK+ alk; induction of latent DM CI: Preg? Nursing mothers? Carcinogenesis, Mutagenesis, Impaired Fertility? SE: Bradycardia; Tachycardia; HTN; Peripheral Edema; Rash; Dizziness DI: May accentuate the electrolyte loss associated with diuretic therapy |
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Conivaptin (Vaprisol®)***
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Vasopressin Receptor Antagonist
Blocks V2 receptors to interfere with aquaporin synthesis Interferes with water reabsorption, promotes water loss. Administered IV ONLY (t½ about 5 hours). Use: Treatment of clinically significant hypervolemic and euvolemic hyponatremia Elevated serum sodium in patients with heart failure, cirrhosis, and syndrome of inappropriate antidiuretic hormone (SIADH) (tolvaptan) Adverse RXN: Hypotensive crisis; Imbalances in serum sodium; Seizures; Coma CI: Hypovolemic hyponatremia; Concurrent use of potent P450 inhibitors Common SE: inc thrist, polyuria, hypoK+ Drug Interactions: CYP3A inhibitors may increase the exposure of conivaptan and are contraindicated. Avoid CYP3A substrates and inducers. Digoxin levels may increased and be monitored. Cyclosporin may elevate levels of tolvaptan. |
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Tolvaptan (Samsca®)***
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Vasopressin Receptor Antagonist
Preferentially blocks V2 receptors Theoretically fewer CNS and vascular effects Interferes with water reabsorption, promotes water loss. Tablets (t½ about 9 hrs), initate in supervised setting Use: Treatment of clinically significant hypervolemic and euvolemic hyponatremia. Elevated serum sodium in patients with heart failure, cirrhosis, and syndrome of inappropriate antidiuretic hormone (SIADH) (tolvaptan) Adverse RXN: hypotensive crisis; Imbalances in serum sodium; Seizures; Coma CI: Hypovolemic hyponatremia; Concurrent use of potent P450 inhibitors Common SE: inc thrist, plyuria, hypoK+ Drug Interactions: CYP3A inhibitors may increase the exposure of conivaptan and are contraindicated. Avoid CYP3A substrates and inducers. Digoxin levels may increased and be monitored. Cyclosporin may elevate levels of tolvaptan. |
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Oxytocin (Pitocin®, Syntocinon®)***
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Synthetic oxytocin stimulates oxytocin receptors. Promotes uterine contraction during the third stage of delivery. ALSO used to control postpartum bleeding or hemorrhage.
CI: Unfavorable fetal positions or presentations which are undeliverable without conversion prior to delivery. Hypertonic uterine patterns. Patients with hypersensitivity to the drug AE: Anaphylactic RXN, postpartum hemorrhage, cardiac arrhythmia, fatal afibrinogenemia, N/V, premature ventricular contractions, pelvic hematomas. Tetanic contraction &rupture of the uterus. Water intoxication (rare) DI: May promote hypertension with vasoconstrictors. Magnesium sulfate (used in preeclampsia labor) may mask effects of oxytocin. |
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Levothyroxine (Levothroid ®)***
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Synthetic thyroxine (T4)
Firmly plasma bound Administered oral tablet (t½ 7 days) Drives mitochrondrial expression and activity Used to treat Hypothyroidism Suppress pituitary TSH and reduce size of goiters SE: redbone density, Cardiac arrhythmias, AI thyroiditis (rare) CI: Patients w/ MI, thyrotoxivosis, hypersensitivity, malignancy (active) DI: MANY drugs. Check on patient history and current details before administering. |
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Liothyronine (Cytomel®)***
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Synthetic thyroxine (T3)
Loosely bound to plasma proteins Administered oral tablet (t½ 2 days) Active thyroxin that drives mitochrondrial expression and activity SE: Red bone density; Cardiac arrhythmias; AI thyroiditis (rare) CI: Patients w/ MI; thyrotoxicosis; hypersensitivity; or active malignancy. DI: Can interact with MANY drugs. Check on patient history and current details before administering. |
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Perchlorate, Thiocyanate (Rhodanide®), Pertechnetate
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Iodine Uptake Inhibs
These agents are similar to size/charge of iodide compete with iodide for cellular uptake via the sodium/iodide co-transporter. Can cause aplastic anemia . ***Less effective than thioamines.*** Compounds still used in contrast dyes. May affect thyroid function. |
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131I
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Radioactive Iodine
Destroys thyroid cells d/t high energy decay Start thyroxin supplementation after destroying thyroid gland |
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Wolff-Chaikov Effect
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High levels of iodide inhibit thyroid hormone synthesis and release
Involves the down-regulation of the sodium iodine symporter Effect is transient Reduces size and vascularity of thyroid for surgery Iodine also used to compete with radioactive iodine taken during nuclear intoxication |
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Propylthiouracil , Methimazole (Northyx®)***
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Thioamines
Propylthiouracil (six carbon ring, prototype) Has a six carbon ring structure. Prototype drug. Competes with thyroglobulin for oxidized iodide Blocks formation of thyroid hormone precursors Methimazole (Northyx®) Has a five carbon ring structure. Similar to Propylthiouracil, but lower incidence of severe events Both used to treat hyperthyroidism and to reduce size/vascularity of thyroid for in preparation for surgery & may interfere w/ VitK dependent pathways. |
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Esmolol (Brevibloc)***
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BB
Hyperthyroidism causes symptoms that resemble sympathetic discharge Beta blockers help to suppress the symptoms --Esmolol often the preferred choice because of its short half-life (9 minutes) Helps partially stabilize patients during a thyroid storm |
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Ipodate (Oragrafiin)***
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Contrast media used for imaging the bile duct and gallbladder.
Also inhibits 5’-deionase and conversion of T4 to T3 Has been used off lable to treat thyroid storm (NOT FDA APPROVED) |
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Lithium
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Actively concentrates in the thyroid
High levels of lithium can inhibit thyroid hormone release Some evidence that they may also interfere with thyroid synthesis Mechanism is unknown |
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Amiodarone
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Iodine containing drug -- promotes hypothyroidism of Wolff-Chaikoff effect
Degradation releases iodine Also structurally related to thyroid hormone |
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Etidronate (Didronel, Didronel IV®)
Tiludronate (Skelid®) Pamidronate (Aredia®) Alendronate (Fosamax®) Risedronate (Actonel®, Atelvia®) Ibandronate (Boniva®, IV and PO) Zoledronate (Reclast® IV, Zometa® IV) |
Bisphosphonates
Uses: Osteoporosis; Osteopenia; Bone metastases; Hypercalcemia; Hyper-parathyroidism Pathophys: Deposits in bone; Retards formation and dissolution of hydroxyapatite crystals; and ***Inhibits bone reabsorption by suppressing osteoclast activity*** Side Effects: Gastric irritation (PO); Adynamic bone; Possible renal failure; Osteonecrosis of the jaw (rare); Atrial fibrillation Special Administration Considerations: PO: Take first thing in the morning on an empty stomach with a full glass of water & do not lie down for 30-60 minutes after taking IV: Pre-medicate to alleviate flu-like syndrome |
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Cinacalcet (Sensipar®)
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Uses:
Hypercalcemia in patients with parathyroid carcinoma . Secondary hyperparathyroidism in patients with chronic kidney disease (***) on dialysis. Severe hypercalcemia in patients with primary hyperparathyroidism who are unable to undergo parathyroidectomy. Effects: ***Allosterically increases the sensitivity of the calcium sensing receptor (CaSR) in the parathyroid gland to calcium*** Lowers PTH Normalizes serum calcium SE: N/V |
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Life Style Mod for hyperPTism
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Hydration
Avoid lithium (desensitizes Ca++ sensing receptor, PT) and thiazides (drive Na/Ca co-transport in distal tubule) Can use loop diuretics in well hydrated patients Low calcium diet Supplement to fix low vitamin D levels |
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Phosphate Binders
Ca++ containing |
Calcium containing:
Calcium carbonate (Tums®, Caltrate®) Calcium acetate (Phos-Lo ®) Action: Form insoluble that bind phosphate and carry through bowel. Side Effects: Hypercalcemia*** Constipation Gas Bloating Pruritis |
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Phosphate Binders
Non-Ca++ containing |
Sevelamer carbonate (Renvela®)***
Sevelamer hydrocholride (Renagel®)*** Lanthanum carbonate (Fosrenol®)*** Action: Non-absorbable polymers that bind phosphate and carry through bowel. Side effects: HTN, Hypotension, N/V/D, Abd Pain |
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Inactive VitD Deriv
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Cholecalciferol (vitamin D3)
Natural form Inactive OTC Ergocalciferol (vitamin D2) Plant-derived Less potent (equivalent effects) Inactive OTC |
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Active VitD Deriv
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Calcitriol (Rocaltrol®, Calcijex®) D3***
Doxercalciferol (Hectorol®) D2 Paricalcitol (Zemplar®) D3 Calcitriol -Most potent agent Stimulate intestinal calcium and phosphate transport and bone reabsorption Rx only Used w/ Hyper/HypoPTism |
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Ca++ Supplementaiton
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Calcium carbonate (Caltrate®)
40 % calcium Better absorption in acidic environment Take with meals Calcium citrate (Citracal®) 21 % calcium Better for patients taking acid reducing medications (protein pump inhibitors or H2 receptor antagonists) |
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Teriparatide (Forteo®)
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Recombinant PTH 1-34
Stimulates bone turnover Indications: Osteoporosis Not PTH deficiency per se… Side effects: Orthostatic hypotension Hypercalcemia Hypercalciuria |
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Sodium Fluoride (Luride®)
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Deposits in bone and teeth
Action: Replaces the hydroxyl group in calcium phosphate salts (hydroxyapatite) Forms fluoroapatite More resistant to decay and absorption Side effects: May be toxic (neurotoxin) Makes bones hard but “brittle”. Fewer breaks but more shattering*** Dental fluorosis |
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Hydrochlorothiazide (HydroDIURIL®)
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One of the hydroclorothiazides
JNC Says: First line of pharmacological treatment for hypertension. USE: hypoPTism Actions: Water and sodium loss Potassium wasting*** CALCIUM RETAINING*** Rationale: Elderly more susceptible to hypertension Elderly more susceptible to osteoporosis Despite potassium wasting, calcium retention is worth it. |
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Dexamethasone (Decadron)***
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Glucocorticoid Receptor Ag (cutaneous)
USE: topical TX of rashes, irritaitons, derm inflamm, & slows scar formation SE: occasional irritaiton, slows local rate of healing USED FOR DEXAMETHASONE SUPPRESSION TEST (shuts off ACTH) |
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Methylprednisolone (Medrol)***
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Depot
SE: easy to administer, very difficult to titrate |
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Budesonide (Rhinocort)***
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Glucocorticoid Receptor Ag (inhaler, nasal spray)
USE: Asthma & other pulm/airway inflamm. SE: oral/pharynangial candidiasis |
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Ketoconazole (Nizoral)***
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Blocks androgen (low does) and all adrenal/gonadal steroid hormones (higher doese)
USE: topical antifungal that inhibit P450 enzyme & cholesterol conversion. SE: rash, hives, resp crisis, depression (watch the liver) |
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Spironolactone (Aldactone)***
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Best choice in hyperaldosteronism TX.
May cause gynecomastia. |
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Etomidate (Amidate)***
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Anesthetic
Low dose shown to control acute cortisole induced psychosis (useful w/ Thyroxine Storm) |
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Mifeprex***
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MOA: progesterone receptor antag. At high conc blocks glucocorticoid receptor.
-->therapeutic abortion (CI in preg) ADE: prolonged bleeding time, bacterial infxn, sepsis SE: N/V/D, cramps, abd vaginal bleeds, HA |
