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Eletriptan brand name and class?
Relpax
Class: Antimigraine Serotonin Receptor Agonist
Eletriptan common FDA label indication, dosing, and titration?
Migraine: 20-40 mg po at onset of migraine, may repeat after 2 h prn; max single dose 40 mg, max daily dose of 80 mg/d
Eletriptan MOA?
Eletriptan binds with high affinity to serotonin (5-HT) subtypes 1B, 1D, and 1F receptors. It has no significant affinity or pharmacological activity at adrenergic α1, α2, or β; dopaminergic D1 or D2; muscarinic; or opioid receptors. Serotonin receptor agonists are believed to be effective in migraine, either through vasoconstriction (via activation of 5-HT1 receptors located on intracranial blood vessels) or through activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system, resulting in the inhibition of proinflammatory neuropeptide release.
Eletriptan box warnings?
None
Eletriptan contraindications?
Hypersensitivity to eletriptan, cerebrovascular syndromes, hemiplegic or basilar migraine, ischemic bowel disease, ischemic heart disease, peripheral vascular disease, severe hepatic impairment, uncontrolled HTN, coronary artery vasospasm, cardiac arrythmias 5-HT1 agonist or ergotamine medication
Eletriptan drug interactions?
SSRIs → additive serotonergic effects → avoid concurrent use; if not possible, monitor carefully for signs of serotonin syndrome
CYP3A4/5 inducers → increased eletriptan metabolism reduces eletriptan effectiveness → monitor and consider dose increases of eletriptan
CYP3A4/5 inhibitors → decreased eletriptan metabolism increases risk of eletriptan toxicity → monitor and consider dose decreases of eletriptan
Other 5-HT agonists → additive pharmacologic effect leading to additive toxicity → administration within 24 h of other serotonin agonists is contraindicated
Eletriptan ADR?
Common - weakness
Less common - chest pain, nausea, asthenia, dizziness, somnolence, palpitations, weakness
Rare but serious - cardiac dysrhythmia, coronary arteriosclerosis, heart block, HTN, AMI, aphasia, cerebral ischemia, stroke, dystonia, hemiplegia, neuropathy, transient ischemic attack, oculogyric crisis
Emplagliflozin brand name and class?
Jardiance
Class: Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitor, Antidiabetic
Emplagliflozin common FDA label indication, dosing, and titration?
Diabetes Mellitus, type 2: 10-25 mg po daily; titrate to effect, max dose 25 mg po daily
Chronic kidney disease: 10 mg po daily
Heart failure, in combination with other agents: 10 mg po daily
Emplagliflozin MOA?
Empagliflozin inhibits sodium-glucose cotransporter 2 (SGLT2) in the proximal renal tubules, reducing reabsorption of filtered glucose from the tubular lumen resulting in increased urinary secretion and reduced plasma glucose.
Emplagliflozin box warnings?
None
Emplagliflozin contraindications?
Hypersensitivity
Emplagliflozin drug interactions?
Beta-blockers → altered glucose metabolism and increased risk of hypoglycemia. Symptoms of hypoglycemia masked → avoid propanolol, use others with caution and increased monitoring
Fluoroquinolones, NSAIDs, fenofibrate, SSRIs, somatostatin analogues → altered glucose metabolism and increased risk of hypoglycemia and hyperglycemia → avoid concurrent use if possible; monitor and consider dose adjustments
MAOIs → stimulation of insulin secretion, hypoglycemic effects → avoid concurrent use if possible; monitor and consider dose adjustments
Psyllium → psyllium may delay absorption of glucose from meals → avoid concurrent use if possible; monitor and consider dose adjustments
Sulfonamides → increased risk of hypoglycemia → monitor blood glucose and consider dose adjustments of sulfonylureas
Emplagliflozin ADR?
Common - none
Less common - urinary tract infection,genititourinary fungal infections, increased hematocrit
Rare but serious - acute kidney injury, hypersensitivity, hypotension, ketoacidosis, increased risk of bone fractures, increased risk of lower limb amputations
Estradiol (PO) brand name and class?
Estrace
Class: Estrogen
Estradiol (PO) common FDA label indication, dosing, and titration?
Abnormal vasomotor function (moderate to severe), menopause: 1-2 mg po daily for 21 d followed by 7 d off
Atrophic vulva or vagina (moderate to severe), menopause: oral tablet, 1-2 mg po daily in a cyclical pattern (3 wk on, 1 wk off)
Breast cancer, metastatic, for palliation only: 10 mg po tid x 3 mo
Carcinoma of prostate, advanced, androgen-dependent, for palliation only: 1-2 mg po tid
Decreased estrogen level, secondary to hypogonadism, castration, or primary ovarian failure: 1-2 mg po daily
Postmenopausal osteoporosis, prophylaxis: 0.5 mg po daily for 23 d followed by 5 d off
Estradiol (PO) MOA?
Estradiol (17β-estradiol; E2) is the most potent of the naturally occurring estrogens and the major estrogen secreted during the reproductive years. Estradiol and other estrogens produce characteristic effects on specific tissues (such as breast), cause proliferation of vaginal and uterine mucosa, increase calcium deposition in bone, and accelerate epiphyseal closure after initial growth stimulation.
Estradiol (PO) box warnings?
Should not be used to decrease risk of CV disease, increased risk of endometrial cancer, breast cancer, or dementia; secondary exposure risk (transdermal solution)
Estradiol (PO) contraindications?
Hypersensitivity to estradiol; history of thromboembolic disorders, breast cancer, any estrogen-dependent neoplasm, known or suspected pregnancy, abnormal uterine bleeding not evaluated by provider
Estradiol (PO) drug interactions?
Aromatase inhibitors → estradiol may counteract the effect of aromatase inhibitors → avoid concurrent use
CYP3A4/5, 1A2, P-gp inducers → increased estradiol metabolism or transport reduces estradiol effectiveness → consider dose increases of estradiol
CYP3A4/5, 1A2, P-gp inhibitors → decreased estradiol metabolism or transport increases risk of estradiol toxicity → consider dose decreases of estradiol
Estradiol (PO) ADR?
Common - none known
Less common - weight change, nausea, vomiting, disturbance in mood, swelling of breast, depression, headache
Rare but serious - heart disease, MI, DM, venous thromboembolism, anaphylaxis, cerebrovascular accident, PE, breast, endometrial or ovarian cancer
Estradiol (transdermal patch) brand name and class?
Alora, Climara, Minivelle, Menostar, Vivelle-DOT
Class: Estrogen
Estradiol (transdermal patch) common FDA label indication, dosing, and titration?
Abnormal vasomotor function or atrophic vagina or vulva (moderate-severe), menopause: 0.025-0.0375 mg/d patch applied to the skin twice weekly (dose and frequency of patch change dependent on specific product selected); adjust dose as necessary based on response and attempt taper and discontinuation at 3-6 mo intervals
Postmenopausal osteoporosis, prophylaxis: 0.014-0.025 mg/d patch applied to the skin once or twice weekly (dose and frequency of patch change dependent on specific product selected); adjust dose as necessary based on response
Decreased estrogen level, secondary to hypogonadism, castration, or primary ovarian failure: 0.1 mg/d patch applied to the skin once or twice weekly (dose and frequency of patch change dependent on specific product selected)
Estradiol (transdermal patch) MOA?
Estradiol (17β-estradiol; E2) is the most potent of the naturally occurring estrogens and the major estrogen secreted during the reproductive years. Estradiol and other estrogens produce characteristic effects on specific tissues (such as breast), cause proliferation of vaginal and uterine mucosa, increase calcium deposition in bone, and accelerate epiphyseal closure after initial growth stimulation.
Estradiol (transdermal patch) box warnings?
Should not be used to decrease risk of CV disease, breast cancer, or dementia; increased risk of endometrial cancer; secondary exposure risk (transdermal solution)
Estradiol (transdermal patch) contraindications?
Hypersensitivity to estradiol; history of thromboembolic disorders, breast cancer, any estrogen-dependent neoplasm, known or suspected pregnancy, abnormal uterine bleeding not evaluated by provider
Estradiol (transdermal patch) drug interactions?
Aromatase inhibitors → estradiol may counteract the effect of aromatase inhibitors → avoid concurrent use
CYP3A4/5, 1A2, P-gp inducers → increased estradiol metabolism or transport reduces estradiol effectiveness → consider dose increases of estradiol
CYP3A4/5, 1A2, P-gp inhibitors → decreased estradiol metabolism or transport increases risk of estradiol toxicity → consider dose decreases of estradiol
Estradiol (transdermal patch) ADR?
Common - edema, application site irritation
Less common - abdominal pain, breakthrough bleeding, nausea, vomiting, disturbance in mood, swelling of breast, depression, weight change
Rare but serious - heart disease, MI, DM, venous thromboembolism, anaphylaxis, cerebrovascular accident, PE, breast, endometrial or ovarian cancer
Etanercept brand name and class?
Enbrel, Erelzi
Class: Antirheumatic, Disease-Modifying, Tumor Necrosis Factor (TNF)-Blocking Agent
Etanercept common FDA label indication, dosing, and titration?
Ankylosing spondylitis, treatment refractory: adults, 50 mg SUBQ once per wk or 25 mg SUBQ twice per wk
Polyarticular juvenile idiopathic arthritis: children > or = 2 y of age and <63 kg, 0.8 mg/kg (max 50 mg) SUBQ once per wk; > or = 63 kg, 50 mg once per wk
Plaque psoriasis: children > or = 4y of age, 0.8 mg/kg/dose (max 50 mg) SUBQ once per wk; adults, 50 mg twice per wk x 3 mo, then 50 mg SUBQ once per wk
Psoriatic arthritis: adults, 50 mg SUBQ once per wk or 25 mg SUBQ twice per wk
Rheumatoid arthritis: adults, 50 mg SUBQ once per wk or 25 mg SUBQ twice per wk
Etanercept MOA?
Etanercept is a recombinant DNA-derived protein composed of tumor necrosis factor receptor linked to the Fc portion of human IgG1. Etanercept binds to soluble human tumor necrosis factor alpha with the p55 and p75 cell surface tumor necrosis factor receptors.
Etanercept box warnings?
Serious infections, malignancies
Etanercept contraindications?
Hypersensitivity, sepsis
Etanercept drug interactions?
Anti-TNF agents → increased risk of serious infection with concurrent use → avoid concurrent use
Immunosuppressants → additive immunosuppression → avoid concurrent use or monitor for additive immunosuppression if combined
Live vaccines → increased risk of vaccine adverse effects → avoid concurrent use and for at least 3 mo after discontinuation of adalimumab
Inactive vaccines → diminished vaccine efficacy → administer vaccine > or = 2 wk prior to treatment initiation
Etanercept ADR?
Common - diarrhea, headache, skin rash, infections antibody development, injection site reactions
Less common - dizziness, nausea
Rare but serious - serious infections, reactivation of latent infections, malignancies, heart failure
Ethinyl Estradiol and Etonogestrel Ring brand name and class?
NuvaRing, EluRyng, EnilloRing
Class: Contraceptive
Ethinyl Estradiol and Etonogestrel Ring common FDA label indication, dosing, and titration?
Contraception: 1 ring inserted vaginally by patient and remaining continuously for 3 wk, then removed for 1 wk; a new ring is then inserted, regardless whether bleeding has or has not finished
Ethinyl Estradiol and Etonogestrel Ring MOA?
See preface c card: general content related to all oral contraceptives
Ethinyl Estradiol and Etonogestrel Ring box warnings?
Cardiovascular risk with concurrent cigarette smoking
Ethinyl Estradiol and Etonogestrel Ring contraindications?
Hypersensitivity to ethinyl estradiol or progestin component; history of thromboembolic disorders, endometrial cancer, breast cancer history, abnormal uterine bleeding not evaluated by HCP, uncontrolled HTN, pregnancy; smoking > or = 15 cigarettes per d and > 35 y of age, hepatic tumors, HCV drug combinations
Ethinyl Estradiol and Etonogestrel Ring drug interactions?
See preface C card: general content related to all oral contraceptions
Ethinyl Estradiol and Etonogestrel Ring ADR?
Common - headache, intermenstrual bleeding, vaginitis
Less common - abdominal pain, acne, amenorrhea, mood changes, nausea, vomiting, vaginal discharge, weight gain
Rare but serious - AMI, anaphylaxis, angioedema, thromboembolism, galactorrhea not associated with childbirth, hypersensitivity reaction, toxic shock syndrome, urticaria, thromboembolism
Ezetimibe brand name and class?
Zetia
Class: Antihyperlipidemic, Cholesterol Absorption Inhibitor
Ezetimibe common FDA label indication, dosing, and titration?
Familial hypercholesterolemia-homozygous, with atorvastatin or simvastatin: adults and children > or = 10 y of age, 10 mg po daily
Mixed hyperlipidemia: 10 mg po daily in combination with fenofibrate
Primary hypercholesterolemia: 10 mg po daily, alone, or in combination with an HMG-CoA reductase inhibitor (statin)
Homozygous famial sitosterolemia: adults and children > or = 9 y of age, 10 mg po daily
Ezetimibe MOA?
Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of statins and of fenofibrate.
Ezetimibe box warnings?
None
Ezetimibe contraindications?
Hypersensitivity to ezetimibe, gallbladder disease, severe hepatic dysfunction, concurrent use with a statin in a pregnant or nursing mother
Ezetimibe drug interactions?
Cholestyramine, colestipol → decreased absorption of ezetimibe → separate administration by 2-4 h
Fibrates → increased risk of cholelithiasis or myopathy → avoid concurrent use or monitor for cholelithiasis and myopathy
Warfarin → increased risk of bleeding → monitor INR and consider dose adjustments
Ezetimibe ADR?
Common - none known
Less common - abdominal pain, constipation, diarrhea, headache, increased liver enzymes, myopathy, nausea
Rare but serious - rhabdomyolysis, cholelithiasis, hepatotoxicity, agranulocytosis, pancreatitis
Febuxostat brand name and class?
Uloric
Class: Xanthine Oxidase Inhibitor
Febuxostat common FDA label indication, dosing, and titration?
Hyperuricemia in patients not adequately treated with, or having adverse effects from, allopurinol: 40 mg po daily, may titrate to 120 mg po daily
Febuxostat MOA?
Selectively inhibits xanthine oxidase, the enzyme responsible for converting xanthine to uric acid. Lowers uric acid and reduces gout.
Febuxostat box warnings?
Increased risk of death (cardiac, all-cause)
Febuxostat contraindications?
Concurrent azathioprine or mercaptopurine
Febuxostat drug interactions?
Substrates for xanthine oxidase (azathioprine, didanosine, mercaptopurine, theophylline) → decreased metabolism of xanthine oxidase substrates and increased toxicity → concurrent use of azathioprine, didanoside, and mercaptopurine is contraindicated; use theophylline with caution
Pegloticase → increased risk of infusion reaction and anaphylaxis to pegloticase → febuxostat should be discontinued prior to pegloticase administration
Rosuvastatin → increased concentration and toxicity of rosuvastatin → limit maximum rosuvastatin dose to 20 mg/d when combined, monitor for increased rosuvastatin toxicity
Ubrogepant → increased concentration and toxicity of Ubrogepant → consider dose reduction of ubrogepant when used concurrently
Febuxostat ADR?
Common - none known
Less common - rash, nausea, elevated LFTs, arthralgia
Rare but serious - ECG abnormalities, hypersensitivity, stroke, mood changes, drug reaction rash with eosinophilia and systemic symptoms