Random pharmacology Flashcards
Fulvestrant
- A “pure” estrogen antagonist
- Associated with a much lower risk of causing endometrial pathology, including cancer than raloxifene or toremifene
Ranolazine
- MECHANISM: inhibits late phase of sodium current thereby reducing diastolic wall tension and oxygen consumption; does not affect HR or contractility
- CLINICAL USE: angina refractory to other medical therapies
- ADVERSE EFFECTS: constipation, dizziness, headache, nausea, QT prolongation
Cinacalcet
- MECHANISM: sensitizes Ca2+ sensing receptor (CaSR) in parathyroid gland to circulating Ca2+, leads to decrease in PTH
- CLINICAL USE: primary or secondary hyperparathyroidism
- ADVERSE EFFECTS: hypocalcemia
Orlistat
- MECHANISM: inhibits gastric and pancreatic lipase and leads to a decrease in breakdown and absorption of dietary fats
- CLINICAL USE: weight loss
- ADVERSE EFFECTS: steatorrhea, decreased absorption of fat-soluble vitamins
Ursodiol (ursodeoxycholic acid)
- MECHANISM: nontoxic bile acid that increases bile secretion and decreases cholesterol secretion and absorption
- CLINICAL USE: primary biliary cirrhosis, gallstone prevention or dissolution
Cladribine
- MECHANISM: purine analog that works through multiple mechanisms (eg inhibition of DNA polymerase, DNA strand breaks); an antimetabolite
- CLINICAL USE: hairy cell leukemia
- ADVERSE EFFECTS: myelosuppression, nephrotoxicity, neurotoxicity
Cytarabine (arabinofuranosyl cytidine)
- MECHANISM: pyrimidine analog that leads to the inhibition of DNA polymerase; an antimetabolite
- CLINICAL USE: leukemias (AML), lymphomas
- ADVERSE EFFECTS: myelosuppression with megaloblastic anemia (“CYTarabine causes panCYTopenia”)
Nitrosureas (carmustine, lomustine, semustine, streptozocin)
- MECHANSIM: requires bioactivation; works as an alkylating agent; crosses blood brain barrier into the CNS where it crosslinks DNA
- CLINICAL USE: brain tumors (including glioblastoma multiforme)
- ADVERSE EFFECTS: CNS toxicity (convulsions, dizziness, ataxia)
Erlotinib
- MECHANISM: EGFR tyrosine kinase inhibitor
- CLINICAL USE: non-small cell lung cancer
- ADVERSE EFFECTS: rash
Cetuximab
- MECHANISM: monoclonal antibody against EGFR
- CLINICAL USE: stage IV colorectal cancer (wild-type KRAS), head and neck cancer
- ADVERSE EFFECTS: rash, elevated LFTs, diarrhea
Vemurafenib
- MECHANISM: small molecule inhibitor of BRAF oncogene (+) melanoma
- CLINICAL USE: metastatic melanoma
Leflunomide
- MECHANISM: reversibly inhibits dihydroorate dehydrogenase, preventing pyrimidine synthesis; suppresses T cell proliferation
- CLINCIAL USE: rheumatoid arthritis, psoriatic arthritis
- ADVERSE EFFECTS: diarrhea, hypertension, hepatotoxicity, teratogenicity
Teriparatide
- MECHANISM: recombinant PTH analog given subcutaneously daily, increases osteoblastic acitivity
- CLINICAL USE: osteoporosis; causes increase in bone growth compared to antiresorptive therapies (eg bisphosphonates)
- ADVERSE EFFECTS: transient hypercalcemia
Etanercept
- MECHANISM: TNF-alpha inhibitor; fusion protein (receptor for TNF-alpha + IgG1, Fc), produced by recombinant DNA; acts as a TNF decoy receptor
- CLINICAL USE: rheumatoid arthritis, psoriasis, ankylosing spondylitis
Infliximab, adalimumab
- MECHANSIM: TNF-alpha inhibitor; anti-TNF-alpha monoclonal antibody
- CLINICAL USE: inflammatory bowel disease, rheumatoid arthritis, psoriasis, ankylosing spondylitis
Rasburicase
- MECHANISM: recombinant uricase that catalyzes metabolism of uric acid to allantoin
- CLINICAL USE: prevention and treatment of tumor lysis syndrome
Cyclobenzaprine
- MECHANISM: centrally acting skeletal muscle relaxant; structurally related to TCAs, similar to anticholinergic side effects
- CLINICAL USE: muscle spasms
Varenicline
- Atypical antidepressant
- Nicotinic ACh receptor partial agonist
- Used for smoking cessation
- TOXICITY: sleep disturbance
Clomiphene
- Selective estrogen receptor modulator
- Antagonist at estrogen receptors in hypothalamus
- Prevents normal feedback inhibition and increases release of LH and FSH from pituitary, which stimulates ovulation
- Used to treat infertility due to anovulation (eg PCOS)
May cause hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances
Tamoxifen
- Selective estrogen receptor modulator
- Antagonist at breast
- Agonist at bone, uterus
- Increase risk of thromboembolic events and endometrial cancer
- Used to treat and prevent recurrence of ER/PR (+) breast cancer
Raloxifene
- Selective estrogen receptor modulator
- Antagonist at breast, uterus
- Agonist at bone
- Increase risk of thromboembolic events but no increased risk of endometrial cancer (vs tamoxifen)
- Used primarily to treat osteoporosis
Anastrozole, letrozole, exemestane
- Aromatase inhibitor
- MECHANISM: inhibit peripheral conversion of androgens to estrogens
- CLINICAL USE: ER(+) breast cancer in postmenopausal women
Mifepristone, ulipristal
- Antiprogestin
- MECHANISM: competitive inhibitors of progestins at progesterone receptors
- CLINICAL USE: termination of pregnancy (mifepristone with misoprostol); emergency contraception (ulipristal)
Terbutaline, ritodrine
- Beta-2 agonists that relax the uterus
- Used to decrease contraction frequency in women during labor
Danazol
- MECHANISM: synthetic androgen that acts as partial agonist at androgen receptor
- CLINICAL USE: endometriosis, hereditary angioedema
- ADVERSE EFFECTS: weight gain, edema, acne, hirsutism, masculinization, decreased HDL levels, hepatotoxicity
Minoxidil
- MECHANISM: direct arteriolar vasodilator
- CLINICAL USE: androgenetic alopecia, severe refractory hypertension
Bosentan
- Pulmonary hypertension drug
- MECHANISM: competitively antagonizes endothelin-1 receptors which leads to a decrease in pulmonary vascular resistance
- CLINICAL NOTES: hepatotoxic (monitor LFTs)
Sildenafil
- MECHANISM: inihibits cGMP PDE-5 and prolongs vasodilatory effect of NO
- CLINICAL NOTES: used for pulmonary hypertension as well as erectile dysfunction
Epoprostenol, iloprost
- Pulmonary hypertension drug
- MECHANISM: PGI2 (prostacyclin) with direct vasodilatory effects on pulmonary and systemic arterial vascular beds, also inhibits platelet aggregation
- ADVERSE EFFECTS: flushing, jaw pain
Fluticasone, budesonide
- Inhaled corticosteroids used for asthma
- Inhibit synthesis of virtually all cytokines
- Inactivate NF-KB , the transcription factor that induces production of TNF-alpha and other inflammatory agents
- 1st line therapy for chronic asthma
Omalizumab
- Anti-IgE monoclonal therapy for asthma
- Binds mostly unbound serum IgE and blocks binding to FcERI
- Used in allergic asthma with increased IgE levels resistant to inhaled steroids and long acting beta-2 agonists
- ADVERSE EFFECTS: anaphylaxis (mostly occurs on initial dose)
Tesamorelin
- GHRH analog
- Used to treat HIV-associated lipodystrophy