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OBI Drugs Exam 3

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Term
Definition
Penicillin G   beta-lactam that inhibits PBP; by injection only covers anaerobes but not Gram -  
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Penicillin V   beta-lactam that inhibits PBP; given orally covers anaerobes but not Gram -  
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Amoxicillin   extended spectrum beta-lactam; improved Gram - coverage  
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Ampicillin   extended spectrum beta-lactam, take around meals; improved Gram - coverage  
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Clavulanic acid   beta-lactamase inhibitor, used in combination with other beta-lactams; extends spectrum of penicillins to include more Gram -  
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Cephalexin   inhibits cross-linking by PBPs; good for odontogenic infects, covers Gram +, Gram - and anaerobes  
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Doxycycline   binds to 30S ribosomal subunit to stop addition of next amino acid by prohibiting tRNA from binding; antibiotic of choice for intracellular and spirochetes  
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Clindamycin   binds to 50S ribosomal subunit and prevents binding of next amino acid; covers Gram + and anaerobes  
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Azithromycin   binds to 50S ribosomal subunit and stalls translocation by blocking exit tunnel; covers Gram + and intracellular bacteria, IE prophylaxis  
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Moxifloxacin   binds to topoisomerase and fragments DNA; bactericidal, used for respiratory infections with Strep pneumonia and Mycoplasma  
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Metronidazole   fragments DNA, narrow spectrum; anaerobic infections and C. diff  
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Sulfamethoxazole/Trimethoprim   deplete folate and synthesis of nucleic acids; fragments DNA, narrow spectrum, bactericidal, covers UTIs, pneumonia, community-acquired MRSA  
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Regular insulin   translocation of GLUT4 receptors to cell surface; fast-acting, peaks in 2-4 hours  
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Glimepride and Nateglinide   blocks ATP-dependent K channels to make more insulin; T2DM add-on therapy  
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Metformin   lowers hepatic glucose production by lowering glucagon; T2DM first-line therapy and oral cancers  
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Acarbose   inhibits alpha-glucosidase so carbohydrates are not absorbed by brush border in intestine; T1&2DM, lowers glucose levels after meals  
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Pioglitazone   'insulin sensitizer'; increases GLUT4 receptors in muscle and adipose tissue and lowers glucagon in liver -also stores FFA's via PPAR  
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Sitaglipin   prolongs GLP-1 action to promote first phase insulin secretion during meals  
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Canagliflozin   blocks SGLT2 in kidney to block glucose reabsorption in proximal tubule  
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Phenytoin   selective Na-channel blocker; treats all seizures except absence, gingival overgrowth  
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Carbamazepine   selective Na-channel blocker; treats tonic-clonic, focal, and trigeminal neuralgia  
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Valproic Acid   Na-channel blocker, weak Ca-channel blocker; multiple seizure disorder, migraines, bipolar disorder  
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Ethosuximide   Ca-channel blocker in thalamus; only treats absence seizures, causes bone marrow depression  
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Levetiracetam   binds to SV2A so vesicles not released by presynaptic neurons; treats tonic-clonic and focal seizures  
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Pregabalin   decreases expression of presynaptic Ca channels; treats focal seizures and chronic pain disorders  
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Paclitaxel   promotes microtubule polymerization so cells are arrested in mitosis; cancer drug that is inactivated by CYP450s  
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Doxorubicin   inhibits topoisomerase II to fragment DNA; useful for blood cancers and solid tumors but generates ROS's  
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Cyclophosphamide   alkylates cell components to damage DNA; used for cancers and transplant rejections (CYP450)  
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Methotrexate   inhibits DHFR to block tetrahydrofolate for nucleotide synthesis; used for cancers, arthritis, psoriasis but highly protein bound and displaced by phenytoin and sulfonamides  
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5-Fluorouracil   inhibits RNA function and pyrimidine formation; cancer drug  
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Tamoxifen   inhibitor and partial agonist of estrogen receptor; for ER+ breast cancers  
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Anastrozole   inhibits aromatase that makes estradiol for ER+ breast cancers  
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Leuprolide   resembles RnRH cousing surge in LH/FSH and decrease in testosterone; treats prostate cancer  
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Cisplatin   cross-links and alkylates DNA; primary drug for treatment of lung cancer  
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Trastuzumab   antibody fragment that disrupts HER-2/neu, a receptor that develops in cancers after first line therapy  
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Ipilimumab   blocks CTLA4 to activate cytotoxic T-cells; inhibits tumor growth, melanoma but very expensive  
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Teriparatide   N-terminal of PTH, increases osteoblast activity; high fracture-risk patients  
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Alondronate   BP, disrupts osteoclasts; oral, for osteoporosis  
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Zoledronic Acid   BP, disrupts osteoclasts; by injection only and more potent, for bone metastases  
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Denosumab   mimics OPG that prevents RANKL from binding to RANK and activating osteoclasts; used for bone metastases pain and hypercalcemia  
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L-DOPA:carbidopa   dopamine supplement, crosses BBB; treatment of Parkinson's disease  
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Pramipexole   dopamine agonist; for mild PD or adjunctive  
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Entacapone   COMT inhibitor, reduces degradation of L-DOPA in periphery so more can get to CNS for PD -caution with epinephrine  
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Selegiline   irreversible MAO-B inhibitor, reduces dopamine degradation in CNS -caution with epinephrine  
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Olanzapine/Clozapine   2nd generation antipsychotics; alleviates positive and negative symptoms of schizophrenia with fewer side effects  
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Chlorpromazine/Halopendol   1st generation antipsychotics; alleviates more positive symptoms with many adverse effects  
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Diazepam, Triazolam, Midazolam   bind GABA receptor to open Cl channel and inhibit cell transmission; conscious sedation, insomnia, anxiety  
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Flumazenil   competitive inhibitor of BDZs; reversal of BDZ sedation and overdose  
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Escitalopram   SSRI; treats depression and anxiety  
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Fluoxetine   SSRI with some norepinephrine reuptake inhibition; treats depression, OCD, panic disorder  
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Bupropion   atypical antidepressant, inhibits dopamine and norepinephrine reuptake; no serotonergic effects, treats depression and nicotine withdrawal  
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Mirtazapine   atypical antidepressant, blocks alpha-2 adrenergic, H1 histaminergics and serotonin reuptake; antidepressant without serotonergic effects  
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Amitryptiline   TCA, blocks serotonin and norepinephrine reuptake, Na, alpha-1, H1 and M1 channels; treats depression and neuropathic pain  
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Cimetidine, birth control, Verapamil, Diltiazem, anti-fungals, Erythromycin, Clarithromycin   inhabited BDZ metabolism  
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Anticonvulsants, corticosteroids, St. John's Wort   induce BDZ metabolism  
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