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Pharm 34X > Midterm 2 drugs > Flashcards

Midterm 2 drugs Flashcards

1
Q

Amantadine

A

prophylaxis + tx of Influenza A
inhibit pH dependent uncoating of the virus in cells by blocking M2 proton channel in viral envelope
CNS effects at higher doses
rapid emergence of resistance

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2
Q

Rimantadine

A

prophylaxis + tx of Influenza A
inhibit pH dependent uncoating of the virus in cells by blocking M2 proton channel in viral envelope
rapid emergence of resistance

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3
Q

Oseltamivir

A

Tamiflu
enables more rapid recovery from influenza A + B
Neuraminidase inhibitor - transition state analogue
side effects: nausea and vomiting

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4
Q

Probenecid

A

transport blocker in kidneys to ↓ drug clearance
co administered with Oseltamivir to maintain peak plasma concentrations

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5
Q

Zanamivir

A

Relenza
enables more rapid recovery from influenza A + B
competitive neuraminidase inhibitor
activity against Oseltamivir resistant H5N1
side effects: nausea, diarrhea, sinusitis

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6
Q

Acyclovir

A

inhibits replication of HSV + VZV
prodrug - acyclic nucleoside analogue = inhibits viral DNApol

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7
Q

Ganciclovir

A

inhibits replication of HSV + CMV (tx of CMV retinitis)
prodrug - acyclic nucleoside analogue = inhibits viral DNApol
dose limiting toxicity = myelosuppression

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8
Q

Phosphonoformic acid

A

tx of CMV retinitis, 2nd line tx of HSV + VZV
pyrophosphate analog → blocks PPi binding site of viral DNApol
dose limiting toxicity = renal toxicity

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9
Q

Ribavirin

A

broad spectrum tx of DNA + RNA viruses
only tx for RSV
prodrug - purine guanosine analog
R5MP = inhibits IMP dehydrogenase = blocks formation of GMP
R5TP = RNA mutagen
= depletion of GTP and dGTP

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10
Q

HAART

A

standard therapy for HIV
triple drug cocktail

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11
Q

AZT (Zidovudine)

A

HIV tx
nucleoside reverse transcriptase inhibitors
bone marrow suppression → severe anemia and neutropenia

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12
Q

Didanosine

A

HIV tx
nucleoside reverse transcriptase inhibitors
dideoxynucleoside
painful peripheral neuropathy + pancreatitis

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13
Q

Zalcitabine

A

HIV tx
nucleoside reverse transcriptase inhibitors
dideoxynucleoside
peripheral neuropathy

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14
Q

3TC (Lamivudine)

A

HIV tx (+HBV)
nucleoside reverse transcriptase inhibitor
cytidine analog
occasional neutropenia
rapid emergence of drug-resistance when used alone

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15
Q

Nevirapine

A

HIV tx
non-nucleoside reverse transcriptase inhibitors
active, bind to allosteric site on enzyme

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16
Q

Efavirenz

A

HIV tx
non-nucleoside reverse transcriptase inhibitors
active, bind to allosteric site on enzyme

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17
Q

Ritonavir

A

(-navir)
HIV tx
protease inhibitor = peptidomimetic
block activity of aspartate protease = blocks viral maturation
inhibitor of CYP3A4 + CYP2D6

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18
Q

Maraviroc

A

HIV tx
entry inhibitor
negative allosteric modulator of CCR5 on cells = prevents interaction with gp120

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19
Q

Enfuvirtide

A

HIV tx
fusion inhibitor
binds to gp41 and interferes with ability to merge two membranes
expensive + inconvenient dosing → salvage therapy

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20
Q

Raltegravir

A

(-tegravir)
HIV tx
integrase inhibitor
interferes with enzyme to insert genetic material into human DNA

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21
Q

Interferon alpha

A

tx of chronic HBV and HCV
(combined with ribavirin for chronic HepC)
natural protein made by monocytes and B cells
induces cellular enzymes to inhibit synthesis of viral mRNA and proteins
toxicity: acute flu-like syndrome; chronic therapy = myelosuppression + neurotoxicity

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22
Q

Telaprevir

A

(-previr)
tx of HCV
protease inhibitor
inhibits HCV serine protease = prevents viral replication → ↓ HCV RNA levels

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23
Q

Sofosbuvir

A

tx HCV
RNA polymerase inhibitor
prodrug
inhibits viral RNApol = RNA chain terminator
used in some combination of ribavirin, interferon, protease inhibitors
less prone to development of resistance

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24
Q

Bamlanivimab + Etesevimab

A

COVID19 tx
monoclonal ab
bind different but overlapping epitopes in spike protein RBD

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25
Casirivimab + Imdevimab
COVID19 tx monoclonal ab bind nonoverlapping epitopes of spike protein RBD
26
Tocilizumab
COVID19 tx monoclonal ab binds + inhibits IL-6 receptor = ↓ CRP tx of hospitalized adults with severe COVID19
27
Tixagevimab + Cilgavimab
COVID19 tx → effective against omicron variant monoclonal ab bind to non-overlapping regions of spike protein RBD tx when immunocompromised → no vaccine
28
Sotrovimab
COVID19 tx → effective against omicron variant monoclonal ab targets epitope in spike protein RBD conserved bw SARS and -2
29
Remdesivir
COVID19 tx viral RNApol inhibitor IV admin
30
Paxlovid
Covid19 tx oral admin of 300mg Nirmatrelvir + 100mg Ritonavir Mpro inhibitor + PK enhancer (inhibits CYP3A4 = ↓ metabolism)
31
Metamucil
tx of dyslipidemia fibre supplement slow gastric emptying + inhibit micelle formation
32
Simvastatin
tx of dyslipidemia statin = prevent cholesterol synthesis str analog = selective, reversible, competitive inhibitor of HMGCoA reductase → rate limiting step of cholesterol synthesis in liver high enz affinity ↓ VLDL secr, ↑ LDLR expr, ↑ HDL metabolized by CYP3A4 = grapefruit ↑ syst. bioavailability
33
Atorvastatin
tx of dyslipidemia statin = prevent cholesterol synthesis metabolized by CYP3A4 = grapefruit ↑ syst. bioavailability
34
Rosuvastatin
tx of dyslipidemia statin = prevent cholesterol synthesis metabolized by CYP2C9 = grapefruit does not affect syst. bioavailability
35
Gemfibrozil
tx of dyslipidemia fibrate activates PPAR-a ↑ HDL synthesis + secr, ↑ hepatic fatty acid uptake + B-oxidation, ↓ lipogenesis + storage, ↓ VLDL synthesis + sec, ↑ LDLR expr
36
Colesevelam
tx of dyslipidemia bile acid sequesterant positively charged = bind bile acids to prevent reabsorption force ↑ bile synthesis from cholesterol via CYP7A1
37
Niacin
tx of dyslipidemia nicotinic acid inhibits lipolysis of TGs by HSL in adipose tissue = ↓ transport of FFA to liver = ↓ plasma VLDL ↑ HDL by ↓ hepatic clearance of apoA1 + ↑ expression of ABCA1 reduces LP(a) side effects = facial flushing + itching
38
Ezetimibe
tx of dyslipidemia cholesterol absorption inhibitor selectively block NPC1L1 in GI epithelial cells does not affect absorption of fat soluble vitamins, TGs, or bile acids
39
Prednisone
medication that can contribute to weight gain corticosteroid induce insulin resistance and trigger visceral adiposity
40
Clozapine
medication that can contribute to weight gain atypical antipsychotic ↓ central serotonergic signaling + ↑ muscarinic signaling + NPY activity = ↑ appetite
41
Amitriptyline
medication that can contribute to weight gain older class of AD (TCA) ↓ central serotonergic signaling = ↑ appetite
42
Phenelzine
medication that can contribute to weight gain older class of AD (MAOI) ↓ central serotonergic signaling = ↑ appetite
43
Insulin / Glitazones
medication that can contribute to weight gain insulin: promotes nutrient storage → lipogenesis glitazones: promote adipose tissue differentiation + water retention
44
Phentermine
therapeutic strategy for obesity: appetite suppression sympthomimetic = blocks NE reuptake NE stimulation of POMC = anorexigenic pathway in hypot. side effects: HTN, tachycardia, addictive potential
45
Topiramate
therapeutic strategy for obesity: appetite suppression GABA signaling enhancer → suppresses NPY activity = enhances satiety also tx of seizures side effects: paraesthesia, dizziness, dysgeusia, insomnia, constipation, dry mouth
46
Qsymia
pill combination of phentermine + topiramate synergistic effects on central + peripheral metabolism side effects: composite of both drugs
47
Bupropion
NE-DA reuptake inhibitor (Wellbutrin = atypical AD) DA → ↓ reward seeking behaviour + ↓ cravings NE → ↓ appetite via POMC
48
Naltrexone
opioid receptor antagonist muOR → block autoinhibitory feedback from MC4R = ↑ POMC signaling
49
Contrave
therapeutic strategy for obesity: appetite suppression + ↑ energy expenditure combination of bupropion and naltrexone side effects: NE mediated = ↑ E/insomnia, dry mouth, headache, agitation
50
Setmelanotide
therapeutic strategy for obesity: appetite suppression MC4R agonist = potentiation of ↓ appetite use in pts with genetic forms of obesity → POMC, LEPR, leptin, BBS deficiency subq inj. → rx for pediatrics side effects: hyperpigmentation, sexual dysfxn, depression
51
Orlistat
therapeutic strategy for obesity: block nutrient absorption irreversible inhibitor of gastric + pancreatic lipases dietary fats are not broken down → no absorption = excreted side effects: ↓ absorption of fat-soluble vitamins, fecal incontinence, flatulence
52
Sitagliptin
therapeutic strategy for obesity: Incretin effect competitive inhibitor of DPP-4 (degrades incretins) small molecule, orally active potentiates actions of GLP-1: ↑ endog GLP-1, ↓ glucagon secr, ↓ hepatic glucose output, ↑ insulin release weight neutral therapy
53
Exenatide
therapeutic strategy for obesity: Incretin effect GLP-1 R agonist t1/2 = 2.4 hrs → twice daily inj.
54
Liraglutide
therapeutic strategy for obesity: Incretin effect GLP-1 R agonist t1/2 = 13 hrs → once daily inj.
55
Semaglutide
therapeutic strategy for obesity: Incretin effect GLP-1 R agonist t1/2 = 7 days → once weekly inj.
56
Rybelsus
oral semaglutide capsule, once daily combined with SNAC to enhance permeability and duration
57
Tirzepatide
therapeutic strategy for obesity dual agonist for GIP and GLP-1 = mitigate GI side effects of GLP-1 + prevent desensitization of GLP-1 receptors
58
Retatrutide
(clinical trials) therapeutic strategy for obesity GLP-1/glucagon co-agonist
59
Orforglipron
(clinical trials) therapeutic strategy for obesity small-molecule based GLP-1 RA overcome difficulties associated with peptides: tissue permeability, half life, production cost
60
Pramlintide
(clinical trials) therapeutic strategy for obesity amylin analogue = slow gastric emptying, suppresses inappropriate post-meal glucagon secretion, ↑ satiety
61
Obinepitide
(clinical trials) therapeutic strategy for obesity PYY analogue = inhibit NPY, AGRP signaling
62
TPN435
(clinical trials) therapeutic strategy for obesity AGRP receptor antagonist
63
Phen-Fen
(failure) therapeutic strategy for obesity combination of phentermine and fenfluramine (5HT - anorexigenic but adverse effects) potentially fatal pulmonary HTN, heart valve problems
64
Sibutramine
(failure) therapeutic strategy for obesity SNRI = inhibits reuptake of 5HT, DA, NE at hypothalamic sites that regulate food intake enhances satiety = appetite suppressant 5HT2C signaling at ARC = ↓ food intake BUT 16% ↑ in risk of major adverse cardiac events
65
Lorcaserin
(failure) therapeutic strategy for obesity 5HT2C R agonist = appetite suppressant stimulates POMC signaling → anorexigenic pathways in ARC small ↑ risk of cancer = withdrawn
66
Recombinant human insulin
tx of diabetes Insulin replacement therapy - human short acting = bolus
67
Protamine (NPH) insulin
tx of diabetes Insulin replacement therapy - human intermediate acting = basal slower absorption/longer duration of action → admin 1/2 per day
68
Lispro (Humalog)
tx of diabetes Insulin replacement therapy - analog rapid acting = bolus
69
Glargine (Tuojeo)
tx of diabetes Insulin replacement therapy - analog long acting = basal
70
Metformin
tx of diabetes insulin sensitizer first line therapy for T2D activates AMPK → potentiates targets of insulin signaling = ↓ glucose output, ↑ glucose uptake (↑ expr of GLUT4), ↓ hepatic fat = ↑ hepatic insulin sensitivity
71
Pioglitazone
tx of diabetes insulin sensitizer - Thiazoladinediones (glitazones) activates PPARy → alters transcription of enzymes involved in metabolism + proteins involved in insulin response ↑ transcription of LPL and GLUT4 adipose tissue = ↓ lipolysis + FFAs, ↓ TNFa + leptin, ↑ adiponectin can cause weight gain
72
Glibenclamide, Glimepiride
tx of diabetes sulfonylureas - target B-cell dysfunction block pancreatic B-cell KATP channel by binding to SUR subunit → depolarization of membrane = opens Ca2+ channels = stimulates insulin release glucose-blind → risk of hypoglycemia only works in early stages of T2D while B-cell function remains side effects = trigger arrhythmias
73
Acarbose
tx of diabetes a-glucosidase inhibitor = prevents release of glucose from complex carbs in intestine slows absorption of glucose, prevents initial post-prandial glucose spike also ↑ secretion of GLP-1 side effects: flatulence, diarrhea
74
Empagliflozin
tx of diabetes (-flozin) SGLT2 inhibitors = insulin independent effects inhibit renal reabsoprtion of glucose also protective against heart failure → osmotic diuresis side effects: risk of bladder infection, ketoacidosis
75
Penicillin
antibiotic (cell wall synthesis) B-lactam drug inhibits PBPs = inactivate peptidoglycan synthesis → ↑ osmotic pressure = cell lysis bactericidal; narrow spectrum of activity (some gram - and +)
76
Cephalosporin
antibiotic (cell wall synthesis) B-lactam drug with dihydrothiazine ring fused same mech of action as penicillin = inhibit PBPs bactericidal more resistant to opening of B-lactam ring gen 1 = narrow, gen 2-4 = broad spectrum
77
Vancomycin
antibiotic (cell wall synthesis) glycopeptide abx binds D-ala-D-ala in peptidoglycan to sequester substrate from transpeptidase = prevents elongation of chain and interferes with cell wall cross linking bactericidal; narrow spectrum (only gram +) side effects: ototoxicity and renal toxicity
78
Daptomycin
antibiotic (cell membranes) bind to cell membrane + cause rapid depolarization of membrane potential = intracellular inhibition of DNA, RNA, protein synthesis → bacterial cell death bactericidal
79
Polymyxin
antibiotic (cell membranes) disrupt charge of phospholipids by targeting lipopolysaccharide (in gram -) → membrane lysis bactericidal B = topical; E = IV (tx highly resistant) side effects: nephrotoxicity + neurotoxicity
80
Streptomycin
antibiotic (protein synthesis) aminoglycoside binds 30s subunit of ribosome → misreading of mRNA = nonfunctional proteins treat gram - infections, in combo with b-lactams to treat gram + bactericidal; narrow therapeutic range side effects: nephrotoxicity, ototoxicity
81
Tetracycline
antibiotic (protein synthesis) bind 30S ribosomal subunit = inhibition of aminoacyl-tRNA and mRNA-ribosome binding complex bacteriostatic; broad spectrum (gram + and -) also Doxycyline contraindicated in pregnancy → risk of maternal hepatotoxicity, permanent fetal teeth discoloration, impairment of fetal long bone growth
82
Erythromycin
antibiotic (protein synthesis) macrolides bind reversibly to 50S subunit of bacterial ribosome → interfere with translocation reactions bacteriostatic; broad spectrum, gram +
83
Azithromycin
antibiotic (protein synthesis) macrolides bind reversibly to 50S subunit of bacterial ribosome → interfere with translocation reactions bacteriostatic; broad spectrum, gram + and -
84
Chloramphenicol
antibiotic (protein synthesis) binds 50S ribosomal subunit + prevents formation of peptide bond bacteriostatic (can be bactericidal in high concentrations); broad spectrum side effects: fatal aplastic anemia, bone marrow suppression, ototoxicity; grey baby syndrome (unable to metabolize drug)
85
Ciprofloxacin
antibiotic (nucleic acid synthesis) fluoroquinolone blocks DNA gyrase (gram-) and topoisomerase IV (gram+) = inhibits bacterial DNA synthesis bactericidal; broad spectrum adverse effects: GI events, neurological effects mech of action decreased by multivitamins, magnesium/aluminum antacids contraindicated in pregnancy - damage to joints
86
Rifampin
antibiotic (nucleic acid synthesis) Rifamycin binds B-subunit of bacterial RNA polymerase = inhibits RNA synthesis bactericidal; broad spectrum frontline tx of tuberculosis
87
Sulfamethoxizole
antibiotic (antimetabolites) Sulfa drugs analog of p-aminobenzoic acid = inhibit dihydropteroate synthase = prevents DNA synthesis
88
Trimethoprim
antibiotic (antimetabolites) inhibits dihydrofolate reductase = prevents DNA synthesis
89
TMP-SMX
combination = synergistic effect of inhibiting folate synthesis inhibit both gram- and + clinical uses: bacterial diarrhea, UTIs, pneumonia
90
Cyclosporine
calcineurin inhibitor lipid soluble abx produced by soil fungi forms complex with cyclophilin →inhibits phosphatase activity of calcineurin = no nuclear translocation of NFAT blocks T cell proliferation suppresses some humoral immunity + innate immunity used adjuvant to GCs for tx + prevention of organ transplant rejection; 2nd line tx of severe + active RA (DMARD)
91
Tacrolimus
calcineurin inhibitor abx produced by streptomyces tsukubaensis forms complex with FKBP12 →inhibits phosphatase activity of calcineurin = no nuclear translocation of NFAT blocks T cell proliferation 100 fold more potent than cyclosporine A prevention of organ transplant rejection affects other calcineurin targets → nephro/neurotoxicity
92
Rapamycin
prototypical mTOR inhibitor macrolide abx produced by bacteria streptomyces hydroscopicus, has antifungal + immunosuppressive properties rapalogs have same effects binds FKBP12 → complex binds mTOR at FRB = allosteric inhibition disrupts association of mTOR to C1 specific components + uncouples it from substrates used as immunosuppressant in renal transplantation to promote immunological tolerance; off label use for other organ transplants cancer therapy → inhibits tumor growth by stopping cell proliferation, inducing apoptosis, and suppressing angiogenesis
93
synthetic glucocorticoids
similar structure to cortisol used to treat various immune related disorders and as immunosuppressive drugs for organ transplants innate immunity: upregulates expr of PRR genes, cytokine receptors, and complement factors; inhibits expr of pro-infl cytokines + chemokines adaptive immunity: inhibits genes involved; suppresses CD4+ T cell activation + signaling used for RA (DMARD) to ↓ bone erosion treat acute relapses in MS
94
Teplizumab
humanized anti CD3 antibody mutated to prevent binding to Fc receptors induce anergy of previously activated TH1 blocks CTLs used to delay onset of T1D
95
Foralumab
human anti CD3 antibody administered intranasally → induce T reg cells suppresses effector features in T cells non active MS + AD
96
Ibalizumab
non-immunosuppressive humanized anti CD4 antibody binds extracellular region of CD4, prevents gp120 from interacting with CCR5 blocks entry of HIV-1 virus into CD4 cells
97
Abatacept
Recombinant fusion protein - inhibits CD28 soluble, EXC domain of CTLA4 fused to Fc of Ig binds CD80/86 on APCs, prevents binding to CD28 on T cells = blocks costim signal = ↓ T cell activation ↓ proliferation, inhibits production of TNFa and IL-2 DMARD → treat RA
98
Rituximab
chimeric anti CD20 antibody tx for B cell non-Hodgkin's lymphoma tx of RA (DMARD) + MS
99
Ocrelizumab
humanized anti CD20 antibody binds to overlapping epitope of rituximab approved for PP MS
100
Ofatumumab
human anti CD20 antibody binds to distinct epitope tx of CLL, relapsing MS
101
Natalizumab
humanized mAb against a4 integrin prevents interaction between integrin and endothelial ligand (vascular cell adhesion molecule) = prevents lymphocytes from crossing BBB approved for MS adverse effect = progressive multifocal leukoencephalopathy
102
Infliximab
chimeric, bivalent anti TNF-a antibody induces cell depletion by CDC or ADCC agonist → activates signaling + induce apoptosis of immune cells expressing TNF
103
Adalimumab
human bivalent anti TNF-a antibody suppress formation of inflammatory cytokines ↓ recruitment of macrophages induces cell depletion by CDC and ADCC
104
Golimumab
human bivalent anti TNF-a antibody suppress formation of inflammatory cytokines ↓ recruitment of macrophages induces cell depletion by CDC and ADCC
105
Certolizumab pegol
humanized monovalent anti TNF-a antibody Fab region conjugated with polyethylene glycol = enhances plasma half life neutralizes membrane-associated + soluble human TNFa
106
Etarnecept
human bivalent anti TNF-a recombinant fusion protein contains TNF R2 and Fc region of human IgG1 higher affinity for TNF than naturally occuring soluble receptors → competitive inhibition of TNFa causes death of cells expressing surface TNFa shorter half life
107
Canakinumab
human bivalent anti IL-1 antibody used in therapy of juvenile idiopathic arthritis (DMARD)
108
Rilonacept
anti IL-1 recombinant fusion protein ligand-binding domain of IL-1 R + Fc of IgG = IL-1 trap tx of auto-inflammatory syndromes, clinical trials for gout and RA (DMARD)
109
Anakinra
Anti IL-1 recombinant fusion protein IL-1 receptor antagonist → competes with IL-1 used for RA (DMARD); short half life = daily subQ inj
110
Ipilimumab
human anti-CTLA4 Ab inhibits CTLA4 = enhances T cell responses to tumor antigens
111
Atezolizumab
humanized anti-PDL-1 Ab blocks ligand = enhance T cell cytotoxicity to tumor cells → enhance cytolysis + limit metastasis
112
Nivolumab
human anti-PD-1 Ab blocks receptor to enhance T cell cytotoxicity to tumor cells → enhance cytolysis + limit metastasis

Pharm 34X (8 decks)

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