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Pharm > Exam 1 Drugs > Flashcards

Exam 1 Drugs Flashcards

1
Q

Chlorpheniramine

A
  1. 1st Generation H1 Histamine Receptor Antagonist
  2. Alkylamine (mild to moderate sedative) class
  3. OTC allergy; cold
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2
Q

Diphenhydramine

A
  1. 1st Generation H1 Histamine Receptor Antagonist
  2. Ethanolamine (marked sedative) class
  3. OTC Sleep Aid; allergies
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3
Q

Promethazine

A
  1. 1st Generation H1 Histamine Receptor Antagonist
  2. Phenothiazine (marked sedative) class
  3. Antiemetic
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4
Q

Cetirizine

A
  1. 2nd Generation H1 Histamine Receptor Antagonist

2. OTC; some sedation

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5
Q

Desloratadine

A
  1. 2nd Generation H1 Histamine Receptor Antagonist
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6
Q

Fexofenadine

A
  1. 2nd Generation H1 Histamine Receptor Antagonist

2. Active metabolite of terfenadine, which was pulled from the market due to propensity to cause cardiac arrhythmias

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7
Q

Loratadine

A
  1. 2nd Generation H1 Histamine Receptor Antagonist

2. OTC

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8
Q

Cimetidine

A
  1. H2 Histamine Receptor Antagonist

2. Inhibits CYP450; may cause confusion in elderly patients with large dose

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9
Q

Ranitidine

A
  1. H2 Histamine Receptor Antagonist

2. Less effect on CYP450

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10
Q

PGE2

A
  1. Prostaglandin
  2. Involved in uterine contraction, fever, GI smooth muscle contraction, pain, mucus secretion, inhibition of gastric secretion and pepsin content
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11
Q

Misoprostol

A
  1. Prostaglandin

2. PGE1 analog; should be co-administered with NSAID for patients at risk for GI toxicity

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12
Q

Montelukast

A
  1. Leukotriene Antagonist

2. Used in bronchiole asthma

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13
Q

Zafirlukast

A
  1. Leukotriene Antagonist

2. Used in bronchiole asthma

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14
Q

Acetaminophen

A
  1. Inhibits COX (mechanism unclear)
  2. Antipyretic and Analgesic
  3. Toxicity: Metabolite formed by oxidation via P450 in liver conjugates with Glutathione; large doses deplete Glutathione causing hepatotoxicity
  4. Prescriptions limited to 325 mg per tablet
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15
Q

Aspirin

A
  1. NSAID; irreversible inhibitor (acetylation) of COX
  2. Low dose: inhibits platelet aggregation; Moderate dose: analgesic and antipyretic effects; Large dose: anti-inflammatory/antirheumatoid effects
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16
Q

Diclofenac

A
  1. NSAID; acetic acid class

2. Treats RA

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17
Q

Diflunisal

A
  1. NSAID; nonacetylated class
  2. Dose-dependent pharmacokinetics
  3. Used as loading dose
  4. Treats RA
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18
Q

Ibuprofen

A
  1. NSAID; propionic acid class

2. T1/2 = 2 hours; mostly renal elimination

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19
Q

Indomethacin

A
  1. NSAID; acetic acid class
  2. Potent COX inhibitor; direct effects on PMNs; reduces antihypertensive benefits; GI and CNS effects
  3. Treats RA, Gout pain and inflammation
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20
Q

Naproxen

A
  1. NSAID; proprionic acid class
  2. T1/2 = 12-14 hours; hepatic elimination
  3. Pediatic use; treats RA
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21
Q

Piroxicam

A
  1. NSAID; Enolic Acid class

2. T1/2 = ~50 hours

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22
Q

Sulindac

A
  1. NSAID; acetic acid class
  2. Prodrug; active sulfide metabolite
  3. Approved for use in pediatric patients
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23
Q

Celecoxib

A
  1. NSAID; COX-2 Selective Inhibitor
  2. 2C9 substrate
  3. Treats RA
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24
Q

N-Acetylcysteine

A
  1. Treatment for Acetaminophen Overdose
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25
Q

Prednisone

A
  1. Corticosteroid; Immunosuppresant
  2. No topical activity; short acting
  3. MOA: Nuclear hormone receptor family; complex translocated to nucleus, binding as homodimer to DNA transcripts w/ GREs
  4. Uses: anti-inflammatory, transplant rejection, RA, SLE, systemic dermatomyositis, Psoriasis, asthma and other allergic disorders
  5. Toxicity: Iatrogenic Cushing’s Syndrome, mineralocorticoid effects @ high doses (heart disease), prolonged therapy (inf., inh. growth, induce myopathy, osteoporosis, cataracts), >2 weeks can induce adrenal suppression (adrenocortical atrophy)
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26
Q

Dexamethasone

A
  1. Corticosteroid; Immunosuppresant
  2. Has topical activity; long acting
  3. MOA: Nuclear hormone receptor family; complex translocated to nucleus, binding as homodimer to DNA transcripts w/ GREs
  4. Uses: anti-inflammatory, transplant rejection, RA, SLE, systemic dermatomyositis, Psoriasis, asthma and other allergic disorders
  5. Toxicity: Iatrogenic Cushing’s Syndrome, mineralocorticoid effects @ high doses (heart disease), prolonged therapy (inf., inh. growth, induce myopathy, osteoporosis, cataracts), >2 weeks can induce adrenal suppression (adrenocortical atrophy)
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27
Q

Cyclosporin A (Cyclosporine)

A
  1. Calcineurin Inhibitor; Immunosuppresant; lipid-soluble peptide
  2. ROA: oral, IV, opthalmic emulsion
  3. MOA: binds Cyclophilin C –> decreases calcineurin (cytoplasmic phosphatase) –> decreases production of cytokines (IL-2) –> reduced response of Tcells to Ags
  4. Uses: GvH disease in bone marrow transplantation, aplastic anemia, transplant rejection, autoimmune diseases, dry eye syndrome
  5. Toxicity: reversible nephrotoxicity (dose-limiting), vasconstriction leading to HTN, neurotoxicity, hyperlipidemia, transient hepatotoxicity, stimulates TGF-beta which increases risk of cancer
  6. Interactions: metabolized by P450; erythromycin, ketoconazole, amphotericin B, and grapefruit juice inhbit metabolism; phenobarbital and rifampin increase clearance
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28
Q

Tacrolimus (FK506)

A
  1. Calcineurin Inhibitor; Immunosuppresant; Macrolide
  2. ROA: oral or injection; 10-100x more potent
  3. MOA: binds FKBP-12 –> inhibits calcineurin –> decreases production of cytokines (IL-2) –> reduced response of Tcells to Ags
  4. Uses: same as Cyclosporine (except dry eye syndrome)
  5. Toxicity & Interactions: same as Cyclosporine
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29
Q

Sirolimus

A
  1. Antiproliferative Agent; Macrocyclic Lactone; Immunosuppresant
  2. ROA: oral
  3. MOA: binds FKBP-12 –> inhibits mTOR –> inhibits T cell activation and proliferation
  4. Uses: transplant rejection (w/ calc inh. + glucocorticoid), GvH rxn, autoimmune diseases, effect persists several months after end therapy
  5. Toxicity: dose-dependent thrombocytopenia, leukopenia, hyperlipidemia (esp. renal transplant pts), anemia, hypotension, hypo/hyperkalemia, fever, GI effects, increased risk of lymphoma or inf
  6. Interactions: same as Cyclosporine
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30
Q

Azathioprine

A
  1. Cytotoxic Agent; Immunosuppresant; 6-MP derivative
  2. ROA: oral or IV
  3. MOA: inhibits S phase of cell division; converted to thioinosinic acid –> competitive inhibitor of purine synthesis; affects T cells more than B cells
  4. Uses: transplant rejection (w/ corticosteroid), RA
  5. Toxicity: bone marrow suppression, GI toxicity, mild hepatotoxicity, may lead to sever inf. + neoplasia
  6. Interactions: Allopurinol increases toxicities
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31
Q

Mycophenoate Mofetil

A
  1. Cytotoxic Agent; Immunosuppresant; produrg
  2. ROA: oral or IV
  3. MOA: inhibits monophosphate dehydrogenase –> decreases purine synthesis –> decreases proliferation of B + T cells
  4. Uses: Allogenic renal transplant rejection (w/ cyclosporine+corticosteroids) and liver, cardiac transplant rejection
  5. Toxicity: diarrhea, leukopenia, cytomegalovirus inf., GI hemorrhage
  6. Interactions: Antacids decrease absorption
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32
Q

Fingolimod (FTY720)

A
  1. SIP-R Agonist; Immunosuppresant
  2. ROA: oral
  3. MOA: “Lymphocyte homing;” reversibly sequesters lymphocytes in lymph nodes and Peyer’s patches –> reducing recirculation of T cells
  4. Uses: relapsing MS
  5. Toxicity: decreases HR and/or AV conduction after 1st dose, inf., macular edema, decrease pulmonary function, hepatotoxicity, fetal risk
  6. Interactions: antiarrhythmic + beta blockers (risk of additive effect on HR), clearance inhibited by ketoconazole (CYP4F inhibitor), avoid live attenuated vaccines
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33
Q

Antithymocyte Globulin (ATG)

A
  1. Cytotoxic Antibody
  2. ROA: oral
  3. MOA: Ab against T cell surface molecules (CD + HLA) –> block their function, deplete T cells from blood and thymus-dependent areas of spleen and lymph nodes
  4. Uses: Renal allograph rejection (alone or w/ corticosteroid + azathioprine)
  5. Toxicity: hypersensitivity, hypotension, nephritis, anaphylaxis (rare), inf.
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34
Q

Muromonab-CD3

A
  1. Anti-CD3 Monoclonal Antibody
  2. MOA: binds CD3 glycoprotein on T cells –> blocks antigen recognition complex –> unable to recognize foreign Ag
  3. Uses: acute kidney/hepatic transplant rejection, prophylaxis in cardiac transplant, depletion of Tcells in marrow b4 bone marrow transplant
  4. Toxicity: fever, pulmonary edema, vomiting, headache, anaphylaxis, inf w/ chronic therapy
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35
Q

Basiliximab

A
  1. IL-2 Receptor (Anti-CD25) Antibody
  2. MOA: block IL-2 receptors on activated T cells
  3. Uses: Acute renal transplant rejection (w/ cyclosporine + corticosteroids)
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36
Q

Daclizumab

A
  1. IL-2 Receptor (Anti-CD25) Antibody
  2. MOA: block IL-2 receptors on activated T cells
  3. Uses: Acute renal transplant rejection (w/ cyclosporine + corticosteroids)
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37
Q

Infliximab

A
  1. Chimeric anti-TNF-alpha monoclonal antibody
  2. MOA: competitively binds TNF-alpha, preventing it from activating its receptors
  3. Uses: RA (w/ Methotrexate), Crohn’s disease
  4. Toxicity: infusion rxn (fever, urticaria, hypotension, dyspnea), URI, UTI, development of antinuclear Abs, with (rare) lupus-like syndrome
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38
Q

Etanercept

A
  1. Contains ligand-binding sequence of a human TNF-alpha receptor fused to human IgG1
  2. MOA: binds TNF-alpha, preventing it from activating its receptors
  3. Uses: RA
  4. Toxicity: injection site rxn, inf.
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39
Q

Rh0 (d) Immune Globulin

A
  1. MOA: blocks the Ab response of an Rh-negative mother to an Rh-positive baby
  2. Uses: prevention of hemolytic disease of Rh-positive newborns
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40
Q

Immune globulin

A
  1. Immunostimulant; human plasma from donors
  2. Uses: provide passive immunization for 1-3 months]
  3. Toxicity: anaphylactoid rxn and severe hypotension, poss. risk of inf.
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41
Q

Methotrexate

A
  1. Folic Acid Analog; Antimetabolite; Choice DMARD for RA
  2. Inhibits enzyme for purine metabolism –> decreased PMN chemotaxis, decreased lymphocyte and macrophage function
  3. Oral, absorbed from GI
  4. Nausea and mucosal ulcers, “hypersensitivity” lung reaction
  5. Take w/folic acid supplements to protect GI and liver. Not for pregnancy
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42
Q

Adalimunab

A
  1. IgG anti-TNF-alpha monoclonal antibody
    subcutaneous administration –> complex with soluble TNF, decreased macrophage and T cell function
  2. RA, psoriatic arthritis, ankylosing spondylitis
  3. Deccreased bone erosions
  4. Increased risk of macrophage dependent infection (TB), maybe vasculitis or leukopenias
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43
Q

Allopurinol

A
  1. Inhibitor of Uric Acid Synthesis; treats Gout
  2. Especially useful in patients with renal insufficiency or calculi
  3. not useful for acute attacks
  4. long lasting inhibitor of xantine oxidase
  5. Drug interactions: ampicillin, thiazides, inhibits oxidation of mercaptopurine to azathioprine, increases toxicity of other cytotoxic drugs (cyclophosphamide)
  6. Stevens–Johnson syndrome can occur
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44
Q

Febuxostat

A
  1. Non-purine like selective inhibitor of xanthine oxidase; treats Gout
  2. Rapidly and extensively absorbed following oral administration, peak plasma level reached within 1 hr
  3. May produce GI intolerance/hepatic alterations
  4. administered orally
  5. use prophylactic NSAIDs or Colchicine at beginning to prevent gout attack
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45
Q

Probenecid/Sulfinpyrazone

A
  1. Uricosuric Agent; treats Gout
  2. Generally well tolerated by most patients. May produce GI intolerance, dermatitis,nephrotic syndrome (rare)
  3. orally administered
  4. with small doses of salicytes = less of an effect
  5. with large doses of salicytes = more of an effect
  6. give with colchicine to prevent gout attack
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46
Q

Colchicine

A

Classification: Acute gouty arthritis
MOA: binds tubulin –> inhibition of leukocyte migration and urate crystal phagocytosis
Use: For Gout Pain and Inflammation
Resistance:
Administration: Oral (at signs of attack), IV

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47
Q

Rasburicase

A
  1. For increasing Uric Acid degradation; treats Gout
  2. catalyzes uric acid conversion to allantoin
  3. lowers urate levels better than allopurinol
  4. Recommended for the initial management of hyperuricemia in pediatric patients with cancer chemotherapy-caused increased uric acid production
  5. problems with production of antibodies, acute renal failure, anaphylaxis, and GI abnormalities
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48
Q

Penicillin G

A
  1. Cell wall synthesis inhibitor
  2. Natural penicillin
  3. Narrow spectrum
  4. Orally administered
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49
Q

Penicillin V

A
  1. Cell wall synthesis inhibitor
  2. Synthetic penicillin
  3. Narrow spectrum
  4. Orally administered
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50
Q

Oxacillin

A

cell wall synthesis inhibitor; narrow spectrum

- anti-staph (isoxazolyl penicillins)

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51
Q

Dicloxacillin

A

cell wall synthesis inhibitor, narrow spectrum

- anti-staph (isoxazolyl penicillins)

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52
Q

Ampicillin

A

cell wall synthesis inhibitor; amino penicillin

broad spectrum; bactericidal

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53
Q

Amoxicillin

A

cell wall synthesis inhibitor; amino penicillin

broad specturm, bactericidal

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54
Q

Ticarcillin

A

cell wall synthesis inhibitor; carboxy penicillin

broad spectrum; bactericidal

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55
Q

Mezlocillin

A

cell wall synthesis inhibitor; acylureido penicillin

bactericidal; broad spectrum

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56
Q

Clavulanate

A

Beta-lactamase inhibitor

- oral; renal excretion

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57
Q

Sulbactam

A

Beta-lactamase inhibitor

- IV, renal excretion

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58
Q

Tazobactam

A

Beta-lactamase inhibitor

  • IV, renal excretion
  • pipercillin increases its half life
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59
Q

Cefazolin

A

1st Generation Cephalosporin (narrow spectrum)

1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)

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60
Q

Cephalexin

A

1st Generation Cephalosporin (narrow)

1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)

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61
Q

Cefuroxime

A

2nd Generation Cephalosporin (broad)

1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)

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62
Q

Cefoxitin

A

2nd Generation Cephalosporin (Broad)

1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)

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63
Q

Cefixime

A

3rd Generation Cephalosporin (broad)

1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)

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64
Q

Cefoperazone

A

3rd Generation Cephalosporin (Broad)

  1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
  2. Antipseudomonal
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65
Q

Cefotaxime

A

3rd Generation Cephalosporin (broad)

1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)

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66
Q

Ceftriaxone

A

3rd Generation Cephalosporin (broad)

1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)

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67
Q

Cefepime

A

4th Generation Cephalosporin (broad)

  1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
  2. Antipseudomonal
68
Q

Cefpirome

A

4th Generation Cephalosporin (broad)

69
Q

Imipenem/Cilastatin

A

Carbapenem
broad spectrum; inhibit transpeptidase like penicillins
- bactericidal and anti-pseudomonal activity
- not effective against die hard bacteria
- reserved for serious infections
- cilastin (polymixin) not typical antibiotic but increases imipenem half life by inhibiting dehydropeptidase

70
Q

Azteronam

A

Monobactam; narrow spectrum (gram - & anaerboes)

- same as carbapenem

71
Q

Vancomycin

A

cell wall synthesis inhibitor
- binds D alanine on membrane preventing binding of transpeptidase
- no beta lactam ring; poor oral absorption
- excreted unchanged by kidney
VRE = mutation of drug binding site
**used to be “drug of last resort” but now infections from VRE treated by streptogramins or linezolid
- Used to treat serious gram+ infections (MRSA)

72
Q

Bacitracin

A

cell wall synthesis inhibitor
MOA = inhibits dephosphorylation of lipid carrier (C55 isoprenyl pyrophosphatase carrier) used for cell wall componenets
- gram + mostly
**only for topical treatments (severe nephrotoxicity)

73
Q

Quinupristin/Dalfopristin (Synercid)

A

Streptogramin; protein synthesis inhibitor
- used together b/c resistance is rapid in monotherapy
**DRUG OF LAST RESORT (only for severe)
MOA = block by binding 50s subunit; inhibits peptidyl transferase thus blocking ELONGATION of peptide chain
Dalfopristin = acts at early phase of protein syn.
Quinupristin = acts at late phase
- gram +, some gram -, anaerobes and chlamydiae (esp. VRE, MRSA, PRSP & S pyogenes)
Resistance = little known
SE = pain and frequent thrombophlebitis at injection site (arthralgia and myalgia)
**poor oral administration; metabolized in liver
**bacteriostatic alone (when combined with linezolid becomes bacteriocidal)
DI = increased levels of warfarin, diazepam, cyclosporine
**high dose = CNS effects

74
Q

Linezolid

A

Oxazolidinones; protein synthesis inhibitor
**DRUG OF LAST RESORT (severe infections only)
- expenisve, narrow spectrum
- good oral administration (can also use IV)
MOA = binding 23s RNA of 50S subunit
**highly reactive against susceptible and resistant gram + (NOT GRAM -); usually used for resistant staph (MRSA) or VRE or PRSP
- mostly bacteriostatic (Except for strep = bactericidal)
resistance = mutation of 23s rRNA
SE = GI distress, nausea, vomitting, thrombocytopenia (chronic); inhibits monoamine oxidase activity
DI = increased action of SSRI & other antidepressants and pseudoephedrine
**high dose - CNS effects

75
Q

Erythromycin

A

Macrolide; protein synthesis inhibitor
- for atypical pneumonia
MOA = binds 50s subunit and blocks aminoacyl translocation and formation of translocation complex
limited spectrum = gram + and - and anaerobes; also chlamydia, myco. pneumonia, mycobacteria
- bacteriostatic (except at high doses)
- HA pneumonia, MAC pneumonia, legionaires

**poor oral unlike other macrolides b/c its acid sensitive
- metabolised in liver
SE = GI distress and cholestatic hepatitis
DI = increased serum levels of theophylline, warfarin, cyclosporine, statins
Resistance = methylation/mutation, decreased cell access and hydrolyzed esterases

76
Q

Clarithromycin

A

Macrolide; protein synthesis inhibitor
- used with ethambutol and rifampin for MAC disseminated infection in late stage AIDS
**good oral and liver metabolized
MOA = same as erythro
DI = increased serum levels of various drugs (like erythro)
Resistance = same

77
Q

Azithromycin

A

Macrolide; protein synthesis inhibitor

  • *can cause abnormal changes in heart’s electrical activity that may lead to a fatal heart rhythm
  • *unlike C and E, it is eliminated unchanged via kidney and feces
78
Q

Telithromycin

A

Ketolide; protein synthesis inhibitor
- semisynthetic macrolide
**effective against many traditional macrolide-resistant strains
**binds to ribosomes of some bacteria with higher affinity than macrolides
Admin = oral, good tissue and intracellular penetration

USE = respiratory tract infection (CA-pneumonia and S pharyngitis)
*resversibly inhbiits CYP3A4 enzyme system, may slightly prolong QTc interval

79
Q

Clindamycin

A

Lincosamide; protein synthesis inhibitor
MOA = binds 23s RNA of 50S subunit and inhibits aminoacyl translocation and formation of initiation complex (similar to oxazolidenones and macrolides)

Spectrum = active against some gram +, most anaerobes, some chlyamydia but NOT GRAM -
**bacteriostatic
**treats penicillin resistant gram + infections
**inhibits strep, staph and pneumococci
HA pneumonia (combine with G3/G4 cephalosporin)

Resistance = methylation or mutation causing MLS-type B resistance; reduced drug access

**good oral, extensive distribution (except brain); meabolized in liver and eliminted by kidneys and feces

SE = GI distress, rash, superinfection, hepatotoxicity, neutropenia
**respiratory paralysis could be induced with muscle relaxants

80
Q

Streptomycin

A

Aminoglycoside; protein synthesis inhibitor; treats TB

  • *1st to be isolated
  • *narrow spectrum, mostly bactericidal
  • active against soe gram -, limited gram +; some anti-pseudomonal (NOT EFFECTIVE AGAINST ANAEROBES)

USE = endocarditis, septicemia, HA pneumonia, chronic UTI

Resistance = mutation at binding site, enzymatic inactivation (acetylation, adenylation, phosphorylation), reduced permability

Kinetics = poor oral, variable distribution

  • reduced activity in low pH, hyperosmolarity and anaerobiosis
  • unmetabolized and eliminated by kidneys

AR = ototoxicity, nephrotoxicity, NM blockade

  • increased ototoxicity with loop diuretics and vanco
  • increased nephrotoxicity with vanco, cyclosporin, NSAIDs, contrast (iodine)
  • respiratory depression with NM blockers
  • *in vitro mixing with penicillins reduces activity of both
81
Q

Amikacin

A

Aminoglycoside; protein synthesis inhibitor (binds to ribosomal subunit

  1. Narrow spectrum, mostly bactericidal
  2. Not effective agains anaerobes
  3. Adverse effects - ototoxicity, nephrotoxicity, neuromuscular blockade
82
Q

Gentamicin

A

Aminoglycoside; protein synthesis inhibitor (binds to ribosomal subunit

  1. Narrow spectrum, mostly bactericidal
  2. Not effective agains anaerobes
  3. Adverse effects - ototoxicity, nephrotoxicity, neuromuscular blockade
83
Q

Kanamycin

A

Aminoglycoside; protein synthesis inhibitor (binds to ribosomal subunit

  1. Narrow spectrum, mostly bactericidal
  2. Not effective agains anaerobes
  3. Adverse effects - ototoxicity, nephrotoxicity, neuromuscular blockade
84
Q

Tobramycin

A

Aminoglycoside; protein synthesis inhibitor (binds to ribosomal subunit

  1. Narrow spectrum, mostly bactericidal
  2. Not effective agains anaerobes
  3. Adverse effects - ototoxicity, nephrotoxicity, neuromuscular blockade
85
Q

Tetracycline

A

Tetracycline; protein synthesis inhibitor;

  1. Treats Balantidiasis
  2. Bacteriostatic
86
Q

Doxycycline

A

Tetracycline; protein synthesis inhibitor

87
Q

Minocycline

A

Tetracycline; protein synthesis inhibitor

88
Q

Tigecycline

A

Tetracycline; protein synthesis inhibitor

  1. IV broad spectrum antibiotic
  2. First glycylcycline
  3. Used against many drug-resistant organisms
89
Q

Chloramphenicol

A

protein synthesis inhibitor

  1. Prevents docking of aminoacyl tRNA
  2. Broad spectrum, bacteriostatic
90
Q

Sulfamethoxazole

A

Sulfonamide; folate metabolism inhibitor

  1. Competitively inhibit folic acid production, interrupting metabolic reactions
  2. Broad spectrum
  3. Good oral absorption
  4. Active against Chlamydia, enterocolitis, burns, ocular infections,
  5. No-no in pregnant women (kernicterus in infant)
91
Q

Sulfasalazine

A

Sulfonamide; folate metabolism inhibitor

  1. Competitively inhibit folic acid production, interrupting metabolic reactions
  2. Broad spectrum
  3. Good oral absorption
  4. Active against Chlamydia, enterocolitis, burns, ocular infections,
  5. No-no in pregnant women (kernicterus in infant)
92
Q

Sulfadiazine

A

Sulfonamide; folate metabolism inhibitor, commonly used with Trimethoprim

  1. Competitively inhibit folic acid production, interrupting metabolic reactions
  2. Broad spectrum
  3. Good oral absorption
  4. Active against Chlamydia, enterocolitis, burns, ocular infections,
  5. No-no in pregnant women (kernicterus in infant)
93
Q

Trimethoprim

A

Folate metabolism inhibitor

  1. Used with sulfamethoxazole
  2. Prevent recurrent UTI, treat upper respiratory infections
  3. No-no with liver impairment patients
94
Q

Ciprofloxacin

A

Fluoroquinolone; DNA replication, transcription, and metabolism inhibitor; treats atypical mycobacteria

95
Q

Levofloxacin

A

Fluoroquinolone; DNA replication, transcription, and metabolism inhibitor

96
Q

Metronidazole

A

Urinary Tract Antiseptic;

  1. Treats Amebiasis, Giardiasis, Trichomoniasis, Balantidiasis
  2. Used for vaginitis
97
Q

Nitrofurantoin

A

Chronic/acute Urinary Tract Antiseptic

98
Q

Methenamine

A

Urinary Tract Antiseptic

1. UTI prophylaxis, but not primary agent for treatment

99
Q

Mupirocin

A

Urinary Tract Antiseptic

  1. Topical for staph caused impetigo
  2. May cause local itching, rash, contact dermatitis
100
Q

Polymyxins

A

Urinary Tract Antiseptic

1. Topical treatment of resistant gram- infections only

101
Q

Isoniazid

A

treats TB

1. Good oral absorption

102
Q

Ethambutol

A

treats TB

  1. Inhibits mycobacterial arabinosyl tranferases enzyme (embCAB operon). They are involved in polymerization reduction of arabinoglycan
  2. Rapid resistance emerging
  3. Adverse effects - dose-related retrobulbar neuritis
103
Q

Pyrazinamide

A

treats TB

104
Q

Rifampin

A

treats TB

  1. Causes red-orange color in urine, feces, sweat, tears, contact lenses
  2. > 2 weeks causes flu-like symptoms
105
Q

p-Aminosalicyclic Acid (PAS)

A

second-line drug for TB

  1. Folate synthesis antagonist
  2. Adverse effects - GI irritation, hypersensitivity reaction
106
Q

Dapsone

A

treats Lepra

1. Competitively inhibit folate synthesis

107
Q

Clofazimine

A

treats Lepra

  1. Erratic absorption, stored in skin and slowly released
  2. Sulfone-resistant leprosy
108
Q

Chloroquine

A

treats Malaria

  1. Principal drug to treat malaria parasites
  2. Prevent hemozoin formation, causes damage to parasite membrane -> death
  3. Resistance - PfCRT
  4. Does not eliminate dormant liver forms of P. vivax/ovale
  5. Contraindications - psoriasis/porphyria, visual field abnormalities, liver disease, neuro/hematologic disorders
109
Q

Quinine and Quinidine

A

treats Malaria

  1. First line therapies for P. falciparum malaria
  2. Erythrocytic schizonticide against 4 plasmodium species (not against liver parasites)
  3. Gametocidal against vivax/ovale, not falciparum
  4. Used with doxycycline to limit duration of use
  5. Can cause Blackwater Fever - hypersensitivity reaction to quinine, marked hemolysis/hemoglobinuria
110
Q

Mefloquine

A

treats Malaria

  1. Strong erythrocytic schizonticidal
  2. Prophylactic agent (FDA approved)
  3. Single dose treatment regime
  4. Only against falciparum/vivax
111
Q

Primaquine

A

treats Malaria

  1. hepatic schizonticidal/gametocidal
  2. Good against all human malaria parasites
  3. Only one against hyponozoite vivax/ovale
112
Q

Pyrimethamine

A

treats Malaria

113
Q

Sulfadoxine

A

Sulfonamide; treats Malaria

114
Q

Suramin

A

treats African Trypanosomiasis

  1. Administered IV, chemoprophylaxis/early hemolymphatic infection treatment ONLY
  2. Adverse effects - GI, CV, neurological/blood
115
Q

Melarsoprol

A

treats African Trypanosomiasis

  1. Administered IV
  2. First line therapy for advanced CNS infection
  3. Adverse effects - serious GI, CV, renal, hepatic side effects. Hemolysis, encephalophaty (may be fatal)
116
Q

Elfornithine

A

treats African Trypanosomiasis

  1. IV treatments for CNS (better tolerated than melarsoprol)
  2. Blocks conversion of ornithine to putrescine
117
Q

Nifurtimox

A

treats American Trypanosomiasis

  1. Inhibits transmission of bugs
  2. Useful in acute only, many times fails and conditions goes to chronic stages
  3. Adverse effects - severe GI, CNS, neurological toxicity
118
Q

Sodium Stibogluconate

A

treats Leishmaniasis

1. Poor availability, safety, efficacy of these drugs

119
Q

Iodoquinol

A

treats intestinal Amebiasis

120
Q

Paromomycin Sulfate

A

treats extraintestinal Amebiasis

121
Q

Nitazoxanide

A

treats Giardia lamblia, metronidazole resistant protozoa strains, several tapeworm helminthes

122
Q

Praziquantel

A

treats Cestodes (Tapeworm); treats Trematodes (Fluke)

  1. Effective to all schistosome infections
  2. Increases parasite cell membrane permeability to calcium, producing paralysis/dislodgment/death
  3. Avoid if pregnant
123
Q

Niclosamide

A

treats Cestodes (Tapeworm)

124
Q

Mebendazole

A

treats Nematodes (Roundworm)

  1. Ascariasis, pinworm, hookworm
  2. Inhibits microtubule synthesis
125
Q

Pyrantel Pamoate

A

treats Nematodes (Roundworm)

126
Q

Piperazine

A

treats Nematodes (Roundworm)

  1. Alternative to mebendazole for ascariasis treatment
  2. Inhibits acetylcholine at the myoneural junction
127
Q

Cyclophosphamide

A

Nitrogen Mustard; Alkylating Agent

1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins

128
Q

Carmustine (BCNU) and Lomustine

A

Nitrosoureas; Alkylating Agent

1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins

129
Q

Busulfan

A

Alkyl Sulfonate; Alkylating Agent

1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins

130
Q

Dacarbazine

A

Triazene; Alkylating Agent

1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins

131
Q

Procarbazine

A

Methylhydrazine; Alkylating Agent

1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins

132
Q

Cis-Plantinum (Cisplatin)

A

Platinum Complex; Alkylating Agent

1. React with nucleophilic sites on DNA and proteins → intrastrand and interstrand cross‐links

133
Q

Carboplatin

A

Platinum Complex; Alkylating Agent

1. React with nucleophilic sites on DNA and proteins → intrastrand and interstrand cross‐links

134
Q

Oxaliplatin

A

Platinum Complex; Alkylating Agent

1. React with nucleophilic sites on DNA and proteins → intrastrand and interstrand cross‐links

135
Q

6-Mercaptopurine (6-MP)

A

6-Thiopurine; Purine Analog/Related Inhibitor; Antimetabolite
1. Competitively inhibit purine synthesis; 6‐TGP incorporated into DNA

136
Q

6-Thioguanine (6-TG)

A

6-Thiopurine; Purine Analog/Related Inhibitor; Antimetabolite
1. Competitively inhibit purine synthesis; 6‐TGP incorporated into DNA

137
Q

Fludarabine-5-Phosphate

A

6-Thiopurine; dPurine Analog/Related Inhibitor; Antimetabolite

138
Q

Leucovorin

A

Folate Antagonist Rescue Agent; Antimetabolite

1. Reduced folate coenzyme

139
Q

5-Fluorouracil (5-FU)

A

Pyrimidine Analog; Antimetabolite

1. Reduced folate coenzyme

140
Q

Cytarabine (AraC)

A

Pyrimidine Analog; Antimetabolite

1. Reduced folate coenzyme

141
Q

Gemcitabine

A

Pyrimidine Analog; Antimetabolite

1. Reduced folate coenzyme

142
Q

Vinblastine

A

Vinca Alkaloid; Plant Alkaloid

1. Bind tubulin, block its ability to polymerize into microtubules

143
Q

Vincristine

A

Vinca Alkaloid; Plant Alkaloid

1. Bind tubulin, block its ability to polymerize into microtubules

144
Q

Paclitaxel

A

Taxane; Plant Alkaloid

1. Promotes microtubule polymerization and stabilization

145
Q

Abraxane

A

(Albumin bound Paclitaxel)

Taxane; Plant Alkaloid

  1. Antimitotic drug, M-phase specific
  2. Promotes microtubule polymerization and stabilization
146
Q

Topotecan

A

Camptothecin; Plant Alkaloid

  1. S-phase specific
  2. Bind to and stabilize the topoisomerase I‐DNA complex
147
Q

Etoposide

A

Epipodophyllotoxin; Plant Alkaloid

  1. S/G2 phase specific,
  2. Forms complex with topoisomerase II
148
Q

Actinomycin D (Dactinomycin)

A

Antitumor Antibiotic

1. Bind to DNA by intercalating between base pairs

149
Q

Adriamycin (Doxorubicin)

A

Anthracycline; Antitumor Antibiotic

1. Bind to DNA by intercalating between base pairs

150
Q

Bleomycin

A

Antitumor Antibiotic

  1. G2 phase specific
  2. Binds DNA, → free radicals
151
Q

L-asparginase

A

Enzyme; Antineoplastic Agent

1. Hydrolyzes circulating asn

152
Q

Hydroxyurea

A

Urea analog; Antineoplastic Agent

1. Inhibits ribonucleotide reductase

153
Q

Tretinoin (ATRA)

A

Differentiating Agent; Antineoplastic Agent

1. Increases transcription of genes expressing retinoic acid response elements

154
Q

Imatinib Mesylate

A

Protein Tyrosine Kinase Inhibitor; Antineoplastic Agent

1. Inhibits Bcr‐Abl & c‐kit receptor protein kinases

155
Q

Gefitinib

A

Protein Tyrosine Kinase Inhibitor; Antineoplastic Agent

1. Inhibits EGFR tyrosine kinase

156
Q

Bortezomib

A

Porteasome Inhibitor; Antineoplastic Agent

1. Reversibly inhibits the 26S proteasome

157
Q

Trastuzumab

A

Monoclonal Antibody; Antineoplastic Agent

1. Binds, blocks HER2/neu

158
Q

Rituximab

A

Monoclonal Antibody; Antineoplastic Agent

1. Binds, blocks the B cell CD20 surface antigen

159
Q

Cetuximab

A

Monoclonal Antibody; Antineoplastic Agent

1. Binds, blocks EGFR ( increase in colorectal cancer)

160
Q

Bevacizumab

A

Monoclonal Antibody; Antineoplastic Agent

1. Binds vascular endothelial growth factor (VEGF)

161
Q

Interferon-alfa

A

Biological Response Modifier; Antineoplastic Agent

1. Cytokine; receptor complex regulates transcription

162
Q

Interleukin-2 (IL-2)

A

Biological Response Modifier; Antineoplastic Agent

1. Binds receptor on activated T cells,  proliferation & NK cytokine production

163
Q

Granulocyte Colony-Stimulating Factor (G-CSF)

A

Biological Response Modifier; Antineoplastic Agent

  1. Increases production of neutrophils and stimulates their phagocytic and cytotoxic activities
  2. Therapeutic use - prophylaxis of chemotherapy-induced neutropenia
  3. Adverse effects - bone pain in lower back, sternum, and pelvis
164
Q

Granulocyte/Macrophage Colony-Stimulating Factor (GM-CSF)

A

Biological Response Modifier; Antineoplastic Agent

  1. Increases production of neutrophils and monocytes, stimulates their migration and phagocytic/cytotoxic activities
  2. Therapeutic use - rescue bone marrow graft failure, speed graft recovery after transplant
  3. Adverse effects - fever, bone pain
165
Q

Mechlorethamine

A

Nitrogen Mustard; Alkylating Agent

  1. Most reactive alkylating agent
  2. Therapeutic use - Hodgkin’s disease
  3. Adverse effects - bone marrow and intestinal mucosa
166
Q

Leuprolide Acetate

A

Long-acting Gonadotropin Releasing Hormone Agent

  1. Downregulation of GnRH receptor number, suppression of gonadotropin release
  2. Therapeutic use - metastatic gonadal steroid-dependant prostate cancer
  3. Adverse effects - hypogonadism, decreased bone mineralization

Pharm (9 decks)

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