Exam 1 Drugs Flashcards
1
Q
Chlorpheniramine
A
- 1st Generation H1 Histamine Receptor Antagonist
- Alkylamine (mild to moderate sedative) class
- OTC allergy; cold
2
Q
Diphenhydramine
A
- 1st Generation H1 Histamine Receptor Antagonist
- Ethanolamine (marked sedative) class
- OTC Sleep Aid; allergies
3
Q
Promethazine
A
- 1st Generation H1 Histamine Receptor Antagonist
- Phenothiazine (marked sedative) class
- Antiemetic
4
Q
Cetirizine
A
- 2nd Generation H1 Histamine Receptor Antagonist
2. OTC; some sedation
5
Q
Desloratadine
A
- 2nd Generation H1 Histamine Receptor Antagonist
6
Q
Fexofenadine
A
- 2nd Generation H1 Histamine Receptor Antagonist
2. Active metabolite of terfenadine, which was pulled from the market due to propensity to cause cardiac arrhythmias
7
Q
Loratadine
A
- 2nd Generation H1 Histamine Receptor Antagonist
2. OTC
8
Q
Cimetidine
A
- H2 Histamine Receptor Antagonist
2. Inhibits CYP450; may cause confusion in elderly patients with large dose
9
Q
Ranitidine
A
- H2 Histamine Receptor Antagonist
2. Less effect on CYP450
10
Q
PGE2
A
- Prostaglandin
- Involved in uterine contraction, fever, GI smooth muscle contraction, pain, mucus secretion, inhibition of gastric secretion and pepsin content
11
Q
Misoprostol
A
- Prostaglandin
2. PGE1 analog; should be co-administered with NSAID for patients at risk for GI toxicity
12
Q
Montelukast
A
- Leukotriene Antagonist
2. Used in bronchiole asthma
13
Q
Zafirlukast
A
- Leukotriene Antagonist
2. Used in bronchiole asthma
14
Q
Acetaminophen
A
- Inhibits COX (mechanism unclear)
- Antipyretic and Analgesic
- Toxicity: Metabolite formed by oxidation via P450 in liver conjugates with Glutathione; large doses deplete Glutathione causing hepatotoxicity
- Prescriptions limited to 325 mg per tablet
15
Q
Aspirin
A
- NSAID; irreversible inhibitor (acetylation) of COX
- Low dose: inhibits platelet aggregation; Moderate dose: analgesic and antipyretic effects; Large dose: anti-inflammatory/antirheumatoid effects
16
Q
Diclofenac
A
- NSAID; acetic acid class
2. Treats RA
17
Q
Diflunisal
A
- NSAID; nonacetylated class
- Dose-dependent pharmacokinetics
- Used as loading dose
- Treats RA
18
Q
Ibuprofen
A
- NSAID; propionic acid class
2. T1/2 = 2 hours; mostly renal elimination
19
Q
Indomethacin
A
- NSAID; acetic acid class
- Potent COX inhibitor; direct effects on PMNs; reduces antihypertensive benefits; GI and CNS effects
- Treats RA, Gout pain and inflammation
20
Q
Naproxen
A
- NSAID; proprionic acid class
- T1/2 = 12-14 hours; hepatic elimination
- Pediatic use; treats RA
21
Q
Piroxicam
A
- NSAID; Enolic Acid class
2. T1/2 = ~50 hours
22
Q
Sulindac
A
- NSAID; acetic acid class
- Prodrug; active sulfide metabolite
- Approved for use in pediatric patients
23
Q
Celecoxib
A
- NSAID; COX-2 Selective Inhibitor
- 2C9 substrate
- Treats RA
24
Q
N-Acetylcysteine
A
- Treatment for Acetaminophen Overdose
25
Prednisone
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)
26
Dexamethasone
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)
27
Cyclosporin A (Cyclosporine)
1. Calcineurin Inhibitor; Immunosuppresant; lipid-soluble peptide
2. ROA: oral, IV, opthalmic emulsion
2. MOA: binds Cyclophilin C --> decreases calcineurin (cytoplasmic phosphatase) --> decreases production of cytokines (IL-2) --> reduced response of Tcells to Ags
3. Uses: GvH disease in bone marrow transplantation, aplastic anemia, transplant rejection, autoimmune diseases, dry eye syndrome
4. Toxicity: reversible nephrotoxicity (dose-limiting), vasconstriction leading to HTN, neurotoxicity, hyperlipidemia, transient hepatotoxicity, stimulates TGF-beta which increases risk of cancer
5. Interactions: metabolized by P450; erythromycin, ketoconazole, amphotericin B, and grapefruit juice inhbit metabolism; phenobarbital and rifampin increase clearance
28
Tacrolimus (FK506)
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
29
Sirolimus
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
30
Azathioprine
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
31
Mycophenoate Mofetil
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
32
Fingolimod (FTY720)
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
33
Antithymocyte Globulin (ATG)
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.
34
Muromonab-CD3
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
35
Basiliximab
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)
36
Daclizumab
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)
37
Infliximab
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
38
Etanercept
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.
39
Rh0 (d) Immune Globulin
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
40
Immune globulin
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.
41
Methotrexate
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
42
Adalimunab
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
43
Allopurinol
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
44
Febuxostat
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
45
Probenecid/Sulfinpyrazone
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
46
Colchicine
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
47
Rasburicase
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
48
Penicillin G
1. Cell wall synthesis inhibitor
2. Natural penicillin
3. Narrow spectrum
4. Orally administered
49
Penicillin V
1. Cell wall synthesis inhibitor
2. Synthetic penicillin
3. Narrow spectrum
4. Orally administered
50
Oxacillin
cell wall synthesis inhibitor; narrow spectrum
| - anti-staph (isoxazolyl penicillins)
51
Dicloxacillin
cell wall synthesis inhibitor, narrow spectrum
| - anti-staph (isoxazolyl penicillins)
52
Ampicillin
cell wall synthesis inhibitor; amino penicillin
| broad spectrum; bactericidal
53
Amoxicillin
cell wall synthesis inhibitor; amino penicillin
| broad specturm, bactericidal
54
Ticarcillin
cell wall synthesis inhibitor; carboxy penicillin
| broad spectrum; bactericidal
55
Mezlocillin
cell wall synthesis inhibitor; acylureido penicillin
| bactericidal; broad spectrum
56
Clavulanate
Beta-lactamase inhibitor
| - oral; renal excretion
57
Sulbactam
Beta-lactamase inhibitor
| - IV, renal excretion
58
Tazobactam
Beta-lactamase inhibitor
- IV, renal excretion
- pipercillin increases its half life
59
Cefazolin
1st Generation Cephalosporin (narrow spectrum)
| 1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
60
Cephalexin
1st Generation Cephalosporin (narrow)
| 1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
61
Cefuroxime
2nd Generation Cephalosporin (broad)
| 1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
62
Cefoxitin
2nd Generation Cephalosporin (Broad)
| 1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
63
Cefixime
3rd Generation Cephalosporin (broad)
| 1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
64
Cefoperazone
3rd Generation Cephalosporin (Broad)
1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
2. Antipseudomonal
65
Cefotaxime
3rd Generation Cephalosporin (broad)
| 1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
66
Ceftriaxone
3rd Generation Cephalosporin (broad)
| 1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
67
Cefepime
4th Generation Cephalosporin (broad)
1. Inhibit cell wall synthesis by blocking transpeptidase (no cross linking)
2. Antipseudomonal
68
Cefpirome
4th Generation Cephalosporin (broad)
69
Imipenem/Cilastatin
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
Azteronam
Monobactam; narrow spectrum (gram - & anaerboes)
| - same as carbapenem
71
Vancomycin
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
Bacitracin
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
Quinupristin/Dalfopristin (Synercid)
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
Linezolid
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
Erythromycin
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
Clarithromycin
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
Azithromycin
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
Telithromycin
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
Clindamycin
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
Streptomycin
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
Amikacin
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
Gentamicin
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
Kanamycin
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
Tobramycin
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
Tetracycline
Tetracycline; protein synthesis inhibitor;
1. Treats Balantidiasis
2. Bacteriostatic
86
Doxycycline
Tetracycline; protein synthesis inhibitor
87
Minocycline
Tetracycline; protein synthesis inhibitor
88
Tigecycline
Tetracycline; protein synthesis inhibitor
1. IV broad spectrum antibiotic
2. First glycylcycline
3. Used against many drug-resistant organisms
89
Chloramphenicol
protein synthesis inhibitor
1. Prevents docking of aminoacyl tRNA
2. Broad spectrum, bacteriostatic
90
Sulfamethoxazole
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
Sulfasalazine
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
Sulfadiazine
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
Trimethoprim
Folate metabolism inhibitor
1. Used with sulfamethoxazole
2. Prevent recurrent UTI, treat upper respiratory infections
3. No-no with liver impairment patients
94
Ciprofloxacin
Fluoroquinolone; DNA replication, transcription, and metabolism inhibitor; treats atypical mycobacteria
95
Levofloxacin
Fluoroquinolone; DNA replication, transcription, and metabolism inhibitor
96
Metronidazole
Urinary Tract Antiseptic;
1. Treats Amebiasis, Giardiasis, Trichomoniasis, Balantidiasis
2. Used for vaginitis
97
Nitrofurantoin
Chronic/acute Urinary Tract Antiseptic
98
Methenamine
Urinary Tract Antiseptic
| 1. UTI prophylaxis, but not primary agent for treatment
99
Mupirocin
Urinary Tract Antiseptic
1. Topical for staph caused impetigo
2. May cause local itching, rash, contact dermatitis
100
Polymyxins
Urinary Tract Antiseptic
| 1. Topical treatment of resistant gram- infections only
101
Isoniazid
treats TB
| 1. Good oral absorption
102
Ethambutol
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
Pyrazinamide
treats TB
104
Rifampin
treats TB
1. Causes red-orange color in urine, feces, sweat, tears, contact lenses
2. >2 weeks causes flu-like symptoms
105
p-Aminosalicyclic Acid (PAS)
second-line drug for TB
1. Folate synthesis antagonist
2. Adverse effects - GI irritation, hypersensitivity reaction
106
Dapsone
treats Lepra
| 1. Competitively inhibit folate synthesis
107
Clofazimine
treats Lepra
1. Erratic absorption, stored in skin and slowly released
2. Sulfone-resistant leprosy
108
Chloroquine
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
Quinine and Quinidine
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
Mefloquine
treats Malaria
1. Strong erythrocytic schizonticidal
2. Prophylactic agent (FDA approved)
3. Single dose treatment regime
4. Only against falciparum/vivax
111
Primaquine
treats Malaria
1. hepatic schizonticidal/gametocidal
2. Good against all human malaria parasites
3. Only one against hyponozoite vivax/ovale
112
Pyrimethamine
treats Malaria
113
Sulfadoxine
Sulfonamide; treats Malaria
114
Suramin
treats African Trypanosomiasis
1. Administered IV, chemoprophylaxis/early hemolymphatic infection treatment ONLY
2. Adverse effects - GI, CV, neurological/blood
115
Melarsoprol
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
Elfornithine
treats African Trypanosomiasis
1. IV treatments for CNS (better tolerated than melarsoprol)
2. Blocks conversion of ornithine to putrescine
117
Nifurtimox
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
Sodium Stibogluconate
treats Leishmaniasis
| 1. Poor availability, safety, efficacy of these drugs
119
Iodoquinol
treats intestinal Amebiasis
120
Paromomycin Sulfate
treats extraintestinal Amebiasis
121
Nitazoxanide
treats Giardia lamblia, metronidazole resistant protozoa strains, several tapeworm helminthes
122
Praziquantel
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
Niclosamide
treats Cestodes (Tapeworm)
124
Mebendazole
treats Nematodes (Roundworm)
1. Ascariasis, pinworm, hookworm
2. Inhibits microtubule synthesis
125
Pyrantel Pamoate
treats Nematodes (Roundworm)
126
Piperazine
treats Nematodes (Roundworm)
1. Alternative to mebendazole for ascariasis treatment
2. Inhibits acetylcholine at the myoneural junction
127
Cyclophosphamide
Nitrogen Mustard; Alkylating Agent
| 1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins
128
Carmustine (BCNU) and Lomustine
Nitrosoureas; Alkylating Agent
| 1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins
129
Busulfan
Alkyl Sulfonate; Alkylating Agent
| 1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins
130
Dacarbazine
Triazene; Alkylating Agent
| 1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins
131
Procarbazine
Methylhydrazine; Alkylating Agent
| 1. Form strong electrophile intermediates that covalently alkylate nucleophilic groups on DNA, proteins
132
Cis-Plantinum (Cisplatin)
Platinum Complex; Alkylating Agent
| 1. React with nucleophilic sites on DNA and proteins → intrastrand and interstrand cross‐links
133
Carboplatin
Platinum Complex; Alkylating Agent
| 1. React with nucleophilic sites on DNA and proteins → intrastrand and interstrand cross‐links
134
Oxaliplatin
Platinum Complex; Alkylating Agent
| 1. React with nucleophilic sites on DNA and proteins → intrastrand and interstrand cross‐links
135
6-Mercaptopurine (6-MP)
6-Thiopurine; Purine Analog/Related Inhibitor; Antimetabolite
1. Competitively inhibit purine synthesis; 6‐TGP incorporated into DNA
136
6-Thioguanine (6-TG)
6-Thiopurine; Purine Analog/Related Inhibitor; Antimetabolite
1. Competitively inhibit purine synthesis; 6‐TGP incorporated into DNA
137
Fludarabine-5-Phosphate
6-Thiopurine; dPurine Analog/Related Inhibitor; Antimetabolite
138
Leucovorin
Folate Antagonist Rescue Agent; Antimetabolite
| 1. Reduced folate coenzyme
139
5-Fluorouracil (5-FU)
Pyrimidine Analog; Antimetabolite
| 1. Reduced folate coenzyme
140
Cytarabine (AraC)
Pyrimidine Analog; Antimetabolite
| 1. Reduced folate coenzyme
141
Gemcitabine
Pyrimidine Analog; Antimetabolite
| 1. Reduced folate coenzyme
142
Vinblastine
Vinca Alkaloid; Plant Alkaloid
| 1. Bind tubulin, block its ability to polymerize into microtubules
143
Vincristine
Vinca Alkaloid; Plant Alkaloid
| 1. Bind tubulin, block its ability to polymerize into microtubules
144
Paclitaxel
Taxane; Plant Alkaloid
| 1. Promotes microtubule polymerization and stabilization
145
Abraxane
(Albumin bound Paclitaxel)
Taxane; Plant Alkaloid
1. Antimitotic drug, M-phase specific
2. Promotes microtubule polymerization and stabilization
146
Topotecan
Camptothecin; Plant Alkaloid
1. S-phase specific
2. Bind to and stabilize the topoisomerase I‐DNA complex
147
Etoposide
Epipodophyllotoxin; Plant Alkaloid
1. S/G2 phase specific,
2. Forms complex with topoisomerase II
148
Actinomycin D (Dactinomycin)
Antitumor Antibiotic
| 1. Bind to DNA by intercalating between base pairs
149
Adriamycin (Doxorubicin)
Anthracycline; Antitumor Antibiotic
| 1. Bind to DNA by intercalating between base pairs
150
Bleomycin
Antitumor Antibiotic
1. G2 phase specific
2. Binds DNA, → free radicals
151
L-asparginase
Enzyme; Antineoplastic Agent
| 1. Hydrolyzes circulating asn
152
Hydroxyurea
Urea analog; Antineoplastic Agent
| 1. Inhibits ribonucleotide reductase
153
Tretinoin (ATRA)
Differentiating Agent; Antineoplastic Agent
| 1. Increases transcription of genes expressing retinoic acid response elements
154
Imatinib Mesylate
Protein Tyrosine Kinase Inhibitor; Antineoplastic Agent
| 1. Inhibits Bcr‐Abl & c‐kit receptor protein kinases
155
Gefitinib
Protein Tyrosine Kinase Inhibitor; Antineoplastic Agent
| 1. Inhibits EGFR tyrosine kinase
156
Bortezomib
Porteasome Inhibitor; Antineoplastic Agent
| 1. Reversibly inhibits the 26S proteasome
157
Trastuzumab
Monoclonal Antibody; Antineoplastic Agent
| 1. Binds, blocks HER2/neu
158
Rituximab
Monoclonal Antibody; Antineoplastic Agent
| 1. Binds, blocks the B cell CD20 surface antigen
159
Cetuximab
Monoclonal Antibody; Antineoplastic Agent
| 1. Binds, blocks EGFR ( increase in colorectal cancer)
160
Bevacizumab
Monoclonal Antibody; Antineoplastic Agent
| 1. Binds vascular endothelial growth factor (VEGF)
161
Interferon-alfa
Biological Response Modifier; Antineoplastic Agent
| 1. Cytokine; receptor complex regulates transcription
162
Interleukin-2 (IL-2)
Biological Response Modifier; Antineoplastic Agent
| 1. Binds receptor on activated T cells, proliferation & NK cytokine production
163
Granulocyte Colony-Stimulating Factor (G-CSF)
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
Granulocyte/Macrophage Colony-Stimulating Factor (GM-CSF)
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
Mechlorethamine
Nitrogen Mustard; Alkylating Agent
1. Most reactive alkylating agent
2. Therapeutic use - Hodgkin's disease
3. Adverse effects - bone marrow and intestinal mucosa
166
Leuprolide Acetate
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
