Pharmacology Flashcards
(256 cards)
1
Q
Penicillin G/V
A
G = IV or IM, V = oral class: beta lactam antibiotic MoA: cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall uses: gram-(+), Neisseria, syphilis SE: hypersensitivity, hemolytic anemia resistance: penicillinase
2
Q
amoxicillin
A
class: beta lactam antibiotic
MoA: cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: gram-(+), H. flu, H. pylori, E. coli, Listeria, Proteus, Salmonella, Shigella (good oral bioavailability)
SE: hypersensitivity, rash, pseudomembranous colitis
resistance: penicillinase (combine with clavulanic acid)
3
Q
ampicillin
A
class: beta lactam antibiotic
MoA: cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: gram-(+), H. flu, H. pylori, E. coli, Listeria, Proteus, Salmonella, Shigella
SE: hypersensitivity, rash, pseudomembranous colitis
resistance: penicillinase (combine with clavulanic acid)
4
Q
nafcillin
A
class: beta lactam antibiotic
MoA: -cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: S. aureus (not MRSA)
SE: hypersensitivity, interstitial nephritis
resistance: penicillinase-resistant
5
Q
piperacillin/ticarcillin
A
class: beta lactam antibiotics
MoA: -cidal; binds pencillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: Pseudomonas, gram-(-) rods
SE: hypersensitivity
resistance: penicillinase (use with beta-lactamase inhibitor)
6
Q
beta-lactamase inhibitors
A
clavulanic acid, tazobactam, sulbactam
7
Q
cephazolin/cephalexin
A
class: beta lactam antibiotics, first-gen cephalosporins
MoA: -cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: gram-(+), Proteus, E. coli, Klebsiella, surgical wound infection prophylaxis (cephazolin)
SE: hypersensitivity, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency, increase nephrotoxicity of aminoglycosides
resistance: structural change in PBP, beta lactamase
8
Q
cefuroxime/cefoxitin
A
class: beta lactam antibiotics, second-gen cephalosporins
MoA: -cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: gram-(+), Proteus, E. coli, Klebsiella, H. flu, Enterobacter, Neisseria, Serratia
SE: hypersensitivity, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency, increase nephrotoxicity of aminoglycosides
resistance: structural change in PBP, beta lactamase
9
Q
ceftriaxone
A
class: beta lactam antibiotics, third-gen cephalosporin
MoA: -cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: meningitis, gonorrhea, disseminated Lyme disease
SE: hypersensitivity, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency, increase nephrotoxicity of aminoglycosides
resistance: structural change in PBP, beta lactamase
10
Q
ceftazidime
A
class: beta lactam antibiotics, third-gen cephalosporin
MoA: -cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: Pseudomonas
SE: hypersensitivity, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency, increase nephrotoxicity of aminoglycosides
resistance: structural change in PBP, beta lactamase
11
Q
cefepime
A
class: beta lactam antibiotics, fourth-gen cephalosporin
MoA: -cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: Pseudomonas, gram-(-), gram-(+)
SE: hypersensitivity, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency, increase nephrotoxicity of aminoglycosides
resistance: structural change in PBP, beta lactamase
12
Q
ceftaroline
A
class: beta lactam antibiotics, fifth-gen cephalosporin
MoA: -cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall
uses: MRSA, broad-spec gram-(+) and gram-(-) (NOT Pseudomonas)
SE: hypersensitivity, autoimmune hemolytic anemia, disulfiram-like reaction, vitamin K deficiency, increase nephrotoxicity of aminoglycosides
resistance: structural change in PBP, beta lactamase
13
Q
imipenem
A
class: beta lactam antibiotic, carbapenem
MoA: -cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall; administer with cilastatian to inhibit inactivation by renal dehydropeptidase I
uses: broad-spec gram-(+) cocci, gram-(-) rods (including Pseudomonas), anaerobes
SE: GI distress, rash, seizures
resistance: beta-lactamase-resistant
14
Q
meropenem
A
class: beta lactam antibiotic, carbapenem
MoA: -cidal; binds penicillin-binding proteins, blocks cross-linking of peptidoglycan cell wall; stable to renal dehydropeptidase I
uses: broad-spec gram-(+) cocci, gram-(-) rods (including Pseudomonas), anaerobes
SE: GI distress, rash
resistance: beta-lactamase-resistant
15
Q
aztreonam
A
class: beta lactam antibiotic (monobactam)
MoA: -cidal; binds penicillin-binding protein 3, blocks cross-linking of peptidoglycan cell wall; synergistic with ahminoglycosides
uses: gram-(-) rods (no activity against gram-(+) or anaerobes)
SE: occasional GI upset; no cross-allergenicity with penicillins
16
Q
vancomycin
A
class: antibiotic
MoA: -cidal; inhibits cell wall peptidoglycan formation by binding D-ala-D-ala residues of cell wall precursors
uses: gram-(+) only - MRSA, S. epidermidis, sensitive Enterococcus, C. difficile
SE: nephrotoxicity, ototoxicity, thrombophlebitis, flushing (pretreat with anti-histamines)
resistance: amino acid modification of D-ala-D-ala to D-ala-D-lac; beta-lactamase resistant
17
Q
gentamycin/neomycin/streptomycin
A
class: aminoglycoside antibiotics
MoA: -cidal; protein synthesis inhibitors; bind 30S ribosome and irreversibly inhibit initiation complex formation; require oxygen for uptake into bacterial cells uses: severe gram-(-) rod infections; synergistic with beta-lactams (esp. aztreonam); bowel surgery (neomycin)
SE: nephrotoxicity, neuromuscular blockade, ototoxicity, teratogenic
resistance: drug inactivation via bacterial transferase enzymes
18
Q
doxycycline
A
class: tetracycline antibiotic
MoA: -static; protein synthesis inhibitor; binds 30S ribosome and prevents attachment of aminoacyl-tRNA; safe for use in pts with renal failure; inhibited by divalent cations
uses: Borrelia burgdorferi, M. pneumoniae, RIckettsia, Chlamydia, acne
SE: GI distress, discoloration of teeth, inhibition of bone growth, photosensitivity
resistance: decreased uptake or increased efflux by plasmid-encoded transport pumps
19
Q
chloramphenicol
A
class: antibiotic
MoA: -static; protein synthesis inhibitor; binds 50S ribosome and blocks peptidyltransferase
uses: meningitis, Rickettsia rickettsii
SE: anemia, aplastic anemia, gray baby syndrome
resistance: drug inactivation via plasmid-encoded acetyltransferase
20
Q
clindamycin
A
class: antibiotic
MoA: -static; protein synthesis inhibitor; binds 50S ribosome and blocks peptide transfer/translocation
uses: anaerobic infections above the diaphragm (aspiration pneumonia, lung abscesses, oral infection), C. perfringens, invasive group A Strep
SE: pseudomembranous colitis, fever, diarrhea
21
Q
linezolid
A
class: oxazolidinone antibiotic
MoA: -static; protein synthesis inhibitor; binds 50S ribosome and prevents formation of initiation complex
uses: gram (+), including MRSA and VRE
SE: bone marrow suppression (esp. thrombocytopenia), peripheral neuropathy, serotonin syndrome
resistance: point mutation of rRNA
22
Q
clarithromycin/erythromycin
A
class: macrolide antibiotics
MoA: -static; protein synthesis inhibitors; bind 50S ribosome and block translocation
uses: atypical pneumonia, chlamydia, gram (+) in pts allergic to penicillin, pertussis
SE: GI motility issues, arrhythmia (prolongs QT), cholestatic hepatitis, rash, eosinophilia, CYP450 inhibition
resistance: methylation of 23S rRNA at drug binding site
23
Q
azithromycin
A
class: macrolide antibiotics
MoA: -static; protein synthesis inhibitors; bind 50S ribosome and block translocation
uses: atypical pneumonia, chlamydia, gram (+) in pts allergic to penicillin, pertussis
SE: similar to other macrolides but fewer (GI motility issues, arrhythmia (prolongs QT), cholestatic hepatitis, rash, eosinophilia)
resistance: methylation of 23S rRNA at drug binding site
24
Q
trimethoprim
A
class: antibiotic
MoA: -static; inhibits bacterial dihydrofolate reductase
uses: TMP-SMX combo for UTIs, Shigella, Salmonella, Pneumocystis pneumonia (tx and prophylaxis), toxoplasma prophylaxis
SE: megaloblastic anemia, leukopenia, granulocytopenia (alleviated with folic acid supplementation)
25
sulfamethoxazole
class: sulfonamide antibiotic
MoA: -static (-cidal when combined with trimethoprim); para-aminobenzoic acid metabolite, inhibits dihydropteroate synthase (folate synthesis)
uses: gram (+), gram (-), Nocardia, Chlamydia
SE: hypersensitivity, hemolysis in G6PD deficiency, nephrotoxicity (tubulointerstitial nephritis), photosensitivity, kernicterus (in infants), displaces other drugs (i.e. warfarin) from albumin
resistance: altered enzyme, decreased uptake, increased PABA synthesis
26
ciprofloxacin/levofloxacin
class: fluoroquinolone antibiotics
MoA: -cidal; inhibits bacterial topoisomerase II and IV; cannot be taken with antacids
uses: gram (-) rods of urinary and GI tracts (including Pseudomonas), Neisseria, some gram (+)
SE: GI upset, superinfection, rash, headache, dizziness, leg cramps, myalsia, damages cartilage in infants/children, tendonitis/tendon rupture in elderly and in pts taking prednisone, prolongs QT interval
resistance: chromosome-encoded DNA gyrase mutation, plasmid-mediated resistance, efflux pumps
27
moxifloxacin
class: fluoroquinolone antibiotics
MoA: -cidal; inhibits bacterial topoisomerase II and IV; cannot be taken with antacids
uses: gram (-) rods of urinary and GI tracts (NOT effective for Pseudomonas), Neisseria, some gram (+)
SE: GI upset, superinfection, rash, headache, dizziness, leg cramps, myalsia, damages cartilage in infants/children, tendonitis/tendon rupture in elderly and in pts taking prednisone, prolongs QT interval
resistance: chromosome-encoded DNA gyrase mutation, plasmid-mediated resistance, efflux pumps
28
daptomycin
class: antibiotic
MoA: disrupts cell membrane of gram (+) cocci; inactivated by surfactant (not effective for pneumonia)
uses: S. aureus (esp. MRSA), bacteremia, endocarditis, VRE
SE: myopathy, rhabdomyolysis
29
metronidazole
class: antibiotic
MoA: -cidal; antiprotozoal; forms toxic free radical metabolites that damage bacterial DNA
uses: anaerobic infections below the diaphragm; GIardia, Entamoeba, Trichomonas, Gardnerella vaginalis, Bacteroides, C. difficile, H. pylori (with proton pump inhibitor and clarithromycin)
SE: disulfiram-like reaction, headache, metallic taste
30
rifampin/rifabutin
class: rifamycin antibiotic
MoA: inhibits DNA-dependent RNA polymerase (mRNA synthesis)
uses: tuberculosis (combined with isoniazid, ethambutol, and pyrazinamide), leprosy (combined with dapsone), meningococcal prophylaxis, Hib prophylaxis in contacts of infected children
SE: hepatotoxicity, induces CYP450s (less in rifabutin), orange body fluids
resistance: mutations reduce drug binding to RNA polymerase; promoted by monotherapy
31
isoniazid
class: antibiotic
MoA: inhibits mycolic acid synthesis; activated by KatG (bacterial catalase-peroxidase)
uses: tuberculosis (in combination with rifampin, ethambutol, and pyrazinamide), TB prophylaxis
SE: neurotoxicity, hepatotoxicity (SE prevented by pyridoxine (vit. B6) supplementation), drug-induced lupus (esp. in slow acetylators)
resistance: low expression of KatG
32
pyrazinamide
class: antibiotic
MoA: intracellular, otherwise unknown
uses: tuberculosis (in combination with rifampin, isoniazid, and ethambutol)
SE: hyperuricemia, hepatotoxicity
33
ethambutol
class: antibiotic
MoA: inhibits mycobacterial cell wall synthesis by blocking arabinosyltransferase (arabinoglycan synthesis/polymerization)
uses: tuberculosis (in combination with rifampin, isoniazid, and pyrazinamide)
SE: optic neuropathy (red-green colorblindness)
34
M. avium-intracellulare prophylaxis
azithromycin, rifabutin
35
M. avium-intracellulare treatment
azithromycin or clarithromycin + ethambutol; may add rifabutin or ciprofloxacin
36
leprosy treatment
tuberculoid: dapsone and rifampin
lepromatous: dapsone and rifampin and clofazimine
37
endocarditis prophylaxis for dental/surgical procedures
amoxicillin
38
gonorrhea exposure prophylaxis
ceftriaxone
39
UTI prophylaxis
TMP-SMX
40
meningococcal exposure prophylaxis
ceftriaxone, ciprofloxacin, or rifampin
41
pregnant woman carrying group B strep peripartum prophylaxis
Penicillin G
42
prevention of gonococcal conjunctivitis in newborn
erythromycin ointment
43
prevention of post surgical S. aureus infection
cefazolin
44
prophylaxis of strep pharyngitis in child with prior rheumatic fever
benzathine penicillin G or or oral penicillin V
45
syphilis exposure prophylaxis
benzathine penicillin G
46
amphotericin B
class: anti-fungal
MoA: binds ergosterol, forms membrane pores; affects renal tubule permeability, supplement K+ and Mg+
uses: systemic mycoses: Cryptococcus (w/ or w/o flucytosine for meningitis), Blastomyces, Coccidioides, Histoplasma, Candida, Mucor; intrathecal for fungal meningitis
SE: fever/chills, hypotension, nephrotoxicity (reduced by hydration), arrhythmias, anemia, phlebitis
47
nystatin
class: anti-fungal
MoA: binds ergosterol, forms membrane pores; topical use only
uses: oral candidiasis, diaper rash, vaginal candidiasis
48
flucytosine
class: anti-fungal
MoA: inhibits DNA/RNA synthesis by conversion to 5-fluorouracil (cytosine deaminase)
uses: systemic fungal infection (esp. Cryptococcus meningitis) in combination with amphotericin B
SE: bone marrow suppression
49
fluconazole
class: anti-fungal
MoA: inhibits ergosterol synthesis by blocking CYP450 enzyme that catalyzes lanosterol --> ergosterol
uses: local and minor systemic mycoses, chronic suppression of cryptococcal meningitis in AIDS pts, Candida
SE: testosterone synthesis inhibition, liver dysfunction
50
itraconazole
class: anti-fungal
MoA: inhibits ergosterol synthesis by blocking CYP450 enzyme that catalyzes lanosterol --> ergosterol
uses: local and minor systemic mycoses: Blastomyces, Coccidioides, Histoplasma
SE: testosterone synthesis inhibition, liver dysfunction
51
clotrimazole/miconazole
class: anti-fungal
MoA: inhibits ergosterol synthesis by blocking CYP450 enzyme that catalyzes lanosterol --> ergosterol
uses: topical fungal infections
SE: testosterone synthesis inhibition, liver dysfunction
52
terbinafine
class: anti-fungal
MoA: inhibits lanosterol synthesis by blocking squalene epoxidase
uses: dermatophytoses (esp. onychomycosis)
SE: GI upset, headaches, hepatotoxicity, taste disturbance
53
caspofungin
class: echinocandin anti-fungal
MoA: inhibits beta-glucan synthesis/fungal cell wall synthesis
uses: invasive aspergillosis, Candida
SE: GI upset, flushing (via histamine release)
54
griseofulvin
class: anti-fungal
MoA: interferes with microtubule function, disrupts mitosis; deposits in keratin-containing tissues
uses: oral treatment of superficial infections (dermatophytes)
SE: teratogenic, carcinogenic, confusion, headaches, CYP450 induction
55
toxoplasma tx
pyrimethamine + sulfadiazene
56
Trypanosoma brucei tx.
suramin + melarsoprol
57
Trypanosoma cruzi tx.
nifurtimox or benznidazole
58
leishmaniasis tx.
sodium stibogluconate or amphotericin B
59
malaria tx
for sensitive spp.: chloroquine
for resistant spp.: mefloquine OR atovaquone + proguanil
for life-threatening: IV quinidine OR artesunate
for P. vivax/ovale: add primaquine
60
babesia tx
atovaquone + azithromycin
61
azathioprine
prodrug of 6-mercaptopurine
62
6-mercaptopurine
class: antimetabolite
MoA: purine analog activated by HGPRT, inhibits de novo purine synthesis
uses: transplant rejection prophylaxis, RA, IBD, SLE, steroid weaning
side effects: myelosuppression, GI, liver; toxicity increased by co-tx with allopurinol or febuxostat
63
6-thioguanine
class: antimetabolite
MoA: purine analog activated by HGPRT, inhibits de novo purine synthesis
uses: transplant rejection prophylaxis, RA, IBD, SLE, steroid weaning
side effects: myelosuppression, GI toxicity, liver toxicity; toxicity increased by co-tx with allopurinol or febuxostat
64
cladribine
class: antimetabolite
MoA: purine analog; inhibits DNA polymerase, induces DNA strand breaks, inhibits adenosine deaminase
uses: hairy cell leukemia
side effects: myelosuppression, nephrotoxicity, neurotoxicity
65
cytarabine
class: antimetabolite
MoA: pyrimidine analog, inhibits DNA polymerase
uses: leukemias (AML), lymphomas
side effects: pancytopenia, megaloblastic anemia
66
5-fluorouracil
class: antimetabolite
MoA: pyrimadine analog, converted to 5F-dUMP, which covalently complexes folic acid and inhibits thymidylate synthase; action enhanced by leucovorin co-tx
uses: colon cancer, pancreatic cancer, basal cell carcinoma
side effects: myelosuppression
67
methotrexate
class: antimetabolite
MoA: folic acid analog, cometitively inhibits dihydrofolate reductase
uses: leukemias (ALL), lymphomas, choriocarcinoma, sarcoma, ectopic pregnancy, medical abortion (+ misoprostol), RA, psoriasis, IBD, vasculitis
side effects: myelosuppression (reversible with leucovorin co-tx), hepatotoxicity, oral ulcers, pulmonary fibrosis
68
bleomycin
class: antibiotic
MoA: induces free radical formation and DNA strand breaks
uses: testicular cancer, Hodgkin lymphoma
side effects: pulmonary fibrosis, skin hyper pigmentation, mucositis
69
dactinomycin (actinomycin D)
class: antibiotic
MoA: intercalates DNA
uses: Wilms tumor, Ewing sarcoma, rhabdomyosarcoma (childhood cancers)
side effects: myelosuppression
70
doxorubicin, danorubicin
class: antibiotic
MoA: generates free radicals, intercalates DNA, induces DNA strand breaks
uses: solid tumors, leukemias, lymphomas
side effects: dilated cardiomyopathy (reduced by dexrazoxane co-tx), myelosuppression, alopecia
71
busulfan
class: alkylating agent
MoA: cross-links DNA
uses: CML, bone marrow transplant pre-tx
side effects: pulmonary fibrosis, severe myelosuppression, hyperpigmentation
72
cyclophosphamide
class: alkylating agent
MoA: activated by the liver; cross-links DNA at guanine N-7
uses: solid tumors, leukemia, lymphoma
side effects: myelosuppression, hemorrhagic cystitis (reduced with mesna co-tx)
73
nitrosoureas (carmustine, lomustine, semustine, streptozocin)
class: alkylating agents
MoA: bioactivated; cross-link DNA; cross BBB
uses: brain tumors
side effects: convulsions, dizziness, ataxia
74
paclitaxel
class: taxol
MoA: hyperstabilizes microtubules
uses: ovarian and breast carcinoma
side effects: myelosuppression, alopecia, hypersensitivity
75
vincristine
class: vinca alkaloid
MoA: binds b-tubulin and prevents microtubule polymerization
uses: solid tumors, leukemias, non-Hodgkin lymphoma
side effects: neurotoxicity (areflexia, peripheral neuritis), paralytic ileus
76
vinblastine
class: vinca alkaloid
MoA: binds b-tubulin and prevents microtubule polymerization
uses: solid tumors, leukemias, Hodgkin lymphoma
side effects: myelosuppression
77
cisplatin, carboplatin
class: anti-tumor agent
MoA: cross-links DNA
uses: testicular, bladder, ovary, and lung carcinoma
side effects: nephrotoxicity (reduced with amifostine co-tx), ototoxicity
78
etoposide
class: anti-tumor agent
MoA: inhibits topoisomerase II, promotes DNA degradation
uses: solid tumors (esp. testicular and small cell lung), leukemias, lymphomas
side effects: myelosuppression, GI upset, alopecia
79
irinotecan
class: anti-tumor agent
MoA: inhibits topoisomerase I, prevents DNA unwinding/replication
uses: colon cancer
side effects: severe myelosuppression, diarrhea
80
topotecan
class: anti-tumor agent
MoA: inhibits topoisomerase I, prevents DNA unwinding/replication
uses: ovarian and small cell lung cancer
side effects: severe myelosuppression, diarrhea
81
hydroxyurea
class: anti-tumor agent
MoA: inhibits ribonucleotide reductase/DNA synthesis
uses: melanoma, CML, sickle cell disease
side effects: severe myelosuppression, GI upset
82
bevacizumab
class: monoclonal Ab
MoA: binds and inactivates VEGF; inhibits angiogenesis
uses: solid tumors (colorectal, renal cell)
side effects: hemorrhage, blood clots, impaired wound healing
83
erlotinib
class: tyrosine kinase inhibitor
MoA: binds and antagonizes EGFR
uses: non-small cell lung carcinoma
side effects: rash
84
imatinib
class: tyrosine kinase inhibitor
MoA: binds and antagonizes BCR-ABL tyrosine kinase and c-kit
uses: CML, GIST
side effects: fluid retention
85
rituximab
class: monoclonal antibody
MoA: binds and antagonizes CD20
uses: non-Hodgkin lymphoma, CLL, IBD, RA
side effects: increased risk of progressive multifocal leukoencephalopathy
86
tamoxifen
class: selective estrogen receptor modulator
MoA: pro-estrogenic effects at bone and endometrium; anti-estrogenic effects at breast; blocks estrogen binding to ER (+) cells
uses: breast cancer treatment and prevention
side effects: hot flashes, increased risk of endometrial carcinoma
87
ralixifene
class: selective estrogen receptor modulator
MoA: pro-estrogenic effect at bone; anti-estrogenic effects at breast and endometrium; blocks estrogen binding to ER (+) cells
uses: osteoporosis, breast cancer prevention
side effects: ?
88
trastuzumab
class: monoclonal antibody
MoA: binds and antagonizes HER-2 tyrosine kinase receptor; inhibits HER-2-initiated cellular signaling; induces antibody-dependent cytotoxicity
uses: HER-2 (+) breast cancer and gastric cancer
side effects: cardiotoxicity
89
vemurafenib
class: small molecule protein inhibitor
MoA: binds and inhibits BRAF
uses: metastatic melanoma
90
mannitol
class: osmotic diuretic
MoA: increases tubular fluid osmolarity and urine flow, decreases intracranial/intraocular pressure
uses: drug overdose, elevated intracranial/intraocular pressure
side effects: pulmonary edema, dehydration; contraindicated in anuria, HF
91
acetazolamide
class: diuretic
MoA: inhibits carbonic anhydrase on apical surface of renal tubules; prevents HCO3- reabsorption; decreases aqueous humor synthesis
uses: glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness, pseudotumor cerebri
side effects: hyperchloremic metabolic acidosis, paresthesias, NH3 toxicity, sulfa allergy
92
furosemide/bumetanide/torsemide
class: loop diuretics
MoA: inhibits Na/K/2Cl transporter in thick ascending loop of Henle; abolish hypertonicity of renal medulla; stimulate PGE release; increase Ca excretion
uses: edema, hypertension, hypercalcemia
side effects: ototoxicity, hypokalemia, dehydration, sulfa allergy, interstitial nephritis, gout
93
ethacrynic acid
class: loop diuretic
MoA: inhibits Na/K/2Cl transporter in thick ascending loop of Henle; abolishes hypertonicity of renal medulla; stimulates PGE release; increases Ca excretion
uses: diuresis in pts allergic to sulfa drugs
side effects: ototoxicity, hypokalemia, dehydration, interstitial nephritis, hyperuricemia
94
chlorthalidone/hydrochlorothiazide
class: thiazide diuretics
MoA: inhibit Na/Cl co-transporter in early DCT; decrease diluting capacity of nephron; decrease Ca excretion/promote Ca reabsorption
uses: hypertension, heart failure, idiopathic hypercalciuria, nephrogenic diabetes insipidus, osteoporosis
side effects: hypokalemic metabolic alkalosis, hyponatremia, hyperglycemia, hyperlipidemia, hyperuricemia, hypercalcemia, sulfa allergy
95
spironolactone/eplerenone
class: potassium-sparing diuretics
MoA: competitive aldosterone receptor antagonists in cortical collecting tubule
uses: hyperaldosteronism, K depletion, heart failure
side effects: hyperkalemia (arrhythmias), endocrine effects (spironolactone - gynecomastia, anti androgen effects)
96
triamterene/amiloride
class: potassium-sparing diuretics
MoA: block sodium channels (ENaC) in the cortical collecting tubule
uses: hyperaldosteronism, potassium depletion, heart failure, Liddle syndrome
side effects: hyperkalemia (arrhythmias)
97
captopril/enalapril/lisinopril/ramipril
class: ACE inhibitors
MoA: inhibit angiotensin converting enzyme; prevent angiotensin II synthesis; decrease GFR by preventing constriction of efferent arterioles (usually leads to an increase in renin); prevent inactivation of bradykinin
uses: hypertension, heart failure, proteinuria, diabetic nephropathy
side effects: cough, angioedema, teratogens (cause fetal renal malformation), increased Cr/decreased GFR, hyperkalemia, hypotension; contraindicated in bilateral renal artery stenosis
98
losartan/candesartan/valsartan
class: angiotensin receptor blockers (ARB)
MoA: selectively block AngII binding to AT1 receptor; effects similar to ACEi, but do not increase bradykinin
uses: hypertension, heart failure, proteinuria, diabetic nephropathy with intolerance to ACEi
side effects: hyperkalemia, decreased renal function, hypotension, teratogens
99
aliskiren
class: direct renin inhibitor
MoA: inhibits renin, prevents conversion of angiotensinogen to angiotensin I
uses: hypertension
side effects: hyperkalemia, decreased renal function, hypotension; contraindicated in diabetics taking ACEi or ARBs concurrently
100
anti-HTN drugs that are safe during pregnancy
hydralazine, methyldopa, beta blockers, nifedipine
101
amlodipine/nifedipine/nicarpidine
class: dihydropyridine Ca-channel blockers
MoA: block L-type calcium channels of vascular smooth muscle, decreases contractility (vasodilation)
uses: hypertension, angina (including Prinzmetal), Raynaud phenomenon
side effects: peripheral edema, flushing, dizziness, constipation, gingival hyperplasia
102
nimodipine
class: dihydropyridine Ca-channel blocker
MoA: block L-type calcium channels of vascular smooth muscle, decreases contractility (vasodilation)
uses: subarachnoid hemorrhage
side effects: peripheral edema, flushing, dizziness, constipation, gingival hyperplasia
103
clevidipine
class: dihydropyridine Ca-channel blocker
MoA: block L-type calcium channels of vascular smooth muscle, decreases contractility (vasodilation)
uses: hypertensive urgency or emergency, hypertension, angina (including Prinzmetal), Raynaud phenomenon
side effects: peripheral edema, flushing, dizziness, constipation, gingival hyperplasia
104
diltiazem/verapamil
class: non-dihydropyridine Ca-channel blockers
MoA: blocks L-type calcium channels of cardiac and smooth muscle, decreases contractility; verapamil has stronger cardioselectivity than diltizem
uses: hypertension, angina, atrial fibrillation, atrial flutter
side effects: cardiac depression, AV block, peripheral edema, flushing, dizziness, constipation, gingival hyperplasia (verapamil only: hyperprolactinemia)
105
hydralazine
class: direct vasodilator
MoA: increases cGMP concentration leading to smooth muscle relaxation; preferentially dilates arterioles over veins; reduces after load
uses: severe hypertension (particularly acute), heart failure (with nitrate), HTN during pregnancy
side effects: reflex tachycardia (contraindicated in angina/CAD; prevented by co-tx with beta blocker), fluid retention, headache, angina, drug-induced lupus
106
drugs used for hypertensive emergency
clevidipine, fenoldopam, labetalol, nicardipine, nitroprusside
107
nitroprusside
class: NO donator
MoA: increases cGMP concentration by direct release of NO
uses: hypertensive emergency
side effects: cyanide toxicity
108
fenoldopam
class: dopaminergic
MoA: D1 receptor agonist; causes coronary, peripheral, renal, and splanchnic vasodilation; decreases blood pressure, increases natriuresis
uses: hypertensive emergency
109
nitroglycerin/isosorbide dinitrate/isosorbide mononitrate
class: nitrates
MoA: increase NO in smooth muscle, increases cGMP and smooth muscle relaxation and subsequent vasodilation; preferentially dilate veins over arteries; decrease preload
uses: angina, acute coronary syndrome, pulmonary edema
side effects: reflex tachycardia (prevent with co-tx with beta blocker), hypotension, flushing, headache, tolerance ("Monday disease")
110
lovastatin/pravastatin/simvastatin/atorvastatin/rosuvastatin
class: statins
MoA: inhibit HMG-CoA reductase/mevalonate synthesis, leads to increased LDL receptor expression; decreases mortality in CAD pts; lowers LDL and triglycerides, increases HDL; drugs target liver by degradation via CYP3A4
uses: hyperlipidemia, CAD
side effects: hepatotoxicity (check LFTs), myopathy (exacerbated by co-tx with vibrates or niacin); myopathy increased by co-tx with CYP3A4 inhibitors (increases statin systemic concentrations) and SLCO1B1 loss-of-function polymorphisms
111
cholestyramine/colestipol/colesevelam
class: bile acid resins
MoA: bind and prevent absorption of bile acids; prevents enterohepatic recycling of bile acids; decrease LDL, slightly raise HDL and TG
uses: hyperlipidemia
side effects: GI upset, decreased absorption of other drugs and fat-soluble vitamins
112
ezetimibe
class: anti-lipid
MoA: prevents cholesterol absorption at small intestine brush border (inhibits NPC1L1 transporter); decreases LDL
uses: hyperlipidemia
side effects: increased LFTs, diarrhea
113
gemfibrozil/clofibrate/bezafibrate/fenofibrate
class: fibrates
MoA: upregulate LPL to increase TG clearance; activate PPAR-a to induce HDL synthesis; decrease triglycerides and LDL, increase HDL
uses: hyperlipidemia (particularly hypertriglyceridemia)
side effects: myopathy, cholesterol gallstones
114
niacin
class: vitamin B3
MoA: inhibits hormone-sensitive lipase in adipose tissue; reduces hepatic VLDL synthesis; decreases LDL and TG, increases HDL (more than other anti-lipid drugs)
uses: hyperlipidemia
side effects: flushing (decreased by NSAIDs or long-term use), hyperglycemia, hyperuricemia
115
digoxin
class: cardiac glycoside
MoA: inhibits basolateral Na/K pump, indirectly inhibits Na/Ca exchanger; positive inotrope; increases vagal tone (decreases AV nodal conduction, depresses SA node)
uses: heart failure, atrial fibrillation
side effects: cholinergic, blurry yellow vision, arrhythmias, AV block, hyperkalemia
contraindications: renal failure, hypokalemia, verapamil, amiodarone, quinidine (decreases clearance)
antidote: normalize potassium, cardiac pacer, Mg, anti-digoxin Fab fragments
116
quinidine
```
class: antiarrhythmic, class IA
MoA: blocks sodium channels, particularly in frequently depolarized cells (i.e. tachycardia); decreases slope of phase 0 depolarization; increases AP duration and effective refractory period; increases QT interval
uses: atrial and ventricular arrhythmias (esp. re-entrant and ectopic SVT and VT)
side effects: cinchonism (headache, tinnitus), thrombocytopenia, torsades de pointes
```
117
procainamide
```
class: antiarrhythmic, class IA
MoA: blocks sodium channels, particularly in frequently depolarized cells (i.e., tachycardia); decreases slope of phase 0 depolarization; increases AP duration and effective refractory period; increases QT interval
uses: atrial and ventricular arrhythmias (esp. re-entrant and ectopic SVT and VT)
side effects: drug-induced lupus, thrombocytopenia, torsades de pointes
```
118
disopyramide
```
class: antiarrhythmic, class IA
MoA: blocks sodium channels, particularly in frequently depolarized cells (i.e., tachycardia); decreases slope of phase 0 depolarization; increases AP duration and effective refractory period; increases QT interval
uses: atrial and ventricular arrhythmias (esp. re-entrant and ectopic SVT and VT)
side effects: heart failure, thrombocytopenia, torsades de pointes
```
119
lidocaine/mexiletine
```
class: antiarrhythmic, class IB
MoA: blocks sodium channels, particularly in frequently depolarized cells (i.e. tachycardia); decreases slope of phase 0 depolarization; decreases AP duration; preferentially affects ischemic or depolarized Purkinje and ventricular tissue
uses: acute ventricular arrhythmias (esp. post-MI), digitalis-induced arrhythmias; safe for pts with long-QT
side effects: CNS stimulation/depression, cardiovascular depression
```
120
flecainide/propafenone
```
class: antiarrhythmic, class IC
MoA: blocks sodium channels, particularly in frequently depolarized cells (i.e., tachycardia); decreases slope of phase 0 depolarization; no effect on AP duration; prolongs effective refractory period in AV node and accessory bypass tracts, no effect on effective refractory period in purkinje or ventricular tissue
uses: SVTs (especially useful for re-entrant circuits), atrial fibrillation, last-resort in refractory VT
side effects: pro arrhythmic (esp. post-MI); contraindicated in structural and ischemic heart disease
```
121
beta blockers (as anti-arrhythmics)
class: antiarrhythmics, class II
MoA: blocks beta adrenergic receptors; decrease SA and AV nodal activity by decreasing cAMP and Ca currents; suppress abnormal pacemakers; decrease slope of phase 4 depolarization in nodal cells; AV node is particularly sensitive --> increase PR interval; esmolol is short-acting
uses: SVT, ventricular rate control for atrial fibrillation and atrial flutter
side effects: impotence, exacerbation of COPD and asthma, cardiovascular effects (bradycardia, AV block, HF), CNS effects (sedation, sleep alterations), masks signs of hypoglycemia; metoprolol can cause dyslipidemia; propranolol can exacerbate vasospasm in Prinzmetal angina; cause unopposed a-agonism if given alone in pheochromocytoma or cocaine toxicity
antidote for overdose: saline, atropine, glucagon
122
amiodarone
class: antiarrhythmic, class III
MoA: blocks potassium channels; prolongs myocyte repolarization; increases AP duration, effective refractory period, and QT interval; has class II, II, III, and IV effects; lipophilic
uses: atrial fibrillation, atrial flutter, ventricular tachycardia
side effects: pulmonary fibrosis, hepatotoxicity, hypothyroidism/hyperthyroidism, acts as a hapten (corneal deposits, blue/gray skin deposits, photo dermatitis), neurologic effects, constipation, cardiovascular effects (bradycardia, heart block, heart failure)
note: check PFTs, LFTs, and TFTs
123
ibutilide/dofetilide
```
class: antiarrhythmic, class III
MoA: blocks potassium channels; prolongs myocyte repolarization; increases AP duration, effective refractory period, and QT interval
uses: atrial fibrillation, atrial flutter
side effects: torsades de pointes (esp. ibutilide)
```
124
sotalol
```
class: antiarrhythmic, class III
MoA: blocks potassium channels; prolongs myocyte repolarization; increases AP duration, effective refractory period, and QT interval
uses: atrial fibrillation, atrial flutter, ventricular tachycardia
side effects: torsades de pointes, excessive beta blockade
```
125
verapamil/diltiazem (as antiarrhythmics)
```
class: antiarrhythmics, class IV
MoA: block L-type calcium channels; decrease conduction velocity; increase effective refractory period and PR interval; cause slow rise of action potential and prolonged repolarization at AV node
uses: prevention of nodal arrhythmias (SVT), rate control in atrial fibrillation
side effects: constipation, flushing, edema, cardiovascular effects (HF, AV block, sinus node depression)
```
126
adenosine
class: antiarrhythmic
MoA: promotes potassium exit from cells, hyper polarizes cells and decreases Ca current; very short-acting; effects blunted by theophylline and caffeine
uses: diagnosis/abolition of SVT
side effects: flushing, hypotension, chest pain, sense of impending doom, bronchospasm
127
magnesium
anti arrhythmic effects used for torsades de pointes, digoxin toxicity, and preterm labor cessation
128
hemicholinium
prevents choline transport into presynaptic cholinergic neurons
129
vesamicol
prevents ACh transport into vesicles in presynaptic cholinergic neurons
130
botulinum
prevents ACh vesicle fusion with presynaptic nerve terminal membrane
131
metyrosine
inhibits tyrosine hydroxylase and norepinephrine synthesis in presynaptic noradrenergic neurons
132
reserpine
inhibits dopamine transport into vesicles in presynaptic noradrenergic neurons
133
bretylium/guanethidine
prevent NE vesicle fusion with presynaptic nerve terminal membrane
134
bethanecol
class: cholinergic agonist
MoA: activates bowel and bladder smooth muscle, resistant to AChE
uses: postoperative ileus, neurogenic ileus, urinary retention
side effects: exacerbation of COPD, asthma, and peptic ulcers
135
carbachol
class: cholinergic agonist
MoA: acetylcholine-like
uses: glaucoma
side effects: exacerbation of COPD, asthma, and peptic ulcers
136
methacholine
class: muscarinic agonist
MoA: stimulates airway muscarinic receptors when inhaled
uses: challenge test for diagnosis of asthma
side effects: exacerbation of COPD, asthma, and peptic ulcers
137
pilocarpine
class: cholinergic agonist
MoA: contracts ciliary muscle and pupillary sphincter; resistant to AChE
uses: glaucoma (open- and closed-angle)
side effects: exacerbation of COPD, asthma, and peptic ulcers
138
donepezil/galantamine/rivastigmine
class: cholinergic
MoA: inhibits AChE
uses: Alzheimer disease
side effects: exacerbation of COPD, asthma, and peptic ulcers
139
edrophonium
class: cholinergic
MoA: inhibits AChE
uses: myasthenia gravis diagnosis
side effects: exacerbation of COPD, asthma, and peptic ulcers
140
neostigmine
class: cholinergic
MoA: inhibits AChE; no CNS penetration
uses: postoperative and neurogenic ileus, urinary retention, myasthenia gravis, reversal of neuromuscular junction blockade
side effects: exacerbation of COPD, asthma, and peptic ulcers
141
physostigmine
class: cholinergic
MoA: inhibits AChE; crosses BBB
uses: anticholinergic (e.g. atropine) toxicity
side effects: exacerbation of COPD, asthma, and peptic ulcers
142
pyridostigmine
class: cholinergic
MoA: inhibits AChE; no CNS penetration
uses: myasthenia gravis
side effects: exacerbation of COPD, asthma, and peptic ulcers
143
atropine
class: anticholinergic
MoA: muscarinic receptor antagonist; does NOT affect ACh-mediated CNS effects, which are due to nicotinic receptors
uses: mydriasis/cycloplegia, organophosphate poisoning antidote
side effects: hyperthermia, tachycardia, dry mouth, dry/flushed skin, cycloplegia, constipation, disorientation, acute angle-closure glaucoma, urinary retention (in men with BPH)
144
tropicamide
class: anticholinergic
MoA: muscarinic receptor antagonist
uses: mydriasis/cycloplegia
145
benztropine
class: anticholinergic
MoA: muscarinic receptor antagonist
uses: Parkinson disease, acute dystonia
146
glycopyrrolate
class: anticholinergic
MoA: muscarinic receptor antagonist
uses: preoperative injection to reduce airway secretions, oral dose for drooling and peptic ulcer
147
hyoscyamine/dicyclomine
class: anticholinergic
MoA: muscarinic receptor antagonist
uses: IBS (antispasmodics)
148
ipratropium/tiotropium
class: anticholinergic
MoA: muscarinic receptor antagonist
uses: COPD, asthma
149
oxybutynin/solifenacin/tolterodine
class: anticholinergic
MoA: muscarinic receptor antagonist
uses: bladder spasms, urge urinary incontinence, overactive bladder
150
scopolamine
class: anticholinergic
MoA: muscarinic receptor antagonist
uses: motion sickness
151
tetrodotoxin
class: pufferfish toxin
MoA: blocks fast voltage-gated sodium channels and neuron depolarization
effects: nausea, diarrhea, paresthesias, weakness, dizziness, loss of reflexes
antidote: supportive care
152
ciguatoxin
class: poison from consumption of reef fish (barracuda, snapper, moray eel)
MoA: opens sodium channels, causing depolarization
effects: temperature-related dysesthesia, cholinergic-like effects
antidote: supportive care
153
scombroid poison
class: formed in dark-meat fish improperly stored at warm temperatures
MoA: bacterial histidine decarboxylase converts histidine --> histamine (not degraded by cooking)
effects: burning of mouth, flushing of face, erythema, urticaria, pruritus, headache (commonly mistaken as a fish allergy)
antidote: supportive care, antihistamines, antianaphylactics
154
albuterol/salmeterol
class: adrenergic
MoA: selectively stimulates b2 adrenergic receptors
uses: asthma (albuterol = acute, salmeterol = long-term/COPD)
155
dobutamine
class: adrenergic
MoA: selectively stimulates b1 adrenergic receptors (some affinity for b2 and a)
uses: heart failure (inotropic effect > chronotropic effect), cardiac stress testing
156
dopamine
class: sympathomimetic
MoA: stimulates D1/D2 receptors with some affinity for beta and alpha at high doses (D1 = D2 > b > a)
uses: unstable bradycardia, heart failure, shock
low dose: renal artery dilation
medium dose: cardiac effects
high dose: vascular effects
157
epinephrine
class: adrenergic
MoA: stimulates adrenergic receptors, b > a; higher affinity for b2 receptor than norepinephrine; decreases aqueous humor synthesis via vasoconstriction
uses: anaphylaxis, asthma, open-angle glaucoma; BP increases with rapid bolus, decreases with slow infusion
side effects: mydriasis (do NOT use in closed-angle glaucoma)
158
isoproterenol
class: adrenergic
MoA: selective beta receptor agonist
uses: electrophysiologic evaluation of tachyarrhythmias; can worsen cardiac ischemia
159
norepinephrine
class: adrenergic
MoA: stimulates adrenergic receptors; a1 > a2 > b1
uses: hypotension (increases TPR)
side effects: decreases renal perfusion
160
phenylephrine
class: adrenergic
MoA: selective alpha agonist (a1 > a2)
uses: hypotension, ocular procedures (mydriatic), rhinitis
161
amphetamine
class: adrenergic
MoA: stimulates release of stored catecholamines, inhibits NE reuptake
uses: narcolepsy, obesity, ADHD
162
cocaine
class: adrenergic
MoA: inhibits NE reuptake
uses: vasoconstriction/local anesthesia
note: do NOT give beta blockers if cocaine intoxication is suspected
163
ephedrine
class: adrenergic
MoA: stimulates release of stored catecholamines
uses: nasal decongestion, urinary incontinence, hypotension
164
clonidine
class: adrenergic
MoA: a2 agonist
uses: hypertensive urgency (does not decrease renal blood flow), ADHD, Tourette syndrome
side effects: CNS depression (sedation/confusion, esp. in elderly), bradycardia, hypotension, respiratory depression, miosis
165
a-methyldopa
class: adrenergic
MoA: a2 agonist
uses: hypertension in pregnancy
side effects: direct Coombs (+) hemolysis, drug-induced lupus
166
phenoxybenzamine
class: anti-adrenergic
MoA: irreversibly and non-selectively inhibits a receptors
uses: pheochromocytoma (pre-op tx to prevent HTN)
side effects: orthostatic hypotension, reflex tachycardia
167
phentolamine
class: anti-adrenergic
MoA: reversibly and non-selectively inhibits a receptors
uses: antidote for tyramine-containing foods in pts on MAO inhibitors
side effects: orthostatic hypotension, reflex tachycardia
168
prazosin
class: anti-adrenergic
MoA: selectively inhibits a1 receptors
uses: BPH, PTSD, HTN
side effects: 1st-dose orthostatic hypotension, dizziness, headache, contraindicated in the elderly
169
terazosin/doxazosin
class: anti-adrenergic
MoA: selectively inhibit a1 receptors
uses: BPH, HTN
side effects: 1st-dose orthostatic hypotension, dizziness, headache, contraindicated in the elderly
170
tamsulosin
class: anti-adrenergic
MoA: selectively inhibits a1 receptors
uses: BPH
side effects: 1st-dose orthostatic hypotension, dizziness, headache, contraindicated in the elderly
171
mirtazapine
class: anti-adrenergic
MoA: selectively inhibits a2 receptors
uses: depression
side effects: sedation, increases serum cholesterol, increases appetite
172
common side effects of beta blockers
impotence, bradycardia, AV block, heart failure, seizures, sedation, sleep alterations, dyslipidemia (metoprolol), asthma/COPD exacerbations; avoid in cocaine users; NOT contraindicated in diabetics (benefits outweigh the risks)
173
beta blockers used post-MI
metoprolol, carvedilol, bisoprolol
174
antidote for acetaminophen toxicity
N-acetylcysteine (replenishes glutathione)
175
antidote for organophosphate toxicity
atropine, pralidoxime
176
antidote for amphetamine overdose
NH4Cl (acidifies urine, traps basic amphetamines)
177
antidote for copper, arsenic, or gold poisoning
penicillamine
178
antidote for cyanide poisoning
nitrate + thiosulfate, hydroxocobalamin
179
antidote for iron poisoning
deferoxamine, deferasirox
180
antidote for lead poisoning
EDTA, dimercaprol, succimer, penicillamine
181
antidote for mercury, arsenic, or gold poisoning
dimercaprol, succimer
182
antidote for methanol or ethylene glycol poisoning
fomepizole, ethanol, dialysis
183
antidote for methemoglobin poisoning
methylene blue, vitamin C
184
antidote for tPA, streptokinase, or urokinase
aminocaproic acid
185
dexrazoxane
prevents dilated cardiomyopathy caused by doxorubicin tx
186
drugs that cause hyperglycemia
tacrolimus, protease inhibitors, niacin, HCTZ, corticosteroids
187
drugs that cause hypothyroidism
lithium, amiodarone, sulfonamides
188
drugs that cause hepatic necrosis
halothane, Amanita phalloides (death cap mushroom), valproic acid, acetaminophen
189
drugs that cause pancreatitis
didanosine, corticosteroids, alcohol, valproic acid, azathioprine, diuretics (Drugs Causing A Violent Abdominal Distress)
190
drugs that cause megaloblastic anemia
phenytoin, methotrexate, sulfonamides
191
drugs that cause hyperuricemia
pyrazinamide, thiazides, furosemide, niacin, cyclosporine
192
drugs that cause photosensitivity
sulfonamides, amiodarone, tetracyclines, 5-fluorouracil
193
drugs that cause Stevens-Johnson syndrome
anti-epileptic drugs (esp. lamotrigine, ethosuximide, phenytoin), allopurinol, sulfonamides, penicillin
194
drugs that cause drug-induced SLE
sulfonamides, hydralazine, isoniazid, procainamide, phenytoin, etanercept
195
drugs that induce CYP450 enzymes
chronic alcohol abuse, St. John's wort, phenytoin, phenobarbital, nevirapine, rifampin, griseofulvin, carbamazepine
196
drugs that are CYP450 substrates
anti-epileptics, theophylline, warfarin, OCPs
197
drugs that inhibit CYP450 enzymes
acute alcohol abuse, ritonavir, amiodarone, cimetidine, ketoconazole, sulfonamides, isoniazid, grapefruit juice, quinidine, macrolides, ciprofloxacin
198
first-generation H1 blockers
diphenhydramine, dimenhydrinate, chlorpheniramine, promethazine, hydroxyzine
199
second-generation H1 blockers
fexofenadine, loratadine, desloratadine, cetirizine
200
H2 blockers
cimetidine, ranitidine, famotidine
201
dextromethorphan
class: antitussive
MoA: synthetic codeine analog; NMDA antagonist; mild opioid effect at high doses
uses: cough
side effects: abuse, serotonin syndrome (when combined with other serotonergics); use naloxone for overdose
202
bosentan
class: vasodilator
MoA: endothelin-1 receptor competitive antagonist
uses: pulmonary hypertension
side effects: hepatotoxicity (monitor LFTs)
203
montelukast/zafirlukast
class: anti-inflammatory
MoA: block leukotriene receptors
uses: asthma, including aspirin-induced
204
zileuton
class: anti-inflammatory
MoA: inhibits 5-lipoxygenase/leukotriene synthesis
uses: asthma
side effects: hepatotoxicity
205
omalizumab
class: monoclonal antibody
MoA: binds and inhibits serum IgE, blocks binding to Fc receptors
uses: asthma refractory to steroids and LABAs
206
theophylline
class: bronchodilator
MoA: inhibits phosphodiesterase, increases cAMP concentration; CYP450 substrate; blocks action of adenosine
uses: asthma
side effects: cardiotoxicity, neurotoxicity
207
brimonidine
class: adrenergic agonist
MoA: stimulates a2 receptors, decreases aqueous humor synthesis
uses: open-angle glaucoma
side effects: blurry vision, ocular hyperemia, foreign body sensation, ocular allergic rein, ocular pruritus
208
timolol/betaxolol/carteolol
class: beta blockers
MoA: block beta adrenergic receptors, decrease aqueous humor synthesis
uses: glaucoma
209
latanoprost
class: prostaglandin analog
MoA: stimulates PGF2a receptors; increases outflow of aqueous humor
uses: glaucoma
side effects: darkens color of iris (browning)
210
morphine/fentanyl/codeine/meperidine/pentazocine
class: opioids
MoA: agonists at mu opioid receptors; open K channels and close Ca channels to inhibit synaptic transmission; inhibit release of ACh, NE, 5-HT, glutamate, and substance P
uses: pain, acute pulmonary edema
side effects: addition, respiratory depression, constipation, mitosis, additive CNS depression with other drugs
211
dextromethorphan
class: opioid
MoA: mu opioid receptor agonist, NMDA antagonist
uses: cough suppression
212
loperamide/diphenoxylate
class: opioids
MoA: mu opioid receptor agonists
uses: diarrhea
213
methadone
class: opioids
MoA: mu opioid receptor antagonists
uses: heroin addiction maintenance
214
naloxone/naltrexone
class: opioids
MoA: mu opioid receptor antagonists
uses: opioid overdose, alcoholism
215
buprenorphine
class: opioid
MoA: mu opioid receptor partial agonist
uses: opioid dependence (mixed with naloxone)
216
butorphanol
class: opioid
MoA: k-opioid receptor agonist, mu-opioid receptor partial agonist
uses: pain
side effects: opioid withdrawal (if pt is concurrently taking full opioid agonist); overdose not easily reversed with naloxone
217
tramadol
class: opioid
MoA: weak opioid agonist; inhibits 5-HT and NE reuptake
uses: chronic pain
side effects: decreased seizure threshold, serotonin syndrome, others similar to other opioids
218
ethosuximide
class: anti-seizure
MoA: blocks thalamic T-type Ca channels
uses: absence seizures
side effects: GI upset, fatigue, headache, urticaria, Stevens-Johnson syndrome
219
phenytoin
class: anti-seizure
MoA: promotes Na channel inactivation (use-dependent Na channel blockade); zero-order kinetics at high doses
uses: partial seizures, generalized tonic-clonic seizures, status epilepticus prophylaxis
side effects: nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, peripheral neuropathy, megaloblastic anemia, teratogenic, drug-induced lupus, CYP450 induction, lymphadenopathy, Stevens-Johnson syndrome
220
carbamazepine
class: anti-seizure
MoA: promotes Na channel inactivation
uses: partial seizures, generalized tonic-clonic seizures, trigeminal neuralgia
side effects: diplopia, ataxia, blood dycrasias, liver toxicity, teratogenesis, CYP450 induction, SIADH, Stevens-Johnson syndrome
221
valproic acid
class: anti-seizure
MoA: promotes Na channel inactivation, increases GABA concentration (inhibits GABA transaminase)
uses: all seizures (not status epilepticus), bipolar disorder
side effects: GI upset, hepatotoxicity (monitor LFTs), neural tube defects, tremor, weight gain
222
gabapentin
class: anti-seizure
MoA: inhibits high-voltage-activated Ca channels
uses: partial seizures, peripheral neuropathy, postherpetic neuralgia
side effects: sedation, ataxia
223
phenobarbital
class: barbiturate
MoA: potentiates GABA action
uses: partial seizures, generalized tonic-clonic seizures; 1st-line in neonates
side effects: sedation, tolerance, dependence, CYP450 induction, cardiorespiratory depression
224
topiramate
class: anti-seizure
MoA: blocks Na channels, increases GABA action
uses: partial seizures, generalized tonic-clonic seizures, migraine prevention
side effects: sedation, mental dulling, kidney stones, weight loss
225
lamotrigine
class: anti-seizure
MoA: blocks voltage-gated Na channels
uses: all seizures (except myoclonic or atonic)
side effects: Stevens-Johnson syndrome (titrate dose slowly)
226
levetiracetam
class: anti-seizure
MoA: unknown; may modulate GABA and glutamate release
uses: partial seizures, generalized tonic-clonic seizures
227
tiagabine
class: anti-seizure
MoA: inhibits GABA reuptake
uses: partial seizures
228
vigabatrin
class: anti-seizure
MoA: increases GABA concentration by irreversibly inhibiting GABA transaminase
uses: partial seizures
229
pentobarbital/secobarbital
class: barbiturates
MoA: potentiate GABA action by increasing duration of Cl channel opening
uses: sedative, anxiety, seizures, insomnia
side effects: respiratory and cardiovascular depression, CNS depression (exacerbated by EtOH use), dependence, CYP450 induction
230
alprazolam/triazolam/oxazepam
class: benzodiazepines
MoA: potentiate GABA action by increasing frequency of Cl channel opening; decrease REM sleep; short-acting with no active metabolites
uses: anxiety, spasticity, alcohol detoxification, night terrors, sleepwalking, general anesthesia, insomnia
side effects: dependence (high-risk), additive CNS depression with alcohol
231
diazepam/lorazepam
class: benzodiazepines
MoA: potentiate GABA action by increasing frequency of Cl channel opening; decrease REM sleep; long half-lives and active metabolites
uses: anxiety, spasticity, status epilepticus, alcohol detoxification, night terrors, sleepwalking, general anesthesia, insomnia
side effects: dependence (lower-risk), additive CNS depression with alcohol
232
temazepam/chlordiazepoxide
class: benzodiazepines
MoA: potentiate GABA action by increasing frequency of Cl channel opening; decrease REM sleep; long half-lives and active metabolites
uses: anxiety, spasticity, alcohol detoxification, night terrors, sleepwalking, general anesthesia, insomnia
side effects: dependence (lower-risk), additive CNS depression with alcohol
233
flumazenil
class: benzodiazepine-like
MoA: competitive antagonist at GABA benzodiazepine receptor
uses: benzodiazepine/hypnotic overdose
234
zolpidem/zaleplon/eszopiclone
class: non-benzodiazepine hypnotics
MoA: potentiate GABA action at the benzodiazepine receptor; rapid metabolism by liver enzymes (short-acting)
uses: insomnia
side effects: ataxia, headaches, confusion, modest day-after psychomotor depression/amnesia, risk of depression less than benzodiazepines
235
halothane
class: inhaled anesthetic
effects: myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreased cerebral metabolic demand)
side effects: hepatotoxicity, malignant hyperthermia (antidote: dantrolene)
236
methoxyflurane
class: inhaled anesthetic
effects: myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreased cerebral metabolic demand)
side effects: nephrotoxicity
side effects: hepatotoxicity, malignant hyperthermia (antidote: dantrolene)
237
enflurane
class: inhaled anesthetic
effects: myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreased cerebral metabolic demand)
side effects: proconvulsant, malignant hyperthermia (antidote: dantrolene)
238
nitrous oxide
class: inhaled anesthetic
effects: myocardial depression, respiratory depression, nausea/emesis, increased cerebral blood flow (decreased cerebral metabolic demand)
side effects: expansion of trapped gas in a body cavity
239
thiopental
class: barbiturates
MoA: potentiate GABA action by increasing duration of Cl channel opening; as an anesthetic: high potency, high lipid solubility, rapid entry into brain; rapidly redistributes into skeletal muscle and fat; decreases cerebral blood flow
uses: sedative, anxiety, seizures, insomnia, anesthesia induction
side effects: respiratory and cardiovascular depression, CNS depression (exacerbated by EtOH use), dependence, CYP450 induction
240
midazolam
class: benzodiazepine
MoA: potentiates GABA action by increasing frequency of Cl channel opening; decrease REM sleep; short-acting with no active metabolites
uses: anxiety, spasticity, alcohol detoxification, night terrors, sleepwalking, general anesthesia (most commonly-used drug for endoscopy as adjunct with gases and narcotics), insomnia
side effects: dependence (high-risk), post-operative respiratory depression, hypotension, anterograde amnesia
241
ketamine
class: PCP analog
MoA: blocks NMDA receptor; cardiovascular stimulant, increases cerebral blood flow
uses: IV anesthetic
side effects: disorientation, hallucination, bad dreams
242
propofol
MoA: potentiates GABAa receptors
uses: ICU sedation, rapid anesthesia induction, short procedures
side effects: less postoperative nausea than thiopental
243
procaine/cocaine/tetracaine
class: local anesthetics (esters)
MoA: blocks Na channels on inner portion of channel; preferentially binds activated channels, most effective in rapidly-firing neurons
uses: minor surgical procedures, spinal anesthesia
side effects: CNS excitation, hypertension, hypotension, arrhythmias (cocaine), methemoglobinemia (benzocaine)
244
lidocaine/mepivacaine/bupivacaine
class: local anesthetics (amides)
MoA: blocks Na channels on inner portion of channel; preferentially binds activated channels, most effective in rapidly-firing neurons
uses: minor surgical procedures, spinal anesthesia
side effects: CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, hypotension
245
succinylcholine
class: depolarizing neuromuscular blocker
MoA: selectively stimulates motor nicotinic receptors, causing sustained depolarization
uses: muscle paralysis in surgery or mechanical ventilation
side effects: hypercalcemia, hyperkalemia, malignant hyperthermia
antidote: phase I = none, phase II = cholinesterase inhibitors
246
tubocurarine/atracurium/mivacurium
| pancuronium/vecuronium/rocuronium
class: nondepolarizing neuromuscular blockers
MoA: competitive antagonists at motor nicotinic recepotrs
uses: muscle paralysis in surgery or mechanical ventilation
blockade reversal: neostigmine + atropine, edrophonium, other cholinesterase inhibitors
247
dantrolene
MoA: prevents Ca release from SR of skeletal muscle
uses: malignant hyperthermia, neuroleptic malignant syndrome
248
cyclobenzaprine
class: structurally related to TCAs
MoA: centrally-acting skeletal muscle relaxant
uses: muscle spasms
side effects: anticholinergic
249
carbidopa
MoA: blocks peripheral DOPA decarboxylase-mediated breakdown of L-DOPA and conversion to dopamine (preventing nausea/vomiting)
uses: administered with L-DOPA in Parkinson disease
side effects: arrhythmias
250
entacapone/tolcapone
MoA: inhibit peripheral COMT-mediated breakdown of L-DOPA (tolcapone also crosses BBB)
uses: administered with L-DOPA in Parkinson disease
251
selegiline
MoA: selective MAO-B inhibitor (MAO-B = central isoform that preferentially degrades dopamine over NE and 5-HT)
uses: administered with L-DOPA in Parkinson disease
side effects: may enhance adverse effects of L-DOPA
252
benztropine
class: antimuscarinic
uses: improves tremor and rigidity in Parkinson disease
253
amantadine
MoA: increases dopamine release and decreases dopamine reuptake
uses: Parkinson disease, influenza A, rubella
side effects: ataxia, lived reticularis
254
memantine
MoA: NMDA receptor antagonist; prevents excitotoxicity
uses: Alzheimer's disease
side effects: dizziness, confusion, hallucinations
255
tetrabenazine/reserpine
MoA: inhibit vesicular monoamine transporter (VMAT); limit dopamine vesicle packaging/release
uses: Huntington disease
256
sumatriptan
MoA: 5-HT1B/1D agonist; inhibits trigeminal nerve activation; prevents vasoactive peptide release; induces vasoconstriction
uses: acute migraine (abortive agent), cluster headaches
side effects: coronary vasospasm (contraindicated in CAD/Prinzmetal angina), mild paresthesia
