FA pharma Flashcards
(161 cards)
1
Q
MOA of polyenes
A
Formation of artificial pores in the ergosterol membranes disrupts membrane permeability
2
Q
Uses of amphotericin B
A
Severe infections by Aspergillus, Candida, Cryptococcus, Histoplasma, Mucor, Sporothrix
3
Q
Uses of nystatin
A
Topical localized infections; too toxic for systemic use
4
Q
Pharmacokinetics of amphotericin B
A
Given by slow IV infusion, does not enter CNS, slow t1/2 > 2 weeks, hepatic metabolism and renal elimination
5
Q
Side effects of amphotericin B
A
Infusion-related: fever chills, muscle rigor, hypotension alleviated by NSAIDs, antihistamines, meperidine, steroids. Dose-dependant: nephrotoxicity, decreased GFR, tubular acidosis, anemia
6
Q
Azole drugs
A
Ketoconazole, fluconazole, itraconazole, clotrimazole
7
Q
MOA of azoles
A
Fungicidal by inhibiting 14-alpha-demethylase which converts lanosterol to ergosterol
8
Q
Uses of ketoconazole
A
DOC for Paracoccidioides; backup for Blastomyces, Histoplasma; Oral use in mucocutaneous candidiasis or dermatophytoses
9
Q
Uses of fluconazole
A
DOC for esophageal and invasive candidiasis and coccidioidomycoses. Prophylaxis and suppression of cryptococcal meningitis
10
Q
Uses of itraconazole
A
DOC in blastomycoses and sporotrichoses
11
Q
Uses of clotrimazole
A
Used topically for candidal and dermatophytic infections
12
Q
Pharmacokinetics of ketoconazole
A
Orally effective; absorption decreased by antacids; metabolized by liver enzymes; inhibits P450
13
Q
Pharmacokinetics of itraconazole
A
Orally effective; absorption increased by food; metabolized by liver enzymes; inhibits P450
14
Q
Pharmacokinetics of fluconazole
A
Orally effective; enters CSF; eliminated in the urine in unchanged form
15
Q
Side effects of azoles
A
Decreased synthesis of cortisol and testosterone –> decreased libido, gynecomastia, menstrual irregularities; Increased liver function tests and rare hepatotoxicity
16
Q
Drugs that block viral penetration and uncoating
A
Amantadine, enfurvitide
17
Q
Drugs that inhibit viral DNA polymerases
A
Acyclovir, foscarnet, ganciclovir
18
Q
Drugs that inhibit viral RNA polymerases
A
Foscarnet, ribavirin
19
Q
Drugs that inhibit viral reverse transcriptase
A
Zidovudine, didanosine, zalcitabine, lamivudine, stavudine, nevirapine, delavirdine, efavirenz
20
Q
Drugs that inhibt viral aspartate protease
A
Indinavir, ritonavir, saquinavir, nelfinavir
21
Q
Drugs that inhibit viral neuraminidase
A
Zanamivir, oseltamivir
22
Q
Drugs used to treat herpes
A
Acyclovir, ganciclovir, foscarnet
23
Q
Acyclovir
A
Activated by viral thymidine kinase, inhibitor and chain terminator of DNA polymerase. Use for HSV ans VZV. Side effects: crystalluria, neurotoxicity
24
Q
Ganciclovir
A
Activated by viral thymidine kinase, inhibitor and chain terminator of DNA polymerase. Use for HSV, VZV, CMV, AIDS retinitis and transplant patients. Side effects: hematotoxicity, crystalluria, rash
25
Foscarnet
Inhibits viral DNA and RNA polymerases. Use for HSV, VZV, CMV, AIDS retinitis, transplant patients. Side effects: nephrotoxic acute tubular necrosis, hypocalcemia (tremors, seizures)
26
Zidovudine (ZDV, AZT)
Converted to triphosphate that inhibits reverse transcriptase and causes chain termination. Resistance by mutations of RT gene.
27
Drug interaction of zidovudine (ZDV, AZT)
Increase levels of ZDV: azoles, cimetidine, indomethacin, probenecid, TMP-SMX. Decrease levels of ZDV: rifampin
28
Side effects of ZDV
Neutropenia, anemia, granulocytopenia, headache, myalgias, neuropathy, lactic acidosis
29
MOA enfuvirtide
Binds gp41 and inhibits fusion of HIV-1 to CD4 cells
30
Needle stick HIV prophylaxis
ZDV + 3TC + indinavir
31
Pregnancy HIV prophylaxis
ZDV trimester 2 and 3 plus 6 weeks to neonate reduces vertical transmission by 80%. Or ZDV intrapartum reduces transmission by 50-60%
32
Amantadine
Blocks attachment, penetration and uncoating of Influenza A. May decrease flu symptoms. Side effects: nervousness, insomnia, atropine-like effects
33
Uses of interferons
Antiviral: HBV, HCV; antiumor: Kaposi, CML, multiple myeloma, renal CA; Immunoregulatory: mutiple sclerosis
34
Effects of H1 receptor activation
Increased capillary dilation and permeability (hypotension, edema), bronchoconstriction, activation of nociceptive receptors (pain, pruritus)
35
Effects of H2 receptor activation
Increased gastric acid secretion (ulcers), positive inotropism
36
H1 antagonist drugs
Diphenhydramine, promethazine, chlorpheniramine, meclizine, hydroxyzine, loratadine, fexofenadine
37
Uses of H1 antagonists
Hay fever, rhinitis, urticaria, motion sickness and vertigo (meclizine), nausea in pregnancy
38
Adverse effects of H1 antagonists
M block and sedation, GI distress, allergic reactions.
39
Substances that increase proton pump activity
ACh, gastrin, histamine (H2 receptors)
40
H2 antagonist drugs
Cimetidine, ranitidine
41
MOA of H2 antagonists
Indirectly decrease proton pump activity (histamine increases proton pump activity)
42
Uses of H2 antagonists
Peptic ulcer disease, GERD, Zollinger-Ellison
43
Side effects of H2 antagonists
GI distress, dizziness, sommnolence; Cimetidine: inhibits P450 --> increases effects of quinidie, phenytoin, TCAs, warfarin; also decreases androgens --> gynecomastia
44
Omeprazole
Direct, irreversible proton pump inhibitor. Uses: PUD, GERD, Zollinger-Ellison, H. pylori. Side effects: decreases bioavailability of weak acids (fluoroquinolones, ketoconazole), inhibits P450
45
Misoprostol
PGE1 analog, increases mucus and bicarbonate, decreases HCL secretion. Use: NSAID-induced ulcers.
46
Sulcralfate
Polymerizes in stomach to coat ulcers. Increases healing and decreases ulcer recurrence.
47
Drugs that require acid stomach pH to be absorbed
Azoles, fluoroquinolones, warfarin
48
Drugs used as antiemetics
5HT3 antagonists (ondansetron), DA antagonists (metoclopramide), H1 blockers (diphenhydramine, meclizine), muscarinic blockers (scopolamine)
49
Metabolism of serotonin
5HT is metabolized by MAOa to 5-hydroxyinolacetic acid (marker for carcinoid)
50
Buspirone
Partial 5HT1a agonist used for generalized anxiety disorder
51
Sumatriptan
5HT1d agonist in cerebral vessels, used for migraine
52
Olanzapine
Atypical antipsychotic, 5HT2A and D2 receptor antagonist, decreases psychosis. Side effects: weight gain, tardive diskinesia, metabolic syndrome
53
Cyproheptadine
5HT2 antagonist used in carcinoid
54
Ondansetron
5HT3 antagonist, used as antiemetic in chemotherapy, radiation and post-op. 5HT3 receptors are found in area postrema
55
Ergonovine
Uterine muscle contraction after placental delivery
56
Ergotamine
Partial 5HT2 and alpha agonist causes vasoconstriction to decrease pulsation in migraine acute attack. Side effect is vasoconstriction (prinzmetal)
57
Prophylaxis of migraine headaches
Propranolol, verapamil, amitriptyline, valproic acid
58
PGE2
Vasodilation in kidneys, increases renal blood flow, increases gastric mucosal blood flow (mucoprotection), activates osteoclasts, fever, pain, maintains ductus arteriosus
59
Prostacyclin (PGI2)
Vasodilation and inhibits platelet aggregation
60
COX1
Constitutive enzyme synthesizes GI PGs and TxA2
61
COX2
Inducible enzyme synthesizes PGs involved in inflammation, fever and pain.
62
Zileuton
Lipoxygenase inhibtor used in asthma
63
Zafirlukast and -lukasts
Leukotriene receptor antagonist used in asthma
64
MOA of aspirin
Nonselective, irreversible COX inhibitor via acetylation of serine near active site
65
Actions of aspirin
Low dose: antiplatelet aggregation (post-MI); moderate dose: analgesia, antipiresis, hyperuricemia; High dose: antiinflammatory, uricosuria
66
Effects of aspirin on acid-base and electrolytes
Antiinflammatory doses: uncoupling of ETC --> increases respiration --> decreased pCO2 --> resp. alkalosis --> renal compensation via HCO3 excretion --> compensated respiratory alkalosis. Toxic doses: inhibits respiratory center --> decreases respiration --> resp. acidosis plus ETC uncoupling --> metabolic acidosis, decreases ATP, hyperthermia, hypokalemia
67
Side effects of aspirin
Gastritis, ulcers, bleeding, tinnitus, vertigo, decreased hearing, bronchoconstriction, hypersensitivity (asthma, nasal polyps, rhinitis), Reye syndrome, increased bleeding time, renal dysfunction at high doses
68
Aspirin overdose management
Gastric lavage, alkalinization of urine (zero-order kinetics at toxic doses)
69
Celecoxib
Selective COX-2 inhibitor. Antiinflammatory. Increases PT when used with warfarin, prothrombotic. Cross hypersensitivity with sulfonamides. Potential cardiotoxicity resulted in withdrawal of rofecoxib.
70
Acetaminophen
Inhibits COX in CNS only. No antiplatelet activity, not implicated in Reye syndrome, no effects on uric acid, no bronchoconstriction. Metabolized via P450. Hepatotoxic due to reactive metabolite N-acetylbenzoquinonemine, which is inactivated by GSH. Upon GSH depletion, metabolite damages hepatocytes, nausea, vomiting, abdominal pain, centrilobular necrosis. Inducers of P450 enhance toxicity. Management of hepatotoxicity: N-acetylcysteine.
71
Hydroxychloroquine
Used for rheumatoid arthritis. Stabilizes lysosomes and decreases chemotaxis. Side effects: GI distress, visual dysfunction, hemolysis in G6PDH deficiency
72
Methotrexate
Used for rheumatoid arthritis. Cytotoxic to lymphocytes. Side effects: hematotoxicity, mucositis, crystalluria
73
Sulfasalazine
Used for rheumatoid arthritis. Decreases B cell function, possibly inhibits COX. Side effects: GI distress, rash, hemolysis in G6PDH deficiency, drug-induced lupus
74
Glucocorticoids
Used in rheumatoid arthritis. Decrease LTs and platelet activating factor (PAF). Side effects: ACTH suppression, Cushingoid state, osteoporosis, GI distress, glaucoma
75
Gold salts
Used in rheumatoid arthritis. Decreases lysosomal and macrophage functions. Side effects: dermatitis, hematotoxicity, nephrotoxicity
76
Penicillamine
Used in rheumatoid arthritis. Suppresses T cells and circulating rheumatoid factor. Side effects: proteinuria, hematotoxicity, autoimmune disease.
77
Etanercept
Used in rheumatoid arthritis. Binds TNF. Side effects: hypersensitivity, injection site reactions, infections
78
Infliximab
Used in rheumatoid arthritis. Monoclonal antibody to TNF. Side effects: infusion reactions, infections
79
Anakinra
Used in rheumatoid arthritis. IL-1 receptor antagonist. Side effects: infections, injection site reactions
80
Colchicine
Used in acute gout. Binds tubulin --> decreases microtubular polymerization ; decreases LTB4 and leukocyte/granulocyte migration. Side effects: diarrhea, GI pain, hematuria, myelosuppression, neuropathy
81
Allopurinol
Prodrug converted by xanthine osidase into alloxanthine which inhibits the enzyme --> decreases purine metabolism --> decreases uric acid. Side effects: GI distress, neuropathy, rash, vasculitis, stones.
82
Probenecid
Inhibits tubular reabsorption of urate. Interactions: inhibits secretion of acidic drugs (cephalosporins, fluoroquinolones). Side effects: GI distress, rash, nephrotic syndrome, crystallization
83
Glucocorticoid drugs
Cortisol, prednisone, triamcinolone, betamethasone, dexamethasone
84
MOA of glucocorticoids
Inhibits leukocyte migration, phagocytosis and capillary permeability, decreases PGs, LTs, expression of COX2, PAF and interleukins
85
Uses of glucocorticoids
Antiinflammatory and immunosuppressive
86
Side effects of glucocorticoids
Suppression of ACTH --> cortical atrophy, shock if abruptly withdrawn, cushingoid syndrome, hyperglycemia (increased gluconeogenesis), osteoporosis with vertebral fractures, gastric acid secretion (ulcers), Na+ and H2O retention with edema and hypertension, hypokalemic alkalosis, hypocalcemia, inhibits bone growth in children, decreases wound healing (infections), increased sorbitol (glaucoma, cataracts), mental dysfunction.
87
Role of beta agonists in asthma
Slective ?2 agonists: Relief of acute bronchoconstriction (albuterol, metaproterenol, terbutaline) and prophylaxis of nightime attacks (salmeterol). Side effects include anxiety, tremors and CV toxicity
88
Ipratropium
Muscarinic blocker causes bronchodilation in acute asthma. Safer than ?1 agonists in patients with cardiovascular disease. DOC in bronchospasm induced by ?-blockers.
89
Theophylline
Inhibits phosphodiesterase --> increases cAMP --> bronchodilation. Also antagonizes adenosine (bronchoconstrictor). Narrow therapeutic index. Side effects: nausea, diarrhea, increases HR, arrhythmias. Increased toxicity with erythromycin, cimetidine and fluoroquinolones.
90
Role of glucocorticoids in asthma
Decreases reactivity by decreasing PGs, LTs and Ils; May cause oropharyngeal candidiasis and retarded bone growth with chronic use; low doses prevent desensitization of ? receptors.
91
Zafirlukast, mentelukast
LTD4 antagonists with slow onset. Used prophylactically for antigen, exercise or drug-induced asthma.
92
Zileuton
Selective inhibitor of lypoxygenases --> decreased ILs. Rapid onset, adjunct to steroids.
93
first generation sulfonylureas
tolbutamide, chlorpropamide; block K+ channels of ? cells --> depolarization --> ?Ca+ --> release of insulin
94
second generation sulfonylureas
glipizide, glyburide, glimepiride; block K+ channels of ? cells --> depolarization --> ?Ca+ --> release of insulin
95
side effects of sulfonylureas
hypoglycemia, weight gain, sulfa allergy, hypoglycemia with cimetidine (fisrt generation), disulfram-like (first generation)
96
hypoglycemia
paresthesia, lethargy, confusion, sweats, tremors, tachychardia, coma, seizures
97
metformin
? gluconeogenesis; can be used in patients with no islet function; side effect: lactic acidosis
98
glitazones
? target cell sensitivity to glucose via PPARs; side effects: weight gain, edema, hepatotoxicity, CV toxicity
99
?-glucosidase inhibitors
acarbose, miglitol; no hypoglycemia; inhibit brush border ?-glucosidase; side effects: GI disturbance
100
xenatide
GLP-1 receptor full agonist --> augments insulin secretion; hypoglycemia when used with sulfonylureas
101
orlistat
inhibits pancreatic lipases; used in obesity; side effects: steatorrhea, fat malabsorption
102
sibutramine
serotonin/norepinephrine reuptake inhibitor; obesity management; side effects: tachychardia
103
propylthiouracil/methimazole
inhibits organification and coupling; side effects: agranulocytosis, aplastic anemia, skin rash
104
anastrozole
aromatase inhibitor --> ? estrogen synthesis; use: estrogen-dependant postmenopausal breast cancer
105
clomiphene
? feedback inhibition --> ?FHS/LH --> ?ovulation; fertility drugs; adverse effects: multiple births
106
tamoxifen/raloxifene
estrogen receptor agonist in bone; estrogen receptor antagonist in breast; partial agonist in endometrium
107
progestins/estrogens/oral contraceptives
medroxyprogesterone, norethindrone, desogestrel, estrogens; ?progesterone --> ?LH/FSH; side effects: ?LDL ?HDL, glucose intolerance, androgenic, antiestrogenic
108
mifepristone
progesterone antagonist --> abortifacient
109
methyltestosterone
ilicit in athletics, used in male hypogonadism; side effects: premature closure of epiphysis, jaundice, aggression
110
flutamide
androgen receptor blocker; used in prostate cancer
111
leuprolide
GnRH analog; prostate cancer
112
finasteride
5-?-reductase inhibitor --> ?dihydrotestosterone; BPH, baldness; teratogenic
113
biphosphonates
use in Paget, osteoporosis; alendronate, etidronate, pamidronate
114
energy source of RBC
anaerobic glycolysis --> lactate (90%) and HMP shunt (10%)
115
antithrombin III
activated by heparin; inactivates thrombin, IXa, Xa, XIa
116
tPA
tissue plasminogen activator; fibrinolytic; generates plasmin from plasminogen; ?PT and ?PTT
117
protein C
inactivates factors Va and VIIIa --> anticoagulation
118
factor V leiden
mutation causes resistance to activated protein C --> hypercoagulable state
119
warm agglutinin
IgG; AIHA seen in SLE, CLL and methyldopa; Warm weather is GGGreat, Cold ice cream MMM""
120
cold agglutinin
IgM; AIHA seen in mycoplasma or infectious mononucleosis infections; Warm weather is GGGreat, Cold ice cream MMM""
121
heparin
activates antithrombin III; measure PTT; use: PE, DVT, AMI, DIC; side effects: bleeding, heparin-induced thrombocytopenia, hypersensitivity
122
protamine sulfate
rapid reversal of heparinization; binds negatively-charged heparin
123
antithrombin III
serine protease inhibitor binds to activated clotting factors (IXa, Xa, XIa) to inactivate them
124
warfarin antidote
vitamin K
125
warfarin
epoxide reductase inhibitor decreases vitamin K-dependant factors; slow onset; check PT; SE: skin necrosis; metabolized by P450
126
warfarin-induced skin necrosis
protein C and VIIa have the shortest half-lives --> transient inactivation of protein C and extrinsic pathway while intrinsic path is still active and unopposed due to longer half-lives of factors --> hypercoagulable state --> thrombosis
127
platelet activators
TxA2, ADP, 5HT --> ?expression of GpIIb/IIIa receptors
128
platelet deactivators
prostacyclin, cAMP, clopidogrel, gpIIb/IIIa blockers (abciximab)
129
clopidogrel
blocks platelet ADP receptors --> ?platelet activation; SE neutropenia
130
abciximab
gpIIb/IIIa antagonist --> ?platelet aggregation
131
methotrexate
inhibits dihydrofolate reductase --> ?dTMP --> ?DNA synthesis; uses: leukemias, lymphomas, abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis
132
5-FU MOA
inhibits thymidylate synthase --> ?dTMP --> ?DNA synthesis; uses: colon cancer and solid tumors, basal cell carcinoma
133
6-MP
activated by HGPRTase --> blocks purine synthesis; uses: leukemias, lymphomas (except CLL or Hodgkin); metabolized by xanthine oxidase (?toxicity with allopurinol); hepatotoxic
134
cytarabine (ara-C)
DNA polymerase inhibitor; use: AML
135
cyclophosphamide
alkylating agent ---> attacks guanine N7 --> denatures DNA; uses: non-Hodgkin lymphoma, ovarian and breast cancer, neuroblastoma
136
cisplatin
alkylating agent cross-links DNA strands; uses testicular, bladder, ovary and lung carcinomas; nephrotoxic
137
doxorubicin
intercalates DNA inhibits topoisomerase II; uses: Hodgkin's, myelomas, solid tumors; dilated cardiomyopathy
138
actinomycin D (dactinomycin)
intercalates DNA inhibits topoisomerase; uses: Wilm's tumor, Ewing's sarcoma. Rhabdomyosarcoma
139
bleomycin
formation of free radicals cause breaks in DNA strands; uses: testicular cancer, lymphomas; pulmonary fibrosis is side effect
140
hydroxyurea
inhibits ribonucleotidde reductase --> decreases DNA synthesis; uses: melanoma, CML, sickle cell disease
141
tamoxifen
estrogen receptor antagonist in breast, agonist in bone; use: breast cancer
142
vincristine
bind tubulin during M phase blocking polymerization of microtubules and formation of mitotic spindle; uses: lymphoma, Wilm's tumor, choriocarcinoma; neurotoxic
143
cyclosporine
binds cyclophillin --> ?calcineurin --> ?IL-2, IL-3, IFN-gamma; use in organ transplants
144
tacrolimus
inhibits calcineurin --> ?IL-2, IL-3, IFN-gamma; use in organ transplants
145
infliximab
monoclonal Ig against TNF; use in rheumatoid arthritis and Crohn's
146
trastuzumab
erb-B2 antagonist; use in breast cancer
147
dacliximab
blocks IL-2 receptors; use in kidney transplants
148
etanercept
Recombinant TNF receptor binds TNF; uses: rheumatoid arthritis, psoriasis, ankylosing spondylitis
149
first generation H1 blockers
reversible; diphenhydramine, chlorpheniramine; uses: allergy, motion sickness, sleep aid; SE: sedation, antimuscarinic and anti-alpha adrenergic effect
150
2nd generation H1 blockers
loratadine, fexofenadine, desloratadine, cetirizine; use: allergy; less sedation
151
salmeterol
beta2 agonist; long-acting; tremor and arrhythmias
152
albuterol
beta2 agonist; use in acute asthma attack
153
theophylline
inhibits phosphodiesterase and increases cAMP --> bronchodilation; cardiotoxic, neurotoxic, narrow therapeutic index; metabolized by P450
154
ipratropium
antimuscarinic used in asthma and COPD
155
cromolyn
stabilizes mast cell membrane; not effective in acute asthma attack just prophylaxis
156
zileuton
5-lipoxygenase inhibitor --> decreases leukotrienes
157
lukasts
leukotriene receptor antagonists; aspirin-induced asthma
158
guainfenesin
expectorant; doesnt suppress cough reflex
159
colchicine
use in acute gout; depolymerizes tubulin microtubules, prevents leukocyte chemotaxis and degranulation; SE: GI disturbances
160
probenecid
use in chronic gout; inhibits reabsorption of uric acid in PCT
161
allopurinol
use in chronic gout and leukemia; inhibits xanthine oxidase and decreases uric acid
