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OMS II - Becom Exam 4 > Lee's Lectures > Flashcards

Lee's Lectures Flashcards

1
Q

which drugs are known as boosters?

A

Ritonavir and Cobacistat

-inhibit CYP3A4 increasing [] of other drugs

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2
Q

NRTIs

A

-Tenofovir, Abacavir, Emtricitabine, Lamivudine, Didanosine, Stavudine, Zidovudine

  • COMPETITIVE inhibition of reverse transcriptase
  • need phosphorylation to become active
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3
Q

which 2 NRTIs have mitochondrial toxicities?

A

Didanosine and Stavudine

-both are also contraindicated in pregnancy

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4
Q

side effects of NRTIs

A
  • hepato-steatosis (fatty liver)
  • lactic acidosis
  • lipodystrophy
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5
Q

Tenofovir

A
  • thymidine NUCLEOTIDE
  • NO phosphorylation needed
  • NEPHROTOXIC (not used w/ GFR <60) and BONE LOSS
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6
Q

what do drugs can treat HIV-1 and chronic hepB?

A

Tenofovir and Lamivudine

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7
Q

Abacavir

A
  • HLA:B5701 allele -> HYPERSENSITIVITY

- Hyperlipidemia -> risk of CAD

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8
Q

Emtricitabine

A

-HYPERPIGMENTATION (palms/soles)

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9
Q

Lamivudine

A

-GI side effects

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10
Q

Didanosine

A
  • Mitochondrial toxicity
  • fatal PANCREATITIS
  • Peripheral Neuropathy
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11
Q

Stavudine

A
  • Mitochondrial toxicity

- also peripheral neuropathy and less severe pancreatitis

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12
Q

NNRTIs

A

-Efavirenz, Etravirine, Delavirdine, Nevirapine

  • highly selective, NON-COMPETITIVE (allosteric) binding to reverse transcriptase
  • NOT need phoshphorylation to be active
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13
Q

Efavirinz

A
  • not used w/ hypersensitivity (SJS, erythema multiforme)
  • strong CYP3A4 inhibition
  • Neural tube defects in pregnancy
  • VIVID DREAMS
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14
Q

Etravirine

A

-active against HIV strains that are resistant to 1st gen NNRTIs

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15
Q

Nevirapine

A
  • not used w/ HEPATIC impairment (child-Pugh) -> increase cholesterol and ALT
  • not used w/ postexposure prophylaxis (PEP)
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16
Q

protease inhibitors

A
  • Atazanavir, Darunavir, Lopinavir, Ritonavir
  • REVERSIBLE inhibitors of HIV aspartyl protease
  • CYP3A4, 2C9 inhibition -> interact w/ many drugs
  • NOT used w/ Rifampin
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17
Q

adverse effects of protease inhibitors

A
  • parasthesias
  • hyperglycemia (diabetes)
  • hypertriglyceridemia, hypercholesterolemia
  • BUFFALO HUMP
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18
Q

Atazanavir

A

-UNBOOSTED

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19
Q

Darunavir

A
  • for HIV-1 and HIV-2

- must be administered w/ Ritonavir

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20
Q

which 2 PIs do you not want to use w/ hypersensitivities like SJS and erythema multiforme?

A

Atazanavir and Lopinavir

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21
Q

Ritonavir***

A

-BOOSTER of PIs -> increase drug []

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22
Q

integrase inhibitors

A

Raltegravir, Dolutagravir

-both inhibit integrase

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23
Q

Raltegravir

A
  • prevent integration of prevail gene into host DNA

- well tolerated

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24
Q

Dolutagravir

A

-binds to integrase active site and inhibits strand transfer step of HIV-1 DNA integration needed for HIV replication cycle

  • QT PROLONGATION (torsades)
  • neural tube defects if pregnant
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25
Fusion inhibitors.
Enfuvirtide, Maraviroc
26
Enfuvirtide
- block confirmational change in gp41 | - injection site pain
27
Maraviroc
- CCR5 antagonist -> inhibit gp120 conformational change | - not used w/ Renal impairment -> end stage renal disease (ESRD)
28
water soluble vitamins
Vit. B
29
fat soluble vitamins
vit. A,D,E,K
30
vit. B1
thiamine - BERIBERI and WERNICKE-KORSAKOFF syndrome - high risk in alcoholics and malnutrition - banana bag
31
vit. B2
riboflavin
32
vit. B3
niacin - deficient -> HARTNUP disease, pallagra - excess -> facial flushing
33
vit. B5
pantothenic acid
34
vit. B6
pyridoxine | -peripheral neuropathy due to isoniazid
35
vit. B7
biotin
36
vit. B9
folate | -supplemented to decrease neural tube defects
37
vit. B12
cobalamin | -defiiency -> abnormal myelin
38
vit. D
-deficient -> rickets, osteomalacia, hypocalcemic tetany
39
vit. K
- required for clotting - deficient -> neonatal hemorrhage; due to CEPHALOSPORIN use - Warfarin inhibits synthesis
40
vit. A
retinol - deficient -> Nyctalopia (night blindness) - excess -> toxicity from polar bear/beef liver, vit. supplement
41
vit. C
ascorbic acid - needed for COLLAGEN synthesis - deficient -> SCURVY - excess -> Ca2+ oxalate stones
42
vit. E
tocopherols - anti-oxidant - can increase effects of warfarin on vit. K
43
St. John's Wort (Hypericum)
- antidepressant, antiviral, anti carcinogenic - many DRUG INTERACTIONS -> CYP450 inducer - AE -> photosensitization, mania, arousal
44
volume of distribution (Vd)
low Vd -> CENTRAL compartment | high Vd -> PERIPHERAL compartment
45
what is the metabolite of acetaminophen w/ toxic effects?
N-acetyl-p-benzoquinone imine (NAPQI)
46
Dimercaprol (BAL) - chelator
- Bidentate chelator | - for ARSENIC and MERCURY poisoning (also LEAD w/ EDTA)
47
Succimer
- H2O soluble - binds LEAD, CADMIUM, MERCURY - less toxic than dimercaprol
48
Penicillamine
- Bidentate chelator | - for COPPER poisoning and WILSON'S disease
49
Edetate (EDTA)
- Polyadentate chelator -> Ca2+ signaling - for LEAD poisoning - AE -> NEPHROTOXIC -> renal tubular necrosis
50
Deferoxamine
- Polyadentate chelator | - for Fe toxicity
51
Deferasirox
- Tridentate chelator | - for Fe toxicity
52
both Deferoxamine and Deferasirox
- chelate Fe | - AE -> SKIN RXNS (blushing, urticaria) and NEUROTOXIC (retinal degeneration)
53
Lead
- dust and paint - lead ENCEPHALOPATHY (death) - treat w/ Succimer or EDTA (if severe)
54
Arsenic
- known carcinogen - garlic odor, rice water stools - treat w/ Dimercaprol - arsine gas -> MASSIVE HEMOLYSIS
55
Mercury
acute -> hemorrhagic gastroenteritis...treat w/ Dimercaprol or Succimer chronic -> treat w/ Succimer and UNITHIOL** (no dimercaprol)
56
Iron
- seen in SMALL CHILDREN | - treat w/ Deferoxamine
57
Organophosphates and Carbamates
- neurotoxic pesticides | - bind to and inhibit AChE**
58
clinical présentation of organophosphates and carbamates
-pinpoint pupils, muscle fasciculations, diaphoresis, emesis, diarrhea, salivation, lacrimation, urinary incontinence, garlic odor
59
how do you rescue AChE?
2-PAM** -> binds to AChE and removes organophosphate -> reactivates AChE
60
carcinogens vs. mutagens
- mutagens -> DNA mutations - carcinogens -> tumor development...affects cell cycle NOT all carcinogens are mutagens
61
IARC - group 1
KNOWN carcinogen WORSE ones
62
IARC - group 2A
PROBABLY carcinogen
63
IARC - group 2B
POSSIBLY carcinogen
64
IARC - group 3
DATA LACKING to suggest carcinogenic
65
IARC - group 4
data says UNLIKELY carcinogenic
66
genotoxic agents
- absorbed -> initiate tumor formation by DNA damage | - INITIATION phase
67
non-genotoxic agents
- increase risk of cancer w/o DNA damage - use tumor promoters -PROMOTION phase
68
teratogens - drugs
- thalidomide | - phenytoin, fosphenytoin, ethotoin (antiepileptics)
69
teratogens - environment
fetal alcohol syndrome
70
what does insulin do?
-recruit GLUT4 to the membrane -> uptake glucose
71
adverse effects of insulin analogs (lispro, NPH, glargine)
hypoglycemia, hypokalemia, Lipodystrophy, Wt. gain
72
Lispro
-RAPID acting insulin analog
73
NPH
-INTERMEDIATE acting insulin analog
74
Glargine
- LONG acting insulin analog | - "peak less"
75
the main side effects w/ non-insulin drugs
1. hypoglycemia 2. GI probs 3. weight gain 4. nausea 5. pancreatitis
76
Metformin
-decrease hepatic glucose production, decrease intestinal glucose absorption, improve insulin sensitivity - 1st line for type 2 diabetes - AE: DIARRHEA, NAUSEA, LACTIC ACIDOSIS
77
Glyburide
- stimulate insulin release from beta cells by blocking K+ channels, decrease hepatic gluconeogenesis, increase insulin sensitivity - AE: life threatening HYPOGLYCEMIA, WEIGHT GAIN
78
Repaglinide
- same MOA as glyburide - GLUCOSE-DEPENDENT - for post-prandial peaks in blood glucose levels**
79
Exenatide
- analog of incretin | - not used w/ GI motility disorders or pancreatic tumors**
80
Sitagliptin
- inhibit DPP-4 -> increase insulin secretion, decrease glucagon secretion, decrease hepatic gluconeogenesis - AE: PANCREATITIS
81
Pioglitazone
-activate PPARy -not used w/ CHF*** AE: FLUID RETENTION/EDEMA, wt gain, OSTEOPOROSIS
82
Canagliflozin
- SGLT-2 inhibitor -> reduce renal absorption of glucose - increase URINATION (diuretic) -AE: female genital mycotic infections (Candida), UTI, urinary frequency
83
Acarbose
-inhibit alpha-amylase and alpha-glucosidase - not used w/ GI disorders** - AE: FLATULENCE, DIARRHEA

OMS II - Becom Exam 4 (8 decks)

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