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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
Q

Fusion inhibitors.

A

Enfuvirtide, Maraviroc

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26
Q

Enfuvirtide

A
  • block confirmational change in gp41

- injection site pain

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27
Q

Maraviroc

A
  • CCR5 antagonist -> inhibit gp120 conformational change

- not used w/ Renal impairment -> end stage renal disease (ESRD)

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28
Q

water soluble vitamins

A

Vit. B

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29
Q

fat soluble vitamins

A

vit. A,D,E,K

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30
Q

vit. B1

A

thiamine

  • BERIBERI and WERNICKE-KORSAKOFF syndrome
  • high risk in alcoholics and malnutrition
  • banana bag
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31
Q

vit. B2

A

riboflavin

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32
Q

vit. B3

A

niacin

  • deficient -> HARTNUP disease, pallagra
  • excess -> facial flushing
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33
Q

vit. B5

A

pantothenic acid

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34
Q

vit. B6

A

pyridoxine

-peripheral neuropathy due to isoniazid

35
Q

vit. B7

A

biotin

36
Q

vit. B9

A

folate

-supplemented to decrease neural tube defects

37
Q

vit. B12

A

cobalamin

-defiiency -> abnormal myelin

38
Q

vit. D

A

-deficient -> rickets, osteomalacia, hypocalcemic tetany

39
Q

vit. K

A
  • required for clotting
  • deficient -> neonatal hemorrhage; due to CEPHALOSPORIN use
  • Warfarin inhibits synthesis
40
Q

vit. A

A

retinol

  • deficient -> Nyctalopia (night blindness)
  • excess -> toxicity from polar bear/beef liver, vit. supplement
41
Q

vit. C

A

ascorbic acid

  • needed for COLLAGEN synthesis
  • deficient -> SCURVY
  • excess -> Ca2+ oxalate stones
42
Q

vit. E

A

tocopherols

  • anti-oxidant
  • can increase effects of warfarin on vit. K
43
Q

St. John’s Wort (Hypericum)

A
  • antidepressant, antiviral, anti carcinogenic
  • many DRUG INTERACTIONS -> CYP450 inducer
  • AE -> photosensitization, mania, arousal
44
Q

volume of distribution (Vd)

A

low Vd -> CENTRAL compartment

high Vd -> PERIPHERAL compartment

45
Q

what is the metabolite of acetaminophen w/ toxic effects?

A

N-acetyl-p-benzoquinone imine (NAPQI)

46
Q

Dimercaprol (BAL) - chelator

A
  • Bidentate chelator

- for ARSENIC and MERCURY poisoning (also LEAD w/ EDTA)

47
Q

Succimer

A
  • H2O soluble
  • binds LEAD, CADMIUM, MERCURY
  • less toxic than dimercaprol
48
Q

Penicillamine

A
  • Bidentate chelator

- for COPPER poisoning and WILSON’S disease

49
Q

Edetate (EDTA)

A
  • Polyadentate chelator -> Ca2+ signaling
  • for LEAD poisoning
  • AE -> NEPHROTOXIC -> renal tubular necrosis
50
Q

Deferoxamine

A
  • Polyadentate chelator

- for Fe toxicity

51
Q

Deferasirox

A
  • Tridentate chelator

- for Fe toxicity

52
Q

both Deferoxamine and Deferasirox

A
  • chelate Fe

- AE -> SKIN RXNS (blushing, urticaria) and NEUROTOXIC (retinal degeneration)

53
Q

Lead

A
  • dust and paint
  • lead ENCEPHALOPATHY (death)
  • treat w/ Succimer or EDTA (if severe)
54
Q

Arsenic

A
  • known carcinogen
  • garlic odor, rice water stools
  • treat w/ Dimercaprol
  • arsine gas -> MASSIVE HEMOLYSIS
55
Q

Mercury

A

acute -> hemorrhagic gastroenteritis…treat w/ Dimercaprol or Succimer

chronic -> treat w/ Succimer and UNITHIOL** (no dimercaprol)

56
Q

Iron

A
  • seen in SMALL CHILDREN

- treat w/ Deferoxamine

57
Q

Organophosphates and Carbamates

A
  • neurotoxic pesticides

- bind to and inhibit AChE**

58
Q

clinical présentation of organophosphates and carbamates

A

-pinpoint pupils, muscle fasciculations, diaphoresis, emesis, diarrhea, salivation, lacrimation, urinary incontinence, garlic odor

59
Q

how do you rescue AChE?

A

2-PAM** -> binds to AChE and removes organophosphate -> reactivates AChE

60
Q

carcinogens vs. mutagens

A
  • mutagens -> DNA mutations
  • carcinogens -> tumor development…affects cell cycle

NOT all carcinogens are mutagens

61
Q

IARC - group 1

A

KNOWN carcinogen

WORSE ones

62
Q

IARC - group 2A

A

PROBABLY carcinogen

63
Q

IARC - group 2B

A

POSSIBLY carcinogen

64
Q

IARC - group 3

A

DATA LACKING to suggest carcinogenic

65
Q

IARC - group 4

A

data says UNLIKELY carcinogenic

66
Q

genotoxic agents

A
  • absorbed -> initiate tumor formation by DNA damage

- INITIATION phase

67
Q

non-genotoxic agents

A
  • increase risk of cancer w/o DNA damage
  • use tumor promoters

-PROMOTION phase

68
Q

teratogens - drugs

A
  • thalidomide

- phenytoin, fosphenytoin, ethotoin (antiepileptics)

69
Q

teratogens - environment

A

fetal alcohol syndrome

70
Q

what does insulin do?

A

-recruit GLUT4 to the membrane -> uptake glucose

71
Q

adverse effects of insulin analogs (lispro, NPH, glargine)

A

hypoglycemia, hypokalemia, Lipodystrophy, Wt. gain

72
Q

Lispro

A

-RAPID acting insulin analog

73
Q

NPH

A

-INTERMEDIATE acting insulin analog

74
Q

Glargine

A
  • LONG acting insulin analog

- “peak less”

75
Q

the main side effects w/ non-insulin drugs

A
  1. hypoglycemia
  2. GI probs
  3. weight gain
  4. nausea
  5. pancreatitis
76
Q

Metformin

A

-decrease hepatic glucose production, decrease intestinal glucose absorption, improve insulin sensitivity

  • 1st line for type 2 diabetes
  • AE: DIARRHEA, NAUSEA, LACTIC ACIDOSIS
77
Q

Glyburide

A
  • stimulate insulin release from beta cells by blocking K+ channels, decrease hepatic gluconeogenesis, increase insulin sensitivity
  • AE: life threatening HYPOGLYCEMIA, WEIGHT GAIN
78
Q

Repaglinide

A
  • same MOA as glyburide
  • GLUCOSE-DEPENDENT
  • for post-prandial peaks in blood glucose levels**
79
Q

Exenatide

A
  • analog of incretin

- not used w/ GI motility disorders or pancreatic tumors**

80
Q

Sitagliptin

A
  • inhibit DPP-4 -> increase insulin secretion, decrease glucagon secretion, decrease hepatic gluconeogenesis
  • AE: PANCREATITIS
81
Q

Pioglitazone

A

-activate PPARy

-not used w/ CHF***
AE: FLUID RETENTION/EDEMA, wt gain, OSTEOPOROSIS

82
Q

Canagliflozin

A
  • SGLT-2 inhibitor -> reduce renal absorption of glucose
  • increase URINATION (diuretic)

-AE: female genital mycotic infections (Candida), UTI, urinary frequency

83
Q

Acarbose

A

-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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