Special Considerations Flashcards

1
Q

When may dose adjustment be required for thyroid replacement therapy?

A

if T4 used with other drugs- Rifampin ↑ T4 clearance and Cholestyramine ↓ GI absorption

in pregnancy or elderly

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2
Q

Thioamides- PTU and MMI

A

If gland suppressed for 2 yrs → permanent remission in some pts but 60-70% relapse

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3
Q

Best drug for hypothyroidism in 1st trimester preg and recommended for nursing mothers

A

Propylthiouracil

PTU

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4
Q

Best drug for hypothyroidism after 1st trimester preg and recommended for nursing mothers at LOW doses

A

Methimazole

MMI

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5
Q

Radioactive Iodine

I131

A

No evidence of cancer risk increase with tx

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6
Q

Metformin

A

Does NOT induce hypoglycemia
NO weight gain

Often used in combo with oral antidiabetics

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7
Q

Glipizide

A

Won’t work if beta cells aren’t working well

No effect on insulin sensitivity

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8
Q

Repaglinide

A

Shorter acting than SU, administer right before a meal

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9
Q

Pioglitazone

A

NO hypoglycemia risk

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10
Q

Sitagliptin

A

Weight neutral

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11
Q

Canagliflozin

A

May facilitate weight loss, improve CV health in patients with CV dz

Can ↑ serum digoxin concentration

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12
Q

Estrogens

A

Tissue specific effects due to tissue specific receptor expression and dimerization

E2 binds to estrogen receptors (ER-α/ER-β) with greater affinity that E1/E3

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13
Q

Levonorgest

A

safe for breastfeeding

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14
Q

Estrogen/Progestin Combo Pill

A

More consistent suppression as combo

Progestins lower dose of estrogen required

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15
Q

Natural family planning

A

Low effectiveness: about 25% failure rate/yr

Only reliable for women with
consistent 26-32 day cycles

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16
Q

Levonorgestrel

A

95% effective in first 24hrs ,effectiveness ↓ after 72 hrs

Less effective if obese

17
Q

Ulipristal

Ella

A

Maintains very high effectiveness to 120 hr

May not be effective if BMI of ≥ 35

18
Q

Tamoxifen

A

Genotyping CYP2D6 no longer FDA recommended

Resistance possibly due to down- regulation of co- repressors, ER- alpha/beta

Avoid combo of tamoxifen and SSRI’s
SSRI’s will inhibit CYP2D6 conversion of tamoxifen to active metabolites endoxifen and 4-hydroxyTAM

Bone sparing effects in post-menopausal women; may cause osteoporosis in pre- menopausal women

19
Q

Toremifene

A

Resistance – see tamoxifen

Equal efficacy to tamoxifen in treating breast cancer

Bone sparing effects in post-menopausal women

20
Q

Leuprolide

A

Initial administration (first months), prior to GnRH receptor desensitization, can lead to ↑ LH and FSH release, with a transitory ↑ in testosterone and estrogen levels. This may result in an initial worsening of the cancer

21
Q

Aromatase Inhibitors

A

Not effective in pre- menopause since fn ovaries in hypothal-pituitary- gonadal axis overcomes AI effects

After menopause, primary source of low estrogen levels is adipose tissue

22
Q

Trastuzumab

A

HER2 testing: Detection of HER2 protein overexpression required for patient selection

23
Q

Pertuzumab

A

HER2 testing: Detection of HER2 protein overexpression required for patient selection

24
Q

Resistance of alkylating agents

A

↑ DNA repair
capacity of tumor cell

↓ transport
of alkylating agent
into cancer cell

↑ glutathione and glutathione ass proteins

↑ glutathione
S-transferase activity

25
Q

Resistance of Methotrexate

A

↓transport
via down-reg of
reduced folate carrier
protein (MTX transporter)

↓ FPGS activity

Amplification of DHFR

Mutation of DHFR w/ ↓ affinity for MTX

MDR1 expression

26
Q

Resistance of 5-Fluorouracil

A

Amplification of TS

gene

27
Q

Resistance of 6-Mercaptopurine

A

Down-regulation of

HGPRT activity

28
Q

Resistance of Plant Alkaloids

A

↑ MDR1

activity

29
Q

Resistance of Doxorubicin

A

↑ MDR1


glutathione
peroxidase activity

Resistance rendering
mutations of
topoisomerase II

30
Q

Resistance of Bleomycin

A

↑levels of
bleomycin
hydrolase

↑ DNA
repair activity