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Pharmacology > mid term - questions > Flashcards

mid term - questions Flashcards

1
Q

write the contraindication of Progesterone?

A
  • Breast cancer
  • Pregnancy
  • Uterine bleeding
  • Liver diseases
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2
Q

Adverse effects of progestins?

A
  • acne
  • weight gain
  • masculinization
  • Lipid profile worsens (↓HDL, ↑LDL)
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3
Q

Clinical uses of progestins?

A
  • Contraception
  • Hormone replacement therapy
  • Treatment of infertility
  • Reduce the risk of recurrent spontaneous preterm birth (off-label)
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4
Q

Contraindications of estrogens?

A
  • Estrogen-dependent neoplasms
  • Breast cancer
  • Liver disease
  • Heavy smokers
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5
Q

Therapeutic uses of estrogens?

A
  • Contraception
  • Hormone replacement therapy
  • Primary hypogonadism
  • Hyperandrogenism
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6
Q

effects of estrogens?

A
  • Growth and sexual maturation of female
  • Decrease bone resorption
  • Enhance coagulability of blood
  • Improved lipid profiles
  • Edema
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7
Q

why Oxytocin is not administered orally?

A

Ph sensitive and polypeptide so it will degrade in stomach

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8
Q

side effects of oxytocin

A
  • Tachysystole
  • tachycardia
  • Hyponatremia
  • Hypotension
  • autism
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9
Q

Most effective tocolytic drugs?

A

*COX inhibitors
*calcium channel blockers
*beta-agonists

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10
Q

Less effective tocolytic drugs?

A

*Oxytocin receptor antagonists
*Magnesium sulfate
*Nitric oxide donors

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11
Q

Why we add Prostaglandin E1 (misoprostol); Prostaglandin E2(dinoprostone) to oxytocin?

A

cervical ripening and an increase in myometrial contractility

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12
Q

symptoms of menopause?

A
  • Vasomotor symptoms
  • Sleep disturbances
  • Psychological disturbances
  • Lipid changes
  • Accelerated bone loss
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13
Q

Low-dose vaginal estrogen (cream, ring) for?

A

genitourinary syndrome of menopause

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14
Q

estrogen plus progestin replacement therapy?

A
  • Breast cancer
  • increased CHD, strokes, thrombosis
  • reduced risk of colon cancer
  • decrease in fracture risk
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15
Q

estrogen preparations?

A

Oral
Transdermal
Topical
Vaginal

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16
Q

progestin preparations?

A
  • Medroxyprogesterone acetate
    the most commonly prescribed progestin historically
  • Oral micronized progesterone
    does not appear to increase the risk of either breast cancer or CHD
  • Levonorgestrel-releasing intrauterine device
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17
Q

oral combination

A

estradiol + norethindrone acetate
CEE + medroxyprogesterone
ethinyl estradiol + norethindrone acetate

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18
Q

Transdermal combination ?

A

17-beta estradiol + norethindrone acetate

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19
Q

Bazedoxifene (SERM)

A

agonist on bone,
antagonist on endometrium
Side Effect/ venous thromboembolic

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20
Q

give me 3 (SERM) drugs ?

A

Raloxifene
Bazedoxifene
Tomaxifene

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21
Q

Side effects of Raloxifene?

A

thrombotic disease

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22
Q

HRT: regimens?

A
  • Unopposed estrogen
    not recommended for healthy women
  • Cyclic combined regimens
    daily estrogen with progestin on days 1 to 14 of each calendar month
  • Continuous combined regimens
    both hormones are given every day
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23
Q

ADV of cyclic and continuous regimens?

A

Decrease risk of endometrial carcinoma

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24
Q

Dis Adv of continuous?

A

irregular bleeding & amenorrhea

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25
Q

HRT: contraindications?

A
  • Breast cancer
  • Endometrial cancer
  • CHD
  • Vaginal bleeding
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26
Q

alternative to relief of vasomotor symptoms?

A

Clonidine

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27
Q

what is the ttt of Hyperprolactinemic anovulation?

A

dopamine agonists

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28
Q

what is the ttt of Polycystic ovary syndrome (PCOS)?

A

Letrozole therapy & Clomiphene citrate

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29
Q

off-label use of Letrozole therapy

A

ovulation induction

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30
Q

Therapy for infertility?

A

1- Clomiphene citrate
2- Letrozole
3- Dopamine agonists
4- Pulsatile GnRH Therapy
5- Gonadotropin Therapy
6- Metformin

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31
Q

what is the MOA of Clomiphene citrate?

A

bind to estrogen receptors in the hypothalamus as an antagonist so it blocks the negative feedback as a result GnRH increases

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32
Q

Which of the following SERM is used for ttt of infertility?

A

Clomiphene citrate

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33
Q

SERM but they aren’t used for infertility?

A

Tamoxifen and raloxifene

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34
Q

Adverse effects of Clomiphene citrate?

A

-ovarian enlargement
-multiple gestation
-hot flash

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35
Q

This drug is an aromatase inhibitor

A

Letrozole

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36
Q

For oligo-ovulatory women with polycystic ovary syndrome (PCOS)
* is not US FDA approved for Letrozole

A

give her clomiphene citrate

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37
Q

why are multiple pregnany caused by clomiphene citrate?

A

bind to estrogen receptors in the hypothalamus as an antagonist so it blocks the negative feedback as a result GnRH increases

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38
Q

give me the Dopamine agonists?

A

Bromocriptine
Cabergoline

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39
Q

Ovarian hyperstimulation syndrome (OHSS) is adverse effect of which drug?

A

Gonadotropin Therapy

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40
Q
  • correction of hyperinsulinemia with metformin
  • increase menstrual cyclicity and improve spontaneous ovulation
A

Metformin

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41
Q

define Hormonal contraception

A
  • Uses drugs that affect the function of estrogens and progestins to essentially eliminate the possibility of pregnancy
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42
Q

Two types of oral preparations?

A
  1. Combination oral contraceptives (COCs): estrogen plus progestin
  2. Progestin only pills
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43
Q

the most commonly used estrogen

A

Ethinyl estradiol

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44
Q

COCs MOA

A
  • inhibition of LH , so no ovulation
  • inhibition of FSH , so suppression of ovarian folliculogenesis
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45
Q

COCs: mild adverse effects

A

Nausea, edema, headache, skin pigmentation

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46
Q

COCs: moderate adverse effects

A
  • Weight gain
  • Acne
  • Hirsutism
  • Amenorrhea
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47
Q

COCs: severe adverse effects

A
  • Thromboembolism
    *cardiovascular disorders
    *MI
  • Cerebrovascular disease
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48
Q

COCs: contraindications

A
  • CVD
  • HTN
  • H.F
  • DIBETES
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49
Q

what is the drug that accelerates COCs metaboLISM?

A

Phenytoin
Rifampin

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50
Q

what is the MOA of progesterone that is taken orally?

A
  • thinning of the endometrium
  • changes the composition of cervical mucous “less volume, and more thick”
  • suppression of ovulation
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51
Q

Examples of Progestin-only pills (oral)

A

norethindrone, desogestrel

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52
Q

side effect of POP

A

Unplanned bleeding and menstrual irregularities

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53
Q

List Short-acting contraceptives

A

transdermal patch
vaginal ring
depot injection

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54
Q

List Long-acting contraceptives:

A

subcutaneous implant
intrauterine devices (IUDs)

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55
Q

non hormonal IUDs

A

Copper-releasing IUDs

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56
Q

what is the drug used as Postcoital contraceptives

A

levonorgestrel

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57
Q

gold standard to diagnose osteoporosis

A

dual-energy x-ray absorptiometry (DXA)

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58
Q

(osteopenia) is defined as

A

T-score between -1.0 to-2.5.

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59
Q

what drugs reduce bone lose (antiresorptive)?

A

bisphosphonates
calcitonin
SERMs
denusomab
calcium

60
Q

what drugs enhance bone formation?

A

PTH
Teriparatide

61
Q

TTT of Rickets and osteomalacia?

A

vitamin D

62
Q

CALCIUM SALTS

A
  • calcium gluconate
    IV emergency ttt of hyperkalaemia
  • calcium lactate
63
Q

Clinical Uses of CALCIUM SALTS

A
  • Dietary deficiency.
  • Hypocalcaemia
    Prevention and treatment of osteoporosis (often with estrogen or
    SERM in women, bisphosphonate, vitamin D).
64
Q

Unwanted effects of CALCIUM SALTS

A

in patients receiving cardiac glycosides
Intravenous administration in the emergency treatment of hyperkalaemia requires care

65
Q

what are the vitamin D preparations?

A

ergocalciferol
alfacalcidol
calcitriol

Paricalcitol (synthetic vitamin D)

66
Q

Excessive intake of vitamin D causes?

A

hypercalcemia
(kidney stones and renal failure)

67
Q

what does BiPHOSPHONATE do?

A

they form tight complex with calcium in bone matrix then when osteoclast reach bonE THEY GOT EXPOSED TO HIGH CONC of bisphosphonate

68
Q

MOA of bisphosphonate?

A

1- etidronate (cause apoptosis to osteoclast)

2- pamidronate, alendronate, risedronate, ibandronate, zoledronate
(prevent osteoclast attachment to bone)

69
Q

Clinical Uses of bisphosphonate?

A

Osteoporosis
Malignant disease
Paget’s disease

70
Q

Unwanted effects of bisphosphonate?

A

Peptic ulcers, oesophagitis, osteonecrosis of jaw

71
Q

RALOXIFENE

A

stimulates osteoblasts and inhibits osteoclasts
agonist on CVS and antagonist on mammary tissue and the uterus

72
Q

Calcitonin reduces calcium levels in the blood by two main mechanisms?

A

Bone – Inhibits osteoclastic activity
Kidney - decrease reabsorption of calcium & phosphorous

73
Q

The main preparation available for clinical use of Calcitonin?

A

salcatonin (synthetic salmon calcitonin)

74
Q

Clinical uses of Calcitonin?

A

Hypercalcaemia
Paget’s disease
osteoporosis

75
Q

recombinant PTH?

A

teriparatide
(stimulating new bone formation and reduces osteoblast apoptosis)

76
Q

peptide analogue

A

ostabolin (increase bone mass)

77
Q

STRONTIUM

A

inhibits bone resorption and also stimulates bone formation

78
Q

this drug prevents vertebral and non-vertebral fractures in older women

A

STRONTIUM

79
Q

side effect of STRONTIUM

A

blocks potassium channels responsible for basal vasodilator tone so increased risk of cardiovascular disease

80
Q

MOA of STRONTIUM

A

Strontium ions stimulate the calcium-sensing receptor causing pre osteoblasts to differentiate into osteoblasts

Strontium inhibits osteoclasts so decreasing bone resorption.

81
Q

Drug act against RANK-L

A

Denosumab
(It is especially useful when bisphosphonates are not appropriate)

82
Q

POTENTIAL NEW THERAPIES (Cathepsin K inhibitors)

A

odanacatib

83
Q

2 drugs causes osteonecrosis of the jaw

A

Denosumab and bisphosphonate

84
Q

Cortisol converted to cortisone by?

A

11 β-hydroxysteroid dehydrogenase-2

85
Q

What are the effect of glucocorticoids?

A

gluconeogenesis
catabolic effect on muscles
lipolysis
conserve glucose to the brain

86
Q

Glucocorticoids with larger doses

A

inhibit Antibody production

87
Q

short-acting Glucocorticoids

A

Hydrocortisone
Cortisone

88
Q

Intermediate acting Glucocorticoids

A

Prednisone
Prednisolone
Methylprednisolone
Triamcinolone

89
Q

Long-acting Glucocorticoids

A

Betamethasone (asthma)
Dexamethason
((both 0 salt retaining activity))

90
Q

Mineralocorticoids (12-36hr) ((Not used for anti inflammatory effect))

A

Fludrocortisone

91
Q

Clinical Uses of GCs

A

-adrenal disorders (adesone, congenital adrenal hyperplasia, cushing)
-lung maturation in fetus
-non-adrenal disorders

92
Q

TTT of Addison’s disease?
(weakness, fatigue, weight loss, hypotension,
hyperpigmentation, inability to maintain blood glucose)

A

Acute phase: IV hydrocortisone with IV fluids
Maintenance: fludrocortisone orally

93
Q

TTT of congenital adrenal hyperplasia?
(deficiency of 21-hydroxylase)

A

hydrocortisone, fludrocortisone

94
Q

what is the use of hydrocortisone in the TTT or diagnosis of crushing syndrome?

A

surgical resection of tumor we need large dose of hydrocortisone after and during the surgery

95
Q

Causes of Cushing syndrome?

A

a) Cushing disease (pituitary adenoma)
b) ectopic ACTH secretion
c) adrenal disorders “adenoma, carcinoma”

96
Q

Mechanism of action of antenatal steroids

A
  • accelerate the development of type 1 and 2 pneumocytes
  • increase surfactant production by type 2 pneumocytes
97
Q

TTT of Lung maturation in fetus?

A

Betamethasone

98
Q

Why betamethasone and not hydrocortisone?

A

Potency, half life, no mineralocorticoid, less binding to plasma proteins, and less placental metabolism

99
Q

Glucocorticoids toxicity

A

insomnia, hypomania, peptic ulcer (early)
Depression (later)
- Iatrogenic Cushing syndrome (moon face)
- Adrenal suppression (if therapy > 2 wks)

100
Q

Indication for Synthesis inhibitors & GC antagonist use?

A

-severe hypercortisolism
-hypercortisolism following pituitary surgery
-while awaiting radiotherapy for Cushing disease
-treatment of ectopic ACTH syndrome

101
Q

Adrenal enzyme inhibitors?

A

Ketoconazole, Metyrapone, and Mitotane

102
Q

antifungal agent
most widely (first line) for Cushing syndrome.

A

Ketoconazole

103
Q

side effect of Ketoconazole

A

headache, Teratogenic, fertility

104
Q

GC antagonist safe in pregnancy

A

Metyrapone

105
Q
  • It inhibits glucocorticoid synthesis by cleavage enzyme and 11-β-hydroxylase.
  • it has a cytotoxic effect on adrenal tissue

It produces medical adrenalectomy

it produces GIT upset, so the administration is better to be at bedtime.

A

Mitotane

106
Q

intravenous anesthetic drug that blocks 11-β hydroxylase

  • It lowers serum cortisol to normal within approximately 10 hours and is the only available agent for patients unable to take medication by mouth
A

Etomidate

107
Q

which hormone is responsible for the onset of
gamatogenic function?

A

FSH by the pituitary

108
Q

With LH stimulation, testosterone is produced by?

A

interstitial or Leydig cells (95%)

109
Q

what are the weak androgens secreted by the testes?

A

androstenedione and dehydroepiandrosterone

110
Q

what are the strong androgens secreted by the testes?

A

dihydrotestosterone (more potent than testosterone )

111
Q

what is the source of testosterone in females?

A

ovaries and adrenals

112
Q

Testosterone is also present in the plasma of women in concentrations of approximately?

A

0.03 mcg/dL

113
Q

what hormones or what are the conditions in which sex hormone binding globulin increases?

A

estrogen
thyroid hormone
Liver cirrhosis

114
Q

what hormones or what are the conditions in which sex hormone binding globulin decreases?

A

androgen
growth hormone
obese individuals

115
Q

65% of circulating testosterone is?

A

bound to sex hormone binding globulin (SHBG)

116
Q

Physiologic Effects of testosterone?

A
  • larynx grows
  • vocal cords become thicker
    -lower-pitched voice
  • Skeletal growth
  • appearance of pubic, axillary, and beard hair
117
Q

androgens do 2 things?

A

stimulate renal erythropoietin secretion and decrease HDL levels

118
Q

what is the Metabolic effects of androgens?

A

increased liver synthesis of clotting factors, triglyceride lipase, α 1 -antitrypsin, haptoglobin, and sialic acid.

119
Q

Testosterone and its derivatives have been used for?

A

their anabolic effects as well as in the treatment of testosterone deficiency.

120
Q

what testosterone derivates active in the mouth?

A

methyltestosterone and fluoxymesterone

121
Q

derivatives of Testosterone

A

propionate, enanthate, undecanoate, or cypionate

122
Q

which enzyme converts testosterone to dihydrotestosterone?

A

5α-reductase

123
Q

if we give large doses of testosterone to adult males what will happen?

A

negative feedback so decrease the releases of (LH & FSH)
prostatic hyperplasia causing urinary retention

124
Q

If women administer more than 200–300 mg of testosterone per month what will happen?

A

hirsutism, acne, amenorrhea and deepening of the voice.

125
Q

side effect of 17-alkyl-substituted steroids ?

A

hepatic dysfunction

126
Q

if we maintain the level of androgen in the blood more than 0.6 mg what will happen?

A

azoospermia and decrease in testicular size

127
Q

if we give alkylated androgens in high doses what will happen?

A

peliosis hepatica, cholestasis, hepatic failure

128
Q

ANTIANDROGENS
1- (Steroid Synthesis Inhibitors)
2- (5α-reductase inhibitor)
3- (Receptor Inhibitors)
4- (competitive inhibitor)

A

1- Ketoconazole
2- Finasteride
2- Dutasteride
3- Cyproterone and cyproterone acetate
3- Flutamide
3- Bicalutamide and nilutamide
4- Spironolactone

129
Q

used primarily in the treatment of fungal disease

A

Ketoconazole

130
Q

side effect of ketoconazole

A

reversible gynecomastia

131
Q

what is the use of Finasteride?

A

reducing prostate size in men with benign prostatic hyperplasia

132
Q

These drugs are not approved for use in women or children

A

Finasteride & Dutasteride

133
Q

why Cyproterone and cyproterone acetate are effective antiandrogens?

A

they have marked progestational effect that suppresses the feedback
enhancement of LH and FSH, leading to a more effective antiandrogen effect

134
Q

treatment of hirsutism in women?

A

Cyproterone acetate with estrogen

135
Q

what is the drug has a competitive antagonist at the androgen receptor?

A

Flutamide

136
Q

what are the 2 disadvantages of Flutamide?

A

-causes mild gynecomastia
- mild reversible hepatic toxicity.

137
Q

what drugs have a combination with a GnRH analog?

A

Bicalutamide and nilutamide

138
Q

What are the 2 MOA of Spironolactone?

A

1-reduces 17α-hydroxylase activity
2-lowering plasma levels of testosterone

139
Q

what are contraceptive use in males?

A

testosterone and testosterone enanthate

140
Q

which combination produces azoospermia in 94% of men?

A

100 mg of testosterone & 500 mg of levonorgestrel daily orally

141
Q

adverse effect of GOSSYPOL

A

Hypokalemia

142
Q

1- Sildenafil/onset, Half-life, Effect of food on absorption, use

2- Tadalafil/onset, Half-life, Effect of food on absorption, use

A

1- 1Hr / 3-4hR / ++ / PRN

2- 2Hr / 18Hr / – / daily

143
Q

contraindication of Phosphodiesterase 5 inhibitors?

A

Nitrates

144
Q

Natural PDE5 inhibitors?

A

Epimedium
Cinnamon
Black Ginger Extract
Tongkat Ali

145
Q

synthetic PGE1, Administered via intra-urethral suppositories

A

Alprostadil

146
Q

Adverse effects of Alprostadil

A

Caution: sexual intercourse with pregnant woman

Pharmacology (6 decks)

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