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Pharmacology > Endocrine > Flashcards

Endocrine Flashcards

1
Q

List of growth hormones.

A

a. Somatropin
b. IGF1 agonist (Mecasermin)
c. Somatostatin analogues (Octreotide, Lanreotide)
d. Growth Hormones antagonists (Pegvisomant)
e. Dopamine agonist (Bromocriptine, Cabergoline, Quinagolide)

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2
Q 
Somatropin
MOA
USES
S/E
CONTRAINDICATIONS
A

MOA:
● GH analog, acts through GH receptors to increase production of IGF1.

Therapeutic uses:
● GH deficiency
● short stature in children with genetic conditions
● AIDS wasting
● Anti-aging
● Short Bowel Syndrome
● Athletes to increase their performance

SE: pseudotumor cerebri, progression of scoliosis, edema, hyperglycemia in children. Peripheral edema, myalgia, arthralgia in adults.

Contra : Pediatric patients with closed epiphysis, Obese patient with Prader Willi (as it cause asphyxiation), Diabetic retinopathy patients

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3
Q

IGF1 agonist (Mecasermin)

MOA
CONTRA
S/E

A

MOA: IGF1 analog.

CA: in children with IGF1 deficiency who are unresponsive to GH therapy.

SE: hypoglycemia, intracranial hypertension, increased liver enzymes.

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4
Q

Somatostatin analogues (Octreotide, Lanreotide)
MOA
CONTRA
SIDE EFECTS

A

MOA: somatostatin receptor agonist. Somatostatin inhibits the release of glucagon, insulin and GH.

CA: acromegaly, carcinoid and other endocrine tumors.

SE: gastrointestinal disturbances, gallstones, cardiac conduction abnormalities, bradycardia.

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5
Q

Growth Hormones antagonists (Pegvisomant)
MOA
C/I
S/E

A

MOA: blocks GH receptor.
USE: acromegaly.
SE: increased liver enzymes.

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6
Q

Dopamine agonist (Bromocriptine, Cabergoline, Quinagolide)

A

MOA: dopamine receptor agonist.

USE: hyperprolactinemia because it inhibits prolactin, but in high doses it has some efficacy in the treatment of small GH secreting tumors. Also in treatment of Parkinsons.

SE: GI disturbances, orthostatic hypotension and headache.

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7
Q

Bromocriptine

A

● D2 agonist - GH and Prolactin antagonist
● mostly inhibit prolactin release than GH, but at high doses inhibit release of GH
and is used in treating GH producing tumours
● Hyperprolactinemia
● Also in treatment of migraine and its effect on adrenergic receptors where its an
alpha adrenergic agonist as well
● SE: GI disturbances, orthostatic hypotension and headache.

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8
Q

Luteinizing Hormone

EXAMPLES

A

a. Menotropins (HMG)
b. LH analogs
1. Human chorionic gonadotropin - 1st Line
2. Lutropin

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9
Q

Menotropins (HMG)

A

Extracted from the urine of post-menpausal women. Contains both FSH and LH.

USE: Initiation of oocyte maturation and ovulation. Male hypogonadotropic hypogonadism.

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10
Q

Human chorionic gonadotropin - 1st Line

A

Purified from human urine or recombinant version (choriogonadotropin alfa). Has a structure similar to LH so it acts through activation of LH receptors.

USE: Initiation of oocyte maturation and ovulation. Male hypogonadotropic hypogonadism.

SE: ovarian hyperstimulation and in multiple pregnancies in wo

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11
Q

Lutropin- 2ND LINE

A

Recombinant form of human LH.

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12
Q

Follicle Stimulating Hormone

A

a. Follitropin alfa
MOA: FSH receptor agonist.

USE: controlled ovulation hyperstimulation in women and infertility due to hypogonadotropic hypogonadism in men.

SE: Ovarian hyperstimulation syndrome and multiple pregnancies. Gynecomastia in men, headache, depression and edema.

b. Urofollitropin
Human FSH purified.

c. Follitropin beta.
Recombinant FSH.

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13
Q

Oxytocin

A

USE : Induction of labor and control of uterine haemorrhage after delivery.

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14
Q

Oxytocin

SIDE EFFECTS

A

SE: Fetal distress, placental abruption, uterine rupture, fluid retention and hypotension.

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15
Q

Oxytocin receptor antagonist (Atosiban)

A

CA: used as a drug to suppress preterm labour, tocolysis SE: not FDA approved. Rates of infant death.

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16
Q

What is Tocolysis

A

● Tocolysis is an obstetrical procedure carried out with the use of medications with
the purpose of delaying the delivery of a fetus in women presenting preterm
contractions.

● These medications are administered with the hope of decreasing fetal morbidity
and mortality.

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17
Q

Drugs used in Tocolysis:

A

● beta2 agonists like salbutamol, terbutaline and atosiban (oxytocin receptor antagonists- limited side effects)

● calcium blockers like nifedipine, magnesium sulfate as myosin light chain inhibitor- as a supportive agent and neuroprotection.

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18
Q

Drugs used for lung maturation

A

Belmethazone

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19
Q

Vasopressin

A

Vasopressin acts on V1 and V2. Sometimes used to control bleeding from esophageal varices.

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20
Q

Vasopressin receptor agonist (Desmopresin)

A

MOA: acts on V2.

CA: pituitary diabetes insipidus, mild hemophilia A and Von Willebrand disease.

SE: GI disturbance, headache, hyponatremia.

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21
Q

Vasopressin receptor antagonist (Conivaptan)

A

MOA: antagonist of V1a and V2 receptor. CA: hyponatremia in hospitalised patients. SE: infusion site reactions.

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22
Q

Tolvaptin

A

Tolvaptin selective for V2 receptors. Administered orally. May cause hepatotoxicity.

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23
Q

GnRH analogs (Leuprolide, Gonadorelin)

A

CA: Prostatic cancer, transgender pubertal adolescents, controlled ovarian suppression.

SE: Headache, nausea, in continuous treatment can cause symptoms of hypogonadism.

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24
Q

GnRH antagonists (Ganirelix, Cetrarelix)

A

CA: prevention of premature LH surges during controlled ovarian stimulation.

Degarelix and Abarelix are for prostate cancer treatment.

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25
Q

Indication and contraindications of thyroid hormones.

A

Indication flag - Graves disease

Contra : children and gravid women (pregnant women)

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26
Q

Thyroid analogs (Levothyroxine - T4, Liothyronine - T3)

A

MOA: Activation of receptors resulting in gene expression and protein synthesis. Their effects include nervous, skeletal, reproductive systems. Metabolism of fats, carbs, proteins and vitamins.

CA: Hypothyroidism.

SE: Thyroid excess - sweating, tachycardia, dyspnea, weight loss.

27
Q

Thioamides (Methimazole, Propylthiouracil) (Carbimazole)

A

MOA: Inhibits peroxidase reaction and iodine organification [Iodination of tyrosine residues and condensation of monoiodotyrosine(mit) and dit(diiodo)]. PTU also inhibits the conversion of T4 into T3.

CA: Hyperthyroidism.

SE: nausea, GI disturbances, rash, agranulocytosis, liver dysfunction, hypothyroidism.

28
Q

Thyrostatics

A

Thyrostatics = Thioamides + Thiamazol (dec synthesis of T3,T4) + PTU (+ inhibits conversion) Titrating regimen or block regimen in Thyrostatins :
● Titration regimen : limit the symptoms of thyrotoxicosis at present then, lower the doses due to side effects (like reverse titration so as to not put patient in hypothyroidism)
● Block Regimen : administer thyrostatics chronically and concomitantly with thyroxine as part of hormone substitution.

29
Q

Iodides

A

Lugol solution and Potassium iodide.

MOA: inhibit iodide organification and hormone release. Decrease the size and vascularity of the thyroid gland.

CA: Prep for surgical thyroidectomy and management of thyroid storm.

SE: rare, drug fever, bleeding disorders.
To protect from absorption of radioactive iodine compounds - Chernobyl

30
Q

Radioactive iodine

A

MOA: radiation induced destruction of the thyroid parenchyma.

CA: hyperthyroidism, permanent cure to thyrotoxicosis.

SE: sore throat, hypothyroidism.

CI: Pregnancy and nursing women.

Anion inhibitors such as thyozionate, perchlorate block uptake of Fe by thyroid because they inhibit iodide transporter. They are unpredictable and can cause aplastic anemia.

31
Q

Wolff-Chaikoff effect

A

● A pharmacologic dose of iodide inhibits the iodination of tyrosines (“Wolff-Chaikoff effect”) (for high doses for iodine - 1 mg/kg) but this effect lasts only a few days.
● More importantly, iodide inhibits the release of thyroid hormones from thyroglobulin
● A normal thyroid gland responds to iodine load through an intrinsic autoregulatory
mechanism, which acutely blocks thyroid hormone synthesis (Wolff-Chaikoff effect) and
causes an increase in serum TSH concentration.
● The normal thyroid gland then escapes this block by reducing iodine transport and
intrathyroidal concentrations to levels insufficient to maintain the Wolff-Chaikof

32
Q

Beta blocker (Propranolol)

A

MOA: inhibition of conversion of T4 to T3.

CA: thyroid storm, controlling tachycardia and other cardiac abnormalities (extreme thyrotoxicosis) (crisis)

SE: Asthma, hypotension, AV blockage, Bradycardia.

Thyroid storm : Thyroid storm presents with extreme symptoms of hyperthyroidism. Treatment - same like Hyperthyroidism but higher dose and more frequently.

33
Q

Amiodarone

A

Iodine contains antiarrhythmic drug.
a) Hypothyroidism
Because it has the ability to block the conversion of T4 to T3. Treated with thyroid
hormone.
b) Hyperthyroidism
Caused in people with underlying thyroid disease such as goitre (Thioamides) or some inflammatory condition that causes leakage of thyroid hormones (Corticosteroids).

34
Q

Why folic acid is given before pregnancy

A

If you’re planning to have a baby, it’s important that you take folic acid tablets for two to three months before you conceive. This allows it to build up in your body to a level that gives the most protection to your future baby against neural tube defects, such as spina bifida.

35
Q

Estrogens

A

Estrogens (Ethinyl estradiol, Mestranol-converted to EE, Estrogen esters-long acting IM)
MOA: Activation of estrogen receptor leading to increased estrogen
CA: Hypogonadism in women, HRT in women with estrogen deficiency (menopause, premature ovarian failure or surgical removal of ovaries), bone loss and osteoporosis, hormonal contraceptive.
PK: Oral,parenteral or transdermal
Tox: Bleeding, nausea, breast tenderness, thromboembolism, hypertension, depression, in post menopausal women can lead to breast cancer, endometrial hyperplasia.
DI: In combination with cytochrome p450 can lead to bleeding and reduced contraceptive efficacy.

36
Q

Antiestrogens

A 
❖ SERM
1. Tamoxifen, Toremifene - 1st Line
2. Raloxifene
3. Bazedoxifene
4. Clomifene
❖ Receptor antagonists (Fulvestrant)
❖ Aromatase inhibitors (Anastrozole, Letrozole, Exemestane-irreversible inhi)
❖ GnRH agonist (Leuprolide)
❖ GnRHantagonist(Ganirelix-F,Abarelix-M)
37
Q

Tamoxifen, Toremifene - 1st Line

A

MOA: Estrogen antagonist effect in Breast tissue and CNS, agonist effects in bone and liver.
CA: Prevention and treatment of hormone responsive breast cancer.
PK: Oral
Tox: Hot flushes, thromboembolism, endometrial hyperplasia.

38
Q

Raloxifene

A

MOA: Antagonist effect in breast tissue, CNS and endometrium, agonist in liver.
CA: Osteoporosis and breast cancer

39
Q

Bazedoxifene

A

CA: treatment of menopausal symptoms and menopausal osteoporosis

40
Q

Clomifene

A

MOA: antagonist effect in pituitary leading to increased gonadotropin secretion

CA: used for ovulation induction

41
Q

Receptor antagonists (Fulvestrant)

A

MOA: Estrogen antagonist in all tissues
CA: Breast cancer treatment when resistant to first line therapy PK: IM
Tox: Hot flushes, headache, injection site reactions.

42
Q

Aromatase inhibitors (Anastrozole, Letrozole, Exemestane-irreversible inhi)

A

MOA: Inhibits aromatase enzyme that is responsible for the conversion of testosterone into estradiol, leading to decreased estrogen.
CA: Treatment of hormone responsive breast cancer
PK: Oral
Tox: Hot flushes, reduced bone mineral density, joint symptoms.

43
Q

GnRH agonist (Leuprolide)

A

MOA: Steady dose leading to activation of GnRH receptor causing the body to down regulate GnRH production leading in reduced ovarian hormones.
CA: Ovarian hyperstimulation, decrease puberty in transgender adolascents, prostatic cancer.
PK: IV, SC and IM
Tox: Headache, nausea, injection site problems and decreased bone density.

44
Q

GnRHantagonist (Ganirelix-F,Abarelix-M)

A

MOA: Antagonist to GnRH receptor causing decrease in ovarian hormones

CA: F - prevention of premature LH surges during controlled ovarian stimulation
M - Prostatic cancer

PK: F - SC injection
Tox: Headache, nausea

45
Q

Progesterone (Norgestrel)

A

MOA: acts on progesterone receptor leading to increased production CA: Hypogonadism, contraceptive, HRT

PK: Oral, parenteral

Tox: weight gain, decreased bone density

46
Q

❏ Antiprogestin (Mifepristone)

A

MOA: antagonist of progesterone and GCS receptor
CA: in combination with prostaglandins - used for medical abortions PK: oral
Tox: GI problems, vaginal bleeding

47
Q

HORMONE REPLACEMENT
THERAPY
(HRT) (Tibolone, Livial)

A

CONJUGATED ESTROGEN, ETHINYL ESTRADIOL + MEDROXY PROGESTERONE ACETATE/NORETHISTERONE
● Suppress perimenopausal syndrome of vasomotor instability, psychological disturbances, dermatological changes as well as in preventing atrophic changes, risk of CVD, and osteoporosis.
● HRT discontinued when vasomotor symptoms(primary indication of HRT) abate
● Calcium + Vit D supplements and exercise aid the beneficial effect. Not the best
option to prevent osteoporosis and fractures
● Protection against coronary artery disease only in early postmenopausal women.
Increase the risk of venous thromboembolism, MI and stroke in elderly women.
● Does not protect against cognitive decline; may increase the risk of dementia.
● Increases the risk of breast cancer, gallstones and migraine.
Osteoporosis treatment: bisphosphonates, vitamin d, calcium in the diet, sodium fluoride?? , estrogens

48
Q

HRT effect on liver

A

● As is the case with the oral contraceptive pill, their use is officially cautioned in but there have been surprisingly few reports of increased
following HRT, and there is evidence that some of the therapeutic advantages may be particularly important to women with liver disease.
● Bone density loss is an important complication of chronic liver disease and may result in pain, fracture of the long bones and vertebrae, deformity and immobility.

49
Q

risks and benefits of HRT

A

Apart from protection against osteoporosis, HRT is associated with favourable changes in serum lipid levels in normal postmenopausal women which could be especially important in women with cholestatic liver disease (especially primary biliary cirrhosis) who have elevated mean serum cholesterol.
● Addition of progestogens in combination with oestrogen for 10 to 14 days of the cycle does not decrease the cardioprotective effect and protects against the increase in endometrial cancer observed with oestrogen therapy alone.
● As with patients without liver disease, caution should be exercised in treating women with venous thromboembolism and those with a history (or family history) of breast cancer23, 24.
● Other benefits of HRT, including preventing or reversing vaginal and breast atrophy, improving hot flushes and psychofunctional disturbances, and (probably) decreasing the incidence of ischaemic heart disease25, are of just as much potential value to women with liver disease as to those without.
● HRT may be used with caution in women with a history (or family history) of jaundice due to specific defects of bilirubin excretion

50
Q

Androgens (Testosterone)

A

MOA: androgen receptor agonist leading to increased production
CA: hypogonadism in males
PK: Transdermal, Buccal, SC and implant
Tox: F- hirsutism, M-gynecomastia, testicular shrinkage, increased doses lead to infertility

51
Q

Antiandrogens

EXAMPLES

A 
5 alpha reductase inhibitor (Finasteride)
Receptor antagonist (Flutamide-M, Spironolactone-F) 1st Line
52
Q

5 alpha reductase inhibitor (Finasteride)

A

MOA: Inhibits 5 alpha reductase enzyme responsible for the conversion of testosterone to DHT, leading to decreased DHT
CA: Benign prostatic hyperplasia, male pattern hair loss.
PK: Oral
Tox: rarely impotence and gynecomastia

53
Q

Receptor antagonist (Flutamide-M, Spironolactone-F) 1st Line

A

MOA: Inhibition of androgen receptor/ spirono-inhibit MCS receptor, K+ sparring diuretic CA: Prostate cancer/ hirsutism
PK: Oral
Tox: gynecomastia, impotence, hot flushes, hepatotoxicity

54
Q

Synthesis inhibitor (Ketoconazole-antifungal properties) 2nd Line

A

MOA: inhibits cytochrome P450 enzyme involved in androgen synthesis CA: prostate cancer resistant to 1st line therapy
PK: Oral
Tox: interfere with other steroids

55
Q

Glucocorticosteroids

EXAMPLES

A

Cortisol/ Prednisone,

Pregnancy - Belmethazone

56
Q

Cortisol/ Prednisone,

Pregnancy - Belmethazone

A

MOA: activation of glucocorticoid receptor alters gene transcription

CA: Adrenal disorders - acute adrenal insufficiency, chronic - Addison’s disease; Inflammatory and immunological disorders, organ transplant rejection, haematological cancers.

PK: Cortisol - lesser duration, lesser topical action, more salt retention and lesser anti-inflammatory activity (compared to Prednisone)

Tox: Adrenal suppression, growth inhibitor, osteoporosis, diabetes.

57
Q

What type of drug is Mifepristone?

A

Glucocorticosteroid antagonists

58
Q

Mifepristone

A

MOA: blocks GCS and progesterone receptors.
CA: +prostaglandins used for medical abortion, rarely in Cushing syndrome. PK: oral
Tox: GI disturbances, vaginal bleeding and abdominal pain.

59
Q

What type of drug is Aldosterone/ Fludrocortizone

A

Mineralocorticosteroid

60
Q

Aldosterone/ Fludrocortizone

A

MOA: ?, limited activation of GCS receptor
CA: Adrenal insufficiency like Addison’s disease
PK: Aldosterone - lesser duration, more salt retention, lesser anti-inflammatory effect. Tox: Salt and fluid retention, CHF and in increased doses lead to GCS toxicities.

61
Q

What type of drug is Spironolactone, Eplernone

A

ineralocorticosteroid antagonists

62
Q

Spironolactone, Eplernone

A

MOA: antagonist of MCS receptor, weak antagonist of androgen receptor.

CA: Aldosteronism, hypokalemia due to diuretics, post MI.

PK: slow onset and offset; 24-48hrs.

Tox: Hyperkalemia, gynecomastia, additional interaction with other K+ retaining drugs.

63
Q

What type of drug is the anti fungal Ketoconazole

A

MOA: blocks cytochrome P450 enzyme involved in androgen synthesis

CA: inhibits mammalian steroid synthesis, fungal ergosterol synthesis

PK: Oral/ topical
Tox: hepatic dysfunction, increased drug-drug interactions.

Pharmacology (22 decks)

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