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203: Theme 1: The Endocrine System > Endocrine pharmacology revision > Flashcards

Endocrine pharmacology revision Flashcards

1
Q

Growth hormone synthesised in

A

Somatotrophe cells of the anterior pituitary

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2
Q

GH secretion controlled by

A

Hypothalamus via

  • GHRH
  • GHRIH
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3
Q

Second messengers with GH

A

Insulin like growth factor 1

Insulin like growth factor 2

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4
Q

Primary effect of GH

A

Promote the linear growth of adolescence

Increases protein synthesis and collagen deposition

Also involved in tissue turnover and repair

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5
Q

GH at physiological concentrations

A

Mimics the actions of insulin on carbohydrates

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6
Q

GH at high concentrations

A

Diabetogenic

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7
Q

Use of GH

A

Treat deficiency of hormone in adults and children

In children used in Prader-WIlli, Turner’s and chronic renal insufficiency

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8
Q

Somatotropin

A

Cautions: diabetes mellitus, malignant disease, intracranial hypertension

Contraindications: evidence of tumour activity, not to be used after renal transplantation

Side effects: headache, visual problems, nausea and vomiting, athraglia, myalgia, carpal tunnel syndrome, parasthesia, hyperglycaemia

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9
Q

Somatomedins

A

Polypeptide hormone structurally related to insulin, known as IGFs

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10
Q

Mecasermin

A

Human insulin like growth factor

Treat growth failure in children and adolescents with severe IGF1 deficiency

Side effects: headaches, cardiomegaly, tachycardia, sleep apnoea, night terrors

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11
Q

Growth hormone receptor antagonist example

A

Pegvisomant

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12
Q

Pegvisomant

A

Highly selective growth hormone receptor antagonist

Treatment of acromegaly without response to surgery and radiation

Contraindications: pregnancy and breast feeding

Side effects: diarrhoea, constipation, nausea, vomiting, abdominal distension, dyspepsia, flatulence, hypertension, tremor, weight gain

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13
Q

Thyroid hormone use

A

Hypothyroidism

Non- toxic goitre

Hashimoto’s thyroiditis

Thyroid carcinoma

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14
Q

Thyroid hormone treatment of choice

A

Levothyroxine sodium

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15
Q

Levothyroxine sodium

A

Cautions: panhypopituitarism, elderly, CV disorders, long standing hypothyroidism, MI, DM, pregnancy

Side effects: diarrhoea, vomiting, anginal pain, arrhythmias, palpitation, tachycardia, tremor, headache, flushing

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16
Q

Thyrotrophin

A

Recombinant form of thyrotrophin

Use with or without radioiodine imaging for detection of thyroid remnants and thyroid cancer in post thyroidectomy patients

17
Q

Antithyroid drugs

A

Used for hyperthyroidism to prepare for thyroidectomy or for long term management

Carbimazole is the most commonly used drug

Propylthiouracil in patients sensitive to carbimazole

Both act by interfering with thyroid hormone synthesis

18
Q

Carbimazole

A

Used to treat hyperthyroidism

Pro-drug, converted to active form methimazole which prevents peroxidase iodinating the tyrosine residues so less T3 and T4 production

Oral bioavailability: >90%
Protein binding: 85%
Excretion: 90% in urine as metabolites

19
Q

Carbimazole side effects

A

Rashes and pruritis

Neutropeania

Agranulocytosis

Tetragenic

20
Q

Propylthiouracil

A

Used to threat hyperthyroidism

Inhibits thyroperoxidase and tetraiodothyronine deiodinase so less T4 to T3

Drug of choice in first trimester

Oral bioavailability: 80-95%
Protein binding: 70%
Excretion: renal

21
Q

Propylthiouracil adverse effects

A

Rashes and pruritis

Agranulocytosis

Serious liver injury (liver failure and death)

22
Q

Oestrogens

A

Necessary for development of female secondary sexual characteristics

Stimulate myometrial hypertrophy with endometrial hyperplasia

Natural oestrogens have more appropriate profile for HRT

Oestrogen therapy given cyclically or continuously

23
Q

Hormone replacement therapy

A

Small dose of oestrogen alleviates menopausal symptoms such as vaginal atrophy or vasomotor instability

24
Q

Combined oral contraceptive

A

Mixture of oestrogen and progestogen

Progestogen inhibits ovulation by LH suppression, thickens cervical mucus and renders endometrium hostile

Oestrogen prevents follicular development by suppression of FSH

Oral bioavailability: 40-55% (EE), 65-80% (NOR)
Protein binding: high
Metabolism: hepatic
Excretion: faeces and urine

25
Q

Combined oral contraceptive adverse effects

A

Nausea and vomiting

Abdominal cramps

Fluid retention

Changes in body weight

Hepatic impairment

DVT

Breast tenderness

Cervical erosion

Migraine

26
Q

Progestogen only oral contraceptive

A

e.g. norethisterone, levonorgestrel, desogestrel

Inhibit ovulation by suppression of LH surge, thicken cervical mucus and render the endometrium hostile

Oral bioavailability: 65-80%
Protein binding: high
Excretion: faeces and urine

27
Q

Progestogen only oral contraceptive adverse effects

A

Menstrual irregularity

Nausea and vomiting

Headache

Breast discomfort

Weight changes

Changes in libido

28
Q

Two subtypes of oestrogen receptor

A

ERalpha: hypothalamus, breast, endometrium

ERbeta: bone and brain

29
Q

Selective oestrogen receptor modulator

A

SERM

e.g. raloxifen

Selectively acts on oestrogen receptor of bone and is used to prevent osteoporosis

30
Q

Raloxifen hydrochloride

A

Cautions: VTE, breast cancer, hypertriglyceridaemia

Contraindications: VTE, uterine bleeding, endometrial cancer, hepatic impairment, cholestasis, severe renal impairment, pregnancy and breast feeding

Side effects: VTE, hot flushes, leg cramps, peripheral oedema, influenza like symptoms, GI disturbances, hypertension

31
Q

Tibolone

A

Has oestrogenic, progestogenic and weak androgenic properties

Used in short term treatment of oestrogen deficiency, osteoporosis prophylaxis

Cautions: vaginal bleeding, renal impairment, liver disease, epilepsy, migraine

Contraindications: hormone dependent tumours, CV or cerebrovascular disease

Side effects: abdominal pain, weight changes, vaginal bleeding, facial hair, amnesia

32
Q

Anti-oestrogens

A

e.g. tamoxifen, clomifene

Used in the treatment of fertility due to oligomenorrhoea or secondary amenorrhoea

Induce gonadotrophin by occupying oestrogen receptors in hypothalamus

33
Q

Breast cancer management

A

Surgery, radiotherapy, drug therapy

Tamoxifen effective in premenopausal, perimenopausal and postmenopausal women

34
Q

Gonadotrophin

A

FSH and LH used in treatment of infertility in women with hypopituitarism

Occasionally used in hypogonadotrophic hypogonadism

Contraindications: ovarian cysts, tumours (pituitary, hypothalamus, breast, uterus, ovaries, testes, prostate), vaginal bleeding

Side effects: ovarian hyperstimulation, multiple pregnancies, miscarriage, hypersensitivity reactions, GI disturbances, headaches, joint pain

35
Q

Hypothalamic hormones

A

Gonadorelin leads to rapid rise in plasma LH and FSH

Indicated in endometriosis and infertility and breast and prostate cancer

36
Q

Long term GnRH

A

Suppresses LH and FSH

Stops oestrogen and testosterone

Used in cancers instead of tamoxifen or anti-androgen

203: Theme 1: The Endocrine System (22 decks)

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