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Endocrinological Pharmacology > 12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones > Flashcards

12. Thyroid and antithyroid drugs. Hypothalamic and pituitary hormones Flashcards

1
Q

Growth hormone analogue

not on the list

A

Somatropin (GH)

Mecasermin (IGF-1)-> recombinant

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2
Q

GH antagonist

A

Somatostatin analogue:
Ocreotide
(Leutrotide)
-inhibtis GH, insulin, glucagon, gastrin release

Receptor antagonist:
(Pegvisomant)

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3
Q

FSH and LH analogues

not on the list

A
  1. follitropin-alpha - recombinant form of FSH
  2. Menotropin -> FSH and LH, infertility men
  3. human chorionic gonadotropin (hCG) -> agonist of LH-receptor
  4. Lutropin -> recombinant LH
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4
Q

GnRH analogue

A

Goserelin
(leuprorelin)

intermittend application: FSH++, LH++
long application: FSH–, LH–

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5
Q

GnRH antagonist

A

Degarelix

Ganirelix

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6
Q

Prolactin

A

Dopamine-Receptor2 agonist:
Bromocriptine
- suppresses PL and GH (less)
(Cabergoline)

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7
Q

controlled ovulation

A
  1. Inhibit endogenous FSH and LH
    GnRH agonist, Goserelin
    or antagonist, degarelix
  2. FSH, follicular development
    (follitropin alpha)
  3. LH, final oocyte development
    (hCG or Lutropin)
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8
Q

Posterior pituitary hormones

A

oxytocin - agonist
oxytocin-receptor antagonist: (Atosiban)

Vasopressin:
V2-agonist: Desmopressin (Centeal diabetes insipidus)
V1+2-agonist: Vasopressin
V1+2-antagonist: (Conivaptan)- Syndrom of inappropriate ADH secretion (SIADH)

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9
Q

Hypothyroidism therapy

A

levothyroxine (T4)

(liothyronine (T3)) -> deionidase enzyme deficiency

Iodine (thyrotoxicosis + dietery insufficiency)

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10
Q

Antithyroid drugs (hyperthyroidism therapy)

A

Thioamines:

  • inhibits thyroid peroxidase+ inhibits deiodinaseenzyme in periphery
    1. Propylthiouracil (PTU), may cause lupus, vasculitis agranulocytosis
    (2. Methimazole) -> (aplasia cutis), teratogenic, lupus, vasculitis agranulocytosis

(thiamazole?)

Iodide salts: 
- inhibits tyrosine iodination+ thyroid hormone release, reduces size and vascularity
(Lugal solution)
(Potassium iodide)
-thyroid storm, thyroidectomy

Radioactive iodine: I131- hyperthyroidism (destruction by radiation)

Anion inhibitors:

  • competitive inhibitors for iodine transport- reduce Iodine uptake
    (1. Thiocyanate)
    (2. Perchlorate)
  • iodine induced Hyperthyroidism

ß-blocker:
inhibit peripheral conversion (deiodinase enzyme)
Propanolol- control thyroid storm , tachycardia, other cardiac abnormalities

Corticosteroids: 
Hydrocortisone
Methylprednisolone
- inhibits deiodinase enzyme
- Thyroid storm
-baselow eyes
-control opthalmopathy
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11
Q

Somatropin (somatotropin)

A

GH analogue

Recombinant form of human GH

  • Subcutaneous injection
  • GH deficiency – dwarfism (genetic, developmental, acquired)
  • Increased final adult height in children with conditions associated with short stature (Prader-Willi syndrome, Turner syndrome)
  • Idiopathic short stature
  • AIDS-associated wasting
  • Malabsorption syndromes in patients who have
    undergone bowel intestinal resection

Side effects:

  1. pseudotumor cerebri,
  2. slipped capital femoral
  3. epiphysis,
  4. edema,
  5. hyperglycemia,
  6. scoliosis,
  7. risk of asphyxia in severely obese patients with Prader-Willi syndrome and upper airway obstruction or sleep apnea
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12
Q

Mecasermin

not on the list

A

GH analogue

Recombinant form of human IGF-1

  • Subcutaneous injection
  • Replacement therapy in IGF-I deficiency
  • Growth retardation in patients not responsive to
    exogenous GH (ex. Laron dwarfism)

Side effects:
hypoglycemia,
intracranial hypertension, increased liver enzymes

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13
Q
  • Octreotide
A

GH release inhibitor

Somatostatin analogues
(- Lantreotide)

Inhibit the release of GH, insulin, glucagon, gastrin

  • Parenteral administration
  • Regular formulation – inject 2-4 times daily
  • Slow-release formulation – inject every 4 w’
  • Acromegaly (pituitary adenoma), gigantism
  • Endocrine tumors (carcinoid, gastrinoma, glucagonoma,
    insulinoma, VIPoma)
  • Control of bleeding from esophageal varices
Side effects: 
GI disturbances, 
steatorrhea (due to impaired pancreatic secretion), 
gall stone, 
cardiac conduction abnormalities
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14
Q

Pegvisomant

not on the list

A

GH receptor antagonist

  • Subcutaneous injections
  • Long-acting
  • Acromegaly

Side effects: increased liver enzymes

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15
Q

Follitropin-α

not on the list

A

Recombinant form of human FSH

  • Parenteral
  • Controlled ovarian stimulation
    (induce follicle development – 2nd stage)
  • Male infertility

Side effects: ovarian hyperstimulation syndrome, multiple pregnancies in women, gynecomastia in men, headache, depression, edema in both sexes

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16
Q

Menotropin

not on the list

A

FSH and LH activity

  • Parenteral
  • Extract of the urine of postmenopausal
    women
  • Male infertility
17
Q

Human chorionic gonadotropin (hCG)

not on the list

A

Agonist of LH receptors

  • Parenteral
  • Controlled ovarian stimulation (3rd stage - oocyte maturation)
  • Male infertility
    Side effects: ovarian hyperstimulation syndrome, headache, depression, edema
18
Q

Lutropin

not on the list

A

Recombinant form of human LH

  • Parenteral
  • Controlled ovarian stimulation (3rd stage - oocyte maturation)
  • Male infertility
    Side effects: ovarian hyperstimulation syndrome, headache, depression, edema
19
Q

Goserelin

Leuprolide

A

Synthetic peptide with GnRH agonist activity

  • Parenteral
  • Long-acting
  • Increased LH and FSH secretion with
    intermittent administration; reduced LH and FSH secretion with prolonged continuous administration
  • Ovarian suppression in women undergoing controlled ovulation induction (1st stage)
  • Ovarian suppression in endometriosis, leiomyoma
  • Central precocious puberty
  • Blockade of endogenous puberty in transgender or
    gender-variant early pubertal adolescents
  • Advanced prostate cancer
Side effects: 
headache, 
nausea, 
injection site reactions, 
symptoms of hypogonadism with continuous treatment
20
Q

Degarelix

Ganirelix

A

GnRH antagonists

  • Parenteral

Degarelix:

  • Advanced prostate cancer

Side effects:
nausea,
headache

Ganirelix:

  • Ovarian suppression in women undergoing controlled ovulation induction (1st stage)

Side effects:
nausea,
headache

Degarelix:

  • Advanced prostate cancer

Side effects:
nausea,
headache

21
Q

Bromocriptine

A

Dopamine D2 receptor agonist
(Cabergoline)

  • Suppresses pituitary secretion of prolactin and GH (to lesser extent)
  • Oral
  • Prolactin-secreting adenoma
  • Acromegaly (effective only in high doses)

Side effects:
GI disturbances,
orthostatic hypotension, headache,
psychiatric disturbances, vasospasm and pulmonary infiltrates in high doses

22
Q

Oxytocin

A

Posterior pituitary hormone

Oxytocin
Mediates uterine contraction via activation of oxytocin receptors (OXTR) – Gq-coupled mechanism

Oxytocin receptor agonist

  • IV
  • Induction and augmentation of labor
  • Control of uterine hemorrhage after delivery
Side effects: 
fetal distress, 
placental abruption, 
uterine rupture, 
fluid retention, 
hypotension
23
Q

Atosiban

A

Oxytocin receptor antagonist

  • IV
  • Not approved in all countries
  • Tocolytic agent (relax uterine contraction, suppress preterm labor)

Side effects:
increased rates of infant death

24
Q

Vasopressin

A

V1, V2 agonist

  • Peptide hormone
  • IV, intranasal, oral, subcutaneous
  • Control bleeding due to esophageal varices or colon diverticula (effect on V1 receptors → vasoconstriction)
  • Central diabetic insipidus (effect on V2 receptors)
25
Q

Desmopressin

A

Selective V2 agonist

  • Synthetic analogue of ADH (peptide)
  • Prolonged half-life and duration of action
    compared to endogenous ADH
  • IV, intranasal, oral, subcutaneous
  • Central diabetic insipidus
  • Hemophilia A – factor VIII deficiency
  • Von-Willebrand disease
Side effects: 
GI disturbances,
headache, 
hyponatremia, 
allergic reaction
26
Q

Conivaptan

not on the list

A

V1, V2 antagonist

  • IV
  • SIADH
  • Offset fluid retention (hyponatremia or heart failure)

Side effects:
infusion site reaction, osmotic demyelination syndrome due to rapid Na+ correction

27
Q

Levothyroxine

A

Levothyroxine (T4)

Synthetic thyroid hormones, used in the management of hypothyroidism.
- Activation of nuclear receptors results in gene expression, RNA formation, protein synthesis and subsequent physiological response

  • Oral, IV
  • Converted to T3 in target cells, liver, kidneys
  • Maximum effect is seen after 6-8 weeks of therapy
  • Hypothyroidism

Side effects:
symptoms of thyroid excess

28
Q

Liothyronine (T3)+

not on the list

A
  • Oral, IV
  • 10X more potent than T4
  • Hypothyroidism; used in case of deiodinase enzyme deficiency (T4 cannot be converted to T3)

Side effects:
symptoms of thyroid excess

29
Q

Iodine

A
  • Essential mineral nutrient, intake with diet
  • Daily requirement 150 μg
  • Iodine salt preparation (KI) for replacement therapy
  • Oral
  • Dietary iodine deficiency (endemic goiter)
  • Thyrotoxicosis crisis (high dose suppresses the gland)

Side effects:
cutaneous and mucus membrane irritation,
allergic reaction,
hypo-/hyper- thyroiditis

30
Q

Propylthiouracil (PTU)

A

Antithyroid drugs
Used in the management of thyroid gland hyperactivity.

Thioamides

  • Inhibit thyroid peroxidase activity
  • Inhibit peripheral conversion of T4 to T3 (deiodinase enzymes)
  • Oral
  • Duration of action 6-8 h’
  • Requires 3-4 weeks for onset of activity (delayed action since the
    release of preformed thyroid hormones is not affected)
  • Hyperthyroidism
  • Used during pregnancy and lactation
Side effects: 
skin rash, 
nausea, 
vasculitis, 
agranulocytosis, 
liver dysfunction, 
hypothyroidism,
drug-induced lupus
31
Q

Methimazole

not on the list

A

Antithyroid drugs
Used in the management of thyroid gland hyperactivity.

Thioamides

  • Inhibit thyroid peroxidase activity
  • Inhibit peripheral conversion of T4 to T3 (deiodinase enzymes)
  • Oral
  • Duration of action 24 h’
  • Requires 3-4 weeks for onset of activity (delayed action since the
    release of preformed thyroid hormones is not affected)
  • No effect on deiodinase enzyme
  • Hyperthyroidism
  • Preferred generally (administered once daily)
Side effects: 
skin rash, 
nausea, 
vasculitis, 
agranulocytosis, 
liver dysfunction, 
hypothyroidism, 
drug-induced lupus, 
teratogenic ('aplasia cutis')
32
Q

Iodide salts

not on the list

A
  • Inhibit tyrosine iodination
  • Inhibit thyroid hormone release
  • Reduce the size and vascularity of hyperplastic thyroid gland

Lugol’s solution
(iodine + potassium iodide)

Potassium iodide
(saturated solution)

  • Oral
  • Onset of action within 2-7 days
  • Effect may be transient (the gland may “escape” the iodide blockage
    after several weeks of treatment)
  • Thyroid storm
  • Preparation for surgical thyroidectomy
  • Toxicity is generally rare
33
Q

Radioactive iodine

not on the list

A
  • Radiation-induced destruction of thyroid parenchyma

I131

  • Oral
  • Not to be used during pregnancy and lactation
  • Hyperthyroidism

Side effects:
pharyngitis,
hypothyroidism

34
Q

Anion inhibitors

A
  • Competitive inhibitors of iodide transporter – reduce the uptake of iodide by the thyroid gland

Thiocyanate (SCN-)
Perchlorate (ClO4-)

  • Unpredictable effect
  • Rarely used clinically
  • Iodide-induced hyperthyroidism

Side effects: aplastic anemia

35
Q

β-blockers

A
  • Inhibit peripheral conversion of T4 to T3 (deiodinase enzymes)
  • Control the tachycardia and other cardiac abnormalities of severe thyrotoxicosis

Propranolol

  • Oral
  • Rapid onset of activity
  • Thyroid storm
Side effects: 
bronchospasm, 
AV block, 
hypotension, 
bradycardia
36
Q

Corticosteroids

A
  • Inhibit peripheral conversion of T4 to T3 (deiodinase enzymes)
  • Control thyroid ophthalmopathy (seen with Graves’ disease)

Hydrocortisone Methylprednisolone

  • Oral or parenteral
  • Moderate to severe thyroid ophthalmopathy
  • Thyroid storm
37
Q

Thyrotoxic crisis (thyroid storm)

A 
Rare condition, presents as a life-threatening exacerbation of hyperthyroidism,
accompanied by:
1. fever, 
2. delirium, 
3. seizures, 
4. coma, 
5. vomiting, 
6. diarrhea, and 
7. jaundice.

Mortality rate due to cardiac failure, arrhythmia, or hyperthermia is as high as 30%, even with treatment.

Thyrotoxic crisis is usually precipitated by acute illness (stroke, infection, trauma, diabetic ketoacidosis), surgery (especially on the thyroid), or radioiodine treatment of a patient with partially treated or untreated hyperthyroidism.

Management:

  • PTU or methimazole (IV bolus, high dose)
  • Potassium-iodide solution (IV)
  • β-blockers to control tachycardia and adrenergic symptoms (IV)
  • Glucocorticoids to control ophthalmopathy (IV)

1st line:
Propanolol
Propylthiouracil or methimazole
hydrocortisone

2nd line
Potassium-iodide solution (IV), Lugol solution or sodium iodide
Lithium carbonate
L-Carnitine

support therapy:

  • depolarising electrolyte solution
  • Paracetamol
  • Phenobarbital
  • Furosemide and ACE-inhibitors in case of cardiac failure

selected cases:

  • assisted mechanical ventilation case of hypoxemia
  • cooled mattresses and cold blankets in case of hyperthermia (if body temperature > 40°C)
38
Q

Myxedema coma

A

Rare condition, life-threatening exacerbation of hypothyroidism.

Presentation:

  • Hypothermia
  • Hypoglycemia
  • Hypotension
  • Altered mental status

Management:

  • Thyroid hormones (IV)
  • Glucocorticoids (pituitary-adrenal axis is impaired in severe hypothyroidism)
  • Supportive management
  • Elimination of triggering event (if possible)

Endocrinological Pharmacology (6 decks)

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