202 ES - Disease & Pharmacology Flashcards
Drugs used in pituitary disorder
Gonadotropin-releasing hormone (GnRH) analogues - Buserelin
Somatostatin analogues - Octreotide
Prolactin inhibitors - Bromocriptine
Growth hormone
Adenocorticoptropic hormone (ACTH) - Corticotropin
Vasopressin and analogues - Desmopressin
Gonadotropin-releasing hormone (GnRH) analogues
pituitary disorder
Buserelin
- stimulate FSH & LH
Somatostatin analogues
pituitary disorder
Octreotide
Lanreotide
Pariteotide
- inhibit pathologically increased secretion of GH
Treatments for acromegaly
Radiation therapy
Somatostatin analogue
- if not work → pituitary-directed medical therapy - Pegvisomant
Acromegaly
Excess GH
Prolactin inhibitors
pituitary disorder
Bromocriptine
Cabergoline
Qionagolide
- inhibit secretion of prolactin
Adrenocorticotropic hormone (ACTH) (pituitary disorder)
Corticotropin
- abandoned
Vasopressin and analogues
pituitary disorder
Desmopressin
Vasopressin
Terliopressin
- sm vasoconstriction
Drugs used in thyroid & parathyroid disorders
Thyroid Hormone Replacements - Levothyroxine (synthetic T4), Liothyronine (T3)
Thyroid Hormone Suppression - Thioamides - Carbimazole
Thyroid Hormone Replacements
thyroid & parathyroid disorders
Levothyroxine (synthetic T4)
Liothyronine (T3)
- converted to T3 which enters the nucleus and binds to a thyroid hormone receptor.
Thyroid Hormone Suppression
thyroid & parathyroid disorders
Thioamides:
- Carbimazole
- Methimazole
- Propylthiouracil
- Reduces the synthesis of thyroid hormones by inhibiting thyroperoxidase
Can radioactive iodine be used in pregnancy?
RAI is contraindicated in pregnancy & breastfeeding
Drugs for bone metabolism disorders
Antiresorptive drugs - Bisphosphonates, SERMs, Calcitonin, mAb
Anabolic Agents - Recombinant form of parathyroid hormone - teriparatide
Vitamin D Preparations - Ergocalciferol
Bisphosphonates
bone metabolism disorders
Alendronate
- anchor to cell surface proteins on osteoclast membrane by prenylation
Selective estrogen receptor modulators (SERMs)
bone metabolism disorders
Raloxifene
- inhibits cytokines that recruit osteoclasts
Calcitonin
bone metabolism disorders
Lowers blood calcium by:
Inhibits bone resorption by binding to a specific receptor on osteoclasts, inhibiting their action
Denosumab
bone metabolism disorders
Antiresorptive - mAb
IgG2 that inhibits RANKL - primary signal for bone resorption
Recombinant form of parathyroid hormone
bone metabolism disorders
Teriparatide
- Stimulation of new bone formation by direct effects on osteoblasts
Vitamin D preparations
bone metabolism disorders
Ergocalciferol
Alfacalcidol
Calcitriol
- act on receptors belonging to the steroid superfamily of receptors to increase serum calcium
Drugs used in adrenal disorders
Mineralocorticoid agonists (for Addison’s disease) & antagonists - fludrocortisone
Adrenal Hormone Replacement - Glucocorticoids
Adrenal Hormone suppression (Cushing’s syndrome) - adrenolytic agents, adrenal steroid inhibitors, glucocorticoid receptor (& progesterone receptor) antagonist
Fludrocortisone
adrenal disorders
Mineralocorticoid agonists
MOA: Mineralocorticoids interact with intracellular receptors in the kidney controlling transcription of specific genes that cause: ↑ number of Na+ channels, ↑ number of Na+ pumps.
Spironolactone
adrenal disorders
Mineralocorticoid antagonists
MOA: Competitive antagonist of aldosterone
Glucocorticoid
adrenal disorders
interact with intracellular receptors to inhibit the transcription of specific genes that code for various cytokines esp. IL-2.
Adrenal hormone replacement therapy (2)
Glucocorticoid Replacement therapy - hydrocortisone
Mineralocorticoid replacement therapy - fludrocortisone
Surgical intervention of Cushing’s syndrome
Transsphenoidal Selective Adenomectomy
Adrenalectomy - unilateral & total bilateral
Adrenolytic agents
adrenal disorders
Mitotane
- inhibits 11-beta hydroxylase & cholesterol side-chain cleavage enzymes
Adrenal steroid inhibitors
adrenal disorders
Metyrapone
Ketoconazole
Etomidate
Aminoglutethimide
Glucocorticoid receptor (& progesterone receptor) antagonist (adrenal disorders)
Mifepristone
- completely binds to glucocorticoid & progesterone receptors at high doses
What are neuroendocrine tumors (NETs)?
Rare tumors that occur in neuroendocrine cells in various organs
Can be malignant or benign
Functioning vs. non-functioning NETs
Functioning - secretes biogenic amines or hormones
Secretory but non-functioning - secretes peptides but cause no clinical symptoms
Non-functioning - non-secretory
Carcinoid syndrome
Develops when carcinoid tumor metastasize to liver & liver function is compromised
Types of NETs
GIT - 50%
- stomach
- small & large intestines
- pancreas
Lungs - 20%
Others
- skin
- prostate
- uterus
Most common origin of carcinoid tumors
Small & large intestines
Carcinoid tumor causes: ↑ histamine ↑ bradykinin
Which leads to?
Symptoms of carcinoid syndrome:
→ Vasodilation
Symptom: flushing itching
Carcinoid tumor causes: ↑ serotonin
Which leads to? (3)
Symptoms of carcinoid syndrome:
→ Fibrosis
Symptom: Pulmonary stenosis, tricuspid regurgitation
→ Bronchoconstriction
Symptom: Asthma, shortness of breath, wheezing
→ ↓ tryptophan → ↓ niacin (Vitamin B3)
Symptoms: Pellagra
Complications of carcinoid syndrome
Carcinoid heart disease
Carcinoid crisis
Bowel obstruction
Carcinoid heart disease
Thickening of heart valves may lead to leaking
Carcinoid crisis
Causes severe episodes of flushing, low bp, confusion & breathing difficulty
Bowel obstruction
Cancer that spreads to lymph nodes next to small intestine may cause narrowing & kinking of intestine
How to screen for carcinoid tumors?
Octreoscan
- Carcinoid tumors express more somatostatin receptors
Octreoscan can be used to image tumors that express an increased amount of somatostatin receptors
Pancreas NET arise from ______ cells.
Endocrine
Types of functional PanNETs
Insulinoma Gastrinoma VIPoma Glucagonoma Somatostatinoma
What is the most common type of PanNETs?
Insulinoma
- arise from β cells
- secrete insulin
- usually benign
- can cause hypoglycemia