Flashcards in Endocrine Drugs Deck (38):
Mention some important features of somatropin?
1. Recombinant form of GH.
2. Used in GH deficiency in children and adults.
3. Genetic diseases : Turner, Noonan, Prader-Willi (short stature).
Mention some rare and serious adverse effects of GH in children?
1. Pseudotumor cerebri
2. Slipped capital femoral epiphysis
3. Progression of scoliosis
6. Monitor for concurrent deficiency of other anterior pituitary hormones.
What are the most important adverse effects of GH in adults?
1. Peripheral edema
Mention some important features of mecasermin?
1. Recombinant human IGF-1.
2. Administered parenterally in children with IGF-1 deficiency.
3. Toxicity : hypoglycemia.
What does somatostatin inhibit?
1. Release of GH
Mention 2 important somatostatin analogs.
What is the clinical use of octreotide and lanreotide?
5. Other endocrine tumors
What are the adverse effects of octreotide and lanreotide?
1. Significant gastrointestinal disturbances
3. Cardiac conduction abnormalities
What is the major dopamine D2 receptor agonist?
Bromocriptine : inhibiting prolactin release.
What is pegvisomant?
1. GH receptor antagonist
2. Treatment of acromegaly
3. Long acting
What are the three basic steps of ovulation induction protocols that use gonadotropins?
1. Endogenous gonadotropin production is inhibited by a GnRH agonist/antagonist.
2. Follicle development is driven by daily injections of a preparation with FSH activity.
3. The final stage of oocyte maturation is induced with an injection of LH or hCG (LH analog).
How are the gonadotropin preparations administered ?
What are the main gonadotropin preparations in use?
1. Menotropins : mixture of FSH and LH purified from postmenopausal urine.
2. FSH and its analogs : urofollitropin - follitropin alpha - follitropin beta.
3. LH and its analogs : hCG - lutropin.
Mention some important GnRH agonists.
What are the adverse effects of treatment with GnRH agonists?
In women :
1. Typical symptoms of menopause : hot flushes, sweats and headache.
2. Long term treatment is avoided for risk of bone loss and osteoporosis.
In men :
1. Hot flushes, sweats and gynecomastia.
2. Reduced libido
3. Decreased hematocrit
4. Reduced bone density
Mention 3 important GnRH antagonists.
Mention 2 oxytocin antagonists.
What is the major ADH agonist?
What is the clinical use of desmopressin?
1. Hemophilia A
2. von Willebrand disease
3. Antidiuretic effects
4. Bleeding from esophageal varices (contracts smooth muscle).
Mention 2 ADH antagonists.
What is the clinical use of thyroid hormone?
1. Levothyroxine (T4)
2. Liothyronine (T3) - faster acting, shorter half-life, more expensive.
What the two major thioamides used as antithyroid drugs?
2. Propylthiouracil (PTU)
What are the principal features of thioamides?
1. Inhibit thyroid hormone synthesis.
2. Blocking of peroxidase-catalyze reactions
3. Blocking of iodination of the tyrosine residues of TG.
4. Blocking of coupling DIT and MIT.
5. Inhibit peripheral conversion of T4 to T3 (mainly PTU).
6. Slow action (3-4 weeks to full potential).
What are the toxic effects of thioamides?
1. Skin rash (common)
2. Severe reactions (rare) - vasculitis, agnulocytosis, hypoprothrombinemia, and liver dysfunction.
What is the main action of iodide salts and iodine?
1. Inhibit iodination of tyrosine .
2. Inhibit thyroid hormone release.
3. Decrease the size and vascularity of the hyperplastic thyroid gland.
What are the usual forms of iodide salts and iodine as antithyroid drugs?
1. Lugol's solution (iodine and K iodide)
2. Saturated solution of potassium iodide
What are the adverse effects of iodide salts and iodine ?
2. Drug fever
3. Metallic taste
4. Bleeding disorders
5. Anaphylactic reactions (rarely)
What anion inhibitors are used as antithyroid drugs?
1. Thiocyanate (SCN-)
2. Perchlorate (CLO4-)
What is the mechanism of action of anion inhibitors?
Block the uptake of iodide by the thyroid gland through competitive inhibition of the iodide transporter.
(Can cause aplastic anemia - so ...rarely used)
Mention some other drugs used in treatment of thyrotoxicosis.
1. β blockers - propranolol.
Mention some synthetic glucocorticoids with function identical to cortisol.
1. Prednisone (and its active metabolite prednisolone)
(Longer half-life, reduced salt retention, better penetration of lipid barriers)
What special glucocorticoid have been developed for use in asthma and other conditions in which good surface activity on mucous membranes or skin is needed and systemic effects are to be avoided?
What is the clinical use of glucocorticoids in adrenal disorders?
1. Chronic adrenal cortical insufficiency (Addison's disease)
2. Acute adrenal insufficiency (shock, infection, trauma)
3. Congenital adrenal hyperplasia (suppression of ACTH)
What is the clinical use of glucocorticoids in nonadrenal disorders?
1. Inflammatory/immunologic disorders (asthma, rheumatic conditions)
2. Hematopoietic cancers
3. Neurologic disorders
4. Chemo-induced vomiting
6. Mountain sickness
7. Betamethasone : hasten maturation of the fetal lungs.
What are the toxic effects of glucocorticoids?
1. Metabolic effects (growth inhibiton, diabetes, muscle wasting, osteoporosis).
2. Salt retention
Besides aldosterone, what other mineralocorticoids are in clinical use?
1. Deoxycorticosterone (precursor of aldosterone)
2. Fludrocortisone : also glucocorticoid activity + long duration - favored for replacement therapy after adrenalectomy.
Mention 3 major corticosteroid receptor antagonists.
3. Mifepristone (RU-486) - competitive inhibitor of glucocorticoid as well as progesterone receptors - Cushing's syndrome.