Endocrine drugs Flashcards
Drug that is purified from the urine of postmenopausal women and is used to promote spermatogenesis
Urofollitropin
A 3 year old boy with failure to thrive and metabolic disturbance was found to have an inactivating mutation in the gene that encodes the growth hormone receptor. Which drug will most likely improve his metabolic function and promote its growth
Mecasermin
- a combiantion of recombinant IGF-1 and the binding protein that protects IGF-1 from immediate destruction
An important difference between leuprolide and ganirelix is that ganirelix _____
immediately reduces gonadotropin secretion
- Leuprolide
- agonist of GnRH receptors
- about 1 week of sustained activity
- Ganirelix
- GnRH antagonist
used to treat the amenorrhea-galctorrhea syndrome
Bromocriptine
- dopamine receptor agonist
- drug should not be used in patients with a history of schizophrenia or other forms of psychotic illness
Patient is a known case of turner syndrome. Which drug will allow her to achive a higher adult height
Somatropin
- recombinant human GH
- Turner syndrome or chronic renal failure
- ACTH
- used in diagnosisng adrenal insuffciency
- CRH
- distringuish cushing’s syndrome from ectopic ACTH secretion
Most appropriate drug to treat precocius puberty
Leuprolide
- GnRH agonist
Pharmacologic treatment for acromegaly
Octreotide
- somatostatin analog. has some efficacy in reducing the excess GH production
The 2nd step in ovulation induction is the administration of a drug with FSH activity.
Follitropin
- Recombinant FSH
- hCG - LH analog
treatment for pituitary diabetes insipidus
Desmopressin
- V2 receptor
Somatropin
Recombinant human GH. Actis through GH receptors to icnrease the production of IGF-1
Replacement in GH deficienct. Icnreased final adult height in children with certain conditions associated with short stature. Wasting in HIV infection. Short bowel syndrome
SQ injection
SE: In children, pseudotumor cerebri, slipped capital femoral epiphysis, progression of scoliosis, edema ,and hyperglycemia. In Adults, peripheral edema, myalgia,and arthralgias. Risk os asphyxia in severely obese patients with Prader Willi syndrome and upper airway obstruction or sleep apnea
Mecasermin
IGF-1 agonist
Replacement of IGF-1 deficiency that is not responsive to exogenous GH
SQ injection
SE: hypoglycemia, intracranial hypertension, increased liver enzymes
Octreotide
Lantreotide: long acting formulation for Acromegaly
Somatostanin receptor agonist
Used in Acromegaly an several other homone secreting tumors. Acute control of bleeding from esophageal varices
SC or IV injection. Long acting formualtion injected IM
SE: GI disturbances, galsstone, bradycardia, cardiac conduction anomalies
Pegvisomant
Blocks GH receptor signalling
USed in acromegaly
SC injection
Increased liver enzymes
Follitropin alfa
FSH receptor agonist
Used in controlled ovulation hyperstimualtion in women. Infertility due to hypogonadotropic hypogonadism in men
SC injection
SE: ovarian hyperstimulation syndrome and multiple pregnancies in women. Gynecomastia in men. Headache, depression, edema, in both sexe
Recombinant product with the same peptide sequence as follitropin alfa but differs in its carbohydrate side chains
Follitropin beta
Human FSH purified from the urine of postmenopausal women
Urofollitropin
Extract of the urine of postmenopausal women; contains both FSH and LH activity
Menotropins (hMG)
hCG
LH receptor agonist
Initiation of final oocyte maturation and ovulation during controlled ovarian stimulation. Male hypogonadotropic hypogonadism
IM or SC injection
SE: ovarian hyperstimualtion syndrome, multiple pregnancies in women. Gynecomastia in men, headache, depression, edema in both sexes
Recombinant fom of hCG
choriogonadotropin alfa
Recombinant form of human LH
Lutropin
Leuprolide
GnRH receptor agonist
Used in ovarian suppresion. Controlled ovarian stimulation. Central precocious puberty in some transgender early pubertal adolescents. Advanced prostate cancer
Adminsitered IV, SC, IM, or intranasally. Depot formulations are available
SE: headache, light headedness, nausea, injection site reactions, with continuous treatment symptoms of hypogonadism
Synthetic human GnRH
Gonadorelin
Ganirelix
Antagonist of GnRH receptors
Prevention of premature LH surges during controlled ovarian stimualtion
SC injection
SE: nausea and vomiting
GnRH receptor antagonists approved for prostate cancer
Degarelix, abarelix
Bromocriptine
Dopaine D2 receptor agonist
Used in hyperprolactinemia, Parkinson’s disease
Administered orally or for hyperprolactemia, vaginally
SE; GI disturbances, orthostatic hypotention, headache, psychiatric disturbances, vasopasm and pulmonary infiltrates in high doses
OXytocin
Oxytocin receptor agonist
Used in induction and augmentation of labor. Control of uterine hemorrhage after delivery
IV infusion
SE: fetal distress, placental abruption, uterine rupture, fluid retetion, hypotension
Atosiban
Antagonist of oxytocin receptor
Tocolysis for preterm labor.
IV infusion
SE: concern about rates of infant death. not FDA approved
Desmopressin
Agonist of vasopressin V2 receptors
used in pituitary diabetes insipidus. Hemophilia A and vWF
Oral, IV, SC, or intranasal adminsitration
SE: GI disturbances, headache, hyponatremia, allergic reactions
Used in treatment of DI and sometimes used to control bleeding from esophageal varices?
Vasopressin
Conivaptan
Antagonist of vasopressin V1a and V2 receptors
used in hyponatremia in hospitalized patients.
Administered as an IV infusion
Infusion site reactions
- Tolvaptan - silimar but more selective for V2 receptors; oral administration limited to 30 day treatment due to hepatoxicity
In grave’s disease, the cause of the hyperthyroidism is the production of an antibody that ___________
Activatesthe thyroid gland TSH receptor and stimulates thyroid hormone synthesis and release
Methimazole reduces serum concentration of T3 by primarily ____________
Preventing the addition of iodine to tyrosine residues on thyroglobulin
A rare but serious toxicity associated with the thioamides
Agranulocytosis
A 56 year old woman presented to the emergency deparment with tachycardia, shortness of breath, and chest pain. She had shortness of breath and diarrhea for the last 2 days and was sweating and anxious. a relative reported that the patient had run out of methimazole 2 weeks earlier. The diagnosisof thyroid storm was made. What drug that is sueful adjuvant in the treatment of thyroid storm?
Propanolol
What drug can be administered for 10-14 days before surgery to reduce the vasuclarity of the thyroid gland?
Lugol’s solution
When initiating T4 therapy for an elderly patient with long standing hypothyroidism, it is important to begin with small dosesto avoid ______
overstimulating of the heart
What hormone is produced in the peripheral tissues when levothyroxine is administered??
T3
A 62 year old woman presents with complaints of fatigue sluggishness and weight gain. She needs to nap several times. She has been taking T4 for the past 15 years without significant problem regarding her energy level. Her recent history is significant of arrythmia and she is currently taking an anti arrythmic drug. What is the most likely cause of her current situation?
Amiodarone
A 25 year old woman presents with insomnia and fears she may habe something wrong with her heart. She describes her heart jumping out of her chest. She feel healthy otherwise and reports she has lots of energy. Lab tests confirms hyperthyroidism. What drug that produces permanent reduction activity?
131I
Thyroid preparations
(Levothyroxine, Liothyronine)
Activation of nuclear receptors results in gene expression with RNA formulation and protein synthesis.
Hypothyroidism
MAximum effect seen after 6-8 weeks of therapy. T4 is converted to T3 in target cells, the liver and the kidneys. T3 is 10x more potent than T4
Thiomides
(PTU, methimazole)
Inhibit thyroid peroxidase reactions, iodine organification and peripheral conversion of T4 to T3
Hyperthyroidism
Oral administration, delayed onset of activity
SE: nausea, GI disturbancs, rash, agranulocytosis, hepatitis (PTU-warning). hypothyroidism
Lugol’s solution, potassium iodide
Inhibit iodine organification and hormone release. Reduce size and vascularity of thyroid gland
Preparation for surgical thyroidectomy
Oral adminsitration, acute onset of activity within 2-7 days
Radioactive Iodine
Radiation-induced destruction of thyroid parenchyma
Used in hyperthyroidism. Patient should be euthyroid or on B-blockers before RAI. Avoid in pregnancy and in nursing mothers
Oral adminsitration
SE: sore throat, hypothyroidism
Beta blockers
(Propanolol, other beta blcokers lacking partial agonist activity)
Inhibition of B receptors; Inhibition of conversion of T4 to T3(propanolol only)
Used in thyroid storm. adjunct to control tachycardia, hypertension, and atrial fibrillation
Rapid onset of activity
SE: asthma, AV blockade, hypotension, bradycardia
What is the pharmacologic effect of exogenous glucocorticoids in asthma?
Inhibition of leukotriene synthesis
One of the adverse metabolic effects of long term glucocorticoid therapy is the ______ of bone, which can result to ________
Net loss
Osteoporosis
A patient is a known case of cushing’s syndrome due to adrenal tumor. What drug woul be expected to reduce the signs and symptoms of the patient?
Ketoconazole
- Inhibits many types of cytochrome P450
- reduce the unregulated overproduction of corticosteroids by adrenal tumors
Describes the therapeutic effect of glucocorticoid administration in patients with 21a-hydroxylase activity
Suppresion of ACTH secretion
Describes a glucocorticoid response element
A specific nucleotide sequence that is recognized by steroid hormone receptor-hormone complex
Gradual tapering of a glucocorticoid is required for recovery of _________
The hypothalamic-pituitary-adrenal system
Most pont antiinflammatory steroid?
Dexamethasone
a 54 year old man has developed signs of severe acute adrenal insufficiency. The patient should be treated immediately with this combination
Cortisol and fludrocortisone
Drug that in high doses blocks the glucocorticoid receptor
Mifepristone
- Competitive antagonist of glucocorticoid and progesterone receptors
Prednisone
Activation of glucocorticoid receptor alters gene transcription
Used in may inflammatory conditions, organ transplantation, hematologic cancers
Druration of activity is longer than pharmacokinetic half life of drug owing to gene transcription effects
SE: adrenal suppression, growth inhibtion, muscle wasting, osteoporosis, salt retention, glucose intolerance, behavioral changes