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16 Cards in this Set

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Somatotropin
Growth Hormone Analog

Mechanism of Action:*Single GH molecule dimerizes 2 surface JAK/STAT cytokine receptors --> ↑ IGF-1 which mediates growth stimulating effects

Adverse reaction:*Children --> less adverse effects than adults, hypothyroidism, pancreatitis, gynecomastia, nevus growth, intracranial hypertension *Adults --> peripheral edema, myalgias, arthralgias, carpal tunnel syndrome, ↑ P450 *Contraindicated in malignancy

Clinical Use:*Growth failure in children --> GH deficiency, Praderwilli syndrome, Turner Syndrome, Chronic renal failure, idiopathic short stature *Patient with AIDS *Short bowel syndrome
Somatrem
Growth Hormone Analog

Mechanism of Action:*Single GH molecule dimerizes 2 surface JAK/STAT cytokine receptors --> ↑ IGF-1 which mediates growth stimulating effects

Adverse reaction:*Children --> less adverse effects than adults, hypothyroidism, pancreatitis, gynecomastia, nevus growth, intracranial hypertension *Adults --> peripheral edema, myalgias, arthralgias, carpal tunnel syndrome, ↑ P450 *Contraindicated in malignancy

Clinical Use:*Growth failure in children --> GH deficiency, Praderwilli syndrome, Turner Syndrome, Chronic renal failure, idiopathic short stature *Patient with AIDS *Short bowel syndrome
Octreotide
Growth Hormone Antagonist

Mechanism of action:*Binds to SSTR2 and SSTR5 receptors --> ↓ adenylate cyclase and cAMP --> ↓ GH release *Somatostatin analog 45X more potent than somatatostatin in inhibiting GH release *2X more potent than somatostatin in reducing insulin secretion

Adverse Reaction:*nausea, vomiting, abdominal pain *sinus bradycardia *gallstones (↓ gall bladder contraction and GI transit time)

Clinical Use:*GH excess
Bromocriptine
Prolactin Antagonist

Mechanism of action:*D2 receptor agonists --> ↓ prolactin secretion from anterior pituitary *small tumor --> therapy discontinued during pregnancy *Large tumor --> therapy continued throughout pregnancy

Adverse Reaction:*orthostatic hypotension, fatigue

Clinical Use:*Hyperprolactenemia *Parkinson’s *Acromegaly
Pergolide
Prolactin Antagonist

Mechanism of action:*D2 receptor agonists --> ↓ prolactin secretion from anterior pituitary *small tumor --> therapy discontinued during pregnancy *Large tumor --> therapy continued throughout pregnancy

Adverse Reaction:*orthostatic hypotension, fatigue

Clinical Use:*Hyperprolactenemia *Parkinson’s *Acromegaly
Follitropin
FSH Analog

Mechanism of action:*Recombinant FSH

Adverse Reaction:*Multiple birth *gynecomastia *Ovarian hyperstimulation syndrome --> Ovarian enlargement, hemoperitoneum from ruptured ovarian cyst, Hypovolemia, Electrolyte abnormaities, Thromboembolic events, Hepatic dysfunction, Abdominal pain, ARDS

Clinical Use:*anovulation caused by hypogonadotropic hypogonadism and polycystic ovary syndrome *Male infertility
Lutropin
LH Analog

Mechanism of action:*Recombinant LH used only in combination with follitropin alpha

Adverse Reaction:*Multiple birth *gynecomastia *Ovarian hyperstimulation syndrome --> Ovarian enlargement, hemoperitoneum from ruptured ovarian cyst, Hypovolemia, Electrolyte abnormaities, Thromboembolic events, Hepatic dysfunction, Abdominal pain, ARDS

Clinical Use:*anovulation caused by hypogonadotropic hypogonadism and polycystic ovary syndrome *Male infertility
hCG
LH Analog

Mechanism of action: LH analog

Adverse Reaction:*Multiple birth *gynecomastia *Ovarian hyperstimulation syndrome --> Ovarian enlargement, hemoperitoneum from ruptured ovarian cyst, Hypovolemia, Electrolyte abnormaities, Thromboembolic events, Hepatic dysfunction, Abdominal pain, ARDS

Clinical Use:*anovulation caused by hypogonadotropic hypogonadism and polycystic ovary syndrome *Male infertility
Gonadorelin
Synthetic Gonadotropin-releasing hormone

Mechanism of action:*Pulsatile GnRH secretion --> stimulates release of FSH and LH
*Sustained, non-pulsatiles administration of GnRH inhibits release of gonadotropin

Adverse Reaction:*Menopause *Ovarian cysts *osteoporosis *Headache,dizziness, nausea

Clinical Use:*Treatment of infertinilty (Pulsatile administration) --> precipitate LH surge and ovulation in infertile women undergoing ovulation induction with gonadotropins *Infertility in men with hypothalamic-hypogonadotropic hypogonatism *Suppression of gonadotropin release (Non-pulsatiles administration) --> 1.Hormonally responsive tumor:prostate, breast and ovarian cancer. 2.Endometriosis: use less than 6 months to protect bone density 3.Uterine leiomyomata (uterine fibroids) 4.Central precious puberty 5. Controlled ovarian hyperstimulation
Goserelin
Gonadotropin-releasing hormone analog

Mechanism of action:*Pulsatile GnRH secretion --> stimulates release of FSH and LH
*Sustained, non-pulsatiles administration of GnRH inhibits release of gonadotropin

Adverse Reaction:*Menopause *Ovarian cysts *osteoporosis *Headache,dizziness, nausea

Clinical Use:*Treatment of infertinilty (Pulsatile administration) --> precipitate LH surge and ovulation in infertile women undergoing ovulation induction with gonadotropins *Infertility in men with hypothalamic-hypogonadotropic hypogonatism *Suppression of gonadotropin release (Non-pulsatiles administration) --> 1.Hormonally responsive tumor:prostate, breast and ovarian cancer. 2.Endometriosis: use less than 6 months to protect bone density 3.Uterine leiomyomata (uterine fibroids) 4.Central precious puberty 5. Controlled ovarian hyperstimulation
Leuprolide
Gonadotropin-releasing hormone analog

Mechanism of action:*Pulsatile GnRH secretion --> stimulates release of FSH and LH
*Sustained, non-pulsatiles administration of GnRH inhibits release of gonadotropin

Adverse Reaction:*Menopause *Ovarian cysts *osteoporosis *Headache,dizziness, nausea

Clinical Use:*Treatment of infertinilty (Pulsatile administration) --> precipitate LH surge and ovulation in infertile women undergoing ovulation induction with gonadotropins *Infertility in men with hypothalamic-hypogonadotropic hypogonatism *Suppression of gonadotropin release (Non-pulsatiles administration) --> 1.Hormonally responsive tumor:prostate, breast and ovarian cancer. 2.Endometriosis: use less than 6 months to protect bone density 3.Uterine leiomyomata (uterine fibroids) 4.Central precious puberty 5. Controlled ovarian hyperstimulation
Cetrorelix
Gonadotropin-releasing hormone antagonist

Mechanism of action:*GnRH antagonist *Advantages over GnRH agonist --> immediate effect, shorter duration, lower risk of Ovarian hyperstimulation syndrome

Adverse Reaction:

Clinical Use:*Prevent LH surge during controlled ovarian hyperstimulation
Ganirelix
Gonadotropin-releasing hormone antagonist

Mechanism of action:*GnRH antagonist *Advantages over GnRH agonist --> immediate effect, shorter duration, lower risk of Ovarian hyperstimulation syndrome

Adverse Reaction:

Clinical Use:*Prevent LH surge during controlled ovarian hyperstimulation
Oxytocin
Mechanism of action:*Stimulates uterine contraction via Gq receptor pathway --> activates PCL-IP3-Ca -->↑ local prostaglandin production

Adverse Reaction:*uncommon *Excessive stimulation of uterus --> uterine rupture, placenta abruption, fetal death *activation of ADH receptors --> hypertensive crisis and H20 retention

Clinical Use:*Induce labor *Control post-partum uterine bleeding
Desmopressin
Mechanism of action:*Long-lasting ADH analogy 4000X greater antidiuretic/pressor ratio --> Binds V2 >>>> V1

Adverse Reaction:*H20 intoxication *hyponatremia

Clinical Use:*Central diabetes insipidus *nocturnal enuresis *coagulopathy in hemophilia A and von Willebrand’s disease
Vasopressin
Mechanism of action:*Binds V1receptor --> vasoconstriction *Bind V2 receptor --> water resorption in collecting tubules

Adverse Reaction:* H20 intoxication *hyponatremia *seizures *Caution in CAD patients

Clinical Use:*3rd line drugs for shock *Bleeding due to esophageal varices or colonic diverticula