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Pharm Hypothalamic and Pituitary Hormones Month 3 Week 1 T3
Pharm Hypothalamic and Pituitary Hormones Month 3 Week 1 T3
44
Medical
Graduate
11/01/2018

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Term
Which anterior pituitary hormone primarily targets breast tissue?
Definition
Prolactin
Term
Which treatment would be most appropriate to treat a hormone-secreting tumor such as carcinoid?
Definition
Octreotide
Term
Hormones
Definition
• Key regulators of metabolism, growth, and reproduction
• Used in the treatment of a variety of endocrine disorders
• Secreted by endocrine glands and transported into circulation
• Exert effects distant from site of excretion
Term
• Most hormones have a specific site of action
Definition
• Hypothalamic hormones act on pituitary to cause release of hormones
• Pituitary hormones act on target tissues such as thyroid, ovary, testis, adrenal cortex
• Growth hormone and thyroid hormones not highly specific because affect most tissues
Term
Hypothalamic-Pituitary System
Definition
• All anterior pituitary hormones except prolactin stimulate production of other hormones by peripheral tissues
• Prolactin and the posterior pituitary hormones act directly on target tissues
Term
Hypothalamic Hormone
Anterior Pituitary Hormone
Target Organ (Associated
Hormones/Mediators)
GH
Definition
Growth hormone-releasing hormone (GHRH) Somatostatin
Growth hormone (GH, somatotropin)
Liver, bone, muscle, kidney, among others
(Insulin-like growth factor-1 (IGF-1))
Term
Hypothalamic Hormone
Anterior Pituitary Hormone
Target Organ (Associated
Hormones/Mediators)
TH
Definition
Thyrotropin-releasing hormone (TRH)
Thyroid-stimulating hormone (TSH)
Thyroid
(Thyroxine, triiodothyronine)
Term
Hypothalamic Hormone
Anterior Pituitary Hormone
Target Organ (Associated
Hormones/Mediators)
CRH
Definition
Corticotropin-releasing hormone (CRH)
Adrenocorticotropin (ACTH)
Adrenal cortex (Cortisol)
Term
Hypothalamic Hormone
Anterior Pituitary Hormone
Target Organ (Associated
Hormones/Mediators)
GnRH
Definition
Gonadotropin-releasing hormone (GnRH)
Follicle-stimulating hormone (FSH)
Luteinizing hormone (LH)
Gonads
(Estrogen, progesterone, testosterone)
Term
Hypothalamic Hormone
Anterior Pituitary Hormone
Target Organ (Associated
Hormones/Mediators)
Dopamine
Definition
Dopamine
Prolactin (PRL)
Breast
Term
Regulatory Hormones
Definition
• Regulate release of other hormones
• Small polypeptides
• Not active orally
• Short-acting when administered intravenously
• Synthetic derivatives relatively easy to produce
Term
Growth Hormone (GH)
Definition
• Required for normal growth during childhood and adolescence
• Important regulator of lipid and carbohydrate metabolism and lean body mass
• Regulates the production of IGF-1 in peripheral tissues to mediate its effects
Term
Somatropin
Definition
- Recombinant human GH
- MOA:acts through GH receptors to increase the production of IGF-1
- Uses:
• GH deficiency in children and adults
• Treatment of children with genetic diseases associated with short stature or with failure to thrive
• AIDS-associated wasting and GH deficiency
• Short bowel syndrome
Term
Somatropin subcutaneous injection ADE
Definition
children:
• Pseudotumor cerebri
• Slipped capital femoral epiphysis
• Progression of scoliosis
• Edema
• Hyperglycemia

adults:
• Peripheral edema • Myalgia
• Arthralgia
Term
Mecasermin
Definition
• Recombinant IGF-1
• MOA: promotes growth (skeletal, cell, and organ) and suppresses liver glucose production, stimulates peripheral glucose utilization, and has an inhibitory effect on insulin secretion
• Use: treatment IGF-1 deficiency unresponsive to exogenous GH
Term
• Adverse effects:
• Hypoglycemia
• Intracranial hypertension • Increased liver enzymes
Definition
Mecasermin
• SC injection
Term
Octreotide
Definition
• Somatostatin analog
• MOA: somatostatin receptor agonist inhibits release of GH, glucagon, insulin, gastrin
• Uses:
-Acromegaly
-Hormone-secreting tumors (e.g., carcinoid)
- Acute control of bleeding from esophageal varices
-SC or IM
Term
• Adverse effects:
• Gastrointestinal disturbances
• Gallstones
• Bradycardia
• Cardiac conduction abnormalities
Definition
Octreotide
Term
Lanreotide
Definition
• Synthetic somatostatin analog
• Similar to octreotide
• SC injection
- Long-acting formulation
- Administered every four weeks
Term
Pegvisomant
Definition
• GH receptor antagonist
• MOA: blocks GH receptor signaling
- Long-acting GH derivative
- Cross-links GH receptors without inducing necessary conformational change for receptor activation
• Use: acromegaly
• SC injection
• Adverse effect: increased liver enzymes
Term
Gonadotropins
Definition
• FSH regulates follicle development in women and spermatogenesis in men.
• LH stimulates testicular androgen production in men.
• FSH and LH help regulate ovarian steroidogenesis in women.
• Gonadotropins are used to stimulate spermatogenesis and induce ovulation.
• Complications of ovulation induction:
- Multiple pregnancies
- Ovarian hyperstimulation syndrome
Term
Ovulation Induction
Definition
1• Inhibition of endogenous gonadotropin production by administration of a GnRH agonist or antagonist
2• Follicle development by agent with FSH activity
3• Oocyte maturation induced with agent with LH activity
Term
Human Chorionic Gonadotropin (HCG)
Definition
• Luteinizing hormone (LH) analog • Urine-derived or recombinant
• MOA: activates LH receptors
• Uses:
- Initiation of final oocyte maturation and ovulation during controlled ovarian stimulation
- Male hypogonadotropic hypogonadism
Term
• Adverse effects:
• Ovarian hyperstimulation syndrome
• Multiple pregnancies in women
• Gynecomastia in men
• Headache
• Depression
• Edema
Definition
-IM injection
Human Chorionic Gonadotropin (HCG)
Term
Follitropin Alfa
Definition
• Recombinant FSH analog
- Follitropin beta: differs in carbohydrate side chain
- Urofollitropin: urine-derived
• MOA: activates FSH receptors
• Uses:
- Controlled ovulation hyperstimulation in women
- Infertility due to hypogonadotropic hypogonadism in men
Term
• Adverse effects:
• Ovarian hyperstimulation syndrome
• Multiple pregnancies in women
• Gynecomastia in men
• Headache
• Depression
• Edema
Definition
Follitropin Alfa
• SC injection
Term
Menotropins
Definition
• Urine-derived mixture of LH and FSH
Term
Leuprolide
Definition
Leuprolide
• MOA:inhibitsgonadotropinreleaseby downregulating GnRH receptors
• Uses:
• Ovarian suppression
• Controlled ovarian stimulation
• Central precocious puberty
• Block of endogenous puberty in some transgender early pubertal adolescents
• Advanced prostate cancer
Term
• Adverse effects:
• Headache
• Light-headedness
• Nausea
• Injection site reactions
• Symptoms of hypogonadism with continuous treatment
Definition
Leuprolide
• Administered IV, SC, IM, or intranasally
• Depot formulations are available
Term
Ganirelix
Definition
• GnRHantagonist
• MOA:suppressesendogenousgonadotropin production by blocking GnRH receptors
• Use:preventionofprematureLHsurgesduring controlled ovarian stimulation
• SCinjection
Term
• Adverse effects:
• Nausea
• Headache
Definition
Ganirelix
Term
Prolactin (PRL)
Definition
• PRL regulates lactation
• Hyperprolactinemia can result in infertility, galactorrhea, and amenorrhea
• Dopamine is a physiologic inhibitor of prolactin release
Term
Bromocriptine
Definition
- MOA: dopamine D2 receptor agonist • Reduces serum prolactin concentrations
- Uses:
• Hyperprolactinemia
• Parkinson’s disease
• High doses can be used in the treatment of acromegaly
Term
• Adverse effects:
• Gastrointestinal disturbances
• Orthostatic hypotension
• Headache
• Psychiatric disturbances
• Vasospasm and pulmonary infiltrates in high
doses
Definition
Bromocriptine
• Administered orally
• For hyperprolactinemia, can be administered vaginally
Term
Vasopressin
Definition
• MOA: increases water reabsorption, thus decreasing urine output (V2 receptors), and increases vasoconstriction (V1 receptors)
• Uses:
• Neurogenic diabetes insipidus
• Bleeding from esophageal varices
Term
• Adverse effects:
• Increased intestinal activity
• Nausea
• Cramps
• Ischemia
Definition
Vasopressin
Term
• ADH analog
• MOA: selective peptide agonist of vasopressin V2 receptors
- Greater antidiuretic effects versus vasopressor activity
• Uses:
- Pituitary diabetes insipidus
- Hemophilia A and von Willebrand disease
Definition
Desmopressin (DDAVP)
Term
• Adverse effects:
• GI disturbances
• Headache
• Hyponatremia
• Allergic reactions
Definition
Desmopressin (DDAVP)
• Long duration of action
• Administered orally, IV, SC, or intranasally
Term
Conivaptan
Definition
• MOA: antagonist of vasopressin V1a and V2 receptors
• Use: hyponatremia in hospitalized patients
• IV infusion
Term
• Adverse effect: infusion site reactions
Definition
Conivaptan
Term
Tolvaptan
Definition
• MOA: vasopressin receptor antagonist • Selective for V2 receptors
• Use: hyponatremia in hospitalized patients • Administered orally
Term
• Adverse effect: hepatotoxicity
Definition
Tolvaptan
Term
Oxytocin
Definition
• 9-amino acid peptide similar to ADH
• MOA: oxytocin receptor agonist • Stimulates uterine contraction
• Uses:
• Induction and augmentation of labor (IV infusion)
• Control of uterine hemorrhage after delivery (IM or IV)
Term
• Adverse effects:
• Fetal distress
• Placental abruption
• Uterine rupture
• Fluid retention
• Hypotension
Definition
Oxytocin
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