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Pituitary Flashcards

1
Q

GH MOA

A

Physiologic effects are exerted either directly or mediated through somatomedins (Insulin-like growth factors-IGF-1 and IGF-2)

In acromegaly, IGF-1 levels are consistently high, reflecting elevated GH

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2
Q

Therapeutic uses of GH

A

Congenital/acquired GH deficiency (Dwarfism)
Prader-Willi syndrome

GH deficiency in adults

AIDS related muscle wasting and cachexia

Turner syndrome (to stimulate growth)

Idiopathic short stature (in children)

also approved for treatment of patients with short bowel syndrome (with glutamine)

used by athletes for a purported increase in muscle mass and athletic performance- one of the drugs banned by the Olympic Committee

FDA also approved in 1993 the use of recombinant bovine Growth Hormone (rbGH) in dairy cattle to increase milk production

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3
Q

GH ADR in children

A 
Increased Intracranial tension
Papilledema
Headache
Hypothyroidism*** 
Scoliosis
DM
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4
Q

GH ADR in adults

A 
Peripheral edema
Arthralgia
Myalgia
Carpal tunnel syndrome
DM
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5
Q

GH contraindication

A

Obese patients

Patients with closed epiphyses who do not have GH deficiency

Patients with a known malignancy

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6
Q

Mecasermin

A

recombinant human (rh) IGF-1

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7
Q

Mecasermin approved for the treatment of patients with?

A

GH deficiency with antibodies against GH
severe IGF-1 deficiency that is not responsive to GH
mutations in the GH receptor
primary IGF-1 deficiency

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8
Q

Most common ADR of mecasermin

A

hypoglycemia

take food 20 min before or after administration of the drug

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9
Q

Octerotide

A

a synthetic octapeptide analog of somatostatin

more potency and longer half-life than the natural compound (Somatostatin)

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10
Q

Octerotide used in?

A

treatment of acromegaly and gigantism caused by hormone-secreting tumors, pituitary tumors that secrete thyroid stimulating hormone (thyrotropinoma)

hypersecretory diarrheas associated with tumors producing the vasoactive intestinal peptide (VIPomas), Carcionoid syndrome

useful in acute variceal bleeding

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11
Q

Lanreotide

A

Long acting octreotide

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12
Q

ADR of somatostatin analogs

A

Gi problems
Gall stones
Vit B12 deficiency on long term use

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13
Q

Pegvisomant

A

GH receptor antagonist [recombinant polyethylene glycol (PEG) variant GH (mutant GH)]
acts as an antagonist at GH receptors

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14
Q

Pegvisomant used in?

A

treatment of acromegaly that is refractory to other modes of surgical, radiologic, or pharmacologic intervention

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15
Q

Gonadorelin

A

Short acting GnRH analog

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16
Q

Gonadorelin uses

A

“Pulsatile”manner to stimulate pituitary to secrete FSH and LH; (however, continuous administration inhibits FSH and LH release)

Diagnostic purpose (hypogonadism)
Female infertility: to induce ovulation and treat infertility in women with Hypothalamic amenorrhea
Male infertility

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17
Q

Goserelin, Nadarelin, Leuprolide, Histrelin, Triptorelin

A

Long acting Synthetic GnRH analogue

After initial stimulation, they will cause suppression of gonadotropin (FSH, LH) release.

18
Q

Uses of long acting GnRH

A 
Precocious puberty 
Breast Ca
Prostate Ca 
Uterine leiomyomata (uterine fibroids)
Endometriosis
19
Q

AdR of GnRH analogue

A

gonadorelin: hypersensitivity, dermatitis and headache

In women, the analogs may cause:
hot flushes and sweating
diminished libido, depression and ovarian cysts

20
Q

Ganirelix, Cetrorelix, Abarelix, Degarelix

A

competitive antagonists at GnRH receptors

inhibit the secretion of FSH and LH in a dose-dependent manner

do not cause surge of testosterone or estradiol upon initiation of therapy

approved for preventing the LH surge during controlled ovarian stimulation (for the purpose of assisted reproductive technologies such IVF)

given SC or IM

21
Q

Menotropins

A

Gonadotropin prep:
(human menopausal gonadotropins, hMG) (LH + FSH)- obtained from the urine of menopausal women
.Largely being replaced by recombinant Gonadotropins

22
Q

hCG

A

gonadotropin prep:
Human chorionic gonadotropin) - a placental hormone, has LH like activity
- also excreted in urine and acts as an LH agonist

23
Q

Urofollitropin

A

FSH obtained from menopausal women and is devoid of LH activity

24
Q

Follitropin

A

human FSH manufactured by recombinant DNA technology

25
Gonadotropin prep uses
Infertility Assisted reproductive techniques (ART) Menotropins are used in concert with hCG to stimulate ovulation in women with functioning ovaries hCG can be used both in men and women to stimulate gonadal steroidogenesis in cases of LH insufficiency Cryptorchidism*** (undescended testes) – hCG hCG- can also be used to induce sexual maturation and spermatogenesis in men with secondary hypogonadism (requires months of treatment)
26
Gonadotropin prep ADR
Multiple Births Ovarian enlargement ``` OHSS (ovarian hyper-stimulation syndrome) Hypovolemia Electrolyte imbalance Fluid accumulation (ascites) Acute respiratory distress syndrome Shock ``` Gynecomastia
27
Prolactin releasing factor
Antipyschotics (Chlorpromazine and halopreridol), antidepressants (Imipramine) increase prolactin secretion Drugs that promote prolactin secretion are used to treat lactation failure
28
Prolactin inhibiting factor
Prolactin secretion can be inhibited by a number of dopamine agonists
29
Bromocriptine PIF
acts as an agonist at dopamine D2 receptors
30
Cabergoline PIF
potent D2 agonist - more effective in reducing hyperprolactinemia than bromocriptine
31
Pergolide PIF
nonselective agonist at both D1 and D2 receptors
32
PIF uses
1. Hyperprolactinemia inhibition of prolactin secretion in amenorrhea, galactorrhea, and prolactin-secreting tumors also to correct female infertility secondary to hyperprolactinemia 2. Parkinsonism 3. Acromegaly - dose required is higher than those used to treat hyperprolactinemia 4. To suppress physiologic lactation - to prevent breast engorgement when breast feeding is not desired
33
Oxytocin theraputic uses
for induction and maintenance of labor to control post-partum hemorrhage
34
Oxytocin ADR
Fetal distress, placental abruption and uterine rupture (due to excessive uterine contraction) Fluid retention/water intoxication, leading to heart failure, hyponatremia, seizures and death (due to activation of vasopressin receptors in high concentration); fetal death contraindicated in fetal distress, abnormal fetal presentation, prematurity and CPD (cephalo-pelvic disproportion)
35
Atosiban
Oxytocin antagonist, a nonapeptide Tocolytic agent Used in preterm labor (tocolysis)
36
Vasopressin receptors
V1a*** (vascular smooth muscle) V1b (CNS and adrenal medulla) & V2*** (renal tubules) : coupled to increased cAMP (increased water permeability and reasorption in the collecting tubules) Extrarenal V2 receptors: mediate the release of coagulation factor VIII and Von willebrand factor V1: coupled to increased inositide turnover and increased intracellular Ca2+ vasoconstriction
37
Drugs enhancing ADH secretion
NSAIDs Carbamazepine Vinca alkaloids
38
Drugs inhibiting ADH
Lithium | Demeclocycline
39
Therapeutic uses of vasopressin
Pituitary diabetes insipidus (neurogenic diabetes insipidus)
40
Desmopressin
long acting, vasopressin synthetic analog more ADH action (V2 receptor) and much less vasoconstrictive (V1 receptor) effect (4000:1) extrarenal V2 receptors mediate the release of coagulation factor – von Willebrand factor- hence useful in the treatment of coagulopathy in hemophilia A and von Willebrand’s disease Nasal spray is available for Neurogenic diabetes insipidus Nocturnal Enuresis
41
ADR vasppressin
Water intoxication Hyponatremia Headache, tremor and bronchoconstriction Caution must be used when treating patients with coronary artery disease, epilepsy and asthma
42
Conivaptan, Tolvaptan
ADH antagonists: Conivaptan: approved for use in SIADH Tolvaptan: has a 30-fold higher affinity for V2 than for V1 receptors. Approved by FDA in 2009

PHarm (7 decks)

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