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PHarm > Pituitary > Flashcards

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
Q

Gonadotropin prep uses

A

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
Q

Gonadotropin prep ADR

A

Multiple Births

Ovarian enlargement

OHSS (ovarian hyper-stimulation syndrome)
Hypovolemia
Electrolyte imbalance
Fluid accumulation (ascites)
Acute respiratory distress syndrome
Shock

Gynecomastia

27
Q

Prolactin releasing factor

A

Antipyschotics (Chlorpromazine and halopreridol), antidepressants (Imipramine) increase prolactin secretion

Drugs that promote prolactin secretion are used to treat lactation failure

28
Q

Prolactin inhibiting factor

A

Prolactin secretion can be inhibited by a number of dopamine agonists

29
Q

Bromocriptine PIF

A

acts as an agonist at dopamine D2 receptors

30
Q

Cabergoline PIF

A

potent D2 agonist - more effective in reducing hyperprolactinemia than bromocriptine

31
Q

Pergolide PIF

A

nonselective agonist at both D1 and D2 receptors

32
Q

PIF uses

A
  1. Hyperprolactinemia
    inhibition of prolactin secretion in amenorrhea, galactorrhea, and prolactin-secreting tumors

also to correct female infertility secondary to hyperprolactinemia

  1. Parkinsonism
  2. Acromegaly
    - dose required is higher than those used to treat hyperprolactinemia
  3. To suppress physiologic lactation
    - to prevent breast engorgement when breast feeding is not desired
33
Q

Oxytocin theraputic uses

A

for induction and maintenance of labor

to control post-partum hemorrhage

34
Q

Oxytocin ADR

A

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
Q

Atosiban

A

Oxytocin antagonist, a nonapeptide

Tocolytic agent

Used in preterm labor (tocolysis)

36
Q

Vasopressin receptors

A

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
Q

Drugs enhancing ADH secretion

A

NSAIDs
Carbamazepine
Vinca alkaloids

38
Q

Drugs inhibiting ADH

A

Lithium

Demeclocycline

39
Q

Therapeutic uses of vasopressin

A

Pituitary diabetes insipidus (neurogenic diabetes insipidus)

40
Q

Desmopressin

A

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
Q

ADR vasppressin

A

Water intoxication
Hyponatremia
Headache, tremor and bronchoconstriction

Caution must be used when treating patients with coronary artery disease, epilepsy and asthma

42
Q

Conivaptan, Tolvaptan

A

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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