Hypothalamic/Pituitary Hormones Flashcards

1
Q

Synthetic GHRH- Available Drugs

A

Sermorelin

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2
Q

Recombinant GH- Available Drugs

A

Somatropin

Somatrem

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3
Q

Recombinant GH: Somatropin, Somatrem- Mech of Action

A

Replace GH

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4
Q

Recombinant GH: Somatropin, Somatrem- Clinical Use

A
GROWTH FAILURE IN CHILDREN ASSOCIATED WITH:
GH deficiency
chronic renal failure
Prader-Willi syndrome
Turner syndrome
idiopathic short stature
small-for-gestational age condition

GH deficiency in adults, wasting in AIDS patients, patients with short-bowel syndromes

Controversially used for anti-aging or by athletes

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5
Q

Recombinant GH: Somatropin, Somatrem- Adverse Effects/Contraindications

A
leukemia
rapid growth of melanocytic lesions
hypothyroidism
insulin resistance
arthralgia

Contraindicated in pediatric patients with closed epiphyses, active underlying intracranial lesion or malignancy, proliferative diabetic retinopathy.

Caution in diabetes.

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6
Q

Recombinant GH: Somatropin, Somatrem- Drug Rxns

A

inducer of Cyp450

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7
Q

Recombinant IGF-1- Available Drugs

A

Mecasermin

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8
Q

Recombinant IGF1: Mecasermin- Clinical Use

A

children where IGF1 deficiency is due to mutations of GH receptor- Laron Dwarfism or the development of ant GH antibodies

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9
Q

Somatostatin Analogues- Available Drugs

A

OCTREOTIDE

Lanreotide

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10
Q

Somatostatin Analogues: OCTREOTIDE, Lanreotide- Mech of Action

A

inhibit GH release

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11
Q

Somatostatin Analogues: OCTREOTIDE, Lanreotide- Elimination

A

long lasting compared to natural Somatostatin

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12
Q

Somatostatin Analogues: OCTREOTIDE, Lanreotide- Clinical Use

A

to control pituitary adenoma growth in Acromegaly, reduction of symptoms in Carcinoid crisis & VIP-secreting tumors, to control acute GI bleeding

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13
Q

Somatostatin Analogues: OCTREOTIDE, Lanreotide- Adverse Effects/Contraindications

A
GI discomfort
cardiac effects (sinus bradycardia
conduction disturbances)
hypoglycemia
gallstone

Contraindicated in hypersensitivity

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14
Q

Somatostatin Analogues: OCTREOTIDE, Lanreotide- Drug Rxn

A

increases availability of Bromocriptine

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15
Q

GH Receptor Antagonist- Available Drugs

A

Pegvisomant

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16
Q

GH Receptor Antagonists: Pegvisomant- Mech of Action

A

antagonist of GH receptor–> decrease IGF1 levels

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17
Q

GH Receptor Antagonists: Pegvisomant- Clinical Use

A

Acromegaly that is refractory to other modes of treatment (such as surgical, radiologic or pharmacologic)

Patients should get regular MRI to check adenoma size, and liver function tests

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18
Q

GH Receptor Antagonists: Pegvisomant- Adverse Effects/Contraindications

A

increased pituitary adenoma size, elevated serum aminotransferase levels

Contraindicated in hypersensitivity

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19
Q

Dopamine Receptor Agonist: Bromocriptine- Clinical Use

A

Acromegaly if pituitary tumor secretes both prolactin and GH

20
Q

Menotropins- Mech of Action

A

FSH and LF from urine of postmenopausal women

21
Q

hCG- Mech of Action

A

LH Agonist

22
Q

Urofollitropin- Mech of Action

A

FSH from urine of postmenopausal women

23
Q

Follitropin- Mech of Action

A

recombinant FSH

24
Q

Short Acting Synthetic GnRH- Available Drugs

A

Gonadorelin

25
GnRH or Short Acting Synthetic GnRH- Gonadorelin- Mech of Action
stimulate gonadal axis
26
Menotropins, hCG, Urofollitropin, Follitropin- Clinical Use
``` ovulaton induction (in hypogonadotropic hypogonadism, polycycstic ovary syndrome, obesity) controlled ovarian hyperstimulation in IVF treatment of male hypogonadotropic hypogonadism ```
27
Menotropins, hCG, Urofollitropin, Follitropin- Adverse Effects/Contraindications
ovarian hyperstimulation syndrome increase in multiple gregnancies increased risk of ovarian cancer, ovarian cysts, & hypertrophy (in women) and gynecomastia (in men) Contraindicated in endocrine disorder other than anovulation, primary gonadal failure, pituitary or sex-hormone-dependent tumors, ovarian cyst or enlargement, pregnancy
28
GnRH or Short Acting Synthetic GnRH- Gonadorelin- Absorption, Distribution
PULSATILE ADMINISTRATION
29
GnRH or Short Acting Synthetic GnRH- Gonadorelin- Elimination
SHORT HALF LIFE
30
GnRH or Short Acting Synthetic GnRH- Gonadorelin- Clinical Use
mostly for diagnosis of hypogonadism, occasionally to stimulate ovulation or to treat infertility in men
31
GnRH or Short Acting Synthetic GnRH- Gonadorelin- Adverse Effects/Contraindications
anaphylaxis w/ multiple administrations light headedness flushing hypersensitivity dermatitis
32
Long Acting Synthetic GnRH- Available Drugs
``` Goserelin Histerelin Nafarelin Triptorelin Leuprolide ```
33
Long Acting Synthetic GnRH- Goserelin, Histrelin, Leuprolide, Nafarelin, Triptorelin- Mech of Action
PRODUCE BIPHASIC RESPONSE IN GONADAL AXIS 1. INITIAL AGONIST "FLARE" 2. LONG LASTING INHIBITORY EFFECT
34
Long Acting Synthetic GnRH- Goserelin, Histrelin, Leuprolide, Nafarelin, Triptorelin- Absorption, Distribution
CONTINUOUS ADMINISTRATION
35
Long Acting Synthetic GnRH- Goserelin, Histrelin, Leuprolide, Nafarelin, Triptorelin- Elimination
LONG HALF LIVES
36
Long Acting Synthetic GnRH- Goserelin, Histrelin, Leuprolide, Nafarelin, Triptorelin- Clinical Use
to keep LH surge low in IVF (leuprolide, nafarelin) for the treatment of Endometriosis & Uterine fibroids (leuprolide, nafarelin, goserelin) as adjunctive in prostate cancer (leuprolide, goserelin, histrelin, triptorelin) central precocious puberty (leuprolide, nafarelin) others include: advanced breast & ovarian cancer, amenorrhea & infertility in polycystic ovary disease
37
Long Acting Synthetic GnRH- Goserelin, Histrelin, Leuprolide, Nafarelin, Triptorelin- Adverse Effects/Contraindications
menopausal symptoms (hot flash, sweats, headache) osteoporosis urogenital atrophy temporary worsening of precocious puberty contraindicated in hypersensitivity, pregnancy and breastfeeding
38
GnRH Receptor Antagonists- Available Drugs
Ganirelix Cetrorelix Abarelix
39
GnRH Receptor Antagonists: Ganirelix, Cetrorelix, and Abarelix- Mech of Action
competitive antagonist of GnRH receptor--> inhibit gonadal axis NO flare
40
GnRH Receptor Antagonists: Ganirelix, Cetrorelix, and Abarelix- Clinical Use
TO KEEP LH SURGE LOW IN IVF (Ganirelix, Cetrorelix) METASTATIC PROSTATE CANCER (Abarelix)
41
GnRH Receptor Antagonists: Ganirelix, Cetrorelix, and Abarelix- Adverse Effects/Contraindications
ovarian hyperstimulation syndrome ABARELIX: QT interval prolongation GANIRELIX: ectopic pregnancy, thrombotic disorder, spontaneous abortion CETRORELIX: anaphylaxis Contraindicated in pregnancy, lactation, ovarian cysts/enlargement not due to poly cystic ovarian syndrome, primary ovarian failure, thyroid/adrenal dysfunction, vaginal bleeding of unknown etiology
42
Dopamine Receptor Agonists- Available Drugs
BROMOCRIPTINE CARBERGOLIDE PERGOLIDE quinaglide
43
Dopamine Receptor Agonist: Bromocriptine, Cabergoline, Pergolide, Qiunaglide- Mech of Action
inhibit pituitary prolactin release | GH release reduced in acromegaly but less effectively
44
Dopamine Receptor Agonist: Bromocriptine, Cabergoline, Pergolide, Qiunaglide- Clinical Use
amenorrhea galactorrhea infertility from hyperprolactinemia premenstrual syndrome (BROMOCRIPTINE, CABERGOLINE) Acromegaly: BROMOCRIPTINE Parkinson's Disease: BROMOCRIPTINE, PERGOLIDE, CABERGOLINE
45
Dopamine Receptor Agonist: Bromocriptine, Cabergoline, Pergolide, Qiunaglide- Adverse Effects/Contraindications
orthostatic hypotension cerebral vascular accident, seizure, acute myocardial infarction (Bromocriptine) arrhythmia, myocardial infarction, heart failure (Pergolide) Pulmonary fibrosis & pleural effusion (Cabergoline) Contraindicated in hypersensitivity to ergot derivatives, uncontrolled hypertension