OUTLINE

I. Endocrinology: General Concepts B. Glycoprotein Hormones On sagittal section, it shows the relationship of the pituitary
II. Pituitary Gland 1. Gonadotropins gland and the hypothalamus
i. Classification of Anterior Pituitary C. Posterior Pituitary Hormones Hypothalamus is situated just above the pituitary gland
Hormones 1. Oxytocin Relationship is very strategic because hypothalamus controls
ii. Cells and Hormones of Anterior the function of pituitary gland
Pituitary Gland III. Drug Summary Pituitary gland sits on the sella turcica
A. Somatotropic Hormones
1. Growth Hormone
2. Prolactin
I. ENDOCRINOLOGY & HORMONES: GENERAL CONCEPTS
Legend Hormones may be divided into 2 classes:
Verbatim Book High yield o Hormones that act predominantly via nuclear receptors (steroid, TH, vit D)
o Hormones that act via membrane receptors to exert rapid effects on signal
This axis is the interconnection of these three transduction pathways (peptide and amino acid hormones)
major organs
Hypothalamus gives out the releasing hormone or II. PITUITARY GLAND (Hypophysis Cerebri)
inhibiting hormone towards the pituitary → ▪Reddish-grey, ovoid body, about 12mm in transverse and 8mm in AP diameter,
pituitary usually produces the tropic or signal
weighs at about 500mg
hormone → directs the adrenals → adrenals
produces the target hormones ▪ Lies in hypophyseal fossa of sphenoid bone
Example: Releasing hormones from the ▪ Covered by diaphragmatic sellae of dura and separates the gland from optic
hypothalamus is CRH → adrenocorticotropic chiasma
hormones → corticosteroids ▪ Inferiorly and front is related to sphenoid air sinus; related on side to cavernous
If there is already increased amounts of
sinus, related behind to dorsum sellae
corticosteroids in the body → send negative
feedback to the hypothalamus to stop producing ▪ The gland consists of:
the hormones Anterior Lobe (Adenohypophysis) Posterior Lobe (Neurohypophysis)
Two types of hormones = Pars distalis = Pars nervosa which is connected by
o Group I – steroids, vit D, thyroid hormone;
= Pars tuberalis infundibulum (pituitary stalk) to the
lipophilic; intracellular receptors
= Pars intermedia median eminence (tuber cinereum) of
o Group II – Polypeptides/Amino acids
hormones/Glycoproteins; water soluble and hypothalamus
receptors are located in membranes
Posterior pituitary produces the oxytocin and vasopressin
There is direct connection between the hypothalamus to
In relation to the whole brain, pituitary gland is small but very posterior pituitary gland so it is the hypothalamus that
powerful produces the hormones (oxytocin, vasopressin) not the
Pea-sized posterior pituitary
Master gland Posterior pituitary hormones only serve as a storage
Anterior pituitary gland produces almost all the hormones
(TSH, ACTH, FSH, LH, GH, PRL, endorphins)

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i. Classification of Anterior Pituitary Hormones iii. Cells and Hormones of the Anterior Pituitary Gland & Their Functions
Somatotropic Hormones Glycoprotein Hormones Pro-opiomelanocortin-derived Cell Hormone Secreted Function
Hormones Somatotropes Growth Hormone ▪ Stimulates body growth
= Growth Hormone = LH = Corticotropin (ACTH) (Somatotropin)
= Prolactin = FSH = α-MSH Mammotropes Prolactin (PRL) ▪ Stimulates milk production
= Placental lactogen = TSH (Acidophilic)
= hCG Thyrotropes Thyroid Stimulating ▪ Stimulates production by follicular cells
(Basophilic) Hormone (TSH)
Gonadotropes Follicle-stimulating ▪ Stimulates follicular cells in ovary &
Discussion (Basophilic) Hormone (FSH) spermatogenesis in testis
o Polypeptides are classified under Group II Luteinizing Hormone (LH) ▪ Stimulates production of estrogen and
o Placental lactogen is only seen in pregnant women but it acts similar to growth hormone progesterone from the ovary and
testosterone from the testis
Table 24-1: HORMONES THAT INTEGRATE THE HYPOTHALAMIC-PITUITARY-ENDOCRINE AXIS Corticotropes Adreno-corticotrophic ▪ Stimulates secretion of glucocorticoids
Hypothalamic Hormone Effect on Pituitary Trophic Target Hormone(s) (Basophilic) Hormones (ACTH) and androgens from adrenal cortex
Hormone
Growth Hormone-Releasing ↑↑ Growth hormone IGF-1 A. SOMATOTROPIC HORMONES
hormone
Somatostatin ↓ Growth hormone ▪ Growth Hormone
↓ Thyroid-stimulating Hormone ▪ Prolactin
Dopamine ↓ Prolactin
Corticotropin-releasing hormone ↑ Corticotropin Cortisol GROWTH HORMONE
Thyrotropin-releasing hormone ↑ Thyroid-stimulating hormone Thyroid hormone = Single, polypeptide chain of 22 kDa; w/ 2 disulfide bonds, not glycosylated
↑ Prolactin = Gene resides on the long arm of Chromosome 17
Gonadotropin-releasing hormone ↑ Follicle-stimulating hormone Estrogen = Most abundant pituitary hormone
↑ Luteinizing hormone Progesterone/Estrogen = Increased secretion in children
Testosterone
= Peaks at puberty (growth spurts during puberty)
= Secreted in pulses (greatest at night shortly after onset of deep sleep)
ii. Link between Hypothalamic, Anterior Pituitary, and Target Organ Hormones or
Mediators GH stimulus GH suppressors
Anterior Pituitary Hypothalamic Target Organ Primary Target Organ =
= Main: GHRH and Ghrelin Increased levels → negative feedback
Hormone Hormones or Mediators
= Minor: Dopamine, 5HT, α2 receptor effect
GH GHRH (+) Liver, Muscle, Bone, Insulin-like Growth Factor 1
agonists; hypoglycemia, exercise, stress, o IGF-1 (from peripheral tissues)
Somatotropin Somatostatin (-) Kidney (IGF-1)
emotional excitement, ingestion of o Somatostatin (from
TSH TRH (+) Thyroid Thyroxine
protein-rich meals hypothalamus)
Somatostatin (-) Triiodothyronine
o GH levels (from anterior
ACTH CRH (+) Adrenal cortex Glucocorticoids
MOA: GNRH → Gs → ↑cAMP and Ca → pituitary)
Mineralocorticoids
Androgens GH synthesis
FSH GnRH (+) Gonads Estrogen Somatostatin (through Gi → inhibits
LH Progesterone = Major peripheral effector of GH: IGF-1 cAMP formation)
Testosterone o SSTR2 and SSTR5 = most
PRL Dopamine (-) Breast important for regulation of GH
TRH (+) secretion

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 Discussion Children Adults
o Ghrelin is an amino acid peptide which stimulates the growth hormone secretion through = Short stature = ↓ muscle mass & exercise capacity
its action on GPCR. Synthesized predominantly on the fundus of the stomach and on other = Delayed bone age = ↓ bone density
sites (pituitary and hypothalamus)
= Low age-adjusted growth velocity = Impaired psychosocial function
Both fasting and hypoglycemia increase circulating stomach-derived ghrelin levels →
stimulates appetite and food intake
= ↑ mortality from cardiovascular
o IGF-1 is produced locally by many tissues in response to presence of growth hormone. If causes
there are increased levels of IGF-1, this will give a negative feedback effect to the
hypothalamus via SST stimulation, and direct effect on anterior pituitary gland Discussion
o Why is there an increase mortality from cardiovascular causes? This is because of the
1. Growth Hormone Regulation function of growth hormone on adipocytes, and this also has increased lipolysis function
o If GH is suppressed, there will be trouble with cholesterol synthesis → atheromatous
Discussion
plaque formation
o IGF-1, if increased, will send a negative feedback effect both on
o Usually for adults, the cause of deficiency is due to a functioning or nonfunctioning
hypothalamus and anterior pituitary
o GH itself will send a negative feedback to the hypothalamus, if pituitary adenoma (tumor) or may be secondary to trauma, related to surgery or
it increases, whereas GHRH has a stimulatory effect on GH and radiotherapy of pituitary area
somatostatin sends the inhibitory signal to hypothalamus to o Growth hormone level checking is usually done for adult patients (in their blood)
stop production of growth hormone and inhibitory effect on o Provocative testing is by using insulin, arginine, glucagon, levodopa
anterior pituitary gland
o Ghrelin has a stimulatory effect on production of GH in anterior a. Treatment of Growth Hormone Deficiency
pituitary and stimulatory effect on the hypothalamus
Somatropin
Physiologic Effects Other Effects ▪ Human GH by recombinant DNA Technology
▪ Brand names: Serostim; Genotropin; Humatrope; Nutropin; Norditropin; Saizen
▪ Stimulate longitudinal growth ▪ ↑bone mineral density
▪ Dose:
of bones (most striking ▪ Myeloblast differentiation & ↑mass
o Children: 25-50ug/kg/day SQ in the evening (it is to mimic the
physiologic effect) ▪ ↑GFR
physiologic effect of GH which peaks after onset of deep sleep)
▪ Pre-adipocytes → adipocyte differentiation
o Adults: 150-300 ug/d
▪ Anti-insulin action:
▪ Normalization of serum IGF-1 levels – used to monitor initial response &
o ↓glucose utilization
compliance
o ↑lipolysis (fat cells)
▪ Long term monitoring: evaluation of height in growth velocity occurs w/in the
o ↑gluconeogenesis (liver)
first 2 yrs of therapy
▪ Induction of insulin-like growth factor (IGF-1)
▪ Continued until closure of epiphysis (21-22 years old)
▪ For adults – normalization of GH levels
2. Clinical Disorders of Growth Hormone ▪ Pharmacokinetics: 70% bioavailability; once daily dosing
A. GROWTH HORMONE DEFICIENCY
❖ Diagnosis:
Tesamorelin
o Height = >2 – 2.5 SD below normal
▪ Synthetic human GHRH
o Delayed bone age via x-ray
▪ ↑ GH and IGF-1 levels
o ↓growth velocity ▪ But its clinical effects are primarily to reduce visceral fat accumulation w/
o Predicted adult height below the mean parental height minimal effects on insulin resistance
o GH level: ▪ FDA-approved for treatment of HIV-associated lipodystrophy but not for GH
o <10 ng/mL following provocative testing deficiency
o <5ng/mL = severe deficiency

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 Mecasermin B. GROWTH HORMONE EXCESS
▪ Recombinant Human IGF-1 e. Diagnosis
▪ Indications: o Clinical + ↑ circulating GH or IGF-1
= For patients with impaired growth secondary to mutations in GHR / o Gold standard: Oral glucose tolerance test
post-receptor signaling pathway ▪ No change or ↑ GH level
= Patients who develop antibodies against GH ▪ Normal: suppression of GH level to <1 ng/mL
= Patients with IGF-1 gene defects → primary IGF-1 deficiency
= Less effective than recombinant GH for impaired growth secondary to
Gigantism Acromegaly
GH deficiency / with idiopathic short stature
= If epiphyses are unfused = Epiphyses have fused
▪ Dose: 40 – 80 ug/kg SQ twice daily (Max: 120 ug/kg/dose BID)
= ↑ longitudinal growth = Arthropathy, carpal tunnel syndrome,
▪ AE: Hypoglycemia, lipodystrophy (destruction of the lipids), lymphoid tissue
generalized visceromegaly, macroglossia,
hypertrophy
hypertension, glucose intolerance, headache,
▪ CI: Closed epiphysis, active or suspected neoplasia
lethargy, excess perspiration, sleep apnea
= Fail to suppress GH level or with paradoxical
b. Adverse Effects of Growth Hormone Therapy increase in GH level
Children Adults
▪ Rare: intracranial hypertension Most frequent in older / obese patients:
= Recommendation: fundoscopic ▪ Peripheral edema
exam at initiation of therapy and ▪ Carpal tunnel syndrome (arthralgias,
periodically thereafter myalgias)
▪ ↑ incidence of pediatric tumors = Respond to decrease in dose
= Consensus: GH should not be given
in the 1st year after treatment of Gigantism Acromegaly Arachnodactyly
tumors
▪ ↑ incidence of Type 2 DM
1. Treatment of Growth Hormone Excess
= Monitor FBG periodically because
GH has anti-insulin action ▪ Transsphenoidal Surgery
▪ Slipped epiphysis or scoliosis due to ▪ Radiation or drugs that inhibit GH
rapid growth secretion or action
▪ Treatment of Choice:
= Surgery for Microadenoma
c. Drug Interactions (<1cm lesion) – 80% cure rate
▪ Estrogens (birth control medications and estrogen supplements) inhibit GH action ▪ Drugs:
so that a larger dose of GH is needed to maintain IGF-1 level Endoscopic Trans-sphenoidal Surgery
= Somatostatin analogues
= GH receptor antagonists
d. Contraindications for GH therapy Goal: ↓ GH levels to <2.5 ng/mL after
▪ Acute critical illness OGTT or normal IGF-1 level
= Due to complications after open heart or abdominal surgery, multiple
accidental trauma, acute respiratory failure Discussion
▪ Active malignancy o If lesion is still small, surgery can be done
o If lesion is already big (>1 cm lesion = macroadenoma), radiation therapy is done or giving
▪ Proliferative retinopathy or severe nonproliferative diabetic retinopathy
of drugs that inhibit the growth and action
▪ Sudden death has been observed in severely obese children or who had severe o However, drug therapy is more preferred than radiation therapy
respiratory impairment

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 Somatostatin Analogs Discussion
o PEG – polyethylene glycol; it has this portion in the structure which increases the half-life
Ocreotide (Sandostatin) Lanreotide (Somatulien LA)
of the drug and reduces the immunogenicity which is why the drug (Pegvisomant) can be
= 100 ug SQ TID; 100% bioactive = Efficacy similar to Ocreotide given once a day
= Peak effect: 30 mins LAR
= t ½: 90 mins = SQ every 4 weeks
= Duration: 12 hours PROLACTIN
= Ocreotide LAR: 10, 20, or 30 mg IM once every = 23, 000-dalton protein of 199 AA with 3 intramolecular disulfide bonds
4 weeks Predominantly inhibitory
= Treatment of acute variceal bleeding and for = Synthesized by lactotrophs in the anterior pituitary gland
perioperative prophylaxis of pancreatic surgery = Synthesis and secretion start on the 5th week of gestation
Pasireotide Maternal serum PRL level starts at 8 weeks of gestation, peaks to 150 – 250
ng/mL
= Long-acting; binds to multiple SST receptors
= Rise markedly during pregnancy, peaks at term & decline thereafter unless the
= Better than Ocreotide and Lanreotide
mother breastfeeds the child
= Stimulus:
2. Adverse Effects: o suckling and breast manipulation (in nursing mothers)
▪ GI (diarrhea, nausea, abdominal pain): 50% o pregnancy
▪ Gallbladder sludge or gallstones: 25% o TRH
Bradycardia, QT prolongation o VIP
▪ May lead to hypothyroidism
▪ All SST analogues ↓ insulin secretion with reduced insulin resistance (balanced Prolactin Secretion and Actions
effect) and may also block other hormones, growth factors, cytokines PRL is the only anterior pituitary hormone for which a
▪ Pasireotide (more problem with glucose tolerance) suppresses ACTH secretion in unique stimulatory releasing factor has not been
Cushing disease; ↓GLP-1 and glucose insulinotropic peptide identified. TRH and VIP, however, can stimulate PRL
▪ Octreotide and Lanreotide = no change in glucose tolerance release; DA inhibits it.
Suckling induces PRL secretion, and PRL not only affects
lactation and reproductive functions but also has effects
Other Therapeutic Uses on many other tissues. PRL is not under feedback control
▪ Treat s/sx associated with metastatic carcinoid tumors and adenomas secreting by peripheral hormones.
VIP
▪ Octreotide & Lanreotide = treat px who have failed surgery (thyrotrope adenomas)
HYPERPROLACTINEMIA
Growth Hormone Antagonists = Caused by prolactin secreting pituitary adenoma
(prolactinomas)
Pegvisomant
▪ Recombinant pegylated variant of human GH = Manifestations:
For acromegaly o Women: galactorrhea (not pregnant but there
▪ Dose: 40 mg SQ loading dose then 10 mg/day (adjust based on serum IGF-1 is milky nipple discharge), amenorrhea,
level) infertility
Not to be used in patients w/ liver disease (monitor transaminases) o Men: loss of libido, erectile dysfunction, infertility
▪ Lipohypertrophy at injection sites = Diagnosis: MRI
▪ May increase growth of GH secreting adenomas = Therapeutic options:
▪ For patients who do not respond to SST analogs or given as adjuncts o Transsphenoidal surgery
o Radiation

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 o Drugs: Dopamine receptor agonists At higher doses = used in some patients with acromegaly alone or in conjunction
▪ suppress prolactin production by activation of D2 dopamine with SST analogues.
receptors ▪ Adverse Effects (AE)
▪ ↓ size of tumor o Less than that of Bromocriptine
▪ Treatment of choice for most patients o Valvular heart disease at high doses

1. Medical Management for Hyperprolactinemia Quinagolide

A. Dopamine Receptor Agonists ▪ Non-ergot D2 receptor agonist; t ½ = 22 h
Ergot-derived Non-ergot ▪ Administered OD at doses of 0.1 – 0.5 mg/d
▪ Bromocriptine (Parlodel) ▪ Quinagolide (Norpralac)
▪ Cabergoline (Dostinex) B. GLYCOPROTEIN HORMONES
*Ergot is a type of fungi Claviceps (source of ergot-derived drugs)
▪ TSH
▪ Gonadotropins (LH, FSH, hCG)
Bromocriptine
▪ Ergot alkaloid GONADOTROPIN-RELEASING HORMONES & GONADOTROPIC HORMONES
▪ Activates D2 (Dopamine) receptors to inhibit spontaneous & TRH-induced
release of prolactin 1. Physiological Effects of Gonadotropins
▪ Normalizes prolactin level (70 to 80%) Gonadotropins Men Women
▪ ↓ tumor size in >50% of patients but if stopped → tumor recurs Luteinizing = acts on Leydig cells = acts on Theca cells →
▪ AE: Hormone (LH) = stimulate de novo synthesis of androstenedione (precursor of
Androgens (primarily ovarian 17β-estradiol)
o Nausea, Vomiting, Headache, postural hypotension
testosterone) from cholesterol = required for rupture of
o Less frequent: nasal congestion, digital vasospasm & CNS effects: dominant follicle during
psychosis, hallucinations, nightmares, insomnia ovulation & for synthesis of
To avoid side effects progesterone by corpus luteum
o Start at low dose (1.25 mg) at bedtime Testosterone = required for gametogenesis & for
o After 1 week, increase to 2x daily maintenance of libido &
o Gradually increase every 3 – 7 days up to 5 mg 2x daily or until secondary sexual characteristics
prolactin becomes normal Follicle- = acts on the Sertoli cells = stimulates growth of
At higher concentrations = tx for Acromegaly stimulating = stimulates production of developing ovarian follicles
Still higher concentrations = for Parkinson’s Disease hormone (FSH) proteins & nutrients for sperm = induces expression of LH
Safe to use in pregnancy maturation receptor on theca and
granulosa cells
Lifetime treatment
= regulates activity of aromatase
in granulosa cells → stimulates
Cabergoline production of 17β-estradiol
Longer half-life, higher affinity and greater selectivity to D2 receptors
Preferred drug for Hyperprolactinemia (greater efficacy and lower adverse 2. Therapeutic Uses of GNRH
effects) ▪ MOA: GPCR-Gq/G11-PLC-IP3-Ca pathway
▪ Dose: Gonadorelin acetate (Lutrepulse)
o 0.25mg 2x a week or 0.5mg once a week; may increase once every 4 ▪ Synthetic GnRH
weeks ▪ Stimulates Gonadotropin release
o Doses of 2 mg/week or less → normalize PRL levels in 80% of pts

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 GnRH Agonist (Leuprolide) ▪ Off label use: polycystic ovarian ▪ ↓ prostate-specific antigen more
▪ Long acting syndrome, endometriosis, uterine rapidly than GnRH agonists without an
▪ Diagnostically to differentiate between GnRH-dependent and GnRH fibroids initial testosterone surge
independent precocious puberty (Leuprolide) ▪ CI: pregnant women ▪ t ½ = 42 days (starting); 28 days
Pharmacologic castration – as management of precocious puberty (maintenance)
Palliative treatment for hormone responsive tumors (breast and prostate Ca) ▪ 90% protein-bound; distributed
Treatment for Endometriosis, uterine fibroids, acute intermittent porphyria, throughout total body water
priapism ▪ SQ in abdomen
▪ Suppression of LH surge – for in-vitro fertilization o Starting dose: 240 mg (120 mg each
▪ Transient increase in hormone levels side of abdomen)
o Maintenance dose: 80 mg q 28 days
*antagonists do not transiently increase gonadotropin secretion & sex steroid biosynthesis
Adverse effects:
▪ hot flashes and ↓ bone density in both sexes
▪ women: vaginal dryness and atrophy in women FSH, HCG, Recombinant Human LH
▪ men: erectile dysfunction a. Diagnostic Uses
▪ treatment for endometriosis and uterine fibroids (only limited to 6 mos due to i. Pregnancy Testing
the above AE) = Diagnosis of pregnancy: presence or absence of hCG in urine or
CI among pregnant women blood
= Plasma hCG (quantitative)
Formulations & Indications o tumor marker or to assess if pregnancy is proceeding or not
Leuprolide Goserelin Histrelin Nafarelin Triptorelin o used to diagnose ectopic pregnancy, H-mole, Chorioca
✓ Multiple ✓ SQ implant ✓ SQ ✓ Nasal spray ✓ Depot b. Timing of Ovulation
doses for (3.6 implant (200ug/spray) IM
mg/month; (50 ✓ 400ug = ✓ For
= Urine LH (measured every 12-24 h) – help predict the time of ovulation
injection
✓ Pediatric 10.8mg/12 mg/12 endometriosis advance = Ovulation occurs approx. 36 hours after onset of LH surge 10 – 12
formulation wks) mos) tx prostate hours after peak of LH → facilitating timing of sexual intercourse to
for central ✓ 1600 ug = CA achieve pregnancy
precocious central
puberty precocious
puberty
c. Localization of Endocrine Disease
= Low / undetectable levels → hypogonadotropic hypogonadism
= High levels → primary gonadal diseases
Discussion
o Why is GnRH agonist used as management for precocious puberty? Because this drug is = ↑ FSH levels: diagnostic of menopause in women with amenorrhea (in
long acting—it may increase hormone levels transiently but in the long run it may appropriate age range)
downregulate GnRH receptors through the GPCR pathway.
o Transient increase in hormone levels can be managed by anti-androgens Therapeutic Uses of Gonadotropins
Male infertility Cryptorchidism
GnRH Antagonists = hCG 1500 – 2000 IU IM / SQ TID → = Reposition testes as early as possible
Ganirelix (Antagon), Cetrorelix (Cetrotide) Degarelix reduced to 2000 IU 2x a week or 1000 = hCG is given if cryptorchidism is not
▪ Suppress the LH surge → prevent Tx for advanced prostate ca IU 3x a week secondary to anatomical blockage
premature follicular luteinization in ▪ Suppresses testosterone levels to 50 = Most common S/E: gynecomastia = hCG 3000 IU/m2 BSA IM every other
ovarian stimulation protocol (for IVF) ng/dL or less (i.e., medical castration) day for 6 doses

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C. POSTERIOR PITUITARY HORMONES Oxytocin at high doses → antidiuretic effects
▪ Oxytocin
❖ Augmentation of Dysfunctional Labor
▪ Arginine vasopressin (ADH)
o Dose usually does not exceed 10 mIU/min

OXYTOCIN ❖ Prevention and Treatment of Post-partum Hemorrhage

▪ A cyclic nonapeptide o 10 IU IM (within 1 minute after delivery of the fetus) or 20 IU of oxytocin
▪ Differs from vasopressin by 2 AA in 1L of IV fluid at 10 mL/min until uterus is contracted then decrease to
▪ Secreted by the posterior pituitary gland
1 – 2 ml/min

1. Physiological Roles of Oxytocin ❖ Tocolytic Therapy for Established Pre-term Labor

❖ Uterus: stimulates the frequency & force of uterine contractions (GPCR-Gq-IP3
o Inhibition of uterine contractions of preterm labor
and Ca2+)
o Delay delivery in 80% of patients but never prevent premature births nor
❖ Breast = milk ejection (suckling or mechanical manipulation) → contraction of the
improve adverse fetal outcomes
myoepithelium that surrounds alveolar channels in mammary gland → into large
collecting sinuses → ready for sucking
Oxytocin Antagonist
✓ Estrogen dependent – bec. Estrogen increases the expression of oxytocin receptors Atosiban
(Relaxin – inhibitory) ▪ Tocolytic therapy for established preterm labor
✓ Progesterone antagonizes the stimulant effect of oxytocin Other Tocolytics
▪ β-adrenergic receptor agonists ▪ Calcium channel blockers
❖ ↑ local prostaglandin production → further uterine contraction ▪ Magnesium sulfate (MgSO4) ▪ COX inhibitors
▪ NO donors
❖ Brain
= CNS regulator of trust
= autonomic NS: linked to anxiety and fear iv. Drug Summary: Drugs that Mimic or Inhibit Hypothalamic & Pituitary
has anti-stress effect Hormones

2. Clinical Uses
❖ Induction of Labor
o Drugs of Choice: Oxytocin (Pitocin, Syntocin)
▪ Administered as IV drip (mIU/mL) at a dose of 1 mIU/min
▪ Titrated as needed
▪ If at 40 mIU/min = no significant increase in uterine contraction
→ higher rates are unlikely to be successful
o If uterine tetany develops → stop infusion
▪ t ½ = 3 minutes (so in a few minutes, the effect will be gone)
o Dose of >20 mIU/min → ↓ water clearance by kidney
o If hypotonic fluids (eg. D5W) is infused rapidly → risk of water intoxication
→ Convulsion, coma, death
= Only infused with normal saline solution (NSS)
Pitocin is not indicated for elective induction of labor

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