Chapter 36

Posterior Pituitary Hormones

 Endocrine Functions of the Pituitary

Anterior pituitary hormones:

adrenocorticotropic hormone (ACTH),
growth hormone (GH),
prolactin, thyroid-stimulating hormone (TSH),
luteinizing hormone (LH),
follicle-stimulating hormone (FSH).

Posterior pituitary hormones:

oxytocin, vasopressin (antidiuretic hormone)
Posterior Pituitary
Hormones
Posterior pituitary:
– Stores and releases 2 hormones that are produced in
the hypothalamus:
• Oxytocin:
– Stimulates contractions of the uterus during parturition.
– Stimulates contractions of the mammary gland alveoli.
• Vasopressin (Antidiuretic hormone, ADH):
– Promotes the retention of water by the kidneys.
 Oxytocin
Oxytocin is a short polypeptide hormone released by the
posterior pituitary that elicits milk ejection in lactating
women and contributes to the initiation of labor.

【 Pharmacokinetics 】
Oxytocin is usually administered intravenously for stimulation
of labor. It is also available as a nasal spray to induce lactation
postpartum. It is inactive if swallowed, because it is destroyed in
the stomach and intestine.
Oxytocin is not bound to plasma proteins and is catabolized by
the kidneys and liver, with a circulating half-life of 5 minutes.
【 Pharmacologic effects 】
Oxytocin alters transmembrane ionic currents in myometrial
smooth muscle cells to produce sustained uterine contraction.
The sensitivity of the uterus to oxytocin is increased during
pregnancy. Oxytocin-induced myometrial contractions can be
inhibited by β-adrenoceptor agonists, magnesium sulfate, or
inhalation anesthetics.
Oxytocin also causes contraction of myoepithelial cells
surrounding mammary alveoli, which leads to milk ejection.
Without oxytocin-induced contraction, normal lactation cannot
occur.
Oxytocin has weak antidiuretic and pressor activity.
【 Therapeutic uses 】
Oxytocin is used to induce labor and augment
dysfunctional labor for
(1) conditions requiring early vaginal delivery
(eg, maternal diabetes, or preeclampsia);
(2) uterine inertia;
(3) incomplete abortion.
Oxytocin can also be used for control of postpartum
uterine hemorrhage. Impaired milk ejection may
respond to nasal oxytocin.
【 Dosage 】
For induction of labor, oxytocin should be administered
intravenously via an infusion pump with appropriate fetal and
maternal monitoring. An initial infusion rate of 1 mU/min is
gradually increased to 5-20 mU/min until a physiologic
contraction pattern is established.
For postpartum uterine bleeding, 10-40 units is added to 1 L of
5% dextrose, and the infusion rate is titrated to control uterine
atony. Alternatively, 10 units can be given intramuscularly after
delivery of the placenta.
To induce milk let-down, one puff is sprayed into each nostril
in the sitting position 2-3 minutes before nursing.
【 Adverse reactions & contraindications 】

When oxytocin is used properly, serious toxicity is rare.

Among the reported adverse reactions are maternal deaths
due to hypertensive episodes, uterine rupture, water
intoxication, and fetal deaths. Afibrinogenemia has also
been reported.
Contraindications include fetal distress, prematurity,
abnormal fetal presentation, cephalopelvic disproportion,
and other predispositions for uterine rupture.
 Vasopressin
(Antidiuretic hormone, ADH)
Vasopressin is a peptide hormone released by the posterior
pituitary that possesses antidiuretic and vasopressor properties.
A deficiency of this hormone results in diabetes insipidus.
【 Pharmacokinetics 】
Vasopressin is administered by intravenous, intramuscular, or
intranasal routes; oral absorption is slight, quickly inactivated
by trypsin. The half-life of circulating ADH is approximately 20
minutes, with renal and hepatic catabolism via reduction of the
disulfide bond and peptide cleavage. A small amount of
vasopressin is excreted as such in the urine.
【 Pharmacologic effects 】
Vasopressin interacts with two types of receptors. V1 receptors
are found on vascular smooth muscle cells, liver and other tissues,
and mediate vasoconstriction. V2 receptors are found on renal
tubule cells and mediate antidiuresis through increased water
permeability and water resorption in the collecting tubules. Thus
the major use of vasopressin is to treat diabetes insipidus.
Desmopressin acetate (DDAVP, 1-desamino-8-D-arginine
vasopressin) is a long-acting synthetic analog of vasopressin with
minimal V1 activity and an antidiuretic-to-pressor ratio 4000
times that of vasopressin.
【 Therapeutic uses 】
Vasopressin and desmopressin are the alternative
treatments of choice for pituitary diabetes insipidus.
Bedtime desmopressin therapy ameliorates
nocturnal enuresis by decreasing nocturnal urine
production.
Vasopressin infusion is effective in some cases of
esophageal variceal bleeding and colonic diverticular
bleeding.
 【 Dosage
1.】
Aqueous vasopressin
Synthetic aqueous vasopressin is a short-acting preparation. The dose is 5-10
units subcutaneously or intramuscularly every 3-6 hours for transient diabetes
insipidus and 0.1-0.5 units/min intravenously for gastrointestinal bleeding.
2. Desmopressin acetate
This is the preferred treatment for most patients with central diabetes
insipidus. Desmopressin may be administered intranasally, intravenously,
subcautaneously, or orally.
The typical nasal dosage is 10-40μg (0.1-0.4mL) daily in one to three divided
doses. Nasal desmopressin is available as a unit dose spray that delivers 0.1 mL
per spray.
The dosage by injection of desmopressin is 1-4μg (0.25-1mL) daily every 12-
24 hours as needed for polyuria, polydipsia, or hypernatremia. For nocturnal
enuresis, desmopressin, 10-20μg (0.1-0.2mL) intranasally at bedtime, is used.
【 Adverse reactions & contraindications 】
Overdosage can result in water intoxication and
hyponatremic convulsions. Headache, nausea,
abdominal cramps, agitation, and allergic reactions
occur rarely.
Vasopressin (but not desmopressin) can cause
vasoconstriction and should be used cautiously in
patients with coronary artery disease.
Nasal insufflation of desmopressin may be less
effective when nasal congestion is present.