NCM 106 (PHARMACOLOGY

[LVL 2 – 1ST SEMESTER – MIDTERM]

DRUGS AFFECTING HYPOTHALAMIC HORMONES
The hypothalamus uses a number of
hormones or factors to either stimulate or
inhibit the release of hormones from the
anterior pituitary.

Factors that stimulate the release of

hormones:
1. Growth hormone-releasing hormone
(GHRH)
2. Thyrotropin-releasing hormone (TRH)
3. Gonadotropin-releasing hormone
(GnRH)
4. Corticotropin-releasing hormone
(CRH)
5. Prolacting-releasing hormone (PRLH)

Factors that inhibits the release of

hormones:
1. Somatostatin (growth hormone
inhibiting factor)
2. Prolactin-inhibitng factor

SUBERE, PATRICIA LORRAINE T. [Colegio San Agustin – Bacolod / BSN]


DRUGS AFFECTING HYPOTHALAMIC HORMONES
THERAPEUTIC ACTIONS AND
INDICATIONS
 Not all of the hypothalamic hormones
are used as pharmacologic agents.
 A number of hypothalamic releasing
hormones are used for diagnostic
purposes only, and others are used
primarily as antineoplastic agents.
 Tesamorelin is used to stimulate GH
and its lipolytic effects, helping to
decrease the excess abdominal fat in
HIV-infected patients with
lipodystrophy.
PHARMACOKINETICS
 For the most part, these drugs are
absorbed slowly when given IM,
subcutaneously, or in depot from (a
slow-release form of medication e.g.,
Leuprolide [Lupron]).
 They tend to have very long half-lives
of das to weeks.
 Because they are hormones or similar
to hormones, they cross the placenta
and they cross into breastmilk. Most
of them are excreted in urine.
 Nafarelin is given in as nasal form.
SUBERE, PATRICIA LORRAINE T.
NCM 106 (PHARMACOLOGY
[LVL 2 – 1ST SEMESTER – MIDTERM]
A drug’s time to onset of action, time to peak effect,
and duration of action are all characteristics defined
by pharmacokinetics.
The half-life of a drug is an estimate of the period
of the time that it takes for the concentration or
amount in the body of that drug to be reduced by
exactly one half (50%).
CONTRAINDICATIONS AND CAUTIONS
 These drugs are contraindicated with
known hypersensitivity to any
component of the drug because of the
risk of hypersensitivity reactions and
during pregnancy and lactation
because of the potential adverse
effects to fetus or baby.
 Caution should be used with renal
impairment which could interfere with
excretion of the drug; with peripheral
disorders which could alter the
absorption of injected drug;
 With rhinitis when sing nafarelin –
could alter the absorption of the nasal
spray.
ADVERSE EFFECTS
Adverse effects are related to stimulation or
blocking or regular hormone control.
 Agonists
- Can lead to increased release of
sex hormones leading to ovarian
overstimulation, flushing, increases
temperature and appetite, and
fluid retention.
 Antagonists
- Can lead to a decrease in
testosterone levels, leading to loss
of energy, decreased sperm count
[Colegio San Agustin – Bacolod / BSN]
 NCM 106 (PHARMACOLOGY
[LVL 2 – 1ST SEMESTER – MIDTERM]
DRUGS AFFECTING HYPOTHALAMIC HORMONES
and activity, potential alterations
in secondary sex characteristics,
or to a decrease in female sex
hormones, leading to a lack of
menstruation, fluid and electrolyte
changes, insomnia, and irritability.

KEY POINTS
 The hypothalamus releases hormones
that act as releasing factors,
stimulating the anterior pituitary to
release specific stimulating factors
and inhibiting factors that act to stop
the production of specific anterior
pituitary hormones.
 Not all the hypothalamic hormones are
available for pharmacological use.
 Those that are available are used
mostly for:
1. Diagnostic testing
2. Treating some forms of cancer
3. As adjuncts in fertility programs.

SUBERE, PATRICIA LORRAINE T. [Colegio San Agustin – Bacolod / BSN]