Endocrine

Drugs
Gigantism
Macabangon | Madria | Magomnang | Maronsing |
Mikunug | Millevo | Mira-ato | Monares | Muti |
Odin | Oquendo | Oti
 Case: Gigantism
A 17-year-old male was referred for medical evaluation
before joining the basketball varsity team. He stood at 195
cm and weighed 80 kg. Both his parents had heights below
150cm. On examination, he has stable vital signs, with clear
breath sounds. Further testing showed elevated IGF-1 and
MRI showed a 3 cm pituitary mass. He underwent surgery
of the pituitary tumor but only partial resection was done.
Because of this, he is advised medical management of
growth hormone excess.The other pituitary hormones were
within normal.
 Endocrine axis
Growth Hormone

- From the anterior pituitary

- Single-chain protein hormone
- Surface receptor of JAK/STAT cytokine
receptor superfamily

Hall, J. E. (2020). Guyton & Hall Physiology Review E-Book: Guyton & Hall Physiology Review E-Book. Elsevier
Health Sciences.
Katzung, B. G., & Trevor, A. J. (2020). Basic and Clinical Pharmacology 15E. McGraw Hill Professional.
 Gigantism vs Acromegaly
Acromegaly
- Abnormal growth of cartilage
and bone tissue, and many
organs including skin, muscle,
heart, liver, GIT.
Gigantism
- GH-secreting adenoma occurs
before long bone epiphyses
close.

Gagel RF, McCutcheon IE. Images in clinical medicine. Pituitary gigantism. N Engl J Med. 1999 Feb 18;340(7):524. doi: 10.1056/NEJM199902183400705. PMID: 10021473.
Katzung, B. G., & Trevor, A. J. (2020). Basic and Clinical Pharmacology 15E. McGraw Hill Professional.
 Gigantism
pathophysiology

● Pituitary adenoma
● Overproduction of GH
● Stimulation of IGF-1
● Due to pituitary mass

Hall, J. E. (2020). Guyton & Hall Physiology Review E-Book: Guyton & Hall Physiology Review E-Book. Elsevier
Health Sciences.
Katzung, B. G., & Trevor, A. J. (2020). Basic and Clinical Pharmacology 15E. McGraw Hill Professional.
 Medical therapy with GH antagonists is
introduced if GH hypersecretion
persists after surgery.

Determined by:
Elevated IGF-1 levels
GH not suppressible to <1 mcg/L

Katzung, B. G., & Trevor, A. J. (2020). Basic and Clinical Pharmacology 15E. McGraw Hill Professional.
 GH
Receptor
Antagonist
 Pegvisomant

Pegvisomant is a highly selective

growth hormone (GH) receptor
antagonist.
Mechanism of Action - blocks GH receptors
 Pharmacokinetics
Absorption Distribution Metabolism Excretion Storage

Peak serum Within the Predominantly by Clearance: stored in a

concentration extracellular fluid the liver 36 to 28 mL/h (for refrigerator at 2°C
(SC): 33-77 hours space and does doses 10 to 20 to 8°C (36°F to
not readily cross mg/day) 46°F). Do not
cell membranes freeze.
Mean serum
Mean apparent half-life: ~60 to
volume of 138 hours
distribution: 7L (approx. 6 days),
<1% recovered in
urine over 96
hours

SOMAVERT® WITH DILUENT VIAL (pegvisomant) Clinical Pharmacology | Pfizer Medical Information - US. (n.d.).
 Toxicity and Drug Interaction

Increased liver enzymes;

Need to monitor for pituitary

adenoma growth.

Katzung, B. G., & Trevor, A. J. (2020). Basic and Clinical Pharmacology 15E. McGraw Hill Professional.
Somatostatin
Analogs
Octreotide and Lanreotide
Mechanism:

Agonist at somatostatin
receptor
 Octreotide Pharmacokinetics

Absorption Distribution Metabolism Excretion Storage

Bioavailability: Crosses the placenta Extensively Via urine (32% as Store between 2-8°C.
100% (SC) and enters breast metabolized in the unchanged drug). Protect from light.
60-63% of SC dose milk. liver Do not freeze.
(IM). Elimination half-life: Reconstituted
Volume of 1.7-1.9 hours solutions for IV
Time to peak plasma distribution: 14 L infusion are stable
concentration: below 25°C for 24
Approx Plasma protein hours.
0.4-0.7 hours (SC); binding: Approx Prefilled pens may be
1 hour (IM) 40-65% stored between
20-25°C for 28 days
after first use.

Mims. (n.d.). Acromegaly Treatment | MIMS Singapore. https://www.mims.com/specialty/acromegaly/treatment

 Lanreotide Pharmacokinetics

Absorption Distribution Metabolism Excretion Storage

Absolute Volume of In the liver Estimated Store between 2-8°

bioavailability: distribution: 15.14 L Clearance: C.
Approx 55-80% 23.1 L/h Do not freeze.
Protect from light.
Time to peak
plasma
concentration:
7-12 hours

Mims. (n.d.). Acromegaly Treatment | MIMS Singapore. https://www.mims.com/specialty/acromegaly/treatment

Toxicity and Drug Interaction

SC or IV injection
Long-acting formulation injected IM monthly

Toxicity:
GI disturbances
Gallstones
Bradycardia
Cardiac conduction problems
 Computations
In the Philippines, only Octreotide acetate is available
for the pharmacologic treatment of gigantism
post-op (based on the Philippine National Formulary
2022). It is available in 100 mcg/mL and 500 mcg/mL,
1mL ampoule for IV infusion. For post-operative
patients, usually 100mcg /mL are given as
maintenance drugs.
 Combination Therapy

Pegvisomant (PEG) monotherapy or in combination with

somatostatin analogues (SSAs) appears to improve glucose
metabolism independently of disease control in patients with
acromegaly.

Mims. (n.d.). Acromegaly Treatment | MIMS Singapore. https://www.mims.com/specialty/acromegaly/treatment

References
Hall, J. E., & Hall, M. E. (2020). Guyton and Hall Textbook of Medical Physiology E-Book: Guyton and Hall Textbook of

Medical Physiology E-Book. Elsevier Health Sciences.

Katzung, B. G., & Trevor, A. J. (2020). Basic and Clinical Pharmacology 15E. McGraw Hill Professional.

Mims. (n.d.). Acromegaly Treatment | MIMS Singapore. https://www.mims.com/specialty/acromegaly/treatment