L5-HYPOTHALAMIC AGENTS.ppt
- 1. L5-HYPOTHALAMIC AGENTS ALICE 2/28/2023 1 ALICE BCM 329 PHARMACOLOGY VI
- 2. Hypothalamic agents • Hypothalamic agents can inhibit or stimulate the release of hormones from the anterior pituitary using hormones or factors. However, not all of these hormones are available for pharmacological use. 2/28/2023 2 ALICE BCM 329 PHARMACOLOGY VI
- 3. Hypothalamic agents • Stimulating factors (agonists) include growth hormone-releasing hormone (GHRH), thyrotropin-releasing hormone (TRH), gonadotropin-releasing hormone (GnRH), corticotropin-releasing hormone (CRH), and prolactin-releasing hormone (PRH). 2/28/2023 3 ALICE BCM 329 PHARMACOLOGY VI
- 4. Hypothalamic agents • Factors that inhibit (antagonists) include somatostatin (growth hormone-inhibiting factor) and prolactin-inhibiting factor. 2/28/2023 4 ALICE BCM 329 PHARMACOLOGY VI
- 5. Hypothalamic agents • Classification • Agonists: goserelin (Zoladex), histrelin, leuprolide, nafarelin, tesamorelin • Antagonists: degarelix, ganirelix 2/28/2023 5 ALICE BCM 329 PHARMACOLOGY VI
- 6. Hypothalamic agents • Therapeutic Action • Not clearly identified as there are only minute quantities found. • Not all of them are used as pharmacological agents. Some are used for diagnostic purposes only and others are primarily used as antineoplastic agents. • Tesamorelin is used to stimulate GH and its lipolytic effects help to decrease the excess abdominal fat in HIV-infected patients with lipodystrophy. 2/28/2023 6 ALICE BCM 329 PHARMACOLOGY VI
- 7. Hypothalamic agents • Indications • Hypothalamic hormones are not all available for pharmacological use; those that are available are used mostly for diagnostic testing, for treating some forms of cancer, or as adjuncts in fertility programs. 2/28/2023 7 ALICE BCM 329 PHARMACOLOGY VI
- 8. Hypothalamic agents • Indications • Agonists like goserelin, histrelin, leuprolide, and nafarelin are analogues of GnRH. • They decrease production of sex hormones. • They are used as treatment for precocious puberty, endometriosis, and advanced prostate cancer. 2/28/2023 8 ALICE BCM 329 PHARMACOLOGY VI
- 9. Hypothalamic agents • Indications • Antagonists of GnRH like degarelix and ganirelix are used as treatment for advanced prostate cancer and inhibition of premature LH surge in women undergoing controlled ovarian stimulation for fertility. 2/28/2023 9 ALICE BCM 329 PHARMACOLOGY VI
- 10. Hypothalamic agents • Use in children • Monitor closely for adverse effects associated with changes in overall endocrine function, particularly growth and development and metabolism. • Standard part of treatment plan should include periodic radiograph of long bones and monitoring of blood sugar and electrolytes. 2/28/2023 10 ALICE BCM 329 PHARMACOLOGY VI
- 11. Hypothalamic agents • Adults • Monitor blood sugar and electrolytes. • Drugs should not be used among pregnant and lactating women unless benefits clearly outweigh the risks. 2/28/2023 11 ALICE BCM 329 PHARMACOLOGY VI
- 12. Hypothalamic agents • Older adults • Evaluate hydration, nutrition, and electrolyte balance periodically. • Review proper administration technique because they are at high risk for dehydrated membranes and ulcerations-Zoladex 2/28/2023 12 ALICE BCM 329 PHARMACOLOGY VI
- 13. Hypothalamic agents • Pharmacokinetics ROUTE ONSET PEAK DURATION IM depot 4h Variable 1,2,3, or 4 mo T1/2: 3 h Metabolism: unknown Excretion: unknow n 2/28/2023 13 ALICE BCM 329 PHARMACOLOGY VI
- 14. Hypothalamic agents • Contraindications and Cautions • Allergy to any component of the drug. • Peripheral vascular disorders. Can alter absorption of drugs. • Rhinitis Alters absorption of nafarelin nasal spray. • Renal or hepatic impairment. Interfere with drug metabolism and excretion. • Pregnancy or lactation. Potential adverse effects to fetus or neonates. 2/28/2023 14 ALICE BCM 329 PHARMACOLOGY VI
- 15. Hypothalamic agents • Adverse Effects • Agonists: increased release of sex hormones, ovarian overstimulation, flushing, increased temperature and appetite, fluid retention 2/28/2023 15 ALICE BCM 329 PHARMACOLOGY VI
- 16. Hypothalamic agents • Adverse Effects • Antagonists: decreased testosterone levels, loss of energy, decreased sperm count and activity, alterations in secondary sex characteristics (decrease in female sex hormones, amenorrhea), fluid and electrolyte changes, insomnia, irritability 2/28/2023 16 ALICE BCM 329 PHARMACOLOGY VI
- 17. Hypothalamic agents • Interactions • Drug interactions of hypothalamic agents are related to the specific hormones that the drug is affecting. 2/28/2023 17 ALICE BCM 329 PHARMACOLOGY VI