Cabgon 0.25
(CABERGOLINE 0.25MG)

Drug Effects

Chemical Structure


Chemical Formula


C26H37N5O2 .

Iupac Name


N-[3-(Dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)-8g-ergoline-8-carboxamide
or
1-[(6-Allylergolin-8β-yl)-carbonyl]-1-[3-(dimethylamino)propyl]-3-ethylurea.

Usage


  • Cabergoline is used to treat hyperprolactinemia (high levels of prolactin, a natural substance that helps breast-feeding women produce milk but can cause symptoms such as infertility, sexual problems, and bone loss in women who are not breast-feeding or men). Cabergoline is in a class of medications called dopamine receptor agonists. It works by decreasing the amount of prolactin in the body

Adverse Effect


  • Nausea

  • Vomiting

  • Heartburn

  • Constipation

  • Tiredness

  • Dizziness

  • Breast pain

  • Painful menstrual periods

  • Burning, numbness, or tingling in the arms, hands, legs, or feet

Mechanism Action


  • Cabergoline is a long-acting dopamine D2 receptor agonist and in vitro rat studies show a direct inhibitory effect on the prolactin secretion in the pituitary's lactotroph cells. Cabergoline decreased serum prolactin levels in reserpinized rats.
  • Receptor binding studies indicate a low affinity for dopamine D1 receptors, α1-adrenergic receptors, and α2-adrenergic receptors

Precaution


  • Tell your doctor and pharmacist if you are allergic to cabergoline, ergot medications such as bromocriptine (Parlodel); dihydroergotamine (D.H.E. 45, Migranal), ergoloid mesylates (Hydergine), ergotamine (in Cafergot, in Ergomar), methylergonovine (Methergine), methysergide (Sansert), and pergolide (Permax); any other medications, or any of the ingredients in cabergoline tablets. Ask your pharmacist for a list of the ingredients.
  • Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: antihistamines; ergot medications such as dihydroergotamine (D.H.E. 45, Migranal), ergotamine (in Cafergot, in Ergomar), and methylergonovine (Methergine); haloperidol (Haldol); levodopa (in Parcopa, Sinemet, and Stalevo); medications for high blood pressure, mental illness, or nausea; metoclopramide (Reglan); or thiothixene (Navane). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
  • Tell your doctor if you use or have ever used street drugs and if you have or have ever had high blood pressure or any condition that causes thickening or scarring in your lungs, heart, or abdomen. Also tell your doctor if you have or have ever had heart valve disease. Your doctor will examine you and will order tests to see if your heart valves are healthy. Your doctor may tell you not to take cabergoline if you have signs of heart valve disease or any of these conditions.
  • Tell your doctor if you have or have ever had liver disease.
  • Tell your doctor if you are pregnant or plan to become pregnant. If you become pregnant while taking cabergoline, call your doctor.
  • Tell your doctor if you are breast-feeding or plan to breast-feed. Cabergoline may slow or stop the production of breast-milk.
  • You should know that cabergoline may cause dizziness, lightheadedness, and fainting when you get up too quickly from a lying position. This is more common when you first start taking cabergoline. To avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up.

Drug Interaction


  • Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.
  • Some products that may interact with this drug include: antipsychotic medications (such as chlorpromazine, haloperidol, thiothixene), metoclopramide,prochlorperazine.
  • Other medications can affect the removal of cabergoline from your body, which may affect how cabergoline works. Examples include certain azole antifungals (such asitraconazole, ketoconazole, posaconazole), macrolide antibiotics (such asclarithromycin, erythromycin), HIV protease inhibitors (such as ritonavir, saquinavir), among others.

 

Pregnancy Category


Pregnancy Category B- Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women OR Animal studies have shown an adverse effect, but adequate and well-controlled studies in pregnant women have failed to demonstrate a risk to the fetus in any trimester.

Absorption


Bioavailability First-pass effect seen; absolute bioavailability unknown.

Distribution


High levels in pituitary (100x of plasma)

Peak Plasma: 30-70 pg/mL following single oral doses of 0.5-1.5 mg.

Metabolism


Hepatic, predominately via hydrolysis of the acylurea bond or the urea moiety.

Elemination


Urine (22%), feces (60%).

References


  1.  "Dostinex at www.rxlist.com". Retrieved 2007-04-27. 
  2.  US Patent 4526892 - Dimethylaminoalkyl-3-(ergoline-8'.beta.carbonyl)-ureas
  3.  Sharif NA, McLaughlin MA, Kelly CR, Katoli P, Drace C, Husain S, Crosson C, Toris C, Zhan GL, Camras C (March 2009). "Cabergoline: Pharmacology, ocular hypotensive studies in multiple species, and aqueous humor dynamic modulation in the Cynomolgus monkey eyes". Experimental Eye Research 88 (3): 386–97. doi:10.1016/j.exer.2008.10.003. PMID 18992242. 
  4.  National Institute ofMental Health. PDSD Ki Database (Internet) [cited 2013 Jul 24]. ChapelHill (NC): University of North Carolina. 1998-2013. Available from: http://pdsp.med.unc.edu/pdsp.php
  5.  Sayyah-Melli, M; Tehrani-Gadim, S; Dastranj-Tabrizi, A; Gatrehsamani, F; Morteza, G; Ouladesahebmadarek, E; Farzadi, L; Kazemi-Shishvan, M (2009). "Comparison of the effect of gonadotropin-releasing hormone agonist and dopamine receptor agonist on uterine myoma growth. Histologic, sonographic, and intra-operative changes". Saudi medical journal 30 (8): 1024–33. PMID 19668882.  edit
  6.  Sankaran, S.; Manyonda, I. (2008). "Medical management of fibroids". Best Practice & Research Clinical Obstetrics & Gynaecology 22 (4): 655. doi:10.1016/j.bpobgyn.2008.03.001. PMID 18468953.  edit http://www.britishfibroidtrust.org.uk/journals/bft_Sankaran.pdf
  7.  Miyoshi, T; Otsuka, F; Takeda, M; Inagaki, K; Suzuki, J; Ogura, T; Date, I; Hashimoto, K et al. (2004). "Effect of cabergoline treatment on Cushing's disease caused by aberrant adrenocorticotropin-secreting macroadenoma". Journal of endocrinological investigation 27 (11): 1055–9. PMID 15754738.  |displayauthors= suggested (help) edit
  8.  Krüger TH, Haake P, Haverkamp J, et al. (December 2003). "Effects of acute prolactin manipulation on sexual drive and function in males". Journal of Endocrinology 179 (3): 357–65. doi:10.1677/joe.0.1790357. PMID 14656205. 
  9.  Youssef MA, van Wely M, Hassan MA, et al. (March 2010). "Can dopamine agonists reduce the incidence and severity of OHSS in IVF/ICSI treatment cycles? A systematic review and meta-analysis". Hum Reprod Update 16 (5): 459–66. doi:10.1093/humupd/dmq006. PMID 20354100. 
  10.  Carnicella, S.; Ahmadiantehrani, S.; He, D. Y.; Nielsen, C. K.; Bartlett, S. E.; Janak, P. H.; Ron, D. (2009). "Cabergoline Decreases Alcohol Drinking and Seeking Behaviors Via Glial Cell Line-Derived Neurotrophic Factor". Biological Psychiatry 66 (2): 146–153. doi:10.1016/j.biopsych.2008.12.022. PMC 2895406. PMID 19232578.  edit
  11.  Colao, A; Abs R. et al. (January 2008). "Pregnancy outcomes following cabergoline treatment: extended results from a 12-year observational study". Clinical Endocrinology 68 (1): 66–71. doi:10.1111/j.1365-2265.2007.03000.x. PMID 17760883.