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Bromocriptine
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| Systematic (IUPAC) name | |
| Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'alpha-(2
-methylpropyl)- |
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| Identifiers | |
| CAS number | |
| ATC code | G02 N04BC01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C32H40BrN5O5 |
| Mol. mass | 654. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component The DrugBank database available at the University of Alberta is a unique Bioinformatics and Cheminformatics resource that combines detailed drug (i A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 595 |
| Pharmacokinetic data | |
| Bioavailability | 28% of oral dose absorbed |
| Metabolism | ? |
| Half life | 12-14 hours |
| Excretion | 85% bile (faeces) |
| Therapeutic considerations | |
| Pregnancy cat. |
A |
| Legal status |
? |
| Routes | oral |
Bromocriptine (brand names include Parlodel), an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors and Parkinson's disease. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction In Pharmacology and Toxicology, a route Ergoline is a Chemical compound whose structural skeleton is contained in a diverse range of Alkaloids and a few Psychedelic drugs A dopamine agonist is a compound that activates Dopamine receptors mimicking the effect of the neurotransmitter Dopamine. The pituitary gland, or hypophysis, is an Endocrine gland about the size of a Pea. See also Cancer A tumor or tumour is the name for a swelling or lesion formed by an abnormal growth of cells (termed neoplastic Parkinson's disease (also known as Parkinson disease or PD) is a degenerative disorder of the Central nervous system that often impairs the sufferer's
Contents |
Uses
Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly may all be caused by pituitary problems, such as hyperprolactinaemia, and therefore, these problems may be treated by this drug. Amenorrhoea ( BE) amenorrhea ( AmE) or amenorrhœa, is the absence of a Menstrual period in a woman of reproductive age Female infertility|Male infertility Infertility primarily refers to the biological inability of a Man or a Woman to contribute to conception. Galactorrhea or galactorrhoea is the spontaneous flow of Milk from the Breast, unassociated with Childbirth or nursing Hypogonadism is a medical term for a defect of the Reproductive system that results in lack of function of the Gonads ( ovaries or testes) Acromegaly (from Greek akros "extreme" or "extremities" and megalos "large" - extremities enlargement is a Syndrome Hyperprolactinaemia ( BrE) or hyperprolactinemia ( AmE) is the presence of abnormally-high levels of Prolactin in the blood
It has also used in some countries to prevent lactation following childbirth if the mother does not wish to breastfeed; one of dopamine's effects on the pituitary is as an antagonist of prolactin production by lactotrophs. Prolactin ( PRL) or Luteotropic hormone ( LTH) is a Peptide hormone primarily associated with Lactation. Lactotrophs (also known as lactotrope mammatroph mammotroph epsilon acidophil prolactin cell and lactotropic cell are cells in the Anterior pituitary which produce However, the FDA removed this indication in 1995, because of concerns with respect to an increased risk of heart attack, seizure and stroke.
Because of prolactin's role in stimulating proliferation of the T-lymphocytes of the immune system, bromocriptine has also been used to suppress the immune system in organ transplant patients. T cells belong to a group of White blood cells known as Lymphocytes, and play a central role in Cell-mediated immunity. An immune system is a collection of mechanisms within an Organism that protects against Disease by identifying and killing Pathogens and Tumor [1]
Since bromocryptine acts as a dopamine agonist, it has potential use in treating cocaine addiction, as the addictive effects of cocaine are caused by it blocking dopamine reuptake. Cocaine ( benzoylmethyl ecgonine) is a Crystalline Tropane Alkaloid that is obtained from the leaves of the Coca plant Reuptake, or re-uptake, is the reabsorption of a Neurotransmitter by the Neurotransmitter transporter of a pre-synaptic Neuron after Although it has negligible subjective effects when administered alone, studies show it has the potential to significantly ease the cocaine withdrawal syndrome. Withdrawal, also known as withdrawal/abstinence syndrome, refers to the characteristic signs and symptoms that appear when a drug that causes Physical dependence is [2][3]
There appear to be some connections between insulin insensitivity and dopamine. Insulin resistance is the condition in which normal amounts of Insulin are inadequate to produce a normal Insulin response from Fat, Muscle Dopamine is a Hormone and Neurotransmitter occurring in a wide variety of animals including both vertebrates and invertebrates A company called Veroscience [4] is using bromocriptine to treat diabetes and obesity, and their website postulates a connection between neurotransmitters and seasonal variation in insulin sensitivity among vetebrate animals. Diabetes mellitus (ˌdaɪəˈbiːtiːz or /ˌdaɪəˈbiːtəs/ /məˈlaɪtəs/ or /ˈmɛlətəs/ often referred to simply as diabetes ( Ancient Greek: grc Obesity is a condition in which excess Body fat has accumulated to such an extent that health may be negatively affected Insulin is a Hormone with intensive effects on both metabolism and several other body systems (eg vascular compliance [5] There are also some connections between temperature and dopamine and serotonin production. [6] In addition, new research indicates that patients with diabetes are more likely to develop Parkinson's disease, which is characterized by a dopamine deficiency in the brain. Diabetes mellitus (ˌdaɪəˈbiːtiːz or /ˌdaɪəˈbiːtəs/ /məˈlaɪtəs/ or /ˈmɛlətəs/ often referred to simply as diabetes ( Ancient Greek: grc Parkinson's disease (also known as Parkinson disease or PD) is a degenerative disorder of the Central nervous system that often impairs the sufferer's
Parkinson's disease
Bromocriptine is an agonist of D2 dopamine receptors and has therefore been used as a treatment for Parkinson's disease. Early studies suggested that treating patients with bromocriptine before levodopa would delay the onset of side effects such as dyskinesia. Dyskinesia refers to involuntary movements similar to a Tic or Chorea. [7] However, a recent Cochrane review found a lack of evidence to support this view. The Cochrane Collaboration is a group of over 11500 volunteers in more than 90 countries who apply a rigorous systematic process to review the effects of interventions tested in biomedical [8]
Structure
Like all ergopeptides, bromocriptine is a cyclol; two peptide groups of its tripeptide moiety (shown in black at the upper left of the Figure) are crosslinked, forming the >N-C(OH)< juncture between the two rings with the amide functionality. Ergoline is a Chemical compound whose structural skeleton is contained in a diverse range of Alkaloids and a few Psychedelic drugs The cyclol hypothesis is the first structural model of a folded, globular Protein. Peptides (from the Greek πεπτίδια, "small digestibles" are short Polymers formed from the linking in a defined order of α- Amino In Chemistry, an amide is one of three kinds of Compounds (sometimes called acid amide the organic Functional group characterized In Organic chemistry, functional groups are specific groups of Atoms within Molecules that are responsible for the characteristic Chemical reactions
See also
External links
Notes and references
- ^ Clodi M, Kotzmann H, Riedl M, Schmidt A, Barnas U, Muhlbacher F, Mustafa G, Horl WH, Waldhausl W, Mayer G, Luger A. Cabergoline (brand names Dostinex and Cabaser an ergot derivative is a potent Dopamine receptor Agonist on D2 receptors MedlinePlus, with the MedlinePlus Medical Encyclopedia, is a website network containing Health information from the world's largest medical Library , 1997. The long-acting dopamine agonist bromocriptine mesylate as additive immunosuppressive drug after kidney transplantation. Nephrol Dial Transplant. 1997 Apr;12(4):748-52.
- ^ Campbell A, Baldessarini RJ, Cremens C, Teicher MH, Marsh E, Kula NS, 1989. Bromocriptine antagonizes behavioral effects of cocaine in the rat. Neuropsychopharmacology 1989 Sep; 2(3):209-24.
- ^ KL Preston, JT Sullivan, EC Strain and GE Bigelow, 1992. Effects of cocaine alone and in combination with bromocriptine in human cocaine abusers. J Pharmacol Exp Ther. 1992 Jul;262(1):279-91.
- ^ VeroScience
- ^ Bromocriptine improves glycaemic control and serum lipid profile in obese Type 2 diabetic subjects: a new approach in the treatment of diabetes. Expert Opin Investig Drugs. 1999 Oct;8(10):1683-1707.
- ^ http://sulcus.berkeley.edu/mcb/165_001/papers/manuscripts/_281.html
- ^ JL Montastruc, O Rascol, JM Senard and A Rascol, 1994. BA randomised controlled study comparing bromocriptine to which levodopa was later added, with levodopa alone in previously untreated patients with Parkinson's disease: a five year follow up. Journal of Neurology, Neurosurgery, and Psychiatry, 1994, Vol 57, 1034-1038
- ^ van Hilten J, Ramaker C, Stowe R, Ives Nj. , 2007. Bromocriptine/levodopa combined versus levodopa alone for early Parkinson's disease. Cochrane Database Syst Rev. 2007 Oct 17;(4):CD003634.
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