bromocriptine

[BROMO- + (ergo)cryptine, alkaloid derived from ergotoxine (a poisonous alkaloid found in the ergot) (from German Ergokryptin : Ergo(t), ergot + Greek kruptos, hidden; see cryptic + -in, -in).]

Brand names: Parlodel®Parlodel® Snap Tabs®

Chemical formula:

Drug Forms:
• Bromocriptine Mesylate Oral tablet (below)
• Bromocriptine Mesylate Oral capsule

Español:
• Mesilato de bromocriptina, Tableta oral
• Mesilato de bromocriptina, Cápsula oral

Bromocriptine Mesylate Oral tablet

What is this medicine?

BROMOCRIPTINE (broe moe KRIP teen) comes from a group of medicines called ergot alkaloids. This medicine is useful in treating menstrual and fertility problems and symptoms caused by certain cancers. It is also used to treat Parkinson's disease and people who have too much growth hormone. This medicine is also used to treat patients with type 2 diabetes.
 
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
•drowsiness
•heart or vessel disease
•high or low blood pressure
•history of heart attack
•kidney disease
•liver disease
•mental illness
•migraines with fainting
•seizures
•an unusual or allergic reaction to bromocriptine, ergot alkaloids, sulfites, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding

How should I use this medicine?

Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take with food to prevent stomach upset. If you are taking Cycloset, take with food within 2 hours of waking in the morning. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.
 
Talk to your pediatrician regarding the use of this medicine in children. While this medicine may be prescribed for children as young as 11 years of age for selected conditions, precautions do apply.
 
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

What may interact with this medicine?

Do not take this medicine with any of the following medications:
•cocaine
•dihydroergotamine, ergotamine, ergoloid mesylates, methysergide, or ergot-type medication
•imatinib
•medicines for fungal infections like ketoconazole and itraconazole
•medicines for HIV infection like amprenavir, delavirdine, efavirenz, indinavir, nelfinavir, ritonavir and saquinavir
•medicines for migraine headache like almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, sumatriptan, zolmitriptan
 
This medicine may also interact with the following medications:
•aspirin and aspirin-like medicines
•chloramphenicol
•isometheptene
•levodopa
•medicines for high blood pressure
•medicines for mental problems and psychotic disturbances
•metoclopramide
•phenylpropanolamine
•probenecid
•stimulant medicines for attention disorders, weight loss, or to stay awake
•sulfa medicines
 
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular checks on your progress. Ask your doctor or health care professional if you should check your blood pressure regularly, especially if you get severe headaches. Report changes in blood pressure if they occur. Contact your doctor or health care professional promptly if you develop an unusual or severe headache or have changes in your vision.
 
If you stop taking this medicine when it is being used for tumor treatment, the tumor may regrow quickly, and your original symptoms may return. Do not stop taking this medicine unless your doctor tells you to.
 
You may get dizzy or drowsy. Do not drive, use machinery, or do anything that requires mental alertness until you know how this medicine affects you. To reduce the risk of dizzy or fainting spells, do not stand or sit up quickly, especially if you are an older patient. Alcohol can make you more dizzy, and increase flushing and rapid heartbeats. Avoid alcoholic drinks. Dizziness is more common after the first dose. Take it before bedtime if possible and be careful getting out of bed.
 
If you find that you have sudden feelings of wanting to sleep during normal activities, like cooking, watching television, or while driving or riding in a car, you should contact your health care professional.
 
Your mouth may get dry. Chewing sugarless gum or sucking hard candy, and drinking plenty of water may help. Contact your doctor if the problem does not go away or is severe.
 
If you have diabetes, learn how to check your blood sugar. Learn the symptoms of low and high blood sugar and how to manage them.
 
If you have low blood sugar, eat or drink something that has sugar. Make sure others know to get medical help quickly if you have serious symptoms of low blood sugar, like if you become unconscious or have a seizure.
 
If you have diabetes, wear a medical identification bracelet or chain to say you have diabetes, and carry a card that lists all your medications.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•changes in vision
•confusion or hallucinations
•dizziness
•fast heartbeat
•feeling anxious
•feeling faint or lightheaded, falls
•increased hunger
•irregular heartbeat
•low blood pressure
•numbness, tingling, or burning in hands or feet
•runny nose
•seizures
•shakiness
•spasm in fingers or toes, or unusual muscle movements
•sweating
•stomach pain
•unusual bleeding, bruising
•unusual or severe headache
•unusually weak or tired
•vomiting
 
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•diarrhea or constipation
•loss of appetite
•mild stomach cramps
•nausea
 
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store below 25 degrees C (77 degrees F). Protect from light. Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 12/1/2003 11:56:00 AM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

A dopamine agonist; as a derivative of ergot alkaloids it is a luteolytic and arbortifacient which suppresses prolactin secretion and lowers plasma ACTH levels. Used as an abortifacient and in the treatment of pituitary-dependent hyperadrenocorticism.

Bromocriptine
Systematic (IUPAC) name
Ergotaman-3',6',18-trione, 2-bromo-12'-hydroxy-2'-(1-methylethyl)-5'alpha-(2 -methylpropyl)-
Identifiers
CAS number	25614-03-3
ATC code	G02CB01 N04BC01
PubChem	31101
DrugBank	APRD00622
ChemSpider	28858
Chemical data
Formula	C32H40BrN5O5
Mol. mass	654.595
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	28% of oral dose absorbed
Metabolism	?
Half life	12-14 hours
Excretion	85% bile (faeces)
Therapeutic considerations
Pregnancy cat.	B(US)
Legal status	?
Routes	oral
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Bromocriptine (Parlodel), an ergoline derivative, is a dopamine agonist that is used in the treatment of pituitary tumors, Parkinson's disease (PD) and neuroleptic malignant syndrome.

Contents 1 Indications 1.1 Parkinson's disease 1.2 Side effects 2 Chemistry 3 See also 4 External links 5 References

Indications

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.

Furthermore, this drug is in a particular class of drugs that are sometimes used to stimulate parts of the HPTA (hypothalamus pituitary testicular axis) which is beneficial for bodybuilders when they have finished a cycle of steroids. The drug in turn aids the pituitary in stimulating the Leydig cells in the testicles.

It has also been 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. 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, at a doseage of 5mg/day orally, has also been used to suppress the immune system in organ transplant patients.^[1]

Since bromocriptine acts as a dopamine agonist, it has potential use in treating cocaine addiction, as the addictive effects of cocaine are caused by its blocking dopamine reuptake. Although bromocriptine has negligible subjective effects when administered alone, studies show it has the potential to significantly ease the cocaine withdrawal syndrome.^[2][3] It is this action that also makes it useful in neuroleptic malignant syndrome.^[4]

There appear to be some connections between insulin insensitivity and dopamine. A company called Veroscience ^[5] 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.^[6] There are also some connections between temperature and dopamine and serotonin production.^[7] 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.

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.^[8] However, a recent Cochrane review found a lack of evidence to support this view.^[9]

Side effects

Bromocriptine use has been associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine).^[10]

Chemistry

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.

See also

• Cabergoline

External links

• www.AcromegalyCommunity.com: Emotional and communal support for those touched by Acromegaly- page discussing drug, side effects, and prescription programs
• MedlinePlus DrugInfo medmaster-a682079
• http://www.drugs.com/pro/bromocriptine.html

References

1. ^ Clodi M, Kotzmann H, Riedl M, Schmidt A, Barnas U, Muhlbacher F, Mustafa G, Horl WH, Waldhausl W, Mayer G, Luger A., 1997. The long-acting dopamine agonist bromocriptine mesylate as additive immunosuppressive drug after kidney transplantation. Nephrol Dial Transplant. 1997 Apr;12(4):748-52.
2. ^ 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.
3. ^ 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.
4. ^ http://www.ncbi.nlm.nih.gov/pubmed/3804991
5. ^ VeroScience
6. ^ 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.
7. ^ http://sulcus.berkeley.edu/mcb/165_001/papers/manuscripts/_281.html
8. ^ 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
9. ^ 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.
10. ^ Boyd, Alan (1995). "Bromocriptine and psychosis: A literature review". Psychiatric Quarterly 66 (1): 87–95. doi:10.1007/BF02238717. http://www.springerlink.com/content/y42v466374524k1m/. Retrieved 2008-09-06. 

v • d • e Other gynecologicals (G02C) Sympathomimetics, labour repressants Ritodrine • Buphenine • Fenoterol Prolactin inhibitors Bromocriptine • Lisuride • Cabergoline • Quinagolide • Metergoline • Terguride Anti-inflammatory products for vaginal administration Ibuprofen • Naproxen • Benzydamine • Flunoxaprofen Other gynecologicals Atosiban

v • d • e Dopaminergics Receptor Ligands Agonists Benzazepines: 6-Br-APB • Fenoldopam • SKF-38,393 • SKF-77,434 • SKF-81,297 • SKF-82,958 • SKF-83,959; Ergot-derivatives: Bromocriptine • Cabergoline • Dihydroergocryptine • Lisuride • LSD • Pergolide; Dihydrexidine-derivatives: 2-OH-NPA • A-86,929 • Dihydrexidine • Dinapsoline • Dinoxyline • Doxanthrine; Morphine-derivatives: Apomorphine • Propylnorapomorphine; Piperazines: ABT-724 • Aripiprazole • Piribedil • WAY-100,635; Others: 7-OH-DPAT • 8-OH-PBZI • A-68,930 • A-77,636 • A-412,997 • ABT-670 • Amantadine • Aplindore • CY-208,243 • Memantine • PD-128,907 • PF-219,061 • Pramipexole • Pukateine • Quinpirole • RDS-127 • Rimantadine • Ropinirole • Rotigotine • SKF-89145 • SKF-89626 Antagonists Typical Antipsychotics: Acepromazine • Azaperone • Benperidol • Bromperidol • Clopenthixol • Chlorpromazine • Chlorprothixene • Droperidol • Flupentixol • Fluphenazine • Fluspirilene • Haloperidol • Loxapine • Mesoridazine • Methotrimeprazine • Molindone • Penfluridol • Perazine • Periciazine • Perphenazine • Pimozide • Prochlorperazine • Promazine • Sulforidazine • Thioridazine • Thiothixene • Trifluoperazine • Triflupromazine • Trifluperidol • Zuclopenthixol; Atypical Antipsychotics: Amisulpride • Asenapine • Clozapine • Iloperidone • Melperone • Olanzapine • Paliperidone • Perospirone • Quetiapine • Risperidone • Sertindole • Sulpiride • Ziprasidone • Zotepine; Antiemetics: AS-8112 • Alizapride • Bromopride • Clebopride • Domperidone • Metoclopramide • Thiethylperazine; Others: Amoxapine • Blonanserin • Buspirone • Butaclamol • N-Ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline • Ecopipam • Eticlopride • Fananserin • Mosapramine • Nafadotride • Nemonapride • Nuciferine • Raclopride • Remoxipride • SB-277,011-A • SCH-23,390 • SKF-83,566 • Spiperone • Spiroxatrine • Stepholidine • Tetrahydropalmatine • Tiapride • UH-232 • Yohimbine Reuptake Inhibitors Plasmalemmal DAT Inhibitors Piperazines: DBL-583 • GBR-12,935 • Nefazodone • Vanoxerine; Piperidines: BTCP • Desoxypipradrol • Dextromethylphenidate • Ethylphenidate • Methylnaphthidate • Methylphenidate • Phencyclidine • Pipradrol; Pyrrolidines: Diphenylprolinol • Methylenedioxypyrovalerone (MDPV) • Naphyrone • Prolintane • Pyrovalerone; Tropanes: β-CPPIT • Altropane • Brasofensine • CFT • Cocaine • Dichloropane • Difluoropine • FE-β-CPPIT • FP-β-CPPIT • Ioflupane • Iometopane • RTI-112 • RTI-113 • RTI-121 • RTI-126 • RTI-150 • RTI-177 • RTI-336 • Tenocyclidine • Tesofensine • Troparil • Tropoxane • WF-11 • WF-23 • WF-31 • WF-33; Others: Amfonelic Acid • Amineptine • Benzatropine • Bromantane • BTQ • BTS-74,398 • Bupropion (Amfebutamone) • Diclofensine • Dimethocaine • Dizocilpine • DOV-102,677 • DOV-21,947 • DOV-216,303 • Etybenzatropine • Fencamine • Fencamfamine • GYKI-52,895 • Indatraline • Ketamine • Lefetamine • LR-5182 • Manifaxine • Medifoxamine • Mesocarb • Nefopam • Nomifensine • NS-2359 • O-2172 • Propylamphetamine • Radafaxine • SEP-225,289 • SEP-227,162 • Sibutramine • Tametraline • Tripelennamine TRPC6 Activators Adhyperforin • Hyperforin Vesicular VMAT Inhibitors Deserpidine • Ibogaine • Reserpine • Tetrabenazine Releasing Agents Oxazolines: 4-Methylaminorex (4-MAR, 4-MAX) • Aminorex • Clominorex • Cyclazodone • Fenozolone • Fluminorex • Pemoline • Thozalinone; Phenethylamines (also Amphetamines, Cathinones, Phentermines, etc): 2-Hydroxyphenethylamine (2-OH-PEA) • 4-Methylamphetamine (4-MA) • 4-Methylmethamphetamine (4-MMA) • α-Ethylphenethylamine (α-Et-PEA) • Alfetamine • Amphetamine (Dextroamphetamine, Levoamphetamine) • Amphetaminil • Amfepentorex • β-Methylphenethylamine (β-Me-PEA) • Benzodioxolylbutanamine (BDB) • Benzodioxolylhydroxybutanamine (BOH) • Benzphetamine • Buphedrone • Butylone • Cathine • Cathinone • Clobenzorex • Clortermine • Diethylcathinone (Diethylpropion, Amfepramone) • Dibutylone • Dimethoxyamphetamine (DMA) • Dimethoxymethamphetamine (DMMA) • Dimethylamphetamine • Dimethylcathinone (Dimethylpropion, Metamfepramone) • Ethcathinone (Ethylpropion) • Ethylamphetamine • Ethylbenzodioxolylbutanamine (EBDB) • Ethylone • Fenethylline • Fenproporex • Flephedrone • Fludorex • Furfenorex • Hordenine • Indanorex • Indanylamphetamine (IAP) • Lophophine (Homomyristicylamine) • Mefenorex • Mephedrone • Methamphetamine (Desoxyephedrine, Methedrine; Dextromethamphetamine, Levomethamphetamine) • Methcathinone (Methylpropion) • Methedrone • Methoxymethylenedioxyamphetamine (MMDA) • Methoxymethylenedioxymethamphetamine (MMDMA) • Methylbenzodioxolylbutanamine (MBDB) • Methylenedioxyamphetamine (MDA; Tenamfetamine) • Methylenedioxyethylamphetamine (MDEA) • Methylenedioxyhydroxyamphetamine (MDOH) • Methylenedioxymethamphetamine (MDMA) • Methylenedioxymethylphenethylamine (MDMPEA; Homarylamine) • Methylenedioxyphenethylamine (MDPEA; Homopiperonylamine) • Methylone • Naphthylamphetamine (NAP) • Ortetamine • Oxaflozane • Parabromoamphetamine (PBA) • Parachloroamphetamine (PCA) • Parafluoroamphetamine (PFA) • Parafluoromethamphetamine (PFMA) • Parahydroxyamphetamine (PHA) • Paraiodoamphetamine (PIA) • Paramethoxyamphetamine (PMA) • Paramethoxyethylamphetamine (PMEA) • Paramethoxymethamphetamine (PMMA) • Paredrine (Norpholedrine, Oxamphetamine) • Phendimetrazine • Phenethylamine (PEA) • Phenmetrazine • Pholedrine • Phenpromethamine • Propylamphetamine • Tiflorex (Flutiorex) • Tyramine (TRA) • Xylopropamine • Zylofuramine; Piperazines: 2,5-Dimethoxy-4-bromobenzylpiperazine (2C-B-BZP) • Benzylpiperazine (BZP) • Methoxyphenylpiperazine (MeOPP; Paraperazine) • Methylbenzylpiperazine (MBZP) • Methylenedioxybenzylpiperazine (MDBZP; Piperonylpiperazine); Others: 2-Aminoindane (2-AI) • 2-Aminotetralin (2-AT) • 4-Benzylpiperidine (4-BP) • Clofenciclan • Cyclopentamine • Cypenamine • Cyprodenate • Feprosidnine • Gilutensin • Heptaminol • Hexacyclonate • Isometheptene • Methylhexanamine • Octodrine • Phthalimidopropiophenone • Propylhexedrine (PHX) • Tuaminoheptane (Tuamine) Enzyme Inhibitors Anabolism PAH Inhibitors 3,4-Dihydroxystyrene TH Inhibitors 3-Iodotyrosine • Aquayamycin • Bulbocapnine • Metirosine • Oudenone AAAD / DDC Inhibitors Benserazide • Carbidopa • Methyldopa Catabolism MAO Inhibitors (MAOIs) Nonselective: Iproclozide • Iproniazid • Isocarboxazid • Nialamide • Phenelzine • Pheniprazine • Tranylcypromine; MAO-A Selective: Befloxatone • Brofaromine • Cimoxatone • Clorgiline • Harmala Alkaloids • Minaprine • Moclobemide • Pirlindole • Toloxatone • Tyrima; MAO-B Selective: Lazabemide • Pargyline • Rasagiline • Selegiline COMT Inhibitors Entacapone • Tolcapone DBH Inhibitors Disulfiram • Nepicastat • Tropolone Others Precursors L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) Cofactors Ferrous Iron (Fe2+) • Tetrahydrobiopterin • Vitamin B3 (Niacin, Nicotinamide → NADPH) • Vitamin B6 (Pyridoxine, Pyridoxamine, Pyridoxal → Pyridoxal Phosphate) • Vitamin B9 (Folic Acid → Tetrahydrofolic Acid) • Vitamin C (Ascorbic Acid) • Zinc (Zn2+) Others Activity Enhancers: Benzofuranylpropylaminopentane (BPAP) • Phenylpropylaminopentane (PPAP)

v • d • e Ergolines Lysergic acid derivatives Bromocriptine • Cabergoline • Ergine • Ergoloid • Ergonovine • Ergotamine • Lysergic acid • Lysergol • LSD • D-Lysergic acid hydroxyethylamide • Lisuride • Lysergic acid methyl ester • Methergine • Methysergide • Pergolide Psychedelic lysergamides AL-LAD • ALD-52 • BU-LAD • CYP-LAD • DAL • DAM-57 • Ergonovine • ETH-LAD • LAE-32 • LSD • LPD-824 • LSM-775 • D-Lysergic acid N-(α-hydroxyethyl)amide • Lysergic acid 2-butyl amide • Lysergic acid 2,4-dimethylazetidide • Methylergonovine • Methylisopropyllysergamide • MLD-41 • PARGY-LAD • PRO-LAD Other ergolines Ergoline Natural sources Argyreia nervosa • Claviceps spp. • Ipomoea tricolor • Ipomoea violacea • Rivea corymbosa

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