Bromocriptine

Category: Medicines

Type

Involuntary and voluntary

Introduction and description

Bromocriptine is sold under the trade names Parlodel, Cycloset, and Brotin (Pakistan), it is an ergoline derivative and a pharmaceutical used in the treatment of:

• Pituitary tumors,
• Parkinson's disease (PD),
• Hyperprolactinaemia,
• Neuroleptic malignant syndrome (NMS)  - a life-threatening neurological disorder  caused by an adverse reaction to antipsychotic drugs 
• Amenorrhea - the absence of a menstrual period in a woman of reproductive age.
• Female infertility
• Galactorrhea - the spontaneous flow of milk from the breast, unassociated with childbirth or nursing
• Hypogonadism - describes a diminished functional activity of the gonads – the testes and ovaries in males and females
• Acromegaly - is a syndrome that results when the anterior pituitary gland produces excess growth hormone

In 2009, bromocriptine mesylate was approved by the FDA for treatment of type 2 diabetes under the trade name Cycloset.

This eclectic mixture of illnesses and diseases means I have had to give it a section on its own.  This is a quote from Wikipedia “It is currently unknown how this drug improves glycemic control”

The more general side effects it produces are shown below, but it has a very impressive record for producing hallucinations.  To quote the literature:

“Bromocriptine use has been anecdotically associated with causing or worsening psychotic symptoms  - its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine.”

This has not gone unnoticed in the so called recreational drug user community.  Bromocriptine directly stimulates Dopamine-2-receptors and it's a LSD-like derivate but is without the effects that LSD has, making it completely ineffective as a recreational drug.  Unfortunately this appears not to be understood by some users.  Being precise, Bromocriptine is a semisynthetic derivative of a natural ergot alkaloid, ergocriptin (a derivative of lysergic acid - LSA), so the link is even weaker than most users seem to think.

This person [from EROWID] used a combination of Bromocriptine, Amantadine [prescribed] and Cannabis.  The next day he realised he had altered his brain.....

 Remember that apart from the cannabis, these drugs were prescribed to this chap.

Background

If we concentrate on the hallucinations first, taking a snapshot in time and using the figures from ehealthme derived from the ADRs submitted by doctors to the FDA and SEDA we find the following:

On Jul, 29, 2015: 772 people reported to have side effects when taking Bromocriptine mesylate. Among them, 27 people (3.50%) have Hallucination.

Time on Bromocriptine mesylate when people have Hallucination  :

	< 1 month	1 - 6 months	6 - 12 months	1 - 2 years	2 - 5 years	5 - 10 years	10+ years
Hallucination	100.00%	0.00%	0.00%	0.00%	0.00%	0.00%	0.00%

Age of people who have Hallucination when taking Bromocriptine mesylate  :

	0-1	2-9	10-19	20-29	30-39	40-49	50-59	60+
Hallucination	0.00%	0.00%	0.00%	3.85%	0.00%	3.85%	0.00%	92.31%

This figure clearly excludes those who are using this drug 'recreationally'.  But we also need to take into account the trade names, so :

On Aug, 11, 2015: 1,795 people reported to have side effects when taking Parlodel. Among them, 77 people (4.29%) have Hallucination.

Time on Parlodel when people have Hallucination  :

	< 1 month	1 - 6 months	6 - 12 months	1 - 2 years	2 - 5 years	5 - 10 years	10+ years
Hallucination	33.33%	33.33%	33.33%	0.00%	0.00%	0.00%	0.00%

Other side effects

Using the figures from eHealthme again we find that the most common Bromocriptine mesylate side effects, calculated by using ADRs are:

• Nausea And Vomiting  (53 reports)
• Nausea  (51 reports)
• Neuroleptic Malignant Syndrome  (50 reports)
• Fever (49 reports)
• Dizziness  (42 reports)
• Abnormal Behaviour  (37 reports)
• Headache  (32 reports)
• Drug Exposure During Pregnancy  (32 reports)
• Fatigue  (31 reports)
• Breathing Difficulty  (30 reports)

Other frequent side effects are , orthostatic hypotension,  vomiting through stimulation of the brainstem vomiting centre. Bromocriptine can cause worsening of liver problems. Vasospasms with serious consequences such as myocardial infarction and stroke have been reported.   Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson's disease. 

Most common side effects of Cycloset  by gender  :

Female	Male
Somnolence	Hypotension
Nausea	Dizziness
Hypotension	Syncope
Hypoglycaemia	Hyperhidrosis
Vomiting	Loss Of Consciousness
Dyskinesia	Anxiety
Dyspnoea	Asthenia
Herpes Zoster	Bradycardia
Cerebrovascular Accident	Renal Failure Acute
Condition Aggravated	Blood Electrolytes Abnormal

Death.

 

Using the ehealthme figures and taking a snapshot we find the following. 

We have included the figures under all the tradenames as well

 

 

 

On Aug, 25, 2015: 773 people reported to have side effects when taking Bromocriptine mesylate. Among them, 8 people (1.03%) have Death [source ehealthme].

Time on Bromocriptine mesylate when people have Death  :

	< 1 month	1 - 6 months	6 - 12 months	1 - 2 years	2 - 5 years	5 - 10 years	10+ years
Death	0.00%	0.00%	100.00%	0.00%	0.00%	0.00%	0.00%

Age of people who have Death when taking Bromocriptine mesylate  :

	0-1	2-9	10-19	20-29	30-39	40-49	50-59	60+
Death	0.00%	0.00%	0.00%	0.00%	0.00%	71.43%	14.29%	14.29%

 

On Jul, 30, 2015: 1,795 people reported to have side effects when taking Parlodel. Among them, 17 people (0.95%) have Death.

Time on Parlodel when people have Death  :

	< 1 month	1 - 6 months	6 - 12 months	1 - 2 years	2 - 5 years	5 - 10 years	10+ years
Death	0.00%	100.00%	0.00%	0.00%	0.00%	0.00%	0.00%

 

 

The chemistry of Bromocriptine

Bromocriptine is a potent agonist at dopamine D2 receptors and various serotonin receptors. It also inhibits the release of glutamate, by reversing the glutamate GLT1 transporter.  Bromocriptine agonizes the following monoamine receptors.

• Dopamine D1 family
  • D1 (Ki=682 nM)
  • D5(Ki=496 nM)
• Dopamine D2 family
  • D2 (Ki=2.96 nM)
  • D3 (Ki=5.42 nM)
  • D4 (Ki=328 nM)
• Serotonin 5-HT
  • 5-HT1A (Ki=12.9 nM)
  • 5-HT1B (Ki=355 nM)
  • 5-HT1D (Ki=10.7 nM)
  • 5-HT2A (Ki=107 nM)
  • 5-HT2B (Ki=56.2 nM)
  • 5-HT2C (Ki=741 nM)
  • 5-HT6 (Ki=33 nM)
• 

   
  Adrenergic alpha family
  • alpha1A (Ki=4.17 nM)
  • alpha1B (Ki=1.38 nM)
  • alpha1D (Ki=1.12 nM)
  • alpha2A (Ki=11.0 nM)
  • alpha2B (Ki=34.7 nM)
  • alpha2C (Ki=28.2 nM)
• Adrenergic beta family
  • beta1 (Ki=589 nM)
  • beta2 (Ki=741 nM)

Other properties for serotonin are yet unknown.

How it works

Look at the list - dopamine, serotonin - this is an unbelievable drug to put onto the market. 

Bromocriptine, 2-bromoergocriptine, is a semisynthetic derivative of a natural ergot alkaloid, ergocriptin.  Ergocriptin is a derivative of lysergic acid, which is synthesized by bromination of ergocriptin using N-bromosuccinimide.

The only mechanism that appears to seem plausible as the means by which hallucinations were achieved is poisoning.

But there are also hints that this drug causes serotonin imbalance.

References and further reading

 

 

The full list of all the Bromocriptine side-effects on the eHealthme website can be seen by following this LINK.

All the photos on this page are by Robert and Shana Parke-Harrison. 

Robert ParkeHarrison (born 1968) is a photographer, best known for his work with wife Shana ParkeHarrison in the area of fine art photography.

 

Related observations

Hallucination

• Addictive psychosis from bromocriptine 005259
• Bromocriptine and psychosis 005257
• Bromocriptine and schizophrenia 005256
• Ergotism and pharmaceuticals 006805
• Giant has hallucinations 005230
• Mid-stimulation psychosis in the course of in vitro fertilization procedure with the use of clomiphene citrate and bromocriptine - case study 027441
• Mid-stimulation psychosis in the course of in vitro fertilization procedure with the use of clomiphene citrate and bromocriptine - case study 017649
• Mother's psychosis after birth 005258
• Transient psychosis in women on clomiphene, bromocriptine, domperidone and related endocrine drugs 017898
• Two new Mums with hallucinations 005231

In time

Synaesthesia, Pure or enhanced perception, Inter composer communication, Vision, Dream, Perception recall, Exploring group perception

• Addictive psychosis from bromocriptine 005259
• Brainkill 005252
• Mother's psychosis after birth 005258