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Bromocriptine

An ergoline derivative.

An ergoline derivative and dopamine agonist that is used in the treatment of pituitary tumors, acromegaly, Parkinson’s disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, type 2 diabetes, conditions associated with hyperprolactinemia like amenorrhea, infertility, and hypogonadism, prolactin-secreting adenomas; it is also used to prevent ovarian hyperstimulation syndrome.

It has also used to treat Parkinson’s disease and type 2 diabetes.

 

Bromocriptine, marketed as Parlodel.

 

 

Bromocriptine, a dopaminergic agent, acts by inhibiting the release of prolactin from the anterior pituitary gland.

Amenorrhea, female infertility, galactorrhea, hypogonadism, and acromegaly that are caused by pituitary problems, such as hyperprolactinaemia may be treated by this drug.

Bioavailability is 28% of oral dose

Pregnancy category US: B (No risk in non-human studies).

Routes of administration oral, vaginal, intravenous.

Bioavailability 28% of oral dose absorbed

Metabolism-extensively by liver.

Elimination half-life 12-14 hours

Excretion 85% in bile via feces.2.5-5.5% urine.

A dopamine agonist that decreases prolactin levels.

Bromocriptine mesylate was approved by the FDA for treatment of type 2 diabetes(Cycloset).

Can reduce HbA1c by approximately 0.5 percentage points.

A potent agonist at dopamine D2 receptors and various serotonin receptors.

 

It is a potent agonist at dopamine D2 receptors and  serotonin receptors. 

It  inhibits the release of glutamate, by reversing the glutamate GLT1 transporter.

Bromocriptine agonizes the following monoamine receptors:

Dopamine D1 family

Serotonin 5-HT

Adrenergic α family

Adrenergic β family

Add to bromocrtone

Inhibits the release of glutamate.

Most frequent side effects: nausea, orthostatic hypotension, headaches and vomiting through stimulation of the brainstem vomiting center.

Vasospasms with serious consequences such as myocardial infarction and stroke that have been reported.

It suppresses lactation and is associated with thrombotic  complications.

Peripheral vasospasm can cause Raynaud’s Phenomenon. 

Associated with causing or worsening psychotic symptoms.

Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson’s disease.

After long-term use of dopamine agonists: , withdrawal syndrome may occur.

Withdrawal syndrome is associated with possible side effects: anxiety, panic attacks, dysphoria, depression, agitation, irritability, suicidal ideation, fatigue, orthostatic hypotension, nausea, vomiting, diaphoresis, generalized pain, and drug cravings. 

Bromocriptine withdrawal symptoms are usually short-lived, but may  persist for months or years.

Can cause worsening of liver problems.

Vasospasms in connection with the puerperium, appears to be extremely rare event.

35% of patients experience hirsutism, flushing and dysfunctional uterine bleeding.

Among agents utilized for mastalgia but requires up to 6 months of use to be effective.

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