Bromocriptine

Bromocriptine is a semi synthetic ergot derivative, having potent effects on dopamine receptors.

Pharmacokinetics

Rapid but partial absorption from GIT. It is given orally but absorption is variable. This is because of extensive 1^st pass metabolism

Plasma peak levels are observed 1.5 – 3 hrs after oral administration

Half life is 3hrs

It is metabolized in the liver and metabolites excreted in bile

To improve its bioavailability, high doses can be given by oral route.

Pharmacological actions

1. Prolactin release suppressed
2. Growth hormone release increased (unknown mechanism)
3. Extra pyramidal effects; acts directly on postsynaptic receptors in the nigrostriatal system (Parkinsonism)
4. Reticular formation non specific arousal in the CNS
5. Chemoreceptor trigger zone stimulation causes vomiting

Therapeutic uses

1. Parkinsonism
2. For prevention & suppression of lactation
3. Rx of hyperprolactinemia associated with hypogonadism, galactorrhea, infertility
4. Benign breast diseases
5. Acromegaly (decreased GH)
6. Hepatic encephalopathy (hepatic coma, drowsiness occurs, arousal is difficult, it causes arousal or may have role)

Adverse effects

1. GIT – Nausea, Vomiting, constipation, bleeding from peptic ulcer, reflex esophagitis.
2. CNS – headache, dizziness, drowsiness
3. CVS – postural hypotension, cardiac arrhythmias

At higher doses

a. Dry mouth

b. Confusion

c. Hallucination

d. Pleural effusion

e. Leg cramps, digital vasospasm

f. Red painful swollen feet and hands

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