Cabergoline

Chemical formula: C₂₆H₃₇N₅O₂  Molecular mass: 451.604 g/mol  PubChem compound: 54746

Interactions

Cabergoline interacts in the following cases:

Macrolides

As with other ergot derivatives, cabergoline should not be used with macrolide antibiotics (e.g. erythromycin) due to increased systemic bioavailability of cabergoline.

Phenothiazines, butyrophenones, thioxanthenes, metoclopramide

Since cabergoline exerts its therapeutic effect by direct stimulation of dopamine receptors, it should not be concurrently administered with drugs which have dopamine-antagonist activity (such as phenothiazines, butyrophenones, thioxanthenes, metoclopramide) since these might reduce the prolactin-lowering effect of cabergoline.

Pregnancy

There are no adequate and well-controlled studies from the use of cabergoline in pregnant women. Animal studies have not demonstrated teratogenic effects, but reduced fertility and embryo-toxicity were observed in association with pharmacodynamic activity.

In a twelve year observational study on pregnancy outcomes following cabergoline therapy, information is available on 256 pregnancies. Seventeen of these 256 pregnancies (6.6%) eventuated in major congenital malformations or abortion. Information is available on 23/258 infants who had a total of 27 neonatal abnormalities, both major and minor. Musculoskeletal malformations were the most common neonatal abnormality (10), followed by cardio-pulmonary abnormalities (5). There is no information on perinatal disorders or long-term development of infants exposed to intra-uterine cabergoline. Based on recent published literature, the prevalence of major congenital malformations in the general population has been reported to be 6.9% or greater. Rates of congenital abnormality vary between different populations. It is not possible to accurately determine if there is an increased risk as no control group was included.

Cabergoline should only be used during pregnancy if clearly indicated and after an accurate benefit/risk evaluation.

Due to the long half-life of the drug and limited data on in utero exposure, women planning to become pregnant should discontinue cabergoline one month before intended conception. If conception occurs during therapy, treatment should be discontinued as soon as pregnancy is confirmed to limit foetal exposure to the drug.

Nursing mothers

In rats, cabergoline and/or its metabolites are excreted in milk. No information is available on the excretion in breast milk in humans; however, mothers should be advised not to breast-feed in case of failed lactation inhibition/suppression by cabergoline. Since it prevents lactation, cabergoline should not be administered to mothers with hyperprolactinemic disorders who wish to breast-feed their infants.

Effects on ability to drive and use machines

Patients should be careful when performing actions which require fast and accurate reaction during treatment initiation.

During the first days of cabergoline administration, patients should be cautioned about re-engaging in activities requiring rapid and precise responses such as driving an automobile or operating machinery.

Patients being treated with cabergoline and presenting with somnolence must be informed to refrain from driving or engaging in activities where impaired alertness may put themselves and others at risk of serious injury or death (e.g. operating machines) until such episodes and somnolence have resolved.

Adverse reactions


Adverse events are generally dose-related. In patients known to be intolerant to dopaminergic drugs, the likelihood of adverse events may be lessened by starting therapy with cabergoline at reduced doses, e.g. 0.25 mg once a week, with subsequent gradual increase until the therapeutic dosage is reached. If persistent or severe adverse events occur, temporary reduction of dosage followed by a more gradual increase, e.g. increments of 0.25 mg/week every two weeks, may increase tolerability.

The following undesirable effects have been observed and reported during treatment with cabergoline with the following frequencies: Very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to ≤1/100); rare (≥1/10,000 to ≤1/1,000); very rare (≤1/10,000), not known (cannot be estimated from the available data).

MedDRA
System Organ Class
Frequency Undesirable Effects
Cardiac disorders Very Common Valvulopathy (including regurgitation) and related disorders
(pericarditis and pericardial effusion)
Uncommon Palpitations
Not Known Angina pectoris
Respiratory, thoracic and
mediastinal disorders
Uncommon Dyspnea, pleural effusion, fibrosis, (including pulmonary
fibrosis), epistaxis
Very rare Pleural fibrosis
Not Known Respiratory disorder, respiratory failure, pleuritis, chest
pain
Immune system disorders Uncommon Hypersensitivity reaction
Nervous system disorders Very common Headache*, dizziness/vertigo*
Common somnolence
Uncommon Transient hemianopsia, syncope, paresthesia
Not Known Sudden sleep onset, tremor
Eye disorders Not Known Visual impairment
Psychiatric disorders Common Depression
Uncommon Increased libido
Not Known Aggression, delusions, hypersexuality, pathological
gambling, psychotic disorder, hallucinations
Vascular disorders Common Cabergoline generally exerts a hypotensive effect in
patients on long-term treatment; Postural hypotension, hot
flushes**
Uncommon Digital vasospasm, fainting
Gastrointestinal disorders Very common Nausea*, dyspepsia, gastritis, abdominal pain*
Common Constipation, vomiting**
Rare Epigastric pain
General disorders and
administration site conditions
Very Common Asthenia***, fatigue
Uncommon Oedema, peripheral oedema
Hepato-biliary disorders Not Known Hepatic function abnormal
Skin and subcutaneous tissue
disorders
Uncommon Rash, alopecia
Musculoskeletal and
connective tissue disorders
Uncommon Leg cramps
Reproductive system and
breast disorders
Common Breast pain
Investigations Common Asymptomatic decreases in blood pressure (≥20 mmHg
systolic and ≥10 mmHg diastolic)
Uncommon A decrease in haemoglobin values have been observed in
amenhorrheic women during the first few months after
menses.
Not Known Blood creatinine phosphokinase increased, liver function
tests abnormal

* Very common in patients treated for hyperprolactinaemin disorders; Common in patients treated for inhibition/supression of lactation
** Common in patients treated for hyperprolactinaemin disorders; Uncommon in patients treated for inhibition/supression of lactation
*** Very common in patients treated for hyperprolactinaemin disorders; Uncommon in patients treated for inhibition/supression of lactation

Impulse control disorders

Pathological gambling, increased libido, hypersexuality, compulsive spending or buying, binge eating and compulsive eating can occur in patients treated with dopamine agonists including cabergoline.

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