Cabergoline can negatively affect the ability to react in some people and this should be considered in cases where a high level of alertness is required, e.g. driving a car and in precision work. Raynaud’s disease (When it is cold the fingers and toes become bluish white, with no pulse, cold, insensitive and numb) There are other medicines such as other ergot alkaloids, medicines to prevent vomiting (metoclopramide), and macrolide antibiotics (such as erythromycin) that may affect the activity and tolerability of Cabergoline. Cabergoline is prescribed for a number of different medical conditions. Your doctor will tell you why it has been prescribed for you. The starting dose of cabergoline should be 1 mg once daily. In view of its long half-life, increases in daily dose of 500 micrograms to 1mg should be made at weekly intervals (initially) or bi-weekly intervals until the optimal dose is reached.

Cabergoline is a tablet treatment used to reduce the production of a hormone called prolactin by the pituitary gland (a gland at the base of the brain). If you have a prolactinoma (overproduction of prolactin by a cluster of cells in the pituitary), cabergoline treatment is also used to shrink the size of the swelling on the pituitary gland. How should I take cabergoline? Martindale: The Complete Drug Reference, 37th edition (2011) ed. Sweetman, S. Pharmaceutical Press, London.

2) what you need to know before you take cabergoline

Cabergoline is a dopaminergic ergoline derivative endowed with potent and long-lasting dopamine D2 receptor agonist properties. In rats the compound, acting at D2 dopamine receptors on pituitary lactotrophic cells, decreases PRL secretion at oral doses of 3-25 mcg/kg, and in vitro at a concentration of 45 pg/ml. In addition, cabergoline exerts a central dopaminergic effect via D2 receptor stimulation at doses higher than those effective in lowering serum PRL levels. Improvement of motor deficit in animal models of Parkinson's disease was present at oral daily doses of 1-2.5 mg/kg in rats and at s.c. doses of 0.5-1 mg/kg in monkeys. Each amber glass bottle contains 20 tablets and a silica gel desiccant sealed with an aluminium membrane and a child-resistant screw cap. Renal insufficiency or ureteral/abdominal vascular obstruction that may occur with pain in the loin/flank, and lower limb oedema, as well as any possible abdominal masses or tenderness that may indicate retroperitoneal fibrosis. The concomitant use of antiparkinson non-dopamine agonists (e.g. selegiline, amantadine, biperiden, trihexyphenidyl) was allowed in clinical studies for patients receiving cabergoline. In studies where the pharmacokinetic interactions of cabergoline with L-dopa or selegiline were evaluated, no interactions were observed. Lower doses of cabergoline should be considered in patients with severe hepatic insufficiency. Compared to normal volunteers and those with lesser degrees of hepatic insufficiency, an increase in AUC has been seen in patients with severe hepatic insufficiency (Child-Pugh Class C) who received a single 1 mg dose.

High levels of prolactin occur in people with prolactinomas. A prolactinoma is a non-cancerous swelling in the pituitary gland. This can cause various symptoms including reduced fertility, breast changes, and headaches. Prolactinomas can be treated successfully with medicines which reduce the production of prolactin, such as cabergoline. In these cases, treatment is usually long-term. Cabergoline can cause somnolence (extreme drowsiness) and sudden sleep onset. Persons affected by this should therefore not drive or take part in activities in which reduced alertness could incur a risk of serious harm (e.g. using machines), until such recurrent episodes and somnolence have resolved. If affected, consult your doctor. The pharmacokinetic and metabolic profiles of cabergoline have been studied in healthy volunteers of both sexes , in female hyperprolactinemic patients and in parkinsonian patients. After oral administration of the labelled compound, radioactivity was rapidly absorbed from the gastrointestinal tract as the peak of radioactivity in plasma was between 0.5 and 4 hours. Ten days after administration about 18/20% and 55/72% of the radioactive dose ( 3H-cabergoline/ 14C-cabergoline) was recovered in urine and faeces, respectively. Unchanged drug in urine accounted for 2-3% of the dose. Patients should be evaluated during dose escalation to determine the lowest dosage that produces the therapeutic response. Monitoring of serum prolactin levels at monthly intervals is advised since, once the effective therapeutic dosage regimen has been reached, serum prolactin normalisation is usually observed within two to four weeks. If the headache is severe or continues, speak with your doctor straightaway; otherwise, ask your pharmacist to recommend a suitable painkillerOn the basis of the elimination half-life, steady state conditions should be achieved after 4 weeks, as confirmed by the mean peak plasma levels of cabergoline obtained after a single dose (37 +8 pg/ml) and after a 4 week multiple-regimen (101 +43 pg/ml). In vitro experiments showed that the drug at concentrations of 0.1-10 ng/ml is 41-42% bound to plasma proteins. Before you are given Cabergoline your doctor will arrange for you to have tests to assess the condition of your heart. Your doctor will continue to monitor your medical condition while taking Cabergoline. As expected for dopamine agonists, dose response for both efficacy and side effects appears to be linked to individual sensitivity. Optimization of dose should be obtained through slow initial dose titration, from starting doses of 1 mg daily. The dosage of concurrent levodopa may be gradually decreased, while the dosage of cabergoline is increased, until the optimum balance is determined. In view of the long half-life of the compound, increments of the daily dose of 0.5-1 mg should be done at weekly (initial weeks) or bi-weekly intervals, up to optimal doses. As cabergoline suppresses milk production, you should not take it whilst breast feeding. It is often helpful to see whether your periods start again when you have stopped breast feeding, and reassess your prolactin levels, before deciding whether or not to resume cabergoline treatment. Sometimes microprolactinomas resolve after a pregnancy. Rarely, women with large macroprolactinomas will be advised to continue cabergoline treatment and not to breast feed. Your endocrinologist will discuss these decisions with you. Are there any medicines I should avoid when taking cabergoline? Cabergoline is indicated for the inhibition of physiological lactation soon after delivery and for suppression of already established lactation:

Cabergoline generally exerts a hypotensive effect in patients on long-term treatment; Postural hypotension, hot flushes** Cabergoline should only be used during pregnancy if clearly indicated and after an accurate benefit/risk evaluation. The pharmacodynamic effects of cabergoline have been studied in healthy volunteers, puerperal women and hyperprolactinaemic patients. After a single oral administration of cabergoline (0.3 - 1.5 mg), a significant decrease in serum PRL levels was observed in each of the populations studied. The effect is prompt (within 3 hours from administration) and persistent (up to 7 - 28 days in healthy volunteers and hyperprolactinaemic patients, and up to 14 - 21 days in puerperal women). The PRL-lowering effect is dose-related both in terms of degree of effect and duration of action. All patients must undergo a cardiovascular evaluation, including echocardiogram to assess the potential presence of asymptomatic valvular disease. Also perform baseline investigations of erythrocyte sedimentation rate or other inflammatory markers, lung function/chest X-ray, serum creatinine and renal function prior to initiation of therapy. If fibrotic valvular disease is detected, the patient should not be treated with cabergoline.Cabergoline prevents the production of a chemical called prolactin. Prolactin is involved in a number of processes within the body, including milk production after childbirth. Cabergoline is therefore helpful in preventing or reducing milk production when this is needed for medical reasons. Cabergoline has been associated with somnolence. Dopamine agonists can be associated with sudden sleep onset episodes in patients with Parkinson's disease. Sudden onset of sleep during daily activities, in some cases without awareness or warning signs, has been reported uncommonly. Patients must be informed of this and advised to exercise caution while driving or operating machines during treatment with cabergoline. Patients who have experienced somnolence and/or an episode of sudden sleep onset must refrain from driving or operating machines. Furthermore a reduction in dosage or termination of therapy may be considered. (See section 4.7) As Cabergoline will stop you from producing milk for your baby, you should not take Cabergoline if you plan to breastfeed. If you need to take Cabergoline you should use another method for feeding your baby. Nursing mothers should note that the quantity of milk can diminish. A decrease in haemoglobin values have been observed in amenhorrheic women during the first few months after menses. Read the directions from your doctor carefully and take cabergoline exactly as you are told to. If you are taking cabergoline for the first time, your doctor may give you a small dose and then gradually increase your dose. Slowly increasing your dose like this will help to reduce side-effects, such as dizziness, which can occur during the first few days of treatment.

are allergic to cabergoline, other ergot alkaloids (e.g. bromocriptine), or to any of the other ingredients of this medicine (listed in section 6) Lower doses should be considered in patients with severe hepatic insufficiency (Child-Pugh Class C). Contraindications

Patient leaflet - CABERGOLINE 2 MG TABLETS

Cabergoline is a dopaminergic ergoline derivative endowed with a potent and long-lasting PRL-lowering activity. It acts by direct stimulation of the D 2-dopamine receptors on pituitary lactotrophs, thus inhibiting PRL secretion. In rats the compound decreases PRL secretion at oral doses of 3-25 mcg/kg, and in-vitro at a concentration of 45 pg/ml. In addition, cabergoline exerts a central dopaminergic effect via D 2 receptor stimulation at oral doses higher than those effective in lowering serum PRL levels. The long lasting PRL-lowering effect of cabergoline is probably due to its long persistence in the target organ as suggested by the slow elimination of total radioactivity from the pituitary after single oral dose in rats (t ½of approximately 60 hours). Development of a widespread itchy rash, difficulty breathing with or without wheezing, feeling faint, unexplained swelling of the body or tongue or any other symptoms which appear to come on rapidly after taking this medication and make you feel unwell. These may be indicative of an allergic reaction. This is an uncommon side effect (may affect up to 1 in 100 people).