Cabergoline: Overcoming Hyperprolactinemia Challenges

Overview:

Cabergoline is used to treat excessive blood levels of prolactin, which can cause difficulties with bone loss, irregular menstruation, infertility, unwanted breast milk, and sexual dysfunction. It also works well to lower elevated prolactin levels brought on by specific cancers. The United States Food and Drug Administration (USFDA) approved the drug administration on December 23, 1996.

Drug Group:

Cabergoline is a member of the class of drugs known as dopamine receptor agonists.

Indications:

Conditions involving excessive prolactin levels in the body are treated with Cabergoline tablets. This may occur as a result of specific pituitary gland growths or for other unidentified causes.

Contraindications:

Patients with the following conditions should not utilize Cabergoline tablets:

• Uncontrolled hypertension or allergy to ergot derivatives (a fungi derivative).

• An echocardiography that reveals thickening or narrowing of the valve, as well as any tests performed before treatment that demonstrate a history of heart valve issues.

• A history of stomach, heart lining, or lung fibrosis (tissue thickening).

Dosage Forms and Available Strengths:

Cabergoline is available as oral tablets. To treat pituitary tumors or elevated prolactin levels, adults should typically begin with 0.25 mg (milligrams) twice a week. Depending on the prolactin levels, the physician may change the dosage every four weeks. If necessary, they may even increase it to one milligram twice a week. The doctor should determine the dosage for children.

For Patients:

What Is Hyperprolactinemia?

An excess of the hormone prolactin in the blood is known as hyperprolactinemia. Normal breast milk production during and after pregnancy is aided by prolactin. A noncancerous tumor in the pituitary gland, which is in charge of producing prolactin, is frequently the cause of this medical condition.

What Are the Clinical Uses of Cabergoline?

Cabergoline is used to treat a medical disorder called hyperprolactinemia. This occurs when the body produces an excessive amount of prolactin, a naturally occurring chemical. Prolactin typically aids in the production of milk in nursing mothers, but excessive levels of the hormone can lead to infertility, sexual dysfunction, and bone loss in males and non-breastfeeding women. Cabergoline is a member of the class of drugs known as dopamine receptor agonists. It functions by lowering the body's prolactin levels, which helps lessen the symptoms brought on by elevated prolactin levels.

How Should Cabergoline Be Used?

Cabergoline is available as an oral tablet. Usually, it is taken twice a week, with or without food. Pay close attention to the instructions on the prescription label, and ask the pharmacist or doctor to clarify any parts one is unsure about. Follow the directions on the capsule exactly. Take it exactly as directed; do not take less or more of it. Most likely, the doctor will begin with a modest dosage of Cabergoline and increase it gradually, no more than once every four weeks. Never discontinue taking Cabergoline without first consulting a doctor. The doctor will progressively reduce the dosage.

What Are the Side Effects of Cabergoline?

Cabergoline may cause adverse reactions. If any of these symptoms affect a lot or persist, let the physician know:

• Exhaustion.

• Difficulty passing gas.

• Heartburn.

• Regurgitating.

• Breast pain.

• Severe menstrual pain.

• Chest pain.

• Feeling like passing out.

• Tingling or numbness in the hands, arms, legs, or feet.

• Lightheadedness.

There could be further negative consequences of Cabergoline. Certain adverse effects may be dangerous. Immediately contact a doctor or seek medical attention if one is experiencing:

• Breathing difficulties.

• Chest pain.

• Less frequent urination.

• Coughing.

• Hand, foot, or leg swelling.

• Weird lumps or pain in the belly.

• Difficulty breathing when lying down.

• Pain in the back, side, or groin.

What Are the Things to Inform the Doctor Before Taking Cabergoline?

• Allergy Information: If one has an allergy to Cabergoline or any related medicine, such as Pergolide, Dihydroergotamine, or Bromocriptine, let the doctor and pharmacist know. Please also list any further medications or ingredient allergies.

• Medication Interactions: Report all vitamins, supplements, herbal items, prescription and over-the-counter drugs, and herbal teas that one is taking or intends to take. Mention in particular antihistamines, blood pressure or mental health medications, and drugs such as Metoclopramide or Haloperidol.

• Medical History: Tell about any prior usage of illegal drugs, high blood pressure, problems with the heart, lungs, or abdomen, or heart valve disease. The doctor might need to closely monitor or change the drug. Inform the physician if one has ever had a liver illness.

• Pregnancy and Breastfeeding: Inform the doctor if one is nursing a baby or intends to become pregnant. Cabergoline may have an impact on lactation.

• Side Effects and Precautions: Recognize that Cabergoline may induce lightheadedness or fainting, particularly when getting up suddenly from a lying position. When getting up, take time to prevent this. It should be noted that some people who use Cabergoline may acquire obsessive habits like gambling or increased sexual desire. Notify the physician if such behaviors are observed, and let family members know about this danger so they can keep an eye on it.

Dietary Consideration: Unless the physician instructs it otherwise, stick to the same diet as usual.

Storage: Keep this medication out of children's reach and keep it in the sealed container it came in. Keep it out of the bathroom and at room temperature, away from sources of heat and moisture.

Disposal: It is important to dispose of leftover drugs properly to avoid pet or child ingestion. Cabergoline should not be flushed down the toilet. The best way to get rid of the medication is to use a service called medicine take-back. To find out more about take-back initiatives in the area, speak with the pharmacist or get in touch with the recycling and trash department. Keep any medications out of children's reach and sight. Many containers are easily opened by young children and are not child-resistant. Always secure the safety caps on medications to prevent poisoning, and store them immediately in a secure spot that is out of their sight and reach.

Missed Dose: Take the missed dosage as soon as recalled. On the other hand, if the next dose is approaching, skip the one that was missed and stick to the usual dosage plan. To make up for a missed dose, never take two.

Overdose: Please contact the poison control hotline if someone takes too much of Cabergoline. Make the emergency services call immediately if the person has passed out, had a seizure, is having difficulty breathing, or cannot be roused.

Indications that this medication is being taken in excess include:

• A stuffy nose.

• Passing out.

• Acquiring perceptions of unseen objects or sounds.

For Doctors

Pharmacodynamics: Both healthy volunteers and those with elevated prolactin levels have had studies done on how Cabergoline lowers prolactin levels. Dosages greater than 0.2 mg (milligrams) began to decrease prolactin in healthy volunteers, with dosages of 0.5 mg or more causing the greatest reduction. Higher doses had longer-lasting effects and performed better and faster. Prolactin was completely halted in nearly all participants in research involving healthy volunteers for three hours at doses of 0.5 mg, 1 mg, and 1.5 mg; the higher levels proved to be more effective. For people with elevated levels of the hormone, a single dosage of 0.6 mg of Cabergoline decreased prolactin by the same amount as 2.5 mg of Bromocriptine; however, the effects of Cabergoline lasted much longer (24 days versus 24 hours). Compared to Cabergoline, which took 48 hours to take full action, Bromocriptine showed results in just six hours. Even at doses as high as 2 mg, Cabergoline did not affect other pituitary hormones, such as growth hormone or thyroid-stimulating hormone, in different research involving 72 healthy volunteers.

Mechanism of Action: Prolactin is a hormone that is normally released by the pituitary gland and is regulated by the hypothalamus, a region of the brain. The primary mechanism of this regulation is releasing dopamine by the brain's specific neurons. A drug called Cabergoline binds to D2 receptors in the same way as dopamine and has a prolonged half-life. Lab studies demonstrate that the animal pituitary gland cells directly inhibit the prolactin released by Cabergoline. In tests, animals receiving Reserpine, a medication that raises prolactin levels, had lower prolactin levels when exposed to Cabergoline. Additionally, research indicates that Cabergoline does not bind strongly to other receptors, such as 5-HT1 (hydroxytryptamine) and 5-HT2-serotonin receptors, dopamine D1, α1 (alpha)- and α2-adrenergic, and others.

Pharmacokinetics:

• Absorption: Within two to three hours of consumption, the blood level of Cabergoline reaches its maximum. The blood level of Cabergoline appears to rise in proportion to the administered dosage. When compared to a single dose, the levels in the blood will be two to three times higher if one takes it consistently.

• Distribution: The body's tissues and organs are among the many places where Cabergoline is found. It especially concentrates and remains for an extended period in the pituitary gland and thus works well to reduce prolactin levels. Although it appears to remain in the uterine wall, Cabergoline does not appear to reach the fetus in pregnant animals. Additionally, nursing neonates may come into contact with it because it is found in the milk of lactating animals.

• Metabolism: The primary mechanism of Cabergoline's substantial breakdown is hydrolysis. There appears to be no effect on specific enzymes within the body. The efficacy of Cabergoline in treating disorders such as elevated prolactin levels is not influenced by its breakdown products.

• Excretion: About 22 percent of the Cabergoline is removed by urine and around 60 percent through feces in over 20 days. Urine contains very little of the medication unaltered. Renal issues have little effect on the body's ability to excrete Cabergoline. Cabergoline levels in the blood can noticeably rise in patients with liver problems, particularly severe ones. Hence, alertness is recommended.

• Special Populations: Moderate-to-severe renal issues do not appear to be associated with Cabergoline. The levels of Cabergoline do not significantly vary in patients with mild-to-moderate liver disease, but in severe situations, there may be a noticeable increase. Much research has not been done on how Cabergoline levels change with age.

• Food-Drug Interaction: Studies on healthy persons have shown that eating does not affect the way Cabergoline functions in the body.

What Is the Prescribed Dosage and Method of Administration for Cabergoline?

Cabergoline Tablets are prescribed at a starting dose of 0.25 mg twice a week. Depending on the patient's prolactin levels, the dose can be increased by 0.25 mg twice a week, with a maximum of one mg twice a week. The doctor should examine the patient's heart and may perform an echocardiography to check for heart valve issues before initiating treatment. At least every four weeks, the doctor should increase the patient's dosage to monitor how well they are responding. The lowest effective dose should be administered, and alternative treatments may be explored if greater doses are ineffective. Long-term Cabergoline users should undergo routine cardiac exams; echocardiograms may be necessary. The doctor may decide to stop Cabergoline if prolactin levels remain normal for six months, but they will still need to monitor prolactin levels at regular intervals to see whether therapy has to be restarted. The efficacy of Cabergoline after a 24-month course of treatment is unknown.

Drug Interactions: It is not recommended to take Cabergoline with other drugs known as D2 antagonists. Metoclopramide, Thioxanthenes, Butyrophenones, and Phenothiazines are a few examples of these medications. Combining these drugs may have unintended consequences or lessen Cabergoline’s efficacy. Therefore, it is crucial to refrain from taking them simultaneously.

Clinical Studies: Studies comparing Cabergoline to placebo and Bromocriptine in women with elevated prolactin levels showed that it was effective in decreasing prolactin levels. Prolactin levels in the placebo trial decreased as a result of Cabergoline, and after four weeks, normalization was seen in 29 percent, 76 percent, 74 percent, and 95 percent of patients at varying doses. During eight weeks, Cabergoline was able to normalize prolactin levels in 77 percent of patients when compared to 59 percent of patients who took Bromocriptine twice daily. Furthermore, Cabergoline decreased galactorrhea (breast milk production) in 73 percent of patients compared to 56 percent with Bromocriptine and helped women resume regular menstrual cycles in 77 percent of cases compared to 70 percent with the drug.

Warnings and Precautions:

• Pregnancy: The use of dopamine agonists should be avoided if one has high blood pressure associated with pregnancy, such as postpartum hypertension or preeclampsia, unless the physician confirms that the advantages of treatment exceed the possible drawbacks.

• Complications From Fibrosis:

  • Heart Valve Issues: To rule out any existing valve illness, all patients should have a complete cardiovascular evaluation, which includes an echocardiography, prior to beginning Cabergoline treatment. Cabergoline is not recommended if valve disease is found. Heart valve issues have been reported in certain Cabergoline users, especially when the medication is taken at high doses for Parkinson's disease or even at lower amounts for other ailments. In addition to routinely checking patients for cardiac problems, usually with echocardiograms every six to twelve months or as clinically indicated, doctors should try to utilize the lowest effective dose. Cabergoline should be stopped if any more heart valve issues are found while the patient is receiving treatment. Cabergoline should also be used with caution in combination with other drugs that are known to be linked to heart valve issues.

  • Other Fibrotic Reactions: After using Cabergoline, some people have reported developing fibrosis in the belly, heart lining, and lungs, among other areas of their bodies. Patients having a history of cardiac or extracardiac fibrotic diseases should thus not use Cabergoline. It is crucial to watch out for fibrosis signs and symptoms, including breathing difficulties, a chronic cough, stomach pain, or symptoms suggesting heart failure, while on Cabergoline medication. Blood and chest X-rays are two examples of clinical and diagnostic tests that should be performed on patients frequently. When pleural effusion or pulmonary fibrosis is identified, stopping Cabergoline has been shown to alleviate symptoms.

• Take Precautions: Cabergoline medication should be started with caution because orthostatic hypotension can happen, especially at first dosages of more than 1.0 mg. Furthermore, cautious monitoring is suggested when taking Cabergoline along with other drugs that are known to reduce blood pressure.

• Inhibition or Suppression of Postpartum Lactation: Cabergoline is not recommended to inhibit or suppress the natural lactation that occurs after childbirth. Usually used for this reason, Bromocriptine is another dopamine agonist; nevertheless, the use of this medication has been linked to serious side effects, including hypertension, stroke, and seizures.

• Hepatic Impairment: When giving Cabergoline to patients who have a hepatic impairment, caution and careful monitoring are advised due to the liver's substantial metabolism of Cabergoline, the drug's active ingredient.

• Psychological: Individuals undergoing treatment with dopamine agonists, such as Cabergoline, have documented a range of psychosocial side effects, including compulsive gambling, increased libido, and hypersexuality. Usually, these effects disappear when the medication is stopped or the dosage is reduced.

Use in Specific Populations:

• Pregnancy: Although studies on animals have revealed certain effects of Cabergoline during pregnancy, it is unclear how these effects apply to humans. High doses in mice affected mothers but did not cause birth abnormalities. Lower doses in rats resulted in higher rates of pregnancy losses, probably because Cabergoline inhibits prolactin production. Higher doses in rabbits resulted in issues like weight loss and birth deformities. However, the same problems were not observed in a different investigation, including rabbits. Doses over a particular threshold during pregnancy and nursing caused harm to the fetuses in rats. The safety of Cabergoline during pregnancy has not been thoroughly studied in enough pregnant subjects. Physicians ought to recommend it only in cases of extreme necessity.

• Nursing Mothers: Although it is unknown if Cabergoline enters human milk, mothers should think about ceasing to nurse their babies while taking Cabergoline. It is not advised to use Cabergoline to interrupt naturally occurring lactation following childbirth as it has been shown to interfere with lactation.

• Pediatric and Geriatric Use: It is unknown if Cabergoline is beneficial or safe for younger people. Not enough research has been done on older persons to determine whether they respond to Cabergoline differently than younger adults. When treating elderly individuals, doctors typically start with lower doses because they may have additional medical conditions or be on other medications that may interfere with Cabergoline.