Ciprofibrate - Uses, Dosage, Warnings, Side Effects, and Pharmacological Aspects

What Is Ciprofibrate?

We get Ciprofibrate from fibric acid. High cholesterol and high triglycerides are considered harmful to our heart health. Ciprofibrate can lower cholesterol and triglyceride levels in the blood. Also, it increases the level of good cholesterol, high-density lipoprotein (HDL), in our body.

Some reports say that Ciprofibrate can effectively reduce triglyceride levels by up to 50% and increase HDL cholesterol levels by up to 20%. Ciprofibrate has also been shown to reduce the risk of cardiovascular events, like heart attacks and strokes. It also reduces the formation of pro-inflammatory mediators. Though this is an effective and popular medicine worldwide, it is not approved by the FDA (Food and Drug Administration).

For Patients

What Are the Available Doses and Dosage Forms of Ciprofibrate?

Ciprofibrate is available as 100 mg (milligrams) tablets.

Administration:

• The medication is to be administered as instructed by the doctor.

• Swallow the tablets as a whole with a glass of water.

• The doctor will decide how long you have to take it based on your underlying medical conditions and medication history.

• Follow the dietary requirements given by the dietician or doctor while taking the medication.

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

Avoid administration in the following conditions:

• The patient is allergic or hypersensitive to Ciprofibrate or other ingredients in the medication.

• Due to an allergy, the patient may develop skin rashes, breathing difficulties, or facial swelling.

• The patient is pregnant, planning to become pregnant, or suspects pregnancy.

• The patient is currently breastfeeding.

• The patient has a history of severe liver or kidney problems.

Inform the doctor if any of the following conditions are present before they prescribe Ciprofibrate:

• If you have a history of unexpected muscle pains, tenderness, weakness, liver or kidney problems, an underactive thyroid gland, or a family history of muscle problems.

• If the patient is over 70 years of age.

• Taking Ciprofibrate may affect the results of some blood tests, so inform the person taking the test that the patient is taking Ciprofibrate.

• During treatment, the doctor may check liver function with blood tests.

• Inform the doctor or pharmacist of all the medications the patient is taking or has recently taken, including alternative or herbal medicines, as Ciprofibrate can affect how some other medicines work and vice versa.

• Inform the doctor if the patient is taking statins, Warfarin, Insulin, Metformin, contraceptive medicines, or hormone replacement therapy (HRT).

• One of the side effects of Ciprofibrate is muscle pain, and alcohol consumption may increase the chance of muscle problems. Therefore, limit alcohol consumption while taking Ciprofibrate and seek advice from the doctor.

What Are the Side Effects of Ciprofibrate?

The common side effects include:

• Loss of hair or balding.

• Gut issues like nausea, vomiting, and diarrhea.

• Muscle pain and body ache.

• Headaches.

• Balance issues.

• Dizziness.

• Drowsiness.

The uncommon side effects of the medication include:

• Impotence.

• Easy bruising.

• Inflammation of the muscles.

• Cramping or stiffness of the muscles

The more serious side effects of Ciprofibrate include:

• An itchy and lumpy rash, sensitivity to sunlight, and itching can indicate an allergic reaction.

• Inflammation of the lungs leads to breathlessness, coughing, and fever.

• Lung damage leads to breathing problems.

• Liver problems result in jaundice, characterized by yellowing of the eyes or skin.

• Severe or excruciating pain in the upper right abdomen may extend to the back and be accompanied by fever and vomiting. These symptoms may indicate biliary colic or gallstones.

If any of these symptoms are experienced, report them to a healthcare professional or the emergency department immediately.

What Are the Warnings and Precautions of Ciprofibrate?

• Galactose Intolerance:

Ciprofibrate is not advised in patients with a known history of galactose intolerance, Lapp-lactose intolerance, or glucose-galactose malabsorption.

• Liver Diseases:

Ciprofibrate may cause adverse effects on the liver. Hence, it is important to notify the doctor of any worsening of liver function (symptoms include vomiting, yellowing of the skin, and severe abdominal pain) at the earliest possible time.

• Muscle Conditions:

Some patients have reported muscle problems while taking this medication, which can lead to severe conditions like myopathy and rhabdomyolysis. Patients may be at higher risk if there is a history of kidney problems, low albumin levels, an underactive thyroid, drinking excessively, a family history of muscular disorders, or muscle problems with other medications. Taking higher doses or using this medication with other similar medications can also increase the risk of muscle problems.

What Should Be Done if a Dose Is Missed?

• If you miss a dose of Ciprofibrate, take it as soon as possible to maintain the dosing schedule and avoid potential adverse effects.

• If your next scheduled dose is near, you can skip the missed dose.

• Do not take a double dose as it can cause side effects.

How to Store Ciprofibrate?

• It is important to keep medications out of the sight and reach of children to avoid accidental ingestion or misuse.

• Using Ciprofibrate beyond its expiration date, clearly stated on the carton, is not advisable. The expiration date refers to the last day of the stated month; after this date, the medication may lose effectiveness or become unsafe to consume.

• When disposing of unused or expired medications, following proper procedures to protect the environment is essential. It is not recommended to dispose of medicines via wastewater or household waste. Instead, it is advisable to consult a pharmacist on the appropriate ways to dispose of the medication.

For Doctors:

Indications:

The non-FDA labeled indications include:

• Severe hypertriglyceridemia.

• Hyperlipidemia.

Adult Dosing:

For hyperlipidemia: 100 mg tablets once daily.

Dosing Considerations

• Mild to moderate renal impairment: 100 mg on alternate days.

• Severe renal impairment: Contraindicated.

• Hepatic impairment: Avoid use.

Pharmacology

Pharmacodynamics:

Clinical trials have demonstrated the efficacy of Ciprofibrate in treating hyperlipidemia characterized by elevated LDL and VLDL levels (classified as types IIa, IIb, III, and IV according to Fredrickson's classification). Ciprofibrate is a useful addition to dietary interventions for managing these conditions.

Mechanism of Action:

Ciprofibrate is a derivative of phenoxy-isobutyric acid that can lower lipids and raise HDL levels. It shares a similar structure with other fibric acid derivatives like Clofibrate, Gemfibrozil, Bezafibrate, and Fenofibrate. Ciprofibrate's exact mode of action is unknown, although it is believed to function via activating a specific receptor known as peroxisome proliferator-activated receptor alpha (PPARα).

• PPARα is a nuclear receptor that regulates lipid metabolism-related genes. These genes regulate lipoprotein lipase (LPL) and increase fatty acid breakdown in the liver and muscles while decreasing triglyceride production.

• Activation of PPARα by Ciprofibrate leads to increased expression of enzymes involved in the beta-oxidation of fatty acids and a decrease in the production of very low-density lipoprotein (VLDL).

• As VLDL can generate LDL cholesterol, a lower level of VLDL causes a lower LDL in the blood.

• Ciprofibrate may have a mild inhibitory effect on hydroxy-methylglutaryl CoA (HMG-CoA) reductase, which could be responsible for its stronger low-density lipoprotein (LDL) cholesterol-lowering effects.

• Ciprofibrate also increases the activity of lipoprotein lipase. This enzyme breaks down fats and triglycerides in the blood.

Pharmacokinetics

Absorption:

Within 1 to 4 hours of intake, Ciprofibrate reaches its peak plasma concentration.

• In a healthy person, plasma concentrations can reach 21 to 36 μg/mL (micrograms per milliliter) with a single dose of 100 mg.

• If someone is taking it for a longer period, the plasma concentration can be very high, ranging from 53 to 165 μg/mL.

Distribution:

Ciprofibrate is highly bound to plasma proteins, with approximately 98% bound within the therapeutic range.

Metabolism:

Ciprofibrate undergoes metabolism in the liver to form two active metabolites. One of the metabolites,1-O-beta-glucuronide, is responsible for most of the hypolipidemic activity. The other metabolite, 1-O-beta-acylglucuronide, is pharmacologically inactive.

Excretion:

• Approximately 30 to 75 percent of a single dose of Ciprofibrate administered to a healthy person is excreted in the urine within 72 hours, either in its unchanged form (20 to 25 percent of total excreted) or as a conjugate.

• The terminal elimination half-life of Ciprofibrate varies from 38 to 86 hours in patients receiving long-term therapy.

Toxicity:

The extent of the overdose of Ciprofibrate is not yet known. The management measures are symptomatic and supportive.

Contraindications:

The contraindications of Ciprofibrate are listed below:

• Concomitant administration with other fibrate drugs.

• Pregnancy and lactation.

• Severe renal or hepatic impairment.

Warnings and Precautions

• Concomitant Administration:

If considering use, assess potential risks and benefits and refer to the prescribing information of HMG-CoA reductase inhibitors for guidance. Avoid simultaneous use.

• Galactose Intolerance:

Do not use it in patients with glucose-galactose malabsorption, lactose intolerance, or galactose intolerance.

• Hepatic:

Patients with liver issues must be cautious. This medicine can cause liver damage. As a result, if you are taking this, you may need regular monitoring of liver functions.

• Musculoskeletal:

It can cause muscle damage, leading to issues such as body and joint pain and loss of muscle function. This is more common among patients with low thyroid, low albumin levels, or a habit of alcoholism, and it can cause muscle damage in older people or patients who are taking HMG-CoA reductase inhibitors.

Conclusion

Ciprofibrate is obtained from phenoxy-isobutyric acid. This medicine can affect your fat metabolism and lower the level of bad cholesterol and triglycerides in the blood. As this medicine helps raise good cholesterol levels in the blood, it reduces the risk of heart disease. However, if the patient is pregnant or has glucose intolerance, it should not be used. If you have any queries, you can consult a heart health specialist for further evaluation.