Interferon Beta-1b: Pharmacology, Side Effects, Warnings, and Precautions

Overview:

Interferon beta-1b is a widely employed medication that is specifically indicated for dealing with a medical condition called multiple sclerosis, which is an immune-mediated condition influencing the nervous system. Interferon beta-1b gained authorization from the drug regulatory body of the United States, the Food and Drug Administration (FDA), for tackling the manifestations associated with multiple sclerosis on 23rd July 1993. It is being licensed and marketed under various brand names with similar generic formulations. Besides interferon beta-1b, several other drug forms work against multiple sclerosis. Concerned doctors analyze each patient and figure out the best choice of medicine for that particular individual by taking into account all the possible influential factors.

Drug Group:

Interferon beta-1b falls under the immunomodulatory class of drugs. Immunomodulators, as the name suggests, bring their action by altering the immune response. The actions can be either through up-regulation or down-regulation of the immune functions. It is employed to guide the immune response to a favorable route by either enhancing or inhibiting the immune reactions.

Available Doses and Dosage Forms:

Interferon beta-1b is marketed in the form of powder and solution, which can be delivered directly into the fatty layer underneath the skin via injection. Each injection formulation is designed to contain about 0.3 milligrams (mg) of powder, which needs to be mixed with a specific quality of liquid to obtain the injection solution with an accurate concentration of Interferon beta-1b.

For Patients:

What Is Multiple Sclerosis?

Multiple sclerosis is a peculiar medical condition arising from aberrant immune function. It is highly prevalent among the adult population within the age range of 20 to 40 years. In multiple sclerosis, the immune cells which are intended to work against foreign substances and other disease-causing agents, get wrongly directed. As a result, these immune cells charge their cells, primarily striking the myelin sheath (that wraps the nerve cells to extend protection). The nerves that constitute the central nervous system encompassing the spinal cord, brain, and optic nerves have myelin-coating, which potentiates the pace of impulse conveyance and simultaneously offers protection. Wrongly directed immune cells impair the myelin and disrupt and deteriorate nerve functions.

Multiple sclerosis precipitates a wide range of manifestations, and it differs on an individual basis. Multiple sclerosis is categorized into various sub-classes by considering the differences in manifestations. However, certain general manifestations are elicited in the majority of cases. Some of the frequently encountered manifestations of multiple sclerosis include visual irregularities and disturbances, muscle cramps, spasms, and loss of muscular tonicity and strength. The involved person may also experience problems with bladder control. There will be altered cognitive functions, tiredness, and unpredictable mood changes in advanced stages. The manifestations may worsen upon encounter with other infections.

How Does Interferon Beta 1b Work?

Being a potent and efficacious immunomodulator, Interferon beta-1b brings about its action by altering the body’s immune response. It critically curbs the immune reaction's intensity, curtailing the immune-mediated attack against the myelin. Furthermore, Interferon beta-1b also possesses antiviral activities, extending its application for certain virus-mediated conditions. Interferon elicits its effects on the immune cells by modulating the pathway through which they are signaled.

What Is the Dosage of Interferon Beta 1b?

0.0625 milligrams (mg) is the recommended starting dose. The Interferon beta-1b is not advised for daily delivery, instead, it needs to be delivered once in two days. The dose is gradually and steadily titrated on a biweekly basis over six-week periods until the preferred dose of 0.25 mg is reached.

How Effective Is Interferon Beta 1b?

Interferon beta-1b is highly efficacious and beneficial in curbing the intensity as well as the frequency of multiple sclerosis exacerbation. Several clinical studies and trials have proven the potency of Interferon beta-1b in tackling multiple sclerosis. However, the study reports in all the subjects were not consistent, and it was demonstrated that the effectiveness was influenced by certain patient factors. The presence of concomitant disease, health status, and disease type can potentially govern the Interferon’s potency. The Interferon extended maximum benefits for multiple sclerosis type with marked relapses, where the treated person projected a dramatic decline in relapse rate.

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

Before commencing therapy using Interferon beta-1b, it is imperative to have proper communication with the concerned medical professional. A thorough understanding of the patient's health status warrants the success of the treatment by guiding the doctors in treatment planning and drug choice.

• Allergy: The doctors must be informed about the patient's prior hypersensitivity or hyperreactivity encounter with Interferon beta-1b or other related medicines. In addition, the entire ingredient list needs to be looked for allergic components, and if there are any, that should be drawn to the doctor's attention. Subsequent delivery of an allergen can trigger severe alarming reactions in the body.

• Medical History: Detailed medical history encompassing all the information on the individual's health, like past illness, current health status, underlying ailments, past surgeries, and undergoing therapies. Certain disease conditions may worsen with Interferon beta-1b therapy; therefore, it is crucial to keep the doctors aware of it beforehand so that necessary alterations in the drug choice can be made.

• Drug History: Besides medical history, the doctors should be informed of the patient's history. The drug history needs to be comprehensive and elaborate such that it should entail all the medicines, be it over-the-counter, herbal, or dietary supplements. Certain medicines may interfere with the working mechanism of Interferon beta-1b. Understanding the patient's drug history aids the medical professional in making appropriate changes in the drug choice and dosage.

• Pregnancy and Lactation: The doctors should be made aware of the pregnancy and lactation status of the patient before commencing Interferon beta-1b. Pregnant women are not supposed to take all kinds of medicine, as it carries potential risks to the baby in the womb. Similarly, lactating women carry the possibility of delivering the medicine into the child’s body through breast milk. Hence, the doctor needs to be updated regarding it.

How Is Interferon Beta 1b Administered?

Interferon beta-1b is approved for delivery underneath the skin (subcutaneous) via shots. Trained medical professionals often perform it. However, caregivers or patients can deliver the shot only if trained for that. Interferon beta-1b injection formulation is marketed as powder and liquid, which have to be reconstituted. The Interferon beta-1b powder is made into a solution by adding a specific concentration of sodium chloride, which is available along with the powder in prefilled syringes. 1.2 milliliters of sodium chloride are introduced into the vial with the powder. The vial is then calmly rotated to ensure thorough dissolving of the powder particles.

Each one milliliter of the injection solution accounts for 0.25 milligrams of the drug molecules. The shelf life for reconstituted injection formulation is three hours, provided it should be kept at two to eight degrees Celsius (35 to 46 degrees Fahrenheit). The medicine can be jabbed underneath the skin with the help of a syringe, which is loaded with the prescribed dosage of the reconstituted solution. The injection site needs to be changed alternatively to check trauma to a specific point.

What Are the Side Effects of Interferon Beta 1b?

Like other medicines, Interferon beta-1b also brings about certain adverse reactions following administration. Some of the routinely reported side effects concerning Interferon beta-1b include the following:

• Abnormal vaginal bleeding, headache, muscle stiffness, generalized weakness, and muscle soreness.

• Altered sexual drive, particularly in males.

• Injection point reactions like tenderness, redness, puffiness, and rarely, bleeding.

• Impaired coordination (troubled walking and body movements).

Apart from the side effects mentioned above, there are certain alarming side effects concerning Interferon beta-1b, which necessitate immediate medical attention. Some of the grave reactions include the following:

• Jaundice skin (skin yellowing).

• Pigmented urine and bloody stool.

• Trouble sleeping.

• Stomach ache.

• Suicidal thoughts, emotional imbalance, and mental instability.

• Seizure (abnormal brain activities).

• Altered heartbeat.

• Short breath.

• Itchy skin rashes.

• Troubled speech.

• Facial puffiness.

• Chest discomfort.

In case the patient flags alarming side effects, immediate medical care needs to be sought as these adverse reactions are capable of endangering one’s life.

Dietary Considerations:

There is no specific dietary consideration advised for Interferon beta-1b therapy. However, each person’s health status may differ; accordingly, the doctors may advise certain dietary guidelines. In such cases, it is essential to adhere to the doctor's instructions to ensure the safety and effectiveness of the medicine.

Missed Dose:

The Interferon injections are to be taken on alternate days. However, at times, the person may miss the injection dose. In such cases, the shot can be delivered once the patient becomes aware of the missed dose. However, a 48-hour interval needs to be maintained between each subsequent dose. If the patient accidentally delivers the medicine consecutively, immediate medical care needs to be sought, as it can give rise to toxicity issues.

Overdose:

Exposure to more than the indicated dosage of Interferon can bring in overdosage issues like an abnormal hike in body temperature, troubled breathing, and general skin redness. Therefore, ensuring that only the stipulated drug dose is being administered is important. To safeguard the patient’s life, it is crucial to ensure immediate medical care following an overdose encounter. The patient must be monitored until all the vital parameters are restored within the normal range.

Storage:

Interferon beta-1b is marketed as a powder and solution vial, and each vial is designed for single use. 20 to 25 degrees Celsius (68 to 77 degrees Fahrenheit) is the ideal temperature range advised for Interferon beta-1b storage. However, temperatures within the range of 15 to 30 degrees Celsius (59 to 86 degrees Fahrenheit) are also reported to be safe for interference storage. After reconstitution, the residual solution is not intended for subsequent usage. It can be stored only for another three hours under refrigeration. Freezing the solution can alter the chemical and physical structure of the medicine, which can alter the therapeutic properties; hence, it is not advised.

For Doctors:

Indication:

• Multiple sclerosis (relapsing form).

Dose:

The approved inceptive dose of Interferon beta-1b is 0.0625 mg, which accounts for 0.25 milliliter of the reconstituted solution. Gradual dose titration is achieved every two weeks until the desired dose of 0.25 mg is attained. The final dose is attained within six weeks following the initial dose. One milliliter of the reconstituted solution contributes 0.25 mg of the drug molecule. The dose delivery is advised only once in two days, such that the subsequent doses are spaced 48 hours apart.

Dosing Considerations:

There is no specific dosing consideration advised for Interferon beta-1b. However, the doctor may advise dose modifications by considering the individual’s health status and underlying disease conditions. The dose is designed so that the inceptive dose bears 25 percent of the intended dose. The dose is inflated by 25 percent on a biweekly basis until the intended dose is attained.

What Are the Pharmacological Aspects of Interferon Beta 1b?

• Mechanism of Action: Interferon beta-1b is a specific type of interferon that alters the body’s immune response. However, limited information is available concerning the mechanism by which interferon beta-1b tackles multiple sclerosis. It suppresses the proinflammatory cytokines but, at the same time, enhances the anti-inflammatory expression. Furthermore, Interferon beta-1b alleviates inflammation, particularly in the central nervous system, thereby checking the immune-mediated nerve cell impairments. All these properties work together to deal with the progression and manifestation of multiple sclerosis.

• Pharmacodynamics: Interferon beta-1b alters the immunological response in distinct ways. The functions of T cells and B cells get modified under interference therapy. The activities of antigen-presenting cells and suppressor T cells will be silenced under the influence of Interferon beta-1b therapy. The trafficking of the immune cells across the blood-brain barrier will be clamped down by Interferon beta-1b. It also depreciates the pro-inflammatory cytokine-mediated activities.

• Pharmacokinetics: Following Interferon beta-1b injection, the drug molecules are immediately taken into the bloodstream. Following uptake, the drug molecules are distributed extensively. Interferon beta-1b can extend its therapeutic effects on the central nervous system as the blood-brain barrier does not restrict them. Though Interferon beta-1b is employed as a drug, it is proteinaceous in structure. Therefore, Interferon metabolism is quite different from other drugs’ metabolism. Interferon beta-1b is broken down into simpler amino acid molecules. The action of specific enzymes triggers this breakdown. The eradication of Interferon is carried out by the kidney, and its half-life is estimated to be five to six hours.

Toxicity:

Interferon beta-1b therapy has demonstrated no carcinogenicity or mutagenicity in non-clinical studies. However, the complete toxicity profile concerning Interferon beta-1b therapy must be explored more to obtain conclusive results.

Clinical Studies:

Clinical trials were conducted to expose the potency and safety aspects of Interferon beta-1b in multiple sclerosis patients. These randomized studies were conducted in various locations as placebo-controlled studies. The study subjects were chosen based on certain inclusion criteria. Patients detected with relapsing-remitting multiple sclerosis (RRMS) who satisfied all other inclusion criteria were chosen as study subjects. The studies demonstrated dramatic depreciation in the relapse frequency associated with multiple sclerosis in patients on Interferon beta-1b therapy. Furthermore, certain patients even demonstrated to be free of remissions following the therapy.

What Are the Contraindications of Interferon Beta 1b?

Interferon beta-1b therapy is not advisable in multiple sclerosis patients who have had prior allergic encounters with Interferon beta-1b or any of the components listed in the Interferon beta-1b injection formulation ingredient list. In addition, patients eliciting allergic responses to albumin-based medications are not supposed to undergo Interferon beta-1b therapy unless the probability of Interferon allergy is ruled out.

Warnings and Precautions:

• Cardiac Issues: Interferon beta-1b therapy is known to precipitate cardiac problems, particularly in patients with known heart problems. Patients who are already detected with cardiomyopathy or congestive heart failure entail caution while undergoing Interferon beta-1b therapy. The exacerbation of heart problems is reported during the inceptive and dose alteration phase. However, there is no evidence to point out that Interferon beta-1b therapy can trigger cardiac issues in patients without any predisposition.

• Liver Damage: Interferon beta-1b can inflict liver damage and deteriorate liver functions. The presence of liver disease or concomitant medications enhances the probability of liver damage. Therefore, periodic assessment of the liver's functional status is warranted to keep track of any advancing liver issues.

• Depressive Disorder: There are reports of depressive disorders in association with Interferon beta therapy. It is reported that Interferon beta-1b therapy enhances the probability of depression. In addition, the patients undergoing the therapy exhibited an enhanced suicidal tendency. Therefore, patients with known depressive disorders should refrain from Interferon-beta therapy. Similarly, the patients undergoing the therapy should be routinely assessed for clinical depression or suicidal thoughts. If depression is diagnosed, Interferon therapy needs to be withdrawn immediately.

• Leukopenia: There are reports of leukopenia in patients undergoing Interferon beta-1b therapy, which necessitates the reduction of Interferon’s dose. Therefore, the blood profile needs to be assessed at regular intervals.

• Anaphylaxis: Rarely, interferon beta may evoke severe allergic reactions in the form of anaphylaxis. Bronchospasm, facial edema, and urticaria are the generally precipitated manifestations of anaphylaxis. In an anaphylactic reaction, immediate medical attention needs to be sought.

• Flu-Like Manifestations: Certain patients on Interferon therapy exhibit flu-like manifestations. In such cases, antipyretics can be employed to deal with the manifestations.

• Lupus Erythematosus: Interferon beta-1b is capable of triggering lupus erythematosus, where the patients on Interferon elicit manifestations like rashes, joint issues, fever, shortness of breath, and many more. This form of lupus erythematosus triggered by medication or drugs is considered to be drug-induced lupus erythematosus.

• Thrombotic Microangiopathy: There are reports of thrombotic microangiopathy cases evoked by Interferon beta therapy. Therefore, patients should be cautioned about it. Immediately withdraw the drug if thrombotic microangiopathy is suspected.

• Injection Point Reactions: Certain skin reactions are seen responding to Interferon delivery at the injection point. Necrosis, soreness, erythema, and puffiness are routinely reported at injection points. Therefore, it is advised to alternate the injection point to minimize the scope for injection point reactions.

What Are the Drug Interactions of Interferon Beta 1b?

There is only limited information available regarding Interferon drug interactions. Interferon beta-1b tends to elicit association with certain anticoagulants. Simultaneous delivery of Interferon beta-1b along with Ardeparin and Argatroban potentiates the anticoagulant property and augments bleeding risk.

Specific Considerations:

1. Interferon Beta-1b During Pregnancy: Expectant women are not supposed to take all sorts of medicines, as they carry the risk of fetal harm. Clinical studies fail to demonstrate an obvious association between Interferon beta-1b therapy and fetal harm or defects when delivered to a pregnant woman. However, considering the scope for fetal harm, Interferon therapy is indicated for a pregnant woman only if the risks override the anticipated maternal benefit.

2. Interferon Beta-1b During Lactation: There is no conclusive evidence about the discharge of Interferon beta-1b through breast milk. Therefore, it is routinely not advised for lactating women.

3. Interferon Beta-1b in the Pediatric Population: No studies have been conducted to assess the safety and efficacy aspects of Interferon beta-1b in the pediatric population.

4. Interferon Beta-1b in the Geriatric Population: The number of seniors in the clinical studies concerning interferon beta-1b needed to be increased to obtain conclusive results.