Ribavirin

Ribavirin exhibits strong antiviral activity; it is a man-made substance with a wide range of therapeutic effects.

It has a significant medicinal effect on a relatively large number of viruses, although the exact principle of the drug's effect has not been fully determined. There is an assumption that the drug weakens the intracellular pool of guanosine 3-phosphate, thereby helping to suppress the processes of viral nucleic acid production.

[ 1 ]

Indications Ribavirin

It is used for inhalation in hospitals for infants and young children suffering from severe lower respiratory tract infections caused by RSV.

In adults, it is often used as part of a combination therapy. The drug is taken orally for hepatitis C, as well as Lassa hemorrhagic fever.

Parenteral administration of drugs is prescribed in case of hemorrhagic fever accompanied by renal syndrome.

[ 2 ], [ 3 ], [ 4 ], [ 5 ], [ 6 ], [ 7 ]

Release form

The component is released in capsules, powder substance or tablets.

[ 8 ], [ 9 ]

Pharmacokinetics

After oral administration of the drug, its bioavailability is 45%. Cmax values are recorded after 0.5-1.5 hours. The active component is not synthesized with intraplasmic protein, but can accumulate inside erythrocytes. The substance also overcomes the BBB.

Biotransformation occurs in the liver; excretion occurs mainly with urine. The half-life of a single dose is 27-36 hours, and in the case of stable values in the blood, 6 days.

After administration via inhalation, approximately 30-55% of the drug is excreted in the form of metabolic components in the urine (over a period of 72-80 hours).

[ 10 ], [ 11 ], [ 12 ], [ 13 ], [ 14 ]

Dosing and administration

Capsules or tablets of the drug must be taken orally, with food. Usually 0.8-1.2 g of the substance is taken per day. The portion should be divided into 2 doses. The therapeutic cycle usually lasts 0.5-1 year. But the duration of treatment for each patient is selected by the attending physician individually.

The drug can be administered intravenously only in a hospital. The mode of use and portion sizes are selected by a medical professional.

Inhalations of the drug should be performed on young children during the first 3 days of infection development. Such procedures should be performed exclusively in a hospital.

Inhalations should be carried out daily, for 12-18 hours. The entire cycle lasts 3-7 days. 10 mg/kg of the medicinal substance should be administered per day. 1 ml of liquid contains 20 mg of the medicinal component.

To make the liquid, 6 g of powder is required, which is dissolved in injection water (0.1 l). The resulting mixture is poured into a special inhalation device, and then water is added to obtain a volume of 0.3 l.

[ 20 ], [ 21 ], [ 22 ]

Use Ribavirin during pregnancy

Ribavirin should not be administered to breastfeeding or pregnant women.

Contraindications

Main contraindications:

• CHF (stages 2-3 of the disease);
• renal failure (creatinine clearance level less than 50 ml per minute);
• severe stage of liver failure;
• pathologies of an autoimmune nature;
• severe depression, in which there is a tendency towards suicide;
• intolerance to ribavirin;
• anemia of a severe nature;
• liver cirrhosis in the decompensated stage;
• incurable thyroid diseases.

[ 15 ], [ 16 ], [ 17 ]

Side effects Ribavirin

Possible side effects include:

• circulatory disorders: thrombocytopenia, neutro-, leukopenia or granulocytopenia, as well as anemia (in case of development of negative manifestations, blood tests should be performed at 2-week intervals);
• allergy symptoms: epidermal irritation or rash, photosensitivity, erythema, urticaria, hyperthermia, SJS, anaphylaxis, TEN and Quincke's edema, as well as conjunctivitis (after inhalation) and chills (after intravenous administration of drugs);
• lesions affecting the cardiovascular system: asystole, decreased blood pressure or bradycardia (it is necessary to constantly monitor the patient’s condition);
• liver disorders: hyperbilirubinemia;
• problems with the nervous system function: severe irritability, depression, malaise, asthenic syndrome, dizziness, confusion and insomnia, as well as anxiety, headaches, emotional instability, fatigue and systemic weakness;
• disorders associated with the respiratory system: pulmonary atelectasis, pneumothorax, pharyngitis and dyspnea. In addition, bronchial spasm, sinusitis, pulmonary edema, runny nose, cough, hypoventilation syndrome and apnea (when performing inhalations);
• digestive disorders: bloating, loss of appetite, stomatitis, constipation, dry mouth or metallic taste, diarrhea and glossitis, as well as nausea, pancreatitis, abdominal pain, changes in taste, vomiting, hyperbilirubinemia and bleeding gums;
• problems with the function of the sense organs: visual or auditory disorders, lesions in the area of the lacrimal glands and tinnitus;
• lesions of the musculoskeletal structure: myalgia or arthralgia;
• disorders associated with the urogenital system: dysmenorrhea, prostatitis, hot flashes, as well as decreased libido or menorrhagia;
• other manifestations: pain in the injection area, hair structure disorder or hair loss, viral infection (for example, herpes), fungus, hypothyroidism, hyperhidrosis, and in addition, a feeling of intense thirst, flu-like syndrome, pain in the sternum area and lymphadenopathy.

During inhalation, doctors may develop the following negative symptoms: ocular hyperemia, swelling in the eyelid area, headaches and epidermal itching.

[ 18 ], [ 19 ]

Overdose

Drug intoxication may cause potentiation of the negative effects of Ribavirin.

In such cases, mandatory drug withdrawal is required. Symptomatic treatment measures are also performed.

[ 23 ]

Interactions with other drugs

Combination with interferons increases the effectiveness of the drug.

The level of bioavailability of the drug decreases when combined with aluminum or magnesium substances, as well as with simethicone.

Interaction of drugs with zidovudine or stavudine may provoke a weakening of the activity of these medications.

It is necessary to take into account the low excretion rate of Ribavirin - because of this, it may affect the use of other drugs for another 2 months after the end of therapy.

[ 24 ], [ 25 ]

Storage conditions

Ribavirin should be stored in a dark and dry place. The temperature level should be within 25°C.

[ 26 ], [ 27 ], [ 28 ], [ 29 ]

Shelf life

Ribavirin is approved for use for a period of 36 months from the date of sale of the therapeutic substance.

[ 30 ], [ 31 ], [ 32 ]

Application for children

The drug is not used in pediatrics.

[ 33 ], [ 34 ], [ 35 ], [ 36 ], [ 37 ], [ 38 ]

Analogues

The drug's analogues are Arviron, Ribapeg, Trivorin, Virazol with Ribamidil, Vero-Ribavirin, Rebetol, Ribavin and Devirs.

[ 39 ], [ 40 ], [ 41 ], [ 42 ], [ 43 ], [ 44 ]

Reviews

Ribavirin usually receives positive feedback from patients. But sometimes the comments say that the medication only eliminates the symptoms of the disease, without eliminating the cause of their occurrence, and therefore recommend using its analogues. At the same time, the reviews quite often mention the appearance of various negative symptoms, which were sometimes eliminated by switching from tablets to the capsule form of the drug.

There is also evidence that in people with relapsed pathology and those who have not previously used interferon α-2β, the effectiveness of treatment increases with the combined use of Ribavirin with Altevir.

[ 45 ], [ 46 ], [ 47 ]