Zidolam

Zidolam is an antiviral medicine. It is included in the category of nucleotide and nucleoside inhibitors of revertase.

Indications of the zidolama

It is indicated for the treatment of HIV - to children 12+ years, and also for adults (with a progressive form of immunodeficiency).

Release form

It is produced in tablets - 10 pieces per 1 blister plate. One medicine package contains 10 blisters with tablets.

Zidolam is used to treat HIV in adolescents from 16 years of age (weight 50+ kg), as well as in adults.

As a fixed combination, the drug may be administered with the patient's existing tolerability (zidovudine, lamivudine, and nevirapine). Assessment of tolerability is performed after a course of combined antiretroviral treatment with nevirapine at a maintenance dosage of 200 mg twice a day, applied for a minimum of 6-8 weeks. Prescribe a maintenance dosage of drugs is allowed only after 2 weeks after applying it in the initial amount - 200 mg per day once.

Pharmacodynamics

Lamivudine, as well as zidovudine, have a synergistic retardation effect on viral replication of HIV-1 and HIV-2 types. The active components of the LS are gradually transformed inside the cell into triphosphate substances. These elements are competitive selective inhibitors of HIV revertase. Clinical trials have confirmed that such a combination can inhibit the emergence of resistance to zidovudine in people who have not previously undergone antiretroviral treatment.

The combination of lamivudine and zidovudine is more effective than combinations of zidovudine with didanosine or zidovudine with zalcitabine. Among the additional properties of these combined substances is the good tolerability of such a combination. In addition, it promotes suboptimal suppression of viral reproduction, and also weakens the concentration level of the substance.

Pharmacokinetics

Zidovudine with lamivudine is well absorbed from the digestive tract, with a bioavailability index of 80-85% (lamivudine) and 60-70% (zidovudine). The peak level in the plasma of these elements is 1.3-1.8 mg / mmol (lamivudine) and 1.5-2.2 mg / mmol (zidovudine) and is reached after 0.5-2 hours and 0.25-2 hours respectively.

In the drug dosage range of lamivudine, linear pharmacokinetics with weak binding to albumin-located albumin (less than 36% in vitro) are observed. The index of zidovudine synthesis with protein is 34-38%.

Both substances are able to pass inside the CSF, as well as in the CNS.

After 2-4 hours after taking Zidolam, the proportions between the zidovudine and lamivudine indices inside the plasma, and with it the cerebrospinal fluid are 0.5 and 0.5, respectively.

The main product of the disintegration of zidovudine inside urine with plasma is 5-glucuronide. In vitro tests demonstrated that intracellular phosphorylation of lamivudine occurs, which is further converted to an active decay product of 5-triphosphate.

Excretion of lamivudine mainly occurs through the kidneys, the substance is excreted unchanged. The half-life of the substance reaches 10.5-15.5 hours.

The half-life of zidovudine is approximately 1.1 hours. About 50-80% of the substance is excreted through the kidneys in the form of 5-glucuronide. In addition, zidovudine can be excreted through breast milk.

Dosing and administration

The medicine should be consumed orally. For children from 12 years and adults, the dosage of the drug is 1 tablet a day twice a day. It is allowed to drink drugs regardless of eating.

[1]

Use of the zidolama during pregnancy

Pregnant women are not allowed to prescribe this medicine.

Contraindications

Among the contraindications of drugs:

• intolerance of the constituent components of the drug;
• Severe neutropenia (with a neutrophil count of less than 0.75 × 10 9 / L) or anemia (hemoglobin less than 7.5 g / dL or 4.65 mmol / L);
• polyneuropathy;
• impairment of renal function (level of creatinine clearance is less than 50 milliliters / minute);
• lactation period;
• children's age is less than 12 years.

Side effects of the zidolama

Due to the use of the medicine, such side effects can develop: feeling tired and unwell, headaches, diarrhea, vomiting, dizziness and nausea. In addition, also the state of fever, the development of neuropathy, anorexia, the emergence of insomnia or chills. Symptoms of nasal mucosa, pain in the musculoskeletal area, neutropenia or baldness, rashes or cough may appear, and bilirubin and liver enzymes may also increase.

Overdose

With the development of an overdose of the drug, supportive care is needed, as well as procedures aimed at eliminating the symptoms. There is no specific antidote for the treatment of an overdose of Zidolam.

Interactions with other drugs

Since the drug contains 2 active substances (zidovudine with lamivudine), it is able to interact in accordance with the characteristics of both of them.

In the case of a combination of a drug with myelosuppressive or nephrotoxic drugs (among these, the systemic use of pentamidine with pyrimethamine, and in addition to this dapsone, flucytosine, co-trimoxazole and interferon, as well as amphotericin B, ganciclovir with doxorubicin, and vinblastine with vincristine) requires continuous monitoring of hematological level and renal function. Dosage is lowered if necessary.

It is required to monitor the indices in the blood of the phenytoin substance - when combined with Zidolam.

Codeine with aspirin and morphine, and in addition oxazepam with ketoprofen, indomethacin with naproxen and cimetidine, as well as dapsone with oxazepam and isoprinosine are able to influence the metabolism of zidovudine (competingly slowing the formation of its glucuronide or directly suppressing the metabolism of the substance with microsomal hepatic enzymes) .

Probenecid can increase zidovudine, suppressing the process of glucuronization or reducing the rate of excretion of the substance through the kidneys.

The use of fluconazole influences metabolic processes and the clearance factor of zidovudine.

Valproic acid slows the 1 st phase of hepatic metabolism of zidovudine, which increases the bioavailability of the latter. Because of this, when combined use of these substances is recommended to monitor the health of patients in order to promptly reveal the increase in the negative reactions to the use of zidovudine.

Separate nucleoside analog drugs can affect the work, as well as the number of white blood cells / erythrocytes, can enhance the toxic properties of zidovudine relative to blood cells, and in addition to this DNA replication process.

Ribavirin antagonizes the antiviral activity of zidovudine relative to the HIV virus (in vitro).

Substances pyrimethamine, trimethoprim, and also acyclovir with sulfamethoxazole are allowed to be used in the process of prevention or treatment of infectious processes provoked by conditionally pathogenic organisms, because with limited use of these drugs their toxic properties are not enhanced.

[2], [3]

Storage conditions

Contain Zidolam is required in a place that will not be accessible to children, and also meet the standard conditions for storing medicines. The temperature is 15-30 ° C.

Shelf life

Zidolam is required to be used within 2 years from the date of release of the drug.