Zidolam

Zidolam is an antiviral drug. It belongs to the category of nucleotide and nucleoside reverse transcriptase inhibitors.

Indications Zidolama

Indicated for the treatment of HIV – for children 12+ years old, as well as for adults (with progressive forms of immunodeficiency).

Release form

Available in tablets - 10 pieces in 1 blister plate. One package of the medicine contains 10 blisters with tablets.

Zidolam-n is used to treat HIV in adolescents aged 16 years and over (weight 50+ kg), as well as in adults.

As a fixed combination, the drug may be prescribed if the patient has existing tolerance to its active ingredients (zidovudine, lamivudine, and nevirapine). Tolerability is assessed after a course of combined antiretroviral treatment with nevirapine in a maintenance dose of 200 mg twice a day, used for at least 6-8 weeks. Prescribing a maintenance dose of the drug is allowed only 2 weeks after its use in the initial amount - 200 mg per day once.

Pharmacodynamics

Lamivudine and zidovudine have a synergistic slowing effect on viral replication of HIV-1 and HIV-2 types. The active components of the drug are gradually converted inside the cell into triphosphate substances. These elements are competitive selective inhibitors of HIV revertase. Clinical testing has confirmed that such a combination is able to prevent the emergence of resistance to zidovudine in individuals who have not previously undergone a course of antiretroviral treatment.

The combination of lamivudine and zidovudine is more effective than the combination of zidovudine and didanosine or zidovudine and zalcitabine. Additional properties of these combined substances include good tolerability of such a combination. In addition, it promotes suboptimal suppression of viral reproduction and reduces the concentration level of the substance.

Pharmacokinetics

Zidovudine and lamivudine are well absorbed from the gastrointestinal tract, with a bioavailability index of 80-85% (lamivudine) and 60-70% (zidovudine). Peak plasma levels of these elements are 1.3-1.8 mg/mmol (lamivudine) and 1.5-2.2 mg/mmol (zidovudine) and are achieved after 0.5-2 hours and 0.25-2 hours, respectively.

Over the medicinal dosage range, lamivudine exhibits linear pharmacokinetics with weak binding to plasma albumins (less than 36% in vitro). The rate of zidovudine synthesis with protein is 34-38%.

Both substances are able to pass into the cerebrospinal fluid, as well as into the central nervous system.

After 2-4 hours after taking Zidolam, the proportions between the zidovudine and lamivudine levels in the plasma, and along with this, the cerebrospinal fluid, are equal to 0.5 and 0.12, respectively.

The major breakdown product of zidovudine in urine and plasma is 5-glucuronide. In vitro testing has demonstrated that lamivudine is phosphorylated intracellularly and then converted to the active breakdown product 5-triphosphate.

Lamivudine is excreted primarily via the kidneys, and the substance is excreted unchanged. The half-life of the substance is 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 in breast milk.

Dosing and administration

The medicine should be taken orally. For children over 12 years of age and adults, the dosage of the medicine is 1 tablet twice a day. It is allowed to take the medicine regardless of food intake.

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Use Zidolama during pregnancy

This medication is contraindicated for pregnant women.

Contraindications

Among the contraindications of the drug:

• intolerance to the components of the drug;
• severe stage of neutropenia (with a neutrophil count less than 0.75 x 10 9/l) or anemia (hemoglobin levels less than 7.5 g/dl or 4.65 mmol/l);
• polyneuropathy;
• impaired renal function (the level of creatinine clearance coefficient is less than 50 milliliters/minute);
• lactation period;
• children under 12 years of age.

Side effects Zidolama

As a result of using the medicine, the following side effects may develop: a feeling of fatigue and malaise, headaches, diarrhea, vomiting, dizziness and nausea. In addition, a state of fever, the development of neuropathy, anorexia, the appearance of insomnia or chills. Symptoms of damage to the nasal mucosa, pain in the musculoskeletal area, the development of neutropenia or baldness, the appearance of rashes or cough, and in addition, an increase in the bilirubin and liver enzymes.

Overdose

In case of drug overdose, supportive treatment is necessary, as well as procedures aimed at eliminating symptoms. There is no specific antidote for the treatment of Zidolam overdose.

Interactions with other drugs

Since the drug contains 2 active substances (zidovudine and lamivudine), it is capable of interacting according to the characteristics of both of them.

In case of combination of the drug with myelosuppressive or nephrotoxic drugs (including systemic use of pentamidine with pyrimethamine, and also dapsone, flucytosine, co-trimoxazole and interferon, as well as amphotericin B, ganciclovir with doxorubicin, and vinblastine with vincristine), constant monitoring of hematological level and renal function is required. The dosage is reduced if necessary.

It is necessary to monitor the blood levels of the substance phenytoin when used in combination with Zidolam.

Codeine with aspirin and morphine, as well as oxazepam with ketoprofen, indomethacin with naproxen and cimetidine, as well as dapsone with oxazepam and isoprinosine can influence the process of zidovudine metabolism (competitively slowing down the processes of formation of its glucuronide or directly suppressing the metabolism of the substance with the help of microsomal liver enzymes).

Probenecid can increase zidovudine levels by inhibiting the glucuronidation process or by reducing the rate of excretion of the substance through the kidneys.

The metabolism and clearance rate of zidovudine are affected by the use of fluconazole.

Valproic acid slows down the first phase of hepatic metabolism of zidovudine, thereby increasing the bioavailability of the latter. Because of this, when using these substances in combination, it is recommended to monitor the health of patients in order to promptly detect an increase in the frequency of negative reactions to the use of zidovudine.

Certain nucleoside analog drugs can affect the function and number of leukocytes/erythrocytes, can enhance the toxic properties of zidovudine in relation to blood cells, and in addition, the process of DNA replication.

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

The substances pyrimethamine, trimethoprim, as well as acyclovir with sulfamethoxazole are permitted to be used in the process of prevention or treatment of infectious processes caused by opportunistic organisms, because with limited use of these drugs, their toxic properties are not enhanced.

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Storage conditions

Zidolam must be kept in a place that is inaccessible to children and must comply with standard conditions for storing medications. The temperature must be: 15-30°C.

Shelf life

Zidolam must be used within 2 years from the date of release of the drug.