Stavudine

Stavudine (stereoisomer of dideoxythymidine) is an antiviral drug used in the treatment of HIV infection. It belongs to the class of nucleoside reverse transcriptase inhibitors (NRTIs). Here are the highlights about Stavudine:

1. Mechanism of Action: Stavudine is incorporated into the viral DNA strand in place of the normal nucleoside. This stops further synthesis of viral DNA and inhibits viral replication.
2. Use: Stavudine is used in combination with other antivirals to treat HIV infection. It can be prescribed as part of first-line HIV therapy, although in some countries its use is declining due to side effects.
3. Side Effects: Stavudine can cause a variety of side effects, including neuropathy (peripheral neuropathy), lactate acidosis, hepatomegaly (enlarged liver), lipodystrophy (changes in fat metabolism), anemia, and neutropenia (decreased levels of neutrophils in the blood).
4. Notes: Stavudine is no longer recommended as a first-line treatment because of its side effects and the possibility of safer alternatives. It can be used as a second-line treatment or when other medications are ineffective or unavailable.

It is important to get your doctor's advice and supervision when using Stavudine, especially because of its potentially serious side effects.

Indications Stavudina

1. Treatment of HIV infection: Stavudine is used as part of combination antiretroviral therapy (ART) to control the replication of the human immunodeficiency virus (HIV) in the body. It is usually given together with other antiviral drugs such as protease inhibitors or other reverse transcriptase inhibitors.
2. Prevention of HIV transmission: In some cases, such as in pregnant women with HIV infection or in people exposed to contaminated material, Stavudine may be prescribed as a prophylactic to prevent HIV transmission.
3. Prevention of HIV infection after possible exposome: In some cases where a person is at possible risk of HIV infection (e.g., after occupational exposure to infected material), Stavudine may be used with other antiviral drugs to prevent the development of infection.
4. Treatment of acute HIV infection in newborns: In newborns infected with HIV, Stavudine may be given together with other antiviral drugs to treat the acute phase of infection.

Release form

1. Capsules

• Dosage: Usually available in 15 mg, 20 mg, 30 mg and 40 mg dosages.
• Use: Capsules are taken orally, with water, regardless of food intake.

2. Powder for preparation of oral solution

• Dosage: The powder is designed to be diluted in water to create a solution that can be taken by mouth.
• Use: This form is especially convenient for children or adults who have difficulty swallowing capsules.

Pharmacodynamics

Stavudine (also known as didanosine) is an antiviral drug used to treat HIV infection. Its pharmacodynamics is that it is an inhibitor of HIV reverse transcriptase. Reverse transcriptase is an enzyme that HIV uses to convert its RNA into DNA so that it can be incorporated into the genome of an infected cell. By inhibiting this enzyme, stavudine helps to slow down viral replication and spread in the body. This reduces the viral load in the blood and slows the progression of HIV infection.

Pharmacokinetics

1. Absorption: Stavudine is usually well absorbed from the gastrointestinal tract after oral administration. Its absorption may be reduced if taken with food.
2. Distribution: It is well distributed throughout the body, including tissues and organs. Stavudine passes through the placenta and is excreted in breast milk.
3. Metabolism: Stavudine is metabolized in the liver. The major metabolite, didanosine trophate, also has antiviral activity.
4. Excretion: Most stavudine and its metabolites are excreted through the kidneys. Stavudine levels may be increased in patients with impaired renal function.
5. Semi elimination: Stavudine's elimination half-life is about 1-2 hours, which means that the drug is rapidly eliminated from the body.
6. Interindividual differences: Stavudine is subject to significant interindividual differences in pharmacokinetics, including metabolic differences and changes in patients with impaired hepatic or renal function.

Dosing and administration

Method of Application:

Stavudine is available in the form of capsules and powder to prepare an oral solution. The drug can be taken with or without food, and it is important to take it at the same time each day to maintain a constant level of the drug in the blood.

Capsules:

• Swallow the capsule whole with a small amount of water.
• Do not chew or open the capsule.

Powder for oral solution:

• Mix the powder thoroughly with the specified amount of water.
• Make sure the powder is completely dissolved.
• Take immediately after preparation.

Dosage:

The dosage of Stavudine depends on the patient's weight and kidney condition. It is important to check renal function regularly, as in case of abnormalities it is necessary to adjust the dose.

Adults and children weighing 60 kg or more:

• Standard dose: 40 mg every 12 hours.

Adults and children weighing less than 60 kg:

• Standard dose: 30 mg every 12 hours.

Children (depending on weight and age):

• Doses for children are calculated individually, usually 1 mg/kg every 12 hours.
• The maximum dose for children should not exceed 40 mg every 12 hours.

Special Instructions:

• If you forget a dose of the drug, take it as soon as possible, but if it is almost time for your next dose, skip the forgotten dose and continue your regular schedule. Do not double the dose.
• Do not stop taking the drug without consulting your doctor, even if you feel improvement.
• Regular medical checkups and lab tests are important to monitor your condition and possible side effects of the medication.

Use Stavudina during pregnancy

Stavudine, also known as didanosine, is an antiviral drug that is commonly used in the treatment of HIV infection. The use of stavudine during pregnancy requires special caution.

Like many other antiviral medicines, stavudine may have potential risks for fetal development. Therefore, it is important that women taking stavudine who are planning a pregnancy or who become pregnant discuss this with their doctor. Your doctor can review your treatment regimen and decide whether you should continue taking stavudine or switch to other medicines that are safe for pregnancy.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to stavudine or other ingredients of the drug should not take it.
2. Diabetes mellitus: Caution should be exercised in patients with diabetes mellitus when treating with stavudine, as the drug may cause hyperglycemia.
3. Hepatic insufficiency: In the presence of severe hepatic insufficiency stavudine may be contraindicated or require special monitoring and cautious prescribing.
4. Peripheral neuropathy: Stavudine use may be contraindicated in patients with pre-existing peripheral neuropathy.
5. Myopathy: In patients with myopathy, the use of stavudine may be undesirable due to the risk of worsening the condition.
6. Pregnancyand lactation: The use of stavudine during pregnancy and lactation may require an assessment of the benefits and risks to the mother and fetus. This should be decided by a physician.
7. Pediatric population: Age restrictions and contraindications may apply to children depending on age and health status.
8. Interaction with other drugs: Stavudine may interact with other medications, which may also affect its contraindications and dosage.

Side effects Stavudina

1. Neuropathy: One of the most well-known side effects of stavudine is peripheral neuropathy, which manifests as numbness, tingling, or pain in the extremities. This symptom may be reversible with dose reduction or discontinuation of the medication.
2. Pancreatitis: In some patients, stavudine may cause inflammation of thepancreas, which manifests as upper abdominal pain, nausea, and vomiting.
3. Hepatotoxicity: In rare cases, stavudine may cause an increase in liver enzyme levels in the blood, indicating liver damage.
4. Lactate acidosis: This is a serious side effect that can manifest as fatigue, weakness, nausea, vomiting, aching muscles, abdominal pain, or respiratory depression.
5. Lipodystrophy: Stavudine may cause changes in body fat distribution, such as fat loss in the face, arms, and legs, and fat accumulation in the abdomen, neck, or chest area.
6. Anemia and neutropenia: Stavudine use may cause a decrease in the number of red blood cells (anemia) and white blood cells (neutropenia).
7. Other Side Effects: Other possible side effects of stavudine include nausea, vomiting, diarrhea, dizziness, headache, insomnia, and allergic reactions.

Overdose

Stavudine overdose can lead to the development of serious side effects, including toxicity to the bone marrow and peripheral nervous system. Symptoms of overdose may include decreased white blood cell count, anemia, neuropathy and other adverse reactions.

In case of suspected overdose with stavudine, immediate medical attention should be sought. Treatment of overdose may include symptomatic therapy, maintenance of organ and system functions, as well as the use of specific antidotes or detoxification methods, if necessary.

Interactions with other drugs

1. Antiviral drugs: Stavudine may interact with other antiretroviral drugs such as zidovudine (AZT), lamivudine (3TC), tenofovir (TDF), efavirenz (EFV), ritonavir (RTV), and others. Some of these interactions may be favorable, for example, combination therapy may enhance treatment efficacy, but others may lead to increased side effects.
2. Antibiotics and antimicrobials: Some antibiotics, such as tetracyclines or fluoroquinolones, and antifungal agents may reduce the absorption of stavudine from the gastrointestinal tract, which may reduce its effectiveness.
3. Drugs affecting gastric acidity: Drugs that reduce gastric acidity, such as antacids or proton pump inhibitors, may increase the risk of elevated blood levels of stavudine due to decreased metabolism.
4. Drugsaffecting hepatic or renal function: Drugs affecting hepatic or renal function may alter the pharmacokinetics of stavudine. Stavudine dosage adjustment may be required in patients with impaired hepatic or renal function.
5. Drugs causing cardiotoxicity: Some drugs, such as amidarone, may increase the cardiotoxic effects of stavudine.

Storage conditions

Stavudine should be stored at room temperature, protected from light and moisture. Storage in places with controlled temperature and humidity helps to maintain the effectiveness of the drug. It is important to avoid storing Stavudine in places where it may be exposed to direct sunlight or extreme temperature conditions, as this may affect its stability and quality. As with any medicinal product, you should store Stavudine out of the reach of children and animals.