Ampholip

Ampholip (amphotericin B) is a drug that is used to treat fungal infections, including severe and dangerous infections such as candidiasis, cryptococcosis, aspergillosis, histoplasmosis, coccidioidomycosis, etc. It belongs to a class of antifungal drugs known as polyene antibiotics.

Ampholip acts by binding to ergosterol, which is an important component of fungal cell membranes. This leads to a change in the permeability of the cell membrane, which ultimately leads to the death of fungal cells.

This drug is usually used for severe cases of fungal infections, especially in immunocompromised patients such as people with HIV/AIDS, those receiving chemotherapy, or those with severe systemic illness. It can also be used in the treatment of fungal infections of intracranial structures, internal organs and other serious complications.

Indications Ampholipa

1. Candidiasis: Including the genitourinary system, skin, mucous membranes, internal organs and systemic forms of infection.
2. Cryptococcosis: Including cryptococcal meningitis and other systemic forms of infection caused by Cryptococcus neoformans.
3. Aspergillosis: A fungal infection caused by Aspergillus spp. That can affect the lungs, sinuses, skin and other organs.
4. Histoplasmosis: Including acute and chronic forms of infection caused by Histoplasma capsulatum.
5. Coccidiomycosis (dolichospora): An infection caused by Coccidioides immitis or Coccidioides posadasii that can affect the lungs, skin and other organs.
6. Mucoromycosis: Including invasive forms of infection caused by Mucorales spp., which can affect the vascular system, eyes, skin and other organs.
7. Blastomycosis: An infection caused by Blasomycetes dermatitidis that can affect the lungs and other organs.
8. Chromoblastomycosis: An infection caused by Chromobacterium spp. That can affect the skin, mucous membranes and other organs.
9. Other fungal infections: Amphotericin B may also be used to treat other severe or systemic fungal infections that do not respond to other antifungals.

Release form

Concentrate for solution: This form is also a concentrated substance that must be dissolved in an appropriate solvent before use. Typically used for intravenous administration.

Pharmacodynamics

1. Interaction with ergosterol: Amphotericin B binds to ergosterol, which is an important component of fungal cell membranes. This interaction leads to changes in the structure and function of the membrane.
2. Damage to the cell membrane: The binding of amphotericin B to ergosterol leads to the formation of pores in the cell membrane of the fungus. This membrane damage causes leakage of cellular components and disruption of cell homeostasis.
3. Selectivity: Amphotericin B is selective for fungal cells due to differences in the composition of cell membranes between fungi and human cells.
4. Wide spectrum of action: The drug is active against various types of fungi, including Candida spp., Aspergillus spp., Cryptococcus neoformans, Histoplasma capsulatum, Coccidioides spp. And others.
5. Mechanism of resistance: Unlike most antibiotics, amphotericin B rarely causes the development of resistance in fungi. This is due to its unique mechanism of action, aimed at physical and chemical changes in the membrane.

Pharmacokinetics

1. Absorption: Amphotericin B is generally poorly absorbed from the gastrointestinal tract when taken orally and is not usually used in oral tablet form due to low bioavailability.
2. Distribution: Once amphotericin B is administered into the blood, it is rapidly distributed throughout the body. The drug is widely distributed in tissues including the skin, lungs, kidneys, liver, spleen, and brain. Its distribution is limited to plasma proteins.
3. Metabolism: Amphotericin B is metabolized to a minor extent. It undergoes minimal biotransformation in the liver.
4. Excretion: Most amphotericin B is excreted unchanged by the kidneys. The drug may persist in tissues for a long time after the end of treatment.
5. Half-life: The half-life of amphotericin B in the blood is about 15 days, indicating that it remains in the body for a long time.
6. Features in patients with impaired renal function: In patients with impaired renal function, an increase in the elimination time of amphotericin B may be observed, which requires dosage adjustment.

Dosing and administration

1. Candidiasis: The usual dose for the treatment of candidiasis may vary from 0.5 to 1 mg/kg per day. The dose may be increased to 1.5 mg/kg per day for severe infections.
2. Cryptococcosis: For the treatment of cryptococcosis, a dose of 0.3-0.6 mg/kg per day is usually used. In some cases, especially with meningitis, the dose can be increased to 0.7-1 mg/kg per day.
3. Aspergillosis: A dose of 0.5-0.7 mg/kg per day is usually used.
4. Histoplasmosis, coccidioidomycosis and other infections: The dose may vary depending on the type and severity of the infection and the patient's response to treatment.

It is important to note that the dosage of Ampholip can be adjusted by your doctor depending on the response to treatment and the toxicity of the drug. The drug is usually injected slowly into a vein over several hours to minimize possible infusion reactions.

Use Ampholipa during pregnancy

1. Benefits of use: In some cases, fungal infections can pose a serious threat to the life of the mother and fetus. In such cases, the use of Ampholip may be justified for the treatment of severe or dangerous infections.
2. Risks to the fetus: There is insufficient data on the safety of Ampholip during pregnancy to draw definitive conclusions about its safety for the fetus. Possible risks to the fetus include the possibility of toxic effects on developing organs and systems of the fetus.
3. Planning pregnancy: If a woman is planning pregnancy or discovers pregnancy while taking Ampholip, it is important to discuss this with her doctor. The doctor may review treatment plans and decide whether to continue or discontinue therapy.
4. Monitoring: If the use of Ampholip is necessary during pregnancy, it is important to carefully monitor the condition of the mother and fetus under the supervision of a physician.

Contraindications

1. Known allergic reaction: Patients with a known allergy to Ampholip or other components of the drug should not take it.
2. Severe renal impairment: Use of Ampholip may aggravate the condition of patients with severe renal impairment. In such cases, the drug may accumulate in the body, causing toxic effects.
3. Hypokalemia: Ampholip may cause hypokalemia (low potassium levels in the blood). Patients with a predisposition to or already diagnosed with hypokalemia may have an increased risk of developing serious cardiovascular complications.
4. Severe heart failure: In patients with severe heart failure, the use of Ampholip may worsen the heart condition and lead to serious complications.
5. Pregnancy and breastfeeding: The use of Ampholip during pregnancy and breastfeeding should be evaluated by a physician and considered in accordance with the potential benefits and risks to the mother and fetus or infant.
6. Patients with hypotension: Ampholip may cause hypotension (low blood pressure). In patients with already low blood pressure, this can lead to serious complications.

Side effects Ampholipa

1. Infusion reactions: Acute reactions may occur during Ampholip infusion, such as fever, chills, headache, hypotension (low blood pressure), nausea, vomiting, diarrhea, arthralgia (joint pain) and myalgia (muscle pain).
2. Electrolyte disturbances: Ampholip may cause hypokalemia (low blood potassium levels), hypomagnesemia (low blood magnesium levels) and other electrolyte disturbances, which can lead to abnormal heart rhythms and myocardial dysfunction.
3. Kidney damage: Long-term use of Ampholip can lead to kidney damage and the development of renal failure.
4. Hepatotoxicity: Some patients may develop elevated liver enzymes, as well as hepatitis and jaundice.
5. Hematopoietic disorders: Ampholip can cause anemia, leukopenia (decreased white blood cell count) and thrombocytopenia (decreased platelet count).
6. Neurological reactions: Headaches, dizziness, peripheral neuropathy and other neurological reactions may occur.
7. Allergic reactions: Allergic reactions may occur, including skin rash, itching, hives and anaphylactic shock.
8. Various other side effects: Other undesirable effects are possible, such as cardiac arrhythmias, hypertension (high blood pressure), hypoxia, hypertensive crisis, etc.

Overdose

Overdose of Ampholip may lead to an increase in its side effects, such as renal toxicity, electrolyte disturbances (eg, hypokalemia, hypomagnesemia), as well as life-threatening infusion reactions such as anaphylactic shock or serious cardiovascular disorders.

Interactions with other drugs

1. Aminoglycoside antibiotics: Concomitant use of amphotericin B with aminoglycoside antibiotics such as gentamicin or amikacin may increase the risk of developing kidney damage.
2. Cyclosporine: Concomitant use of Ampholip with cyclosporine may lead to increased concentrations of cyclosporine in the blood and increased kidney toxicity.
3. Digoxin: Amphotericin B may affect the blood concentration of digoxin, which may result in increased cardiac toxicity.
4. Lipid drugs: The use of Ampholip with lipid drugs such as aminophylline or levothyroxine may reduce their effectiveness due to interference with blood plasma proteins.
5. Carbamazepine: Ampholip may affect the blood concentration of carbamazepine, which may require dosage adjustment.
6. Allopurinol: Use of allopurinol with amphotericin B may increase the risk of developing allopurinol nephropathy.
7. Other drugs that affect renal function: Ampholip may increase the toxic effects of drugs that affect renal function, such as nephrotoxic antibiotics or nonsteroidal anti-inflammatory drugs.