таблетки ивермектина в блистерной упаковке, содержащие 3мг активного вещества
таблетки ивермектина в блистерной упаковке, содержащие 3мг активного вещества

Ivermectin: Side Effects | Instructions for Use | Information

ivermectin tablets in blister packaging, containing 3mg of active substance per tablet

Information about Ivermectin

Ivermectin is an antiparasitic drug used to treat infections caused by parasites, helminths, and arthropods.

Therapeutic category: Antiparasitic, Anthelmintic

Active ingredients: Ivermectin

Chemical structure: C₉₅H₁₄₆O₂₈

Mechanism of action: Ivermectin works by binding to glutamate-gated chloride channels in the nerve and muscle cells of parasites. This causes increased permeability of the cell membrane to chloride ions, leading to hyperpolarization of the cells, resulting in paralysis and death of the parasites.

Therapeutic indications: It is used to treat parasitic infections such as onchocerciasis, strongyloidiasis, ascariasis, and scabies. It is also used to treat demodicosis and other dermatological conditions.

History of the drug

Ivermectin was discovered in the 1970s by Satoshi Ōmura in Japan, who isolated bacteria of the genus Streptomyces from soil samples. This discovery led to the development of one of the most effective antiparasitic drugs in medical history.

According to research by Nabi-Afjadi et al., ivermectin has been proven highly effective in combating parasitic infections worldwide, with an excellent safety profile and broad spectrum of action. The drug has significantly contributed to combating severe parasitic diseases in developing countries.

 

Usage Instructions/Indications for Ivermectin

Ivermectin is administered for the treatment of various parasitic infections. The dosage is determined by the attending physician based on the patient’s body weight and the type of infection.

Common dosages:

  • For onchocerciasis: 150-200 μg/kg once
  • For strongyloidiasis: 200 μg/kg daily for 1-2 days
  • For scabies: 200 μg/kg once with possible repetition after 7 days

Method of administration:

  • Taken orally on an empty stomach
  • Recommended to take with water
  • Avoid food 2 hours before and after taking

Contraindications and Precautions

Contraindications:

  • Hypersensitivity to ivermectin
  • Central nervous system disorders
  • Severe liver failure

Precautions:

  • Regular liver function monitoring
  • Monitoring for neurological side effects
  • Avoid driving and operating machinery

Special warnings for the elderly, children, and pregnant women

Elderly:

  • Caution required in dosage
  • More frequent monitoring of kidney function
  • Increased risk of interactions with other drugs

Children:

  • Not recommended for children under 15 kg
  • Dosage adjustment based on body weight
  • Close monitoring for side effects

Pregnancy and breastfeeding:

  • Contraindicated during the first trimester of pregnancy
  • Administration only if the benefit outweighs the risk
  • Discontinue breastfeeding for 24 hours after taking

As highlighted in research by Gwee et al., the safety and efficacy of ivermectin in pediatric populations require careful evaluation and individualized approach.

 

Dosage and administration

Ivermectin is administered in individualized dosages based on the patient’s body weight and condition. It is usually given orally on an empty stomach.

Recommended dosages:

  • For parasitic infections: 150-200 μg/kg body weight once
  • For scabies: A dose of 200 μg/kg, with possible repetition after 7-14 days
  • For demodicosis: 200-400 μg/kg per week for 3-4 weeks

What to do if you miss a dose of Ivermectin?

If you miss a dose, take it as soon as you remember. However, if it is close to the time for your next scheduled dose, skip the missed dose and continue with your regular schedule. Do not take a double dose to make up for the missed one.

Overdose

As explained by Naggie in his research, an overdose of ivermectin can cause:

  • Nausea and vomiting
  • Diarrhea
  • Hypotension
  • Abdominal pain
  • Neurological manifestations
  • Allergic reactions

In case of overdose, immediate medical attention is required.

Side effects

Common side effects:

  • Headache
  • Dizziness
  • Myalgias
  • Fatigue
  • Gastrointestinal disturbances

Rare side effects:

  • Liver dysfunction
  • Severe skin reactions
  • Hematological disorders
  • Neurotoxicity

Very rare side effects:

  • Stevens-Johnson syndrome
  • Toxic epidermal necrolysis
  • Severe neurological complications

In case of severe side effects, discontinue treatment and contact your healthcare provider immediately.

 

Interactions

Ivermectin presents significant interactions that require attention during its administration. According to studies conducted by Adeleye et al., understanding drug interactions is crucial for the safe use of the medication. The metabolic pathway of ivermectin through cytochrome P450 makes it susceptible to interactions with many other drugs.

Drug-drug interactions

Ivermectin significantly interacts with drugs that affect the cytochrome P450 system. Special attention is required when co-administered with anticoagulant drugs, as it may enhance their action. Additionally, drugs like ketoconazole and erythromycin can increase ivermectin levels in the blood. Antiepileptic drugs may reduce ivermectin plasma concentration. As noted by Sulik et al., co-administration with immunosuppressants requires careful monitoring.

Drug-food interactions

Food consumption can significantly affect the absorption of ivermectin. It is recommended to take the drug on an empty stomach, as fatty meals can increase its bioavailability by 2.5 times. Alcohol consumption should be avoided during treatment, as it may enhance the drug’s side effects. Also, products containing grapefruit juice may increase drug levels in the blood due to CYP3A4 enzyme inhibition. It is recommended to avoid consuming herbal extracts and dietary supplements during treatment, as unpredictable interactions may occur.

 

ivermectin is indicated for the treatment of gastrointestinal parasitic infections The molecular structure of Ivermectin is characterized by a macrocyclic lactone ring[/caption

Additional important information

Ivermectin is an important antiparasitic drug with a broad spectrum of action. Its pharmacokinetic characteristics and effectiveness have been extensively studied over the past decades, providing valuable information for its clinical use.

Development of resistance

The phenomenon of resistance to ivermectin is a significant challenge. Findings by the team of Carrillo Heredero et al. highlight the need for continuous monitoring of the drug’s effectiveness. The development of resistance is associated with genetic mutations in target organisms and may affect the long-term effectiveness of the treatment.

Preclinical and Clinical Studies

Laboratory research by Antoszczak et al. has documented the mechanism of action of ivermectin at the cellular level. Preclinical studies in experimental animals have confirmed the drug’s safety, while clinical trials have demonstrated its effectiveness in treating various parasitic infections.

Post-marketing studies, Pharmacovigilance, and Pharmacokinetic characteristics

The results of post-marketing studies, as reported by the team of Mohebi et al., confirm the favorable safety profile of ivermectin. Pharmacovigilance has highlighted rare but significant side effects that require attention. Pharmacokinetic characteristics include rapid absorption from the gastrointestinal system, extensive distribution in tissues, and hepatic metabolism, with a half-life ranging from 18 to 35 hours.

 

Preclinical and Clinical Studies

Preclinical studies on Ivermectin include extensive research in various experimental models. The findings reveal the complex mechanism of the drug’s interaction with glutamate-gated chloride channels in parasitic organisms. Extensive toxicological studies have confirmed the favorable safety profile in various animal species. A significant analysis by the laboratory of Boulware et al. has provided new data on the therapeutic potential of the drug in various pathological conditions.

Post-marketing studies, Pharmacovigilance, and Pharmacokinetic characteristics

Extensive pharmacovigilance data support the safety of long-term use of the drug. Pharmacokinetic characteristics, according to the research team of Stewart et al., demonstrate high lipophilicity that facilitates penetration into target tissues. The presence of food in the gastrointestinal system significantly affects absorption, with bioavailability increasing after fatty meals. Hepatic metabolism via the cytochrome P450 system is the main route of degradation, while excretion occurs primarily through the fecal route, with a smaller percentage excreted through the kidneys.

 

Comparative effectiveness

Ivermectin has been extensively compared with other antiparasitic drugs in terms of effectiveness and safety. Comparative analyses show high effectiveness in combating parasitic infections. As indicated by laboratory data from Zalpoor et al., the drug presents a particularly favorable therapeutic index compared to other therapeutic options.

Systematic reviews and meta-analyses

Systematic reviews have confirmed the clinical value of ivermectin in various therapeutic indications. According to findings from the laboratory of Menotta et al., the drug’s effectiveness has been documented through multiple clinical trials. Data analysis consistently shows positive results in the treatment of parasitic infections.

Current research directions and future prospects

Research on ivermectin continues with unabated interest. Laboratory studies by Steer et al. are exploring new therapeutic applications and improved forms of administration. The development of new formulations with improved bioavailability and the investigation of combination therapies are important directions of current research. Additionally, innovative strategies are being studied to address resistance and optimize therapeutic effectiveness.

 

Summary

The active substance (Ivermectin drug) is characterized by a broad spectrum of antiparasitic action. It shows particular effectiveness in treating gastrointestinal parasitic infections and skin conditions. It is contraindicated in individuals with hypersensitivity to the drug, in pregnant women during the first trimester, and in children under 15 kg. The most common side effects include gastrointestinal disturbances, headache, and transient elevation of liver enzymes. Special caution is required when co-administered with drugs metabolized via the cytochrome P450.

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WARNING: Never take medication without consulting a doctor. Always read the medication leaflet. This encyclopedic article refers to the specific active substance and does not replace the instructions of your doctor or pharmacist.

 

Bibliography

  1. ACS Omega – Advanced LC-MS/MS technique for environmental ivermectin detection
  2. European Journal – Antiparasitic activity of ivermectin: Four decades of research
  3. JAMA – Effect of higher-dose ivermectin for 6 days vs placebo
  4. Journal of Water Process Engineering – Recent strategies for remediation
  5. Molecular Biology – A cellular and molecular biology-based update
  6. The Lancet Regional Health – Ivermectin therapy for young children