Cynive-12

Mechanism Of Action:

Ivermectin binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate muscle and nerve cells of the microfilaria. This binding causes an increase in the permeability of the cell membrane to chloride ions and results in hyperpolarization of the cell, leading to paralysis and death of the parasite. Ivermectin also is believed to act as an agonist of the neurotransmitter gamma-aminobutyric acid (GABA), thereby disrupting GABA-mediated central nervous system (CNS) neurosynaptic transmission. Ivermectin may also impair normal intrauterine development of O. volvulus microfilariae and may inhibit their release from the uteri of gravid female worms.

Pharmacokinetics:

Absorption

Moderately well absorbed. Improved absorption with high fat meal.

Volume of distribution

The volume of distribution is 3 to 3.5 L/kg and it does not cross the blood-brain barrier.

Protein binding

93%

Metabolism

Primarily hepatic,Ivermectin is metabolized in the liver

Route of elimination

Ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine.

Side effects:

Ivermectin may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

• dizziness
• loss of appetite
• nausea
• vomiting
• stomach pain or bloating
• diarrhea
• constipation
• weakness
• sleepiness
• uncontrollable shaking of a part of the body
• chest discomfort

If you are taking ivermectin to treat onchocerciasis, you may also experience the following side effects. Tell your doctor if any of these symptoms are severe or do not go away:

• swelling of the eyes, face, arms, hands, feet, ankles, or lower legs
• joint pain and swelling
• painful and swollen glands of the neck, armpit or groin
• rapid heartbeat
• eye pain, redness, or tearing
• swelling of the eye or eyelids
• abnormal sensation in the eyes

Some side effects can be serious. If you experience any of these symptoms, call your doctor immediately:

• fever
• blistering or peeling skin
• rash
• hives
• itching

Drug-Drug Interactions

Ivermectin can interact with a number of other medications, vitamins or herbs you may be taking. This can be harmful or prevent the drug from working well. To help avoid interactions, your doctor should manage all of your medications carefully. Be sure to tell your doctor about all medications, vitamins, or herbs you’re taking. To find out how this drug might interact with something else you’re taking, talk to your doctor or pharmacist.

A few examples are -: Warfarin, Abametapir, dasatinib, deferasirox, itraconazole, nevirapine, rifapentine, etc

Precautions

• Tell your doctor and pharmacist if you are allergic to ivermectin or any other medications.
• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention if you are taking medications for anxiety, mental illness or seizures; muscle relaxants; sedatives; sleeping pills; or tranquilizers. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
• Tell your doctor if you have or have ever had meningitis, human African trypanosomiasis (African sleeping sickness; an infection that is spread by the bite of the tsetse fly in certain African countries), or conditions that affect your immune system, such as human immunodeficiency virus (HIV).

Dosage

Ivermectin is generally administered as a single dose of 150-200 µg/kg.

Half-life – The half-life of ivermectin in humans is 12–36 hours, while metabolites may persist for up to three days.

Adverse Effects

In the absence of parasitic infection, the adverse effects of ivermectin in therapeutic doses are minimal. Adverse effects seen in filarial infections include fever, myalgia, malaise, lightheadedness, and occasionally postural hypotension. In onchocerciasis, skin oedema, pruritis and mild eye irritation may be seen.

Storage

Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture

Overdosage

Symptoms of overdose may include:

• rash
• hives
• seizure
• headache
• tingling of hands or feet
• weakness
• loss of coordination
• stomach pain
• nausea
• vomiting
• diarrhea
• dizziness
• shortness of breath
• swelling of the face, arms, hands, feet, ankles, or lower legs

Contraindications:

Asthma, Hepatic diseases, HIV infection, Loa-Loa coinfections, Onchodermatitis, Pregnancy, Children, Breastfeeding etc.