The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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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.
How should I take Ivermectin?
Use Ivermectin exactly as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor tells you. Do not change your treatment without checking first with your doctor.
Ivermectin comes with a patient information leaflet. Read and follow the instructions carefully. Ask your doctor if you have any questions.
To use Sklice™ topical lotion:
Use Sklice™ on the hair and scalp only. Keep the medicine out of your eyes, nose, mouth, and vagina. If the medicine gets in your eyes, rinse them well with water.
Wash your hands before and after using Ivermectin.
Apply the medicine directly to dry hair (up to 1 tube) closest to the scalp and then apply outwards. Completely cover your entire head. Leave the medicine on the hair and scalp for 10 minutes.
After 10 minutes, rinse your hair with warm water and dry with a clean towel. Comb hair with a fine-toothed comb to remove any nits (eggs) or nit shells. They look like small white dots.
If live lice are seen 7 days after using Ivermectin, tell your doctor right away.
Do not use Ivermectin again without talking to your doctor first.
Children will need an adult to apply the medicine for them.
Throw away any unused medicine left in the tube after each use.
Do not use cosmetics and other hair products on the treated hair and scalp areas.
To use Soolantra™ topical cream:
Ivermectin is for use on the skin only. Do not get it in your eyes, mouth, or vagina. Do not use it on skin areas that have cuts or scrapes. If it does get on these areas, rinse it off right away.
Wash your hands before and after using Ivermectin.
Use a pea-sized amount for each affected area of the face (forehead, chin, nose, cheeks).
Spread a thin layer and avoid the eyes and lips.
Dosing
The dose of Ivermectin will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Ivermectin. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
For topical dosage form (cream):
For rosacea:
Adults—Apply to the affected area(s) of the face once a day.
Children—Use and dose must be determined by your doctor.
For topical dosage form (lotion):
For head lice:
Adults, teenagers, and children 6 months of age and older—Apply directly to dry hair and scalp one time only.
Infants younger than 6 months of age—Use is not recommended.
Storage
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Ivermectin administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Oral: Administer on an empty stomach with water.
Pediculosis pubis and scabies treatment: To increase bioavailability in the epidermis, Ivermectin is recommended to be taken with food (CDC [Workowski 2015]; Currie 2010).
Ivermectin pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
Pharmacokinetics
Following oral administration of Ivermectin, plasma concentrations are approximately proportional to the dose. In two studies, after single 12-mg doses of Ivermectin in fasting healthy volunteers (representing a mean dose of 165 mcg/kg), the mean peak plasma concentrations of the major component (H2B1a) were 46.6 (±21.9) (range: 16.4 to 101.1) and 30.6 (±15.6) (range: 13.9 to 68.4) ng/mL, respectively, at approximately 4 hours after dosing. Ivermectin is metabolized in the liver, and 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. The plasma half-life of Ivermectin in man is approximately 18 hours following oral administration.
The safety and pharmacokinetic properties of Ivermectin were further assessed in a multiple-dose clinical pharmacokinetic study involving healthy volunteers. Subjects received oral doses of 30 to 120 mg (333 to 2000 mcg/kg) Ivermectin in a fasted state or 30 mg (333 to 600 mcg/kg) Ivermectin following a standard high-fat (48.6 g of fat) meal. Administration of 30 mg Ivermectin following a high-fat meal resulted in an approximate 2.5-fold increase in bioavailability relative to administration of 30 mg Ivermectin in the fasted state.
In vitro studies using human liver microsomes and recombinant CYP450 enzymes have shown that Ivermectin is primarily metabolized by CYP3A4. Depending on the in vitro method used, CYP2D6 and CYP2E1 were also shown to be involved in the metabolism of Ivermectin but to a significantly lower extent compared to CYP3A4. The findings of in vitro studies using human liver microsomes suggest that clinically relevant concentrations of Ivermectin do not significantly inhibit the metabolizing activities of CYP3A4, CYP2D6, CYP2C9, CYP1A2, and CYP2E1.
Microbiology
Ivermectin is a member of the avermectin class of broad-spectrum antiparasitic agents which have a unique mode of action. Compounds of the class bind selectively and with high affinity to glutamate-gated chloride ion channels which occur in invertebrate nerve and muscle cells. This leads to an increase in the permeability of the cell membrane to chloride ions with hyperpolarization of the nerve or muscle cell, resulting in paralysis and death of the parasite. Compounds of this class may also interact with other ligand-gated chloride channels, such as those gated by the neurotransmitter gamma-aminobutyric acid (GABA).
The selective activity of compounds of this class is attributable to the facts that some mammals do not have glutamate-gated chloride channels and that the avermectins have a low affinity for mammalian ligand-gated chloride channels. In addition, Ivermectin does not readily cross the blood-brain barrier in humans.
Ivermectin is active against various life-cycle stages of many but not all nematodes. It is active against the tissue microfilariae of Onchocerca volvulus but not against the adult form. Its activity against Strongyloides stercoralis is limited to the intestinal stages.
Clinical Studies
Stongyloidiasis
Two controlled clinical studies using albendazole as the comparative agent were carried out in international sites where albendazole is approved for the treatment of strongyloidiasis of the gastrointestinal tract, and three controlled studies were carried out in the U.S. and internationally using thiabendazole as the comparative agent. Efficacy, as measured by cure rate, was defined as the absence of larvae in at least two follow-up stool examinations 3 to 4 weeks post-therapy. Based on this criterion, efficacy was significantly greater for Ivermectin (a single dose of 170 to 200 mcg/kg) than for albendazole (200 mg b.i.d. for 3 days). Ivermectin administered as a single dose of 200 mcg/kg for 1 day was as efficacious as thiabendazole administered at 25 mg/kg b.i.d. for 3 days.
In one study conducted in France, a non-endemic area where there was no possibility of reinfection, several patients were observed to have recrudescence of Strongyloides larvae in their stool as long as 106 days following Ivermectin therapy. Therefore, at least three stool examinations should be conducted over the three months following treatment to ensure eradication. If recrudescence of larvae is observed, retreatment with Ivermectin is indicated. Concentration techniques (such as using a Baermann apparatus) should be employed when performing these stool examinations, as the number of Strongyloides larvae per gram of feces may be very low.
Onchocerciasis
The evaluation of Ivermectin in the treatment of onchocerciasis is based on the results of clinical studies involving 1278 patients. In a double-blind, placebo-controlled study involving adult patients with moderate to severe onchocercal infection, patients who received a single dose of 150 mcg/kg Ivermectin experienced an 83.2% and 99.5% decrease in skin microfilariae count (geometric mean) 3 days and 3 months after the dose, respectively. A marked reduction of >90% was maintained for up to 12 months after the single dose. As with other microfilaricidal drugs, there was an increase in the microfilariae count in the anterior chamber of the eye at day 3 after treatment in some patients. However, at 3 and 6 months after the dose, a significantly greater percentage of patients treated with Ivermectin had decreases in microfilariae count in the anterior chamber than patients treated with placebo.
In a separate open study involving pediatric patients ages 6 to 13 (n=103; weight range: 17 to 41 kg), similar decreases in skin microfilariae counts were observed for up to 12 months after dosing.
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