Product Code: AH-04
Composition: Each 5 ml contains:
Albendazole IP 200 mg Ivermectin IP 1.5mg
Dosage Form: SUSPENSION
INFORMATION FOR THE USER
Albendazole 200mg and Ivermectin 1.5mg/5ml Syrup
Read all of this information carefully before you start taking this medicine because it contains important information for you.
- Keep this information. You may need to read it again.
- If you have any further questions, ask your doctor, pharmacist or nurse.
- This medicine is prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this information.
- COMPOSITION:
Each 5ml of syrup contains:
Albendazole – 200mg
Ivermectin – 1.5mg
For oral use only.
2. DESCRIPTION:
Albendazole is a drug useful for the treatment of parasitic worm diseases. Ivermectin is also a drug useful for the treatment of parasite infestations.
3. PHARMACOLOGICAL ACTION:
Albendazole causes degenerative alterations in the intestinal cells of the worm by binding to the colchicine-sensitive site of β-tubulin, thus inhibiting its polymerization or assembly into microtubules (it binds much better to the β-tubulin of parasites than that of mammals). It leads to impaired uptake of glucose by the larval & adult stages of the susceptible parasites & depletes their glycogen stores. It also prevents the formation of spindle fibers needed for cell division, which in turn blocks egg production & development; existing eggs are prevented from hatching. Cell motility, maintenance of cell shape & intracellular transport are also disrupted. At higher concentrations, it disrupts the helminths’ metabolic pathways by inhibiting metabolic enzymes such as malate dehydrogenase & fumarate reductase, with inhibition of the latter leading to less energy produced by the Krebs cycle. Due to diminished ATP production, the parasite is immobilized and eventually dies.
Ivermectin is a member of the avermectin class of broad-spectrum antiparasitic agents, which have a unique mode of action. It binds selectively & with high affinity to glutamate-gated chloride ion channels, which occur in invertebrate nerve & muscle cells. This leads to an increase in the permeability of the cell membrane to chloride ions with hyperpolarization of the nerve /muscle cell, resulting in paralysis & death of the parasite. 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 & that the avermectins have a low affinity for mammalian ligand-gated chloride channels. In addition, ivermectin does not readily cross the blood-brain barrier.
4. CLINICAL PHARMACOKINETICS:
Albendazole is poorly absorbed from the GI tract due to its low aqueous solubility. Its concentrations are negligible/undetectable in plasma as it is rapidly converted to the sulphoxide metabolite prior to reaching the systemic circulation. The systemic anthelmintic activity has been attributed to the primary metabolite, albendazole sulphoxide. Oral bioavailability appears to be enhanced when it is co-administered with a fatty meal (estimated fat content: 40g) as evidenced by higher (up to 5-fold) plasma concentrations of albendazole sulphoxide as compared with the fasted state. Maximal plasma concentrations of albendazole sulphoxide are typically achieved 2-5 hours after dosing & are on average, 1.31mcg/mL (range: 0.46-1.58mcg/mL) following oral dose. Plasma concentrations of albendazole sulphoxide increase in a dose-proportional manner over the therapeutic dose range following ingestion of a fatty meal (fat content: 43.1 g). The mean apparent terminal elimination half-life of albendazole sulphoxide typically ranged from 8-12 hours. Following 4 weeks of treatment plasma concentrations of albendazole sulphoxide in 12 patients were approximately 20% lower than those observed during the first half of the treatment period, suggesting that albendazole may induce its own metabolism. Albendazole sulphoxide is 70% bound to plasma protein & is widely distributed throughout the body; it has been detected in urine, bile, liver, cyst wall, cyst fluid & CSF. Concentrations in plasma were 3-10-fold and 2-4-fold higher than those simultaneously determined in cyst fluid & CSF, respectively. Limited in vitro & clinical data suggest that albendazole sulphoxide may be eliminated from cysts at a slower rate than observed in plasma. It is rapidly converted in the liver to the primary metabolite, albendazole sulphoxide, which is further metabolized to albendazole sulphone and other primary oxidative metabolites that have been identified in human urine. It has not been detected in human urine. Urinary excretion of albendazole sulphoxide is a minor elimination pathway with less than 1% of the dose recovered in the urine. Biliary elimination presumably accounts for a portion of the elimination as evidenced by biliary concentrations of albendazole sulphoxide similar to those achieved in plasma.
Following oral administration of ivermectin plasma concentrations are approx. proportional to dose. The mean peak plasma concentrations of the major component were 46.6 (±21.9) (range: 16.4-101.1) & 30.6 (±15.6) (range: 13.9-68.4) ng/mL resp. at approx. 4 hours after dosing. It is metabolized in the liver & ivermectin and/or its metabolites are excreted almost exclusively in the faeces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine. The plasma half-life in humans is approx. 18 hours. The safety & pharmacokinetic properties were further assessed in a multiple-dose clinical pharmacokinetic study involving healthy volunteers. Administration following a high-fat meal resulted in an approx. 2.5-fold increase in bioavailability relative to administration in fasted state. It is primarily metabolized by CYP3A4.
- INDICATIONS:
Albendazole and Ivermectin is indicated for the treatment of the following infections:
- Parenchymal neurocysticercosis due to active lesions caused by larval forms of tapeworm, Taenia solium & for the treatment of cystic hydatid disease of the liver, lung & peritonium caused by the larval form of Echinococcus granulosus.
- Intestinal (i.e. non disseminated) strongyloidiasis due to nematode parasites like Strongyloides stercoralis.
- Onchocerciasis (river blindness) due to the nematode parasite Onchocerca volvulus.
- Can be used to treat scabies caused by Srcoptes scabiei.
5. CONTRAINDICATIONS:
Contraindicated in patients with a known hypersensitivity to the benzimidazole class of compounds or any components of albendazole.
6. WARNINGS AND PRECAUTIONS:
Rare fatalities associated with the use of albendazole have been reported due to granulocytopenia or pancytopenia. Albendazole has been shown to cause bone marrow suppression, aplastic anaemia and agranulocytosis in patients with & without underlying hepatic dysfunction. Patients with liver disease appear to be more at risk for bone marrow suppression leading to pancytopenia, aplastic anaemia, agranulocytosis & leucopenia attributable to albendazole & warrant closer monitoring of blood counts.
Should not be used in pregnant women except in clinical circumstances where no alternative management is appropriate.
Patients being treated for neurocysticercosis should receive appropriate steroid & anticonvulsant therapy as required.
Pre-existing neurocysticercosis may also be uncovered in patients treated with albendazole for other conditions. Patients may experience neurological symptoms (e.g. seizures) as a result of an inflammatory reaction caused by death of the parasite within the brain.
Cysticercosis may, in rare cases, involve the retina. Before initiating therapy for neurocysticercosis, the patient should be examined for the presence of retinal lesions.
Has been shown to cause occasional reversible reductions in the total WBC count. Rarely, more significant reductions may be encountered, including granulocytopenia, agranulocytosis or pancytopenia.
Has been associated with mild-to-moderate elevations of hepatic enzymes in approximately 16% of patients.
Liver function tests (transaminases) should be performed before the start of each treatment cycle and at least every 2 weeks during treatment.
Patients with abnormal liver function test results are at increased risk for hepatotoxicity & bone marrow suppression.
Microfilaricidal drugs such as diethylcarbamazine citrate, might cause cutaneous and/or systemic reactions of varying severity & ophthalmological reactions in patients with onchocerciasis. These reactions are probably due to allergic & inflammatory responses to the death of microfilariae.
Patients with hyperreactive onchodermatitis may be more likely than others to experience severe adverse reactions, especially oedema and aggravation of onchodermatitis.
7. ADVERSE EFFECTS:
Common side effects associated with albendazole are:
- Abnormal liver function
- Abdominal pain
- Nausea/vomiting
- Headache
- Fever
- Reversible alopecia
- Pruritis
8. DRUG INTERACTIONS:
Dexamethasone: Steady-state trough concentrations of albendazole sulphoxide were about 56% higher when 8mg dexamethasone was co-administered with each dose of albendazole.
Praziquantel: In the fed state, praziquantel increased mean maximum plasma concentration & the AUC of albendazole sulphoxide by about 50%.
Cimetidine: Albendazole sulphoxide concentrations in bile & cystic fluid were increased (about 2-fold) patients treated with cimetidine compared with albendazole alone.
Theophylline: The pharmacokinetics of theophylline was unchanged following a single oral dose of albendazole.
Postmarketing reports of increased International Normalized Ratio (INR) have been reported when was co-administered with warfarin.
9. DOSAGE:
The recommended dosage is 2 TSF once daily.
10. ADMINISTRATION:
Shake the bottle well before use to ensure proper mixing of contents. Pour a measured amount of the syrup on to a tea spoon and administer. Make sure there is no spilling of the measured dose. May be followed up by a little fruit juice to increase palatability.
After administration, screw the cap back tightly and store.
11. STORAGE:
Do not store above 25°C. Store in the original package. Keep away from children. Do not expose to direct sunlight.
12. MANUFACTURED BY:
13. MARKETED BY:
Last revised on May 2019.