Zstop
Zstop Uses, Dosage, Side Effects, Food Interaction and all others data.
Zstop, a synthetic antiprotozoal agent. Zstop is well absorbed from GIT. It interferes with the Pyruvate Ferredoxin Oxidoreductase (PFOR) enzyme dependent electron transfer reaction which is essential to anaerobic glucose energy metabolism. This results in cell swelling, membrane damage resulting in dysfunction of the parasite.
The general effect of this medication is the prevention of microbe activity through disruption of important energy pathways for survival and proliferation . Zstop exhibits antiprotozoal activity by interfering with the pyruvate ferredoxin/flavodoxin oxidoreductase dependent electron transfer reaction, an essential reaction need for anaerobic energy metabolism of various microorganisms. Sporozoites of Cryptosporidium parvum and trophozoites of Giardia lamblia are therefore inhibited, relieving symptoms of diahrrea . Interference with the PFOR enzyme-dependent electron transfer reaction may only be one of the many pathways by which nitazoxanide exhibits antiprotozoal activity .
| Trade Name | Zstop |
| Availability | Prescription only |
| Generic | Nitazoxanide |
| Nitazoxanide Other Names | Nitaxozanid, Nitaxozanide, Nitazoxanida, Nitazoxanide, Nitazoxanidum |
| Related Drugs | doxycycline, metronidazole, Flagyl, albendazole, mebendazole, Vibramycin, tinidazole, chloroquine, praziquantel, paromomycin |
| Type | Tablet |
| Formula | C12H9N3O5S |
| Weight | Average: 307.282 Monoisotopic: 307.026291103 |
| Protein binding | Very High (greater than 99%), bound to proteins in the plasma . |
| Groups | Approved, Investigational, Vet approved |
| Therapeutic Class | Anti-diarrhoeal Antiprotozoal |
| Manufacturer | Maneesh Pharmaceuticals Ltd |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Zstop is used for diarrhoea caused by Cryptosporidium parvum and Giardia lamblia, Amebiasis and helminth infections.
Zstop is also used to associated treatment for these conditions: Ascariasis, Cestode infections, Clostridium difficile infection recurrence, Cryptosporidiosis infection, Diarrhea caused by Cryptosporidium parvum, Diarrhea caused by Giardia lamblia, Giardiasis, Trichuriasis
How Zstop works
The most widely accepted mechanism of NTZ is believed to be the disruption of the energy metabolism in anaerobic microbes by inhibition of the pyruvate: ferredoxin/flavodoxin oxidoreductase (PFOR) cycle . In parasitic-protozoa, Zstop also induces lesions in the cell membranes and depolarizes the mitochondrial membrane while inhibiting quinone oxidoreductase NQO1, nitroreductase-1 and protein disulphide isomerase enzymes. In addition, this drug also inhibits the glutathione-S-transferase (a major detoxifying enzyme) and modulates the Avr-14 gene, encoding for the alpha-type subunit of glutamate-gated chloride ion channel present in nematodes. Aside from its well understood non-competitive inhibition of the PFOR in anaerobic bacteria, NTZ also demonstrates various other antibacterial mechanisms. It inhibits pyruvate dehydrogenase in E Coli, disrupts the membrane potential and pH homeostasis in the Mycobacterium tuberculosis, suppresses the chaperone/usher (CU) pathway of the gram-negative bacteria, and stimulates host macrophage autophagy in tuberculosis patients . NTZ also suppresses viral replication by inhibiting the maturation of the viral hemagglutinin and the viral transcription factor immediate early 2 (IE2) as well as by activating the eukaryotic translation initiation factor 2α (an antiviral intracellular protein). Lastly, NTZ exhibits an inhibitory effect on tumor cell progression by altering drug detoxification (glutathione-S-transferase P1), unfolded protein response, autophagy, anti-cytokines activity, and c-Myc inhibition .
Dosage
Zstop dosage
Age 1-3 years: 5 ml (100 mg) twice daily for 3 days
Age 4-11 years: 10 ml (200 mg) twice daily for 3 days
Age >12 years: 25 ml or 1 tablet (500 mg) twice daily for 3 days
The suspension or tablet should be taken with food.
30 ml suspension: Shake the bottle well before adding water. Then add 20 ml of boiled and cooled water (with the help of provided cup) into the bottle and shake well to make 30 ml suspension.
60 ml suspension: Shake the bottle well before adding water. Then add 40 ml of boiled and cooled water (with the help of provided cup) into the bottle and shake well to make 60 ml suspension.
Side Effects
Zstop is generally well tolerated. However abdominal pain, diarrhoea vomiting and headache have been reported rarely
Toxicity
Data on nitazoxanide overdosage is not available . In studies in rodents and dogs, the oral LD50 was higher than 10,000 mg/kg. One-time oral doses of up to 4000 mg nitazoxanide have been given to healthy adult volunteers without severe adverse effects. Gastric lavage may be appropriate soon after oral administration if overdose occurs. Supportive and symptomatic treatment should also be administered .
According to previous studies , less than 1% of the patients age 12 years and older participating in clinical trials with NTZ suffered from the following adverse effects: Systemic: asthenia, fever, pain, allergic reaction, pelvic pain, back pain, chills, fever, flu-like syndrome. Central Nervous System: dizziness, somnolence, insomnia, tremor, hypesthesia. Gastrointestinal System: vomiting, dyspepsia, anorexia, flatulence, constipation, dry mouth, thirst. Urogenital System: discolored urine, dysuria, amenorrhea, metrorrhagia, kidney pain, edema labia. Metabolic & Nutrition: increased SGPT. Hemic & Lymphatic Systems: anemia, leukocytosis. Skin: rash, pruritus. Special Senses: eye discoloration, ear ache. Respiratory System: epistaxis, lung disease, pharyngitis. Cardiovascular System: tachycardia, syncope, hypertension. Muscular System: myalgia, leg cramps, spontaneous bone fracture.
Precaution
Zstop should be administrated with caution to patients with hepatic, renal and biliary disease.
Interaction
Zstop is highly bound to plasma protein (>99.9%). Therefore, caution should be used when administering Zstop concurrently with other highly plasma-protein bound drugs.
Food Interaction
- Take with food. Food improves oral bioavailability.
[Moderate] ADJUST DOSING INTERVAL: Food enhances the bioavailability of the pharmacologically active metabolite tizoxanide (desacetyl-nitazoxamide) from nitazoxanide administration.
According to the product labeling, administration of nitazoxanide tablets with food increases the area under the plasma concentration-time curve (AUC) of tizoxanide and tizoxanide glucuronide in plasma by almost 2-fold and the peak plasma concentration (Cmax) by almost 50%.
Administration of nitazoxanide oral suspension with food increases the AUC of tizoxanide and tizoxandie glucuronide by about 45% to 50% and the Cmax by less than 10%.
MANAGEMENT: Zstop tablets and oral suspension were administered with food in clinical trials and are recommended to be administered with food to ensure maximal drug levels in plasma.
Zstop Drug Interaction
Moderate: valproic acidUnknown: amphetamine / dextroamphetamine, amoxicillin / clavulanate, sulfamethoxazole / trimethoprim, mupirocin topical, celecoxib, ciprofloxacin, loratadine, sulfamethoxazole / trimethoprim, ubiquinone, duloxetine, meperidine, clonazepam, escitalopram, acetaminophen, bioflavonoids, cyanocobalamin, ascorbic acid, cholecalciferol, zinc sulfate
Zstop Disease Interaction
Elimination Route
The relative bioavailability of the suspension compared to the tablet was 70%. When administered with food the AUC and Cmax increased by two-fold and 50%, respectively, for the tablet and 45 to 50% and ≤ 10%, respectively, for the oral suspension .
Half Life
7.3h
Clearance
Zstop is cleared in the urine and feces. The metabolite, tizoxanide, is also found in the urine, plasma, and breastmilk . The drug is not found unchanged in the urine .
Elimination Route
Tizoxanide is excreted in the urine, bile and feces, and tizoxanide glucuronide is excreted in urine and bile. Approximately 2/3 of the oral dose of nitazoxanide is excreted in the faeces and 1/3 in the urine .
Pregnancy & Breastfeeding use
Pregnancy category B. This drug should be used during pregnancy only if clearly needed.
Nursing mother: It is not known whether Zstop is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Zstop is administrated to a nursing woman.
Contraindication
Known hypersensitivity to Zstop or any other ingredient in the formulations
Special Warning
Paediatric Use: Safety and effectiveness of Zstop for Oral Suspension in paediatric patients less than one year of age have not been studied.
Impaired renal or hepatic function: The pharmacokinetics of Zstop in patients with impaired renal or hepatic function have not been studied. Therefore, Zstop must be administered with caution to patients with hepatic and biliary disease, to patients with renal disease and to patients with combined renal and hepatic disease.
Acute Overdose
Information on Zstop overdosage is not available. Single oral doses of up to 4000 mg Zstop have been administered to healthy adult volunteers without significant adverse effects.
Storage Condition
Store in a cool and dry place, away from light and moisture. Once reconstituted suspension should be used within 7 days.
Innovators Monograph
You find simplified version here Zstop
Zstop contains Nitazoxanide see full prescribing information from innovator Zstop Monograph, Zstop MSDS, Zstop FDA label
FAQ
What is Zstop used for?
Zstop is a broad-spectrum antiparasitic and broad-spectrum antiviral medication that is used in medicine for the treatment of various helminthic, protozoal, and viral infection. Zstop is used to treat diarrhea caused by Giardia or Cryptosporidium. These conditions are sometimes called "Traveler's diarrhea."
How safe is Zstop?
Zstop demonstrates a good safety profile at approved doses. However, further evidence is required regarding hepatorenal and cardiovascular effects, as well as teratogenicity.
How does Zstop work?
Zstop works by interfering with the conversion of chemicals to energy in protozoal cells.
What are the common side effects of Zstop?
Common side effects of Zstop are include:
- abdominal pain,
- nausea,
- diarrhea,
- vomiting, or.
- headache.
Is Zstop safe during pregnancy?
This Zstop should be used during pregnancy only if the benefit outweighs the risk. No data available on use of this drug in pregnant women to inform a drug-related risk.
Is Zstop safe during breastfeeding?
The effects in the nursing infant are unknown; potential side effects in the breastfed child due to this drug or the mother's underlying condition should be considered. Until more data are available, an alternative agent may be preferred, particularly while breastfeeding newborn or preterm infants; caution is recommended.
Can I drink alcohol with Zstop?
No interactions were found between Alcohol (contained in alcoholic beverages) and Zstop. This does not necessarily mean no interactions exist. Always consult your healthcare provider.
How long does Zstop take to work ?
It may take up to 5 days for diarrhea to resolve in approximately 80% of patients 4.
How long does Zstop stay in my system?
Elimination half-life of Zstop 3.5 hours.
Can I take Zstop in empty stomach?
Zstop should be taken just after eating food. Do not take it on an empty stomach. This will make it easier for your body to absorb the medication.
When should be taken of Zstop?
Zstop is usually taken with food every 12 hours for 3 days. Take Zstop at around the same times every day.
Can I take Zstop for a long time?
Do not take more of this Zstop and do not take it more often than your doctor ordered. This Zstop works best if there is a constant amount in the blood.
How much Zstop can I take daily?
Adults and children 12 years or older 25 milliliters (mL) every 12 hours, taken with food, for 3 days. Children 4 to 11 years of age 10 mL every 12 hours, taken with food, for 3 days.
How long should I take Zstop?
Zstop is usually taken once every 12 hours for 3 days.
Who should not take Zstop?
You should not use Zstop if you are allergic to it. To make sure Zstop is safe for you, tell your doctor if you have: liver or kidney disease; HIV or AIDS; or a weak immune system.
What happens if I miss a dose?
Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.
What happens if I take too much medication?
The more medications you are taking, the higher the risk of those drugs interacting dangerously with each other. Multiple medications can cause confusion, lightheadedness and even internal bleeding — all dangerous and injurious conditions.
Can Zstop affects my liver?
Zstop has some adverse effects on liver and kidney of rats. Therefore, Zstop should be used with caution by people with liver.
Can Zstop affect my kidneys?
Zstop should be used with caution by people with kidney problems.
