Zilast
Zilast Uses, Dosage, Side Effects, Food Interaction and all others data.
Zilast is a preparation of Zilast which is a quinolinone derivative. The mechanism of action is to specifically inhibit cellular phosphodiesterase III (PDE III) and suppress cAMP degradation with a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.
Zilast reduces the symptoms of intermittent claudication, as indicated by an increased walking distance. Intermittent claudication is pain in the legs that occurs with walking and disappears with rest. The pain occurs due to reduced blood flow to the legs.
Trade Name | Zilast |
Availability | Prescription only |
Generic | Cilostazol |
Cilostazol Other Names | Cilostazol, Cilostazole, Cilostazolum |
Related Drugs | pentoxifylline, Pletal, Trental, Pentoxil |
Type | Tablet |
Formula | C20H27N5O2 |
Weight | Average: 369.4607 Monoisotopic: 369.216475133 |
Protein binding | 95-98% |
Groups | Approved, Investigational |
Therapeutic Class | Peripheral Vasodilator drugs: Intermittent Claudication |
Manufacturer | Ipca Laboratories |
Available Country | India |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Zilast is used for the reduction of symptoms of intermittent claudication, as used by an increased walking distance.
Zilast is also used to associated treatment for these conditions: Intermittent Claudication
How Zilast works
Zilast and several of its metabolites are cyclic AMP (cAMP) phosphodiesterase III inhibitors (PDE III inhibitors), inhibiting phosphodiesterase activity and suppressing cAMP degradation with a resultant increase in cAMP in platelets and blood vessels, leading to inhibition of platelet aggregation and vasodilation.
Dosage
Zilast dosage
The recommended dosage of Zilast is 100 mg bid, taken at least half an hour before or two hours after breakfast and dinner.
A dose of 50 mg bid should be considered during coadministration of Fluconazole, Ketoconazole, Itraconazole, Erythromycin, Clarithromycin, Fluvoxamine, Fluoxetine, Nefazodone, Sertraline and Diltiazem.
Side Effects
The most common side effects are headache, diarrhoea, vomiting, leg cramps, rash etc. The less frequent side effects are anorexia and edema.
Toxicity
Information on acute overdosage with cilostazol in humans is limited. The signs and symptoms of an acute overdose can be anticipated to be those of excessive pharmacologic effect: severe headache, diarrhea, hypotension, tachycardia, and possibly cardiac arrhythmias. The oral LD50 of cilostazol is >5.0 g/kg in mice and rats and >2.0 g/kg in dogs.
Precaution
Zilast should be used with caution in patients with any degree of heart failure. There is no information with respect to the efficacy or safety of the concurrent use of Zilast and Clopidogrel.
Interaction
Co-admin with drugs that affect CYP3A4 (erythromycin, other macrolides, diltiazem) or CYP2C19 (omeprazole) may influence the pharmacokinetics of cilostazol.
Food Interaction
- Avoid grapefruit products.
- Take on an empty stomach. A high fat meal will increase absorption.
[Moderate] GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of cilostazol.
The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruits.
The extent and clinical significance are unknown.
Moreover, pharmacokinetic alterations associated with interactions involving grapefruit juice are often subject to a high degree of interpatient variability.
MANAGEMENT: Until more information is available, the manufacturer recommends avoiding consumption of grapefruit juice during cilostazol therapy.
Orange juice is not expected to interact with cilostazol.
Zilast Drug Interaction
Moderate: aspirin, aspirin, aspirin, aspirin, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, clopidogrel, clopidogrelUnknown: pregabalin, pregabalin, metoprolol, metoprolol, metoprolol, metoprolol, tiotropium, tiotropium, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Zilast Disease Interaction
Major: bleeding, heart failureModerate: hepatic impairment, ischemic heart disease
Elimination Route
Zilast is absorbed after oral administration. A high fat meal increases absorption, with an approximately 90% increase in Cmax and a 25% increase in AUC. Absolute bioavailability is not known.
Half Life
11-13 hours.
Elimination Route
Zilast is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Zilast is eliminated predominately by metabolism and subsequent urinary excretion of metabolites. The primary route of elimination was via the urine (74%), with the remainder excreted in feces (20%). No measurable amount of unchanged cilostazol was excreted in the urine, and less than 2% of the dose was excreted as 3,4-dehydro-cilostazol. About 30% of the dose was excreted in urine as 4'-trans-hydroxy-cilostazol.
Pregnancy & Breastfeeding use
There are no adequate and well controlled studies in pregnant women. Transfer of Zilast into milk has been reported in experimental animals. Because of the potential risk to nursing infants, a decision should be made to discontinue nursing or to discontinue Zilast.
Contraindication
Zilast is contraindicated in patients with congestive heart failure of any severity. Zilast is also contraindicated in patients with known or suspected hypersensitivity to any of its components.
Special Warning
Paediatric use: The safety and effectiveness of Zilast in paediatric patients have not been established.
Acute Overdose
Severe headache, diarrhoea, hypotension, tachycardia, and possibly cardiac arrhythmias. Careful observation and supportive treatment are recommended.
Storage Condition
Store in a cool & dry place, protected from light and moisture
Innovators Monograph
You find simplified version here Zilast
Zilast contains Cilostazol see full prescribing information from innovator Zilast Monograph, Zilast MSDS, Zilast FDA label