Stilpidem

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Stilpidem uses

• Pharmacological action
• Pharmacokinetics
• Why is Stilpidem prescribed?
• Dosage and administration
• Stilpidem side effects, adverse reactions
• Contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Stilpidem drug interactions
• Stilpidem in case of emergency / overdose
• Stilpidem reviews

Pharmacological action

Stilpidem is a sleeping drug from the group of imidazopyridine, specific agonist of omega1-receptors in CNS. It shortens the time to sleep, reduces the number of nighttime awakenings, increased sleep duration and improves its quality. This medication extends phase II of sleep, phases III and IV of deep sleep, does not affect the duration of REM sleep. Stilpidem characterized also by a central muscle relaxant and anticonvulsant effects.

Pharmacokinetics

After oral administration, C_max plasma levels observed after 0.5-3 hours. Bioavailability is approximately 70%. Plasma protein binding is 92%. There is a linear relationship between the magnitude of the dose and concentration of the active substance in the plasma. V_d is 0.52-0.56 L / kg. Stilpidem is metabolized in the liver and in the form of inactive metabolites are excreted in the urine and feces (37%). It does not induce liver enzymes.

T_1/2 is from 0.7 hours to 3.5 hours (mean is 2.4 h).

In elderly patients may decreases plasma clearance of Stilpidem, while T_1/2 increased slightly (to an average of 3 hours), C_max increased by 50%, V_d decreased to 0.29-0.39 L / kg.

In patients with severe renal impairment the clearance of Stilpidem is reduced slightly, other pharmacokinetic parameters were not changed. In patients with severe liver dysfunction increases the bioavailability of Stilpidem, clearance is somewhat reduced, T_1/2 increases to 10 hours.

Why is Stilpidem prescribed?

Episodic, transient and chronic insomnia.

Dosage and administration

For oral administration for adults aged under 65 years a single dose is 10 mg, if necessary, may increases to 15-20 mg. For patients older than 65 years or with concomitant hepatic insufficiency initial single dose is 5 mg. Stilpidem is taken just before bedtime. The course of treatment is from several days to 4 weeks. Maximum dose is 10 mg / day.

Stilpidem side effects, adverse reactions

Digestive system: in some cases - abdominal pain, nausea, vomiting, diarrhea.

CNS and peripheral nervous system: depending on the dose and individual sensitivity - vertigo, imbalance, ataxia, headache, daytime sleepiness, distraction, muscle weakness, double vision, anterograde amnesia, paradoxical or mental disorders; also it is possible ricochet insomnia when used in high doses or long-term treatment.

Allergic reactions: skin rash, itching.

Other: rarely - violation of sexual desire; development of addiction, the formation of psychic and physical dependence (when applying for a few weeks).

Contraindications

Severe respiratory failure, nocturnal apnea, severe hepatic insufficiency, childhood and adolescence to 15 years, I trimester of pregnancy, lactation (breastfeeding), increased sensitivity to Stilpidem.

Using during pregnancy and breastfeeding

Stilpidem is contraindicated in pregnancy and lactation.

Special instructions

Stilpidem is not recommended for use with myasthenia gravis.

With careful use in patients with respiratory failure. In case of insufficiency of liver function may be necessary to decrease the dose.

If you cancel the therapy dose should be reduced gradually. The likelihood of habituation increases with prolonged use of Stilpidem.

Avoid alcohol during the period of treatment.

During the period of treatment should refrain from potentially hazardous activities that require concentration and a high speed of psychomotor reactions.

Stilpidem drug interactions

When Stilpidem used with opioid analgesics, antitussives, barbiturates, antidepressants, sedatives, antihistamines, benzodiazepines, clonidine, neuroleptics, ethanol may develop symptoms of CNS depression and respiratory center.

When Stilpidem used with rifampicin, the concentration of Stilpidem in the blood plasma, which is accompanied by a decrease in its hypnotic effect. Interaction is due to induction of isoenzyme CYP3A4.

Simultaneous administration with inducers of CYP3A4 isoenzyme may be possible reducing the concentration of Stilpidem in the blood plasma.

Simultaneous administration with clozapine increases the risk of collapse, stop breathing and circulation.

Stilpidem in case of emergency / overdose

Symptoms: disturbance of consciousness (from lethargy to mild coma). There was recorded one case of cardiovascular and respiratory disorders; observed a full recovery after receiving doses of Stilpidem tartrate up to 400 mg.

Treatment: immediate induction of vomiting or gastric lavage (depending on state), the appointment of activated carbon. Should abandon the use of any sedative drugs (even when expressed excitation). Hemodialysis is ineffective. Specific antidote is flumazenil (benzodiazepine receptor antagonist).

Stilpidem pharmaceutical active ingredients containing related brand and generic drugs:

• Zolpidem

Stilpidem available forms, composition, doses:

• Tablets; Oral; Zolpidem 10 mg
• Tablets; Oral; Zolpidem 5 mg

Stilpidem destination | category:

• Human:
• Anxiolytics
• Hypnotics and sedatives

Stilpidem Anatomical Therapeutic Chemical codes:

• N05CF02 - Zolpidem

Stilpidem pharmaceutical companies:

• Quality Pharmaceutical Laboratory
• Vai Tat Hong

References

1. "zolpidem". https://pubchem.ncbi.nlm.nih.gov/co... (accessed August 28, 2018).
2. "zolpidem". http://www.drugbank.ca/drugs/DB0042... (accessed August 28, 2018).
3. "7K383OQI23: The UNique Ingredient Identifier (UNII) is an alphanumeric substance identifier from the joint FDA/USP Substance Registration System (SRS).". https://www.fda.gov/ForIndustry/Dat... (accessed August 28, 2018).

Frequently asked Questions

Depending on the reaction of the Stilpidem after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Stilpidem not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.

Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.

Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.

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The information was verified by Dr. Rachana Salvi, MD Pharmacology