Pinarof
Generic Name
Pinazepam
Manufacturer
Square Pharmaceuticals Ltd.
Country
Bangladesh
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| pinarof 1 cream | ৳ 1,500.00 | N/A |
Description
Overview of the medicine
Pinazepam is a benzodiazepine derivative primarily used for its anxiolytic properties. It has sedative, muscle relaxant, and anticonvulsant effects.
Uses & Indications
Dosage
Adults
Typically 5-15 mg daily, divided into 2-3 doses. Dose should be individualized based on patient response and tolerance.
Elderly
Lower initial doses (e.g., 2.5 mg once or twice daily) are recommended due to increased sensitivity and slower metabolism. Adjust cautiously.
Renal_impairment
Use with caution and reduced dosage. Monitor renal function closely.
How to Take
Administer orally, with or without food. Swallow tablets whole with water.
Mechanism of Action
Enhances the effect of gamma-aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system, by binding to specific benzodiazepine receptors on the GABA-A receptor complex. This binding increases chloride ion influx, leading to neuronal hyperpolarization and reduced neuronal excitability.
Pharmacokinetics
Onset
Onset of action is relatively rapid, typically within 30-60 minutes.
Excretion
Excreted mainly by the kidneys as conjugated metabolites.
Half life
Pinazepam itself has a relatively short half-life, but its active metabolite N-desmethyldiazepam (nordiazepam) has a very long elimination half-life of 30-100 hours.
Absorption
Well absorbed after oral administration, peak plasma concentrations reached within 1-2 hours. It is a prodrug.
Metabolism
Extensively metabolized in the liver via cytochrome P450 enzymes (mainly CYP3A4 and CYP2C19) into active metabolites, primarily nordiazepam, oxazepam, and temazepam.
Side Effects
Contraindications
- Hypersensitivity to benzodiazepines
- Severe respiratory insufficiency
- Severe hepatic insufficiency
- Sleep apnea syndrome
- Myasthenia gravis
- Acute narrow-angle glaucoma
Drug Interactions
Opioids
Increased risk of profound sedation, respiratory depression, coma, and death.
CYP Inducers (e.g., rifampin, carbamazepine)
May decrease pinazepam plasma levels and reduce its effects.
CYP3A4/2C19 Inhibitors (e.g., azole antifungals, cimetidine)
May increase pinazepam plasma levels and prolong its effects.
Other CNS Depressants (e.g., alcohol, barbiturates, antidepressants, antihistamines)
Additive CNS depressant effects.
Storage
Store below 30°C, in a dry place, away from direct sunlight and moisture. Keep out of reach of children.
Overdose
Symptoms of overdose include somnolence, confusion, ataxia, diminished reflexes, and coma. Management is primarily supportive, including maintaining airway, breathing, and circulation. Flumazenil may be used as an antidote in selected cases, but with caution due to risk of seizures.
Pregnancy & Lactation
Not recommended during pregnancy due to potential for fetal harm and neonatal withdrawal syndrome. Excreted into breast milk and may cause sedation in breastfed infants; use with caution or avoid during lactation.
Side Effects
Contraindications
- Hypersensitivity to benzodiazepines
- Severe respiratory insufficiency
- Severe hepatic insufficiency
- Sleep apnea syndrome
- Myasthenia gravis
- Acute narrow-angle glaucoma
Drug Interactions
Opioids
Increased risk of profound sedation, respiratory depression, coma, and death.
CYP Inducers (e.g., rifampin, carbamazepine)
May decrease pinazepam plasma levels and reduce its effects.
CYP3A4/2C19 Inhibitors (e.g., azole antifungals, cimetidine)
May increase pinazepam plasma levels and prolong its effects.
Other CNS Depressants (e.g., alcohol, barbiturates, antidepressants, antihistamines)
Additive CNS depressant effects.
Storage
Store below 30°C, in a dry place, away from direct sunlight and moisture. Keep out of reach of children.
Overdose
Symptoms of overdose include somnolence, confusion, ataxia, diminished reflexes, and coma. Management is primarily supportive, including maintaining airway, breathing, and circulation. Flumazenil may be used as an antidote in selected cases, but with caution due to risk of seizures.
Pregnancy & Lactation
Not recommended during pregnancy due to potential for fetal harm and neonatal withdrawal syndrome. Excreted into breast milk and may cause sedation in breastfed infants; use with caution or avoid during lactation.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
24 to 36 months from manufacturing date
Availability
Available in pharmacies and hospitals
Approval Status
Approved for medical use
Patent Status
Patent expired
Clinical Trials
Clinical trials have evaluated pinazepam's efficacy and safety in anxiety disorders and insomnia, often comparing it with other benzodiazepines like diazepam and lorazepam.
Lab Monitoring
- Monitor liver function tests periodically, especially with long-term use.
- Monitor renal function in patients with renal impairment.
- Complete blood count (CBC) occasionally.
Doctor Notes
- Prescribe for the shortest possible duration.
- Gradual tapering is essential when discontinuing to avoid severe withdrawal symptoms.
- Assess for substance abuse history before initiating treatment.
- Monitor elderly patients closely for sedation and falls.
Patient Guidelines
- Do not stop taking this medicine suddenly without consulting your doctor, as withdrawal symptoms may occur.
- Avoid alcohol and other CNS depressants.
- Take exactly as prescribed by your doctor.
- Inform your doctor about all other medications you are taking.
Missed Dose Advice
If a dose is missed, take it as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and continue with your regular dosing schedule. Do not double the dose.
Driving Precautions
This medicine may cause drowsiness, dizziness, and impaired concentration, which can affect your ability to drive or operate machinery. Exercise caution.
Lifestyle Advice
- Avoid driving or operating heavy machinery until you know how this medicine affects you.
- Maintain good sleep hygiene practices.
- Avoid excessive caffeine.
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Global Brand Names
International brand names for this medicine. Click a brand to search for detailed information.