Zopir Tab 50 Mg 60’s

Potential Overview:

Mechanism of Action (MOA):

• Zopiclone is a sedative-hypnotic that belongs to the class of non-benzodiazepine hypnotics. It works by binding to a specific site on the GABA-A receptor (gamma-aminobutyric acid) in the brain. This increases the activity of GABA, a neurotransmitter that inhibits brain activity, promoting relaxation and sedation. As a result, Zopiclone helps to induce and maintain sleep.

Indications:

Zopiclone (Zopir) is primarily used for the following conditions:

1. Insomnia:
   • Short-term treatment of sleep disturbances, especially those associated with difficulty falling asleep or staying asleep.
2. Sleep Disorders:
   • It may be used for people experiencing transient or short-term insomnia, including those related to stress or jet lag.

Dosage:

• Adults:
  • Initial Dose: 7.5 mg orally, taken once per day, typically just before bedtime.
  • Elderly or Hepatically Impaired Patients: 3.75 mg orally, once a day (start with a lower dose due to slower metabolism).
  • The dose can be adjusted based on the individual’s response and tolerance.
• Duration of Treatment:
  • Zopiclone should generally be used for short-term treatment (usually 2-4 weeks) to avoid dependency and tolerance.

Note: Zopiclone should not be taken for extended periods without medical supervision, as tolerance and dependence can develop.

Side Effects:

Common side effects include:

• Drowsiness or sedation
• Bitter or metallic taste in the mouth
• Headache
• Dizziness
• Dry mouth
• Nausea

Serious side effects (less common):

• Memory problems or amnesia
• Confusion or disorientation
• Allergic reactions (e.g., rash, swelling)
• Hallucinations
• Sleep-driving or other unusual behaviors during sleep (complex sleep behaviors)
• Respiratory depression (especially in combination with other CNS depressants)

Precautions:

1. Dependence and Tolerance:
   • Zopiclone should only be used for short-term treatment to avoid dependence and tolerance. Patients may develop a psychological or physical dependency, especially with prolonged use.
2. CNS Depression:
   • Use with caution if the patient has any condition that can be aggravated by CNS depressants, such as respiratory disorders, alcohol use, or other sedative medications.
3. Elderly Patients:
   • Older adults may be more susceptible to side effects like sedation, confusion, and falls. Dosage adjustments are usually recommended (starting at 3.75 mg).
4. Liver or Kidney Impairment:
   • Patients with liver or kidney impairment may need a lower dose due to slower metabolism and excretion of the drug.
5. Pregnancy and Breastfeeding:
   • Pregnancy: Zopiclone should be avoided during pregnancy, especially in the first trimester, unless necessary. It may cause harm to the fetus.
   • Breastfeeding: Zopiclone is excreted in breast milk and should be avoided or used with caution in breastfeeding mothers.
6. Driving and Operating Machinery:
   • Due to sedative effects, patients should avoid driving or operating heavy machinery until they know how Zopiclone affects them.

Contraindications (CI):

• Hypersensitivity to Zopiclone:
  • Zopiclone should not be used in patients with a known allergy to the drug or any of its components.
• Severe Hepatic Impairment:
  • Zopiclone is contraindicated in patients with severe liver dysfunction because it is metabolized by the liver, and impaired liver function may lead to drug accumulation and increased side effects.
• Severe Respiratory Insufficiency:
  • Zopiclone should not be used in patients with severe breathing problems, such as severe chronic obstructive pulmonary disease (COPD) or sleep apnea, as it may worsen respiratory depression.
• Acute Alcohol Intoxication or Drug Overdose:
  • Zopiclone should not be used in patients who are intoxicated or have taken a significant overdose of alcohol, sedatives, or other CNS depressants.
• Pregnancy (especially in the first trimester)
  • Zopiclone is contraindicated during pregnancy unless absolutely necessary due to potential risks to the developing fetus.

Pharmacist Related Data

Chemical Formula:

• Zopiclone:
  • Chemical Formula: C17H15ClN6O3

Half-life:

• Zopiclone has a half-life of approximately 5 to 6 hours in healthy individuals. The elimination half-life can vary based on factors such as age, liver function, or other health conditions.

Metabolism:

• Zopiclone is metabolized in the liver by the CYP3A4 enzyme, which is part of the cytochrome P450 enzyme system.
• It is primarily converted into inactive metabolites, which are then excreted through the urine.
• The metabolite half-life is shorter, but the active effects of Zopiclone typically last for a few hours after ingestion.

Drug Interactions:

1. With Food:
   • Food can delay the absorption of Zopiclone, but it does not significantly affect the bioavailability. For faster onset of action, it is recommended to take it on an empty stomach.
2. With Other Medications:
   • CNS Depressants:
     • Concomitant use with other central nervous system (CNS) depressants such as alcohol, benzodiazepines, barbiturates, and other sedatives can increase the sedative effects, leading to enhanced drowsiness, respiratory depression, or coma.
   • Antidepressants (SSRIs, SNRIs, etc.):
     • Antidepressants can increase the sedative effect of Zopiclone. Caution should be taken when combining these drugs.
   • Antifungals (e.g., Ketoconazole, Itraconazole):
     • Drugs that inhibit CYP3A4 (e.g., ketoconazole) can increase the levels of Zopiclone in the bloodstream, leading to increased sedation and other side effects.
   • Anticonvulsants:
     • Drugs like carbamazepine that induce CYP3A4 could reduce the effectiveness of Zopiclone.
3. With Alcohol:
   • Alcohol should be avoided as it can potentiate the sedative effects of Zopiclone, leading to severe drowsiness, respiratory depression, and even coma.
4. With Antihistamines:
   • First-generation antihistamines (e.g., diphenhydramine) can increase the sedative effect of Zopiclone, increasing drowsiness and cognitive impairment.

Pharmacodynamics:

• Zopiclone is a sedative-hypnotic drug used to treat insomnia. It works by modulating the GABA-A receptor, enhancing the effects of gamma-aminobutyric acid (GABA), which is the primary inhibitory neurotransmitter in the brain. This leads to:
  • Sedation, reducing the time to fall asleep.
  • Anxiolysis, reducing anxiety that might interfere with sleep.
  • Muscle relaxation and anti-convulsant effects at higher doses, though this is secondary to its sedative properties.
• Zopiclone’s action is dose-dependent, and its hypnotic effect is most pronounced at the lower recommended doses (e.g., 7.5 mg).

Pharmacokinetics (Absorption, Distribution, Metabolism, Excretion):

1. Absorption:
   • Zopiclone is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within 1-2 hours after oral administration.
   • The bioavailability of Zopiclone is approximately 80%, which is relatively high for an oral medication.
2. Distribution:
   • Zopiclone is widely distributed throughout the body, with a volume of distribution (Vd) of approximately 1.5 L/kg.
   • It is highly protein-bound (about 80%) in the bloodstream, primarily to albumin.
3. Metabolism:
   • Zopiclone is metabolized in the liver by the CYP3A4 enzyme, forming inactive metabolites.
   • The metabolism is affected by age and liver function. Elderly patients or those with impaired liver function may have prolonged drug clearance, leading to higher plasma concentrations and increased sedative effects.
4. Excretion:
   • Zopiclone and its metabolites are excreted in the urine, with a small fraction of the drug being eliminated unchanged (less than 10%).
   • The elimination half-life of the active form is about 5-6 hours, with the overall effect lasting about 6-8 hours, depending on the individual.