Each tablet contains : Zaleplon USP 5 mg, 10 mg. DESCRIPTION :
Sleep Fine (Zaleplon) is an ultra - short acting sedative - hypnotic drug. It is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class. Zaleplon is a full agonist for the benzodiazepine GABAA α1 sub-receptor site which help produce the primary therapeutic hypnotic properties and it has lower afﬁnity for the α2 and α3 subsites which help produce anxiolytic and muscle relaxant effects. The absorption rate o f Zaleplon is rapid and the onset of therapeutic effects is reached within 5 - 15 minutes following ingestion and the protein binding is 60%. Zaleplon is metabolized mainly by the liver. The elimination half-life of Zaleplon is 1 - 1.5 hour and excreted mainly in urine 71% and feces 17%. INDICATIONS : Zaleplon is effective in the management or treatment of insomnia, primarily characterized by difﬁculty falling asleep.
DOSAGE & ADMINISTRATION :
It is not recommended to take food at least 2 hours before administration of Sleep Fine dose. because food delays the absorption of drug. Sleep Fine should be taken immediately before going to bed. If patient forgets to take it at bedtime, he should not take it at any other time .It should not be taken a second dose in the same night if patient experience difﬁculty sleeping after taking the ﬁrst dose or if he wake in the night .
- Adults : The total daily dose should not exceed 10 mg.
- Elderly and patients with mild to moderate hepatic impairment : The recommended dose is 5 mg
- Renal impairment : No dose adjustment is required in patients with mild to moderate renal impairment. RESTRICTIONS ON USE : Contraindications
- Hypersensitivity to Zaleplon .
- Myasthenia gravis.
- Severe hepatic or renal impairment.
- People with severe breathing problems .
- Sleep apnea syndrome .
- Children and adolescents under 18 years old. Precautions
- Cessation of administration of the drug should be gradually , because sudden cessation of administration of the drug can lead to withdrawal symptoms such as headache, muscles pain, anxiety , tension, irritability, confusion.
- Sleep Fine should not be taken for a longer period than prescribed by the doctor.
- Some behaviors have been reported during night after taking the drug – the patient was not fully awake - and the patient usually do not remember these events when he wake up in the next morning, the use of alcohol or other central nervous system depressant drugs increase the risk of such behaviors (which include sleepwalking , eating food).
- To reduce the risk of anterograde amnesia and psychomotor impairment after taking these drugs, the patient should not undertake activities requiring psychomotor co-ordination until 4 hours after taking the drug.
- Severe anaphylactic reactions have been reported such as skin rash, dyspnea, angioedema involving the larynx or tongue, nausea or vomiting, the patient should consult the doctor.
-Insomnia may persist or worsen after a short course of Zaleplon treatment ,this indicate a need to re-evaluate the patient.
- Caution should be taken in patients with a history of alcohol or medicinal product addiction or abuse, because the risk of dependence may increase with these patients.
- Zaleplon is not recommended to be prescribed to the patients with psychotic illness or suffering from depression as primary treatment or alone.
Effects on the capacity to drive vehicles or use machines
The patient may feel sleepy or impaired muscle function and may lose concentration especially, if sleep duration is less than 7 – 8 hours after taking Sleep Fine which affect the ability to drive or use machines.
Use in Pregnancy & Lactation
There are no sufﬁcient clinical experiments on the safety of use of Sleep ﬁne during pregnancy, due to that it is not recommended to be used during this period particularly in the third trimester of pregnancy. Signiﬁcant amounts of this medicine may pass into breast milk, so it should not be used by nursing mothers as it may be harmful to the infant. Dependence :
Zaleplon has the potential for dependence, addiction and withdrawal symptoms such as headache, muscle pain, anxiety , tension, restlessness, confusion if it is used for longer periods or in high doses.
DRUG INTERACTIONS :
- Co administration of Zaleplon with alcohol, antiepileptics, antipsychotics, baclofen, barbiturates , hypnotics, benzodiazepines , MAOI antidepressants, tricyclic antidepressants, sedating antihistamines, anesthetics, strong opioid pain killers increase the sedative effect.
- The amount of Zaleplon in the blood may be increased by the co administration with drugs that inhibit CYP3A4 enzyme (that is one of the enzymes which are responsible for Zaleplon metabolism) such as erythromycin and H2 antagonist cimetidine, while it may decrease the amount of Zaleplon in the blood by the co administration with drugs that induce CYP3A4 enzyme such as rifampicin and carbamazepine. SIDE EFFECTS : Somnolence, paraesthenia, temporary memory loss, dysmenorrhea, loss of appetite, asthenia, numbness in the hands and feet, confusion , hallucinations, dizziness, double vision, slurred speech, rash, angioedema involving the tongue, glottis or larynx, anaphylactic reaction .OVER DOSAGE :
- Symptoms : In mild cases, symptoms include drowsiness and mental confusion , in more serious cases, symptoms include , hypotension rarely coma and very rarely death.
- Management of overdose : induce vomiting or gastric lavage , if there is no advantage in emptying the stomach, the patient should be given activated charcoal to reduce the absorption, monitor respiratory and cardiovascular system. Flumazenil may be used as an antidote.
STORAGE INSTRUCTIONS : Store below 30oC , in a dry place.
Sleep Fine 5 Tablets : Pack of 10 tablets and hospital packs of different size. Sleep Fine 10 Tablets : Pack of 10 tablets and hospital packs of different size.
INSTRUCTIONS TO THE PATIENT
- Medicament is a product which affects your health, and its consumption contrary to instructions is dangerous for you.
- Follow strictly the doctor’s prescription, the method of use and the instructions of the pharmacist who sold the medicament.
- The doctor and the pharmacist are experts in medicine, its beneﬁts and risks.
- Do not by yourself interrupt the period of treatment prescribed for you.
- Do not repeat the same prescription without consulting your doctor.
Keep medicament out of reach of children Mfd. By
Council of Arab Health Ministers Unio