Zolpidem Genoptim: composition and presentation
One film-coated tablet contains 10 mg of zolpidem tartrate. The medicine acts quickly, so it has to be taken immediately before lying down to sleep, or once already in bed.
One dose is taken per night, and a second dose is not taken the same night — that is a rule of its own, not a general recommendation. The composition includes lactose, so the medicine does not suit people with rare disorders such as galactose intolerance, Lapp lactase deficiency and glucose-galactose malabsorption syndrome.
How Zolpidem Genoptim works
Zolpidem tartrate is an imidazopyridine derivative, and it is not a benzodiazepine, although it works through the same system. The substance binds preferentially to the omega-1 subtype, also known as subtype 1 of the benzodiazepine receptor; it corresponds to the GABA-A receptor containing the α-1 subunit. Benzodiazepines, unlike zolpidem, bind non-selectively to both omega-1 and omega-2.
The effect follows from that selectivity: modulating the activity of the chloride channel through this receptor produces specifically a sedative action. The kinship is confirmed from the other side too — the action of zolpidem is reversed by flumazenil, a benzodiazepine antagonist. That is why all the warnings written for benzodiazepines apply to it as well.
Indications
Short-term treatment of insomnia in adults, in situations where the insomnia causes weakness or considerable exhaustion in the patient. The wording is narrow, and the word "short-term" is not in it by chance.
Even before a hypnotic is prescribed, the leaflet requires that the cause of the insomnia be established as far as possible and that the cause itself be treated. If insomnia does not resolve after 7–14 days of treatment, that may point to an underlying psychiatric or physical illness, and then what is needed is the appropriate investigation rather than continued dosing. It is not prescribed to children and adolescents under 18: there is no data to justify use in that age group.
Method of use and dosage
Adults are recommended 10 mg a day immediately before sleep. The lowest effective daily dose should be used, and 10 mg must not be exceeded. Treatment usually lasts from a few days to two weeks, at most four weeks, and in clinically justified cases the dose is reduced gradually before it is stopped altogether.
| For whom | Dose |
| Adults | 10 mg a day immediately before sleep; this dose must not be exceeded |
| Elderly and frail patients | 5 mg: they are particularly sensitive to the medicine's effect |
| Impaired liver function | treatment starts at 5 mg, because the clearance and metabolism of zolpidem are reduced; in adults under 65 the dose may be raised to 10 mg only if the clinical response is insufficient and tolerance is good |
| Impaired kidney function | the dose need not be changed, but caution is needed |
| Children and adolescents under 18 | the medicine is not used |
| Duration | from a few days to 2 weeks, at most 4 weeks including the period of gradual dose reduction; long-term use is not recommended |
That period should not be extended without reassessing the patient, and it is worth telling the patient at the very start that treatment will be limited in time. This is not a formality: it is precisely an unexpected end to the course that makes withdrawal symptoms frightening.
Contraindications
The medicine is contraindicated in hypersensitivity to zolpidem tartrate or to any excipient. The other prohibitions have to do with breathing, muscle and the liver: obstructive sleep apnoea, myasthenia gravis, severe impairment of liver function, acute or severe respiratory depression.
Listed separately are the groups to whom it is not given for lack of data or because the indication does not fit.
- children and adolescents under 18;
- patients with psychiatric illness — benzodiazepines and similar medicines are not recommended as the primary treatment of psychotic disorders;
- people with rare inherited conditions: galactose intolerance, Lapp lactase deficiency, glucose-galactose malabsorption;
- it is separately stated that benzodiazepines and similar medicines must not be used as the sole treatment of depression or of anxiety accompanying depression: in such patients this may provoke a suicide attempt.
Special warnings and precautions
The main practical rule turns on the number 8. The risk of next-day psychomotor impairment, including impaired ability to drive, rises if zolpidem was taken less than 8 hours before activities requiring alertness; if a dose higher than recommended was taken; if the medicine was combined with other substances that depress the central nervous system or raise the blood concentration of zolpidem, with alcohol or with illicit substances. The same 8 hours of uninterrupted sleep are needed to reduce the risk of anterograde amnesia, which usually arises in the first hours after a dose. The medicine's influence on driving is large: drowsiness, a longer reaction time, dizziness, sluggishness, blurred or double vision and reduced alertness persist into the morning, and cases of "falling asleep at the wheel" have been described even on monotherapy at therapeutic doses.
- tolerance: after several weeks of use the hypnotic effect of short-acting benzodiazepines and similar medicines may weaken;
- dependence: physical and psychological dependence develops the more readily the higher the dose and the longer the treatment, and especially in people with a history of alcohol or substance misuse — such patients are watched particularly closely;
- withdrawal symptoms on abrupt discontinuation: headache and muscle pain, very intense anxiety and nervous tension, restlessness, disorientation, irritability and insomnia; in severe cases derealisation, depersonalisation, sharpened hearing, numbness and tingling in the limbs, hypersensitivity to light, sound and touch, hallucinations and epileptic seizures;
- rebound insomnia: after the hypnotic is stopped, whatever it was taken for returns in a stronger form, sometimes together with mood swings, anxiety and restlessness; warning the patient about this in advance reduces their fear;
- with short-acting medicines withdrawal symptoms can appear even between doses, especially at high doses, which is why the dose is reduced gradually.
A separate and most unusual topic is behaviour during sleep. In patients who took zolpidem and did not fully wake, sleepwalking and other similar behaviour have been described: driving a car, preparing and eating food, holding telephone conversations, sexual activity — followed by complete loss of memory of these events. Such behaviour is more likely with alcohol and other substances that depress the nervous system, and when the maximum dose is exceeded; if a patient reports anything of the kind, withdrawing zolpidem should be seriously considered. Alongside this come restlessness, psychomotor agitation, irritability, aggression, delusions, fits of rage, nightmares, hallucinations and psychoses — if they appear, the medicine is stopped, and they occur most often in the elderly. In the elderly something else matters too: because skeletal muscle is relaxed, the risk of falls and injuries grows, especially if the person gets out of bed at night. Caution is also needed in chronic respiratory failure, and in depression the medicine is prescribed carefully and in the smallest possible quantity, because of the risk of a deliberate overdose.
Interactions with other medicines
The main interaction is with alcohol and with any substances that depress the central nervous system. The patient is warned not to consume alcohol or psychoactive substances while taking zolpidem: the combination increases drowsiness, the likelihood of complex sleep behaviour, and the risk of next-day impairment.
The second line is substances that affect the blood concentration of zolpidem. Those that raise it increase daytime sluggishness and the risk of impairment at the wheel, so prescribing such combinations calls for a separate decision by the doctor.
- combining it with other substances that depress the central nervous system raises the risk of next-day psychomotor impairment;
- exceeding the recommended dose leads to the same consequences;
- taking it less than 8 hours before an activity that requires attention is dangerous in itself — and all the more so in combination with the above.
Pregnancy and breastfeeding
Animal studies showed no teratogenic or embryotoxic effect, but the safety of use in pregnancy has not been established. As with all medicines, use during pregnancy should be avoided, especially in the first trimester. A woman of childbearing age is told when it is prescribed that if she intends to become pregnant or suspects she is, she should see her doctor about stopping it.
If for well-founded medical reasons the medicine is nonetheless given at the end of pregnancy or during labour, manifestations of its pharmacological action are to be expected in the newborn: a fall in body temperature, hypotonia and moderate respiratory depression. Newborns of women who took benzodiazepines or similar medicines for a long time in the last part of pregnancy may be physically dependent and therefore at risk of withdrawal symptoms after birth. Small amounts of the medicine pass into human milk, so it is not recommended for breastfeeding women.
Adverse reactions
The severity of adverse reactions depends on the dose, particularly for some disturbances of the central nervous system and the digestive tract. At least in theory they should be milder if the medicine is taken immediately before sleep or once in bed. They occur most often in elderly patients.
Commonly recorded are drowsiness, headache, dizziness, hallucinations, psychomotor agitation and nightmares. Uncommonly, confusion and irritability. With unknown frequency, angioneurotic oedema, restlessness, aggression, delusions, anger, psychosis, atypical behaviour, sleepwalking, dependence with withdrawal or rebound symptoms after treatment ends, and disturbances of libido have been reported. Most of these psychiatric disturbances belong to paradoxical reactions — that is, the opposite of what is expected — and that is precisely why their appearance is a reason to stop the medicine rather than to increase the dose.
Overdose
After an overdose of zolpidem — on its own or together with other substances depressing the central nervous system, alcohol included — disturbances of consciousness from drowsiness to coma have been described, and even fatal cases.
General symptomatic treatment and support of the basic vital functions are used. If gastric lavage brings no result, activated charcoal is given to reduce absorption. Sedatives are withheld, even if there are signs of agitation. In severe cases flumazenil may be considered, but its elimination half-life is only 40–80 minutes, so the patient must remain under close observation: further doses may be needed. Flumazenil itself, moreover, can provoke neurological symptoms, including convulsions. The role of dialysis has not been established: in patients with renal failure receiving therapeutic doses of zolpidem, dialysis did not lower its concentration. And with any overdose it is remembered that the person may have taken several different substances at once.
How to get a Zolpidem Genoptim prescription online
The medicine is available on prescription, and the doctor's first question will not be about the dose but about the cause of the insomnia: the leaflet requires that it be established and treated where possible, and that the hypnotic be prescribed for a short time. So it is worth describing how long sleep has been disturbed, what exactly fails — falling asleep, staying asleep without waking, or not waking too early — and what has already been tried.
For the online consultation prepare information about obstructive sleep apnoea and snoring with pauses in breathing, about myasthenia gravis, lung and liver disease, about depression and thoughts of self-harm, about past misuse of alcohol or psychoactive substances, and about pregnancy and any plans for one. Say too how your day is arranged: whether you can secure yourself 8 hours of uninterrupted sleep and whether you will have to get behind the wheel in the morning. List the medicines you take, especially hypnotics, sedatives, antidepressants and painkillers. The doctor will assess these circumstances and, if there are no contraindications, will issue an electronic prescription.
